Side effects of clarinex

Clarinex Side Effects

Generic Name: desloratadine

Medically reviewed by Drugs.com. Last updated on Dec 29, 2018.

  • Overview
  • Side Effects
  • Dosage
  • Professional
  • Interactions
  • More

Note: This document contains side effect information about desloratadine. Some of the dosage forms listed on this page may not apply to the brand name Clarinex.

In Summary

More frequent side effects include: fatigue, pharyngitis, and nausea. See below for a comprehensive list of adverse effects.

For the Consumer

Applies to desloratadine: oral syrup, oral tablet, oral tablet disintegrating

Along with its needed effects, desloratadine (the active ingredient contained in Clarinex) may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking desloratadine:

Rare

  • Anaphylaxis, such as, cough, difficulty swallowing, dizziness, fast heartbeat, hives, itching, puffiness or swelling of eyelids or around the eyes or face or lips or tongue, shortness of breath, skin rash, tightness in chest, unusual tiredness or weakness, wheezing
  • dyspnea, such as, shortness of breath, difficult or labored breathing, tightness in chest, wheezing
  • edema, such as, swelling
  • pruritus, such as, itching skin
  • rash
  • tachycardia, such as, fast, pounding, or irregular heartbeat or pulse
  • urticaria, such as, hives or welts, itching, redness of skin, skin rash.

Some side effects of desloratadine may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Headache

Less common

  • Dizziness
  • dry mouth
  • dysmenorrhea, such as, difficult or painful menstruation
  • dyspepsia, such as, acid or sour stomach, belching, heartburn, indigestion, stomach discomfort , upset or pain,
  • fatigue, such as, unusual tiredness or weakness
  • myalgia, such as, joint pain, swollen joints, muscle aching or cramping, muscle pains or stiffness, difficulty in moving
  • pharyngitis, such as, body aches or pain, congestion, cough, dryness or soreness of throat, fever, hoarseness, runny nose, tender swollen glands in neck, trouble in swallowing, voice changes.
  • somnolence, such as, sleepiness or unusual drowsiness
  • nausea

For Healthcare Professionals

Applies to desloratadine: oral solution, oral tablet, oral tablet disintegrating

General

The most commonly reported side effects included upper respiratory tract infections, diarrhea, fever, and headache.

Respiratory

Upper respiratory tract infections were reported in 21.2% of patients 6 to 11 months of age given oral solution formulations, and coughing was reported in 10.8% of patients 12 to 23 months of age given oral solution formulations.

Very common (10% or more): Upper respiratory tract infections (up to 21.2%), coughing (up to 10.8%)

Common (1% to 10%): Bronchitis, epistaxis, rhinorrhea

Very rare (less than 0.01%): Dyspnea

Gastrointestinal

Very common (10% or more): Diarrhea (up to 19.7%)

Common (1% to 10%): Dry mouth, dyspepsia, nausea, pharyngitis, vomiting

Very rare (less than 0.01%): Abdominal pain

In patients treated for chronic idiopathic urticaria, nausea was reported in up to 5%, pharyngitis was reported in 3%, and dyspepsia was reported in 3% of patients 12 years and older.

Diarrhea was reported in 19.1% of patients 6 to 11 months of age given oral solution formulations.

Other

Fever was reported in 16.9% of patients 12 to 23 months of age given oral solution formulations.

In patients treated for chronic idiopathic urticaria, fatigue was reported in up to 5% of patients 12 years and older.

Very common (10% or more): Fever (up to 16.9%)

Common (1% to 10%): Fatigue

Frequency not reported: Asthenia

Nervous system

Very common (10% or more): Headache (up to 14%)

Common (1% to 10%): Dizziness, somnolence

Very rare (less than 0.01%): Psychomotor hyperactivity, seizures

Postmarketing reports: Dystonia, extrapyramidal symptoms, movement disorder

In patients treated for chronic idiopathic urticaria, headache was reported in up to 14% and dizziness was reported in 4% of patients 12 years and older.

Seizures have been reported in patients with and without seizure disorders.

Movement disorders included dystonia, extrapyramidal symptoms, and tics.

Psychiatric

Very common (10% or more): Irritability (up to 12.1%)

Common (1% to 10%): Emotional lability, insomnia

Very rare (less than 0.01%): Hallucinations

Frequency not reported: Abnormal behavior, aggression

Postmarketing reports: Tics

Irritability was reported in 12.1% of patients 6 to 11 months of age given oral solution formulations.

Insomnia was reported in 2.3% of patients 6 to 23 months of age given oral syrup formulations.

Dermatologic

Common (1% to 10%): Erythema, rash maculopapular

Very rare (less than 0.01%): Pruritus, rash, urticaria

Frequency not reported: Photosensitivity

Metabolic

Common (1% to 10%): Anorexia, appetite increased

Frequency not reported: Weight increased

Immunologic

Common (1% to 10%): Parasitic infection, varicella

Genitourinary

Common (1% to 10%): Dysmenorrhea, urinary tract infection

Musculoskeletal

In patients treated for chronic idiopathic urticaria, myalgia was reported in up to 3%of patients 12 years and older.

Common (1% to 10%): Myalgia

Ocular

Common (1% to 10%): Otitis media

Hepatic

Very rare (less than 0.01%): Hepatitis, increased bilirubin, liver enzyme elevations

Frequency not reported: Jaundice

Hypersensitivity

Very rare (less than 0.01%): Anaphylaxis, angioedema, hypersensitivity reactions

Cardiovascular

Very rare (less than 0.01%): Palpitations, tachycardia

Frequency not reported: QT prolongation

Postmarketing reports: Arrhythmia, bradycardia, edema

1. Cerner Multum, Inc. “Australian Product Information.” O 0

2. Cerner Multum, Inc. “UK Summary of Product Characteristics.” O 0

3. “Product Information. Clarinex (desloratadine).” Schering Corporation, Kenilworth, NJ.

Further information

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

Some side effects may not be reported. You may report them to the FDA.

Medical Disclaimer

More about Clarinex (desloratadine)

  • During Pregnancy or Breastfeeding
  • Dosage Information
  • Drug Images
  • Drug Interactions
  • Pricing & Coupons
  • En Español
  • 5 Reviews
  • Generic Availability
  • Drug class: antihistamines

Consumer resources

  • Clarinex
  • Clarinex (Desloratadine Syrup)
  • Clarinex (Desloratadine Tablets)
  • Clarinex (Advanced Reading)

Professional resources

  • Clarinex (AHFS Monograph)
  • … +1 more

Other Formulations

  • Clarinex-D 12 Hour
  • Clarinex Reditabs
  • Clarinex-D 24 Hour

Related treatment guides

  • Allergic Rhinitis
  • Urticaria

Clarinex

SIDE EFFECTS

The following adverse reactions are discussed in greater detail in other sections of the label:

  • Hypersensitivity reactions.

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 clinical practice.

Adults And Adolescents

Allergic Rhinitis

In multiple-dose placebo-controlled trials, 2834 patients ages 12 years or older received CLARINEX Tablets at doses of 2.5 mg to 20 mg daily, of whom 1655 patients received the recommended daily dose of 5 mg. In patients receiving 5 mg daily, the rate of adverse events was similar between CLARINEX and placebo-treated patients. The percent of patients who withdrew prematurely due to adverse events was 2.4% in the CLARINEX group and 2.6% in the placebo group. There were no serious adverse events in these trials in patients receiving desloratadine. All adverse events that were reported by greater than or equal to 2% of patients who received the recommended daily dose of CLARINEX Tablets (5 mg once daily), and that were more common with CLARINEX Tablets than placebo, are listed in Table 1.

Table 1: Incidence of Adverse Events Reported by ≥2% of Adult and Adolescent Allergic Rhinitis Patients Receiving CLARINEX Tablets

Adverse Event CLARINEX Tablets 5 mg
(n=1655)
Placebo
(n=1652)
Infections and Infestations
Pharyngitis 4.1% 2.0%
Nervous System Disorders
Somnolence 2.1% 1.8%
Gastrointestinal Disorders
Dry Mouth 3.0% 1.9%
Musculoskeletal and Connective Tissue Disorders
Myalgia 2.1% 1.8%
Reproductive System and Breast Disorders
Dysmenorrhea 2.1% 1.6%
General Disorders and Administration Site Conditions
Fatigue 2.1% 1.2%

The frequency and magnitude of laboratory and electrocardiographic abnormalities were similar in CLARINEX and placebo-treated patients.

There were no differences in adverse events for subgroups of patients as defined by gender, age, or race.

Pediatrics

Two hundred and forty-six pediatric subjects 6 months to 11 years of age received CLARINEX Oral Solution for 15 days in three placebo-controlled clinical trials. Pediatric subjects aged 6 to 11 years received 2.5 mg once a day, subjects aged 1 to 5 years received 1.25 mg once a day, and subjects 6 to 11 months of age received 1.0 mg once a day.

In subjects 6 to 11 years of age, no individual adverse event was reported by 2 percent or more of the subjects.

There were no clinically meaningful changes in any electrocardiographic parameter, including the QTc interval. Only one of the 246 pediatric subjects receiving CLARINEX Oral Solution in the clinical trials discontinued treatment because of an adverse event.

Post-Marketing Experience

Because adverse events 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. The following spontaneous adverse events have been reported during the marketing of desloratadine:

Cardiac disorders: tachycardia, palpitations

Respiratory, thoracic and mediastinal disorders: dyspnea

Skin and subcutaneous tissue disorders: rash, pruritus

Nervous system disorders: psychomotor hyperactivity, movement disorders (including dystonia, tics, and extrapyramidal symptoms), seizures (reported in patients with and without a known seizure disorder)

Immune system disorders: hypersensitivity reactions (such as urticaria, edema and anaphylaxis)

Investigations: elevated liver enzymes including bilirubin

Hepatobiliary disorders: hepatitis

Metabolism and nutrition disorders: increased appetite

Read the entire FDA prescribing information for Clarinex (Desloratadine)

Desloratadine syrup

What is this medicine?

DESLORATADINE (des lor AT a deen) is an antihistamine. It helps to relieve sneezing, runny nose, and itchy, watery eyes. This medicine is used to treat or prevent symptoms of allergies. It is also used to treat itchy skin rash and hives.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

COMMON BRAND NAME(S): Clarinex

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:

  • asthma

  • kidney disease

  • liver disease

  • an unusual or allergic reaction to desloratadine, loratadine, other antihistamines, medicines, foods, dyes, or preservatives

  • pregnant or trying to get pregnant

  • breast-feeding

How should I use this medicine?

Take this medicine by mouth. Follow the directions on your prescription label. Shake well before using. Use the specially marked spoon or dropper supplied with this medicine to measure every dose. Household spoons are not accurate. Ask your pharmacist if you do not have one. You may give this medicine with food or on an empty stomach. Take your medicine at regular intervals. Do not take it more often than directed.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed. This medicine has been used in children as young as 6 months.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.

NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.

What may interact with this medicine?

  • other medicines for colds or allergies

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for checks on your progress. Tell your doctor if your symptoms do not improve.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:

  • allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue

  • breathing problems

  • fast heartbeat or chest pain

  • fever or infection

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):

  • dry or irritated mouth or throat

  • headache

  • irritable

  • menstrual changes

  • muscle aches

  • stomach upset, nausea

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 59 and 86 degrees F (15 and 30 degrees C). Protect from light. Throw away any unused medicine after the expiration date.

NOTE: This sheet is a summary. It may not cover all possible information. If you have questions about this medicine, talk to your doctor, pharmacist, or health care provider.

Share Facebook Twitter LinkedIn Email Get useful, helpful and relevant health + wellness information enews

Cleveland Clinic is a non-profit academic medical center. Advertising on our site helps support our mission. We do not endorse non-Cleveland Clinic products or services. Policy

CLINICAL PHARMACOLOGY

Mechanism Of Action

Desloratadine is a long-acting tricyclic histamine antagonist with selective H1-receptor histamine antagonist activity. Receptor binding data indicates that at a concentration of 2-3 ng/mL (7 nanomolar), desloratadine shows significant interaction with the human histamine H1-receptor. Desloratadine inhibited histamine release from human mast cells in vitro. Results of a radiolabeled tissue distribution study in rats and a radioligand H1-receptor binding study in guinea pigs showed that desloratadine did not readily cross the blood brain barrier. The clinical significance of this finding is unknown.

Pharmacodynamics

Wheal And Flare

Human histamine skin wheal studies following single and repeated 5-mg doses of desloratadine have shown that the drug exhibits an antihistaminic effect by 1 hour; this activity may persist for as long as 24 hours. There was no evidence of histamine-induced skin wheal tachyphylaxis within the desloratadine 5-mg group over the 28-day treatment period. The clinical relevance of histamine wheal skin testing is unknown.

Effects On QTc

Single daily doses of 45 mg were given to normal male and female volunteers for 10 days. All ECGs obtained in this study were manually read in a blinded fashion by a cardiologist. In CLARINEX-treated subjects, there was an increase in mean heart rate of 9.2 bpm relative to placebo. The QT interval was corrected for heart rate (QTc) by both the Bazett and Fridericia methods. Using the QTc (Bazett) there was a mean increase of 8.1 msec in CLARINEX-treated subjects relative to placebo. Using QTc (Fridericia) there was a mean increase of 0.4 msec in CLARINEX-treated subjects relative to placebo. No clinically relevant adverse events were reported.

Pharmacokinetics

Absorption

Following oral administration of a desloratadine 5-mg tablet once daily for 10 days to normal healthy volunteers, the mean time to maximum plasma concentrations (Tmax) occurred at approximately 3 hours post dose and mean steady state peak plasma concentrations (Cmax) and AUC of 4 ng/mL and 56.9 ng.hr/mL were observed, respectively. Neither food nor grapefruit juice had an effect on the bioavailability (Cmax and AUC) of desloratadine.

The pharmacokinetic profile of CLARINEX Oral Solution was evaluated in a three-way crossover study in 30 adult volunteers. A single dose of 10 mL of CLARINEX Oral Solution containing 5 mg of desloratadine was bioequivalent to a single dose of 5-mg CLARINEX Tablet. Food had no effect on the bioavailability (AUC and Cmax) of CLARINEX Oral Solution.

The pharmacokinetic profile of CLARINEX RediTabs Tablets was evaluated in a three-way crossover study in 24 adult volunteers. A single CLARINEX RediTabs Tablet containing 5 mg of desloratadine was bioequivalent to a single 5-mg CLARINEX RediTabs Tablet (original formulation) for both desloratadine and 3-hydroxydesloratadine. Food and water had no effect on the bioavailability (AUC and Cmax) of CLARINEX RediTabs Tablets.

Distribution

Desloratadine and 3-hydroxydesloratadine are approximately 82% to 87% and 85% to 89% bound to plasma proteins, respectively. Protein binding of desloratadine and 3-hydroxydesloratadine was unaltered in subjects with impaired renal function.

Metabolism

Desloratadine (a major metabolite of loratadine) is extensively metabolized to 3-hydroxydesloratadine, an active metabolite, which is subsequently glucuronidated. The enzyme(s) responsible for the formation of 3-hydroxydesloratadine have not been identified. Data from clinical trials indicate that a subset of the general population has a decreased ability to form 3hydroxydesloratadine, and are poor metabolizers of desloratadine. In pharmacokinetic studies (n=3748), approximately 6% of subjects were poor metabolizers of desloratadine (defined as a subject with an AUC ratio of 3-hydroxydesloratadine to desloratadine less than 0.1, or a subject with a desloratadine half-life exceeding 50 hours). These pharmacokinetic studies included subjects between the ages of 2 and 70 years, including 977 subjects aged 2 to 5 years, 1575 subjects aged 6 to 11 years, and 1196 subjects aged 12 to 70 years. There was no difference in the prevalence of poor metabolizers across age groups. The frequency of poor metabolizers was higher in Blacks (17%, n=988) as compared to Caucasians (2%, n=1,462) and Hispanics (2%, n=1,063). The median exposure (AUC) to desloratadine in the poor metabolizers was approximately 6-fold greater than in the subjects who are not poor metabolizers. Subjects who are poor metabolizers of desloratadine cannot be prospectively identified and will be exposed to higher levels of desloratadine following dosing with the recommended dose of desloratadine. In multidose clinical safety studies, where metabolizer status was identified, a total of 94 poor metabolizers and 123 normal metabolizers were enrolled and treated with CLARINEX Oral Solution for 15-35 days. In these studies, no overall differences in safety were observed between poor metabolizers and normal metabolizers. Although not seen in these studies, an increased risk of exposure-related adverse events in patients who are poor metabolizers cannot be ruled out.

Elimination

The mean plasma elimination half-life of desloratadine was approximately 27 hours. Cmax and AUC values increased in a dose proportional manner following single oral doses between 5 and 20 mg. The degree of accumulation after 14 days of dosing was consistent with the half-life and dosing frequency. A human mass balance study documented a recovery of approximately 87% of the 14C-desloratadine dose, which was equally distributed in urine and feces as metabolic products. Analysis of plasma 3hydroxydesloratadine showed similar Tmax and half-life values compared to desloratadine.

Special Populations

Geriatric Subjects

In older subjects (≥65 years old; n=17) following multiple-dose administration of CLARINEX Tablets, the mean Cmax and AUC values for desloratadine were 20% greater than in younger subjects (<65 years old). The oral total body clearance (CL/F) when normalized for body weight was similar between the two age groups. The mean plasma elimination half-life of desloratadine was 33.7 hr in subjects ≥65 years old. The pharmacokinetics for 3-hydroxydesloratadine appeared unchanged in older versus younger subjects. These age-related differences are unlikely to be clinically relevant and no dosage adjustment is recommended in elderly subjects.

Pediatric Subjects

In subjects 6 to 11 years old, a single dose of 5 mL of CLARINEX Oral Solution containing 2.5 mg of desloratadine, resulted in desloratadine plasma concentrations similar to those achieved in adults administered a single 5-mg CLARINEX Tablet. In subjects 2 to 5 years old, a single dose of 2.5 mL of CLARINEX Oral Solution containing 1.25 mg of desloratadine, resulted in desloratadine plasma concentrations similar to those achieved in adults administered a single 5-mg CLARINEX Tablet. However, the Cmax and AUC of the metabolite (3-hydroxydesloratadine) were 1.27 and 1.61 times higher for the 5-mg dose of Oral Solution administered in adults compared to the Cmax and AUC obtained in children 2 to 11 years of age receiving 1.25-2.5 mg of CLARINEX Oral Solution.

A single dose of either 2.5 mL or 1.25 mL of CLARINEX Oral Solution containing 1.25 mg or 0.625 mg, respectively, of desloratadine was administered to subjects 6 to 11 months of age and 12 to 23 months of age. The results of a population pharmacokinetic analysis indicated that a dose of 1 mg for subjects aged 6 to 11 months and 1.25 mg for subjects 12 to 23 months of age is required to obtain desloratadine plasma concentrations similar to those achieved in adults administered a single 5-mg dose of CLARINEX Oral Solution.

The CLARINEX RediTabs 2.5-mg tablet has not been evaluated in pediatric patients. Bioequivalence of the CLARINEX RediTabs Tablet and the original CLARINEX RediTabs Tablets was established in adults. In conjunction with the dose-finding studies in pediatrics described, the pharmacokinetic data for CLARINEX RediTabs Tablets supports the use of the 2.5-mg dose strength in pediatric patients 6 to 11 years of age.

Renally Impaired

Desloratadine pharmacokinetics following a single dose of 7.5 mg were characterized in patients with mild (n=7; creatinine clearance 51-69 mL/min/1.73 m²), moderate (n=6; creatinine clearance 34-43 mL/min/1.73 m²), and severe (n=6; creatinine clearance 5-29 mL/min/1.73 m²) renal impairment or hemodialysis dependent (n=6) patients. In patients with mild and moderate renal impairment, median Cmax and AUC values increased by approximately 1.2-and 1.9-fold, respectively, relative to subjects with normal renal function. In patients with severe renal impairment or who were hemodialysis dependent, Cmax and AUC values increased by approximately 1.7-and 2.5-fold, respectively. Minimal changes in 3-hydroxydesloratadine concentrations were observed. Desloratadine and 3-hydroxydesloratadine were poorly removed by hemodialysis. Plasma protein binding of desloratadine and 3-hydroxydesloratadine was unaltered by renal impairment. Dosage adjustment for patients with renal impairment is recommended .

Hepatically Impaired

Desloratadine pharmacokinetics were characterized following a single oral dose in patients with mild (n=4), moderate (n=4), and severe (n=4) hepatic impairment as defined by the Child-Pugh classification of hepatic function and 8 subjects with normal hepatic function. Patients with hepatic impairment, regardless of severity, had approximately a 2.4-fold increase in AUC as compared with normal subjects. The apparent oral clearance of desloratadine in patients with mild, moderate, and severe hepatic impairment was 37%, 36%, and 28% of that in normal subjects, respectively. An increase in the mean elimination half-life of desloratadine in patients with hepatic impairment was observed. For 3-hydroxydesloratadine, the mean Cmax and AUC values for patients with hepatic impairment were not statistically significantly different from subjects with normal hepatic function. Dosage adjustment for patients with hepatic impairment is recommended .

Gender

Female subjects treated for 14 days with CLARINEX Tablets had 10% and 3% higher desloratadine Cmax and AUC values, respectively, compared with male subjects. The 3-hydroxydesloratadine Cmax and AUC values were also increased by 45% and 48%, respectively, in females compared with males. However, these apparent differences are not likely to be clinically relevant and therefore no dosage adjustment is recommended.

Race

Following 14 days of treatment with CLARINEX Tablets, the Cmax and AUC values for desloratadine were 18% and 32% higher, respectively, in Blacks compared with Caucasians. For 3-hydroxydesloratadine there was a corresponding 10% reduction in Cmax and AUC values in Blacks compared to Caucasians. These differences are not likely to be clinically relevant and therefore no dose adjustment is recommended.

Drug Interactions

In two controlled crossover clinical pharmacology studies in healthy male (n=12 in each study) and female (n=12 in each study) volunteers, desloratadine 7.5 mg (1.5 times the daily dose) once daily was coadministered with erythromycin 500 mg every 8 hours or ketoconazole 200 mg every 12 hours for 10 days. In three separate controlled, parallel group clinical pharmacology studies, desloratadine at the clinical dose of 5 mg has been coadministered with azithromycin 500 mg followed by 250 mg once daily for 4 days (n=18) or with fluoxetine 20 mg once daily for 7 days after a 23-day pretreatment period with fluoxetine (n=18) or with cimetidine 600 mg every 12 hours for 14 days (n=18) under steady-state conditions to normal healthy male and female volunteers. Although increased plasma concentrations (Cmax and AUC0-24 hrs) of desloratadine and 3hydroxydesloratadine were observed (see Table 2), there were no clinically relevant changes in the safety profile of desloratadine, as assessed by electrocardiographic parameters (including the corrected QT interval), clinical laboratory tests, vital signs, and adverse events.

Table 2: Changes in Desloratadine and 3-Hydroxydesloratadine Pharmacokinetics in Healthy Male and Female Volunteers

Animal Toxicology And/Or Pharmacology Reproductive Toxicology Studies

Desloratadine was not teratogenic in rats at doses up to 48 mg/kg/day (estimated desloratadine and desloratadine metabolite exposures were approximately 210 times the AUC in humans at the recommended daily oral dose) or in rabbits at doses up to 60 mg/kg/day (estimated desloratadine exposures were approximately 230 times the AUC in humans at the recommended daily oral dose). In a separate study, an increase in pre-implantation loss and a decreased number of implantations and fetuses were noted in female rats at 24 mg/kg (estimated desloratadine and desloratadine metabolite exposures were approximately 120 times the AUC in humans at the recommended daily oral dose). Reduced body weight and slow righting reflex were reported in pups at doses of 9 mg/kg/day or greater (estimated desloratadine and desloratadine metabolite exposures were approximately 50 times or greater than the AUC in humans at the recommended daily oral dose). Desloratadine had no effect on pup development at an oral dose of 3 mg/kg/day (estimated desloratadine and desloratadine metabolite exposures were approximately 7 times the AUC in humans at the recommended daily oral dose).

Clinical Studies

Seasonal Allergic Rhinitis

The clinical efficacy and safety of CLARINEX Tablets were evaluated in over 2300 patients 12 to 75 years of age with seasonal allergic rhinitis. A total of 1838 patients received 2.5 to 20 mg/day of CLARINEX in 4 double-blind, randomized, placebo-controlled clinical trials of 2 to 4 weeks’ duration conducted in the United States. The results of these studies demonstrated the efficacy and safety of CLARINEX 5 mg in the treatment of adult and adolescent patients with seasonal allergic rhinitis. In a dose-ranging trial, CLARINEX 2.5 to 20 mg/day was studied. Doses of 5, 7.5, 10, and 20 mg/day were superior to placebo; and no additional benefit was seen at doses above 5.0 mg. In the same study, an increase in the incidence of somnolence was observed at doses of 10 mg/day and 20 mg/day (5.2% and 7.6%, respectively), compared to placebo (2.3%).

In two 4-week studies of 924 patients (aged 15 to 75 years) with seasonal allergic rhinitis and concomitant asthma, CLARINEX Tablets 5 mg once daily improved rhinitis symptoms, with no decrease in pulmonary function. This supports the safety of administering CLARINEX Tablets to adult patients with seasonal allergic rhinitis with mild to moderate asthma.

CLARINEX Tablets 5 mg once daily significantly reduced the Total Symptom Score (the sum of individual scores of nasal and non-nasal symptoms) in patients with seasonal allergic rhinitis. See Table 3.

Table 3: TOTAL SYMPTOM SCORE (TSS) Changes in a 2-Week Clinical Trial in Patients with Seasonal Allergic Rhinitis

There were no significant differences in the effectiveness of CLARINEX Tablets 5 mg across subgroups of patients defined by gender, age, or race.

Perennial Allergic Rhinitis

The clinical efficacy and safety of CLARINEX Tablets 5 mg were evaluated in over 1300 patients 12 to 80 years of age with perennial allergic rhinitis. A total of 685 patients received 5 mg/day of CLARINEX in two double-blind, randomized, placebo-controlled clinical trials of 4 weeks’ duration conducted in the United States and internationally. In one of these studies CLARINEX Tablets 5 mg once daily was shown to significantly reduce the Total Symptom Score in patients with perennial allergic rhinitis (Table 4).

Table 4: TOTAL SYMPTOM SCORE (TSS) Changes in a 4-Week Clinical Trial in Patients with Perennial Allergic Rhinitis

Chronic Idiopathic Urticaria

The efficacy and safety of CLARINEX Tablets 5 mg once daily was studied in 416 chronic idiopathic urticaria patients 12 to 84 years of age, of whom 211 received CLARINEX. In two double-blind, placebo-controlled, randomized clinical trials of six weeks duration, at the pre-specified one-week primary time point evaluation, CLARINEX Tablets significantly reduced the severity of pruritus when compared to placebo (Table 5). Secondary endpoints were also evaluated, and during the first week of therapy CLARINEX Tablets 5 mg reduced the secondary endpoints, “Number of Hives” and the “Size of the Largest Hive,” when compared to placebo.

Table 5: PRURITUS SYMPTOM SCORE Changes in the First Week of a Clinical Trial in Patients with Chronic Idiopathic Urticaria

The clinical safety of CLARINEX Oral Solution was documented in three, 15-day, double-blind, placebo-controlled safety studies in pediatric subjects with a documented history of allergic rhinitis, chronic idiopathic urticaria, or subjects who were candidates for antihistamine therapy. In the first study, 2.5 mg of CLARINEX Oral Solution was administered to 60 pediatric subjects 6 to 11 years of age. The second study evaluated 1.25 mg of CLARINEX Oral Solution administered to 55 pediatric subjects 2 to 5 years of age. In the third study, 1.25 mg of CLARINEX Oral Solution was administered to 65 pediatric subjects 12 to 23 months of age and 1.0 mg of CLARINEX Oral Solution was administered to 66 pediatric subjects 6 to 11 months of age. The results of these studies demonstrated the safety of CLARINEX Oral Solution in pediatric subjects 6 months to 11 years of age.

About the author

Leave a Reply

Your email address will not be published. Required fields are marked *