Source: Health Products Regulatory Authority (IE) Revision Year: 2021 Publisher: Johnson & Johnson (Ireland) Limited, Airton Road, Tallaght, Dublin 24, Ireland
Pharmacotherapeutic group: Sympathomimetics, pseudoephedrine, combinations
ATC code: R01BA52
Triprolidine provides symptomatic relief in conditions believed to depend wholly, or partly, upon the triggered release of histamine. Triprolidine is a potent, competitive H1-receptor antagonist of the pyrrolidine class with mild central nervous system depressant properties which may cause drowsiness.
Pseudoephedrine has direct and indirect sympathomimetic activity and is an effective upper respiratory decongestant. Pseudoephedrine is less potent than ephedrine in producing both tachycardia and elevation of systolic blood pressure and is less potent in causing stimulation of the central nervous system.
After oral administration of a single dose of 2.5 mg triprolidine to adults the onset of action, as determined by the ability to antagonise histamine-induced weals and flares in the skin, is within 1 to 2 hours. Peak effects occur at about 3 hours, and although activity declines thereafter, significant inhibition of histamine-induced weals and flares still occurs 8 hours after dose. Pseudoephedrine produces its decongestant effect within 30 minutes persisting for at least 4 hours.
After the administration of 10 ml ACTIFED Syrup in healthy adult volunteers, the peak plasma concentration (Cmax) of triprolidine is approximately 5.5-6.0 ng/ml, occurring at about 1.5 hours (Tmax) after drug administration. The plasma half-life of triprolidine is approximately 3.2 hours. The peak plasma concentration (Cmax) of pseudoephedrine is approximately 180 ng/ml, with Tmax approximately 1.5 hours after drug administration. The plasma half-life is approximately 5.5 hours (urine pH maintained between 5.0-7.0). The plasma half-life of pseudoephedrine is markedly decreased by acidification of urine and increased by alkalination.
In a limited study, three mothers nursing healthy infants were given an antihistamine-decongestant preparation containing 60 mg of pseudoephedrine and 2.5 mg of triprolidine. Milk concentrations of pseudoephedrine were higher than plasma levels in all three patients, with peak milk concentrations occurring at 1.0–1.5 hours. The investigators calculated that 1000 ml of milk produced during 24 hours would contain approximately 0.5%–0.7% of the maternal dose. However, following a single-blind, crossover study of a single dose of pseudoephedrine 60 mg vs. placebo conducted in 8 lactating mothers, and assuming maternal intake of 60 mg pseudoephedrine hydrochloride four times daily, the estimated infant dose of pseudoephedrine based on AUC and an estimated milk production rate of 150 ml/kg/day was 4.3% (95% CI, 3.2, 5.4%; range 2.2 to 6.7%) of the weight-adjusted maternal dose.
There is insufficient information available to determine whether triprolidine or pseudoephedrine have mutagenic potential.
There is insufficient information available to determine whether triprolidine or pseudoephedrine has carcinogenic potential.
In rats and rabbitssystemic administration of triprolidine up to 75 times the human daily dosage did not produce teratogenic effects. Systemic administration of pseudoephedrine up to 50 times the human daily dosage in rats, and up to 35 times the human daily dosage in rabbits, did not produce teratogenic effects.
No studies have been conducted in animals to determine whether triprolidine or pseudoephedrine have potential to impair fertility. There is no information on the effect of ACTIFED Syrup on human fertility.
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