No-shpa - 64 tablets, drotaverin 40mg, for abdominal pain

Round biconvex tablets of yellow with a greenish or orange tinge, with spa engraving on one side.

Pharmacodynamics

Drotaverine is an isoquinoline derivative that exhibits a potent antispasmodic effect on smooth muscle by inhibiting the type IV phosphodiesterase enzyme (PDE IV).

Inhibition of the enzyme PDE IV leads to an increase in the concentration of cAMP, inactivation of myosin light chain kinase, which further causes relaxation of smooth muscles.

The effect of drotaverine through cAMP, which reduces the concentration of Ca 2+ ions, explains the antagonistic effect of drotaverine in relation to Ca 2+ ions.

In vitro, drotaverine inhibits the PDE IV enzyme without inhibiting the PDE III and PDE V enzymes.

Therefore, the effectiveness of drotaverine depends on the concentrations of PDE IV in different tissues.

PDE IV is most important for suppressing the contractile activity of smooth muscles, and therefore selective inhibition of PDE IV may be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by a spastic state of the gastrointestinal tract.

Hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs mainly with the help of the enzyme PDE III, which explains the fact that with high spasmolytic activity, drotaverine does not have serious side effects from the heart and blood vessels and pronounced effects on the cardiovascular system.

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 the genitourinary system.

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

Thus, the above-described mechanisms of action of drotaverine eliminate smooth muscle spasm, which leads to a decrease in pain.

Pharmacokinetics

Absorption

Compared with papaverine, when taken orally, drotaverine is absorbed faster and more completely from the gastrointestinal tract.

After presystemic metabolism, 65% of the taken dose of drotaverine enters the systemic circulation.

The maximum concentration (C max) of drotaverine in the blood plasma is reached after 45-60 minutes.

Distribution

In vitro, drotaverine has a high binding to plasma proteins (95-98%), especially albumin,?

and? - globulins.

Drotaverine is evenly distributed in tissues, penetrates into smooth muscle cells.

Does not penetrate the blood-brain barrier.

Drotaverine and / or its metabolites can slightly penetrate the placental barrier.

Metabolism

Drotaverine is almost completely metabolized in the liver.

Withdrawal

The half-life of drotaverine is 8-10 hours.

Within 72 hours, drotaverine is almost completely excreted from the body.

About 50% of drotaverine is excreted by the kidneys and about 30% through the gastrointestinal tract.

Drotaverine is mainly excreted in the form of metabolites, the unchanged form of drotaverine is not found in urine.

Name ENG

NO-SPA

Clinical and pharmacological group

Myotropic antispasmodic

ATX code

A03A D02

Dosage

drotaverine hydrochloride - 40 mg

Structure

1 tablet contains:

active substance: drotaverine hydrochloride - 40 mg

excipients: magnesium stearate - 3 mg, talc - 4 mg, povidone - 6 mg, starch

corn - 35 mg, lactose monohydrate - 52 mg.

Indications

Spasms of smooth muscles in diseases of the biliary tract: cholecystolithiasis,

cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis.

- Spasms of smooth muscles of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis,

cystitis, bladder spasms.

As adjunctive therapy

- With spasms of smooth muscles of the gastrointestinal tract: peptic ulcer

stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis,

colitis, spastic colitis with constipation, irritable bowel syndrome with flatulence.

- With tension headaches.

- With dysmenorrhea (menstrual pain).

Storage conditions and periods

At a temperature of 15-25 degrees. (In the original packaging) - bottles

at a temperature not higher than 25 degrees.

- blisters.

Expiration date: 3 years

5 years - vials

Contraindications

Hypersensitivity to the active substance or to any of

excipients of the drug.

- Severe hepatic or renal impairment.

- Severe heart failure (low cardiac output syndrome).

- Children under 6 years old.

- Breastfeeding period (lack of clinical data).

- Hereditary galactose intolerance, lactase deficiency and malabsorption syndrome

glucose-galactose (due to the presence of lactose monohydrate in the preparation).

Carefully

- With arterial hypotension.

- In children (lack of clinical experience of use).

- In pregnant women (see the section Use during pregnancy and breastfeeding

feeding ").

INN / Active ingredient

drotaverine hydrochloride

Specifications

Category

Pain relievers

Scope of the medicinal product

General

Release form

Tablet

Manufacturer country

Hungary

Package quantity, pcs

64

Scope of application

Gastroenterology

,

obstetrics and gynecology

Minimum age from

6 years

Way of introduction

Through the mouth

Vacation conditions

Without recipe

Brand name

Sanofi

The amount of the dosage form in the primary package

64 pcs.

Primary packaging type

Bottle

Type of consumer packaging

Pack of cardboard

Pharmaco-therapeutic group

Antispasmodic

Anatomical and therapeutic characteristics

A03AD02 Drotaverin

Dosage form

Pills

Packaging

Box

The target audience

Adult

Dosage (volume) of the substance in the preparation

drotaverine hydrochloride - 40 mg

Expiration date in days

1826

Package weight, g

twenty

Mode of application

:

1-2 tablets at a time 2-3 times a day.

The maximum daily dose is 6 tablets (which

corresponds to 240 mg).

Children

Clinical studies on the use of drotaverine in children have not been conducted.

In the case of the appointment of drotaverine to children:

- from 6 to 12 years: 1 tablet at a time, 1-2 times a day.

Maximum daily dose - 2

tablets (corresponding to 80 mg)

- over 12 years old: 1 tablet at one time 1-4 times a day or 2 tablets at one time 1-2

once a day.

The maximum daily dose is 4 tablets (which corresponds to 160 mg). When taking the drug without consulting a doctor, the recommended duration of administration

the drug is usually 1-2 days.

In cases where drotaverine is used as

auxiliary therapy, the duration of treatment without consulting a doctor may be

more (2-3 days).

If pain persists, the patient should see a doctor.

Information on technical characteristics, delivery set, country of manufacture "