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Pharmacological properties

naftidrofuril has an antispasmodic effect on the smooth muscles of arteries, reduces the tone of arterioles and opss, improves tissue perfusion, especially in the central nervous system. naftidrofuril specifically blocks s2 receptors in platelets and vascular smooth muscle (antiserotonin, vasodilating and antiplatelet effect). in addition, naftidrofuril is an antagonist of nicotine and bradykinin. the drug stimulates energy metabolism in neurons, reduces the production of lactic acid in cells during ischemia. activates succinate dehydrogenase, increases oxygen supply to tissues, improves glucose utilization, increases the level of atf. due to the expansion of blood vessels and the activation of cellular metabolism, the blood supply to peripheral tissues and their supply with energy substrates improves, which helps to reduce the intensity of pain in the extremities during ischemia due to a deficiency of oxygen and nutrients in the tissues. naftidrofuril also affects brain function: normalizes sleep, improves memory and ability to concentrate, eliminates dizziness, headache.

Pharmacokinetics After oral administration, naftidrofuril is well absorbed in the digestive tract. Due to the slow release of the active substance, its effective concentration in the blood plasma is maintained for 3-5 hours after administration. Naftidrofuril binds to blood plasma proteins (about 80%), is excreted from the body mainly with bile in the form of metabolites, and in a small amount with urine. T½ - 40-60 minutes Naftidrofuril easily penetrates the BBB and can pass into breast milk.

Indications

Disturbance of peripheral circulation, including intermittent claudication, trophic ulcers, the initial stage of gangrene, diabetic angiopathy, Raynaud’s disease and syndrome, acrocyanosis, pain in the extremities at rest, paresthesia, cramps in the calf muscles.

Cerebrovascular accident, including cerebral insufficiency and cerebral atherosclerosis.

Behavioral disorders in old age, the rehabilitation period after a stroke, the acute stage of a stroke, conditions after coma and injuries, Menieres disease, ischemic damage to the retina and eye function, impaired blood supply to the inner ear.

Application

The dose is set individually depending on the nature and severity of the disease.

If peripheral circulation is disturbed, usually 100–200 mg 2-3 times a day is prescribed orally. The maximum effect is achieved when prescribed in a daily dose of 400-600 mg. The course of treatment is at least 3 months.

In the treatment of dementia and other conditions associated with impaired cerebral circulation, 100 mg 3 times a day are prescribed; with ischemic stroke - 200 mg 3 times a day or 300-400 mg 2 times a day. Therapy is long.

The tablets must be swallowed whole without chewing, washed down with a neutral liquid.

Contraindications

Hypersensitivity to naftidrofuril or any other component of the drug, recent acute myocardial infarction, acute hemorrhagic stroke, severe heart failure (grade III – IV), severe coronary insufficiency, arrhythmia, conditions accompanied by bleeding, history of vascular collapse, severe arterial hypotension , disorders of orthostatic regulation, severe violations of the liver and kidneys, pregnancy and lactation; children under 14 years old.

Side effects

The drug is well tolerated, adverse reactions are mild and transient.

From the cardiovascular system: lowering blood pressure, orthostatic hypotension, heart rhythm disturbance.

From the side of the central nervous system: anxiety, dizziness, weakness, headache.

From the gastrointestinal tract: nausea, hepatopathy, disorders of the stomach, pain in the epigastric region.

On the part of the skin: rash.

special instructions

It is not recommended to smoke and drink alcohol during treatment.

Exceptionally when using the drug in high doses (mainly at the beginning of treatment in some patients), you may experience a feeling of fatigue, dizziness, decreased blood pressure or orthostatic hypotension.

During pregnancy and breastfeeding. The drug is contraindicated during pregnancy. During treatment, it is recommended to stop breastfeeding.

Children. The drug is not used to treat children under the age of 14 years.

The ability to influence the speed of reactions when driving vehicles and working with other mechanisms. The use of the drug can affect activities that require a high speed of mental and physical reactions, the adoption of quick decisions (for example, driving vehicles, servicing machines and mechanisms, working at heights, etc.), so for the period of treatment you should refrain from driving vehicles , maintenance of machines and mechanisms, work at heights, etc.

Interactions

With the simultaneous use of antiarrhythmic drugs and β-adrenergic blockers, a cardio-depressive effect, a negative dromotropic effect, up to av blockade, are possible.

Overdose

Symptoms: anxiety, convulsions of central genesis, tachyarrhythmia, decreased hell.

The treatment is symptomatic and supportive, aimed at maintaining the vital functions of the body.

Storage conditions

In a dry place at a temperature of 10-25 ° C.

Tags: Enelbin® [Naftidrofuril]