Combined preparation. The action of the drug due to the pharmacological properties of its components.

Paracetamol has analgesic and antipyretic effect. The mechanism of action associated with inhibition of the synthesis of prostaglandins (PGs) by blocking both forms of cyclooxygenase enzyme (COX-1 and COX-2). It operates mainly in the central nervous system, acting on pain centers and thermoregulation. In peripheral tissues cellular peroxidase neutralize the effect of paracetamol on COX, which explains the almost complete absence of anti-inflammatory effect. The absence of a blocking effect on PG synthesis in these tissues leads to lack of a negative effect on the mucosa of the gastro-intestinal tract and water-salt metabolism (delay Na + ions and water).

Caffeine has a direct stimulating effect on the central nervous system: regulates and strengthens the processes of excitation in the cerebral cortex, respiratory and vasomotor centers, activates the positive conditioned reflexes and motor activity. It stimulates mental activity, enhances mental and physical performance, shortens the reaction time. After receiving the vigor appears temporarily eliminated or reduced fatigue and drowsiness. It is quickening and deepening of breathing, especially against the oppression of the respiratory center. Influence on the cardiovascular system: strength and increases the heart rate (especially in high doses), blood pressure increases, especially at hypotension. Extends bronchi, bile ducts, blood vessels, skeletal muscle, heart, kidney, constricts blood vessels of the abdominal organs (especially when dilation). It decreases platelet aggregation. It has a moderate diuretic effect, mainly due to the reduced electrolyte reabsorption in the renal tubules. It stimulates the secretion of gastric glands. It increases the basal metabolic rate, increases glycogenolysis, causing hyperglycemia.

Сlorpheniramine maleate has antagonistic properties to histamine H1 – receptors, thereby facilitating the following symptoms: rhinitis, nasal congestion, redness of the eyes and hypersensitivity.

Phenylephrine gidrohlorid.- adrenoagonists, has a stimulating effect on alpha-adrenergic receptors, causing narrowing of arterioles of the nasal mucosa, thereby helps to eliminate swelling and mucus, reduction of rhinorrhea, and nasal congestion.

The preparation generally has analgesic, antipyretic, anti-inflammatory, tonic, antihistaminic activity.

Pharmacokinetics
Paracetamol Paracetamol after ingestion rapidly and completely absorbed in the upper gastrointestinal tract. The maximum concentration (Cmax) in plasma is reached within 10-60 minutes. Binding to plasma proteins is less than 10%. Quickly and evenly distributed in most tissues. The half-life (T1 / 2) is 1-4 hours. It is metabolized primarily in the liver via glucuronide conjugation, conjugation with sulphate and oxidation, with the participation of mixed liver oxidase and cytochrome P450.

Hydroxylated metabolite of the negative effect – N-acetyl-p-benzoquinoneimine which is formed in very small amounts in the liver and kidneys under the influence of mixed oxidases and generally detoxify by binding to glutathione, may accumulate an overdose of paracetamol and cause tissue damage. Provided mainly kidneys.

Caffeine is well absorbed in the intestine, T1 / 2 in plasma is 5-10 hours, mainly excreted by the kidneys in the form of metabolites.

Сlorpheniramine maleate after oral administration, slowly and completely absorbed in the gastrointestinal tract, the time to reach C max of 2.5 to 6 hours.

The index of bioavailability of about 25% to 50%. Most of the drug (70%) bound to plasma proteins. Distributed mainly in soft tissues, including the central nervous system. T? It varies from 2 to 43 hours and a duration of action of 4 to 6 hours. Most of the substance is metabolized. Unchanged part and its metabolites are excreted in the urine, a small amount – with the feces.

Phenylephrine hydrochloride after its oral absorption is variable. It undergoes extensive first-pass metabolism. As a result of systemic bioavailability is only 40%, with peak plasma concentrations achievement for 1-2 hours. The average plasma half-life of 2-3 hours.

Symptomatic therapy of infectious and inflammatory diseases (SARS, influenza), accompanied by high temperature, fever, headache and muscle pain, runny nose, nasal congestion.

Dosing and Administration

Adults and adolescents over 15 years: 1 tablet 3 times a day or prescribed by a doctor.

The maximum daily dose – 4 tablets.

For the treatment of colds better start taking the drug as soon as possible, immediately after the first symptoms. The drug is taken by mouth, preferably after a meal. The interval between doses should be at least 4 hours. Patients with renal insufficiency drug is given every 8 hours. The duration of treatment is determined individually on average 3 – 5 days. It is recommended not to use this drug for more than 5 days with consulting a doctor. If there is no improvement or there are new symptoms should consult a doctor.

Often:
– Drowsiness;

Rarely:
– Headache, dizziness;
– Insomnia, anxiety, restlessness, nervousness, irritability;
– Thrombocytopenia, leukopenia, agranulocytosis, pancytopenia;
– Palpitations, increased blood pressure;
– Allergic reactions (skin rash, urticaria, angioedema edema);
– Dry mouth;

There are:
– Nausea, vomiting, epigastric pain, diarrhea;
– Mydriasis, increased intraocular pressure;
– Hepatotoxic and nephrotoxic effects with prolonged excess dose.

Concomitant use of barbiturates, anticonvulsants, rifampicin and alcohol with the drug increases the risk of hepatotoxicity. zidovuddina activity may be reduced when taking Ying-flu.

Caffeine increases the analgesic effect of the Institute of flu.

With the simultaneous use of the drug with alcohol and other means, oppressive CNS activity {hypnotics, sedatives, tranquilizers, and narcotic analgesics) may increase the effect of depressing the central nervous system when taken concomitantly with anticholinergic drugs and tricyclic antidepressants may increase their effects.

At the same time taking the drug with ganglioblokiruyuschimi, adrenoceptor blocking agents, Rauwolfia alkaloids and methyldopa may experience hypertension.

Simultaneous treatment with probenecid drug may change the concentration of paracetamol in plasma and excretion. Suction Ying-reduced flu while taking cholestyramine cimetidine, disulfiram, oral steroidal contraceptives increases when taking domperidone and metoklopromida.

Withdrawal is increased in smokers.

Special instructions

The drug is prescribed with caution to elderly or debilitated patients, in patients with impaired liver and kidney function.

Do not exceed the prescribed dose by your doctor. In case of serious side effects, the drug should be discontinued.

During treatment, you can not simultaneously take other medicines containing paracetamol, alcohol and sedatives.

This drug can cause drowsiness and decreased attention, so the period of treatment, patients should not drive vehicles or machines / mechanisms.

The drug should be stored out of reach of children and do not use after the expiration date.

Overdose
Symptoms: pale skin, anorexia, nausea, vomiting; gepatonekroz (necrosis severity is directly dependent on the degree of overdose). The toxic effect of the drug in adults is possible after receiving more than 10-15 g of paracetamol: increased activity of “liver” transaminases, increased prothrombin time (after 12-48 hours after admission); detailed clinical picture of liver damage manifests itself in 1-6 days. Rarely hepatic dysfunction develops lightning speed and can be complicated by renal failure (interstitial nephritis).

Treatment:. Donators administering SH-groups, and the synthesis of glutathione precursors – methionine after 8-9 hours after the overdose and N-acetylcysteine ​​- 12 hours The need for additional therapeutic measures is determined depending on the concentration of paracetamol in the blood, and the time elapsed after his admission.

Contraindications
– Hypersensitivity to the drug;
– Concomitant use of monoamine oxidase inhibitors (MAOIs);
– Pregnancy and lactation;
– Glaucoma (high intraocular pressure);
– Voiding disorders in benign prostatic hypertrophy;
– Cardiac arrhythmias, hypertension;
– The expressed disturbances of liver function;
– Children up to age 15 years.