Drugs of Abuse Flashcards
morphine
Morphine: po, iv, im n PO: IR, SR (MS contin) n Oral: 35-70% bioavail n Half-life 2-3.5 hrs n Duration 4-6 hrs n Metabolism: hepatic glucuronidation – Excreted urine & bile
codeine
Codeine: PO only n Methyl morphine n ~90% bioavailable n Half-life: 2.5-3 hrs n Duration: 4-6 hrs n 10% De-methylated to morphine (analgesia) by CYP2D6
heroin
diacetyl morphine- acetyl groups make it go into brain faster- more sought after by users
Short acting n Prodrug→6MAM→MS n Lipid-soluble: IV: rapid penetration of BBB n 2-3x “high” of morphine n Half life: 3 min IV – 6MAM: 30 min n First-pass metabolism – PO: not bioavailable
oxycodone
Oxycodone (“Perc’s”)- synthetic
n Onset: 30m, peak 1 hr n Half-life: 3-4 hrs n Duration: 6-8 hrs n Oxycontin®: 12 hrs n High bioavailability po – 60-87% n Metabolite: oxymorphone (active, potent) n Metab: CYP 450:3A4, 2D6
hydrocodone
Hydrocodone (“vicodins”)- synthetic
n Onset: 30 m, Peak: 1 hr n Half-life: 2-3 hrs n Duration: 3-4 hrs n Pain relief: thought to be about 50% of oxycodone by miosis; ? more n Likeability similar to oxycodone n Changed DEA III to II 2014 n Metab: cyp450: 2D6, 3A4
methadone
Full mu agonist n Slow development of opioid tolerance n High bioavailability PO (>90%) n Long half-life (24 hrs) n Delayed onset of action, long duration (24 hrs) n Less “likeable” n Highly protein bound Chronic use: stored and accumulated in liver tissue n Slow release into the blood: extends duration n HD (80-120mg) yields more abstinence than LD n Metabolized CYP3A4, 2B6 n Excreted urine/feces – ↓GFR: excreted mostly GI – Not detected standard UDS
buprenorphine
n 4:1 ratio: given SL, 50-60% bioavailability of Bupe, <1% of naloxone n IV: Naloxone blunts “high”: blocks mu receptors initially n 2mg: 37-47% opioid receptors occupied n 16mg: 85-92% n 32mg: 85-97% n “blocker” is buprenorphine not naloxone n Metab.: CYP: 3A4.- high first pass effect- take SL other: partial agonist- low abuse potential, lower physical dependence, safety in overdose. slow dissociation rate- 72 hrs
abuse n Abuse of Suboxone occurs n Dissolved and snorted or inj n Popular among teens – Perceived as safe n Subutex® (bupe w/o naloxone) street value twice that of Suboxone – 25% naloxone absorbed IN – Delays “high”: less likeable
cocaine
Cocaine: crystalline (IV or IN), freebase/crack
smoked (denatured with strong alkali or NaCO3
yielding low temp [98 c] for vaporization)
n Intense euphoria, but short-lasting
– IV/smoke: Peak 4-7min, diminish by half 17-30 min
– IN: peak 30 min, weaker high, longer duration
n Metab: CYP 3A4 to benzoylecgonine, excreted in
urine (measured in urine drug screens)
n Expensive: use tends to be binge (can’t stop until
run out of money)
n Sometimes used with other drugs (speedball, eg:
heroin and cocaine)
meth
Oral, IN, IV, smoked
n
indication- obesity, ADHD
Euphoria, well-being, confidence n Sexual confidence, enhancement n Alertness, hyperactivity, ↑energy n increased heart rate, blood pressure, body temperature, tremors, and RR psychiatric- hypomania, grandiosity, insomnia, irratibility, appetite suppression, weight loss, skin picking
frank psychosis
long term use: depression with abstinence
carbohydrate craving
withdrawal: depression, irritability, suicidal ideation
marijuana
psychomotor effects- dose related
- slowed time perception, slow rxn or judgement time
psychiatric effects Transient panic and anxiety – Depersonalization – Delusions (inc paranoia), hallucinations – Acute mania, depression (possibly) – Aggression – Cognitive effects: – Impaired short term memory – Decreased verbal IQ – Decreased attention, focus – Decreased executive functioning
Withdrawal dney, Hughes: UVM 2004) n Irritability up to 28 days n Decreased appetite up to 9 days n Anxiety up to 11 days n “Physical discomfort” up to 21 days n Low mood 3-9 days n Increased aggression/anger n Insomnia n Restlessness n Sx reversed by THC
