Instructions Coldrex MaxGrip lemon powder for oral solution sachet No. 10
Composition
active ingredients: paracetamol, phenylephrine hydrochloride, ascorbic acid;
1 packet contains paracetamol 1000 mg, phenylephrine hydrochloride 10 mg, ascorbic acid 40 mg;
excipients: sucrose, anhydrous citric acid, sodium citrate, corn starch, sodium cyclamate, sodium saccharin, anhydrous colloidal silicon dioxide, lemon flavoring, curcumin (E 100).
Dosage form
Powder for oral solution.
Main physicochemical properties: heterogeneous, free-flowing powder of light yellow color with a lemon odor.
Pharmacotherapeutic group
Analgesics and antipyretics. Paracetamol, combinations without psycholeptics. ATX code N02B E51.
Pharmacological properties
Pharmacodynamics
Paracetamol is an analgesic and antipyretic. Its mechanism of action is due to the inhibition of prostaglandin synthesis, primarily in the central nervous system. The lack of inhibition of peripheral prostaglandin synthesis results in the preservation of protective prostaglandins in the gastrointestinal tract. Paracetamol is therefore suitable, in particular, for patients with a history of disease or concomitant therapy in whom inhibition of peripheral prostaglandin synthesis would be undesirable (e.g., patients with a history of gastrointestinal bleeding or the elderly).
Phenylephrine hydrochloride is a sympathomimetic. Its action is primarily associated with direct stimulation of adrenoreceptors, mainly alpha-adrenoreceptors. Phenylephrine hydrochloride reduces swelling of the nasal mucosa.
Ascorbic acid is a vital vitamin that is added to the preparation to compensate for the loss of vitamin C that may occur at the beginning of a viral infection.
Pharmacokinetics
Paracetamol is rapidly and almost completely absorbed from the gastrointestinal tract. Binding to plasma proteins at therapeutic concentrations is minimal. Paracetamol is metabolized in the liver and excreted in the urine mainly as glucuronide and sulfate conjugates. Less than 5% is excreted as unchanged paracetamol.
Phenylephrine is unevenly absorbed from the gastrointestinal tract. It undergoes presystemic metabolism under the influence of monoamine oxidases in the intestine and liver, so when administered orally, the bioavailability of phenylephrine is reduced. It is almost completely excreted in the urine as sulfate conjugates.
Ascorbic acid is rapidly absorbed from the gastrointestinal tract and widely distributed throughout the body. Binding to plasma proteins is 25%. Excess ascorbic acid is excreted from the body in the urine in the form of metabolites.
Indication
Short-term relief of symptoms of colds and flu, such as headache, sore throat, nasal congestion, sinusitis and associated pain, body aches and pains, fever.
Contraindication
Hypersensitivity to any of the components of the drug, severe cardiovascular insufficiency, severe liver and/or kidney dysfunction, congenital hyperbilirubinemia, glucose-6-phosphate dehydrogenase deficiency, alcoholism, blood diseases (including severe anemia, leukopenia), thrombosis, thrombophlebitis, states of increased excitement, acute pancreatitis, prostatic hypertrophy with urinary retention, severe forms of diabetes mellitus, epilepsy, pheochromocytoma, hyperthyroidism, angle-closure glaucoma, severe forms of arterial hypertension, atherosclerosis, ischemic heart disease; sleep disorders.
Do not use with monoamine oxidase inhibitors (MAOIs) and within 2 weeks after stopping their use, with tricyclic antidepressants, beta-blockers or other antihypertensive drugs.
Interaction with other medicinal products and other types of interactions
The rate of absorption of paracetamol may be increased by concomitant use with metoclopramide and domperidone and decreased by cholestyramine. The anticoagulant effect of warfarin and other coumarins may be enhanced with an increased risk of bleeding with concomitant long-term, regular, daily use of paracetamol. With short-term use according to the recommended regimen, these interactions are not clinically significant.
Barbiturates reduce the antipyretic effect of paracetamol.
Anticonvulsants (including phenytoin, barbiturates, carbamazepine) that stimulate the activity of liver microsomal enzymes may enhance the toxic effect of paracetamol on the liver due to an increase in the degree of conversion of the drug to hepatotoxic metabolites.
The interaction of phenylephrine with MAO inhibitors causes a hypertensive effect, with tricyclic antidepressants (e.g. amitriptyline) and other sympathomimetics - increases the risk of cardiovascular side effects, with digoxin and cardiac glycosides - leads to heart rhythm disturbances or myocardial infarction. Phenylephrine may reduce the effectiveness of beta-blockers and other antihypertensive drugs (including debrisoquine, guanethidine, reserpine, methyldopa) with an increased risk of arterial hypertension and other adverse reactions from the cardiovascular system. Simultaneous use with ergot alkaloids (e.g. ergotamine and methysergide) may increase the risk of ergotism.
Ascorbic acid when taken orally enhances the absorption of penicillin, iron, reduces the effectiveness of heparin and indirect anticoagulants, increases the risk of crystalluria during treatment with salicylates. Antidepressants, antiparkinsonian and antipsychotic drugs, phenothiazine derivatives increase the risk of urinary retention, dry mouth, constipation. Glucocorticosteroids increase the risk of glaucoma, large doses of the drug reduce the effectiveness of tricyclic antidepressants.
Vitamin C absorption is reduced with the simultaneous use of oral contraceptives, consumption of fruit or vegetable juices, and alkaline drinks.
Ascorbic acid should be taken only 2 hours after deferoxamine injection, as their simultaneous administration increases iron toxicity, especially in the myocardium.
Prolonged administration of large doses in individuals treated with disulfiram inhibits the disulfiram-alcohol reaction.
Application features
Consult a doctor before using the drug. Contains paracetamol.
Concomitant use with other paracetamol-containing drugs may lead to overdose. Paracetamol overdose may cause liver failure, which may require liver transplantation or be fatal.
Cases of hepatic dysfunction/failure have been reported in patients with reduced glutathione levels, such as those who are severely malnourished, anorexic, have a low body mass index, or suffer from chronic alcohol dependence.
Patients with arterial hypertension, cardiovascular disease, diabetes, hyperthyroidism, angle-closure glaucoma, pheochromocytoma, prostatic hypertrophy, Raynaud's disease, liver and kidney dysfunction should consult a doctor before using the drug. Underlying liver disease increases the risk of liver damage associated with paracetamol.
In patients with severe infections such as sepsis, which are accompanied by a decrease in glutathione levels, the risk of metabolic acidosis may be increased when taking paracetamol. Symptoms of metabolic acidosis include deep, rapid or difficult breathing, nausea, vomiting, loss of appetite. You should immediately consult a doctor if these symptoms occur. Phenylephrine, which is part of the drug, can cause angina attacks.
The drug should not be used in patients taking other sympathomimetics (e.g., decongestants, cold and flu remedies, appetite suppressants, and amphetamine-like psychostimulants). Do not exceed recommended doses. If symptoms persist or worsen within 7 days of treatment with the drug, are accompanied by high fever, rash, or persistent headache, consult a doctor.
Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency should not take this medicine. One sachet (1 dose) contains 3.725 g of sucrose. This should be taken into account by patients with diabetes. 1 dose contains 130 mg of sodium. This should be taken into account by patients on a controlled sodium diet.
Use during pregnancy or breastfeeding
The drug is not used during pregnancy, except in cases where the expected benefit to the woman justifies the potential risk to the fetus. It should be used in the lowest effective dose and for the shortest duration of treatment. Use only as directed by a doctor.
Paracetamol and phenylephrine may pass into breast milk. During breastfeeding, it should be used only as directed by a doctor.
Ability to influence reaction speed when driving vehicles or other mechanisms
If dizziness occurs while using the drug, it is not recommended to drive a vehicle or operate complex machinery.
Method of administration and doses
The drug is intended for oral administration.
Adults and children over 12 years of age: 1 sachet every 4-6 hours as needed. Do not take more often than every 4 hours. The maximum daily dose is 4 sachets. The course of treatment without medical advice is no more than 7 days. Do not exceed the indicated doses. If the patient's condition does not improve during treatment with the drug, you should consult a doctor. You should take the lowest dose necessary to achieve effectiveness.
Children
The drug is not recommended for use in children under 12 years of age.
Overdose
The risk of overdose is increased in patients with liver disease.
Overdose is usually caused by paracetamol and is manifested by pale skin, anorexia, nausea, vomiting, abdominal pain, hepatonecrosis, increased activity of hepatic transaminases, increased prothrombin index. Symptoms of liver damage are observed 24–48 hours after overdose and may reach a peak after 4–6 days. Glucose metabolism disorders and metabolic acidosis may occur. In severe poisoning, liver failure may progress and lead to the development of toxic encephalopathy with impaired consciousness, hemorrhages, hypoglycemia, cerebral edema, in some cases - to the need for liver transplantation or death.
Acute renal failure with acute tubular necrosis may present with severe back pain, hematuria, and proteinuria and may occur even in the absence of severe liver damage. Cardiac arrhythmias have also been reported. Acute pancreatitis has been reported in patients with liver dysfunction and toxicity.
Liver damage is possible in adults who have taken more than 10 g of paracetamol and in children who have taken more than 150 mg/kg of body weight. Ingestion of 5 g or more of paracetamol may lead to liver damage in patients with risk factors (long-term treatment with carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St. John's wort or other drugs that induce liver enzymes; regular intake of excessive amounts of ethanol; glutathione cachexia (digestive disorders, cystic fibrosis, HIV infection, starvation, cachexia).
Treatment: Paracetamol overdose requires immediate medical attention, even if no symptoms of overdose are present. The patient should be taken to hospital immediately, even if early symptoms of overdose are absent. Symptoms may be limited to nausea and vomiting or may not reflect the severity of the overdose or the risk of organ damage.
Activated charcoal should be considered if paracetamol overdose has been taken within 1 hour. Plasma paracetamol concentrations should be measured 4 hours or later after ingestion (earlier concentrations are unreliable). N-acetylcysteine treatment can be used up to 24 hours after ingestion of paracetamol, but maximum protection is achieved when administered within 8 hours of ingestion. The efficacy of the antidote decreases sharply after this period. If necessary, N-acetylcysteine should be administered intravenously to the patient according to the established dose schedule. In the absence of vomiting, oral methionine may be used as a suitable alternative in remote areas outside the hospital.
Overdose due to phenylephrine may lead to effects similar to those listed in the section "Adverse reactions". Other symptoms include irritability, restlessness, hypertension and possibly reflex bradycardia. In severe cases, confusion, hallucinations, convulsions and arrhythmia may occur. However, the amount of the drug that can lead to serious phenylephrine toxicity is greater than the amount required to develop toxic effects on the liver of paracetamol.
Treatment: in case of overdose, gastric lavage, administration of activated charcoal, symptomatic therapy, use of alpha-blockers such as phentolamine, in case of severe arterial hypertension are necessary.
High doses of ascorbic acid (over 3000 mg) may cause temporary osmotic diarrhea and gastrointestinal disturbances such as nausea and abdominal discomfort. The effects of ascorbic acid overdose may be attributed to severe liver failure caused by paracetamol overdose.
Adverse reactions
Skin and subcutaneous tissue disorders: rash, urticaria, allergic dermatitis, Stevens-Johnson syndrome, pruritus, erythema multiforme, toxic epidermal necrolysis.
Immune system disorders: allergic reactions (including angioedema), anaphylactic shock, hypersensitivity reactions.
Mental disorders: psychomotor agitation and disorientation, anxiety, nervousness, feelings of fear, irritability, sleep disturbances, insomnia, confusion, depression, hallucinations.
From the nervous system: headache, dizziness, paresthesia.
From the side of the organs of hearing and vestibular apparatus: tinnitus.
On the part of the organs of vision: mydriasis, acute angle-closure glaucoma (more often in patients with glaucoma), visual impairment and accommodation.
On the part of the hepatobiliary system: impaired liver function, increased activity of liver enzymes, hepatonecrosis (dose-dependent effect), liver failure.
From the blood and lymphatic system: anemia (including hemolytic), sulfhemoglobinemia and methemoglobinemia, thrombocytopenia, leukopenia, agranulocytosis, pancytopenia, bruising or bleeding.
On the part of the kidneys and urinary system: urination disorders, urinary retention (more likely in patients with prostatic hypertrophy), renal colic, nephrotoxic effect.
Cardiovascular system: increased blood pressure, tachycardia or reflex bradycardia, palpitations, shortness of breath, heart pain.
Respiratory, thoracic and mediastinal disorders: bronchospasm in patients sensitive to aspirin and other nonsteroidal anti-inflammatory drugs.
Others: general weakness, fever, hypoglycemia, glycosuria, zinc and copper metabolism disorders.
The drug may have a slight laxative effect.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C, out of the reach and sight of children.
Packaging
5 or 10 bags in a cardboard box.
Vacation category
Without a prescription.
Producer
SmithKline Beecham SA, Spain.
Address
Ctra. de Ajalvir, Km. 2.500, Alcalа de Henares 28806 (Madrid), Spain/Ctra. de Ajalvir, Km. 2.500, Alcalа de Henares 28806 (Madrid), Spain.
