No-shpa, 40 mg tablets 24 pcs

No-shpa is an antispasmodic agent.

Pharmacodynamics

Drotaverine is an isoquinoline derivative. It has a powerful antispasmodic effect on smooth muscle by inhibiting the enzyme phosphodiesterase (PDE).

PDE enzyme is necessary for hydrolysis of cAMP to AMP. Inhibition of FDE 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 (CLSM), phosphorylation of CLSM leads to a decrease in its affinity for the Ca2+-calmodulin complex, resulting in the inactivated form of CLSM supporting muscle relaxation. In addition, cAMP affects the cytosolic concentration of Ca2+ ion by stimulating Ca2+ transport into the extracellular space and the sarcoplasmic reticulum.

This lowering of Ca2+ ion concentration by drotaverine via the cAMP explains the antagonistic effect of drotaverine with respect to Ca2+.

In vitro, drotaverine inhibits the FDE4 isoenzyme without inhibiting the FDE3 and FDE5 isoenzymes. Therefore, the efficacy of drotaverine depends on the concentrations of FDE4 in tissues, which vary from tissue to tissue. FDE4 is most important for suppression of contractile activity of smooth muscles, therefore selective inhibition of FDE4 may be useful for treatment of hyperkinetic dyskinesias and various diseases accompanied by spastic state of the GIT.

The hydrolysis of CAMP in the myocardium and vascular smooth muscle occurs mainly by isoenzyme FDE3, which explains the fact that with high antispasmodic activity, drotaverine has no serious side effects on the heart and vessels and pronounced effects on the CSS.

Drotaverine is effective for smooth muscle spasms of both neurogenic and muscular origin. Regardless of the type of autonomic innervation, drotaverine relaxes the smooth muscles of the gastrointestinal tract, biliary tract, and urogenital system.

Due to its vasodilator effect, drotaverine improves blood flow to tissues.

Pharmacokinetics

Drotaverine when taken orally is quickly and completely absorbed from the gastrointestinal tract. Absorption is 100%. However, after metabolism during the first passage through the liver, 65% of the administered dose enters the systemic bloodstream. Cmax in plasma is reached after 45-60 min.

In vitro drotaverine has high binding to plasma proteins (95-97%), especially to albumin, γ- and β-globulins.

Drotaverine is evenly distributed in tissues, penetrates smooth muscle cells. It does not penetrate through the HEB. Drotaverine and/or its metabolites may slightly penetrate through the placental barrier.

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

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

Indications

Urolithiasis, Colic, Headache, Painful menstruation (algodysmenorrhea), Gastroduodenitis, Gallstone disease, Colitis, Gallic colic, Abdominal bloating, Pain

• Spasms of smooth muscles associated with diseases of biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis.
• spasms of the smooth muscles of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder tenesm.

Auxiliary therapy:

• In spasms of the smooth muscles of the gastrointestinal tract: Gastric and duodenal ulcers, gastritis, cardiac and gatekeeper spasms, enteritis, colitis, spastic, colitis with constipation and irritable bowel syndrome with flatulence after excluding diseases manifesting the “acute stomach” syndrome (appendicitis, peritonitis, perforated ulcer, acute pancreatitis, etc.
• Tension headaches.
• Dysmenorrhea.

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Active ingredient

Drotaverine

Composition

Active substance:

drotaverine hydrochloride;

Supplementary substances:

magnesium stearate;

talc;

povidone;

corn starch;

lactose monohydrate.

How to take, the dosage

Ingestion.

The average daily dose is usually 120-240 mg (the daily dose is divided into 2-3 doses).

Interaction

Levodopa. When used concomitantly, drotaverine may weaken the anti-Parkinsonian effect of levodopa, i.e., increase stiffness and tremor.

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

Morphine. Reduction of the spasmogenic activity of morphine.

Phenobarbital. Enhancement of the antispasmodic action of drotaverine.

Special Instructions

The use of the drug in case of arterial hypotension requires increased caution.

Each tablet contains 104 mg of lactose.

Lactose can take up to 156 mg (1.5 tablets) when taken, which can cause GI disorders in patients who are lactose intolerant.

The tablets are not appropriate for patients with lactose deficiency, galactosemia, or impaired glucose/galactose absorption syndrome (see Contraindications).

Impact on the ability to drive a car or perform work requiring increased speed of physical and mental reactions.

When taken orally in therapeutic doses, drotaverine has no effect on the ability to drive and perform work requiring increased attention.

If any side effects occur, driving and operating machinery require individual consideration.

In case of dizziness, potentially hazardous activities such as driving and operating machinery should be avoided.

Contraindications

• High sensitivity to drotaverine and/or excipients in the drug;
• Extensive hepatic or renal impairment;
• Heart insufficiency (decreased cardiac output)
• hereditary lactose intolerance, lactose deficiency, galactosemia or syndrome.
• Healthy 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

Systemic system disorders: rarely – palpitations, decreased blood pressure.

CNS disorders: rarely – headache, dizziness, insomnia.

Gastrointestinal disorders: rarely – nausea, constipation.

The immune system: rare – allergic reactions (angioedema, urticaria, rash, itching); unknown frequency of anaphylactic shock with and without fatal outcome has been reported with the use of the drug.

Overdose

Symptoms: cardiac rhythm and conduction disorders, including complete Gis bundle leg block and cardiac arrest, which can be fatal.

Treatment: In cases of overdose, patients should be under medical supervision and, if necessary, should receive symptomatic and supportive treatment for basic body functions, including induction of vomiting or gastric lavage.

Pregnancy use

During pregnancy and lactation can be used when indicated.

It is contraindicated in children under 6 years of age.

Similarities

No-shpa, Drotaverine, Spasmonet, Drotaverine-Teva