GALIDOR

Active material: Bencyclane
When ATH: C04AX11
CCF: Myotropic antispasmodic
ICD-10 codes (testimony): A09, G45, H34, H36.0, I63, I67.2, I69, I73.0, I73.1, I73.9, I79.2, K25, K26, K29, K51, K52, K80, K82.8, K91.5, R10.4, Z51.4
When CSF: 01.14.05
Manufacturer: EGIS PHARMACEUTICALS Plc (Hungary)

Pharmaceutical form, composition and packaging

Pills white or grayish white color, round, flat, chamfered, Engraved “HALIDOR” on one side, with a faint characteristic odor.

Excipients: potato starch, polyvinyl, magnesium stearate, karʙomer 934 P, sodium carboxymethyl (Type A), Colloidal anhydrous silica, talc.

50 PC. – vials of dark glass (1) – packs cardboard.

Solution for in / and the / m clear, colorless, without smell.

Excipients: sodium chloride, etc. and /, water d / and.

2 ml – ampoule (5) – packings Valium planimetric (2) – packs cardboard.
2 ml – ampoule (5) – packings Valium planimetric (10) – cardboard boxes.

Pharmacological action

Myotropic antispasmodic with a pronounced vasodilating action. Bentsiklana vasodilator effect is mainly due to its ability to block calcium channels, antiserotoninovym action, and to a lesser extent – the blockade of sympathetic ganglia. Bentsiklan may cause a dose-dependent inhibition of Na / K-dependent ATPase and aggregation of platelets and red blood cells, as well as increasing the elasticity of red blood cells. These effects occur mainly in the peripheral vessels, coronary and cerebral vessels.

Besides, bentsiklan has antispasmodic effect on visceral musculature (GI, urinary tract, Respiratory).

The drug causes a slight increase in heart rate. We also know his weak tranquilizing effect.

Pharmacokinetics

Absorption

After taking the drug inside bentsiklan absorbed from the gastrointestinal tract rapidly and almost completely. C_max plasma levels achieved after 2-8 no (usually via 3 no) after ingestion. Because of the effect “first pass” bioavailability of the drug through the liver after oral administration is 25-35%.

Distribution

About 30-40% bentsiklana number in the circulation bound to plasma proteins, 30% – erythrocytes, 10% – platelet; free fraction of 20%.

Metabolism

Metabolism in the liver, mainly in two ways: dealkylation gives demethylated derivative, break the ester bond yields benzoic acid, which is further converted to hippuric.

Deduction

T_1/2 is 6-10 no. Write mainly with urine (97%) active metabolites, but also in unchanged form (2-3%). Most of the metabolites (90%) is displayed in the unconjugated form, and a small part – in conjugated form (about 50% as a conjugate with glucuronic acid). The total clearance of 40 l /, renal clearance less 1 l /.

Pharmacokinetics in special clinical situations

T_1/2 It does not change in elderly patients, as well as impaired renal function and liver.

Testimony

Vascular disease:

- Peripheral vascular disease – Raynaud's disease, Other diseases with acrocyanosis and vasospasm, as well as chronic obliterating diseases of arteries;

- cerebral vascular diseases: in the treatment of acute and chronic cerebral ischemia.

To eliminate the spasm of the internal organs:

- gastrointestinal diseases – gastroenteritis of various etiologies (particularly infectious), infectious and inflammatory colitis, functional bowel disease, tenesmus, posleoperatsyonnыy flatulence, cholecystitis, cholelithiasis, condition after cholecystectomy, dysmotility in the sphincter of Oddi dyskinesia, gastric ulcer and duodenal ulcer (in a combination therapy).

Dosage regimen

Vascular disease

Inside Halidorum^® appoint 100 mg 3 times / day for 2-3 months. The maximum daily dose for oral administration is 400 mg. The interval between courses – 2-3 of the month.

The drug can also be used as I / infusion at a daily dose of 200 mg, razdelennoy of 2 introduction. Before the infusion 100 mg (4 ml) the drug is diluted in 100-200 ml of isotonic sodium chloride solution and injected into / in the drip for 1 no 2 times / day.

To eliminate spasm of internal organs

Inside Halidorum^® administered at a dose of 100-200 mg dose, but not more 400 mg / day. For maintenance therapy designate 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 symptoms and, usually, less than 1-2 of the month.

In acute cases Halidorum^® administered in / slow dose 100-200 mg (4-8 ml) or / m deep dose 50 mg (2 ml). Before the on / in the required amount of solution diluted with isotonic sodium chloride solution to 10-20 ml. Course of treatment 2-3 weeks, followed by transfer of the patient, if necessary, on the drug Halidorum^® inside.

Side effect

From the digestive system: dry mouth, abdominal pain, satiety, nausea, vomiting, decreased appetite, diarrhea, increase in liver transaminases in blood serum.

CNS: anxiety, dizziness, headache, gait disturbance, tremor, sleep disorders, insomnia, memory disorders; rarely – transient confused state of mind, epileptiform seizures, hallucinations in elderly patients; in a few cases – Symptoms of focal CNS.

Cardio-vascular system: tachycardia; sometimes – Atrial and ventricular tachyarrhythmia (especially when co-administered with other drugs proaritmogennoe).

Other: general malaise, weakness, weight gain, leukopenia, allergic reactions; rarely – thrombophlebitis at / introduction.

Contraindications

- Severe respiratory distress;

- Severe renal insufficiency;

- Severe hepatic impairment;

- Decompensated heart failure;

- Acute myocardial infarction;

- AV блокада;

- Paroxysmal supraventricular or ventricular tachycardia, acute;

- Epilepsy and other forms spazmofilii;

- Recent history of hemorrhagic stroke;

- Traumatic brain injury (during the last 12 months);

- Pregnancy;

- Lactation (breast-feeding);

- Childhood and adolescence up 18 years (lack of experience with);

- Hypersensitivity to the drug.

Pregnancy and lactation

Adequate and well-controlled clinical trials of the drug Halidorum^® during pregnancy and lactation has not been carried out.

If necessary, use during lactation should decide the issue of termination of breastfeeding during treatment.

These pre-clinical studies have not revealed any embryotoxic or teratogenic effects.

Cautions

When concomitant administration Halidorum^® with drugs, cause hypokalemia, cardiac glycosides, with drugs, depressing myocardial function, daily dose Halidorum^® should not exceed 150-200 mg.

For parenteral administration should change the venue of injections, tk. the drug can cause damage to the vascular endothelium and thrombophlebitis.

It should refrain from injecting the drug to patients with severe cardiovascular or respiratory failure, prone to collapse, as well as hypertrophy of the prostate and urinary retention (retention rate is increased by relaxing the bladder muscles).

With prolonged use Halidorum^® It recommended a systematic (at least 1 times a 2 Months) conduct laboratory studies of blood rheological properties.

Effects on ability to drive vehicles and management mechanisms

At the beginning of treatment, patients should be particularly careful when driving vehicles and other potentially dangerous activities.

Overdose

Symptoms: increase in heart rate, decrease in blood pressure, predisposition to collapse, impairment of renal function, urinary incontinence, drowsiness, anxiety, hallucinations, in severe cases – epileptiform seizures (elderly patients). A large overdose can cause tonic clonic seizures. Allergic reactions.

Treatment: symptomatic therapy. To treat seizures recommended benzodiazepines. Spetsificheskiy no known antidote. Information about the possible breeding bentsiklana by dialysis there.

Drug Interactions

In an application Halidorum^® dampening effect on the central nervous system of means for anesthesia and sedation.

In an application Halidorum^® with sympathomimetics increases the risk of tachycardia, atrial and ventricular tachyarrhythmias.

In an application Halidorum^® and preparations, reducing the potassium level in the blood (incl. Diuretic, cardiac glycosides), quinidine and possible effects summation proaritmogennoe.

In an application Halidorum^® with digitalis drugs increases risk of arrhythmia in overdose of cardiac glycosides.

In an application Halidorum^® with beta-blockers may need dose adjustment of beta-blocker due to opposition chronotropic effects (have a negative beta-blockers and have a positive bentsiklana).

In an application Halidorum^® with calcium channel blockers and other antihypertensive agents may increase their effect.

In an application Halidorum^® medicine, causing side effects such as spazmofilii, possible summation of these effects.

In an application Halidorum^® acetylsalicylic acid may increase the inhibition of platelet aggregation.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at temperature from 15 ° to 25 ° C. Shelf life Tablets – 5 years. Shelf-life solution for injection – 3 year.