Term
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Definition
neurotransmitter that modulate mood, sleep rate cycle, motivation, pain perception
-starts as tryptophan
5 choices:(auto) 5ht1D receptor
reuptaken into neuron broken down by MAO
post synpatic receptor
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Term
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Definition
building block: tyrosine
synthesized into dopamine
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Term
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Definition
| causes increased appetite improved sleep improved mood |
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Term
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Definition
| 5ht receptor that specifically improves mood |
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Term
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Definition
| 5ht receptor with s/e of increased anxiety sexual dysfunction sleep disturbances |
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Term
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Definition
receptor for NE -increased interest energy concentration, mood
s/e: increased hr bp anxiety |
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Term
| tricyclic antidepressants |
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Definition
| non-selective, prevents inhibiting serotonin and norepi |
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Term
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Definition
MAE:inhibit packaging of norep/dopamine,serotonin, epi
A/E: induce depression |
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Term
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Definition
CLINICAL APP: depression
MAE: non-selective inhibit degradation of 5ht/dopamine/NTs
A/E: tyramine toxicity (> with diet with red wine cheese etc) leading to HTN crisis
DRUG-DRUG INTERACTIONS: cyp450 drugs, tca, ssris, pseuo=doephedrine, dextromethorpan (cold meds)
METABOLIZE: hepatic Pharmakokinetics: lipophilic, well absorbed
*transdermal patch avoids first pass, safer |
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Term
| Irreversiblephenelzine, isocarboxazie |
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Definition
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Term
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Definition
| MAOI Nonselective/ reversible |
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Term
| meclobemide, befloxatone, brofaromine |
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Definition
MAOI-A selective/reversible RIMAs
selective for prevention of breakdown serotonin, norepi and epi |
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Term
| selegiline and rasagiline |
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Definition
MAOI-B
selective block of dopamine degradation -more useful in parkinsons |
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Term
| nortriptyline/desipramine |
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Definition
Tricyclics Secondary Amines
MAE: more effects on NE than 5ht
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Term
amitriptyline, impramine, clomipramind
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Definition
Tricyclic Teriary Amines
MAE: antagonize 5ht and NE reuptake (>5ht then NE) transporters which increases level at cleft
S/E: CARDIAC- 1st degree AV block (usually higher doses)
DRUG-DRUG INTERACTIONS: drugs that inhibit 2D6 (HIV drug- rotanavir)
CLINICAL APP: neuropathic pain (low dose), sleep (low dose), antidepressive (high dose)
On-TARGET RECEPTOR:CYP450, 2D6
Off-TARGET RECEPTOR:muscarinic cholinergic (n/v dry, blurry, confused), histamine (tired and fat), adrenergic (hypotensive tachycardia sleepy dizzy)
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Term
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Definition
Examples: Prozac, celexa, luvox, paxil, zoloft, lexapro
CLINICAL APP: first line for Depression, anxiety due to higher selectivity and less A/E
MAE: selective for 5ht transporters increasing synaptic serotonin (lose selectivity at high doses)
A/E: sexual dysfunction, serotonin syndrome,
PHARM-KINET: paxil and prozac substrate and inihibitors of CYP2d6
DRUG-DRUG : less than TCAs/ drugs that work on same CYP2d6 mechanism
METABOLIZED by:
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Term
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Definition
examples: Effexor, Cymbalta
CLINICAL APP: Depression, neuropathic pain
MAE: blocks 5ht and NE reuptake transporter
A/E: increased BP, increased transaminases
DRUG-DRUG :
METABOLIZED by: CYP2D6 |
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Term
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Definition
CLASS: ATYPICAL
CLINICAL APP: antidepress, less sexual sideeffects
MAE: inhibits dopamine and NE reuptake
A/E: insomnia, alertness
DRUG-DRUG : effectiveness less when given with (faverins? HIV drugs)
METABOLIZED by: Hepatic CYP2B6
CONTRAINDICTATION: Sz or eating disorders
FORMULATIONS: IR(not used)/SR(bid dose) /XL( once daily) |
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Term
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Definition
Class: atypical
CLINICAL APP: depression, high doses for less histamine effects and better serotonin effect
MAE: mechanism unknown, less sexual dys
A/E: increased app, sedation
ON TARGET RECEPTOR: 5ht2/3, alpha adrenergic
OFF TARGET-histamine
DRUG-DRUG : other CYP3a4s
METABOLIZED by: CYP3A4 |
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Term
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Definition
CLINICAL APP: antianxiety/depression
MAE: inhibits 5ht transporter
A/E: sedation ortho stasis, hepatoxoic, fulminant liver failure
On-TARGET RECEPTOR: 5ht antagonize
Off-TARGET RECEPTOR: antagonizes histamine and alpha 1
METABOLIZED by:CYP3A4 |
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Term
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Definition
CLINCAL APP:used for sleep (low) Depression (high)
AE: priapism
Metabolized by: CYP3a4 |
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Term
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Definition
CLASS: Serotonin receptor agonists
CLINICAL APP: anxiety
MAE: agonizes 5ht1a receptor, non benzo, non addictive
A/E: dizziness nausea
On-TARGET RECEPTOR:5ht1a
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Term
| AMPTHETAMINE, METHAMPHETAMINE, METHYLPHENIDATE |
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Definition
Clinical app: ADD
MOA: may interfere with storage of MAO
may displace 5ht DA NE and revent reuptake
AE: induction of psychosis alertness |
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Term
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Definition
CLINICAL APP: controls mania and depression
MAE: not known (may interfere with cAMP IP3)
A/E: nausea, thirst, polyuria, tremor, weak,
INTERACTION : diuretics, renal insufficient, probenecid (gout)
METABOLIZED by:RENAL
CONSIDERATIONS: Long half-life, narrow therapeutic index, TERATOGENIC |
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Term
| Carbamazepine/Valproic Acid |
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Definition
| Mood stabilizers for Bipolar |
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