Molecular biology
Site of Action
Pharmacology
Fentanyl
Side Effects
100
Commonly used opioids (morphine, fentanyl, etc) primarily bind to this receptor
What is the mu receptor
100
Mu 2 opioids work here presynaptically to decrease the release of substance P and hyperpolarize post synaptic neurons
What is the spinal cord (also accept substantia gelatinosa of the dorsal spinal cord)
100
This active metabolite of morphine accumulates in renal failure
What is Morphine 6 glucuronide
100
Fentanyl administered immediately before incision reduces MAC by
What is 70%
100
Increasing useage necessitates increased dosage
What is tolerance
200
Opioid receptors are coupled to these proteins which regulate adenylate cyclase and ion channels
What are G proteins
200
Activation of the mu1 receptor in the periaqueductal gray, locus cerulus, and the nucleus raphe magnus for example
What is supra spinal opioid action (will also accept: what initiates descending modulatory systems of analgesia)
200
This active metabolite of meperidine causes CNS excitation
What is normeperidine
200
High dose fentanyl (50-150 mcg/kg) blocks the hemodynamic response to surgery but does not reliably produce this
What is loss of consciouisness (and/or amnesia)
200
Tolerance does not develop to this side effect
What is opioid induced bowel dysfunction (or constipation)
300
The binding of mixed agonist antagonists (like butorphanol or nalbuphine) to this receptor is responsible for their antipruritic and sedating properties
What is the kappa receptor
300
Activates peripheral opioid receptors
What is infammation
300
The terminal elimination half life of fentanyl is longer or shorter than morphine
What is longer (6.6 vs 3.1 hours)
300
Rapid metabolism by this enzyme is responsible for the short duration of action of remifentanil
What is tissue and plasma esterases
300
This side effect is NOT caused by histamine release
What is pruritus
400
Decreased gastric transit (constipation or anti-diarrheal) is a central or peripheral opioid receptor effect
What is peripheral receptor effect
400
Binding of opioids in this part of the brain causes nausea and vomiting
What is the chemotactic trigger zone (in the area postrema of the medulla)
400
CYP 2D6 converts this common inactive prodrug into morphine
What is codeine
400
The most potent fentanyl
What is carfentanil (will accept sufentanil)
400
Dextroisomers of opioids which do not produce analgesia cause this side effect
What is cough suppression (or what are the anti-tussive effects of opioids)
500
This opioid receptor is found on vascular tissues and leukocytes and is important in tumor surveillance and anti-inflammation
What is the mu 3 receptor
500
Name 2 opioids that release histamine
What is morphine and meperidine
500
When given by infusion, the time required for a drug's concentration in the central compartment to decrease by 50%
What is the context senstive half time
500
Despite its hemodynamic stability, this cardiovascular effect of fentanyl can compromise cardiac output
What is bradycardia (will accept benzodiazepine coadministration)
500
Opioid induced increases in sphincter of Odi tone can be reveresed by
What are naloxone or nitroglycerine or atropine
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