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choline magnesium trisalicylate (Trilisate ASA combination)

 

Classes: NSAIDs

Dosing and uses of Trilisate ASA combination (choline magnesium trisalicylate)

 

Adult dosage forms and strengths

liquid

  • 500mg/5mL (294 mg choline salicylate, 362 mg magnesium salicylate)

tablet

  • 500mg (294 mg choline salicylate, 362 mg magnesium salicylate)
  • 750mg (440 mg choline salicylate, 544 mg magnesium salicylate)
  • 1000mg (587 mg choline salicylate, 725 mg magnesium salicylate)

 

Osteoarthritis

1000-3000 mg PO q8-12hr

 

Rheumatoid Arthritis

1000-3000 mg PO q8-12hr

 

Fever

1000-1500 mg PO q12hr

 

Renal Impairment

Avoid use in severe renal impairment

 

Other Indications & Uses

Shoulder pain

 

Pediatric dosage forms and strengths

liquid

  • 500mg/5mL salicylate (294 mg choline salicylate, 362 mg magnesium salicylate)

tablet

  • 500mg salicylate (294 mg choline salicylate, 362 mg magnesium salicylate)
  • 750mg salicylate (440 mg choline salicylate, 544 mg magnesium salicylate)
  • 1000mg salicylate (587 mg choline salicylate, 725 mg magnesium salicylate)

 

Mild to Moderate Pain

<37 kg: 50 mg/kg PO divided q12hr

>37 kg: 2250 mg PO divided q12hr

 

Fever

<37 kg: 50 mg/kg PO divided q12hr

>37 kg: 2250 mg PO divided q12hr

 

Geriatric dosage forms and strengths

 

Osteoarthritis

750 mg PO q8hr

 

Rheumatoid arthritis

500-1500 mg PO q8-12hr

 

Trilisate ASA combination (choline magnesium trisalicylate) adverse (side) effects

Frequency not defined

GI pain/ulceration/bleeding

Tinnitus, hearing loss

Hepatotoxicity

Renal damage

Premature hemolysis

CNS alteration

Pulmonary edema (salicylate-induced/noncardiogenic)

Dermatologic problems, urticaria

Angioedema

Bronchospasm

 

Warnings

Contraindications

Absolute: bleeding disorders, chronic advanced renal insufficiency, GI hemorrhage, hemorrhagic diathesis, salicylate allergy

Relative: Erosive gastritis, GI ulcer, NOs

 

Cautions

Anemia, gout, hepatic function impairment, hypertension, hypoprothrombinemia, nasal polyps, renal function impairment, thyrotoxicosis, vitamin K deficiency

Use of salicylates in pediatric pts with varicella or influenza-like illness is associated with incr incidence of Reye's Syndrome

 

Pregnancy and lactation

Pregnancy category: C; D if used for prolonged periods or near term

Lactation: excreted in human breast milk; adverse effect on the nursing infant

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Trilisate ASA combination (choline magnesium trisalicylate)

Mechanism of action

Inhibits cyclooxygenase; [at least 2 isoenzymes, cyclooxygenase-1 (COX-1) and -2 (COX-2)], thereby inhibiting prostaglandin synthesis

 

Pharmacokinetics

Half-Life: 2-3 hr (low-dose); 15-30 hr (high dose)

Duration: 3-6 hr (PO); >7 hr (PR)

Onset: 5-30 min (PO); 1-2 hr (PR)

Peak Plasma: 2 hr (PO); 4-5 hr (PR)

Vd: 0.15-0.2 L/kg

Metabolism: Liver, microsomal enzyme system

Metabolites: Salicylurate, salicyl phenolic glucuronide, salicyl acyl glucuronide, 2,5-dihydroxybenzoic acid (gentisic acid), 2,3-dihydroxybenzoic acid, 2,3,5-trihydroxybenzoic acid, gentisuric acid (active)

Clearance: 24-72 hr

Excretion: Principally in urine (80-100%), sweat, saliva, feces

Dialyzable: Yes

Enzymes inhibited: Prostaglandin synthesis (insignificant)

Concentration

  • Analgesia and antipyresis 30-100 mcg/mL
  • Anti-inflammatory effect 150-300 mcg/mL
  • Rheumatic fever 250-350 mcg/mL

Protein Bound

  • 90-95% with concentrations up to 100 mcg/mL
  • 70-85% with concentrations up to 100-400 mcg/mL
  • 25-60% with higher concentrations