Dimedrol

General characteristics. Structure:

Active ingredient: 0,01 g of a difengidramin of a hydrochloride in 1 ml of solution.

Excipient: water for injections.

Pharmacological properties:

Pharmacodynamics. The blocker of H1-gistaminoretseptorov of the I generation, eliminates the effects of a histamine mediated through this type of receptors. Action on the central nervous system (CNS) is caused by blockade of H3-gistaminoretseptorov of a brain and oppression of the central cholinergic structures. Has the expressed antihistaminic activity, reduces or warns the spasms of smooth muscles, increase in permeability of capillaries, hypostasis of fabrics, an itch and a hyperemia caused by a histamine. Causes local anesthesia (at intake there is a short-term numbness of mucous membranes of an oral cavity), blocks holinoretseptor vegetative ганглиев (reduces the arterial pressure (AP)) and TsNS, renders sedative, somnolent, protivoparkinsonichesky and antiemetic effects.

Antagonism with a histamine is shown more in relation to local vascular reactions at an inflammation and an allergy, than to system, i.e. to decrease in the ABP. However at parenteral administration to patients with deficit of volume of the circulating blood decrease in the ABP and strengthening of the available hypotonia owing to ganglioblokiruyushchy action is possible. At people with local injuries of a brain and epilepsy activates (even in low doses) epileptic categories on an encephalography and can provoke an epileptic attack. It is more effective at the bronchospasm caused by histamine liberator (tubocurarine, morphine), and to a lesser extent - at a bronchospasm of the allergic nature. Sedative and somnolent effects are more expressed at repeated receptions.

Pharmacokinetics. Bioavailability – 50%. TCmax - 20-40 min. (in the greatest concentration is defined in lungs, a spleen, kidneys, a liver, a brain and muscles). Communication with proteins of plasma – 98–99%. Gets through a blood-brain barrier.

It is metabolized mainly in a liver, partially - in lungs and kidneys. It is brought out of fabrics through the 6th p. T1/2 – 4-10 h During the day are completely brought by kidneys in the form of the metabolites conjugated with glucuronic acid. Essential quantities are removed with milk and can cause sedation in the children who are on breastfeeding (the paradoxical reaction which is characterized by hyperexcitability can be observed).

Indications to use:

• Allergic reactions (urticaria, hay fever, Quincke's disease, capillary toxicosis), allergic conjunctivitis, acute iridocyclitis, vasculomotor rhinitis, rhinosinusopathy, allergic dermatitis, pruritic dermatosis.
• As a part of a combination therapy for treatment of a peptic ulcer of a stomach and a 12-perstny gut, hyperacid gastritis.
• Parkinsonism, chorea, sleeplessness.
• Vomiting of pregnant women, Menyer's syndrome, sea and aeroembolism, radial illness.
• Extensive traumatic injuries of skin and soft tissues (burns, crushes), hemorrhagic vasculitis, serum disease.
• Premedication.

Route of administration and doses:

Intramusculary 10 50 mg. The highest single dose р 50 mg, daily 150 mg.

Features of use:

With care use at patients with the hyperthyroidism raised by the intraocular pressure, diseases of cardiovascular system at advanced age. During treatment it is necessary to avoid the use of alcoholic beverages and UF-radiation.

It is necessary to inform the doctor on use of this drug: antiemetic action can complicate diagnosis of appendicitis and recognition of symptoms of overdose of other medicines.

The persons accepting medicine should not be engaged in potentially dangerous types of activity requiring special attention and bystry mental reactions.

Side effects:

Drowsiness, dryness in a mouth, numbness of a mucous membrane of an oral cavity

dizziness, tremor, nausea, headache, adynamy, reduction in the rate of psychomotor reaction, photosensitization, paralysis of accommodation, lack of coordination of movements. At children perhaps paradoxical development of sleeplessness, irritability and euphoria.

Interaction with other medicines:

Strengthens effect of ethanol and HP, the oppressing TsNS.

Monoamine oxidase inhibitors increase anticholinergic activity of a difengidramin.

Antagonistic interaction is noted at joint appointment with psychostimulants.

Reduces efficiency of Apomorphinum as emetic HP at treatment of poisoning.

Strengthens anticholinergic effects of HP with M-holinoblokiruyushchey activity.

Contraindications:

Hypersensitivity, feeding by a breast, children's age (the period of a neonatality and a condition of prematurity), closed-angle glaucoma, a prostatauxe, the stenosing stomach ulcer and a duodenum, piloroduodenalny obstruction, a bladder neck stenosis, pregnancy, bronchial asthma.

Overdose:

Symptoms: oppression of TsNS, excitement development (especially at children) or depressions, expansion of pupils, dryness in a mouth, paresis of bodies of digestive tract.

Treatment: there is no specific antidote, a gastric lavage, if necessary - the HP raising the ABP, oxygen in/in administration of plasma substituting liquids. It is impossible to use Epinephrinum and analeptics.

Storage conditions:

List B. In the place protected from light, at a temperature not over 25 ºС. To store in unavailable to children the place. A period of validity - 3 years. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 1% in ampoules on 1 ml.