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CNS > Opioids > Flashcards

Opioids Flashcards

1
Q

Opium

A

resinous extract from the capsule of poppy plant (Papaver somniferum)

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2
Q

Analgesic opioids

A

Phenanthrene derivatives

morphine
codeine

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3
Q

Non analgesic opioids

A

Benzoisoquino derivatives

Noscarpine (cough suppressant)
Papaverine (phosphodiesterase inhibitor)

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4
Q

opioid receptors and effects

A

Mu - endomorphic or endorphins
Kappa - Dynorphin
Delta - Enkephalins
4th receptor - ORPHAnin/ FQ receptor - Nociceptin

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5
Q

Mu receptor effects

A

sedation
analgesia (spinal, supra spinal)
constipation, cough suppression
respiratory depression
euphoria
miosis - pin point pupil
nausea/vomiting
gall stones (biliary colic)
abdominal colic (spasm of sphincters)
prolactin release

SACRUM No GAP

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6
Q

kappa receptor effects

A

all effects are like mu receptors except no euphoria

Dysphoria: psychotic symptoms

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7
Q

delta receptor effects

A

analgesia - mainly supraspinal > spinal (reduces pain perception- emotional/affective)
convulsions
constipation
respiratory depression

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8
Q

morphine

A

analgesic
MI - vagomimetic & reduces chest pain, apprehension, symptoms outflow
acute LVF/pulm edema- ventilator

routes- oral, iv, I’m, epidural, spinal, transdermal, except intrathecal (risk of hypotension as it suppresses VMC
except intranasal and sublingual

morphine undergoes glucuronide conjugation to form morphine-6-glucuronide and morphine-3-glucuronide (minor form; toxic-convulsions in children)

morphine-basic drug-histamine release from mast cells - SE: asthma, pruritis

oral/iv morphine - produces miosis
eye drops morphine - does not produce miosis

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9
Q

Opioids contraindicated in renal failure

A

Pethidine
Codeine
Morphine

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10
Q

Least potent opioid

A

Codeine (methyl morphine) - 1/10th analgesic
equally antitussive (suppresses cough centre)
codeine is metabolised by CYP2D6 into morphine

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11
Q

10x more potent analgesic and more addictive

A

Heroin (Diacetyl morphine) / brown sugar/ smack

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12
Q

100x more potent than morphine

A

fentanyl

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13
Q

1000x more potent than morphine
max plasma protein bound

A

Sulfentanyl

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14
Q

mu agonist plus snri

A

Tramadol
Tapentadol

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15
Q

Antitussives

A

Codeine
Hydrocodone
Oxycodone
Pholcodeine

Morphine
Hydromorphone
Oxymorphone
Levorphanol

SE: addiction, sedation

non addictive
Dextromethorphan- NMDA Antagonist
Noscarpine: Sigma agonist

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16
Q

Pethidine/Merperdine

A

mu agonist + anticholinergic

DOC for pregnancy and post anesthesia shivering

prodrug: pethidine converted into merperdine (active) and norpethidine (minor) - SE: seizures

CI: MAO inhibitors/ in renal failure

atropine like effects : increases heart rate - CI: MI
antispasmodic: least risk of colicky pain

17
Q

opioids with least risk of causing coliky pain

A

Pethidine

18
Q

Fentanyl

A

highly LS drug - best analgesic

all routes except oral - high FPM in liver
transdermall- chronic cancer pain
epidural injection- epidural analgesics
iv inj, SL, buccal - acute pain

rare SE: wooden chest syndrome- muscle rigidity

19
Q

Remifentanyl

A

shortest opioid - rapidly metabolised by plasma esterase

iv drug

DOC for day care surgery and total iv anesthesia (add to Propofol)

20
Q

Day care surgery

A

General anesthetic: Propofol
Analgesic: Remifentanyl
Skeletal muscle relaxants: Mivacurium

21
Q

Longest opioid

A

Methadone
mu agonist and NMDA antagonist

iv action starts in 10-20 mins
oral action starts in 30-40 min

use - opioid deaddiction (no kick, prevents withdrawal)

SE: increase QT interval

22
Q

partial Kappa agonist and mu antagonist

A

Pentazocine: reduces risk of colicky pain- renal colic

Nalorphine

Butarphanol- migraine headaches

ADV: less risk of respiratory depression

SE: dysphoria

CI: opioid deaddiction

23
Q

pure Kappa agonist

A

Nalfurafine- uremic pruritus in CKD

Asimadoline and Eluxadoline - diarrhoea in IBS

SE: dysphoria/psychosis

24
Q

partial mu agonist and Kappa antagonist

A

Buprenorphine - opioid deaddiction, less risk of respiratory depression as compared to Methadone, effect cannot be reversed by Naloxone

Dezocine - iv analgesic, less risk of respiratory depression

25
Q

Pure antagonists

A

Naloxone - iv - antidote of opioid poisoning

Naltrexone - oral - opioid deaddiction; SE: hepatotoxic

Nalmefene - oral, iv - both above uses; liver safe

new: Naloxol, Naloxegol, Nalmedine

26
Q

tolerance to opioids

A

tolerance does not develop to constipation, convulsion, constricted pupil
Max convulsion develops to euphoria

27
Q

symptoms of opioid paining

A

pin point pupil
constipation
dry eyes/mouth
convulsions
resp depression

28
Q

symptoms of opioid withdrawal

A

mydriasis
diarrhoea
running nose/ increased salivation/ increased lacrimation
(no convulsions)
yawning

29
Q

Acute opioid poisoning

A

iv Naloxone repetitive inj

30
Q

Maintenance or detoxification of opioids

A

Opioids - Buprenorphine, Methadone, Tramadol

Non opioids - Clonidine, Lofexidine

31
Q

Relapse of opioid addiction

A

Oral Naltrexone

32
Q

Treatment of opioid induced constipation

A

Alvimopan (mu opioid antagonist)

oral Naloxone, Methyl Naltrexone, Naldemidine - not absorbed in GIT - blocks mu/kappa/delta in GIT

33
Q

opioids used in diarrhoea

A

Loperamide (mu agonist) - DOC for diarrhoea in IBS and drug induced (Irinotecan) - not absorbed from GIT and does not cross BBB - non addictive

Diphenoxin (mu agonist) - addictive - combined with atropine: reduce GIT absorption - reduce addiction

Diphenoxylate (mu agonist)

Asimadoline, Eluxadoline, Fedotozine (Kappa agonist) IBS

Racecadrotil - enkephalinase inhibitor - safest drug in children

Ziconotide - Omega conotoxin - intrathecal analgesic - blocks N type of calcium channel in brain, 1000 times more effective painkiller than morphine

CNS (5 decks)

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