Opioid Analgesics and Antagonists

Question 1

Opioid with the shortest half life

Answer 1

Remifentanil

3-4 mins

Question 2

Opioid with the longest half life

Answer 2

Buprenorphine

4-8 hours

Question 3

Receptor that inhibits respiration

Answer 3

Mu (Mabagal Huminga)

Question 4

Receptor involved in development of tolerance

Answer 4

Delta (Tolerance)

Question 5

Receptor involved in slowed GI transit

Answer 5

Kappa (Konstipation)

Question 6

Analgesic of choice for MI due to reduction in preload
Full Opioid Agonist, nonselective
Acts on Mu receptors
SE: Pruritus
Exerts hemodynamic effects on pulmonary circulation

Answer 6

Morphine

Question 7

Full Opioid Agonist
Acts on Mu receptors
Drug for chronic pain, breakthrough cancer pain
May be given transdermally or via lollipop

Answer 7

Fentanyl

Question 8

Most potent opioid (18000x)

Answer 8

Ohmefentanyl

Question 9

Full Opioid Agonist
Acts on Mu and Kappa receptors
Muscarinic blocking actions
Drug for moderate to sever pain, spasmodic pain (biliary, renal), preop sedation, antiemetic
Does NOT CAUSE MIOSIS or biliary spasm
Serotonin syndrome when used with SSRIs or MAOIs

Answer 9

Meperidine

Question 10

Opioid of choice for pain relief in pancreatitis and biliary colic

Answer 10

Meperidine

Question 11

Metabolite of Meperidine that decreases seizure threshold

Answer 11

Normeperidine

Question 12

Full Opioid Agonist
Acts on Mu receptors
Drug for moderate to severe pain, Opioid dependence, opioid withdrawal
Used in methadone Maintenance Therapy (MMT) for dependence
Investigated as novel tx for Leukemia
Drug?

Answer 12

Methadone

Question 13

Partial Opioid Agonist
Acts on Mu and Kappa receptors
Drug for Mod to Severe pain, Cancer pain, Neuropathic pain, Chronic pain
SE: Hypogonadism, hearing loss
Drug?

Answer 13

Hydrocodone

Question 14

Partial Opioid Agonist
Decreases sensitivity of cough receptors through sigma receptor stimulation
Drug for cough
SE: Addiction liability
Serotonin syndrome when used with SSRIs or MAOI

Answer 14

Dextrometorphan

Question 15

Weak Opioid Agonist
Acts on Mu receptors
Drug for mild to moderate pain, restless legs syndrome, opioid withdrawal
SE: Seizures, pulmo edema, fatal arrhythmia
WITHDRAWN due to fatal cardiotoxicity
Used in suicides

Answer 15

Propoxyphene

Question 16

Mixed Opioid Agonist - Antagonist
Strong Kappa agonist
Weak Mu antagonist
Drug for Moderate to severe pain, opioid dependence, alcohol dependence, balanced anesthesia
SE: Sedation, dizziness
Resistant to naloxone reversal

Answer 16

Nalbuphine

Buprenorphine, Butorphanol, Pentazocine

Question 17

Opioids that can reduce craving in alcohol dependence

Answer 17

Buprenorphine

Naloxone

Question 18

Systemic opioid antagonist
Blocks, mu, kappa and delta
Drug for opioid overdose
Precipitates abstinence syndrome in pxs with opioid dependence

Answer 18

Naloxone

Question 19

Dual acting opioid analgesic
Weak agonist at mu receptor, inhibits neuronal reuptake of serotonin and NE
Drug for mod pain, chronic pain syndromes, neuropathic pain, fibromyalgia
SE: Seizures
Lowers seizure threshold
Contraindicated in pxs with epilepsy
Serotonin syndrome when used with SSRIs

Answer 19

Tramadol

Tapentadol

Question 20

Triad of Opioid Overdose

Answer 20

PCR
Pupilary Constriction
Comatose State
Respiratory Depression

Question 21

How do you confirm opioid overdose pharmacologically?

Answer 21

IV injection of Naloxone results in recovery