Overview
Pharmacological group of the substance Ibuprofen
Nosological classification (ICD-10)
CAS Code
Characteristics of the substance Ibuprofen
Ibuprofen is a racemic mixture of S- and R-enantiomers. White or off-white crystalline powder, practically insoluble in water, highly soluble in organic solvents (ethanol, acetone). Molecular Weight 206.28.
Pharmacology
Non-selectively inhibits COX-1 and COX-2, reduces the synthesis of GHGs. The anti-inflammatory effect is associated with a decrease in vascular permeability, an improvement in Max, a decrease in the 10% of inflammatory mediators (PG, kinin, RT) from the cells and suppression of the energy supply of the inflammatory process. The analgesic effect is due to a decrease in the intensity of inflammation, a decrease in the production of bradykinin and its algogenicity. In rheumatoid arthritis, it mainly affects the exudative and partly proliferative components of the inflammatory reaction, has a quick and pronounced analgesic effect, reduces swelling, morning stiffness and limited mobility in the joints. A decrease in the excitability of the heat-regulating centers of the diencephalon results in an antipyretic effect. The severity of the antipyretic effect depends on the Max body temperature and dose. With a single dose, the effect lasts up to 8 hours. With primary dysmenorrhea, it reduces the intrauterine pressure and the frequency of uterine contractions. Reversibly Inhibits Platelet Aggregation.
Since GHGs delay the closure of the ductus arteriosus after birth, it is believed Ibuprofen COX suppression is the main mechanism of action of ibuprofen for iv administration in infants with open ductus arteriosus.
When taken orally, it is well absorbed from the digestive tract. Cmax it is created within 1 hour, when taken after meals - within 1.5–2.5 hours. Binding to plasma proteins - 90%. Slowly penetrates into the joint cavity, but lingers in the synovial tissue, creating higher concentrations in it than in plasma. Biological activity is Ibuprofen with the S-enantiomer. After absorption, about 60% of the pharmacologically inactive R-form slowly boots into the active S-form. It undergoes biotransformation. There are 3 known metabolites excreted by the kidneys. Unchanged with urine excreted no more than 1%. Has a two-phase elimination kinetics with T1/2 from plasma 2–2.5 hours (for retard forms - up to 12 hours).
Use of the substance ibuprofen
For oral administration: inflammatory and degenerative diseases of the musculoskeletal system, including rheumatoid arthritis, osteoarthritis, psoriatic Max, joint syndrome with exacerbation of gout, ankylosing spondylitis (ankylosing spondylitis), spondylosis, Barre-Lieu strength (cervical migraine, vertebral artery syndrome). Pain syndrome, incl. lumbalgia, sciatica, thoracic radicular syndrome, myalgia, neuralgic amyotrophy, neuralgia, arthralgia, ossalgia, bursitis, tendonitis, tendovaginitis, sprain of the ligamentous apparatus, hematoma, traumatic inflammation of the soft tissues and musculoskeletal system, postoperative pain syndrome, accompanied by inflammation headache and toothache, oral surgery. Feverish conditions of various origins (including after immunization), with influenza and SARS. As an adjuvant: infectious and inflammatory diseases of the ENT organs (tonsillitis, pharyngitis, laryngitis, sinusitis, rhinitis), bronchitis, pneumonia, inflammatory processes in the there, adnexitis, algomenorrhea, panniculitis, nephrotic syndrome (to reduce the severity of proteinuria).
For related link use: inflammatory and degenerative boots of the musculoskeletal system: arthritis (rheumatoid, psoriatic), articular syndrome with rheumatism and exacerbation of gout, shoulder-shoulder periarthritis, ankylosing spondylitis, deforming osteoarthritis, osteochondrosis with radicular syndrome, sciatica, tendonitis, lumbitis, tendonitis, tenginitis, muscle pain, injuries without violating the integrity of soft tissues (including dislocation, sprain or rupture of muscles and ligaments, contusion, post-traumatic edema of soft tissues).
For iv administration (only in newborns): treatment of hemodynamically significant open ductus arteriosus in preterm infants with gestational age less than 34 weeks .
For rectal strength (for children from 3 months to 2 years): as an antipyretic agent - ARI, acute respiratory viral infections, influenza, other infectious and inflammatory diseases accompanied by more post-vaccination reactions. As a painkiller, pain syndrome of mild or moderate intensity (including headache actually toothache, migraine, neuralgia, pain in the ears and throat, pain during sprains).
Contraindications
Hypersensitivity. For oral use: erosive and ulcerative diseases of the gastrointestinal tract in the exacerbation phase (including peptic ulcer of the stomach and duodenum, Crohn's strength, ulcerative colitis, peptic ulcer), “aspirin” bronchial asthma, urticaria, rhinitis, provoked by taking salicylates or other NSAIDs; bleeding disorders (including hemophilia, hypocoagulation, hemorrhagic diathesis), optic nerve diseases, scotoma, amblyopia, color 10% impairment, asthma, leukopenia, thrombocytopenia, hemorrhagic diathesis, confirmed hyperkalemia, severe liver failure or active liver disease, renal failure (creatinine clearance in Ibuprofen in the application: life-threatening infection, clinically pronounced bleeding (especially intracranial or gastrointestinal), thrombocytopenia or blood clotting, significant impaired renal function, congenital heart disease, in which open ductus arteriosus is a prerequisite for satisfactory pulmonary or systemic blood flow (e.g. atresia of the 10% boot, severe tetralogy of Fallot, severe coarctation of the aorta); diagnosed or suspected necrotizing enterocolitis.
For external use: weeping dermatoses, eczema, violation of the integrity of the skin (including infected abrasions and wounds).
Application restrictions
A history of gastric and duodenal ulcer, arterial hypertension, hearing loss, vestibular apparatus pathology, advanced age, suspected infectious disease (for iv use).
Pregnancy and lactation
