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Claritin D
(loratadine and pseudoephedrine) 12 hour and 24 hour Extended Release Tablets
Now available Over-the-Counter
Claritin-D 12 Hour Extended Release Tablets: Claritin-D 12 hour extended release tablets contain 5 mg loratadine in the tablet coating for immediate release and 120 mg pseudoephedrine sulfate equally distributed between the tablet coating for immediate release and the barrier-coated extended release core.
The inactive ingredients are acacia, butylparaben, calcium sulfate, carnauba wax, corn starch, lactose, magnesium stearate, microcrystalline cellulose, neutral soap, oleic acid, povidone, rosin, sugar, talc, titanium dioxide, white wax, and zein.
Claritin-D 24 Hour Extended Release Tablets: Claritin-D 24 hour extended release tablets contain 10 mg loratadine in the tablet film coating for immediate release and 240 mg pseudoephedrine sulfate in the tablet core which is released slowly allowing for once-daily administration.
The inactive ingredients for oval, biconvex Claritin-D 24 hour extended release tablets are calcium phosphate, carnauba wax, ethylcellulose, hydroxypropyl methylcellulose, magnesium stearate, polyethylene glycol, povidone, silicon dioxide, sugar, titanium dioxide, and white wax.
Loratadine is a long-acting antihistamine having the empirical formula C22H23ClN2O2; the chemical name ethyl 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylate.
The molecular weight of loratadine is 382.89. It is a white to off-white powder, not soluble in water, but very soluble in acetone, alcohol, and chloroform.
Pseudoephedrine sulfate is the synthetic salt of one of the naturally occurring dextrorotatory diastereomers of ephedrine and is classified as an indirect sympathomimetic amine. The empirical formula for pseudoephedrine sulfate is (C10H15NO)2H2SO4; the chemical name is a-[1-(methyl-amino) ethyl]-[S-(R*,R*)]-benzenemethanol sulfate (2:1)(salt).
The molecular weight of pseudoephedrine sulfate is 428.54. It is a white powder, freely soluble in water and methanol and sparingly soluble in chloroform.
Loratadine; pseudoephedrine sulfate extended release tablets are indicated for the relief of symptoms of seasonal allergic rhinitis. Loratadine; pseudoephedrine sulfate extended release tablets should be administered when both the antihistaminic properties of loratadine and the nasal decongestant activity of pseudoephedrine are desired (see CLINICAL PHARMACOLOGY).
Adults and Children 12 Years of Age and Over: 12 Hour Tablet: One tablet twice a day (every 12 hours); 24 Hour Tablet: One tablet daily taken with a full glass of water (see PRECAUTIONS and ADVERSE REACTIONS). Because the doses of this fixed combination product cannot be individually titrated and hepatic insufficiency results in a reduced clearance of loratadine to a much greater extent than pseudoephedrine, loratadine; pseudoephedrine sulfate extended release tablets should generally be avoided in patients with hepatic insufficiency. Patients with renal insufficiency (GFR
Loratadine; Pseudoephedrine Sulfate 12 Hour Extended Release Tablets
Experience from controlled and uncontrolled clinical studies involving approximately 10,000 patients who received the combination of loratadine; pseudoephedrine sulfate for a period of up to 1 month provides information on adverse reactions. The usual dose was one tablet every 12 hours for up to 28 days.
In controlled clinical trials using the recommended dose of one tablet every 12 hours, the incidence of reported adverse events was similar to those reported with placebo, with the exception of insomnia (16%) and dry mouth (14%).
| TABLE 2 Reported Adverse Events with an Incidence of ³2% in Loratadine; Pseudoephedrine Sulfate 12 Hour Extended Release Tablets in Placebo-Controlled Clinical Trials | ||||
| Percent of Patients Reporting | ||||
| Loratadine; Pseudoephedrine Sulfate 12 Hour | Loratadine | Pseudoephedrine | Placebo | |
|---|---|---|---|---|
| n=1023 | n=543 | n=548 | n=922 | |
| Headache | 19 | 18 | 17 | 19 |
| Insomnia | 16 | 4 | 19 | 3 |
| Dry Mouth | 14 | 4 | 9 | 3 |
| Somnolence | 7 | 8 | 5 | 4 |
| Nervousness | 5 | 3 | 7 | 2 |
| Dizziness | 4 | 1 | 5 | 2 |
| Fatigue | 4 | 6 | 3 | 3 |
| Dyspepsia | 3 | 2 | 3 | 1 |
| Nausea | 3 | 2 | 3 | 2 |
| Pharyngitis | 3 | 3 | 2 | 3 |
| Anorexia | 2 | 1 | 2 | 1 |
| Thirst | 2 | 1 | 2 | 1 |
Adverse event rates did not appear to differ significantly based on age, sex, or race, although the number of non-white subjects was relatively small.
In addition to those adverse events reported above (³2%), the following less frequent adverse events have been reported in at least one patient treated with loratadine; pseudoephedrine sulfate 12 hour extended release tablets.
Autonomic Nervous System: Abnormal lacrimation, dehydration, flushing, hypoesthesia, increased sweating, mydriasis.
Body as a Whole: Asthenia, back pain, blurred vision, chest pain, conjunctivitis, earache, ear infection, eye pain, fever, flu-like symptoms, leg cramps, lymphadenopathy, malaise, photophobia, rigors, tinnitus, viral infection, weight gain.
Cardiovascular System: Hypertension, hypotension, palpitations, peripheral edema, syncope, tachycardia, ventricular extrasystoles.
Central and Peripheral Nervous System: Dysphonia, hyperkinesia, hypertonia, migraine, paresthesia, tremors, vertigo.
Gastrointestinal System: Abdominal distension, abdominal distress, abdominal pain, altered taste, constipation, diarrhea, eructation, flatulence, gastritis, gingival bleeding, hemorrhoids, increased appetite, stomatitis, taste loss, tongue discoloration, toothache, vomiting.
Liver and Biliary System: Hepatic function abnormal.
Musculoskeletal System: Arthralgia, myalgia, torticollis.
Psychiatric: Aggressive reaction, agitation, anxiety, apathy, confusion, decreased libido, depression, emotional lability, euphoria, impaired concentration, irritability, paroniria.
Reproductive System: Dysmenorrhea, impotence, intermenstrual bleeding, vaginitis.
Respiratory System: Bronchitis, bronchospasm, chest congestion, coughing, dry throat, dyspnea, epistaxis, halitosis, nasal congestion, nasal irritation, sinusitis, sneezing, sputum increased, upper respiratory infection, wheezing.
Skin and Appendages: Acne, bacterial skin infection, dry skin, eczema, edema, epidermal necrolysis, erythema, hematoma, pruritus, rash, urticaria.
Urinary System: Dysuria, micturition frequency, nocturia, polyuria, urinary retention.
24 Hour Extended Release Tablets
Information on adverse reactions is provided from placebo-controlled studies involving over 2000 patients, 605 of whom received loratadine; pseudoephedrine sulfate 24 hour extended release tablets once daily for up to 2 weeks. In these studies, the incidence of adverse events reported with loratadine; pseudoephedrine sulfate 24 hour extended release tablets was similar to those reported with twice-daily (q12h) 120 mg sustained-release pseudoephedrine alone.
| TABLE 3 Reported Adverse Events With an Incidence of ³2% in Loratadine; Pseudoephedrine Sulfate 24 Hour Extended Release Tablets Treatment Group in Double-Blind, Randomized, Placebo-Controlled Clinical Trials | |||||||||||||||||
| Percent of Patients Reporting | |||||||||||||||||
| Loratadine; phedrine Sulfate 24 Hour | Loratadine 10 mg | Pseudoephedrine 120 mg q12h | Placebo | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| (n = 605) | (n = 449) | (n = 220) | (n = 605) | ||||||||||||||
| Dry Mouth | 8 | 2 | 7 | 2 | |||||||||||||
| Somnolence | 6 | 4 | 5 | 4 | |||||||||||||
| Insomnia | 5 | 1 | 9 | 1 | |||||||||||||
| Pharyngitis | 5 | 5 | 5 | 5 | |||||||||||||
| Dizziness | 4 | 2 | 3 | 2 | |||||||||||||
| Coughing | 3 | 2 | 3 | 1 | |||||||||||||
| Fatigue | 3 | 4 | 1 | 2 | |||||||||||||
| Nausea | 3 | 2 | 4 | 2 | |||||||||||||
| Nervousness | 3 | 1 | 4 | 1 | |||||||||||||
| Anorexia | 2 |
DRUG INTERACTIONSNo specific interaction studies have been conducted with loratadine; pseudoephedrine extended release tablets. However, loratadine (10 mg once daily) has been safely coadministered with therapeutic doses of erythromycin, cimetidine, and ketoconazole in controlled clinical pharmacology studies. Although increased plasma concentrations (AUC 0-24 hrs) of loratadine and/or descarboethoxyloratadine were observed following coadministration of loratadine with each of these drugs in normal volunteers (n=24 in each study), there were no clinically relevant changes in the safety profile of loratadine, as assessed by electrocardiographic parameters, clinical laboratory tests, vital signs, and adverse events. There was no significant effects on QTc intervals, and no reports of sedation of syncope. No effects on plasma concentrations of cimetidine or ketoconazole were observed. Plasma concentrations (AUC 0-24 hrs) of erythromycin decreased 15% with coadministration of loratadine relative to that observed with erythromycin alone. The clinical relevance of this difference is unknown. These above findings are summarized in TABLE 1.
There does not appear to be an increase in adverse events in subjects who received oral contraceptives and loratadine. Loratadine; pseudoephedrine sulfate extended release tablets (pseudoephedrine component) are contraindicated in patients taking monoamine oxidase inhibitors and for 2 weeks after stopping use of an MAO inhibitor. The antihypertensive effects of beta-adrenergic blocking agents, methyldopa, mecamylamine, reserpine, and veratrum alkaloids may be reduced by sympathomimetics. Increased ectopic pacemaker activity can occur when pseudoephedrine is used concomitantly with digitalis.
Warnings
WARNINGSLoratadine; pseudoephedrine sulfate extended release tablets should be used with caution in patients with hypertension, diabetes mellitus, ischemic heart disease, increased intraocular pressure, hyperthyroidism, renal impairment, or prostatic hypertrophy. Central nervous system stimulation with convulsions or cardiovascular collapse with accompanying hypotension may be produced by sympathomimetic amines. Use in Patients Approximately 60 Years of Age and Older: The safety and efficacy of loratadine; pseudoephedrine sulfate extended release tablets in patients greater than 60 years old have not been investigated in placebo-controlled clinical trials. The elderly are more likely to have adverse reactions to sympathomimetic amines. Precautions
PRECAUTIONSGeneral Loratadine; Pseudoephedrine Sulfate 24 Hour Extended Release Tablets: Because there have been reports of esophageal obstruction and perforation in patients who have taken a previously marketed formulation of CLARITIN-D 24 HOUR Extended Release Tablets, it is recommended that patients who have a history of difficulty in swallowing tablets or who have known upper gastrointestinal narrowing or abnormal esophageal peristalsis not use this product. Furthermore, since it is not known whether this formulation of CLARITIN-D 24 HOUR Extended Release Tablets has the potential for this adverse event, it is reasonable to recommend that all patients take this product with a full glass of water (see Information for the Patient, ADVERSE REACTIONS and DOSAGE AND ADMINISTRATION). Loratadine; Pseudoephedrine Sulfate 12 and 24 Hour Extended Release Tablets: Because the doses of this fixed combination product cannot be individually titrated and hepatic insufficiency results in a reduced clearance of loratadine to a much greater extent than pseudoephedrine, loratadine; pseudoephedrine sulfate extended release tablets should generally be avoided in patients with hepatic insufficiency. Patients with renal insufficiency (GFR OVERDOSEIn the event of overdosage, general symptomatic and supportive measures should be instituted promptly and maintained for as long as necessary. Treatment of overdosage would reasonably consist of emesis (ipecac syrup), except in patients with impaired consciousness, followed by the administration of activated charcoal to absorb any remaining drug. If vomiting is unsuccessful, or contraindicated, gastric lavage should be performed with normal saline. Saline cathartics may also be of value for rapid dilution of bowel contents. Loratadine is not eliminated by hemodialysis. It is not known if loratadine is eliminated by peritoneal dialysis. Somnolence, tachycardia, and headache have been reported with doses of 40 to 180 mg of loratadine; pseudoephedrine. In large doses, sympathomimetics may give rise to giddiness, headache, nausea, vomiting, sweating, thirst, tachycardia, precordial pain, palpitations, difficulty in micturition, muscular weakness and tenseness, anxiety, restlessness, and insomnia. Many patients can present a toxic psychosis with delusions and hallucinations. Some may develop cardiac arrhythmias, circulatory collapse, convulsions, coma, and respiratory failure. The oral median lethal dose for the mixture of the two drugs was greater than 525 and 1839 mg/kg in mice and rats, respectively (approximately 10 and 58 times the maximum recommended human daily oral loratadine; pseudoephedrine sulfate 24 hour dose on a mg/m2 basis). The oral median lethal dose for loratadine was greater than 5000 mg/kg in rats and mice (greater than 2000 times the maximum recommended human daily oral loratadine; pseudoephedrine sulfate 24 hourdose on a mg/m2 basis). Single oral doses of loratadine showed no effects in rats, mice, and monkeys at doses as high as 10 times the maximum recommended human daily oral dose on a mg/m2 basis. Contraindications
CONTRAINDICATIONSLoratadine; pseudoephedrine sulfate extended release tablets are contraindicated in patients who are hypersensitive to this medication or to any of its ingredients. This product, due to its pseudoephedrine component, is contraindicated in patients with narrow-angle glaucoma or urinary retention, and in patients receiving monoamine oxidase (MAO) inhibitor therapy or within fourteen (14) days of stopping such treatment (see DRUG INTERACTIONS). It is also contraindicated in patients with severe hypertension, severe coronary artery disease, and in those who have shown hypersensitivity or idiosyncrasy to its components, to adrenergic agents, or to other drugs of similar chemical structures. Manifestations of patient idiosyncrasy to adrenergic agents include: insomnia, dizziness, weakness, tremor, or arrhythmias.
Clinical Pharmacology
CLINICAL PHARMACOLOGYThe following information is based upon studies of loratadine alone or pseudoephedrine alone, except as indicated. Loratadine is a long-acting tricyclic antihistamine with selective peripheral histamine H1-receptor antagonistic activity. Human histamine skin wheal studies following single and repeated oral doses of loratadine have shown that the drug exhibits an antihistaminic effect beginning within 1 to 3 hours, reaching a maximum at 8 to 12 hours, and lasting in excess of 24 hours. There was no evidence of tolerance to this effect developing after 28 days of dosing with loratadine. Pharmacokinetic studies following single and multiple oral doses of loratadine in 115 volunteers showed that loratadine is rapidly absorbed and extensively metabolized to an active metabolite (descarboethoxyloratadine). Approximately 80% of the total dose administered can be found equally distributed between urine and feces in the form of metabolic products after 10 days. The mean elimination half-lives found in studies in normal adult subjects (n = 54) were 8.4 hours (range = 3 to 20 hours) for loratadine and 28 hours (range = 8.8 to 92 hours) for the major active metabolite (descarboethoxyloratadine). In nearly all patients, exposure (AUC) to the metabolite is greater than exposure to parent loratadine. Loratadine and descarboethoxyloratadine reached steady-state in most patients by approximately the fifth dosing day. The pharmacokinetics of loratadine and descarboethoxyloratadine are dose independent over the dose range of 10 to 40 mg and are not significantly altered by the duration of treatment. In vitro studies with human liver microsomes indicate that loratadine is metabolized to descarboethoxyloratadine predominantly by P450 CYP3A4 and, to a lesser extent, by P450 CYP2D6. In the presence of a CYP3A4 inhibitor ketoconazole, loratadine is metabolized to descarboethoxyloratadine predominantly by CYP2D6. Concurrent administration of loratadine with either ketoconazole, erythromycin (both CYP3A4 inhibitors), or cimetidine (CYP2D6 and CYP3A4 inhibitor) to healthy volunteers was associated with significantly increased plasma concentrations of loratadine (see DRUG INTERACTIONS). In a study involving 12 healthy geriatric subjects (66 to 78 years old), the AUC and peak plasma levels (Cmax) of both loratadine and descarboethoxyloratadine were significantly higher (approximately 50% increased) than in studies of younger subjects. The mean elimination half-lives for the elderly subjects were 18.2 hours (range = 6.7 to 37 hours) for loratadine and 17.5 hours (range = 11 to 38 hours) for the active metabolite. Loratadine; Pseudoephedrine Sulfate 12 hour Extended Release Tablets Only: In the clinical efficacy studies, loratadine was administered before meals. In a single-dose study, food increased the AUC of loratadine by approximately 40% and of descarboethoxyloratadine by approximately 15%. The time of peak plasma concentration (Tmax) of loratadine and descarboethoxyloratadine was delayed by 1 hour with a meal. In patients with chronic renal impairment (creatinine clearance £30 ml/min) both the AUC and peak plasma levels (Cmax) increased on average by approximately 73% for loratadine; and approximately by 120% for descarboethoxyloratadine, compared to individuals with normal renal function. The mean elimination half-lives of loratadine (7.6 hours) and descarboethoxyloratadine (23.9 hours) were not significantly different from that observed in normal subjects. Hemodialysis does not have an effect on the pharmacokinetics of loratadine or its active metabolite (descarboethoxyloratadine) in subjects with chronic renal impairment. In patients with chronic alcoholic liver disease the AUC and peak plasma levels (Cmax) of loratadine were double while the pharmacokinetic profile of the active metabolite (descarboethoxyloratadine) was not significantly changed from that in normals. The elimination half-lives for loratadine and descarboethoxyloratadine were 24 hours and 37 hours, respectively, and increased with increasing severity of liver disease. There was considerable variability in the pharmacokinetic data in all studies of loratadine, probably due to the extensive first-pass metabolism. Individual histograms of area under the curve, clearance, and volume of distribution showed a log normal distribution with a 25-fold range in distribution in healthy subjects. Loratadine is about 97% bound to plasma proteins at the expected plasma concentrations (2.5 to 100 ng/ml) after a therapeutic dose. Loratadine does not affect the plasma protein binding of warfarin and digoxin. The metabolite descarboethoxyloratadine is 73% to 77% bound to plasma proteins (at 0.5 to 100 ng/ml). Whole body autoradiographic studies in rats and monkeys, radiolabeled tissue distribution studies in mice and rats, and in vivo radioligand studies in mice have shown that neither loratadine nor its metabolites readily cross the blood-brain barrier. Radioligand binding studies with guinea pig pulmonary and brain H1-receptors indicate that there was preferential binding to peripheral versus central nervous system H1-receptors. In a study in which loratadine alone was administered at four times the clinical dose for 90 days, no clinically significant increase in the QTc was seen on ECGs. In a single-rising dose study of loratadine alone in which doses up to 160 mg (16 times the clinical dose) were administered, no clinically significnt changes on the QTc interval in the ECGs were observed. Pseudoephedrine sulfate (d-isoephedrine sulfate) is an orally active sympathomimetic amine which exerts a decongestant action on the nasal mucosa. It is recognized as an effective agent for the relief of nasal congestion due to allergic rhinitis. Pseudoephedrine produces peripheral effects similar to those of ephedrine and central effects similar to, but less intense than, amphetamines. It has the potential for excitatory side effects. The bioavailability of loratadine; pseudoephedrine sulfate from loratadine; pseudoephedrine sulfate 24 hour extended release tablets is similar to that achieved with separate administration of the components. Coadministration of loratadine and pseudoephedrine does not significantly affect the bioavailability of either component. In a single-dose study, food increased the AUC of loratadine by approximately 125% and Cmax by approximately 80%. However, food did not significantly affect the pharmacokinetics of pseudoephedrine sulfate or descarboethoxyloratadine. Loratadine; Pseudoephedrine Sulfate 12 hour Extended Release Tablets Only: The pseudoephedrine component of loratadine; pseudoephedrine sulfate 12 hour extended release tablets was absorbed at a similar rate and was equally available from the combination tablet as from a pseudoephedrine sulfate repetabs 120 mg tablet. Mean (%CV) steady-state peak plasma concentration of 464 ng/mL (22) was attained at 3.9 hours (50). The terminal half-life of pseudoephedrine from the combination tablet administered twice daily was 6.3 hours (23). The ingestion of food was found not to affect the absorption of pseudoephedrine from loratadine; pseudoephedrine sulfate 12 hour extended release tablets. Loratadine and pseudoephedrine sulfate do not influence the pharmacokinetics of each other when administered concomitantly. CLINICAL STUDIES12 Hour Extended Release Tablets Clinical trials of loratadine; pseudoephedrine sulfate 12 hour extended release tablets in seasonal allergic rhinitis involved approximately 3700 patients who received either the combination product, a comparative treatment, or placebo, in double-blind, randomized controlled studies. Four of the largest studies involved approximately 1600 patients in comparisons of the combination product, loratadine (5 mg bid), pseudoephedrine sulfate (120 mg bid), and placebo. Improvement in symptoms of seasonal allergic rhinitis for patients receiving loratadine; pseudoephedrine sulfate 12 hour extended release tablets was significantly greater than the improvement in those patients who received the individual components or placebo. The combination reduced the intensity of sneezing, rhinorrhea, nasal pruritus, and eye tearing more than pseudoephedrine and reduced the intensity of nasal congestion more than loratadine, demonstrating a contribution of each of the components. The onset of antihistamine and nasal decongestant actions occurred after the first dose of loratadine; pseudoephedrine sulfate 12 hour extended release tablets. Loratadine; pseudoephedrine sulfate 12 hour extended release tablets were well tolerated, with a frequency of sedation similar to that seen with placebo, and an adverse event profile clinically similar to that of pseudoephedrine. 24 Hour Extended Release Tablets Clinical trials of loratadine; pseudoephedrine sulfate 24 hour extended release tablets involved a total of approximately 2000 patients with seasonal allergic rhinitis. One study involved 879 patients, who received either the combination product (loratadine 10 mg and pseudoephedrine sulfate 240 mg), loratadine (10 mg once daily) or pseudoephedrine sulfate (120 mg twice daily) alone, or placebo, in a double-blind randomized design. Improvement in nasal and non-nasal symptoms of seasonal allergic rhinitis including nasal congestion in patients receiving loratadine; pseudoephedrine sulfate 24 hour extended release tablets was significantly greater than in placebo recipients, and generally greater than that achieved with loratadine or pseudoephedrine sulfate alone. In this study, loratadine; pseudoephedrine sulfate 24 hour extended release tablets were well tolerated, with a frequency of sedation similar to that seen with placebo, and a frequency of nervousness and insomnia similar to that seen with pseudoephedrine sulfate given alone. In another study of 469 patients, once-daily administration of loratadine; pseudoephedrine sulfate 24 hour extended release tablets provided effects similar to those achieved with twice-daily administration of loratadine; pseudoephedrine sulfate 12 hour extended release tablets, a combination product containing 5 mg loratadine plus 120 mg pseudoephedrine sulfate, extended release. The end of dosing interval efficacy of the pseudoephedrine component of loratadine; pseudoephedrine sulfate 24 hour extended release tablets on the symptom of nasal stuffiness was evaluated in a study of 695 patients who were randomized to receive loratadine; pseudoephedrine sulfate 24 hour extended release tablets, loratadine; pseudoephedrine sulfate tablets, or placebo. Patients who received loratadine; pseudoephedrine sulfate 24 hour extended release tablets had significantly more improvement in nasal stuffiness scores at the end of the dosing interval than those patients receiving loratadine; pseudoephedrine sulfate tablets or placebo throughout the course of the trial. 12 and 24 Hour Extended Release Tablets In a 6-week, placebo-controlled study of 193 patients with seasonal allergic rhinitis and concomitant mild to moderate asthma, loratadine; pseudoephedrine sulfate 12 and 24 hour extended release tablets twice daily improved seasonal allergic rhinitis signs and symptoms with no decrease in pulmonary function or adverse effect on asthma symptoms. This supports the safety of administering loratadine; pseudoephedrine sulfate 12 and 24 hour extended release tablets to seasonal allergic rhinitis patients with asthma.
Medication Guide
PATIENT INFORMATIONSee WARNINGS, CONTRAINDICATIONS, and PRECAUTIONS. From
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