Pharm (Advanced) Flashcards

(138 cards)

1
Q

amphetamine

A

Use: Narcolepsy, ADHD

MOA: Nervous system stimulant (incr. DA levels in CNS)

CI/Toxicity: Depresses appetite, ascorbic acid decr. absorption /alkaline incr. absorp.

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2
Q

methamphetamine

A

Use: Narcolepsy, Anorexiant, ADHD, Drug of abuse

MOA: Like amphetamine but higher central to peripheral effects (reaches CNS better than amphetamine w/ longer lasting effects)

CI/Toxicity:

  • Schedule II stimulant, high degree of abuse
  • toxic to nerve cells due to inhibiting DA reuptake & increasing synth
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3
Q

ephedrine

A

Use:

MOA: Activates β-receptors, Orally active, Long duration of action

CI/Toxicity: Cardiac problems

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4
Q

tyramine

A

Use: Normal byproduct of tyrosine metabolism

MOA:
-Metabolized by MAO in liver

  • High first pass effect (low bioavailability)
  • Indirect sympathomimetic when given parenterally → increased release of stored catecholamines

CI/Toxicity: Caution to those on MAOI → intensified effect → increased BP and HR

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5
Q

modafinil

A

Use: Promotes wakefulness (narcolepsy)

MOA: Psychostimulant w different structure and effects than amphetamines

-MOA not fully understood but inhibits DA and NE transporters → increased DA, NE, Serotonin, Glutamate, and decreased GABA

CI/Toxicity: Increased BP and HR

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6
Q

atomoxetine

A

Use: ADHD (adults + children)

  • Does not increase alertness or motor activity
  • Slower onset than stimulants

MOA: Non-stimulant compound

  • Selective reuptake inhibitor of NE
  • Incr. NE transmission
  • Decr. sympathetic outflow in CNS and increased NE effects in periphery
  • not a controlled substance, b/c it’s not a stimulant

CI/Toxicity: May be less effective than stimulants because it DOES NOT have DA effects.

  • Avoid MAOIs
  • *t1/2 goes from 5 hrs to 24 hrs in poor metabolizers
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7
Q

methylphenidate

A

Ritalin

Use: ADHD, Narcolepsy, Postural Orthostatic Tachycardia Syndrome

MOA: Piperidine class of compounds (amphetamine variant)

  • Increases NE and DA levels in the brain.
  • Reuptake inhibitors of monoamine transporters
  • short acting w/ t1/2 3-5 hrs

CI/Toxicity: Facial tics, tachycardia,

Avoid MAOIs → avoid HTN crisis

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8
Q

dexmethylphenidate

A

Use: ADHD

MOA: D-enantiomer only,

  • Blocks reuptake of DA, NE, via transporter blockade
  • Available in short, intermediate, and long lasting formulas

CI/Toxicity: Facial tics, tachycardia,

Avoid MAOIs → avoid HTN crisis

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9
Q

dextroamphetamine

A

Use: ADHD

MOA: D-enantiomer only, Blocks reuptake of DA and NE

CI/Toxicity: Facial tics, tachycardia,
-C/I w/ cardiac abnormalities
Avoid MAOIs → avoid HTN crisis

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10
Q

lisdexamfetamine

A

Use: ADHD

MOA: Dextromphetamine + L-Lysine, Blocks reuptake of DA and NE

CI/Toxicity: Facial tics, tachycardia,
-C/I w/ cardiac abnormalities
Avoid MAOIs → avoid HTN crisis

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11
Q

amphetamine mixed salts

A

Adderall

Use: ADHD

MOA: mixture of d- and l-enantiomers attached to different salts
-Increased presynaptic release of DA, NE, 5HT via transporter reversal

CI/Toxicity: Facial tics, tachycardia,

Avoid MAOIs → avoid HTN crisis

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12
Q

valproic acid

A

aka: Depakene

Class: conventional anticonvulsant

Use: migraine headache prophylaxis
-Bipolar disorder

MOA: Unclear, may increase GABA or block Na channels

CI/Toxicity: nausea, fatigue, tremor, weight gain, hair loss, lipid abnormalities, hyperinsulinemia, hirsutism and menstrual disturbances. not recommended for use during pregnancy

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13
Q

phenobarbital

A

aka: Luminal

Class: conventional anticonvulsant

Use: sedation and relief of anxiety; amnesia; hypnosis; anesthesia; coma and respiratory depression; steeper dose-response relationship than benzodiazepines

MOA:

  • Bind to specific GABAA receptor subunits at CNS neuronal synapses increasing duration of GABA-mediated chloride ion channel opening
  • Enhance membrane hyperpolarization

CI/Toxicity:

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14
Q

carbamazepine

A

aka: Tegretol

Class: conventional anticonvulsant

Use: Simple & complex partial seizures & generalized tonic- clonic seizures
-Bipolar disorder

MOA: Slows rate of recovery of Na+ channels from inactivation

CI/Toxicity: aplastic anemia

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15
Q

phenytoin

A

aka: Dilantin

Class: conventional anticonvulsant

Use: All types of partial & tonic- clonic seizures
* Not absence seizures

MOA: Slows rate of recovery of Na+ channels from inactivation. *Half life increases with concentration

CI/Toxicity: Cardiac toxicity; CNS depression

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16
Q

diazepam

A

aka: Vailum

Class: conventional anticonvulsant

Use: effective for status epilepticus, but it has a short duration of action & isn’t used as much

MOA:

  • Enhance GABA- mediates synaptic inhibition via the GABAA receptor (incr frequency of GABA- activated Cl- channels)
  • At higher conc’n, reduces high- freq firing of neurons

CI/Toxicity:

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17
Q

clonazepam

A

aka: Klonopin

Class: conventional anticonvulsant

Use: useful in absence & myoclonic seizures in children (but tolerance develops after 1- 6 months)

MOA:

  • Enhance GABA- mediates synaptic inhibition via the GABAA receptor (incr frequency of GABA- activated Cl- channels)
  • At higher conc’n, reduces high- freq firing of neurons

CI/Toxicity:

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18
Q

primidone

A

Class: conventional anticonvulsant (barbiturate)

Use: Effective against partial seizures & generalized tonic- clonic seizures

MOA: Like that of phenytoin (Slows rate of recovery of Na+ channels from inactivation)

CI/Toxicity:

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19
Q

ethosuximide

A

aka: Zarontin

Class: newer anticonvulsant

Use: Primary agent for tx of absence seizures
* Not for tonic- clonic seizures

MOA: Reduces low threshold Ca2+ currents (T- type currents) in thalamic neurons

CI/Toxicity:

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20
Q

gabapentin

A

aka: Neurontin

Class: newer anticonvulsant

Use: Effective for partial seizures, w/ & w/o secondary generalization when used in addition to other anti- seizure meds

MOA: Bind to protein in cortical membrane w/ an a.a. sequence identical to Ca2+ subunit α2δ1; full MOA is unclear

CI/Toxicity:

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21
Q

pregabalin

A

aka: Lyrica

Class: newer anticonvulsant

Use: Effective for partial seizures, w/ & w/o secondary generalization when used in addition to other anti- seizure meds

MOA: Bind to protein in cortical membrane w/ an a.a. sequence identical to Ca2+ subunit α2δ1; full MOA is unclear

CI/Toxicity:

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22
Q

tiagabine

A

aka: Gabitril

Class: newer anticonvulsant

Use: Add on therapy for partial seizures in adults (w/ or w/o secondary generalization)

MOA: Inhibits the GABA transporter, GAT-1, & thereby reduces GABA uptake into neurons & glia

CI/Toxicity:

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23
Q

topiramate

A

aka: Topamax

Class: newer anticonvulsant

Use: Partial & primary generalized seizures, migraine prophylaxis

MOA:

  • Reduces VG Na+ currents in cerebellar cells & may act on the inactivated state of the channel
  • Activates a hyperpolarizing K+ current, enhancing postsynaptic GABAA- receptor currents
  • Limits activation of the AMPA- kainite- subtype of glutamate receptor

CI/Toxicity:

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24
Q

lamotrigine

A

aka: Lamictal

Class: newer anticonvulsant

Use: Monotherapy & add- on therapy for partial & secondarily generalized tonic- clonic seizures

MOA:

  • Blocks sustained repetitive firing & delays recovery from inactivation of Na+ channels
  • May have other MOAs that explain its broader spectrum of use than phenytoin & carbamazepine

CI/Toxicity:

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zonisamide
aka: Zonegran Class: newer anticonvulsant Use: Add- on therapy in partial seizures MOA: - Inhibits T- type Ca2+ currents - Inhibits sustained, repetitive firing of neurons by prolonging inactivated state of Na+ channels CI/Toxicity:
26
Acyclovir
aka: Zovirax Class: antiviral Use: viral encephalitis caused by HSV (for HSV-1,2 and to a lesser extent VZV) MOA: - Competition with deoxyGTP for the viral DNA polymerase, resulting in binding to the DNA template as an irreversible complex - Chain termination following incorporation into the viral DNA. CI/Toxicity: Nausea, diarrhea, and headache, rarely reversible renal toxicity and neuro effects
27
rabies immune globulin
Use: prophylaxis for rabies MOA: passive immunization (IgG mainly) CI/Toxicity:
28
sumatriptan
aka: Imitrex Class: triptan Use: Migraines, best if used during aura phase MOA: 5-HT(1D/1B agonist), inhibits release of vasodilating peptides and has vasoconstrictive properties Toxicity: tingling, dizziness, drowsiness and fatigue and rarely cardiac problems CI: patients that have coronary, cerebrovascular or any other arterial disease, Triptans should not be used within 24h of another triptan or ergot compound, don't give with MAOIs or SSRIs
29
ergotamine
Class: ergot Use: Migraines MOA: nonspecific serotonin agonist w/vasoconstrictive properties - also partial agonist at alpha-adrenergic and dopamine receptors - give when attack starts (prodrome period) - caffeine helps increase absorption - LONG LASTING AND ADDITIVE VASOCONSTRICTION Toxicity: nausea and vomiting, rarely vascular occlusion CI: uncontrolled hypertension or arterial disease. Triptans, beta blockers, dopamine, nicotine or CYP3A4 inhibitors can all potentiate the effects of ergots. Ergots and triptans should not be taken within 24h of each other.
30
timolol
Class: Beta blocker Use: Migraine prophylaxis MOA: Beta blocker CI/Toxicity: fatigue and orthostatic hypertension, should not be used in patients with decompensated heart failure, or asthma. Worsens depressive symptoms
31
propanolol
Class: Beta blocker Use: Migraine prophylaxis MOA: Beta blocker CI/Toxicity: not stressed in powerpoint
32
valproate
Class: anti-epileptic Use: Migraine prophylaxis MOA: Toxicity: nausea, fatigue, tremor, weight gain, hair loss, lipid abnormalities, hyperinsulinemia, hirsutism and menstrual disturbances. Rarely acute hepatic failure and pancreatitis CI: not recommended for use during pregnancy (lower IQ)
33
topiramate
Class: anti-epileptic Use: Migraine prophylaxis MOA: Toxicity: paresthesias, fatigue, cognitive and language impairment, taste perversion and weight loss. Rarely secondary narrow angle glaucoma, oligohydrosis (diminished ability to sweat, which can result in hyperthermia), nephrolithiasis (kidney stones) and metabolic acidosis. CI: not recommended for use during pregnancy (cleft lip and cleft palate)
34
donepezil
aka: Aricept Class: cholinesterase inhibitor Use: Adjunct to memantine for Alzheimer's MOA: reversible cholinesterase antagonist CI/Toxicity: nausea, diarrhea, vomiting
35
rivastigmine
aka: Exelon Class: cholinesterase inhibitor Use: Adjunct to memantine for Alzheimer's MOA: reversible cholinesterase antagonist CI/Toxicity: nausea, diarrhea, vomiting
36
galantamine
aka: Class: cholinesterase inhibitor Use: Adjunct to memantine for Alzheimer's MOA: reversible cholinesterase antagonist CI/Toxicity: nausea, diarrhea, vomiting
37
memantine
aka: Namenda Class: non-competitive NMDA glutamate receptor antagonist Use: Alzheimer's MOA: Binds to Mg+ binding site in activated NMDA receptor and blocks the channel (voltage dependent, Na+ channel must be open to bind) CI/Toxicity: avoid drugs that alkalinize the urine, such as carbonic anhydrase inhibitors and/or sodium bicarbonate (this will increase the reabsorption)
38
morphine
aka: Class: Strong Opioid Agonist Use: analgesic for severe constant pain MOA: potent mu agonist, indirectly activates delta and kappa receptors Toxicity: - Respiratory depression - severe constipation - addiction - convulsions CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard
39
hydromorphone
aka: Dilaudid Class: Strong Opioid Agonist Use: analgesic for severe constant pain MOA: more potent version of morphine Toxicity: - Respiratory depression - severe constipation - addiction - convulsions CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard
40
oxymorphone
aka: Class: Strong Opioid Agonist Use: analgesic for severe constant pain MOA: more potent version of morphine Toxicity: - Respiratory depression - severe constipation - addiction - convulsions CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard
41
methadone
aka: Class: Strong Opioid Agonist Use: rehab for opioid withdrawal, analgesic for severe constant pain MOA: antagonizes more potent mu agonists like morphine without euphoric effect Toxicity: same as morphine CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard
42
fentanyl
aka: Class: Strong Opioid Agonist Use: analgesic for severe constant pain, adjunct in anesthesia MOA: Toxicity: same as morphine CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard
43
meperidine
aka: Demerol Class: Strong Opioid Agonist Use: analgesic for severe constant pain, adjunct in anesthesia MOA: strong mu agonist w/ anticholinergic effects Toxicity: same as morphine CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard
44
codeine
aka: Class: Mild to Moderate Opioid Agonist Use: Mild-moderate pain; cough MOA: Like strong agonists; weaker effects Toxicity: same as morphine CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard
45
hydrocodone
aka: Class: Mild to Moderate Opioid Agonist Use: Mild-moderate pain; cough MOA: Like strong agonists; weaker effects Toxicity: same as morphine CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard
46
oxycodone
aka: Oxycontin Class: Mild to Moderate Opioid Agonist Use: Mild-moderate pain; cough MOA: Like strong agonists; weaker effects Toxicity: same as morphine CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard
47
propoxyphene
aka: Class: Mild to Moderate Opioid Agonist Use: mild analgesic and cough suppressant MOA: partial mu agonist Toxicity: Minimal when taken as directed
48
nalbuphine
aka: Class: Mixed Actions at Opioid Receptors Use: analgesic w/o respiratory depression MOA: kappa opioid agonist, mu antagonist Toxicity: dysphoric reactions and have limited potency CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard, no preggers either
49
buprenorphine
aka: Subutex (oral), Suboxone (combined w/naloxone) Class: Mixed Actions at Opioid Receptors Use: moderate pain, opioid withdrawal MOA: mu partial agonist w/ high affinity; kappa antagonist (slows withdrawal symptoms) Toxicity: dysphoric reactions and have limited potency CI: Don't give to people with pissing problems, bad prostates, livers, kidneys, lungs, or anyone who's been hit in the head really hard, no preggers either (abstinence syndrome), can't take with booze,
50
butorphanol
aka: Class: Mixed Actions at Opioid Receptors Use: analgesic w/o respiratory depression MOA: kappa opioid agonist Toxicity: same as morphine CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard
51
tramadol
aka: Class: Opioid with Other Effects Use: Moderate pain; adjunct to opioids in chronic pain syndromes MOA: weak μ agonist, moderate SERT inhibitor, weak NET inhibitor Toxicity: Seizures; risk of serotonin syndrome CI: Don't give to people with bad livers, kidneys, lungs, or anyone who's been hit in the head really hard
52
dextromethorphan
aka: Robitussin Class: Opioid with Other Effects Use: cough suppressant, psychedelic drug of abuse MOA: partial mu agonist; blocks NMDA-type glutamate receptors → disinhibition; blocks serotonin reuptake Toxicity: Minimal when taken as directed CI: shouldn’t be combined w MAO inhibitors- results in restlessness, extreme hyperpyrexia, death (serotonin syndrome)
53
naloxone
aka: Narcan Class: Opioid Antagonist Use: reverse opioid effects (ex. overdose), added to subuxone to keep rehabbing druggies from shooting it up (causes instant withdrawal symptoms #sucking) MOA: mu, kappa, and delta antagonist CI/Toxicity: precipitates abstinence syndrome in abusers (don't give to preggers)
54
naltrexone
aka: Class: Opioid Antagonist Use: reverse opioid effects (ex. overdose), treats dependance (for alcohol too) MOA: like naloxone but longer duration of action CI/Toxicity:
55
percocet
aka: oxycodone + acetaminophen
56
percodan
aka: oxycodone + aspirin
57
vicodin/lortab
aka: hydrocodone + acetaminophen
58
vicoprofen
aka: hydrocodone + ibuprofen
59
fluoxetine
aka: Prozac Class: SSRI Use: antidepressant, possibly OCD MOA: blocks serotonin reuptake, has a long-lasting active metabolite Toxicity: GI disturbances, sexual dysfunction, decreased libido are common side effects CI: no MAOIs, must 2 week washout period before you can give MAOIs -Metabolized by P450, so avoid other drugs that are also metabolized by P450
60
sertraline
aka: Zoloft Class: SSRI Use: antidepressant MOA: blocks serotonin reuptake Toxicity: GI disturbances, sexual dysfunction, decreased libido are common side effects CI: Metabolized by P450, so avoid other drugs that are also metabolized by P450
61
citalopram
aka: Celexa Class: SSRI Use: antidepressant MOA: blocks serotonin reuptake Toxicity: GI disturbances, sexual dysfunction, decreased libido are common side effects CI: not metabolized by p450 so has fewer drug interactions
62
paroxetine
aka: Paxil Class: SSRI Use: antidepressant MOA: blocks serotonin reuptake Toxicity: GI disturbances, sexual dysfunction, decreased libido are common side effects CI: Metabolized by P450, so avoid other drugs that are also metabolized by P450
63
fluvoxamine
THIS IS ALL THAT WAS STRESSED IN POWERPOINT Class: SSRI Use: OCD MOA: Toxicity: CI: *don't give with ramelteon*
64
escitalopram
aka: Lexapro Class: SSRI Use: antidepressant MOA: blocks serotonin reuptake Toxicity: GI disturbances, sexual dysfunction, decreased libido are common side effects CI: not metabolized by p450 so has fewer drug interactions
65
venlafaxine
aka: Effexor Class: SNRI Use: antidepressant MOA: potent serotonin reuptake inhibitor, weak NE reuptake inhibitor Toxicity: CI: little interaction with CYP enzymes, so few drug interactions
66
desvenlaxafine
aka: Pristique same as venlafaxine minus a methyl group Class: SNRI Use: antidepressant MOA: potent serotonin reuptake inhibitor, weak NE reuptake inhibitor Toxicity: CI: little interaction with CYP enzymes, so few drug interactions
67
duloxetine
aka: Cymbalta Class: SNRI Use: antidepressant MOA: Blocks serotonin and NE reuptake Toxicity: little sedation CI:
68
desipramine
aka: Norpramin Class: TCA Use: antidepressant MOA: blocks NE reuptake, does NOT block serotonin reuptake (exception to the rule) Toxicity: also block histamine, alpha-adrenergic and muscarinic receptors=lots of side effects (Sedation, orthostatic hypotension, urinary retention, constipation, weight gain), -O.D. IS FATAL (cardiac arrythmias due to muscarinic blockade) CI: No alcohol!
69
imipramine
aka: Tofranil Class: TCA Use: antidepressant MOA: block NE and serotonin reuptake Toxicity: also block histamine, alpha-adrenergic and muscarinic receptors=lots of side effects (Sedation, orthostatic hypotension, urinary retention, constipation, weight gain), -O.D. IS FATAL (cardiac arrythmias due to muscarinic blockade) CI: No alcohol!
70
amitriptyline
aka: Elavil Class: TCA Use: antidepressant MOA: block NE and serotonin reuptake Toxicity: also block histamine, alpha-adrenergic and muscarinic receptors=lots of side effects (Sedation, orthostatic hypotension, urinary retention, constipation, weight gain), -O.D. IS FATAL (cardiac arrythmias due to muscarinic blockade) CI: No alcohol!
71
nortriptyline
aka: Pamelor Class: TCA Use: antidepressant MOA: block NE and serotonin reuptake Toxicity: also block histamine, alpha-adrenergic and muscarinic receptors=lots of side effects (Sedation, orthostatic hypotension, urinary retention, constipation, weight gain), -O.D. IS FATAL (cardiac arrythmias due to muscarinic blockade) CI: No alcohol!
72
trazodone
aka: Desyrel Class: 5-HT(2A) receptor antagonist Use: antidepressant, sometimes as a hypnotic MOA: 5-HT(2A) receptor antagonist - weak serotonin reuptake inhibitor - also activates 5-HT1 receptors Toxicity: sleepiness CI:
73
nefazodone
aka: Class: 5-HT(2A) receptor antagonist Use: antidepressant MOA: 5-HT(2A) receptor antagonist - also has anti-muscarinic properties, - also a weak inhibitor of SERT and NET Toxicity: sleepiness, hepatic toxicity, fewer sexual side effects than SSRIs CI:
74
buproprion
aka: Wellbutrin Class: Tetracyclics/Unicyclics Use: antidepressant, smoking cessation MOA: blocks DA reuptake but NOT serotonin or NE Toxicity: CI:
75
mirtazapine
aka: Remeron Class: Tetracyclics/Unicyclics Use: depression w/insomnia MOA: antagonist at 5-HT2 and alpha2 adrenergic receptors (indirectly increases release of NE) -no activity at NE, 5-HT transporters Toxicity: antihistaminic activity=sedation, weight gain CI:
76
amoxapine
aka: Class: Tetracyclics/Unicyclics Use: depression in psychotic patients MOA: Potent blockade of NE reuptake; less so for serotonin -also blocks DA D2 receptors and muscarinic receptors (retains some antipsychotic properties) Toxicity: similar to TCAs w/ a few toxicities from antipsychotics CI:
77
maprotiline
aka: Class: Tetracyclics/Unicyclics Use: antidepressant MOA: Potent inhibitor of NE reuptake; less potent inhibition of 5-HT reuptake -anticholinergic as well Toxicity: muscarinic blockade symptoms CI:
78
phenelzine
aka: Nardil Class: MAOI Use: last resort antidepressants for atypical and treatment resistant depression MOA: non-selective irreversible inhibitor of both MAO-A and MAO-B Toxicity: orthostatic hypotension, Sleep disturbances, weight gain CI: Assume it's still in the system for 2-3 weeks, avoid indirect sympathomimetics (e.g. OTC phenylephrine), stimulants for ADHD, tyramine-rich foods, SSRIs, opiods.
79
isocarboxazid
NOT IN POWERPOINT aka: Marplan Class: MAOI Use: MOA: Toxicity: CI: avoid indirect sympathomimetics (e.g. OTC phenylephrine), stimulants for ADHD, tyramine-rich foods, SSRIs, opiods.
80
tranylcypromine
aka: Parnate Class: MAOI Use: last resort antidepressants for atypical and treatment resistant depression MOA: non-selective prolonged inhibitor of both MAO-A and MAO-B Toxicity: orthostatic hypotension, Sleep disturbances, weight gain CI: Assume it's still in the system for 7 days, avoid indirect sympathomimetics (e.g. OTC phenylephrine), stimulants for ADHD, tyramine-rich foods, SSRIs, opiods.
81
selegeline
NOT IN POWERPOINT aka: Eldepryl Class: MAOI Use: MOA: Toxicity: CI: avoid indirect sympathomimetics (e.g. OTC phenylephrine), stimulants for ADHD, tyramine-rich foods, SSRIs, opiods.
82
St John's Wort
aka: Class: Common herbal supplement Use: hippie happiness MOA: inhibition of nerve terminal reuptake of serotonin, NE and DA -if dose is high enough MAO-A and -B inhibitor properties (recommended dose not strong enough for these effects) Toxicity: headache, possible photosensitization CI: don't take w/MAOIs, SSRIs, or anything that blocks serotonin reuptake
83
lithium
aka: Class: Mood stabilizer Use: bipolar disorder (most common drug) MOA: inhibits inositol substrate recycling (this depletes PIP2, which reduces IP3 and DAG, which decreases PKC activation, which leads to changes in gene expression) -may also inhibit NE-stimulated adenylyl cyclase (turns everything down a notch) Toxicity: serum levels must be monitored - shaky shaky (tremors) - thirsty and pissing a lot CI: diuretics will change clearance rates - newer NSAIDs can reduce clearance rate - avoid typical antipsychotics (increases EP side effects of antipsychotics)
84
gamma hydroxybutyrate
aka: GHB Class: Drug of Abuse Use: Get high, CNS depressant MOA: acts on GABAergic neurons and interferes with memory formation Toxicity: CI:
85
rohypnol
aka: Roofies Class: Drug of Abuse Use: Get high, rape chicks, steal Mike Tyson's tiger, CNS depressant MOA: acts on GABAergic neurons and interferes with memory formation Toxicity: CI:
86
inhalants
enhance/alter mood Nitrites-blood vessel dilation, sexual enhancers
87
phencyclidine
aka: PCP Class: Drugs of Abuse Use: psychedelic drug MOA: NMDA receptor antagonist Toxicity: CI:
88
lysergic acid diethylamine
aka: Class: Drug of Abuse Use: psychedelic drug MOA: agonist at 5-HT2 and 5-HT1A receptors Toxicity: CI:
89
3,4-methylenedioxymethamphetamine
aka: MDMA Class: Drug of Abuse Use: psychedelic, psychostimulant MOA: serotonin transporter reversal, w/ a smaller effect on NE and DA Toxicity: CI:
90
delta-9-tetrahydrocannabinol
aka: THC Class: Drug of Abuse Use: MOA: binds to cannabinoid receptors Toxicity: CI:
91
oxazepam
aka: Class: Benzodiazepine (intermediate acting) Use: alcohol withdrawal of patients w/ liver problems MOA: binds to activated GABAA receptor between alpha and gamma subunits (GABA binds at alpha) and facilitates increased activation of the receptor. Lower dose=anxiolytic, higher dose=hypnotic Toxicity: dependence (withdrawal syndrome: anxiety, insomnia, convulsions) CI: not metabolized by P450 in liver (exception to rule) so less contraindications
92
disulfuram
aka: Class: Use: long term alcohol cessation MOA: blocks aldehyde dehydrogenase, acetylaldehyde levels rise and make patient feel terrible Toxicity: CI: watch out for hidden sources of alcohol like Nyquil
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varenicline
aka: Chantix Class: Use: smoking cessation MOA: partial nAChR agonist w/ greater affinity than nicotine Toxicity: CI:
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flumazenil
aka: Class: Benzodiazepine antagonist Use: reverse the effects of a benzodiazepine MOA: competes at benzodiazepine binding site on GABAA receptor. -Cleared very rapidly and has a short half-life, must give several doses for benzodiazepines w/long half-lives Toxicity: agitation, hostility, depression, suicidal tendencies CI:
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triazolam
aka: Halcion Class: Benzodiazepine (short acting, half-life less than 6hrs) Use: panic disorder MOA: binds to activated GABAA receptor between alpha and gamma subunits (GABA binds at alpha) and facilitates increased activation of the receptor. - Lower dose=anxiolytic, higher dose=hypnotic - tolerance w/chronic use due to down regulation of binding sites. Toxicity: dependence (withdrawal syndrome: anxiety, insomnia, convulsions) CI: don't take w/ alcohol, opioids, anticonvulsants, phenothiazines due to highly additive CNS depression -don't take with antihistamines, antihypertensives, tricyclic antidepressants due to partially additive CNS depression
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alprazolam
aka: Class: Benzodiazepine (intermediate acting half-life; between 6 and 24 hours)) Use: panic disorder MOA: binds to activated GABAA receptor between alpha and gamma subunits (GABA binds at alpha) and facilitates increased activation of the receptor. - Lower dose=anxiolytic, higher dose=hypnotic - tolerance w/chronic use due to down regulation of binding sites. Toxicity: dependence (withdrawal syndrome: anxiety, insomnia, convulsions) CI: don't take w/ alcohol, opioids, anticonvulsants, phenothiazines due to highly additive CNS depression -don't take with antihistamines, antihypertensives, tricyclic antidepressants due to partially additive CNS depression
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chlordiazepoxide
aka: Class: Benzodiazepine (long acting, t1/2>24hrs) Use: bunch of stuff (anxiety, balanced anesthesia, sedation/amnesia during procedures, sleep problems MOA: binds to activated GABAA receptor between alpha and gamma subunits (GABA binds at alpha) and facilitates increased activation of the receptor. - Lower dose=anxiolytic, higher dose=hypnotic - tolerance w/chronic use due to down regulation of binding sites. Toxicity: dependence (withdrawal syndrome: anxiety, insomnia, convulsions) CI: don't take w/ alcohol, opioids, anticonvulsants, phenothiazines due to highly additive CNS depression -don't take with antihistamines, antihypertensives, tricyclic antidepressants due to partially additive CNS depression
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desmethyldiazepam
aka: Class: Benzodiazepine (long acting, t1/2>24hrs) Use: bunch of stuff (anxiety, balanced anesthesia, sedation/amnesia during procedures, sleep problems MOA: binds to activated GABAA receptor between alpha and gamma subunits (GABA binds at alpha) and facilitates increased activation of the receptor. - Lower dose=anxiolytic, higher dose=hypnotic - tolerance w/chronic use due to down regulation of binding sites. Toxicity: dependence (withdrawal syndrome: anxiety, insomnia, convulsions) CI: don't take w/ alcohol, opioids, anticonvulsants, phenothiazines due to highly additive CNS depression -don't take with antihistamines, antihypertensives, tricyclic antidepressants due to partially additive CNS depression
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flurazepam
aka: Class: Benzodiazepine (long acting, t1/2>24hrs) Use: bunch of stuff (anxiety, balanced anesthesia, sedation/amnesia during procedures, sleep problems MOA: binds to activated GABAA receptor between alpha and gamma subunits (GABA binds at alpha) and facilitates increased activation of the receptor. - Lower dose=anxiolytic, higher dose=hypnotic - tolerance w/chronic use due to down regulation of binding sites. Toxicity: dependence (withdrawal syndrome: anxiety, insomnia, convulsions) CI: don't take w/ alcohol, opioids, anticonvulsants, phenothiazines due to highly additive CNS depression -don't take with antihistamines, antihypertensives, tricyclic antidepressants due to partially additive CNS depression
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diazepam
aka: Class: Benzodiazepine (long acting, t1/2>24hrs) Use: bunch of stuff (anxiety, balanced anesthesia, sedation/amnesia during procedures, sleep problems MOA: binds to activated GABAA receptor between alpha and gamma subunits (GABA binds at alpha) and facilitates increased activation of the receptor. - Lower dose=anxiolytic, higher dose=hypnotic - tolerance w/chronic use due to down regulation of binding sites. Toxicity: dependence (withdrawal syndrome: anxiety, insomnia, convulsions) CI: don't take w/ alcohol, opioids, anticonvulsants, phenothiazines due to highly additive CNS depression -don't take with antihistamines, antihypertensives, tricyclic antidepressants due to partially additive CNS depression
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lorazepam
aka: Class: Benzodiazepine (intemediate acting, t1/2=6-24hrs) Use: bunch of stuff (anxiety, balanced anesthesia, sedation/amnesia during procedures, sleep problems MOA: binds to activated GABAA receptor between alpha and gamma subunits (GABA binds at alpha) and facilitates increased activation of the receptor. - Lower dose=anxiolytic, higher dose=hypnotic - tolerance w/chronic use due to down regulation of binding sites. Toxicity: dependence (withdrawal syndrome: anxiety, insomnia, convulsions) CI: don't take w/ alcohol, opioids, anticonvulsants, phenothiazines due to highly additive CNS depression -don't take with antihistamines, antihypertensives, tricyclic antidepressants due to partially additive CNS depression
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thiopental
aka: Class: Barbiturate Use: General Anesthetic (IV) MOA: increases duration of GABA(A) opening - Knocks pt out quickly (Highly soluble; plasma:brain equilibrium occurs rapidly) - Pt can come back quickly (rapidly diffuses out of brain and into muscle and fat) - potent respiratory depressant - dose dependent decrease in cardiac output - OK for pts with increased ICP Other stuff same as other barbiturates
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secobarbital
aka: Class: Barbiturate Use: MOA: binds to activated GABAA receptor between alpha and gamma subunits (GABA binds at alpha) and facilitates increased activation of the receptor. - Lower dose=anxiolytic, higher dose=hypnotic - tolerance w/chronic use due to increased metabolism of drug Toxicity: dependence (withdrawal syndrome: anxiety, insomnia, convulsions) CI: don't take w/ alcohol, opioids, anticonvulsants, phenothiazines due to highly additive CNS depression -don't take with antihistamines, antihypertensives, tricyclic antidepressants due to partially additive CNS depression
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phenobarbital
aka: Class: Barbiturate Use: MOA: binds to activated GABAA receptor between alpha and gamma subunits (GABA binds at alpha) and facilitates increased activation of the receptor. - Lower dose=anxiolytic, higher dose=hypnotic - tolerance w/chronic use due to increased metabolism of drug Toxicity: dependence (withdrawal syndrome: anxiety, insomnia, convulsions) CI: don't take w/ alcohol, opioids, anticonvulsants, phenothiazines due to highly additive CNS depression -don't take with antihistamines, antihypertensives, tricyclic antidepressants due to partially additive CNS depression
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benzodiazepines for sleep
- shortens sleep latency - decreases time in slow wave sleep (stages 3-4) - increases time in non-REM light sleep (stage 2) - increases cycles of REM but decreases time spent in REM
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zolpidem
aka: Ambien, Intermezzo Class: hypnotic Use: fall asleep faster MOA: bind to same spot as benzos -sublingual dose (Intermezzo) for middle of night awakenings Toxicity: -increases slow wave sleep - decreases time in REM - sleep longer - alterations in REM after you stop taking it (rebound insomnia) - amnesia at high doses CI:
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zaleplon
aka: Sonata Class: hypnotic Use: fall asleep faster MOA: bind to same spot as benzos - fast acting with short half-life - less amnesia and grogginess than zolpidem and benzos Toxicity: little effect on total sleep time (REM or non-REM) CI:
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eszopiclone
aka: Lunesta Class: Use: fall asleep faster MOA: bind to same spot as benzos -long half life Toxicity: increases total sleep time - increases stage 2 sleep - less amnesia and grogginess than zolpidem and benzos CI:
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buspirone
aka: Buspar Class: other sedative-hypnotic Use: anxiolytic for all types of anxiety (not for panic attacks cause it takes too long to kick in) MOA: 5-HT1A and DA D2 partial agonist (doesn't make sense but it works) - Does NOT interact with GABA(A) receptors - takes longer than a week to kick in Toxicity: CI:
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ramelteon
aka: Class: other sedative-hypnotic Use: fall asleep faster MOA: melatonin receptor agonist - No direct action on GABA(A) receptors - active form has long half-life Toxicity: dizziness, grogginess, endocrine changes, decreases in testosterone and prolactin. -no rebound insomnia or withdrawal symptoms CI: don't use w/fluvoxamine (inhibits CYP1A2)
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clonidine
aka: Class: sympatholytic Use: short term opioid detox MOA: alpha-2 adrenergic receptor agonist Toxicity: CI:
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chlorpromazine
aka: Class: Typical antipsychotic (phenothiazine) Use: antipsycotic MOA: Strong D2 antagonist (relatively lower so less EP side effects) -also blocks alpha-adrenergic, muscarinic, H1, and serotonin receptors Toxicity: lots of side effects due to extra MOAs - stiff neck (acute dystonia), can't sit still (akathisia), dry mouth, urinary retention, orthostatic hypotension, sedation, neuroleptic malignant hypothermia - hyperprolactinemia (results in amenorrhea-galactorrhea in females, and hypogonadism in males) CI: No opioids!
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fluphenazine
aka: Class: Typical antipsychotic (phenothiazine) Use: antipsycotic MOA: Strong D2 antagonist -also blocks alpha-adrenergic, muscarinic, H1, and serotonin receptors Toxicity: lots of side effects due to extra MOAs - stiff neck (acute dysonia), can't sit still (akathisia), dry mouth, urinary retention, orthostatic hypotension, sedation, neuroleptic malignant hypothermia - hyperprolactinemia (results in amenorrhea-galactorrhea in females, and hypogonadism in males) CI: No opioids!
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thioridizine
aka: Class: Typical antipsychotic (phenothiazine) Use: antipsycotic MOA: Strong D2 antagonist -also blocks alpha-adrenergic, muscarinic, H1, and serotonin receptors Toxicity: lots of side effects due to extra MOAs - stiff neck (acute dysonia), can't sit still (akathisia), dry mouth, urinary retention, orthostatic hypotension, sedation, neuroleptic malignant hypothermia - hyperprolactinemia (results in amenorrhea-galactorrhea in females, and hypogonadism in males) CI: No opioids!
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haloperidol
aka: Class: Typical antipsychotic Use: antipsycotic MOA: Strong D2 antagonist - more potent than phenothiazines - fast onset Toxicity: fewer side effects that phenothiazines CI: No opioids!
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thiothixene
aka: Class: Typical antipsychotic Use: antipsycotic MOA: Strong D2 antagonist -slightly less potent than phenothiazines Toxicity: stiff neck (acute dysonia), can't sit still (akathisia), dry mouth, urinary retention, orthostatic hypotension, sedation, neuroleptic malignant hypothermia -hyperprolactinemia (results in amenorrhea-galactorrhea in females, and hypogonadism in males) CI: No opiods!
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clozapine
aka: Class: Atypical antipsychotic Use: positive and negative symptoms of schizophrenia -mood stabilizer MOA: serotonin-dopamine antagonists -greater affinity for 5-HT(2A) receptors than for D2 receptors (full D2 agonist though) Toxicity: reduced extrapyramidal side effects - weight gain - hypertriglyceridemia - agranulocytosis (decrease in WBCs) CI:
118
olanzapine
aka: Class: Atypical antipsychotic Use: positive and negative symptoms of schizophrenia -mood stabilizer MOA: serotonin-dopamine antagonists -greater affinity for 5-HT(2A) receptors than for D2 receptors (full D2 agonist though) Toxicity: reduced extrapyramidal side effects - weight gain - hypertriglyceridemia CI:
119
quetiapine
aka: Class: Atypical antipsychotic Use: positive and negative symptoms of schizophrenia -mood stabilizer MOA: serotonin-dopamine antagonists -greater affinity for 5-HT(2A) receptors than for D2 receptors (full D2 agonist though) Toxicity: reduced extrapyramidal side effects CI:
120
ziprasidone
aka: Class: Atypical antipsychotic Use: positive and negative symptoms of schizophrenia -mood stabilizer MOA: serotonin-dopamine antagonists -greater affinity for 5-HT(2A) receptors than for D2 receptors (full D2 agonist though) Toxicity: reduced extrapyramidal side effects CI:
121
risperidone
aka: Class: Atypical antipsychotic Use: positive and negative symptoms of schizophrenia -mood stabilizer MOA: serotonin-dopamine antagonists -greater affinity for 5-HT(2A) receptors than for D2 receptors (full D2 agonist though) Toxicity: reduced extrapyramidal side effects CI:
122
aripiprazole
aka: Class: Atypical antipsychotic Use: positive and negative symptoms of schizophrenia -mood stabilizer MOA: serotonin-dopamine antagonists -greater affinity for 5-HT(2A) receptors than for D2 receptors (only a PARTIAL D2 agonist, which means it acts as an antagonist) Toxicity: reduced extrapyramidal side effects CI:
123
asenapine
aka: Class: Atypical antipsychotic Use: positive and negative symptoms of schizophrenia -mood stabilizer MOA: serotonin-dopamine antagonists -greater affinity for 5-HT(2A) receptors than for D2 receptors (full D2 agonist though) Toxicity: reduced extrapyramidal side effects CI:
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Stages of General Anesthesia
Stage I: Analgesia Stage II: Excitement Stage III: Surgical Anesthesia Stage IV: Medullary Depression
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Stage I of General Anesthesia
Analgesia -Relaxed with no amnesia
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Stage II of General Anesthesia
Excitement -Delirium, irregular respiration, amnesia Need to get through this phase quickly
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Stage III of General Anesthesia
Surgical Anesthesia - Begins with recurrence of normal respiration and extends to complete cessation of spontaneous respiration - Loss of responsiveness to noxious stimuli
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Stage IV of General Anesthesia
Medullary Depression -Severe depression of vasomotor and respiratory centers in medulla
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1 MAC = ?
1 MAC = immobility in 50% of patients "Minimum Alveolar Anesthetic Concentration" Median concentration (as percentage of alveolar gas mixture) that results in immobility in 50% of patients ED50 on a dose response curve
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nitrous oxide
aka: Class: General Anesthetic (Inhaled) Use: MOA: Toxicity: cerebral blood flow is increased due to decreased cerebral vascular resistance -malignant hyperthermia (genetic disorder, tachycardia, hypertension, muscle rigidity, hyperthermia, hyperkalemia) CI: pts w/increased intracranial pressure
131
sevoflurane
aka: Class: General Anesthetic (Inhaled) Use: MOA: Toxicity: cerebral blood flow is increased due to decreased cerebral vascular resistance -malignant hyperthermia (genetic disorder, tachycardia, hypertension, muscle rigidity, hyperthermia, hyperkalemia) CI: pts w/increased intracranial pressure
132
isoflurane
aka: Class: General Anesthetic (Inhaled) Use: MOA: Toxicity: cerebral blood flow is increased due to decreased cerebral vascular resistance -malignant hyperthermia (genetic disorder, tachycardia, hypertension, muscle rigidity, hyperthermia, hyperkalemia) CI:pts w/increased intracranial pressure
133
halothane
aka: Class: General Anesthetic (Inhaled) Use: MOA: Toxicity: cerebral blood flow is increased due to decreased cerebral vascular resistance -malignant hyperthermia (genetic disorder, tachycardia, hypertension, muscle rigidity, hyperthermia, hyperkalemia) CI:pts w/increased intracranial pressure
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midazolam
aka: Class: Benzodiazepine (short acting) Use: General Anesthetic (IV) MOA: increases frequency of GABA(A) channel openings - water soluble - slower onset of CNS depressant effects than barbs - won't produce surgical anesthesia all by its lonesome; usually given prior to entry into OR - more rapid onset and shorter half-life than other benzos
135
propofol
aka: Class: General Anesthetic Use: Most Popular IV Anesthetic (for induction and maintenance MOA: Not fully understood, probably something to do with GABA -rate of onset and action similar to barbs, but recovery is more rapid Toxicity: Less post-op nausea and vomiting than barbs CI:
136
etomidate
aka: Class: General Anesthetic Use: Induction of anesthesia MOA: Not fully understood, probably something to do with GABA - rapid loss of consciousness - short duration of action - NO ANALGESIC EFFECTS; may need opiods w/it Toxicity: minimal cardiac and respiratory depression (good for someone in shock) CI:
137
ketamine
aka: Class: General Anesthetic, drug of abuse Use: Produces dissociative amnesia, psychedelic drug MOA: NMDA receptor antagonist - highly lipophilic - analgesic and anesthetic - minimal ventilatory depression; can give w/ other stuff - good in geriatrics and septic shock pts Toxicity: psychic phenomena (lucid dreams, hallucinations, etc.); can be helped by adding benzos CI:
138
sulfentanil
aka: Class: Opioid Use: adjunct in anesthesia MOA: Toxicity: CI: