Nicotinic acid bufus, 1% 1 ml 10 pcs

Nicotinic acid is a specific antipellagic agent. It has a pronounced short-term vasodilating effect, improves carbohydrate and nitrogen metabolism, has hypolipidemic activity, reduces total cholesterol, low-density lipoproteins, improves microcirculation.

In the body nicotinic acid is converted to nicotinamide, which binds to codohydrogen coenzymes I and II (NAD and NADPH), carrying hydrogen, is involved in the metabolism of fats, proteins, amino acids, purines, tissue respiration, glycogenolysis, synthetic processes. It compensates for the lack of vitamin PP (vitamin B3), is a specific antipellagic agent (vitamin PP avitaminosis).

Normalizes the concentration of blood lipoproteins.

It has a vasodilator effect at the level of small vessels (including brain).It also improves microcirculation and slightly anticoagulant effect (increases blood fibrinolytic activity).

Pharmacokinetics

During parenteral administration the drug is quickly distributed in body tissues. In body it is transformed into nicotinamide. It accumulates mainly in liver as well as in adipose tissue and kidneys. In the liver nicotinic acid is converted into amine, which is incorporated into nicotinamide adenine dinucleotide (NAD), which is a prosthetic group of enzymes that carry hydrogen and carry out redox processes.

Metabolized in the liver. Main metabolites are N-methyl-2-pyridone-3-carboxamide and N-methyl-2-pyridone-5-carboxamide have no pharmacological activity.

It can be synthesized in the intestine by bacterial flora from ingested tryptophan (from 60 mg of tryptophan 1 mg of nicotinic acid is formed) with the participation of pyridoxine (vitamin B6) and riboflavin (vitamin B12). Elimination half-life is 45 minutes.

It is excreted by kidneys as metabolites, at high doses – mainly unchanged. Renal clearance depends on the level of nicotinic acid in plasma and may decrease at high plasma concentrations.

Indications

Hepatitis, Raynaud’s disease, Neuritis, Hypovitaminosis, Impaired cerebral circulation, Diabetic nephropathy, Vascular lesions in diabetes, RR hypovitaminosis, RR avitaminosis (pellagra).

Ischemic cerebral circulatory disorders, obliterating vascular diseases of the extremities (obliterating endarteritis, Raynaud’s disease), vasospasm of the extremities, biliary and urinary tract, facial neuritis.

Diabetes mellitus, including its complications (diabetic polyneuropathy, microangiopathy.

Hartnup disease (hereditary disease accompanied by impaired absorption of certain amino acids, including tryptophan).

Composition

1 ml of the solution contains:

The active ingredient:

Nicotinic acid -10 mg,

Excipients:

Sodium bicarbonate,

water for injection.

How to take, the dosage

In case of pellagra in adults parenterally (subcutaneously, intramuscularly, intravenously (slowly) – 10 mg (1% solution in 1 ml) 2-3 times a day for 10-15 days.

In case of ischemic stroke 10 mg of solution is slowly injected intravenously.

For other indications – 10 mg 1-2 times a day for 10-15 days. The highest doses for adults: single – 0.1 g, daily – 0.3 g.

Hartnup disease 40-200 mg per day.

Interaction

Potentiates the effect of fibrinolytic agents, antispasmodics and cardiac glycosides, the toxic effects of alcohol on the liver.

Limits absorption of bile acid sequestrants (an interval of 1.5-2 hours between doses is necessary) and hypoglycemic effect of antidiabetic drugs.

Possible interaction with hypotensive agents, acetylsalicylic acid, anticoagulants.

Special Instructions

During treatment it is necessary to monitor liver function.

To prevent liver complications it is recommended to include in the diet foods rich in methionine (cottage cheese), or use methionine, lipoic acid and other lipotropic drugs.

Taking into account the injection route of the drug, side effects, it is not necessary for use during pregnancy.

Contraindications

Hypersensitivity, marked arterial hypertension, atherosclerosis, gout, hyperuricemia, childhood. Pregnancy, lactation.

With caution

Hemorrhage, glaucoma, hepatic insufficiency, arterial hypotension, hyperacid gastritis, peptic ulcer (acute stage).

Overdose

High doses of nicotinic acid may cause temporary blood rush to the head and upper torso, itching, gastrointestinal disorders. Treatment: symptomatic.

Pregnancy use

With caution in pregnancy and lactation (high doses are contraindicated).