Naproxen

When ATH: M01AE02

Naproxen – Characteristic

NSAIDs. Naproxen - white or almost white, crystalline powder;. Soluble in lipids, practically insoluble in water at low pH, freely soluble in water at high pH. Octanol / water at pH 7,4 It is 1.6-1.8. Molecular weight 230,26.

Naproxen sodium - a white crystalline solid or white-cream color, freely soluble in water at neutral pH. Molecular weight 252,24.

Pharmacological action

Anti-inflammatory, analgesic, pyretic, antiagregatine.

Application

Inflammatory and degenerative diseases of the musculoskeletal system, incl. rheumatoid arthritis, osteoarthritis, ankiloziruyushtiy spondylitis, articular syndrome in exacerbation of gout, juvenile rheumatoid arthritis; pain syndrome: neuralgia, myalgia, ossalgia, radiculitis, headache and toothache, Tendinitis, pain in oncology, postoperative pain, accompanied by inflammation, injuries of the musculoskeletal system and soft tissue, adnexitis, primary dysmenorrhea; pain and fever in infectious and inflammatory diseases of the upper respiratory tract (in the complex therapy).

Contraindications

Hypersensitivity, «Aspirinovaya» asthma, "Aspirinovaâ" triad (a combination of asthma, recurrent nasal polyposis, and paranasal sinuses and intolerance of aspirin and drugs pirazolonovogo series), erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, hemodyscrasia, liver and / or kidney failure, Children up to age 1 year.

Restrictions apply

Severe heart failure, adolescence (to 16 years).

Pregnancy and breast-feeding

Teratogenic effects. In reproduction studies in animals when administered to rats at doses of naproxen 20 mg / kg / day (125 mg / m²/d), which is roughly equivalent 0,23 MRDC, Krolik - 20 mg / kg / day (220 mg / m²/d), or 0,27 MRDC, mice - 170 mg / kg / day (510 mg / m²/d), or 0,28 MRDC, there was no evidence of impaired fertility or harm to the fetus.

However, reproductive studies in animals do not always predict effects in humans. There are no adequate and well-controlled studies in pregnant women have not held. Application during pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus.

Nonteratogenic effects. Since it is known, that means, ingibiruyushtie synthesis NG, used to delay premature birth, it increases the risk of neonatal complications, such as necrotizing enterocolitis, patent ductus arteriosus, intracranial hemorrhage. The use of naproxen in late pregnancy may lead to delay childbirth, persistent pulmonary hypertension, renal dysfunction, Abnormal levels of prostaglandin E in premature infants. Since the known effects of this class of substances on the cardiovascular system of the fetus (closing arterial duct), Use in III trimester excluded.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Naproxen is determined in the breast milk of women (concentration is about 1% serum). Because of possible adverse effects of substances, ingibiruyushtih synthesis NG, in newborn, nursing mothers should not be used naproxen.

Side effects

Side effects, most frequently encountered in clinical trials (possibly involving the use of naproxen):

From the digestive tract: 3-9% - Heartburn, abdominal pain, nausea, constipation; >1% - Diarrhea, dyspepsia, stomatitis; <1% - Flatulence, bleeding / perforation, GI ulcers (gastro-duodenalʹnye), vomiting, increase in liver transaminases.

From the nervous system and sensory organs: 3-9% - Headache, drowsiness, dizziness, tynnyt, blurred vision, hearing loss; >1% - Vertigo.

Cardio-vascular system and blood (hematopoiesis, hemostasis): >1% - Palpitations; <1% - Anemia, increase in bleeding time.

From the respiratory system: 3-9% - Dyspnoea.

For the skin: 3-9% - Ekximoz.

With the genitourinary system: <1% - Renal dysfunction.

Allergic reactions: 3-9% - Itching, skin rashes, anaphylactoid reactions.

Other: 3-9% - Edema; >1% - Excessive sweating, purpura, thirst.

Side effects, occurs with a frequency <1% in clinical trials and post-marketing studies (possibly involving the use of naproxen):

From the digestive tract: colitis, gematemezis, jaundice, pancreatitis, ground.

With the genitourinary system: glomerular nephritis, hematuria, hyperkalemia, interstitial nephritis, nephrotic syndrome, renal failure, renal papillary necrosis.

Cardio-vascular system and blood (hematopoiesis, hemostasis): agranulocytosis, eozinofilija, granulocytopenia, leukopenia, thrombocytopenia.

From the nervous system and sensory organs: depression, unusual dreams, inability to focus, insomnia, malaise, myalgia, muscular weakness.

Side effects, occurs with a frequency <1% (a causal relationship to the use of naproxen is not installed):

Cardio-vascular system and blood (hematopoiesis, hemostasis): aplasticheskaya anemia, gemoliticheskaya anemia.

From the nervous system and sensory organs: aseptic meningitis, cognitive dysfunction.

From the digestive tract: nepepticheskoe gastrointestinal ulceration, ulcerative stomatitis.

Allergic reactions: epidermal necrolysis, erythema multiforme, Stevens-Johnson syndrome, hives; photosensitivity reaction, epidermolysis bullosa like porfiricheskomu.

Other: vasculitis, hyper / hypoglycemia, alopecia, photodermatitis.

Cooperation

Increases toxicity hydantoin, anticoagulants, sulfonamides, methotrexate (blocks tubular secretion). Reduces natriuretic and diuretic effect of furosemide, gipotenziю, caused by beta-blockers. Reduces the excretion of lithium salts and increases its concentration in plasma. Antacids, containing magnesium and aluminum, and sucralfate may reduce the absorption of naproxen.

Overdose

Symptoms: drowsiness, slackness, dizziness, epigastric pain, abdominal discomfort, heartburn, dyspepsia, nausea, transient hepatic dysfunction, gipoprotrombinemii, renal dysfunction, metabolic acidosis, apnea, disorientation, vomiting; possible bleeding from the gastrointestinal tract; rarely - hypertension, acute renal failure, respiratory depression, coma.

Treatment: gastric lavage, induction of vomiting and / or administration of activated charcoal (60100 g - adult, 1-2 G / kg - children) and / or the appointment of osmotic laxatives, symptomatic and supportive therapy. The specific antidote is not found. Forced diuresis, urinary alkalization or hemodialysis is not effective due to the high protein binding.

Dosing and Administration

Inside, the average dose for adults - 250-500 mg 2 once a day, The maximum single dose - 500 mg, maximum daily - 1750 mg 2 admission (in the morning and at night).

The average daily intake for children 1 Year to 5 s - 2.5-10 mg / kg body weight in 1-3 reception, older children 5 years - 10 mg / kg per day 2 admission, usual duration of treatment - 2 Sun (preferred dosage form is a suspension for children); in juvenile arthritis in children older 5 s daily dose of 10 mg / kg.

Precautions

With prolonged use is necessary to control the function of the liver and kidneys, the peripheral blood.

If you want to determine the 17-ketosteroids or 5 oxyindoleacetic acid treatment should be suspended for 48 h before the test.

Cooperation