快樂小藥師 Im pharmacist nichts glücklich

Tolmetin，商品名：Artrocaptin (ES);Tolectin

用途：

Treatment of rheumatoid arthritis and osteoarthritis, juvenile rheumatoid arthritis

治療風濕性關節炎、骨關節炎，幼年型風濕性關節炎

機轉：

Reversibly inhibits cyclooxygenase-1 and 2 (COX-1 and 2) enzymes, which results in decreased formation of prostaglandin precursors; has antipyretic, analgesic, and anti-inflammatory properties.

Other proposed mechanisms not fully elucidated (and possibly contributing to the anti-inflammatory effect to varying degrees) include inhibiting chemotaxis, altering lymphocyte activity, inhibiting neutrophil aggregation/activation, and decreasing proinflammatory cytokine levels.

其實就是NSAID，不過比較不同的，他的結構並非是pyrine，也不是水楊酸，也沒有indene，也看不到proprionic acid，所以可以用在對於aspirin或是ibuprofen及cataflam反應比較差的病患。

合成過程：

治療劑量：

Inflammation, arthritis: Oral: 400 mg 3 times/day; usual dose: 600 mg to 1.8 g/day; maximum: 1.8 g/day

JRA: Oral: Children ≥2 years: Initial: 20 mg/kg/day in 3-4 divided doses; Maintenance: 15-30 mg/kg/day in 3-4 divided doses (maximum 30 mg/kg/day)

Analgesic (unlabeled use): Oral: Children ≥2 years: 5-7 mg/kg/dose every 6-8 hours
Dosing: Elderly

懷孕分級：C

Pregnancy Implications

Adverse events were not observed in the initial animal reproduction studies; therefore, the manufacturer classifies tolmetin as pregnancy category C. NSAID exposure during the first trimester is not strongly associated with congenital malformations; however, cardiovascular anomalies and cleft palate have been observed following NSAID exposure in some studies. The use of an NSAID close to conception may be associated with an increased risk of miscarriage. Nonteratogenic effects have been observed following NSAID administration during the third trimester including myocardial degenerative changes, prenatal constriction of the ductus arteriosus, fetal tricuspid regurgitation, failure of the ductus arteriosus to close postnatally; renal dysfunction or failure, oligohydramnios; gastrointestinal bleeding or perforation, increased risk of necrotizing enterocolitis; intracranial bleeding (including intraventricular hemorrhage), platelet dysfunction with resultant bleeding; pulmonary hypertension. Because they may cause premature closure of the ductus arteriosus, use of NSAIDs late in pregnancy should be avoided (use after 31 or 32 weeks gestation is not recommended by some clinicians). The chronic use of NSAIDs in women of reproductive age may be associated with infertility that is reversible upon discontinuation of the medication.
Lactation

Enters breast milk/not recommended (AAP rates “compatible”)
Breast-Feeding Considerations

Tolmetin is found in breast milk and breast-feeding is not recommended by the manufacturer. The AAP considers tolmetin to be "usually compatible with breast-feeding."

其他飲食上的建議：

May be taken with antacids to minimize stomach upset. Administration with food or milk decreases bioavailability by 16%. Sodium content: 200 mg: 0.8 mEq; 400 mg: 1.568 mEq; 600 mg: 2.35 mEq.