Salicylamide (Salicylamidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Non-narcotic analgesics, including non-steroidal and other anti-inflammatory drugs

NSAIDs - Salicylic acid derivatives

Included in the formulation
АТХ:

N.02.B.A   Salicylic acid and its derivatives

N.02.B.A.05   Salicylamide

Pharmacodynamics:

Anti-inflammatory, analgesic and antipyretic effect.

Anti-inflammatory effect as in acetylsalicylic acid is due to inhibition of COX-2 activity, which leads to a decrease in the production of inflammatory mediators - prostaglandins Pg D2, E2 and I2.

The analgesic effect is associated with a decrease in the synthesis of PgE2, which prevents sensitization of pain receptors to bradykinin, histamine and other chemicals synthesized or released in the inflammatory focus.

The antipyretic effect is caused by the disruption of the production of eicosanoide PgE2, which, when inflamed, stimulates the thermoregulatory center in the anterior parts of the hypothalamus. This reduces only febrile body temperature due to increased heat transfer as a result of increased sweating and widening of peripheral vessels, while normal body temperature does not decrease.

Antiaggregant effect is associated with its inhibitory effect on cyclooxygenase-1 activity in platelets, as a result of which the synthesis of thromboxane A2 is disrupted.Irreversibly inhibits cyclooxygenase (causes irreversible acetylation of this enzyme), disrupting the formation of arachidonic acid cyclic endoperoxides - precursors of thromboxane A2 and prostaglandins. Therefore, the action of acetylsalicylic acid not only reduces the synthesis of thromboxane A2 in platelets, but also the synthesis of prostacyclin in endothelial cells of the vessels. Data on effective use as an antiplatelet agent are not available.

Pharmacokinetics:

Absorption is good. The connection with plasma proteins is low. Biotransformation in the liver, but not hydrolyzed to salicylic acid. Elimination in the form of metabolites.

Indications:

Feverish syndrome (catarrhal and infectious diseases); pain syndrome of mild and moderate intensity: arthralgia, myalgia, neuralgia, migraine, dental and headache, algodismenorea; pain with injuries, burns; inflammatory diseases of the joints (rheumatoid arthritis, reactive arthritis, osteoarthritis, spondyloarthropathy, ankylosing spondylitis, gout) and soft tissues (bursitis, tenosynovitis); rheumatic heart disease.

ICD-10

VI.G40-G47.G43.1   Migraine with aura [classic migraine]

VI.G40-G47.G43.0   Migraine without aura [simple migraine]

VI.G40-G47.G43.9   Migraine, unspecified

VI.G40-G47.G43.8   Another migraine

VI.G40-G47.G43.3   Complicated migraine

VI.G40-G47.G43   Migraine

X.J10-J18.J10.8   Influenza with other manifestations, influenza virus identified

X.J10-J18.J10.1   Influenza with other respiratory manifestations, influenza virus identified

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

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

XIII.M70-M79.M79.0   Rheumatism, unspecified

XIII.M65-M68.M67.3   Migrating synovitis

XIII.M05-M14.M12.3   Palindromia rheumatism

Contraindications:

Hypersensitivity, erosive and ulcerative lesions of the gastrointestinal tract, peptic ulcer of the stomach and duodenum, ulcerative colitis; bronchial asthma, heart failure, edema, arterial hypertension, hemophilia, hypocoagulation states, renal and / or hepatic insufficiency, hearing loss, vestibular apparatus pathology, glucose-6-phosphate dehydrogenase deficiency, blood diseases.

Carefully:

Pregnancy, breast-feeding.

Pregnancy and lactation:

Action category for the fetus by FDA - D

Adequate and well-controlled studies in humans have not been conducted. Animals have a teratogenic effect.Penetrates into breast milk. May cause disruption in children.
Dosing and Administration:

Inside (after eating, squeezed a sufficient amount of liquid) to 0.25-0.5 g 2-3 times a day; with rheumatism, 0.5-1 g 3-8 times a day.

The maximum daily dose of 8 g / day.

The maximum antirheumatic effect - after 2-3 weeks of continuous use.

At children - inside on 0,4-0,5 g / day for each year of a life.

Side effects:

From the nervous system and sensory organs: headache, dizziness, hearing loss, tinnitus.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): heart failure, increased blood pressure, agranulocytosis, leukopenia, thrombocytopenia, anemia.

On the part of the digestive system: NSAID-gastropathy: abdominal pain, nausea, vomiting, heartburn, diarrhea.

Other: bleeding - gastrointestinal, gingival, uterine, hemorrhoidal; bronchospasm, swelling, impaired liver and kidney function, increased sweating; allergic reactions; with prolonged use in large doses - ulceration of the mucosa of the gastrointestinal tract, bleeding.

Overdose:

Symptoms: salicylism (confusion, diarrhea, abdominal pain, headache, dizziness, drowsiness, rapid or deep breathing, nausea, vomiting, visual impairment).

Severe overdose: blood in the urine, convulsions, hallucinations, increased excitability, agitation, confusion, shortness of breath or excruciating breath, fever, respiratory alkalosis, metabolic acidosis, hyper- or hypoglycemia, ketonuria, hyponatremia, hypokalemia.

The sequence of development of toxic effects with increasing serum concentrations of salicylates: minimal toxic effects (hearing impairment, tinnitus - 200 mcg / ml), hepatotoxicity (impaired functional liver tests), decreased renal function, decreased PV, deafness, hyperventilation, metabolic acidosis (400 μg / ml).

Treatment: symptomatic; hemodialysis, peritoneal dialysis, hemoperfusion.

Interaction:

Inductors of microsomal oxidation (incl. phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites; ethanol promotes the development of acute pancreatitis.

Increases the activity of anticoagulants, antiplatelet agents, fibrinolytics, as well as side effects of mineral and glucocorticoids, estrogens, hepato- and nephrotoxic agents.

Reduces the effectiveness of uricosuric drugs, hypotensive and diuretics.

Antacids and colestramine reduce absorption.

Special instructions:

It is necessary to monitor the picture of peripheral blood and the functional state of the liver during treatment.

Instructions
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