Term
|
Definition
| similar structure to NE -> uptaken by NET -> into VMAT -> displaces NE into synapse |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| blocks NET & secondarily DAT |
|
|
Term
| Indirect-Acting Sympathomimetic Central ADRs |
|
Definition
| insomnia, decreased appetite, some euphoria, some dependence (due to DA) |
|
|
Term
| Indirect-Acting Sympathomimetic Peripheral ADRs |
|
Definition
| tachycardia, HTN, bladder constriction (trigone) & bladder urgency (detrusor) |
|
|
Term
|
Definition
miscellaneous indirect-acting sympathomimetic
for weight loss |
|
|
Term
|
Definition
miscellaneous indirect-acting sympathomimetic
for weight loss |
|
|
Term
|
Definition
miscellaneous indirect-acting sympathomimetic
for weight loss |
|
|
Term
|
Definition
Provigil
miscellaneous indirect-acting sympathomimetic
for narcolepsy |
|
|
Term
|
Definition
Nuvigil
miscellaneous indirect-acting sympathomimetic
for narcolepsy |
|
|
Term
atomoxetine
MOA, Metab, ADR |
|
Definition
Strattera
miscellaneous indirect-acting sympathomimetic
for ADD
MOA: selective NET blocker
Metab: 2D6 (genomics apply)
ADRs: hepatotoxicity, xerostomia, sedation, appetite suppression |
|
|
Term
|
Definition
MIxed Acting Sympathomimetic
Indirect: uptaken into NET -> VMAT -> displaces NE
Direct: agonist at alpha1, alpha2, beta1, beta2
Use: cough & cold for nasal decon & bronchodil |
|
|
Term
imipramine
-desipramine
-clomipramine |
|
Definition
|
|
Term
amitriptyline
-nortriptyline |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
low dose: nocturnal enuresis
low dose: sedative for sleep
neuropathic pain (increased 5HT in synapse decreases substance P & glutamate) |
|
|
Term
|
Definition
MOA: inhibit NE & 5HT Reuptake
OOA: 2ndary adaptation -> takes 8 weeks |
|
|
Term
|
Definition
muscarinic antagonism: dry mouth, slow GIT
histamine antagonism: sedation
alpha1 antagonism: orthostatic hypoTN
weight gain
prolonged QRS interval |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
Prozac
SSRI
metabolite: norfluoxetine; 2d6 inhibitor |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| fluvoxamine, fluoxetine, paroxetine |
|
|
Term
|
Definition
wakefulness
decreased appetite
ED & sex problems
2D6, 3A4, 2C19 inhibition |
|
|
Term
| MOA of Neurogenesis in Antidepressants |
|
Definition
increased monoamine receptor activation ->
increased CAMP ->
increased phosphorylation of CREB transcrip factor ->
increased BDNF (growth factor prot) ->
neurogenesis |
|
|
Term
|
Definition
Effexor
SNRI
ADR: increased BP |
|
|
Term
|
Definition
|
|
Term
|
Definition
Cymbalta
SNRI
ADR: hepatotoxic
Uses: fibromyalgia & neuropathic pain |
|
|
Term
|
Definition
Savella
SNRI
Uses: fibromyalgia |
|
|
Term
|
Definition
insomnia
decreased appetite
sexual dysfxn |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
Emsam
MAOb inhibitor
TD for depression; PO for Parkinson's |
|
|
Term
|
Definition
irreversibly inhibits MAO
(metabolizes Epi, NE, tyramine, 5HT, DA that leaks out of vesicle) -> much more enters synapse |
|
|
Term
|
Definition
-cheese/aged foods
contain tyramine which is usually broken down by MAOa; excess tyramine -> indirect sympathomimetic effect -> increased BP, CO -> HTN Crisis
-dextromethorphan (weak SRI) -> serotonin syndrome
-pseudoephedrine/phenylephrine -> alpha1 agonist -> HTN Crisis
-amephetamines (contraindicated) -> HTN Crisis |
|
|
Term
Serotonin Syndrome
MOA, s/sx, treatment |
|
Definition
MOA: excess activation of 5HT2a in periphery&brain
s/sx: restless -> tremor -> clonus -> mental changes -> muscle hypertonicity -> hyperthermia
trt: cool down pt; give cyproheptidine |
|
|
Term
|
Definition
Periactin
5HT2a antagonist for serotonin syndrome
other uses:
h1 antag for child's allergies
counteract sexual dysfxn |
|
|
Term
|
Definition
Wellbutrin
atypical antidepressant
MOA: NET & DAT Blocker
ADR: insomnia, weight loss, some abuse potential |
|
|
Term
|
Definition
atypical antidepressant
MOA: alpha-2 & H1 antagonist
alpha-2 heteroreceptor on 5HT -> increased 5HT when blocked |
|
|
Term
|
Definition
atypical antidepressant
MOA: SNRI
ADR: hepatotoxicity |
|
|
Term
|
Definition
SNRI + alpha1 antag + H1 antag
atypical antidepressant |
|
|
Term
|
Definition
Viibryd
SSRI
atypical antidepressant
less sexual ADRs & faster OOA |
|
|
Term
| 3 Possible Etiologies of Psychosis |
|
Definition
1) increased DA in limbic system
2) decreased glutamate
3) increased 5HT
**high genetic risk |
|
|
Term
| List 4 Dopaminergic receptors & effects |
|
Definition
1) CTZ (D2) -> nausea/vomiting
2) Basal ganglia (D1,D2) -> mvmt/posture control
3) Limbic (D1-D4) -> aggression, hallucination
4) Pituitary gland (D2) -> decreased prolactin |
|
|
Term
|
Definition
Thorazine
D2 antagonist
Antipsychotic |
|
|
Term
|
Definition
Mellaril
D2 antagonist
Antipsychotic |
|
|
Term
|
Definition
Prolixin
D2 antagonist
Antipsychotic |
|
|
Term
|
Definition
Trilafon
D2 antagonist
Antipsychotic |
|
|
Term
|
Definition
D2 antagonist
Antipsychotic |
|
|
Term
|
Definition
Navane
D2 antagonist
Antipsychotic |
|
|
Term
|
Definition
Haldol
D2 antagonist
Antipsychotic |
|
|
Term
|
Definition
D2 antagonist
Antipsychotic |
|
|
Term
|
Definition
D2 antagonist
Antipsychotic |
|
|
Term
|
Definition
Orap
D2 antagonist
Tourette's |
|
|
Term
|
Definition
Compazine
D2 antagonist
Antiemetic |
|
|
Term
|
Definition
Torecan
D2 antagonist
Antiemetic |
|
|
Term
| D2 antagonist ADRs due to D2 Blockade (5) |
|
Definition
1) Dystonia: neck & face spasms upon drug initiation 1-2wk
2) EPS: first few months on drug
-tremors, akinesia, bradykinesia (treat with benztropine to balance Ach)
-akathisia/RLS (treat with propranolol)
3)Tardive dyskinesia: years into therapy
-irreversible twisted limbs & facial twitches
4) pituitary problems
-F: increased milk production, amenorrhea, breast cancer risk
-M: gynecomastia, ED
5) neurolyptic malignant syndrome
-like malignant hyperthermia but worse due to outpt
-heat, tremors, cardiac instability; rapid onset
-treat with dantrolene |
|
|
Term
| D2 antagonist ADRs due to nonselectivity (7) |
|
Definition
1) sedation due to H1 antagonism
2) orthostatic hypoTN due to alpha1 antagonism
3) seizures
4) prolonged QT interval
5) dermatitis
6) retinopathies
7) blood dyscrasias |
|
|
Term
|
Definition
Abilify
atypical antipsychotic
partial agonist @ D2 used as antagonist
least metabolic disorder risk |
|
|
Term
|
Definition
Zyprexa
atypical antipsychotic
worst metabolic disorder risk |
|
|
Term
|
Definition
Symbax
atypical antipsychotic combo for bipolar |
|
|
Term
|
Definition
Seroquel
atypical antipsychotic |
|
|
Term
|
Definition
Risperdal
atypical antipsychotic |
|
|
Term
|
Definition
Geodon
atypical antipsychotic
worst arrhythmia risk
least metabolic disorder risk |
|
|
Term
|
Definition
Invega
atypical antipsychotic |
|
|
Term
|
Definition
Clozaril
atypical antipsychotic
ADRs:
0% risk Tardive Dyskinesia
worst metabolic disorder risk
blocks D1&D4 more
myocarditis
agranulocytosis in first 18wk -> must get WBC count qwk
(risk is worse in elderly women) |
|
|
Term
| Atypical Antipsychotic MOA |
|
Definition
1) less D2 affinity (60% receptor occupancy)
2) 5HT2a postsynaptic antag -> reduces (-) s/sx
3) 5HT2a presynaptic heterorecep antag -> increases DA in basal ganglia -> less mvmt disorders |
|
|
Term
| Atypical Antipsychotic ADRs |
|
Definition
mvmt disorders (less)
tardive dyskinesia (less)
metabolic disorders: wt gain, triglycerides, blood glucose
blood dyscrasias
QT prolongation (less) |
|
|
Term
|
Definition
use: bipolar mania
MOA:
1) inhibit DA release
2) prevent D2 (GqPCR) action by inhib IP3
ADRs: muscle tremor, rash, polyuria (due to ADH resistance)
*greater effect when hyponatremic |
|
|
Term
|
Definition
Aricept
cholinesterase inhibitor for alzheimers
M: CYP |
|
|
Term
|
Definition
Razadyne
cholinesterase inhibitor
M: CYP |
|
|
Term
|
Definition
Exelon
cholinesterase inhibitor
M: CYP |
|
|
Term
| Cholinesterase Inhibitors Use & ADR |
|
Definition
for alzheimers
delay delcine for 1-2 years
ADR: peripheral muscarinic effects |
|
|
Term
|
Definition
Namenda
NMDA Antagonist for Alzheimer's |
|
|
Term
|
Definition
Rilutek
NMDA Antagonist for ALS
increases lifespan by 2months |
|
|
Term
|
Definition
| Increases transcription of GLT-1 transporter on astrocytes -> decreased glutamate in synapse |
|
|
Term
|
Definition
MOA: converted by AAAD in brain -> DA
*crosses BBB via AA transporter |
|
|
Term
|
Definition
AAADi in periphery
-minimizes peripheral ADRs (vasodil)
-maximizes amount of L-dopa delivered to brain |
|
|
Term
|
Definition
|
|
Term
|
Definition
Comtan
COMTi
doesn't cross BBB thus only prevents L-Dopa metabolism & inactivation |
|
|
Term
|
Definition
COMTi
crosses BBB thus prevents L-Dopa metabolism & DA metabolism
hepatotoxic |
|
|
Term
| L-Dopa + carbidopa + entacapone |
|
Definition
|
|
Term
|
Definition
1) brown body fluid
2) psychosis
-due to elevated limbic DA
3) on/off phenomenon
-tk q3h to avoid
-subtherapeutic: return of s/sx
-supratherapeutic: dyskinesia
4) wearing off
-drug only works if neurons are alive to metabolize to DA
5) free radical generation
-due to L-Dopa -> DA |
|
|
Term
|
Definition
D2 agonist
ergot d/dx
use: hyperprolactinemia |
|
|
Term
|
Definition
D2 agonist
ergot d/dx
use: hyperprolactinemia (@low dose) |
|
|
Term
|
Definition
D2 agonist
ergot d/dx
off the market |
|
|
Term
| Ergot D/dx for Parkinson's |
|
Definition
5HT-1B, 5HT-1D, 5HT-2B, D2 agonism
*5HT-2B causes heart valve dysfxn -> PAH
not used much anymore for Parkinson's |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| D2/D3 agonist benefits (4) |
|
Definition
1) longer t1/2 -> no on/off
2) not prodrug -> no wearing off
3) metabolism doesn't generate free radicals
4) neuroprotective -> binds presynaptic D2 receptor telling neuron to decrease DA -> less free radicals created from L-Dopa to DA |
|
|
Term
|
Definition
1) psychosis due to D2
2) sedation
3) impulse control disorders due to D3 |
|
|
Term
|
Definition
D2/D3 short acting agonist
use: rescue therapy for off-period of L-Dopa
*must coadmin with antiemetic |
|
|
Term
|
Definition
Eldepryl
MAOb inhibitor
HTN, anorexia, insomnia (due to amphetamine-like metabolite)
*add-on prn |
|
|
Term
|
Definition
Azilect
MAOb inhibitor
*add-on prn |
|
|
Term
|
Definition
muscarinic antagonist for Parkinson's
*add-on prn |
|
|
Term
|
Definition
muscarinic antagonist for Parkinson's
*add-on prn |
|
|
Term
|
Definition
antiviral
MOA:
1) increased DA release from neurons
2) muscarinic antagonist
3) NMDA antagonist |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| Very selective GR agonist |
|
|
Term
|
Definition
| Very selective GR agonist |
|
|
Term
|
Definition
| Very selective GR agonist |
|
|
Term
|
Definition
1) replacement therapy for adrenal insufficiency
2) immune suppression
3) anti-inflammatory |
|
|
Term
|
Definition
Cosyntropin
Diagnostic agent for primary adrenal insufficiency |
|
|
Term
|
Definition
Achtrel
Diagnostic agent for secondary adrenal insufficiency |
|
|
Term
| 3 Inflammatory Proteins Increased by Cytokines via NFKB |
|
Definition
1) Integrins
2) Cytokines
3) COX-2 |
|
|
Term
| 3 Effects of GR Activation |
|
Definition
1) Increased transcription of IFKB gene
2) Increased transcription of annexin-1 gene
-inhibits PLA2 -> decreased AA -> decreased PGE2
3) Binds NFKB to inhibit inflammatory protein transcription |
|
|
Term
|
Definition
1) insomnia
2) N/V
3) increased blood glucose (via increased transcription of gluconeogenesis pathway) |
|
|
Term
|
Definition
1) decreased bone mineral density
-via decreased osteoblast activity
2) decreased muscle mass
3) skin thinning
4) redistribution of fat -> buffalo hump
5) increased stomach acid
6) increased BP
-via MR activation -> water rtn
-via increased AngII & AngII receptor -> vasocon
7) increaed IOP
8) cataracts in children
9) rare aggression/psychosis
10) decreased immune fxn |
|
|
Term
|
Definition
| Cortisol synthesis inhibitor |
|
|
Term
|
Definition
| Cortisol synthesis inhibitor |
|
|
Term
|
Definition
| Cortisol synthesis inhibitor |
|
|
Term
|
Definition
| Cortisol synthesis inhibitor |
|
|
Term
|
Definition
High dose IV corticosteroids
1) decrease immune fxn -> less proliferation
2) decrease inflammation -> less T cells can enter BBB |
|
|
Term
|
Definition
Avonex, Rebif, Betaseron
DOC for MS
MOA:
1) decreased mvmt of T-cells into CNS
2) decreased T cell activation
3) decreased cytokine release from T cells |
|
|
Term
|
Definition
1) flu-like s/sx initially
2) injexn site rxns (due to large molec)
3) depression & suicidal thoughts
4) seizures
5) CHF
6) creation of neutralizing Abs against IFB |
|
|
Term
glatiramer acetate
MOA, ADR |
|
Definition
Copaxone
2nd Line for MS
MOA: decreased T cell activity
ADR: intense chest pain 15min after injection |
|
|
Term
|
Definition
Tysabri
MAb ag. alpha-4 beta-1 integrin on T cells
2nd line in MS
MOA: prev T-cell interaction with VCAM1 endothelial integrin -> decreased diapedesis
ADR: PML infection in brain due to latent virus awakening during intense immune suppression |
|
|
Term
teriflunomide
MOA, ADR, T1/2, DF |
|
Definition
Aubagio
MOA: inhibs enz that synth pyrimidines -> no DNA -> no cell division -> no T Cell proliferation
ADR: hepatotoxicity, teratogenicity
LONG T1/2
DF: PO |
|
|
Term
|
Definition
Gilenya
MOA: S1P1 receptor agonist -> moves T cells out of thymus into circulation but quickly desensitizes so it can't happen anymore
ADR: 1st dose extreme bradycardia
DF: PO |
|
|
Term
|
Definition
Ampyra PO
Blocks K channels to improve walking speed (unmyelinated neurons leak K) |
|
|
