Ple-Spa - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 31.75 mg, calcium phosphate 25.00 mg, calcium hydrophosphate 13.00 mg, carboxymethyl starch sodium 11.00 mg, sodium lauryl sulfate 2.00 mg, silicon dioxide colloid 1.75 mg, povidone 2.00 mg, magnesium stearate 1.50 mg.

Film Sheath: a ready-mix for film coating [hypromellose 35.0% macrogol-6000 12.0%, titanium dioxide 23.0%, lactose monohydrate 25.0%, talc 5.0%] 3.9 mg, quinoline yellow color 0.1 mg.

Description:Round biconvex tablets, covered with a film membrane, yellow.

Pharmacotherapeutic group:Spasmolytic agent

ATX: & nbsp

A.03.A.D.02 Drotaverine

Pharmacodynamics:

Drotaverin is a derivative of isoquinoline, it is close in chemical structure and pharmacological properties to papaverine, but it has a more pronounced and prolonged effect. Drotaverine has a pronounced spasmolytic effect on smooth muscles due to the inhibition of phosphodiesterase-4, which hydrolyses the cyclo-adenosine monophosphate (c-AMP) to adenosine monophosphate. Inhibition phosphodiesterase-4 (PDE-4) leads to an increase in the concentration (c-AMP), which activates the c-AMP-dependent phosphorylation of the myosin light chain kinase. Phosphorylation of myosin light chain kinase leads to a decrease in its affinity for calcium-calmodulin complex, as a result of which the inactivated form kinase light chain myosin supports muscle relaxation. Cyclo-adenosine monophosphate, in addition, affects the cytosolic concentration of calcium (Ca2 +), due to the stimulation of the transport of Ca2 + into the extracellular space and sarcoplasmic reticulum.

In vitro inhibits the enzyme PDE-4 without suppression of isoenzymes PDE-3 and PDE-5, therefore the effectiveness of drotaverine depends on the activity of PDE-4, the content of which in different different tissues. A high content of phosphodiesterase-4 is noted in bile and urinary tract, uterus, gastrointestinal tract. Hydrolysis of c-AMP in the myocardium and smooth muscles of blood vessels occurs mainly with the help of PDE-3, therefore, drotaverine less affects the cardiovascular system. Drotaverine Effective in spasms of smooth muscles, both neurogenic and muscular.

Pharmacokinetics:

Quickly and well absorbed in the gastrointestinal tract. Absorption - 100%.

However, 65% of the dose received enters the systemic circulation (the effect of the "first passing through the liver.) Time to reach the maximum concentration (TCmah) 45-60 minutes. The connection with plasma proteins is 95-97%, mainly with albumin, gamma and beta-globulins, as well as lipoproteins, high, density. Evenly distributed on the tissues, penetrates into the smooth muscle cells. Does not penetrate the blood-brain barrier. Drotaverine and / or its metabolites can penetrate insignificantly through the placental barrier.

Almost completely metabolized in the liver by O-de-ethylation. Metabolites are rapidly conjugated with glucuronic acid. The main metabolite is 4-desethyltraderin, other metabolites are 6-deethyldroverine and 4-desethylditaveraldine.

The half-life (T1 / 2) is 8-10 hours.For 72 hours almost completely removed from the body, more than 50% of the kidneys, (mainly in the form of metabolites) and about 30% of the intestines. Unchanged drotaverine in the urine is not found.

Indications:

Spasm of smooth muscles in diseases of bile ducts: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, inflammation of the papilla duodenum.

Spasm of smooth muscles in diseases of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder tenesmus.

As an auxiliary therapy:

with spasms of smooth muscles of the gastrointestinal tract: peptic ulcer of stomach and duodenum, gastritis, spasms of cardia and pylorus, enteritis, spastic colitis, irritable bowel syndrome;

tensor headache;
dysmenorrhea.

In carrying out some instrumental research, incl. cholecystography.

Contraindications:

- hypersensitivity to the active substance or other components of the finished dosage form;

- severe hepatic or renal insufficiency;

- severe heart failure;

- the period of childbirth;

- lactation period;

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption (the preparation contains lactose monohydrate);

- children under 12 years (for this dosage form).

Carefully:

- arterial hypotension;

- pronounced atherosclerosis of the coronary vessels;

- hyperplasia of the prostate;

- glaucoma;

- during pregnancy.

Pregnancy and lactation:

Drotaverin does not have teratogenic and embryotoxic effects. but use of the drug during pregnancy (possible only if The estimated benefit to the mother exceeds the potential risk to the fetus.

Due to the lack of necessary clinical data drotaverine Not recommended appoint in the period lactation, during the treatment should stop breastfeeding.

Dosing and Administration:

Inside, adults and children over 12 years - 40-80 mg 2-3 times a day.

The maximum single dose is 80 mg, the maximum daily dose is 240 mg.

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.

From the digestive system: infrequently - nausea; constipation.

Allergic reactions: rarely - angioedema, urticaria, rash, itching; frequency unknown - anaphylactic shock.

Overdose:

No cases of overdose have been reported.

Interaction:

Relieves the antiparkinsonian effect of levodopa (increased rigidity and tremor). Strengthens the spasmolytic effect of papaverine, bendazole and other antispasmodics, including m-holinoblokatory. Reduces the spasmogenic activity of morphine. Phenobarbital enhances the spasmolytic effect of drotaverine.

Increases the severity of the reduction in blood pressure caused by tricyclic antidepressants, quinidine and procainamide.

Special instructions:

In patients with low and unstable blood pressure, treatment should be under the control of arterial pressure.

Effect on the ability to drive transp. cf. and fur:

During the treatment period it is necessary to refrain from driving and occupations by other potentially dangerous activities requiring an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets, film-coated, 40 mg.

Packaging:

For 10 tablets in a blister of PVC / aluminum. One or two blisters in a cardboard box with instructions for use.

Storage conditions:

Keep in dry the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-000997

Date of registration:18.10.2011

The owner of the registration certificate:Plethiko Pharmaceuticals Co., Ltd. Plethiko Pharmaceuticals Co., Ltd. India

Manufacturer: & nbsp

PLETHICO PHARMACEUTICALS, Ltd. India

Representation: & nbspREZLOV ZAO REZLOV ZAO Kazakhstan

Information update date: & nbsp02.12.2015

Illustrated instructions

Instructions

Ple-Spa (Ple-Spa)