Instructions Antiflu powder for oral solution package No. 5
Composition
active ingredients: 1 packet contains paracetamol (acetaminophen) 650 mg, phenylephrine hydrochloride 10 mg, chlorpheniramine maleate 4 mg;
excipients: confectioner's sugar, sucrose, lemon flavoring, citric acid, colloidal anhydrous silicon dioxide, silicon dioxide, sodium citrate dihydrate, ascorbic acid, titanium dioxide (E 171), calcium phosphate, sunset yellow FCF (E 110), quinoline yellow (E 104), corn starch.
Dosage form
Powder for oral solution.
Main physicochemical properties: white or almost white powder containing crystalline particles with a slight lemon odor.
Pharmacotherapeutic group
Analgesics and antipyretics. ATX code N02B E51.
Pharmacological properties
Pharmacodynamics
Paracetamol has analgesic, antipyretic and weak anti-inflammatory effects. Its mechanism of action is to inhibit prostaglandin synthesis and affect the thermoregulation center in the hypothalamus.
Phenylephrine hydrochloride is an α-adrenomimetic that, due to its vasoconstrictor effect, reduces edema and hyperemia of the mucous membranes of the upper respiratory tract and paranasal sinuses.
Chlorpheniramine maleate is an antihistamine from the alkylamine class, a blocker of H1-histamine receptors. It has antiallergic effects, eliminates rhinorrhea, lacrimation and itching in the eyes and nose. The therapeutic effect develops within one hour after oral administration and lasts for 24 hours.
The components of the drug are metabolized independently of each other.
Pharmacokinetics
After oral administration, paracetamol is rapidly absorbed, mainly in the upper digestive tract. It is rapidly distributed in tissues. Binding to blood proteins is less than 10%. Paracetamol is metabolized mainly in the liver: most of it is bound to glucuronic acid, less to sulfuric acid. The half-life of paracetamol is 2-2.5 hours. It is prolonged in people with liver diseases.
Paracetamol is excreted in the urine (85% of a single dose of paracetamol is excreted within 24 hours). Excretion is significantly impaired in cases of impaired renal excretory function, which can lead to accumulation of paracetamol and its metabolites in the body. The half-life of chlorpheniramine maleate is 8 hours. The metabolites and the unmetabolized part of the drug are excreted in the urine.
Phenylephrine hydrochloride is partially excreted in the urine unchanged, the rest is inactivated by monoamine oxidase in the blood, liver and other tissues. Inactive products are partially excreted by the kidneys, the rest by the liver in the form of glucuronides.
Indication
Symptomatic treatment of influenza, acute respiratory viral infections and colds to reduce fever, eliminate headache, muscle and joint pain, and swelling of the respiratory tract mucosa.
Contraindication
– Increased individual sensitivity to the ingredients of the drug;
– pronounced liver and kidney dysfunction;
– congenital deficiency of glucose-6-phosphate dehydrogenase (as evidenced by hemolytic anemia);
– hematopoiesis disorders;
– blood diseases;
– severe leukopenia;
– anemia;
– severe cardiovascular diseases, including conduction disorders, severe atherosclerosis, severe ischemic heart disease;
– severe form of arterial hypertension;
– bronchial asthma;
– congenital hyperbilirubinemia;
– diabetes;
– hyperthyroidism;
- closed-angle glaucoma;
– bladder neck obstruction;
– pyloroduodenal obstruction;
– stomach ulcer in the acute stage;
– alcoholism;
– do not use together with monoamine oxidase inhibitors (MAOIs) and within 2 weeks after discontinuing the use of MAOIs.
Interaction with other medicinal products and other types of interactions
When used simultaneously with paracetamol, the following types of interactions may occur:
– the rate of absorption of paracetamol may be increased by metoclopramide and domperidone, and decreased by cholestyramine;
– the elimination of antibiotics from the body may be slowed down;
– barbiturates and ethanol can increase the hepato- and nephrotoxicity of paracetamol, barbiturates reduce the antipyretic effect;
– anticonvulsants (phenytoin, barbiturates, carbamazepine), isoniazid, rifampicin may enhance the hepatotoxic effects of paracetamol;
– tetracycline increases the risk of developing anemia and methemoglobinemia caused by paracetamol;
– the effect of indirect anticoagulants may be enhanced with an increased risk of bleeding with prolonged regular use of paracetamol;
– may reduce the effectiveness of diuretics;
– antacids and food reduce the absorption of paracetamol.
Concomitant use of Antiflu® with the following drugs may significantly increase the suppressive effect of chlorpheniramine maleate:
– sleeping pills;
– barbiturates;
– sedatives;
– neuroleptics;
– tranquilizers;
– anesthetics;
– narcotic analgesics;
– chlorpheniramine enhances the anticholinergic effect of atropine, antispasmodics, tricyclic antidepressants, and antiparkinsonian drugs.
Phenylephrine hydrochloride may cause the development of hypertensive crisis or arrhythmia when used simultaneously with other adrenomimetics or MAO inhibitors, cause severe arterial hypertension when combined with indomethacin and bromocriptine. Rauwolfia alkaloids reduce the therapeutic effect of phenylephrine hydrochloride.
Application features
Concomitant use with other drugs intended for the symptomatic treatment of colds and flu, or drugs containing paracetamol, should be avoided.
This medicine is not recommended for use concurrently with sedatives, hypnotics or beverages containing alcohol due to the increased risk of hepatotoxicity.
This medicinal product contains paracetamol, which, due to hepatotoxicity, should not be used for longer periods and in higher doses than recommended in the section "Method of administration and dosage". Long-term use may lead to serious liver complications, such as cirrhosis. Acute or chronic overdose may lead to severe liver damage and, in rare cases, to death.
Patients suffering from liver disease or liver infections, such as viral hepatitis, should consult their doctor before using this medication.
Patients with mild to moderate hepatic impairment (<9 points on the Child-Pugh scale) should use this medicine with caution.
During the use of paracetamol in therapeutic doses, an increase in alanine aminotransferase (ALT) is possible.
Patients with kidney disease should consult their doctor before starting this medication, as dose adjustment may be necessary. In case of severe renal impairment (creatinine clearance < 10 ml/min), the doctor should assess the risk/benefit ratio before starting the medication. Dose adjustment is necessary, and continuous monitoring should be ensured.
Long-term use of paracetamol, especially in combination with other analgesics, may lead to irreversible kidney damage and the risk of developing renal failure (analgesic nephropathy).
Prolonged use of high doses may lead to liver and kidney damage; multiple concomitant medications, alcoholism, alcoholic liver disease, sepsis, or diabetes mellitus may increase the risk of hepatotoxicity of paracetamol at therapeutic doses.
The risk of overdose occurs in patients with non-cirrhotic alcoholic liver disease.
Severe skin reactions have been reported very rarely. If you experience redness, rash, blistering or peeling of the skin, stop using paracetamol and seek medical attention immediately.
The use of paracetamol in patients with Gilbert's syndrome may lead to more severe hyperbilirubinemia and clinical symptoms such as jaundice. Therefore, paracetamol should be used with caution in these patients.
Before using the drug, it is necessary to consult a doctor if the patient is using warfarin or similar drugs that have an anticoagulant effect.
Paracetamol may affect the results of laboratory tests for blood glucose and uric acid.
The drug should be prescribed by a doctor only after assessing the risk/benefit ratio in the following cases:
– arterial hypertension;
– epilepsy;
– prostate adenoma;
– heart rhythm disturbances;
– urination disorders.
If, on the recommendation of a doctor, the drug is used for a long period, it is necessary to monitor the functional state of the liver and the peripheral blood picture.
It should be noted that 1 sachet (1 dose) contains 15.4 g of sugar.
Do not exceed the specified dose. Do not take the drug with other products containing paracetamol. If symptoms persist, consult a doctor. If the headache becomes persistent, consult a doctor.
The drug should be used with caution in the elderly.
Use during pregnancy or breastfeeding
It is not recommended to use the medicine during pregnancy.
Women should stop breastfeeding while taking the drug.
Fertility.
There is limited evidence of a possible impairment of female fertility due to the effect on ovulation of drugs that inhibit cyclooxygenase/prostaglandin synthesis, which is reversible and disappears after discontinuation of treatment. Since paracetamol is thought to inhibit prostaglandin synthesis, it may have a negative effect on fertility, although no such cases have been reported.
Ability to influence reaction speed when driving vehicles or other mechanisms
Due to the possibility of drowsiness, you should refrain from driving vehicles or operating machinery for 4 hours after using the drug.
Method of administration and doses
A single dose for adults and children over 12 years of age is 1 packet. If necessary, repeat every 4 hours. The maximum daily dose of 4 packets per day should not be exceeded. The maximum period of use without consulting a doctor is 3 days. Further use is possible only under the supervision of a doctor.
Children
Do not use in children under 12 years of age.
The maximum dose for children is up to 100 mg/kg per day or 4000 mg per day.
Overdose
Symptoms of overdose due to paracetamol in the first 24 hours are pallor of the skin, nausea, vomiting, anorexia and abdominal pain. When taking large doses, disorientation, psychomotor agitation or depression of the central nervous system, increased sweating, dizziness and sleep disturbances may also be observed. Cardiac arrhythmias and pancreatitis have also been observed.
In isolated cases, acute renal failure with acute tubular necrosis has been reported after paracetamol overdose, which may manifest as severe lower back pain, haematuria, proteinuria, and may develop even in the absence of severe liver damage; nephrotoxicity (renal colic, interstitial nephritis, papillary necrosis).
In severe cases, especially in the presence of alcohol, liver damage (hepatocellular necrosis) and deterioration of liver function may occur, which may progress to hepatic encephalopathy, hepatic coma, cerebral edema and fatal outcomes. Clinical signs of liver damage may not appear for 12-48 hours after overdose. Glucose metabolism disorders, hypokalemia and metabolic acidosis (including lactic acidosis), increased activity of "liver" transaminases and an increase in the prothrombin index, hemorrhage may occur. Liver damage in an adult may develop after the use of 10 g or more of paracetamol and more than 150 mg / kg of body weight in a child.
Common clinical manifestations that appear after 3-5 days include jaundice, fever, hemorrhagic diathesis, hypoglycemia, hepatic halitosis, and liver failure.
The use of 5 g or more of paracetamol can 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).
With prolonged use in high doses, aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, and thrombocytopenia are possible.
Emergency care. The patient should be taken to hospital immediately, even if there are no early symptoms of overdose. Symptoms may be limited to nausea and vomiting or may not reflect the severity of the overdose or the risk of organ damage. Treatment with activated charcoal should be considered if an overdose of paracetamol has been taken within 1 hour. The concentration of paracetamol in the blood plasma should be measured 4 hours or later after ingestion (earlier concentrations are unreliable). Gastric lavage should be performed within 6 hours of a suspected paracetamol overdose. Cytostatic effects can be reduced by administering methionine orally or by administering cysteamine or N-acetylcysteine intravenously within 8 hours of the overdose. The effectiveness of the antidote decreases sharply after this time.
Overdose due to the action of phenylephrine and chlorpheniramine maleate may cause increased sweating, psychomotor agitation or depression of the central nervous system, headache, dizziness, drowsiness, impaired consciousness, cardiac arrhythmias, tachycardia, extrasystole, tremor, hyperreflexia, convulsions, nausea, vomiting, irritability, anxiety, increased blood pressure.
In case of an overdose of chlorpheniramine maleate, atropine-like symptoms may be observed: mydriasis, photophobia, dryness of the skin and mucous membranes, increased body temperature, intestinal atony. Central nervous system depression is accompanied by respiratory disorders and disorders of the cardiovascular system (decreased pulse rate, decreased blood pressure up to vascular insufficiency).
In case of overdose, symptomatic therapy is necessary, in case of severe hypertension, the use of α-adrenergic blockers is required.
Adverse reactions
In most cases, the drug is well tolerated.
In rare cases, the following undesirable effects may occur after prolonged use in amounts exceeding the recommended daily doses:
– from the blood system: anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, dyspnea, heart pain), thrombocytosis, thrombocytopenia, agranulocytosis, hemolytic anemia, bruising or bleeding;
– from the digestive tract: heartburn, nausea, vomiting, dry mouth, discomfort and pain in the epigastrium, hypersalivation, decreased appetite, constipation, diarrhea, flatulence;
– from the hepatobiliary system: increased activity of liver enzymes, usually without the development of jaundice; hepatonecrosis (dose-dependent effect);
– from the endocrine system: hypoglycemia up to hypoglycemic coma;
– from the nervous system: headache, weakness, dizziness, psychomotor agitation and disorientation, anxiety, feelings of fear, sleep disorders, drowsiness, insomnia, dyskinesia, behavioral changes, irritability or nervousness, tremor, confusion, depressive states, tingling and heaviness in the limbs, tinnitus, epileptic seizures, coma;
– from the urinary system: renal colic and interstitial nephritis, urinary retention and difficulty urinating, aseptic pyuria;
– on the part of the organs of vision: impaired vision and accommodation, dry eyes, mydriasis;
– from the skin and subcutaneous tissues: itching, rash on the skin and mucous membranes (usually generalized rash, erythema, urticaria), allergic and angioedema, acute generalized exanthematous pustulosis, local drug dermatitis, erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), including fatal outcomes;
– from the cardiovascular system: tachycardia, reflex bradycardia, shortness of breath, heart pain, increased blood pressure, arrhythmia; with prolonged use in high doses, myocardial dystrophy is possible;
– on the part of the respiratory system: bronchospasm in patients sensitive to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 ºС.
Keep out of reach of children.
Packaging
Powder, dosed at 17 g in bags made of paper laminated with aluminum foil and polyethylene. 5 bags in a cardboard box.
Vacation category
Without a prescription.
Producer
Contract Pharmacal Corporation, USA.
Location of the manufacturer and its business address
135 Adams Avenue, Hauppauge, New York 11788, USA/135 Adams Avenue, Hauppauge, New York, 11788, USA.
Applicant
Bayer Consumer Care AG, Switzerland.
Location of the applicant and its business address
Peter Merian-Strasse 84, 4052 Basel, Switzerland.
