Side effects of actonel

SIDE EFFECTS: Stomach upset may occur. If this effect persists or worsens, tell your doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: increased or severe bone/joint/muscle pain, new or unusual hip/thigh/groin pain, jaw pain, eye/vision problems.This medication may infrequently cause irritation and ulcers in your stomach or esophagus. Get medical help right away if any of these serious side effects occur: new/severe/worsening heartburn, chest pain, difficult or painful swallowing, severe stomach/abdominal pain, black/tarry stools, vomit that looks like coffee grounds.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking risedronate, tell your doctor or pharmacist if you are allergic to it; or to other bisphosphonates (such as alendronate, etidronate, pamidronate); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: esophagus problems (such as heartburn, narrowing of the esophagus, achalasia), difficult or painful swallowing, low levels of calcium in the blood (hypocalcemia), inability to sit upright or stand for at least 30 minutes, stomach/intestinal disorders (such as ulcers), severe kidney disease.Infrequently, people taking this class of medication (bisphosphonates) have had serious jawbone problems (osteonecrosis). Lack of proper dental hygiene, poorly fitting dentures, or certain dental procedures (such as tooth extraction, dental surgery) may increase your risk. Medical conditions (such as gum disease/infection, cancer, anemia) might also increase the risk. If you develop jaw pain, tell your doctor and dentist immediately.Before having any surgery (especially dental procedures), tell your doctor and dentist about this medication and all other products you use (including prescription drugs, nonprescription drugs, and herbal products). Your doctor or dentist may tell you to stop taking risedronate before your surgery. Ask for specific instructions about stopping or starting this medication.Caution is advised if you are pregnant or planning to become pregnant in the future. This medication may stay in your body for many years. Its effects on an unborn baby are not known. Discuss the risks and benefits with your doctor before starting treatment with risedronate.It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.

Contents

QUESTION

What is another medical term for osteoporosis? See Answer

PMC

3. Discussion

We describe a 53-year-old woman who developed a severe pain and weakness after taking one pill of Risedronate for treatment of osteopenia. The side effect of medication was so profound that patient lost ability to ambulate and two and a half years later is still not completely recovered.

According to 2004 Surgeon General report on bone health and osteoporosis, 33.6 million individuals over age 50 have low bone mass or osteopenia of the hip and are at risk of osteoporosis and its potential complications. The prevalence of osteoporosis and low bone mass is expected to increase to 12 million cases of osteoporosis and 40 million cases of low bone mass among individuals over the age of 50 by 2010, and to nearly 14 million cases of osteoporosis and over 47 million cases of low bone mass in individuals over that age by 2020 . Bisphosphonates are approved for treatment of Paget’s disease of bone, osteoporosis, and osteopenia.

Absorption of Risedronate after the oral dose is relatively rapid (Tmax 1 hour). There is no evidence of systemic metabolism of Risedronate with 80% of the drug excreted with urine and 20% absorbed by bone. Bioavailability of Risedronate sodium is poor (0.54%–0.75%) and half-life is 480 hours. Approximately half of the absorbed dose is excreted in urine within 24 hours .

Risedronate was used in the treatment of the patient presented in this case report. The FDA has received six serious adverse event reports of severe bone, joint, or muscle pain for this medication . Pain (described as “incapacitating,” “disabling”) and loss of ability to climb stairs, ambulate, and perform the usual activities were reported as side effects of a different bisphosphonate, Alendronate (Fosamax), which may suggest a possible class effect . According to the FDA article published in 2006, many patients underwent numerous diagnostic tests with mostly normal findings . Details on the exact number of patients and the names of diagnostic tests patients performed are not provided. There have not been other reported cases of proximal muscle weakness after Risedronate use.

Symptoms experienced by the patient described in this case report (rise in temperature and accompanying flu-like symptoms) resemble an acute phase response. The mechanism for this response in general appears to be associated with the release of tumor necrosis factor (TNF)α, interferon γ (INF-γ), interleukin 1 (IL1), and interleukin 6 (IL-6) although the effector cells that release these cytokines and the mechanism of action remains not completely understood . Aminobisphosphonates (including Risedronate) increase serum levels of proinflammatory cytokines . Therefore, it is possible that patient’s muscle weakness might be an inflammatory response to the drug toxicity. Such hypothesis cannot be supported by patient’s levels of proinflammatory cytokines because they were not measured during the course of the disease. Muscle biopsy was not performed in this case, however will be an essential test to perform in similar cases to better assess etiology of symptoms. Pain and muscle weakness as adverse events of Risedronate may be underreported and not taken into consideration because of the subjective nature of pain, confusion with the pain from osteoporosis, and attribution of the loss of ambulation to pain. Combined with normal diagnostic tests, it may result in failure to recognize this potential side effect and a delay in stopping the bisphosphonate. Four of the bisphospohonates are listed in the Top 200 Brand Drugs By Units in 2007 accounting for almost 31 million prescriptions . Given the number of patients receiving bisphosphonate therapy and the paucity of reports, the incidence of the complex of symptoms is assumed to be relatively low. However, the formal reporting of adverse drug events is known to understate their true incidence .

For each patient, decisions regarding the therapy must also take into consideration the long period of treatment, substantial costs, and potential side effects. At this point, the risk factors and incidence of the incapacitating muscle pain and profound muscle weakness are unknown. Additional studies are needed to investigate the possible mechanism of pain, muscle weakness, and edema following bisphosphonate treatment. Even if low, the awareness of these side effects is very important because of the serious nature of the problem.

Actonel

SIDE EFFECTS

Clinical Studies Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Treatment Of Postmenopausal Osteoporosis

Daily Dosing

The safety of ACTONEL 5 mg once daily in the treatment of postmenopausal osteoporosis was assessed in four randomized, double-blind, placebo-controlled multinational trials of 3232 women aged 38 to 85 years with postmenopausal osteoporosis. The duration of the trials was up to three years, with 1619 patients exposed to placebo and 1613 patients exposed to ACTONEL 5 mg. Patients with preexisting gastrointestinal disease and concomitant use of non-steroidal anti-inflammatory drugs, proton pump inhibitors, and H antagonists were included in these clinical trials. All women received 1000 mg of elemental calcium plus vitamin D supplementation up to 500 international units per day if their 25- hydroxyvitamin D level was below normal at baseline.

The incidence of all-cause mortality was 2.0% in the placebo group and 1.7% in the ACTONEL 5 mg daily group. The incidence of serious adverse events was 24.6% in the placebo group and 27.2% in the ACTONEL 5 mg group. The percentage of patients who withdrew from the study due to adverse events was 15.6% in the placebo group and 14.8% in the ACTONEL 5 mg group. The most common adverse reactions reported in greater than 10 percent of subjects were: back pain, arthralgia, abdominal pain and dyspepsia. Table 1 lists adverse events from the Phase 3 postmenopausal osteoporosis trials reported in greater than or equal to 5% of patients. Adverse events are shown without attribution of causality.

Table 1: Adverse Events Occurring at a Frequency greater than or equal to 5% in Either Treatment Group Combined Phase 3 Postmenopausal Osteoporos is Treatment Trials

Body System Placebo
N = 1619
%
5 mg ACTONEL
N = 1613
%
Body as a Whole
Infection 29.9 31.1
Back Pain 26.1 28.0
Accidental Injury 16.8 16.9
Pain 14.0 14.1
Abdominal Pain 9.9 12.2
Flu Syndrome 11.6 10.5
Headache 10.8 9.9
Asthenia 4.5 5.4
Neck Pain 4.7 5.4
Chest Pain 5.1 5.0
Allergic Reaction 5.9 3.8
Cardiovascular System
Hypertension 9.8 10.5
Digestive System
Constipation 12.6 12.9
Diarrhea 10.0 10.8
Dyspepsia 10.6 10.8
Nausea 11.2 10.5
Metabolic & Nutritional Disorders
Peripheral Edema 8.8 7.7
Musculoskeletal System
Arthralgia 22.1 23.7
Arthritis 10.1 9.6
Traumatic Bone Fracture 12.3 9.3
Joint Disorder 5.3 7.0
Myalgia 6.2 6.7
Bone Pain 4.8 5.3
Nervous System
Dizziness 5.7 7.1
Depression 6.1 6.8
Insomnia 4.6 5.0
Respiratory System
Bronchitis 10.4 10.0
Sinusitis 9.1 8.7
Rhinitis 5.1 6.2
Pharyngitis 5.0 6.0
Increased Cough 6.3 5.9
Skin and Appendages
Rash 7.1 7.9
Special Senses
Cataract 5.7 6.5
Urogenital System
Urinary Tract Infection 10.4 11.1

Gastrointestinal Adverse Events

The incidence of adverse events in the placebo and ACTONEL 5 mg daily groups were: abdominal pain (9.9% versus 12.2%), diarrhea (10.0% versus 10.8%), dyspepsia (10.6% versus 10.8%), and gastritis (2.3% versus 2.7%). Duodenitis and glossitis have been reported uncommonly in the ACTONEL 5 mg daily group (0.1% to 1%). In patients with active upper gastrointestinal disease at baseline, the incidence of upper gastrointestinal adverse events was similar between the placebo and ACTONEL 5 mg daily groups.

Musculoskeletal Adverse Events

Laboratory Test Findings

Throughout the Phase 3 studies, transient decreases from baseline in serum calcium (less than 1%) and serum phosphate (less than 3%) and compensatory increases in serum PTH levels (less than 30%) were observed within 6 months in patients in osteoporosis clinical trials treated with ACTONEL 5 mg once daily. There were no significant differences in serum calcium, phosphate, or PTH levels between placebo and ACTONEL 5 mg once daily at 3 years. Serum calcium levels below 8 mg/dL were observed in 18 patients, 9 (0.5%) in each treatment arm (placebo and ACTONEL 5 mg once daily). Serum phosphorus levels below 2 mg/dL were observed in 14 patients, 3 (0.2%) treated with placebo and 11 (0.6%) treated with ACTONEL 5 mg once daily. There have been rare reports (less than 0.1%) of abnormal liver function tests.

Endoscopic Findings

In the ACTONEL clinical trials, endoscopic evaluation was encouraged in any patient with moderate-to-severe gastrointestinal complaints, while maintaining the blind. Endoscopies were performed on equal numbers of patients between the placebo and treated groups . Clinically important findings (perforations, ulcers, or bleeding) among this symptomatic population were similar between groups (51% placebo; 39% ACTONEL).

Once-A-Week Dosing

The safety of ACTONEL 35 mg once-a-week in the treatment of postmenopausal osteoporosis was assessed in a 1-year, double-blind, multicenter study comparing ACTONEL 5 mg daily and ACTONEL 35 mg once-a-week in postmenopausal women aged 50 to 95 years. The duration of the trials was one year, with 480 patients exposed to ACTONEL 5 mg daily and 485 exposed to ACTONEL 35 mg oncea- week. Patients with pre-existing gastrointestinal disease and concomitant use of non-steroidal antiinflammatory drugs, proton pump inhibitors, and H2 antagonists were included in these clinical trials. All women received 1000 mg of elemental calcium plus vitamin D supplementation up to 500 international units per day if their 25-hydroxyvitamin D3 level was below normal at baseline.

The incidence of all-cause mortality was 0.4% in the ACTONEL 5 mg daily group and 1.0% in the ACTONEL 35 mg once-a-week group. The incidence of serious adverse events was 7.1% in the ACTONEL 5 mg daily group and 8.2% in the ACTONEL 35 mg once-a-week group. The percentage of patients who withdrew from the study due to adverse events was 11.9% in the ACTONEL 5 mg daily group and 11.5% in the ACTONEL 35 mg once-a-week group. The overall safety and tolerability profiles of the two dosing regimens were similar.

Gastrointestinal Adverse Events:

Musculoskeletal Adverse Events:

Arthralgia was reported in 11.5% of patients in the ACTONEL 5 mg daily group and 14.2% of patients in the ACTONEL 35 mg once-a-week group. Myalgia was reported by 4.6% of patients in the ACTONEL 5 mg daily group and 6.2% of patients in the ACTONEL 35 mg once-a-week group.

Laboratory Test Findings:

Monthly Dosing

Two Consecutive Days per Month

The safety of ACTONEL 75 mg administered on two consecutive days per month for the treatment of postmenopausal osteoporosis was assessed in a double-blind, multicenter study in postmenopausal women aged 50 to 86 years. The duration of the trial was two years; 613 patients were exposed to ACTONEL 5 mg daily and 616 were exposed to ACTONEL 75 mg two consecutive days per month. Patients with pre-existing gastrointestinal disease and concomitant use of non-steroidal antiinflammatory drugs, proton pump inhibitors, and H2 antagonists were included in this clinical trial. All women received 1000 mg of elemental calcium plus 400 to 800 international units of vitamin D supplementation per day.

The incidence of all-cause mortality was 1.0% for the ACTONEL 5 mg daily group and 0.5% for the ACTONEL 75 mg two consecutive days per month group. The incidence of serious adverse events was 10.8% in the ACTONEL 5 mg daily group and 14.4% in the ACTONEL 75 mg two consecutive days per month group. The percentage of patients who withdrew from treatment due to adverse events was 14.2% in the ACTONEL 5 mg daily group and 13.0% in the ACTONEL 75 mg two consecutive days per month group. The overall safety and tolerability profiles of the two dosing regimens were similar.

Acute Phase Reactions:

Symptoms consistent with acute phase reaction have been reported with bisphosphonate use. The overall incidence of acute phase reaction was 3.6% of patients on ACTONEL 5 mg daily and 7.6% of patients on ACTONEL 75 mg two consecutive days per month. These incidence rates are based on reporting of any of 33 acute phase reaction-like symptoms within 5 days of the first dose. Fever or influenza-like illness with onset within the same period were reported by 0.0% of patients on ACTONEL 5 mg daily and 0.6% of patients on ACTONEL 75 mg two consecutive days per month.

Gastrointestinal Adverse Events:

The ACTONEL 75 mg two consecutive days per month group resulted in a higher incidence of discontinuation due to vomiting (1.0% versus 0.2%) and diarrhea (1.0% versus 0.3%) compared to the ACTONEL 5 mg daily group. Most of these events occurred within a few days of dosing.

Ocular Adverse Events:

None of the patients treated with ACTONEL 75 mg two consecutive days per month reported ocular inflammation such as uveitis, scleritis, or iritis; 1 patient treated with ACTONEL 5 mg daily reported uveitis.

Laboratory Test Findings:

When ACTONEL 5 mg daily and ACTONEL 75 mg two consecutive days per month were compared in postmenopausal women with osteoporosis, the mean percent changes from baseline at 24 months were 0.2% and 0.8% for serum calcium, -1.9% and -1.3% for phosphate, and – 10.4% and -17.2% for PTH, respectively. Compared to the ACTONEL 5 mg daily group, ACTONEL 75 mg two consecutive days per month resulted in a slightly higher incidence of hypocalcemia at the end of the first month of treatment (4.5% versus 3.0%). Thereafter, the incidence of hypocalcemia with these regimens was similar at approximately 2%.

Once-A-Month

The safety of ACTONEL 150 mg administered once-a-month for the treatment of postmenopausal osteoporosis was assessed in a double-blind, multicenter study in postmenopausal women aged 50 to 88 years. The duration of the trial was one year, with 642 patients exposed to ACTONEL 5 mg daily and 650 exposed to ACTONEL 150 mg once-a-month. Patients with pre-existing gastrointestinal disease and concomitant use of non-steroidal anti-inflammatory drugs, proton pump inhibitors, and H2 antagonists were included in this clinical trial. All women received 1000 mg of elemental calcium plus up to 1000 international units of vitamin D supplementation per day.

The incidence of all-cause mortality was 0.5% for the ACTONEL 5 mg daily group and 0.0% for the ACTONEL 150 mg once-a-month group. The incidence of serious adverse events was 4.2% in the ACTONEL 5 mg daily group and 6.2% in the ACTONEL 150 mg once-a-month group. The percentage of patients who withdrew from treatment due to adverse events was 9.5% in the ACTONEL 5 mg daily group and 8.6% in the ACTONEL 150 mg once-a-month group. The overall safety and tolerability profiles of the two dosing regimens were similar.

Acute Phase Reactions:

Symptoms consistent with acute phase reaction have been reported with bisphosphonate use. The overall incidence of acute phase reaction was 1.1% in the ACTONEL 5 mg daily group and 5.2% in the ACTONEL 150 mg once-a-month group. These incidence rates are based on reporting of any of 33 acute phase reaction-like symptoms within 3 days of the first dose and for a duration of 7 days or less. Fever or influenza-like illness with onset within the same period were reported by 0.2% of patients on ACTONEL 5 mg daily and 1.4% of patients on ACTONEL 150 mg once-a-month.

Gastrointestinal Adverse Events:

A greater percentage of patients experienced diarrhea with ACTONEL 150 mg once-a-month compared to 5 mg daily (8.2% versus 4.7%, respectively). The ACTONEL 150 mg once-a-month group resulted in a higher incidence of discontinuation due to abdominal pain upper (2.5% versus 1.4%) and diarrhea (0.8% versus 0.0%) compared to the ACTONEL 5 mg daily regimen. All of these events occurred within a few days of the first dose. The incidence of vomiting that led to discontinuation was the same in both groups (0.3% versus 0.3%).

Ocular Adverse Events:

None of the patients treated with ACTONEL 150 mg once-a-month reported ocular inflammation such as uveitis, scleritis, or iritis; 2 patients treated with ACTONEL 5 mg daily reported iritis.

Laboratory Test Findings:

When ACTONEL 5 mg daily and ACTONEL 150 mg once-a-month were compared in postmenopausal women with osteoporosis, the mean percent changes from baseline at 12 months were 0.1% and 0.3% for serum calcium, -2.3% and -2.3% for phosphate, and 8.3% and 4.8% for PTH, respectively. Compared to the ACTONEL 5 mg daily regimen, ACTONEL 150 mg once-a-month resulted in a slightly higher incidence of hypocalcemia at the end of the first month of treatment (0.2% versus 2.2%). Thereafter, the incidence of hypocalcemia with these regimens was similar at approximately 2%.

Prevention Of Postmenopausal Osteoporosis

The safety of ACTONEL 5 mg daily in the prevention of postmenopausal osteoporosis was assessed in two randomized, double-blind, placebo-controlled trials. In one study of postmenopausal women aged 37 to 82 years without osteoporosis, the use of estrogen replacement therapy in both placebo- and ACTONEL-treated patients was included. The duration of the trial was one year, with 259 exposed to placebo and 261 patients exposed to ACTONEL 5 mg. The second study included postmenopausal women aged 44 to 63 years without osteoporosis. The duration of the trial was one year, with 125 exposed to placebo and 129 patients exposed to ACTONEL 5 mg. All women received 1000 mg of elemental calcium per day.

In the trial with estrogen replacement therapy, the incidence of all-cause mortality was 1.5% for the placebo group and 0.4% for the ACTONEL 5 mg group. The incidence of serious adverse events was 8.9% in the placebo group and 5.4% in the ACTONEL 5 mg group. The percentage of patients who withdrew from treatment due to adverse events was 18.9% in the placebo group and 10.3% in the ACTONEL 5 mg group. Constipation was reported by 1.9% of the placebo group and 6.5% of ACTONEL 5 mg group.

In the second trial, the incidence of all-cause mortality was 0.0% for both groups. The incidence of serious adverse events was 17.6% in the placebo group and 9.3% in the ACTONEL 5 mg group. The percentage of patients who withdrew from treatment due to adverse events was 6.4% in the placebo group and 5.4% in the ACTONEL 5 mg group. Nausea was reported by 6.4% of patients in the placebo group and 13.2% of patients in the ACTONEL 5 mg group.

Once-a-Week Dosing

Treatment To Increase Bone Mass In Men With Osteoporosis

In a 2-year, double-blind, multicenter study, 284 men with osteoporosis were treated with placebo (N = 93) or ACTONEL 35 mg once-a-week (N = 191). The overall safety and tolerability profile of ACTONEL in men with osteoporosis was similar to the adverse events reported in the ACTONEL postmenopausal osteoporosis clinical trials, with the addition of benign prostatic hyperplasia (placebo 3%; ACTONEL 35 mg 5%), nephrolithiasis (placebo 0%; ACTONEL 35 mg 3%), and arrhythmia (placebo 0%; ACTONEL 35 mg 2%).

Treatment And Prevention Of Glucocorticoid-Induced Osteoporosis

The safety of ACTONEL 5 mg daily in the treatment and prevention of glucocorticoid-induced osteoporosis was assessed in two randomized, double-blind, placebo-controlled multinational trials of 344 patients aged 18 to 85 years who had recently initiated oral glucocorticoid therapy (less than or equal to 3 months, prevention study) or were on long-term oral glucocorticoid therapy (greater than or equal to 6 months, treatment study). The duration of the trials was one year, with 170 patients exposed to placebo and 174 patients exposed to ACTONEL 5 mg daily. Patients in one study received 1000 mg elemental calcium plus 400 international units of vitamin D supplementation per day; patients in the other study received 500 mg calcium supplementation per day.

The incidence of all-cause mortality was 2.9% in the placebo group and 1.1% in the ACTONEL 5 mg daily group. The incidence of serious adverse events was 33.5% in the placebo group and 30.5% in the ACTONEL 5 mg daily group. The percentage of patients who withdrew from the study due to adverse events was 8.8% in the placebo group and 7.5% in the ACTONEL 5 mg daily group. Back pain was reported in 8.8% of patients in the placebo group and 17.8% of patients in the ACTONEL 5 mg daily group. Arthralgia was reported in 14.7% of patients in the placebo group and 24.7% of patients in the ACTONEL 5 mg daily group.

Treatment Of Paget’s Disease

ACTONEL has been studied in 392 patients with Paget’s disease of bone. As in trials of ACTONEL for other indications, the adverse experiences reported in the Paget’s disease trials have generally been mild or moderate, have not required discontinuation of treatment, and have not appeared to be related to patient age, gender, or race.

The safety of ACTONEL was assessed in a randomized, double-blind, active-controlled study of 122 patients aged 34 to 85 years. The duration of the trial was 540 days, with 61 patients exposed to ACTONEL and 61 patients exposed to Didronel®. The adverse event profile was similar for ACTONEL and Didronel: 6.6% (4/61) of patients treated with ACTONEL 30 mg daily for 2 months discontinued treatment due to adverse events, compared to 8.2% (5/61) of patients treated with Didronel 400 mg daily for 6 months. Table 2 lists adverse events reported in greater than or equal to 5% of ACTONEL-treated patients in Phase 3 Paget’s disease trials. Adverse events shown are considered to be possibly or probably causally related in at least one patient.

Table 2 Adverse Events Reported in greater than or equal to 5% of ACTONEL-Treated Patients * in Phase 3 Paget’s Disease Trials

Body System 30 mg/day x 2 months ACTONEL
%
(N = 61)
400 mg/day x 6 months Didronel
%
(N = 61)
Body as a Whole
Flu Syndrome 9.8 1.6
Chest Pain 6.6 3.3
Gastrointestinal
Diarrhea 19.7 14.8
Abdominal Pain 11.5 8.2
Nausea 9.8 9.8
Constipation 6.6 8.2
Metabolic and Nutritional Disorders
Peripheral Edema 8.2 6.6
Musculoskeletal
Arthralgia 32.8 29.5
Nervous
Headache 18.0 16.4
Dizziness 6.6 4.9
Skin and Appendages
Rash 11.5 8.2
*Considered to be possibly or probably causally related in at least one patient.

Gastrointestinal Adverse Events:

During the first year of the study (treatment and nontreatment follow-up), the proportion of patients who reported upper gastrointestinal adverse events was similar between the treatment groups; no patients reported severe upper gastrointestinal adverse events. The incidence of diarrhea was 19.7% in the ACTONEL group and 14.8% in the Didronel group; none were serious or resulted in withdrawal.

Ocular Adverse Events:

Three patients who received ACTONEL 30 mg daily experienced acute iritis in 1 supportive study. All 3 patients recovered from their events; however, in 1 of these patients, the event recurred during ACTONEL treatment and again during treatment with pamidronate. All patients were effectively treated with topical steroids.

Postmarketing Experience

Because these adverse reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Hypersensitivity Reactions

Hypersensitivity and skin reactions have been reported, including angioedema, generalized rash, bullous skin reactions, Stevens-Johnson syndrome and toxic epidermal necrolysis.

Gastrointestinal Adverse Events

Events involving upper gastrointestinal irritation, such as esophagitis and esophageal or gastric ulcers, have been reported .

Musculoskeletal Pain

Bone, joint, or muscle pain, described as severe or incapacitating, have been reported rarely .

Eye Inflammation

Reactions of eye inflammation including iritis and uveitis have been reported rarely.

Jaw Osteonecrosis

Osteonecrosis of the jaw has been reported rarely .

Pulmonary

Asthma exacerbations

Read the entire FDA prescribing information for Actonel (Risedronate Sodium)

Risedronate

Before taking risedronate,

  • tell your doctor and pharmacist if you are allergic to risedronate, any other medications, or any of the ingredients in risedronate tablets or delayed-release tablets. Ask your pharmacist or check the Medication Guide for a list of the ingredients
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: angiogenesis inhibitors such as bevacizumab (Avastin), everolimus (Afinitor, Zortress), pazopanib (Votrient), sorafenib (Nexavar), or sunitinib (Sutent); aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (Advil, Ibu-Tab, Motrin, others) and naproxen (Aleve, Naprelan, Naprosyn, others); cancer chemotherapy; or oral steroids such as dexamethasone, methylprednisolone (Medrol), and prednisone (Rayos). If you are taking the delayed-release tablets, you should also tell your doctor if you are taking an H2 blocker such as cimetidine, famotidine (Pepcid), nizatidine (Axid), and ranitidine (Zantac) or a proton pump inhibitor such as esomeprazole (Nexium, in Vimovo), lansoprazole (Prevacid), omeprazole (Prilosec, Zegerid), pantoprazole (Protonix), and rabeprazole (AcipHex). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • you should know that Actonel and Atelvia both contain risedronate. You cannot take both of these medications at the same time.
  • if you are taking any other oral medications including vitamins, supplements, or antacids, take them at least 30 minutes after you take risedronate.
  • tell your doctor if you have or have ever had a low level of calcium in your blood or any problems with your esophagus and if you are unable to sit upright or stand upright for at least 30 minutes. Your doctor may tell you that you should not take risedronate.
  • tell your doctor if you are undergoing radiation therapy; if you have or have ever had difficulty swallowing; heartburn; ulcers or other problems with your stomach; anemia (condition in which the red blood cells do not bring enough oxygen to all the parts of the body); cancer; any type of infection, especially in your mouth; problems with your mouth, teeth, or gums; any condition that stops your blood from clotting normally; or dental or kidney disease.
  • tell your doctor if you are pregnant or are breastfeeding. Also tell your doctor if you plan to become pregnant at any time in the future, because risedronate may remain in your body for years after you stop taking it. Call your doctor if you become pregnant during or after your treatment with risedronate.
  • you should know that risedronate may cause severe bone, muscle, or joint pain. You may begin to feel this pain within days, months, or years after you first take risedronate. Although this type of pain may begin after you have taken risedronate for some time, it is important for you and your doctor to realize that it may be caused by risedronate. Call your doctor right away if you experience severe pain at any time during your treatment with risedronate. Your doctor may tell you to stop taking risedronate and your pain may go away after you stop taking the medication.
  • you should know that risedronate may cause osteonecrosis of the jaw (ONJ, a serious condition of the jaw bone), especially if you have dental surgery or treatment while you are taking the medication. A dentist should examine your teeth and perform any needed treatments, including cleaning or fixing ill-fitted dentures, before you start to take risedronate. Be sure to brush your teeth and clean your mouth properly while you are taking risedronate. Talk to your doctor before having any dental treatments while you are taking this medication.
  • talk to your doctor about other things you can do to prevent osteoporosis from developing or worsening. Your doctor will probably tell you to avoid smoking and drinking large amounts of alcohol and to follow a regular program of weight-bearing exercise.

Risedronic acid

Identification

Are you a new drug developer? Contact us to learn more about our customized products and solutions. Stay in the know! As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages. #DrugBankUpdates Name Risedronic acid Accession Number DB00884 (APRD00410, DB02782) Type Small Molecule Groups Approved, Investigational Description

Alendronic acid is a bisphosphonate that is used for the treatment of some forms of osteoperosis and Paget’s diseaseLabel1. It functions by preventing resorption of boneLabel1.

Structure 3D Download Similar Structures

Structure for Risedronic acid (DB00884)

× Close Synonyms

  • Acide risédroniqe
  • Acido risedronico
  • Acidum risedronicum
  • Risedronate
  • Risedronic acid
  • Risedronsäure

External IDs NE-58095 Product Ingredients

Ingredient UNII CAS InChI Key
Risedronate sodium OFG5EXG60L 115436-72-1 DRFDPXKCEWYIAW-UHFFFAOYSA-M
Risedronate sodium hemi-pentahydrate HU2YAQ274O 329003-65-8 HYFDYHPNTXOPPO-UHFFFAOYSA-L
Risedronate sodium monohydrate F67L43UT5C 353228-19-0 KLQNARDFMJRXSF-UHFFFAOYSA-M

Product Images Prescription Products

Name Dosage Strength Route Labeller Marketing Start Marketing End
Unlock Additional Data
Actonel Tablet, film coated 30 mg/1 Oral Warner Chilcott 1998-03-27 Not applicable US
Actonel Tablet, film coated 35 mg/1 Oral Physicians Total Care, Inc. 2002-09-16 Not applicable US
Actonel Tablet, film coated 35 mg/1 Oral Warner Chilcott 2002-05-17 Not applicable US
Actonel Tablet, film coated 5 mg/1 Oral Physicians Total Care, Inc. 2002-03-15 Not applicable US
Actonel Tablet 150 mg Oral Allergan 2008-12-01 Not applicable Canada
Actonel Tablet 75 mg Oral Warner Chilcott 2007-08-13 2016-08-05 Canada
Actonel Tablet, film coated 75 mg/1 Oral Warner Chilcott 2007-04-16 2010-03-31 US
Actonel Tablet 35 mg Oral Allergan 2002-12-10 Not applicable Canada
Actonel Tablet, film coated 150 mg/1 Oral Warner Chilcott 2008-04-22 Not applicable US
Actonel Tablet 5 mg Oral Allergan Pharma Co. 2000-07-25 2019-01-04 Canada

Additional Data Available

  • Application Number Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products

Name Dosage Strength Route Labeller Marketing Start Marketing End
Unlock Additional Data
Apo-risedronate Tablet Oral Apotex Corporation 2012-05-17 Not applicable Canada
Apo-risedronate Tablet Oral Apotex Corporation 2010-11-10 Not applicable Canada
Auro-risedronate Tablet Oral Auro Pharma Inc Not applicable Not applicable Canada
Auro-risedronate Tablet Oral Auro Pharma Inc Not applicable Not applicable Canada
Auro-risedronate Tablet Oral Auro Pharma Inc 2016-04-13 Not applicable Canada
Auro-risedronate Tablet Oral Auro Pharma Inc 2013-07-08 Not applicable Canada
Dom-risedronate Tablet Oral Dominion Pharmacal 2011-04-19 Not applicable Canada
Jamp-risedronate Tablet Oral Jamp Pharma Corporation 2011-10-04 Not applicable Canada
Mylan-risedronate Tablet Oral Mylan Pharmaceuticals 2013-09-30 2017-08-02 Canada
Mylan-risedronate Tablet Oral Mylan Pharmaceuticals 2011-06-16 2017-11-14 Canada

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  • Product Code Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products International/Other Brands Benet (Takeda ) / Ridron Categories UNII KM2Z91756Z CAS number 105462-24-6 Weight Average: 283.1123
Monoisotopic: 283.001074735 Chemical Formula C7H11NO7P2 InChI Key IIDJRNMFWXDHID-UHFFFAOYSA-N InChI InChI=1S/C7H11NO7P2/c9-7(16(10,11)12,17(13,14)15)4-6-2-1-3-8-5-6/h1-3,5,9H,4H2,(H2,10,11,12)(H2,13,14,15) IUPAC Name phosphonic acid SMILES OC(CC1=CN=CC=C1)(P(O)(O)=O)P(O)(O)=O

Pharmacology

Indication

Risedronic acid is indicated for the treatment of osteoperosis in men, treatment of Paget’s disease, treatment and prevention of osteoperosis in postmenopausal women, and treatment and prevention of glucocorticoid-induced osteoperosisLabel.

Associated Conditions

  • Hypercalcemia of Malignancy
  • Osteoporosis
  • Paget’s Disease

Pharmacodynamics

Risedronate is a pyridine-based bisphosphonate that inhibits bone resorption caused by osteoclastsLabel.

Mechanism of action

Risedronatic acid binds to bone hydroxyapatiteLabel. Bone resorption causes local acidification, releasing risedronic acid which is that taken into osteoclasts by fluid-phase endocytosis1. Endocytic vesicles are acidified, releasing risedronic acid to the cytosol of osteoclasts where they induce apoptosis through inhbition of farnesyl pyrophosphate synthase1. Inhibition of osteoclasts results in decreased bone resorption1.

Target Actions Organism
AFarnesyl pyrophosphate synthase inhibitor Humans
AHydroxylapatite antagonist Humans

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Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

Learn more Absorption

Oral bioavailability is 0.63% and maximum absorption is approximately 1 hour after dosingLabel. Administration half and hour before a meal reduces bioavailability by 55% compared to fasting and dosing 1 hour before a meal reduces bioavailability by 30%Label.

Volume of distribution

13.8 L/kgLabel.

Protein binding

~24%Label.

Metabolism

Risedronic acid is not likely not metabolized before eliminationLabel. The P-C-P group of bisphosphonates is resistant to chemical and enzymatic hydrolysis preventing metabolism of the molecule1.

Route of elimination

Risedronate is excreted by the kidneys and the unabsorbed dose is eliminated in the fecesLabel.

Half life

The initial half life of risedronic acid is approximately 1.5 hours2, with a terminal half life of 561 hoursLabel.

Clearance

Mean renal clearance was 52mL/min and mean total clearance was 73mL/minLabel.

Toxicity

In clinical trials, over 10% of patients experienced back pain, arthralgia, abdominal pain, and dyspepsiaLabel. Less commonly, patients experience angioedema, generalized rash, bullous skin reactions, iritis, and uveitisLabel.

Patients experiencing an overdose may experience a decrease in serum calcium and phosphorusLabel. Patients can be given milk or antacids to bind the drug and reduce its absorptionLabel. In more severe cases, patients may require gastric lavage and intravenous calciumLabel. A lethal dose in rats is equivalent to 320 to 620 times the human dose based on surface areaLabel.

Affected organisms

  • Humans and other mammals

Pathways

Pathway Category
Risedronate Action Pathway Drug action

Pharmacogenomic Effects/ADRs Not Available

Interactions

Drug Interactions This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

  • All Drugs
  • Approved
  • Vet approved
  • Nutraceutical
  • Illicit
  • Withdrawn
  • Investigational
  • Experimental
Drug Interaction
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Aceclofenac The risk or severity of gastrointestinal bleeding can be increased when Aceclofenac is combined with Risedronic acid.
Acemetacin The risk or severity of gastrointestinal bleeding can be increased when Acemetacin is combined with Risedronic acid.
Acetylsalicylic acid The risk or severity of gastrointestinal bleeding can be increased when Acetylsalicylic acid is combined with Risedronic acid.
Acipimox The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Risedronic acid is combined with Acipimox.
Acyclovir The risk or severity of nephrotoxicity and hypocalcemia can be increased when Acyclovir is combined with Risedronic acid.
Adefovir The risk or severity of nephrotoxicity and hypocalcemia can be increased when Adefovir is combined with Risedronic acid.
Adefovir dipivoxil The risk or severity of nephrotoxicity and hypocalcemia can be increased when Adefovir dipivoxil is combined with Risedronic acid.
Alclofenac The risk or severity of gastrointestinal bleeding can be increased when Alclofenac is combined with Risedronic acid.
Alendronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Alendronic acid is combined with Risedronic acid.
Almasilate The serum concentration of Risedronic acid can be decreased when it is combined with Almasilate.

Additional Data Available

  • Extended Description Extended Description

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  • Severity Severity

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  • Evidence Level Evidence Level

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  • Action Action

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Food Interactions Not Available Synthesis Reference

Srinivasa Rao V.N Divvela, Lenin Racha, Sivakumaran Meenakshisunderam, Ramesh Dandala, “Process for the preparation of risedronate sodium hemi-pentahydrate.” U.S. Patent US20070173484, issued July 26, 2007.

US20070173484 General References External Links Human Metabolome Database HMDB0015022 KEGG Drug D08484 KEGG Compound C08233 PubChem Compound 5245 PubChem Substance 46507526 ChemSpider 5055 BindingDB 12576 ChEBI 8869 ChEMBL CHEMBL923 Therapeutic Targets Database DAP000658 PharmGKB PA451255 HET RIS RxList RxList Drug Page Drugs.com Drugs.com Drug Page PDRhealth PDRhealth Drug Page Wikipedia Risedronate ATC Codes M05BB07 — Risedronic acid and colecalciferol

  • M05BB — Bisphosphonates, combinations
  • M05B — DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
  • M05 — DRUGS FOR TREATMENT OF BONE DISEASES
  • M — MUSCULO-SKELETAL SYSTEM

M05BB02 — Risedronic acid and calcium, sequential

  • M05BB — Bisphosphonates, combinations
  • M05B — DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
  • M05 — DRUGS FOR TREATMENT OF BONE DISEASES
  • M — MUSCULO-SKELETAL SYSTEM

M05BB04 — Risedronic acid, calcium and colecalciferol, sequential

  • M05BB — Bisphosphonates, combinations
  • M05B — DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
  • M05 — DRUGS FOR TREATMENT OF BONE DISEASES
  • M — MUSCULO-SKELETAL SYSTEM

M05BA07 — Risedronic acid

  • M05BA — Bisphosphonates
  • M05B — DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
  • M05 — DRUGS FOR TREATMENT OF BONE DISEASES
  • M — MUSCULO-SKELETAL SYSTEM

AHFS Codes

  • 92:24.00 — Bone Resorption Inhibitors

PDB Entries 1rqj / 1yhl / 1yq7 / 1yv5 / 2o1o / 2qis / 4kpd / 4kqs / 4n9u / 4ng6 … show 6 more FDA label (229 KB) MSDS (69.7 KB)

Clinical Trials

Clinical Trials

Phase Status Purpose Conditions Count
1 Completed Not Available Bioavailability 1
1 Completed Not Available Non-lactating / One to five years postmenopausal / Surgically Sterile 1
1 Completed Not Available Osteopenia / Osteoporosis 1
1 Completed Not Available Osteoporosis 2
1 Completed Treatment Healthy Volunteers 1
1, 2 Completed Treatment Renal Transplant Osteodystrophy 1
2 Completed Basic Science Osteogenesis Imperfecta 1
2 Completed Treatment Postmenopausal Osteoporosis (PMO) 2
2 Completed Treatment Postmenopausal Women 1
2 Completed Treatment One to five years postmenopausal 1
2 Recruiting Treatment Lung Tumors 1
2, 3 Active Not Recruiting Treatment Involutional Osteoporosis 1
2, 3 Completed Treatment Anorexia Nervosa (AN) 1
2, 3 Completed Treatment Involutional Osteoporosis 1
2, 3 Unknown Status Treatment Fibrous Dysplasia of Bone 1
3 Active Not Recruiting Treatment Osteopenia 1
3 Completed Not Available Osteoporosis 1
3 Completed Diagnostic Breast Cancer / Osteoporosis 1
3 Completed Prevention Osteopenia 1
3 Completed Prevention Postmenopausal Osteoporosis (PMO) 1
3 Completed Prevention Prostate Cancer 1
3 Completed Prevention Spinal Cord Injury, Acute 1
3 Completed Supportive Care Breast Cancer / Osteoporosis 1
3 Completed Supportive Care Osteoporosis / Prostate Cancer 1
3 Completed Treatment Back Pain, Unspecified / Postmenopausal Osteoporosis (PMO) / Vertebral Fractures 1
3 Completed Treatment Breast Cancer / Menopause / Osteopenia 1
3 Completed Treatment Glucocorticoid-induced Ostepor / Steroid-induced Osteopor / Steroid-induced Osteopor, Glucocorticoid-induced Ostepor / Steroid-induced Osteopor., Glucocorticoid-induced Ostepor 1
3 Completed Treatment Leukemias / Malignant Lymphomas 1
3 Completed Treatment Osteogenesis Imperfecta 1
3 Completed Treatment Osteoporosis 7
3 Completed Treatment Other Osteoporosis 1
3 Completed Treatment Paget’s Disease of Bone 2
3 Completed Treatment Postmenopausal Osteoporosis (PMO) 6
3 Completed Treatment Postmenopausal Women Osteoporosis 1
3 Completed Treatment Postmenopausal Women With Osteoporosis 1
3 Terminated Prevention Metastatic Hormone Refractory Prostate Cancer 1
3 Terminated Treatment Prosthesis Loosening 1
3 Withdrawn Supportive Care Breast Cancer / Osteoporosis 1
4 Active Not Recruiting Supportive Care Bariatric Surgery Candidate / Bone Loss / Weight Loss 1
4 Completed Not Available Crohn’s Disease (CD) / Low Bone Mineral Density 1
4 Completed Not Available Osteoporosis 1
4 Completed Prevention Bone Loss / Breast Cancer / Osteoporosis 1
4 Completed Prevention Bone Loss / Epilepsies / Fracture Bone / Osteoporosis 1
4 Completed Prevention Cystic Fibrosis (CF) / Muscular Dystrophy / Osteoporosis 1
4 Completed Prevention Postmenopausal Osteoporosis (PMO) 1
4 Completed Treatment Bone Loss 1
4 Completed Treatment Breast Cancer 1
4 Completed Treatment Colles’ Fracture 1
4 Completed Treatment Osteoporosis 6
4 Completed Treatment Postmenopausal Osteoporosis (PMO) 7
4 Completed Treatment Prostate Cancer 1
4 Not Yet Recruiting Prevention Osteogenesis Imperfecta 1
4 Recruiting Treatment Fracture of Neck of Femur / Osteoporotic Fractures 1
4 Terminated Prevention Postmenopausal Osteoporosis (PMO) 1
4 Terminated Treatment Osteoporosis 2
4 Unknown Status Prevention Periodontal Diseases 1
Not Available Completed Not Available Adenocarcinomas / Esophageal Cancers / Squamous Cell Carcinoma (SCC) 1
Not Available Completed Not Available Osseous Paget’s Disease 1
Not Available Completed Not Available Osteoporosis 2
Not Available Completed Prevention Hip Fracture 1
Not Available Completed Prevention Osteoporosis 1
Not Available Completed Treatment Anorexia Nervosa (AN) / Osteopenia / Osteoporosis 1
Not Available Enrolling by Invitation Not Available Atypical Femoral Fractures / Bisphosphonate Therapy / Osteoporosis 1
Not Available Terminated Treatment Osteopenia 1

Pharmacoeconomics

Manufacturers

  • Warner chilcott co llc
  • Teva pharmaceuticals usa
  • Procter & Gamble

Packagers

  • Diversified Healthcare Services Inc.
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • Norwich Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Procter & Gamble
  • Resource Optimization and Innovation LLC
  • Stat Rx Usa
  • Warner Chilcott Co. Inc.
  • WC Pharmaceuticals

Dosage forms

Form Route Strength
Tablet Oral 150 mg
Tablet Oral 30 mg
Tablet Oral 35 mg
Tablet Oral 5 mg
Tablet Oral 75 mg
Tablet, film coated Oral 150 mg/1
Tablet, film coated Oral 30 mg/1
Tablet, film coated Oral 35 mg/1
Tablet, film coated Oral 5 mg/1
Tablet, film coated Oral 75 mg/1
Tablet, delayed release Oral
Granule, effervescent; kit; tablet Oral
Kit Oral
Tablet, delayed release Oral
Tablet Oral
Tablet, delayed release Oral 35 mg/1
Tablet, film coated Oral
Powder Not applicable 1 kg/1kg
Tablet Oral
Kit; tablet Oral

Prices

Unit description Cost Unit
Actonel 150 mg tablet 125.1USD tablet
Actonel 4 35 mg tablet Disp Pack 119.43USD disp
Actonel 75 mg tablet 54.83USD tablet
Actonel 30 mg tablet 29.32USD tablet
Actonel 35 mg tablet 28.75USD tablet
Actonel 5 mg tablet 4.13USD tablet
Actonel with calcium tablet 3.92USD tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only. Patents Additional Data Available

  • Filed On Filed On

    The date on which a patent was filed with the relevant government.

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Properties

State Solid Experimental Properties Predicted Properties

Property Value Source
Water Solubility 10.4 mg/mL ALOGPS
logP -0.75 ALOGPS
logP -3.3 ChemAxon
logS -1.4 ALOGPS
pKa (Strongest Acidic) 0.68 ChemAxon
pKa (Strongest Basic) 4.91 ChemAxon
Physiological Charge -2 ChemAxon
Hydrogen Acceptor Count 8 ChemAxon
Hydrogen Donor Count 5 ChemAxon
Polar Surface Area 148.18 Å2 ChemAxon
Rotatable Bond Count 4 ChemAxon
Refractivity 57.12 m3·mol-1 ChemAxon
Polarizability 21.91 Å3 ChemAxon
Number of Rings 1 ChemAxon
Bioavailability 1 ChemAxon
Rule of Five Yes ChemAxon
Ghose Filter No ChemAxon
Veber’s Rule No ChemAxon
MDDR-like Rule No ChemAxon

Predicted ADMET features

Property Value Probability
Human Intestinal Absorption 0.9357
Blood Brain Barrier + 0.9172
Caco-2 permeable 0.6795
P-glycoprotein substrate Non-substrate 0.6846
P-glycoprotein inhibitor I Non-inhibitor 0.9582
P-glycoprotein inhibitor II Non-inhibitor 1.0
Renal organic cation transporter Non-inhibitor 0.9542
CYP450 2C9 substrate Non-substrate 0.8452
CYP450 2D6 substrate Non-substrate 0.8162
CYP450 3A4 substrate Non-substrate 0.7208
CYP450 1A2 substrate Non-inhibitor 0.8778
CYP450 2C9 inhibitor Non-inhibitor 0.8792
CYP450 2D6 inhibitor Non-inhibitor 0.9062
CYP450 2C19 inhibitor Non-inhibitor 0.8777
CYP450 3A4 inhibitor Non-inhibitor 0.9068
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.989
Ames test Non AMES toxic 0.7663
Carcinogenicity Non-carcinogens 0.8386
Biodegradation Not ready biodegradable 0.5058
Rat acute toxicity 2.1053 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.9095
hERG inhibition (predictor II) Non-inhibitor 0.9303

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST) Not Available Spectra

Spectrum Spectrum Type Splash Key
Predicted GC-MS Spectrum – GC-MS Predicted GC-MS Not Available
Predicted MS/MS Spectrum – 10V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum – 20V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum – 40V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum – 10V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum – 20V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum – 40V, Negative (Annotated) Predicted LC-MS/MS Not Available

Taxonomy

Description This compound belongs to the class of organic compounds known as bisphosphonates. These are organic compounds containing two phosphonate groups linked together through a carbon atoms. Kingdom Organic compounds Super Class Organic acids and derivatives Class Organic phosphonic acids and derivatives Sub Class Bisphosphonates Direct Parent Bisphosphonates Alternative Parents Pyridines and derivatives / Organic phosphonic acids / Heteroaromatic compounds / Azacyclic compounds / Organopnictogen compounds / Organophosphorus compounds / Organooxygen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives Substituents Bisphosphonate / Pyridine / Heteroaromatic compound / Organophosphonic acid / Azacycle / Organoheterocyclic compound / Organic nitrogen compound / Organic oxygen compound / Organopnictogen compound / Organic oxide Molecular Framework Aromatic heteromonocyclic compounds External Descriptors pyridines (CHEBI:8869)

Targets

Binding Properties

× Details Binding Properties1. Farnesyl pyrophosphate synthase Kind Protein Organism Humans Pharmacological action Yes Actions Inhibitor General Function Poly(a) rna binding Specific Function Key enzyme in isoprenoid biosynthesis which catalyzes the formation of farnesyl diphosphate (FPP), a precursor for several classes of essential metabolites including sterols, dolichols, carotenoids… Gene Name FDPS Uniprot ID P14324 Uniprot Name Farnesyl pyrophosphate synthase Molecular Weight 48275.03 Da

  1. Bergstrom JD, Bostedor RG, Masarachia PJ, Reszka AA, Rodan G: Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41.
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
  3. Coxon FP, Ebetino FH, Mules EH, Seabra MC, McKenna CE, Rogers MJ: Phosphonocarboxylate inhibitors of Rab geranylgeranyl transferase disrupt the prenylation and membrane localization of Rab proteins in osteoclasts in vitro and in vivo. Bone. 2005 Sep;37(3):349-58.
  4. Dunford JE, Thompson K, Coxon FP, Luckman SP, Hahn FM, Poulter CD, Ebetino FH, Rogers MJ: Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J Pharmacol Exp Ther. 2001 Feb;296(2):235-42.
  5. Ortiz-Gomez A, Jimenez C, Estevez AM, Carrero-Lerida J, Ruiz-Perez LM, Gonzalez-Pacanowska D: Farnesyl diphosphate synthase is a cytosolic enzyme in Leishmania major promastigotes and its overexpression confers resistance to risedronate. Eukaryot Cell. 2006 Jul;5(7):1057-64.
  6. Russell RG, Xia Z, Dunford JE, Oppermann U, Kwaasi A, Hulley PA, Kavanagh KL, Triffitt JT, Lundy MW, Phipps RJ, Barnett BL, Coxon FP, Rogers MJ, Watts NB, Ebetino FH: Bisphosphonates: an update on mechanisms of action and how these relate to clinical efficacy. Ann N Y Acad Sci. 2007 Nov;1117:209-57.

Kind Small molecule Organism Humans Pharmacological action Yes Actions Antagonist

Enzymes

Kind Protein Organism Humans Pharmacological action Unknown Actions Inducer General Function Prostaglandin-endoperoxide synthase activity Specific Function Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and… Gene Name PTGS2 Uniprot ID P35354 Uniprot Name Prostaglandin G/H synthase 2 Molecular Weight 68995.625 Da ×Unlock Data

There is additional data available for commercial users including Adverse Effects, Contraindications, and Blackbox Warnings. Contact us to learn more about these and other features.

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Drug created on June 13, 2005 07:24 / Updated on February 02, 2020 04:20

Osteonecrosis of the Jaw

Actonel and Osteonecrosis of the Jaw

Actonel is a drug used to treat bone loss caused by conditions such as osteoporosis, Paget’s disease of bone, and osteoporosis from menopause. It is a member of a class of drugs called bisphosphonates. Actonel works to alter the cycle that regulates the formation and breakdown of bone in the body. Research shows that Actonel and other bisphosphonates work to slow down a patient’s bone loss while increase the bone mass. As a result, fractures may be reduced. Actonel is manufactured by Warner Chilcott, which purchased the pharmaceuticals unit of manufacturing giant Procter & Gamble.

However, Actonel patients may experience severe side effects including osteonecrosis of the jaw (ONJ). Actonel osteonecrosis of the jaw is a rare yet devastating condition. Patients who develop severe cases of Actonel osteonecrosis of the jaw may experience a collapse of their jawbone. Other Actonel side effects include bladder cancer, bone fractures, low blood calcium, and esophageal ulcers and inflammation.

What Is Osteonecrosis of the Jaw?

Osteonecrosis of the jaw is a condition during which the jawbone starts to weaken and die. The term osteonecrosis literally translates to “bone death.” For this reason, osteonecrosis of the jaw is also known as “dead jaw syndrome.” The condition typically begins after the patient receives dental work of experiences other minor trauma in the mouth. When this trauma occurs, a lesion exposes an area of the patient’s gums.

Instead of healing, this area becomes infected. As a result of infection, the surrounding soft tissue erodes. Erosion causes a lack of proper blood flow to the area, which equates to a lack of proper blood flow to the jawbone itself. The jawbone essentially becomes starved from this inadequate blood supply. The American College of Rheumatology defines that osteonecrosis of the jaw is classified after a minimum of 8 weeks. The classification of each patient’s condition depends on the severity, the number of lesions present, and the size of the lesions.

Signs and Symptoms

The primary symptom of Actonel osteonecrosis of the jaw is the presence of lesions in the gums. This leads to the exposure of patient’s mandible or maxilla. The mandible is the jawbone, while the maxilla is the bone that creates the top part of the patient’s mouth. Patients who suffer Actonel osteonecrosis of the jaw will typically develop these lesions after dental procedures such as tooth extractions.

However, Actonel osteonecrosis of the jaw has also developed spontaneously. Patients with Actonel osteonecrosis of the jaw have reported no symptoms for weeks or months until they developed lesions that exposed bone. It is reported that Actonel osteonecrosis of the jaw occurs most commonly in the mandible than in the maxilla.

Symptoms of Actonel osteonecrosis of the jaw include:

  • Pain
  • Inflammation of the soft tissue
  • Secondary infection or drainage

Actonel Osteonecrosis of the Jaw Risk

Research indicates that patients who take bisphosphonates such as Actonel, Fosamax, and Boniva are more likely to develop osteonecrosis of the jaw. Patients may develop Actonel osteonecrosis of the jaw after as little as 12 months of taking Actonel and respective bisphosphonate drugs. The longer the drug is taken, the higher the chance of developing osteonecrosis of the jaw. The majority of Actonel osteonecrosis of the jaw cases occur in patients who received treatment for longer than 5 years.

The Actonel osteonecrosis of the jaw risk is higher in patients who receive bisphosphonate as a treatment for cancer. It is estimated that dosages of Actonel and other bisphosphonates can be as much as 10 times higher when used to treat cancer. Additionally, cancer patients often receive the drug intravenously as often as every month. Osteoporosis patients may only receive one IV dose per year.

Generic Name: risedronate sodium
Product Name: Actonel

Indication: What Actonel is used for

Actonel is used to treat bone disease and belongs to a group of medicines called bisphosphonates.

Actonel 5mg daily, 35mg once-a-week and 150mg once-a-month tablets are used to treat:

  • Osteoporosis (brittle or fragile bones that may fracture easily);
  • Osteoporosis caused by taking steroids.

Actonel 30mg tablets are used to treat:

  • Paget’s disease of the bone.

These conditions are caused by changes in the way bone is normally maintained.

Do not give Actonel to children or adolescents under 18 years of age. There have been no studies of its effects in this age group.

There is no evidence that Actonel is addictive.

This medicine is available only with a doctor’s prescription.

Action: How Actonel works

Actonel works directly on your bones to make them stronger and therefore less likely to break or fracture.

Actonel works by slowing down the process of old bone being removed. This allows the bone-forming cells time to rebuild normal bone. Actonel also helps to rebuild bone mass. This creates stronger bone which is less likely to fracture. Therefore Actonel can help reverse the progression of osteoporosis.

Each Actonel 5mg tablet contains 5 mg risedronate sodium per tablet.

Each Actonel 30mg tablet contains 30mg risedronate sodium per tablet.

Each Actonel 35mg Once-a-Week tablet contains 35 mg risedronate sodium per tablet.

Actonel 150mg once-a-month tablets contain 150mg risedronate sodium per tablet.

Other inactive ingredients include microcrystalline cellulose, lactose (5mg, 30mg and 35mg only), crospovidone, magnesium stearate, hypromellose, macrogol 400, macrogol 8000, silicon dioxide, titanium dioxide, hydroxypropyl cellulose, iron oxide yellow (5mg and 35mg only), iron oxide red (35mg tablet only), and indigo carmine CI73015 (150mg tablet only).

Actonel does not contain sucrose, gluten, tartrazine or any other azo dyes.

Dose advice: How to use Actonel

Before you take Actonel

When you must not take Actonel

Do not take Actonel if you:

  • Have an allergy to Actonel or any of the ingredients listed here;
  • Are unable to stand or sit upright for at least 30 minutes;
  • Have a condition called hypocalcaemia (a low level of calcium in the blood);
  • Have severe kidney problems.

Do not take Actonel if you are pregnant. Actonel is not recommended for use during pregnancy unless you and your doctor have discussed the risks and benefits involved.

Do not take Actonel if you are breastfeeding. It is not known whether Actonel passes into breast milk.

Do not take Actonel after the expiry date printed on the pack. If you take this medicine after the expiry date has passed, it may not work as well. Do not take Actonel if the packaging is torn or shows signs of tampering.

Talk to your doctor or pharmacist if you are not sure whether you should start taking Actonel.

Before you start to take it

Tell your doctor or pharmacist if you have allergies to:

  • Any other medicines;
  • Any other substances, such as foods, preservatives or dyes.

Tell your doctor if you are pregnant or intend to become pregnant.

Your doctor will discuss the possible risks and benefits of using Actonel during pregnancy.

Tell your doctor or pharmacist if you are breastfeeding or plan to breastfeed.

Tell your doctor if you have or have had any medical conditions, especially the following:

  • Disturbances of bone and mineral metabolism (for example vitamin D deficiency, parathyroid hormone abnormalities);
  • Problems with the tube that takes food from your mouth to your stomach (oesophagus) such as ulcers;
  • Pain, swelling or numbness of the jaw or a “heavy jaw feeling” or loosening of a tooth.

Check with your doctor or dentist to see if a dental check-up is required before starting Actonel. This is especially important if you are receiving medicines or therapy used to treat cancer or taking corticosteroids, such as prednisone or cortisone.

Tell your doctor about any of the above, before you start taking Actonel.

Taking other medicines

Tell your doctor or pharmacist if you are taking any other medicines, including any that you buy without a prescription from your pharmacy, supermarket or health food shop. Some medicines and Actonel may interfere with each other if taken at the same time. These include:

  • Antacids, medicines used to treat indigestion eg Gaviscon, Mylanta;
  • Other products containing calcium;
  • Iron supplements.

Check with your doctor or pharmacist if you are not sure whether you are taking any of these products. You may need to stop taking these products or take them at a different time of day to Actonel.

You can take aspirin while you are being treated with Actonel.

Your doctor and pharmacist may have more information on medicines to be careful with while taking Actonel.

How to take Actonel

How much to take

For osteoporosis, the usual dose is one 5mg tablet each day, one Actonel 35mg tablet once a week or one 150mg tablet once a month.

For Paget’s disease of the bone, the usual dose is one 30 mg tablet each day for 2 months.

Follow all directions given to you by your doctor or pharmacist. If you do not understand the instructions on the box, ask your doctor or pharmacist for help.

How to take it

Take your Actonel tablet in the morning, at least 30 minutes before your first meal, drink or medication of the day. Actonel is most effective when your stomach is empty.

Take your Actonel tablet while sitting or standing upright. Do not lie down immediately after swallowing it. It is important to stay upright, for example, sitting, standing or walking around, for at least 30 minutes after swallowing your tablet. It is also very important to stay upright until after you have eaten your first food of the day. This will help make sure the tablet reaches your stomach quickly and helps avoid irritation to your oesophagus.

Swallow your Actonel tablet whole with a glass of plain water. Do not chew or suck the tablet.

It is important to take Actonel with plain water only (120 mL), not mineral water. Mineral water and other drinks, including fruit juices, coffee, and tea, will reduce the effect of Actonel.

When to take it

Take Actonel in the morning, 30 minutes to 1 hour before your first meal, drink or medication of the day.

Take your Actonel 5mg and 30mg tablet at the same time of day every day. Taking your tablets at the same time each day will have the best effect. It will also help you remember when to take the tablets.

Take your Actonel 35mg once-a-week tablet on the same day each week.This tablet should be taken each week. Choose a day of the week that suits you the best.

Take your Actonel 150mg once-a-month tablet on the same day each month. This tablet should be taken each month. Choose a day of the month that suits you the best.

If you forget to take your tablet

For Actonel 5mg and 30mg tablets

If it is almost time for your next tablet skip the tablet you missed and take your next tablet when you are meant to.

Do not take a double dose to make up for the tablet that you missed. This may increase the chance of you getting an unwanted side effect.

For Actonel 35mg once-a-week tablets

If you have forgotten to take your 35mg tablet, just take your tablet on the day you remember.

Do not take two tablets in one day to make up for the tablet you missed. Return to taking one tablet once a week, as originally scheduled on your chosen day.

For Actonel 150mg once-a-month tablets

If you have forgotten to take your 150mg tablet, and your next monthly dose is more than 7 days ahead just take one tablet the next morning.

If you have forgotten to take your 150mg tablet, and your next monthly dose is within 7 days do not take it. Return to taking one tablet once a month, as originally scheduled on your chosen day.

If you are not sure what to do, ask your doctor or pharmacist. If you have trouble remembering to take your medicine, ask your pharmacist for some hints.

How long to take it

Continue taking Actonel for as long as your doctor recommends it. Do not stop taking Actonel without checking with your doctor or pharmacist.

If you take too much (overdose)

Immediately telephone your doctor or pharmacist or the Poisons Information Centre (13 11 26) or go to accident and emergency at your nearest hospital. If you or somebody else has accidentally taken a large number of tablets, drink a full glass of milk or antacids. Do this even if there are no signs of discomfort or poisoning. You may need urgent medical attention.

While you are using Actonel

Things you must do

Tell any other doctors, dentists, and pharmacists who are treating you that you are taking Actonel.

If you require a dental procedure, tell your dentist that you are taking Actonel. Invasive dental procedures should be avoided where possible. This type of medicine may cause jaw-bone problems in some people. Jaw-bone problems may include infection, and delayed healing after teeth are pulled out or other work that involves drilling into the jaw.

If you develop a toothache, jaw pain, painful exposed bone or swelling, especially following dental work, tell your doctor or dentist immediately.

Speak to your doctor and dentist about good oral hygiene and regular dental check-ups while you are using Actonel.

If you are about to be started on any new medicine, tell your doctor, dentist or pharmacist that you are taking Actonel.

If you become pregnant while taking Actonel tell your doctor or pharmacist.

If you develop new or unusual pain in your hip or thigh, tell your doctor. Rarely, patients have experienced a fracture in a specific part of the thigh bone.

Things you must not do

Do not lie down for 30 minutes after taking Actonel.

Do not have any food or drink, except for plain water for 30 minutes after taking Actonel.

Do not give Actonel to anyone else, even if they have the same condition as you.

Do not take Actonel to treat any other complaints unless your doctor or pharmacist tells you to.

Do not stop taking Actonel without checking with your doctor or pharmacist.

After using Actonel

Storage

Keep your tablets in the pack until it is time to take them. If you take the tablets out of the pack they may not keep well.

Keep your tablets in a cool dry place where the temperature stays below 25°C. Do not store Actonel or any other medicine in the bathroom or near a sink. Do not leave medicines in the car on hot days or on window sills. Heat and dampness can destroy some medicines.

Keep medicines where children cannot reach it. A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Disposal

If your doctor or pharmacist tells you to stop taking Actonel or the tablets have passed their expiry date, ask your pharmacist what to do with any tablets that are left over.

Schedule of Actonel

Actonel is a Schedule 4 (prescription only) medicine.

Side effects of Actonel

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are taking Actonel. All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Ask your doctor or pharmacist to answer any questions you may have.

Tell your doctor or pharmacist if you notice any of the following and they worry you:

  • Stomach pain;
  • Diarrhoea;
  • Aching muscles, joints or bones;
  • Headache;
  • Nausea;
  • Runny nose;
  • Sore throat;
  • Dizziness.

These side effects are usually mild.

Tell your doctor immediately if you notice any of the following:

  • Skin rash or redness of the skin, sometimes made worse by sunlight, itchiness;
  • Blurred vision, pain or redness in the eyes;
  • Problems with your jaw or teeth, associated with delayed healing and/or infection often following a tooth extraction or invasive dental work.

These side effects are rare.

If any of the following happen, stop taking Actonel and tell your doctor immediately:

  • Difficulty or pain when swallowing;
  • New or worsening heartburn.

These side effects may be due to irritation or ulceration of the food pipe. They may worsen if you continue taking the tablets. These side effects are rare.

If any of the following happen, stop taking Actonel and tell your doctor immediately or go to accident and emergency at your nearest hospital:

  • Swelling of the face, lips, mouth, throat or tongue;
  • Severe skin reactions.

These may be serious side effects. You may need urgent medical attention.

Other side effects not listed above may occur in some patients. Tell your doctor or pharmacist if you notice anything that is making you feel unwell.

Do not be alarmed by this list of possible side effects. You may not experience any of them.

For further information talk to your doctor.

How does this medication work? What will it do for me?

Risedronate belongs to a group of medications called bisphosphonates. It is used to treat and prevent osteoporosis for women who are past menopause, and to treat and prevent osteoporosis caused by treatment with corticosteroids (e.g., prednisone) for men and women. It is also used to improve bone mineral density for men with osteoporosis, and to treat a condition called Paget’s disease. The long-acting form of risedronate is used only to treat osteoporosis in women who are past menopause.

Risedronate increases the thickness of bone (bone mineral density) by slowing down the cells that usually break down bone (osteoclasts). This allows the cells that build bone (osteoblasts) to work more efficiently. By making bones stronger, risedronate can help to reduce the incidence of osteoporosis-related fractures.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

What form(s) does this medication come in?

5 mg (i.e., daily osteoporosis dose)
Each film-coated, oval, yellow tablet with “RSN” engraved on one face and “5 mg” engraved on the other contains the equivalent of 5 mg of anhydrous risedronate sodium in the form of the hemi-pentahydrate with small amounts of monohydrate. Nonmedicinal ingredients: crospovidone, ferric oxide yellow, hydroxypropyl cellulose, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, silicon dioxide, and titanium dioxide.

30 mg (i.e., daily Paget’s dose)
Each film-coated, oval, white tablet with “RSN” engraved on one face and “30 mg” engraved on the other contains the equivalent of 30 mg of anhydrous risedronate sodium in the form of the hemi-pentahydrate with small amounts of monohydrate. Nonmedicinal ingredients: crospovidone, hydroxypropyl cellulose, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, silicon dioxide, and titanium dioxide.

35 mg (i.e., once a week osteoporosis dose)
Each film-coated, oval, orange tablet with “RSN” engraved on one face and “35 mg” engraved on the other contains the equivalent of 35 mg of anhydrous risedronate sodium in the form of the hemi-pentahydrate with small amounts of monohydrate. Nonmedicinal ingredients: crospovidone, ferric oxide red, ferric oxide yellow, hydroxypropyl cellulose, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, silicon dioxide, and titanium dioxide.

75 mg (i.e., twice-monthly osteoporosis dose)
Each film-coated, oval, pink tablet with “RSN” engraved on one face and “75 mg” engraved on the other contains the equivalent of 75 mg of anhydrous risedronate sodium in the form of the hemi-pentahydrate with small amounts of monohydrate. Nonmedicinal ingredients: crospovidone, ferric oxide red, hydroxypropyl cellulose, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, silicon dioxide, and titanium dioxide.

150 mg (i.e., once-monthly osteoporosis dose)
Each film-coated, oval, blue tablet with “RSN” engraved on one face and “150 mg” engraved on the other contains the equivalent of 150 mg of anhydrous risedronate sodium in the form of the hemi-pentahydrate with small amounts of monohydrate. Nonmedicinal ingredients: crospovidone, hydroxypropyl cellulose, hypromellose, indigo carmine, magnesium stearate, microcrystalline cellulose, polyethylene glycol, silicon dioxide, and titanium dioxide.

How should I use this medication?

For preventing osteoporosis in women who are past menopause, the recommended dose of risedronate is 5 mg once daily or 35 mg once weekly.

For treating osteoporosis in women who are past menopause, there are multiple schedules for taking risedronate. It may be taken 5 mg once daily, 35 mg once weekly, 75 mg on 2 consecutive days per month on the same calendar days each month, or 150 mg once a month on the same calendar day each month.

For treating osteoporosis in men, the recommended dose of risedronate is 35 mg once weekly.

For treating and preventing osteoporosis caused by treatment with corticosteroids, the recommended dose of risedronate is 5 mg daily.

For treating Paget’s disease, the recommended dose is 30 mg once daily for 2 months.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important to take this medication exactly as prescribed by your doctor.

The tablet should be taken with plain water at least 30 minutes before the first food or drink of the day. It may also be taken at least 2 hours after any food or drink other than plain water. Do not eat or drink for 2 hours before and for at least 30 minutes after taking the tablet.

All strengths of risedronate should be taken while sitting in an upright position and swallowed whole (not chewed) with at least a half glass of water (i.e., at least 120 mL). Do not lie down for at least 30 minutes after taking the medication to prevent any irritation to your esophagus (the tube connecting the mouth and stomach).

If you are taking calcium supplements or aluminum-, iron-, or magnesium-containing medications (e.g., antacids and mineral supplements), you should take them at a different time of day. When taken together with risedronate, they will decrease the amount of risedronate that is delivered from your stomach into your body and reduce the effectiveness of the risedronate.

If you are taking this medication on a once-daily schedule and then miss a dose, do not take it later in the day. Resume your usual schedule the next morning. Do not take 2 doses at the same time.

If you are taking this medication on a once-weekly basis and you forget to take it on the regularly scheduled day, take one tablet on the day you first remember. Then, return to taking one tablet once a week on your regularly scheduled day. Do not take 2 tablets on the same day.

If you are taking this medication on a twice-monthly basis (schedule of 2 doses on 2 consecutive days per month) and miss a dose and the next month’s scheduled doses are more than 7 days away, take the missed tablet in the morning after the day it is remembered. If both tablets are missed, take one tablet in the morning after the day it is remembered and the second tablet on the next consecutive morning. If you remember the missed dose and are within 7 days of the next month’s scheduled doses, skip the missed dose(s), and wait until the next month’s scheduled dose to continue.

If you are taking this medication on a once-monthly basis and miss a dose and the next month’s scheduled dose is more than 7 days away, take the missed dose in the morning after the day it is remembered. If a dose is missed within 7 days of the next month’s scheduled dose, skip the missed dose and wait until the next month’s scheduled dose to continue.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Do not take risedronate if you:

  • are allergic to risedronate or any ingredients of this medication
  • have low levels of calcium in the blood

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • abdominal pain
  • constipation
  • diarrhea
  • flu-like symptoms (e.g., fever, sore throat)
  • heartburn
  • leg cramps
  • nausea
  • pain in bones, muscles, or joints

Although most of the side effects listed below don’t happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • delayed healing and infection of mouth and jaw (usually after tooth extraction)
  • difficulty swallowing
  • new or unusual pain in the hip, groin or thigh (symptoms of fracture in the thigh bone)
  • numbness, tingling, or muscle spasms (signs of low levels of calcium)
  • painful tongue or mouth sores
  • severe pain in bones, muscles, or joints
  • vision changes or eye pain or inflammation

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • signs of damage to the esophagus (e.g., pain in the esophagus or behind the breastbone, chest pain, difficulty swallowing, pain when swallowing, or new or worsening heartburn)
  • symptoms of a severe allergic reaction (e.g., swelling of the hands, feet, ankles, face, lips, mouth, or throat; difficulty breathing or swallowing)
  • symptoms of a stomach or intestinal ulcer (e.g., nausea, vomiting, abdominal pain, loss of weight or appetite, black or bloody stools, or vomiting blood)

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Atypical femur fracture: There is evidence that long-term use of this class of medication may contribute to a type of rare fracture of the long bone in the thigh (femur) without any form of trauma.

If you experience new or unusual pain in the groin, hip, or thigh area, contact your doctor as soon as possible.

Bone, joint, and muscle problems: On rare occasions, people taking this medication experience severe bone, joint, or muscle pain. This pain usually goes away when the medication is stopped.

Calcium and vitamin D: Calcium and vitamin D are important contributors to bone growth and strength. It may be necessary to take calcium or vitamin D supplements to get the best effect from risedronate if you are not getting enough from your diet. Your doctor may test you for low calcium levels or vitamin D deficiency before you start taking risedronate.

Effects on the esophagus: Risedronate can cause irritation or ulcers of the esophagus (the passage from the throat to the stomach). In some cases, these effects have been severe and have required hospitalization. Stop taking the medication and contact your doctor immediately if you suddenly experience problems swallowing, find it painful to swallow, develop pain behind the sternum (breastbone), or have new or worsening heartburn.

To reduce the risk of irritation of the esophagus, swallow this medication with a full glass of plain water first thing in the morning when you get up. Do not lie down until 30 minutes have passed and you have eaten your first food of the day. Do not chew or suck on the tablet, as this may lead to ulcers in the mouth or throat. Do not take this medication at bedtime or before getting up for the day.

Effects on the stomach and intestines: Rarely, people taking this medication have developed ulcers of the stomach or intestines. Get immediate medical attention if you have symptoms of a stomach or intestinal ulcer, such as nausea, vomiting, abdominal pain, loss of weight or appetite, black or bloody stools, or vomiting blood.

If you have a history of ulcer or other stomach problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Inflammation of the eye: Conditions of eye inflammation have been reported by people using risedronate. If you experience changes to your vision, red eyes, or eye pain, contact your doctor as soon as possible.

Jaw problems: Rarely, risedronate can cause severe jaw problems associated with delayed healing and infection, especially in people with cancer or after tooth extractions. If you experience any mouth sores, pain, swelling, or infection of the mouth or jaw, especially after having a tooth removed, contact your doctor immediately. It is important to maintain good oral hygiene, and undergo regular dental check-ups while taking this medication. Dental work should be done before you start treatment with this medication and if possible dental procedures should be avoided during treatment.

Kidney function: Risedronate is removed from the body by the kidneys. If you have reduced kidney function or kidney disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Risedronate is not recommended for use by people with severely reduced kidney function.

People who cannot stand or sit upright for at least 30 minutes: This medication can cause irritation or ulcers of the esophagus (the tube connecting the mouth and stomach). People who cannot stand or sit upright for at least 30 minutes should use risedronate only if the benefits outweigh the risks.

Pregnancy: Risedronate is not intended for use during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: It is not known if risedronate passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

Children: The safety and effectiveness of using this medication have not been established for children.

What other drugs could interact with this medication?

There may be an interaction between risedronate and any of the following:

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

All material copyright MediResource Inc. 1996 – 2020. Terms and conditions of use. The contents herein are for informational purposes only. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition. Source: www.medbroadcast.com/drug/getdrug/Actonel

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