Pharmacodynamics. Paracetamol (CombiGrip, CombiGrip Dex) is an analgesic and antipyretic agent. the analgesic and antipyretic effect of paracetamol is associated with the effect of the preparation on the center of thermoregulation in the hypothalamus and the ability to inhibit the synthesis of prostaglandins.
Caffeine (CombiGrip, CombiGripDex) is a central nervous system stimulant. It stimulates the respiratory center, which increases the speed and the depth of oxygen saturation of the lungs, increases the tone of skeletal muscles, and decreases the hypercapnia threshold. To obtain the same effect with a decaffeinated analgesic, a dose approximately 40% higher than 1 dose combined with caffeine is required. Thus, caffeine is used as an adjuvant for paracetamol.
Phenylephrine hydrochloride (CombiGrip, CombiGrip Dex) stimulates postsynaptic α-adrenergic receptors, constricts the pulmonary vessels and increases the pressure in the pulmonary artery. As a vasoconstrictor, it has an anti-congestive effect: it reduces swelling and hyperemia of the nasal mucosa, the severity of exudative manifestations, and restores free breathing.
Chlorpheniramine maleate (CombiGrip, CombiGrip Dex) is an H1 blocker that inhibits smooth muscle response to histamine. Has antiallergic effect, reduces lacrimation, itching of the nasal mucosa.
Dextromethorphan hydrobromide (CombiGripDex) is a centrally acting antitussive agent. It suppresses the cough center, directly acting on it, and increases the threshold of sensitivity of the cough center to irritating agents.
Pharmacokinetics. Paracetamol (CombiGrip, CombiGripDex) is rapidly absorbed in the gastrointestinal tract, binds to blood plasma proteins. The half-life from blood plasma is 1–4 hours. It is metabolized in the liver to form glucuronide and paracetamol sulfate. It is excreted by the kidneys mainly in the form of conjugation products, 5% is excreted unchanged.
Caffeine (CombiGrip, CombiGrip Dex) and its water-soluble salts are rapidly absorbed in the intestine (including the large intestine). The half-life from blood plasma is about 5 hours, in some individuals - up to 10 hours. The main part is demethylated and oxidized. About 10% is excreted by the kidneys unchanged. In the body of full-term newborns and older (1.5-2 months), it is eliminated more slowly (half-life - from 80 to 26.3 hours, respectively).
Phenylephrine hydrochloride (CombiGrip, CombiGrip Dex) has low bioavailability due to uneven absorption and the effect of MAO in the gastrointestinal tract and liver during the first passage. It is excreted by the kidneys in the form of metabolites. With an acidic pH of urine, excretion from the body is accelerated.
Chlorpheniramine maleate (CombiGrip, CombiGrip Dexa) is a component that reduces the severity of the characteristic effects of histamine, which is especially important in preventing and reducing the severity of many allergic symptoms. It is absorbed relatively slowly in the gastrointestinal tract, the maximum plasma concentration is reached from 2.5 to 6 hours after oral administration. Bioavailability is low and amounts to 25-50%. Chlorpheniramine is metabolized during the first passage in the liver. Chlorpheniramine maleate is extensively metabolized in the liver to form the metabolites desmethyl and didesmethylchlorpheniramine. About 70% of it binds to blood plasma proteins. Chlorpheniramine is distributed throughout the body, passes through the BBB. In unchanged form and in the form of metabolites, it is excreted mainly in the urine; excretion depends on urine pH and renal excretory function. Traces were found in the feces. The duration of action is 4-6 hours. Faster and more extensive absorption, faster elimination and a shorter half-life have been observed in children.
Dextromethorphan hydrobromide (CombiGrip, CombiGrip Dex) is rapidly absorbed in the gastrointestinal tract. It is metabolized in the liver and excreted in the urine as dextromethorphan unchanged and as demethylated metabolites, including dextrorphan, which suppresses cough. The half-life of dextromethorphan hydrobromide is 4 hours.
Combigrip: symptomatic therapy of influenza and ARVI.
CombiGrip Dex: symptomatic therapy of influenza and ARVI (hyperthermia, headache, rhinitis, cough) in adults and children over the age of 6 years.
CombiGrip
Adults and children over the age of 12 years: 1-2 tablets up to 4 times a day.
Children aged 6-12 years: 1 / 2-1 tablet 3-4 times a day. It is necessary to adhere to the interval between doses of at least 4 hours.
The preparation is taken at least 30 minutes after eating.
The duration of treatment is no more than 7 days.
CombiGrip Dex
Adults and children over the age of 12: 1 tablet up to 4 times a day, with an interval of at least 3-4 hours.
Children aged 6-12 years: 1/2 tablet 4 times a day.
The preparation is taken at least 30 minutes after eating.
The duration of treatment is no more than 7 days.
Alcoholism, prostatic hypertrophy, severe forms of atherosclerosis, ag, acute pancreatitis and hepatitis, peripheral arterial thrombosis, severe coronary heart disease, cardiac conduction disturbances, ventricular tachycardia, hypersensitivity to preparation components, combined use with MAO inhibitors, children under 6 years of age ...
Agranulocytosis, thrombocytopenia, anemia, renal colic, aseptic pyuria, interstitial glomerulonephritis, allergic reactions. also possible anxiety, agitation, insomnia, drowsiness, dizziness, confusion, tachycardia, arrhythmia, increased blood pressure, nausea, vomiting, decreased appetite, diarrhea, constipation, pain in the epigastric region.
CombiGrip, CombiGrip Dex. before using the preparation, you should make sure that the underlying cause of the cough has been identified and that a decrease in the intensity of the cough will not increase the risk of complications. the preparation can reduce the reaction rate when driving and operating machinery. phenylephrine may cause tachycardia, dizziness, or heart palpitations; patients should be warned about this.
Do not recommend the use of the preparation during pregnancy. The effect of the preparation during lactation has not been studied.
Use with caution in diseases of the liver, heart and blood vessels, alcoholism.
During treatment with the preparation, alcohol should be excluded.
CombiGrip. if combination therapy is contemplated, the dosage of one or both agents should be reduced. the peculiarities of the interaction of the preparation are due to the properties of its constituent components.
Caffeine increases the effect of indirect anticoagulants (coumarin derivatives) and the likelihood of liver damage from hepatotoxic preparations. Metoclopramide increases, and cholestyramine decreases the rate of absorption. Barbiturates reduce the antipyretic effect of paracetamol.
Caffeine reduces the effect of hypnotics and narcotic preparations, increases (improving bioavailability) - acetylsalicylic acid, paracetamol and other NSAIDs. Improves the absorption of ergotamine in the gastrointestinal tract.
The use of phenylephrine with other sympathomimetic amines and MAO inhibitors can lead to an additional increase in blood pressure. MAO inhibitors can prolong the anticholinergic effect of antihistamines. Blockers of α-adrenergic receptors (phentolamine), phenothiazines, furosemide and other diuretics prevent vasoconstriction.
The incompatibility of chlorpheniramine maleate with calcium chloride, kanamycin sulfate, norepinephrine, phenobarbital was noted.
CombiGrip Dex. The use of dextromethorphan hydrobromide with enzyme inhibitors, including amiodarone, fluoxetine, haloperidol, paroxetine, propafenone, and thioridazine, may interfere with cognitive function.
Overdose symptoms are due to the properties of the individual components of the preparation.
High dose paracetamol causes hepatonecrosis. Clinical and biochemical signs of liver damage are detected after 24–72 hours: increased activity of hepatic transaminases, hyperbilirubinemia, and a decrease in prothrombin levels. Manifested by anorexia, nausea, vomiting, abdominal pain, pallor of the skin.
An overdose of caffeine is manifested by a feeling of anxiety, anxiety, tremors, headache, confusion, extrasystole.
An overdose of phenylephrine hydrochloride is manifested by ventricular extrasystole and paroxysms of ventricular tachycardia, a feeling of heaviness in the head and limbs, a significant increase in blood pressure.
In case of an overdose of chlorpheniramine maleate, the mental state can vary from depressed to agitated (anxiety and convulsions). Atropine-like symptoms may occur.
CombiGrip Dex. An overdose of dextromethorphan hydrochloride can present with agitation and mental illness. In very high doses, it can cause respiratory depression.
Treatment: gastric lavage, administration of N-acetylcysteine, symptomatic therapy.
In a dry, dark place at a temperature of 15-25 ° c.
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