Pharm (Advanced) Flashcards
amphetamine
Use: Narcolepsy, ADHD
MOA: Nervous system stimulant (incr. DA levels in CNS)
CI/Toxicity: Depresses appetite, ascorbic acid decr. absorption /alkaline incr. absorp.
methamphetamine
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
ephedrine
Use:
MOA: Activates β-receptors, Orally active, Long duration of action
CI/Toxicity: Cardiac problems
tyramine
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
modafinil
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
atomoxetine
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
methylphenidate
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
dexmethylphenidate
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
dextroamphetamine
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
lisdexamfetamine
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
amphetamine mixed salts
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
valproic acid
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
phenobarbital
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:
carbamazepine
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
phenytoin
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
diazepam
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:
clonazepam
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:
primidone
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:
ethosuximide
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:
gabapentin
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:
pregabalin
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:
tiagabine
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:
topiramate
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:
lamotrigine
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:
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:
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
rabies immune globulin
Use: prophylaxis for rabies
MOA: passive immunization (IgG mainly)
CI/Toxicity:
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
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.
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
propanolol
Class: Beta blocker
Use: Migraine prophylaxis
MOA: Beta blocker
CI/Toxicity: not stressed in powerpoint
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)
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)
donepezil
aka: Aricept
Class: cholinesterase inhibitor
Use: Adjunct to memantine for Alzheimer’s
MOA: reversible cholinesterase antagonist
CI/Toxicity: nausea, diarrhea, vomiting
rivastigmine
aka: Exelon
Class: cholinesterase inhibitor
Use: Adjunct to memantine for Alzheimer’s
MOA: reversible cholinesterase antagonist
CI/Toxicity: nausea, diarrhea, vomiting
galantamine
aka:
Class: cholinesterase inhibitor
Use: Adjunct to memantine for Alzheimer’s
MOA: reversible cholinesterase antagonist
CI/Toxicity: nausea, diarrhea, vomiting
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)
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
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
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
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
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
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
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
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
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
propoxyphene
aka:
Class: Mild to Moderate Opioid Agonist
Use: mild analgesic and cough suppressant
MOA: partial mu agonist
Toxicity: Minimal when taken as directed
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
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,
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
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
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)
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)
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:
percocet
aka: oxycodone + acetaminophen
percodan
aka: oxycodone + aspirin
vicodin/lortab
aka: hydrocodone + acetaminophen
vicoprofen
aka: hydrocodone + ibuprofen
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
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
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
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
fluvoxamine
THIS IS ALL THAT WAS STRESSED IN POWERPOINT
Class: SSRI
Use: OCD
MOA:
Toxicity:
CI: don’t give with ramelteon
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
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
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
duloxetine
aka: Cymbalta
Class: SNRI
Use: antidepressant
MOA: Blocks serotonin and NE reuptake
Toxicity: little sedation
CI:
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!
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!
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!
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!
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:
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:
buproprion
aka: Wellbutrin
Class: Tetracyclics/Unicyclics
Use: antidepressant, smoking cessation
MOA: blocks DA reuptake but NOT serotonin or NE
Toxicity:
CI:
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:
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:
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:
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.
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.
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.
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.
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
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)
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:
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:
inhalants
enhance/alter mood
Nitrites-blood vessel dilation, sexual enhancers
phencyclidine
aka: PCP
Class: Drugs of Abuse
Use: psychedelic drug
MOA: NMDA receptor antagonist
Toxicity:
CI:
lysergic acid diethylamine
aka:
Class: Drug of Abuse
Use: psychedelic drug
MOA: agonist at 5-HT2 and 5-HT1A receptors
Toxicity:
CI:
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:
delta-9-tetrahydrocannabinol
aka: THC
Class: Drug of Abuse
Use:
MOA: binds to cannabinoid receptors
Toxicity:
CI:
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
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
varenicline
aka: Chantix
Class:
Use: smoking cessation
MOA: partial nAChR agonist w/ greater affinity than nicotine
Toxicity:
CI:
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:
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
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
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
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
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
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
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
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
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
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
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
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:
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:
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:
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:
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)
clonidine
aka:
Class: sympatholytic
Use: short term opioid detox
MOA: alpha-2 adrenergic receptor agonist
Toxicity:
CI:
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!
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!
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!
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!
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!
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:
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:
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:
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:
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:
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:
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:
Stages of General Anesthesia
Stage I: Analgesia
Stage II: Excitement
Stage III: Surgical Anesthesia
Stage IV: Medullary Depression
Stage I of General Anesthesia
Analgesia
-Relaxed with no amnesia
Stage II of General Anesthesia
Excitement
-Delirium, irregular respiration, amnesia
Need to get through this phase quickly
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
Stage IV of General Anesthesia
Medullary Depression
-Severe depression of vasomotor and respiratory centers in medulla
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
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
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
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
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
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
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:
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:
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:
sulfentanil
aka:
Class: Opioid
Use: adjunct in anesthesia
MOA:
Toxicity:
CI:
