Papaverine gidrokhlorid-Darnitsa

General characteristics. Structure:

Active ingredient: papaverine; 1 ml of solution contains 20 mg of a papaverine of a hydrochloride in terms of 100% dry matter; excipients: dinatrium эдетат, DL methionine, water for injections.

Pharmacological properties:

Pharmacodynamics. A papaverine – the alkaloid which is contained in opium. The papaverine is a myotropic antispasmodic. It lowers a tone, reduces sokratitelny activity of unstriated muscles and causes in this regard vasodilating and spasmolytic action. The papaverine is inhibitor of enzyme of the fosfordiesteraza causing intracellular accumulation cyclic 3 adenosinemonophosphates (tsAMF). Accumulation of tsAMF leads to disturbance of contractility of unstriated muscles and their relaxation at spastic states. Effect of drug on the central nervous system is expressed poorly, only in the raised doses he shows some sedation.

Pharmacokinetics. At parenteral administration drug quickly forms strong complexes with blood serum albumine. Easily gets through gistogematichesky barriers. It is metabolized in a liver. About 60% are allocated in the form of connections, mainly, phenolic, with glucuronic acid and only in a small amount in not changed look. An elimination half-life (T1/2) – 1-3 hours.

Pharmaceutical characteristics.
Main physical and chemical properties: transparent slightly yellowish liquid.

Incompatibility. Pharmaceutical we will combine with Dibazolum, it is chemically incompatible about caffeine-sodium benzoate. To use only the recommended solvent.

Indications to use:

– Spasms of unstriated muscles of abdominal organs (pylorospasm, spastic colitis, cholecystitis, cholelithiasis attacks);
– spasms of urinary tract, renal colic;
– spasm of brain vessels;
– the spasm of coronary vessels (connected, for example, with an acute myocardial infarction, stenocardia);
– spasms of peripheral vessels (endarteritis).

Route of administration and doses:

Drug is used subcutaneously, intramusculary and intravenously.
Subcutaneously and intramusculary enter to adults and children aged from 14 years on 0,5-2 ml (10-40 mg) of 2% of solution, and intravenously enter very slowly, with a speed of 3-5 ml/min., having dissolved 1 ml of 2% hydrochloride papaverine solution (20 mg) in 10-20 ml of 0,9% of solution of sodium of chloride. The most effectively intravenous administration. For patients of advanced age the single dose in an initiation of treatment should not exceed 10 mg (0,5 ml of 2% of solution). The maximum doses for adults at hypodermic or intramuscular introduction: one-time – 100 mg (5 ml of 2% of solution), daily – 300 mg (15 ml of 2% of solution); at intravenous administration: one-time – 20 mg (1 ml of 2% of solution), daily – 120 mg (6 ml of 2% of solution).
To children aged from 1 year up to 14 years drug is used by 2-3 times a day. The single dose makes 0,7-1 mg/kg of body weight.
The maximum daily dose for children makes (irrespective of a way of introduction): at the age of 1-2 years – 20 mg (1 ml of 2% of solution), 3-4 years – 30 mg (1,5 ml of 2% of solution), 5-6 years – 40 mg (2 ml of 2% of solution), 7-9 years – 60 mg (3 ml of 2% of solution), 10-14 years – 100 mg (5 ml of 2% of solution).

Features of use:

Use during pregnancy or feeding by a breast.
During pregnancy or feeding by a breast safety and efficiency of use of drug are not established.

Children.
Drug is used to children aged 1 years are more senior.
With care and in doses below, than sredneterapevtichesky, it is necessary to appoint drug:
– to the elderly and weakened patients;
– the patient with a craniocereberal injury;
– the patient with a chronic renal failure;
– the patient with supraventricular tachycardia, heavy heart failure with the decompensation phenomena;
– at insufficiency of function of adrenal glands, a hypothyroidism, a prostate hyperplasia, depressed cases.
Intravenously the drug should be administered very slowly and under control of arterial pressure, heart rate, the electrocardiogram.
With care it is necessary to appoint intravenous injections of drug at the stenosing coronarosclerosis.
At elderly people emergence of a hyperemia is possible.
Smoking worsens efficiency of drug.
During use of drug it is necessary to exclude alcohol intake.

Ability to influence speed of response at control of motor transport or work with other mechanisms.
During treatment by drug it is necessary to abstain from control of motor transport or work with other difficult mechanisms.

Side effects:

From the central and peripheral nervous system: drowsiness, the increased perspiration, weakness, a headache, dizziness.
From sense bodys: vision disorder, diplopia.
From digestive tract: anorexia, nausea, a lock, dryness in an oral cavity, diarrhea.
From a liver and biliary tract: increase in activity of hepatic transaminases.
From cardiovascular system: arrhythmias, tachycardia, arterial hypotension, partial or total atrioventricular block, asystolia, ventricular premature ventricular contraction, trembling of ventricles, collapse.
From system of blood: eosinophilia.
From a respiratory organs: apnoea.
Dermatological disturbances: dermahemia of an upper part of a trunk, person and hands; itch; rash on skin, a small tortoiseshell.
Allergic reactions: hypersensitivity reactions.
Another: reactions in an injection site.

Interaction with other medicines:

At simultaneous use with cardiac glycosides the expressed strengthening of sokratitelny function of a myocardium owing to reduction of the general peripheric resistance of vessels is observed.
Methyldopum, the levodopa, dopegit – efficiency of these drugs decreases.
Anti-hypertensive means – the anti-hypertensive effect amplifies.
Drugs, the oppressing TsNS – at simultaneous use toxicity of these drugs increases.

Contraindications:

Hypersensitivity to drug components, arterial hypotension, disturbance of atrioventricular conductivity, coma, respiratory depression, a concomitant use of monoamine oxidase inhibitors; glaucoma, a liver failure, children's age till 1 year.

Overdose:

Symptoms: a vision disorder, a diplopia, weakness, dryness in an oral cavity, a lock, erubescence of an upper part of a trunk, a hyperventilation, a nystagmus, an ataxy, tachycardia, arterial hypotension, an asystolia, trembling of ventricles, a collapse. At use of high doses of drug and its bystry introduction to a vein development of arrhythmias or a total atrioventricular block is possible.
Treatment. To stop drug use. Symptomatic treatment. There is no specific antidote.

Storage conditions:

Period of validity. 3 years. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 2 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.