Xanthinol Nicotinate

Pharmacological properties

xantinol nicotinate has the effects of theophylline and nicotinic acid: the mechanism of action is realized due to the blockade of PDE activity, competition with adenosine for receptors, accumulation of cAMP, stimulation of the synthesis of nicotinamide coenzymes and prostanticycline in the walls of blood vessels. the drug dilates peripheral blood vessels, improves collateral and cerebral blood flow, reduces manifestations of cerebral hypoxia, reduces platelet aggregation, improves microcirculation in the retina, enhances contractile function of the heart, improves metabolic processes in the brain tissue in the postoperative period, reduces the level of cholesterol, atherogenic lipoproteins, and urinary acid, fibrinogen, increases the activity of lipoprotein lipase, enhances fibrinolysis.

Pharmacokinetics It is well absorbed in the digestive tract. In the body, the drug quickly turns first into theophylline and nicotinic acid, then into their metabolites. Excreted mainly with urine in the form of metabolites. With a / m introduction, the effect develops after 5-10 minutes.

Indications

Obliterating atherosclerosis of the vessels of the lower extremities (intermittent claudication), Raynaud’s disease, diabetic angiopathy, retinopathy, angioeuropathy, acute thrombophlebitis, acute thrombosis, embolism of blood vessels, migraine, atherosclerotic cerebrovascular disorders after removal of the brain, postoperative malignant, postoperative trophic ulcers of the lower extremities, retinal vascular diseases, degeneration, retinal detachment.

Application

Tablets. xanthinol nicotinate tablets are prescribed for adults by mouth after meals, without chewing. intake begins with 1 tablet 3 times a day. if necessary, increase the dose to 2-3 tablets 3 times a day. tablets are swallowed without chewing. as the condition improves, the dose is reduced to 1 tablet 2-3 times a day. the course of treatment is usually 2 months. in acute disorders of the cerebral and peripheral circulation, an injection form of the drug is preferable. the maximum daily dose is 1800 mg.

Rr for injections. Assign to adults in / in and / m in acute disorders of the cerebral and peripheral circulation. In / in (very slowly, since the rapid introduction may cause dizziness, shortness of breath, pain behind the sternum, severe arterial hypotension), administered in acute disorders of peripheral and cerebral circulation. Adults are prescribed iv in 2 ml of 15% solution 1-2 times a day with the transition to i / m injection - 2 ml 1-3 times a day. At the same time, 2 tablets of Xanthinol nicotinate are administered orally 3 times a day. In severe cases, iv is administered dropwise: 10 ml of 15% solution of the drug (1.5 g) is diluted in 200-500 ml of 5% solution of glucose or 0.9% solution of sodium chloride. Enter for 1-4 hours up to 4 times a day. The course of treatment is determined individually, tentatively - up to 21 days, but there may be a longer treatment. If blood supply to the tissues is disturbed, 2 ml of 15% solution (0.3 g) are administered 3–3 times a day, gradually increasing the dose to 4–6 ml of 15% solution 2-3 times a day. The course of treatment depends on the course of the disease (up to 2-3 weeks).

In ophthalmic practice in adults, the drug is used by iontophoresis on the eyeball - up to 300 mg once a day. The duration of the first procedure is 15 minutes; the subsequent ones can be gradually increased to 20-30 minutes. The course of treatment is 15-20 days.

Contraindications

Hypersensitivity to the components of the drug, as well as to theophylline and nicotinic acid; acute and chronic heart failure, grade II – III; myocardial infarction; stenosis of the left atrioventricular valve; opn; acute hemorrhages; peptic ulcer of the stomach and duodenum in the acute stage; glaucoma; During pregnancy and breastfeeding. for the drug in the form of tablets also - childrens age.

Side effects

Hypersensitivity reactions: skin rashes (urticarial, erythematic-papular), itching, chills, fever, burning sensation, tingling, flushing of the skin in the upper body, especially the neck and head, in rare cases - angioedema;

from the central and peripheral nervous system: headache, dizziness; these symptoms usually disappear after 10-20 minutes and do not require special treatment;

from the digestive tract: diarrhea, anorexia, gastralgia, nausea, vomiting, increased activity of hepatic transaminases and alkaline phosphatase;

on the part of the cardiovascular system: arterial hypotension, moderate tachycardia, in some cases it is possible to provoke angina attacks, cardiac arrhythmias, the development of a robbery syndrome;

from the respiratory system: in some cases - a feeling of lack of air, shortness of breath;

from the endocrine system: with prolonged use in high doses - a decrease in glucose tolerance;

others: general weakness, hyperuricemia.

The occurrence of these symptoms with repeated use of the drug is a contraindication to continue treatment.

special instructions

If necessary, the simultaneous use of cardiac glycosides in order to prevent the development of bradycardia and arrhythmias, treatment should be carried out under the supervision of an ecg.

Caution is prescribed for patients with hypertension or labile blood pressure while using antihypertensive drugs or cardiac glycosides due to the possible risk of a significant decrease in blood pressure and / or the development of arrhythmia.

As a result of a possible increase in the level of transaminases and alkaline phosphatase with prolonged use of xanthinol nicotinate, caution is necessary when it is prescribed to patients with hepatic or renal failure.

With caution is prescribed for severe atherosclerosis of coronary and cerebral vessels, tachysystolic heart rhythm disturbances, as well as elderly patients.

With prolonged use of the drug in high doses, a change in glucose tolerance, a change in blood biochemical parameters is possible, which requires drug withdrawal. In patients with diabetes mellitus, it is necessary to more often determine the level of glucose in the blood. Patients with an implanted pacemaker are prescribed the drug in low doses.

The drug should not be used with alcohol and coffee.

During pregnancy and breastfeeding. The drug is not prescribed during pregnancy and lactation.

Children. There is no experience with children.

The ability to influence the reaction rate when driving vehicles and working with other mechanisms. Care must be taken when driving vehicles and working with other mechanisms, given the possibility of developing dizziness.

Interactions

To avoid a sharp decrease in hell, the drug should not be combined with antihypertensive drugs (α- and β-adrenergic receptor blockers, sympatholytics, ganglioblockers, ergot alkaloids). the drug is incompatible with strophanthin, MAO inhibitors, alcohol and coffee. when combined with cardiac glycosides, the risk of developing bradycardia and arrhythmia is increased. enhances the anticoagulant effect of heparin, streptokinase, fibrinolysin.

Incompatibility. The drug in the form of a solution is incompatible with strophanthin, MAO inhibitors. Do not mix in the same syringe with other medicines.

Overdose

The drug is low toxic. acute overdose may occur arterial hypotension (weakness, dizziness), tachycardia, abdominal pain, vomiting. symptomatic treatment.

Storage conditions

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