Drotaverin-UBF - instructions for use, dose, side effects, contraindications

Drotaverin is a derivative of isoquinoline, it is close in chemical structure and pharmacological properties to papaverine, but it has a more pronounced and prolonged effect. Drotaverine has a pronounced antispasmodic effect on smooth muscles due to inhibition of phosphodiesterase-4 (PDE-4). PDE-4 hydrolyses adenosine monophosphate (cAMP) to adenosine monophosphate (AMP). Inhibition of PDE-4 leads to an increase in the concentration of cAMP, which activates cAMP-dependent phosphorylation of myosin light chain kinase (CMLC). Phosphorylation of CLCM leads to a decrease in its affinity for the Ca2 + -calmodulin complex, as a result of which the inactivated form of CLCM supports muscular relaxation of cAMP, In addition, it affects the cytosolic concentration of calcium ions by stimulating the transport of calcium ions into the extracellular space and the sarcoplasmic reticulum.

In vitro drotaverin inhibits the isoenzyme PDE-4 without inhibiting the isoenzymes PDE-3 and PDE-5, therefore the effectiveness of drotaverin depends on the activity of PDE-4, the content of which in different tissues is different. High content of PDE-4 is noted in the bile and urinary tract, uterus, gastrointestinal tract. The hydrolysis of cAMP in the myocardium and smooth muscles of blood vessels is mainly due to PDE-3, therefore drotaverine less affects the cardiovascular system. Drotaverine Effective in spasms of smooth muscles, both neurogenic and muscular.

Pharmacokinetics:

Quickly and well absorbed into the gastrointestinal tract. Absorption - 100%. However, 65% of the accepted dose (the "first pass" effect through the liver) enters the systemic circulation. Time to reach the maximum concentration (TCmah) - 45-60 minutes.

The connection with plasma proteins is 95-97%, mainly with albumin, gamma and beta globulins, as well as high-density lipoproteins. Evenly distributed on the tissues, penetrates into the smooth muscle cells. Does not penetrate the blood-brain barrier. Drotaverine and / or its metabolites can penetrate insignificantly through the placental barrier.

Almost completely metabolized in the liver by O-de-ethylation. Metabolites are rapidly conjugated with glucuronic acid. The main metabolite is 4-desethyltraderin, the other metabolites are 6-desethyltraderin and 4-deethyldrothaveraldin.

Half-life (T1/2) - 8-10 hours. For 72 hours almost completely removed from the body, more than 50% of the kidneys (mainly in the form of metabolites) and about 30% of the intestine. Unchanged drotaverine in the urine is not found.

Indications:

Spasm of smooth muscles in diseases of the bile ducts: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, inflammation of the papilla of the duodenum.

Spasm of smooth muscles in diseases of the urinary tract: nephrourolythiasis, urethrolithiasis, pyelitis, cystitis, bladder spasm.

As an auxiliary therapy: with spasms of smooth muscles of the gastrointestinal tract: peptic ulcer of stomach and duodenum, gastritis, spasm of cardia and pylorus, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome, with flatulence; tensor headache; Algodismenorea, threatening miscarriage, threatening premature birth; spasm of uterus pharynx during labor, prolonged disclosure of throat, postnatal fights.

When: conducting some instrumental studies, including cholecystography.

Contraindications:

Hypersensitivity, expressed hepatic and renal insufficiency, severe chronic heart failure, lactose deficiency, lactose intolerance, glucose-galactose malabsorption.

The dosage form in this dosage is not used in children under 12 years of age.

Carefully:

With caution appoint the drug to patients with severe arteriosclerosis of the coronary arteries, prostatic hyperplasia, glaucoma.

Pregnancy and lactation:The drug is contraindicated in pregnancy and lactation.

Dosing and Administration:

Adults prescribe inside for 40 - 80 mg (1-2 tablets) 2-3 times a day.

Children over 12 years of age prescribe 40 mg (1 tablet) 1-3 times a day.

Side effects:

Frequency: very often - more than 1/10, often - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, rarely - more than 1/10000 and less than 1/1000, very rarely - more 1/10000, including individual messages.

From the central nervous system: infrequently - headache, dizziness, insomnia.

From the cardiovascular system: infrequently - tachycardia, lowering blood pressure.

From the digestive system: infrequently - nausea, constipation.

Allergic reactions: infrequently - angioedema, urticaria, rash, itching.

If Any of the side effects indicated in the manual are aggravated, or you notice any other side effects not listed in the instructions, inform the doctor about it.

Overdose:

In high doses, it disrupts the atrioventricular conduction, reduces the excitability of the heart muscle, can cause heart failure and paralysis respiratory center.

Treatment: withdrawal of the drug, symptomatic therapy.

Interaction:

Relieves the antiparkinsonian effect of levodopa (increased rigidity and tremor).Enhances the spasmolytic effect of papaverine, bendazole, and other antispasmodics, including m-holinoblokatory.

Reduces the spasmogenic activity of morphine.
Phenobarbital enhances spasmolytic action drotaverina.

Effect on the ability to drive transp. cf. and fur:When ingestion should refrain from driving vehicles and employment by potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets of 40 mg.

Packaging:

For 10, 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered or paper with a polymer coating. By 20, 25, 30, 40, 50, 60 tablets in cans of polymeric.

Each bank or 1,2, 3, 4, 5 contour packs of 10 tablets together with the instruction for use are placed in a pack of cardboard for consumer containers.

Banks of polymer or contour packs of 10, 20 tablets with an equal number of instructions for use are placed in a bag of polyethylene film or a box of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:P N002247 / 01

Date of registration:08.09.2008 / 11.09.2012

The owner of the registration certificate:URALBIOFARM, OJSC URALBIOFARM, OJSC Russia

Manufacturer: & nbsp

URALBIOFARM, OJSC Russia

Information update date: & nbsp16.06.2016

Illustrated instructions

Instructions

Drotaverin-UBF (Drotaverine-UBF)