Saphris and weight gain

Contents

Saphris

SIDE EFFECTS

The following adverse reactions are discussed in more detail in other sections of the labeling:

  • Use in Elderly Patients with Dementia-Related Psychosis
  • Neuroleptic Malignant Syndrome
  • Tardive Dyskinesia
  • Metabolic Changes
  • Hypersensitivity Reactions
  • Orthostatic Hypotension, Syncope, and other Hemodynamic Effects
  • Falls
  • Leukopenia, Neutropenia, and Agranulocytosis
  • QT Interval Prolongation
  • Hyperprolactinemia
  • Seizures
  • Potential for Cognitive and Motor Impairment
  • Body Temperature Regulation
  • Dysphagia

The most common adverse reactions ( ≥ 5% and at least twice the rate of placebo) reported with acute treatment in adults with schizophrenia were akathisia, oral hypoesthesia, and somnolence. The safety profile of SAPHRIS in the maintenance treatment of schizophrenia in adults was similar to that seen with acute treatment.

The most common adverse reactions ( ≥ 5% and at least twice the rate of placebo) reported with acute monotherapy treatment of manic or mixed episodes associated with bipolar I disorder in adults were somnolence, oral hypoesthesia dizziness, extrapyramidal symptoms (excluding akathisia) and akathisia; and during the adjunctive therapy trial in bipolar I disorder in adults were somnolence and oral hypoesthesia. The rates were lower at the 5mg twice daily dose than the 10mg twice daily dose for all of these most common adverse reactions. The safety profile of SAPHRIS in the maintenance treatment of manic or mixed episodes associated with bipolar I disorder in adults was similar to that seen with acute treatment.

The adult information below is derived from a clinical trial database for SAPHRIS consisting of over 5355 patients and/or healthy subjects exposed to one or more sublingual doses of SAPHRIS. A total of 1427 SAPHRIS-treated patients were treated for at least 24 weeks and 785 SAPHRIS-treated patients had at least 52 weeks of exposure at therapeutic doses.

In a 3-week monotherapy trial, the most common adverse reactions ( ≥ 5% and at least twice the rate of placebo) reported in pediatric patients with bipolar I disorder treated with SAPHRIS were somnolence, dizziness, dysgeusia, oral hypoesthesia, nausea, increased appetite, fatigue, and increased weight. No new major safety findings were reported from a 50-week, open-label, uncontrolled safety trial.

A total of 651 pediatric patients were treated with SAPHRIS. Of these patients, 352 pediatric patients were treated with SAPHRIS for at least 180 days and 58 pediatric patients treated with SAPHRIS had at least 1 year of exposure. The safety of SAPHRIS was evaluated in 403 pediatric patients with bipolar I disorder who participated in a 3-week, placebo-controlled, double-blind trial, of whom 302 patients received SAPHRIS at fixed doses ranging from 2.5 mg to 10 mg twice daily.

The stated frequencies of adverse reactions represent the proportion of individuals who experienced a treatment-emergent adverse event of the type listed. A reaction was considered treatment emergent if it occurred for the first time or worsened while receiving therapy following baseline evaluation.

Clinical Trials 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.

Adult Patients with Schizophrenia: The following findings are based on the short-term placebo-controlled pre-marketing trials for schizophrenia (a pool of three 6-week fixed-dose trials and one 6-week flexible-dose trial) in which sublingual SAPHRIS was administered in doses ranging from 5 to 10 mg twice daily.

Adverse Reactions Associated with Discontinuation of Treatment: A total of 9% of SAPHRIS-treated patients and 10% of placebo-treated patients discontinued due to adverse reactions. There were no drug-related adverse reactions associated with discontinuation in patients treated with SAPHRIS at the rate of at least 1% and at least twice the placebo rate.

Adverse Reactions Occurring at an Incidence of 2% or More in SAPHRIS-Treated Patients with Schizophrenia: Adverse reactions associated with the use of SAPHRIS (incidence of 2% or greater, rounded to the nearest percent, and SAPHRIS incidence greater than placebo) that occurred during acute therapy (up to 6-weeks in patients with schizophrenia) are shown in Table 8.

Table 8: Adverse Reactions Reported in 2% or More of Adult Patients in Any SAPHRIS Dose Group and Which Occurred at Greater Incidence Than in the Placebo Group in 6-Week Schizophrenia Trials

System Organ Class/ Preferred Term Placebo
N=378 %
SAPHRIS 5 mg twice daily
N=274 %
SAPHRIS 10 mg twice daily
N=208 %
All SAPHRIS§ 5 mg or 10 mg twice daily
N=572 %
Gastrointestinal disorders
Constipation 6 7 4 5
Dry mouth 1 3 1 2
Oral hypoesthesia 1 6 7 5
Salivary hypersecretion 0 < 1 4 2
Stomach discomfort 1 < 1 3 2
Vomiting 5 4 7 5
General disorders
Fatigue 3 4 3 3
Irritability < 1 2 1 2
Investigations
Increased weight < 1 2 2 3
Metabolism disorders
Increased appetite < 1 3 0 2
Nervous system disorders
Akathisia* 3 4 11 6
Dizziness 4 7 3 5
Extrapyramidal symptoms (excluding akathisia)† 7 9 12 10
Somnolence‡ 7 15 13 13
Psychiatric disorders
Insomnia 13 16 15 15
Vascular disorders
Hypertension 2 2 3 2
* Akathisia includes: akathisia and hyperkinesia.
† Extrapyramidal symptoms included dystonia, oculogyration, dyskinesia, tardive dyskinesia, muscle rigidity, parkinsonism, tremor, and extrapyramidal disorder (excluding akathisia).
‡ Somnolence includes the following events: somnolence, sedation, and hypersomnia.
§ Also includes the Flexible-dose trial (N=90).

Dose-Related Adverse Reactions: In the short term schizophrenia trials the incidence of akathisia appeared to be dose-related (see Table 8).

Monotherapy In Adult Patients With Bipolar Mania

The following findings are based on the short-term placebo-controlled trials for bipolar mania (a pool of two 3-week flexible-dose trials and one 3-week fixed-dose trial) in which sublingual SAPHRIS was administered in doses of 5 mg or 10 mg twice daily.

Adverse Reactions Associated with Discontinuation of Treatment: Approximately 10% (61/620) of SAPHRIS-treated patients in short-term, placebo-controlled trials discontinued treatment due to an adverse reaction, compared with about 7% (22/329) on placebo. There were no adverse reactions associated with discontinuation in patients treated with SAPHRIS at the rate of at least 1% and at least twice the placebo rate

Adverse Reactions Occurring at an Incidence of 2% or More Among SAPHRIS-Treated (Monotherapy) patients with Bipolar I Disorder: Adverse reactions associated with the use of SAPHRIS (incidence of 2% or greater, rounded to the nearest percent, and SAPHRIS incidence greater than placebo) that occurred during acute monotherapy (up to 3-weeks in patients with bipolar mania) are shown in Table 9.

Table 9: Adverse Reactions Reported in 2% or More of Adult Patients in Any SAPHRIS Dose Group and Which Occurred at Greater Incidence Than in the Respective Placebo Group in 3-Week Bipolar Mania Fixed and Flexible Dose Trials

System Organ Class/Preferred Term (Fixed Dose Study) All Placeboa All SAPHRIS 5 mg or 10 mg twice dailyb
Placebo SAPHRIS 5 mg twice daily SAPHRIS 10 mg twice daily
N=126 % N=122 % N=119 % N=329 % N=620 %
Gastrointestinal disorders
Oral Hypoesthesiac 2 13 24 1 10
Nausea 3 4 5 5 5
Constipation 2 4 3 4 4
Dyspepsiah 6 4 5 4 4
Vomiting 2 1 3 3 3
Abdominal Paind 0 2 3 3 3
Dry Mouth 5 3 1 2 3
Toothache 1 2 2 2 3
General disorders
Fatiguee 2 2 5 2 4
Infections and Infestations
Nasopharyngitisi 2 1 5 2 3
Investigations
Weight Increase 1 0 1 1 3
Alanine Aminotransferase Increase 0 0 3 0 1
Metabolism disorders
Increased appetite 2 1 6 2 4
Musculoskeletal and connective tissue disorders
Arthralgia 1 1 2 1 2
Nervous system disorders
Somnolencef 4 20 26 5 23
Dizziness 5 3 5 4 8
Extrapyramidal symptoms (excluding akathisia)g 7 7 11 4 8
Akathisia 1 4 15 2 6
Dysgeusia 0 3 9 < 1 4
Psychiatric Disorders
Bipolar Disorder/Mania j 3 8 3 5 6
Agitation 1 4 3 3 4
Anxiety 3 0 3 2 3
a Includes fixed and flexible dose trials
b SAPHRIS 5 mg to 10 mg twice daily with fixed and flexible dosing.
c Oral Hypoesthesia includes the preferred terms: oral hypoesthesia, oral paresthesia, and oral dysaesthesia. d Abdominal pain includes the preferred terms: abdominal pain, abdominal pain upper, abdominal pain lower, and abdominal discomfort.
e Fatigue includes the preferred terms: fatigue and lethargy.
f Somnolence includes the preferred terms: somnolence, sedation, and hypersomnia.
g Extrapyramidal symptoms (excluding akathisia) includes the preferred terms: dyskinesia, dystonia, resting tremor, tremor, oromandibular dystonia, myoclonus, muscle spasms, muscle rigidity, musculoskeletal stiffness, muscle contractions involuntary, blepharospasm, tongue disorder, and Parkinsonism.
h Dyspepsia includes the preferred terms: dyspepsia and gastrooesophageal reflux disease.
i Nasopharyngitis includes the preferred terms: nasopharyngitis and upper respiratory tract infection.
j Bipolar Disorder/Mania includes the preferred terms: bipolar disorder, bipolar I disorder and mania.

Monotherapy In Pediatric Patients With Bipolar Mania

The following findings are based on a 3-week , placebo-controlled trial for bipolar mania in which SAPHRIS was administered at doses of 2.5 mg, 5 mg, or 10 mg twice daily.

Adverse Reactions Leading to Discontinuation of Treatment: A total of 6.7% (7/104) of patients treated with SAPHRIS 2.5 mg twice daily, 5.1% (5/99) of patients treated with SAPHRIS 5 mg twice daily, and 5.1% (5/99) of patients treated with SAPHRIS 10 mg twice daily discontinued treatment due to adverse reactions compared to 4% (4/101) on placebo. The most common adverse reactions that led to discontinuation in pediatric patients treated with SAPHRIS (rates at least 2% in any SAPHRIS arm and at least twice the placebo rate) were somnolence (3% in the 2.5mg twice daily group, 1% in the 5mg twice daily group, and 2% in the 10mg twice daily group), abdominal pain (2% in the 10mg twice daily group), and nausea (2% in the 10mg twice daily group) No placebo-treated patients dropped out for these events.

Adverse Reactions Occurring with SAPHRIS at an Incidence of 2% or More in SAPHRIS-treated Bipolar I Patients: Adverse reactions associated with the use of SAPHRIS (incidence of ≥ 2% in any SAPHRIS dose group and greater than placebo) that occurred during acute therapy are shown in Table 10.

Table 10: Adverse Reactions Reported in 2% or More of Pediatric Patients (Ages 10 to 17 Years) in Any SAPHRIS Dose Group and Which Occurred at Greater Incidence Than in the Placebo Group in a 3-Week Bipolar Mania Trial

System Organ Class/ AE Preferred Term Placebo SAPHRIS 2.5 mg twice daily SAPHRIS 5 mg twice daily SAPHRIS 10 mg twice daily All SAPHRIS 2.5, 5, and 10 mg
N=101 % N=104 % N=99 % N=99 % N=302 %
Cardiac Disorders
Tachycardia1 0 3 0 1 1
Gastrointestinal Disorders
Oral hypoesthesia2 4 25 25 30 27
Nausea 3 6 6 6 6
Vomiting 3 4 4 4 4
Abdominal pain3 7 9 3 5 6
Glossodynia 0 0 2 0 1
General Disorders and Administrative Site Disorders
Fatigue4 5 4 8 14 9
Irritability 1 1 1 2 1
Injury, Poisoning, and Procedural Complications
Muscle strain 0 0 0 2 1
Investigations
Increased weight 0 6 2 2 3
Hyperinsulinemia5 0 1 3 1 2
ALT increased 0 0 0 2 1
AST increased 0 0 0 2 1
Metabolism and Nutrition Disorders
Increased appetite 2 10 9 6 8
Dehydration 1 0 2 0 1
Musculoskeletal and Connective Tissue Disorders
Myalgia 0 0 2 1 1
Nervous System Disorders
Somnolence6 12 46 53 49 49
Headache 6 8 11 9 9
Dizziness 3 6 10 5 7
Dysgeusia 2 4 5 9 6
Akathisia 0 2 2 1 2
Parkinsonism 0 1 0 2 1
Psychiatric Disorders
Insomnia 3 3 4 3 3
Suicidal ideation 1 4 1 3 3
Anger 0 0 0 2 1
Reproductive System and Breast Disorders
Dysmenorrhea 1 0 2 0 1
Respiratory, Thoracic, and Mediastinal Disorders
Oropharyngeal pain 2 0 3 1 1
Nasal congestion 1 0 2 0 1
Dyspnea 0 0 2 0 1
Skin and Subcutaneous Tissue Disorders
Rash 1 0 1 2 1
1 Includes the preferred terms tachycardia and heart rate increased.
2 Includes the preferred terms oral hypoesthesia, oral paresthesia, and oral dysesthesia.
3 Includes the preferred terms abdominal pain, abdominal pain upper, abdominal pain lower, and abdominal discomfort.
4 Includes the preferred terms fatigue and lethargy.
5 Includes the preferred terms hyperinsulinemia and blood insulin increased.
6 Includes the preferred terms somnolence, sedation, and hypersomnia.

Dose-Related Adverse Reactions: In the short term pediatric bipolar I trial the incidence of fatigue appeared to be dose-related (see Table 10).

Adjunctive Therapy In Adult Patients With Bipolar Mania

The following findings are based on a 12 week placebo-controlled trial (with a 3 week efficacy endpoint) in adult patients with bipolar mania in which sublingual SAPHRIS was administered in doses of 5 mg or 10 mg twice daily as adjunctive therapy with lithium or valproate.

Adverse Reactions Occurring at an Incidence of 2% or More Among SAPHRIS-Treated (Adjunctive) Bipolar I Patients: Adverse reactions associated with the use of SAPHRIS (incidence of 2% or greater, rounded to the nearest percent, and SAPHRIS incidence greater than placebo) that occurred during acute adjunctive therapy at 3 weeks, a time when most of the patients were still participating in the trial, are shown in Table 11.

Table 11: Adverse Reactions Reported in 2% or More of Adult Patients In Any SAPHRIS-Dose Group and Which Occurred at Greater Incidence Than in the Placebo Group at 3 Weeks in Adjunctive Bipolar Mania Trials

System Organ Class/
Preferred Term
Placebo
N=166 %
SAPHRIS 5 mg or 10 mg twice daily*
N=158 %
Gastrointestinal disorders
Dyspepsia 2 3
Oral hypoesthesia 0 5
General disorders
Fatigue 2 4
Edema peripheral < 1 3
Investigations
Increased weight 0 3
Nervous system disorders
Dizziness 2 4
Other extrapyramidal symptoms (excluding akathisia)† 5 6
Somnolence‡ 10 22
Psychiatric disorders
Insomnia 8 10
Vascular disorders
Hypertension < 1 3
* SAPHRIS 5 mg to 10 mg twice daily with flexible dosing.
† Extrapyramidal symptoms included: dystonia, parkinsonism, oculogyration, and tremor (excluding akathisia).
‡ Somnolence includes the following events: somnolence and sedation.

Dystonia

Symptoms of dystonia, prolonged abnormal contractions of muscle groups, may occur in susceptible individuals during the first few days of treatment. Dystonic symptoms include: spasm of the neck muscles, sometimes progressing to tightness of the throat, swallowing difficulty, difficulty breathing, and/or protrusion of the tongue. While these symptoms can occur at low doses, they occur more frequently and with greater severity with high potency and at higher doses of first generation antipsychotic drugs. An elevated risk of acute dystonia is observed in males and younger age groups .

Extrapyramidal Symptoms

In the short-term, placebo-controlled schizophrenia and bipolar mania adult trials, data was objectively collected on the Simpson Angus Rating Scale for extrapyramidal symptoms (EPS), the Barnes Akathisia Scale (for akathisia) and the Assessments of Involuntary Movement Scales (for dyskinesias). The mean change from baseline for the all-SAPHRIS 5 mg or 10 mg twice daily treated group was comparable to placebo in each of the rating scale scores.

In the short-term, placebo-controlled schizophrenia adult trials, the incidence of reported EPS-related events, excluding events related to akathisia, for SAPHRIS-treated patients was 10% versus 7% for placebo; and the incidence of akathisia-related events for SAPHRIS-treated patients was 6% versus 3% for placebo. In short-term placebo-controlled bipolar mania adult trials, the incidence of EPS-related events, excluding events related to akathisia, for SAPHRIS-treated patients was 8% versus 4% for placebo; and the incidence of akathisia-related events for SAPHRIS-treated patients was 7% versus 3% for placebo. The incidence rates of all EPS events (including akathisia) were lower at the 5mg twice daily dose (11% of N=122) than the 10mg twice daily dose (25% of N=119) in a fixed-dose study.

In a 3-week, placebo-controlled pediatric trial with bipolar I disorder, the incidences of EPS-related events, excluding events related to akathisia, were 4%, 3%, and 5% for patients treated with SAPHRIS 2.5 mg, 5 mg, and 10 mg twice daily, respectively, as compared to 3% for placebo-treated patients. EPS-related events include: bradykinesia, dyskinesia, dystonia, oromandibular dystonia, muscle contractions involuntary, muscle twitching, musculoskeletal stiffness, parkinsonism, protrusion tongue, resting tremor, and tremor.

For events of akathisia, incidences were 2%, 2%, and 1% for pediatric patients treated with SAPHRIS 2.5 mg, 5 mg, and 10 mg twice daily, respectively, as compared to 0% for placebo-treated patients.

Other Findings

Oral hypoesthesia and/or oral paresthesia may occur directly after administration of SAPHRIS and usually resolves within 1 hour.

Laboratory Test Abnormalities

Transaminases: Transient elevations in serum transaminases (primarily ALT) in the short-term schizophrenia and bipolar mania adult trials were more common in treated patients. In short-term, placebo-controlled schizophrenia adult trials, the mean increase in transaminase levels for SAPHRIS-treated patients was 1.6 units/L compared to a decrease of 0.4 units/L for placebo-treated patients. The proportion of patients with transaminase elevations ≥ 3 times ULN (at Endpoint) was 0.9% for SAPHRIS-treated patients versus 1.3% for placebo-treated patients. In short-term, placebo-controlled bipolar mania adult trials, the mean increase in transaminase levels for SAPHRIS-treated patients was 6.1units/L compared to a decrease of 3.9units/L in placebo-treated patients. The proportion of patients with transaminase elevations ≥ 3 times upper limit of normal (ULN) (at Endpoint) was 2.1% for SAPHRIS-treated patients versus 0.7% for placebo-treated patients. The incidence rate of transaminase elevations ≥ 3 times ULN is 3% of N=95 for 10mg twice daily dose, and 0% of N=108 for the 5mg twice daily dose and 0% of N=115 for placebo in a fixed-dose study.

In a 52-week, double-blind, comparator-controlled trial that included primarily adult patients with schizophrenia, the mean increase from baseline of ALT was 1.7 units/L.

In a 3-week, placebo-controlled pediatric trial with bipolar I disorder, transient elevations in serum transaminases (primarily ALT) were more common in treated patients. The proportion of pediatric patients with ALT elevations ≥ 3 times upper limit of normal (ULN) was 2.4% for patients treated with SAPHRIS 10 mg twice daily versus none for the other SAPHRIS dose groups and placebo-treated patients.

Prolactin: In short-term, placebo-controlled adult schizophrenia trials, the mean decreases in prolactin levels were 6.5 ng/mL for SAPHRIS-treated patients compared to 10.7 ng/mL for placebo-treated patients. The proportion of patients with prolactin elevations ≥ 4 times ULN (at Endpoint) were 2.6% for SAPHRIS-treated patients versus 0.6% for placebo-treated patients. In short-term, placebo-controlled bipolar mania adult trials, the mean increase in prolactin levels was 6.7ng/mL for SAPHRIS-treated patients compared to a decrease of 1.0 ng/mL for placebo-treated patients. The proportion of patients with prolactin elevations ≥ 4 times ULN (at Endpoint) were 2.0% for SAPHRIS-treated patients versus 0.8% for placebo-treated patients.

In a long-term (52-week), double-blind, comparator-controlled adult trial that included primarily patients with schizophrenia, the mean decrease in prolactin from baseline for SAPHRIS-treated patients was 26.9 ng/mL.

In a 3-week, placebo-controlled pediatric trial with bipolar I disorder, the mean increases (at Endpoint) in prolactin levels were 3.2 ng/mL for patients treated with SAPHRIS 2.5 mg twice daily, 2.1 ng/mL for patients treated with SAPHRIS 5 mg twice daily, and 6.4 ng/mL for patients treated with SAPHRIS 10 mg twice daily compared to an increase of 2.5 ng/mL for placebo-treated patients. There were no reports of prolactin elevations ≥ 4 times ULN (at Endpoint) for patients treated with SAPHRIS or placebo. Galactorrhea or dysmenorrhea were reported in 0% of patients treated with SAPHRIS 2.5 mg twice daily, 2% of patients treated with SAPHRIS 5 mg twice daily, and 1% of patients treated with SAPHRIS 10 mg twice daily compared to 1% of placebo-treated patients. There were no reports of gynecomastia in this trial.

Creatine Kinase (CK): The proportion of adult patients with CK elevations > 3 times ULN at any time were 6.4% and 11.1% for patients treated with SAPHRIS 5 mg twice daily and 10 mg twice daily, respectively, as compared to 6.7% for placebo-treated patients in pre-marketing short-term, fixed-dose trials in schizophrenia and bipolar mania. The clinical relevance of this finding is unknown.

The proportion of patients with CK elevations ≥ 3 times ULN during a 3-week trial in pediatric bipolar I disorder at any time were 1%, 0%, and 1% for patients treated with SAPHRIS 2.5 mg, 5 mg, and 10 mg twice daily, respectively, versus 3% for placebo-treated patients.

Other Adverse Reactions Observed During The Premarketing Evaluation Of SAPHRIS

Following is a list of MedDRA terms that reflect adverse reactions reported by patients treated with sublingual SAPHRIS at multiple doses of ≥ 5 mg twice daily during any phase of a trial within the database of adult patients. The reactions listed are those that could be of clinical importance, as well as reactions that are plausibly drug-related on pharmacologic or other grounds. Reactions already listed for either adults or pediatric patients in other parts of Adverse Reactions (6), or those considered in Contraindications (4), Warnings and Precautions (5) or Overdosage (10) are not included. Reactions are further categorized by MedDRA system organ class and listed in order of decreasing frequency according to the following definitions: those occurring in at least 1/100 patients (frequent) (only those not already listed in the tabulated results from placebo-controlled trials appear in this listing); those occurring in 1/100 to 1/1000 patients (infrequent); and those occurring in fewer than 1/1000 patients (rare).

Blood and lymphatic disorders: infrequent: anemia; rare: thrombocytopenia

Cardiac disorders: infrequent: temporary bundle branch block

Eye disorders: infrequent: accommodation disorder

Gastrointestinal disorders: infrequent: swollen tongue

General disorders: rare: idiosyncratic drug reaction

Investigations: infrequent: hyponatremia

Nervous system disorders: infrequent: dysarthria

Following is a list of MedDRA terms not already listed either for adults or pediatric patients in other parts of Adverse Reactions (6), or those considered in Contraindications (4), Warnings and Precautions (5) or Overdosage (10) that reflect adverse reactions reported by pediatric patients (Ages 10 to 17 years) treated with sublingual SAPHRIS at doses of 2.5 mg, 5 mg, or 10 mg twice daily during any phase of a trial within the database of pediatric patients.

Eye disorders: infrequent: diplopia, vision blurred

Gastrointestinal disorders: infrequent: gastroesophageal reflux disease

Injury, Poisoning, and Procedural Complications: infrequent: fall

Skin and subcutaneous tissue disorders: infrequent: photosensitivity reaction

Renal and urinary disorders: infrequent: enuresis

Postmarketing Experience

The following adverse reactions have been identified during post-approval use of SAPHRIS. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to establish a causal relationship to drug exposure. In many cases, the occurrence of these adverse reactions led to discontinuation of therapy.

  • Application site reactions, primarily in the sublingual area, have been reported. These application site reactions included oral ulcers, blisters, peeling/sloughing, and inflammation.
  • Choking has been reported by patients, some of whom may have also experienced oropharyngeal muscular dysfunction or hypoesthesia.

Read the entire FDA prescribing information for Saphris (Asenapine Sublingual Tablets)

Saphris is the brand name of the prescription drug asenapine, used to treat symptoms of schizophrenia.

The drug is also used by itself or with other medications to treat or prevent episodes of mania (abnormal, frenzied excitement) or mixed mania (abnormal, frenzied excitement along with depression) in people with bipolar disorder.

Saphris is in a class of drugs known as atypical antipsychotics.

The medication was approved by the Food and Drug Administration (FDA) in 2009 to treat schizophrenia and bipolar disorder. It’s manufactured by Forest Pharmaceuticals, Inc.

Saphris Black-Box Warning

Saphris carries a black-box warning because it may increase the risk of death in older adults with dementia.

Saphris isn’t FDA approved to treat behavioral problems in this group of people.

Saphris can cause serious neurologic problems. You should call your doctor immediately if you experience:

  • Stiff muscles
  • High fever
  • Sweating
  • Confusion
  • Fast or uneven heartbeat
  • Lightheadedness
  • Tremors
  • Twitching
  • Uncontrollable movement of the eyes, lips, tongue, face, arms, or legs

Before taking this medication, tell your doctor if you have or have ever had:

  • Diabetes (or a family history of the disease)
  • Signs of dehydration, including severe diarrhea or vomiting
  • Prolonged QT interval (a problem with the heart that may cause an irregular heartbeat)
  • Low blood pressure
  • A heart attack
  • A slow or irregular heartbeat
  • A stroke or mini stroke
  • Seizures
  • Breast cancer
  • A low white blood cell count
  • Low levels of potassium or magnesium in your blood
  • Heart disease
  • Liver disease

You should also alert your physician if you have ever used street drugs or abused prescription drugs before taking this medicine.

This drug may make it harder for your body to cool down when it gets hot. Avoid vigorous exercise and excessive heat while taking Saphris. Also, make sure you consume plenty of fluids.

You might experience dizziness, fainting, or lightheadedness when you get up from a lying position too quickly while taking Saphris.

Try resting your feet on the floor for a few minutes before standing to avoid this side effect.

Tell your doctor you are taking Saphris before having any kind of surgery, including a dental procedure.

Saphris may cause an increase in blood sugar and may increase your risk for diabetes. Tell your doctor if you experience frequent urination, extreme thirst, extreme hunger, blurred vision, or weakness.

This medicine will help control your symptoms, but it won’t cure your condition. Continue to take Saphris even if you feel well.

Saphris Withdrawal

You shouldn’t stop taking Saphris without first talking to your doctor.

Stopping the medication suddenly could cause unwanted withdrawal symptoms.

Your doctor might decide to take you off the drug slowly to avoid this potential effect.

Pregnancy and Saphris

Saphris is an FDA Pregnancy Category C drug, which means harm to an unborn baby is possible.

Tell your doctor if you are pregnant or plan to become pregnant while taking this drug.

Taking antipsychotic medications during the last three months of pregnancy can cause withdrawal symptoms in newborns.

However, you might have withdrawal symptoms if you stop taking the drug during pregnancy.

Talk to your doctor about the risks and benefits of taking Saphris while pregnant.

It’s not known whether Saphris passes into breast milk or could harm a breastfeeding baby.

You shouldn’t breastfeed while taking this medicine without first talking to your doctor.

What is Saphris?

Saphris is a medication known as an atypical antipsychotic that is used to treat symptoms of schizophrenia.

When did the U.S. Food and Drug Administration (FDA) approve the medication?

Saphris was first approved by the FDA to treat schizophrenia in 2009.

Is there a generic version of Saphris?

No, there are no generic versions of the drug available for use in the United States.

Are there any major differences between Saphris and other antipsychotics used to treat Saphris?

Saphris belongs to the class of medications known as atypical antipsychotics or second generation psychotics. Atypical antipsychotics generally have fewer side effects than conventional antipsychotics. Talk to your doctor about what might work best for you and the costs and benefits of taking the medication. Some people may need to try several different antipsychotics before they find the most effective with the fewest side effects.

Can children take Saphris?

The medication has not been approved for children or teens with schizophrenia, but the FDA recently approved use of the drug for treating bipolar disorder in pediatric patients ages 10 and older. Talk to your child’s doctor about the risks of using the medication, which may include increased suicidal thoughts.

Are there potential interaction issues for people taking Saphris and any other drugs?

There are hundreds of drugs which are known to interact with Saphris in major, moderate, or mild ways, so let your doctor know what other medications you are taking before you begin taking the medication. Some of these include antihypertensive drugs, fluvoxamine, paroxetine, antibiotics, antidepressants, antihistamines, dextromethorphan, anxiety medication, seizure medication, sedatives, and tranquilizers, among others.

Are there any other medical conditions that would make someone ineligible for Saphris therapy?

Talk to your doctor about other medical conditions before you take Saphris, such as diabetes, cardiovascular disease or events, low white blood cell count, tardive dyskinesia, dementia, seizures, neuroleptic malignant syndrome (NMS), or a history of suicidal thoughts.

What is the typical dose that would be prescribed to someone taking Saphris?

Dosages for the medication typically range between 5 and 10 mg taken twice daily.

What do I do if I miss a dose?

Take the dose of Saphris when you remember, but skip the missed dose if it it’s almost time for your next dose. You should never take extra doses of the medication to make up for missed doses.

What side effects can Saphris cause?

The side effects of Saphris can include:

  • Stomach pain
  • Constipation
  • Increased appetite
  • Weight gain
  • Changes in taste
  • Dry mouth
  • Vomiting
  • Heartburn
  • Increased saliva
  • Toothache
  • Join, arm, or leg pain
  • Fatigue
  • Loss of feeling in mouth
  • Restlessness
  • Anxiety or irritability
  • Trouble sleeping
  • Missed menstrual periods
  • Decreased sexual ability

It also is recommended that you wait to drive or operate machinery until you know how the medication affects you. It is also not recommend that people avoid alcohol and illegal drugs while on the medication, as they can worsen adverse effects. Report major side effects to your doctor immediately, which can include itching, rash, muscle pain, sweating, irregular heartbeat, trouble swallowing or breathing, confusion, fever, swelling, hoarse throat, wheezing, dizziness, seizures, uncontrollable movement, or discolored urine. You can also report side effects to the FDA at 1-800-FDA-1088 or online.

What are the potential long-term effects of taking Saphris?

Your doctor should monitor for progression of potential long-term side effects, which can include tardive dyskinesia (TD). Atypical antipsychotics may also increase the risk of cardiovascular side effects, diabetes, weight gain, and high cholesterol.

Is it safe for a woman who is pregnant, about to become pregnant, or nursing to take Saphris?

There have been no controlled human pregnancy studies on the effects of Saphris, but animal studies have demonstrated risk and decreased birth weight. It is not known whether the drug can be transferred via breast milk and harm a baby. Therefore, talk to your doctor if you are pregnant, planning to become pregnant, or are nursing before you take Saphris.

Can symptoms occur if Saphris is discontinued?

It’s important not to discontinue use of the drug if you feel better. Maintain contact with your doctor and seek medical attention if necessary when discontinuing the drug. Withdrawal symptoms of Saphris can include vomiting, nausea, fever, headache, and dizziness.

What should I do if I overdose on Saphris?

An overdose of Saphris could be fatal, so seek immediately help or call the Poison Help Line at 1-800-222-1222 if you overdose. Overdose symptoms can include agitation, confusion, and restless muscle movement.

Is Saphris habit-forming?
Saphris has no habit-forming potential, but it is not recommended that you discontinue use of the drug before talking with your doctor, as withdrawal symptoms can occur.

How much does Saphris cost?

According to goodrx.com, 30 orally disintegrating tablets of of 10 mg of Saphris cost approximately $600.

Are there any disadvantages to Saphris?

The biggest disadvantages of Saphris are potential side effects and the potential long-term side effects, which can include tardive dyskinesia.

DISCLAIMER: The information contained herein should NOT be used as a substitute for the advice of an appropriately qualified and licensed physician or other health care provider. This article mentions drugs that were FDA-approved and available at the time of publication and may not include all possible drug interactions or all FDA warnings or alerts. The author of this page explicitly does not endorse this drug or any specific treatment method. If you have health questions or concerns about interactions, please check with your physician or go to the FDA site for a comprehensive list of warnings.

Article Sources Last Updated: Nov 25, 2018

Generic Name: asenapine (a SEN a peen)
Brand Names: Saphris, Saphris Black Cherry

Medically reviewed by Sophia Entringer, PharmD Last updated on Apr 21, 2019.

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What is Saphris?

Saphris (asenapine) is an antipsychotic medication. It works by changing the actions of chemicals in the brain.

Saphris sublingual tablets are used to treat schizophrenia in adults, and bipolar I disorder in adults and children who are at least 10 years old.

Saphris may also be used for purposes not listed in this medication guide.

Important information

You should not use Saphris if you are allergic to asenapine, or if you have severe liver disease.

Saphris can cause serious neurologic problems. Stop taking this medicine and call your doctor at once if you have: very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, feeling light-headed, tremors, twitching, or uncontrollable movements of your eyes, lips, tongue, face, arms, or legs.

Saphris is not FDA-approved for use in psychotic conditions related to dementia. Asenapine may increase the risk of death in older adults with dementia-related conditions.

Before taking this medicine

You should not use Saphris if you are allergic to asenapine, or if you have:

  • severe liver disease; or

  • a history of severe allergic reaction to asenapine.

To make sure Saphris is safe for you, tell your doctor if you have:

  • liver disease;

  • heart disease, high blood pressure, heart rhythm problems;

  • a history of heart attack or stroke;

  • a history of breast cancer;

  • seizures or epilepsy;

  • diabetes (asenapine may raise your blood sugar);

  • trouble swallowing;

  • Parkinson’s disease;

  • a history of low white blood cell (WBC) counts; or

  • a personal or family history of Long QT syndrome.

It is not known whether Saphris will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

Taking antipsychotic medication during the last 3 months of pregnancy may cause problems in the newborn such as withdrawal symptoms, breathing problems, feeding problems, fussiness, tremors, and limp or stiff muscles. However, you may have withdrawal symptoms or other problems if you stop taking your medicine during pregnancy. If you become pregnant while taking Saphris, do not stop taking it without your doctor’s advice.

It is not known whether asenapine passes into breast milk or if it could affect the nursing baby. Tell your doctor if you are breast-feeding.

Saphris should not be given to a child younger than 10 years old. Saphris is not FDA-approved for schizophrenia in anyone younger than 18 years old.

How should I take Saphris?

Saphris is usually taken 2 times per day. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Read all patient information, medication guides, and instruction sheets provided to you. Ask your doctor or pharmacist if you have any questions.

To take Saphris sublingual (under the tongue) tablets:

  • Keep the tablet in its blister pack until you are ready to take the medicine. Open the package and peel back the colored tab from the tablet blister. Do not push a tablet through the blister or you may damage the tablet.

  • Using dry hands, gently remove the tablet and place it under your tongue. Do not crush or break the tablet. It will begin to dissolve right away.

  • Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing.

  • Do not eat or drink anything for 10 minutes after the tablet has dissolved.

Saphris may cause you to have high blood sugar (hyperglycemia). Symptoms include increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, and blurred vision. If you are diabetic, check your blood sugar levels on a regular basis while you are taking Saphris.

Your doctor will need to check your progress while you are using Saphris.

Store at room temperature away from moisture and heat.

Saphris dosing information

Usual Adult Dose of Saphris for Schizophrenia:

Acute treatment:
Starting dose: 5 mg sublingually twice a day
Recommended dose: 5 mg sublingually twice a day, if tolerated may increase to 10 mg sublingually twice a day after 1 week if necessary
Maximum dose: 10 mg sublingually twice a day
Comments: Controlled trials revealed no added benefit with the higher dose, but a clear increase in certain adverse reactions. The safety of doses above 10 mg twice daily has not been evaluated in clinical studies.
Maintenance Treatment:
Recommended dose: 5 to 10 mg sublingually twice a day
Maximum dose: 10 mg sublingually twice a day
Comments: There is no available evidence to answer the question of how long the schizophrenic patient should remain on therapy; it is generally recommended that responding patients be continued beyond the acute response.
Use: Treatment of schizophrenia.

Usual Adult Dose of Saphris for Bipolar Disorder:

Monotherapy:
Starting dose: 10 mg sublingually twice a day
Recommended dose: 5 to 10 mg sublingually twice a day
Maximum dose: 10 mg sublingually twice a day
Comment: In controlled trials, the starting dose was 10 mg twice daily. On the second and subsequent days, the dose could be lowered to 5 mg twice daily, however less than 10% of patients had their dose reduced.
Adjunctive Therapy:
Starting dose: 5 mg sublingually twice a day
Maintenance dose: 5 to 10 mg sublingually twice a day
Maximum dose: 10 mg sublingually twice a day

-The dose should be titrated based on clinical response and tolerability.
-There is no available evidence to answer the question of how long the patient should remain on therapy; it is generally recommended that responding patients be continued beyond the acute response.
Uses: For the acute treatment of manic or mixed episodes associated with bipolar 1 disorder either as monotherapy or as adjunctive therapy with either lithium or valproate.

Usual Pediatric Dose for Bipolar Disorder:

Age: 10 years or older
Starting dose: 2.5 mg sublingually twice a day
Dose titration: After 3 days, may increase to 5 mg sublingually twice daily, and after an additional 3 days to 10 mg twice a day, as needed and as tolerated
Recommended dose: 2.5 to 10 mg sublingually twice a day
Maximum dose: 10 mg sublingually twice a day
Comment: Pediatric patients appear to be more sensitive to dystonia with initial dosing and therefore gradual dose escalation is recommended. The safety of doses above 10 mg twice a day has not been studied.
Use: As monotherapy for the acute treatment of manic or mixed episodes associated with bipolar 1 disorder.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking Saphris?

While you are taking Saphris, you may be more sensitive to temperature extremes such as very hot or cold conditions. Avoid getting too cold, or becoming overheated or dehydrated. Drink plenty of fluids, especially in hot weather and during exercise. It is easier to become dangerously overheated and dehydrated while you are taking Saphris.

Saphris may impair your thinking or reactions. Avoid driving or operating machinery until you know how this medicine will affect you.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Dizziness or severe drowsiness can cause falls, fractures, or other injuries.

Avoid drinking alcohol. Dangerous side effects could occur.

Saphris side effects

Get emergency medical help if you have signs of an allergic reaction to Saphris: hives; fast heartbeats, feeling light-headed; wheezing, difficult breathing; swelling of your face, lips, tongue, or throat.

Saphris can cause serious neurologic problems. Stop taking this medicine and call your doctor at once if you have: very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, feeling light-headed, tremors, twitching, or uncontrollable movements of your eyes, lips, tongue, face, arms, or legs.

High doses or long-term use of Saphris can cause a serious movement disorder that may not be reversible. Symptoms of this disorder include uncontrollable muscle movements of your lips, tongue, eyes, face, arms, or legs. The longer you take Saphris, the more likely you are to develop a serious movement disorder. The risk of this side effect is higher in women and older adults.

Call your doctor at once if you have:

  • slow heartbeats, a light-headed feeling (like you might pass out);

  • uncontrolled muscle movements in your face (chewing, lip smacking, frowning, tongue movement, blinking or eye movement);

  • sudden weakness or ill feeling, fever, chills, sore throat, swollen gums, painful mouth sores, skin sores, cold or flu symptoms, cough;

  • breast pain or swelling, nipple discharge;

  • trouble swallowing; or

  • sudden numbness or weakness (especially on one side of the body), sudden severe headache, slurred speech, problems with vision or balance.

Common Saphris side effects may include:

  • dizziness, drowsiness, feeling tired;

  • inability to sleep;

  • feeling restless or being unable to sit still;

  • numbness or tingling inside or around your mouth;

  • ulcers, blisters, swelling, or peeling of your gums;

  • nausea, altered sense of taste; or

  • increased appetite, weight gain.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Saphris?

Taking Saphris with other drugs that make you sleepy or slow your breathing can cause dangerous or life-threatening side effects. Ask your doctor before taking a sleeping pill, narcotic pain medicine, prescription cough medicine, a muscle relaxer, or medicine for anxiety, depression, or seizures.

Tell your doctor about all your current medicines and any you start or stop using, especially:

  • an antibiotic;

  • an antidepressant;

  • anti-malaria medication;

  • cancer medicine;

  • heart or blood pressure medicine; or

  • other antipsychotic medications.

This list is not complete. Other drugs may interact with asenapine, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Saphris only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Copyright 1996-2020 Cerner Multum, Inc. Version: 6.05.

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Asenapine

Before taking asenapine,

  • tell your doctor and pharmacist if you are allergic to asenapine, any other medications, or any of the ingredients in asenapine sublingual tablets. Ask your pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what other 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: certain antibiotics including gatifloxacin (Tequin) (not available in the U.S.) and moxifloxacin (Avelox); antidepressants including clomipramine (Anafranil), duloxetine (Cymbalta), fluvoxamine (Luvox), and paroxetine (Paxil, Pexeva); antihistamines; dextromethorphan (in Delsym, in Mucinex); ipratropium; medications for anxiety and high blood pressure; certain medications for irregular heartbeat such as amiodarone (Cordarone, Pacerone), procainamide, quinidine, and sotalol (Betapace, Sorine); medications for glaucoma, inflammatory bowel disease, motion sickness, myasthenia gravis, Parkinson’s disease, ulcers, or urinary problems;medications for mental illness such as chlorpromazine (Thorazine), thioridazine, and ziprasidone (Geodon); medications for seizures;sedatives; sleeping pills; and tranquilizers.Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you or anyone in your family has or has ever had diabetes; if you have severe diarrhea or vomiting or you think you may be dehydrated; if you have ever used street drugs or misused prescription medications; and if you have or have ever had thoughts about harming or killing yourself; a prolonged QT interval (a rare heart problem that may cause irregular heartbeat, fainting, or sudden death); low blood pressure; a heart attack; heart failure; a slow or irregular heartbeat; a stroke or TIA (ministroke); seizures; breast cancer; a low level of white blood cells in your blood or a decrease in white blood cells caused by a medication you have taken; a low level of potassium or magnesium in your blood; dyslipidemia (high cholesterol levels); trouble keeping your balance; any condition that makes it difficult for you to swallow; or heart or liver disease.
  • tell your doctor if you are pregnant, especially if you are in the last few months of your pregnancy, or if you plan to become pregnant or are breastfeeding. If you become pregnant while taking asenapine, call your doctor. Asenapine may cause problems in newborns following delivery if it is taken during the last months of pregnancy.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking asenapine.
  • you should know that asenapine may make you drowsy. Do not drive a car or operate machinery until you know how this medication affects you.
  • ask your doctor about the safe use of alcoholic beverages while you are taking asenapine. Alcohol can make the side effects of asenapine worse.
  • you should know that asenapine may cause dizziness, lightheadedness, and fainting when you get up too quickly from a lying position. This is more common when you first start taking asenapine. To help avoid this problem, get out of bed slowly, resting your feet on the floor for a few minutes before standing up.
  • you should know that asenapine may make it harder for your body to cool down when it gets very hot. While you are taking asenapine, you should avoid excessive exercise, stay inside as much as possible and dress lightly in hot weather, stay out of the sun, and drink plenty of fluids.
  • you should know that you may experience hyperglycemia (increase in your blood sugar) while you are taking this medication, even if you do not already have diabetes. If you have schizophrenia, you are more likely to develop diabetes than people who do not have schizophrenia, and taking asenapine or similar medications may increase this risk. Tell your doctor immediately if you have any of the following symptoms while you are taking asenapine: extreme thirst, frequent urination, extreme hunger, blurred vision, or weakness. It is very important to call your doctor as soon as you have any of these symptoms, because high blood sugar can cause a serious condition called ketoacidosis. Ketoacidosis may become life-threatening if it is not treated at an early stage. Symptoms of ketoacidosis include dry mouth, nausea and vomiting, shortness of breath, breath that smells fruity, and decreased consciousness.

Saphris (Asenapine) & Weight Gain: What Should You Expect?

Saphris (Asenapine) is an atypical antipsychotic medication that was approved in 2009 for the treatment of schizophrenia and bipolar disorder. It is a relatively new atypical antipsychotic, and is considered a chemical derivative of the tetracyclic antidepressant (TeCA) mianserin. It is manufactured in a sublingual format, which some may perceive as an upgraded or novel modality of administration.

Due to the fact that the drug is relatively new and many people fail to achieve symptomatic relief from older medications, many people have turned to Saphris. Although evidence suggests that it may not be as effective as other antipsychotics for schizophrenia, certain individuals find it highly effective. Perhaps most alarming was that there were significant rates of discontinuation of the medication in clinical trials.

High discontinuation rates during clinical trials are generally a sign of intolerable, adverse reactions. One of many common adverse reactions associated with Saphris is weight gain. While most medical professionals consider the weight gain to be moderate, gaining a significant amount of weight on Saphris may contribute to depressive symptoms stemming from poor self-image and may create an entirely new set of health risks associated with obesity.

Saphris (Asenapine) and Weight Changes (Scientific Research)

There is significant scientific research suggesting that Saphris is unlikely to cause significant weight gain, regardless of the term of administration. While users gained slightly more weight in long-term trials (12+ weeks), the weight gain was not significantly different from individuals involved in short-term trials (less than 12 weeks). The average reported weight gain from Saphris was under 3 lbs. after an entire year’s worth of treatment at 5 mg or 10 mg dosages.

2014: Researchers compiled a report documenting weight changes and metabolic effects derived from Saphris and Zyprexa compared to placebos in adults. Data was extracted from 17 trials comparing Saphris to a placebo at dosages of 5 mg to 10 mg (taken twice per day). The number of participants was 1,748 and the medication was ingested for a period of up to 6 weeks.

Baseline bodyweight, BMI, fasting lipids, and glucose levels were assessed. It was reported that weight changes from Saphris were more significant than a placebo and similar regardless of psychiatric diagnosis. Changes in fasting glucose were considered significantly elevated among Saphris users compared to those taking a placebo.

That said, when Saphris was compared to Zyprexa, it appeared to produce less substantial weight change and superior levels of various biomarkers (e.g. cholesterol, glucose, LDL, triglycerides). While each respective drugs’ efficacy is subject to individual variation, it appears as though Saphris is less likely to significantly disrupt various homeostatic biological processes compared to Zyprexa.

  • Source: http://www.ncbi.nlm.nih.gov/pubmed/24499969

2013: A study published in 2013 documented various adverse effects that occurred in at least 2% of Saphris users. One of these adverse effects happened to be an increase in bodyweight, occurring in approximately 3.5% of users compared to just 0.4% of individuals assigned to a placebo. Other adverse effects that may have contributed to weight gain were sedation (occurring in 9.1% of users) and somnolence (occurring in 8.4% of users).

  • Source: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3539266/

2012: A publication from 2012 reviewed the literature of new atypical antipsychotics and determined that of Saphris, Fanapt, Latuda, and Invega – Saphris was most associated with significant weight gain. Not only was weight increase more likely to be statistically significant based on a review of 5 trials (with 1,360 participants), the average weight increase was more substantial.

Based on 3 placebo-controlled, short-term trials (spanning less than 12 weeks), average weight gain associated with those taking Saphris was an estimated 2.55 lbs. Longer-term, placebo-controlled trials suggested that average weight gain on Saphris was just under 3 lbs.

  • Source: http://www.ncbi.nlm.nih.gov/pubmed/22900950

2011: A report from 2011 documented side effects associated with Saphris for the treatment of bipolar disorder. It was documented that an estimated 31% of participants reported significant weight gain. This figure differs from the estimates promoted to the general public by the manufacturers of Saphris; they suggest that only 6% of users gain weight.

The 31% of individuals experiencing weight gain is thought to be an improvement over an estimated 55% of users who report weight gain on the medication Zyprexa. The mechanisms associated with weight gain from Saphris may be related to alterations in fasting blood glucose levels that have been noted in approximately 18% of users.

  • Source: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3140314/

2011: Another publication from 2011 documents the likelihood of gaining weight on Saphris. Based on placebo-controlled trials, the likelihood of individuals experiencing significant weight gain (at least 7% of bodyweight increase) occurred in an estimated 5% of users. Authors noted that no significant metabolic alterations were recorded as a result of Saphris.

They did note that Saphris had increased propensity to cause somnolence in an estimated 24% of users. That said, it is important to note that the reported weight gain experienced in less than 5% of users was based off of data from 3-week trials. Longer-term trials of the medication may have resulted in more substantial weight change.

  • Source: http://www.ncbi.nlm.nih.gov/pubmed/20950326

2011: A study published in 2011 reported the side effects associated with Saphris for the treatment of schizophrenia. It was administered sublingually in 5 mg or 10 mg dosages and was considered well-tolerated by participants. Researchers suggested that Saphris didn’t significantly affect lipids and glucose levels.

They did note that it promoted sedation, but was associated with a relatively low likelihood of weight gain. This report documented average weight gain of less than 2.2 lbs. after a full year’s treatment. Perhaps some of the weight gain experienced from Saphris is based on its sedating properties.

  • Source: http://www.ncbi.nlm.nih.gov/pubmed/22217438

2011: Another report from 2011 documented that some weight gain is observed among those taking Saphris compared to a placebo. However, the weight gain is generally less significant when compared to other atypical antipsychotic medications such as Risperdal and Zyprexa. Authors highlighted the fact that in a clinical trial spanning over 6 weeks, only 4.3% of Saphris users experienced significant weight gain.

It was suggested that Saphris may be less likely to cause weight gain as a result of its mechanism of action. Specifically, compared to other antipsychotics, Saphris doesn’t elicit significant effects on the M3 muscarinic receptor as an antagonist. It has long been suggested that various antipsychotics like Zyprexa have a high affinity for the M3 muscarinic receptors which ultimately contribute to significant weight gain.

  • Source: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2924192/

2011: Researchers document that no more than 5% of those taking Saphris experience clinically relevant weight gain. In addition, they report that no substantial changes in baseline lipids, glucose, or liver enzymes are apparent among individuals taking Saphris at 5 mg and 10 mg (trice daily) compared to a placebo. According to this report, your chances of gaining weight as a result of Saphris are relatively slim.

  • Source: http://www.ncbi.nlm.nih.gov/pubmed/21655346

2010: In a double-blind trial of Saphris for those with schizophrenia, it was determined that dosages of 5 mg or 10 mg daily resulted in modest weight gain. The study incorporated a large sample of 913 participants. That said, weight gain after a full year of treatment was under 2 lbs. – substantially less than Zyprexa.

  • Source: http://www.ncbi.nlm.nih.gov/pubmed/20205074

2009: A Phase III randomized, double-blind clinical trial assessed Saphris for the treatment of schizophrenia in 1,219 participants. Significant weight gain was reported in just under 15% of those taking Saphris compared to 36% of those taking Zyprexa. Results from this clinical trial indicate that Saphris is less than half as likely to cause clinically significant weight gain among users compared to Zyprexa.

  • Source: http://www.ncbi.nlm.nih.gov/pubmed/19851515

Consensus: Saphris causes modest weight gain; nearly weight neutral

It appears as though Saphris may cause a small amount of clinically significant weight gain (at least 7% of your bodyweight) in between 5% and 7% of users. Therefore many doctors and psychiatrists may consider this atypical antipsychotic to be relatively “weight neutral” compared to others. When compared to older atypical antipsychotics like Zyprexa and Risperdal, the likelihood of weight gain is miniscule.

Assuming you end up gaining weight from Saphris, the literature indicates that average weight gain after 1 year is under 3 lbs. Between 5 and 7 people out of 100 will gain more than 7% of their bodyweight on the drug. For most people, gaining a little bit of weight from Saphris won’t be a big deal assuming it is successfully managing symptoms of schizophrenia or bipolar disorder.

How Saphris Causes Weight Gain

It is important to acknowledge the fact that weight gain associated with Saphris may be underreported in the literature. Many studies are relatively short-term (several weeks) and even the long-term trials do not mimic outcomes among those who have taken the drug for much longer than a full year (e.g. 5 years). Weight gain from Saphris may be due to a unique combination of the factors listed below.

  • Appetite increase: It is well known that many antipsychotic medications stimulate appetite. If you start taking Saphris and notice that your stomach is constantly growling and you have suddenly developed an insatiable appetite, it may contribute to your weight gain. Keep in mind that appetite changes may be temporary as your body adjusts to the medication. However, assuming your appetite skyrockets and you find yourself raiding the fridge – it’ll be tough to keep the weight off.
  • Blood sugar increase: Some studies have demonstrated that Saphris spikes fasting blood glucose levels in an estimated 18% of users. Assuming your fasting blood sugar levels increase as a result of the medication, you may have a tougher time avoiding weight gain. High levels of blood sugar result in increased stores of body-fat and elicit a cascade of other physiological changes that promote weight gain.
  • Fatigue: Certain users of Saphris will notice that their energy levels plummet and they feel lethargic. Individuals that experience lethargy as a result of the medication may end up spending more time on the couch, sedentary, or sleeping in bed. As a result of lethargy-induced sedentarism, less calories will be burned and metabolism slows; the perfect storm for weight gain.
  • Fat storage: In many cases, users of antipsychotics like Saphris will notice that they begin building excess body fat. An increase in body fat may be caused by a variety of factors including metabolism slowing, hormone alterations, blood glucose concentrations, etc. Saphris is thought to alter an array of physiological functions, which may lead to accumulation of fat stores.
  • Food cravings: In addition to an appetite increase, some people may notice that they develop significant cravings for sweets (sugary foods) and carbohydrates. When consumed in excess, sweets and carbohydrates further spike blood glucose levels and contribute to weight gain. Should you notice that you’re craving candies, potato chips, and fast-food – it could be related to the medication.
  • Hormone levels: There is preliminary evidence that long-term administration of antipsychotics can lead to spikes in the hormone ghrelin. Heightened levels of ghrelin are associated with increased hunger. In other words, consistent administration of Saphris may be increasing your ghrelin, which causes you to feel hungry all the time. When you feel hungrier, you’ll have a difficult time resisting food and will gain weight. It is important to consider that an array of other hormones may be affected by Saphris such as testosterone, estrogen, cortisol, etc.
  • Metabolism slowing: It is common for your metabolism to slow while taking Saphris. The slowed metabolism may be due to increased sedation, hormonal changes, and less physical activity. While you may make a concerted effort to counteract this metabolism slowing my hitting the gym harder and selecting healthier foods, it may not prove effective for everyone.
  • Motivational deficit: It is possible to experience a decrease in motivation to hit the gym or make healthy choices as a result of Saphris. Since the drug is substantially altering your neurochemistry, the drug-induced changes may alleviate your symptoms of schizophrenia (or bipolar disorder), but may simultaneous sap you of energy and motivation. A reduction in motivation can indirectly cause weight gain.
  • Sedation: Saphris is known to cause significant sedation and somnolence among users. In fact, the sedation and somnolence are much more likely to occur than weight gain. However, it is important to consider that a consequence of sedation from Saphris could be increased weight gain. If you feel sedated, you may sleep excessively and avoid exercising – which will likely promote weight gain.
  • Social eating: Assuming Saphris is successfully managing symptoms of your psychiatric condition, you may feel happier and more inclined to socialize. Increased socialization is often associated with going out to eat. The cultural revolution of the past hundred years resulted in an increased number of unhealthy fast-food restaurants and choices. If you’re going out to eat more since taking Saphris, the foods you’re eating may be causing the weight gain.
  • Taste improvement: Saphris is known to significantly alter neurochemistry, which helps alleviate symptoms of psychiatric illnesses. Some of the alterations to neurotransmitters may result in perceived taste enhancement. Those that experience enhanced taste as a result of taking Saphris may be more drawn to food, particularly unhealthy foods like simple carbs and other sugar-laden sweets.

Note: It is important to consider that weight gain on Saphris may be caused by a variety of the aforementioned factors. In other words, someone may gain weight as a result of sleepiness, metabolic slowing, motivational deficits, junk food cravings, and blood sugar increases. Other individuals may gain weight mostly due to just one or two factors.

  • Source: http://www.ncbi.nlm.nih.gov/pubmed/21474903

Factors that influence weight gain on Saphris (Asenapine)

It is important to consider the fact that weight gain on any medication is due to an array of individual factors. Two people may take Saphris, yet one may experience major weight gain in a short period of time, while another may experience no significant weight gain. Factors that may influence weight gain include: medication interactions, lifestyle, genetics, duration of treatment, and dosage.

1. Interactions

It is important to consider the possibility that Saphris may be interacting with other medications to cause weight gain. Furthermore, if you start another medication at the same time as Saphris, you may want to investigate whether the weight gain may be more related to that particular drug. In many cases, people gain weight as a result of synergistic mechanisms of psychiatric medications.

For example, someone taking Saphris along with an antidepressant may experience amplified food cravings, neurotransmitter alterations, hormone alterations, and metabolic slowing. The combined effect of multiple (or a cocktail) of psychiatric drugs may be more likely to induce weight gain. Similarly, certain medications that have a stimulatory effect may help offset any weight gain that may occur as a result of Saphris.

2. Lifestyle

It is important to consider an array of lifestyle choices that may contribute to weight gain including: dietary choices, circadian rhythm management, sleep hours per night, stress level, and daily physical activity. Someone who normally eats an unhealthy diet, fails to get enough sleep, and is physically inactive may be more likely to gain weight on Saphris.

Someone who engages in an unhealthy lifestyle may have a difficult time distinguishing whether the Saphris caused the weight gain or whether increases in weight were caused by lifestyle choices. It is also important to consider the fact that Saphris could exacerbate the effects of certain lifestyle choices such as sedentarism and/or eating unhealthy. Exacerbation of poor lifestyle choices may result in more substantial weight increases.

3. Genetics

Many people make healthy lifestyle choices and don’t take any other medications along with Saphris that could promote weight gain, but still end up gaining weight. This could be due to both neurophysiology and genetics. People with certain genetic polymorphisms are thought to be at increased risk for obesity and weight gain.

Assuming you have unfavorable genetics for weight management, gaining weight on Saphris may be more likely. In addition, some people have genes that don’t respond well to administration of Saphris. You may want to consider using a test like GeneSight to investigate any potential interactions between Saphris and your genetics.

4. Dosage

In general, the greater the dosage you’re taking, the more likely you are to gain weight. Specifically, the propensity of weight gain on Saphris may be a result of the dosage in relationship to your baseline bodyweight and/or size. A larger person may require a greater dosage of the drug compared to a smaller person, but if the smaller person is administered the same dosage – weight gain may be more likely.

Increased dosages tend to provoke more weight gain due to the fact that more of the drug has influence over neurophysiological function. Therefore if you want to minimize the likelihood that you’ll gain weight on Saphris, you should strive to take the minimal effective dose. By taking the minimal amount of Saphris necessary for symptomatic relief, you minimize the drug’s influence over your body and likelihood of side effects, including weight gain.

5. Time Span

It appears as though the longer you’ve been taking Saphris, the more weight you’ll end up gaining. In part this may be due to establishing a tolerance to a particular dosage after an extended term. Despite the fact that weight gain wasn’t significant for most over the course of a full year’s treatment, many people have taken Saphris for much longer than a year.

Those that have been taking Saphris for several years may end up gaining weight as a result of long-term neurophysiological changes made by the drug. In addition, the longer term of administration may have resulted in dosage increases, which make weight gain more likely. Short-term users of Saphris are less likely to gain significant weight compared to those taking it over a longer term.

How much weight will you gain on Saphris?

It is difficult to determine how much weight you’ll gain while taking Saphris. Much of the weight gain you experience will be based on the aforementioned factors such as: medication interactions, lifestyle choices, genetics, duration over which you’ve taken the drug, and your dosage. Someone who has been taking a high dose of Saphris and has certain genetic polymorphisms that predispose them to weight gain may pack on more significant weight than other individuals.

Short-term: Those that take Saphris over a term of less than 12 weeks tend to gain just under 2 lbs. within the first 3 weeks of treatment. The literature suggests that you are unlikely to gain any significant weight if you use Saphris on a short-term basis.

Long-term: The FDA packaging insert for Saphris suggests that substantial weight gain is unlikely over long-term. This is likely due to the fact that it is less likely to alter metabolic processes than other antipsychotics. After a year’s worth of treatment, weight gain was reported as being under 3 lbs. on average. It is unknown as to whether more substantial weight gain is experienced after several years of treatment.

  • Source: http://www.ncbi.nlm.nih.gov/pubmed/21318056

Does everyone gain weight on Saphris?

Certainly not everyone will report significant weight gain on Saphris. The exact percentage of people who experience clinically significant weight gain from Saphris isn’t well established. However, most large-scale trials and reviews suggest that between 5% and 7% of all users will end up gaining significant weight.

The manufacturers of Saphris suggest that clinically relevant weight gain occurs in an estimated 6 out of 100 users. Clinically relevant weight gain is defined as an increase of at least 7% baseline bodyweight following administration of Saphris. In other words, if you weighed 200 lbs, you’d end up gaining a minimum of 14 lbs.

Despite the fact that most studies suggest weight gain occurring in an estimated 6% of users, other studies suggest more substantial figures. For example, one study discovered that 19% of patients treated with Saphris experienced weight gain; this is over double the percentage reported in other studies. Some have theorized that weight gain on Saphris may be related to a low baseline BMI and bodyweight before taking it, whereas those with higher BMIs may be less susceptible to weight increases.

Does Saphris’ therapeutic benefit outweigh the weight gain?

If you are taking Saphris, it is important to conduct a cost-benefit analysis to determine whether the therapeutic efficacy trumps the weight gain (and other side effects). It is important to work with your doctor to assess degree of symptomatic improvement that you’ve derived from Saphris and compare the improvement to the unwanted side effects. If Saphris is working brilliantly and has your symptoms of schizophrenia (or bipolar disorder) under control, you may not care about weight gain.

However, if you’ve packed on some serious poundage as a result of the medication, and it’s not working very well to manage your symptoms, it may be time to consider other options. Understand that excess weight gain can contribute to a cascade of other general health problems such as diabetes and cardiovascular problems. If you’ve gained a moderate amount of weight, and the drug is working fairly well, it may be tougher to determine whether continued treatment is warranted.

If you’re having a tough time determining whether to continue treatment and/or switch medications – talk to a medical professional. They will help you track your weight, various physiological biomarker changes, and assess how well the drug is working. Most research suggests that people are less likely to have a problem with weight gain compared to its degree of efficacy; many people have poor responses.

Have you gained weight from Saphris?

If you’ve taken Saphris, feel free to mention any weight changes you’ve experienced in the comments section below. Report how much weight you gained, the dosage of Saphris you were (or are currently) taking, and the duration over which you’ve been taking it. Can you be sure that the weight gain you experienced was from Saphris – or have you started other medications along with it?

Understand that it’s difficult for many people to accurately determine whether they gained weight from a medication and/or as a result of other lifestyle changes. By maintaining the same: level of physical activity, sleep, stress, and diet – it is easier to chalk weight fluctuations up to Saphris. For most people, Saphris will not be associated with nearly as significant weight gain as other atypical antipsychotics.

Weight loss on antipsychotics is possible: study

NEW YORK (Reuters Health) – The drugs people take to help ease serious mental illnesses often contribute to weight and blood sugar problems – but researchers say a lifestyle intervention can be helpful on both fronts.

The so-called “antipsychotic drugs” that patients take to control their symptoms tend to stimulate hunger and thirst and cause metabolic changes.

But in a new test of a year-long intervention, people taking these drugs for illnesses like schizophrenia or bipolar disorder were able to lose weight and improve their blood sugar levels.

“The results are somewhat surprising because people with serious mental illnesses have many barriers to losing weight,” said lead author Carla A. Green, of the Center for Health Research at Kaiser Permanente Northwest in Portland, Oregon. “That is really important because people with serious mental illness are already at much higher risk for obesity and obesity-related disease and they have a reduced life expectancy because of this.”

A number of medication side-effects, including weight gain, deter some people from taking their prescribed antipsychotics, Green said.

“Our study showed that if given the right tools, they can lose similar amounts of weight as people without severe mental illnesses,” she told Reuters Health by email.

Clozapine (FazaClo), olanzapine (Zyprexa), quetiapine (Seroquel) and risperidone (Risperdal), which treat schizophrenia, bipolar disorder or other mental illnesses, have all been linked to increased risk of weight gain.

Green and her team studied 200 adults who’d been taking antipsychotic medications for at least a month and who had a body mass index (BMI) of at least 27. BMI is a measure of weight relative to height; the cutoff for “overweight” is 25. (You can calculate your own BMI here: 1.usa.gov/XcVMat.)

They explain in the American Journal of Psychiatry that patients were randomly assigned to an “intervention” group that participated in the new program, or a comparison group that just got their usual medical care

In the intervention group, participants attended weekly two-hour group meetings for the first six months of the study. At each session, they met with mental health counselors and nutritionists; each meeting also included 20 minutes of physical activity.

In addition, participants recorded what and how much they ate, how much they slept and how much they exercised, with a goal of at least 25 minutes of moderate activity per day.

The intervention was focused on improved diet with more vegetables, fruits, and low-fat dairy, moderate caloric restriction, increased exercise primarily from walking, stress management, and improved sleep, Green said.

For the second half of the year, the participants met to discuss strategies for maintaining weight loss.

The comparison group did not participate in the weight loss or maintenance interventions.

People in the intervention group lost an average of about 10 pounds over the duration of the study. Those in the comparison group also lost some weight, but much smaller amounts, the authors write.

In the intervention group, 40 percent of participants lost at least five percent of their initial body weight, and 18 percent lost at least 10 percent of their initial weight.

Over the course of the year, fasting blood sugar levels went down in the intervention group, but they went up in the comparison group.

Use of antipsychotic drugs in the U.S. has been on the rise since the 1990’s, especially among kids (see Reuters story of August 7, 2012 here: reut.rs/1ph77xl).

The intervention resulted in a relatively modest weight loss, and did not depend on the type of medication, said Dr. Daniel J. Mueller, who has done research on ways to improve psychiatric drug treatment at the Center for Addiction and Mental Health in Toronto.

Individual motivation is key when addressing weight loss, Mueller told Reuters Health by email. Although patients with serious mental illness face more difficulties, some will be motivated enough to overcome them, he said.

“Some doctors will now routinely start treatment with relatively weight neutral antipsychotics first, like aripiprazole (Abilify) or ‎ziprasidone (Geodon), if they work,” he said.

But the drugs that work the best on average also have high weight gain risk, like clozapine and olanzapine, or at least moderate risk, like risperidone, Mueller said.

“In our qualitative interviews, we found that group support was one of the most important components of our intervention,” Green said. “Many of our participants said they benefited from the camaraderie of others who faced the same challenges, and this may be particularly important among people with serious mental health problems because they tend to be more socially isolated.”

People taking antipsychotics can talk to their doctors about weight gain and medication alternatives, weight management programs and support groups while increasing physical activity, decreasing calories and portion size, she said.

“Perhaps more importantly, lifestyle change programs of this type are not routinely offered in community mental health centers because the programs focus on physical health concerns and this makes reimbursement for those services difficult if not impossible in mental health settings,” Green said.

That makes it hard to provide lifestyle change programs in the places where people with serious mental illnesses are most likely to be able to take advantage of them, she said.

SOURCE: bit.ly/1oRD8fW American Journal of Psychiatry, online September 15, 2014

Our Standards:The Thomson Reuters Trust Principles.

Saphris (Asenapine) Patient Information

Generic Name: Asenapine
Brand Name: Saphris

Pronounced: a SEN a peen

Find out why Saphris is prescribed, Saphris side effects, Saphris warnings and drug interactions, more – in plain English.

Saphris (asenapine) full prescribing information

What is Saphris (asenapine)?

Asenapine (Saphris) is an antipsychotic medication. It works by changing the actions of chemicals in the brain.
Asenapine is used to treat the symptoms of psychotic conditions such as schizophrenia and bipolar disorder (manic depression) in adults.
Asenapine may also be used for other purposes not listed in this medication guide.

What is the most important information I should know about Saphris (asenapine)?

Asenapine is not for use in psychotic conditions related to dementia. Asenapine may cause heart failure, sudden death, or pneumonia in older adults with dementia-related conditions. While you are taking asenapine, you may be more sensitive to temperature extremes such as very hot or cold conditions. Avoid getting too cold, or becoming overheated or dehydrated. Drink plenty of fluids, especially in hot weather and during exercise. It is easier to become dangerously overheated and dehydrated while you are taking asenapine. Asenapine can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert.
Before taking asenapine, tell your doctor if you have liver disease, heart disease, high blood pressure, seizures, low white blood cell counts, diabetes, trouble swallowing, or a history of heart breast cancer, heart attack, stroke, or “Long QT syndrome.”
Avoid drinking alcohol, which can increase some of the side effects of asenapine. Stop taking asenapine and call your doctor at once if you have fever, stiff muscles, confusion, sweating, fast or uneven heartbeats, restless muscle movements in your face or neck, tremor (uncontrolled shaking), trouble swallowing, feeling light-headed, or fainting.

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What should I discuss with my healthcare provider before taking Saphris (asenapine)?

Asenapine is not for use in psychotic conditions related to dementia. Asenapine may cause heart failure, sudden death, or pneumonia in older adults with dementia-related conditions.
If you have any of these other conditions, you may need a dose adjustment or special tests to safely use this medication:

  • liver disease;
  • heart disease, high blood pressure, heart rhythm problems;
  • a history of heart attack or stroke;
  • a history of breast cancer;
  • seizures or epilepsy;
  • diabetes (asenapine may raise your blood sugar);
  • trouble swallowing;
  • Parkinson’s disease;
  • a history of low white blood cell (WBC) counts; or
  • a personal or family history of”Long QT syndrome.”

FDA pregnancy category C. It is not known whether asenapine is harmful to an unborn baby. Before taking this medication, tell your doctor if you are pregnant or plan to become pregnant during treatment. Asenapine can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby. Do not give this medication to anyone younger than 18 years old without the advice of a doctor.

How should I take Saphris (asenapine)?

Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.
Take this medicine with a full glass of water.
Asenapine is usually taken 2 times per day. Follow your doctor’s instructions.
To take asenapine sublingual (under the tongue) tablets:

  • Keep the tablet in its blister pack until you are ready to take the medicine. Open the package and peel back the colored tab from the tablet blister. Do not push a tablet through the blister or you may damage the tablet.
  • Using dry hands, gently remove the tablet and place it under your tongue. It will begin to dissolve right away.
  • Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing.

Swallow several times as the tablet dissolves. Do not eat or drink anything for 10 minutes after the tablet has dissolved.
Asenapine may cause you to have high blood sugar (hyperglycemia). Symptoms include increased thirst, loss of appetite, increased urination, nausea, vomiting, drowsiness, dry skin, and dry mouth. If you are diabetic, check your blood sugar levels on a regular basis while you are taking asenapine.
To be sure this medication is helping your condition, your doctor will need to check your progress on a regular basis. Do not miss any scheduled appointments.
Store asenapine at room temperature away from moisture and heat.

Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and take the medicine at the next regularly scheduled time. Do not take extra medicine to make up the missed dose.

Seek emergency medical attention if you think you have used too much of this medicine. Overdose symptoms may include agitation, confusion, and restless muscle movements in your eyes, tongue, jaw, or neck.

What should I avoid while taking Saphris (asenapine)?

While you are taking asenapine, you may be more sensitive to temperature extremes such as very hot or cold conditions. Avoid getting too cold, or becoming overheated or dehydrated. Drink plenty of fluids, especially in hot weather and during exercise. It is easier to become dangerously overheated and dehydrated while you are taking asenapine. Asenapine can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert.
Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.
Avoid drinking alcohol, which can increase some of the side effects of asenapine.

Asenapine (Saphris) side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using asenapine and call your doctor at once if you have any of these serious side effects:

  • very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, feeling like you might pass out;
  • twitching or uncontrollable movements of your eyes, lips, tongue, face, arms, or legs;
  • tremor (uncontrolled shaking);
  • trouble swallowing;
  • sudden numbness or weakness, especially on one side of the body;
  • sudden and severe headache, or problems with vision, speech, or balance;
  • easy bruising or bleeding, fever, chills, body aches, flu symptoms;
  • white patches or sores inside your mouth or on your lips;
  • seizure (convulsions); or
  • unusual thoughts or behavior, hallucinations, or thoughts about hurting yourself.

Less serious side effects may include:

  • dizziness, drowsiness;
  • restless feeling;
  • numbness or tingling inside or around your mouth;
  • constipation;
  • dry mouth;
  • sleep problems (insomnia);
  • upset stomach; or
  • weight gain.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Saphris (asenapine)?

Before using asenapine, tell your doctor if you regularly use other medicines that make you sleepy (such as cold or allergy medicine, narcotic pain medicine, sleeping pills, muscle relaxers, and medicine for seizures, depression, or anxiety). They can add to sleepiness caused by asenapine.
The following drugs can interact with asenapine. Tell your doctor if you are using

This list is not complete and there may be other drugs that can interact with asenapine. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

Where can I get more information?

  • Your pharmacist can provide more information about asenapine.
  • Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

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Last revision: 09/2009

Saphris (asenapine) full prescribing information

back to: Psychiatric Medication Patient Information Index

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