Lecture 23- Opiates+ Alc (spec. opiates) Flashcards
Exam 3
What dose opium come from?
- comes from papaver somniferum
- papver- frost tolerant annuals
- somnifer-sleep related
Where is opium cultivated?
- native to middle east/Mediterranean sea area
- also cultivated throughout Asia
Extraction of opium process
- petals fall off poppy blooms, revelaing a round, egg-sized seedpod
- seedpod is lightly scored
- white sap (opium) is collected and allowed to dry
- thick and gummy when dry
- effects can be experienced when this is orally consumed or smoked
Historical evidence
earliest opiate historical evidence
- 6000 years ago w sumerians and assyrians
Historical evidence
Egypt
- 3500 years ago
- medical uses -“therapeutic papyrus of thebes” book of herbal knowledge
Historical evidence
Greeks and Romans
- around 150 AD
- medical uses- physician Galen health panacea (remedy)
Historical evidence
Islamic cultures
- widespread
- Koran did not exculde opiate use (only excludes use of intoxicant substances)
Historical evidence
China
- high addiction rates (smoked)
- Opium Wars between China and Britain
Historical evidence
Western use beginning
- Western use began in the 19th century
- medicinal uses- Laudanum, Paregoric patent meds
- orally consumed
Historical evidence
F.W Serturner
- identified morphine as major active compound (10x more potent than crude opium)
- started to become more widespread in the 1800s w/ the hypodermic syringe and Civil War (soldier’s disease)
Historical evidence
Alder Wright
- Diacetylmorphine (heroin)
- 2x more potent than morphine
- used as a cough suppressant in addition to a pain killer
US regulation of opiates
Harrison Narcotic Act (1914)
- marked beginning of drug crime in America
- escalation of prices
- change in user/addict
- placed in hands of physicians’ decision
US regulation of opiates
1915
- prescriptions ok if shown that doses decreased over time
US regulation of opiates
1917
- not prescribed to addicts
US regulation of opiates
1924
Heroin never prescribed
Major producers of heroin
- mexico
- colombia
- golden cresent: afghanistan, pakistan
- golden triangle: myanmar, thailand, laos, vietnam
today- prescription opiates
from the poppy
opium and morphine
Today- prescription opiates
modifications
- codeine
- dilaudid (semi-synthetic)
- oxycodone/oxycontin (semi-synthetic)
huge rise in preseription rates for these drugs
today-prescription opiates
modifications (med mixes)
- percodan (aspirin and oxycodone)
- percocet (acetaminophen and oxycodone)
- vicodin (acetaminophen and hydrocodone)
huge rise in preseription rates for these drugs
synthetic opiates
overdose deaths
raes of over-dose deaths higher than heroin and cocain for synthetic opiates
synthetic opiates
oxycontin
- same active ingredient (oxycodone) found in percodan, but higher concentration
- meant to be used for extended release (around 12 hours)
- instead users crush then snort/inject, getting veryyyyy high doses
synthetic opiates
fentanyl (Actiq, Duragesic, and Sublimaze)
- more likely to be sedative than euphoric
- due to higher potency (reduced therapeutic window)
ADMET
route of admin
- orally- absorbed from the gastrointestinal tract
- injected- intravenous (much quicker absp) or intramusclue/subcutaneous (slower absp)
- smoked (inhaled)-abs through the nasal mucosa and lungs
how is heroin most commonly administered
smoked or injected iv. “mainlining”
ADMET
Distribution
- throughout body
- for some opiods, only a small amount crosses BBB (ex. morphine)
- heroin is more lipid solube, converted to morphine inside brain (prodrug)
What is a prodrug
- drug that turns into active form once in the body
- ex. heroin (gets converted to morphine)
ADMET
Metabolism
- metabolized by liver in around 2 hours
- small amounts metabolized into normorphine
- codeine metabolized to morphine
ADMET
influential factors on metabolism
sex, age, diet, genetics, disease state, use of other medications
ADMET
Eliminated by…
kidneys/urine
opiod neurotransmitters
Naloxone
- slight chemical difference with morphine, synthesized in 1960s
- blocked effects of morphine/heroin, reversed overdoses of morphine/heroin
- antagonist of opiates
- narcan
opioid neurotransmitters
Endorphins
- discovery of endorphines “endogenous morphine” and their receptors in 1970s
- candace pert and solomon snyder of johns hopkins
- NTs mimicked by opiates: beta-endorphin, enkephalin, and dynorphin
