Drug MOA (Semester List) Flashcards
SSRI
Block presynaptic 5-HT reuptake pump –> INC synaptic 5-HT
SNRI
Psych: inhibitor 5-HT & NE
Pain mgmt: unknown
SSRI & Partial 5-HT1A Rec AG
Inhibit serotonin reuptake & AG of 5-HT1A rec
Bupropion
MOA not fully understood, somewhat stimulating
Blocks NE & DA uptake
Trazadone
- AAG at 5-HT2A & 2C rec (hypnotic effect?)
- SSRI
- AAG at H1 (sedation) and a1 rec (postural hypoTN)
Mirtazapine
- AAG of central pre/post synaptic a2 rec (INC NE) & 5HT2/3 (INC serotonin)
- Potent H1 rec AAG (sedation)
TCA - Tertiary Amines
SSRI-like: INC synaptic serotonin concentration +/- NE in CNS by inhibiting reuptake
Other:
- a1 (orthostasis)
- histaminic (sedation, wt gain)
- muscarinic (anticholinergic)
TCA - Secondary Amines
More SNRI-like: INC synaptic NE in CNS by inhibiting reuptake
Hits same receptors as tertiary amines (a, h, m) but less interaction
MOAI-A
INC all endogenous (NE, DA, 5-HT) through inhibition of MAO
MOAI-B
DA
Barbiturates
Modulate GABA system
BZD
Bind BZD receptor on post-synaptic GABA neuron –> potentiates endogenous GABA (main inhibitory NT)
Shift in Cl- ions results in hyperpolarization & stabilization
Lithium
Uncertain MOA
Alters cation transport across cell membrane in nerves, muscle cells.
Influences reuptake of 5-HT +/- NE
1st Gen Antipsychotics
AAG of postsynaptic mesolimbic DA receptors
AAG of:
- alpha (orthostasis)
- histaminic (sedation, wt gain)
- muscarinic (anticholinergic)
2nd Gen Antipsychotics
Additional AAG
- alpha
- histaminic
- muscarinic
2nd Gen Antipsychotics
AAG of 5HT2 & D4
Clozapine
2nd Gen Antipsychotics
AAG of 5HT2
Risperidone Olanzapine Quetiapine Ziprasidone Paliperidone Asenapine Iloperidone Lurasidone
2nd Gen Antipsychotics
Partial AG at D2 & 5HT1A
and
AAG 5HT2A
Aripiprazole
Brexpiprazole
Cariprazine
1st Gen Antihistamine
Anticholinergic
NBRAs
AG on GABA-A rec complexes (close to or coupled w/BZD1 rec)
Minimal AG of BZD2 receptor = minimal anxiolytic, myorelaxant, anticonvulsant properties
Melatonin Receptor AG
Selective AG of melatonin rec MT1 > MT2 w/in suprachiasmatic nucleus of hypothalamus
M1: induce sleepiness
M2: influences regulation of sleep-wake cycle
Orexin Rec AAG
Block orexin neuropeptides from binding to their receptors - prevents “wakefulness”
Stimulants (ADHD)
INC NE, DA in BS, midbrain, frontal cortex
Methylphenidate
Block reuptake of NE/DA into presynaptic neurons in CNS - INC concentration in synapse
Amphetamine
Promote release of NE/DA from vesicles in presynaptic nerve terminals
Atomoxetine
SNRI
Guanfacine
Selective a2A AG
Clonidine
NON-selective a2A, B, C, and imidazoline rec AG [non-selective alpha modulator]