Pharm 101: Sumatriptan

Class

Serotonin agonist


Pharmacodynamics
  • Structural analogue of 5-HT
  • Selective 5-HT (1D/1B) agonist
    • These receptors are found in cerebral and meningeal vessels and mediate vasoconstriction
    • May reduce release of calcitonin gene-related peptide and perivascular edema in cerebral circulation

Pharmacokinetics
  • Administration: PO, SC, IN, PR
  • Bioavailability 15%
  • Time to onset: 1.5 hours (0.2 hours for SC)
  • Half-life 2 hours
    • Short duration of action, often shorter than duration of headache, therefore several doses may be required during prolonged attack

Clinical uses
  • First line for acute severe migraine

Adverse effects
  • Altered sensations (tingling, warmth)
  • Dizziness
  • Muscle weakness
  • Neck pain
  • Injection site reactions with parenteral administration
  • Chest discomfort in 1-5%, probably due to coronary vasospasm

Contraindications
  • Ischaemic heart disease or angina (due to coronary vasospasm)
  • Caution with co-administration of other vasoconstrictors

Further reading

References

Pharm 101 700

Pharmacology 101

Top 200 drugs

MBBS (UWA) CCPU Emergency Medicine Trainee based in Melbourne, Australia. Co-author of the LITFL ECG Library. Likes Ultrasound, Echo, ECGs, and anything and everything with caffeine | Twitter | ECG Library |

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