Opioid Analgesics and Antagonists

Question 1

opioid with shortest half-life

Answer 1

remifentanil (3-4 mins)

Question 2

opioid with longest half-life

Answer 2

buprenorphine (4-8 hours)

Question 3

opioid receptors and their functions

Answer 3

mu = respiration inhibition
delta = tolerance development
kappa = slowed GI transit

Question 4

full agonist
for severe pain, acute MI, pulmonary edema, adjunct in anesthesia
SE: respiratory depression
EXERTS HEMODYNAMIC EFFECTS ON PULMONARY CIRCULATION

Answer 4

morphine = standard in pain control

hydromorphone, oxymorphone (synthetic derivatives)

Question 5

full agonist
for severe pain, adjunct in anesthesia, chronic pain, breakthrough cancer pain
may be given TRANSDERMALLY or via LOLLIPOP

Answer 5

fentanyl

Question 6

most potent opioid

Answer 6

OHMFENTANYL

Question 7

full agonist
moderate to severe pain, labor analgesia, spasmodic pain, pre-op sedation
SE: seizures
does NOT cause miosis and biliary spasm
OPIOID OF CHOICE FOR PAIN RELIEF IN PANCREATITIS
SEROTONIN SYNDROME when used with SSRIs or MAOIs

Answer 7

meperidine

metabolite: normeperidine

Question 8

full agonist
for moderate to severe pain, opioid dependence, opioid withdrawal
used in methadone maintenance therapy (MMT) for opioid dependence
SE: respiratory depression
being investigated as NOVEL TREATMENT FOR LEUKEMIA

Answer 8

methadone

levomethadyl acetate, levorphanol

Question 9

partial agonist
for moderate to severe pain, cancer pain, neuropathic pain, chronic pain
SE: HYPOGONADISM, HEARING LOSS

Answer 9

hydrocodone
oxycodone

medium strength opiate

Question 10

partial agonist
for COUGH SUPPRESSION
SE: addiction liability
SEROTONIN SYNDROME when used with SSRIs or MAOIs

Answer 10

dextromethorphan

codeine

Question 11

weak agonist
for mild to moderate pain, restless legs syndrome, opioid withdrawal
SE: seizures, pulmonary edema, fatal arrhythmias (group 1C anti-arrhythmic)
WITHDRAWN BECAUSE OF FATAL CARDIOTOXICITY
COMMMONLY USED IN SUICIDES

Answer 11

propoxyphene

levopropoxyphene, dextropropoxyphene

Question 12

mixed agonist-antagonist
for moderate to severe pain, opioid dependence, alcohol dependence, balanced anesthesia
SE: sedation
REDUCES CRAVING IN ALCOHOL DEPENDENCE
EFFECTS RESISTANT TO NALOXONE REVERSAL

Answer 12

nalbuphine

buprenorphine (K antagonist), butorphanol, pentazocine, levallorphan

Question 13

antagonist (systemic)
for OPIOID OVERDOSE
precipitates abstinence syndrome in patients with opioid dependence

Answer 13

naloxone

naltrexone (reduces cravings in alcohol, nicotine, and opioid dependence), nalmefene, alvimopan, methylnaltrexone

Question 14

dual-acting (weak agonist)
for moderate pain, chronic pain syndromes, neuropathic pain, fibromyalgia
SE: SEIZURES
lowers seizure threshold
CI IN PATIENTS WITH EPILEPSY
SEROTONIN SYNDROME when used with SSRIs

Answer 14

tramadol

tapentadol

Question 15

signs of opioid overdose

Answer 15

PCR

pupillary constriction
comatose state
respiratory depression