Halidor solution 25mg / ml, 2ml # 10

Vascular diseases

Peripheral vascular disease :

• Raynaud's disease

• other diseases with acrocyanosis and vasospasm, as well as chronic obliterating arterial diseases.

Diseases of cerebral vessels : in the complex therapy of acute and chronic cerebral ischemia.

Elimination of spasm of internal organs

Gastrointestinal diseases :

• gastroenteritis of various etiologies (especially infectious),

• infectious and inflammatory colitis,

• functional diseases of the large intestine,

• tenesmus,

• postoperative flatulence,

• cholecystitis,

• cholelithiasis,

• condition after cholecystectomy,

• motility disorders with dyskinesia of the Odzi sphincter,

• stomach or duodenal ulcer - in combination with other drugs.

Urological syndromes :

• spasms and tenesmus of the bladder,

• concomitant therapy of urolithiasis (in combination with analgesics for renal colic),

• preparation for instrumental research methods.

Solution for intravenous injection (after dilution) or infusion.

Vascular diseases
Infusion :
For vascular diseases, the drug can be used in a daily dose of 200 mg, divided into 2 infusions. 100 mg (4 ml) of the drug is diluted in 100-200 ml of isotonic NaCl solution. The drug is administered by intravenous drip within 1 hour, 2 times a day.

Elimination of spasm of internal organs
Injections :
In acute cases, 2-4 ampoules (4-8 ml) of the drug diluted with saline solution up to 10-20 ml or deep intramuscularly 2 ml are injected into the vein slowly.
The course of treatment is 2-3 weeks, if necessary, with the subsequent transfer of the patient to taking the drug Halidor tablets.

active substance: bencyclane fumarate - 50mg

excipients: sodium chloride for parenteral dosage forms 8 mg and water for injection up to 2 ml.

• Hypersensitivity to the active or any other component of the drug.

• Severe respiratory, renal, or hepatic impairment.

• Decompensated heart failure, acute myocardial infarction, atrioventricular block.

• Epilepsy and other forms of spasmophilia.

• Recently suffered hemorrhagic stroke.

• Traumatic brain injury (within the last 12 months).

• Pregnancy and lactation (see section on pregnancy and lactation).

Tradename:

GALIDORЃ

International non-proprietary name:

bencyclan

Dosage form:

solution for intravenous and intramuscular administration

Composition: for 1 ampoule 2 ml

active substance: bencyclane fumarate - 50mg

excipients: sodium chloride for parenteral dosage forms 8 mg and water for injection up to 2 ml.

Description :

Transparent colorless solution, odorless.

Pharmacotherapeutic group:

antispasmodic

ATX code : —04ј ’11

Pharmacological properties

Pharmacodynamics

Bencyclan is a myotropic antispasmodic with a pronounced vasodilating effect. The vasodilating effect of bencyclane is mainly associated with its ability to block calcium channels, antiserotonin action, and to a lesser extent - with the blockade of sympathetic ganglia. In addition, bencyclan has an antispasmodic effect on the visceral muscles (gastrointestinal tract, urogenital organs, respiratory organs). The drug causes a slight increase in heart rate. Its weak tranquilizing effect is also known.

Mechanism of action
Bencyclan can cause dose-dependent suppression of Na / K-dependent ATPase and aggregation of platelets and erythrocytes, as well as an increase in the elasticity of erythrocytes. These effects are observed mainly in peripheral vessels, coronary arteries and cerebral vessels.

Pharmacokinetics

The maximum concentration in blood plasma is reached 2-8 hours (usually 3 hours) after ingestion. Due to the metabolism of the first passage through the liver, the bioavailability of the drug after oral administration is 25-35%. Approximately 30-40% of the amount of bencyclane in the circulating blood is associated with plasma proteins, 30% with erythrocytes, 10% with platelets; the free fraction is 20%. Metabolism is carried out in the liver, mainly in two ways: dealkylation gives a demethylated derivative, cleavage of the ester bond gives benzoic acid, which is further converted into hippuric acid. The main part of the administered dose is excreted in the kidneys, mainly in the form of metabolites, but also unchanged (2-3%). The vast majority of metabolites (90%) are excreted in unconjugated form,and a small part is excreted in conjugated form (approximately 50% in the form of conjugate with glucuronic acid).
The half-life is 6-10 hours; this parameter does not change in elderly patients, as well as with impaired renal and liver function. The total clearance is 40 l / h, the renal clearance is less than 1 l / h.

Indications for use

Vascular diseases

Peripheral vascular disease :

• Raynaud's disease

• other diseases with acrocyanosis and vasospasm, as well as chronic obliterating arterial diseases.

Diseases of cerebral vessels : in the complex therapy of acute and chronic cerebral ischemia.

Elimination of spasm of internal organs

Gastrointestinal diseases :

• gastroenteritis of various etiologies (especially infectious),

• infectious and inflammatory colitis,

• functional diseases of the large intestine,

• tenesmus,

• postoperative flatulence,

• cholecystitis,

• cholelithiasis,

• condition after cholecystectomy,

• motility disorders with dyskinesia of the Odzi sphincter,

• stomach or duodenal ulcer - in combination with other drugs.

Urological syndromes :

• spasms and tenesmus of the bladder,

• concomitant therapy of urolithiasis (in combination with analgesics for renal colic),

• preparation for instrumental research methods.

Contraindications

• Hypersensitivity to the active or any other component of the drug.

• Severe respiratory, renal, or hepatic impairment.

• Decompensated heart failure, acute myocardial infarction, atrioventricular block.

• Epilepsy and other forms of spasmophilia.

• Recently suffered hemorrhagic stroke.

• Traumatic brain injury (within the last 12 months).

• Pregnancy and lactation (see section on pregnancy and lactation).

Pregnancy and lactation

Preclinical data did not reveal any embryotoxic or teratogenic effects. However, there have been no sufficient reliable studies on the use of the drug during pregnancy and lactation in humans. Therefore, the administration of the drug to patients in the first trimester of pregnancy is not recommended. During lactation, you should refrain from prescribing the drug, or decide on the termination of breastfeeding during treatment.

Method of administration and dosage

Solution for intravenous injection (after dilution) or infusion.

Vascular diseases
Infusion :
For vascular diseases, the drug can be used in a daily dose of 200 mg, divided into 2 infusions. 100 mg (4 ml) of the drug is diluted in 100-200 ml of isotonic NaCl solution. The drug is administered by intravenous drip within 1 hour, 2 times a day.

Elimination of spasm of internal organs
Injections :
In acute cases, 2-4 ampoules (4-8 ml) of the drug diluted with saline solution up to 10-20 ml or deep intramuscularly 2 ml are injected into the vein slowly.
The course of treatment is 2-3 weeks, if necessary, with the subsequent transfer of the patient to taking the drug Halidor tablets.

Side effects

Gastrointestinal : dry mouth, abdominal pain, satiety, nausea, vomiting.
Central nervous system : anxiety, headache, dizziness, gait disturbance, tremor, insomnia, memory disorders, rarely - transient confusion, hallucinations, very rarely - symptoms of focal lesions of the central nervous system.
Cardiovascular : sometimes atrial or ventricular tachyarrhythmias may occur (especially when co-administered with other proarrhythmogenic drugs).
Laboratory indicators : a transient increase in the activity of aspartate aminotransferase and alamine aminotransferase, a decrease in the number of white blood cells.
Others: general malaise, weight gain, allergic reactions, rarely - thrombophlebitis when administered intravenously.

Overdose

Symptoms : increased heart rate, decreased blood pressure, predisposition to collapse, urinary incontinence, drowsiness, anxiety, and in severe cases, epileptiform seizures. A significant overdose can cause tonic and clonic seizures.
Treatment : No specific antidote known. In case of overdose, symptomatic treatment should be used. Benzodiazepines are recommended for the treatment of seizures. There is no data on the possible elimination of bencyclane by dialysis.

Interaction with other medicinal products

Caution should be exercised when combined with the following:

• anesthetics and sedatives - their effects may be enhanced;

• sympathomimetics - due to the risk of atrial and ventricular tachyarrhythmias;

• drugs that reduce the level of potassium in the blood - due to the possible summation of proarrhythmogenic effects;

• digitalis drugs - the risk of arrhythmia increases with digitalis overdose;

• beta-blockers - due to the opposite chronotropic effects (negative for beta-blockers and positive for bencyclane), it may be necessary to select the dosage of the beta-blocker;

• calcium channel blockers and other antihypertensive drugs - due to the possibility of enhancing their effect;

• drugs that cause side effects in the form of spasmophilia - due to the possibility of the summation of these effects;

• aspirin - due to increased inhibition of platelet aggregation.

special instructions

The injection sites should be changed periodically, because the drug can cause damage to the vascular endothelium and thrombophlebitis.
You should refrain from parenteral administration of the drug to patients with severe cardiovascular or respiratory failure, prone to collapse, as well as with prostatic hypertrophy and urinary retention (the degree of retention increases with relaxation of the bladder muscles).
With prolonged therapy with bencyclan, regular laboratory tests are recommended (at least once every 2 months).

Influence on the ability to drive vehicles and control mechanisms
At the beginning of the course of treatment, driving vehicles and performing work with an increased risk of accidents requires special care.

Release form

Solution for intravenous and intramuscular administration of 25 mg / ml.
2 ml in an ampoule with a break point and two code rings (blue lower ring and yellow upper ring), 5 ampoules in a blister (pallet), 2 blister packs in a cardboard box with instructions for use or 10 blisters in a cardboard box sealed with a label along with instructions for use.

Shelf life

3 years. Do not use after the date indicated on the packaging.

Storage conditions

Store at a temperature of 15-25 ? C out of the reach of children.

Conditions of dispensing from pharmacies

On prescription.