September 2, 2015 - Narcotics

Question 1

Components of Pain

Answer 1

Production

Perception

Expression

Question 2

Opiates vs Opioids

Answer 2

Opiates are naturall present in opium

Opioids are manufactured. These can be semisynthetic or synthetic

Question 3

Bioavailability of Morphine

Answer 3

Has a big first-pass.

Bioavailability is 40-50%

Question 4

Elimination of Morphine

Answer 4

Excreted by kidney. Short half-life.

Question 5

Function at Receptors: Full Agonist

Answer 5

Binds to the receptor.

Ie. Morphine

Question 6

Function at Receptors: Partial Agonist

Answer 6

Binds to the receptor and produces smaller effects at full dosage than a full agonist.

When given with an agonist, partial agonists may act as an antagonist by preventing agonist binding (reducing agonist effect).

Ie. Buprenorphine

Question 7

Function at Receptors: Antagonists

Answer 7

Drugs bind to the receptor but do NOT activate the receptor.

Competitive antagonist can be overcome by increasing the dose of the agonist, but non-competitive antagonists cannot be overcome by increasing the dose of the agonist.

ie. Naloxone and Naltrexone

Question 8

Opioid Toxicity

Answer 8

Common: nausea, sedation, constipation

Narcosis: reversible with naloxone

Neurotoxicity: anxiety, agitation, restlessness, confusion, hyperalgesia, delirium