Amtolmethine guacyl (Amtolmetinum guacilum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Included in the formulation
АТХ:

   

Pharmacodynamics:

Amtolmethine guacyl - nonsteroidal anti-inflammatory drug, a nonselective inhibitor cyclooxygenases. The drug has a desensibilizing, anti-inflammatory, analgesic and antipyretic effect. It restores disturbed microcirculation and reduces pain sensitivity in the inflammatory focus, reduces morning stiffness and swelling, increases the amount of movement in the affected joints after 4 days of treatment.

Has a protective effect on the gastric mucosa due to stimulation of the capsaicin receptors present in the walls stomach and intestines. Amtolmethine guacyl well tolerated by patients with prolonged use (within 6 months).

Pharmacokinetics:

After oral administration, the drug is absorbed rapidly, concentrating in the walls of the stomach and intestines (within 2 hours after intake, its very high concentration is maintained). After suction amtolmethine guacyl immediately undergoes hydrolysis with plasma esterases with the formation of three metabolites. The connection with plasma proteins is 99%. Half-life in adults - about 5 hours. Within 24 hours the drug is almost completely removed from the body in the form of glucuronides (with urine - 80%, with bile - 20%).

Indications:

Inflammatory diseases: rheumatoid arthritis, osteoarthrosis, ankylosing spondylitis, articular syndrome with exacerbation of gout, bursitis, tendovaginitis.

Pain syndrome (weak and moderate intensity): arthralgia, myalgia, neuralgia, migraine, dental and headache, algodismenorea, pain with injuries, burns.

Designed for symptomatic therapy, reducing pain and inflammation at the time of use; on the progression of the disease is not affected.

ICD-10

   

   

   

   

   

   

   

   

   

   

   

   

   

   

   

   

   

   

Contraindications:

Individual intolerance of amtolmethine, tolmetin.

Erosive-ulcerative changes in the mucous membrane of the stomach and duodenum and / or active gastrointestinal hemorrhage.

Complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (in t.ch. in the anamnesis).

Cerebrovascular or other bleeding.

Deficiency of glucose-6-phosphate dehydrogenase.

Inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation.

Hemophilia and other bleeding disorders.

Arterial hypertension.

Decompensated heart failure.

Hepatic insufficiency or active liver disease.

Severe renal insufficiency (Cl creatinine less than 30 ml / minute), progressive kidney disease, confirmed hyperkalemia.

The period after aortocoronary bypass surgery.

Congenital lactase deficiency, lactose intolerance, glucosogalactose malabsorption.

Pregnancy and lactation.

Children under 18 years.

Carefully:

Hyperbilirubinemia, dyslipidemia / hyperlipidemia.

Chronic heart failure and ischemic heart disease.

Chronic renal failure.

Cerebrovascular diseases.

Diabetes.

Diseases of peripheral arteries.

Smoking and alcoholism.

Ulcerative lesions gastrointestinal tract in the anamnesis.

Presence of infection H. pylori.

Simultaneous reception of oral glucocorticosteroids, antiaggregants, anticoagulants.

Long-term use NSAIDs.

Severe somatic diseases.

Elderly age.

Pregnancy and lactation:

Action category for the fetus by Food and Drug Administration (US Food and Drug Administration) - FROM.The drug is prohibited for use during pregnancy and breastfeeding.

Dosing and Administration:

It is recommended to take the drug on an empty stomach - 600 mg 2 times a day. Depending on the degree of control of the symptoms of the disease, the maintenance dose can be reduced to 600 mg once a day. The maximum daily dose is 1800 mg.

Side effects:

Digestive system: often - nausea, infrequent - bloating, dyspepsia, discomfort in the stomach and intestines, rarely - abdominal pain, diarrhea or constipation, gastritis, very rarely - a peptic ulcer, a violation of the liver.

Urinary system: an increase in the content of urea nitrogen in the blood, urinary tract infection.

Nervous system and sensory organs: often - dizziness, headache, drowsiness, rarely - noise in the ears, visual impairment, depression.

Respiratory system: rarely - bronchospasm, dyspnea, rhinitis, laryngeal edema.

The cardiovascular system: often - increased blood pressure.

Blood: rarely - anemia, thrombocytopenia, agranulocytosis, leukopenia.

Leather: infrequently - a skin rash, purpura; rarely - exfoliative dermatitis), urticaria, Stevens-Johnson syndrome, Lyell's syndrome.

Allergic reactions: rarely anaphylaxis or anaphylactoid reactions.

Others: often - weakness; rarely - swelling, weight gain; rarely - excessive sweating, fever, lymphadenopathy; very rarely - swelling of the tongue.

Overdose:

When an overdose is observed abdominal pain, nausea, vomiting, erosive-ulcerative lesion gastrointestinal tract, renal dysfunction, metabolic acidosis. For treatment appoint gastric lavage, enterosorbents, symptomatic therapy.

Interaction:

Phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants with simultaneous application lead to an increase in the production of hydroxylated active metabolites.

Joint use leads to a decrease in the effectiveness of uricosuric, hypotensive drugs and diuretics.

Amtolmethine guacil enhances the hypoglycemic effect of derivatives of sulfonylurea, the effect of anticoagulants, antiaggregants, fibrinolytic agents, side effects of glucocorticosteroids, mineralocorticoids and estrogens.

Antacids and cholestyramine reduce the absorption of the drug.

Amtolmethine guacyl promotes an increase in the concentration in the blood of lithium preparations, methotrexate.

With kidney diseases against the background of taking the drug may worsen the condition.

Myelotoxic drugs increase the manifestation of hematotoxicity amtolmethine guacyl.

Special instructions:

When the drug is used, it is necessary to control the pattern of peripheral blood and the functional state of the liver and kidneys.

The drug should be discontinued 2 days before the analysis for the determination of 17-ketosteroids.

During treatment, one should refrain from engaging in potentially dangerous activities that require increased attention and speed of mental and motor reactions.

Instructions
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