Do triptans (e.g. sumatriptan, rizatriptan) cause an intermittent burning sensation in the brain?

Triptans and Burning Sensations in the Brain

Triptans do not specifically cause an intermittent burning sensation in the brain, but they can cause various sensory disturbances as side effects. 1

Common Triptan Side Effects

• Triptans are generally well-tolerated when used appropriately, but they do cause a range of sensory symptoms often referred to as "triptan symptoms" 2
• Common sensory disturbances include:
  • Tingling sensations 2
  • Sensations of warmth 2
  • Chest pressure or heaviness 1
  • Paresthesias (abnormal sensations) 1

Mechanism of Action and CNS Effects

• Triptans work as 5-HT1B/1D receptor agonists that:

  • Decrease neurogenic inflammation in the meninges 3
  • Cause vasoconstriction of meningeal vessels 3
  • Modulate second-order neurons in the brainstem 3
  • Block synaptic transmission between peripheral and central trigeminovascular neurons 4

• CNS side effects vary among different triptans based on:

  • Lipophilicity (ability to cross the blood-brain barrier) 5
  • Presence of active metabolites 5
  • Individual triptan pharmacokinetic properties 5

Triptan Selection and Side Effect Profiles

• At clinically relevant doses, the incidence of CNS side effects varies by medication:

  • Lower incidence: almotriptan 12.5mg, naratriptan 2.5mg, sumatriptan 50mg 5
  • Higher incidence: eletriptan 40-80mg, rizatriptan 10mg, zolmitriptan 2.5-5mg 5

• The most likely explanations for differences in CNS side effects among triptans are:

  • Presence of active metabolites (eletriptan, rizatriptan, and zolmitriptan have these) 5
  • Lipophilicity (lowest for almotriptan and sumatriptan) 5

Clinical Considerations

• If a patient experiences unpleasant sensory disturbances with one triptan, trying a different triptan may be beneficial 1
• Patients should try a medication for 2-3 headache episodes before abandoning that line of therapy 1
• If sensory disturbances are a concern, consider using triptans with lower lipophilicity and no active metabolites 5
• Triptans are contraindicated in patients with:
  • Ischemic vascular conditions 1
  • Vasospastic coronary disease 1
  • Uncontrolled hypertension 1
  • Other significant cardiovascular disease 1

Important Considerations for Perioperative Management

• If a patient is scheduled for surgery, triptans should be taken preoperatively but held on the day of operation 1
• This recommendation is based on theoretical concerns regarding drug-drug interactions with commonly used perioperative medications 1