Product information

PRODUCT INFORMATION
CLARATYNE-D WITH DECONGESTANT REPETABS TABLETS
NAME OF DRUG
Loratadine and pseudoephedrine sulfate
DESCRIPTION
Each Claratyne-D w ith Decongestant Repetabs Tablet contains loratadine 5 mg and
pseudoephedrine sulfate 60 mg in the tablet coating, as w ell as pseudoephedrine sulfate 60 mg
in the barrier-coated core. The active components in the coating are quickly liberated; release
of the decongestant in the core is delayed for several hours. Each tablet also contains lactose,
povidone, magnesium stearate, acacia, dried calcium sulfate, carnauba w ax, oleic acid, purified
talc, maize starch, sucrose, microcrystalline cellulose, neutral w hite soap – Polaris 134,
colophony, zein, titanium dioxide and w hite beesw ax.
PHARMACOLOGY
Loratadine is a potent long-acting tricyclic antihistamine w ith relative selectivity for peripheral
H -receptors. It exhibits greater affinity for peripheral H -receptors than for central H -
receptors. These properties account for the observed lack of sedation. The incidence of sedation w ith loratadine is comparable to that of placebo. Specific clinical pharmacology studies w ere conducted w ith concomitant administration of loratadine w ith therapeutic doses of erythromycin, ketoconazole, and cimetidine for 10 days in healthy subjects. Although increased plasma concentrations (AUC active metabolite descarboethoxyloratadine w ere observed, there w ere no clinically relevant
changes in the safety profile of loratadine as assessed by electrocardiographic parameters
including QTc interval, clinical laboratory tests, vital signs and adverse events. Additionally,
cardiac repolarisation w as not altered, nor w ere other electrocardiographic parameters. (See
Drug Interactions section.)
Pseudoephedrine sulfate, one of the naturally occurring alkaloids of Ephedra and an orally
administered vasoconstrictor, produces a gradual but sustained decongestant effect facilitating
shrinkage of congested mucosa in upper respiratory areas. The mucous membrane of the
respiratory tract is decongested through the action on the sympathetic nerves.
Pharmacokinetics
Loratadine is w ell absorbed w ith peak plasma levels occurring at approximately one or tw o
hours after dosing. The drug is almost totally metabolised. It has an active metabolite,
descarboethoxyloratadine (SCH 34117); this metabolite corresponds to 1% to 2% of the dose.
In man, loratadine is extensively bound to plasma protein (97 to 99% ) and SCH 34117
moderately bound (73 to 76%). Approximately 40% of the dose is excreted in the urine and
42% in the faeces in a 10-day period. Concomitant ingestion of food w ith loratadine may
delay absorption (by approximately one hour) and may increase the AUC for both loratadine
(40% ) and its active metabolite SCH 34117 (approximately 15%). These differences w ould
not be expected to be clinically important.
The pseudoephedrine component of Claratyne-D w ith Decongestant Repetabs tablets w as
absorbed at a similar rate and w as equally available from the combination tablet as from a
pseudoephedrine sulfate 120mg Repetabs tablet. Mean (% CV) steady-state peak plasma
concentration of 464ng/mL (22) w as attained at 3.9 hours (50). The terminal half -life of
pseudoephedrine from Claratyne-D w ith Decongestant administered tw ice-daily w as 6.3 hours
(23). Loratadine and pseudoephedrine sulfat e do not influence the pharmacokinetics of each
other w hen administered concomitantly.
INDICATIONS
Claratyne-D w ith Decongestant Repetabs tablets are indicated for the relief of symptoms
associated w ith acute seasonal allergic rhinitis including nasal congestion, sneezing,
rhinorrhoea, pruritus and lacrimation.
CONTRAINDICATIONS
Claratyne-D w ith Decongestant Repetabs tablets are contraindicated in those w ho have show n
sensitivity or idiosyncrasy to their components, to adrenergic agents or to other drugs of similar
chemical structure. Claratyne-D w ith Decongestant Repetabs tablets are also contraindicated in
patients receiving monoamine oxidase (MAO) inhibitor therapy or w ithin fourteen days of
discontinuing such treatment and in patients w ith narrow angle glaucoma, urinary retention,
severe hypertension, severe coronary artery disease and hyperthyroidism.
PRECAUTIONS
Sympathomimetics should be used w ith caution in patients w ith glaucoma, stenosing peptic
ulcer, pyloroduodenal obstruction, prostatic hypertrophy or bladder neck obstruction,
cardiovascular disease, increased intraocular pressure or diabetes mellitus.
Sympathomimetics should be used w ith caution in patients receiving digitalis.
Sympathomimetics may cause central nervous system (CNS) stimulation, excitability,
convulsions, and/or cardiovascular collapse w ith accompanying hypotension.
In patients 60 years of age or older, sympathomimetics are also more likely to cause adverse
reactions such as confusion, hallucination, convulsions, CNS depression and death. No studies
have been conducted w ith Claratyne-D w ith decongestant Repetabs tablets in patients over 60
years of age. Consequently, caution should be exercised w hen administering a repeat -action
formulation to elderly patients.
Immune System: In a 17-month study in monkeys, loratadine demonstrated no functional
impairment of the immune system as indicated by mortality, peripheral leucocyte count or
incidences of inflammatory reactions, autoimmune disease and malignancy. Specific studies
investigating the effect of loratadine on immune function in humans have not been performed.
Cardiovascular: No studies have been conducted in patients w ith cardiovascular disease.
Caution should be used w ith products containing sympathomimetics in patients w ith
cardiovascular disease.
Carcinogenesis, mutagenesis, impairment of fertility: Loratadine administered in the diet to
mice for 18 months at doses greater than 12mg/kg/day resulted in an increased incidence of
benign hepatic tumours. A 2-year study in rats show ed no increase in the incidence of
carcinogenicity in loratadine-treated animals compared w ith control animals at dietary doses up to 25mg/kg/day. Animal studies show ed that loratadine had an adverse effect on male fertility w hen administered to rats at doses greater than 24mg/kg/day. The clinical relevance of this observation is unknow n at this time. Drug Abuse and Dependence: There are no data available to indicate that abuse or dependency occurs w ith loratadine. Pseudoephedrine sulfate, like other CNS stimulants, has been abused. At high doses, subjects commonly experience an elevation of mood, decreased appetite and a sense of increased physical energy, mental capacity and alertness. Anxiety, irritability and loquacity also have been experienced. Continued use of any CNS stimulant results in tolerance. Increased doses ultimately produce toxicity. Depression may follow rapid w ithdraw al. Use in Children: Safety and efficacy of Claratyne-D w ith Decongestant Repetabs tablets in children younger than 12 years of age have not yet been established. Usage During Pregnancy (B2) and Lactation: The safe use of Claratyne-D w ith Decongestant Repetabs tablets during pregnancy has not been established. Therefore, the product should only be used if the potential benefit justifies the potential risk to the foetus. Reproductive studies in pregnant rats and rabbits show ed no evidence of teratogenic activity at doses of the combination of up to 150 and 120mg/kg/day respectively. Reproductive studies in pregnant rats and rabbits show ed no evidence of embryotoxic or teratogenic activity at loratadine doses up to 96mg/kg/day. In pregnant rats, loratadine and its metabolite crossed the placental barrier, distributing in foetal tissues in a pattern similar to that in maternal tissues but at low er concentrations. Similar data on the effect of pseudoephedrine on the foetus are unavailable. The safe use of loratadine during lactation has not been established. A study in lactating w omen show ed that breast milk levels of loratadine and its active metabolite parallel their respective plasma concentrations after oral administration. Acute toxicity studies have demonstrated that neonatal rats and mice are more sensitive to loratadine than adults of the corresponding species. Pseudoephedrine sulfate is also excreted in breast milk. The use of Claratyne-D w ith Decongestant by breastfeeding mothers is therefore not recommended. Drug Interactions: When administered concomitantly w ith alcohol, loratadine has no potentiating effect as measured by psychomotor performance studies. Loratadine (10 mg once daily) has been safely coadministered w ith therapeutic doses of erythromycin, cimetidine and ketoconazole in controlled clinical pharmacology studies. Although descarboethoxyloratadine w ere observed follow ing coadministration of loratadine w ith each
of these drugs in normal volunteers, there w ere no clinically relevant changes in the safety
profile of loratadine and no reports of sedation or syncope. (See PHARMACOLOGY section.)
When sympathomimetics are given to patients receiving MAO inhibitors, hypertensive
reactions, including hypertensive crises may occur. The antihypertensive effects of
methyldopa, mecamylamine, reserpine and veratrum alkaloids may be reduced by
sympathomimetics. Beta-adrenergic blocking agents may also interact w ith sympathomimetics.
Increased ectopic pacemaker activity can occur w hen pseudoephedrine is used concomitantly
w ith digitalis. Antacids increase the rate of pseudoephedrine absorption; kaolin decreases it.
Laboratory Interactions
Antihistamines should be discontinued approximately 48 hours prior to skin testing procedures
since these drugs may prevent or diminish otherw ise positive reactions to dermal reactivity
indicators.
The in vitro addition of pseudoephedrine to sera containing the cardiac isoenzyme MB of serum
creatine phosphokinase progressively inhibits the activity of the enzyme. The inhibition
becomes complete over six hours.
ADVERSE REACTIONS
During controlled clinical studies w ith the recommended dosage, the incidence of adverse
effects associated w ith Claratyne-D w ith Decongestant Repetabs tablets w as comparable to
that of placebo, w it h the exception of insomnia (16% vs placebo 3% ) and dry mouth (14% vs
placebo 4% ). Other most frequently reported side effects include headache (10% vs placebo
10%), sedation (6% vs placebo 4% ), nervousness (5% vs placebo 1% ), dizziness (4% vs
placebo 1% ) and fatigue (4% vs placebo 2%).
Rare adverse reactions in decreasing order of frequency included nausea, abdominal distress,
anorexia, thirst, tachycardia, pharyngitis, rhinitis, acne, pruritus, rash, urticaria, arthralgia,
confusion, dysphonia, hyperkinesia, hypoaesthesia, decreased libido, paraesthesia, tremor,
vertigo, flushing, postural hypotension, increased sw eating, eye disorders, earache, tinnitus,
taste abnormality, agitation, apathy, depression, euphoria, nightmares, increased appetite,
change in bow el habits, dyspepsia, eructation, haemorrhoids, tongue discolouration, tongue
disorder, vomiting, transient abnormal hepatic function, dehydration, increased w eight,
hypertension, palpitation, migraine, bronchospasm, coughing, dyspnoea, epistaxis, nasal
congestion, sneezing, nasal irritation, dysuria, micturition disorder, nocturia, polyuria, urinary
retention, asthenia, back pain, leg cramps, malaise and rigors.
During the marketing of loratadine, alopecia, anaphylaxis, abnormal hepatic function,
supraventricular tachyarrhythmias and dizziness have been reported rarely.
DOSAGE AND ADMINISTRATION
Adults and children 12 years of age and over:
One Claratyne-D w ith Decongestant Repetabs tablet every 12 hours.
For patients w ith severe hepatic impairment a low er initial dose of one tablet daily is
recommended.
OVERDOSAGE
In the event of overdosage, general symptomatic and supportive treatment should be started
immediately and maintained for as long as necessary.
Manifestations: These may vary from CNS depression (sedation, apnoea, diminished mental alertness, cyanosis, coma, cardiovascular collapse) to stimulation (insomnia, hallucination, tremors or convulsions) to death. Other signs and symptoms may be euphoria, excitement, tachycardia, palpitations, thirst, perspiration, nausea, dizziness, tinnitus, ataxia, blurred vision and hypertension or hypotension. Stimulation is particularly likely in children, as are atropine-like signs and symptoms (dry mouth; fixed, dilated pupils; flushing; hyperthermia; and gastrointestinal symptoms). In large doses sympathomimetics may give rise to giddiness, headache, nausea, vomiting, sw eating, thirst, tachycardia, precordial pain, palpitations, difficulty in micturition, muscular w eakness and tenseness, anxiety, restlessness and insomnia. Many patients can present a toxic psychosis w ith delusions and hallucinations. Some may develop cardiac arrhythmias, circulatory collapse, convulsions, coma and respiratory failure. Treatment: Treatment of the signs and symptoms of overdosage is symptomatic and supportive. Stimulants (analeptic agents) should not be used. Vasopressors may be used to treat hypotension. Short -acting barbiturates, diazepam or paraldehyde may be administered to control seizures. Hyperpyrexia, especially in children, may require treatment w ith tepid w ater sponge baths or hypothermic blanket. Apnoea is treated w ith ventilatory support. PRESENTATION
Repetabs tablets - Loratadine 5 mg and pseudoephedrine sulfate 120 mg (w hite, round,
biconvex coated tablet): 6’ s.
Storage Conditions
Store below 25C. Protect from excessive moisture.
Poison Schedule
S3 - Pharmacist Only Medicine
SPONSOR
Merck Sharp & Dohme (Australia) Pty Limited 54 – 68 Ferndell Street,
South Granville, NSW 2142, AUSTRALIA
This Product Information w as approved by the Therapeutic Goods Administration on: 18 December
2012

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