Ley: Opioids Flashcards
Diacetylmorphine- derived from morphine alkaloid, 2-3 more potent. Scheduled as a class I drug in 1970. Purity ranges from 40-60%. Often cut with sugar, lactose, mannitol, quinine, strychnine.
heroin
Number one drug in the US
vicodin
At least 5% of American high school students have tried (blank). ~8% have tried (blank)
oxycodone; vicodin
Among those who try heroin, how many become addicted? How many overdose?
25%
75% OD
What are the 3 opioid receptors? Which receptors have abuse potential?
mu, kappa, delta; opioids w abuse potential are selective for mu
When are you more likely to get sick from opioids?
if they are used for pain when pain isn’t present
Risk of (blank) depression increases w increasing dose of opioids
respiratory
What are the effects of opioids?
cardiovascular - suppression of reflex vasoconstriction
depressed cough reflex, constrict pupils
direct effect on respiratory center
may trigger emesis, decrease gastric motility, constipation
reduce testosterone and cortisol
(blank) is a full opiate receptor agonist; it readily crosses the BBB; onset 30 minutes after snorting, 15 after subq injection, instant with IV.
heroin
100x more potent than morphine (can inject, use patch, smoke it, eat it, etc).
fentanyl
spasm of sphincter of Oddi, risk of seizures
demerol
10% methylated to morphine. Low affinity for opioid receptors.
codeine
“the dragon” Escalating doses Long-acting, variable half-life Cytochrome p450 (cyp 3a4) Multiple side effects- teeth, no libido, weight gain, insomnia, irregular menstruation Diversion/overdose
methadone
similar to hydrocodone, but not a prodrug. Made in 1917. 2d6 activity. High bioavailability (but snorted, shot, smoked, PR)
oxycodone
3 stages of dependence?
initiation - reinforced via mu receptors
continuation - multiple neurotransmitters involved
detox/withdrawal - glutamate and NE involved in detox symptoms
What do opioid receptors cause on a molecular level?
G proteins which make adenyl cyclase more sensitized
effects on trx factors
alters transmembrane signaling
Treatment for heroin addicted pts?
treatment centers
injection rooms
What to use for opioid overdose? Also used in treatment…
suboxone/naloxene - can reverse coma
What percentage of opiate abusers relapse during treatment? When do withdrawal symtpoms peak?
80%; after 2-3 days
Can last up to 6-7 months after withdrawal
Vague sense of feeling abnormal
Depression (increased propensity to sleep)
Abnormal response to stress
Abnormal respiration and temperature
Decreased self-esteem
Anxiety
Craving
Confounded by high comorbidity with other psychiatric disorders
protracted abstinence syndrome
This can be used during opiate withdrawal; may have effects on reward systems
clonidine
Are abstinence programs effective for getting off of opiates?
no :(
Opioids commonly used to treat (blank)
chronic pain
