No-spa solution 20mg/ml 2ml ampoules, 25pcs

Composition

Active ingredient:

drotaverine hydrochloride;

Auxiliary substances:

sodium disulfite (sodium metabisulfite) — 2 mg;

ethanol 96% – 132 mg;

water for injection-up to 2 ml

Pharmacological action

No-spa is an antispasmodic agent.

Pharmacodynamics

Drotaverine is a derivative of isoquinoline. It has a powerful antispasmodic effect on smooth muscles due to inhibition of the enzyme phosphodiesterase (PDE). The enzyme PDE is necessary for the hydrolysis of cAMP to AMP.

Inhibition of PDE leads to an increase in the concentration of cAMP, which triggers the following cascade reaction: high concentrations of cAMP activate cAMP-dependent phosphorylation of myosin light chain kinase (MLCM), phosphorylation of MLCM leads to a decrease in its affinity for the Ca2+-calmodulin complex, as a result of which the inactivated form of MLCM supports muscle relaxation. cAMP also affects the cytosolic concentration of the Ca2+ion by stimulating the transport of Ca2+ into the extracellular space and sarcoplasmic reticulum. This Ca2+ – lowering effect of drotaverine via cAMP explains the antagonistic effect of drotaverine with respect to Ca2+.

In vitro, drotaverine inhibits the PDE4 isoenzyme without inhibiting the PDE3 and PDE5 isoenzymes. Therefore, the effectiveness of drotaverine depends on the concentrations of PDE4 in the tissues, which differ in different tissues. PDE4 is most important for suppressing the contractile activity of smooth muscles, and therefore selective inhibition of PDE4 can be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by a spastic state of the gastrointestinal tract.

cAMP hydrolysis in the myocardium and vascular smooth muscle occurs mainly with the help of PDE3 isoenzyme, which explains the fact that with high antispasmodic activity, drotaverine has no serious side effects from the heart and blood vessels and pronounced effects on CVS.

Drotaverine is effective in treating smooth muscle spasms of both neurogenic and muscular origin. Regardless of the type of vegetative innervation, drotaverine relaxes the smooth muscles of the gastrointestinal tract, biliary tract, and genitourinary system.

Due to its vasodilating effect, drotaverine improves blood supply to tissues.

Pharmacokinetics

Drotaverine is rapidly and completely absorbed from the gastrointestinal tract when taken orally. The absorption rate is 100%. However, after metabolism, at the first passage through the liver,65% of the dose taken enters the systemic bloodstream. Cmax in plasma is reached in 45-60 minutes.

In vitro, drotaverine is highly bound to plasma proteins (95-97%), especially albumin, gamma – and beta-globulins.

Drotaverine is evenly distributed throughout the tissues, penetrates into smooth muscle cells. It does not penetrate the BBB. Drotaverine and / or its metabolites may only slightly cross the placental barrier.

In humans, drotaverine is almost completely metabolized in the liver by O-deethylation. Its metabolites rapidly conjugate with glucuronic acid. The main metabolite is 4′ – desethyldrotaverine, in addition to which 6-desethyldrotaverine and 4′-desethyldrotaveraldine have been identified.

T1 / 2 of drotaverine is 8-10 hours. Within 72 hours, drotaverine is almost completely eliminated from the body. More than 50% of the drug is excreted by the kidneys (mainly in the form of metabolites) and about 30% — through the gastrointestinal tract (bile excretion). Unchanged drotaverine is not detected in the urine.

Indications

• stomach and intestinal spasms
• renal colic
• painful menstruation
• increased excitability of the uterus during pregnancy
• biliary dyskinesia, biliary colic, cholecystitis.

Use during pregnancy and lactation

During pregnancy and lactation, it can be used according to indications.

Contraindicated in children under 6 years of age.

Contraindications

• hypersensitivity to drotaverine and / or excipients included in the preparation;
• severe hepatic or renal insufficiency;
• severe heart failure (decreased cardiac output);
• hereditary lactose intolerance, lactase deficiency, galactosemia or glucose/galactose malabsorption syndrome (due to the presence of lactose in the preparation).

With caution:  arterial hypotension.

Side effects

From the CCC side:  rarely-rapid heartbeat, decreased blood pressure.

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

From the gastrointestinal tract:  rarely — nausea, constipation.

From the immune system:  rarely-allergic reactions (angioedema, urticaria, rash, pruritus); unknown frequency — with the use of the drug, the development of anaphylactic shock with or without a fatal outcome has been reported.

Interaction

Levodopa. When used concomitantly, drotaverine may weaken the antiparkinsonian effect of levodopa, i. e. increase rigidity and tremor.

Papaverine, bendazole and other antispasmodics (including m-cholinolytics). Increased antispasmodic effect.

Morphine. Reduction of spasmodic activity of morphine.

Phenobarbital. Increased antispasmodic effect of drotaverine.

How to take, course of use and dosage

Intramuscularly, intravenously.

Adults: the average daily dose is 40-240 mg divided into 1-3 I / m injections.

In acute renal and cholelithiasis colic — 40-80 mg IV, slowly (the duration of use is about 30 seconds).

Overdose

Symptoms:  cardiac arrhythmias and conduction disorders, including complete blockage of the bundle branch legs and cardiac arrest, which can be fatal.

Treatment:  in case of overdose, patients should be under medical supervision, and if necessary, they should receive symptomatic and maintenance-oriented treatment, including induction of vomiting or gastric lavage.

Special instructions

Contains sodium disulfite, which may cause allergic reactions, including anaphylactic symptoms and bronchospasm in sensitive individuals, especially those with asthma or a history of allergic diseases.

In case of hypersensitivity to sodium disulfite, parenteral use of the drug should be avoided (see “Contraindications”).

When intravenous drotaverine is administered in patients with low blood pressure, the patient should be in a horizontal position due to the risk of collapse.

Influence on the ability to drive a car or perform work that requires an increased rate of physical and mental reactions.

During the treatment period, it is necessary to refrain from driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Solution for intravenous and intramuscular use

Storage conditions

At a temperature not exceeding 25 °C.

Shelf life

5 years

Active ingredient

Drotaverine

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion

Description

For pregnant women as prescribed by a doctor, For adults as prescribed by a doctor

Indications

Cholecystitis, Gastroduodenitis, Urolithiasis, Spasm of the gastrointestinal tract, Cholelithiasis, Threatened Miscarriage, Colitis, Enteritis