Choline Salicylate

Usage

• Choline salicylate is prescribed for the relief of pain and inflammation associated with mouth ulcers, cold sores, denture sore spots, infant teething, and orthodontic appliance irritation. It also provides relief from the pain and discomfort of minor mouth and throat infections.
• Pharmacological Classification: Non-steroidal anti-inflammatory drug (NSAID), Analgesic, Anti-inflammatory, Antipyretic.
• Mechanism of Action: Choline salicylate works by inhibiting cyclooxygenase (COX) enzymes, reducing the production of prostaglandins, which are responsible for pain and inflammation.

Alternate Names

• International/Regional Variations: Choline magnesium trisalicylate (when combined with magnesium salicylate)
• Brand Names: Bonjela, Teejel

How It Works

• Pharmacodynamics: Choline salicylate exerts its analgesic and anti-inflammatory effects by inhibiting prostaglandin synthesis. The choline component may facilitate the penetration of salicylate into the oral mucosa.
• Pharmacokinetics:
  • Absorption: Rapidly absorbed through the oral mucosa.
  • Metabolism: Metabolized to salicylic acid.
  • Elimination: Primarily renal excretion of salicylic acid and its metabolites.
• Mode of Action: Inhibits COX-1 and COX-2 enzymes, decreasing prostaglandin production.
• Receptor Binding/Enzyme Inhibition: COX-1 and COX-2 enzyme inhibition.

Dosage

Standard Dosage

Adults:

• Gel: Apply a small amount (about 1 cm strip) to the affected area every three hours as needed.
• Lozenges: Allow one lozenge to dissolve slowly in the mouth every two to three hours as needed.

Children:

• Gel (over 4 months): Apply a pea-sized amount (about 0.5 cm strip) to the affected area up to every three hours, not exceeding six times in 24 hours.
• Children under 4 months: Use only as directed by a physician.

Special Cases:

• Elderly Patients: No specific dosage adjustments are typically required, but start with the lowest effective dose and monitor for adverse effects.
• Patients with Renal Impairment: Use with caution. Dose adjustments may be necessary.
• Patients with Hepatic Dysfunction: Use with caution. Dose adjustments may be necessary.
• Patients with Comorbid Conditions: Use with caution in patients with asthma, peptic ulcer disease, or bleeding disorders.

Clinical Use Cases

Choline salicylate is not typically used in clinical settings such as intubation, surgical procedures, mechanical ventilation, or the ICU. Its primary use is for localized oral pain and inflammation.

Dosage Adjustments

Dose adjustments may be necessary in patients with renal or hepatic dysfunction, as per physician guidance.

Side Effects

Common Side Effects

• Mild burning or stinging sensation at the application site.
• Temporary discoloration of the tongue or oral mucosa.

Rare but Serious Side Effects

• Allergic reactions (rash, itching, swelling).
• Salicylate toxicity (with excessive use or ingestion): nausea, vomiting, tinnitus, dizziness, hyperventilation, confusion.

Long-Term Effects

No significant long-term effects are typically associated with topical use as directed.

Adverse Drug Reactions (ADR)

• Angioedema.
• Bronchospasm.

Contraindications

• Hypersensitivity to salicylates.
• Patients with active bleeding disorders.
• Infants under 4 months of age (unless directed by a physician).

Drug Interactions

• Other NSAIDs: Increased risk of gastrointestinal bleeding or other adverse effects.
• Anticoagulants (e.g., warfarin): Increased risk of bleeding.

Pregnancy and Breastfeeding

• Pregnancy Safety Category: C (consult physician)
• Limited information is available on the safety of choline salicylate during pregnancy. Use only if clearly needed and after consultation with a physician.
• Small amounts of salicylates are excreted in breast milk. Short-term use as directed is generally considered safe, but consult a physician for extended use or concerns.

Drug Profile Summary

• Mechanism of Action: Inhibits COX enzymes, reducing prostaglandin synthesis.
• Side Effects: Burning or stinging sensation, allergic reactions (rare).
• Contraindications: Salicylate hypersensitivity, active bleeding disorders, infants under 4 months.
• Drug Interactions: Other NSAIDs, anticoagulants.
• Pregnancy & Breastfeeding: Use with caution; consult a physician.
• Dosage: Topical application to affected area as needed (see detailed dosage guidelines).
• Monitoring Parameters: Observe for local irritation or signs of salicylate toxicity (if ingested).

Popular Combinations

Choline salicylate is often combined with lignocaine for enhanced local anesthetic effect.

Precautions

• General Precautions: Avoid contact with eyes. Do not swallow the gel or lozenges. Do not use on large areas of skin or for extended periods.

• Specific Populations: Use cautiously during pregnancy and breastfeeding. Use cautiously in infants under 4 months old. Use cautiously in patients with asthma, peptic ulcers, or bleeding disorders.

• Lifestyle Considerations: No specific lifestyle considerations.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Choline Salicylate?

A: Adults: Apply a 1 cm strip of gel to the affected area every three hours as needed. Lozenges: Dissolve one lozenge slowly in the mouth every two to three hours. Children (over 4 months): Apply a pea-sized amount of gel to the affected area up to every three hours, not exceeding six times in 24 hours. Consult a physician for use in children under 4 months.

Q2: Can Choline Salicylate be used during pregnancy?

A: Consult your physician before using Choline Salicylate during pregnancy, as its safety has not been fully established.

Q3: What are the common side effects of Choline Salicylate?

A: Common side effects include a mild burning or stinging sensation at the application site and temporary discoloration of the tongue or oral mucosa.

Q4: How does Choline Salicylate work?

A: Choline salicylate inhibits COX enzymes, thereby reducing the production of prostaglandins, which cause pain and inflammation.

Q5: What should I do if I accidentally swallow Choline Salicylate gel?

A: If a significant amount of gel is swallowed, seek immediate medical attention.

Q6: Can I use Choline Salicylate with other pain relievers like ibuprofen?

A: Consult your doctor before combining choline salicylate with other NSAIDs like ibuprofen, as this may increase the risk of side effects.

Q7: Is Choline Salicylate safe for infants?

A: Choline salicylate should not be used in infants under 4 months old unless under the direction of a physician. For infants over 4 months, use a pea-sized amount of gel and do not exceed six applications in 24 hours.

Q8: How long does the pain relief from Choline Salicylate last?

A: The pain-relieving effect typically lasts for two to three hours.

Q9: Can choline salicylate be used for other types of pain?

A: Choline salicylate is specifically formulated for oral pain and inflammation. It is not recommended for other types of pain. Consult your physician for appropriate pain management options.