Pharmacodynamics. Paracetamol has analgesic, antipyretic and mild anti-inflammatory effects. the mechanism of its action is to inhibit the synthesis of prostaglandins and affect the center of thermoregulation in the hypothalamus.
Phenylephrine hydrochloride is an α-adrenergic agonist, which, due to its vasoconstrictor action, reduces edema and hyperemia of the mucous membrane of the upper respiratory tract and paranasal sinuses.
Chlorpheniramine maleate is an antihistamine of the alkylamine class, a blocker of H1-histamine receptors. It has an anti-allergic 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 preparation are metabolized independently of each other.
Pharmacokinetics. After oral administration, paracetamol is rapidly absorbed, mainly in the upper digestive tract. It is quickly distributed in tissues. The blood protein binding is less than 10%. Paracetamol is metabolized in the liver: most of it binds to glucuronic acid, less to sulfuric acid. The half-life of paracetamol is 2–2.5 hours. It increases in individuals with liver disease.
Paracetamol is excreted in the urine (85% of a single dose of paracetamol is excreted within 24 hours). Excretion significantly deteriorates in case of impaired renal excretory function, which can lead to the accumulation of paracetamol and its metabolic products in the body. T½ of chlorpheniramine maleate is 8 hours. Metabolic products and the unchanged part of the preparation are excreted in the urine.
Phenylephrine hydrochloride is partially excreted in the urine unchanged, the rest is inactivated by MAO 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.
Symptomatic treatment of influenza, colds and colds with the aim of lowering body temperature, eliminating headaches, pain in muscles and joints, edema of the mucous membrane of the respiratory tract.
Take internally. dissolve the contents of the package in a glass of hot water before use.
Single dose for adults and children from 12 years old - 1 packet. If necessary, repeat every 4 hours. The maximum daily dose - 4 packets per day - should not be exceeded. The maximum period of application without consulting a doctor is 3 days. Further use is possible only under medical supervision.
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.
Hypersensitivity to the components of the preparation; severe violations of liver and kidney function; congenital deficiency of glucose-6-phosphate dehydrogenase (as evidenced by hemolytic anemia); Gilbert's syndrome (intermittent benign jaundice resulting from glucuronyl transferase deficiency); violation of hematopoiesis; blood diseases; severe leukopenia; anemia; severe cardiac conduction disorders; decompensated heart failure; pronounced atherosclerosis of the coronary vessels of the heart; severe form of ischemic heart disease; severe form of ag; ba; emphysema; chronic obstructive pulmonary disease; congenital hyperbilirubinemia; club-johnson syndrome; diabetes; hyperthyroidism; angle-closure glaucoma; obstruction of the bladder neck; pyloroduodenal obstruction; a stomach ulcer in an exacerbation stage; alcoholism; arrhythmias; adenoma of the prostate gland with difficulty urinating; acute pancreatitis; increased excitability; sleep disturbance; pheochromocytoma; epilepsy; elderly age; patients at risk of respiratory failure.
Do not use simultaneously with MAO inhibitors and within 2 weeks after discontinuation of MAO inhibitors; with tricyclic antidepressants, β-adrenergic receptor blockers.
In most cases, the preparation is well tolerated.
In rare cases, the following side effects may occur after prolonged use in quantities exceeding the recommended daily dose:
from the blood system: anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), thrombocytosis, thrombocytopenia, leukopenia, agranulocytosis, hemolytic anemia, bruising or bleeding;
from the digestive tract: heartburn, nausea, vomiting, dry mouth, epigastric discomfort and pain, hypersalivation, loss of appetite, constipation, diarrhea, flatulence;
from the hepatobiliary system: impaired liver function, increased activity of hepatic enzymes, usually without the development of jaundice; hepatonecrosis (dose-dependent effect);
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, fear, sleep disorders, drowsiness, insomnia, dyskinesia, change in behavior, irritability or nervousness, tremor, confusion, depression, tingling sensation, 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 organ of vision: visual impairment 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 preparation dermatitis, erythema multiforme (including) Stevens-Jones syndrome , toxic epidermal necrolysis (Lyell's syndrome), including death;
on the part of 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;
from the respiratory system: bronchospasm in patients sensitive to acetylsalicylic acid and other NSAIDs.
Special instructions
Simultaneous use with other preparations intended for the symptomatic treatment of colds and flu, preparations containing paracetamol should be avoided.
This medicinal product is not recommended for concomitant use with sedatives, hypnotics, or medicinal products containing alcohol due to the increased risk of hepatotoxicity.
The medicinal product contains paracetamol, which, due to hepatotoxicity, cannot be used longer and in doses higher than those recommended in the APPLICATION section. Long-term use can lead to severe liver complications such as cirrhosis. Acute or chronic overdose can lead to severe liver damage and, in rare cases, death.
Long-term use of paracetamol, especially in combination with other analgesics, can lead to irreversible kidney damage and the risk of developing renal failure (analgesic nephropathy).
Long-term use of paracetamol in high doses can lead to liver and kidney damage. A large number of medications used at the same time, alcoholism, alcoholic liver damage, sepsis or diabetes mellitus may increase the risk of hepatotoxicity of paracetamol in therapeutic doses. The danger of overdose arises in patients with non-cirrhotic alcoholic liver disease.
If, on the recommendation of a doctor, the preparation is used for a long period, it is necessary to monitor the functional state of the liver and the picture of peripheral blood.
In patients with severe infections, such as sepsis, accompanied by a decrease in glutathione levels, taking paracetamol may increase the risk of metabolic acidosis (see OVERDOSE).
Before using the preparation, you need to consult a doctor:
if the patient is using warfarin or similar preparations that have an anticoagulant effect;
if the patient has breathing problems, chronic lung disease, emphysema, or chronic bronchitis;
a patient with liver disease or liver infections such as viral hepatitis;
a patient with kidney disease, as dose adjustment may be required.
In the case of renal impairment, the physician should assess the risk / benefit ratio before starting the use of the preparation. Dose adjustment is necessary, continuous monitoring should be ensured:
with hypertension;
with daily use of analgesics for mild arthritis.
Use with caution in patients with:
the presence of chronic malnutrition and dehydration;
mild to moderate hepatic impairment (9 points on the Child-Pugh scale);
Raynaud's disease;
diseases of the thyroid gland, except for hyperthyroidism, which is indicated in the section CONTRAINDICATIONS;
glaucoma, except for angle-closure glaucoma, which is indicated in the CONTRAINDICATIONS section.
You should consult a doctor:
if symptoms persist and / or are accompanied by a high body temperature that lasts more than 3 days;
if the headache becomes persistent.
Cases of severe skin reactions have been reported very rarely. If skin redness, rash, blistering or peeling occurs, stop using paracetamol and seek immediate medical attention.
With the appointment of paracetamol in therapeutic doses, an increase in ALT is possible.
Paracetamol may interfere with laboratory test results for blood glucose and uric acid.
Do not exceed the indicated dose.
The excipient Sun Sunset Yellow Dye may cause allergic reactions.
Sugar and sucrose warning: If a patient has an intolerance to some sugars, consult a doctor before taking this medication; the preparation may be harmful to the teeth.
Use during pregnancy and lactation. It is not recommended to use the preparation during pregnancy. Women should stop breastfeeding while taking the preparation.
Fertility There are limited data on the possibility of impaired fertility in women due to the effect on ovulation of preparations that inhibit the synthesis of COX / prostaglandin, which is reversible and disappears after discontinuation of treatment. Since paracetamol is thought to inhibit prostaglandin synthesis, it can negatively affect fertility, although this is not the case.
The ability to influence the reaction rate when driving or working with other mechanisms.
Due to the possibility of drowsiness, one should refrain from driving vehicles, working with mechanisms for 4 hours after using the preparation.
Interactions
When used simultaneously with paracetamol, the following types of interactions may occur:
the rate of absorption of paracetamol may increase with simultaneous use with metoclopramide and domperidone, decrease with cholestyramine;
the elimination of antibiotics from the body may slow down;
barbiturates and alcohol can increase the hepato- and nephrotoxicity of acetaminophen, barbiturates reduce the antipyretic effect;
anticonvulsants (phenytoin, barbiturates, carbamazepine), isoniazid and rifampicin can increase the hepatotoxic effect of paracetamol;
tetracycline increases the risk of anemia and methemoglobinemia caused by paracetamol;
the effect of indirect anticoagulants may increase with an increased risk of bleeding with prolonged regular use of paracetamol;
may decrease the effectiveness of diuretics;
antacids and food decrease the absorption of paracetamol.
With the simultaneous use of paracetamol with hepatotoxic agents, the toxic effect of preparations on the liver increases.
The preparation is not recommended to be used simultaneously with sedatives, hypnotics or preparations containing alcohol, due to the increased risk of hepatotoxicity.
It is not recommended to use it simultaneously with vasoconstrictor agents.
The simultaneous use of Antiflu® with the following preparations can significantly increase the inhibitory effect of chlorpheniramine maleate:
- hypnotics;
- barbiturates;
- sedatives;
- antipsychotics;
- tranquilizers;
- anesthetics;
- narcotic analgesics;
- ethanol-containing agents.
Chlorpheniramine enhances the anticholinergic effect of atropine, antispasmodics, tricyclic antidepressants, antiparkinsonian preparations.
Chlorphenamine can inhibit the effect of anticoagulants.
Phenylephrine hydrochloride can cause the development of hypertensive crisis or arrhythmias when used simultaneously with other adrenomimetics or MAO inhibitors, cause severe hypertension when combined with indomethacin and bromocriptine.
The simultaneous use of phenylephrine with other sympathomimetic agents or tricyclic antidepressants (eg amitriptyline) may increase the risk of developing side effects from the cardiovascular system. Rauwolfia alkaloids reduce the therapeutic effect of phenylephrine hydrochloride.
Phenylephrine may reduce the effectiveness of β-adrenergic receptor blockers and other antihypertensive preparations (eg, debrisoquine, guanethidine, reserpine, methyldopa). There may be an increased risk of hypertension and other cardiovascular side effects.
The simultaneous use of phenylephrine with digoxin and cardiac glycosides may increase the risk of heartbeat disorders or heart attack.
Antidepressants, antiparkinsonian and antipsychotic preparations, phenothiazine derivatives increase the risk of urinary retention, dry mouth, and constipation.
Concomitant use with ergot alkaloids (ergotamine, methysergide) increases the risk of ergotism.
Overdose
Overdose symptoms due to the action of paracetamol in the first 24 hours are pallor of the skin, nausea, vomiting, anorexia and abdominal pain. when taken in high doses, disorientation, psychomotor agitation or depression of the central nervous system, increased sweating, dizziness and sleep disturbance may also occur. cardiac arrhythmias and pancreatitis were also noted.
In rare cases, after an overdose of paracetamol, ARF with acute tubular necrosis has been reported, which can manifest itself as severe pain in the lumbar region, hematuria, proteinuria and 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 can occur, which can progress to hepatic encephalopathy, hepatic coma, cerebral edema and death. Clinical signs of liver damage may not appear for 12–48 hours after an overdose. Disorders of glucose metabolism, hypokalemia and metabolic acidosis (including lactic acidosis), increased activity of hepatic transaminases and an increase in the prothrombin index, hemorrhages may occur. Liver damage in an adult can develop after the use of 10 g or more of paracetamol and more than 150 mg / kg of body weight in a child.
Jaundice, fever, hemorrhagic diathesis, hypoglycemia, hepatic breath odor, liver failure belong to the frequent clinical manifestations that occur after 3-5 days.
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. , cystic fibrosis, HIV infection, starvation, cachexia)).
With prolonged use in high doses, aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, thrombocytopenia are possible.
Urgent care. The patient should be taken to the clinic 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 excessive dose of paracetamol has been taken within 1 hour. The plasma concentration of paracetamol should be measured 4 hours or later after ingestion (earlier concentrations are unreliable). Gastric lavage should be performed within 6 hours after a suspected paracetamol overdose. Cytostatic effects can be reduced by oral administration of methionine or administration of cysteamine or N-acetylcysteine within 8 hours after overdose. The effectiveness of the antidote decreases sharply after this time.
Overdose due to the action of phenylephrine and chlorpheniramine maleate can cause increased sweating, psychomotor agitation or depression of the central nervous system, headache, dizziness, drowsiness, impaired consciousness, heart rhythm disturbances, tachycardia, extrasystole, tremor, hyperreflexia, convulsions, vomiting, nausea anxiety, increased blood pressure.
In case of an overdose of chlorpheniramine maleate, atropine-like symptoms may occur: mydriasis, photophobia, dry skin and mucous membranes, fever, intestinal atony. Inhibition of the central nervous system is accompanied by impaired respiration and the function of the cardiovascular system (decrease in heart rate, decrease in blood pressure to vascular insufficiency).
In case of overdose, symptomatic therapy is necessary, in severe hypertension, the use of α-adrenergic receptor blockers.
Storage conditions
At a temperature not higher than 25 ° C.