Composition, form of production and packaging
Tablets are white or grayish-white, round, flat, chamfered, engraved with "HALIDOR" on one side, with a weak characteristic odor.
1 tab.
bicyclan fumarate 100 mg
Auxiliary substances: potato starch, polyvinyl acetate, magnesium stearate, carbomer 934 P, sodium carboxymethyl starch (type A), silicon dioxide colloidal anhydrous, talc.
50 pcs. - bottles of dark glass (1) - packs of cardboard.
The solution for intravenous and / or injection is clear, colorless, odorless.
1 ml of 1 amp.
bicyclic fumarate 25 mg 50 mg
Excipients: sodium chloride for parenteral medicinal forms - 8 mg, water d / and - up to 2 ml.
2 ml - ampoules (5) - packings, cellular outline (2) - packs cardboard.
2 ml - ampoules (5) - packings of cellular outline (10) - cardboard boxes.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Myotropic antispasmodic with pronounced vasodilating effect. The vasodilator effect of benzyclane is mainly due to its ability to block calcium channels, antiserotonin action, and to a lesser extent - with blockade of sympathetic ganglia. Benzyclane can cause a dose-dependent suppression of Na + / K + -dependent ATPase and platelet and erythrocyte aggregation, as well as increased erythrocyte elasticity. These effects are observed mainly in peripheral vessels, coronary arteries and cerebral vessels.
In addition, benzyclan has an antispasmodic effect on the visceral musculature (GI tract, urinary tract, respiratory system).
The drug causes a slight increase in heart rate. It is also known for its weak tranquilizing effect.
PHARMACOKINETICS
Suction
After taking the drug inside, bicyclic is absorbed from the gastrointestinal tract quickly and almost completely. C max in blood plasma is achieved after 2-8 hours (usually after 3 hours) after ingestion. Because of the "first pass" effect through the liver, the bioavailability of the drug after ingestion is 25-35%.
Distribution
Approximately 30-40% of the amount of bcycliklan in circulating blood is associated with plasma proteins, 30% with red blood cells, 10% with platelets; the free fraction is 20%.
Metabolism
Metabolism is carried out in the liver, mainly along two routes: dealkylation gives a demethylated derivative, the rupture of the ester bond gives benzoic acid, which later turns into a hippuric acid.
Excretion
T 1/2 is 6-10 hours. It is excreted mainly with urine in the form of inactive metabolites, but also in unchanged form (2-3%). Most metabolites (90%) are excreted unconjugated, and a small part is conjugated (approximately 50% as a conjugate with glucuronic acid). The total ground clearance is 40 l / h, the renal clearance is less than 1 l / h.
Pharmacokinetics in special clinical cases
T 1/2 does not change in elderly patients, as well as in the violation of kidney and liver.
INDICATIONS
Vascular diseases:
- peripheral vascular disease - Raynaud's disease, other diseases with acrocyanosis and spasm of blood vessels, as well as chronic obliterating diseases of the arteries;
- diseases of the cerebral vessels: in the complex therapy of acute and chronic cerebral ischemia.
Elimination of spasm of internal organs:
- gastrointestinal diseases - gastroenteritis of various etiology (especially infectious), infectious and inflammatory colitis, functional diseases of the colon, tenesmus, postoperative flatulence, cholecystitis, cholelithiasis, condition after cholecystectomy, motor disorders with dyskinesia sphincter Oddy, peptic ulcer and duodenal ulcer intestines (as part of combination therapy);
- urological syndromes: spasms and tenesmus of the bladder, concomitant therapy of urolithiasis (in combination with analgesics in renal colic).
Preparation for instrumental methods of research in urology.
DOSING MODE
Vascular diseases
Inside Halidor В® is prescribed for 100 mg 3 times / day for 2-3 months. The maximum daily intake 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 injections. Before the infusion, 100 mg (4 ml) of the drug is diluted in 100-200 ml of isotonic sodium chloride solution and injected / drip for 1 hour 2 times / day.
To eliminate spasm of internal organs
Inside, Halidor В® is prescribed in a dose of 100-200 mg once, but not more than 400 mg / day. For maintenance therapy appoint 100 mg 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 В® is administered iv slowly in a dose of 100-200 mg (4-8 ml) or in / m deep in a dose of 50 mg (2 ml). Before / in the introduction of the required amount of solution is diluted with an 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 receive the preparation Galidor В® inside.
SIDE EFFECT
On the part of the digestive system: dry mouth, abdominal pain, feeling full, nausea, vomiting, increased activity of hepatic transaminases in the serum.
From the side of the central nervous system: anxiety, dizziness, headache, gait disturbance, tremor, sleep disorders, insomnia, memory disorders; rarely - a transitory confused state of consciousness, epileptiform seizures, hallucinations; in isolated cases - symptoms of focal lesion of the central nervous system.
From the cardiovascular system: sometimes - atrial and ventricular tachyarrhythmia (especially when co-administered with other pro-arrhythmogenic drugs).
Other: general malaise, weight gain, leukopenia, allergic reactions; rarely - thrombophlebitis with iv introduction.
CONTRAINDICATIONS
- severe respiratory failure;
- severe renal failure;
severe hepatic impairment;
Decompensated heart failure;
acute myocardial infarction;
- AV blockade;
- epilepsy and other forms of spasmophilia;
- recently transferred hemorrhagic stroke;
- craniocerebral trauma (during the last 12 months);
- Pregnancy;
- the period of lactation (breastfeeding);
- children's and adolescents under 18 years of age (insufficient experience of application);
- Hypersensitivity to the components of the drug.
PREGNANCY AND LACTATION
Pre-clinical data showed no embryotoxic or teratogenic effects, but no adequate and rigorously controlled clinical trials for the use of the GalidorВ® preparation were made during pregnancy and lactation. Therefore, the administration of the drug to patients in the first trimester of pregnancy is not recommended.
If it is necessary to use the drug during lactation, the question of stopping breastfeeding during treatment should be resolved.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe hepatic insufficiency.
APPLICATION FOR CHILDREN
Contraindications: children and adolescents under 18 years of age (insufficient experience of use).
APPLICATION IN ELDERLY PATIENTS
Contraindicated in children and adolescents under 18 years.
SPECIAL INSTRUCTIONS
With the simultaneous appointment of Halidor with drugs that cause hypokalemia, cardiac glycosides, with drugs that depress myocardial function, the daily dose of Halidor should not exceed 150-200 mg.
When parenteral application should be changed place of injection, tk. the drug can cause damage to the vascular endothelium and thrombophlebitis.
It should refrain from parenteral administration of the drug to patients with severe cardiovascular or respiratory failure, predisposed to collapse, as well as prostatic hypertrophy and urinary retention (the degree of delay increases with relaxation of the bladder muscles).
With prolonged use of Galidor, a systematic (at least 1 time in 2 months) laboratory testing of the rheological properties of the blood is recommended.
Impact on the ability to drive vehicles and manage mechanisms
At the beginning of the course of treatment, patients should take special care when driving vehicles and other potentially hazardous activities.
OVERDOSE
Symptoms: increased heart rate, decreased blood pressure, collapse, impaired renal function, urinary incontinence, drowsiness, anxiety, in severe cases - epileptiform convulsive seizures. A significant overdose can cause tonic and clonic convulsions.
Treatment: symptomatic therapy. When you take a large number of tablets, you should wash the stomach. To treat convulsive seizures, it is recommended to use benzodiazepines. The specific antidote is not known. Data on the possible excretion of bcyclical by dialysis are not available.
DRUG INTERACTION
With the simultaneous use of Halidor В® enhances the depressing effect on the central nervous system 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 lower the level of potassium in the blood (including diuretics, cardiac glycosides), and quinidine, a possible combination of pro-arrhythmic effects.
With the simultaneous use of Galidor with digitalis preparations, the risk of arrhythmia increases with an overdose of cardiac glycosides.
With the simultaneous use of Galidor with beta-blockers, it may be necessary to select a dose of beta-adrenoblocker because of the opposite of chronotropic effects (negative in beta-adrenoblockers and positive in benzyclane).
With the simultaneous use of Halidor with calcium channel blockers and other antihypertensive drugs, it is possible to enhance their effect.
With the simultaneous use of Halidor with drugs that cause side effects in the form of spasmophilia, it is possible to sum these effects.
With the simultaneous use of Halidor with acetylsalicylic acid, inhibition of platelet aggregation is possible.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of 15 В° to 25 В° C. Shelf life of the tablets is 5 years. Shelf life of the injection solution is 3 years.
