opioids

Question 1

Morphine

Answer 1

Phenanthrene alkaloids-

Question 2

Codeine

Answer 2

Phenanthrene derivative- metabolized to morphine

Question 3

Opiate

Answer 3

Natural

Question 4

mu receptors

Answer 4

endorphins –>enkephalins–>dynorphins

Question 5

delta

Answer 5

enkephalins—>endorphins —dynorphins

Question 6

kappa

Answer 6

Dynorphine —>endorphins—>enkephalins

Question 7

Opioid receptors are

Answer 7

GPCRs

Question 8

We have natural ligands that activate our

Answer 8

mu receptors (in CNS and GI system)

Question 9

Until 1990s, these receptors were known as

Answer 9

orphan receptors —we weren’t able to identify molecules that activated them. Molecules identified were fatty molecules :

Question 10

Molecule that was discovered which activated the orphan receptors

Answer 10

Andamamide

Question 11

Endogenous opioid peptides

Answer 11

endorphins and enkefalin— “Runners High”

Question 12

Most of these opioids are well absorbed, but they undergo

Answer 12

First pass effect –these drugs may be better absorbed –IV. IM TD

Question 13

Morphine is metabolized to

Answer 13

M3G (90%-excitatory/ euphoric) and M6G (10% analgesia)

Question 14

Heroin is metabolized to

Answer 14

6-monoacetylmorphine (6-MAM is looked for in the urine) and morphine . Heroin is esterified morphine

Question 15

How do opioids work?

Answer 15

Opioid receptors are on both the pre syn and post sun – opioids will activate both.

Pre syn- associated with voltage calcium channels.

Post syn-associated with voltage gated potassium channels.

If ligand binds to post syn=efflux of potassium

If ligand binds to pre syn=blocks calcium channels

The receptors are in the brain and spinal cord.

Question 16

Organ system effected my morphine

Answer 16

Miosis
Euphoria

Cough suppression 
analgesia
n/v
truncal rigidity 
sedation 

Peripheral effects

Cardio
Renal
GI
Uterus 
Billary tract
pruritus

Question 17

No tolerance with opioids regarding

Answer 17

constipation

myosis

Question 18

Overdose with opioid treatment

Answer 18

increase O2 or give antagonist

Question 19

Morphine is a

Answer 19

strong agonist (phenantrenes)

Question 20

Heroin

Answer 20

strong agonist (phenantrenes)

Question 21

Oxymorphone

Answer 21

strong agonist (phenantrenes)

Question 22

Fentanyl

Answer 22

strong agonist (phenylpiperidines)

Question 23

Methadone

Answer 23

strong agonist (phenylheptylamines)

Question 24

Hydrocodone

Answer 24

Mild to moderate agonist (works as prodrug)

Question 25

Oxycodone

Answer 25

Mild to moderate agonist (works as a prodrug)

Question 26

Loperamide

Answer 26

Mild to moderate agonist (works as a prodrug)

Question 27

Buprenorphine

Answer 27

Ago-antagonist (antagonist is added incase it is criushed)

phenantrenes

Question 28

Ago antagonist activate which kind of receptors

Answer 28

mu and kappa

Question 29

NALOXONE

Answer 29

ANTAGONIST

Question 30

Naltrexone

Answer 30

antagonist

Question 31

Antitussives

Answer 31

Dextromrthorphan–this drug penetrates the BBB and with EtOH may give effects of other opioids .