Paracytolgin, 400 mg+325 mg 10 pcs

Pharmacotherapeutic group Anallergic agent, combined (NSAID + non-narcotic analgesic).

ATX code: M01AE51

Pharmacological properties

Pharmacodynamics.

A combination drug, the action of which is due to its constituent components. It has a directed effect against pain (analgesic), antipyretic and anti-inflammatory effects.

Ibuprofen and paracetamol differ in mechanism and site of action. Their mutually reinforcing action results in a more pronounced decrease in pain sensitivity and an increase in antipyretic effect than separately.

Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory, antipyretic effects. Inhibiting cyclooxygenase (COX) 1 and 2, disrupts metabolism of arachidonic acid, reduces the number of prostaglandins (mediators of pain, inflammation and hyperthermia), both in the focus of inflammation and in healthy tissues, inhibits the exudative and proliferative phases of inflammation. Ibuprofen inhibits the migration of leukocytes to the center of inflammation.

The analgesic effect of ibuprofen is provided by its inhibitory action at the peripheral level. Antipyretic effect of ibuprofen is associated with central inhibition of prostaglandin synthesis in hypothalamus.

Paracetamol is an analgesic non-narcotic agent and has analgesic, antipyretic and mild anti-inflammatory effects. Paracetamol indiscriminately blocks COX, mainly in the central nervous system, has little effect on water-salt metabolism and the mucosa of the gastrointestinal tract (GIT). It has analgesic and antipyretic effects. Paracetamol can also stimulate the activity of descending serotonin pathways, which leads to knocking out the transmission of the pain impulse in the spinal cord. At the peripheral level, paracetamol has a weak effect on COX-1 and COX-2.

It relieves arthralgia at rest and on movement, reduces morning stiffness and joint swelling, and promotes increased range of motion.

Pharmacokinetics

Ibuprofen<

Absorption is high, rapidly and almost completely absorbed from the gastrointestinal tract. Detected in blood plasma 5 minutes after the drug is taken on an empty stomach, time to reach maximum concentration (T_Cmah) after oral administration – about 1-2 hours. Binding to plasma proteins is more than 90%. The elimination half-life (T_1/2) is about 2 hours. Slowly penetrates into the joint cavity, accumulates in synovial fluid, creating higher concentrations in it than in blood plasma. After absorption, about 60% of the pharmacologically inactive R-form is slowly transformed into the active S-form. It is metabolized in the liver. More than 90% is excreted by the kidneys (not more than 1% unchanged) and to a lesser extent in the bile as metabolites and their conjugates.

Paracetamol

Absorption is high, quickly absorbed from the gastrointestinal tract. Binding to plasma proteins is less than 10% and increases slightly in overdose. Sulfate and glucuronide metabolites do not bind to plasma proteins even in relatively high concentrations. Cmax value is 5-20 µg/ml, Tcmax is 0.5-2 hours.

It is quite evenly distributed in the fluid medium of the body. It penetrates through the blood-brain barrier.

It is detected in plasma 5 minutes after the drug intake on an empty stomach, C_max in plasma is reached 30-40 minutes after intake. The degree of absorption of paracetamol is independent of food intake. About 90-95% of paracetamol is metabolized in the liver to form inactive conjugates with glucuronic acid (60%), taurine (35%) and cysteine (3%), and a small amount of hydroxylated and deacetylated metabolites. A small part of the drug is hydroxylated by microsomal enzymes to form highly active N-acetyl-n-benzoquinonimine, which binds to sulfhydryl groups of glutathione. When glutathione stores in the liver are depleted (in overdose) the enzyme systems of hepatocytes can be blocked, leading to the development of their necrosis.

The elimination half-life (T_1/2) is 2-3 hours. In patients with cirrhosis the T_1/2 increases slightly. The drug clearance is decreased and the elimination half-life is increased in elderly patients. It is excreted by the kidneys mainly as glucuronide and sulfate conjugates (less than 5% unchanged). Less than 1% of the administered dose of paracetamol penetrates into breast milk. In children the ability to form conjugates with glucuronic acid is lower than in adults.

Indications

– headache (including migraine);

– toothache;

– back pain;

p> – myalgia;

– algodysmenorrhea (painful menstruation);

– neuralgia;

– joint pain, pain syndrome in inflammatory and degenerative diseases of the joints and spine;

– pain from contusions, sprains, dislocations, fractures;

– post-traumatic and postoperative pain syndrome.

– febrile states (including influenza and colds), accompanied by fever, chills, headache, pain in muscles and joints, sore throat.

The drug is intended for symptomatic therapy, reduction of pain and inflammation at the time of use. The drug has no effect on the progression of the disease.

Active ingredient

Composition

How to take, the dosage

Inhaled (before or 2-3 hours after a meal), without chewing, with plenty of water. 1 tablet 3 times a day. Maximum daily dose is 3 tablets.

The treatment duration should not exceed 3 days as an antipyretic and not more than 5 days as an analgesic. It is possible to continue treatment with the drug only after consultation with a doctor.

If there is no improvement after treatment, or if symptoms get worse or new symptoms develop, you should consult a doctor. Use the drug only according to the indication, route of administration, and dosage listed in the directions.

Interaction

In concomitant use of the drug Paracytolgin with drugs, various interaction effects may occur:

If you are using the drugs listed above or other drugs (including over-the-counter drugs), consult your physician before using Paracytolgin.

Special Instructions

It is recommended that the drug be taken in the shortest possible course and at the lowest effective dose necessary to relieve symptoms.

In patients with bronchial asthma or allergic diseases in the acute stage, as well as in patients with a history of bronchial asthma/allergic disease, the drug may provoke bronchospasm.

The use of the drug in patients with systemic lupus erythematosus or mixed connective tissue disease is associated with an increased risk of aseptic meningitis.

Patients with hypertension, including a history of and/or chronic heart failure should consult a physician before using the drug, since the drug may cause fluid retention, increased blood pressure and edema. In patients with uncontrolled arterial hypertension, NYHA class II-III congestive heart failure, coronary heart disease, peripheral artery disease and/or cerebrovascular disease, ibuprofen should only be prescribed after careful assessment of the benefit-risk ratio, and high doses of ibuprofen (≥2400 mg/day) should be avoided.

The use of NSAIDs in patients with chickenpox may be associated with an increased risk of severe suppurative complications of infectious and inflammatory skin and subcutaneous fat diseases (e.g., necrotizing fasciitis). In this regard, it is recommended to avoid using the drug in case of chicken pox.

Information for women planning pregnancy: the drug inhibits COX and prostaglandin synthesis, affects ovulation, disrupting female reproductive function (reversible after discontinuation of the drug).

The concomitant use of the drug with other drugs containing paracetamol and/or nonsteroidal anti-inflammatory drugs should be avoided. When using the drug for more than 5-7 days, peripheral blood parameters and functional state of the liver should be monitored by the doctor’s prescription.

In concomitant use of indirect anticoagulants it is necessary to monitor the parameters of the blood coagulation system.

To avoid possible damaging effect on the liver, alcohol should not be consumed while taking the drug.

The drug may interfere with the results of laboratory tests when quantitative determination of glucose, uric acid in the blood serum, 17-ketosteroids (the drug should be changed 48 hours before the study).

At the time of treatment, the patient must refrain from potentially dangerous activities requiring increased attention and rapid psychomotor reactions.

Synopsis

Contraindications

Hypersensitivity to the components of the drug (including other NSAIDs).

Errotic and ulcerative diseases of the gastrointestinal tract (including gastric and duodenal ulcer, Crohn’s disease, ulcerative colitis) or ulcer bleeding in the active phase or in the history (two or more confirmed episodes of peptic ulcer disease or ulcer bleeding).

Cerebrovascular or other bleeding.

Hemophilia or other blood clotting disorders (including hypocoagulation), hemorrhagic diathesis, intracranial hemorrhage.

Severe renal failure (creatinine clearance (CK) less than 30 ml/min).

The complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and sinuses, and intolerance of acetylsalicylic acid or other NSAIDs (including a history).

Severe heart failure (NYHA class IV).

Decompensated heart failure.

Optic nerve damage.

Genetic absence of glucose-6-phosphate dehydrogenase.

Diseases of the blood system.

The period after aortocoronary bypass surgery.

Progressive kidney disease.

Severe liver failure or active liver disease.

Confirmed hyperkalemia.

Pregnancy (3rd trimester).

Children under 18 years of age.

Ischemic heart disease, chronic heart failure, peripheral artery disease, arterial hypertension, blood diseases of unclear etiology (leukopenia and anemia), cerebrovascular disease, dyslipidemia/hyperlipidemia.

He has a history of a single episode of gastric and duodenal ulcer disease or GI ulcer bleeding, history of Helicobacter pylori infection, gastritis, enteritis, colitis, ulcerative colitis.

Viral hepatitis, mild to moderate hepatic insufficiency, benign hyperbilirubinemia (Gilbert, Dubin-Johnson, and Rotor syndrome), cirrhosis with portal hypertension.

Kidney failure, including in dehydration (CK less than 30-60 ml/min), nephrotic syndrome.

Bronchial asthma or allergic diseases in the acute stage or in the history of bronchospasm may develop.

Systemic lupus erythematosus or mixed connective tissue disease (Sharp syndrome) – increased risk of aseptic meningitis.

Chicken pox, severe somatic diseases, diabetes mellitus.

. Concomitant use of other NSAIDs, oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).

Elderly age, smoking, alcoholism.

Pregnancy I-II trimester, period of breastfeeding.

Side effects

The following classification is used to determine the frequency of side effects of the drug: very frequently (≥1/10), frequently (≥1/100 and <1/10), infrequently (≥1/1000 and <1/100), rarely (≥1/10 000 and <1/1000), very rarely (≥1/10 000).

Gastrointestinal disorders

NSAID gastropathy – nausea, vomiting, heartburn, anorexia, epigastric discomfort or pain, diarrhea, flatulence; rare – erosive ulcerative lesions, bleeding; liver dysfunction, hepatitis, pancreatitis: irritation or dryness in the mouth, pain in the mouth, ulceration of the mucous membrane of the gums, aphthous stomatitis; constipation. Peptic ulcer, melena, bloody vomiting, in some cases with fatal outcome, especially in elderly patients, gastritis, exacerbation of colitis and Crohn’s disease, increased activity of “liver” transaminases, jaundice.

Nervous system and sensory disorders

Headache, dizziness, insomnia, anxiety, nervousness, irritability, agitation, drowsiness, depression, confusion, hallucinations; rarely – aseptic meningitis (more common in patients with autoimmune diseases); decreased hearing, tinnitus, visual impairment, toxic optic nerve damage, blurred vision or double vision, scotoma, amblyopia.

Cardiovascular disorders

Heart failure, peripheral edema, with prolonged use there is an increased risk of thrombotic complications (e.g., myocardial infarction), increased blood pressure, tachycardia.

Disorders of the blood and lymphatic system

Anemia (including hemolytic and aplastic), thrombocytopenia, thrombocytopenic purpura, agranulocytosis, leukopenia, pancytopenia.

Respiratory and mediastinal disorders

Dyspnea, bronchospasm, bronchial asthma.

River and urinary tract disorders

Allergic nephritis, acute renal failure, nephrotic syndrome, edema, polyuria, cystitis, hematuria, proteinuria, nephritic syndrome, papillary necrosis, interstitial nephritis.

Allergic reactions

. Skin rash, skin itching, urticaria, Quincke’s edema, bronchospasm, dyspnea, allergic rhinitis, dry and irritated eyes, conjunctival and eyelid edema, eosinophilia, fever, anaphylactic shock, erythema multiforme exudative (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome).

Laboratory indices

Decreased serum glucose concentration, decreased hematocrit and hemoglobin, increased bleeding time, increased serum creatinine concentration.

Others

Enhanced sweating.

In prolonged use in high doses: gastrointestinal mucosal ulceration, bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), visual disorders (color vision disorders, scotoma, amblyopia).

If you experience or worsen the side effects listed in the instructions, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Symptoms: gastrointestinal disorders (diarrhea, nausea, vomiting, anorexia, epigastric pain), increased prothrombin time, bleeding after 12-48 hours, lethargy, drowsiness, depression, headache, tinnitus, impaired consciousness, heart rhythm disturbances, decreased blood pressure, hepato- and nephrotoxicity, seizures, hepatonecrosis may develop. In case of suspected overdose it is necessary to seek medical help immediately.

The treatment: gastric lavage during the first 4 hours; alkaline drinking, forced diuresis; activated carbon orally, administration of SH-group donators and precursors of glutathione-methionine synthesis 8-9 hours after overdose and N-acetylcysteine orally or intravenously – 12 hours later antacids; hemodialysis; symptomatic therapy.

The need for additional therapeutic measures (further methionine administration, intravenous N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as the time elapsed after its administration.

Pregnancy use

In I and II trimester of pregnancy the drug may be used only by prescription in cases when the potential benefit exceeds the possible risk to the mother and the potential risk to the fetus. The drug use in the III trimester of pregnancy is contraindicated.

If it is necessary to use the drug during breast-feeding, breast-feeding must be stopped.

In experimental studies embryotoxic, teratogenic and mutagenic effects of the drug components have not been established.

Consult your doctor before using the drug if you are pregnant or think you may be pregnant, or if you are planning to become pregnant.

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