opiates and pain meds

Question 1

what things are seen in other types of withdrawal but not opiate withdrawal?

Answer 1

hallucinations, delirium, fever, seizures

Question 2

when would HTN and tachycardia be seen with opiate withdrawal? why?

Answer 2

iatrogenically-induced withdrawal

catecholamine surge

Question 3

what is given to inpatients with opiate withdrawal?

Answer 3

methadone

Question 4

what is given to outpatients with opiate withdrawal? what doesn’t it alleviate?

Answer 4

clonidine (alpha2 agonist)

GI symptoms, MSK pain, insomnia

Question 5

what is used to treat opiate dependence? what is used in pregnant women? what is used as maintenance therapy?

Answer 5

buprenorphine

methadone and methadone

Question 6

what opiate is often coformulated with an NSAID? what is it used for primarily? what is its potency?

Answer 6

codeine
cough suppression
0.1

Question 7

what is probably the way codeine primarily works? what is the problem with that?

Answer 7

metabolized to morphine

dangerously high levels in rapid metabolizers

Question 8

what opiate is used as a patch? what is its potency?

Answer 8

fentanyl, 100

Question 9

what two drugs are used in renal insufficiency? why? when should you use one over other? what’s an alternative 3rd drug

Answer 9

fentanyl and hydromorphone (may use oxycodone)
no active metabolites
use hydromorphone for short-term analgesia

Question 10

what are three adverse effects of methadone?

Answer 10

1. additive respiratory depression with heroine
   - >concern in opiate withdrawal/dependence management
2. decreased testosterone
3. prolonged QTc, arrhythmia, torsades

Question 11

what drug has an active metabolite and what is concerning about it?

Answer 11

meperidine->normeperidine

an SSRI, can cause seizures

Question 12

what is on off-target effect of meperidine and what is the consequence on overdose?

Answer 12

anti-muscarinic

overdose won’t show miosis

Question 13

which full opiate agonist also is an agonist of kappa receptors?

Answer 13

morphine

Question 14

what’s a significant adverse effect of morphine?

Answer 14

pulmonary edema

Question 15

what is the most potent opiate agonist? 2nd? how potent?

Answer 15

sufentanil 1000x

remifentanil 200x

Question 16

what is the potency of tramadol? how does it probably work?

Answer 16

0.1x

SSRI probably accounts for most of effects (and NE reuptake inhibition)

Question 17

what are two adverse effects of tramadol?

Answer 17

seizures

blood sugar regulation problems

Question 18

why is loperamide useful for treatment of diarrhea?

Answer 18

doesn’t cross BBB, so no analgesia or addiction

Question 19

why is diphenoxylate useful as an anti-diarrheal? how is it formulated?

Answer 19

no analgesia at recommended doses

formulated with atropine to discourage abuse

Question 20

what opiates are used in anesthesia?

Answer 20

the -fentanil’s: afentanil, fentanyl, sufentanil, and remifentanil

Question 21

what two drugs are coformulated with acetaminophen? 2 reasons why?

Answer 21

hydrocodone and codeine

1. reduce opiate overdoses
2. diversify MOA/site of action

Question 22

what are the three main signs of opiate overdose?

Answer 22

1. coma
2. pinpoint pupils
3. respiratory depression

Question 23

what are three drug classes contraindicated with opiates and why?

Answer 23

1. sedative hypnotics: respiratory depression
2. antipsychotic tranquilizers: increased sedation, CV effects
3. MAOI’s: hyperpyrexic coma

Question 24

what agonist/antagonists also are agonists of kappa? which are antagonists of kappa and delta?

Answer 24

butorphanol, pentazocine, and nalbuphine

buprenorphine

Question 25

what is the main adverse effect of kappa agonists?

Answer 25

dysphoria

Question 26

what is the indicated use of butorphanol?

Answer 26

relief of acute/post-operative pain | migraines

Question 27

what agonist/antagonist can be given to patients with stable CAD?

Answer 27

nalbuphine

Question 28

what drug is used for severe respiratory depression and obtundation/acute opioid overdose?

Answer 28

naloxone

Question 29

what opiate antagonist is being used for alcohol addiction?

Answer 29

naltrexone

Question 30

what opiate antagonist is used to prevent adverse effects? why?

Answer 30

methyltrexone | doesn't cross BBB so still get central analgesia

Question 31

what does ketamine do? what is its limitation? what is it used for?

Answer 31

NDMA blocker limited by psychomimetic effects useful to avoid respiratory depression and treat acute severe pain

Question 32

what is dextromethrophan? how is it used? what is its limitation?

Answer 32

NDMA blocker cough suppression, and chronic and post-operative pain psychomimetic effects

Question 33

what are two reasons TCA's are useful in pain? how are they metabolized/excreted?

Answer 33

NE and serotonin reuptake blocking properties many chronic pain patients have depression CYP2D6 hepatic metabolism

Question 34

how does gabapentin work? what is the other drug like it?

Answer 34

Ca-channel blocker, prevents trafficking to surface preventing hypersensitization to pain pregabalin

Question 35

what drug induces its own metabolism?

Answer 35

carbamazepine

Question 36

how does carbamazepine work?

Answer 36

Na-channel blocker | blocks synaptic transmission in trigeminal nucleus

Question 37

how does lamotrigene work? what is it useful for?

Answer 37

Na-channel blocker | neuropathy, stroke, MS, phantom limb

Question 38

what pain drug has a BBB? what is it? what are three other adverse effects?

Answer 38

lamotrigene: SJ-syndrome | blurred vision, diplopia, hepatic toxicity