Description
Drotaverine Pharmacodynamics
Myotropic antispasmodic, isoquinoline derivative. It inhibits phosphodiesterase (PDE) IV, which leads to accumulation of intracellular cyclic adenosine monophosphate (cAMP) and consequently to inactivation of myosin light chain kinase, resulting in relaxation of smooth muscles. Regardless of the type of autonomic innervation, drotaverine acts on smooth muscles in the gastrointestinal tract, biliary, urogenital and vascular systems. In the myocardium and vessels, the enzyme that hydrolyzes the CAMP is FDE III, which explains the absence of serious cardiovascular system (CVS) side effects and the unexpressed therapeutic effect on the CVS.
The direct effect on the smooth muscles allows using as an antispasmodic in cases where drugs from the group of m-cholinoblockers are contraindicated (closed-angle glaucoma, prostatic hyperplasia).
Indications
Spasm of smooth muscles of the urinary and biliary tract (renal colic, pyelitis, tenesmus, biliary colic, intestinal colic, biliary and gallbladder dyskinesia of hyperkinetic type, cholecystitis, postcholecystectomy syndrome). Spasm of smooth muscles of the gastrointestinal tract (usually as a part of combined therapy): pylorospasm, gastroduodenitis, gastric and 12 duodenal ulcer, spastic constipation, spastic colitis, proctitis. Tensor headache. Dysmenorrhea, threatened miscarriage, threatened preterm labor, postpartum contractions. In some instrumental studies, cholecystography.
Contraindications
Hypersensitivity to the components of the drug, expressed hepatic, renal, chronic heart failure, atrioventricular block of II-III degree, cardiogenic shock, arterial hypotension, lactation period. Children under 3 years of age.
With caution:
Severe atherosclerosis of the coronary arteries, prostatic hyperplasia, closed-angle glaucoma; during pregnancy.
Pregnancy and lactation:
Use of the drug is recommended only if the benefit to the mother exceeds the potential risk to the fetus. Due to the lack of necessary clinical data, drotaverine is not recommended for administration during lactation (breast-feeding).
Dosage and administration method
- Adults, orally: 40-80 mg 3 times daily.
- For children, orally, aged 3-6 years: 40-120 mg in 2-3 doses, maximum daily dose – 120 mg; for children aged 6-18 years: 80-200 mg in 2-5 doses, maximum daily dose – 240 mg.
