Properties
What is it?
Active ingredients per sachet: Paracetamol 500 mg Guaifenesin 200 mg Phenylephrine hydrochloride 10 mg Excipients: Sucrose (compressible); Ascorbic acid; Citric acid, anhydrous; Sodium citrate; Sodium cyclamate (E 952); Aspartame (E 951); Acesulfame potassium; Silicon dioxide, colloidal anhydrous; Lemon flavour (mixture of flavouring substances and maltodextrin); Mint flavour (mixture of flavouring substances, menthol and maltodextrin) Therapeutic indications: Short-term symptomatic treatment of cold and acute viral diseases accompanied by pain, headache, nasal congestion, sore throat and cough in adults and children over 12 years of age. Dosage: Adults and children over 12 years of age Single dose: 1 sachet (Paracetamol 500 mg, Guaifenesin 200 mg, Phenylephrine 10 mg) as needed, at intervals of 4-6 hours. Maximum daily dose: 4 single doses Children under 12 years of age: This product is not intended for use in children under 12 years of age. Elderly patients: No dose adjustment is required in elderly patients. Method of administration: - Empty the contents of the sachet into a cup of hot (but not boiling) water (150 ml), stir well to obtain a homogeneous solution. - When the solution has reached a suitable temperature, take orally. - The duration of treatment should not exceed 5 days, unless prescribed by a doctor. Contraindications: - Hypersensitivity to paracetamol, guaifenesin, phenylephrine or any of the excipients; - Severe liver or kidney disorders; - Heart diseases and cardiovascular system disorders, including severe hemolytic anemia; - Arterial hypertension; - Hyperthyroidism; - Diabetes mellitus; - Pheochromocytoma; - Angle-closure glaucoma; - Urinary retention; - Use of tricyclic antidepressants or beta-blockers - Patients taking or who have taken MAO inhibitors within the last 14 days; - Patients taking other sympathomimetics (decongestants, appetite suppressants and amphetamine-like psychostimulants). Special warnings and precautions for use: - This preparation is recommended for use only in patients with confirmed clinical symptoms (muscle and joint pain, fever, nasal congestion and cough). - Before use, it is necessary to check (with a doctor or pharmacist) whether other preparations containing sympathomimetics can be taken, regardless of their route of administration (oral or topical, including eye or nasal drops, inhalers). - Preparations of the sympathomimetic group should be used with caution in patients with ischemic heart disease (IHD). In the following patient groups, this medicinal product should be used after consulting a doctor: - Prostatic hyperplasia or other conditions causing urinary disorders - Vascular occlusive diseases (e.g., Raynaud's disease) - Cardiovascular diseases - Myasthenia gravis - Severe gastrointestinal diseases Avoid taking with other paracetamol-containing preparations to reduce the risk of overdose. The maximum daily dose of paracetamol should not exceed 3 g. The use of paracetamol should be limited in patients with severe kidney or liver disease. Paracetamol overdose is particularly dangerous in subjects with liver disease associated with alcohol abuse. In patients with chronic cough and asthma, the preparation should be used after consulting a doctor. Consultation is also necessary if the cough lasts longer than 5 days, if there is recurrent cough after stopping treatment, or if the cough is accompanied by significant fever, rash, or persistent headache. This medicinal product contains: - Sucrose, therefore the preparation should not be used in patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltase deficiency. - A source of phenylalanine/aspartame (E951). It may be harmful for patients with phenylketonuria. - 49.1 mg of sodium per dose. This should be taken into account by patients on a low-sodium diet. Interactions with other medicinal products and other forms of interaction: Paracetamol - Regular long-term intake of paracetamol may increase the anticoagulant effect of warfarin and other coumarin anticoagulants, which may lead to an increased risk of bleeding, although usual doses do not have a significant effect. - The hepatotoxic effect of paracetamol may be enhanced by significant alcohol consumption. Barbiturates, MAO inhibitors and tricyclic antidepressants may increase the hepatotoxicity of paracetamol, especially in case of overdose. - Absorption of paracetamol is increased when taken with metoclopramide or domperidone and decreased when taken with cholestyramine. - Regular use of paracetamol may lead to decreased metabolism of zidovudine (increased risk of neutropenia). - Use of salicylates/aspirin may prolong the plasma half-life of paracetamol. - Concurrent administration of paracetamol and NSAIDs increases the risk of kidney dysfunction. - Paracetamol can alter the results of some laboratory tests for blood glucose and uric acid. Phenylephrine Products containing phenylephrine should be used with caution due to possible reactions with the following preparations: - MAO inhibitors (including moclobemide): Hypertensive reactions may occur with the simultaneous administration of sympathomimetic amines (e.g., phenylephrine) and MAO inhibitors. - Sympathomimetic amines: Simultaneous use of phenylephrine and other sympathomimetic amines may increase the risk of cardiovascular side effects. - Beta-blockers and other antihypertensive agents (debrisoquine, guanethidine, reserpine, methyldopa): Phenylephrine may reduce the effectiveness of beta-blockers and antihypertensive agents. The risk of hypertension and other cardiovascular side effects may increase. - Tricyclic antidepressants (e.g., amitriptyline): Concurrent administration with phenylephrine may increase the risk of cardiovascular side effects. - Ergot alkaloids (ergotamine and methylsergide): Increased risk of ergotism. - Digoxin and other cardiac glycosides: Increased risk of arrhythmias and heart attack. - Phenothiazines as sedatives: CNS effects may be enhanced. - Halogenated general anesthetics (cyclopropane, halothane, enflurane, isoflurane): Possible provocation or worsening of ventricular arrhythmias. Guaifenesin - It enhances the effect of sedatives and muscle relaxants. - During a 24-hour urine collection after taking this preparation, its metabolites may affect the color in the determination of 5-hydroxyindoleacetic acid (5-HIAA) and vanillylmandelic acid (VMA). Fertility: There is no data on the effect of active substances on fertility. Pregnancy According to epidemiological studies, paracetamol does not have a negative impact on pregnancy and the health of the fetus and newborn in humans when the drug is used at recommended doses and duration. There is no data on fetotoxic and teratogenic effects. The safety of guaifenesin and phenylephrine during pregnancy in humans has not been established. Lactation Paracetamol and phenylephrine are excreted in breast milk in clinically insignificant amounts. This medicinal product should not be used during pregnancy and breastfeeding unless prescribed by a doctor. Effects on ability to drive and use machines: Patients should be advised not to drive or operate machinery if they experience dizziness after taking the preparation. Side effects: Paracetamol - Disorders of the blood and lymphatic system: Thrombocytopenia; agranulocytosis; these side effects were not necessarily causally related to paracetamol. - Immune system disorders: Anaphylaxis; hypersensitivity skin reactions: rash, angioneurotic edema, Stevens-Johnson syndrome; toxic epidermal necrolysis. - Respiratory, thoracic and mediastinal disorders: Bronchospasm* - Hepatobiliary disorders: Liver dysfunction. - Gastrointestinal disorders: Acute pancreatitis* *More likely in asthmatic patients sensitive to aspirin or other NSAIDs. Guaifenesin - Immune system disorders: Allergic reactions, angioneurotic edema, anaphylactic reactions. - Respiratory, thoracic and mediastinal disorders: Dyspnea. - Gastrointestinal disorders: Nausea, vomiting, abdominal discomfort, diarrhea. - Skin and subcutaneous tissue disorders: Rash, urticaria. Phenylephrine Most common: - Psychiatric disorders: Restlessness, irritability, anxiety, agitation. - Nervous system disorders: Headache, dizziness, insomnia. - Cardiac disorders: Increased blood pressure. - Gastrointestinal disorders: Nausea, vomiting, diarrhea. Rare: - Eye disorders: Mydriasis, acute angle-closure glaucoma (more common in patients with angle-closure glaucoma). - Cardiac disorders: Tachycardia, palpitations. - Skin and subcutaneous tissue disorders: Allergic reactions (rash, urticaria, allergic dermatitis), hypersensitivity reactions, including cross-hypersensitivity reactions to other sympathomimetics. - Kidney and urinary tract disorders: Dysuria, urinary retention (most common in patients with bladder outlet obstruction, e.g., prostatic hypertrophy). Overdose Paracetamol In adults, liver dysfunction may occur after taking 10 g or more of paracetamol. A dose of 5 g may cause liver dysfunction in high-risk patients, such as: - Long-term treatment with liver enzyme inducers (carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St. John's wort-containing preparations); - Regular consumption of alcohol in amounts exceeding the recommended permissible level; - Diseases and conditions that reduce glutathione levels, e.g., eating disorders, starvation, cachexia, cystic fibrosis, HIV infection. Symptoms - Symptoms of overdose in the first 24 hours include pallor, nausea, vomiting, loss of appetite, anorexia, and abdominal pain. - Liver dysfunction usually appears 12-48 hours after administration, with impaired glucose metabolism and metabolic acidosis. - In severe cases, it can progress to encephalopathy, bleeding, hypoglycemia, cerebral edema, and death. - Acute kidney dysfunction with acute tubular necrosis, manifested by flank pain, hematuria, proteinuria, may develop without liver dysfunction. - There are reports of cardiac arrhythmias and pancreatitis. Treatment - Paracetamol overdose requires urgent treatment. Despite the absence of early symptoms, patients should be hospitalized and symptomatic treatment should be provided. - Treatment with activated charcoal is recommended within the first hour of ingestion. - Plasma paracetamol concentration should be monitored 4 hours or later after ingestion. - Treatment with N-acetylcysteine, which can also be administered parenterally, is recommended within 24 hours of ingestion, with maximum protective effect observed within 8 hours. The effectiveness of N-acetylcysteine decreases after this period. Phenylephrine Symptoms: Phenylephrine overdose usually manifests with symptoms similar to the described side effects. Hypertension and bradycardia may also occur; in severe cases, confusion, hallucinations, seizures, and arrhythmias. Treatment: Treatment is symptomatic. Severe hypertension sometimes requires the use of alpha-blockers such as phentolamine. Guaifenesin Symptoms: Ingestion of very high doses may cause nausea and vomiting. Treatment: In case of vomiting, rehydration with water and electrolytes may sometimes be necessary. Pharmacodynamic properties: Pharmacotherapeutic group: Combinations of paracetamol, excluding psycholeptics. Paracetamol has analgesic and antipyretic properties, due to the inhibition of prostaglandin synthesis in the CNS and less so by peripheral mechanisms related to the blockade of painful impulses. Paracetamol has an antipyretic effect by acting on the thermoregulatory center, leading to peripheral vasodilation, which increases blood flow to the skin, resulting in sweating and heat loss. Guaifenesin is believed to loosen and facilitate expectoration by increasing the volume and reducing the viscosity of bronchial secretions; it increases mucociliary clearance. Phenylephrine is a sympathomimetic decongestant that acts on alpha-adrenergic receptors in the respiratory system, causing vasoconstriction and reducing inflammation and swelling of the nasal and sinus mucosa. By the same mechanism, it reduces mucus production, thereby preventing secretion buildup in the nasal cavity and reducing pressure and pain associated with secretion retention. Pharmacokinetic properties: Paracetamol is rapidly absorbed from the gastrointestinal tract. Peak plasma concentrations are reached 10-60 minutes after oral administration. It is metabolized in the liver and excreted in the urine mainly as glucuronide and sulfate conjugates. Its plasma half-life is 1-3 hours. Guaifenesin is rapidly absorbed after oral administration, with peak plasma concentrations reached in approximately 15 minutes. It is rapidly metabolized by oxidation to β-(2-methoxyphenoxy)lactic acid, which is excreted in the urine. The elimination half-life is approximately 1 hour. Phenylephrine is unevenly absorbed from the gastrointestinal tract and undergoes first-pass metabolism by monoamine oxidase in the intestinal wall and liver. Phenylephrine has low oral bioavailability. Peak plasma concentrations are reached 1-2 hours after administration. It is excreted in the urine as sulfate conjugates. The plasma half-life is 2-3 hours. Preclinical safety data: Based on standard studies of pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, and reproductive toxicity, non-clinical data do not reveal any special hazard to humans. Shelf life: 3 years Special precautions for storage: Store at a temperature not exceeding 25°C. Dispensing category: Pharmaceutical product group III, available without prescription. Marketing authorization holder: Adipharm EAD 130, Simeonovsko Shosse Blvd., Sofia 1700, Bulgaria