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Pharm Exam 3
opioids, peripheral analgesic, abuse
97
Pharmacology
Graduate
11/13/2010

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Term
diacetyl morphine
Definition
heroin
Term
drug more potent than heroin
Definition
hydromorphone
fentanyl
Term
drug in darvon
Definition
propoxyphene
(also contains caffeine, aspirin)
Term
has highest affinity for opioid receptor
Definition
naloxone
Term
Mu 1 operates at
Mu 2 operates at
Definition
1- supraspinal analgesia
2- spinal analgesia
Term
delta-
kappa-
Definition
delta- supraspinal
kappa- spinal
Term
natural pain relief mechanism of body, during stress
Definition
endorphins
Term
what drug can be added to opiod regiment to increase effects
Definition
calcium channel blockers
Term
opiod mechanism of action in supraspinal pathway...
Definition
stimulates inhibitory descending pathway
Term
opioid mechanism in spinal pathway
Definition
1) decrease adenylate cyclase, cAMP
2) increase K+ EFFLUX
3) hyperpolarization
4) decrease Ca INFLUX
5) decrease substance p release
Term
opioids produce hypo/hyper tension and how?
Definition
HYPOTENSION
directly: depresses CNS
indirect: histamine release=peripheral vasodilation
Term
opioids may produce miosis/mydriasis?
Definition
miosis, pupillary CONSTRICTION
-can be problematic in dark lighting
Term
opioids increase/decrease smooth muscle tone
Definition
INCREASE TONE
primarily in non-vascular smooth muscle
which makes you shit bricks
Term
potential problem of codeine for cough
Definition
suppresses a normal reflex, i.e. ejecting mucous
-best used to suppress NON-PRODUCTIVE COUGH
Term
opioid contraindications
Definition
convulsions
increased intracranial pressure (trauma)
undiagnosed acute abdominal conditions
Term
withdraw reactions are opposite/same as drug's effect
Definition
opposite to the drug
Term
oxycontin
Definition
an extended release formulation of oxycodone
Term
Embeda
Definition
extended release drug
morphine with naltrexone
-added so drug can't be abused
Term
why isn't meperidine used much
Definition
weaker
in the sub-group of fentanyl
can produce a toxic renal metabolite with chronic use
Term
buprenorphine
Definition
partial agonist
used in drug treatment programs, will let pt. function
Term
methadone
Definition
--ve has short pain relief, but long resp. dep times
Term
tramadol
Definition

hits BOTH mu receptors blocks reuptake of 5HT

only PARTIALLY reversed by naloxone

Term
agonist-antagonists act where...
Definition
agonist at kappa
antagonist at mu 1 +2
Term
Talwin NX
Definition
pentazocine with naloxone, to prevent abuse
Term
pentazocine
Definition
originally marketed as non-addictive..but it is
can produce nightmares, hallucinations
Term
narcan challenge
Definition
giving them a antagonist will determine if they have it in their system (naloxone=narcan)
Term
naltrexone
Definition
longer acting narcan
(antagonist...)
treats narcotic AND ETOH addictions
Term
naltrexone mechanism on ETOH addiction
Definition
1) decreases the increased cerebral blood flow to frontal/thalamic/limbic systems
2) pharmacoDYNAMIC- reduces euphoric effects of ETOH
3) enhances it's positive effects, so less needed
Term
caffeine effects
Definition
cerebral vasoCONSTRICTOR
enhances weak acid absorption (..combined with aspirin)
blocks inflammatory mediators
Term
NSAIDS with slight COX-2 blocking effect
Definition
Diclofenac
Etodolac (Lodine)
Ketorolac
--> easier on GI as a result
Term
Rx ibuprofen dosages
Definition
400 600 800 mg
Term
vicodin
Definition
500 mg acetaminophen
5 mg Hydrocodone
Term
percodan
Definition
325 mg aspirin
5 mg oxycodone
Term
percocet
Definition
325 acetaminophen
5 mg oxycodone
Term
schedule of percocet, percodan, vicodin
Definition
perc's are schedule II
vicodin is schedule III
Term
aspirin's effect on cox enzymes
Definition
irreversible binding of cox 1 + 2
(cox 1 at lOW doses...i.e. baby aspirin daily)
Term
-gold standard NSAID
-dosage amount
Definition
ibuprofen (Advil, Motrin)
OTC max dose is 200mg
Term
naproxen compared to ibuprofen
Definition
longer half-life
more cox-1 selective (so rougher on stomach)
Term
meclofenamate compared to ibuprofen
Definition
4x as powerful (50mg meclo=200mg Ibu)
produces stomach cramps, diahrrea after several days
Term
diflumasil
Definition
nsaid
Dolorbid
-slow onset, requires a loading dose
Term
diclofenac, etodolac (Lodine)
Definition
slightly cox 2 favoring
so don't inhibit platlet agg as much
Term
NSAID associated with liver toxicity
Definition
diclofenac
Term
only NSAID approved as an IV, IM
Definition
ketorolac
-very effective pain reduction
-i.e. kidney stones
BUT highly cox-1 selective (BLEEDING!!)
Term
reason for cox-2 development
Definition
blocking cox-2 only avoids GI issues
-less bleeding + ulcers
Term
what led to removal of coxibs
Definition
rofexcoxib and valdecoxib removed
due to increased CV problems
also stephen johnsons
Term
which pain drugs do not interact with Lithium
Definition
aspirin
acetaminophen
narcotics
Term
why codeine, hydrocodone, oxycodone effective orally?
Definition
their metabolites are active
so as first pass kicks in, they can still be effective
Term
sign of aspirin overdose
Definition
fever goes UP
(even though its antipyretic at therapeutic dose)
Term
compared to aspirin, NSAIDS have _____ platlet binding
Definition
NSAIDS reversible antiplatlet action
Term
which drug has no affect on platelets
Definition
acetaminophen
Term
opioid side effects
Definition
dizziness
drowsiness
psychomotor impairment
constipation
Term
alkalizing urine is antidote for ____ overdose
Definition
aspirin
NSAIDS
cox-2 inhibitors
Term
acetaminophen overdose treatment
Definition
n-acetyl cysteine
(Mucomist)
Term
oral version of naloxone
Definition
naltrexone
-has higher half-life...which is good because some opioids have longer half-lives than naloxone
Term
drug(s) which reduce HTN drug effects
Definition
NSAIDS
COX-2
aspirin (at high dose)
Term
which drugs increase methotrexate (cancer drug) levels
Definition
aspirin, nsaids, cox-2
all INCREASE levels of this anti-cancer drug
(*not when taking low amounts for RA)
Term
SSRI's and platelets..
Definition
SSRI's oppose aggregation, lead to bleeding
-possible issues when taking ASPIRIN, NSAID, COX-2
Term
SSRI's block activation of ____
Definition
codeine, tramadol
(upregulate enzyme)
Term
hepatotoxicity associated with
Definition
NSAID
-drugs have warning for alcoholics..
Term
don't work on anyone with an INR above..
Definition
3
Term
Reye's syndrome
Definition
occurs after viral infection
fatty degeneration of nervous tissue, organs
linked to receiving aspirin with viral infection
Term
5% of asthmatics are sensitive to ____
Definition
aspirin
but also can't take nsaid, cox-2
Term
5% of acetaminophen goes to ____ via ____
Definition
NAPQI via CYP-2E1
*but is then inactivated by Glutathione in healthy individual
Term
where does the efficacy come from in a combination analgesic
Definition
it comes from the NSAID
(side effects come from opioid component)
Term
advil liquigel effect on pharmacodynamic and kinetics
Definition
higher Cmax (higher peak blood level_
lower Tmax (quicker onset)
Term
a benefit of naproxen sodium
Definition
increased staying power
(--ve not as good on GI)
Term
study of arthritis and autoimmune diseases
Definition
rheumatology
Term
what does RA affect?
Definition
synovial membranes of diarthrodial joints
Term
most significant factor in dependence
Definition
low self-esteem
Term
cocaine pham effects
Definition
increased dopamine
tachycardia
hypertension
hyperthermia
Term
a primary screen is qualitative/quantitative
Definition
qualitative--tells WHAT is in system
Term
cocaine has a low/high T 1/2 and is biotransformed by ______
Definition
LOW (only 30-60 min drug duration
plasma cholinesterase
Term
active metabolite of cocaine when consuming alcohol
Definition
cocaethylene
Term
cocaine MOA
Definition
blocks DA + NE reuptake
Term
developing tolerance very quickly
Definition
tachyphylaxis
Term
drugs used to combat cocaine addiction
Definition
bromocryptine (DA agonist, parkinson drug)
antidepps
Term
belladonna alkaloids include which 2 drugs, and have what pharmacological activity
Definition
atropine, scopolamine
anticholinergics
Term
active metabolite in shrooms
Definition
psilocin
(metabolized from psilocybin)
Term
tryptaminergic drugs are similar to which endogenous substance
-and include which abused drug
Definition
similar to serotonin
LSD is a tryptaminergic
Term
T/F LSD produces hallucinations, illusions, synethesia
Definition
NOT hallucinations (unless person psychotic)
but does produce illusions and synethesia (hearing a color...)
Term
which drugs produce visual pseudohallucinations?
which drugs also produce audio pesudohallucinations?
Definition
LSD, mescaline, psyocybin, amphetamines

belladonna alkaloids have visual AND audio pseudohallucinations
Term
a very common side effects of belladonna alkaloids
Definition
amnesia
Term
writing a schedule II prescription requires...
Definition
DEA registration
state medical license
Term
protocol for emergency schedule II prescription
Definition
limited to amount required
original Rx within 7 days
Term
requirements for office use substances..
Definition
detailed inventory
site-specific DEA registration
detailed dispensing records
Term
an opioid addict can develop tolerance to many effects except for...
Definition
pupillary constriction
constipation
Term
an early sign of an NSAID overdose
Definition
tinnitus
Term
which type of diabetes is ketosis prone
Definition
type 1
-breakdown in mm./fat to produce ketone bodies as energy
-leads to kidney problems
Term
type of diabetes that involves an imbalanced supply and demand
Definition
type II
-body can't produce enough insulin for the high CHO
Term
diabetes complications
Definition
CV
kidney failure
neuropathy
blindness (optic nerve damage)
infections --> amputation
Term
oral presentation of an uncontrolled diabetic
Definition
dry mouth
exaggerated response to irritants (think dentures)
Term
insulin action on
-fat
-ptein
-CHO
Definition
fat: increased synth, decreases lipolysis
ptein: decrease breakdown, increase synth and AA uptake
CHO: increased CHO mvmt, less gluconeogenesis, increased glycogen synth
Term
T/F insulin has 3 chains, and has a pro form
Definition
insulin has 2 chains (A + B)
it does have a pro form: proinsulin
Term
pathway of insulin release...starting with glucose entry
Definition
glucose entry
ATP produced
K channel closes
cell depolarizes (++++)
Ca ENTERS (more ++++)
Insulin released
Term
opioid partial agonists
Definition
buprenorphine
Term
agonist-antagonists
Definition
pentazocine
nalbuphine
dezocine
Term
morphine's active metabolite
Definition
M-6-G morphine-6-glucuronide
-high affinity for mu receptor
-high buildup in chronic user (so they can take less drug)
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