45 - 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

Most potent opioid (80000x more potent that morphine)

Answer 6

Ohmefentanyl

Question 7

Opioid of choice for pain relief in pancreatitis and biliary colic

Answer 7

Meperidine

Question 8

• 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
• Currently being investigated as a novel treatment for leukemia

Answer 8

Methadone

Question 9

• 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

Answer 9

Hydrocodone

Question 10

• Partial Opioid Agonist
• Decreases sensitivity of cough receptors through sigma receptor stimulation
• Drug for cough
• SE: Addiction liability
• What is the adverse effect when combined with SSRIs of MAOIs?

Answer 10

• Dextrometorphan
• Serotonin syndrome

Question 11

• 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• WITHDRAWN due to fatal cardiotoxicity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 11

Propoxyphene

Question 12

• 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 12

Nalbuphine (Buprenorphine, Butorphanol, Pentazocine)

Question 13

Opioids that can reduce craving in alcohol dependence

Answer 13

Buprenorphine

Question 14

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

Answer 14

Naloxone

Question 15

• 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 patients with epilepsy
• What is the adverse effect when this is used with SSRIs?

Answer 15

Tramadol (Tapentadol)

Serotonin syndrome

Question 16

Triad of Opioid Overdose

Answer 16

• Pupilary Constriction
• Comatose State
• Respiratory Depression

PCR

Question 17

How do you confirm opioid overdose pharmacologically?

Answer 17

IV injection of Naloxone results in recovery

Question 18

Analgesic of choice for MI due to reduction in preload

Answer 18

Morphine

Question 19

Full Opioid Agonist, nonselective

Acts on Mu receptors

SE: Pruritus

Exerts hemodynamic effects on pulmonary circulation

Answer 19

Morphine

Question 20

• Full Opioid Agonist Acts on Mu receptors; Drug for chronic pain, breakthrough cancer pain:
• Methods of administration: (2)

Answer 20

• Fentanyl
• May be given transdermally or via lollipop

Question 21

Full Opioid Agonist Acts on Mu and Kappa receptors; Muscarinic blocking actions; Drug for moderate to severe pain, spasmodic pain (biliary, renal), preop sedation, antiemetic

Answer 21

Meperidine

Question 22

The only opiod that DOES NOT CAUSE MIOSIS or biliary spasm

Answer 22

Meperidine

Question 23

Metabolite of Meperidine that decreases seizure threshold

Answer 23

Normeperidine

Question 24

adverse effect of meperidine when given with MAOi:

Answer 24

hyperpyrexic coma

Question 25

adverse effect of meperidine when given with SSRI:

Answer 25

serotonin syndrome