Description
Release form
Solution for intravenous and intramuscular administration.
Pharmacological action
Drotaverinum is a derivative of isoquinoline, in chemical structure and pharmacological properties it is close to papaverine, but it has a more pronounced and long-lasting effect. Drotaverin 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).
bending of PDE-4 leads to an increase in cAMP concentration, which activates cAMP-dependent phosphorylation of myosin light chain kinase (MLC). Phosphorylation of MLCK leads to a decrease in its affinity for the calcium-calmodulin complex, as a result of which the inactivated form of MLCK supports muscle relaxation of cAMP, in addition, affects the cytosolic concentration of calcium, due to the stimulation of calcium transport to extracellular space and sarcoplasmic reticulum.
In vitro drotaverin inhibits PDE-4 isoenzyme without inhibiting PDE-3 and PDE-5 isoenzymes, therefore, the effectiveness of drotaverine depends on the activity of PDE-4, the content of which in different tissues is different.
High levels of PDE-4 are found in the bile and urinary tract, uterus, and the gastrointestinal tract (GIT). The hydrolysis of cAMP in the myocardium and smooth muscle of blood vessels occurs mainly with the help of PDE-3, therefore drotaverin has less effect on the cardiovascular system.
Drotaverinum is effective for spasms of smooth muscles of both neurogenic and muscular origin.
Indications
– smooth muscle spasms associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis.
– spasms of smooth muscles of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, tenesmus of the bladder.
As an adjuvant (when the dosage form: tablets cannot be used):
– for smooth muscle spasms of gastrointestinal origin: gastric and duodenal ulcer, gastritis, cardia and pyloric spasms, enteritis, colitis
– for gynecological diseases: dysmenorrhea, severe labor pains.
Contraindications
– Hypersensitivity to the active substance or to any of the excipients of the drug.
– Hypersensitivity to sodium disulfite (see Special instructions).
– Severe hepatic and renal failure.
– Severe chronic heart failure.
– Children under 18 years old.
– Lactation.
Use during pregnancy and lactation
As reproductive studies in animals and clinical studies have shown, the use of drotaverine during pregnancy did not have any teratogenicity, no embryotoxic effect.
In pregnant women, the use of drotaverine is possible only in cases where the potential benefit to the mother outweighs the potential risk to the fetus.
Due to the lack of necessary clinical data, it is not recommended to use the drug during lactation.
Composition of
1 ml of solution contains:
Active ingredient:
Drotaverina hydrochloride – 20 mg
Excipients:
sodium disulfite – 1 mg,
ethanol 96% – 66 mg,
water for injection up to 1 ml.
Dosage and administration
Dose set individually. For adults, the drug is usually administered intramuscularly, 2-4 ml (40-80 mg) 1-3 times a day.
To relieve hepatic or renal colic, it is recommended to inject 40-80 mg intravenously, slowly.
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 than 1/10000, including individual messages.
From the central nervous system: infrequently – headache, dizziness, insomnia.
From the cardiovascular system: infrequently – tachycardia, lowering blood pressure, collapse (with intravenous administration).
From the digestive system: infrequently – nausea, constipation.
Allergic reactions: infrequently – angioedema, urticaria, skin rash, itching.
Overdose
In case of overdose, patients should be carefully monitored and symptomatic therapy and treatment should be carried out to maintain the basic functions of the body.
Storage conditions
In the dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
Expiration
3 years
Deystvuyuschee substances
Drotaverine
Terms and conditions otpuska IZ pharmacy prescription
Dosage form
solution for injection and infusion
Appointment
Adult, Adult doctor’s appointment p15rorew473 Lactating mothers
