Halidor^® (Tablets, Solution) Instructions for Use

ATC Code

C04AX11 (Bencyclane)

Active Substance

Bencyclane (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Myotropic antispasmodic

Pharmacotherapeutic Group

Spasmolytic agent

Pharmacological Action

Myotropic spasmolytic with a pronounced vasodilatory action. It reduces the tone and motor activity of the smooth muscles of blood vessels and internal organs.

The vasodilatory effect of bencyclane is mainly associated with its ability to block calcium channels, its antiserotonin action, and to a lesser extent, with the blockade of sympathetic ganglia.

Bencyclane may cause dose-dependent suppression of Na⁺-K⁺-ATPase and aggregation of platelets and erythrocytes, as well as an increase in erythrocyte elasticity.

These effects are observed mainly in peripheral vessels, coronary arteries, and cerebral vessels.

It has a spasmolytic effect on visceral muscles (gastrointestinal tract, urinary tract, respiratory organs).

It causes a slight increase in heart rate. It has a weak sedative effect.

Pharmacokinetics

After oral administration, Bencyclane is absorbed from the gastrointestinal tract rapidly and almost completely.

C_max in blood plasma is reached in 2-8 hours (usually in 3 hours) after oral administration.

Due to the first-pass effect through the liver, bioavailability after oral administration is 25-35%.

Binding to plasma proteins is about 30-40%, to erythrocytes – 30%, to platelets – 10%; the free fraction is 20%.

Metabolism occurs in the liver, mainly via two pathways: dealkylation yields a demethylated derivative, and cleavage of the ester bond yields benzoic acid, which is further converted to hippuric acid.

T_1/2 is 6-10 hours. It is excreted mainly in the urine (97%) as inactive metabolites, but also unchanged (2-3%). Most metabolites (90%) are excreted in an unconjugated form, and a small part – in a conjugated form (approximately 50% as a conjugate with glucuronic acid). Total clearance is 40 L/h, renal clearance is less than 1 L/h.

Indications

Vascular diseases: peripheral vascular diseases – Raynaud’s disease, other diseases with acrocyanosis and vascular spasm, as well as chronic obliterative arterial diseases; cerebral vascular diseases: in the complex therapy of acute and chronic cerebral ischemia.

For the relief 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 in sphincter of Oddi dyskinesia, gastric and duodenal ulcer (as part of combination therapy); urological syndromes: spasms and tenesmus of the bladder, concomitant therapy of urolithiasis (in combination with analgesics for renal colic).

Preparation for instrumental examination methods in urology (for solution for IV and IM administration).

ICD codes

Dosage Regimen

For oral administration, administer tablets or solution. The single dose is 100 mg to 200 mg. The frequency of administration is one to two times per day. Do not exceed the maximum daily dose of 400 mg.

For intramuscular (IM) administration, inject 50 mg. Administer once or twice daily.

For intravenous (IV) or intra-arterial (IA) administration, inject 50 mg to 100 mg as a slow bolus. Administer once or twice daily.

Adjust the dosage based on individual patient response and therapeutic indication. For long-term therapy, use the lowest effective dose.

For parenteral administration, rotate injection sites regularly to minimize the risk of vascular endothelial damage and thrombophlebitis.

In patients receiving concomitant therapy with cardiac glycosides, drugs causing hypokalemia, or myocardial depressants, the daily dose should not exceed 150 mg to 200 mg.

Adverse Reactions

From the central nervous system anxiety, dizziness, headache, gait disturbance, tremor, sleep disorders, insomnia, memory disorders; rarely – transient confusion, epileptiform seizures, hallucinations in elderly patients; in isolated cases – symptoms of focal CNS lesions.

From the digestive system dry mouth, abdominal pain, feeling of fullness, nausea, vomiting, decreased appetite, diarrhea, increased activity of liver transaminases in blood serum.

From the cardiovascular system sometimes – atrial and ventricular tachyarrhythmia (especially with concomitant administration of other arrhythmogenic drugs).

Other general malaise, weight gain, leukopenia, allergic reactions; rarely – thrombophlebitis with IV administration.

Contraindications

Severe respiratory failure, severe renal failure, severe hepatic failure, decompensated heart failure, acute myocardial infarction, AV block, paroxysmal supraventricular or acute ventricular tachycardia, epilepsy and other forms of spasmophilia, recent hemorrhagic stroke, traumatic brain injury (within the last 12 months), pregnancy, lactation period (breastfeeding), children and adolescents under 18 years of age, hypersensitivity to bencyclane.

Use in Pregnancy and Lactation

Bencyclane is contraindicated for use during pregnancy and during the lactation period (breastfeeding).

Use in Hepatic Impairment

Contraindicated in severe hepatic failure.

Use in Renal Impairment

Contraindicated in severe renal failure.

Pediatric Use

The drug is not used in children and adolescents under 18 years of age.

Special Precautions

It should not be administered parenterally in cases of reduced function of the cardiovascular system and/or respiratory system, predisposition to collapse, as well as in prostatic hypertrophy with impaired urine outflow.

With long-term use, systematic (at least once every 2 months) complete blood count and assessment of liver function are recommended.

With simultaneous use with drugs causing hypokalemia, cardiac glycosides, drugs that have a depressant effect on the myocardium, the daily dose of bencyclane should not exceed 150-200 mg.

With parenteral administration, the injection sites should be changed, because Bencyclane can cause vascular endothelial damage and thrombophlebitis.

With long-term use of bencyclane, systematic (at least once every 2 months) laboratory tests of the rheological properties of blood are recommended.

Influence on the ability to drive vehicles and machinery

At the beginning of the course of treatment, patients should exercise particular caution when driving vehicles and engaging in other potentially hazardous activities.

Drug Interactions

With simultaneous use, the depressant effect on the central nervous system of anesthetics and sedative drugs is enhanced.

With simultaneous use with sympathomimetics, the risk of developing tachyarrhythmia increases.

With simultaneous use of bencyclane and drugs that lower blood potassium levels (including diuretics, cardiac glycosides), and quinidine, summation of proarrhythmic effects is possible.

With simultaneous use of bencyclane with digitalis preparations, the risk of arrhythmia increases in case of overdose of cardiac glycosides.

With simultaneous use of bencyclane with beta-blockers, it may be necessary to adjust the dose of the beta-blocker due to the opposite chronotropic effects (negative for beta-blockers and positive for bencyclane).

With simultaneous use of bencyclane with calcium channel blockers and other antihypertensive drugs, their effect may be enhanced.

With simultaneous use of bencyclane with medicinal products that cause side effects in the form of spasmophilia, summation of these effects is possible.

With simultaneous use of bencyclane with acetylsalicylic acid, enhanced inhibition of platelet aggregation is possible.

Storage Conditions

Store at 15°C (59°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.