Acetylsalicylic acid + Chlorfenamine + Phenylpropanolamine (Acidum acetylsalicylicum + Chlorphenaminum + Phenylpropanolaminum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

NSAIDs - Salicylic acid derivatives

Included in the formulation
АТХ:

A.01.B.A.51   Phenylpropanolamine in combination with other drugs

Pharmacodynamics:

Combined drug. Acetylsalicylic acid has anti-inflammatory, antipyretic and analgesic effect. By blocking cyclooxygenase-1 and cyclooxygenase-2, acetylsalicylic acid violates the synthesis of prostaglandins and the production of adenosine triphosphate; has anti-inflammatory, antipyretic and analgesic effect, inhibits the aggregation of platelets. The analgesic effect is due to both central and peripheral action. Affects the center of thermoregulation, reduces body temperature in febrile states. Reduces aggregation, platelet adhesiveness and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets.

Phenylpropanolamine hydrochloride is a sympathomimetic, stimulates the release of norepinephrine from the nerve endings, excites predominantly central alpha-adrenergic receptors, has a vasoconstrictor effect, reduces edema and hyperemia of the mucous membranes of the upper respiratory tract and accessory sinuses of the nose. Oppresses the hypothalamic appetite center (anorexigenic effect).

Chlorphenamine (chlorpheniramine) maleate - a blocker of histamine H1 receptors; has anti-allergic effect, reduces the permeability of the vessels of the mucous membrane of the upper respiratory tract, eliminates tearing, itching in the eyes and nose. Drug form of the drug can reduce the irritating effect of acetylsalicylic acid on the mucosa of the digestive system.

Pharmacokinetics:

Acetylsalicylic acid

When ingested quickly absorbed mainly from the proximal part of the small intestine and to a lesser extent from the stomach. The presence of food in the stomach significantly alters the absorption of acetylsalicylic acid.

Metabolised in the liver by hydrolysis with the formation of salicylic acid, followed by conjugation with glycine or glucuronide. The concentration of salicylates in the blood plasma is variable.

About 80% of salicylic acid binds to blood plasma proteins. Salicylates easily penetrate into many tissues and body fluids, including. in spinal, peritoneal and synovial fluid. In small amounts, salicylates are found in the brain tissue, traces - in bile, sweat, feces.Rapidly penetrates the placental barrier, in small quantities excreted in breast milk.

It is excreted mainly by active secretion in the renal tubules in unchanged form (60%) and in the form of metabolites. Excretion of unchanged salicylate depends on the hydrogen index of urine (with alkalinization of urine ionization of salicylates increases, their reabsorption worsens and the excretion increases significantly). PSemi-elimination half-lifecetylsalicylic acid is approximately 15 minutes. PThe half-elimination period (half-life) salicylate when taken in low doses is 2-3 hours, with an increase in the dose may increase to 15-30 hours.

Chlorphenamine

After ingestion, chlorphenamine is relatively slowly absorbed from the gastrointestinal tract. Cmax is achieved in 2,5-6 hours. Bioavailability is low - 25-50%. Exposed to the effect of "first passage" through the liver. Binding to plasma proteins is about 70%. Chlorphenamine is widely distributed in the organs and tissues of the body, penetrates into the central nervous system.

Intensively metabolized in the liver with the formation of desmethyl- and didesmethylchlorophenamine.Unchanged drug and its metabolites are excreted mainly with urine. Excretion depends on the pH of the urine and the urine flow rate. In feces only trace amounts of chlorphenamine are detected.

Chlorphenamine is characterized by a significant interindividual variability of pharmacokinetic parameters: nThe half-elimination period (half-life) varies from 2 to 43 hours.

Children have a faster absorption of chlorphenamine, a higher clearance and shorterThe half-elimination period (half-life).

Phenylpropanolamine

When taken orally, absorbed quickly and completely. Metabolized in the liver to form a hydroxylated active metabolite.

Indications:

Symptomatic treatment of influenza and other acute respiratory viral infections.

ICD-10

X.J10-J18.J11   Influenza, virus not identified

Contraindications:

Hypersensitivity, gastric ulcer and duodenal ulcer in the acute stage, bronchial asthma, angle-closure glaucoma, prostate adenoma cancer, pregnancy, lactation (for the period of treatment should abandon breastfeeding), children's age (12 years).

Carefully:

With caution appoint a drug for bronchial asthma, coronary heart disease, arterial hypertension, hyperthyroidism, glaucoma, diabetes, prostatic hyperplasia, as well as during pregnancy and children with increased excitability.

Pregnancy and lactation:

Action category for the fetus by Food and Drug Administration (US Food and Drug Administration) not determined. Application in pregnancy is not indicated.

The use of the drug in the third trimester of pregnancy can lead to a disruption in the fetal development of the fetus or cause complications during childbirth. For the period of treatment it is necessary to refuse breastfeeding.

Dosing and Administration:

1 tablet contains acetylsalicylic acid 325 mg, phenylpropanolamine hydrochloride 15 mg and chlorpheniramine maleate 20 mg.

Inside, previously dissolved in a glass of water. Adults - 2 tablets every 4 hours, but not more than 8 tablets per day. For patients older than 60 years, the maximum daily dose is 4 tablets.

Side effects:

On the part of the gastrointestinal tract: nausea, vomiting, constipation, heartburn (especially in predisposed patients or when the recommended doses are not observed).
From the cardiovascular system: a feeling of tightness in the chest, tachycardia, increased blood pressure, ventricular extrasystole, cardialgia.
Allergic reactions: rarely - skin itching, rash.
Other: dilated pupils, painful urination, dryness of the oral mucosa, nose, throat, headache, paresis, accommodation, insomnia, psychomotor agitation, tremor, thrombocytopenia, leukopenia, agranulocytosis, urinary retention.

Overdose:

Symptoms: nausea, vomiting, abdominal pain, diarrhea; increased excitability, dizziness, sleep disturbances, euphoria, hand tremors, impaired coordination, hallucinations, delusions; increased blood pressure, tachycardia, arrhythmia; retention of urine.

Treatment: symptomatic. Stomach washing is shown. There is no specific antidote.

Interaction:

Do not recommend taking the drug immediately after eating or after taking a lot of fluids.

Phenylpropanolamine increases the effect of heparin, oral anticoagulants and hypoglycemic agents. Inhibitors of monoamine oxidase and beta-adrenomimetics increase, and reserpine weakens sympathomimetic properties.

With simultaneous use with beta-blockers, digitalis preparations, means for inhalation anesthesia, the risk of arrhythmia increases. When used simultaneously with funds that stimulate the central nervous system (caffeine, ephedrine and others), it is possible to develop a rapid increase in respiration, tremor, and increased excitability.

When combined with monoamine oxidase inhibitors, there is an increase in blood pressure, in predisposed people - the development of hypertensive crisis. Long-term use of reserpine weakens the effect of the drug.

Chlorphenamine, which is part of the drug, increases the inhibitory effect on the central nervous system of barbiturates, tranquilizers of the benzodiazepine series, sedatives, ethanol.

Special instructions:

If symptoms persist for more than 7 days, you should consult your doctor.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Instructions
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