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Pharmacological properties

paracetamol (combigripp, combigripp dex) is an analgesic and antipyretic. the analgesic and antipyretic effect of paracetamol is associated with the effect of the drug on the thermoregulation center in the hypothalamus and the ability to inhibit prostaglandin synthesis.

Caffeine (Combigripp, Combigripp Dex) - CNS stimulator. It stimulates the respiratory center, due to which the speed increases and the depth of oxygen saturation of the lungs increases, the skeletal muscle tone increases, and the threshold of hypercapnia decreases. To obtain the same effect when using a caffeine-free analgesic, a dose of about 40% higher than 1 dose in combination with caffeine is needed. Thus, caffeine is used as an adjuvant of paracetamol.

Phenylephrine hydrochloride (Combigripp, Combigripp Dex) stimulates postsynaptic α-adrenergic receptors, constricts pulmonary vessels and increases pulmonary artery pressure. 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 (Combigripp, Combigripp Dex) is H1- a blocker that inhibits the smooth muscle response to histamine. It has an antiallergic effect, reduces lacrimation, itching of the nasal mucosa.

Dextromethorphan Hydrobromide (Combigripp Dex) is an antitussive agent of central action. It suppresses the cough center, acting directly on it, and increases the threshold of sensitivity of the cough center to irritating agents.

Menthol (Combigripp ointment) has a local irritant, analgesic, distracting, antipruritic, antiseptic, soothing effect. The effect is mainly due to reflex reactions associated with irritation of sensitive nerve endings: irritation of the skin receptors stimulates the formation and release of endogenous biologically active substances (enkephalins, endorphins, peptides, kinins) involved in the regulation of pain, vascular permeability and other processes that provide painkiller, distracting and antipruritic effects. Antiseptic activity is manifested by indiscriminate damage to microbial cells. Annoying (distracting) effect helps to reduce pain. Local action is accompanied by a narrowing of blood vessels, a feeling of cold, which is replaced by a sensation of light burning and tingling. Skin-visceral reflexes (a reflex arc bypasses the brain) improve trophic tissue (according to the innervation zones). The tone of the vessels, both superficial and deeply located in the tissues and internal organs, changes reflexively.

Camphor (Combigripp ointment) has an antiseptic, local irritant, analgesic, antiplatelet effect. Reflexively excites the vasomotor and respiratory centers, revealing analeptic activity. It has peripheral vasopressor activity. Inhibits platelet aggregation. Standing out from the body through the respiratory tract, it helps expectoration of sputum. With local application has a distracting effect.

Thymol (Combigripp ointment) is an antiseptic and disinfectant. Destroying enzymes important for the viability of microorganisms, prevents the spread of the rotting process and delays it at the very beginning. Thymol is used as an inhalation for bronchitis and other diseases of the respiratory system, accompanied by sputum production. It stimulates the mucous membranes of the respiratory system, reduces the secretion of sputum, dilutes it, greatly reduces the amount of mucus in it, eliminates the specific odor, prevents excessive secretion, thus preventing sepsis.

Methyl Salicylate (Combigripp ointment) has an anti-inflammatory, analgesic effect. It non-selectively inhibits COX, reduces the synthesis of prostaglandins. It normalizes the increased permeability of capillaries, improves microcirculation processes, reduces edema and infiltration of inflamed tissues.

Eucalyptus oil (Combigripp ointment) has an antiseptic and disinfecting effect. When applied topically, it weakens sensitivity. Eucalyptus oil also stimulates cardiac activity.

Turpentine oil (Combigripp ointment) used locally as a distracting and warming agent.

Pharmacokinetics Paracetamol (Combigripp, Combigripp Dex) is rapidly absorbed in the digestive tract, binds to plasma proteins. The plasma half-life is 1–4 hours. It is metabolized in the liver with the formation of glucuronide and paracetamol sulfate. It is excreted by the kidneys mainly in the form of conjugation products, 5% is excreted unchanged.

Caffeine (Combigripp, Combigripp Dex) and its water-soluble salts are rapidly absorbed in the intestine (including the colon). 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 (elimination half-life is from 80 to 26.3 hours, respectively).

Phenylephrine hydrochloride (Combigripp, Combigripp Dex) has a low bioavailability due to uneven absorption and the influence of MAO in the digestive tract and liver during the first passage. It is excreted by the kidneys in the form of metabolites. At acidic pH, urine excretion is accelerated.

Chlorpheniramine Maleate (Combigripp, Combigripp Dex) Is a component that reduces the severity of the characteristic effects of histamine, which is especially important in the prevention and reduction of the severity of many allergic symptoms. It is absorbed relatively slowly in the digestive 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 the first time it passes through the liver. Chlorpheniramine maleate is significantly metabolized in the liver to form metabolites desmethyl and didemethylchlorpheniramine. About 70% of it binds to blood plasma proteins. Chlorpheniramine is distributed throughout the body, passes through the BBB. Unchanged and in the form of metabolites excreted mainly in the urine; excretion depends on the pH of the urine and excretory function of the kidneys. Traces found in feces. The duration of action is 4–6 hours. Faster and more extensive absorption, faster elimination, and a shorter half-life were observed in children.

Dextromethorphan Hydrobromide (Combigripp, Combigripp Dex) is rapidly absorbed in the digestive tract. It is metabolized in the liver and excreted in the urine as dextromethorphan unchanged and in the form of demethylated metabolites, including dextrorphan, which suppresses cough. The half-life of dextromethorphan hydrobromide is 4 hours.

Combigripp ointment

Menthol after absorption is biotransformed in the liver and excreted in the urine and bile in the form of glucuronides.

Camphor is easily absorbed from all surfaces of application, is hydroxylated in the liver to hydroxycamphor metabolites that bind to glucuronic acid, and is excreted in the urine. Camphor crosses the placenta.

Methyl salicylate quickly penetrates into the deeper layers of the skin, is absorbed, hydrolyzed, converted into an anion of salicylic acid and excreted in the urine. The clearance of salicylates depends on the pH of the urine.

Indications

Combigripp: symptomatic treatment of influenza and ARVI.

Dex combigripp: symptomatic treatment of influenza and SARS (hyperthermia, headache, rhinitis, cough) in adults and children over the age of 6 years.

Combigripp ointment:

inflammatory diseases of the respiratory tract (rhinitis, pharyngitis, laryngitis, tracheitis);

myalgia;

arthralgia.

Application

Combigripp

Adults and children over the age of 12 years: 1-2 tablets up to 4 times a day.

Children aged 6-12 years: by1/2-1 tablet 3-4 times a day. It is necessary to adhere to the interval between doses of at least 4 hours.

The drug is taken at least 30 minutes after a meal.

The duration of treatment is no more than 7 days.

Combigripp Dex

Adults and children over the age of 12 years: 1 tablet up to 4 times a day, with an interval of at least 3-4 hours.

Children aged 6-12 years: by1/2 tablet 4 times a day.

The drug is taken at least 30 minutes after a meal.

The duration of treatment is no more than 7 days.

Combigripp ointment

In diseases of the respiratory tract, a thick layer is applied to the skin in the chest and neck and rubbed. If desired, the area of ​​the application can be covered with a warm, dry cloth, but it must not be applied tightly to allow the vapors to reach the nose and throat.

For pain in muscles and joints, apply a thick layer to the area of ​​muscles or joints and rub it gently.

In adults and children aged 2-12 years, the drug is used up to 3 times a day or as directed by a doctor.

The duration of treatment is no more than 7 days. If the symptoms of a cold do not disappear, the use of the drug should be discontinued.

Contraindications

Alcoholism, prostatic hypertrophy, severe forms of atherosclerosis, ag, acute pancreatitis and hepatitis, peripheral arterial thrombosis, severe forms of coronary heart disease, impaired cardiac conduction, ventricular tachycardia, hypersensitivity to the drug, combined use with MAO inhibitors, children under 6 years of age .

Combigripp ointment: epilepsy or increased convulsive readiness, as pungent odors can trigger an attack; children under the age of 2 years; period of pregnancy, since camphor and eucalyptus oil easily penetrate the skin and placental barrier.

Side effects

Agranulocytosis, thrombocytopenia, anemia, renal colic, aseptic pyuria, interstitial glomerulonephritis, allergic reactions. anxiety, agitation, insomnia, drowsiness, dizziness, confusion, tachycardia, arrhythmia, increased hell, nausea, vomiting, decreased appetite, diarrhea, constipation, pain in the epigastric region are also possible.

Combigripp ointment. Mild local irritation, erythema, rashes, peeling and itching of the skin in the area of ​​application of the ointment are possible. There may also be a mild transient discoloration of the skin and the appearance of spots on the fabric.

Menthol can cause hives, erythema, or other skin lesions (dermatitis).

With prolonged use, sensitivity to the drug and analgesic effect may decrease.

special instructions

Combigripp, Combigripp dex. Before using the drug, make sure that the main cause of the cough is identified and that a decrease in the intensity of the cough will not lead to an increased risk of complications. the drug can reduce the reaction rate when driving vehicles and working with mechanisms. phenylephrine may cause tachycardia, dizziness, or a feeling of increased heartbeat; patients should be warned about this.

Do not recommend the use of the drug during pregnancy. The effect of the drug during lactation has not been studied.

Used with caution in diseases of the liver, heart and blood vessels, alcoholism.

During treatment with the drug, alcohol should be excluded.

Combigripp ointment. Avoid contact with eyes and mucous membranes.

With local irritation, the use of the drug is stopped, appropriate therapy is used.

The drug should be applied only to intact skin; it cannot be applied to open wounds.

Do not use in children for lubrication of the nasopharynx.

Persistent coughing can be a sign of a serious illness. If the cough does not disappear within 1 week, recurs or is accompanied by fever, rashes, persistent headache, treatment tactics should be reviewed.

Do not use the drug for prolonged or chronic cough in smokers, asthma, emphysema or if cough is accompanied by profuse sputum removal.

Do not apply the drug to large areas of the skin.

The drug is not recommended for use during lactation.

Interactions

Combigripp. if combination therapy is expected, the dosage of one or both agents should be reduced. Features of the drug’s interaction are due to the properties of its constituent components.

Caffeine increases the effect of indirect anticoagulants (coumarin derivatives) and the likelihood of liver damage with hepatotoxic drugs. Metoclopramide increases, and cholestyramine reduces the rate of absorption. Barbiturates reduce the antipyretic effect of paracetamol.

Caffeine reduces the effect of sleeping pills and drugs, increases (improves bioavailability) - acetylsalicylic acid, paracetamol and other NSAIDs. Improves the absorption of ergotamine in the digestive tract.

The use of phenylephrine with other sympathomimetic amines and MAO inhibitors can lead to an additional increase in blood pressure. MAO inhibitors may prolong the anticholinergic effect of antihistamines. Α-adrenoreceptor blockers (phentolamine), phenothiazines, furosemide and other diuretics prevent vasoconstriction.

Incompatibility of chlorpheniramine maleate with calcium chloride, kanamycin sulfate, norepinephrine, phenobarbital was noted.

Combigripp of Dex. The use of dextromethorphan hydrobromide with enzyme inhibitors, including amiodarone, fluoxetine, haloperidol, paroxetine, propafenone and thioridazine, can affect cognitive function.

There are no reports of the interaction of Combigrippa ointment with other drugs.

Overdose

Symptoms of an overdose are due to the properties of the individual components of the drug.

A high dose of paracetamol causes hepatonecrosis. Clinical and biochemical signs of liver damage are detected after 24–72 hours: an increase in hepatic transaminase activity, hyperbilirubinemia, and a decrease in prothrombin level. It manifests itself as anorexia, nausea, vomiting, abdominal pain, pallor of the skin.

An overdose of caffeine is manifested by a sense of anxiety, anxiety, tremor, 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, and a significant increase in blood pressure.

With an overdose of chlorpheniramine maleate, the mental state can vary from suppressed to excited (anxiety and convulsions). Atropine-like symptoms may occur.

Combigripp of Dex. An overdose of dextromethorphan hydrochloride can be manifested by agitation and mental disorders. In very high doses, it can cause respiratory depression.

Treatment: gastric lavage, administration of N-acetylcysteine, symptomatic therapy.

Combigripp ointment. Perhaps an increase in the severity of side effects, ataxia, drowsiness, reflex respiratory arrest.

Storage conditions

In a dry, dark place at a temperature of 15-25 ° c. do not freeze combigripp ointment.

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