Clemastinum

General characteristics. Structure:

Active ingredient: 1 mg of Clemastinum in 1 ml of solution.

The drug rendering antiallergic, antipruritic, anti-exudative, antihistaminic action.

Pharmacological properties:

Pharmacodynamics. Blocks histamine H1 receptors. Prevents development of a vazodilatation and reduction of the unstriated muscles induced by a histamine. Reduces permeability of capillaries, brakes exudation and formation of hypostasis, reduces an itch. Blocks holinoretseptor in TsNS and peripheral fabrics, has moderate sedative effect, shows mestnoanesteziruyushchy activity.

According to results of pilot studies has no cancerogenic, mutagen and teratogenic effect. At the dose, by 312 times exceeding the recommended therapeutic dose for adults adversely influences fertility of rats.

Pharmacokinetics. After intake it is soaked up almost completely. Cmax  in a blood plasma is reached during 2–4 h, the maximum effect develops in 5–7 h. Linkng with proteins of plasma makes 90–95%. Passes through GEB, gets into breast milk. It is metabolized in a liver. It is removed in 2 phases: T1/2  of the first phase — 3,6 ± 0,9 h, the second — 37 ± 16 h. It is excreted with urine, it is preferential in the form of metabolites (45–65%). Duration of action makes 8–12 h (in certain cases to 24 h).

Indications to use:

For intake: a small tortoiseshell, a serum disease, a hemorrhagic vasculitis, rhinitis (allergic, vasculomotor), a pollinosis, a skin itch, a pruritic dermatosis, contact dermatitis, eczema (acute, chronic), the acute iridocyclitis, a medicinal dieback, allergic reactions caused by stings of insects.

For parenteral use: Quincke's disease, acute or anaphylactoid anaphylaxis (complex therapy), prevention of allergic and pseudo-allergic manifestations (use of X-ray contrast means, hemotransfusion, introduction of a histamine).

Route of administration and doses:

Inside (to food) adults and children are later 12 years old — 1 mg (tablet) or 20 ml (1,5 tablespoons of syrup) 2 times a day (in the morning and in the evening), if necessary to 6 mg or 120 ml of syrup a day; to children at the age of 6–12 years — 0,5–1 mg 2 times a day. Syrup: to children of 1-3 years — 1–2 h a spoon, 4–6 years — on 2 h a spoon, 7–12 — 1 tablespoon. Parenterally: the adult in/in (slowly) or 2 mg in oil 2 times a day to children — in oil 25 mkg/kg/days in a dose in 2 receptions.

Features of use:

Use at pregnancy and feeding by a breast. Contraindicated at pregnancy. Category of action on a fruit on FDA — B. For the period of treatment it is necessary to stop breastfeeding.

With care to appoint to patients with a hyperthyroidism and diseases of cardiovascular system, including arterial hypertension. For treatment it is necessary to refuse alcohol intake. Careful observation of children and patients of advanced age is necessary (hypersensitivity to antihistaminic drugs). In an initiation of treatment drivers of vehicles and people whose profession is connected with the increased concentration of attention should not apply in operating time; further — extent of restriction is defined by individual portability of drug.

Special instructions. It is necessary to exclude an opportunity in / and introductions. Ampoule solution contains ethanol. For prevention of distortion of results of skin scarifying tests on allergens, drug it is necessary to cancel for 72 h before allergological testing.

Side effects:

From a nervous system and sense bodys: sedation, weakness, feeling of fatigue, block, a headache, dizziness, drowsiness, a lack of coordination of movements, it is rare — a promoting effect (usually at children): concern, acrimony, excitement, nervousness, sleeplessness, hysteria, euphoria, tremor, spasms; paresthesia, neuritis, sight misting, diplopia, acute labyrinthitis, sonitus.

From bodies of a GIT: nausea, dryness in a mouth, gastric discomfort, it is rare — pain in epigastriums, a lock, in some cases — anorexia, vomiting, diarrhea.

From respiratory system: a condensation of a bronchial secret and difficulty of an otkhozhdeniye of a phlegm, feeling of pressure in a thorax, breath disturbance, a nose congestion.

From cardiovascular system: hypotension (is more often at elderly people), heartbeat, tachycardia, premature ventricular contraction; hemolitic anemia, thrombocytopenia, agranulocytosis.

From urinogenital system: very seldom — difficulty of department of urine, an ischuria, increase of an urination, change of menstrual function.

Allergic reactions: very seldom — urticaria, skin rash, at in introduction — an asthma, a bronchospasm, an acute anaphylaxis.

Others: photosensitization.

Interaction with other medicines:

Exponentiates action of neuroleptics, alcohol, sedative, somnolent, narcotic and other drugs, the oppressing TsNS, effect of holinoblokator. It is incompatible with MAO inhibitors (extend and strengthen cholinolytic action).

Contraindications:

Hypersensitivity, children's age till 1 year (syrup and injections) or up to 6 years (tablet), pregnancy, feeding by a breast.

Restrictions to use. Closed-angle glaucoma, the stenosing stomach ulcer, the obstructive phenomena in peloric and duodenal departments of a GIT or in a bladder neck, the prostatauxe which is followed by disturbances of an urination.

Overdose:

Symptoms: Children have a mydriasis, lack of reaction of pupils to light, dryness in a mouth, face reddening, fever, cyanosis, excitement, hallucinations, an incoordination of movements, an ataxy, an athetosis, a tremor, a hyperreflexia, toniko-clonic spasms, a depression, oppression of cordial activity and breath (the lethal outcome is possible). Adults have an oppression TsNS, drowsiness, a collapse, spasms, a coma.

Treatment: Induction of vomiting, purpose of salt laxatives (at intake); symptomatic and maintenance therapy: at fever at children it is possible to use the cooling rubdown, in case of hypotension — administration of vasoconstrictive drugs, for stopping of spasms — diazepam or short-range barbiturates, if necessary — physostigmine, IVL; monitoring of the vital functions.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 0,1%, on 2 ml in each ampoule. On 5 or on 10 ampoules, together with the application instruction in cardboard packaging.