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PDA EXAM 2
Drugs for exam 2 of PDA
55
Pharmacology
Professional
02/09/2010

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Term
morphine
Definition
opioid agonist
acts primarily on mu receptors
decreases GI motility
cough suppressant
euphoria
respiratory depression
emesis
miosis
histamine release
tolerance
dependence
Term
loperamide
Definition
opioid agonist
used as an opioid anti-diarrheal
poorly distributed in the brain
Term
fentanyl
Definition
opioid agonist
highly potent
short duration of action with rapid onset
used for acute pain
Term
sufentanil
Definition
opioid agonist
highly potent
short duration of action with rapid onset
used for acute pain
Term
methadone
Definition
opioid agonist
duration of action is considerably longer than morphine's
used for opioid based addictions and chronic pain management
acts via mu receptors
Term
heroin
Definition
opioid agonist
far more lipophilic than morphine
heavy abuse potential
Term
codeine
Definition
opioid agonist
20% of the analgesic effects of morphine
antitussive
less euphoria than morphine
Term
meperidine
Definition
opioid agonist
similar to morphine but causes restlessness instead of sedation
dry mouth
blurred vision
dependence
Term
tramadol
Definition
opioid agonist
postoperative pain
atypical opioid analgesic
weak agonist at mu receptors
actions at NE, 5HT, and GABA receptors
10% as potent as morphine (IV/IM)
better side effect profile than other opiates
Term
pentazocine
Definition
opioid agonist
mixed agonist/antagonist
agonist at kappa receptors
2 enantiomers one has affinity for kappa receptors and one has affinity for sigma receptors.
Term
buprenorphine
Definition
opioid mixed agonist/antagonist
partial agonist to mu receptor
long duration of action
behaves like morphine
can antagonize morphine
Term
naloxone
Definition
opioid antagonist
blocks all 3 subtypes of opioid receptors
produces rapid reversal of the effects of morphine
little effect on pain threshold
competitive antagonist
blocks respiratory depression
half life of 60 minutes
Term
naltrexone
Definition
opioid antagonist
long duration of action
nullifies the effects of opiates if a recovering addict fails
competitive antagonist
also used to manage alcoholism, reduces the rewarding effects of alcohol
Term
diazepam
Definition
benzodiazepine
antianxiety
Term
alprazolam
Definition
benzodiazepine
anti anxiety
panic disorders
Term
flurazepam
Definition
benzodiazepine
sedative (hypnosis)
long acting
Term
diazepam
Definition
benzodiazepine
sedative (hypnosis)
long acting
Term
temazepam
Definition
benzodiazepine
sedative (hypnosis)
middle acting
Term
triazolam
Definition
benzodiazepine
sedative (hypnosis)
short acting
re-occurring insomnia (rebound insomnia)
Term
clonazepam
Definition
benzodiazepine
anticonvulsant
relatively selective for anti-seizure
Term
buspirone
Definition
partial agonist at serotonin receptor 5HT1A
slow onset of action
minimal sedation
less side effects
no withdrawal after discontinuation
Term
flumazenil
Definition
benzodiazepine antagonist
used to treat overdose
can also antagonize the actions of zolpidem
can induce withdrawal symptoms in dependent patients
Term
phenobarbital
Definition
barbiturate
lasts greater than a day
used to inhibit seizures
Term
pentobarbital
Definition
barbiturate
lasts hours
Term
thiopental
Definition
bartiturate
acts in seconds and lasts 30 minutes
iv anesthetic
Term
paroxetine
Definition
antidepressant
FDA approved for treatment of GAD
serotonin selective reuptake inhibitor
Term
venlafaxine XR
Definition
antidepressant
FDA approved for the treatment of GAD
serotonin selective reuptake inhibitor
inhibits the reuptake of NE
Term
imipramine
Definition
first generation tricyclic antidepressant
used when SSRIs do not work
effects serotonin reuptake and NE reuptake
Term
hydroxyzine
Definition
antihistamine with antiemetic activity
competes with histamine for the H1 receptor
low tendancy for habituation (used with people addicted to barbs or benzo)
Term
chloral hydrate
Definition
sedative and hypnotic
can cause serious GI distress
Term
ethanol
Definition
anti anxiety and sedative
narrow, unpredictable therapeutic window
Term
zolpidem
Definition
non-benzodiazepine sedative hypnotic
used for short term treatment of insomnia (7-10 days)
binds to the same spot on GABAa as benzodiazepines (enhances GABA transmission)
no cognitive impairment, no rebound insomnia
Term
eszopiclone
Definition
nonbenzodiazepine hypnotic
used to treat insomnia (used for 6-12 months)
Term
ramelteon
Definition
melotonin 1 and 2 receptor agonist
used to treat insomnia
MT1 regulates sleepiness
MT2 shifts body from night to day
no cognitive impairment, no rebound insomnia, no drug dependence
contraindications: severe hepatic disease, COPD (has respiratory depressant effects), endocrine disease (associated with increased testosterone and prolactin)
Term
desipramine
Definition
first generation tricyclic antidepressant
active metabolite of imipramine
most potent and selective for the inhibition of the reuptake of NE
used for bulimia
Term
amitriptyline
Definition
first generation tricyclic antidepressant
used to treat depression, eating disorders, ADHD, neuropathic pain, social anxiety disorder
Term
amoxapine
Definition
second generation tricyclic antidepressant
faster onset of action than imipramine or amitriptyline
Term
maprotiline
Definition
second generation tricyclic antidepressant
NE selection (does not effect the reuptake of serotonin)
causes sedation
Term
fluoxetine
Definition
serotonin selective reuptake inhibitor
no antimuscarinic side effects
Term
escitalopram
Definition
serotonin selective reuptake inhibitor
no anti muscarinic side effects
Term
duloxetine
Definition
inhibits the reuptake of serotonin and NE
potency is greater for serotonin than NE
Term
meperidine
Definition
Term
phenelzine
Definition
MAOi (inhibit metabolism of serotonin, dopamine, and NE)
inhibits monoamine oxidase irreversibly and are non specific
Term
tranylcypromine
Definition
MAOi (inhibits the metabolism of serotonin, dopamine, and NE)
inhibits monoamine oxidse irreversibly and is non specific
Term
moclobemide
Definition
MAOi (inhibits metabolism of serotonin, dopamine, NE)
inhibits monoamine oxidase reversibly
MAOa selective
less side effects
Term
bupropion
Definition
antidepressant
used in patient who have experienced orthostatic hypotension, aide to smoking cessation
inhibits reuptake of dopamine
noncompetitive nicotinic antagonist
Term
trazodone
Definition
inhibits serotonin reuptake
enhances serotonin and NE release
Term
carbamezepine
Definition
mood stabilizing drug
anti-epileptic
sodium channel blocker
in acute attack, only effective on manic state, not depressive state
takes 3-4 weeks to develop
Term
valproate
Definition
mood stabilizing drug
anti epileptic
GABAa receptor agonist, increasing GABAa activity
in acute attack, only effective on manic state, not depressive state
takes 3-4 weeks to develop
Term
lithium
Definition
used to treat bipolar disorder and unipolar disorder
interferes with the synthesis, storage, release, and reuptake of monoamine neurotransmitters
narrow therapeutic window and long duration of action
reabsorbed through tubular reabsorption, so diuretics may cause toxicity
inhibits ADH --> polyuria
Term
disulfiram
Definition
used to treat alcoholism
adversive therapy
inhibits alcohol dehydrogenase leading to unpleasant effects
Term
mecamylamine
Definition
nicotinic acetylcholine receptor noncompetitive antagonist
small doses actually increase smoking because effect can be overcome
in higher doses, abolishes the effects of nicotine
Term
acamprosate
Definition
used to treat alcoholism
weak NMDA receptor agonist
reduces craving
may work by interfering with synaptic plasticity
Term
dronabinol
Definition
synthetic cannabinoid, derived from the cannabis plant
used for anorexia and nausea
antiemetic - opposes effects of serotonin in the medulla vomiting center of brain (5HT3)
appetite - cannabinoid receptors in the hypothalamus
Term
nabilone
Definition
synthetic cannabinoid, not derived from the cannabis plant
antiemetic and neuropathic pain
antiemetic - opposes effects of serotonin in the medulla vomiting center of brain (5HT3)
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