Dimedrol-Darnitsa solution

General characteristics. Structure:

Active ingredient: diphenhydramine;

1 ml of solution contains a difengidramin of a hydrochloride (Dimedrol) of 10 mg;

excipient: water for injections.

Pharmacological properties:

Pharmacodynamics. H1 blocker - histamine receptors of the I generation eliminates the effects of a histamine mediated through this type of receptors. Action on TsNS is caused by blockade of H3 - histamine receptors 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. Renders effect of local anesthesia (at intake there is a short-term numbness of mucous membranes of an oral cavity), blocks holinoretseptor ганглиев (the ABP reduces) 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 EEG 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. Linkng with proteins of plasma – 98-99%. The most part is metabolized in a liver, smaller – is removed in not changed view with urine in 24 hours. The elimination half-life (T1/2) makes 1-4 hours. It is well distributed in an organism, gets through a blood-brain barrier.

It is metabolized mainly in a liver by a hydroxylation and a konjyugirovaniye in glucuronides; products of biotransformation eliminirutsya with urine. It is excreted with milk of mother and can cause sedation in children of chest age. The maximum activity develops in 1 hour, action duration – from 4 to 6 hours.

Pharmaceutical characteristics.

Main physical and chemical properties: transparent colourless liquid.

Incompatibility.

Not to mix with other medicines in one capacity. To use only the recommended solvent.

Indications to use:

Acute anaphylaxis, small tortoiseshell, hay fever, serum disease, hemorrhagic vasculitis (capillary toxicosis), polymorphic exudative erythema, Quincke's edema, pruritic dermatosis, itch, allergic conjunctivitis and the allergic diseases of eyes, allergic reactions connected with reception of medicines, a trochee, Menyer's disease; postoperative vomiting.

Route of administration and doses:

Drug is appointed the adult intramusculary and intravenously kapelno.

Subcutaneously the drug is not administered owing to irritant action.

At intramuscular introduction the single dose makes 10-50 mg (1-5 ml), the maximum single dose – 50 mg (5 ml), the maximum daily dose – 150 mg (15 ml). Intravenously the drug is administered kapelno in a dose of 20-50 mg (2-5 ml) of Dimedrol in 100 ml of 0,9% of solution of sodium of chloride. Duration of treatment depends on the reached effect and portability of drug.

Features of use:

Use during pregnancy or feeding by a breast.

Dimedrol is contraindicated during pregnancy as there are no adequate data on safety and efficiency of its use.

In need of use of drug it is necessary to stop feeding by a breast.
Children.
Drug is not used in pediatric practice.

It is not recommended for hypodermic introduction. As Dimedrol possesses atropinopodobny action, follows with care it apply: to the patients with recent respiratory diseases in the anamnesis (including asthma) raised by intraocular pressure at a hyperthyroidism, diseases of cardiovascular system, arterial hypotension. Can worsen the course of obstructive diseases of a slight, serious illness of cardiovascular system, Ilheus, a state at obstruction of bilious ways. Dimedrol can cause block, and also cause excitement and hallucinations, spasms, especially at overdose. With care apply to patients aged from 60 years and is more senior since development of dizziness, sedation and arterial hypotension is more probable.

With care appoint to patients with abnormal liver functions and kidneys.

During treatment by drug it is necessary to avoid Uv-radiation and the use of ethanol. Patients need to inform the doctor on use of this drug: antiemetic action can complicate diagnosis of appendicitis and recognition of symptoms of overdose by other medicines.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

As Dimedrol has sedative and somnolent effects, during treatment by drug it is necessary to abstain from potentially dangerous types of activity requiring special attention and speed of psychomotor reactions.

Side effects:

From a nervous system and sense bodys: general weakness, fatigue, sedative action, decrease in attention, dizziness, drowsiness, headache, incoordination of movements, reduction in the rate of psychomotor reactions, concern, hypererethism, irritability, nervousness, sleeplessness, euphoria, fear of death, confusion of consciousness, tremor, neuritis, spasms, paresthesias; expansion of pupils, increase in intraocular pressure, vision disorder, diplopia, acute labyrinthitis, sonitus. At patients with local damages of a brain or epilepsy are activated (even at use of low doses of Dimedrol) convulsive categories on EEG and that can provoke an epileptic attack.

From cardiovascular system: arterial hypotension, heart consciousness, tachycardia, premature ventricular contraction.

From system of blood: agranulocytosis, thrombocytopenia, hemolitic anemia.
From a digestive tract: dryness in a mouth, short-term numbness of a mucous membrane of an oral cavity, anorexia, nausea, pain in epigastric area, vomiting, diarrhea, a lock.
From urinogenital system: the frequent and/or complicated urination, an urination delay, early periods.

From respiratory system: a xeromycteria and throats, a nose congestion, a condensation of a secret of bronchial tubes, feeling of compression in a thorax, the complicated breath, an asthma.

From skin and its derivatives: hyperemia, itch, polymorphic rashes, cyanosis of skin and mucous membranes.

Allergic reactions: rashes, urticaria, acute anaphylaxis.

Reactions in an injection site: local necroses at hypodermic and intradermal introduction.

Others: the increased perspiration, a fever, fever, a hyper thermal syndrome, a photosensitization.

Interaction with other medicines:

Dimedrol exponentiates effects of anesthetics, hypnotic drugs, sedatives, narcotic analgetics and local anesthetics. At use with tricyclic antidepressants strengthening of the holinoblokiruyushchy and oppressing action on the central nervous system is possible. Possible risk of development of spasms at use with analeptics. Simultaneous use of MAO inhibitors and Dimedrol can lead to increase in arterial pressure, and also influence the central nervous and respiratory systems. Use of Dimedrol together with hypotensive drugs can strengthen feeling of fatigue. Drug strengthens effect of ethanol, reduces efficiency of Apomorphinum as vomitive at treatment of poisonings. It is not necessary to appoint along with the drugs containing Dimedrol including for topical administration.

Contraindications:

Hypersensitivity to drug. An attack of bronchial asthma, a pheochromocytoma, epilepsy, the inborn extended QT syndrome or long administration of drugs which can prolong a QT interval, closed-angle glaucoma, a prostate hyperplasia, the stenosing peptic ulcers of a stomach and duodenum, a bladder neck stenosis, bradycardia, disturbance of a heart rhythm. Porphyria.

Overdose:

Symptoms: dryness in a mouth, respiratory depression, a resistant mydriasis, face reddening, oppression or excitement of the central nervous system, a depression, confusion of consciousness, a hyperkinesia, spasms, nonsense, tachycardia, arrhythmia. The case of development of a rabdomioliz after Dimedrol overdose is described.

Treatment: a symptomatic and maintenance therapy at careful control of respiratory function and arterial pressure. Intravenous drop administration of plasma substituting liquids, oxygenotherapy. It is not allowed to apply Epinephrinum and analeptics. As the antidote at overdose of diphenhydramine of a hydrochloride can be appointed physostigmine (0,02-0,06 mg/kg of body weight intravenously) several times if anticholinergic symptoms accrue. In cases of overdose of physostigmine administration of atropine is recommended. At development of spasms and symptoms of excitement of TsNS parenterally enter diazepam.

Storage conditions:

Period of validity 4 years. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C. Not to freeze.

Issue conditions:

According to the recipe

Packaging:

On 1 ml in an ampoule, on 10 ampoules in a box; on 5 ampoules in a blister strip packaging, on the 2nd blister strip packagings in a pack.