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Choline Magnesium Trisalicylate


General


Pronunciation

(KOE leen mag NEE zhum trye sa LIS i late)


Indications


Use: Labeled Indications

Acute painful shoulder: Management of acute painful shoulder

Analgesia: Relief of mild to moderate pain

Antipyresis: Management of pyrexia

Arthritis: Relief of signs/symptoms of osteoarthritis, rheumatoid arthritis, and other arthritis (long-term management and acute flares)

Juvenile idiopathic arthritis: Anti-inflammatory or analgesic management (in children) of juvenile idiopathic arthritis and other appropriate conditions


Contraindications


Hypersensitivity to choline magnesium trisalicylate, other nonacetylated salicylates, or any component of the formulation


Dosing and Administration


Dosing: Adult

Note: Dosing is based on salicylate content. Individualize dose based on response; may require 2 to 3 weeks to achieve optimal effect.

Acute painful shoulder, osteoarthritis, rheumatoid arthritis, or other severe arthritis: Oral: Initial: 1500 mg twice daily or 3000 mg once daily at bedtime

Analgesia (mild to moderate pain) or pyrexia: Oral: 2000 mg to 3000 mg daily in 2 or 3 divided doses; adjust dose to obtain optimal therapeutic response.


Dosing: Geriatric

Usual dose: 750 mg 3 times daily; adjust dose to obtain optimum therapeutic response.


Dosing: Pediatric

Note: Dosing is based on salicylate content. Individualize dose based on response; may require 2 to 3 weeks to achieve optimal effect.

Juvenile idiopathic arthritis:

Children and Adolescents ≤37 kg: Oral: 25 mg/kg/dose twice daily

Children and Adolescents >37 kg: Oral: 1,125 mg twice daily


Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer 's labeling; use with caution in acute or chronic renal impairment. Avoid use in severe renal impairment; monitor salicylate levels and adjust dose accordingly.


Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer 's labeling; use with caution in acute or chronic hepatic impairment; monitor salicylate levels and adjust dose accordingly.


Administration

Administer with food or large volume of water or milk to minimize GI upset. Liquid may be mixed with fruit juice just before drinking.


Storage

Store between 15 ‚ °C and 30 ‚ °C (59 ‚ °F and 86 ‚ °F).


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Liquid, Oral:

Generic: 500 mg/5 mL (240 mL)

Tablet, Oral:

Generic: 1000 mg


Drug Interactions

ACE Inhibitors: Salicylates may enhance the nephrotoxic effect of ACE Inhibitors. Salicylates may diminish the therapeutic effect of ACE Inhibitors. Monitor therapy

Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.): May enhance the adverse/toxic effect of Salicylates. Increased risk of bleeding may result. Monitor therapy

Ajmaline: Salicylates may enhance the adverse/toxic effect of Ajmaline. Specifically, the risk for cholestasis may be increased. Monitor therapy

Ammonium Chloride: May increase the serum concentration of Salicylates. Monitor therapy

Anticoagulants: Salicylates may enhance the anticoagulant effect of Anticoagulants. Monitor therapy

Benzbromarone: Salicylates may diminish the therapeutic effect of Benzbromarone. Monitor therapy

Blood Glucose Lowering Agents: Salicylates may enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy

Carbonic Anhydrase Inhibitors: Salicylates may enhance the adverse/toxic effect of Carbonic Anhydrase Inhibitors. Salicylate toxicity might be enhanced by this same combination. Management: Avoid these combinations when possible.Dichlorphenamide use with high-dose aspirin as contraindicated. If another combination is used, monitor patients closely for adverse effects. Tachypnea, anorexia, lethargy, and coma have been reported. Exceptions: Brinzolamide; Dorzolamide. Consider therapy modification

Corticosteroids (Systemic): Salicylates may enhance the adverse/toxic effect of Corticosteroids (Systemic). These specifically include gastrointestinal ulceration and bleeding. Corticosteroids (Systemic) may decrease the serum concentration of Salicylates. Withdrawal of corticosteroids may result in salicylate toxicity. Monitor therapy

Ginkgo Biloba: May enhance the anticoagulant effect of Salicylates. Management: Consider alternatives to this combination of agents. Monitor for signs and symptoms of bleeding (especially intracranial bleeding) if salicylates are used in combination with ginkgo biloba. Consider therapy modification

Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry): May enhance the adverse/toxic effect of Salicylates. Bleeding may occur. Consider therapy modification

Hyaluronidase: Salicylates may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving salicylates (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required. Consider therapy modification

Influenza Virus Vaccine (Live/Attenuated): May enhance the adverse/toxic effect of Salicylates. Specifically, Reyes syndrome may develop. Avoid combination

Loop Diuretics: Salicylates may diminish the diuretic effect of Loop Diuretics. Loop Diuretics may increase the serum concentration of Salicylates. Monitor therapy

Methotrexate: Salicylates may increase the serum concentration of Methotrexate. Salicylate doses used for prophylaxis of cardiovascular events are not likely to be of concern. Consider therapy modification

Potassium Acid Phosphate: May increase the serum concentration of Salicylates. Monitor therapy

PRALAtrexate: Salicylates may increase the serum concentration of PRALAtrexate. Salicylate doses used for prophylaxis of cardiovascular events are unlikely to be of concern. Consider therapy modification

Probenecid: Salicylates may diminish the therapeutic effect of Probenecid. Monitor therapy

Salicylates: May enhance the anticoagulant effect of other Salicylates. Monitor therapy

Sulfinpyrazone: Salicylates may decrease the serum concentration of Sulfinpyrazone. Avoid combination

Thrombolytic Agents: Salicylates may enhance the adverse/toxic effect of Thrombolytic Agents. An increased risk of bleeding may occur. Monitor therapy

Treprostinil: May enhance the adverse/toxic effect of Salicylates. Bleeding may occur. Monitor therapy

Valproate Products: Salicylates may increase the serum concentration of Valproate Products. Monitor therapy

Varicella Virus-Containing Vaccines: Salicylates may enhance the adverse/toxic effect of Varicella Virus-Containing Vaccines. Reye's Syndrome may develop. Consider therapy modification

Vitamin K Antagonists (eg, warfarin): Salicylates may enhance the anticoagulant effect of Vitamin K Antagonists. Consider therapy modification


Monitoring Parameters

Serum salicylate levels, renal function, hearing changes or tinnitus, abnormal bruising, and response (ie, pain)


Lab Test Interferences


Test Interactions

False-negative results for glucose oxidase urinary glucose tests (Clinistix ‚ ®); false-positives using the cupric sulfate method (Clinitest ‚ ®); also, interferes with Gerhardt test (urinary ketone analysis), VMA determination; 5-HIAA, xylose tolerance test, and T3 and T4; increased PBI


Adverse Reactions


Frequency not defined.

<20%:

Gastrointestinal: Constipation, diarrhea, dyspepsia, epigastric pain, heartburn, nausea, vomiting

Otic: Tinnitus

<2%:

Central nervous system: Dizziness, drowsiness, headache, lethargy

Otic: Auditory impairment

<1% (Limited to important or life-threatening): Anorexia, asthma, bruise, confusion, duodenal ulcer, dysgeusia, edema, epistaxis, erythema multiforme, esophagitis, gastric ulcer, hallucination, hearing loss (irreversible), increased blood urea nitrogen, increased liver enzymes, increased serum creatinine, occult blood in stools, pruritus, skin rash, weight gain


Warnings/Precautions


Concerns related to adverse effects:

- Gastrointestinal (GI) adverse effects: Nausea, vomiting, gastric upset, indigestion, heartburn, diarrhea, constipation, and/or epigastric pain may occur frequently.

- Tinnitus: Tinnitus is a common adverse effect; may indicate toxicity; reduce dose until tinnitus resolves.

Disease-related concerns:

- Asthma: Use with caution in patients with asthma. Non-acetylated salicylate products are associated with cross reactivity in aspirin-sensitive patients, although choline magnesium trisalicylate has been demonstrated to be well tolerated (with respect to respiratory symptoms) in patients with aspirin-sensitive asthma.

- Gastrointestinal disease: Use with caution in patients with gastritis or peptic ulcer disease. Avoid coadministration with ethanol; may enhance GI adverse effects, including GI bleeding.

- Hepatic impairment: Use with caution in patients with acute or chronic hepatic impairment.

- Renal impairment: Use with caution in patients with acute or chronic renal impairment.

Concurrent drug therapy issues:

- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

- Elderly: Use lowest effective dose for shortest period possible in the elderly; they are a high-risk population for adverse effects from salicylates/NSAIDs. Tinnitus may be a difficult and unreliable indication of toxicity due to age-related hearing loss or eighth cranial nerve damage.

- Pediatric: Children and teenagers who have or are recovering from chickenpox, influenza, or flu-like symptoms should not use salicylate products, including choline magnesium trisalicylate. Changes in behavior (along with nausea and vomiting) may be an early sign of Reyes syndrome; patients should be instructed to contact their healthcare provider if these occur.


Pregnancy Risk Factor

C


Pregnancy Considerations

Animal reproduction studies have not been conducted. Due to the known effects of other salicylates on the fetal cardiovascular system (closure of ductus arteriosus), use during late pregnancy should be avoided.


Actions


Pharmacology

Weakly inhibits cyclooxygenase enzymes, which results in decreased formation of prostaglandin precursors; 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.


Absorption

Liquid: Rapid from stomach and small intestine


Distribution

Readily distributes into most body fluids and tissues


Metabolism

Conjugated to glycine and glucuronide metabolites; the glycine conjugation pathway is rapidly saturated at higher doses.


Excretion

Urine (major route; primarily as metabolites; 10% excreted as unchanged drug); bile (minor route)


Time to Peak

Serum: Liquid: 1 to 2 hours


Half-Life Elimination

Dose dependent: Tablet: 9 to 17 hours


Protein Binding

90% to 95%


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience heartburn, nausea, vomiting, constipation, or diarrhea. Have patient report immediately to prescriber signs of liver problems (dark urine, feeling tired, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin or eyes); bruising; bleeding; severe abdominal pain; tinnitus; black, tarry, or bloody stools; vomiting blood; hearing impairment; confusion; or hallucinations (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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