Drotaverine hydrochloride
Drotaverine hydrochloride: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Drotaverine
ATX code: A03AD02
Active ingredient: drotaverine (Drotaverine)
Manufacturer: JSC "Borisov Plant of Medical Products" (JSC "BZMP") (Republic of Belarus)
Description and photo update: 2019-09-07
Drotaverine hydrochloride is an antispasmodic drug.
Release form and composition
Dosage form - tablets: flat-cylindrical, beveled, yellow or yellow with a greenish tinge (in a cardboard box 2 cell contour packs of 10 tablets and instructions for the use of Drotaverine hydrochloride).
Composition of 1 tablet:
- active substance: drotaverine hydrochloride - 40 mg;
- auxiliary components: potato starch, lactose monohydrate, stearic acid, talc.
Pharmacological properties
Pharmacodynamics
Drotaverine is an isoquinoline derivative with antispasmodic activity on smooth muscles. The mechanism of action is due to its ability to suppress the enzyme phosphodiesterase IV (PDE IV), which increases the concentration of cyclic adenosine monophosphate (cAMP). This leads to inactivation of myosin light chain kinase (MLCK) and, as a consequence, to relaxation of smooth muscles.
Drotaverine does not depress the isoenzymes PDE III and PDE V, inhibiting only PDE IV, which is functionally very significant in reducing the contractility of smooth muscles. Being a selective PDE IV inhibitor, Drotaverine hydrochloride can be used in the treatment of hyperkinetic diseases and various pathologies associated with spastic conditions of the gastrointestinal tract. The drug is also used for spasms of smooth muscles caused by impaired nervous regulation and self-regulation of muscle or nervous etiology.
Regardless of the type of autonomic innervation, the drug has an effect on smooth muscles located in the gastrointestinal tract, biliary, vascular and urogenital systems. Improves tissue blood flow.
Unlike papaverine, drotaverine has a stronger effect, is absorbed faster and more fully when taken orally, and binds less to plasma proteins. Its advantage is the absence of a stimulating effect on the respiratory system, which is observed with parenteral administration of papaverine.
Since the enzyme that hydrolyzes cAMP in myocardial and vascular smooth muscle cells is mainly an isoenzyme of PDE III, drotaverine has a pronounced antispasmodic effect without significantly affecting the cardiovascular system and without causing side effects on its part.
Pharmacokinetics
After oral administration, drotaverine hydrochloride is rapidly absorbed from the gastrointestinal tract: the half-absorption period is 12 minutes. The drug is characterized by a very high bioavailability - about 100%. The maximum concentration in the blood serum reaches within 45-60 minutes.
Drotaverine does not cross the blood-brain barrier. Metabolized in the liver. It is excreted from the body within 72 hours mainly in the form of metabolites: with urine - 50%, with feces - 30%.
Indications for use
Drotaverine hydrochloride is recommended to be used to relieve spasms of smooth muscles associated with diseases:
- biliary tract: papillitis, cholangitis, cholecystitis, pericholecystitis, cholangiolithiasis, cholecystolithiasis;
- urinary tract: bladder tenesmus, cystitis, urethrolithiasis, nephrolithiasis, pyelitis.
As an adjunctive therapy, Drotaverine hydrochloride is prescribed in the following cases:
- spasms of smooth muscles of gastrointestinal origin: colitis, enteritis, spastic colitis with constipation and flatulence, gastritis, gastric ulcer and duodenal ulcer, spasms of the cardia and pylorus;
- tension headaches;
- dysmenorrhea.
Contraindications
Absolute:
- severe heart failure (low cardiac output syndrome);
- severe renal / hepatic impairment;
- lactase deficiency, galactosemia, impaired glucose / galactose absorption syndrome;
- children's age up to 1 year;
- hypersensitivity to any component of the drug.
It is not recommended to prescribe Drotaverine hydrochloride tablets during lactation.
An antispasmodic should be used with caution in patients with arterial hypotension, as well as in the treatment of children 1–6 years old.
Drotaverine hydrochloride, instructions for use: method and dosage
Drotaverine hydrochloride tablets should be taken orally.
Recommended dosages:
- adults - 1-2 tablets (40-80 mg) 3 times a day;
- children 6–12 years old - ½ tablet (20 mg) 2-3 times a day. The maximum daily dose is 5 tablets (200 mg);
- children 1–6 years old - ¼ – ½ tablets (10–20 mg) 2–3 times a day. The maximum daily dose is 3 tablets (120 mg).
Side effects
Drotaverine hydrochloride is generally well tolerated. In rare cases (from 1/10 000 to <1/1000), the following side effects are noted:
- from the gastrointestinal tract: nausea, constipation;
- on the part of the cardiovascular system: heart palpitations, decreased blood pressure;
- from the nervous system: insomnia, headache, dizziness;
- from the immune system: allergic reactions (rash, hives, itching, Quincke's edema).
Overdose
Taking an excessive dose of the drug can contribute to disturbances in heart rhythm and conduction, up to a complete blockade of the bundle branch and cardiac arrest, which is fraught with death.
In case of taking an excessive dose of the drug inside, it is recommended to induce vomiting and / or wash out the stomach. The patient is hospitalized. Symptomatic and supportive therapy is performed.
special instructions
Each tablet contains 53 mg of lactose. If the recommended dosage regimen is observed, the patient receives up to 159 mg of lactose with each single dose of the drug. In this regard, Drotaverine hydrochloride in this dosage form is contraindicated in patients with lactase deficiency, galactosemia, syndrome of impaired absorption of galactose / glucose.
Influence on the ability to drive vehicles and complex mechanisms
If dizziness occurs during therapy, it is recommended to avoid potentially hazardous activities, including driving and working with complex mechanisms.
Application during pregnancy and lactation
Drotaverine does not cause the development of teratogenic and embryotoxic effects, therefore it can be used as directed by a doctor during pregnancy.
It is not recommended to prescribe the drug during lactation.
Pediatric use
The experience of using Drotaverine hydrochloride in pediatrics is limited, and therefore, the drug should be used with caution when treating children. The appointment of an antispasmodic is contraindicated in children under 1 year of age.
With impaired renal function
Drotaverine is contraindicated in patients with severe renal impairment.
For violations of liver function
Drotaverine is contraindicated in patients with severe hepatic impairment.
Use in the elderly
There is no need for dose adjustment in elderly patients.
Drug interactions
Drotaverine may reduce the antiparkinsonian effect of levodopa.
Analogs
Analogs of Drotaverine hydrochloride are Galidor, Dibazol, Doverin, Duspatalin, Mebeverin, No-shpa, Niaspam, Nosh-bra, Platifillin, Papaverin, Papazol, Spazmol, Spakovit, Sparex, etc.
Terms and conditions of storage
Store in a place protected from light and moisture, out of reach of children, at a temperature not exceeding 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Available without a prescription.
Reviews about Drotaverine hydrochloride
The drug is an analogue of the popular drug No-shpa. Patients leave positive reviews about Drotaverine hydrochloride, noting no less effectiveness at a lower cost. The antispasmodic effectively relieves various spasms of smooth muscles and pain syndrome, is well tolerated, available in pharmacies. Many women write that this drug was prescribed to them with an increased tone of the uterus.
At the same time, there are reports that indicate that the effect of Drotaverine hydrochloride is much lower than that of No-shpa, therefore, patients, despite the high cost, prefer the latter.
The price of Drotaverine hydrochloride in pharmacies
The approximate price of Drotaverine hydrochloride for a pack of 20 tablets is 15–18 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
