Chapter 11: Opioids Flashcards
What’s the plant that opiates are derived from?
Papaver somniferum
In the 1500’s in western Europe opiates were considered what?
a panacea, cure all
Used in apothecaries as?(2)
laudanum : opium + alcohol+ flavourings
paten medicines
What are the alkaloids in opium?
- morphine, codeine, papaverine (naturally occurring)
Use of opiates in the USA increase because of what?
- analgesic - civil war
- hypodermic needle
- patent medicine industry
By when was the habit forming properties discovered in the USA?
- 1870
Heroin was discovered when? marketed as what?
- 1874, non addictive drug by Bayer
Social attitudes towards opiates in the 1900s?3
- punishable loss of self control
- unearned pleasure
- repressive legislation = best way to address issue. (control laws over them)
Pure food and drug act of 1906?
- importation of dangerous substances= illegal
- labels!
- compounds had to meet standards of identity and purity
Harrison Narcotics Tax Act (1914)
- control non medical use of drugs and to monitor their legitimate medical use
- black market in narcotics occurred
- heroin was not covered by this act..remained legal until 1924
Anslinger Era (1930-1962)?
- drug abuse = immoral, requiring harsh penalties
- exaggerated drug dangers
Opiate refers to what?
- naturally occurring substances like morphine and codeine
Opioid refers to what?
- synthetic and semi-synthetic compounds….now more general seems to refer to alls rugs in this class
Narcotic?
- drug that causes sleep
Narcotic Analgesic?
- pain reduction
Narcotic has become to mean what?
- addictive…and includes non-narcotic drugs
Sap from the speed pod of Papaver somniferum contains what?
- morphine (10%)
- Codeine (.5%)
- Thebaine (0.1%)
Heroin?
- semisynthetic made by modifying morphine…ten times more lipid soluble than morphine
Canadian use for medical purposes is _____ restrictive than in the USA. example?
- less
- ex: codeine is available legally over the counter in canada
Thebaine is the source of what synthetic compounds?
Oxycodone ( Percoet, Percodan, Oxycontin trade names) , Etorphine (main ones)
- buprenorphine, nalorphine and naloxone.
OxyContin????
- high concentration ocycodone tablet in slow release form.
- crushed, dissolved, and injected the effect is powerful and highly addictive.
Synthetic opioids? Characteristics?(2)
- bear little chemical resemblance to morphine but occupy the same receptors
- some are more and some are less effective than morphine.
Synthetic opioids :
Mepridine (Demerol)
-short acting
Synthetic Opioids?
Methadone (Dolophine)
- long acting, more effective given orally
Synthetic Opioids?
Buprenorphine?
has been used in the treatment of opiate addiction - long lasting prevention of withdrawal
Synthetic opioids?
Fentanyl ( Sublimaze)
- designer drugs are based on this molecule
- MPTP : metabolized into neurotoxin that destroys the substantial nigra
Heroin ????
- invented in 1898 at Bayer co (creators of aspirin)….non addictive analgesic…haha
- causes less nausea and vomiting than morphine and is a more effective analgesic ( 10x)
- diacetylmorphine… added an acetyl group to morphine..
Administration?
Morphine
L> base…Kpa 8..most of its molecules are ionized in stomach acid, not lipid soluble
- not rapidly absorbed orally
- significant first pass metabolism in the stomach and liver
- recreational purposes: non oral routes are used
Administration?
Heroin
- can be snorted unlike morphine
- can be vaporized and the vapour inhaled..chasing the dragon
- iv injection ( still used but less common)
Distribution? (2)
heroin
codeine
- heroin (highly lipid soluble) molecule is inactive in the brain but is rapidly converted into it’s metabolites, mainly morphine but also monoacetylmorphine
- codeine, too metabolizes into morphine
After absorption occurs most opioids are highly concentrated where?
Why do opioids pass through readily via placental but not brain barrier.
- lungs, spleen, liver and proteins in the blood
- poor lipid solubility except heroin