Acetylsalicylic acid + Phenylephrine + Chlorfenamine - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Other non-narcotic analgesics, including non-steroidal and other anti-inflammatory drugs

NSAIDs - Salicylic acid derivatives

Included in the formulation

Aspirin® Complex

powder inwards

BAYER, AO Russia

АТХ:

N.02.B.A.51 Acetylsalicylic acid in combination with other drugs, excluding psycholeptics

Pharmacodynamics:

Combined drug, the effect of which is due to its active components.

Acetylsalicylic acid has analgesic, antipyretic, anti-inflammatory action. The main mechanism of the effect of acetylsalicylic acid is inactivation of the enzyme cyclooxygenase, as a result of which the synthesis of prostaglandins, prostacyclin and thromboxane is disrupted. Due to a decrease in the production of prostaglandins, the severity of their pyrogenic effect on the thermoregulatory centers decreases. In addition, the sensitizing effect of prostaglandins on sensitive nerve endings is reduced, which leads to a decrease in the sensitivity of the latter to mediators of pain. The antiaggregant effect of acetylsalicylic acid is due to the irreversible disruption of synthesis in platelets of thromboxane A2, and its property is reversibly blocking the cyclooxygenase of endothelial cells, in which prostacyclin is synthesized, which has antiplatelet activity.

Phenylephrine is an alpha1-adrenomimetic. Stimulating alpha1-adrenoreceptors, causes a narrowing of the arterioles of the nasal mucosa: reduces edema and hyperemia of the nasal mucosa, the severity of exudative manifestations, restores free breathing; lowers the pressure in the paranasal cavities and in the middle ear.

Chlorphenamine is a blocker of histamine H1 receptors, has antiserotonin, antihistaminic, weak anticholinergic, sedative effects. Reduces the severity of allergic reactions mediated by histamine, reduces the permeability of capillaries, narrows the vessels, eliminates swelling and flushing of the mucous membrane of the nasal cavity, nasopharynx and accessory sinuses of the nose; reduces local exudative manifestations, suppresses the symptoms of allergic rhinitis: sneezing, rhinorrhea, itching of the eyes, nose. The onset of action is in 20-30 minutes, the duration is 4-4.5 hours.

Pharmacokinetics:

After oral administration acetylsalicylic acid turns into the main metabolite - salicylic acid. Absorption of acetylsalicylic and salicylic acid in the digestive tract occurs quickly and completely. Maximum the concentration of a substance in plasma (serum) blood is reached after 10-20 minutes (Acetylsalicylic Acid) or 45-120 minutes (total salicylate level). The degree of binding to plasma proteins depends on the concentration and is 49-70% for acetylsalicylic and 66-98% for salicylic acid. 50% of the administered dose of the drug is metabolized by primary passage through the liver. Metabolites of acetylsalicylic and salicylic acid are glycine conjugate of salicylic acid, gentisic acid and its glycine conjugate. The drug is excreted as metabolites mainly by the kidneys. PThe half-elimination period (half-life) acetylsalicylic acid is 20 minutes; salicylic acid - increases proportionally to the dose taken and is 2, 4 and 20 hours at a dose of 0.5, 1 and 5 g, respectively. The drug penetrates the blood-brain barrier, as well as into breast milk and synovial fluid.

Phenylephrine is absorbed into the gastrointestinal tract, metabolized in the walls of the intestine and in the liver by the formation of sulfate conjugates. Elimination by the kidneys (in the form of metabolites, unchanged, 2.6-16%). PThe half-elimination period (half-life) 2.62 ± 0.67 hours. F 38%. V_d 4.86 ± 2.48 l / kg (increase in elderly patients). Clearance 29.9 ± 11.6 ml / min / kg. Does not bind to plasma proteins.

Chlorphenamine is relatively slowly absorbed in the gastrointestinal tract, the maximum concentration of substance in blood plasma (serum) is achieved 2-6 hours after oral administration. PThe half-elimination period (half-life) about 24 hours in adults, 9-11 hours - in children and more than 24 hours - in the elderly. 78-90% of chlorphenamine binds to blood plasma proteins and is distributed in tissues, it penetrates the blood-brain barrier. Chlorphenamine is metabolized primarily in the liver by dimethylation to form 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: half-elimination period (half-life) varies from 2 to 43 hours.

Children experience faster absorption of chlorphenamine, higher clearance and shorter half-elimination period (half-life).

Indications:Symptomatic treatment of influenza, acute respiratory viral infections and other colds accompanied by fever, chills, headache and muscle pain, rhinitis and / or nasal congestion, sore throat and sneezing.

ICD-10

X.J00-J06.J00 Acute nasopharyngitis (runny nose)

X.J00-J06.J06 Acute upper respiratory tract infections of multiple and unspecified sites

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

XIII.M70-M79.M79.1 Myalgia

XVIII.R00-R09.R06.7 Sneeze

XVIII.R00-R09.R07.0 A sore throat

XVIII.R50-R69.R50.0 Fever with chills

XVIII.R50-R69.R51 Headache

Contraindications:

Hypersensitivity to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs or other components of the drug; erosive-ulcerative lesion of the gastrointestinal tract (in the phase of exacerbation); bronchospasm caused by the intake of salicylates or other non-steroidal anti-inflammatory drugs; such blood clotting disorders as hemophilia, hypoprothrombinemia; severe dysfunction of the liver and / or kidney; polyposis of the nose,associated with bronchial asthma and intolerance to acetylsalicylic acid; arterial hypertension; angina pectoris; an increase in the thyroid gland; combined use with oral anticoagulants; combined use with monoamine oxidase inhibitors, including 15 days after discontinuation; combined use of methotrexate in a dose of 15 mg per week or more; retention of urine; pregnancy (I and III trimester); the period of breastfeeding.

The drug is not prescribed for children under 15 with acute respiratory infections caused by viral infections, because of the risk of developing Reye's syndrome (encephalopathy and acute fatty liver disease with acute development of liver failure).

Carefully:

Precautions prescribed drug for diseases of the lungs and kidneys, glaucoma, pheochromocytoma, cardiovascular diseases, diabetes, prostatic hypertrophy, anemia.

Pregnancy and lactation:

Recommendations for Food and Drug Administration (US Food and Drug Administration) - Category D.

Contraindicated in pregnancy (during I and III trimesters).Chlorphenamine can cause lactemia depression. For the duration of treatment, breastfeeding should be discontinued.

Dosing and Administration:

Adults and children over the age of 15 years are prescribed 1 packet (contains 500 mg aspirin, 15.58 mg phenylephrine bitartrate, 2 mg chlorphenylamine maleate) every 6-8 hours. The maximum daily dose is 4 sachets, the interval between doses should be at least 6 hours.

Duration of treatment (without consulting a doctor) should not exceed 5 days when used as an anesthetic and more than 3 days - as an antipyretic.

The drug should be taken orally after a meal, previously dissolving the contents of the sachet in a glass of water at room temperature.

Side effects:

Acetylsalicylic acid

From the digestive system: dyspepsia, nausea, vomiting, stomach and duodenal ulcers, gastrointestinal bleeding, including hidden ones; rarely - toxic liver damage, especially in patients with juvenile rheumatoid arthritis.

From the side of the blood coagulation system: hypoprothrombinemia.

From the hemopoietic system: rarely - anemia.

From the central nervous system: dizziness, ringing in the ears, headache, hearing loss.

From the side of the urinary system: renal failure, acute interstitial glomerulonephritis.

Allergic reactions: urticaria, exanthema, angioedema, rhinitis, bronchospasm, dyspnea.

On the part of the body as a whole: hyperhidrosis; rarely - Reye's syndrome in children.

Phenylephrine

From the side of the central nervous system: headache, dry mouth, insomnia, nausea, excitability, anxiety; rarely - severe headache, inadequate behavior.

From the cardiovascular system: rarely - increased blood pressure, tachycardia.

From the genitourinary system: rarely - painful or difficult urination.

Chlorphenamine

On the part of the body as a whole: dry mouth, dry mucous membrane of the mouth and nose, disruption of accommodation (blurred vision).

From the cardiovascular system: tachycardia.

From the digestive system: constipation.

On the part of the urinary system: retention of urination, difficulty and pain when urinating.

From the central nervous system: violation of attention, drowsiness, dizziness. In children and elderly patients, retardation, agitation, dizziness, anxiety, irritability are possible.

The patient should be informed that if any adverse reactions occur, stop taking the medication and consult a doctor.

Overdose:

Symptoms: nausea, vomiting, ringing in the ears, deterioration of hearing and sight, rapid breathing, severe headache, imbalance, pronounced drowsiness, disturbance of the heart rhythm.

Treatment: gastric lavage, the appointment of activated charcoal, symptomatic therapy.

Interaction:

Acetylsalicylic acid

With the simultaneous use of ethanol, cimetidine and ranitidine with acetylsalicylic acid, the toxic effect of the latter increases.

With the simultaneous use of heparin and indirect anticoagulants with acetylsalicylic acid increases the risk of bleeding by suppressing the function of platelets and the displacement of indirect anticoagulants from the connection with blood plasma proteins.

Acetylsalicylic acid reduces the absorption of indomethacin, fenoprofen, naproxen, flurbiprofen, ibuprofen, diclofenac, piroxicam.

With the simultaneous use of glucocorticosteroids with acetylsalicylic acid, the risk of secondary damage to the mucous membrane of the gastrointestinal tract is increased.

Acetylsalicylic acid with simultaneous application can increase the concentration of phenytoin because of its displacement from the bond with proteins.

With the simultaneous use of antidiabetic drugs (including insulin) with acetylsalicylic acid, the hypoglycemic effect is increased due to the fact that acetylsalicylic acid in a high dose has hypoglycemic properties and displaces the derivatives of sulfonylureas from the connection with blood plasma proteins.

Acetylsalicylic acid with simultaneous application can enhance the ototoxic effect of vancomycin.

With the simultaneous use of methotrexate with acetylsalicylic acid, the effect of methotrexate is enhanced by reducing renal clearance and displacing it from the bond with proteins.

Salicylates with simultaneous application reduce the uricosuric effect of probenecid and sulfinpyrazone due to competitive tubular elimination of uric acid.

With the simultaneous use of zidovudine with acetylsalicylic acid, there is a mutual increase in toxic effects.

Phenylephrine

With simultaneous use of phenylephrine and monoamine oxidase inhibitors (antidepressants - tranylcypromine, moclobemide; antiparkinsonian drugs - selegiline) severe side effects are possible in the form of intense headache, increased blood pressure and body temperature.

With the simultaneous use of phenylephrine with beta-adrenoblokatorami possible increase in blood pressure and pronounced bradycardia.

With the simultaneous use of phenylephrine with sympathomimetics, the influence of the latter on the central nervous system and cardiovascular system is enhanced. Perhaps stimulation, irritability, insomnia.

The use of phenylephrine before inhalation anesthesia increases the risk of cardiac arrhythmia. It is necessary to stop phenylephrine treatment several days before the planned surgical treatment.

With the simultaneous use of alkaloids rauwolfia can reduce the therapeutic effect of phenylephrine.

With the simultaneous use of phenylephrine and caffeine, the therapeutic and toxic effects of phenylephrine can be enhanced.

In single cases with the simultaneous use of phenylephrine with indomethacin or bromocriptine, the development of severe arterial hypertension is possible.

With the simultaneous use of phenylephrine with antidepressants, a group of selective serotonin reuptake inhibitors (fluvoxamine, paroxetine, sertraline) may increase as the sensitivity of the body to sympathomimetics, and the risk of developing serotonergic syndrome increases.

With simultaneous application phenylephrine reduces the antihypertensive effect of antihypertensive drugs from the group of sympatholytics (reserpine, guanethidine).

Chlorphenamine

With the simultaneous use of chlorphenamine can increase the inhibitory effect on the central nervous system of ethanol, hypnotics, tranquilizers, antipsychotics (neuroleptics), analgesics of central action.

With the simultaneous use of chlorphenamine enhances the anticholinergic effect of anticholinergic drugs (atropine, antispasmodics, tricyclic antidepressants, monoamine oxidase inhibitors).

Special instructions:

Acetylsalicylic acid can cause bronchospasm, an attack of bronchial asthma or other hypersensitivity reactions. Risk factors are the presence of bronchial asthma, polyps of the nose, fever, chronic bronchopulmonary diseases, cases of allergy in the history (allergic rhinitis, rashes on the skin).

Acetylsalicylic acid can increase the tendency to bleeding, which is due to its inhibitory effect on platelet aggregation. This should be considered when surgical interventions are required, including minor interventions such as tooth extraction. Before surgery, to reduce bleeding during surgery and in the post-operation period, you should cancel taking the drug for 5-7 days and inform the doctor.

Children should not be prescribed drugs containing acetylsalicylic acid, because in the case of a viral infection, the risk of developing Reye syndrome increases. Symptoms of Reye's syndrome include prolonged vomiting, acute encephalopathy, and enlargement of the liver.

During treatment, it is not recommended to drink alcohol because of the increased risk of side effects from the gastrointestinal tract associated with taking acetylsalicylic acid and enhancing the sedative effect of chlorphenamine.

In connection with the fact that with the use of chlorphenamine it is possible to change the parameters of skin allergic tests, it is recommended to inform the doctor about the use of the drug and to cancel it 3 days before the skin tests.

During treatment, it is not recommended to use anesthetics, sympathomimetics, guanethidine and beta-blockers.

It is not recommended to take the drug systematically and with a preventive goal before the vaccination.

With renal insufficiency with a decreased level of albumin in the plasma, the risk of the toxic effect of the drug increases.

Active component phenylephrine, which is part of the drug, can cause a positive result in the doping test for athletes.

The drug may cause drowsiness and, in this regard, worsen the ability to drive and move vehicles.

Patients who limit the use of salt, must take into account that each packet contains sodium bicarbonate.

Instructions

Acetylsalicylic acid + Phenylephrine + Chlorphenamine (Acidum acetylsalicylicum + Clopidogrelum)