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BMB > Opioid Anagelsics > Flashcards

Opioid Anagelsics Flashcards

1
Q

Opioid vs narcotic

A

Opioid is anything that binds to the Mu receptor and inhibits pain
Narcotics are anything that produce sedation/drowsiness

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2
Q

Classification 1: weak vs strong

A

Codeine is weak
Everything else is considered strong
Antitussives and antidiarrheals are excluded

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3
Q

Mu receptor agonists

Antagonists

A

Morphine, merperidine, hydromorphone, etc.

Mu antagonists, bind to this receptor and elicit no response (also but less at kappa and delta)- naloxone and naltrexone

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4
Q

Agonist/antagonists

Partial agonist

A

Kappa agonist/Mu antagonist: nalbuphine

Partial Mu agonist but HIGH affinity: buprenorphine (used for opioid maintenance in addiction)

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5
Q

High vs low lipophilicity

A

High- fast onset (1min IV), short duration (20 min): fentanyl, merperidine
Low- slow onset (10 min IV), long duration (hour): morphine, hydromorphone

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6
Q

Opioid receptors

A

Mu, kappa, delta: one gene codes for each one. Subtypes come from splice variants. All involved in spinal and supraspinal sites

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7
Q

Mu receptor produces:

Site:

A

Analgesia, euphoria, dependence, respiratory depression, miosis
Mu1 is more supraspinal, Mu2 is more spinal

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8
Q

Kappa receptors produce:

A

Mild analgesia, less respiratory depression, psychomimetic effects (unlike euphoria)

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9
Q

Locations of opioid receptors and what they elicit

A

Thalamus/amygdala:suffering of pain, emotional perception of it
Brainstem ventilation nuclei: can knock out and stop breathing
PAG: gateway in MB when switched on to send endorphins down spinal cord to blunt pain transmission and reduce suffering
Area postrema: nausea
Spinal trigeminal nucleus: itchy AEs
Substantial gelatinosa: pain relief
*GI tract (enteric NS layer): constipation

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10
Q

Opioid mechanism

A

Work via G receptor proteins which then inhibit cellular adenylyl cyclase. Increase K+ and decrease Ca++ currents, causes hyperpolarization, and decreased nociceptive transmission.
Doesn’t affect touch and motor fibers like with alcohol and local anesthetics dampening touch receptors

In SG, the opioid receptors are primary pre-synaptic on C fibers.

Opioids also activate the PAG- trigger descending inhibitory paths to release endorphins by inhibiting GABA releasing inhibitory neurons in the PAG (freeing them of inhibition)

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11
Q

What drug is notable for having a half life of 24 hours?

A

Methadone. Can range from 12-104 hours. Which is why you never start treatment with methadone*

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12
Q

What is special about the miosis effect of opioids?

A

There is no tolerance built to this effect

Same with constipation, if this SE is present.

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13
Q

What is a good opioid to use/switch to deal with opioid side effects?

A

Antagonist
Agonist/antagonist
Amphetamines

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14
Q

Abstinence syndrome

A

Withdrawal occurs after cessation of use

Unique to someone who has been exposed to the opioid before

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15
Q

Symptoms of opioid withdrawal

A

Sweating, HTN/tachycardia, hyperventilation, mydriasis- essentially opposing sympathetics of each opioid parasympathetic effect, except diarrhea/abdominal cramping occurs via direct withdrawal from gut receptors.
NON LETHAL WITHDRAWAL

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16
Q

Opioid agonists

A

Morphine, codeine, oxycodone, hydrocodone (Vicodin), heroin, meperidine, hydromorphone (Dilaudid), fentanyl, methadone, tramadol

17
Q

Antagonists

A

Naloxone- near an. IV form

Naltrexone- oral form

18
Q

Agonist/antagonist

A

Nalbuphine

Buprenorphine (technically a partial agonist)

19
Q

Diarrhea opioids

A

Loperamide

Dephenoxylate

20
Q

Antitussive

A

Dextromethorphan

21
Q

Morphine metabolites

A

Morphine 3-Glucoronide and 6-Glucoronide in liver. If there is kidney dysfunction, build up of 6-G in blood will harm, get into spinal fluid and be 50-100x more potent than morphine, cannot cross BBB unless you have a lot of it by mass effect

22
Q

Oxycontin

A

Extended release oxycodone. Matrix releases during GI transit. Abuse by crushing- but no ER should be crushed. Started new formulations that prevented this.

23
Q

What is special about methadone?

A

Takes 3-5 half lives to see full effect: takes this long to see the steady state, so need to watch for accumulation, keep on same dose for a full week to watch for sedation.
NMDA receptor blocker- blunts central sensitization, but analgesic mechanisms are unknown

24
Q

Meperidine caution

A

Metabolite: normeperidine- half life is 10 hours, cleared by kidneys, can cause seizures, DO NOT use in kidney failure patients

25
Q

Fentanyl uses

A

Transdermal- chronic or cancer pain. NOT FOR ACUTE PAIN or for the opioid naive, do not apply heat, sub-Q depot before absorbed in blood so watch for overdose, depot continues in blood even after patch is removed
Lollipop is for cancer pain breakthrough- not for sustained effect

26
Q

Tramadol- works by two mechanisms

A

Mu receptor agonism and blocks reuptake of 5-HT and NE

Technically a pro-drug and the M1 metabolite is Mu agonist

27
Q

Agonist/antagonist: Nalbuphine

A

Analgesia is kappa mediated, weak Mu antagonism (avoids Mu side effects), ceiling effects, less GI side effects and less respiratory suppression
DO NOT USE IN OPIOID TOLERANT PERSON- will cause withdrawal
Problem- kappa agonism causes psychomimetic effects
Low doses used to reverse opioid side effects while maintaining analgesia

28
Q

Partial agonist- buprenorphine

A

Only partial Mu agonist
HIGH affinity, makes naloxone reversal difficult in OD
Has ceiling on agonism*
Currently use for opioid maintenance: less intense than heroin withdrawal and briefer than methadone withdrawal
suboxone= buprenorphine +naltrexone

29
Q

What is special about naloxone?

A

It can reverse the effects of a placebo and acupuncture

Reversal is SHORT LIVED

30
Q

Opioids for diarrhea

A

Poorly absorbed orally, do not enter CNS very well, constipation side effect (naloxone type formulations exist designed to stay in gut and block this side effect)
Loperamide (Imodium)
Dephenoxylate- with atropine: Lomotil

31
Q

Dextromethorphan antitussive

A

No analgesic or habituation get properties
Acts centrally, but not via opioid receptors
NMDA antagonist
Similar potency to codeine

BMB (10 decks)

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