McNeil Healthcare (Ireland) Ltd

ACTIFED 60 mg / 2.5 mg Tablets

Each tablet contains 2.5 mg Triprolidine hydrochloride and 60 mg Pseudoephedrine hydrochloride.

Excipients: Each tablet also includes 127.5 mg Lactose monohydrate

For a full list of excipients, see section 6.1

Tablet.

White, round biconvex tablet with bisecting score and M2A engraved on one side.

The score line is only to facilitate breaking for ease of swallowing and not to divide into equal doses.

ACTIFED Tablets are indicated for the symptomatic relief of upper respiratory tract disorders which are benefited by a combination of a nasal decongestant and H₁-receptor antagonist, for example allergic rhinitis, vasomoter rhinitis and the common cold.

Adults and children 12 years and over:

Oral. One tablet to be taken every 4-6 hours, up to four times a day.

Children under 12 years:

Not recommended

The Elderly:

There have been no specific studies of ACTIFED Tablets in the elderly. Experience has indicated that normal adult dosage is appropriate, although it may be advisable to monitor renal and/or hepatic function. If there is serious impairment then caution should be exercised.

ACTIFED Tablets is contra-indicated in individuals with known hypersensitivity to the product or any of its components.

ACTIFED Tablets is contra-indicated in patients with hypertension, acute ischemic heart disease, thyrotoxicosis, glaucoma or urinary retention.

ACTIFED Tablets is contra-indicated in patients who are taking, or have taken, monoamine oxidase inhibitors within the preceding two weeks. The concomitant use of a pseudoephedrine and this type of product may occasionally cause a rise in blood pressure.

The antibacterial agent Furazolidone is known to cause a dose-related inhibition of monoamine oxidase. Although there are no reports of hypertensive crises caused by the concurrent administration of ACTIFED Tablets and furazolidone, they should not be taken together.

Use in patients who are currently receiving other sympathomimetic drugs.

Do not exceed the stated dose

ACTIFED Tablets may cause drowsiness and impair performance in tests of auditory vigilance. Patients should be cautioned about engaging in activities requiring mental alertness, until they have established their own response to the drug.

Patients should be advised that concomitant use of alcohol or other central nervous depressants whilst taking ACTIFED Tablets may produce additional impairment in mental awareness in some individuals.

Caution should be exercised when administering to patients with severe hepatic impairment or moderate to severe renal impairment particularly if accompanied by cardiovascular disease.

Although pseudoephedrine has virtually no pressor effects in patients with normal blood pressure, ACTIFED Tablets should be used with caution in patients taking antihypertensive agents and tricyclic antidepressants. The effects of a single dose on the blood pressure of these patients should be observed before recommending repeated or unsupervised treatment.

The physician or pharmacist should check that sympathomimetic containing preparations are not simultaneously administered by several routes i.e. orally and topically (nasal, aural and eye preparations).

Patients with prostatic hypertrophy may have increased difficulty with micturition.

This product may act as a cerebral stimulant giving rise to insomnia, nervousness, hyperpyrexia, tremors and epileptiform convulsions.

Patients with rare hereditary problems of galactose intolerance, the Lapp lactose deficiency or glucose-galactose malabsorption should not take this medicine.

Concomitant use of ACTIFED Tablets with alcohol or other central nervous system depressants may, in some individuals, produce additional impairment in mental alertness.

The effects of anti-cholinergics e.g., some psychotropic drugs and atropine, may be potentiated by this product, giving rise to tachycardia, mouth dryness, gastrointestinal disturbances, e.g., colic, urinary retention and headache.

Concomitant use of ACTIFED Tablets with tricyclic antidepressants, other sympathomimetic agents (such as decongestants, appetite suppressants and amphetamine-like psychostimulants) or with monoamine oxidase inhibitors (including furazolidone), which interfere with the catabolism of sympathomimetic amines, may occasionally cause a rise in blood pressure.

The effect of antihypertensive agents which interfere with sympathetic activity may be partially reversed by the pseudoephedrine in ACTIFED Tablets, eg., bretylium, bethanidine, guanethidine, reserpine, debrisoquine, methyldopa, alpha- and beta-adrenergic blocking agents.

Concurrent use with halogenated anaesthetic agents such as chloroform, cyclopropane, halothane, enflurane or isoflurane may provoke or worsen ventricular arrhythmias.

This product should not be used during pregnancy unless considered essential by a physician. Although pseudoephedrine and triprolidine have been in widespread use for many years without apparent ill consequence, there are no specific data on their use during pregnancy. Caution should therefore be exercised by balancing the potential benefit of treatment to the mother against any possible hazards.

Pseudoephedrine and triprolidine are excreted in breast milk in small amounts but the effect of this on breast-fed infants is not known. It has been estimated that approximately 0.5 to 0.7% of a single dose of pseudoephedrine ingested by a nursing mother will be excreted in the breast milk over 24 hours.

ACTIFED Tablets may cause drowsiness and impair performance in tests of auditory vigilance. Patients should be cautioned about engaging in activities requiring mental alertness, such as driving a car or operating machinery, until they have established their own response to the drug.

It is recommended that patients are advised not to undertake tasks requiring mental alertness whilst under the influence of alcohol or other CNS depressants. Concomitant administration of ACTIFED Tablets may, in some patients, produce additional impairment.

This product may act as a cerebral stimulant in children and occasionally adults giving rise to insomnia, nervousness, hyperpyrexia, tremors and epileptiform convulsions. Care should be taken when used in epileptic patients.

Skin rashes, with or without irritation, tachycardia, dryness of mouth, nose and throat, and headache have occasionally been reported.

Urinary retention has been reported occasionally in men receiving pseudoephedrine; prostatic enlargement could have been an important predisposing factor.

Symptoms and signs

The effects of acute toxicity from ACTIFED Tablets may include drowsiness, lethargy, dizziness, ataxia, weakness, hypotonicity, respiratory depression, dryness of skin and mucous membranes, tachycardia, hypertension, hyperpyrexia, hyperactivity, irritability, palpitations, convulsions and difficulty with micturition.

Treatment

The treatment of overdosage is likely to be symptomatic and supportive. Necessary measures should be taken to maintain and support respiration and control convulsions. Gastric lavage should be performed up to 3 hours after ingestion if indicated. Catheterisation of the bladder may be necessary. If desired, the elimination of pseudoephedrine can be accelerated by acid diuresis or by dialysis.

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 one ACTIFED Tablet in healthy adult volunteers, the peak plasma concentration (C_max) of triprolidine is approximately 5.5 - 6.0 ng/ml, occurring at about 2.0 hours (T_max) after drug administration. The plasma half-life of triprolidine is approximately 3.2 hours. The peak plasma concentration (C_max) of pseudoephedrine is approximately 180 ng/ml, with T_max approximately 2 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.

Mutagenicity

There is insufficient information available to determine whether triprolidine or pseudoephedrine has mutagenic potential.

Carcinogenicity

There is insufficient information available to determine whether triprolidine or pseudoephedrine has carcinogenic potential.

Teratogenicity

In rats and rabbits systemic 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.

Fertility

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 Tablets on human fertility.

Lactose monohydrate

Maize starch

Povidone

Magnesium stearate (E572)

Not applicable

3 years

Do not store above 25˚C. Store in original container to protect from moisture and light.

12 tablets in PVC/PVDC Aluminium foil blister packs.

500 tablets in polypropylene containers with polyethylene snap-fitting lids.

Not all pack sizes may be marketed.

No special requirements

McNeil Healthcare (Ireland) Limited,

Airton Road,

Tallaght,

Dublin 24,

Ireland

PA 823/6/3

Date of first authorisation: 01 April 1978

Date of last renewal: 01 April 2008

October 2010