Instructions Antiflu film-coated tablets blister No. 12
Composition
active ingredients: acetaminophen, phenylephrine hydrochloride, chlorpheniramine maleate;
1 tablet contains 325 mg of acetaminophen, 5 mg of phenylephrine hydrochloride, and 2 mg of chlorpheniramine maleate;
excipients: microcrystalline cellulose, croscarmellose sodium, colloidal anhydrous silicon dioxide, stearic acid, magnesium silicate, magnesium stearate, hypromellose, polyethylene glycol, mineral oil, D&C yellow № 10 lake dye (E 104).
Dosage form
Film-coated tablets
Main physicochemical properties: capsule-shaped tablet, yellow in color, with a transparent film coating and engraved with the designation "AntiFlu" on one side.
Pharmacotherapeutic group
Analgesics and antipyretics.
ATX code N02B E51.
Pharmacological properties
Pharmacodynamics.
Acetaminophen (paracetamol) has analgesic, antipyretic, and weak anti-inflammatory effects. Its mechanism of action is to inhibit prostaglandin synthesis and affect the thermoregulatory 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-histaminergic receptors. It has an antiallergic effect, eliminates rhinorrhea, lacrimation and itching in the eyes and nose. The therapeutic effect develops within 1 hour after oral administration and lasts for 24 hours.
The components of the drug are metabolized independently of each other.
Pharmacokinetics.
After oral administration, acetaminophen is rapidly absorbed, mainly in the upper gastrointestinal tract. It is rapidly distributed in tissues. Binding to blood proteins is less than 10%. Acetaminophen is metabolized primarily in the liver: most of it is conjugated with glucuronic acid, and less with sulfuric acid. The half-life of acetaminophen is 2–2.5 hours. It is prolonged in individuals with liver disease.
Acetaminophen is excreted in the urine (85% of a single dose of acetaminophen is excreted within 24 hours). Excretion is significantly impaired in renal excretory function disorders, which can lead to accumulation of acetaminophen and its metabolites in the body. The half-life of chlorpheniramine maleate is 8 hours. Metabolism products and the unmetabolized portion 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 - through 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 active or auxiliary substances of the drug; severe liver dysfunction (more than 9 points on the Child-Pugh scale) and kidneys; congenital deficiency of glucose-6-phosphate dehydrogenase (as evidenced by hemolytic anemia); Gilbert's syndrome (intermittent benign jaundice resulting from glucuronyltransferase deficiency); hematopoietic disorders; blood diseases; severe leukopenia; anemia; severe cardiac conduction disorders; decompensated heart failure; severe atherosclerosis of the coronary vessels of the heart; severe ischemic heart disease; severe arterial hypertension; bronchial asthma; congenital hyperbilirubinemia; Dubin-Johnson syndrome; diabetes mellitus; hyperthyroidism; angle-closure glaucoma; bladder neck obstruction; pyloroduodenal obstruction; peptic ulcer disease in the acute stage; alcoholism; arrhythmias; Prostate adenoma with difficulty urinating; acute pancreatitis; increased excitability; sleep disorders; pheochromocytoma; epilepsy. Elderly age. Risk of respiratory failure.
Do not use with monoamine oxidase inhibitors (MAOIs) and within 2 weeks after discontinuing MAOIs; with tricyclic antidepressants, ß-blockers.
Interaction with other medicinal products and other types of interactions
When used simultaneously with acetaminophen, the following types of interactions may occur:
- the rate of absorption of acetaminophen may increase when used simultaneously with antiemetics (metoclopramide and domperidone), and decrease with cholestyramine;
- the elimination of antibiotics from the body may be slowed down;
- barbiturates and alcohol can increase the hepato- and nephrotoxicity of acetaminophen, barbiturates reduce the antipyretic effect;
- simultaneous use of high doses of paracetamol with isoniazid may increase the risk of hepatotoxicity;
- tetracycline increases the risk of developing anemia and methemoglobinemia caused by acetaminophen;
- the effect of indirect anticoagulants may be enhanced with an increased risk of bleeding with long-term regular use of acetaminophen; simultaneous long-term use of coumarin derivatives may enhance their effect and increase the risk of bleeding, blood clotting monitoring is recommended;
- tropisetron and granisetron, type 3 5-hydroxytryptamine antagonists, can completely inhibit the analgesic effect of paracetamol due to pharmacodynamic interaction;
- simultaneous use of paracetamol and AZT (zidovudine) increases the tendency to decrease the number of white blood cells (neutropenia); therefore, AZT and paracetamol should not be used simultaneously, use is possible only on the recommendation of a doctor;
- may reduce the effectiveness of diuretics;
̶ Antacids and food reduce the absorption of acetaminophen.
With the simultaneous use of paracetamol with hepatotoxic drugs, the toxic effect of the drugs on the liver increases.
The drug is not recommended for use simultaneously with sedatives, hypnotics, or drugs containing alcohol due to the increased risk of hepatotoxicity.
It is not recommended to use simultaneously with vasoconstrictors.
Concomitant use of Antiflu® with the following drugs may significantly increase the suppressive effect of chlorpheniramine maleate:
- sleeping pills;
̶ barbiturates;
- sedatives;
- neuroleptics;
̶ tranquilizers or alcohol;
- anesthetics;
̶ narcotic analgesics.
Chlorpheniramine maleate may cause drowsiness. This effect may be increased when used concomitantly with sedatives, tranquilizers, or alcohol.
Chlorpheniramine enhances the anticholinergic effect of atropine, antispasmodics, tricyclic antidepressants, and antiparkinsonian drugs.
Chlorpheniramine maleate may inhibit the action of anticoagulants.
Chlorpheniramine may increase chloroquine levels when used concomitantly. The clinical consequences of this interaction are unknown.
Phenylephrine hydrochloride may cause the development of hypertensive crisis or arrhythmia when used simultaneously with other adrenomimetics or MAO inhibitors, and cause severe arterial hypertension when combined with indomethacin and bromocriptine.
Concomitant use of phenylephrine with other sympathomimetic agents or tricyclic antidepressants (e.g. amitriptyline) may increase the risk of cardiovascular side effects. Rauwolfia alkaloids reduce the therapeutic effect of phenylephrine hydrochloride.
Phenylephrine may reduce the effectiveness of ß-blockers and other antihypertensive drugs (e.g. debrisoquine, guanethidine, reserpine, methyldopa). The risk of developing arterial hypertension and other side effects from the cardiovascular system may increase.
Concomitant use of phenylephrine with digoxin and cardiac glycosides may increase the risk of heart rhythm disturbances or heart attack.
Antidepressants, antiparkinsonian and antipsychotic drugs, and phenothiazine derivatives increase the risk of urinary retention, dry mouth, and constipation.
Concomitant use with ergot alkaloids (ergotamine, methysergide) increases the risk of ergotism.
Caution should be exercised when using paracetamol concomitantly with flucloxacillin, as concomitant administration has been associated with high anion gap metabolic acidosis, especially in patients with risk factors (see section 4.4).
Application features
Concomitant use with other drugs intended for the symptomatic treatment of colds and flu, drugs containing paracetamol, antihistamines or oral decongestants should be avoided.
This medicine is not recommended for use concurrently with sedatives, hypnotics or medicines containing alcohol due to the increased risk of hepatotoxicity.
The medicine 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 can lead to serious liver complications, such as cirrhosis. Acute or chronic overdose can lead to severe liver damage and in rare cases - to death.
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 paracetamol in high doses can lead to liver and kidney damage. A large number of concomitant medications, alcoholism, alcoholic liver disease, sepsis or diabetes mellitus can increase the risk of hepatotoxicity of paracetamol at therapeutic doses. The risk of overdose occurs in patients with non-cirrhotic alcoholic liver disease.
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.
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 (see "Overdose").
Caution is advised when prescribing paracetamol concomitantly with flucloxacillin due to the increased risk of high anion gap metabolic acidosis (HAGMA), particularly in patients with severe renal insufficiency, sepsis, malnutrition and other sources of glutathione deficiency (e.g. chronic alcoholism), and those taking maximum daily doses of paracetamol. Close monitoring, including measurement of urinary 5-oxoproline, is recommended.
Before using the drug, you should consult a doctor:
- if the patient is taking warfarin or similar drugs that have an anticoagulant effect;
- if the patient has breathing problems, chronic lung disease, emphysema or chronic bronchitis;
- if the patient suffers from liver disease or infectious liver lesions, such as viral hepatitis;
- if the patient suffers from kidney disease, as a dose adjustment may be necessary. In case of severe renal insufficiency (creatinine clearance < 10 ml/min), the doctor should assess the risk/benefit ratio before starting the drug. Dose adjustment is necessary, and the patient's condition should be constantly monitored;
- with arterial hypertension, cardiovascular diseases;
- with daily use of analgesics for mild arthritis.
Use with caution in patients:
- with the presence of chronic malnutrition and dehydration;
- with mild to moderate hepatic insufficiency (< 9 points on the Child-Pugh scale);
- with Raynaud's disease;
- with thyroid diseases;
- with glaucoma.
You should consult a doctor:
- if symptoms persist and/or are accompanied by a high fever that lasts more than 3 days;
- if the headache becomes constant.
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.
During the use of paracetamol in therapeutic doses, an increase in ALT is possible.
Paracetamol may affect the results of laboratory tests for blood glucose and uric acid.
Do not exceed the indicated dose and adhere to the recommended duration of treatment.
Antiflu® may cause nervousness, dizziness or insomnia. In such cases, it is recommended to discontinue use of the drug.
It should be used with caution when administered concomitantly with sedatives or tranquilizers.
Use during pregnancy or breastfeeding
It is not recommended to use the drug during pregnancy and breastfeeding, as there is no information for this combination of active ingredients.
Fertility.
There is limited evidence of a potential impairment of fertility in women, as drugs that inhibit cyclooxygenase/prostaglandin synthesis affect ovulation. This effect 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 or operating other machinery for 3–6 hours after using the drug.
Method of administration and doses
Adults and children over 12 years of age: 2 tablets as a single dose every 4 hours. Take with water. The maximum daily dose of 12 tablets 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/day or 4000 mg/day.
Overdose
Symptoms of an overdose of Antiflu® consist of signs of an overdose of individual components of the drug.
In case of an overdose of paracetamol, you should immediately contact a doctor or poison control center. Prompt medical attention is critical for both adults and children, even if there are no visible symptoms of overdose.
In isolated cases, acute renal failure with acute tubular necrosis, which may present with severe lower back pain, hematuria, proteinuria, and may occur even in the absence of severe liver damage, has been reported following acetaminophen overdose; nephrotoxicity (renal colic, interstitial nephritis, papillary necrosis).
The overdose threshold may be lowered in individuals with significantly reduced body weight.
The most important effect in acute paracetamol poisoning is hepatotoxicity. Hepatocellular damage is caused by the binding of reactive metabolites of paracetamol to proteins of liver cells. At therapeutic doses, these metabolites bind to glutathione and form non-toxic conjugates. In massive overdose, the liver's supply of SH-groups, which contribute to the formation of glutathione, is depleted, toxic metabolites accumulate and liver cell necrosis occurs.
In severe cases, especially with simultaneous alcohol consumption, liver damage (hepatocellular necrosis) and deterioration of its function to the onset of liver failure are possible, which can progress to hepatic encephalopathy, hepatic coma, cerebral edema and be fatal. Clinical signs of liver damage may not appear for 12–48 hours after overdose. In acute and chronic poisoning, glucose metabolism disorders may occur, hypokalemia and metabolic acidosis (including lactic acidosis) may develop. Symptoms of metabolic acidosis are deep, rapid or difficult breathing, nausea, vomiting, loss of appetite. You should immediately consult a doctor if these symptoms appear. Increased activity of "liver" transaminases, bilirubin and an increase in the prothrombin index, hemorrhages, decreased urine output, mild azotemia may also be observed. Liver damage in adults can develop after taking 10 g or more of paracetamol, and in children after using more than 150 mg/kg of body weight. 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, liver dysfunction, aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, thrombocytopenia are possible.
Emergency care. The patient should be transferred immediately to the intensive care unit, even if there are no early symptoms of overdose, and vital signs, laboratory data and cardiovascular status should be monitored. 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. Hemodialysis and hemoperfusion help to remove the active substance. 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 acetaminophen overdose. Cytostatic effects can be reduced by administering methionine SH-group donors orally or by intravenous administration of cysteamine or N-acetylcysteine within 48 hours of 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, irritability, restlessness, headache, dizziness, drowsiness, insomnia, nausea, vomiting, tremor, impaired consciousness, cardiac arrhythmias, tachycardia, extrasystole, hyperreflexia, increased blood pressure, convulsions, coma. In severe poisoning with phenylephrine hydrochloride, cyanosis, cardiac arrhythmias, myocardial ischemia or myocardial infarction, pulmonary edema, hypotension, convulsions, stroke, acidosis are possible.
In case of an overdose of chlorpheniramine maleate, atropine-like (antimuscarinic), gastrointestinal symptoms and changes in the CNS may be observed. In case of mild and moderate overdose, nausea, vomiting, drowsiness, depression of consciousness, hallucinations, facial flushing, mydriasis, photophobia, dry skin and mucous membranes, increased body temperature, intestinal atony, tachycardia and a moderate increase in blood pressure are observed. In case of severe intoxication, delirium, psychosis, dyskinesia, convulsions are observed. CNS depression is accompanied by respiratory disorders and disorders of the cardiovascular system (decreased pulse rate, widened QRS complex and ventricular arrhythmias, including torsade de pointe, decreased blood pressure up to vascular insufficiency).
In children, CNS stimulation is first observed, followed by depression. Symptoms include ataxia, agitation, tremor, psychosis, hallucinations, and convulsions. Hyperpyrexia may also be observed. Deterioration may lead to deep coma, cardiovascular collapse, and death.
In case of overdose, symptomatic and supportive therapy is necessary, including artificial ventilation of the lungs, and in case of severe arterial hypertension, the use of α-blockers.
Side effects
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 and lymphatic system - anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, dyspnea, pain in the heart area), hemolytic anemia (if the patient has glucose-6-phosphate dehydrogenase deficiency), thrombocytopenia, agranulocytosis, thrombocytopenic purpura, leukopenia, bruising or bleeding;
from the gastrointestinal tract - heartburn, nausea, vomiting, dry mouth, discomfort and pain in the epigastrium, hypersalivation, decreased appetite, dyspepsia, constipation, diarrhea, flatulence;
from the hepatobiliary system - impaired liver function, hepatitis, dose-dependent liver failure, increased activity of liver enzymes, usually without the development of jaundice, hepatonecrosis (including fatal); prolonged use without a doctor's recommendation can lead to fibrosis, cirrhosis of the liver, which can be fatal;
from the endocrine system – hypoglycemia up to hypoglycemic coma;
from the immune system - hypersensitivity reactions (including allergic reactions), anaphylactic reactions and anaphylactic shock;
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, hallucinations, epileptic seizures, coma;
from the kidneys and urinary tract - renal colic and interstitial nephritis, urinary retention and difficulty urinating, aseptic pyuria, dysuria;
on the part of the organs of vision – impaired vision and accommodation, dry eyes, mydriasis, increased intraocular pressure;
Skin and subcutaneous tissue disorders: 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), which can be fatal;
from the cardiovascular system - tachycardia, reflex bradycardia, shortness of breath, heart pain, increased blood pressure, arrhythmia, myocardial dystrophy (dose-dependent effect with prolonged use), pain or discomfort in the precardial area;
on the part of the respiratory system - bronchospasm in patients with hypersensitivity to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs.
Expiration date
3 years.
Storage conditions
Store in original packaging at a temperature not exceeding 25 ºС.
Keep out of reach of children.
Packaging
12 tablets in a blister. 1 blister in a cardboard box.
Vacation category
Without a prescription.
Producer
Contract Pharmacal Corporation/Contract Pharmacal Corporation.
Location of the manufacturer and its business address
135 Adams Avenue, Hauppauge, New York 11788, USA/135 Adams Avenue, Hauppauge, New York, 11788, USA.
