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60 Cards in this Set

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Opioids
Morphine, fentanyl, codeine, heroin, methadone, meperidine, destromethorphan

agonist at mu rectprs,open K+ channels decreasing vesicle release of ACh, NE, 5-HT, glutamate, substance P
Use: pain, cough suppressant (dextromethorpan), diarrhea (loperamide and diphenoxylate), acute pulmonary edema. maintenance for addicts (methadone)

Toxicity: addiction, respiratory depression, constipation, miosis, additive CNS depression with other drugs, no tolerance to miosis and constipation. treat with naloxone/naltrexone
Butorphanol
partial agonist at mu receptors and kappa receptors
Use: pain, causes less respiratory depression than full agonist
tramodol
weak opioid agonist and inhibits serotonin and NE reuptake
use: chronic pain

Toxicity: similar to opioids, decreases the seizure threshold
Phenytoin
increase sodium channel inactivation, increase refractory period, inhibit glutamate release from excitatory neurons
Use: GTC seizures, class IB antiarrythmics

nystagmus, diploxia, ataxia, sedation, gingival hyperplasia, hirsuitism, megaloblastic anemia (decreased folate absorption), teratogenesis (fetal hydantoin syndrome), SLE like syndrome, P450 inducer, peripheral neuropathy
Carbamazepine
increases sodium channel inactivation
diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenesis, P450 inducter, SIADH, stevens-johnson syndrome
Lamotrigine
blocks voltage gated sodium channels
stevens-johnson
gabapentin
inhibits calcium channels
sedation, ataxia
topiramate
blocks sodium channels, increase GABA action
sedation, mental dulling, kidney stones, weight loss
phenobarbital
increase GABA action by increasing the duration of Cl channel opening
Use: sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental)

Toxicity: sedation, tolerance, dependence, P450 inducer, respiratory or cardiac depression, drug interactions because of induction of liver microsomal enzymes
Treat overdose with symptom management
valproic acid
increase sodium channel inactivation, increase GABA concentration
GI distress, rare but fatal hepatotoxicity, neural tube defects, tremor, weight gain
diazepam
facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep
Use: anxiety, spasticity, status epilepticus, detoxification, night terrors, sleep walking, general anesthetic, hypnotic

Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates
Treat OD with flumazenil
lorazepam
facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep
Use: anxiety, spasticity, status epilepticus, detoxification, night terrors, sleep walking, general anesthetic, hypnotic

Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates
Treat OD with flumazenil
triazolam
facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep, short acting
Use: anxiety, spasticity, detoxification, night terrors, sleep walking, general anesthetic, hypnotic

Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates
Treat OD with flumazenil
oxazepam
facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep, short acting
Use: anxiety, spasticity, detoxification, night terrors, sleep walking, general anesthetic, hypnotic

Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates
Treat OD with flumazenil
midzolam
facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep, short acting
Use: anxiety, spasticity, detoxification, night terrors, sleep walking, general anesthetic, hypnotic

Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates
Treat OD with flumazenil
chlordiazepoxide
facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep
Use: anxiety, spasticity, detoxification, night terrors, sleep walking, general anesthetic, hypnotic

Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates
Treat OD with flumazenil
alprazolam
facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep
Use: anxiety, spasticity, detoxification, night terrors, sleep walking, general anesthetic, hypnotic

Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates
Treat OD with flumazenil
zolpidem
act via the BZ1 receptor subtye and is reversed by flumazenil
Use: non-anxiety related insomnia

Toxicity: ataxia, headaches, confusion. short duration with rapid metabolism by liver. only modest day after psychommotor depression and few amnestic effects
zaleplon
act via the BZ1 receptor subtye and is reversed by flumazenil
Use: non-anxiety related insomnia

Toxicity: ataxia, headaches, confusion. short duration with rapid metabolism by liver. only modest day after psychommotor depression and few amnestic effects
eszopiclone
act via the BZ1 receptor subtye and is reversed by flumazenil
Use: non-anxiety related insomnia

Toxicity: ataxia, headaches, confusion. short duration with rapid metabolism by liver. only modest day after psychommotor depression and few amnestic effects
halothane
myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
hepatotoxicity
enflurane
myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
proconvulsant
isoflurane
myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
sevoflurane
myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
methoxyflurane
myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
nephrotoxicity
nitrous oxide
myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
expansion of trapped gas
thiopental
IV anesthetic, high potency, high lipid solubility
induction of anesthesia and short surgical procedures

effect terminated by redistribution to fat and tissue , decreases cerebral blood flow
midazolam
IV anesthetic, adjunctively with gaseous anesthetics and narcotics
most common drug for endoscoppy

postoperative respiratory depression, decreased BP (treat OD with flumazenil), and amnesia
Ketamine
IV anesthetic, dissociative anesthetic, blocks NMDA receptors
cardiovascular stimulant

disorientation, hallucination, bad dreams, increases cerebral blood flow
morphine and fentanyl
IV anesthetic with other CNS depressants during general anasthesia
propofol
IV anesthetic, potentiates GABA receptor
rapid anesthesia induction and short procedures

less post-operative nausea than thiopental
Local anesthetics - esters
procaine, cocaine, tetracaine
Local anesthetics - amides
lidocaine, mepivacaine, bupivacaine
Local anesthetics`
block Na channels on inner portation of channel preferentially at activated NA channels (rapidly firing neurons)
in infected tissue, alkaline anesthetics are charged, so they can't penetrate tissue - need more

small diameter nerve fibers blocked more readibly than large, myelin more than non-myelin and size matters more
Local anesthetics Use
minor surgical procedures, spinal anesthesia
toxicity: CNS excitation, severe CV toxicity (bupicaine), hypertension, hypotension, arrythmias (cocaine)
Succinylcholine
selective for motor nicotinic receptor, depolarizing NM blocking drug
Phase I - prolonged depolarization (no antidote)

Phase II - repolarized but blocked, reverse with neostigmine
tubocurarine
nondepolarizing muscle blocking drugs, compete with ACh for receptors
reverse blockade with cholinesterase inhibitors
atracurium
nondepolarizing muscle blocking drugs, compete with ACh for receptors
reverse blockade with cholinesterase inhibitors
mivacurium
nondepolarizing muscle blocking drugs, compete with ACh for receptors
reverse blockade with cholinesterase inhibitors
pancuronium
nondepolarizing muscle blocking drugs, compete with ACh for receptors
reverse blockade with cholinesterase inhibitors
vecuronium
nondepolarizing muscle blocking drugs, compete with ACh for receptors
reverse blockade with cholinesterase inhibitors
rocuronium
nondepolarizing muscle blocking drugs, compete with ACh for receptors
reverse blockade with cholinesterase inhibitors
dantrolene
prevents release of Ca from sarcoplasmic reticulum of skeletal muscle
Use: malignant hyperthermia from inhalation anesthetics and succinylcholine & neuroleptic malignant syndrome
Bromocriptine
agonize dopamine receptors
Use: Parkinson's
pramipexole
agonize dopamine receptors
Use: Parkinson's
ropinirole
agonize dopamine receptors
Use: Parkinson's
amantadine
agonize dopamine receptors and may increase dopamine levels
Use: parkinson's and antiviral against influenza A
L-dopa/Carbidopa
L dopa can cross BBB and is converted to dopamine in CNS and carbidopa inhibits peripheral conversion
Use: Parkinsonism

Toxicity: arrhythmias from peripheral conversion, long term can cause dyskinesia after administration and akinesia between doses; these are limited by carbidopa
selegiline
selective MAO B inhibitor which preferentially metabolizes dopamine over NE and serotonin, increasing availability of dopamine
Use: Parkinson's with L-dopa

Toxicity: may enhance adverse of L-dopa
entacapone
COMT inhibitor, prevents L dopa degredation and increases availability
Use: Parkinson's
tolcapone
COMT inhibitor, prevents L dopa degredation and increases availability
Use: Parkinson's
benzotropine
curb excess cholinergic activity, antimuscarinic
Parkinson's; improves tremor and rigiditiy but has little effect on bradykinesia
essential/familial tremors
beta blockers
memantine
NMDA receptor antagonist that helps prevent excitotoxicity
Use: Alzheimer's

Toxicity: dizziness, confusion, hallucinations
donepezil
acetylcholineresterase inhibitor
nausea dizziness, insomnia
galantamine
acetylcholineresterase inhibitor
nausea dizziness, insomnia
rivastigmine
acetylcholineresterase inhibitor
nausea dizziness, insomnia
reserpine and tetrabenazine
amine depleting
huntington's
haloperidol
dopamine receptor antagonist
huntington's
sumatriptan
5HT1b/1d agpnost. causes vasconstriction and inhibits trigeminal activation and vasoactive peptide release, t1/2 = less than hours
Use: acute migraine, cluster H/As

Toxicity: coronary vasospasm (contraindicated in patients with CAD and prinzmetal's angina), mild tingling