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BMS60048
Drugs acting on Serotonin Receptors and Pumps
| Question | Answer |
|---|---|
| what is the only ionotropic 5-HT receptor? | 5-HT3 |
| 5-HT 1A receptors (agonist/antagonists; suffix; tx) | agonist; -pirones and -pidil; anxiety and hypertension |
| 5-HT 1D/1F receptors (agonist/antagonists; suffix; tx) | agonist; -triptans; migranes |
| 5-HT 2 receptors (agonist/antagonists; tx) | antagonist; psychosis |
| 5-HT 3 receptors (agonist/antagonists; suffix; tx) | antagonist; -setrons; emesis |
| 5-HT 4 receptors (agonist/antagonists; suffix; tx) | agonist; -prides; gastroparesis |
| urapidil | 5-HT 1A agonist; alpha1 receptor antagonist => vasodilation, lowers BP |
| buspirone | 5-HT 1A partial agonist; also has some D2 and weak 5-HT2 affinity; anti-anxiety and restlessness; onset of effect is slow and full effect may take months; not useful for acute attacks but good for long term; low chance of addiction |
| triptans | 5-HT1 D/F agonist; b/f - arterial/cerebral vasoconstriction; d - reduce nociceptive transmission (inflammatory soup); used for migraines |
| what is the first generation triptan? | sumatriptan |
| what is the major difference between the later generation triptans and the older ones? | the later generations have longer t1/2 |
| which triptan is not metabolized via MAO-A? | naratriptan with CYP450 |