Choline magnesium trisalicylate is a type of nonsteroidal anti-inflammatory drug (NSAID) that is used to reduce pain, inflammation, and fever. Unlike more commonly known NSAIDs such as ibuprofen and aspirin, choline magnesium trisalicylate does not inhibit cyclooxygenase (COX) enzymes as significantly, potentially offering a different side effect profile, particularly regarding gastrointestinal irritation and platelet aggregation.

Trilisate (Choline magnesium trisalicylate) inhibits the cyclooxygenase enzyme, resulting in the inhibition of prostaglandins. It is used to treat the following conditions:

• Mild to moderate pain
• Fever
• Acute painful conditions like mild arthritis.

Choline magnesium trisalicylate Dose in Adult

Note: When taking this medication, it's important to adjust the dose based on how much relief you get from it, and it might take 2 to 3 weeks to feel the full benefit.

Choline magnesium trisalicylate For Acute painful conditions:

• Is typically administered orally in a starting dose of 1.5 grams twice daily or 3 grams once daily at bedtime.
• This dosage helps manage pain and inflammation associated with these conditions.

Choline magnesium trisalicylate For Mild to moderate pain as an analgesic and antipyretic:  

• Is typically taken orally at a dose of 2 to 3 grams per day, divided into 2 or 3 doses.
• It's important to adjust the dosage as needed to achieve the best pain relief or fever reduction while minimizing side effects.

Choline magnesium trisalicylate Dose in Children

Note: When taking this medication, it's important to adjust the dose based on how much relief you get from it, and it might take 2 to 3 weeks to feel the full benefit.

Choline magnesium trisalicylate for Mild to moderate pain in inflammatory conditions:

Manufacturer's Labeling:

Weight-Directed Dosing:

• Children weighing ≤37 kg: The recommended dose is 25 mg/kg, taken orally twice daily.

Fixed-Dosing (Weight-Band):

• 12 to 13 kg: 250 mg twice daily
• 14 to 17 kg: 375 mg twice daily
• 18 to 22 kg: 500 mg twice daily
• 23 to 27 kg: 625 mg twice daily
• 28 to 32 kg: 750 mg twice daily
• 33 to 37 kg: 875 mg twice daily
• Children weighing >37 kg: The recommended dose is 1,125 mg taken orally twice daily.

Alternate Dosing (Limited Data):

According to a source such as Kliegman 2016, an alternate dosing regimen can be:

• Oral: 10 to 20 mg/kg per dose every 8 to 12 hours, depending on the specific needs and response of the child.

It’s crucial to follow the dosing guidelines and adjust as necessary based on the child's response and any side effects.

Pregnancy Risk Factor C

• Choline magnesium trisalicylate is categorized as Pregnancy Risk Factor C, which means there hasn't been sufficient research on its effects during pregnancy in animals or humans.
• However, because other similar medications, known as salicylates, have been shown to potentially harm the developing fetus by affecting the cardiovascular system (specifically by closing a vital blood vessel called the ductus arteriosus), it is advised to avoid using this medication during the later stages of pregnancy to prevent possible risks to the unborn baby.

Trilisate use during breastfeeding:

• Choline magnesium trisalicylate can pass into breast milk, and its highest levels are typically reached between 9 to 12 hours after taking a dose.
• Because of this, caution is advised when breastfeeding mothers take this medication.
• While there's no specific data on the potential effects on infants, it's generally recommended to be careful.

Choline magnesium trisalicylate Dose in Renal Disease:

• The manufacturer's instructions do not include specific dosage adjustments for choline magnesium trisalicylate in cases of renal impairment.
• However, caution should be exercised when using this medication in individuals with either acute or chronic kidney problems.

Choline magnesium trisalicylate Dose in Liver Disease:

• The manufacturer's guidelines for choline magnesium trisalicylate do not specify dosage adjustments for individuals with hepatic (liver) impairment.
• However, it's recommended to exercise caution when using this medication in individuals with either acute or chronic liver issues.

Common Side Effects of trilisate:

• Otic:
  • Tinnitus
• Gastrointestinal:
  • Nausea
  • Vomiting
  • Dyspepsia
  • Epigastric pain
  • Constipation
  • Diarrhea
  • Heartburn

Less Common Side Effects:

• Otic:
  • Auditory impairment
• Central nervous system:
  • Headache
  • Dizziness
  • Drowsiness
  • Lethargy

Contraindications to Trilisate include:

• Individuals who have a hypersensitivity or allergic reaction to choline magnesium trisalicylate, other nonacetylated salicylates, or any component of the medication's formulation should avoid its use.
• Hypersensitivity reactions can range from mild symptoms like rash or itching to more severe reactions such as difficulty breathing or swelling of the face, tongue, or throat.

Warnings and Precautions

Gastrointestinal (GI) adverse effects:

• Gastrointestinal (GI) adverse effects are common with choline magnesium trisalicylate and may include nausea, vomiting, stomach upset, indigestion, heartburn, diarrhea, constipation, and/or epigastric pain.
• These symptoms can occur frequently and may vary in severity from person to person.

Tinnitus

• Tinnitus, or ringing in the ears, is a common side effect associated with choline magnesium trisalicylate.
• It can sometimes indicate medication toxicity.

Asthma

• Choline magnesium trisalicylate should be used cautiously in patients with asthma.
• While non-acetylated salicylate products like choline magnesium trisalicylate are generally considered to be better tolerated in individuals with aspirin-sensitive asthma compared to aspirin, there is still a risk of cross-reactivity.

Gastrointestinal Disease:

• In patients with gastritis or peptic ulcer disease, choline magnesium trisalicylate should be used cautiously.
• The medication can potentially exacerbate symptoms or lead to worsening of these conditions.

Hepatic impairment

• Choline magnesium trisalicylate should be used cautiously in patients with acute or chronic hepatic (liver) impairment.
• While specific dosage adjustments are not provided in the manufacturer's labeling, individuals with liver issues may be at an increased risk of adverse effects from the medication.

Renal impairment

• Choline magnesium trisalicylate should be used cautiously in patients with acute or chronic renal (kidney) impairment.

Choline magnesium trisalicylate: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring Parameters:

• Serum Salicylate Levels: Regular checks of salicylate levels in the blood are important to ensure they stay within safe limits.
• Renal Function: Monitoring kidney function is crucial, especially in individuals with kidney issues, to prevent any adverse effects on the kidneys.
• Hearing Changes or Tinnitus: Pay attention to any changes in hearing or the development of tinnitus (ringing in the ears), as these could indicate medication toxicity.
• Abnormal Bruising: Keep an eye out for unusual bruising, as it may signal potential bleeding issues related to the medication.
• Response (Pain): Assess how well the medication is managing pain. Adjustments to the dosage may be necessary based on individual response.

How to administer Choline magnesium trisalicylate?

• With Food or Fluids: Take the medication with food or a large volume of water or milk to reduce the risk of gastrointestinal (GI) upset.
• Mixing with Fruit Juice: If taking the liquid form, it can be mixed with fruit juice just before drinking to make it more palatable.

These measures can help improve tolerance and reduce the likelihood of experiencing GI discomfort when taking choline magnesium trisalicylate.

Mechanism of action of Choline magnesium trisalicylate (trilisate):

• Choline magnesium trisalicylate weakly inhibits cyclooxygenase enzymes, which are involved in the formation of prostaglandin precursors.
• This action leads to reduced inflammation and pain, making it useful as an antipyretic (fever reducer), analgesic (pain reliever), and anti-inflammatory agent.
• Additionally, it may exert its effects through other mechanisms that are not fully understood, such as inhibiting chemotaxis (movement of cells toward inflammation), altering lymphocyte activity, inhibiting neutrophil aggregation and activation, and reducing levels of proinflammatory cytokines.
• These various actions collectively contribute to its anti-inflammatory effects, although the exact extent of each mechanism's contribution is not fully elucidated.

Absorption:

• Liquid Form: Choline magnesium trisalicylate is rapidly absorbed from the stomach and small intestine.

Distribution:

• It easily spreads throughout most body fluids and tissues once absorbed.

Protein Binding:

• Approximately 90% to 95% of the medication binds to proteins in the blood.

Metabolism:

• It undergoes metabolism in the body, primarily being converted into glycine and glucuronide metabolites.
• The pathway involving glycine conjugation becomes saturated at higher doses.

Half-Life Elimination:

• For tablets, the half-life ranges from 9 to 17 hours, with duration depending on the dose.

Time to Peak Serum Levels:

• When taken in liquid form, it reaches peak serum levels within 1 to 2 hours after ingestion.

Excretion:

• The major route of excretion is through urine, primarily as metabolites, with only about 10% excreted unchanged.
• A minor amount is excreted via bile.

Choline magnesium trisalicylate Brands in Pakistan: