opioid analgesics and antagonists

Question 1

opioids

Answer 1

morphine is the prototype.

Question 2

classification includes

Answer 2

full agonists,partial agonists and antagonists.

Question 3

endogenous opioid peptides

Answer 3

3 families:endorphins,enkephalins and dynorphins

Question 4

opioid receptors

Answer 4

u (mu),delta and kappa.

Question 5

mu

Answer 5

mu 1 and mu2 .have a high affinity to endorphins.Their stimulation leads to physical dependence,Euphoria ,suprasoinal analgesia and respiratory depression.PEAR).

Question 6

kappa

Answer 6

kappa 1 and 3.have a high affinity to dynorphins.Their stimulation causes ;sedation,spinal analgesia and miosis.

Question 7

delta

Answer 7

delta 1 and 2.have a high affinity to enkephalins.Their stimulation leads to spinal and supraspinal analgesia and release of growth hormone.

Question 8

sigma

Answer 8

causes dysphoria, hallucination,respiratory and vasomotir stimulation and mydriasis.

Question 9

MOA of opioids

Answer 9

they bind to specific G protein -coupled receptors thay are located in the brain and spinal cord.

Question 10

clinical use of opioid analgesics

Answer 10

analgesia,pulmonary edema,cough,diarrhea ,anasthesia,shivering

Question 11

strong agonists

Answer 11

phenanthrenes-morphine,hydromorphone and oxymorphone.Heroin,methadone.phenylpiperidines-fentanyl ,fentanyk subgroup includes sulfentanil,alfentanil and remifentanil.meperidine and levorphanol.

Question 12

mild to moderate agonists

Answer 12

codeine,oxycodone ,dihydrocodeine and hydrocodone.proloxyphene, diphenoxykate and loperamide.

Question 13

partial agonists

Answer 13

Nalbuphine,beprenorphine,butorphanol,pentazocind.

Question 14

tramadol

Answer 14

blocks serotonin reuptake also inhibits norepinephrine transporter function

Question 15

antagonists

Answer 15

naloxone,naltrexone and nalmefene