Analgesics

Question 1

3 main opioid receptors

Answer 1

Mu
Delta
Kappa

Question 2

Opioids examples

Answer 2

Morphine (mu receptor agonist)
Codeine (less potent than morphine)
Heroin (more potent than morphine, especially in addictive properties)
Hydromorphone (5x as potent as morphine)
Hydrocodone (equivalent potency to morphine)
Oxymorphone and oxycodone (low oral potency, but similar to hydromorphone when injected)

Question 3

Phenyl and anilidopiperidines

Answer 3

Removal of B ring: increased flexibility

Examples: fentanyl, diphenoxylate, meperidine, etc.

Question 4

Methadone

Answer 4

Only agent available for opioid addiction

Diphenylheptane

Question 5

Opioid antagonists

Answer 5

Reverse effects of opioids (compete for receptors)
Recovering from anesthesia, treating overdose, relieving constipation
Naltrexone, etc.

Question 6

NSAIDs (Non-steroidal anti-inflammatory drugs)

Answer 6

Relieve mild to moderate pain

Side effects: GI irritation and bleeding, kidney damage

Question 7

How NSAIDs work

Answer 7

Inhibit cyclooxygenase (father of prostaglandins- produce pain and excrete gastric juices)

Question 8

NSAIDs examples

Answer 8

Aspirin
Conventional non-selective cyclooxygenase inhibitors (ibuprofen, etc.)
Selective COX-2 inhibitors (Celebrex, etc.; attempt to avoid side effects of NSAIDs)
Antipyretics (acetaminophen, etc.)
Antirheumatic drugs
Treatments for gout and hyperuricemia

Question 9

Triptans

Answer 9

Used to treat moderate to severe migraines and headaches
Reduce inflammation through constriction of cranial vessels
by stimulating 5-HT receptors 1B and 1D
Decrease firing of neurons that release peptides that cause inflammation