Pharmacological properties.
Pharmacodynamics.
Nicotinic acid is a prosthetic group of enzymes of codehydrase I and codehydrase II - enzymes that carry hydrogen and carry out redox processes. Codehydrase II also plays a role in the transport of phosphate. Lack of niacin leads to pellagra. Nicotinic acid improves the metabolism of carbohydrates, dilates blood vessels. It has lipoproteinemic activity, with hypercholesterolemia, it lowers the cholesterol / phospholipid index.
Pharmacokinetics.
It is absorbed within 6-8 hours, since nicotinic acid is gradually and evenly released from the tablet. During the first hour, about 50% is absorbed, by the eighth hour - about 96%. It is metabolized in the liver, kidneys and muscles. Metabolic products are excreted by the kidneys.
Compound:
Active substance: nicotinic acid;
1 tablet contains 50 mg of nicotinic acid;
excipients: glucose monohydrate, magnesium stearate.
Indications.
Prevention and treatment of pellagra (avitaminosis pp); atherosclerosis; hypoacid gastritis; spasms of blood vessels (brain, kidneys, extremities); neuritis of the facial nerve; long-term non-healing wounds and ulcers of various localization and genesis.
Contraindications
Hypersensitivity to nicotinic acid or to other components of the preparation. arterial hypertension (severe forms), stomach and duodenal ulcers (in the acute stage), severe liver dysfunctions, including cirrhosis, active hepatitis.
Decompensated diabetes mellitus, urolithiasis, hyperuricemia, gout.
Recent myocardial infarction, a history of sudden decrease in peripheral vascular resistance.
Interaction with other medicinal products.
Oral contraception and isoniazid reduce the conversion of tryptophan to nicotinic acid and thus may increase the need for nicotinic acid.
Nicotinic acid reduces the effectiveness and toxicity of probenecid, neomycin, barbiturates, anti-tuberculosis preparations, sulfonamides.
Antibiotics can increase the redness of the skin caused by niacin.
Acetylsalicylic acid reduces the reddening effect of the skin caused by niacin.
Lovastatin, pravastatin, due to the increased risk of adverse reactions, is not recommended to be combined with nicotinic acid. There are reports of cases of rhabdomyolysis when using nicotinic acid with lovastatin.
Care must be taken when combined with antihypertensive preparations (possibly increased hypotensive action), anticoagulants, acetylsalicylic acid (due to the risk of hemorrhages).
The preparation potentiates the action of fibrinolytic agents, antispasmodics and cardiac glycosides, the toxic effect of alcohol on the liver.
Concomitant use with methyldopa or β-adrenergic receptor blockers leads to a strong decrease in blood pressure; with antidiabetic agents - to the hypoglycemic effect of the latter.
Nicotinic acid is incompatible with vitamins B1, B12, B6, euphyllin, salicylates, tetracycline, sympathomimetics, hydrocortisone.
If alcohol is consumed during treatment with nicotinic acid, acute vascular insufficiency may occur.
Features of the application.
To minimize side effects and improve treatment tolerance, it is recommended:
during treatment, it is necessary to control blood glucose levels and liver function in order to identify the side effects of nicotinic acid;
take nicotinic acid only with food, which leads to a gradual absorption of the preparation and helps to reduce side effects;
do not take nicotinic acid with hot drinks (especially coffee), alcohol;
do not take a hot shower (bath) immediately after taking the preparation.
Use with caution in patients with hemorrhages, with glaucoma, renal failure, moderate arterial hypotension, hyperacid gastritis, gastric ulcer and duodenal ulcer (in remission). With caution, nicotinic acid should be used by alcohol abusers, patients with unstable angina pectoris and acute myocardial infarction, receiving nitrates, calcium channel antagonists and beta-blockers.
With prolonged use of nicotinic acid in high doses, fatty infiltration of the liver may develop, therefore, monitoring of liver function is necessary.
It is necessary to regularly monitor the level of uric acid in the blood due to the possible increase in it as a result of long-term therapy.
To prevent complications from the liver, it is recommended to include in the diet foods rich in methionine (cottage cheese) or to use methionine and other lipotropic agents.
The preparation contains glucose, which should be taken into account in patients with diabetes mellitus.
It is inappropriate to use nicotinic acid for the correction of dyslipidemia in patients with diabetes mellitus.
Application during pregnancy or lactation.
It is not recommended to prescribe the preparation to women during pregnancy or lactation.
The ability to influence the reaction rate when driving vehicles or other mechanisms.
Studies on the effect of the preparation on the reaction rate have not been carried out, however, the possible appearance of dizziness and drowsiness when using nicotinic acid should be taken into account.
Method of administration and dosage.
Take orally after meals.
In case of pellagra, adults should be prescribed 100 mg 2–4 times a day for 15–20 days; children from 12 years old - 50 mg 2-3 times a day.
For other diseases, adults should be prescribed 50 mg (up to 100 mg) 2 times a day, children from 12 years old - 25 mg (the tablet has a separate stroke) 2 times a day.
Higher doses for adults: single - 100 mg, daily - 500 mg.
Higher doses for children: single dose - 50 mg, daily dose - 200 mg.
In atherosclerosis (in the absence of side effects), a single dose can be gradually increased to 500 mg-1 g, and the daily dose - up to 2-3 g.
Children.
It is not recommended to prescribe the preparation to children under 12 years of age.
Overdose.
Symptoms large doses of niacin can cause peripheral vasodilation, skin redness, nausea, vomiting, heartburn, diarrhea, increased liver enzyme activity, brown skin pigmentation, less often hyperuricemia, itching of the skin, headache, arterial hypotension, possible loss of consciousness, dizziness, skin paresthesias (tingling, burning sensation, sensation of heat, creeping sensation), impaired glucose metabolism, visual impairment, cholestatic jaundice.
Treatment. It is necessary to stop taking the preparation, therapy is symptomatic.
Adverse reactions.
From the side of the cardiovascular system: a feeling of hot flashes, which may be accompanied by shortness of breath, tachycardia, palpitations, sweating, chills, edema.
From the central nervous system and peripheral nervous system: paresthesia, dizziness, headache.
From the side of the skin: hyperemia of the skin of the face and upper body with a tingling and burning sensation, dry skin and mucous membranes of the eyes, debilitating itching of the skin, rashes.
From the liver and biliary tract: with prolonged use - fatty degeneration of the liver, increased blood levels of aspartate aminotransferase (ATC), lactate dehydrogenase (LDH), alkaline phosphatase.
From the side of metabolism: with prolonged use in large doses - a decrease in glucose tolerance, an increase in blood glucose levels, uric acid levels in the blood, hypophosphatemia.
Others: allergic reactions (including urticaria).
Very rarely, against the background of taking nicotinic acid in patients with coronary heart disease, the frequency of atrial arrhythmias increases, and acanthosis (brown spots on the skin with a velvety surface) occurs. Rarely, retinal edema may occur. These symptoms are unstable and disappear after discontinuation of the preparation.
When taking high doses: hyperpigmentation, convulsions, diarrhea, nausea, vomiting, anorexia, exacerbation of stomach ulcers, jaundice, amblyopia, decreased platelet count, prolonged prothrombin time. Insomnia, myalgia, arterial hypotension, rhinitis may occur. Blurred vision, eyelid edema, myopathy, exfoliative dermatitis are possible. Cases of rhabdomyolysis have been reported with the use of nicotinic acid with lovastatin.
Best before date.
4 years.
Storage conditions.
Store in its original packaging at a temperature not exceeding 25 ° C.