Pharmacology of by
Type of Opioids
Brent Scobie, PhD
Codeine
 Mild analgesic potential
 3 hour half-life
 Can suppress the cough reflex
 1/5th the potency of morphine
 Usually administered orally
 Commonly mixed with OTC aspirin or acetaminophen
 (ex. Tylenol 3)
Fentanyl
 A synthetic opioid introduced in 1968
 Popular during and immediately after surgery
 A typical intravenous dose is one microgram
 Suppresses respiration longer than it induces analgesia
 8-10 hour half-life
 100 times more potent than morphine
Heroin
 Heroin is just two morphine molecules
joined together by an oxygen molecule
 Twice as potent as morphine
 .7-1.5 hour half-life
 Not used medically in the US but is used in
other countries to treat severe pain
 Pharmacology of heroin
 Is metabolized into morphine
 Crosses blood-brain barrier 100 times more rapidly than morphine
Hydrocodone/
Hydromorphone
 Semisynthetic narcotic derived from codeine
 Used to control coughs and mild to moderate levels
of pain relief
 Half-life of 3.8 hours
 Orally administered doses of hydromorphone are
thought to be 5-7 times as potent as morphine
 Side effects include dizziness, sedation, mental
confusion, anxiety, fear, nausea and or vomiting,
dysphoria and respiratory depression
Methadone
 Synthetic opioid developed in the 1930’s
 Used as a substitute for morphine during WWII
 Used in Methadone Maintenance Programs
 Half-life of 24 hours
 About as potent as Morphine
 Tolerance to euphoria develops quickly
 Can induce cardiac arrhythmias both when used at
therapeutic doses and when it is abused
 When used as prescribed has a very good safety profile
Morphine
 First isolated more than 150 years ago
 Usually administered by intramuscular or intravenous injections
 Half-life 2-3 hours
 Analgesic affects last approximately 4 hours
OxyContin
 Introduced in 1995
 A time released form of oxycodone, a synthetic opioid
 Half-life 2-3 hours
 A relatively stable blood level of OxyContin could be
reached after 2-3 doses, providing better pain control
than could be achieved using short-acting narcotic
analgesics
 OxyContin has become a major drug of abuse
Tramadol
 A distant cousin to codeine
 Used to treat mild to moderate levels of pain
 Half-life 6 hours
 Thought to be about as potent as morphine
 May be more toxic than originally thought

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SA 202 Week 3 lecture 3 opioids

  • 1. Pharmacology of by Type of Opioids Brent Scobie, PhD
  • 2. Codeine  Mild analgesic potential  3 hour half-life  Can suppress the cough reflex  1/5th the potency of morphine  Usually administered orally  Commonly mixed with OTC aspirin or acetaminophen  (ex. Tylenol 3)
  • 3. Fentanyl  A synthetic opioid introduced in 1968  Popular during and immediately after surgery  A typical intravenous dose is one microgram  Suppresses respiration longer than it induces analgesia  8-10 hour half-life  100 times more potent than morphine
  • 4. Heroin  Heroin is just two morphine molecules joined together by an oxygen molecule  Twice as potent as morphine  .7-1.5 hour half-life  Not used medically in the US but is used in other countries to treat severe pain  Pharmacology of heroin  Is metabolized into morphine  Crosses blood-brain barrier 100 times more rapidly than morphine
  • 5. Hydrocodone/ Hydromorphone  Semisynthetic narcotic derived from codeine  Used to control coughs and mild to moderate levels of pain relief  Half-life of 3.8 hours  Orally administered doses of hydromorphone are thought to be 5-7 times as potent as morphine  Side effects include dizziness, sedation, mental confusion, anxiety, fear, nausea and or vomiting, dysphoria and respiratory depression
  • 6. Methadone  Synthetic opioid developed in the 1930’s  Used as a substitute for morphine during WWII  Used in Methadone Maintenance Programs  Half-life of 24 hours  About as potent as Morphine  Tolerance to euphoria develops quickly  Can induce cardiac arrhythmias both when used at therapeutic doses and when it is abused  When used as prescribed has a very good safety profile
  • 7. Morphine  First isolated more than 150 years ago  Usually administered by intramuscular or intravenous injections  Half-life 2-3 hours  Analgesic affects last approximately 4 hours
  • 8. OxyContin  Introduced in 1995  A time released form of oxycodone, a synthetic opioid  Half-life 2-3 hours  A relatively stable blood level of OxyContin could be reached after 2-3 doses, providing better pain control than could be achieved using short-acting narcotic analgesics  OxyContin has become a major drug of abuse
  • 9. Tramadol  A distant cousin to codeine  Used to treat mild to moderate levels of pain  Half-life 6 hours  Thought to be about as potent as morphine  May be more toxic than originally thought