Usage
Choline salicylate + lidocaine is a topical combination medication primarily prescribed for the relief of pain and inflammation associated with mouth ulcers (aphthous stomatitis), denture irritation, orthodontic appliance-related sore spots, and minor mouth and gum injuries. It can also be used to provide temporary relief during infant teething (for infants older than 5 or 6 months depending on the brand).
It combines a non-steroidal anti-inflammatory drug (NSAID), choline salicylate, and a local anesthetic, lidocaine. Thus, it provides both analgesic and anti-inflammatory actions.
Alternate Names
There are no widely recognized alternate names for the combination product itself. However, it may be referred to as “choline salicylate and lidocaine.” Brand names vary by region and may include Bonjela (containing cetalkonium chloride, choline salicylate, and sometimes lidocaine), Orajel, and various generic formulations.
How It Works
Pharmacodynamics:
- Choline Salicylate: Inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis. Prostaglandins are mediators of pain and inflammation.
- Lidocaine: Blocks voltage-gated sodium channels in neuronal membranes, preventing the transmission of pain signals.
Pharmacokinetics:
- Absorption: Both drugs are absorbed through the oral mucosa upon topical application. Systemic absorption is minimal when used as directed.
- Metabolism: Choline salicylate is hydrolyzed to choline and salicylic acid, which is further metabolized in the liver. Lidocaine is also primarily metabolized in the liver by CYP enzymes.
- Elimination: Metabolites of both drugs are primarily excreted in the urine.
Dosage
Standard Dosage
Adults:
Apply a pea-sized amount (approximately 0.2g of gel containing 4mg lidocaine hydrochloride) of the gel or a small quantity of ointment to the affected area with a clean fingertip. Repeat up to four times daily, as needed. Avoid eating or drinking for at least one hour after application.
Children:
Children under 16 years of age should not use products containing choline salicylate due to a potential association with Reye’s syndrome, a rare but serious condition affecting the brain and liver. Lidocaine preparations without choline salicylate may be used for teething pain in infants 5 months or older according to product-specific instructions. Always consult with a pediatrician before using any medication in children.
Special Cases:
- Elderly Patients: No specific dose adjustments are typically required.
- Patients with Renal Impairment: Use with caution. Monitor for systemic side effects.
- Patients with Hepatic Dysfunction: Use with caution. Monitor for systemic side effects.
- Patients with Comorbid Conditions: Patients with bleeding disorders or those taking blood thinners should avoid use.
Clinical Use Cases:
The primary clinical use is for the topical treatment of mouth and gum pain and inflammation. It is not indicated for systemic conditions requiring intubation, surgical procedures, mechanical ventilation, or use in the ICU. In emergency situations, lidocaine is administered intravenously, not topically in combination with choline salicylate.
Dosage Adjustments:
Dose adjustments based on renal/hepatic dysfunction are not well-defined for topical application, but caution is advised.
Side Effects
Common Side Effects:
- Mild burning or stinging sensation at the application site
- Temporary numbness or tingling
- Changes in taste
Rare but Serious Side Effects:
- Allergic reactions (rash, itching, swelling of lips or tongue)
Long-Term Effects:
Not typically associated with long-term adverse effects when used topically as directed.
Adverse Drug Reactions (ADR):
Severe allergic reactions require immediate medical intervention. Salicylate toxicity can occur with excessive application.
Contraindications
- Hypersensitivity to salicylates, NSAIDs, lidocaine, or any components of the formulation
- Children under 16 years of age (for formulations containing choline salicylate)
- Active peptic ulcer disease
- Bleeding disorders or concomitant use of anticoagulants (e.g., warfarin)
- Aspirin-induced asthma
Drug Interactions
- Anticoagulants: May enhance the effects of anticoagulants.
- Uricosurics: May inhibit the action of uricosurics (e.g., probenecid).
- NSAIDs: Avoid concomitant use of other NSAIDs.
Pregnancy and Breastfeeding
The safety of this combination during pregnancy and breastfeeding has not been definitively established. Salicylates can cross the placenta and are present in breastmilk. Consult with a physician before use, especially during the first or second trimester or while breastfeeding.
Drug Profile Summary
- Mechanism of Action: Choline salicylate inhibits prostaglandin synthesis; lidocaine blocks sodium channels, inhibiting nerve impulse transmission.
- Side Effects: Burning, stinging, numbness, taste changes, allergic reactions.
- Contraindications: Hypersensitivity, children under 16 (with choline salicylate), peptic ulcer disease, bleeding disorders, anticoagulant use.
- Drug Interactions: Anticoagulants, uricosurics, NSAIDs.
- Pregnancy & Breastfeeding: Consult a physician before use.
- Dosage: Topical application up to four times daily.
- Monitoring Parameters: Observe for local irritation or allergic reactions.
Popular Combinations
Choline salicylate and lidocaine are commonly combined in topical gels and ointments. Some formulations also include benzalkonium chloride, an antiseptic, to prevent secondary infections.
Precautions
- Apply only to the affected area in the mouth.
- Avoid swallowing the gel.
- Do not exceed the recommended dose or frequency.
- Discontinue use and consult a doctor if symptoms persist or worsen.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Choline Salicylate + Lidocaine?
A: Apply a pea-sized amount to the affected area up to four times a day.
Q2: Can children use this medication?
A: Children under 16 should not use products containing choline salicylate. Lidocaine-only products may be suitable for teething infants, but consult a pediatrician.
Q3: What are the potential side effects?
A: Common side effects include burning, stinging, numbness, and taste changes. Allergic reactions are rare but possible.
Q4: Is it safe to use during pregnancy or breastfeeding?
A: Consult a physician before use, especially during pregnancy or breastfeeding.
Q5: What if I accidentally swallow the gel?
A: Small amounts are unlikely to cause harm, but contact a poison control center or seek medical advice if a large quantity is swallowed.
Q6: Can I use it with other pain relievers?
A: Avoid concomitant use of other NSAIDs. Consult your physician about interactions with other medications.
Q7: How long should I use it?
A: If symptoms persist for more than seven days, consult a doctor or dentist.
Q8: How should I store this medication?
A: Store in a cool, dry place away from direct sunlight and out of reach of children.
Q9: What should I do if I miss a dose?
A: Apply the missed dose as soon as you remember, but do not double the dose to catch up.
