Niacin Bufus

General characteristics. Structure:

Active ingredient: 10 mg of niacin.

Excipients: Natrii hydrocarbonas, water for injections.

Pharmacological properties:

Pharmacodynamics. Niacin is specific antipellagric means. Has the expressed short vasodilating effect, improves a carbohydrate and nitrogen metabolism, has hypolipidemic activity, reduces the content of the general cholesterol, lipoproteids of low density, improves microcirculation.

In an organism niacin turns into niacinamide which contacts the coenzymes of a kodegidrogen of I and II (NAD and NADF) transferring hydrogen participates in metabolism of fats, proteins, amino acids, purines, tissue respiration, a glycogenolysis, synthetic processes. Fills shortage of RR vitamin (B3 vitamin), is specific antipellagric means (RR vitamin avitaminosis).

Normalizes concentration of lipoproteins of blood.

Has vazodilatiruyushchy effect at the level of small vessels (including a brain), improves microcirculation, has weak anticoagulating effect (increases fibrinolitic activity of blood).

Pharmacokinetics. At parentalny introduction it is quickly distributed in body tissues. In an organism it is transformed to niacinamide. Collects generally in a liver, and also in fatty tissue and in kidneys. In a liver niacin turns into amine which is built in the nicotinamide adenine dinucleotide (NAD) which is prosthetic group of the enzymes which are transferring hydrogen and carrying out oxidation-reduction processes.

It is metabolized in a liver. The main metabolites – N-methyl-2-pyridone-3-karboksamid and N-methyl-2-pyridone-5-karboksamid have no pharmacological activity.

It can be synthesized in intestines by a bacterial flora from the tryptophane which arrived with food (1 mg of niacin is formed of 60 mg of tryptophane) with the participation of a pyridoxine (B6 vitamin) and Riboflavinum (B12 vitamin). An elimination half-life – 45 minutes.

It is removed by kidneys in the form of metabolites, at reception of high doses – it is preferential in an invariable look. The renal clearance depends on niacin level in a blood plasma and can decrease at its high concentration in plasma.

Indications to use:

RR hypovitaminosis, avitaminosis of RR (pellagra). The ischemic disturbances of cerebral circulation obliterating diseases of vessels of extremities (an obliterating endarteritis, a Raynaud's disease), a vasospasm of extremities, zhelche-and urinary tract, neuritis of a facial nerve. Diabetes mellitus, including its complications (diabetic polyneuropathy, mikroangiopatiya. Hartnup's disease (the hereditary disease which is followed by disturbance of digestion of some amino acids, including tryptophane).

Route of administration and doses:

At a pellagra appoint the adult parenterally (subcutaneously, intramusculary, intravenously (slowly) – 10 mg (1% solution on 1 ml) 2-3 times a day, within 10-15 days.

At an ischemic stroke intravenously slowly enter 10 mg of solution.

At other indications – on 10 mg 1-2 times a day, within 10-15 days. The highest doses for adults: one-time – 0,1 g, daily – 0,3 g.

Hartnup's disease of 40-200 mg a day.

Features of use:

In the course of treatment it is necessary to control function of a liver. For the prevention of complications from a liver it is recommended to include in a diet the products rich with methionine (cottage cheese), or to use methionine, lipoic acid, etc. lipotropic HP.

In view of an injection way of administration of drug, by-effects, there is no need for use during pregnancy.

Side effects:

Allergic reactions (skin rash, skin itch, stidor breath, small tortoiseshell).

After intravenous bystry administration: orthostatic hypotension, collapse.

Dermahemia of the person and an upper half of a trunk, paresthesia, dizziness, "inflows" of blood to face skin, a headache, dizziness.

Local reactions: morbidity in places of hypodermic and intramuscular introduction.

Interaction with other medicines:

At combined use with drugs of sulphonylurea can increase glucose level in blood.

It is necessary to be careful at a combination with hypotensive HP, anticoagulants and ascorbic acid.

Reduces toxicity of Neomycinum and prevents the reduction of concentration of cholesterol and lipoproteins of high density induced by it.

Contraindications:

Hypersensitivity, the expressed arterial hypertension, atherosclerosis, gout, hyperuricemia, children's age. Pregnancy, lactation period.

With care. Hemorrhages, glaucoma, a liver failure, arterial hypotension, hyperacid gastritis, a peptic ulcer of a stomach and a 12-perstny gut (in an aggravation stage).

Overdose:

High doses of niacin can cause temporary rush of blood to the head and an upper half of a trunk, an itch, gastrointestinal frustration. Treatment: symptomatic.

Storage conditions:

List B. In the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 5 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 10 mg/ml. On 1 ml in ampoules of neutral glass or in ampoules polymeric of polyethylene of high pressure, or from polyethylene of low pressure, or from polyethylene for the medical purposes, or from polyethylene or polypropylene for infusion solutions and injection drugs. On ampoules paste labels.

On 10 ampoules of neutral glass with the application instruction place in a box from a cardboard with a corrugated insert from paper. Put a knife in each box ampoule or the scarificator. When packaging ampoules with notches, rings and points ampoule or scarificators do not put knives. The box is pasted over with the label parcel post. On 10 ampoules polymeric with the application instruction place in a pack from a cardboard.