Eletriptan

Eletriptan is a second-generation triptan. It has good CNS penetration.

The medication is of particular interest for patients in whom other triptans are not sufficiently effective. Tolerability is good, and the rate of side effects is comparable to that of other triptans.

The well-known brand name is Relpax®.

Eletriptan acts as a highly selective serotonin agonist:

Mechanism of action:

• High affinity for 5-HT1B/1D receptors
• Constriction of dilated cranial blood vessels
• Inhibition of CGRP release
• Blockade of trigeminal pain signals

Special features:

• High selectivity for the relevant receptors
• Good lipophilicity – penetrates well into the CNS

Onset of action:

• 30 minutes to 1 hour
• Plasma half-life: about 4 hours
• The headache can come back within 24 hours after responding to treatment

Eletriptan is suitable for:

• Adults with acute migraine attacks
• Patients in whom other triptans are not sufficiently effective
• Severe migraine attacks

Particularly suitable for:

• Non-responders to other triptans
• Frequent recurrence of headaches

Not suitable in cases of:

• Cardiovascular diseases
• Severe liver impairment
• Concomitant use of strong CYP3A4 inhibitors

Tablets:

• 20 mg
• 40 mg (standard dose)

Recommended dosage:

• Standard dose: 40 mg
• If 40 mg does not work well enough in an adequate treatment trial (e.g. no response in 2 out of 3 attacks with good tolerability): 80 mg (2 × 40 mg) for the following attacks
• If the headache comes back within 24 hours after responding to treatment: a further dose of the same strength, at the earliest 2 hours after the first
• No second 80 mg dose within 24 hours
• Maximum: 80 mg in 24 hours

How to take:

• Take at the onset of the headache
• Swallow with water
• Regardless of meals
• Not during the aura

Timing:

• Taking it early improves the effect
• If the headache returns: repeat after 2 hours
• If the first dose is ineffective: no second dose for the same attack

Eletriptan must not be taken in cases of:

• Coronary heart disease, vasospasms
• History of heart attack, stroke, TIA
• Peripheral arterial occlusive disease
• Severe or uncontrolled hypertension
• Severe liver impairment
• Hemiplegic or basilar migraine
• Concomitant use of strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, ritonavir)
• Use of ergotamine (24h interval)

Caution in cases of:

• Moderate liver impairment
• Cardiovascular risk factors

Common (1-10%):

• Dizziness
• Lightheadedness
• Fatigue, asthenia
• Paresthesias
• Headache

Triptan-specific sensations:

• Feeling of warmth
• Feeling of tightness in the chest/throat
• Tingling, numbness
• Feeling of pressure

Uncommon:

• Palpitations
• Hypertension
• Dry mouth
• Abdominal pain

Rare:

• Coronary spasms
• Allergic reactions

Contraindicated with:

• Strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, ritonavir, nelfinavir)
• Ergotamine (24h interval)
• Other triptans on the same day

Caution with:

• Moderate CYP3A4 inhibitors (erythromycin, verapamil, fluconazole)
• SSRI/SNRI (serotonin syndrome)
• Propranolol (slight increase in eletriptan levels)