Primalan^® (Syrup) Instructions for Use

Marketing Authorization Holder

Pierre Fabre Medicament Production (France)

ATC Code

R06AD07 (Mequitazine)

Active Substance

Mequitazine (Rec.INN registered by WHO)

Dosage Forms

	Primalan®	Syrup 1.25 mg/2.5 ml: bottle 60 ml 1 pc. in a set with a measuring spoon
		Tablets 5 mg: 14 pcs.
		Tablets 10 mg: 14 pcs.

Dosage Form, Packaging, and Composition

Syrup from colorless to light yellow, with a fruity odor.

Excipients: ascorbic acid, sucrose solution, tangerine essence flavor, methylparaben, propylparaben, water.

60 ml – dark glass type III bottles (1) in a set with a measuring spoon – cardboard packs.

Tablets white-cream (almost white) in color, oval, with a score on one side.

Excipients: lactose, starch, acacia gum, colloidal silicon, talc, sodium carboxymethylcellulose, magnesium stearate.

14 pcs. – blisters (1) – cardboard packs.

Tablets white-cream (almost white) in color, round, with a score on one side.

Excipients: lactose, starch, acacia gum, colloidal silicon, talc, sodium carboxymethylcellulose, magnesium stearate.

14 pcs. – blisters (1) – cardboard packs.

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

H1 histamine receptor blocker

Pharmacological Action

Histamine H₁-receptor blocker, a phenothiazine derivative. It has antiallergic, antipruritic, and anti-edema effects. The anticholinergic effect is weak. Prevents the release from mast cells of biologically active substances that are mediators of allergy and inflammation. Does not have a pronounced effect on the CNS. The action begins within 30 minutes and lasts for 24 hours.

Pharmacokinetics

Absorption is rapid and complete. Food intake does not affect the extent of absorption, but the rate of absorption is somewhat reduced. Time to reach C_max in plasma after a single dose of 5 mg is 3.2 hours, 10 mg is 4 hours; C_max in plasma is 3.26 ng/ml and 6.5 ng/ml, respectively.

It is well distributed in organs and tissues. Does not penetrate the blood-brain barrier. Metabolized in the liver to form active metabolites. T_1/2 of the drug is 18 hours. Excreted as metabolites, mainly in feces, and only a small amount is excreted unchanged by the kidneys.

Indications

Symptomatic treatment of adults and children over 6 years of age:

• Perennial and seasonal allergic rhinitis;
• Acute and chronic recurrent urticaria;
• Allergic conjunctivitis;
• Atopic dermatitis.

ICD codes

Dosage Regimen

Orally, regardless of meals, with water. Adults and children over 12 years – 5 mg 2 times/day, in the morning and evening (before bedtime) or 10 mg once/day (in the evening).

Children from 6 to 12 years: with body weight less than 30 kg (6-10 years) – 2.5 mg 2 times/day (in the morning and evening) or 5 mg once/day (in the evening); with body weight from 30 to 40 kg (10-12 years) – 2.5 mg in the morning and 5 mg in the evening or 7.5 mg (1.5 tab.) once/day (in the evening). When taking the syrup, it should be taken into account that one measuring spoon of syrup (2.5 ml) contains 1.25 mg of the drug. The course of treatment depends on the nature of the disease.

Adverse Reactions

From the digestive system: dry mouth; in rare cases – dyspeptic disorders.

From the CNS: drowsiness (not pronounced and quickly passing), headache, feeling of fatigue, in some cases – mood lability in elderly patients and children.

Adverse reactions occur rarely, are usually mild and transient.

Contraindications

• Angle-closure glaucoma;
• Prostatic hypertrophy;
• Concomitant use of MAO inhibitors;
• Pregnancy;
• Lactation period;
• Children under 6 years of age;
• Hypersensitivity (including to other phenothiazine derivatives);

With caution – hepatic insufficiency (risk of accumulation), elderly age, tendency to constipation, epilepsy.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Use in Hepatic Impairment

With caution – hepatic insufficiency (risk of accumulation).

Pediatric Use

Contraindicated in children under 6 years of age.

Children from 6 to 12 years: with body weight less than 30 kg (6-10 years) – 2.5 mg 2 times/day (in the morning and evening) or 5 mg once/day (in the evening); with body weight from 30 to 40 kg (10-12 years) – 2.5 mg in the morning and 5 mg in the evening or 7.5 mg (1.5 tab.) once/day (in the evening). When taking the syrup, it should be taken into account that one measuring spoon of syrup (2.5 ml) contains 1.25 mg of the drug. The course of treatment depends on the nature of the disease.

Geriatric Use

With caution – elderly age.

Special Precautions

During treatment, it is necessary to refrain from consuming ethanol and from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms (with accidental single ingestion of large doses): intensification of adverse reactions.

Treatment: no specific antidote. Gastric lavage, symptomatic therapy.

Drug Interactions

When taken concomitantly with antihypertensive drugs – enhancement of the hypotensive effect.

Enhances the effect of drugs that depress the CNS (antidepressants with sedative effect, barbiturates, benzodiazepines, clonidine, hypnotics, analgesics, antitussives, and antipsychotic drugs (neuroleptics).

Does not alter the effect of ethanol.

When used concomitantly with atropine and other drugs with anticholinergic action, tricyclic antidepressants of the imipramine type, antiparkinsonian drugs, myotropic antispasmodics, disopyramide, antipsychotic drugs, phenothiazine derivatives, an increase in side effects is possible.

Storage Conditions

Store in a place inaccessible to children at a temperature not exceeding 25°C (77°F), in a light-protected place.

Shelf Life

Shelf life – tablets – 3 years, syrup – 2 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.