Ibuprofen + Paracetamol - instructions for use, dose, side effects, contraindications

Non-selective reversible cyclooxygenase inhibitor, an enzyme that catalyzes the reaction of the conversion of arachidonic acid to prostaglandin H₂, which is the precursor of the remaining prostaglandins, thromboxane A₂ and prostacyclin. Has anti-inflammatory and analgesic, as well as antipyretic effect. It inhibits the aggregation of platelets.

Ibuprofen also inhibits the synthesis of leukotrienes, reduces bradykinin activity, stabilizes lysosomal membranes.With articular syndrome reduces the severity of arthralgia (at rest and during movement), morning stiffness and swelling of the joints, helps reduce the degree of their functional insufficiency.

Paracetamol

Has antipyretic analgesic and anti-inflammatory effect. Inhibits cyclooxygenase, mainly in the central nervous system, affects the centers of pain and thermoregulation. It does not have a negative effect on water-salt metabolism and mucous membranes of the gastrointestinal tract, and therefore has little effect on the synthesis of prostaglandins in peripheral tissues.

Pharmacokinetics:

Ibuprofen

After oral administration, up to 80% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 1-2 hours.

After absorption, about 60% of the pharmacologically inactive R-form is slowly transformed into an active S-form. The connection with plasma proteins is 99%. The therapeutic concentration persists longer in the synovial fluid than in the blood plasma.

Metabolism in the liver.

The half-life is 6-7 days. Elimination by the kidneys.

Paracetamol

After oral administration, it is completely absorbed in the gastrointestinal tract.The maximum concentration in the blood plasma is reached in 20-30 minutes. The connection with plasma proteins is 15%. Penetrates through the blood-brain barrier, enters the breast milk.

Metabolism in the liver by glucuronation and sulfation (80%) with the formation of inactive metabolites, about 17% is hydroxylated to active metabolites, which are subsequently deactivated after conjugation with sulfates and glutathione. With a lack of glutathione, these metabolites block the enzyme systems of the liver, causing necrosis of hepatocytes.

Half-life is 2-3 hours. Elimination by the kidneys, about 3% unchanged.

Indications:

It is used for the treatment of rheumatism, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, sciatica, lumbago, tendovaginitis, synovitis, bursitis, trauma of the musculoskeletal system and soft tissues, pain syndrome of various genesis (including postoperative period), primary algodismenorea. Used for febrile conditions accompanying colds, to relieve the pain syndrome of mild or moderate severity in arthralgia, myalgia, migraine, neuralgia, headache and toothache,as well as with algodismenorrhea.

ICD-10

X.J00-J06.J06.9 Acute upper respiratory tract infection, unspecified

X.J10-J18.J10 Influenza caused by an identified influenza virus

XI.K00-K14.K08.8 Other specified changes in teeth and their supporting apparatus

XIII.M20-M25.M25.5 Pain in the joint

XIII.M50-M54.M54 Dorsalgia

XIII.M70-M79.M70 Diseases of soft tissues associated with exercise, overload and pressure

XIII.M70-M79.M79.1 Myalgia

XIII.M70-M79.M79.2 Neuralgia and neuritis, unspecified

XIV.N80-N98.N94.4 Primary dysmenorrhea

XIV.N80-N98.N94.5 Secondary dysmenorrhea

XVIII.R50-R69.R50 Fever of unknown origin

XVIII.R50-R69.R51 Headache

XVIII.R50-R69.R52.0 Acute pain

XVIII.R50-R69.R52.2 Another constant pain

XIX.T08-T14.T13.2 Dislocation, stretching and overstrain of the capsular-ligament apparatus of the unspecified joint of the lower limb, level unspecified

Contraindications:Peptic ulcer of stomach and duodenum, ulcerative colitis, gastritis, individual intolerance, bleeding in the gastrointestinal tract, phenylketonuria, glucose-6-phosphate dehydrogenase deficiency, portal hypertension, anemia, leukopenia, thrombocytopenia, individual intolerance, children under 12 years.

Carefully:

Severe renal and hepatic insufficiency, Gilbert's syndrome, viral hepatitis, old age, alcoholism.

Pregnancy and lactation:

Recommendations for FDA - Category C.Contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside 1 tablet 2-3 times a day, before or after 2-3 hours after eating.

The highest daily dose: 4 tablets.

The highest single dose: 1 tablet.

Side effects:

Central and peripheral nervous system: dizziness, drowsiness, hallucinations.

The system of hematopoiesis: rarely - thrombocytopenia.

Digestive system: nausea, heartburn, diarrhea.

Urinary system: rarely - oliguria.

Allergic reactions.

Overdose:

Ibuprofen

Pain in epigastrium, nausea, vomiting, drowsiness. Rarely - gastrointestinal bleeding, muscle twitching, respiratory depression, coma.

Symptomatic therapy.

Paracetamol

Diarrhea, anorexia - with acute overdose (develops 6-14 hours after exceeding the dose), with chronic (develops 2-4 days after exceeding the dose) - hypocoagulation, DIC syndrome, cerebral edema, rarely - fulminant renal failure due to tubular necrosis .

Necrosis of liver cells, due to the formation of a toxic metabolite of acetaminophen - N-acetyl-p-benzoquinonimine.

Treatment: application of donators SH-groups (precursors of the synthesis of glutathione: methionine and N-acetylcysteine) for 12 hours after an overdose.

Interaction:

Ibuprofen

Increases the effectiveness of oral hemocoagulants.

With simultaneous use with barbiturates, narcotic analgesics, caffeine, phenothiazine derivatives, diphenhydramine, phenacetin, analgesic effects are enhanced.

Anti-inflammatory effect increases salicylates and metamizol sodium.

Paracetamol

Strengthens the effect of indirect coagulants and toxicity of chloramphenicol.

The intake of ethanol in the treatment of the drug leads to the development of acute pancreatitis.

Simultaneous use with stimulators of microsomal oxidation in the liver (barbiturates, rifampicin, ethanol, phenylbutazone, phenytoin) increases the toxicity of paracetamol.

Reduces the risk of hepatotoxic effects of microsomal oxidation inhibitors (cimetidine).

Special instructions:

Coagulogram monitoring with prolonged use of the drug. During treatment with the drug should refrain from driving the car and works requiring increased concentration of attention.

Instructions

Ibuprofen + Paracetamol (Ibuprophenum + Paracetamolum)