Drotaverin-Solofarm, 20 mg/ml 2 ml 10 pcs

Spasmodic agent

ATH code

A03AD02

Pharmacodynamics:

Drotaverine is an isoquinoline derivative with a chemical structure and pharmacological properties similar to papaverine but with a more pronounced and prolonged effect.

Drotaverine has a pronounced antispasmodic effect on smooth muscles by inhibiting phosphodiesterase-4 (FDE-4). FDE-4 hydrolyzes cyclic adenosine monophosphate (cAMP) to adenosine monophosphate (AMP). Inhibition of FDE-4 leads to an increase in the concentration of cAMP, which activates cAMP-dependent phosphorylation of myosin light chain kinase (CLKM). Phosphorylation of CLSM leads to a decrease in its affinity for calcium ions, the calmodulin complex, resulting in the inactivated form of CLSM maintaining muscle relaxation. Cyclic adenosine monophosphate also affects the cytosolic concentration of calcium ions by stimulating the transport of calcium ions into the extracellular space and the sarcoplasmic reticulum.

In vitro drotaverine inhibits FDE-4 isoenzyme without inhibiting FDE-3 and FDE-5 isoenzymes, so the effectiveness of drotaverine depends on the activity of FDE-4, which varies in different tissues. A high content of FDE-4 is observed in the biliary and urinary tracts of the uterus and gastrointestinal tract. Hydrolysis of cAMP in myocardium and smooth muscle of blood vessels occurs mainly by FDE-3, so drotaverine has less effect on the cardiovascular system. Drotaverine is effective for smooth muscle spasms of both neurogenic and muscular origin.

Pharmacokinetics:

Indications

Spasms of smooth muscles in diseases of the biliary tract: cholecystolithiasis cholangiolithiasis pericholecystitis cholangitis papillitis.

Spasms of the smooth muscles of the urinary tract: nephrolithiasis urolithiasis pyelitis cystitis spasm of the bladder.

As adjunctive therapy (when the tablet form cannot be used): in spasms of the smooth muscles of the gastrointestinal tract: gastric and duodenal ulcer gastritis cardiac and gateway spasm enteritis colitis spastic colitis with constipation irritable bowel syndrome postcholecystectomy syndrome; in gynecological diseases: dysmenorrhea; in some instrumental studies including cholecystography.

Active ingredient

Composition

The active ingredient:

Drotaverine hydrochloride

20 mg

Excipients:

Ethanol 95%

67 mg

Sodium disulfite

1 mg

Water for injection

up to 1 ml

How to take, the dosage

Intramuscularly 2-4 ml (40-80 mg) 1-3 times a day.

The course of treatment is 1-2 weeks. If prolonged treatment is necessary, the drug is taken orally in tablet form.

In case of acute colic (renal or cholelithiasis) – 2-4 ml (40-80 mg) in 10-20 ml of 09% sodium chloride solution or 5% dextrose solution intravenously slowly (duration of infusion about 30 seconds).

Do not mix in the same syringe with aminophylline solution.

Interaction

Weaken the antiparkinsonian effect of levodopa (increase stiffness and tremor).

Enhances (especially when administered intravenously) the antispasmodic effects of papaverine bendazole and other antispasmodics including m-cholinoblockers.

Enhances hypotension caused by tricyclic antidepressants quinidine procainamide.

Limits the antispasmodic activity of morphine.

Phenobarbital enhances the antispasmodic effects of drotaverine.

Special Instructions

In intravenous administration of Drotaverine in patients with low blood pressure, the patient should be in a horizontal position due to the risk of collapse.

The drug contains disulfite, which may cause allergic reactions including anaphylactic symptoms and bronchospasm in sensitive individuals, especially in those with a history of asthma or allergic diseases. In cases of hypersensitivity to disulfite, parenteral administration of the drug should be avoided.

At the time of treatment, it is not recommended to operate vehicles and machinery or engage in activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

– Hypersensitivity to the active substance or any of the excipients of the drug;

– hypersensitivity to sodium disulfite;

– severe hepatic or renal failure;

– severe chronic heart failure;

– grade II-III AV blockade;

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– childhood under 18 years of age;

– period of childbirth;

– breastfeeding period.

In arterial hypotension marked atherosclerosis of the coronary arteries adenoma prostate glaucoma pregnancy.

Side effects

Central nervous system: headache dizziness insomnia.

Cardiovascular system: tachycardia decreased blood pressure arrhythmia collapse (when administered intravenously).

Digestive system: nausea, vomiting, constipation.

Allergic reactions: angioedema urticaria rash itching anaphylactic shock.

Local reactions: reactions at the site of administration.

Others: fever sweating.

Overdose

In case of overdose, dose-dependent side effects may increase.

Symptoms: atrioventricular block cardiac arrest respiratory center paralysis.

Treatment: In case of overdose, patients should be under close medical supervision and should receive symptomatic therapy and treatment to maintain basic body functions.

Pregnancy use

Prenatal use of the drug is possible only when the estimated benefit to the mother exceeds the potential risk to the fetus.

If it is necessary to use the drug during breastfeeding, it is necessary to consider stopping breastfeeding.

Similarities