Pharmacological properties
Pharmacodynamics.
drotaverine, an isoquinoline derivative, has an antispasmodic effect on smooth muscles by inhibiting the action of the PDE IV enzyme, which leads to an increase in the concentration of camp and, due to the inactivation of myosin light chain kinase (mlck), leads to relaxation of smooth muscles. In vitro, drotaverine inhibits the action of the PDE IV enzyme and inhibits PDE III and V isoenzymes. PDE IV is of great functional importance for reducing the contractile activity of smooth muscles, therefore selective inhibitors of this enzyme may be useful for the treatment of patients with diseases that are accompanied by hypermobility, as well as various diseases that cause gastrointestinal spasms.
In the smooth muscle cells of the myocardium and blood vessels, cAMP is hydrolyzed mainly by the PDE III isoenzyme, therefore drotaverine is an effective antispasmodic agent, does not cause significant side effects on the cardiovascular system and does not have a pronounced therapeutic effect on this system.
Drotaverine is effective against smooth muscle spasms of both nervous and muscular origin. Drotaverine acts on the smooth muscles of the digestive, biliary, genitourinary and vascular systems, regardless of the type of their autonomous innervation. The product increases blood circulation in tissues due to its ability to dilate blood vessels.
The effect of drotaverine is stronger than that of papaverine, absorption is faster and more complete, it binds less to blood plasma proteins. The advantage of drotaverine is also that, unlike papaverine, after its parenteral administration there is no such side effect as stimulation of respiration.
Pharmacokinetics. Drotaverine is quickly and completely absorbed after oral administration. In many ways (95–98%) binds to blood plasma proteins, especially albumin, gamma and beta globulins. Cmax in the blood after oral administration is achieved within 45–60 minutes. After primary metabolism, 65% of the dose taken enters the bloodstream unchanged. Metabolized in the liver. T½ is 8–10 hours. Within 72 hours, drotaverine is almost completely eliminated from the body, more than 50% is excreted in the urine, 30% in feces. Drotaverine is mainly excreted in the form of metabolites and is not detected unchanged in the urine.
Drotaverine solution for IV and IM administration 20 mg/ml in 2 ml ampoules No. 10
Name
Drotaverina-Borimed solution 2% 2ml No. 10
Description
Transparent liquid from yellow to yellowish-green. The presence of the smell of acetic acid is allowed.
Compound
One ampoule (2 ml of solution) contains: active substance – drotaverine hydrochloride – 40 mg; excipients: sodium metabisulfite, sodium acetate trihydrate, glacial acetic acid, ethyl alcohol, water for injection.
Pharmacotherapeutic group
A drug for the treatment of functional disorders of the gastrointestinal tract. Papaverine and its derivatives. ATX code: A03AD02.
Pharmacological properties
Pharmacodynamics Drotaverine is an isoquinoline derivative that exhibits an antispasmodic effect on smooth muscle by inhibiting the enzyme phosphodiesterase IV (PDE IV). Inhibition of the enzyme phosphodiesterase IV results in increased concentrations of cAMP, which inactivates myosin light chain kinase (MLCK), which in turn leads to smooth muscle relaxation. Drotaverine inhibits the PDE IV enzyme without inhibiting the PDE III and PDE V isoenzymes. PDE IV is functionally very important in reducing smooth muscle contractility and selective PDE IV inhibitors may be useful in the treatment of hyperkinetic diseases and various conditions associated with spastic conditions of the gastrointestinal tract. The enzyme that hydrolyzes cAMP in myocardial and vascular smooth muscle cells is mainly an isoenzyme of PDE III, which explains why drotaverine is an effective antispasmodic agent without serious cardiovascular side effects and pronounced effects on the cardiovascular system. Drotaverine is effective for smooth muscle spasms caused by disturbances in nervous regulation and self-regulation of both nervous and muscular etiologies. Regardless of the type of autonomic innervation, drotaverine acts on smooth muscles located in the gastrointestinal, biliary, urogenital and vascular systems. Thanks to its vasodilating effect, it improves tissue blood circulation. The effect of drotaverine is stronger than that of papaverine, and absorption is faster and more complete; it binds less to plasma proteins. The advantage of drotaverine is that it does not have a stimulating effect on the respiratory system, which was observed after parenteral administration of papaverine. Pharmacokinetics Drotaverine is rapidly and completely absorbed both after oral administration and after parenteral administration. It binds to a high degree (95–98%) to plasma proteins, especially albumin, gamma and beta globulins. After primary metabolism, 65% of the administered dose enters the bloodstream unchanged. Peak serum levels after oral administration are achieved within 45–60 minutes. Metabolized in the liver. The biological half-life is 8–10 hours. Within 72 hours, drotaverine is almost completely eliminated from the body, more than 50% is excreted in the urine, 30% in feces. Drotaverine is mainly excreted in the form of metabolites and is not found unchanged in the urine.
Indications for use
- spasms of smooth muscles associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;
- spasms of smooth muscles of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder tenesmus.
As an adjuvant therapy (when the tablet form cannot be used):
- for spasms of smooth muscles of the gastrointestinal tract: peptic ulcer of the stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis, colitis;
- for gynecological diseases: dysmenorrhea.
Contraindications
Hypersensitivity to the active substance or to any of the excipients of the drug (especially sodium methyl bisulfite), severe hepatic, renal or heart failure (low cardiac output syndrome), childhood.
Precautionary measures
Caution should be used in case of arterial hypotension, severe atherosclerosis of the coronary arteries, and during pregnancy. When administering drotaverine intravenously, due to the risk of collapse, the patient must lie down! In case of hypersensitivity to sodium methyl bisulfite, parenteral use of the drug should be avoided. This medicine contains sodium methyl bisulfite, which may cause allergic-type reactions, including anaphylactic shock and bronchospasm in sensitive individuals, especially those with a history of asthma or allergic diseases. Clinical studies on the use of the drug in children have not been conducted.
Pregnancy, breastfeeding and fertility
Parenteral use of drotaverine during pregnancy does not lead to teratogenic and embryotoxic effects. However, caution is required when prescribing the drug during pregnancy. Drotaverine should not be used during childbirth. Due to the lack of necessary clinical data, it is not recommended to prescribe during breastfeeding. There are no data on the effect of the drug on fertility.
Impact on the ability to drive vehicles or other machinery
After parenteral, and especially intravenous, administration of the drug, patients are advised to refrain from driving vehicles and engaging in potentially hazardous activities that require quick physical and mental reactions.
Directions for use and doses
The average daily dose for adults is 40–240 mg drotaverine hydrochloride (divided into 1–3 administrations per day) intramuscularly. For acute colic (cholelithiasis and urolithiasis) - 40–80 mg (2–4 ml of the drug) slowly intravenously.
Side effect
If adverse reactions occur, you should consult a doctor. The assessment of undesirable effects is based on the following data on the frequency of occurrence: very often (?1/10), often (?1/100 to
Interaction with other drugs
Drotaverine may weaken the antiparkinsonian effect of levodopa. Drotaverine enhances the effect of papaverine, bendazole and other antispasmodics (including m-anticholinergics). When tricyclic antidepressants, quinidine and procainamide are used simultaneously with drotaverine, the hypotensive effect is enhanced. Drotaverine reduces the spasmogenic activity of morphine. Phenobarbital increases the severity of the antispasmodic effect of drotaverine.
Overdose
Symptoms: In high doses, it can cause cardiac arrhythmia and conduction disturbances, including complete bundle branch block and cardiac arrest, which can be fatal. Treatment: observation, symptomatic and supportive treatment.
Package
2 ml in glass ampoules. 10 ampoules along with instructions for medical use are placed in a cardboard box (No. 10). 10 ampoules, together with instructions for medical use, are placed in a pack with a cardboard insert for fixing the ampoules (No. 10).
Storage conditions
In a place protected from light, at a temperature from 15? C to 25? C. Keep out of the reach of children.
Best before date
2 years. The medicine cannot be used after the expiration date.
Conditions for dispensing from pharmacies
On prescription.
Indications
For therapeutic purposes for smooth muscle spasms associated with diseases of the biliary tract (cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis); spasms of smooth muscles in diseases of the urinary tract (nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder tenesmus).
As an auxiliary treatment for spasms of smooth muscles of the gastrointestinal tract (stomach and duodenal ulcers, gastritis, cardio- and/or pylorospasm, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome accompanied by flatulence); tension headache; gynecological diseases (dysmenorrhea).
Drotaverine hydrochloride 40 mg No. 50 tab.
Instructions for medical use of the drug Drotaverine Trade name Drotaverine International nonproprietary name Drotaverine Dosage form Tablets 0.04 g Composition One tablet contains the active substance - drotaverine hydrochloride (in terms of 100% substance) - 0.04 g, excipients: lactose monohydrate ( milk sugar), potato starch, povidone (low molecular weight medical polyvinylpyrrolidone), magnesium stearate, talc. Description Tablets of yellow color with a greenish tint, flat-cylindrical with a chamfer. Pharmacotherapeutic group Drugs for the treatment of functional intestinal disorders. Papaverine and its derivatives. Drotaverine. ATC code A03AD02 Pharmacological action Pharmacokinetics When taken orally, absorption is high, half-absorption period is 12 minutes. Bioavailability - 100%. Evenly distributed in tissues, penetrates smooth muscle cells. Time to reach maximum concentration (TCmax) - 2 hours. Communication with blood plasma proteins - 95-98%. The half-life is 2.4 hours. It is mainly excreted by the kidneys, to a lesser extent - with bile. Does not penetrate the blood-brain barrier (BBB). Pharmacodynamics An antispasmodic agent from the group of isoquinoline derivatives, has a pronounced relaxing effect on the smooth muscles of internal organs and blood vessels. The mechanism of action is associated with inhibition of the enzyme phosphodiesterase type IV (PDE IV). Inhibition of PDE IV leads to the cessation of the destruction of cAMP and its accumulation inside the smooth muscle cell. In terms of chemical structure and pharmacological properties, it is close to papaverine, but has a stronger and longer-lasting effect. Reduces the tone and motor activity of the smooth muscles of internal organs, dilates blood vessels. In the smooth muscle cells of the myocardium and blood vessels, cAMP hydrolysis occurs mainly with the participation of the PDE III isoenzyme, which explains the high selectivity of the action of drotaverine as an antispasmodic in the absence of a pronounced therapeutic effect on the cardiovascular system and the development of serious cardiovascular adverse events. Indications for use - spasms of smooth muscles in diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis - spasms of smooth muscles of the urinary tract: nephrolithiasis, ureterolithiasis, pyelitis, cystitis, bladder tenesmus As an adjuvant therapy: - for spasms of smooth muscles muscles of the gastrointestinal tract: peptic ulcer of the stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis, colitis, spastic colitis with constipation and flatulence with irritable bowel syndrome - with tension headaches - with gynecological diseases: dysmenorrhea (painful menstruation) Method Applications and doses Adults are prescribed 0.04-0.08 g (1-2 tablets) orally 2-3 times a day. For children over 12 years of age, the drug is prescribed 0.04 g (1 tablet) 1-3 times a day. Side effects Possible - dizziness, headache, insomnia - palpitations, arterial hypotension - feeling of heat, sweating - nausea, constipation - allergic reactions: infrequently angioedema, urticaria, rash, itching Contraindications - hypersensitivity to drotaverine or to any excipient of the drug - severe renal or liver failure - severe heart failure (low cardiac output syndrome), AV block II-III degree - lactation period - lactose deficiency - galactosemia - impaired glucose/galactose absorption syndrome - children under 12 years of age Drug interactions With simultaneous use, drotaverine may weaken the antiparkinsonian effect of levodopa. When used simultaneously, it enhances the effect of papaverine, bendazole and other antispasmodics (including m-anticholinergics). When tricyclic antidepressants, quinidine and procainamide are used simultaneously with drotaverine, their hypotensive effect is enhanced. Special instructions Prescribe the drug with caution to patients with severe atherosclerosis of the coronary arteries, prostate adenoma, and glaucoma. Caution should be exercised when prescribing to patients with coronary vascular pathology and benign prostatic hyperplasia. Pregnancy Drotaverine does not have teratogenic or embryotoxic effects. However, the use of the drug is recommended only after carefully weighing the benefit-risk ratio in the mother and fetus. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms Considering the side effects, care should be taken when driving vehicles and potentially dangerous mechanisms. Overdose Symptoms: in large doses, it disrupts atrioventricular conduction, reduces the excitability of the heart muscle, and can cause cardiac arrest and paralysis of the respiratory center. Treatment: drug withdrawal, symptomatic therapy aimed at eliminating the resulting disorders. There is no specific antidote. Release form and packaging 10 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil. 2 or 5 blister packs with instructions for medical use in the state and Russian languages are placed in a cardboard pack. Storage conditions Store in a dry place, protected from light, at a temperature not exceeding 25 ºС. Keep out of the reach of children! Shelf life: 4 years Do not use after expiration date. Conditions for dispensing from pharmacies Without a prescription 623856, Sverdlovsk region, Irbit, st. Kirova, 172 Tel/fax (34355) 3-60-90 Name and country of the owner of the registration certificate OJSC “Irbitsky Chemical-Pharmaceutical Plant”, Russia Address of the organization receiving complaints from consumers regarding the quality of products (products) OJSC “Irbitsky Chemical and Pharmaceutical Plant” 623856, Sverdlovsk region, Irbit, st. Kirova, 172 Tel/fax (34355) 3-60-90 Email address
Application
Pills. apply the drug internally.
Adults: the average daily dose is 120–240 mg (3–6 tablets), divided into 2–3 doses.
Children aged 6–12 years: the maximum daily dose is 80 mg, divided into 2 doses.
Children over 12 years of age: the maximum daily dose is 160 mg, divided into 2–4 doses.
The duration of treatment is determined individually.
R-r. The drug is used for adults intramuscularly at a dose of 40–240 mg in 1–3 administrations.
For acute colic, the drug should be administered to adults intravenously slowly at a dose of 40–80 mg.
Side effects
Side effects that were observed during clinical studies and may have been caused by drotaverine are divided by organ system and frequency of occurrence: very common (1/10), common (1/100, 1/10), uncommon (1/1000, 1/100), rare (1/10,000, 1/1000), very rare (1/10,000).
From the gastrointestinal tract: rarely - nausea, vomiting, constipation.
From the nervous system: rarely - headache, dizziness, insomnia.
From the cardiovascular system: rarely - rapid heartbeat, arterial hypotension.
From the immune system: rarely - allergic reactions, including angioedema, urticaria, skin rashes, itching, skin flushing, fever, chills, increased body temperature, weakness.
The drug in the form of a solution contains metabisulfite, which can cause allergic reactions, including symptoms of anaphylactic shock and bronchospasm in sensitive patients, especially with a history of asthma or allergies.
General disorders: hypersensitivity reactions at the injection site.
special instructions
Use the drug with caution in case of arterial hypotension.
Excipients. Drotaverine-Darnitsa contains 64 mg of lactose, so patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use the drug.
Hypersensitivity reactions. Drotaverine is a histamine liberator drug and can cause non-allergic (false-allergic) reactions that do not have immunological mechanisms, but imitate allergic symptoms (the phenomenon of mimicry). They are usually associated with non-immune release of histamine, bradykinin, activation of complement, induction of leukotriene synthesis, which, in turn, induces bronchospasm and skin manifestations. The drug should be prescribed with caution to patients with allergic reactions or a history of asthma. If symptoms of a hypersensitivity reaction appear after taking drotaverine (rash, itching, swelling of the tissues of the upper respiratory tract), the drug should be immediately discontinued and appropriate therapy should be prescribed. If symptoms of angioedema or urticarial rash occur, oral antihistamines should be used.
If the patient is known to have asthma, an inhaled β2-agonist should be administered. It is necessary to monitor the patient's condition over the next 4 hours. If there is continuous vomiting and/or abdominal pain, the possibility of administering epinephrine intramuscularly should be considered.
When administering the drug intravenously, the patient should be in a horizontal position due to the risk of collapse.
Use the drug with caution in case of arterial hypotension.
Caution should be exercised when administering the drug parenterally to pregnant women (see Use during pregnancy and lactation).
The drug in the form of a solution contains metabisulfite, which can cause allergic reactions, including symptoms of anaphylactic shock and bronchospasm in sensitive patients, especially those with a history of asthma or allergies.
In case of hypersensitivity to sodium metabisulfite, parenteral administration of the drug should be avoided.
Use during pregnancy and lactation. As shown by the results of animal studies, oral administration of the drug did not cause any signs of any direct or indirect effect on pregnancy, embryonic development, childbirth or postpartum development. However, it is necessary to use the drug with caution during pregnancy. Do not use drotaverine during childbirth.
Due to the lack of relevant research data, use of the drug during breastfeeding is not recommended.
Children. The use of the drug is contraindicated for children under 6 years of age. The use of drotaverine in children has not been evaluated in clinical studies. The drug in solution form is not used in children.
The ability to influence reaction speed when driving vehicles or working with other mechanisms. If patients experience dizziness after using the drug, they should avoid potentially hazardous activities such as driving and performing tasks that require increased alertness. You should refrain from driving vehicles or operating other machinery while using (especially IV) the drug.
Drotaverine hydrochloride tablets 40 mg No. 10x2
Name
Drotaverine hydrochloride, tablets, 40 mg in container cells, 20 pcs.
Description
Transparent yellow with a greenish tint solution.
Main active ingredient
Drotaverine.
Release form
Solution.
Dosage
40 mg.
pharmachologic effect
Drotaverine is an isoquinoline derivative that exhibits an antispasmodic effect on smooth muscle by inhibiting the enzyme phosphodiesterase IV (PDE IV). Inhibition of the PDE IV enzyme results in increased concentrations of cAMP, which inactivates myosin light chain kinase and leads to smooth muscle relaxation. Drotaverine inhibits PDE IV in vitro without inhibiting the isoenzymes PDE III and PDE V. To reduce smooth muscle contractility, PDE IV is functionally very important, and its selective PDE IV inhibitors may be useful in the treatment of hyperkinetic diseases and various symptoms caused by spastic conditions of the gastrointestinal tract. tract. Drotaverine has no side effects on the cardiovascular system, because the smooth muscle cells of the myocardium and blood vessels mainly contain the PDE III isoenzyme. The enzyme that hydrolyzes cAMP in myocardial and vascular smooth muscle cells is mainly a PDE III isoenzyme, which explains why drotaverine is an effective antispasmodic agent without serious cardiovascular side effects and strong cardiovascular therapeutic activity. The drug is effective for spasms of smooth muscles of both nervous and muscular etiology. Regardless of the type of autonomic innervation, drotaverine acts on smooth muscles located in the gastrointestinal, biliary, urogenital and vascular systems. Thanks to its vasodilating effect, it enhances tissue blood circulation. Its effect is stronger than that of papaverine, and absorption is faster and more complete; it binds less to plasma proteins. The advantage of drotaverine is that it does not have a stimulating effect on the respiratory system, which was observed after parenteral administration of papaverine.
Indications for use
spasms of smooth muscles associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis; spasms of smooth muscles of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder tenesmus. As an adjuvant treatment (if the patient cannot take tablets):
- for spasms of smooth muscles of gastrointestinal origin: peptic ulcer of the stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis;
- in gynecology: algodismenorrhea.
Directions for use and doses
Unless otherwise directed by the physician, the usual average dose for adults is 40 to 240 mg of drotaverine hydrochloride (divided into 1 to 3 doses per day) intramuscularly daily. For acute colic (cholelithiasis and urolithiasis) 40-8() mg intravenously.
Use during pregnancy and lactation
As shown by the results of preclinical studies in animals and retrospective studies of clinical data, oral use of drotaverine during pregnancy does not lead to either teratogenic or embryotoxic effects. However, caution is required when prescribing the drug during pregnancy. Drotaverine should not be used during childbirth. Due to the lack of necessary clinical data, it is not recommended to prescribe during breastfeeding.
Impact on the ability to drive vehicles and potentially dangerous mechanisms
After parenteral, and especially intravenous administration of the drug, patients are advised to refrain from driving and working on machines.
Precautionary measures
Clinical studies of the drug in children are not presented. With low blood pressure, the use of the drug requires caution. When administering drotaverine intravenously, due to the risk of loss of consciousness, the patient must lie down! In case of hypersensitivity to sodium metabisulfite, parenteral use of the drug should be avoided. Caution should be exercised when taking the drug parenterally by pregnant women.
Interaction with other drugs
When taken together with levodopa, the drug reduces the effect of the latter on the symptoms of Parkinson's disease, while increasing muscle stiffness and shaking (tremor).
Contraindications
hypersensitivity to the active substance or to any of the excipients of the drug (especially to sodium metabisulfite); severe liver, kidney or heart failure (low cardiac output syndrome); childhood.
Compound
active substance - drotaverine hydrochloride - 40.0 mg; excipients - sodium metabisulfite, rectified ethyl alcohol from food raw materials 95%, water for injection.
Overdose
An overdose of drotaverine can cause cardiac arrhythmia and conduction disturbances, including complete bundle branch block and cardiac arrest, which can be fatal. In case of overdose, the patient should be monitored and receive symptomatic and supportive treatment.
Side effect
During clinical trials, the following side effects were reported by investigators as being associated with drotaverine and presented the following incidence: very common (> 1/10); common (> 1/100, 1/1000, 1/10000,
Storage conditions
In a place protected from light at a temperature not exceeding 25 °C. Keep out of the reach of children.
Buy Drotaverine g / cold tablet 40 mg in container pack No. 10x2 in the pharmacy
Price for Drotaverine g/cold tablet 40 mg in container pack No. 10x2
Instructions for use for Drotaverine g/chlor tablet 40 mg in container pack No. 10x2
Note!
Description of the drug Drotaverin-Darnitsa solution d/in. 20mg/ml amp. 2ml No. 5 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
