Nicotinic Acid

Pharmacological properties

Nicotinic acid (vitamin PP), alone or as an amide, is a prosthetic group of enzymes - codehydrase i (diphosphopyridine nucleotide - above) and codehydrase ii (triphosphopyridine nucleotide - nadf), which carry out hydrogen transfer in redox reactions, as well as phosphate transfer.

Participating in the metabolism, tissue respiration, synthesis processes, nicotinic acid normalizes the content of lipoproteins and triglycerides in the blood.

It has a vasodilating effect at the level of prearteriol and arterioles (including the brain), resulting in improved microcirculation.

It has a weak anticoagulant effect (increases the fibrinolytic activity of the blood), has detoxification properties due to increased detoxification function of the liver and kidneys.

Eliminates a deficiency of vitamin PP, is a specific antipellagric remedy.

Pharmacokinetics Niacin is rapidly absorbed from the injection site with parenteral administration. Evenly distributed over all organs and tissues. It is inactivated mainly by methylation and to a lesser extent by conjugation. Biotransformation products are excreted in the urine. Niacin can be detected in urine in an active form if an increased amount enters the body.

Indications

Treatment of pellagra (vitamin pp vitamin deficiency). ischemic cerebrovascular accident. spasm of limb vessels (obliterating endarteritis, Raynauds disease). spasm of the vessels of the kidneys. wounds, ulcers that do not heal for a long time. complications of diabetes mellitus (diabetic polyneuropathy, microangiopathy). hypoacid gastritis, enterocolitis, colitis. liver diseases (acute and chronic hepatitis). neuritis of the facial nerve. intoxication of various origins: professional, alcoholic, medication (aniline derivatives, barbiturates, anti-TB drugs, sulfonamides).

Application

Assign to adults and children over the age of 15 years intravenously (slowly), intravenously and s / c (intravenous and s / c injections are painful).

For iv injection, a single dose of the drug should be diluted in 10 ml of 0.9% sodium chloride solution and administered in at least 5 minutes (no more than 2 mg of nicotinic acid in 1 minute).

For iv drip administration, a single dose of the drug should be diluted in 100–200 ml of 0.9% sodium chloride solution; the rate of administration is 30–40 drops per minute.

Pellagra. Assign in / in or in / m at 10 mg (1 ml) 1-2 times a day. The course of treatment is 10-15 days.

Ischemic cerebrovascular accident. In / in (slowly) inject 10 mg (1 ml).

Other indications. Prescribe s / c or i / m at 10 mg (1 ml) 1 time per day for 10-15 days. It is possible to add to the infusion solution 10 mg (1 ml) of nicotinic acid per 100-200 ml of solution.

Higher doses for iv administration: single - 100 mg (10 ml), daily - 300 mg (30 ml).

Contraindications

Hypersensitivity to the components of the drug. peptic ulcer of the stomach and duodenum (in the acute stage), gout, hyperuricemia, severe liver failure (including cirrhosis), severe forms of ag and atherosclerosis (iv), decompensated diabetes mellitus, recent myocardial infarction, sudden decrease in peripheral vascular history of resistance.

Side effects

From the cardiovascular system: flushing, which may be accompanied by shortness of breath, tachycardia, palpitations, sweating, chills, swelling, tingling and burning sensations; arrhythmia; with rapid iv administration - a significant decrease in hell, orthostatic hypotension, collapse.

From the central and peripheral nervous system: dizziness, paresthesia, headache.

On the part of the immune system, skin and subcutaneous tissue: hyperemia of the skin of the face and upper body with a sensation of tingling and burning sensation, dry skin and mucous membranes of the eyes, rarely - retinal edema, very rarely in patients with coronary artery disease - acanthosis. These symptoms are unstable and disappear after discontinuation of the drug. Hypersensitivity reactions, including those from the respiratory system, urticaria, pruritus, rash.

Local reactions: pain, swelling at the site of SC and / m injection.

With prolonged use in high doses - hyperuricemia, decreased glucose tolerance, impaired liver function, fatty liver, jaundice, increased levels of AcAT, LDH, alkaline phosphatase, uric acid, hypophosphatemia, decreased platelet count, increased prothrombin time, hyperpigmentation, hyperkeratosis, convulsions , diarrhea, nausea, vomiting, anorexia, exacerbation of stomach ulcers, amblyopia, insomnia, myalgia, decreased blood pressure, rhinitis, blurred vision, swelling of the eyelids, myopathy, exfoliative dermatitis.

special instructions

Since prolonged use can lead to fatty liver, to prevent the latter, methionine-rich foods should be included in the diet of patients or methionine, lipoic acid, should be prescribed. during treatment it is necessary to control liver function. when hypersensitivity to the drug appears (except when used as a vasodilator), it can be replaced with nicotinamide.

Use with caution in case of hyperacid gastritis, gastric and duodenal ulcer (outside the stage of exacerbation), hemorrhages, glaucoma, renal failure, moderate arterial hypotension, alcohol abuse, unstable angina (in patients taking nitrates, calcium channel antagonists, β-adrenore blockers )

The use of the drug can lead to an increase in the need for insulin in patients with diabetes mellitus. It is inappropriate to use for the correction of dyslipidemia in patients with diabetes mellitus.

It is necessary to regularly monitor the level of glucose in connection with a possible decrease in glucose tolerance, as well as the level of uric acid in blood plasma due to a possible increase as a result of prolonged therapy.

Use during pregnancy and lactation. The drug is contraindicated during pregnancy. If necessary, the use of the drug should stop breast-feeding.

Children. The drug is prescribed for children over the age of 15 years.

The ability to influence the reaction rate when driving vehicles or other mechanisms. Studies on the effect of the drug on the reaction rate have not been conducted, however, if dizziness and drowsiness are observed during treatment, one should refrain from working with mechanisms.

Interactions

Oral contraceptives and isoniazid reduce the conversion of tryptophan to nicotinic acid and thus may increase the need for nicotinic acid.

Niacin reduces the effectiveness and toxicity of probenecid, neomycin, barbiturates, anti-TB drugs, sulfonamides.

Antibiotics can increase redness caused by nicotinic acid.

Acetylsalicylic acid reduces the effect of redness of the skin that occurs under the influence of nicotinic acid.

Ciprofibrate is not recommended to be combined with nicotinic acid.

Lovastatin, pravastatin due to an increased risk of adverse reactions is not recommended to be combined with nicotinic acid. There are reports of rhabdomyolysis when using nicotinic acid with lovastatin.

Caution must be exercised when combined with antihypertensive drugs (an increase in the antihypertensive effect is possible), anticoagulants, acetylsalicylic acid (due to the risk of hemorrhage).

The drug potentiates the effect of fibrinolytic agents, antispasmodics and cardiac glycosides, the toxic effect of alcohol on the liver.

Incompatibility. Do not mix with solutions of thiamine chloride (thiamine is destroyed), pyridoxine hydrochloride, cyanocobalamin, aminophylline, salicylates, tetracycline, sympathomimetics, hydrocortisone.

Overdose

Symptoms: increased side effects from the cardiovascular system - arterial hypotension, headache, possible loss of consciousness, dizziness, sensation of rush.

Treatment: drug withdrawal, detoxification therapy, symptomatic treatment. There is no specific antidote.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° C. do not freeze.