Instruction for use: Drotaverine 40mg

International Nonproprietary Name (INN): Drotaverine

Pharmaceutic group: Antispasmodic

Presentation:

Tablets 40 mg ¹20, ¹50 and ¹100.

Available without prescription

Indications for Drotaverine

Drotaverine (INN, also known as drotaverin) is an antispasmodic drug, structurally related to papaverine. Drotaverine is a selective inhibitor of phosphodiesterase 4, and has no anticholinergic effects. Drotaverine has been shown to possess dose-dependant analgesic effects in animal models. One small study has shown drotaverine to be eliminated mainly non-renally.

A few small 2003 studies found drotaverine to be nearly 80% effective in treating renal colic. It has also been studied in accelerating labor by speeding up cervical dilation, but the results have been conflicting. Drotaverine has been shown to be effective in paracervical block in managing pain during hysteroscopy and endometrial biopsy when administered together with mefenamic acid. Irritable bowel syndrome patients presenting with predominant diarrhea are more likely to benefit from Buscopan. Drotaverin has also been tested in combination with rimantadine for antiviral activity against A and B type influenza. Drotaverin has an adverse effects frequency of 0.9%, side effects being relatively uncommon.

Drotaverine is sold under brand name No-Spa (Chinoin Pharmaceutical and Chemical Works, Hungary, a member of the Sanofi-Aventis). It was concluded that drotaverine is highly effective in reducing the duration of active phase of labour by hastening cervical dilatation, more effective when given in more dilated cervix than with less dilatation and more effective in multigravida than in primigravida. There was no interference with uterine contractility and no increase in operative delivery. It reduces the incidence of traumatic postpartum haemorrhage by reducing the incidence of cervical tear. It is a safe drug for the mother as well as for the baby.

Trade name of the drug – Drotaverine

Rational chemical name: 1- (3,4-diethoxyphenyl) methylene-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline (as hydrochloride)

Dosage Form: tablets.

Active substance:

drotaverina hydrochloride - 40 mg;

Excipients: Potato starch - 30.1 mg monohydrate lactose (milk sugar) - 60.1 mg, povidone (polyvinylpyrrolidone) - 5.8 mg Talc - 2.6 mg magnesium stearate - 1.4 mg.

Description:

Round tablets yellow with greenish hue color, flat-cylindrical, with a facet and Valium

Pharmacotherapeutic group: Antispasmodic

ATX code: À03ÀD02

Pharmacological Properties of Drotaverine

Myotropic antispasmodic, a derivative of isoquinoline. Inhibits phosphodiesterase (PDE) IV, which leads to the accumulation of intracellular cyclic adenosine monophosphate (cAMP) and hence in inactivation of the myosin light chain kinase, resulting in smooth muscle relaxation.

Regardless of the type of the autonomic innervation drotaverine acts on the smooth muscle in the gastrointestinal tract, biliary, genitourinary, and cardiovascular systems. In the myocardium and blood vessels enzyme hydrolyzing cAMP is a PDE III of, which explains the lack of serious side effects of the cardiovascular system (CVS) and the unexpressed therapeutic effect with respect to the CAS.

It has direct effect on smooth muscle can be used as an antispasmodic when contraindicated drugs from the group m-anticholinergics (angle-closure glaucoma, prostatic hyperplasia).

Pharmacokinetics. When taken orally, the absorption - high, poluabsorbtsii period - 12 min. Bioavailability - 100%. Evenly distributed in the tissues, it penetrates into smooth muscle cells. The time to reach maximum concentration in the blood - 2 hours Connection with the plasma protein -. 95-98%. Mainly excreted by the kidneys, to a lesser extent - in the bile. It does not cross the blood-brain barrier.

Indications for Drotaverine

Smooth muscle spasm urinary and biliary organs (kidney colic, pyelitis, tenesmus, biliary colic, intestinal colic, biliary dyskinesia and gallbladder hyperkinetic type, cholecystitis, postcholecystectomical syndrome).

Spasm of smooth muscles of the gastrointestinal tract (usually as part of combination therapy): pilorospazm, gastro, gastric ulcer and duodenal ulcers, spastic constipation, spastic colitis, proctitis.

Tensor headache.

Dysmenorrhea, threatening miscarriage, threatening preterm delivery, postpartum contractions.

In carrying out some instrumental studies holetsistografii.

Contraindications for Drotaverine

Hypersensitivity to the drug, pronounced hepatic and renal insufficiency, severe heart failure (low cardiac output syndrome), lactation.

This dosage form is not used in children younger than 3 years.

Due to the presence of the drug lactose monohydrate (milk sugar), its reception is contraindicated in congenital lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Precautions

Drotaverine should be used with caution in patients with arterial hypotension, atherosclerosis of the coronary arteries, prostatic hyperplasia, angle-closure glaucoma, pregnancy.

Drotaverine Dosage and Administration

Adults designate the interior of 40-80 mg (1-2 tablets) 2-3 times a day. The maximum daily dose - 240 mg.

Children aged 3 to 6 years of age - a single dose of 20 mg, the maximum daily dose - 120 mg (2-3 hours); aged 6 to 12 years of single - 40 mg, the maximum daily dose - 200 mg; multiplicity of application - 2-5 times a day.

Side effect ofDrotaverine

Dizziness, headache, insomnia, palpitations, blood pressure, allergic reactions, nausea, constipation, sensation of heat, sweating

overdose

Information on overdose in respect of the drug is not.

Interaction

In an application can weaken antiparkinsonian effect of levodopa.

It enhances the effect of papaverine, bendazol and other antispasmodics (including m-anticholinergics) decrease in blood pressure caused by tricyclic antidepressants, quinidine and procainamide.

Reduces spazmogennoe morphine activity.

Phenobarbital increases the severity of antispasmodic action Drotaverine.

special instructions for Drotaverine

In the treatment of gastric ulcer and duodenal ulcer is used in combination with other drugs commonly prescribed for the treatment of this group of diseases of the esophagus, stomach and duodenum.

When administered at therapeutic doses, Drotaverine does not affect the ability to drive and perform work requiring special attention. If there are any side effects, the issue of driving transport and work on machine tools requires individual consideration.

Release form of Drotaverine

40 mg tablets. 10 tablets in blisters.

1, 2, 3, 4 or 5, the contour of cellular packages together with instructions for use in a stack of cardboard.

100 tablets in polymer bank. Each jar along with instructions for use are placed in a pile of cardboard.

Storage conditions of Drotaverine

In a dry, dark place at a temperature no higher than 25 ° C.

Keep out of the reach of children.

Shelf life of Drotaverine

3 years.

Do not use beyond the expiration date printed on the package.

Conditions of supply of Drotaverine from pharmacies

Without prescription.