Drotaverin-Teva, tablets 40 mg 20 pcs

Pharmacological group: spasmolytic agent

ATX code: A03AD02

Pharmacological properties

Pharmacodynamics

Drotaverine is an isoquinoline derivative that has an antispasmodic effect on smooth muscle by inhibiting the enzyme phosphodiesterase 4 (PDE-4). Inhibition of FDE-4 leads to increased concentrations of cyclic adenosine monophosphate (cAMP), which inactivates myosin light chain kinase (MLCK), which, in turn, leads to relaxation of smooth muscles.

Drotaverine inhibits the enzyme FDE-4 in vitro without inhibiting the FDE-3 and FDE-5 isoenzymes. FDE-4 appears to be functionally very important in reducing smooth muscle contractility, so selective FDE-4 inhibitors may be effective in the treatment of hyperkinetic diseases and diseases associated with gastrointestinal (GI) spasticity.

The enzyme that hydrolyzes zAMP in myocardial and vascular smooth muscle cells is primarily an FDE-3 isoenzyme, which explains the high efficacy of drotaverine as an antispasmodic with no pronounced cardiovascular effects or serious cardiovascular adverse reactions.

Drotaverine is effective for smooth muscle spasms of both nervous and muscular etiology. Regardless of the type of autonomic innervation, drotaverine acts on the smooth muscles of the gastrointestinal tract, biliary tract, as well as the urogenital and vascular systems. Due to its vasodilator effect, drotaverine improves blood supply to tissues.

Pharmacokinetics

absorption and distribution<

In oral and parenteral administration, drotaverine is rapidly and completely absorbed.

The maximum plasma concentration (C_max) is reached within 45-60 minutes. It binds to plasma proteins (alpha-albumin, alpha- and beta-globulin).

Metabolism and excretion

Metabolized in the liver. The half-life (T_1/2) is 16-22 hours.

Drotaverine is eliminated from the body after 72 hours mainly as metabolites, 50% – by the kidneys, 30% – through the intestine.

Indications

Enteritis, Painful menstruation (algodysmenorrhea), Abdominal bloating, Pain, Urolithiasis, Gastroduodenitis, Cholecystitis, Colitis, Gallic colic, Headache, Threatened miscarriage, Colic, Gallstone, Gastritis, Peptic ulcer, Renal colic

• Smooth muscle spasms associated with liver and biliary tract diseases: cholelithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;
• spasms of the smooth muscles of the urinary system: urolithiasis, pyelitis, cystitis, bladder tenesms.

Auxiliary therapy:

• spasms of the smooth muscles of the gastrointestinal tract: gastric and duodenal ulcer, gastritis, cardiac and gateway spasms, enteritis, colitis, accompanied by constipation and flatulence;
• tensor headache;
• dysmenorrhea.

.

Active ingredient

Drotaverine

Composition

1 tablet contains:
active ingredient:

• drotaverine hydrochloride 40.00 mg;

excipients:

• lactose monohydrate 67.00 mg;
• povidone-K25 4.00 mg;
• croscarmellose sodium 5.00 mg;
• magnesium stearate 3.00 mg.

.

How to take, the dosage

Overly with plenty of fluid.

The recommended daily dose for adults is 120-240 mg (in 2-3 doses).

For children aged 6 to 12 years the maximum daily dose is 80 mg divided into 2 doses; For children over 12 years of age, the maximum daily dose is 160 mg divided into 2 to 4 doses.

The recommended duration of treatment without medical advice is 1-2 days.

Interaction

With levodopa

Concomitant use may weaken the anti-Parkinsonian effect of levodopa, i.e. increase stiffness and tremor.

With papaverine, bendazole and other antispasmodics (including M-cholinoblockers)

Augment the antispasmodic effect.

With morphine

Decreasing the spasmogenic activity of morphine.

With phenobarbital

Enhancing the antispasmodic action of drotaverine.

Special Instructions

Caution should be exercised when using Drotaverin-Teva in patients with arterial hypotension.

The tablets contain lactose, therefore the drug Drotaverin-Teva is not indicated in patients with lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

Influence on driving and operating ability

When taken orally in therapeutic doses, drotaverine has no effect on the ability to drive vehicles and perform work requiring increased concentration.

If any adverse reactions occur, driving and operating machinery requires individual consideration. If dizziness occurs after taking the drug, the patient should avoid potentially hazardous activities, such as driving and operating machinery.

Synopsis

Round flat beveled tablets, yellow with a greenish tint. Slight “marbling” is possible.

Contraindications

Hypersensitivity to drotaverine or to any of the drug components; severe renal failure; severe hepatic failure (class C on the Child-Pugh scale); severe heart failure (low cardiac output syndrome); children under 6 years of age; breastfeeding period; lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

Cautions

Pregnancy, arterial hypotension, concomitant use with levodopa.

Side effects

Side effects are classified according to the following frequency: very common – at least 10%; common – at least 1%, but less than 10%; infrequent – at least 0.1%, but less than 1%; rare – at least 0.01%, but less than 0.1%; very rare (including individual reports) – less than 0.01%; frequency unknown – insufficient data to estimate the frequency of occurrence in the population.

Gastrointestinal disorders: rarely – nausea, constipation.

From the central nervous system: rarely – headache, dizziness, insomnia.

Cardiovascular system disorders: rarely – palpitations; very rarely – decreased blood pressure.

Overdose

There are no data on overdose with Drotaverin-Teva. Symptoms of overdose may be cardiac arrhythmias and conduction disorders (including complete Gis bundle leg block), cardiac arrest, up to death. Treatment: gastric lavage, symptomatic therapy.

Pregnancy use

Drotaverine has no teratogenic and embryotoxic effects. However, the use of Drotaverin-Teva is recommended only after careful weighing of the ratio of expected benefits and possible risks. Due to the lack of necessary clinical data, Drotaverin-Teva is not recommended for administration during breastfeeding.

Similarities

No-shpa, Drotaverine, Spasmonet