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37 Cards in this Set

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  • Back
Which receptors do most opioid drugs bind to?
mu receptors
Name the 3 different groups of opioid receptor.
kappa, delta, and mu
Which receptors share the ost similarity in ligand binding?
mu and delta
What type of receptors are the opioid family?
They are a family of G protein coupled receptors
What is the principle active alkaloid in opium?
Morphine, which is present at a concentration of ~10%
Why are the use of delta opioid receptors limited?
Because they are peptides and are too polar to cross the blood-brain barrier, and must therefore be injected by intraspinal routes in order to have analgesic properties.
Which opioid's produce analgesia without euphoria?
opioid drugs which interact with kappa receptors
Kappa agonist
may lack the negative adverse effects of mu agonists, respiratory depression but they produce dysphoria and physchotomimetic effects.
What are the four groups in which opioid are divided into?
1. Full agonist
2. Partial agonist
3. Mixed agonist/antagonist
4. Antagonist
Morphine-like agonist
derivatives of morphine, the natural opioid derived from opium
Heroin
a synthetic, rapid-acting derivative of morphine, is not currently marketed for medical use in humans; rather, the importance of heroin lies in its abuse.
Name 3 full morphine-like agonist
morphine, hydromorphone, and oxymorphone
Name 3 partial morphine-like agonist
Codeine, hydrocodone, and oxycodone
Codeine
synthetic version of morphine that is relatively weak mu receptor agonist.
What converts codeine to morphine?
CYP2D6, most of it analgesic activity somes from this conversion. However, the antitussive activity of codeine is due mostly to codeine itself
What is the full mu receptor agonist of methadone-like agonist?
Methadone
Is Methadone long-acting or short-acting?
Long-acting synthetic mu opioid agonist
What is the partial mu receptor agonist of methadone-like agonist?
propoxyphene
What is Methadone known for?
Its potency as an analgesic and for its long duration of action. It has especially long-acting effects at relieving symptoms of opioid withdrawal when administered to patients recovering from opioid addiction (heroin addiction)
What is potent full mu opioid agonist of Meperidine-Like agonist?
Meperidine
What has meperidine fallen into disfavor for the use of?
chronic pain relief, and its use is now somewhat limited to acute pain relief
What is meperidine metabolized to?
Meperidine is metabolized to a long-lasting active metabolite, normeperidine, by the liver. This metabolite is believed to be a cause of CNS-related adverse effects of meperidine (hallucinations, tremors, and seizures).
What are the partial mu receptor agonist of Meperidine-like agonist?
Diphenoxylate and loperamide
What are diphenoxylate and loperamide useful for?
They are useful as constipating agents for patient with diarrhea.
What happens at higher doses of diphenoxylate?
It may be absorbed and penetrate the blood-barrier sufficiently to cause meperidine-like effects on the CNS
What happens at higher doses of Loperamide?
It still fails to sifficiently penetrate the blood-brain barrier at high enough concentrations to cause a meperidine-like effect. This is due to exclusion of loperamide from the CNS by P-glycoprotein (PGP), a protein which pumps drugs out of cells of the blood-brain barrier as the drug attempts to absorb into the CNS by passive diffusion.
What are the full mu receptor agonist of Fentanyl-like agonist?
Fentanyl (well-known for its high potency) and Sufentanil
TRUE/FALSE. Fentanyl and Sulfentanil are more potent then morphine.
TRUE
Describe 2 characteristics of the fentanyl-like agonist.
very lipophilic. As a result, they distribute well and fast to the CNS.
Which drug has excellent transdermal penetration and why?
Fentanyl has excellent transdermal penetration due to high lipophilicity, and it has gained popularity as a transdermal anagelsic in chronic pain management.
Nalbuphine
-opioid with strong agonist activity at kappa opioid receptors
-also mu receptor antagonist
Buphrenorphine
-partial mu opioid receptor agonist and partial kappa receptor agonist
-extremely long duration of action
Butorphanol
-an opioid with predominant kappa agonist activity
-may also function as a partial mu agonist or as an antagonist at my opioid receptors
Pentazocine
-oldest mixed agonist/antagonist opioid drug, has kappa agonist activity as well as weak agonist acitivity at mu opioid receptors.
Which 2 drugs are antagonist at mu opioid receptors?
Naltrexone and Naloxone
Which drug is the "gold standard" in terms of opioid antagonists?
Naloxone
Which opioid antagonistic drug is useful as an antidote for opioid overdose?
Naloxone