Term
| what type of receptors are 5HT-R? |
|
Definition
| all are metabotropic, except 5HT3 - ionotropic |
|
|
Term
| 5HT-1A, drug suffix? drug action? use? examples? |
|
Definition
pirone/pidil
agonists
anxiety and hypertension
Buspirone, Urapidil |
|
|
Term
|
Definition
5HT-1A agonist
also alpha-1 adrenergic antagonist |
|
|
Term
| Buspirone, action? onset? use? |
|
Definition
5HT-1A agonist, moderate D2 affinity, 5HT-2 agonist
onset 4-6 weeks, months for full effect
chronic anxiety |
|
|
Term
| 5HT-1D/F, drug suffix? drug action? use? |
|
Definition
triptan
agonists
Migraine - cerebral vasoconstriction and anti-inflammatory |
|
|
Term
| what is the main difference between the various "triptans"? |
|
Definition
| t1/2 and metabolism - most by MAO-A, naratriptan by CYP enzymes |
|
|
Term
| what is the most efficacious triptan? administration efficacy? |
|
Definition
sumatriptan
subcutaneous > nasal > oral |
|
|
Term
| triptans are contraindicated in which patients? why? |
|
Definition
cardiovascular disease
they are vasoconstrictors and will increase BP |
|
|
Term
| what drug interactions are possible with triptans? why? |
|
Definition
MAO-I
because triptans are metabolized by MAO-A |
|
|
Term
| MAO-A metabolizes what? MAO-B |
|
Definition
|
|
Term
|
Definition
| MAO-A and B inhibitor - antidepressant |
|
|
Term
|
Definition
| MAO-A and B inhibitor - anti-Parkinsons |
|
|
Term
|
Definition
|
|
Term
|
Definition
5HT-2 antagonist and H1 antagonist
migraines |
|
|
Term
|
Definition
5HT-2 antagonist
anxiety and depression |
|
|
Term
|
Definition
5HT-2 antagonist
anxiety and depression |
|
|
Term
|
Definition
5HT2 antagonist and alpha1-blocker
hypertension, Raynaud's (spasm of femoral artery) |
|
|
Term
|
Definition
5HT2 antagonist and SSRI
antidepressant
off market - liver damage |
|
|
Term
|
Definition
5HT2 and SSRI
antidepressent
still on market |
|
|
Term
|
Definition
5HT2 antagonist and D2 blocker (equally)
antipsychotic |
|
|
Term
|
Definition
5HT2 antagonist > D2 blocker
antipsychotic |
|
|
Term
|
Definition
5HT2 antagonist >>> D2 blocker
antipsychotic |
|
|
Term
|
Definition
5HT2 antagonist and 5HT-1A agonist
antipsychotic
no weight gain or risk of torsades |
|
|
Term
| 5HT3, drug suffix, drug action, use |
|
Definition
setrons
antagonist
anti-emesis, diarrhea, IBS |
|
|
Term
|
Definition
5HT3 antagonist
extremely long acting
given i.v. once before each cycle of chemotherapy |
|
|
Term
| 5HT-4, drug suffix, drug action, use |
|
Definition
pride
agonist (increase ACh)
gastroparesis |
|
|
Term
| metoclopramide; action, use, SEs |
|
Definition
5HT-4 agonist, D2 agonist, 5HT-3 antagonist, cholinesterase inhibitor
anti-nausea and vomiting
tarditive dyskinesia |
|
|
Term
|
Definition
5HT-4 agonist
off market - interfered with K-channel blockers -> torsades |
|
|
Term
|
Definition
5HT-4 agonist
essentially cisapride w/o K-blockage |
|
|
Term
|
Definition
| delayed ejaculation and hyperthermia |
|
|
Term
| which SSRIs don't inhibit CYP P450 enzymes |
|
Definition
| citalopram and sertraline |
|
|
Term
| what is the most popular SSRI? why? |
|
Definition
| citalopram, it is the most selective for 5HT, and has minimal P450 inhibition |
|
|
Term
|
Definition
| essentially a tricyclic antidepressant without the SEs |
|
|
