pharm II test II opiods

• morphine - strong
• codeine - moderate

• pentazocine - Talwin
• butorphanol
• buprenorphin - buprenex

naloxone -

• enkephalins
• beta endorphins

dynorphins

• enkephalins
• beta endorphin

• morphine
• fentanyl
• methadone
• meperidine
• buprenorphine

• pentazocine
• butorphanol

• sufentanil
• morphine
• codeine

• analgesia
• euphoria
• respiratory depression
• physical dependence

• analgesia at the spinal cord level
• sedation
• dysphoria

may contribute to anagesia

• coupled to adenylyl cyclase through Gi, decreases cAMP
• decrease Ca2+ conductance on presynaptic terminals = decrease release of neurotransmitters
• increased K+ conductance on postsynaptic neurons = hyperpolarization and inhibition

fentanyl

rapid redistribution in the tissues; liver, spleen, kidney and lung

• conjugated to
• morphine-3-glucuronide M3G - inactive but has neuroexcitatory effects
• morphine-6-glucuuronide M6G - more potent than morphine but slowly crosses the BBB

• hydrolyzed to
• 6-mono-acetylmorphine - active
• morphine

• CYP2D6
• 10% O-demethylated to morphine

• N-demethylation to
• normeperidine - can cause seizures if it accumulates especially in children

CYP3A4 intestinally - dealkylation

Reduces the affective response to pain stimulation and increases pain tolerance without altering the threshold for perception of the stimulus.

Decreased responsiveness to increases in CO2 concentration; also depresses centers involved in regulating rhythmicity.

Delays passage of GI contents due to increase in tone and sphincter spasm.

• postural hypotension
• vasodilation
• CO2 retention and increase in CSF pressure

• phenylpiperidine
• CNS effects comparable to morphine but shorter acting & less effect on smooth muscle.
• Significant anticholinergic effects
• Seizures with accumulation of metabolite, normeperidine.
• Contraindicated with MAOI

• phenylpiperidine
• approved for surgical analgesia; metabolized very rapidly by plasma esterases → very short duration of action (3-4)minutes

• phenylpiperidine
• 5-7 times more potent than fentanyl.

• phenylpiperidine
• Rapid onset and short duration; used in anesthesiology

• phenylheptylamine
• pharmacological properties qualitatively similar to morphine
• longer duration of action
• more effective orally
• withdrawal has a slower onset, more prolonged

• phenylheptylamine
• approved for use in detoxification clinics; may be given once every 2-3 days.

• phenanthrene
• lower analgesic potency 
• lower addiction liability than morphine
• very high oral efficacy
• antitussive
• Usually combined in formulations containing aspirin, acetaminophen or other drugs for analgesia*.

• phenylpiperidine
• prominent effect is constipation
• atropine added primarily to discourage abuse

• phenylpiperidine
• anti-diarrheal　
• potential for abuse is low because very little crosses BBB

• phenanthrene
• long acting Mu receptor agonist
• parenterally for sever pain
• slow dissociation causing long duration and resistance to naloxone

• phenanthrenes
• kappa agonist
• Mu antagonist
• ceiling to respiratory depression but resistant to naloxone

• morpinan
• predominantly Kappa agonist
• parenterally produces analgesia =to bupronex

• predominantly Kappa
• moderate analgesic weak antagonistic

• analog of codeine
• weak Mu agonist
• analgesic effect from block of NE 5HT reuptake (mainly 5HT)

• more potent version of tramadol
• more effect on decreasing NE reuptake

• non-narcotic
• no analgesia or addictive properties
• anti-tussive

• opioid antagonist
• duration 1-2 hrs
• highest affinity for Mu receptors
• few effects when given w/o agonist
• reversal in 1-3 min. of IV administration
• no tolerance

• opioid antagonist
• duration 48 hrs
• oral

• opioid antagonist
• IV
• duration 8-10 hrs

• peripheral antagoinist
• Tx of constipation