From what tablets drotaverine 40 mg. Application for violations of kidney function. Interaction with other drugs
Name:
Drotaverine (Drotaverine)
Pharmachologic effect:
Drotaverine hydrochloride is a drug that has antispasmodic activity in relation to the smooth muscles of the gastrointestinal tract, biliary and urogenital systems, as well as in relation to the smooth muscle layer of blood vessels. The drug helps to relax smooth muscles, eliminates spastic pain, by expanding the lumen of blood vessels improves the flow of oxygen to the tissues. The mechanism of action of the drug is associated with its ability to change the potential of cell membranes and their permeability. The drug reduces the activity of the phosphodiesterase enzyme, promotes a consistent increase in the level of cAMP and an increase in the initial uptake of calcium ions by cells.
Beta-adrenergic blockade may mask certain Clinical signs hyperthyroidism. Therefore, abrupt discontinuation of propranolol hydrochloride may be accompanied by exacerbation of symptoms of hyperthyroidism, including thyroid disorders.
For impaired renal function
In a number of cases of Wolff-Parkinson-White syndrome, it was observed that after the use of propranolol hydrochloride, tachycardia was replaced by intense bradycardia, which required a pacemaker. In one case, this occurred after an initial dose of 5 mg propranolol hydrochloride.
The drug is characterized by a low degree of connection with plasma proteins (it binds mainly to albumins, alpha and beta globulins). After oral administration, the peak plasma concentration of the active substance is reached within 45-60 minutes. Metabolized in the liver. The half-life is about 22 hours. It is excreted mainly in the urine in the form of metabolites, a certain amount of the drug is excreted in the feces. Drotaverine penetrates the hematoplacental barrier.
Carcinogenesis, mutagenesis, deterioration of fertility. Long-term animal studies have been conducted to evaluate toxic effects and carcinogenic potential. No tumor effects have been reported due to the drug at any doses. Reproductive studies in animals have not revealed any fertility problems associated with this drug. The effect of propranolol hydrochloride on human fertility is unknown.
Use in Pregnancy: Animal studies have shown that propranolol hydrochloride can be embryotoxic at doses up to 10 times the maximum recommended human dose. There are no adequate and well-controlled studies in pregnant women. Therefore, the safety of using propranolol hydrochloride during pregnancy has not been established. Propranolol hydrochloride should not be used during pregnancy unless the expected benefit to the patient outweighs the potential risk to the fetus, according to medical criteria.
Indications for use:
The drug in the form of tablets and solution for injection is used to relieve spasm and eliminate spastic pain, including:
Spasms in cholecystitis, cholelithiasis, gastric ulcer and/or duodenum, constipation of spastic etiology, spasms smooth muscle cardial and pyloric parts of the stomach, spastic colitis, intestinal colic caused by gas retention.
Use during lactation: propranolol hydrochloride is excreted from breast milk therefore it should be used with caution in women who are breastfeeding. Pediatric use: Evaluation of the effect of propranolol hydrochloride in children related to the efficacy and safety of the drug has not been conducted as systematically as in adults. Information is available in the medical literature for satisfactory estimates. Cardiovascular disease, common in adults and children, usually responds to treatment with propranolol hydrochloride.
In addition, the drug is used to relieve spasm of smooth muscles in proctitis, pyelitis, cystitis, urethrolithiasis and nephrolithiasis.
The drug can be prescribed during diagnostic procedures, including cholecystography.
Drotaverine is used as a vasodilator for spasms of the smooth muscle layer of blood vessels, to eliminate headaches caused by spasm of cerebral vessels.
Adverse reactions are also similar, such as bronchospasm and congestive heart failure. The normal echocardiogram evolves through a series of modifications as children's hearts grow and develop. ECG changes associated with the age of children should be considered when using echocardiography to monitor treatment with propranolol hydrochloride in children. Elevated serum levels of propranolol hydrochloride have been observed in patients with Down syndrome, indicating that the bioavailability of propranolol hydrochloride may be increased in patients with Down syndrome.
The drug is also used in gynecological practice for algomenorrhea, to prevent and eliminate spasm of the smooth muscles of the uterus during pregnancy, including threatening abortion. The drug is indicated for spasm of the pharynx of the uterus during childbirth, prolonged opening of the pharynx and postpartum contractions.
Application method:
Tablets:
The drug is taken orally, it is recommended to swallow the tablet whole, without chewing or crushing, drinking plenty of water. The drug is taken regardless of the meal. The duration of the course of treatment and the dose of the drug is determined by the attending physician individually for each patient.
Drug Interactions Propranolol
Cardiovascular system: bradycardia; congestive heart failure; strengthening of the atrioventricular block; hypotension; paresthesia of the hands; thrombocytopenic purpura; arterial insufficiency, usually Raynaud's type. Central nervous system: mental depression, manifested by insomnia, fatigue, weakness, fatigue; reversible mental depression progressing to catatonia; visual disturbances; hallucinations, vivid dreams; an acute reversible syndrome characterized by disorientation of time and space, temporary memory loss, emotional lability, mild sensory disturbances, deterioration of psychomotor performance.
Adults and adolescents over the age of 2 years with spastic pain are usually prescribed 40-80 mg of the drug (1-2 tablets of the drug Drotaverin or 1 tablet of the drug Drotaverin Forte) 2-3 times a day. Maximum daily dose the drug is 240 mg.
Children under the age of 12 years should be given the drug strictly according to the doctor's prescription.
A total daily dose above 160 mg may be associated with an increased frequency of fatigue, lethargy and vivid dreams. Gastrointestinal tract: nausea; vomit; epigastric pain; abdominal colic; diarrhea; constipation; mesenteric arterial thrombosis; ischemic colitis.
Allergic: pharyngitis; agranulocytosis; erythematous rash; fever associated with pain and inflammation of the throat; laryngospasm; labored breathing. Hematological: agranulocytosis; non thrombocytopenic purpura; thrombocytopenic purpura. Autoimmune: In extremely rare cases, systemic lupus erythematosus has been reported.
Children aged 6 to 12 years are usually prescribed 20 mg of the drug (1/2 tablet of Drotaverine) 1-2 times a day.
Children aged 2 to 6 years are usually prescribed 10-20 mg of the drug (1 / 4-1 / 2 tablets of the drug Drotaverine) 1-2 times a day.
Injection:
The drug is intended for intramuscular injection. Patients with hepatic or renal colic are allowed intravenous slow administration of the drug. Intravenous administration of the drug is permissible only in the patient's supine position, due to the risk of collapse. Patients with peripheral circulatory disorders caused by spasm of the smooth muscle layer of the vessels, the drug can be administered intra-arterially slowly.
Other: alopecia; reactions similar to systemic lupus erythematosus; psoriasis eruptions; dry eyes; male impotence and Peyronie's disease have rarely been reported. Interactions with Laboratory Tests Propranolol hydrochloride may alter some laboratory clinical tests by causing elevated blood urea levels in patients with severe heart failure, elevated serum transaminase, alkaline phosphatase and lactic dehydrogenase.
Indications for use
The usual starting dose is 40 mg propranolol hydrochloride twice daily, either alone or in combination with a diuretic. The dose can be gradually increased until adequate control is achieved. blood pressure. The usual content is from 120 mg to 240 mg per day. In some cases, doses higher than 640 mg per day may be required. The time required to obtain a complete response to hypertension for a given dose varies and can range from several days to several weeks.
The duration of the course of treatment and the dose of the drug is determined by the attending physician individually for each patient.
Adults are usually prescribed 2-4 ml of the drug (40-80 mg of drotaverine) 1-3 times a day intramuscularly. Patients with hepatic or renal colic are usually prescribed 2-4 ml of the drug (40-80 mg of drotaverine) intravenously slowly after dissolving the drug in 5-10 ml of 0.9% sodium chloride solution.
Although twice daily doses are effective in maintaining blood pressure reduction throughout the day, some patients, especially at low doses, may show a slight increase in blood pressure at the end of the 12-hour interval. To determine if adequate blood pressure control is being maintained throughout the day, it is recommended to measure blood pressure at the end of the interval. If blood pressure control is insufficient at the end of the 12-hour interval, it is recommended to increase the dose or divided doses 3 times a day for better control.
Adolescents over the age of 12 are usually prescribed 1-2 ml of the drug (20-40 mg of drotaverine) 1-3 times a day.
Women in physiological childbirth to reduce the phase of cervical dilatation are usually prescribed 2 ml of the drug (40 mg of drotaverine) intramuscularly at the beginning of the dilatation period. If necessary, after 2 hours, re-inject 2 ml of the drug intramuscularly.
Although patients may respond individually to any dose, the average satisfactory dose is about 160 mg per day. In angina pectoris, safety at doses exceeding 320 mg per day has not been established. A total daily dose of 80 mg to 320 mg taken orally, two, three or four times a day has been shown to increase tolerance to physical activity and reduces ischemic changes on the ECG.
If treatment is discontinued, the dose should be gradually reduced over several weeks. Although a 3-month treatment regimen was used in a study in the United States and a 4-month regimen in a multicenter study in Norway, there is sufficient scientific basis for a 2 or 3 times daily dosing regimen. The efficacy and safety of daily doses greater than 240 mg in the prevention of cardiac death have not been established. However, higher doses may be needed for effective treatment coexisting diseases such as angina pectoris or hypertension.
Patients suffering from peptic ulcer of the stomach and duodenum, the drug should be prescribed in combination with other antiulcer drugs.
Undesirable phenomena:
The drug is usually well tolerated by patients, however, in isolated cases, the following side effects may develop:
From the gastrointestinal tract: nausea, vomiting, stool disorders.
The recommended starting oral dose is 80 mg propranolol hydrochloride per day in divided doses, gradually increased until an effective dose for migraine prevention is reached. Usually an effective dose is usually reached from 160 mg to 240 mg per day. If a satisfactory response is not received within 4-6 weeks after reaching maximum dose, treatment should be discontinued. It should be warned that the drug should be discontinued gradually over several weeks.
For inoperable antitumor control, 30 mg daily in divided doses is recommended. The pediatric maintenance dose is 2 mg to 4 mg per kg per day in two equal doses. A weight-based dose for children will generally give plasma levels in the therapeutic range similar to those in adults. On the other hand, pediatric doses calculated on a body surface basis generally result in plasma levels above the adult therapeutic mean.
From the side of the central nervous system: sleep disturbance and wakefulness, fainting, headache.
From the side of the cardiovascular system: tachycardia, lowering blood pressure, arrhythmia, feeling of heat.
From the respiratory system: swelling of the nasal mucosa, bronchospasm (mainly in patients with a tendency to bronchospasm).
If treatment with propranolol hydrochloride is to be discontinued, the dose should be gradually reduced over a period of 7 to 14 days. General information: If there has been a recent meal, empty the contents of the stomach, being careful to prevent pulmonary aspiration.
Bradycardia: Atropine should be given. If there is no response to vagal block, carefully administer isoproterenol. Heart failure: digitization and diuretics. Hypotension: vasopressors with norepinephrine or epinephrine. Bronchospasm: Isoproterenol and aminophylline should be given.
allergic reactions: skin rash, itching, allergic dermatitis, angioedema.
In addition, excessive sweating may develop.
At intravenous administration drug in patients may develop arterial hypotension, atrioventricular blockade, respiratory depression.
If side effects develop, stop taking the drug and contact your doctor.
Pharmacological properties
Propranolol hydrochloride has an antiarrhythmic effect at concentrations associated with beta-adrenergic blockade and this appears to be its main mechanism of antiarrhythmic action. At doses higher than those required for a beta-blocker, propranolol hydrochloride has a similar or similar anaexcidic effect of quinidine, which affects the cardiac action potential. The significance of this membrane action in the treatment of arrhythmias is uncertain. The mechanism of antimigraine action of propranolol hydrochloride has not been established.
Contraindications:
Common for both dosage forms:
Increased individual sensitivity to the components of the drug.
Severe heart failure, severe arterial hypotension, atrioventricular block II-III degree. The drug is also contraindicated in patients with cardiogenic shock.
The drug is contraindicated in patients suffering from severe renal and / or hepatic insufficiency.
Propranolol hydrochloride is used to reduce the risk of cardiovascular mortality in patients who have experienced the acute phase of myocardial infarction and are clinically stable. In the United States, a multicenter study found that long-term administration of propranolol hydrochloride reduced mortality from cardiovascular disease, mortality from atherosclerotic heart disease and sudden death in patients with atherosclerosis. A multicenter study in Norway provided results that support those in the United States.
The drug in the form of tablets Drotaverin and Drotaverin Forte contains lactose, so it should not be used to treat patients with congenital lactase deficiency, as well as glucose-galactose malabsorption syndrome.
The drug in the form of tablets Drotaverin Forte is not used to treat children under the age of 12 years.
The drug, regardless of the form of release, should be used with caution in patients suffering from prostatic hyperplasia, angle-closure glaucoma and atherosclerosis of the coronary arteries, as well as patients with suspected atherosclerosis of the coronary arteries.
Terms and conditions of storage
Propranolol hydrochloride is almost completely absorbed from the gastrointestinal tract. It then passes to the liver, where it attaches to non-specific binding sites. Large individual differences in liver saturation are due to differences in liver flow. Following oral administration, the drug does not reach the general circulation until the liver binding sites are saturated. Once saturated, hepatic compounds no longer interfere with the passage of propranolol hydrochloride into the bloodstream.
The amount of propranolol hydrochloride that reaches the circulation after an oral dose also depends on the amount of drug metabolized during the first pass through the liver. Propranolol hydrochloride is widely distributed in body tissues, including the liver, heart, kidneys, and lungs. The drug rapidly crosses the blood-brain barrier and the placenta. Propranolol hydrochloride is more than 90% bound to plasma proteins. Both free propranolol hydrochloride and protein-bound propranolol hydrochloride are metabolized.
The drug should be used with caution in women during pregnancy and lactation.
The drug is not recommended for patients whose work is related to the management of potentially dangerous mechanisms and driving a car. If necessary, the appointment of the drug should be within an hour after taking drotaverine to refrain from work requiring increased attention.
During pregnancy:
The drug penetrates the hematoplacental barrier, so its appointment during pregnancy is possible only if the expected benefit to the mother is higher than the potential risks to the fetus.
If necessary, the use of the drug during lactation should decide on the possible interruption of breastfeeding.
Interaction with other drugs:
When combined, the drug may reduce the effectiveness of levodopa.
With the simultaneous use of drotaverine with other medicines with antispasmodic activity, there is a mutual enhancement of therapeutic effects.
When using the drug simultaneously with tricyclic antidepressants, procainamide and quinidine, there is an increase in arterial hypotension caused by these drugs.
Drotaverine helps to reduce the spasmodic effect of morphine.
With the simultaneous use of phenobarbital increases antispasmodic action drotaverine.
Overdose:
When using excessive doses of the drug in patients, the development of atrioventricular blockade, cardiac arrest and paralysis of the respiratory center is noted.
There is no specific antidote. In case of overdose, drug withdrawal and symptomatic therapy are indicated. In atrioventricular blockade, atropine and isoprenaline are used intravenously; in case of cardiac arrest, the use of intravenous atropine or adrenaline and temporary pacing are indicated; in case of respiratory arrest due to paralysis of the respiratory center, artificial lung ventilation is indicated.
Treatment of an overdose of the drug should be carried out under the constant supervision of medical personnel.
Release form of the drug:
Drotaverin tablets containing 40 mg of the active substance, 10 pieces in a blister pack, 2 blister packs in a carton box.
Tablets Drotaverin Forte containing 80 mg of the active substance, 10 pieces in a blister, 2 blisters in a carton.
Solution for injection of 2 ml in dark glass ampoules, 5 ampoules in blister packs, 2 blister packs in a carton box.
Storage conditions:
The shelf life of the drug in the form of tablets is 3 years.
The shelf life of the drug in the form of a solution for injection is 2 years.
Synonyms:
No-shpa, No-shpa Forte, Spazmol.
Composition:
1 ml solution for injection Drotaverine contains:
Drotaverine hydrochloride (in terms of pure substance) - 20 mg,
Excipients.
1 tablet of Drotaverine contains:
Drotaverine hydrochloride (in terms of pure substance) - 40 mg,
1 tablet of the drug Drotaverin Forte contains:
Drotaverine hydrochloride (in terms of pure substance) - 80 mg,
Excipients, including lactose.
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Many thanks!Name:
Drotaverine hydrochloride.
Analogues: No-shpa noshpalgin
INN:
Drotaverine (Drotaverine).
Dosage form:
tablets 40 mg.
Description:
Tablets of yellow or yellow color with a greenish tinge, ploskotsilindrichesky, with a facet.
Composition:
Each tablet contains:
Active ingredient: drotaverine hydrochloride - 40 mg;
Excipients: lactose monohydrate, potato starch, talc, stearic acid.
Pharmacotherapeutic group:
Synthetic antispasmodics. Derivatives of papaverine.
ATX code: A03AD02.
Pharmacological properties
Pharmacodynamics
Drotaverine is an isoquinoline derivative that exhibits an antispasmodic effect on smooth muscles by inhibiting the enzyme phosphodiesterase IV (PDE IV). Inhibition of the enzyme phosphodiesterase IV leads to an increased concentration of cAMP, which inactivates the myosin kinase (MLCK) light chain, which in turn leads to smooth muscle relaxation.
Drotaverine inhibits the enzyme phosphodiesterase (PDE) IV without inhibiting the isoenzymes PDE III and PDE V. 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. intestinal tract. 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 cardiovascular side effects and pronounced effect on the cardiovascular system. The drug is effective in spasms of smooth muscles caused by a violation of the nervous regulation and self-regulation 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. Due to its vasodilating effect, it improves tissue circulation. Its action 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 respiratory system observed after parenteral administration of papaverine.
Pharmacokinetics
Suction
When ingested, drotaverine hydrochloride is rapidly absorbed from the gastrointestinal tract, the half-absorption period is 12 minutes. Bioavailability - about 100%. Cmax in serum is reached in 45 - 60 minutes.
Distribution
Drotaverine hydrochloride does not penetrate the blood-brain barrier.
Metabolism
Drotaverine hydrochloride is biotransformed in the liver.
breeding
After 72 hours, it is practically excreted from the body in the form of metabolites - 50% in the urine and 30% in the feces.
Indications for use
Spasms of smooth muscles associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;
Spasms of smooth muscles urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder tenesmus.
As adjuvant therapy:
With spasms of smooth muscles of gastrointestinal origin: peptic ulcer stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis, colitis, spastic colitis with constipation and meteoristic forms of mucous colitis;
Tension-type headaches;
In obstetrics and gynecology: aldismenorrhea, to reduce the increased tone of the uterus during pregnancy, with threatened abortion.
Contraindications
- Hypersensitivity to active substance or to any of the excipients of the medicinal product;
- Severe liver and kidney failure;
- Severe heart failure (low cardiac output syndrome);
- Childhood up to 1 year.
Precautionary measures
C caution should be prescribed for arterial hypotension, severe atherosclerosis of the coronary arteries, during pregnancy, in children from 1 to 6 years of age.
Dosage and administration
Take by mouth
Adults appoint 40 - 80 mg (1 - 2 tablets) 3 times a day; children aged 1-6 years are prescribed in a single dose of 10-20 mg (1/4-1/2 tablets), the maximum daily dose is 120 mg (3 tablets); at the age of 6 to 12 years - a single dose - 20 mg (1/2 tablet), the maximum daily dose - 200 mg (5 tablets). Multiplicity of appointment - 2 - 3 per day.
Side effects
. From the gastrointestinal tract: rarely (> 1/10000,< 1/1000) - тошнота, запор;
. From the side of the nervous system: rarely (> 1/10000,< 1/1000) - головная боль, головокружение, бессонница;
. From the side of the cardiovascular system: rarely (> 1/10000,< 1/1000) - учащенное сердцебиение, гипотензия.
special instructions
The use of the drug in hypotension requires increased caution.
Drotaverine tablets contain 53 mg of lactose. When taken according to the recommended dosage, each dose contains up to 159 mg of lactose. It can cause gastrointestinal disturbances in individuals suffering from lactose intolerance. This dosage form unacceptable for patients suffering from lactase deficiency, galactosemia or impaired glucose / galactose absorption syndrome.
Pregnancy and lactation
The use of drotaverine during pregnancy does not lead to teratogenic and embryotoxic effects. However, when prescribing the drug during pregnancy, caution is necessary.
Due to the lack of necessary clinical data during lactation, it is not recommended to prescribe.
Impact on the ability to drive vehicles:
Patients should be informed that if dizziness occurs, they should avoid potentially hazardous activities, such as driving vehicles and potentially dangerous machinery.
Interaction with other drugs
With simultaneous use, drotaverine can weaken the anti-Parkinsonian effect of levodopa.
Overdose
To date, no cases of overdose have been reported.
Package
10 tablets in a blister pack; 2 contour packs in a pack of cardboard.
Storage conditions
In a place protected from light and moisture, at a temperature not exceeding 25ºС.
Best before date
2 years.
Manufacturer:
Open Joint Stock Company "Borisov Plant of Medical Preparations", Republic of Belarus,