Drotaverinum Forte tab. of 80 mg No. 20

Structure and form of release

Structure

Active ingredient: drotaverine;

1 tablet contains a hydrochloride of Drotaverinum 80 mg;

Other components: lactose, monohydrate; potato starch; povidone; magnesium stearate; sodium of a kroskarmeloz.

release Form

Tablet

Pharmacological properties

Pharmacodynamics.

Drotaverinum – the isoquinoline derivative – has spasmolytic effect directly on smooth muscles by oppression of effect of enzyme of phosphodiesterase IV (FDE IV) that leads to increase in concentration of cyclic adenosinemonophosphate (tsAMF) and thanks to an inactivation of a kinase of light chains.

In vitro Drotaverinum inhibits effect of FDE IV enzyme and does not inhibit isoenzymes of phosphodiesterase III (FDE III) and phosphodiesterase V (FDE V). FDE IV has great functional value for decrease in sokratitelny activity of unstriated muscles therefore selective inhibitors of this enzyme can be useful to treatment of the diseases which are followed by hyper mobility and also various diseases during which there are digestive tract spasms.

In cells of unstriated muscles of a myocardium and vessels of tsAMF it is hydrolyzed generally by FDE III isoenzyme therefore Drotaverinum is the effective antispasmodic which does not have considerable side effects from a cardiovascular system and strong therapeutic impact on this system.

at spasms of smooth muscles of both nervous, and muscular origin. Drotaverinum affects smooth muscles of gastrointestinal, biliary, urinogenital and vascular systems, irrespective of type of their autonomous innervation.

It strengthens blood circulation in fabrics thanks to the ability to expand vessels.

Effect of Drotaverinum is stronger than action of a papaverine, absorption is faster and full, it contacts serum proteins less. Advantage of Drotaverinum is also that unlike a papaverine after its parenteral administration such side effect as breath stimulation is not observed.

Pharmacokinetics.

after oral administration. It highly (95–98%) contacts albumine of plasma, gamma and beta globulins. The maximum concentration in blood is reached within 45–60 min. after oral administration. After primary metabolism of 65% of the entered dose comes to blood circulation in not changed look. It is metabolized in a liver. Elimination half-life makes 8–10 hours.

In 72 hours from an organism, about 50% are removed with urine and about 30% – with a stake. Generally Drotaverinum is removed in the form of metabolites, in not changed form in urine it is not found.

Indication

With the medical purpose at:

– the spasms of smooth muscles connected with diseases of a biliary path: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;

– spasms of smooth muscles at diseases of an uric path: nephrolithiasis, ureterolithiasis, pyelitis, cystitis, bladder tenesmus.

As auxiliary treatment at:

– spasms of smooth muscles of digestive tract: a peptic ulcer of a stomach and a duodenum, gastritis, kardio and/or a pylorospasm, enteritis, colitis, a spastic colitis with a constipation and a syndrome of the angry intestines, followed by a meteorism;

– tension headache;

– gynecologic diseases (dysmenorrhea).

Contraindication

Hypersensitivity to Drotaverinum or any component of medicine. Heavy liver, renal or heart failure (syndrome of small warm emission). Deficiency of lactase, galactosemia or glucose galactose sprue.

Route of administration and doses

Adult: the usual average dose makes 120–240 mg/days in 2–3 receptions.

Children of 12 years: in case of need on doctor's orders the maximum daily dose makes 160 mg (divided into 2–4 receptions).

should apply dosage forms of Drotaverinum with the corresponding content of active ingredient To achievement of the appointed medicament doses.

Duration of treatment is defined by the doctor individually.

Children. Use of medicine for treatment of children is younger than 12 years contraindicated.

to Apply

Feature of application

Drug contains lactose. If at the patient the intolerance of some sugars is established, it is necessary to consult with the doctor before accepting this medicine.

Use during pregnancy or feeding by a breast

any signs of direct or indirect impact on pregnancy, embryonic development, childbirth or postnatal development. However pregnant women should appoint medicine with care.

due to the lack of these corresponding researches during feeding.

to Drivers

If after use of medicine observes dizziness, it is necessary to avoid the driving and works requiring special attention.

Overdose

Symptoms: at considerable overdose of Drotaverinum, violations of a warm rhythm and conductivity, including a total block of a ventriculonector and cardiac arrest which can be lethal were observed.

At overdose the patient has to be under careful observation of the doctor and receive the symptomatic and supporting treatment. It is recommended to cause vomiting and/or to wash out a stomach.

Side reactions

Side effects which were observed during clinical trials and, perhaps, were caused by Drotaverinum, distributed on the systems of bodies and frequency of emergence: are very widespread (> 1/10), are widespread (> 1/100, 1/1000, 1/10000

from the immune system: rare: allergic reactions, including a Quincke's disease, a small tortoiseshell, rash, the naggers, a dermahemia, fever, a fever, fervescence, weakness.

from a cardiovascular system: single: cardiopalmus, arterial hypotension.

from nervous system: single: headache, dizziness, insomnia.

from digestive tract: single: nausea, lock, vomiting.

Interaction

phosphodiesterase Inhibitors, such as papaverine, reduce antiparkinsonichesky effect of a levodopa. It is necessary to use with care medicament along with a levodopa as the antiparkinsonichesky effect of the last decreases, and the rigidity and a tremor amplify.

to Store

in original packing at a temperature not above 25 °C. An expiration date - 5 years.

to Store

out of children's reach.