21-22 Analgesia Flashcards

1
Q

Where do NSAIDs modulate pain?

A

at the initial signal transduction, and spinal cord transmission

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2
Q

Where do Na channel blockers modulate pain?

A

they are local anisthetics that block signal conduction in nociceptive fibers

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3
Q

Where do opioids modulate pain?

A

spinal cord and central perception

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4
Q

How do NE, GABA, endogenous opiates, endorphin, and encephalin inhbit spinal cord transmission?

A

they decrease pre-synaptic Ca entry and activate post-synaptic K channels to hyperpolarize the cells.

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5
Q

What receptor is involved in pain sensitization? What drugs inhibit it to prevent it?

A

NMDA. inhibited by ketamine and dextromethorphan

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6
Q

MOA of ketamine

A

NMDA inhibitor. Prevents pain sensitization

??

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7
Q

ADE of ketamine

A

hallucinations, amnesia, HTN (intracranial too)

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8
Q

MOA of dextromethorphan

A

NMDA inhibitor. Prevents pain sensitization

antitussive that acts on CNS cough center.

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9
Q

ADE of dextromethorphan

A

dizzy, confusion, fatigue.

Hallucinations when abused.

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10
Q

What effect do substance P (SP) and CGRP have?

A

generate inflammatory response and alter pain perception

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11
Q

What is a treatable cause of neuropathic pain? What drug would you use?

A

Na channel expression changes.
Na 1.3 goes up and cells are more easily excited.

Carbamazepine is a Na channel blocker used to treat trigeminal neuralgia and such neuropathic pain

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12
Q

MOA of carbamazepine

A

Na channel blocker. Can prevent neuropathic pain

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13
Q

ADE of carbamazepine

A

??

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14
Q

Which opioid receptor suppresses respiration and GI motility heavily?

A

OP-3 (mu)

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15
Q

Which opioids have the highest oral:IV potency ratio and what does that mean?

A

methadone, and meperidine slightly less so.
means that oral dosage requirement is similar to the IV dose, whereas a low oral:IV potency ratio would mean you need to give a lot more orally to equal what IV can do.

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16
Q

Which opioid is IV only?

A

remifentanil

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17
Q

Which opioids are mu (OP-3) selective?

A

H-FORMMM

hydromorphone, fentanyl, oxymorphone, remifentanil, methadone, and morphine (morphine has slight k (OP-2) action)

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18
Q

What drug has analgesic effects due to its metabolism in the body?

A

codeine and oxycodone, metabolized in part to morphine. Only effective after oral administration.

19
Q

Which opioids act mainly on k (OP-2) receptor?

A

butorphanol, nalbuphine and pentazocine

20
Q

Which opioids are delivered transdermal via patches?

A

fentanyl

21
Q

Can morphine be given orally?

A

could, but it suffers from high first pass, unlike codeine and oxycodone, so oral dose has to be huge and that’s not recommended

22
Q

How does sensitization to opioids occur?

A

GRK increases receptor affinity for beta-arrestin that leads to receptor internalization.

23
Q

Which side effects of opioids do patients never really develop tolerance too?

A

miosis, constipation and convulsions

squint, shit and shake

24
Q

What is major stimulatory transmitter for GI peristalsis?

A

Ach. Opioids inhibit it.

25
Q

What is a benefit of fentanyl

A

less constipation than oral sustained release morphine

26
Q

What is classical triad of opiate overdose?

A

coma, pinpoint pupils and respiratory depression

27
Q

What are the opiate antagonists?

A

the Nal’s. Naloxone, naltrexone, and nalmefene.

28
Q

Which opiate antagonist is used to treat opiate intoxication and why?

A

Naloxone because it has short duration of action

29
Q

Which opiate antagonist is used to treat addiction and why?

A

naltrexone becuase of longer duration.

Or buprenorphine mixed with naloxone

30
Q

How is naltrexone useful for alcoholics?

A

decreases alcohol craving in alcoholics by decreasing baseline B-endorphin release

31
Q

What is an absolute contraindication of opiates?

A

MOA inihibitors because it will cause hyperpyrexic coma.

Also be careful with antipsychotics and sedatives.

32
Q

ADE of meperidine?

A

is converted to normeperidine witch isn’t as potent of an analgesic but 3x more toxic to CNS.
Inhibits 5-HT and NE reuptake.

33
Q

Which opiate is used to withdrawal treatment?

A

methadone because of its long elimination half-life.

clonidine because it treats drug craving, sweating, piloerection, anxiety and agitation (patient will still have insomnia, cramps and GI symptoms)

34
Q

Symptoms of opiate withdrawal?

A

agitation, diaphoresis, heavy lacrimation, piloerection and dilated pupils

35
Q

What is mechanism of naloxone?

A

IV only opiate antagonist. Mixed with buprenorphine (to treat dependence) to prevent abuse and help cure addiction. When taken orally it has no effects.

36
Q

What is drug of choice for opiate-dependent preggers?

A

methadone

37
Q

ADE of methadone?

A

QTc prolongation and arrhythmia.

Reduced testosterone and libido, ED.

38
Q

What is used to identify morphine, heroin, hydrocodone and codiene use?

A

EIAs(antibody enzymatic immunoassays). Downfall is it won’t pick up synthetics like fenatyl

39
Q

MOA of gabapentin?

A

upregulate Ca channels via alpha-2delta subunit to prevent trafficking to cell surface. Inhibits neuron excitability.

40
Q

MOA of lamotrigine?

A

Na channel blocker useful for Neuropathy and phantom limb

41
Q

ADE of lamotrigine?

A

BBW for rash and steven-johnson syndrome.

Diplopia and rarely hematologic toxic.

42
Q

MOA of loperamide?

A

nonprescription opioid agonist used to treat diarrhea. No BBB access so no analgesia

43
Q

MOA of diphenoxylate? What is it mixed with to prevent abuse?

A

prescription opioid agonist used for diarrhea. High doses can have analgesic effect. Atropine to prevent abuse