Drugs use in Migraine and Other

Primary Headache
Dr. Pagan Pambudi, M.Si, Sp.S
 Primary headache
• Tension type headache
• Migraine
• Cluster headache and trigemianl autonomic
cephalgia
• Other primary headache
 Migraine patophysiology
Neurogenic
SP/CGRP
inflamation

MAST CELL NERVE TERMINAL SENS/

ACTIVATION FLUID EXTRAVASATION IN
DURAL VESSEL

PG
NO BRAD

C-fos induction in
trigeminal nucl
caudalis
NOCICEPTOR
SENSITIZATION

CORTICAL SPREADING
Migraine Patophysiology
 Drugs used in Migraine
• Abortion
– NSAID, NSAID + caffeine
– Ergot
– Triptans
• Prevention
– AED
– Beta blockers
– Antidepresant
– CCB
 Triptans
• Mechanism of Action
– Serotonin receptor 5HT-1B/D agonist
• Vasoconstriction cerebral vascular bed
• block the release of proinflammatory neuropeptides at
the level of the nerve terminal in the perivascular space
 Triptans Pharmacokinetics
Sumatriptan Zolmitptan Naratriptan Rizatriptan
Route Oral, oral oral oral
intranasal, SC
BA Oral, nasal: 40% 45% 70%
14%, SC 97%
Peak 1-2 hrs 1,5-2 hrs 2-3 hrs 1-1,5 hrs
Active metab No yes No No
Dose 6 mg sc, 5-20 1,25-2,5 mg 1-2,5 mg/day 5-10 mg
mg nasal repeat 2 hrs repeat in 4 repeat after2
spray max 10 hrs max 5 rs, max 30
mg/day mg/day mg/day
 Triptans Adverse Effects
• coronary artery vasospasm, transient
myocardial ischemia, atrial and ventricular
arrhythmias, and myocardial infarction,
predominantly in patients with risk factors for
coronary artery disease
 Triptans Contraindication
• a history of ischemic or vasospastic coronary
artery disease,
• cerebrovascular
• or peripheral vascular disease,
• or other significant cardiovascular diseases
• uncontrolled hypertension
• who are taking monoamine oxidase inhibitors
• Renal failure
 Ergots and Ergot alkaloids
• MOA:
– 5-HT1B/1D receptors agonist
• should be restricted to patients having
frequent, moderate migraine or infrequent,
severe migraine attacks. As with other
medications used to abort an attack, the
patient should be advised to take ergot
preparations as soon as possible after the
onset of a headache.
 Ergot Alkaloids
• Pharmacokinetics
– Gastrointestinal absorption of ergot alkaloids is erratic
– Metabolized by liver, extensive first pass metabolism
– Excreted by bile
• SE
– Nausea and vomiting
– Numbness and tingling
– transient tachycardia or bradycardia
 Ergot Alkaloids
Contraindications
• Pregnancy
• Peripheral vascular disease

Dosage
• Ergotamine 2 mg SL repeat 30 min, max 6 mg day or 10
mg/weeks
• Dehydroergotamine:
– IV : 2 mg IV repeat 1 hrs max 6 mg/day, 10 mg/weeks
– IM/SC: 3 mg
– Intranasal: 0,5 mg each, repeat 15 min, max 2 mg/day, 4
mg/weeks
 Other drugs can be used in headache
• Indometachine  especially esee in NSAID
lecture
• Barbiturates  see in Hipnotics sedatives lect
• Opioids  see Analgesics lecture
 Drugs Overuse headache
• Headache present on >15 days/month
• Regular overuse for > 3 months of one or more
acute/symptomatic treatment drugs as defined
– Ergotamine, triptans, opioids, or combination analgesic
medications on ≥10 days/month on a regular basis for >3
months
– Simple analgesics or any combination of ergotamine,
triptans, analgesics opioids on ≥ 15 days/month on a
regular basis for > 3 months without overuse of any single
class alone
• Headache has developed or markedly worsened during
medication overuse
Thanks