Drugs inflammatory and related disorder_ drugs acting on Serotonergic systems Flashcards
(27 cards)
5HT
Serotonin (5-hydroxytrptamine)
_________ is autacoid synthesized and stored in GI cells, neurons, and platelets
Serotonin (5HT)
5HT is metabolized by ___________ and its metabolite 5-hyrdoxyinolacetic acid (5HIAA), a marker for carcinoid
MAO type A
metabolite 5-hyrdoxyinolacetic acid (5HIAA) from
serotonin
ALL serotonin are G-coupled except______ which is coupled directly to ion channel
5HT3
_________ is found in CNS (usually inhibitory) and smooth muscle (excitatory or inhibitory)
5HT1 (a-h)
partial agonists at 5HT-1a receptors
Buspirone (anxiolytic used in generalized anxiety disorder GAD))
Agonists at 5HT-1d receptors in cerebral vessels
Sumatriptan and other “triptans” (decreases migraines)
Side effects of sumatriptan and other “triptans”
possible asthenia (physical weakness, low energy), chest or throat pressure or pain
drug used for Rx of generalized anxiety disorder
buspirone
drug used for Rx of migraine
sumatriptan and other triptans
5HT2 (a-c) is found in _________ that is excitatory
CNS
5HT 2(a-c) activation in periphery leads to
vasodilation, contraction of GI, bronchial and uterine smooth muscle and platelet aggregation
Drugs acting on 5HT2 (a-c)
Olanzapine and cyproheptadine
___________ and other atypical antipsychotic are antagonists at 5HT2a receptors in CNS leading to decreased symptoms of __________
Olanzapine; psychosis
__________ 5HT2 antagonist used in carcinoid and other GI tumors and postgastroectomy; as well as anorexia nervosa and serotonin syndrome
Cyproheptadine
_____ has H1-blocking action which is used in seasonal allergy
Cyproheptadine
5HT3 is found in ________/________/__________; it works by activation of open ion channels (no 2nd messengers)
Area postrema; peripheral sensory; enteric nerves
drugs of 5HT3
ondansetron and “_setrons”
ondansetron is ___________ that decreases emesis in chemotherapy and radiation and postoperatively
Antagonists
Drugs used in migraine headaches
sumatriptan/ “_triptans” agonist at 5HT 1d; ergot alkaloids (Ergotamine)
mechanism of action of Ergotamine
acts as partial agonists at both alpha and 5HT2 receptors in vasculature and possibly in CNS; it has vasoconstrictive actions to decreased pulsation in cerebral vessels relevant to acute actions of ergotamine (rx migraine attack)
Uses of ergotamine
acute attacks (migraine and others)
Side effects of ergotamine
GI distress; prolonged vasoconstriction leading to ischemia and gangrene, abortion near term