Platyphyllinum gidrotartrat-Darnitsa

General characteristics. Structure:

Active ingredient: platyphylline hydrotartrate;

1 ml of solution contains Platyphyllinum of hydrotartrate 2 mg;

excipient: water for injections.

Pharmacological properties:

Pharmacodynamics. Platyphyllinum – the natural alkaloid showing M-holinoblokiruyushchee action. In comparison with atropine exerts smaller impact on peripheral M-holinoretseptory (on spasmolytic action on smooth muscle cells of bodies of digestive tract and a circular muscle of an iris is 5-10 times weaker than atropine). Blocking M-holinoretseptory, breaks transfer of nervous impulses from postganglionic cholinergic nerves on the effector bodies and fabrics (heart, smooth muscle bodies, glands of external secretion) innervated by them. Partially blocks N-holinoretseptory. Holinoblokiruyushchy action is more shown against the background of the raised tone of the parasympathetic autonomic nervous system or action of M-cholinomimetics. To a lesser extent, than atropine, causes tachycardia, especially at use in high doses. Reducing influence of a vagus nerve, improves conductivity of heart, increases excitability of a myocardium, increases the minute volume of heart. Has ganglioblokiruyushchy and direct myotropic spasmolytic effect, causes expansion of small vessels of skin. In high doses the vasomotor center oppresses and blocks sympathetic a ganglion owing to what vessels extend and arterial pressure (mainly – decreases at intravenous administration). More weakly than atropine oppresses secretion of hemadens, causes the expressed decrease in a tone of unstriated muscles, amplitudes and frequencies of peristaltic reductions of a stomach, a duodenum, thin and thick guts, moderate decrease in a tone of a gall bladder (in persons with a hyperkinesia of biliary tract). At a hypokinesia the tone of a gall bladder raises before normal contents. Causes relaxation of smooth muscles of a uterus, bladder and urinary tract. Having spasmolytic effect, eliminates a pain syndrome. Relaxes smooth muscles of bronchial tubes at its spasm caused by increase in a tone of a vagus nerve or cholinomimetics increases breath volume, oppresses secretion of bronchial glands. At parenteral administration causes a mydriasis owing to relaxation of a circular muscle of an iris of the eye. At the same time intraocular pressure increases and there comes accommodation paralysis (relaxation of a ciliary muscle of a ciliary body). In comparison with atropine influence on accommodation is expressed less and well. Excites a brain and a respiratory center, more – a spinal cord (in high doses spasms, oppression of the central nervous system, the vasomotor and respiratory centers are possible). Gets through a blood-brain barrier.

Pharmacokinetics. After parenteral administration quickly and easily gets through gistogematichesky barriers, cellular and synaptic membranes. At introduction of the raised doses collects in the central nervous system in considerable concentration. In an organism is exposed to hydrolysis with formation of a platinetsin and platinetsinovy acid. It is excreted by kidneys with urine and intestines with excrements. At the correct use (doses, intervals between introductions) it does not kumulirutsya.

Pharmaceutical characteristics.

Main physical and chemical properties: transparent colourless liquid.

Incompatibility. Not to mix with other medicines. To use only the recommended solvent.

Indications to use:

As a part of complex therapy: gastroduodenit, functional dyspepsia, a pylorospasm, cholecystitis, a cholelithiasis, intestinal colic, renal colic, bilious colic. Bronchial asthma for the prevention of a bronchospasm, a bronchorrhea. Algodismenorey. Spasm of cerebral arteries. Angiotrofonevroz.

Route of administration and doses:

To adults and children 15 years subcutaneously, for stopping of spastic pains, a long attack of bronchial asthma, a cerebral and peripheral vasomotor spasm – on 1-2 ml of solution 1-2 times a day are more senior. At course treatment 1-2 times a day for 10-15-20 days subcutaneously enter 1-2 ml.

The highest doses for adults: one-time – 10 mg, daily – 30 mg.

One-time and daily doses, frequency to a vvedeniya|vstup | are established individually by the doctor depending on indications and age of the patient.

Features of use:

Use during pregnancy or feeding by a breast.

During pregnancy and feeding by a breast drug is used with care only when the expected advantage for mother exceeds potential risk for a fruit or the child.

Children.

Drug is used to children from 15 years.

With care to apply at patients with a prostatauxe without obstruction of urinary tract, a Down syndrome, cerebral palsy, a reflux esophagitis, hernia of an esophageal opening of the diaphragm which is combined about a reflux esophagitis; nonspecific ulcer colitis, megacolon; at patients with a xerostomia;
at patients of advanced age or the weakened patients, at chronic diseases of lungs without reversible obstruction, at chronic diseases of the lungs proceeding with the insignificant products dense which are difficult separated, phlegms, especially at children of younger age and the weakened patients; at vegetative (autonomous) neuropathy.

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

At use of drug it is necessary to abstain from driving or performance of other potentially dangerous types of activity which require special attention and speed of psychomotor reactions.

Side effects:

Gastrointestinal frustration: dryness in a mouth, thirst, disturbance of flavoring feelings, a dysphagy, reduction of motility of intestines up to an atony, reduction of a tone of biliary tract and a gall bladder.

From kidneys and urinary tract: difficulty and delay of an urination.
Cordial frustration: tachycardia, arrhythmia, including premature ventricular contraction, myocardium ischemia.
Vascular frustration: face reddening, feeling of inflows.

Neurologic frustration: headache, dizziness, nervousness, sleeplessness.
From organs of sight: expansion of pupils, photophobia, accommodation paralysis, increase in intraocular pressure.

From respiratory system and bodies of a mediastinum: reduction of secretory activity and a tone of bronchial tubes that leads to formation of a viscous phlegm that hard clears the throat.
Changes from skin and hypodermic cellulose: skin rash, small tortoiseshell, exfoliative dermatitis.

From immune system: anaphylactic reactions, acute anaphylaxis.

Others: sweating reduction, xeroderma, dysarthtia.

Interaction with other medicines:

At simultaneous use with a haloperidol for patients with schizophrenia decrease in antipsychotic effect is possible.

Strengthens sedative and somnolent effect of phenobarbital, pentobarbital, magnesium of sulfate and an etaminal of sodium. Eliminates bradycardia from verapamil reception; the nausea, vomiting and bradycardia caused morphine.

Blocks effects of a prozerin.

Increases effects H2-gistaminolitikov, appointed inside, digoxin and Riboflavinum (slows down a peristaltics and improves absorption).

Adrenomimetiki and organic nitrates exponentiate increase in pressure in an eye.
M-holinoblokatory, амантадин, a haloperidol, fenotiazina, MAO inhibitors, tricyclic antidepressants, бензактизин, quinidine sulfate, an isoniazid, some antihistaminic drugs (дифенгидрамин), Disopyramidum, новокаинамид increase risk of development of anticholinergic side effects.

Shows antagonism with cholinesterase inhibitors. Not to apply along with antikholinesterazny drugs.

Morphine strengthens the oppressing action on cardiovascular system, MAO inhibitors – positive hrono-and bathmotropic effect, cardiac glycosides – positive bathmotropic action, quinidine, новокаинамид – holinoblokiruyushchy action.
At the pains connected with spasms of smooth muscles, effect of drug is strengthened by analgetics, sedatives, tranquilizers, at vascular spasms – hypotensive and sedatives.

Contraindications:

Hypersensitivity to drug components. Diseases of cardiovascular system at which increase in heart rate can be undesirable: ciliary arrhythmia, tachycardia, chronic heart failure, coronary heart disease, mitral stenosis, heavy arterial hypertension. Acute bleeding. Thyrotoxicosis. Hyper thermal syndrome. The digestive tract diseases which are followed by impassability (a gullet achalasia, a pyloric stenosis, an intestines atony). Glaucoma. Liver and renal failure. gravis myasthenia. Ischuria or predisposition to it. Injury of a brain.

Overdose:

Symptoms: strengthening of manifestations of side reactions, nausea, vomiting, lowering of arterial pressure, excitement, tremor, spasms, sleeplessness, drowsiness, hallucinations, irritability, hyperthermia, oppression of the central nervous system, suppression of activity of the respiratory and vasomotor centers.

Treatment. Gastric lavage, parenteral administration of cholinomimetics and antikholinesterazny means. At a hyperthermia wet rubdowns and antipyretics are shown, at excitement – intravenous administration of thiopental of sodium or hydroxybutyrate of sodium; at a mydriasis – locally in the form of eye drops Phosphacolum, physostigmine, Pilocarpinum. In case of development of an attack of glaucoma immediately in a conjunctival sac dig in 1% Pilocarpinum solution each hour on 2 drops and subcutaneously 3-4 times a day enter 1 ml of 0,05% of solution of a prozerin.

Storage conditions:

Period of validity. 5 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 5 ampoules in a blister strip packaging, on the 2nd blister strip packagings in a pack; on 10 ampoules in a box.