Opioid Agonists And Antagonists

Front 1

Which receptors do most opioid drugs bind to?

Back 1

mu receptors

Front 2

Name the 3 different groups of opioid receptor.

Back 2

kappa, delta, and mu

Front 3

Which receptors share the ost similarity in ligand binding?

Back 3

mu and delta

Front 4

What type of receptors are the opioid family?

Back 4

They are a family of G protein coupled receptors

Front 5

What is the principle active alkaloid in opium?

Back 5

Morphine, which is present at a concentration of ~10%

Front 6

Why are the use of delta opioid receptors limited?

Back 6

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.

Front 7

Which opioid's produce analgesia without euphoria?

Back 7

opioid drugs which interact with kappa receptors

Front 8

Kappa agonist

Back 8

may lack the negative adverse effects of mu agonists, respiratory depression but they produce dysphoria and physchotomimetic effects.

Front 9

What are the four groups in which opioid are divided into?

Back 9

1. Full agonist
2. Partial agonist
3. Mixed agonist/antagonist
4. Antagonist

Front 10

Morphine-like agonist

Back 10

derivatives of morphine, the natural opioid derived from opium

Front 11

Heroin

Back 11

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.

Front 12

Name 3 full morphine-like agonist

Back 12

morphine, hydromorphone, and oxymorphone

Front 13

Name 3 partial morphine-like agonist

Back 13

Codeine, hydrocodone, and oxycodone

Front 14

Codeine

Back 14

synthetic version of morphine that is relatively weak mu receptor agonist.

Front 15

What converts codeine to morphine?

Back 15

CYP2D6, most of it analgesic activity somes from this conversion. However, the antitussive activity of codeine is due mostly to codeine itself

Front 16

What is the full mu receptor agonist of methadone-like agonist?

Back 16

Methadone

Front 17

Is Methadone long-acting or short-acting?

Back 17

Long-acting synthetic mu opioid agonist

Front 18

What is the partial mu receptor agonist of methadone-like agonist?

Back 18

propoxyphene

Front 19

What is Methadone known for?

Back 19

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)

Front 20

What is potent full mu opioid agonist of Meperidine-Like agonist?

Back 20

Meperidine

Front 21

What has meperidine fallen into disfavor for the use of?

Back 21

chronic pain relief, and its use is now somewhat limited to acute pain relief

Front 22

What is meperidine metabolized to?

Back 22

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).

Front 23

What are the partial mu receptor agonist of Meperidine-like agonist?

Back 23

Diphenoxylate and loperamide

Front 24

What are diphenoxylate and loperamide useful for?

Back 24

They are useful as constipating agents for patient with diarrhea.

Front 25

What happens at higher doses of diphenoxylate?

Back 25

It may be absorbed and penetrate the blood-barrier sufficiently to cause meperidine-like effects on the CNS

Front 26

What happens at higher doses of Loperamide?

Back 26

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.

Front 27

What are the full mu receptor agonist of Fentanyl-like agonist?

Back 27

Fentanyl (well-known for its high potency) and Sufentanil

Front 28

TRUE/FALSE. Fentanyl and Sulfentanil are more potent then morphine.

Back 28

TRUE

Front 29

Describe 2 characteristics of the fentanyl-like agonist.

Back 29

very lipophilic. As a result, they distribute well and fast to the CNS.

Front 30

Which drug has excellent transdermal penetration and why?

Back 30

Fentanyl has excellent transdermal penetration due to high lipophilicity, and it has gained popularity as a transdermal anagelsic in chronic pain management.

Front 31

Nalbuphine

Back 31

-opioid with strong agonist activity at kappa opioid receptors
-also mu receptor antagonist

Front 32

Buphrenorphine

Back 32

-partial mu opioid receptor agonist and partial kappa receptor agonist
-extremely long duration of action

Front 33

Butorphanol

Back 33

-an opioid with predominant kappa agonist activity
-may also function as a partial mu agonist or as an antagonist at my opioid receptors

Front 34

Pentazocine

Back 34

-oldest mixed agonist/antagonist opioid drug, has kappa agonist activity as well as weak agonist acitivity at mu opioid receptors.

Front 35

Which 2 drugs are antagonist at mu opioid receptors?

Back 35

Naltrexone and Naloxone

Front 36

Which drug is the "gold standard" in terms of opioid antagonists?

Back 36

Naloxone

Front 37

Which opioid antagonistic drug is useful as an antidote for opioid overdose?

Back 37

Naloxone