Paresthesias, dizziness, coronary vasoconstriction • Interactions: Additive with other vasoconstrictors • Other triptans (almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, zolmitriptan): Similar to sumatriptan except for pharmacokinetics (2–6 h duration of action); much more expensive than generic sumatriptan
Subclass, Drug Mechanism of Action Effects Clinical Applications Pharmacokinetics, Toxicities, Interactions SEROTONIN BLOCKERS 5-HT2: 5-HT3: • Ondansetron, others (see Chapter 62) •ErgotamineMixed partial agonist effects at 5-HT2 and α adrenoceptors Causes marked smooth muscle contraction but blocks α-agonist vasoconstriction Migraine and cluster headache Oral,parenteral•duration12–24h•Toxicity: Prolonged vasospasm causing angina, gangrene; uterine spasm Uteroselective: •ErgonovineMixed partial agonist effects at 5-HT2 and α adrenoceptors Sameasergotamine•someselectivity for uterine smooth muscle Postpartum bleeding •migraineheadacheOral,parenteral(methylergonovine)•duration2–4h•Toxicity: Same as ergotamine CNS selective: •Lysergicaciddiethylamide Central nervous system 5-HT2 and dopamine agonist •5-HT2 antagonist in periphery Hallucinations •psychotomimeticNone•widelyabused Oral•durationseveralhours•Toxicity: Prolonged psychotic state, flashbacks • Bromocriptine, pergolide: Ergot derivatives used in Parkinson’s disease (see Chapter 28) and prolactinoma (see Chapter 37). Pergolide used in equine Cushing’s disease
Azelastine Generic, Astelin (nasal), Optivar (ophthalmic)
Brompheniramine Brovex, Dimetapp, others
Carbinoxamine Generic, Histex
Cetirizine Generic, Zyrtec
Chlorpheniramine Generic, Chlor-Trimeton
Clemastine Generic, Tavist
Cyclizine Generic, Marezine
Cyproheptadine Generic, Periactin
Desloratadine Generic, Clarinex
Dimenhydrinate† Generic, Dramamine
Diphenhydramine Generic, Benadryl
Doxylamine Diclegis (combination with pyridoxine), Unisom Sleep Tabs
Fexofenadine Generic, Allegra
Hydroxyzine Generic, Vistaril
Ketotifen Generic, Zaditor
Levocetirizine Generic, Xyzal
Loratadine Generic, Claritin
Meclizine Generic, Antivert, Bonine
Olopatadine Patanol, Pataday
Promethazine Generic, Phenergan
Triprolidine Generic, Zymine, Tripohist
Epinastine Generic, Elestat