opioids Flashcards Preview

Pharm Block 3 > opioids > Flashcards

Flashcards in opioids Deck (31):
1

endogenous opioid peptides

enkephalins endorphins dynorphins

2

endogenous ligands for mu receptor

enkephalins, B-endorphin

3

drug ligands for mu receptor

morphine, fentanyl, methadone, meperidine, buprenorphine

4

endogenous ligands for kappa receptor

dynorphins

5

drug ligands for kappa receptor

butorphanol, pentazocine, nalbuphine

6

endogenous ligands for delta receptor

enkephalins, B-endorphin

7

drug ligands for delta receptor

none

8

opioid pharmacology

analgesia, cough suppression, antidiarrheal effect/constipation, euphoria, sedation, respiratory depression, nausea, endocrine effects, pupillary constriction

9

mu agonist, low oral to parenteral potency ratio (3/4:1); IV/oral/sustained oral/suppository available, 4-5 hr analgesia

morphine

10

mild to moderate pain, some metabolized to morphine, often used with NSAID/acetaminophen

codeine

11

more efficacious than codeine, used alone for moderate to severe pain, available as sustained release oral

oxycodone

12

moderate to moderate/severe pain, usually combined with NSAID/acetaminophen, sustained release available

hydrocodone

13

diacetyl morphine, more lipophilic than morphine, converted to 6-mono-acetyl morphine and morphine

heroin

14

phenylheptylamine, mu agonist, equipotent with morphine, good oral availability, longer duration of action, used in treatment of opioid abuse and pain, long half life (a day)

methadone

15

phenylpiperidine, shorter duration of analgesia, forms toxic metabolite that can accumulate, interactions with MAO inhibitors

meperidine

16

related to meperidine, mu agonist, 100X potency of morphine, short acting (1-1.5 hr), injectable, transdermal patches, soluble buccal film, used for conscious procedures

fentanyl

17

other opioid agonist, 2-3X potency of morphine

hydromorphone

18

mu antagonist, kappa agonist, similar in efficacy/potency to morphine, little euphoria, low abuse potential can precipitate withdrawal in opiate-dependent patients; only injection

nalbuphine

19

partial mu agonist, 25-50X greater potency than morphine, moderate to severe pain, transdermal patch available

buprenorphine

20

oral buprenorphine + naloxone used to treat opioid dependence

suboxone

21

antagonist w/ high affinity for mu receptor (less for K and D), parenteral > oral activity, short duration (1-2 hr), treatment of opioid overdoses, combined with opioids to decrease parenteral abuse liability, component of suboxone

naloxone

22

orally active with long half-life ( >24 hrs), used in treatment of alcoholism & opiate addiction, competitive antagonist

naltrexone

23

D-isomer of levorphanol, cough suppressant, also NMDA receptor antagonist

dextromethorphan

24

weak mu agonist activity, blocks NE and serotonin uptake, mild-moderate pain, oral, sustained release available

tramadol

25

clinical problems with opioids

respiratory depression, sedation, interactions with CNS-depressant drugs, constipation, nausea, vomiting, endocrine disturbances, tolerance to analgesic effect, physical dependence, abuse potential

26

tolerance to N/V vs miosis & constipation

rapid tolerance to nausea/vomiting, little to no tolerance to miosis and constipation

27

morphine withdrawal symptoms 6-12 hr

drug seeking behavior, restlessness, lacrimation, sweating, rhinorrhea

28

morphine withdrawal symptoms 12-24 hr

restless sleep, irritability, tremor, dilated pupils, anorexia, gooseflesh

29

morphine withdrawal symptoms 24-72 hr

increased intensity of symptoms, increased HR/BP, involuntary movements of arms and legs

30

morphine withdrawal symptoms later on

symptoms continue 7 to 10 days, alternating autonomic hyperactivity with brief periods of restless sleep delayed growth/devo in infants born to addicted mothers detected up to 1 year

31

treatment of opioid abuse

methadone, suboxone, naltrexone