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Pharm (Advanced) Flashcards

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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25
Q

zonisamide

A

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:

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26
Q

Acyclovir

A

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

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27
Q

rabies immune globulin

A

Use: prophylaxis for rabies

MOA: passive immunization (IgG mainly)

CI/Toxicity:

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28
Q

sumatriptan

A

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

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29
Q

ergotamine

A

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.

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30
Q

timolol

A

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

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31
Q

propanolol

A

Class: Beta blocker

Use: Migraine prophylaxis

MOA: Beta blocker

CI/Toxicity: not stressed in powerpoint

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32
Q

valproate

A

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)

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33
Q

topiramate

A

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)

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34
Q

donepezil

A

aka: Aricept

Class: cholinesterase inhibitor

Use: Adjunct to memantine for Alzheimer’s

MOA: reversible cholinesterase antagonist

CI/Toxicity: nausea, diarrhea, vomiting

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35
Q

rivastigmine

A

aka: Exelon

Class: cholinesterase inhibitor

Use: Adjunct to memantine for Alzheimer’s

MOA: reversible cholinesterase antagonist

CI/Toxicity: nausea, diarrhea, vomiting

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36
Q

galantamine

A

aka:

Class: cholinesterase inhibitor

Use: Adjunct to memantine for Alzheimer’s

MOA: reversible cholinesterase antagonist

CI/Toxicity: nausea, diarrhea, vomiting

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37
Q

memantine

A

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)

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38
Q

morphine

A

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

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39
Q

hydromorphone

A

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

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40
Q

oxymorphone

A

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

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41
Q

methadone

A

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

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42
Q

fentanyl

A

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

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43
Q

meperidine

A

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

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44
Q

codeine

A

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

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45
Q

hydrocodone

A

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

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46
Q

oxycodone

A

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

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47
Q

propoxyphene

A

aka:

Class: Mild to Moderate Opioid Agonist

Use: mild analgesic and cough suppressant

MOA: partial mu agonist

Toxicity: Minimal when taken as directed

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48
Q

nalbuphine

A

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

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49
Q

buprenorphine

A

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,

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50
Q

butorphanol

A

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

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51
Q

tramadol

A

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

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52
Q

dextromethorphan

A

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)

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53
Q

naloxone

A

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)

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54
Q

naltrexone

A

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:

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55
Q

percocet

A

aka: oxycodone + acetaminophen

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56
Q

percodan

A

aka: oxycodone + aspirin

57
Q

vicodin/lortab

A

aka: hydrocodone + acetaminophen

58
Q

vicoprofen

A

aka: hydrocodone + ibuprofen

59
Q

fluoxetine

A

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
Q

sertraline

A

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
Q

citalopram

A

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
Q

paroxetine

A

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
Q

fluvoxamine

A

THIS IS ALL THAT WAS STRESSED IN POWERPOINT

Class: SSRI

Use: OCD

MOA:

Toxicity:

CI: don’t give with ramelteon

64
Q

escitalopram

A

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
Q

venlafaxine

A

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
Q

desvenlaxafine

A

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
Q

duloxetine

A

aka: Cymbalta

Class: SNRI

Use: antidepressant

MOA: Blocks serotonin and NE reuptake

Toxicity: little sedation

CI:

68
Q

desipramine

A

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
Q

imipramine

A

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
Q

amitriptyline

A

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
Q

nortriptyline

A

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
Q

trazodone

A

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
Q

nefazodone

A

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
Q

buproprion

A

aka: Wellbutrin

Class: Tetracyclics/Unicyclics

Use: antidepressant, smoking cessation

MOA: blocks DA reuptake but NOT serotonin or NE

Toxicity:

CI:

75
Q

mirtazapine

A

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
Q

amoxapine

A

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
Q

maprotiline

A

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
Q

phenelzine

A

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
Q

isocarboxazid

A

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
Q

tranylcypromine

A

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
Q

selegeline

A

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
Q

St John’s Wort

A

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
Q

lithium

A

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
Q

gamma hydroxybutyrate

A

aka: GHB

Class: Drug of Abuse

Use: Get high, CNS depressant

MOA: acts on GABAergic neurons and interferes with memory formation

Toxicity:

CI:

85
Q

rohypnol

A

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
Q

inhalants

A

enhance/alter mood

Nitrites-blood vessel dilation, sexual enhancers

87
Q

phencyclidine

A

aka: PCP

Class: Drugs of Abuse

Use: psychedelic drug

MOA: NMDA receptor antagonist

Toxicity:

CI:

88
Q

lysergic acid diethylamine

A

aka:

Class: Drug of Abuse

Use: psychedelic drug

MOA: agonist at 5-HT2 and 5-HT1A receptors

Toxicity:

CI:

89
Q

3,4-methylenedioxymethamphetamine

A

aka: MDMA

Class: Drug of Abuse

Use: psychedelic, psychostimulant

MOA: serotonin transporter reversal, w/ a smaller effect on NE and DA

Toxicity:

CI:

90
Q

delta-9-tetrahydrocannabinol

A

aka: THC

Class: Drug of Abuse

Use:

MOA: binds to cannabinoid receptors

Toxicity:

CI:

91
Q

oxazepam

A

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
Q

disulfuram

A

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

93
Q

varenicline

A

aka: Chantix

Class:

Use: smoking cessation

MOA: partial nAChR agonist w/ greater affinity than nicotine

Toxicity:

CI:

94
Q

flumazenil

A

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:

95
Q

triazolam

A

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

96
Q

alprazolam

A

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

97
Q

chlordiazepoxide

A

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

98
Q

desmethyldiazepam

A

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

99
Q

flurazepam

A

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

100
Q

diazepam

A

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

101
Q

lorazepam

A

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

102
Q

thiopental

A

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

103
Q

secobarbital

A

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

104
Q

phenobarbital

A

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

105
Q

benzodiazepines for sleep

A
  • 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
106
Q

zolpidem

A

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:

107
Q

zaleplon

A

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:

108
Q

eszopiclone

A

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:

109
Q

buspirone

A

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:

110
Q

ramelteon

A

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)

111
Q

clonidine

A

aka:

Class: sympatholytic

Use: short term opioid detox

MOA: alpha-2 adrenergic receptor agonist

Toxicity:

CI:

112
Q

chlorpromazine

A

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!

113
Q

fluphenazine

A

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!

114
Q

thioridizine

A

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!

115
Q

haloperidol

A

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!

116
Q

thiothixene

A

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!

117
Q

clozapine

A

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
Q

olanzapine

A

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
Q

quetiapine

A

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
Q

ziprasidone

A

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
Q

risperidone

A

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
Q

aripiprazole

A

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
Q

asenapine

A

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:

124
Q

Stages of General Anesthesia

A

Stage I: Analgesia

Stage II: Excitement

Stage III: Surgical Anesthesia

Stage IV: Medullary Depression

125
Q

Stage I of General Anesthesia

A

Analgesia

-Relaxed with no amnesia

126
Q

Stage II of General Anesthesia

A

Excitement

-Delirium, irregular respiration, amnesia

Need to get through this phase quickly

127
Q

Stage III of General Anesthesia

A

Surgical Anesthesia

  • Begins with recurrence of normal respiration and extends to complete cessation of spontaneous respiration
  • Loss of responsiveness to noxious stimuli
128
Q

Stage IV of General Anesthesia

A

Medullary Depression

-Severe depression of vasomotor and respiratory centers in medulla

129
Q

1 MAC = ?

A

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

130
Q

nitrous oxide

A

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
Q

sevoflurane

A

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
Q

isoflurane

A

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
Q

halothane

A

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

134
Q

midazolam

A

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
Q

propofol

A

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
Q

etomidate

A

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
Q

ketamine

A

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
Q

sulfentanil

A

aka:

Class: Opioid

Use: adjunct in anesthesia

MOA:

Toxicity:

CI:

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