Pharmacological Management of Orofacial Pain

I. Types of Orofacial Pain

  • Nociceptive Pain: Caused by actual or threatened tissue damage. Common origins are odontogenic (teeth) and musculoskeletal (TMJ disorders).

  • Neuropathic Pain: Caused by a lesion or disease of the somatosensory nervous system. Examples include trigeminal neuralgia and burning mouth syndrome (BMS). Often involves central sensitization (CNS changes).

  • Nociplastic Pain: Pain without evidence of tissue damage, but with central sensitization. Fibromyalgia is a classic example; often mimics nociceptive and neuropathic pain.

  • Acute Pain: Short-term, associated with tissue damage.

  • Chronic/Persistent Pain: Long-lasting, not necessarily linked to ongoing tissue damage; more related to changes in the nervous system.

II. Pharmacological Management: Key Medications

Medication

Indication(s)

Mechanism of Action

Dosage (example)

Absolute Contraindications

Relative Contraindications

Adverse Effects

Amitriptyline

TMD, neuropathic pain, headache disorders

Non-selective monoamine reuptake inhibitor; blocks Na+, K+, Ca2+ channels; enhances GABA.

10-25mg OD (PM)

Heart block, MI aftermath, arrhythmias, bipolar mania, hypersensitivity

Diabetes, epilepsy, bipolar disorder, liver disease, hyperthyroidism, glaucoma, suicide risk. Careful use in elderly or those with cardiovascular disease.

Drowsiness, xerostomia, blurred vision, increased ocular pressure, urinary retention

Nortriptyline

TMD, neuropathic pain

Inhibits noradrenaline reuptake; blocks Na+, K+, Ca2+ channels.

10-25mg OD (PM)

Heart block, MI aftermath, arrhythmias, bipolar mania, hypersensitivity

Similar to Amitriptyline

Drowsiness (less than amitriptyline), xerostomia, increased appetite

Gabapentin

Neuropathic pain, TMD

Interacts with α2δ Ca2+ channels; increases GABA synthesis & release.

Initially 300mg OD

Hypersensitivity

Diabetes, psychotic illness, substance dependence, seizures, low weight, pregnancy, elderly, respiratory compromise, neurological disease.

Confusion, weight gain, xerostomia, constipation, diarrhea, visual impairment, hypertension. Risk of substance misuse.

Pregabalin

Neuropathic pain

Binds to Ca2+ channels; reduces Ca2+ influx; decreases neurotransmitter release (glutamate, substance P).

150mg daily

Hypersensitivity

Epilepsy, glaucoma, hepatic or renal conditions, psychiatric illness, uncontrolled hypertension, substance dependence.

Confusion, weight gain, xerostomia, constipation, diarrhea, visual impairment, hypertension. Risk of substance misuse.

Duloxetine

Neuropathic pain

Inhibits serotonin & norepinephrine reuptake.

20-30mg OD (titrate)

Epilepsy, glaucoma, hepatic or renal impairment, psychiatric illness, uncontrolled hypertension, hypersensitivity

Elderly, hypovolemic patients, bleeding disorders, cardiac conditions

Nausea, vomiting, cardiovascular effects, hypertension, sexual dysfunction, hepatic damage

Carbamazepine

Trigeminal neuralgia (first-line)

Na+ and Ca2+ channel blocker; metabolite limits repetitive neuronal firing.

100mg OD-BD

Acute porphyrias, AV conduction abnormalities, bone marrow depression, hypersensitivity, HLA-B*1502 allele

Cardiac conditions, bleeding disorders, skin reactions, glaucoma, seizures, liver disease.

Weight gain, nausea, vomiting, dizziness, drowsiness, xerostomia, fatigue, blood abnormalities, SJS/TEN.

Oxcarbazepine

Trigeminal neuralgia

Blocks Na+ channels.

150mg OD (titrate)

Acute porphyrias, heart failure, cardiac conduction abnormalities, hyponatremia, hypersensitivity, HLA-B*1502 allele

Liver and renal impairment, breastfeeding, pregnancy.

Abdominal pain, nausea, dizziness, drowsiness, emotional liability, impaired concentration, SJS/TEN.

Baclofen

Trigeminal neuralgia, TMD

GABAB receptor agonist; decreases neurotransmitter release; increases K+ conductance.

5mg TDS (titrate)

Active peptic ulceration, hypersensitivity

Cardiovascular disease, diabetes, epilepsy, history of peptic ulcers, Parkinson’s disease, respiratory impairment.

Confusion, xerostomia, hypotension, nausea, dizziness, drowsiness, headaches.

Lamotrigine

Trigeminal neuralgia

Na+ and Ca2+ channel blocker; stabilizes neuronal membranes; decreases glutamate; enhances GABAergic transmission

25mg OD (titrate)

Hypersensitivity

Parkinson's disease, myoclonic seizures, hepatic/renal impairment.

Drowsiness, fatigue, nausea, headaches, xerostomia, agitation, sleep disorders, SJS/TEN.

Alpha-Lipoic Acid

BMS

Antioxidant.

200mg TDS

Hypersensitivity

Possible interactions with cisplatin, cyclophosphamide, gentamicin, and amikacin.

Low blood sugar, vision changes (rare), urticaria (rare).

Lidocaine HCl

Acute rescue (trigeminal neuralgia), post-herpetic neuralgia

Amino-amide local anesthetic; reduces Na+ influx.

Topical application

Hypersensitivity

Inflamed/infected tissues, avoid near middle ear.

Hypotension, edema, irritation, nausea, vomiting, numbness, tingling, drowsiness, tremor, arrhythmia, methemoglobinemia

Benzydamine HCl

Inflammatory conditions (oral)

Weak inhibitor of prostaglandin & TNF-α synthesis; membrane stabilizer.

0.15% mouthwash

Hypersensitivity

Potential systemic interactions.

Angioedema, photosensitivity, respiratory disorders, skin reactions.

Capsaicin

BMS

Activates TRPV1 receptors; depletes substance P.

Topical application

None known

Caution with hypertension or recent cardiovascular events.

Burning, abnormal sensations to the area of skin applied.

Clonazepam

BMS

Enhances GABA activity.

500µg, dissolve in mouth

Myasthenia gravis, acute pulmonary insufficiency, neuromuscular respiratory weakness, alcohol/drug dependence, respiratory depression, hypersensitivity

Personality disorders, elderly (reduced dose).

Drowsiness, increased oral burning, xerostomia.

III. Additional Considerations

  • Medication Overuse Headache: Regular use of simple analgesics (paracetamol, NSAIDs) or codeine can lead to this condition.

  • Simple Analgesia: Paracetamol is usually first-line for acute, mild-to-moderate pain; NSAIDs (like ibuprofen) may be added if needed. Opioids are considered for short-term use only and usually as a last resort.

  • Combination Analgesics: Combining different analgesics (e.g., paracetamol and ibuprofen) may be more effective than using a single agent.

  • Off-label Prescribing: Many of the drugs are prescribed "off-label" for orofacial pain, meaning not specifically licensed for the condition. It is crucial for clinicians to document this, justify the rationale, and inform the patient.

  • Drug Interactions: Be aware of potential interactions with other medications a patient may be taking.

  • Driving: Many medications can impair cognitive function and driving ability; inform patients of the risks and requirements for reporting to driving regulatory bodies (like the DVLA in the UK).

  • Biopsychosocial Approach: A holistic approach is vital, including psychological and social factors in addition to the physical aspects.

  • Tapering Medications: When discontinuing long-term medications, especially those with dependence potential, gradually reduce the dose over several weeks to minimize withdrawal symptoms.