Term
|
Definition
1.) euphoria
2.) physical dependence
3.) psychological dependence
4.) respiratory depression
5.) CNS depression (miosis)
6.) increased seizures
7.) decreased cough reflex
8.) increased N/V |
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Term
| Peripheral Opioid ADRs (4) |
|
Definition
1.) slowed GIT motility
2.) urinary rtn
3.) itchinng, burning, flushing, bronchocon
4.) tolerance (EXCEPT to miosis/constipation) |
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Term
|
Definition
MOR agonist
Phase II metabolism -> more active, polar metabolite with BBB crossing mechanism |
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Term
|
Definition
weak MOR agonist
10% via Cyp2D6 -> morphine
*thus pharmacogenomics influence efficacy |
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Term
|
Definition
Demerol
MOR agonist
metabolism -> normeperidine which can cause seizures if builds up; 48hr admin max |
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Term
|
Definition
MOR agonist
w/APAP -> Vicodin
w/homatropine (muscarantag) -> Hycodan (antitussive) |
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Term
|
Definition
Nucynta
weak MOR agonist
+ inhibit NE reptake @ dorsal horn
-> greater alpha2 activation -> less glutamate&SP release |
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Term
|
Definition
Ultram
weak MOR agonist
+inhibit NE reuptake @ dorsal horn
+inhibit 5HT reuptake @ dorsal horn
-> greater 5HT activation -> less glutamate&SP release
+ direct alpha2 agonist activity |
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Term
|
Definition
MOR agonist
controlled release -> Oxycontin
w/APAP -> Percocet
w/ASA -> Percodan |
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Term
|
Definition
MOR agonist
long-acting & slow BBB crossing |
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Term
|
Definition
Dilaudid
MOR agonist
ADR: inhibits insulin release -> increases blood glucose |
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
Duragesic/Actiq
strong MOR agonist |
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Term
|
Definition
Lomotil
non-BBB cross MOR agonist for diarrhea |
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Term
|
Definition
Immodium
P-gp effluxed MOR agonist for diarrhea |
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Term
|
Definition
| opium d/dx used for infant diarrhea |
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Term
|
Definition
Narcan IV
MOR/KOR antagonist
use: overdose |
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Term
|
Definition
MOR/KOR antagonist
PO
use: opioid dependence |
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Term
|
Definition
MOR/KOR antagonist
IV
doesn't cross BBB
use: opioid-induced constipation |
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Term
|
Definition
MOR/KOR antagonist
PO
doesn't cross BBB
use: opioid-induced constipation |
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Term
|
Definition
KOR agonist/MOR antagonist
use: moderate analgesia |
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Term
|
Definition
KOR agonist/MOR antagonist
use: moderate analgesia |
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Term
|
Definition
Talwin
KOR agonist/MOR antagonist
+ sigma receptor agonist (PCP site)
use: moderate analgesia |
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Term
|
Definition
Talwin NX
KOR agonist/MOR antagnoist
prevents PCP-related abuse |
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Term
|
Definition
Subutex
MOR partial agonist/KOR antagonist
use: moderate analgesia (or addiction with pregnancy) |
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Term
|
Definition
Suboxone
MOR partial agonist/KOR agonist with MOR antagonist
use: addiction (C.I. in pregnancy) |
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Term
|
Definition
Prialt
conototoxin; blocks N-type Ca channel in dorsal horn
-> decreased glutamate & Substance P release
*novel MOA; no respiratory depression like opioids |
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Term
|
Definition
1.) inflammation
2.) vasodilation
3.) pain NT |
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
MOA: Serotonin agonist
5HT-1D (peripheral neurons) -> decrease CGRP release
5HT-1B (vessels) -> vasocon cerebral/meningial vessels
ADR: chest tightness, dizziness, parasthesias
CI: CAD, HTN, MI |
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|
Term
|
Definition
MOA: same as triptan
ADR: dopaminergic & adrenergic effects |
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Term
|
Definition
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Term
| ASA + butalbital (sedative) + caffeine |
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Definition
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Term
| APAP + butalbital + caffeine |
|
Definition
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Term
|
Definition
synthetic ergot
use: postpartum bleeding or abortion |
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Term
|
Definition
ergot
use: migraine relief |
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Term
| Preventative Drugs for MIgraines |
|
Definition
| BB, CCB, gabapentin, topiramate, botox |
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Term
| Hypnotic & Anxiolytic Drug Classes (4) |
|
Definition
1.) BDZ
2.) BDZ-related
3.) Barbs
4.) Melatonin Receptor Agonists |
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Term
| gabaA & gabaC receptor type |
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Definition
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Term
|
Definition
|
|
Term
| AMPA & NMDA receptor type |
|
Definition
| glutamate-gated ion channels |
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|
Term
| gabaA alpha subunits & actions |
|
Definition
alpha1: sedation/hypnosis
alpha2: anxiety
alpha3: muscle relaxant |
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Term
|
Definition
1.) anxiolytic (major use)
2.) insomina
3.) alcohol withdrawal syndrome
4.) acute anticonvulsant
5.) muscle relaxant |
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Term
|
Definition
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|
Term
|
Definition
Versed
short-acting BDZ
use: bedside procedure sedation |
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Term
|
Definition
short-acting BDZ
use: insomnia
ADR: rebound insomnia |
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Term
| Intermediate-acting BDZs (5) |
|
Definition
alprazolam
estazolam
lorazepam
oxazepam
temazepam |
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Term
|
Definition
intermediate-acting BDZ
use: anxiety
ADR: severe withdrawal |
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Term
|
Definition
intermediate-acting BDZ
use: insomnia |
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Term
|
Definition
intermediate-acting BDZ
use: anxiety, acute seizure
metabolism: Phase II -> less patient variability & DDIs |
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Term
|
Definition
intermediate-acting BDZ
use: anxiety
metab: PhII |
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Term
|
Definition
intermediate-acting BDZ
use: insomnia
metab: PhII |
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Term
|
Definition
chlordiazepoxide
clonazepam
diazepam
chlorazepate
flurazepam
quazepam |
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Term
|
Definition
|
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Term
|
Definition
long-acting BDZ
use: muscle relaxant & alcohol withdrawal |
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
MOA: high-affinity binding to gabaA alpha1
Use: insomnia only |
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Term
|
Definition
competitive antagonist @ gabaA
use: BDZ overdose, reversal after procedure
ADR: seizure precipitation |
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Term
|
Definition
MOA:
1.)(+)allosteric mod of gabaA (higher affin than BDZ)
2.) weak agonist at gabaA
3.) noncompetitively binds & stabilizes closed conformation of Na/K channel on AMPA receptor |
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Term
|
Definition
ultra-short acting barb
uses: general anesthetic & decrease ICP |
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Term
|
Definition
ultra-short acting barb
use: general anesthetic |
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Term
|
Definition
ultra-short acting barb
use: acute seizure |
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Term
|
Definition
long-acting barb
use: anticonvulsant |
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
Melatonin Receptor Agonist
MT1: induce sleep
MT2: regulate rhythm
hypnotic |
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Term
|
Definition
MOA: selective partial agaonist @ 5HT 1-A
Use: adjunct treatment for moderate anxiety
ADR: D2 antagonism -> restlessness |
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|
Term
gabaB receptor
locations & type |
|
Definition
Gi-PCR
1.) pre-synapse: inhibits Ca entry
2.) post-synapse: stims K efflux |
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|
Term
baclofen
MOA, use, ADR, additional benefit |
|
Definition
MOA: gabaB agonist
1.) inhibit Ca entry -> less glutamate release
2.) stim K efflux -> decreased activation of motor neuron\
Use: muscle spasms
ADR: sedation, muscle weakness, additive effect with other CNS depressants, withdrawal, tolerance
(*) shown to decrease alcohol craving |
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|
Term
| Centrally-Acting Muscle Relaxant MOAs (4) |
|
Definition
1.) gabaB agonist
2.) alpha2 agonist
3.) TCAs
4.) Unknown |
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Term
|
Definition
alpha2 agonist
MOA:
1.) inhibits glutamate release (additional pain relief benefit)
2.) inhibits alpha motor neuron activity
Use: muscle spasms
ADRs: sedation, xerostomia, hypoTN, bradycardia |
|
|
Term
cyclobenzaprine
MOA, use, ADRs |
|
Definition
TCA
MOA: inhibits NE & 5HT reuptake
Use: muscle spasms
ADRs: sedation, xerostomia, arrhythmia, fatal combo w/MAOi |
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|
Term
|
Definition
MOA: CNS depression
Use: muscle spasms & tetanus |
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Term
|
Definition
MOA: CNS depression
Use: muscle spasms |
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Term
|
Definition
MOA: CNS dperession
Use: Muscle spasms |
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|
Term
| Direct-Acting Muscle Relaxant MOAs (2) |
|
Definition
1.) inhibit Ach release from nicotinic neuron
2.) ryanodine antagonism |
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|
Term
Botulinum Toxin
Structure, SOA, MOA, DOA, ADR |
|
Definition
SOA: neuromuscular junction
Structure&MOA:
heavy chain: recognizes NMJ terminus
light chain: endopeptidase hydrolyzes VAMP&SNAP to prevent ACh release
DOA: one month
ADR: neutralizing Ab reaction |
|
|
Term
|
Definition
SOA: ryanodine receptor on SR
MOA: blocks receptor -> less Ca release -> less muscle contraction |
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Term
|
Definition
1.) NaCBs
2.) T-Type CCBs
3.) L-Type CCBs
4.) GABA potentiators
5.) Glutamate receptor blockers
6.) K channel stabilizers
7.) SV2A Binders |
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|
Term
|
Definition
| phenytoin, carbamazepine, oxcabazepine, eslicarbazepine, lamotrigine |
|
|
Term
| phenytoin kinetics, metab, formulation, ADR |
|
Definition
NaCB AED zero order kinetics metab: CYP2C9 (*)CYP3A4 Inhibitor formulation: organic solvents -> cause hypoTN ADR: hypersensitivity
ginger hyperplasia
nystagmia
teratogenic |
|
|
Term
|
Definition
NaCB AED
ADR: aplastic anemia & ADH secretion -> hyponatremia
(*)CYP3A4 Inhibitor |
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|
Term
|
Definition
NaCB AED
-> less hyponatremia
-> less CYP3A4 inhibition |
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|
Term
|
Definition
NaCB AED
-> least hyponatremia
-> least CYP3A4 inhibition |
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
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Term
|
Definition
N-Type CCB AED
(*) NO CYP INTERACTION |
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Term
|
Definition
| block alpha2/delta subunit of neuronal Ca channel -> decrease release of NTs Glutamate, NE, DA, Substance P |
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Term
|
Definition
| inhibits GAT1 (reuptake by GABA neuron) |
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|
Term
|
Definition
inhibits gabaT (transaminase in glial cell) (*) NO CYP INTERACTION :)
*Ocular toxicity --> need to get check up |
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Term
|
Definition
|
|
Term
|
Definition
NMDA antagonist & NaCB
ADR: hematological disorders |
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Term
|
Definition
K+ channel stabilizer
-> hyperpolarization with extended K efflux (m current) |
|
|
Term
|
Definition
SV2A binder
-> inhibits NT vesicle fusion
(*) NO CYP INTERACTION :) |
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|
Term
|
Definition
1.) NaCB
2.) CtCB
3.) inhibits carbonic anhydrase (decreases seizures)
ADR: metabolic acidosis |
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|
Term
|
Definition
|
|
Term
|
Definition
NaCB; new AED
(*)3A4 INDUCER |
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|
Term
| What AEDs have no CYP involvement? (4) |
|
Definition
| Gabapentin, pregabalin, levetiracetam, vigabatrin |
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|
Term
Emergence from Anesthesia
Symptoms & Treatment |
|
Definition
1.) overstimulation -> tachycardia
2.) shivers -> give meperidine
3.) CTZ stimulation -> give odansetron
4.) malignant hyperthermia -> give dantrolene |
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|
Term
|
Definition
acute IV anesthetic
gabaA potentiation
(+): no effect on BP
(-): only used acutely due to adrenal inhibition |
|
|
Term
|
Definition
acute IV anesthetic
NMDA blocker & sympathomimetic
(*) analgesia |
|
|
Term
|
Definition
IV anesthetic
gabaA potentiation
(+): good for long-term use; intrinsic anti-emetic activity
(-): emulsion containing eggs; grows bacteria |
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|
Term
|
Definition
acute IV anesthetic
gabaA potentiation
(-): builds up in body to give long recovery time |
|
|
Term
|
Definition
IV anesthetic
alpha2 agonist
(*) analgesia |
|
|
Term
fentanyl-related drugs
use |
|
Definition
| intrinsic CNS depression: combine with anesthetics to reduce doses |
|
|
Term
| Local Anesthetic Duration Depends on... (3) |
|
Definition
1.) structure (ester vs amide linked)
2.) degree of systemic absorption
3.) affinity to tissue proteins |
|
|
Term
|
Definition
Benzocaine
Procaine
Tetracaine
Topical Cocaine
Chloroprocaine |
|
|
Term
|
Definition
Lidocaine
Dibucaine
Mepivacaine
Bupivacaine
Prilocaine
EMLA
Ropivacaine
Articaine |
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|
