Lecture 23- Opiates+ Alc (spec. opiates) Flashcards

Exam 3

1
Q

What dose opium come from?

A
  • comes from papaver somniferum
  • papver- frost tolerant annuals
  • somnifer-sleep related
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2
Q

Where is opium cultivated?

A
  • native to middle east/Mediterranean sea area
  • also cultivated throughout Asia
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3
Q

Extraction of opium process

A
  • 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
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4
Q

Historical evidence

earliest opiate historical evidence

A
  • 6000 years ago w sumerians and assyrians
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5
Q

Historical evidence

Egypt

A
  • 3500 years ago
  • medical uses -“therapeutic papyrus of thebes” book of herbal knowledge
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6
Q

Historical evidence

Greeks and Romans

A
  • around 150 AD
  • medical uses- physician Galen health panacea (remedy)
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7
Q

Historical evidence

Islamic cultures

A
  • widespread
  • Koran did not exculde opiate use (only excludes use of intoxicant substances)
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8
Q

Historical evidence

China

A
  • high addiction rates (smoked)
  • Opium Wars between China and Britain
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9
Q

Historical evidence

Western use beginning

A
  • Western use began in the 19th century
  • medicinal uses- Laudanum, Paregoric patent meds
  • orally consumed
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10
Q

Historical evidence

F.W Serturner

A
  • 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)
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11
Q

Historical evidence

Alder Wright

A
  • Diacetylmorphine (heroin)
  • 2x more potent than morphine
  • used as a cough suppressant in addition to a pain killer
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12
Q

US regulation of opiates

Harrison Narcotic Act (1914)

A
  • marked beginning of drug crime in America
  • escalation of prices
  • change in user/addict
  • placed in hands of physicians’ decision
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13
Q

US regulation of opiates

1915

A
  • prescriptions ok if shown that doses decreased over time
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14
Q

US regulation of opiates

1917

A
  • not prescribed to addicts
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15
Q

US regulation of opiates

1924

A

Heroin never prescribed

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16
Q

Major producers of heroin

A
  • mexico
  • colombia
  • golden cresent: afghanistan, pakistan
  • golden triangle: myanmar, thailand, laos, vietnam
17
Q

today- prescription opiates

from the poppy

A

opium and morphine

18
Q

Today- prescription opiates

modifications

A
  • codeine
  • dilaudid (semi-synthetic)
  • oxycodone/oxycontin (semi-synthetic)

huge rise in preseription rates for these drugs

19
Q

today-prescription opiates

modifications (med mixes)

A
  • percodan (aspirin and oxycodone)
  • percocet (acetaminophen and oxycodone)
  • vicodin (acetaminophen and hydrocodone)

huge rise in preseription rates for these drugs

20
Q

synthetic opiates

overdose deaths

A

raes of over-dose deaths higher than heroin and cocain for synthetic opiates

21
Q

synthetic opiates

oxycontin

A
  • 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
22
Q

synthetic opiates

fentanyl (Actiq, Duragesic, and Sublimaze)

A
  • more likely to be sedative than euphoric
  • due to higher potency (reduced therapeutic window)
23
Q

ADMET

route of admin

A
  • 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
24
Q

how is heroin most commonly administered

A

smoked or injected iv. “mainlining”

25
Q

ADMET

Distribution

A
  • throughout body
  • for some opiods, only a small amount crosses BBB (ex. morphine)
  • heroin is more lipid solube, converted to morphine inside brain (prodrug)
26
Q

What is a prodrug

A
  • drug that turns into active form once in the body
  • ex. heroin (gets converted to morphine)
27
Q

ADMET

Metabolism

A
  • metabolized by liver in around 2 hours
  • small amounts metabolized into normorphine
  • codeine metabolized to morphine
28
Q

ADMET

influential factors on metabolism

A

sex, age, diet, genetics, disease state, use of other medications

29
Q

ADMET

Eliminated by…

A

kidneys/urine

30
Q

opiod neurotransmitters

Naloxone

A
  • slight chemical difference with morphine, synthesized in 1960s
  • blocked effects of morphine/heroin, reversed overdoses of morphine/heroin
  • antagonist of opiates
  • narcan
31
Q

opioid neurotransmitters

Endorphins

A
  • 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