Ksatinola-nikotinat

General characteristics. Structure:

Active ingredient: 150 mg of Xantinoli nicotinas in 1 ml of solution.

Excipient: water for injections.

Pharmacological properties:

Pharmacodynamics. Vasodilating, antiagregantny and hypolipidemic means.

The mechanism of action is connected with being a part of a molecule of medicine ksantinoly and niacin. The niacin which is contained in a molecule causes emission of prostacyclin from an endothelium that provides vasodilation and antiagregantny effect, substratno stimulates synthesis of nicotinamide adenine dinucleotide (NAD) and OVER phosphate (NADF). Ksantinol – is a weak antagonist of A1 - purine receptors and, blocking them, strengthens effects of niacin: it is broken ADF-zavisimy a way of aggregation of thrombocytes, there is a relaxation of smooth muscle cells of vessels due to blockade of purine receptors on their surface.

Causes expansion of peripheral vessels, reduces their resistance to a blood flow, improves microcirculation, oxygenation and food of fabrics. Strengthens cerebral circulation, activates processes of a fibrinolysis, reduces viscosity of blood, reduces aggregation of thrombocytes.

At prolonged use it is capable to detain progressing of atherosclerosis, to reduce the level of cholesterol and atherogenous lipoproteins, to increase activity of lipoproteinlipase.

The pharmacokinetics of Xantinoli nicotinas is badly studied. After intramuscular introduction it is soaked up quickly and fully. At repeated use of medicine its pharmacokinetics does not change. Cumulation of medicine is not noted.

After introduction is exposed to intensive metabolism in a liver. At patients with an abnormal liver function and kidneys delay of elimination of Xantinoli nicotinas and increase in its bioavailability is noted. The similar situation takes place at elderly persons (60 years are aged more senior), in comparison with young patients.

Indications to use:

* obliterating diseases of vessels of extremities: a Raynaud's disease, a Thrombangiitis obliterans, the obliterating endarteritis obliterating atherosclerosis;

* diabetic angiopatiya of vessels of extremities and retina;

* vascular fibrinferments and embolisms, postromboflebitichesky syndrome;

* trophic ulcers of shins, decubituses, the hardly healing wounds;

* tranzitorny ischemic attacks and other disturbances of cerebral circulation;

* atherosclerosis of coronary vessels, hypercholesterolemia and gipertriglitseridemiya;

* pre-natal and puerperal asphyxia of a fruit;

* migraine, Menyer's syndrome.

Route of administration and doses:

Apply intramusculary and intravenously.

The adult intramusculary enter in a dose 300 - 900 mg (2 – 6 ml of 15% of solution) a day daily, within 2 - 3 weeks.

Intravenously struyno slowly enter, in a dose of 1 - 2 ml of 15% of solution of 1 - 2 times/days, within 5 - 10 days (the patient has to be in horizontal position).

Intravenously kapelno enter with a speed of 40 - 50 of caps/mines, the dose averages 150 – 900 mg. Part 15% with solution to 10 ml in solution of a dextrose of 5% from 200 to 500 ml or in solution of sodium of chloride of 0,9% to 200 ml.

At acute disorders of blood supply of fabrics along with parenteral administration of Xantinoli nicotinas apply inside 300 mg of 3 times/days.

To children appoint at the rate of 5 - 10 mg/kg/days.

Features of use:

With care apply with a labile arterial pressure.

With extra care apply along with hypotensive medicines.

Influence on ability to driving of motor transport and control of mechanisms. With care to apply at drivers of vehicles, and also at the patients who are engaged in potentially dangerous types of activity.

Side effects:

* lowering of arterial pressure;

* passing caumesthesia, reddening of integuments, weakness, dizziness;

* seldom – nausea, diarrhea, anorexia, a gastralgia;

* at prolonged use – disturbance of tolerance to glucose, increase in level of transaminases and an alkaline phosphatase, uric acid in blood serum;

* allergic reactions.

Interaction with other medicines:

At simultaneous use with the medicines having hypotensive effect (beta adrenoblockers, ergot alkaloids, alpha adrenoblockers, sympatholytics, ganglioblokator) with strophanthin perhaps sharp strengthening of their action.

At simultaneous use of Xantinoli nicotinas with medicines of theophylline increase in concentration of theophylline in a blood plasma and increase of risk of its toxic action is observed.

Anticonvulsants (carbamazepine, dipheninum), barbituric medicines accelerate metabolism of Xantinoli nicotinas and reduce its concentration in plasma.

The combined oral contraceptives, makrolidny antibiotics (кларитромицин, erythromycin), medicines of interferon and antifungal means (кетоконазол, флуконазол) change expressiveness of effect of Xantinoli nicotinas, slow down his metabolism and increase concentration of medicine in plasma.

When using Xantinoli nicotinas at the smoking persons of its concentration in a blood plasma below, than at non-smoking patients.

Contraindications:

* acute bleeding;

* hemorrhagic stroke;

* acute myocardial infarction;

* mitral stenosis;

* acute heart failure;

* chronic heart failure in a decompensation stage;

* arterial hypotension;

* a peptic ulcer of a stomach and duodenum in an aggravation phase;

* acute renal failure;

* glaucoma;

* pregnancy (especially I trimester);

* breastfeeding;

* hypersensitivity to Xantinoli nicotinas.

Overdose:

Symptoms of intoxication arise in 4 - 5 h after introduction of Xantinoli nicotinas and proceed for 12 h. In the beginning heat inflows, a hyperemia of an upper half of a trunk, nausea, dizziness, tachycardia, a lowering of arterial pressure are possible; further – temperature increase, excitement, a loss of consciousness, an areflexia, toniko-clonic spasms, vomiting.

The specific antidote does not exist. Measures of the help include the medicine cancellation supporting and the symptomatic therapy directed to elimination of the arisen disturbances, respiratory support, control of level of arterial pressure and stopping of a convulsive syndrome.

Storage conditions:

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

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 15% in ampoules. On 10 ampoules together with a knife for opening of ampoules in a box from a cardboard. On 10 ampoules on 2 ml or on 5 ampoules on 5 ml in the blister packaging from a film polyvinyl chloride. On 1 or 2 blister packagings together with a knife for opening of ampoules and the application instruction or a leaf insert in a pack from a cardboard.