Paraverin

General characteristics. Structure:

Active ingredients: paracetamol; drotaverine hydrochloride; 1 tablet contains paracetamol 500 mg and Drotaverinum of a hydrochloride of 40 mg.

Excipients: povidone, ascorbic acid, magnesium stearate, starch prezhelatinizirovanny, silicon dioxide colloid anhydrous, talc, кросповидон, cellulose microcrystallic, ferrous oxide yellow (Е 172).

Pharmacological properties:

Paracetamol has anesthetic and febrifugal effect is preferential by inhibition of synthesis of prostaglandins in the central nervous system and to a lesser extent - in peripheral, blocking synthesis of prostaglandins or their action and other substances stimulating pain receptors.
Paracetamol after oral administration is quickly and completely absorbed in a small bowel; its maximum concentration in a blood plasma is reached in 30-90 min., plasma elimination half-life makes about 2 hours. It poorly contacts proteins of plasma and erythrocytes, is distributed quickly and evenly. Paracetamol is metabolized in a liver, its metabolites are removed by glomerular filtering. He is brought with urine in the form of a glucuronide and sulfate (about 85%) or in not changed look (2-3%). About 10% of the received dose are detoxified by glutathione in a liver.

Drotaverinum is a derivative of isoquinoline which has spasmolytic effect on smooth muscles by phosphodiesterase IV enzyme inhibition. Efficiency of Drotaverinum depends on the content of enzyme of phosphodiesterase IV in various fabrics, irrespective of the nature of fabrics. The increased concentration of Drotaverinum also leads to a weak inhibiting effect on calcium - a dependent calmodulin.
Drotaverinum after oral administration is absorbed quickly and completely. Its maximum concentration in a blood plasma is reached in 45-60 min. after oral administration; 95-98% of Drotaverinum contact proteins of a blood plasma, are preferential with albumine, a-and b-globulins. Its elimination half-life makes 2,4 hours, and a biological elimination half-life - from 8 to 10 hours. Drotaverinum accumulates in the central nervous system, fatty tissue, a myocardium, kidneys and lungs, and also passes through a placenta. It is metabolized in a liver, more than 50% are removed with urine and 30% - with a stake.
Paracetamol and Drotaverinum do not interact at the level of linkng with proteins. In the research in vitro it was shown that paracetamol (in the quantity corresponding to therapeutic doses) does not suppress metabolism of Drotaverinum specifically, but by 2-7 times increases the period of its existence in not changed form. Therefore it is possible that it also suppresses metabolism of Drotaverinum of in vivo.

Indications to use:

Pain relief of weak and moderate intensity, including a headache of tenzionny type (both acute, and chronic forms).

Route of administration and doses:

Adults. The recommended dose makes 1-2 tablets of Paraverin which in case of need it is possible to repeat each 8 hours. The daily dose should not exceed 6 tablets.
At prolonged treatment (more than 3 days) the dose of Paraverina® should not exceed 4 tablets a day.

Children. To children at the age of 6-12 years appoint a dose 1/2 tablets once which if necessary can be repeated in 10-12 hours, the maximum daily dose (1 tablet) should not be exceeded.
Patients of advanced age. Usually apply a dose to adults. At a liver and renal failure do not apply (see. "Contraindications").

Features of use:

The recommended dose should not be exceeded (see. "Route of administration and doses").
Therapy continuation is possible more than 3 days under observation of the doctor.
Clinical symptoms of toxic hepatitis and changes of laboratory indicators can be observed in 48-72 h after administration of drug.
At prolonged use it is recommended to control quantity of leukocytes and thrombocytes, and also creatinine and levels of liver enzymes.
Short-term use of drug is recommended to the patients who is constantly accepting peroral anticoagulants. Increase in bleeding is sometimes observed.
As drug contains Drotaverinum, it should be applied with care to patients with arterial hypotension and patients with atherosclerosis of coronary arteries.

Use during pregnancy or feeding by a breast.
Use is contraindicated.

Ability to influence speed of response at control of motor transport or work with other mechanisms.
For treatment it is necessary to refrain from driving and performance of the work requiring special attention if use of medicine causes dizziness.

Children.
Use of drug for treatment of children up to 6 years is contraindicated.

Side effects:

- Allergic reactions: anaphylaxis, skin itch, enanthesis and mucous membranes (usually generalized, erythematic rashes, urticaria), Quincke's disease, multiformny exudative erythema (including Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease), dermahemia, fever, fever, fervescence, weakness.
- From digestive tract: nausea, pain in epigastriums, a lock, vomiting, increase in activity of liver enzymes, as a rule, without development of jaundice.
- From endocrine system: a hypoglycemia, up to a hypoglycemic coma.
- From the hemopoietic bodies: anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, short wind, heartaches), hemolitic anemia.
- From respiratory system: a bronchospasm at the patients sensitive to aspirin and other NPVS.
- From a nervous system: headache, dizziness, sleeplessness.
- From cardiovascular system: tachycardia, arterial hypotension.

Interaction with other medicines:

For Drotaverinum.
Levodopa. The Protivoparkinsonichesky effect can be reduced if Drotaverinum is applied along with a levodopa, for example, rigidity and a tremor can worsen. 

For paracetamol.
Speed of absorption of paracetamol can increase at use with Metoclopramidum and domperidony and decrease at use with holestiraminy. The anti-coagulative effect of warfarin and other coumarins can be strengthened at simultaneous prolonged regular daily use of paracetamol, with increase in risk of bleeding. Periodic reception does not render considerable effect.
Barbiturates reduce febrifugal effect of paracetamol.
Anti-convulsive drugs (including Phenytoinum, barbiturates, carbamazepine) which stimulate activity of microsomal enzymes of a liver, can strengthen toxic impact of paracetamol on a liver owing to increase in extent of transformation of drug on hepatotoxic metabolites. At simultaneous use of paracetamol with hepatotoxic means toxic influence of drugs on a liver increases.
Simultaneous use of high doses of paracetamol with an isoniazid increases risk of development of a hepatotoxic syndrome. Paracetamol reduces efficiency of diuretics.
Not to apply along with alcohol.

Contraindications:

Hypersensitivity to any of components of drug or other NPVS, a renal and liver failure, heart failure of heavy degree, insufficiency glyukozo-6-fosfatdegidrogenazy, AV-blockade of II and III degrees, glaucoma, cardiogenic shock, alcoholism, intracranial hypertensia, thrombocytopenia, a leukopenia, an agranulocytosis, the treatment period MAO inhibitors and the next 14 days after their cancellation, reception of other drugs containing paracetamol.

Overdose:

Symptoms of overdose and treatment at overdose.
Damage of a liver is possible at adults who accepted 10 g and more paracetamol and at children who accepted more than 150 mg/kg of body weight. At patients with risk factors (prolonged treatment by carbamazepine, phenobarbital, Phenytoinum, Primidonum, rifampicin, a St. John's Wort or other medicines which induce liver enzymes; regular reception of excess amounts of ethanol; the glutationovy cachexia (digestive disturbances, a mucoviscidosis, HIV infection, hunger, a cachexia)) can lead reception of 5 g or more paracetamol to damage of a liver.
Overdose symptoms in the first 24 hours: pallor, nausea, vomiting, anorexia and abdominal pain. Damage of a liver can become explicit in 12-48 hours after overdose. There can be disturbances of metabolism of glucose and a metabolic acidosis. At a serious poisoning the liver failure can progress in encephalopathy, hemorrhages, a hypoglycemia, a coma and a lethal outcome. The acute renal failure with an acute necrosis of tubules can be shown by severe lumbar pain, a hamaturia, a proteinuria and to develop even in the absence of severe damage of a liver. Also cardiac arrhythmia and pancreatitis were noted.

At prolonged use of drug in high doses from bodies of a hemopoiesis aplastic anemia, a pancytopenia, an agranulocytosis, a neutropenia, a leukopenia, thrombocytopenia can develop. At reception of high doses from TsNS - dizziness, psychomotor initiation and disturbance of orientation, from an urinary system - nephrotoxicity (renal colic, intersticial nephrite, a capillary necrosis).
At overdose emergency medical service is necessary. The patient should be taken immediately to hospital even if there are no early symptoms of overdose. Symptoms can be limited to nausea and vomiting or can not reflect weights of overdose or risk of defeat of bodies. It is necessary to consider treatment by absorbent carbon if the overdose of paracetamol was accepted within 1 hour. Concentration of paracetamol has to be measured in a blood plasma in 4 hours or later after reception (earlier concentration are doubtful). Treatment by N-Acetylcysteinum can be applied within 24 hours after paracetamol reception, but the maximum protective effect is gained at its use within 8 hours after reception. Efficiency of an antidote sharply decreases after this time. If necessary to the patient intravenously enter N-Acetylcysteinum according to the established list of doses. In the absence of vomiting methionine orally as the corresponding alternative in the remote areas out of hospital can be applied.
At overdose of Drotaverinum such symptoms can appear: AV-blockade, decrease in excitement of a cardiac muscle, arrhythmia. In case of overdose of Drotaverinum it is necessary to carry out symptomatic therapy.

Storage conditions:

To store at a temperature not above 25 °C in dry, protected from light and the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in the blister; on 1 or 3 blisters in cardboard packaging.