Gripaut-Ekstra

General characteristics. Structure:

Active ingredients: 500 mg of paracetamol, 10 mg of Phenylephrinum of a hydrochloride, 2 mg of chlorpheniramine of a maleate, 30 mg of caffeine in 1 tablet.

excipients: sodium krakhmalglikolit, gelatin, starch corn, methylparaben (Е 218), propylparaben (Е 216), magnesium stearate, talc, cellulose microcrystallic, dye yellow "sunset" (Е 110).

Pharmacological properties:

Pharmacodynamics. The combined drug. Paracetamol blocks cyclooxygenase that leads to the termination of synthesis of prostaglandins, has febrifugal and analgeziruyushchy effect.

Chlorpheniramine the maleate blocks N-1-gistaminovye receptors. Has antiallergenic and antiedematous effect. Promotes decrease in permeability of vessels of a mucous membrane of upper respiratory tracts, eliminates hypostasis and a hyperemia mucous a nose, suppresses symptoms of allergic rhinitis, facilitates breath.

Phenylephrinum a hydrochloride – a stimulator preferential alpha 1 - adrenoceptors. Finds sudinozvuzhuyuchy effect, mainly concerning vessels of upper respiratory tracts, reduces raised слизоутворення and thus promotes elimination of a congestion of a nose.

Caffeine shows a promoting effect on the central nervous system, strengthens analgeziruyushchy effect of paracetamol, reduces fatigue and drowsiness, increases physical and intellectual effeciency.

Pharmacokinetics. Paracetamol quickly and almost is completely absorbed from a digestive tract, is preferential in a small bowel. After a single dose in a dose of 500 mg the maximum concentration in a blood plasma is reached in 10-60 minutes. Paracetamol is quickly and evenly distributed in the majority of body tissues. About 25% of paracetamol in blood contact proteins of plasma. Paracetamol is metabolized by means of microsomal enzymatic system of a liver. About 80-85% of paracetamol in an organism are exposed to conjugation generally with glucuronic acid and to a lesser extent – with sulphuric acid. The elimination half-life makes 1-3 hours. Paracetamol is removed with urine generally in a look paracetamol glucuronide with small amounts paracetamol-sulfate and a merkaptata and in not changed look.

Phenylephrinum is unevenly absorbed from a digestive tract and easily metabolized. After oral administration its action is shown in 15-20 minutes and зберігатється a current of 2-4 hours. Bioavailability of Phenylephrinum low. Fenilefrin biotransformirutsya in intestines walls at absorption and in a liver. Less than 16% of the entered dose in not reversed look together with metabolites are almost removed with urine.

Chlorpheniramine is absorbed rather slowly from a digestive tract, peak concentration in plasma are reached in 2,5-6 hours after oral administration. Bioavailability its low (25-50%). Chlorpheniramine is exposed to considerable metabolism of the first passing. About 70% to a hlorfen_ramin in a system blood-groove contact proteins of plasma. The elimination half-life fluctuates from 2 to 43 hours. Chlorpheniramine is widely distributed in an organism, gets into the central nervous system. Chlorpheniramine is actively metabolized. Metabolites include desmetit and дидесметилхлорфенірамін. Not changed chlorpheniramine and metabolites are removed generally with urine. Duration of action makes 4-6 hours. At children more bystry and more considerable absorption, more bystry clearance and shorter elimination half-life were observed.

Caffeine is well absorbed after oral administration. The maximum concentration in plasma is reached in 15-45 minutes. It is proved that caffeine improves absorption of other components of drug. Caffeine is quickly distributed in body tissues, easily breaks placental and hematoencephalic barriers. About 17-36% of a dose contact proteins of plasma. Metabolism of caffeine included hepatic P450 (CYP) cytochrome an isoenzyme 1A2. At adults drug is quickly metabolized in a liver to 1-metilurovo ї acids and 7 methylxanthines. The elimination half-life makes about 3 hours. Caffeine and its metabolites are removed by kidneys

Indications to use:

Symptomatic treatment of cold and flu which are followed by head and muscular pain, fever, dacryagogue, cold, a nose congestion.

Route of administration and doses:

At the first symptoms of flu or cold for adults and children 12 years are more senior the dose makes 2 tablets to 4 times a day, for children aged from 6 up to 12 years – 1 tablet to 4 times a day with an interval of 4-6 hours. A course of treatment – no more than 5 days.

Features of use:

Drug is not used along with monoamine oxidase inhibitors and with other drugs containing paracetamol. It is necessary to appoint drug with care at arterial hypertension, to persons with heart diseases, at atherosclerosis of cerebral vessels, diseases of kidneys and a liver.

During treatment it is necessary to exclude alcohol intake.

Use during pregnancy or feeding by a breast. Not to use drug during pregnancy or feeding by a breast.

Ability to influence speed of response at control of motor transport or work with other mechanisms. During therapy work with vehicles and mechanisms is not recommended.

Children. Drug is not used to children age up to 6 years.

Side effects:

From skin and hypodermic cellulose: skin rashes, itch, urticaria, multiformny exudative erythema, Stephens-Johnson's syndrome, toxic epidermal necrolysis.

From immune system: in isolated cases – an acute anaphylaxis, a Quincke's disease.

Neurologic frustration: a headache, dizziness, psychomotor initiation and disturbance of orientation, concern, nervous irritability, sensation of fear, irritability, a sleep disorder, sleeplessness, confusion of consciousness, depressions, a tremor, feeling of a pricking and weight in extremities, a sonitus.

From organs of sight: vision disorder and accommodations, increase in intraocular pressure.

From system of digestion: nausea, vomiting, dryness in a mouth, discomfort and pain in epigastric area, hypersalivation, a loss of appetite, increase in activity of liver enzymes, гепатонекроз (at use of high doses).

From bodies of a hemopoiesis: anemia, a sulfhemoglobinemia and a methemoglobinemia, hemolitic anemia (especially for patients with deficit glyukozo-6-fosfatdegidrogenazy). At prolonged use in high doses – aplastic anemia, a pancytopenia, an agranulocytosis, a neutropenia, a leukopenia, thrombocytopenia.

From an urinary system: at use of high doses – nephrotoxicity (renal colic, intersticial nephrite, a papillary necrosis), disturbance of an urination.

From cardiovascular system: arterial hypertension, tachycardia or reflex bradycardia, asthma, heartaches.

Others: the general weakness, the strengthened sweating, a hypoglycemia.

Interaction with other medicines:

At simultaneous use of barbiturates, tricyclic antidepressants, and also alcohol intake increase in an elimination half-life of paracetamol is possible. Prolonged use of anticonvulsant drugs can reduce activity of paracetamol. Simultaneous use of high doses of paracetamol with an isoniazid increases risk of development of a hepatotoxic syndrome.

Paracetamol reduces efficiency of diuretics.

At simultaneous use of Phenylephrinum of a hydrochloride with atropine tachycardia can be observed. Chlorpheniramine along with MAO inhibitors, furasolidone can lead to hypertensive crisis, nervous excitement, a hyper pyrexia.

Tricyclic antidepressants strengthen own sympathomimetic action.

Drug reduces hypotensive action of a guanetidin who, in turn, increases alpha адреностимулирующие activity of Phenylephrinum.

Drug strengthens effect of indirect anticoagulants (coumarin derivatives). Metaklopramid raises, and холестирамин reduces absorption speed. Barbiturates reduce febrifugal effect of drug.

Antidepressants, protivoparkinsonichesky and antipsychotic drugs, fenotiazinovy derivatives increase risk of development of an ischuria, dryness in a mouth, locks.

Glucocorticosteroids increase risk of development of glaucoma.

Contraindications:

Hypersensitivity to drug components, heavy abnormal liver functions and/or kidneys, an inborn hyperbilirubinemia, deficit glyukozo-6-fosfatdegidrogenazy, alcoholism, heavy arterial hypertension, unstable stenocardia, the acute period of a myocardial infarction, a hyperthyroidism, dekompensirovanny heart failure, disturbance of cordial conductivity, acute pancreatitis, a prostatauxe, severe forms of a diabetes mellitus, closed-angle glaucoma, the expressed anemia, a leukopenia, pregnancy and the period of feeding by a breast, children's age up to 6 years.

Not to apply together with monoamine oxidase inhibitors (MAO) and within 2 weeks after phase-out of MAO inhibitors.

Overdose:

Overdose it is, as a rule, caused by paracetamol and it is shown by pallor of skin, anorexia, nausea, vomiting, an abdominal pain, gepatonekrozy, increase in activity of "hepatic" transaminases, increase in a prothrombin ratio.

Symptoms of damage of a liver are observed 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 and lead to development of toxic encephalopathy with consciousness disturbance, in some cases – with a lethal outcome. The acute renal failure with an acute necrosis of tubules can develop even in the absence of severe damage of kidneys. Also cardiac arrhythmia was noted. 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.

In case of overdose the increased sweating, psychomotor excitement or oppression of the central nervous system, drowsiness, consciousness disturbance, disturbance of a cordial rhythm, tachycardia, premature ventricular contraction, a tremor, a hyperreflexia, spasms can be observed.

Treatment: a gastric lavage with the subsequent use of absorbent carbon, symptomatic therapy. Methionine use orally or Acetylcysteinum it is intravenously effective within 48 hours after overdose. It is also necessary to accept all-supporting actions. If necessary apply alpha adrenoblockers.

Storage conditions:

Period of validity - 3 years. To store at a temperature not above 25 °C in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in the blister, after 1 blister in a cardboard box.