Producer
Experimental Plant "DNCLZ", LLC for "Vertex FF, LLC", Kharkiv, Ukraine
international name
Drotaverine
PBX code
Drotaverine - A03AD02
Pharmacotherapeutic group
Drugs used for functional gastrointestinal disorders. Drotaverine.
Registration
No. UA / 10344/01/02 from 01.09.2010 to 01.09.2015. Order No. 752 (1) from 01.09.2010
composition of the medicinal product:
Active ingredients: drotaverine;
1 tablet contains drotaverine hydrochloride in terms of 100% dry substance 80 mg;
Excipients: lactose monohydrate, potato starch, povidone, magnesium stearate, croscarmellose sodium.
Dosage form.
Pills.
Tablets are light yellow to yellowish-green in color.
Name and location of the manufacturer.
Limited Liability Company "Research Plant" DNTSLZ ", Ukraine.
Ukraine, 61057, Kharkiv, Vorobyova St., 8.
Pharmacotherapeutic group.
Drugs used for functional gastrointestinal disorders.
PBX code A03A D02.
Drotaverine is an isoquinoline derivative that has an antispasmodic effect on smooth muscles by inhibiting the action of the enzyme phosphodiesterase IV (PDE IV), which causes an increase in the concentration of cAMP I, due to the inactivation of myosin light chain kinase (MLCK), which is produced in relaxed smooth muscle.
In vitro, drotaverine inhibits the action of the enzyme PDE IV and inhibits the isoenzymes phosphodiesterase III (PDE III) and phosphodiesterase V (PDE V). PDE IV has a great functional importance in reducing the contractile activity of smooth muscles, therefore, selective inhibitors of this enzyme may be useful for the treatment of diseases accompanied by hypermotility, as well as various diseases during which spasms of the gastrointestinal tract occur.
In the cells of the smooth muscles of the myocardium and blood vessels, cAMP is hydrolyzed mainly by the PDE III isoenzyme, therefore drotaverine is an effective antispasmodic agent that does not have significant side effects on the cardiovascular system and has a strong therapeutic effect on this system.
Drotaverine is effective in spasms of smooth muscles of both nervous and muscular origin. Drotaverine acts on the smooth muscles of the gastrointestinal, biliary, genitourinary and vascular systems, regardless of the type of their autonomic innervation.
The remedy enhances blood circulation in tissues due to its ability to dilate blood vessels.
The effect of drotaverine is stronger than that of papaverine, absorption is faster and more complete, it binds less to serum proteins. The advantage of drotaverine is also that, unlike papaverine, after its parenteral administration, there is no such side effect as respiratory stimulation.
Drotaverine is rapidly and completely absorbed after oral administration. It is highly (95-98%) bound to plasma proteins, especially albumin, gamma- and beta-globulins. The maximum concentration is reached within 45-60 minutes after oral administration. After primary metabolism, 65% of the dose taken enters the bloodstream unchanged.
Metabolized in the liver. Half-life is estimated at 8-10 hours.
Within 72 hours, drotaverine is almost completely excreted from the body, more than 50% is excreted in the urine and about 30% in the feces. Drotaverine is mainly excreted in the form of metabolites; it is not detected in the urine in unchanged form.
Indications for! Application.
For therapeutic purposes in adults with:
- smooth muscle spasms associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;
- spasms of smooth muscles in diseases of the urinary tract: nephrolithiasis, ureterolithiasis, pyelitis, cystitis, tenesmus of the urinary bladder.
As an adjunctive treatment for:
- spasms of smooth muscles of the gastrointestinal tract: gastric and duodenal ulcer, gastritis, cardio- and / or pylorospasm, enteritis, colitis, spastic colitis with lock and irritable bowel syndrome, which is accompanied by flatulence;
- tension headache;
- gynecological diseases (dysmenorrhea).
Contraindication.
Hypersensitivity to drotaverine or any component of the drug. Severe hepatic, renal or heart failure (small cardiac output syndrome). Lactase deficiency, galactosemia or glucose-galactose malabsorption syndrome. Breastfeeding period. Children's age.
Special precautions.
Use with special caution in case of arterial hypotension.
Each tablet of Drotaverine Forte contains 104 mg of lactose. When used in accordance with the recommended doses, up to 156 mg of lactose may enter the body per dose, which may cause gastrointestinal complaints in patients suffering from lactose intolerance.
Not used to treat patients with lactase deficiency, galactosemia or glucose-galactose malabsorption syndrome.
! Use during pregnancy or breastfeeding.
As shown by the results of retrospective clinical studies, oral administration of the drug did not cause any cases of teratogenicity and embryotoxicity. However, during pregnancy, the drug is recommended to be prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus.
Due to the lack of relevant RESEARCH data during breastfeeding! The use of the drug is not recommended.
Ability to influence the SPEED of reactions when driving or working with other mechanisms.
If after using the drug dizziness is observed, you should avoid driving and performing work that requires increased attention.
Children: Do not use.
Method! Application and dosage.
Adults are prescribed orally. The usual average dose is 120 - 240 mg per day in 2 - 3 doses. The duration of treatment is determined individually.
Overdose.
There is no data on overdose of drotaverine. In case of overdose, the patient should be under close medical supervision and receive symptomatic and supportive treatment. It is recommended to induce vomiting and/or gastric lavage.
Side effects.
Side effects observed during clinical studies and possibly caused by drotaverine are listed by system organ class and frequency of occurrence: very common (> 1/10), common (> 1/100, <1/10), uncommon (> 1/1000, <1/100), rare (> 1/10,000, <1/1000), very rare (<1/10,000).
On the part of the digestive tract: Rarely - Nausea, constipation.
From the nervous system: Rarely common - headache, dizziness, insomnia.
From the cardiovascular system: Rarely, common - tachycardia, arterial hypotension.
There are SOME REPORTS of cases of allergic reactions, including angioedema.
Interaction with other drugs and other types of interactions.
Phosphodiesterase inhibitors (No-Spa Forte, Papaverine) reduce the antiparkinsonian effect of levodopa.
Drotaverine forte should be used with caution simultaneously with levodopa, since the antiparkinsonian effect of the latter is reduced, and rigidity and tremor are increased.
Expiration date.
5 years.
Storage conditions.
Store in a place protected from light at a temperature not exceeding 25 °C.
Keep out of the reach of children.
Packaging.
10 or 20 tablets in a blister; 1 blister in a cardboard pack.
10 tablets in a blister; 2 blisters in a cardboard pack.
Vacation category.
Without a prescription.
