Pharmacology of Opiods

Question 1

What is the flower opium come from

Answer 1

Papaver somiferum L.

Question 2

What are the constituents of opium used in healthcare

Answer 2

Morphine, Codeine, thebaine, papaverine (smooth muscle relaxant), noscapine (antitussive agent)

Question 3

T/F: If a change is made at position 3 or 6 of morphine there would be a change to how well the drug works

Answer 3

True

Question 4

What aspects are associated with mu receptor, sigma, kappa

Answer 4

Analglesia and euphoria, analgesia, analgesia and dysphoria

Question 5

Where are opiod receptors located

Answer 5

brian, spinal cord, and periphery

Question 6

T/F: Opiod receptors are G coupled receptors

Answer 6

True

Question 7

What is analgesia, analgesics

Answer 7

Absence of pain, drugs that produce analgesia withot causing loss of consciousness

Question 8

T/F: Hydromorphone is the gold standard for all opiod nalgesics

Answer 8

False: Morphine is the gold standard for all opioid analgesics

Question 9

What intracellular mechanisms occur after activation of opiod receptors

Answer 9

Inhibition of adenylyl cyclase (Gi), acivation of potassium channels (Go), Inhibiton of Calcium channels (Go)

Question 10

What intracellur mechanisms stops pain transmission in the spinal cord and brain when using opiods

Answer 10

Inhibiting presynaptic calcium channels: reduces pain neutransmitters release
Activating postynaptic potassium channels: leads to hyperpolarization of postsynaptic neurons and prevents the activation of these neurons

Question 11

What is the main cause of death in opiod posining, what can potentially make this work

Answer 11

Respiratory depression, combination of other CNS inhibitors (alchojol, sedatives, hypontics, anesthsics, tranquilzers)

Question 12

What is the major caution with tolerance of opiods

Answer 12

When patients become tolerant they take larger doses for the same effect BUT after detoxification the same tolerated dose can be dangerous to a patient

Question 13

What are other CNS effects of opiods

Answer 13

Drowsiness, depresses the cough reflex, nausea and vomiting, miosis (constriction of pupil), orthostatic hypotension

Question 14

T/F: Switching to a transdermal pack from an oral pack will reduce nausea and vomitting associated with opiods

Answer 14

False: Nausea and vomiting may be present despite formulation change due to triggering of the chemorecptor trigger zone

Question 15

T/F: Opiods can causes, hypothermia, hyperthermia, adn possibly pruritus (itching)

Answer 15

True

Question 16

What do opiods do in the gastrointestinal tract, opiod used peripherally due to these effects

Answer 16

Decrease contractions of GI smooth muscles, decreases GI motility, Increases Gi empyting time, Decreases HCl secretion/ Loperamide

Question 17

What are the common opiods

Answer 17

Codeine, Fentanyl, Hydromorphone, oxycodone, methadone (detox)

Question 18

What are the endogenous opiate peptides, which is mostly mu selective

Answer 18

Enkephalin, Dynoprohin, beta-endorphin, endomorphins/ beta-endorphin

Question 19

What are the opiod antagonists used in opiod overdose, peripherally acting mu opiod receptor antagonists

Answer 19

Naloxone, Naltrexone/ methylnatrexone, alvimopan, naloxegol

Question 20

T/F: Opiods are usually highly lipophillic and oral administration is less effective because of first pass metabolism

Answer 20

True

Question 21

What opiod is converted to morphin, how

Answer 21

Codeine, demthylation that is catalyzed by cytochrome P450 2D6