PT6 JAM - exam 1 (opioid pharmacology study guide)

buprenorphine

opioid that is partial agonist of u-receptor

naloxone, naltrexone

opioid antagonist that act as reversal agents

u-receptor

most opioids are selective for _____

Tyr-Gly-Gly-Phe-(Met/Leu)

all endogenous opioid peptides contain the ____ sequence

semi-synthetic

natural, semi-synthetic, or synthetic. . .

oxycodone

hydrocodone

hydromorphone

oxymorphone

heroin

synthetic

natural, semi-synthetic, or synthetic. . .

methadone

fentanyl

tramadol

buprenorphine

opium

plant-based component of poppy plant

hypnosis

opioids are NOT part of the selective ____ class, but opioids can cause drowsiness

respiratory depression

primary cause of death from opioid toxicity

medulla

part of brain suppressed during opioid use that leads to respiratory depression

pruritus

_____ is more common with IV injections due to non-allergic histamine release from mast cells

nucleus accumbens

brain center known as "reward center," where dopamine is released

chemoreceptor trigger zone

nausea + emesis (u-mediated) occurs when opiates irritate ____ in area postrema in medulla

skeletal muscle rigidity

_____ (u-mediated) can occur with large IV doses due to striatal dopamine synthesis

(most commonly observed with fentanyl)

miosis, constipation, pruritus

patients can develop tolerance to opioid pharmacological actions EXCEPT ____ (3)

glutamate

opioid agonists inhibit _____ release by binding to opioid receptors (u, K, delta), which reduces Ca influx + hyperpolarizes nerve terminals

efflux

opioid agonists open G-protein coupled receptors, causing potassium (K) ______, leading to hyperpolarization

submaximal

full agonist bind + trigger full, maximal response, while partial agonist produce _____ response even at full occupancy

mydriasis

opioid withdrawal and antagonism administration causes ______ of eyes

miosis

opioid use can cause ____ of eyes

sphincter of Oddi

reduced bile flow due to constriction of ______, which is a muscular valve controlling digestive fluid flow from liver + pancreas into small intestine

acetylcholine

slowed intestinal motility occurs when opiates activate u-receptors in enteric nervous system, which decreases _______ release at neuromuscular junction, leading to constitpation

labor

opioids given during ____ may cause respiratory depression in babies

CYP2D6

mothers given codeine with extensive __________ metabolizer status may produce too much morphine + pass to nursing child via breast milk

innate tolerance

type of tolerance characterized by an insensitivity to opioids before exposure

acquired tolerance

type of tolerance characterized by reduction in effect with repeated / prolonged use

physical dependence

_____ occurs when body relies on substance to function normally, resulting in withdrawal symptoms if stopped

phosphorylated

u-receptors _____ by GRKs leads to desensitization via attracting protein beta-arrestin

CYP3A4

fentanyl + oxycodone have dependence on ____ for metabolism

increase

if CYP3A4 metabolism is inhibited, oxycodone or fentanyl concentrations will ___, leading to intensified opioid effects

methadone

opioid that causes QT prolongation

sublingual

buprenorphine + naloxone are combined in ___ form to deter misuse

when administered this way, naloxone does not produce strong opioid antagonism

injected

if _____, naloxone portion of buprenorphine + naloxone inhibits opioid agonistic effects

serotonin syndrome

potential risk of opioids if given with MAOIs, SSRIs, SNRIs, tricyclics, triptan-type drugs

tramadol

pronounced risk of serotonin syndrome compared to other opioids when given with serotonergic drugs

first pass metabolism

when heroin given PO, heroin is converted to morphine with __________ leading to little morphine in brain (due to BBB)

deacetylated

when heroin given IV, heroin rapidly enters brain due to higher lipophilicity, then is _______ into morphine, leading to lots of morphine in brain

zero order

transdermal fentanyl patches are released at near constant rate, which is ______ absorption

72

fentanyl patches, since zero order, releases constant drug over about _____ hours

residual drug

if person removes patch before depleted, ______ in dermis continues to be absorbed with 50% drop in 24h

bioavailability

if fentanyl lozenge is swallowed instead of used appropriately buccally, _____ significantly reduces due to first pass metabolism

buccal

____ route of fentanyl has 25% absorption due to bypass of first pass metabolism

remaining 75% absorbed in GI tract (25% = escapes first pass, 50% destroyed)