28 opioids drugs

Question 1

what is the edogenous ligand for the Mu receptor?

Answer 1

beta-endorphins

Question 2

how do opiod receptors work when an endogneous binds to them?

Answer 2

they are Gi .

when the ligand binds to them they decrease the activity of adenylate cyclase.

this decrease the amount of cAMP

increase efflux of K

leads to decrease of influx of Ca.

there is alot less neurotransmitter released.

Question 3

what is the edogenous ligand for Kappa?

Answer 3

dynorphins

Question 4

what is teh endogenous ligand for delta?

Answer 4

enkephalins

Question 5

what drugs are activated by metabolism?

Answer 5

codeine and heroin

Question 6

what opioids are also cough suppresants?

Answer 6

Codeine, hydrocodone and dextromethorphan

Question 7

what drugs go thorgh extensive first pass effects?

Answer 7

morphine and naloxone.

Question 8

μ agonist

with a Low oral to parenteral potency ratio - about 3 or 4 to 1

Answer 8

morphine

Question 9

More lipophilic than morphine.

?

Answer 9

heroin

Question 10

what mu agonists are for mild to moderate pain?

and often used in combination with NSIAD or acetominophen?

Answer 10

codeine hydrocodone oxycodone

Question 11

mu agonist

Equipotent with morphine; has good oral availability

Longer duration of action

Answer 11

methadone

Question 12

mu agonist

Shorter duration of analgesia than morphine

Forms toxic metabolite, normeperidine, that can accumulate with frequent use

Interactions with MAO inhibitors

Answer 12

Meperidine

Question 13

μ agonist

100 X as potent as morphine

Short-acting – 1 to 1.5 hours

Answer 13

fentanyl

Question 14

2-3 X as potent as morphine

Answer 14

hydromorphone

Question 15

μ antagonist and kappa agonist

Similar in efficacy and potency to morphine

Much lower abuse potential

Answer 15

nalbuphine

Question 16

Partial μ agonist

Used to treat moderate to severe pain – now available as patch

Oral buprenorphine combined with naloxone (Suboxone®) is used to treat opioid dependence

Answer 16

buprenorphine

Question 17

opioid antagonist

High affinity for μ receptors. Significantly less for kappa and delta

Much greater activity parenterally than orally

Short duration of action – 1 to 2 hours

Used to treat opioid overdoses

Answer 17

naloxone

Question 18

opioid antagonist

Orally active with long half-life

Can be used in treatment of alcoholism and opiate addiction

Answer 18

naltrexone

Question 19

Antitussive, but not analgesic. Also is an NMDA antagonist.

Answer 19

dextromethorphan

Question 20

weak mμ agonist. Also blocks NE and 5-HT uptake

1. Used for mild to moderate pain

available in oral form

Answer 20

tramadol

Question 21

what drug can you use for opioid abuse?

Answer 21

suboxone