Halidor (Halidor) - a drug belonging to the group of myotropic antispasmodics.
Halidor is the proprietary name of the drug. The active ingredient in it is Bencyclan fumarate (Bencyclani fumaras). Chemical name: N, N-dimethyl-3 - ((1-benzylcycloheptyl) oxy) -1-propanamine fumarate. Formula: C 23 H 35 NO 5. In appearance, it is a white crystalline powder, odorless, poorly soluble in water, and well soluble in ethyl alcohol.
Mechanism of action
The pharmacological value of this drug is due to its antispasmodic and vasodilation effect - the ability to relax the smooth muscles of internal organs and expand the lumen of blood vessels. These effects are achieved through several physiological mechanisms.
Under the influence of Bencyclane, the so-called. calcium channels. Through these channels, which look like receptors on the surface of the cell membrane, active transport of calcium ions is carried out into the cell. Calcium plays a key role in promoting muscle contraction.
When the cells of muscle fibers (myofibrils) enter the cytoplasm, it activates motor or motor proteins - actin and myosin. With the participation of calcium, these proteins form an actomyosin complex among themselves, which triggers the process of muscle contraction.
The blockade of calcium channels by Halidor prevents the entry of calcium into the cell, which leads to relaxation of smooth muscle fibers.
In addition, Halidor has an antiserotonin effect. Serotonin is a biologically active substance belonging to the group of neurotransmitters.
It is secreted by serotoninergic neurons located in the central nervous system - in the brain stem and in the spinal cord. Among the variety of effects of serotonin are vascular spasm and increased blood pressure. The inhibition of Serotonin by Bencyclan prevents the development of these effects.
Bencyclan has a direct blocking effect on the sympathetic ganglia - the nodal clusters of neurons in the thoracic sympathetic trunk.
Under the influence of sympathetic impulses, vascular spasm also develops. In addition, Bencyclan inhibits the activity of sodium-potassium-dependent ATPase, which ensures the transport of sodium outside the cell and potassium into the cell.
The movement of sodium and potassium ions in this case is carried out against the concentration gradient, which requires energy consumption. The source of energy in this case is ATP molecules.
This process is usually referred to as a sodium-potassium pump. Thanks to the sodium-potassium pump and the difference in the concentrations of various ions supported by it, the so-called transmembrane potential is formed on both sides of the cell membrane - the magnitude of the electrical activity of the cell membrane.
Due to the change in the transmembrane potential in different parts of the nerve fiber, the passage of the nerve impulse along this fiber is ensured. Inhibition of sodium-potassium-dependent ATP-ase changes the characteristics of the cellular potential.
This is an additional mechanism for the implementation of the vasodilation and spasmolytic action of Galidor. Other properties of Galidor are also associated with this mechanism.
Under the action of this drug, the elasticity of erythrocytes improves and the adhesion and aggregation (gluing, formation of conglomerates) of erythrocytes and platelets becomes difficult. As a result, the rheology (fluidity) of the blood is improved.
Thrombus formation and associated ischemia (insufficient blood supply to tissues) are prevented. Red blood cells pass more easily through capillaries with a small diameter.
Oxygen transport to hard-to-reach areas is facilitated. In addition, there is evidence that Halidor improves the utilization of glucose in tissues and has mild local anesthetic properties. From all this it follows that Halidor has a complex effect on the human body.
It relaxes the smooth muscles of the internal organs of the gastrointestinal tract, respiratory and genitourinary systems. And dilatation of blood vessels and improvement of rheological properties of blood improves blood supply to the brain and peripheral tissues.
History of creation
The drug was synthesized over 40 years ago in the laboratory of the EGIS pharmaceutical plant in Hungary. Initially, the new drug was named EGIT-201.
Subsequently, the serial production of Galidor was established, which was exported to various countries, incl. and to the Soviet Union. At present, OJSC Pharmaceutical Plant EGIS continues to produce Galidor, which, in addition to the Russian Federation, is used in 50 more countries. 
Production technology
Bencyclane in the form of a fumarate salt is obtained in several sequential organic synthesis reactions. Subsequently, depending on the required dosage form, crystals of Bencyclane fumarate are dried and pressed into tablet forms, or a sterile solution is prepared from them.
Release forms
- 100 mg tablets;
- Ampoules 2 ml - 2.5% solution.
Galidor, produced by JSC EGIS, has no synonyms. But in clinical practice, other myotropic antispasmodics are also used. Perhaps this is the most diverse drug group. No-shpa, Duspatalin, Meverin, Papaverin,
Platyphylline is just a small part of a long list of antispasmodics. And this list is updated every day with more and more new drugs. However, the active substance in them is not Bencyclan, but completely different compounds. And in terms of the mechanism of action, they can differ significantly from Galidor.
Indications
- Atherosclerotic and spastic diseases of the cerebral vessels, incl. and disorders of cerebral circulation.
- Peripheral circulatory disorders after injuries and operations, as well as Raynaud's disease, arteritis obliterans.
- Diseases of the gastrointestinal tract, accompanied by spasm and increased peristalsis: dyskinesia of the esophagus, stomach, duodenum 12, large intestine. Peptic ulcer and 12 duodenal ulcer, cholecystitis, cholelithiasis, spastic colitis.
- Diseases of the urinary system: spasms of smooth muscles of the bladder, urolithiasis, renal colic.
- Bronchial asthma, bronchospastic syndrome in other conditions.
Dosage
In case of vascular pathology, the drug is taken orally at 100 mg (1 tablet) 3 times a day. The maximum daily dose for internal administration is 400 mg.
When combined with drugs that cause hypokalemia (a decrease in the content of potassium in the blood plasma), inhibiting myocardial contractility, and cardiac glycosides, the daily dose of the drug should not exceed 200 mg.
The course of therapy is 2-3 months. Subsequently, after the same period of time, the course is repeated. The drug can be administered intravenously. For intravenous infusions, Halidor is used 2 times a day. 100 mg (4 ml, 2 ampoules) are dissolved in 100 or 200 ml of saline, and injected intravenously over 1 hour.
To eliminate vascular spasm in diseases of internal organs, the drug is prescribed in 100-200 mg (1-2 tablets) 2 times a day, or 100 mg 3 times a day.
After 3-4 weeks, they switch to a maintenance dose of 100 mg 1-2 times a day. If it is necessary to urgently eliminate the vascular spasm, the drug is administered intramuscularly or intravenously. For intramuscular administration, the drug is injected in 2 ml (1 ampoule), and for intravenous administration, slowly in 4-8 ml (4-8 ampoules), previously dissolved in 20 ml of saline.
When administered intravenously, Halidor can cause thrombophlebitis. Therefore, it is advisable to change the injection site. The duration of parenteral administration should not exceed 2-3 weeks, after which it is recommended to switch to internal medication. Parenteral administration of Galidor is not recommended for patients with cardiovascular and respiratory failure.
Pharmacodynamics
The drug is rapidly absorbed into the digestive tract. The maximum concentration in blood plasma when taken internally is 2-8 hours (on average - 3 hours). Bioavailability of Halidor is 25-35%.
In blood plasma, 20% of Halidor remains unchanged, 30-40% binds to plasma proteins, 30% - to erythrocytes, and 10% - to platelets.
Part of the drug is metabolized in the liver by dealkylation and breaking of ether bonds. 2-3% of Halidor is excreted unchanged through the kidneys, the rest is in the form of metabolites, some of which are conjugated with glucuronic acid. The half-life of Halidor is 6-10 hours.
Side effects
- Gastrointestinal tract: nausea, vomiting, dry mouth, abdominal pain, an increase in the level of transaminase enzymes in the blood plasma;
- Cardiovascular system: tachycardia, some types of tachyarrhythmias;
- CNS: headache, dizziness, general weakness, tremor of the extremities, sleep disturbances, memory disturbances, gait changes, rarely - transient disturbances of consciousness, hallucinations, epileptiform seizures;
- Blood: leukopenia;
- Metabolism: an increase in body weight;
- Skin: Allergic rash with itching.
Contraindications
- Decompensated heart failure;
- Severe respiratory distress;
- Severe renal and hepatic impairment;
- TBI (traumatic brain injury), suffered during the last year;
- Recent hemorrhagic stroke;
- Atrioventricular block;
- Acute myocardial infarction;
- Epilepsy and other convulsive conditions;
- Age under 18.
Instructions
Halidor (in Latin - Halidor) is an antispasmodic agent used for the symptomatic treatment of diseases accompanied by spasms and pain. It has a number of contraindications, so a doctor's appointment is required.
Halidor (in Latin - Halidor) is an antispasmodic agent used for the symptomatic treatment of diseases accompanied by spasms and pain.
Composition and action
The composition of the medicinal product includes:
- bencyclane fumarate (50 or 100 mg);
- rice starch;
- polyvinyl acetate;
- magnesium stearate;
- carboxymethyl starch;
- dehydrated silicon dioxide;
- talc;
- sodium chloride.
The active substance has the following properties:
- Expands peripheral vessels. This action is attributed to the ability to block calcium channels, inhibit serotonin production, and block sympathetic ganglia.
- Does not increase blood pressure.
- Suppresses the synthesis of Na / K-dependent ATPase, prevents the adhesion of platelets and red blood cells, increases the elasticity of red blood cells. These actions are manifested in the capillaries, coronary and cerebral arteries.
- Has a mild analgesic effect.
Release form
The drug is available as:
- Tablets for oral use. They are round and white in color. Covered with enteric film. Packed in plastic bottles. The cardboard box contains 1 bottle and instructions for use.
- Solution for intramuscular and intravenous administration. Presented by a clear, colorless, odorless liquid. It is bottled in 2 ml ampoules, which are packaged in cardboard boxes of 10 pcs.
Pharmacological properties of the drug Halidor
Pharmacological action - antispasmodic, vasodilator.
Pharmacodynamics
When taken orally, the active substance is rapidly absorbed by the intestinal walls. The maximum concentration of bencyclane in the blood is reached after 4 hours. 30% of the active substance interacts with plasma proteins.
Pharmacokinetics
The transformation of the active substance into metabolites takes place in the liver. As a result of dealkylation, demethylated compounds are formed. The destruction of the ester bond is accompanied by the release of benzoic acid. Subsequently, it is converted into hippuric acid. Most of the active ingredient is excreted by the kidneys as a metabolite. 2% of bencyclane leaves the body unchanged. The half-life lasts 8 hours.
Indications for use
Indications for the use of Galidor are:
- acute disturbance of cerebral circulation in atherosclerosis and spasm of the arteries of the brain (as part of complex therapeutic regimens);
- obliterating pathologies of peripheral vessels of various origins;
- vascular diseases arising after surgery;
- chronic gastritis, gastric ulcer and duodenal ulcer;
- spastic dyskinesia of the esophagus and stomach;
- spasm of the bile ducts;
- intestinal disorders, accompanied by inflammation, pain and false urge to defecate;
- pain syndrome that occurs after removal of the gallbladder;
- chronic pancreatitis;
- acute and sluggish prostatitis, accompanied by impaired urination;
- multiple sclerosis.
Urolithiasis
The drug for urolithiasis is used to eliminate pain and facilitate the release of stones in the acute stage.
With renal colic
For renal colic caused by a spasm of smooth muscles, Galidor's injections are used for emergency treatment. It is not recommended to use the drug as the only therapeutic agent.
How to take Galidor
Tablets
The dosage and the scheme of using the tablets depends on the type of pathology:
- Vascular diseases. The drug is taken at 100 mg 3 times a day. The maximum daily dose should not exceed 400 mg.
- Spasm of smooth muscles. Take 100-200 mg once. Do not drink more than 4 capsules per day. As a maintenance therapy, the drug is taken at 100 mg 3 times a day.
Solution
For vascular pathologies, the solution is administered using droppers. The average daily dose (200 mg) can be divided into 2 applications. 4 ml of the drug is diluted in 200 ml of saline. The drug is administered slowly, over 1-2 hours. To eliminate spasmodic pain syndrome, injections are given intramuscularly or intravenously. 2-4 ampoules are mixed with 10-20 ml of saline. 2 ml of the resulting mixture is injected deep into the gluteus muscle.
Before or after meals
How many days to take Galidor
The therapeutic course for vascular diseases is 60-90 days. The break between courses of treatment is 2-4 months. For muscle spasms, the medicine is taken for a month. The need to continue therapy depends on the nature of the course of the disease and the individual characteristics of the organism.
Contraindications
The drug is not used for:
- intolerance to the ingredients of the drug;
- respiratory diseases;
- supraventricular ventricular tachycardia;
- severe respiratory failure;
- acute heart failure;
- myocardial infarction.
Side effects
While taking an antispasmodic, the following undesirable consequences may occur:
- gastrointestinal disorders (dryness of the mucous membranes of the mouth, false feeling of fullness, nausea, vomiting, loose stools);
- neurological disorders (anxious thoughts, pain in the back of the head, impaired coordination of movements, confusion, hallucinations, insomnia, epileptic seizures);
- cardiovascular pathology (heart palpitations, heart rhythm disturbances);
- dysfunction of the hematopoietic system (thrombocytopenia, leukopenia, neutropenia);
- other side effects (weight gain, general weakness, allergic skin rashes).
Overdose
When taking high doses of the drug, heart rhythm disturbances, a drop in blood pressure, and urinary incontinence are observed. In rare cases, orthostatic collapse develops, epileptic seizures and tonic-clonic seizures occur. Treatment is supportive; there is no specific antidote.
special instructions
In some cases, the drug should be discarded. A dosage change is sometimes required.
Can i take during pregnancy and lactation?
The introduction of Halidor in the first 12 weeks of pregnancy is not recommended. In the 2-3 trimester, the drug is used in the presence of absolute indications.
If it is necessary to use an antispasmodic during lactation, breastfeeding is temporarily suspended.
Childhood use
The safety of bencyclane for the child's body has not been proven, therefore it is not prescribed for underage patients.
With impaired renal function
For violations of liver function
The drug is not prescribed for liver diseases.
Alcohol compatibility
Drinking alcohol during treatment can lead to increased side effects. Doctors do not recommend drinking alcoholic beverages while taking Galidor.
Drug interactions
Bencyclan increases the effectiveness of sedatives and pain relievers. The risk of arrhythmia increases with the combined administration of an antispasmodic and sympathomimetics. If it is necessary to take Halidor during treatment with beta-blockers, dose adjustment is required.
The drug enhances the effect of antihypertensive drugs.
Analogs
Cheaper drugs have a similar effect:
- Dibazol-Darnitsa;
- Enelbin 100;
- Papazol;
- Papaverine;
- Vinoxin.
Papaverine is one of the analogues of the drug.
Terms and conditions of storage
The tablets and solution are kept in a cool, dark place, protected from children. The shelf life of the tablet forms is 3 years, the solution is 5 years.
Galidor in its pharmacological group is an antispasmodic drug. The active ingredient is a bencyclan. The dosage form of the drug is a colorless, odorless, transparent solution intended for parenteral administration (both intravenous and intramuscularly).
Each ampoule contains 50 mg of the active substance bencyclane fumarate (concentration 25 mg / ml), excipients are represented by a physiological solution for parenteral dosage forms of 8 ml, water for injection 2 ml.
The release form of an ampoule with a volume of 2 ml has a break point and two rings (blue lower and yellow - upper).
Pharmacodynamically Halidor is an antispasmodic agent that combines, along with myotropic and vasodilatory effect.
Bencyclan acts antispasmodically on the visceral muscles of the internal organs - the gastrointestinal tract, genitourinary, and respiratory organs. The vasodilating effect of bencyclane is based on blocking calcium ion channels, as well as antiserotonin action and (to a lesser extent) with the possibility of blocking sympathetic ganglia. Also Halidor can increase the heart rate, as well as cause a slight tranquilizing effect.
The drug has a dose-dependent suppression of potassium-dependent ATPase, reduces the level of platelet and erythrocyte aggregation, and increases the elasticity of erythrocytes. It is observed mainly in the microvasculature of the peripheral circulation, coronary arteries and cerebral vessels.
Pharmacokinetically, the maximum concentration of Halidor in blood plasma is reached 2-7 hours (usually 3 hours) after application. Approximately 30% of the amount of Halidor binds to plasma proteins, 30% binds to erythrocytes, and 10% to platelets, the amount of free circulating fraction is 20% of the total amount.
Hepatic metabolism, mainly in two ways: dealkylation (with the formation of a demethylated derivative), as well as the breaking of the ester bond (the formation of benzoic acid with its subsequent transformation into hippuric acid). The main part of the administered dose of Halidor is excreted by the kidneys, mainly in the form of its metabolites, in unchanged form about 2-3%. Most of the metabolites (over 80%) are excreted in a free state, and a small part in conjugated with glucoronic acid.
The half-life is 6-10 hours and does not depend on the patient's age, and also does not decrease with suffering from the functions of the kidneys and liver. Total clearance is 40 L / h, renal clearance is less than 1 L / h.
Indications
Galidor is indicated for use in various neurological and vascular diseases.
- In cases of cerebrovascular diseases, Halidor is used as an integral part of complex treatment.
- Cases of peripheral vascular disease, such as, as well as chronic obliterating arterial vascular disease.
- The drug is prescribed in cases where there is a need to relieve spasm of internal organs. This is important for gastrointestinal diseases such as gastroenteritis of various origins (for example, infectious), infectious or inflammatory colitis, as well as functional diseases of the large intestine, tenesmus, flatulence after surgery. Halidor as an antispasmodic can be used for cholecystitis, cholelithiasis, after cholecystectomy, in cases of motor impairment with dyskinesia of the sphincter of Oddi.
- Halidor is indicated for spasms and tenesmus of the bladder as a concomitant agent in the treatment of urolithiasis (should be combined with analgesics for renal colic).
- It is used as a tool for preparing for diagnostic instrumental studies.
Contraindications
The drug has a number of contraindications. These include hypersensitivity to bencyclane, cases of severe respiratory, renal, heart and hepatic failure, existing atrioventricular block or acute myocardial infarction.
Halidor is not used in the case of epilepsy, other forms of spasmophilia, as well as in patients with hemorrhagic stroke or severe traumatic brain injury suffered over the past year.
Due to the lack of reliable studies on the use of Halidor in pregnant and lactating women, the appointment of Halidor is not recommended in the first trimester of pregnancy. At the time of breastfeeding, it is also advisable to abandon the use, or stop breastfeeding for the entire duration of treatment.
Mode of application
Halidor's solution is intended for intravenous infusion (after dilution), and can also be used intramuscularly. For vascular diseases, Halidor's solution is prescribed in a daily dose of 200 mg, usually the dose is divided into 2 infusions. 100 mg of Halidor is diluted in 200 ml of saline.
To eliminate spasm of internal organs, in acute cases, the drug is injected into the vein slowly in the amount of 2-4 ampoules (4-8 ml) of the drug diluted with saline solution up to 10 ml, or deeply intramuscularly 2 ml.
The course of treatment lasts 2-3 weeks, then, if necessary, it is recommended that the patient be transferred to Galidor in tablet form.
Side effects
Side effects from the gastrointestinal tract can be manifested by abdominal pain, a feeling of fullness, nausea, and vomiting. From the side of the central nervous system: anxiety, dizziness, gait disturbance, tremor, headache, insomnia, hallucinations may very rarely develop.
There may be cases of tachyarrhythmia (ventricular or atrial, development is significantly more frequent when used together with other proarrhythmogenic drugs).
Other side effects can be expressed in a state of general malaise, an increase in body weight, in allergic reactions, transient increases in the activity of ASAT, ALAT, as well as a decrease in the number of leukocytes, there is rarely a likelihood of thrombophlebitis with intravenous administration.
Overdose
Galidor overdose is rare. Symptoms in case of overdose: tachycardia, drop in blood pressure, drowsiness, urinary incontinence, with severe overdose, epileptiform seizures are possible.
Due to the lack of a specific antidote, symptomatic therapy is used in cases of overdose. Benzodiazepines are indicated for the relief of seizures. The effectiveness of dialysis in case of a benzyclane overdose is questionable, but reliable data are not available.
special instructions
In cases of joint use, caution is required when combining with a number of drugs. When using Halidor with anesthetics and sedatives, their effects can be dramatically increased.
Co-administration with sympathomimetics increases the risk of tachyarrhythmias. Diuretics and other drugs that lower the level of potassium in the blood can lead to the summation of proarrhythmogenic effects. Foxglove remedies, when taken together with bencyclan, also increase the risk of arrhythmias, but only in case of an overdose of the latter.
Beta-blockers have the opposite chronotropic effect (positive in Halidor and negative in the beta-blocker group), therefore, it may be necessary to select the dosage of the beta-blocker. Calcium channel blockers and other antihypertensive drugs, when used with Halidor, increase the risk of hypotensive reactions. When used with aspirin preparations, the degree of inhibition of platelet aggregation increases.
The injection sites must be periodically changed, since Halidor can cause endothelial vascular dysfunction at the injection site and thrombophlebitis.
Patients with severe cardiovascular and respiratory failure who are prone to collapse should refrain from injecting the drug. With prostatic hypertrophy and cases of urinary retention, the risk of urinary retention increases (since the degree of retention increases when the smooth muscles of the bladder relax).
With prolonged use of Galidor, it is required to regularly monitor laboratory parameters (at least once every 2 months). Due to the risk of side effects when taking Galidor, driving and performing potentially hazardous work is not indicated.
Storage conditions
Halidor is stored at room temperature, out of the reach of children. The shelf life is three years.
Analogs
There are no complete analogues of Galidor. Others with muscle relaxant effects may be relative analogs.
Price
Halidor is a prescription drug. Average prices for the drug are:
- Pack of 10 ampoules of 2 ml 510-615 rubles.
You can not engage in self-prescription and uncontrolled intake of medicines. Consult your doctor before using Halidor!
Halidor is an antispasmodic drug with a pronounced vasodilating pharmacological effect.
The main active ingredient is benziclan. When used, its cell membranes become more resistant to damage. In addition, the drug has a vasoconstrictor and antispasmodic effect on the muscle structures of the internal organs.
On this page you will find all the information about Galidor: full instructions for use for this drug, average prices in pharmacies, complete and incomplete analogues of the drug, as well as reviews of people who have already used Galidor. Want to leave your opinion? Please write in the comments.
Clinical and pharmacological group
Myotropic antispasmodic.
Terms of dispensing from pharmacies
Dispensed by prescription.
Prices
How much is Galidor worth? The average price in pharmacies is 650 rubles.
Release form and composition
Halidor is available in two dosage forms - a solution for parenteral administration (intramuscularly or intravenously) and tablets. The solution contains the main active ingredient of the drug bencyclane fumarate in the amount of 25 and 50 mg in 1 ampoule.
The Halidor solution is contained in 2 ml glass ampoules, which are packaged in a blister strip packaging of 10 pieces. The carton pack contains 1 or 5 blister packs with the appropriate number of ampoules and instructions for use of the drug.
Pharmacological effect
Myotropic antispasmodic with a pronounced vasodilating effect. The vasodilating 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. 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.
In addition, bencyclan has an antispasmodic effect on the visceral muscles (gastrointestinal tract, urinary tract, respiratory system). The drug causes a slight increase in heart rate. Its weak tranquilizing effect is also known.
Indications for use
Indications for the use of Galidor are vascular diseases:
- Cerebral circulation disorders: complex treatment of chronic and acute cerebral ischemia.
- Dysfunctions of peripheral vessels: Raynaud's syndrome and other diseases with vasospasm and acrocyanosis, chronic obliterating arterial diseases.
Also, Galidor is prescribed to eliminate spasm of internal organs:
- Urological syndromes: tenesmus and spasms of the bladder, adjuvant treatment of urolithiasis (together with analgesic drugs for renal colic).
- Gastrointestinal diseases: inflammatory and infectious, tenesmus, gastroenteritis of various origins, functional diseases of the large intestine, postoperative flatulence, condition after surgical removal of the gallbladder, or stomach (in combination therapy with other drugs).
An additional indication for the use of Halidor in the form of a solution for injection is preparation for cystoscopy, retrograde pyelography, cystography, urethrography and intravenous urography.
Contraindications
Among the contraindications to the use of the drug Halidor are: severe forms of respiratory, renal, hepatic and decompensated heart failure, myocardial infarction, ventricular tachycardia, epilepsy, hemorrhagic stroke, traumatic brain injury (suffered during the last year), age up to 18 years.
Application during pregnancy and lactation
Preclinical data did not reveal any embryotoxic or teratogenic effects.
Despite the absence of embryotoxic effects with widespread use of the drug, its administration to patients in the first trimester of pregnancy is not recommended. In the absence of reliable data from human studies, the use of this drug during breastfeeding requires careful analysis.
Instructions for use
The instructions for use indicate that Halidor in tablet form should be taken orally. In the form of a solution - in the form of intravenous injections or infusions and deep intramuscular injections.
Dosage to relieve spasm of internal organs:
- Inside Galidor 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 intravenously slowly at a dose of 100-200 mg (4-8 ml) or intramuscularly in a deep dose of 50 mg (2 ml). Before intravenous administration, the required amount of solution is 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 take the drug Halidor inside.
- Inside Galidor is prescribed 100 mg 3 times / day for 2-3 months. The maximum daily oral dose is 400 mg. The interval between courses is 2-3 months.
- The drug can also be used as an intravenous infusion 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 intravenously for 1 hour 2 times / day.
The doctor prescribes the course of treatment and the dosage form of the drug individually, taking into account clinical indications and the patient's condition.
Side effects
When using the drug Halidor, the following side effects are possible: general malaise, dizziness, headache, dry mouth, nausea, vomiting, decreased (or increased) appetite, abdominal pain, diarrhea, tremors, sleep disturbances.
Also, memory disorders similar to epileptic seizures, heart rhythm disturbances, weight gain, and a decrease in the level of leukocytes in the blood (leukopenia) are possible. Therefore, long-term use of the drug is necessary under the control of blood composition.
While undergoing treatment with Halidor, one should also take into account the possibility of a negative effect of this drug on the ability to drive a car and potentially dangerous mechanisms.
Overdose
Overdose can cause increased heart rate, lower blood pressure, a tendency to collapse, urinary incontinence, drowsiness, anxiety, and in severe cases, epileptiform seizures.
Overdose Treatment: No specific antidote known. In case of an overdose, the stomach should be flushed and symptomatic treatment should be taken. Benzodiazepines are recommended for the treatment of seizures. There are no data on the possible elimination of bencyclane by dialysis.
special instructions
The use of the drug for use in the form of injections requires a change in the injection sites, since there is a risk of the drug breaking the integrity of the vascular endothelium. When using Halidor with drugs that can cause hypokalemia, suppression of myocardial function or taking cardiac glycosides, it is necessary to reduce its dose per day to 150-200 mg.
- retention of urine;
- hypertrophy of the prostate;
- having a tendency to collapse;
- severe cardiovascular insufficiency;
- respiratory failure in severe form.
Long-term use of Galidor should be accompanied by regular blood tests (every 2 months). People involved in hazardous work and transport drivers should be careful when using Halidor at the beginning of treatment.
The medicine can enhance the effects of sedatives and general anesthetics. You should use them carefully at the same time.
Drug interactions
When Halidor is prescribed simultaneously with cardiac glycosides, drugs that cause hypokalemia or inhibit myocardial function, the daily dose of the drug should be in the range of 150-200 mg.
Myotropic antispasmodic with a pronounced vasodilating effect.
Preparation: GALIDOR®
The active substance of the drug:
bencyclane
ATX encoding: C04AX11
KFG: Myotropic antispasmodic
Registration number: P No. 012430/01
Date of registration: 29.12.06
Owner reg. ID: EGIS PHARMACEUTICALS Plc (Hungary)
Galidor release form, drug packaging and composition.
Tablets
1 tab.
bencyclane fumarate
100 mg
Excipients: carbomer 934 P, anhydrous colloidal silicon dioxide, magnesium stearate, polyvinyl acetate, sodium amylopectin glycolate (type A), starch, talc.
50 pcs. - dark glass bottles (1) - cardboard boxes.
Transparent, colorless, odorless.
1 ml
1 amp.
bencyclane fumarate
25 mg
50 mg
Excipients: sodium chloride, water d / i.
2 ml - ampoules (5) - contoured cell packs (2) - cardboard packs.
2 ml - ampoules (5) - contoured cell packaging (10) - cardboard boxes.
The description of the product is based on the officially approved instructions for use.
Pharmacological action Galidor
Myotropic antispasmodic with a pronounced vasodilating effect. The vasodilating 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. Does not cause stealing syndrome, practically does not affect blood pressure. 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. Possesses antiplatelet properties and poorly expressed local anesthetic activity.
In addition, bencyclan reduces the tone and motor activity of the smooth muscles of the internal organs (gastrointestinal tract, urinary tract, respiratory system).
The drug causes a slight increase in heart rate. Its weak tranquilizing effect is also known.
Pharmacokinetics of the drug.
Suction
After taking the drug inside, bencyclan is absorbed from the digestive tract quickly and almost completely. Cmax in blood plasma is reached 2-8 hours (usually 3 hours) after oral administration. Due to the effect of "first pass" through the liver, the bioavailability of the drug after oral administration is 25-35%.
Distribution
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
Metabolism is carried out in the liver, mainly in two ways: dealkylation gives a demethylated derivative, cleavage of the ether bond gives benzoic acid, which is further converted into hippuric acid.
Withdrawal
T1 / 2 is 6-10 hours. It is excreted mainly in the urine (97%) in the form of inactive metabolites, but also unchanged (2-3%). Most of the metabolites (90%) are excreted in unconjugated form, and a small part is excreted in conjugated form (approximately 50% as a conjugate with glucuronic acid). Total clearance is 40 L / h, renal clearance is less than 1 L / h.
Pharmacokinetics of the drug.
in special clinical cases
T1 / 2 does not change in elderly patients, as well as in impaired renal and liver function.
Indications for use:
Tablets
Cerebral circulation disorders in cerebrovascular diseases of atherosclerotic and angiospastic genesis (in complex therapy);
Vascular diseases of the eyes (including occlusion of the central retinal artery, diabetic angiopathy);
Obliterating diseases of peripheral arteries of various origins, angioedema, postoperative and post-traumatic circulatory disorders;
Peptic ulcer and duodenal ulcer and other diseases of the gastrointestinal tract, accompanied by spastic or hypermotor dyskinesia of the esophagus, stomach, biliary tract, intestine (gastritis, enteritis, colitis, tenesmus, cholecystopathy, cholelithiasis, postcholecystectomy syndrome);
Urinary tract spasms, adjuvant therapy for urolithiasis.
Solution for i / v and i / m administration
Diseases of peripheral vessels (including Raynaud's disease, other diseases with acrocyanosis and vascular spasm, chronic obliterating arterial diseases);
Diseases of cerebral vessels (in the complex therapy of acute and chronic cerebral ischemia).
To eliminate spasm of internal organs
Gastroenteritis of various etiologies (especially infectious), infectious colitis, functional diseases of the large intestine, tenesmus, postoperative flatulence, cholecystitis, cholelithiasis, condition after cholecystectomy, motility disorders with dyskinesia of the sphincter of Oddi, stomach ulcer or duodenal ulcer (in combination with other drugs) ;
Spasms and tenesmus of the bladder, concomitant therapy of urolithiasis (in combination with analgesics for renal colic), preparation for instrumental research methods.
Dosage and method of administration of the drug.
Inside Galidor is prescribed 100-200 mg (1-2 tablets) 1-2 times / day for 3-4 weeks, then they switch to maintenance therapy at 100 mg 2 times / day.
The maximum daily oral dose is 400 mg.
Parenterally, the drug is administered intravenously by jet (after dilution) or by infusion.
In case of vascular diseases, the drug can be used by infusion 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 intravenously for 1 hour 2 times / day.
To eliminate spasm of internal organs in acute cases, Halidor is injected intravenously in a jet slowly at a dose of 100-200 mg (4-8 ml) or deep intramuscularly at a dose of 50 mg (2 ml). Before intravenous administration, the required amount of solution is diluted with isotonic sodium chloride solution to 10-20 ml. The course of treatment is 2-3 weeks, followed by the transfer of the patient, if necessary, to take the drug Halidor inside.
Side effect of Galidor:
From the digestive system: dry mouth, abdominal pain, satiety, nausea, vomiting, loss of appetite, diarrhea, increased activity of hepatic transaminases in the blood serum.
From the side of the central nervous system: anxiety, dizziness, headache, gait disturbance, tremors, sleep disturbances, insomnia, memory disorders; rarely - transient confused state of consciousness, epileptiform seizures, hallucinations in elderly patients; in isolated cases - symptoms of focal lesions of the central nervous system.
On the part of the cardiovascular system: tachycardia; sometimes - atrial and ventricular tachyarrhythmias (especially when administered together with other proarrhythmogenic drugs).
From the hematopoietic system: leukopenia.
Others: general malaise, weakness, weight gain, allergic reactions; rarely - thrombophlebitis with intravenous injection.
Contraindications to the drug:
Pregnancy;
Lactation (breastfeeding) period;
Hypersensitivity to drug components.
Tablets
Renal failure;
Liver dysfunction;
Respiratory failure;
Paroxysmal supraventricular or acute ventricular tachycardia;
Children and adolescents up to 18 years of age (insufficient experience of use).
Solution for i / v and i / m administration
Severe respiratory distress;
Severe renal impairment;
Severe liver failure;
Decompensated heart failure;
Acute myocardial infarction;
AV block;
Recently suffered hemorrhagic stroke;
Epilepsy and other forms of spasmophilia;
Traumatic brain injury (within the last 12 months).
Application during pregnancy and lactation.
Sufficient reliable studies on the use of the drug Halidor during pregnancy and lactation in humans have not been conducted. Therefore, the introduction of the drug in the first trimester of pregnancy is not recommended.
During lactation, you should also refrain from prescribing the drug, or decide on the termination of breastfeeding during treatment.
Preclinical data did not reveal any embryotoxic or teratogenic effects.
Special instructions for the use of Galidor.
With the simultaneous appointment of Halidor with drugs that cause hypokalemia (diuretics, antihypertensive drugs); cardiac glycosides; drugs that inhibit myocardial function (beta-blockers, quinidine), the daily dose of Halidor should not exceed 150-200 mg.
In case of parenteral administration, the injection sites should be changed. 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).
If a solution of the drug gets under the skin, a local inflammatory tissue reaction is observed.
Control of laboratory parameters
With long-term course use of Halidor, it is recommended to systematically (at least 1 time in 2 months) conduct a general blood test (counting blood cells).
Influence on the ability to drive vehicles and use mechanisms
During the treatment period, care should be taken when driving vehicles and performing other potentially hazardous activities.
Drug overdose:
Symptoms: an increase in heart rate, a decrease in blood pressure, a predisposition to collapse, impaired renal function, urinary incontinence, drowsiness, anxiety, hallucinations, in severe cases, epileptiform seizures (in elderly patients). A significant overdose can cause tonic and clonic seizures. Allergic reactions.
Treatment: carrying out symptomatic therapy. Benzodiazepines are recommended for the treatment of seizures. No specific antidote is known. There are no data on the possible elimination of bencyclane by dialysis.
Interaction of Halidor with other drugs.
With the simultaneous use of Halidor enhances the depressing effect on the central nervous system of drugs 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), the summation of proarrhythmogenic effects is possible.
With the simultaneous use of Halidor with digitalis preparations, the risk of arrhythmia increases with an overdose of cardiac glycosides.
With the simultaneous use of Halidor with beta-blockers, it may be necessary to select a dose of a beta-blocker due to the opposite chronotropic effects (negative for beta-blockers and positive for bencyclane).
Use Halidor with caution at the same time as quinidine, which weakens the force of heart contractions.
With the simultaneous use of Halidor with calcium channel blockers and other antihypertensive drugs, their effect may be enhanced.
With the simultaneous use of Halidor with drugs that cause side effects in the form of spasmophilia, the summation of these effects is possible.
With the simultaneous use of Halidor with acetylsalicylic acid, an increase in the inhibition of platelet aggregation is possible.
Conditions of sale in pharmacies.
The drug is available by prescription.
Terms of storage conditions of the drug Halidor.
The drug should be stored out of the reach of children at a temperature of 15 ° to 25 ° C. The shelf life of the tablets is 5 years. The shelf life of the solution for injection is 3 years.
