Instructions for Flucold sachet powder 5 g with lemon flavor No. 10
Composition
active ingredients: paracetamol, ascorbic acid, phenylephrine hydrochloride;
1 sachet of 5 g contains: paracetamol 750 mg, phenylephrine hydrochloride 10 mg,
ascorbic acid, coated 60 mg;
excipients: mannitol (E 421), anhydrous lactose, aspartame (E 951), starch, anhydrous citric acid, sodium citrate, lemon flavor, quinoline yellow (E 104), calcium gluconate.
Dosage form
Lemon-flavored powder for oral solution.
Main physicochemical properties: pale yellow powder.
Pharmacotherapeutic group
Analgesics and antipyretics. Paracetamol, combinations without psycholeptics. ATX code N02B E51.
Pharmacological properties
Pharmacodynamics
Paracetamol has analgesic and antipyretic effects. It has the ability to inhibit prostaglandin synthesis by inhibiting arachidonic acid cyclooxygenase in the central nervous system (CNS). This results in a decrease in the sensitivity of the CNS to the action of kinins and serotonin, which leads to a decrease in sensitivity to pain. In addition, a decrease in the concentration of prostaglandins in the hypothalamus has an antipyretic effect. Paracetamol does not affect platelet aggregation.
Phenylephrine hydrochloride belongs to the sympathomimetic amines, mainly directly affecting adrenoreceptors, predominantly acting on α-adrenoreceptors, which leads to a decrease in hyperemia of the nasal mucosa.
Ascorbic acid (vitamin C) is a vital vitamin, a deficiency of which can occur at the onset of acute viral infections.
The sedative effect of the active ingredients of the drug has not been established.
Pharmacokinetics
Paracetamol is rapidly and almost completely absorbed from the gastrointestinal tract and is evenly distributed throughout all body fluids. The rate of absorption is reduced when paracetamol is taken with food. In therapeutic doses, paracetamol binds to plasma proteins to a negligible extent. The drug is metabolized in the liver and is almost completely excreted in the urine, mainly in the form of glucuronides and sulfate conjugates.
The potentially hepatotoxic intermediate metabolite N-acetyl-p-benzoquinoneimine (NAPQI), which is formed in small amounts (5%), is excreted with cysteine or mercapturic acid after conjugation with glutathione. When using large doses of paracetamol, glutathione reserves in the liver are depleted, which leads to the accumulation of toxic metabolites in the liver. This can lead to damage to hepatocytes, their death and acute liver failure.
Less than 5% of the administered dose of paracetamol is excreted unchanged.
The average half-life of paracetamol is 1 to 4 hours.
Patients with impaired liver function. The half-life of paracetamol in subjects with compensated liver failure is the same as in healthy subjects. In case of severe liver failure, the half-life of paracetamol may be increased. The clinical significance of the increase in the half-life of paracetamol in patients with liver disease is unknown. No accumulation, hepatotoxicity or impaired conjugation with glutathione was observed.
Patients with renal impairment. More than 90% of a therapeutic dose of paracetamol is usually excreted in the urine as metabolites within 24 hours. In patients with chronic renal failure, the ability to excrete polar metabolites is limited, which may lead to their accumulation. In patients with chronic renal failure, it is recommended to increase the interval between doses of paracetamol.
Ascorbic acid (vitamin C) is rapidly absorbed in the gastrointestinal tract and delivered to all body tissues, 25% binds to blood plasma proteins. Excess ascorbic acid, exceeding the body's needs, is excreted in the urine in the form of metabolites.
Phenylephrine hydrochloride is easily and rapidly absorbed from the gastrointestinal tract. It undergoes primary metabolism by monoamine oxidase in the intestine and liver, its bioavailability reaches 40%. The maximum concentration of the drug in the blood plasma is reached after 1–2 hours. The half-life is from 2 to 3 hours. It is excreted in the urine mainly in the form of sulfates.
Indication
Short-term relief of symptoms of colds and flu, including headache, fever, nasal congestion, sinusitis and associated pain, sore throat, body aches.
Contraindication
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 and sympathomimetics.
Interaction with other medicinal products and other types of interactions
The rate of absorption of paracetamol may increase with simultaneous use with metoclopramide and domperidone and decrease with cholestyramine. The anticoagulant effect of warfarin and other coumarins may be enhanced with an increased risk of bleeding with simultaneous 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.
Simultaneous use of high doses of paracetamol with isoniazid increases the risk of developing hepatotoxic syndrome. Paracetamol reduces the effectiveness of diuretics. Do not use simultaneously with alcohol.
The interaction of phenylephrine with monoamine oxidase inhibitors causes a hypertensive effect, with tricyclic antidepressants (e.g. amitriptyline) - increases the risk of cardiovascular side effects, with digoxin and cardiac glycosides - leads to heart rhythm disturbances or myocardial infarction. Phenylephrine with other sympathomimetics increases the risk of adverse reactions from the cardiovascular system. 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.
Concomitant use of phenylephrine with ergot alkaloids (ergotamine and methysergide) may increase the risk of developing 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.
Absorption of vitamin C is reduced by concomitant use of oral contraceptives, consumption of fruit or vegetable juices, alkaline drinks. Ascorbic acid can be taken only 2 hours after the injection of deferoxamine, since their simultaneous administration increases iron toxicity, especially in the myocardium. Long-term administration of large doses in persons treated with disulfiram inhibits the disulfiram-alcohol reaction.
Application features
Before using the drug, you should consult a doctor.
Contains paracetamol. Avoid concomitant use with other medicines for the symptomatic treatment of colds and flu, vasoconstrictors for the treatment of rhinitis, medicines containing paracetamol. Concomitant use with other medicines containing paracetamol may lead to overdose. Paracetamol overdose may cause liver failure, which may require liver transplantation or be fatal. The risk of overdose is higher in patients with non-cirrhotic alcoholic liver disease.
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, sepsis.
Before using the drug, people taking warfarin, with Raynaud's disease (which can manifest as pain in the fingers and toes in response to cold or stress), with hypertension, cardiovascular diseases, impaired liver and kidney function should consult a doctor.
The drug contains phenylephrine, which may cause angina attacks.
This medicinal product should not be used in patients taking other sympathomimetics (e.g. decongestants, appetite suppressants and amphetamine-type psychostimulants). Use with caution in patients taking digoxin, cardiac glycosides or ergot alkaloids (e.g. ergotamine, methysergide).
Patients should consult a doctor if symptoms persist for more than 5 days, worsen, or if symptoms are accompanied by high fever, skin rash, or persistent headache.
This medicinal product contains 69 mg of sodium per sachet as sodium citrate. Caution should be exercised when used in patients on a controlled sodium diet. Aspartame is a derivative of phenylalanine, which may be dangerous for patients with phenylketonuria.
The medicine may have a mild laxative effect due to the mannitol content in the composition. If the patient has been diagnosed with intolerance to some sugars, consult a doctor before taking this medicine.
Use during pregnancy or breastfeeding
Do not use the drug during pregnancy.
Paracetamol and phenylephrine can pass into breast milk, so if necessary, breastfeeding should be discontinued.
Ability to influence reaction speed when driving vehicles or other mechanisms
If certain side effects develop, such as dizziness, the drug may affect the ability to drive or operate complex machinery.
Method of administration and doses
Dissolve the contents of 1 sachet in a glass of hot water, stir until completely dissolved and drink.
Adults and children over 12 years of age: 1 sachet.
The drug should be taken every 4-6 hours, depending on the need.
The minimum interval between doses is 4 hours.
The maximum daily dose is 5 sachets.
Do not use the drug for more than 5 days without consulting a doctor.
Do not exceed recommended doses.
The lowest dose necessary to achieve effectiveness should be taken for the shortest period of time.
Children.
The drug is not recommended for use in children under 12 years of age.
Overdose
Overdose is usually caused by paracetamol and is manifested by pale skin, anorexia, nausea, vomiting, abdominal pain, hepatonecrosis, increased activity of hepatic transaminases, and an increase in the prothrombin index.
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 alcohol consumption; with glutathione cachexia (digestive disorders, cystic fibrosis, HIV infection, malnutrition, cachexia) when taking 5 g or more of paracetamol, liver damage is possible in patients with risk factors.
Symptoms of liver damage are observed 12–48 hours after overdose and may peak after 4–6 days. Glucose metabolism disorders and metabolic acidosis may occur. In severe poisoning, liver failure may progress and lead to toxic encephalopathy with impaired consciousness, in some cases - to the need for liver transplantation or to death. Liver damage is possible in adults who have taken 10 g or more of paracetamol, and in children who have taken paracetamol in excess of 150 mg/kg of body weight.
Acute renal failure with acute tubular necrosis may present with severe low back pain, hematuria, and proteinuria, and may occur even in the absence of severe liver damage. Cardiac arrhythmias and pancreatitis have also been reported.
With prolonged use in high doses, aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, and thrombocytopenia are possible.
Treatment: In case of paracetamol overdose, immediate medical attention is required, even if no symptoms of overdose are observed. Symptoms may be limited to nausea and vomiting or may not reflect the severity of the overdose or the risk of organ damage. Gastric lavage, administration of activated charcoal (within 1 hour of overdose) and symptomatic therapy should be performed. The use of paracetamol antidotes - N-acetylcysteine intravenously and methionine orally - may have a positive effect within 24 hours of overdose.
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 are possible. 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 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 an overdose of ascorbic acid may be categorized as those caused by severe liver damage resulting from an overdose of paracetamol.
Adverse reactions
Skin and subcutaneous tissue disorders: rash, itching, urticaria, allergic dermatitis, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
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.
Gastrointestinal: nausea, vomiting, dry mouth, abdominal discomfort and pain, hypersalivation, decreased appetite, heartburn, diarrhea.
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: arterial hypertension, 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.
Reporting of suspected adverse reactions
Reporting of suspected adverse reactions occurring after the marketing authorisation of a medicinal product plays an important role. This allows for continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals should report any suspected adverse reactions via the national reporting system.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
5 g of powder in a sachet; 5 or 10 sachets in a cardboard box.
Vacation category
Without a prescription.
Producer
Nabros Pharma Pvt. Ltd., India/Nabros Pharma Pvt. Ltd., India.
Address
Survey No. 110/A/2, Amit Farm, Jain Upasrya, Near Coca Cola Factory, NH No. 8, Kajipura – 387411, Kheda, India.
Applicant
Nabros Pharma Pvt. Ltd., India/Nabros Pharma Pvt. Ltd., India.
Applicant's location
Nabros House, 3rd floor, Behind British Library, Orr. Art Galary, Law Garden, Ellisbridge, Ahmedabad – 380006, Gujarat, India.
