Nicotinic acid-darnitsa

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT NICOTINIC ACID-DARNITSA (NICOTINIC ACID-DARNITSA)

Composition:

Active substance: nicotinic acid;

1 ml of solution contains 10 mg of nicotinic acid;

Excipients: sodium bicarbonate, water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear, colourless liquid.

Pharmacotherapeutic group. Peripheral vasodilators. Nicotinic acid and its derivatives. ATC code C04AC01.

Pharmacological properties.

Pharmacodynamics.

Nicotinic acid (vitamin PP) and its amide are prosthetic groups of the enzymes dehydrogenase I (diphosphopyridine nucleotide – NAD) and dehydrogenase II (triphosphopyridine nucleotide – NADP), which mediate hydrogen transfer in redox reactions, as well as phosphate transfer.

Participating in metabolism, tissue respiration, and synthetic processes, nicotinic acid normalizes blood levels of lipoproteins and triglycerides.

It exerts a vasodilatory effect at the level of precapillary arterioles and arterioles (including in the brain), thereby improving microcirculation.

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

It eliminates vitamin PP deficiency and is a specific anti-pellagric agent.

Pharmacokinetics.

Nicotinic acid is rapidly absorbed from the site of administration following parenteral administration. It is evenly distributed throughout all organs and tissues. Inactivation occurs mainly via methylation, and to a lesser extent via conjugation. Metabolites are excreted in urine. Nicotinic acid may be present in urine in its active form when administered in elevated amounts.

Clinical characteristics.

Indications.

Treatment of pellagra (vitamin PP deficiency).

Ischemic disorders of cerebral circulation. Vascular spasms of the extremities (obliterating endarteritis, Raynaud's disease). Renal vascular spasm.

Chronic non-healing wounds and ulcers. Complications of diabetes mellitus (diabetic polyneuropathy, microangiopathy).

Hypochlorhydric gastritis, enterocolitis, colitis. Liver diseases (acute and chronic hepatitis).

Facial nerve neuritis.

Intoxications of various origins: occupational, alcohol-related, drug-induced (aniline derivatives, barbiturates, antituberculosis agents, sulfonamides).

Contraindications.

Hypersensitivity to the components of the drug. Peptic ulcer of the stomach and duodenum (in the acute phase), gout, hyperuricemia, severe hepatic insufficiency (including cirrhosis), severe forms of arterial hypertension and atherosclerosis (intravenous administration), decompensated diabetes mellitus, recent myocardial infarction, history of sudden decrease in peripheral vascular resistance.

Interaction with other medicinal products and other types of interactions.

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

Nicotinic acid reduces the efficacy and toxicity of probenecid, neomycin, barbiturates, antituberculosis agents, and sulfonamides.

Antibiotics may enhance the skin flushing caused by nicotinic acid.

Acetylsalicylic acid reduces the skin flushing effect induced by nicotinic acid.

Cyproheptadine is not recommended to be combined with nicotinic acid.

Lovastatin, pravastatin are not recommended to be combined with nicotinic acid due to increased risk of adverse reactions. Cases of rhabdomyolysis have been reported when nicotinic acid was used concomitantly with lovastatin.

Caution is required when combining with antihypertensive agents (possible enhancement of hypotensive effect), anticoagulants, and acetylsalicylic acid (due to the risk of hemorrhage).

The drug potentiates the effects of fibrinolytic agents, spasmolytics, and cardiac glycosides, as well as the hepatotoxic effect of alcohol.

Special precautions for use

Since prolonged use may lead to hepatic fatty degeneration, to prevent this condition, patients' diet should include methionine-rich products or methionine and lipoic acid should be prescribed. Liver function must be monitored during treatment. In case of increased sensitivity to the drug (except when used as a vasodilator), it can be replaced with nicotinamide.

The drug should be used with caution in hyperacid gastritis, peptic ulcer of the stomach and duodenum (outside the exacerbation phase), hemorrhages, glaucoma, renal insufficiency, moderate arterial hypotension, alcohol abuse, and unstable angina (in patients taking nitrates, calcium channel antagonists, β-blockers).

Use of the drug may increase insulin requirements in patients with diabetes mellitus. It is not advisable to use the drug for correcting dyslipidemia in patients with diabetes mellitus.

Regular monitoring of glucose levels is necessary due to possible decreased glucose tolerance, as well as monitoring serum uric acid levels due to possible increase resulting from long-term therapy.

Important information about excipients

This medicinal product contains less than 1 mmol (23 mg)/dose of sodium, i.e. essentially sodium-free.

Use during pregnancy or breastfeeding

The drug is contraindicated during pregnancy. If it is necessary to use the drug, breastfeeding should be discontinued.

Ability to influence reaction rate while driving or operating machinery

Studies on the effect of the drug on reaction speed have not been conducted; however, if dizziness or drowsiness occurs during treatment, patients should refrain from working with complex machinery.

Administration and Dosage

For use in adults and children aged 15 years and older, administered intravenously (slowly), intramuscularly, or subcutaneously (intramuscular and subcutaneous injections are painful).

For intravenous bolus injection, dilute a single dose of the drug in 10 mL of 0.9% sodium chloride solution and administer over not less than 5 minutes (no more than 2 mg of nicotinic acid per minute).

For intravenous infusion, dilute a single dose of the drug in 100–200 mL of 0.9% sodium chloride solution; the infusion rate should be 30–40 drops per minute.

Pellagra. Administer intravenously or intramuscularly, 10 mg (1 mL), 1–2 times daily. Treatment duration: 10–15 days.

Ischemic cerebrovascular disorders. Administer intravenously (slowly), 10 mg (1 mL).

Other indications. Administer subcutaneously or intramuscularly, 10 mg (1 mL) once daily for 10–15 days. May be added to infusion solutions: 10 mg (1 mL) of nicotinic acid per 100–200 mL of infusion solution.

Higher doses for intravenous administration: single dose – 100 mg (10 mL), daily dose – 300 mg (30 mL).

Children

The drug is indicated for children aged 15 years and older.

Overdose.

Symptoms: intensification of adverse effects on the cardiovascular system – arterial hypotension, headache, possible loss of consciousness, dizziness, sensation of flushing.

Treatment: discontinue the drug, administer detoxification therapy, and provide symptomatic treatment. There is no specific antidote.

Adverse Reactions.

Central and peripheral nervous system disorders: dizziness, paresthesia, headache.

Cardiovascular system disorders: sensation of flushing, which may be accompanied by dyspnea, tachycardia, palpitations, increased sweating, chills, edema, sensation of tingling and burning; arrhythmias; with rapid intravenous administration – significant decrease in arterial blood pressure, orthostatic hypotension, collapse.

Skin and subcutaneous tissue disorders: facial and upper trunk skin hyperemia with sensation of tingling and burning, dryness of the skin and ocular mucous membranes, rarely – retinal edema, very rarely in patients with ischemic heart disease – acanthosis. These symptoms are transient and disappear after discontinuation of the drug. Hypersensitivity reactions, including respiratory tract involvement, urticaria, pruritus, rash.

General disorders and administration site conditions: pain, swelling at the site of subcutaneous and intramuscular injections.

With prolonged use in high doses – hyperuricemia, decreased glucose tolerance, liver function disturbances, hepatic fatty degeneration, jaundice, increased levels of aspartate aminotransferase, lactate dehydrogenase, alkaline phosphatase, uric acid, hypophosphatemia, decreased platelet count, prolonged prothrombin time, hyperpigmentation, hyperkeratosis, seizures, diarrhea, nausea, vomiting, anorexia, peptic ulcer exacerbation, amblyopia, insomnia, myalgia, decreased arterial pressure, rhinitis, blurred vision, eyelid edema, myopathy, exfoliative dermatitis.

Reporting suspected adverse reactions.

Reporting of suspected adverse reactions after drug registration is an important procedure. It enables continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are required to report any suspected adverse reactions via the national reporting system.

Shelf life. 5 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Do not freeze.

Keep out of reach of children.

Incompatibilities.

Should not be mixed with solutions of thiamine chloride (results in thiamine degradation), pyridoxine hydrochloride, cyanocobalamin, aminophylline, salicylates, tetracycline, sympathomimetics, hydrocortisone.

Packaging.

1 ml in an ampoule; 5 ampoules in a blister pack; 2 blister packs in a carton.

Prescription status. Prescription only.

Manufacturer. JSC "Pharmaceutical Company "Darnitsya".

Manufacturer's address and place of business.

13, Borispilska Street, Kyiv, 02093, Ukraine.