Opiods Flashcards
morphine, codeine, thebaine
Opiates
compounds structurally related to products found in opium
Opiates
substances that are endogenous/synthetic that produce morphine-like effects that are blocked by antagonists such as naloxone
Opioids
derived from beta lipoprotein
endorphins
o newly discovered
o localized in areas in the CNS associated with pain
endormorphines
first discovered opioid peptides
enkephalins
site at which all the currently available pure agonists act to produce analgesia
A. MU RECEPTORS
B. KAPPA RECEPTORS
C. DELTA RECEPTORS
MU RECEPTORS
responsible for most of the analgesic effects of opioids & for some major unwanted effects
A. MU RECEPTORS
B. KAPPA RECEPTORS
C. DELTA RECEPTORS
MU RECEPTORS
o dysphoria
o hallucinations
A. MU RECEPTORS
B. KAPPA RECEPTORS
C. DELTA RECEPTORS
B
can be preconvulsant
A. MU RECEPTORS
B. KAPPA RECEPTORS
C. DELTA RECEPTORS
C
opioid antagonist
naloxone
related to pain or is painful stimuli
nociceptive stimuli
has direct effect on the heart because of its antimuscarinic action → tachycardia
MEPERIDINE
equal in potency to morphine but less euphoria & longer
duration of action
METHADONE
→ 100-fold analgesic potency of morphine
FENTANYL
→ highly lipophilic
→ metabolized by cytochrome P-450
FENTANYL
True or false
FENTANYL is use for anesthetic and management of severe pain
True
→ more lipid soluble than morphine
→ 3x more potent than morphine
→ more euphoria
HEROIN (DIACETYLMORPHINE)
sometimes formulated with Aspirin or Acetaminophen
OXYCODONE
→ used in management of severe pain
→ metabolized and excreted through the kidneys
OXYCODONE
often used in combination with Aspirin or Acetaminophen
CODEINE
→ less potent analgesic and less euphoria than morphine
→ lower potential for abuse than morphine
→ greater oral efficacy because of lower first pass metabolism in the liver
CODEINE
often used in combination with Aspirin & Acetaminophen for analgesia
PROPOXYPHENE
k receptor agonist
PENTAZOCINE
a partial agonist acting at mu receptor
BUPRENORPHINE
25-50x more potent than morphine
BUPRENORPHINE
major use:
o opiate detoxification
BUPRENORPHINE
→ treatment of chronic pain
→ exhibit a ceiling effect
NALBUPHINE & BUTORPHANOL
effective in labor pains & causes less neonatal depression
TRAMADOL
competitive antagonist with a 10-fold affinity for mu receptors than kappa receptors
NALOXONE
“renarcotization”
NALOXONE
→ in combination with buprenorphine → used for rapid opioid detoxification
→ beneficial in the treatment of chronic alcoholism
NALTREXONE
