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Pharm Block 3 > opioids > Flashcards

opioids Flashcards

1
Q

endogenous opioid peptides

A

enkephalins endorphins dynorphins

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2
Q

endogenous ligands for mu receptor

A

enkephalins, B-endorphin

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3
Q

drug ligands for mu receptor

A

morphine, fentanyl, methadone, meperidine, buprenorphine

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4
Q

endogenous ligands for kappa receptor

A

dynorphins

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5
Q

drug ligands for kappa receptor

A

butorphanol, pentazocine, nalbuphine

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6
Q

endogenous ligands for delta receptor

A

enkephalins, B-endorphin

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7
Q

drug ligands for delta receptor

A

none

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8
Q

opioid pharmacology

A

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

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9
Q

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

A

morphine

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10
Q

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

A

codeine

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11
Q

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

A

oxycodone

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12
Q

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

A

hydrocodone

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13
Q

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

A

heroin

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14
Q

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)

A

methadone

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15
Q

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

A

meperidine

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16
Q

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

A

fentanyl

17
Q

other opioid agonist, 2-3X potency of morphine

A

hydromorphone

18
Q

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

A

nalbuphine

19
Q

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

A

buprenorphine

20
Q

oral buprenorphine + naloxone used to treat opioid dependence

A

suboxone

21
Q

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

A

naloxone

22
Q

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

A

naltrexone

23
Q

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

A

dextromethorphan

24
Q

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

A

tramadol

25
Q

clinical problems with opioids

A

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

26
Q

tolerance to N/V vs miosis & constipation

A

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

27
Q

morphine withdrawal symptoms 6-12 hr

A

drug seeking behavior, restlessness, lacrimation, sweating, rhinorrhea

28
Q

morphine withdrawal symptoms 12-24 hr

A

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

29
Q

morphine withdrawal symptoms 24-72 hr

A

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

30
Q

morphine withdrawal symptoms later on

A

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
Q

treatment of opioid abuse

A

methadone, suboxone, naltrexone

Pharm Block 3 (15 decks)

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