zolmitriptan (Zomig)

Introduction

Tradename: Zomig.

Indications

migraine headache

Contraindications

• ischemic heart disease
• Prinzmetal's angina
• concurrent use of MAO inhibitors

Dosage

• start 2.5 mg every 2 hours PRN
• 1 spray (5 mg)
• maximum 10 mg QD

Tabs: 2.5 mg (yellow) & 5 mg (pink) (store at room temp; protect from light & moisture)

Zomig ZMT: oral disintegrating tablets

Nasal spray: 5 mg

No dose adjustment for renal failure needed

Pharmacokinetics

• well absorbed after oral administration
• onset of action:
  • 15 minutes (nasal spray)
  • 30 minutes (tablet)
• peak concentration in serum (8 ng/mL) reached 2 hours after oral administration
• metabolized in the liver to N-desmethyl derivative
  • N-desmethyl derivative is 2-6 times as active as the parent compound
  • 1/2 life of the N-desmethyl derivative is 3 hours

elimination via liver

1/2life = 3 hours

protein binding = 25 %

Adverse effects

(similar to other triptans)

• dizziness
• asthenia
• paresthesia
• drowsiness
• limb heaviness
• nausea
• throat or neck tightness/pressure
• coronary vasoconstriction has been reported
• frequent use may exacerbate migraines
• bad taste

• drug adverse effects of triptan(s)

Mechanism of action

• 5-HT 1B & 1D receptor agonist

More general terms

• serotonin agonist (5-HT receptor agonist, triptan)
• heterocyclic compound, 2 rings
• amine

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=60857
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=441240
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5731