Cetirizine hydrochloride, pseudoephedrine hydrochloride.
Each film coated tablet of Cetrizet D contains: Cetirizine Hydrochloride BP 5 mg; Pseudoephedrine Hydrochloride BP (as extended release) 120 mg.
Combination of antihistamine and decongestant used to relieve allergic rhinitis.
Pharmacology: Pharmacodynamics: Cetirizine is a potent antihistamine with a low potential for drowsiness at pharmacologically active doses and with additional anti-allergic properties. It is selective H1-antagonist with negligible effects on other receptors and so is virtually free from anti-cholinergic and anti-serotonin effects. At pharmacologically active doses, it induces neither sedation nor behaviour changes. This may be explained by the fact that cetirizine does not cross the blood-brain barrier.
It was shown in human pharmacology studies that cetirizine inhibits certain effects produced by exogenous histamine. This activity appears rapidly. Cetirizine also inhibits the effects produced by endogenous histamine released in vivo by any agent. It also inhibits the cutaneous reaction induced by VIP (Vasoactive Intestinal Polypeptide) and substance P, neuropeptides, which are believed to take part in the allergic reaction.
Cetirizine inhibits the histamine-mediated 'early' phase of the allergic reaction and also reduces the migration of inflammatory cells and the release of mediators associated with the 'late' allergic response.
Cetirizine markedly reduces bronchial hyper-reactivity to histamine in the asthmatic patient. It also reduces the allergic reaction induced by specific allergens. These effects are obtained without any central effects being demonstrated either by psychometric tests or by quantified EEG.
Pseudoephedrine has direct and indirect sympathomimetic activity and is an orally effective upper respiratory tract decongestant. Pseudoephedrine is substantially less potent than ephedrine in producing both tachycardia and elevation in systolic blood pressure and considerably less potent in causing stimulation of the central nervous system.
Pharmacokinetics: Cetirizine: After oral administration, cetirizine is rapidly and almost completely absorbed. Under fasting conditions, Cmax is about 1 hour. The extent of absorption is not reduced by food; however, the rate of absorption is reduced and the peak levels are expected about 3 hrs after dosing. Cetirizine does not undergo any appreciable first-pass metabolism. After repeated oral administration, the daily urinary excretion of unchanged cetirizine is approximately 65% of the dose. The absorption and the elimination of cetirizine are independent of the dose. Inter- and intra-subject variations are low. The plasma half-life of cetirizine is approximately 9 hours. This value is increased in patients with reduced renal function. Cetirizine is strongly bound to plasma proteins.
Pseudoephedrine: Pseudoephedrine is rapidly and completely absorbed after oral administration. Pseudoephedrine, given as a sustained-release formulation, provides maximum plasma levels 8 hrs after administration. About ¼-½ of the administered dose of pseudoephedrine is transformed by the liver into inactive metabolite through N-demethylation. This metabolite and the remaining non-metabolized pseudoephedrine are excreted via the kidneys.
The rate of urinary excretion is increased when the urine is acidic, and reduced in case of alkalinization of urine. The absorption of pseudoephedrine is not affected by fatty meals. After repeated oral administration (every 12 hrs), the steady state is obtained within 6 days and the effective half-life is estimated to 15 hrs.
There was no evidence for a relevant pharmacokinetic interaction between cetirizine and pseudoephedrine.
Treatment of symptoms associated with seasonal allergy or hay fever, perennial allergic rhinitis and common cold e.g., nasal congestion, sneezing, rhinorrhea, nasal and ocular pruritus.
Cetrizet-D should be administered when both the antiallergic properties of cetirizine HCl and the nasal decongestant activity of pseudoephedrine HCl are desired.
Recommended Dosage, Dosage Schedule: Adult and children ≥12 years: The recommended dosage is 1 tablet, twice daily. Do not take more often than one tablet every twelve hours.
The tablet should preferably be swallowed with some liquid and should not be chewed.
Treatment should normally not exceed the symptomatic period. When adequate relief from nasal symptoms is obtained, treatment with an antihistaminic drug should be continued, if appropriate.
Mode of Administration: Oral.
Symptoms and Treatment For Overdosage: Cetirizine Hydrochloride: Drowsiness can be a symptom of overdosage, occurring from administration of 50 mg of Cetirizine dihydrochloride as a single dose. In the case of massive overdosage, gastric lavage should be performed together with the usual supportive measures. To date, there is no specific antidote. Apart from the usual supportive measures, all vital parameters have to be monitored regularly.
Pseudoephedrine Hydrochloride: Symptoms of overdosage include irritability, restless, tremor, convulsions, palpitations, hypertension, difficulty in micturition, tachycardia, arrhythmia, signs of CNS depression (sedation, apnea, unconsciousness, cyanosis and cardiovascular collapse) or stimulation (insomnia, hallucination, tremor, seizures) which can be fatal.
Treatment preferably in a hospital setting, should be symptomatic and supportive, taking into account any concomitantly ingested medication. Necessary steps should be taken to maintain the support respiration and control convulsions. Gastric lavage should be performed if indicated. After vomiting, the drug still remaining in the stomach can be absorbed using a suspension of charcoal in water. Apart from the usual supportive measures, all vital parameters have to be monitored regularly. There are no known antidotes. Catheterisation of the bladder may be necessary. If desired, the elimination of pseudoephedrine can be accelerated by acid diuresis or by dialysis. Sympathomimetic amines should not be used.
Hypertension can be controlled with alpha-blockers and tachycardia with beta-blockers. Seizures can be treated with 10 mg of IV diazepam or 0.5 mg/kg of diazepam given rectally in the case of children.
In patients with a history of hypersensitivity to any of the constituents, to ephedrine or to any of piperazines.
In lactating women since it is excreted in breast milk.
In patients who had previous intolerance to pseudoephedrine.
In patients with severe hypertension or severe coronary artery disease. Patients taking antihypertensive e.g., beta-blockers, sympathomimetic drugs and amphetamines.
In patients who are taking or have taken monoamine oxidase inhibitors within the preceding two weeks. The concomitant use of pseudoephedrine and this type of product may occasionally cause a rise in blood pressure.
Concurrent administration of furazolidone and pseudoephedrine.
Patients with renal insufficiency, uncontrolled hyperthyroidism, severe arrhythmia, increased intraocular pressure or with urinary retention.
Cetrizet-D should be used with caution in patients with diabetes, hyperthyroidism, hypertension, tachycardia, arrhythmia, renal or hepatic insufficiency, prostatic hypertrophy or urethral dysfunction, in patients taking alcohol although there is no potentiation of alcohol by cetirizine, and in the elderly.
Cetirizine Hydrochloride: Studies in healthy volunteers at 20 to 25 mg/day have not revealed effects on alertness or reaction time; however, patients are advised not to exceed the recommended dose if driving or operating machinery.
Pseudoephedrine Hydrochloride: Pseudoephedrine should be used with caution in patients taking antihypertensive agents, tricyclic anti-depressants, other sympathomimetic agents such as decongestants, appetite suppressants, amphetamine-like psychostimulants and digitalis. As with other centrally acting stimulants, abuse has been observed for pseudoephedrine. Caution should be exercised in the presence of severe renal or hepatic impairment.
Pseudoephedrine should be used with caution in patients with hypertension, heart disease, diabetes, hyperthyroidism, elevated intraocular pressure and prostatic enlargement. There is no information on the effect of pseudoephedrine on human fertility.
Use in Children: Although cetirizine and pseudoephedrine have both proven to be efficacious in children >2 years, Cetrizet-D has not been tested in children <12 years.
Use in the elderly: Caution is required when administering the drug to patients >50 years.
There is no specific data on the use of cetirizine or pseudoephedrine during pregnancy. Therefore, Cetrizet-D should be given only if the potential benefit justifies the potential risks to the fetus/neonate. Cetirizine and pseudoephedrine are excreted in breast milk in small amounts but the effect of this on breast-fed infants is not known.
Cetirizine Hydrochloride: In objective tests of psychomotor function, the incidence of sedation with Cetirizine was similar to that of placebo. There have been occasional reports of mild and transient side effects such as headache, dizziness, drowsiness, agitation, dry mouth, insomnia, somnolence, asthenia, tachycardia, nervousness, vertigo, nausea and gastrointestinal discomfort.
Pseudoephedrine Hydrochloride: Serious adverse effects associated with the use of pseudoephedrine are rare. Symptoms of central nervous system excitation may occur, including sleep disturbances and rarely hallucinations have been reported. Skin rashes, with or without irritation, have occasionally been reported. Urinary retention has been reported occasionally in men receiving pseudoephedrine; prostatic enlargement could have been an important predisposing factor. Other reactions include fear, anxiety, tenseness, restlessness, tremor, weakness, pallor, respiratory difficulty, dysuria, convulsions, CNS depression, arrhythmias and cardiovascular collapse with hypotension.
Cetirizine Hydrochloride: As cetirizine is only minimally metabolised, being excreted unchanged primarily via the kidneys, it may have a low potential for adverse drug reactions involving or inhibition metabolic enzyme systems.
Potentially hazardous interactions: There are no reports of hazardous interactions with other drugs to date. Concomitant administration with alcohol or diazepam does not impair psychomotor performance any more than the impairment of performance produced by alcohol alone. Nevertheless, caution is recommended if sedatives are also being taken. Allergy skin tests are inhibited by antihistamines and an appropriate wash out period is required before performing them.
Pseudoephedrine Hydrochloride: Increased ectopic pacemaker activity can occur when pseudoephedrine is used concomitantly with digitalis; use of Cetrizet-D is therefore to be avoided in digitalized patients. Antacids increase the rate of pseudoephedrine absorption; kaolin decreases it. Concomitant use of pseudoephedrine with other sympathomimetic agents such as decongestants, tricyclic antidepressants, appetite suppressants and amphetamine-like psychostimulants or with monoamine oxidase inhibitors, which interfere with the catabolism of sympathomimetic amines, may occasionally cause a rise in blood pressure. Interaction with MAO inhibitor is still possible for up to 15 days after stopping treatment due to the long duration of action of MAO inhibitor.
The effect of antihypertensive agents which interfere with sympathetic activity may be partially reversed by pseudoephedrine, e.g., bretylium, bethanidine, guanethidine, reserpine, debrisoquine, methyldopa, alpha and beta-adrenergic blocking agents.
Store in a cool dry place below 30°C, protected from light.
R01BA52 - pseudoephedrine, combinations ; Belongs to the class of systemic sympathomimetic preparations used as nasal decongestants.
Cetrizet D XR-FC tab
10 × 10's
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