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

Smooth muscle spasms in diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, pericholecystitis, cholangitis, papillitis.

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

As an adjuvant therapy (when the tablet form cannot be used): for spasms of smooth muscles of the gastrointestinal tract: peptic ulcer of the stomach and duodenum gastritis spasm of the cardia and pylorus enteritis colitis spastic colitis with constipation irritable bowel syndrome postcholecystectomy syndrome; for gynecological diseases: dysmenorrhea; when conducting some instrumental studies, including cholecystography.

Pharmacological effect

Antispasmodic

ATX code

A03AD02

Pharmacodynamics:

Drotaverine, an isoquinoline derivative, is close in chemical structure and pharmacological properties to papaverine, but has a more pronounced and long-lasting effect.

Drotaverine has a pronounced antispasmodic effect on smooth muscles due to the inhibition of phosphodiesterase-4 (PDE-4). PDE-4 hydrolyzes cyclic 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 (MLCK). Phosphorylation of MLCK leads to a decrease in its affinity for calcium ions – the calmodulin complex, as a result of which the inactivated form of MLCK maintains 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 the PDE-4 isoenzyme without inhibiting the PDE-3 and PDE-5 isoenzymes; therefore, the effectiveness of drotaverine depends on the activity of PDE-4, the content of which varies in different tissues. A high content of PDE-4 is observed in the bile and urinary tract of the uterus and gastrointestinal tract. Hydrolysis of cAMP in the myocardium and smooth muscles of blood vessels occurs mainly with the help of PDE-3, so drotaverine has less effect on the cardiovascular system. Drotaverine is effective against smooth muscle spasms of both neurogenic and muscular origin.

Pharmacokinetics:

Special instructions

When administering drotaverine intravenously 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-type reactions including anaphylactic symptoms and bronchospasm in sensitive individuals, especially those with a history of asthma or allergic diseases. In case of hypersensitivity to disulfite, parenteral use of the drug should be avoided.

Impact on the ability to drive vehicles. Wed and fur.:

During the treatment period, it is not recommended to drive vehicles or engage in activities requiring increased concentration and speed of psychomotor reactions.

Active ingredient

Drotaverine

Composition

1 ml of the drug contains:

Active ingredient:

Drotaverine hydrochloride

20 mg

Excipients:

Ethanol 95%

67 mg

Sodium disulfite

1 mg

Water for injections

up to 1 ml

Pregnancy

The use of the drug during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus.

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

Contraindications

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

– hypersensitivity to sodium disulfite;

– severe liver or kidney failure;

– severe chronic heart failure;

– AV blockade II-III degree;

– children under 18 years of age;

– period of childbirth;

– period of breastfeeding.

With caution:

With arterial hypotension, severe atherosclerosis of the coronary arteries, prostate adenoma, glaucoma, pregnancy.

Side Effects

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

From the cardiovascular system: tachycardia, decreased blood pressure, arrhythmia collapse (with intravenous administration).

From the digestive system: nausea, vomiting, constipation.

Allergic reactions: angioedema, urticaria, rash, itching, anaphylactic shock.

Local reactions: reactions at the injection site.

Other: feeling hot, sweating.

Interaction

Weakens the antiparkinsonian effect of levodopa (increased rigidity and tremor).

Strengthens (especially when administered intravenously) the antispasmodic effect of papaverine bendazole and other antispasmodics including m-anticholinergics.

Strengthens hypotension caused by tricyclic antidepressants quinidine procainamide.

Reduces the spasmogenic activity of morphine.

Phenobarbital enhances the antispasmodic effect of drotaverine.

Overdose

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

Symptoms: atrioventricular block, cardiac arrest, paralysis of the respiratory center.

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

Storage conditions

At a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf life

2 years.

Do not use after the expiration date.

Manufacturer

Grotex LLC, Russia