Nicotinic acid bufus Renewal solution for injection 1% 1ml ampoules, 10pcs

Composition

>

1 ml of the solution contains:

Active ingredient:

Nicotinic acid -10 mg,

Auxiliary substances:

Sodium bicarbonate,

water for injection.

Pharmacological action

Nicotinic acid is a specific anti-allergic agent. It has a pronounced short-term vasodilating effect, improves carbohydrate and nitrogen metabolism, has hypolipedemic activity, reduces the content of total cholesterol, low-density lipoproteins, improves microcirculation. In the body, nicotinic acid is converted into nicotinamide, which binds to codehydrogen coenzymes I and II (NAD and NADP), which transport hydrogen, participates in the metabolism of fats, proteins, amino acids, purines, tissue respiration, glycogenolysis, and synthetic processes. It makes up for the deficiency of vitamin PP (vitamin B3), is a specific anti-allergic agent (vitamin PP beriberi). Normalizes the concentration of blood lipoproteins. It has a vasodilating effect on the level of small vessels (including the brain), improves microcirculation, has a weak anticoagulant effect (increases the fibrinolytic activity of the blood). Pharmacokinetics When administered parenterally, it is rapidly distributed in the body’s tissues. In the body, it is transformed into nicotinamide. It accumulates mainly in the liver, as well as in adipose tissue and in the kidneys. In the liver, nicotinic acid is converted to an amine, which is incorporated into nicotinamide adenine dinucleotide (NAD), which is a prosthetic group of enzymes that transfer hydrogen and carry out redox processes. It is metabolized in the liver. The main metabolites, N-methyl-2-pyridone-3-carboxamide and N-methyl-2-pyridone-5-carboxamide, have no pharmacological activity. It can be synthesized in the gut by bacterial flora from tryptophan received from food (from 60 mg of tryptophan,1 mg of nicotinic acid is formed) with the participation of pyridoxine (vitamin B6) and riboflavin (vitamin B12). The elimination half-life is 45 minutes. It is excreted by the kidneys in the form of metabolites, with high doses – mainly in unchanged form. Renal clearance depends on the level of nicotinic acid in the blood plasma and may decrease with a high concentration of it in the plasma.

Indications

Hypovitaminosis PP, avitaminosis PP (pellagra). Ischemic disorders of the cerebral circulation, obliterating diseases of the vessels of the extremities (obliterating endarteritis, Raynaud’s disease), spasm of the vessels of the extremities, bile and urinary tracts, neuritis of the facial nerve. Diabetes mellitus, including its complications (diabetic polyneuropathy, microangiopathy. Hartnup’s disease (a hereditary disorder associated with impaired absorption of certain amino acids, including tryptophan).

Use during pregnancy and lactation

Use caution during pregnancy and lactation (taking high doses is contraindicated).

Contraindications

Hypersensitivity, severe arterial hypertension, atherosclerosis, gout, hyperuricemia, childhood. Pregnancy and lactation.

With caution

Hemorrhages, glaucoma, liver failure, hypotension, hyperacid gastritis, peptic ulcer of the stomach and duodenum 12 (in the acute stage).

Side effects

Due to the release of histamine: redness of the skin, including the face and upper half of the trunk with a tingling and burning sensation, a feeling of blood rush to the head, dizziness, hypotension, orthostatic hypotension (with rapid intravenous use), increased secretion of gastric juice, itching, dyspepsia, urticaria. With prolonged use of high doses: diarrhea, anorexia, vomiting, impaired liver function, fatty liver, ulceration of the gastric mucosa, arrhythmia, paresthesia, hyperuricemia, decreased glucose tolerance, hyperglycemia, transient increase in the activity of AST, LDH, alkaline phosphatase, irritation of the gastrointestinal mucosa.

Interaction

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

Reduces the absorption of bile acid sequestrants (an interval of 1.5–2 hours between doses is required) and the hypoglycemic effect of antidiabetic drugs.

Possible interaction with antihypertensive agents, acetylsalicylic acid, anticoagulants.

How to take, course of use and dosage

When pellagra is prescribed to adults parenterally (subcutaneously, intramuscularly, intravenously (slowly) – 10 mg (1% solution 1 ml) 2-3 times a day, for 10-15 days. In case of ischemic stroke,10 mg of the solution is slowly administered 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’s disease 40-200 mg per day.

Overdose

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

Special instructions

Liver function should be monitored during treatment. To prevent liver complications, it is recommended to include foods rich in methionine (cottage cheese) in the diet, or use methionine, lipoic acid, and other lipotropic drugs. Taking into account the injectable route of use of the drug, side effects, there is no need for use during pregnancy.

Form of production

Solution for injection

Storage conditions

In a dark place, at a temperature not exceeding 25 °C

Shelf life

5 years

Active ingredient

Nicotinic acid

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Indications

Hypovitaminosis, Hepatitis, Cerebrovascular accident, Diabetic Nephropathy, Vascular damage in diabetes mellitus, Neuritis, Raynaud ‘s disease