Nicotinic acid - instructions for use, dose, side effects, contraindications

Nicotinic acid is a specific anti-pelagic agent. It has a pronounced short vasodilating effect, improves carbohydrate and nitrogen metabolism, has lipid-lowering activity, reduces the content of total cholesterol, low-density lipoproteins, triglycerides, increases the high-density lipoprotein content, improves microcirculation.

In organism a nicotinic acid turns into nicotinamide , which binds to the coenzymes of codohydrase I and codehydrogen II (NAD and NADP), which carry hydrogen, participates in the metabolism of fats, proteins, amino acids, purines, tissue respiration, glycogenolysis, and synthetic processes.

It replenishes the vitamin PP deficiency (vitamin B3), is a specific anti-pellagra agent.

Has vasodilating effect at the level of small vessels (incl.brain), improves microcirculation, has a weak anticoagulant effect (increases the fibrinolytic activity of the blood).

Pharmacokinetics:

With parenteral administration, it is quickly distributed in the tissues of the body.

It accumulates mainly in the liver, as well as in adipose tissue and in the kidneys.

In the liver a nicotinic acid is converted into an amine that is embedded in nicotiumamidenidine dinucleotide (NAD), which is a prosthetic group of enzymes that carry hydrogen and carry out oxidation-reduction processes. The main metabolites are N-methyl-2-pyridone-3-carboxamide and N-methyl-2-pyridone-5-carboxamide, which do not possess pharmacological activity.

It can be synthesized in the intestine by a bacterial flora from the tryptophan that comes with food (1 mg of nicotinic acid is formed from 60 mg of tryptophan) with the participation of pyridoxine (vitamin B6) and riboflavin (vitamin B2). The elimination half-life is 45 minutes.

It is excreted from the body by the kidneys in unmodified form and in the form of metabolites. Kidney clearance depends on the level of nicotinic acid in the blood plasma and can decrease with a high concentration of it in the plasma.

Indications:

Hypovitaminosis PP, avitaminosis PP (pellagra), spasms of the vessels of the extremities,

in the combination therapy with ischemic stroke, obliterating diseases of the vessels of the extremities (obliterating endarteritis, Raynaud's disease), neuritis of the facial nerve

diabetes mellitus, including its complications (diabetic polyneuropathy, microangiopathy)

Hartnup disease (a hereditary disease, accompanied by a disruption in the assimilation of certain amino acids, including tryptophan).

Contraindications:

Atherosclerosis, hypersensitivity to nicotinic acid, peptic ulcer of the stomach and duodenum (at the stage of exacerbation), gout, hyperuricemia, hepatitis, cirrhosis, decompensated diabetes mellitus.

Carefully:hemorrhage, glaucoma, hyperacid gastritis, peptic ulcer and duodenumishki (outside the stage of exacerbation), arterial hypotension, pregnancy, lactation, children's age.

Dosing and Administration:

When pellagra, adults are prescribed parenterally (intravenously, intramuscularly or subcutaneously) 1 ml of 1% (10 mg) solution 2-3 times a day for 10-15 days.

With ischemic stroke, 10 mg of solution is slowly injected intravenously.

At other indications - on 10 mg 1-2 times a day, within 10-15 days.

Higher doses for adults: single-100 mg, daily - 300 mg.

Disease Hartnup 40-200 mg per day.

Side effects:

After intravenous administration it is rare: allergic reactions (skin rash, itchy skin, breathy breath, hives).

Paresthesia, dizziness, sensation of "tidal" blood to the scalp, hyperemia of the face and upper body, orthostatic hypotension, collapse, sensation of fever, headache. As a rule, these effects disappear on their own. With rapid intravenous administration, a significant reduction in blood pressure, dizziness.

With long-term use - fatty liver disease, hyperuricemia, decreased glucose tolerance, asthenia, increased activity in the blood of aspartate aminotransferase, lactate dehydrogenase, alkaline phosphatase.

Subcutaneous and intramuscular injections are painful.

Overdose:

High doses of nicotinic acid can cause a temporary rush of blood to the head and upper body, itching, and gastrointestinal upsets.

Treatment: symptomatic.

Interaction:

When combined with drugs, sulfonylureas can increase
blood glucose level. When administered with lovastatin increases the risk of myopathy.

Care should be taken when combining with antihypertensive drugs, anticoagulants and ascorbic acid.

Reduces the toxicity of neomycin and prevents the induced decrease in the concentration of high-density cholesterol and lipoproteins.

Special instructions:

To prevent complications from the liver it is recommended to include in the diet products 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, there is no need for use during pregnancy.

Effect on the ability to drive transp. cf. and fur:

Form release / dosage:

Solution for injection 10 mg / ml.

1 ml in ampoules.

5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film. 2 contour squares are placed in a pack of cardboard.

10 ampoules are placed in a box of cardboard with corrugated paper partitions.

In each pack, the box is enclosed with instructions for use, ampoule knife or ampoule scapper (when packing ampoules with a kink ring, point and notch ampoule opener or ampoule scarifier do not put).

Packaging:(1) - ampoule (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packs cardboard

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

Shelf life - 5 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003608 / 01

Date of registration:13.07.2009

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp11.08.2015

Illustrated instructions

Instructions

A nicotinic acid (Nicotinic acid)