Salicylate Combination

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|Salicylate Combination

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Salicylate Combination

Pronouncation: (suh-LIS-ih-late)
Class: CNS agent

Trade Names:
Choline Magnesium Trisalicylate
- Liquid 500 mg salicylate (as 294 mg choline salicylate, 362 mg magnesium salicylate)
- Tablets 500 mg salicylate (as 293 mg choline salicylate, 362 mg magnesium salicylate)
- Tablets 750 mg salicylate (as 440 mg choline salicylate, 544 mg magnesium salicylate)
- Tablets 1000 mg salicylate (as 587 mg choline salicylate, 725 mg magnesium salicylate)

Mechanism of Action

Pharmacology

Relieves pain by inhibiting prostaglandin synthesis and release; reduces fever by vasodilation of peripheral vessels. Unlike aspirin, does not inhibit platelet aggregation.

Pharmacokinetics

Absorption

Salicylate is absorbed rapidly and reaches C max in approximately 1 to 2 hr after a single dose of a tablet or liquid doseform.

Metabolism

The primary salicylate metabolites are glycine and glucuronide conjugates.

Elimination

The primary route of excretion of salicylate is renal. Serum salicylate concentrations are increased by conditions that decrease glomerular filtration rate or proximal tubular secretion. Salicylate t ½ is approximately 9 to 17 hr.

Indications and Usage

Relief of mild-to-moderate pain; treatment of rheumatic fever and rheumatoid arthritis including juvenile arthritis and osteoarthritis; management of fever.

Contraindications

Hypersensitivity to nonacetylated salicylates, NSAIDs or aspirin; advanced chronic renal insufficiency; bleeding disorders; GI bleeding.

Dosage and Administration

Inflammatory Conditions
Adults

PO 1500 mg bid or 3000 mg qd.

Elderly Patients

PO 750 mg tid.

Fever, Mild-to-Moderate Pain
Adults

PO 1000 to 1500 mg bid.

Children under 37 kg

PO 50 mg/kg/day in 2 divided doses.

Children over 37 kg

PO 2250 mg/day in 2 divided doses. Doses are adjusted based on patient"s response, tolerance and serum salicylate concentration.

Storage/Stability

Store in tight, light-resistant container.

Drug Interactions

Carbonic anhydrase inhibitors (eg, acetazolamide)

Accumulation of carbonic anhydrase inhibitor and toxicity.

Corticosteroids

Decreased plasma salicylate concentration.

Methotrexate

Could cause methotrexate toxicity.

Oral hypoglycemics or insulin

Could cause hypoglycemia.

Urinary acidifiers

Increased salicylate serum concentration.

Urinary alkalinizers (eg, chronic antacids)

Decreased salicylate serum concentration.

Warfarin

Enhanced anticoagulant activity of oral anticoagulants. Creates potential for increased prothrombin time due to protein-binding displacement.

Laboratory Test Interactions

Phenolsulfonphthalein

Salicylates decrease renal excretion.

Thyroid function tests

Drug causes increased free T 4 and decreased total T 4 ; thyroid function is not affected.

Urine glucose

Drug causes false-negative results by glucose oxidase method and false-positive results by copper reduction method with moderate to high doses of salicylates.

Urine 5-HIAA

Salicylates interfere with fluorescent method.

Urine ketones

Drug causes interference with ferric chloride (Gerhardt) method by turning urine a reddish color.

Urine vanillylmandelic acid

Salicylates can interfere with determination.

Adverse Reactions

Dermatologic

Hives; rash; angioedema.

EENT

Tinnitus.

GI

Nausea; dyspepsia; gastric ulceration.

Hematologic

Prolonged bleeding time.

Hepatic

Hepatotoxicity.

Metabolic

Uric acid levels elevated by salicylate concentrations less than 10 mg/dL and decreased by levels greater than 10 mg/dL.

Respiratory

Bronchospasm.

Miscellaneous

Anaphylaxis; salicylism may occur with large doses or chronic therapy (symptoms include dizziness, tinnitus, vomiting, diarrhea, confusion, CNS depression, headache, sweating, hyperventilation, and lassitude); fever.

Precautions

Monitor

Monitor pain relief and temperature after medication administration. If tinnitus, flushing, tachycardia, hyperventilation, sweating, or thirst occurs, withhold medication.


Pregnancy

Category C . Do not use during third trimester; could prematurely close ductus arteriosus in the fetus.

Lactation

Excreted in breast milk.

Children

May increase risk of Reye"s syndrome; do not use in individuals under 18 yr if chickenpox or flu symptoms are suspected.

Special Risk Patients

Use drug with caution in patients with renal or hepatic dysfunction, peptic ulcer disease, or gastritis.

Aspirin or NSAID hypersensitivity

Nonacetylated salicylates have been tolerated in aspirin-sensitive asthmatic patients; however, cases of cross-sensitivity including bronchospasm have been reported.

Overdosage

Symptoms

Respiratory alkalosis, hyperpnea, tachypnea, nausea, vomiting, hypokalemia, tinnitus, neurologic abnormalities (disorientation, irritability, lethargy, stupor), dehydration, hyperthermia, seizures, coma.

Patient Information

  • Advise patient to take medication with food or after meals with full glass of water.
  • Emphasize need to avoid alcohol ingestion and use of NSAIDs during therapy (which increase risk of GI irritation/GI bleeding), especially if patient is undergoing long-term therapy.
  • Instruct patients with diabetes to monitor blood levels closely during treatment.
  • Instruct patient to call health care provider immediately if ringing in ears or persistent GI pain occurs while taking this medication.




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