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Active ingredients
Bentsiklan
Release form
Pills
Composition
1 tablet contains: Active substances: benzklana fumarat 100 mg. Auxiliary substances: potato starch, polyvinyl acetate, magnesium stearate, carbomer 934 P, sodium carboxymethyl starch (type A), silicon dioxide, colloidal anhydrous, talc.
Pharmacological effect
Myotropic antispasmodic with a pronounced vasodilating action. The vasodilating action of the bentsklan is mainly associated with its ability to block calcium channels, the antiserotonin action, and to a lesser extent with the blockade of sympathetic ganglia. Bentsyklan can cause dose-dependent suppression of Na + / K + -dependent ATPase and platelet aggregation and erythrocytes, as well as increasing the elasticity of erythrocytes. These effects are mainly observed in peripheral vessels, coronary arteries and cerebral vessels. In addition, benzclan has a spasmolytic effect on the visceral muscles (gastrointestinal tract, urinary tract, respiratory organs). The drug causes a certain increase in heart rate. Its weak tranquilizing effect is also known.
Pharmacokinetics
AbsorptionAfter taking the drug inside benzikan absorbed from the gastrointestinal tract quickly and almost completely. Cmax in plasma is reached 2-8 hours (usually 3 hours) after ingestion. Due to the effect of the first passage through the liver, the bioavailability of the drug after oral administration is 25-35%. Distribution Approximately 30-40% of the amount of benziklan in the circulating blood is associated with plasma proteins, 30% with erythrocytes, 10% with platelets; the free fraction is 20%. Metabolism Metabolism takes place in the liver, mainly in two ways: dealkylation gives a demethylated derivative, breaking the ester bond gives benzoic acid, which later turns into hippuric acid. Excretion of T1 / 2 is 6-10 hours as inactive metabolites, but also unchanged (2-3%). Most of the metabolites (90%) are excreted in an unconjugated form, and a small part in a conjugated form (approximately 50% in the form of a conjugate with glucuronic acid). The total clearance is 40 l / h, the renal clearance is less than 1 l / h. The pharmacokinetics in special clinical situations T1 / 2 does not change in elderly patients, as well as in violation of the functions of the kidneys and liver.
Indications
Vascular diseases: - peripheral vascular diseases - Raynaud's disease, other diseases with acrocyanosis and vascular spasm, and chronic arterial occlusive disease; - cerebral vascular diseases: in complex therapy of acute and chronic cerebral ischemia. Elimination of internal organs spasm: - gastrointestinal diseases - gastroenteritis of various etiologies (especially infectious), infectious and inflammatory colitis, functional diseases of the large intestine, tenesmus, postoperative meteorism , cholecystitis, cholelithiasis, condition after cholecystectomy, motility disorders in dyskinesia of the sphincter of Oddi, gastric ulcer and duodenal ulcer (as part of combination therapy); - urological syndromes: spasms and tenesmus of the bladder, concomitant therapy of urolithiasis (in combination with analgesics) renal colic). Preparation for instrumental methods of research in urology.
Contraindications
- severe respiratory failure; - renal failure; severe; - severe liver failure; - decompensated heart failure; - acute myocardial infarction; - AV blockade; - epilepsy and other forms of spasmophilia; - recent hemorrhagic stroke; - craniocerebral injury ( during the last 12 months); - pregnancy; - lactation period (breastfeeding); - children and adolescents under 18 years of age (insufficient experience of use); - hypersensitivity to the components of the preparation that
Use during pregnancy and lactation
The data of preclinical studies did not reveal any embryotoxic or teratogenic effects, however, adequate and strictly controlled clinical studies on the use of the drug Halidor during pregnancy and lactation were not carried out. Therefore, the introduction of the drug to patients in the first trimester of pregnancy is not recommended. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding during treatment.
Dosage and administration
Vascular diseases. Inside Halidor, 100 mg is prescribed 3 times / day for 2-3 months. The maximum daily dose for oral administration is 400 mg.The interval between courses is 2-3 months. The drug can also be used in the form of intravenous infusions in a daily dose of 200 mg, divided into 2 administrations. Before the infusion, 100 mg (4 ml) of the drug is diluted in 100-200 ml of isotonic sodium chloride solution and injected into / into the drip for 1 h 2 times / day. To eliminate the spasm of the internal organs, Halidor is prescribed in a dose of 100-200 mg once, but not more than 400 mg / day. For maintenance therapy, 100 mg is prescribed 3 times / day for 3-4 weeks, then 100 mg 2 times / day. The duration of treatment is determined individually depending on the disappearance of the symptoms of the disease and, as a rule, does not exceed 1-2 months. In acute cases, Halidor is administered IV slowly at a dose of 100-200 mg (4-8 ml) or intramuscularly deeply at a dose 50 mg (2 ml). Before the on / in the introduction of the required amount of solution diluted with isotonic sodium chloride solution to 10-20 ml. The course of treatment is 2-3 weeks with the subsequent transfer of the patient, if necessary, to the intake of the drug Halidor.
Side effects
On the part of the digestive system: dry mouth, abdominal pain, feeling of satiety, nausea, vomiting, increased serum liver transaminases. For the central nervous system: anxiety, dizziness, headache, impaired gait, tremor, sleep disorders, insomnia, disorders memory; rarely - transient confused state of consciousness, epileptiform seizures, hallucinations; in rare cases, symptoms of focal CNS lesions. From the cardiovascular system: sometimes atrial and ventricular tachyarrhythmia (especially when given in combination with other proarrhythmic drugs). Others: general indisposition, weight gain, leukopenia, allergic reactions; rarely - thrombophlebitis with a / in the introduction.
Overdose
Symptoms: increased heart rate, decreased blood pressure, collapse, impaired kidney function, urinary incontinence, drowsiness, anxiety, in severe cases - epileptiform convulsive seizures. Significant overdose can cause tonic and clonic convulsions. Treatment: symptomatic therapy. When taking a large number of pills should be a gastric lavage. Benzodiazepines are recommended for the treatment of seizures. The specific antidote is not known.There is no data on the possible elimination of a benziklan by dialysis.
Interaction with other drugs
With the simultaneous use of Halidor increases the inhibitory effect on the central nervous system means for anesthesia and sedatives. With the simultaneous use of Halidor with sympathomimetics, the risk of developing tachycardia, atrial and ventricular tachyarrhythmias increases. With the simultaneous use of Halidor and drugs that reduce the level of potassium in the blood (including diuretics, cardiac glycosides), and quinidine, summation of proarrhythmogenic effects is possible. With the simultaneous use of Halidor with digitalis preparations, the risk of arrhythmia during overdose increases cardiac glycosides. If Halidor is used simultaneously with beta-blockers, it may be necessary to adjust the dose of beta-blocker because of the opposite chronotropic effects (negative on beta-blockers and positive on the benticlan). At the same time, Halidor has calcium channel blockers and other antihypertensives. their effect can be enhanced. With the simultaneous use of Halidor with drugs that cause side effects in the form of spasmophilia, summation of these effektov.Pri simultaneous application Halidorum with acetylsalicylic acid may increase platelet aggregation inhibition.
special instructions
With the simultaneous appointment of Halidor with drugs that cause hypokalemia, cardiac glycosides, with drugs that inhibit myocardial function, the daily dose of Halidor should not exceed 150-200 mg. In parenteral use, injection sites should be changed, because The drug may cause damage to the vascular endothelium and thrombophlebitis. It is necessary to refrain from parenteral administration of the drug to patients with severe cardiovascular or respiratory failure predisposed to collapse, as well as with prostatic hypertrophy and urinary retention (the degree of delay increases when the bladder muscles relax). long-term use of Halidor is recommended systematically (at least 1 time in 2 months) laboratory studies of the rheological properties of blood. The effect on the method spine to drive vehicles and management mehanizmamiV the beginning of treatment, patients should be particularly careful when driving vehicles and other potentially hazardous activities.