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56 Cards in this Set

  • Front
  • Back
What opiate receptor do morphine, and most opioids work at?
How/where are opioids metabolized?
Conjugated with glucuronic acid in the liver
How does the excretion of morphine break down?
90% urinary, 10% bile
How does an oral dose compare to an I.M. injection of morphine?
(in terms of peak effect)
1/5 - 1/6 of the peak effect
(due to 1st pass metabolism and slow absorption)
How does morphine withdrawal compare
to that of EtOH, BDZs, and barbiturates?
LESS severe
What are the 3 major effector systems of the μ-receptor?
Opening of K channels
Decreased opening of Ca channels
Inhibition of adenylate cyclase
Analgesic effects are due to morphine action where (in body)?
Spinal cord and supraspinal structures
What is allodynia?
Pain caused by previously innocuous stimuli
What type of pain is best relieved by morphine?
Dull, continuous pain
What effects do TCAs and SSRIs have on the effects of opioids?
Potentiate the analgesic effects
By what mechanism are NSAID analgesic effects additive with morphine's?
Decreased PGs --> Decreased activation of nociceptors
Respiratory depression is due to morphine action where (in body)?

What aspect of respiration is primarily affected?
Medulla oblongata and pons

Rate is primarily affected

NOTE: in a morphinized pt. hypoxia may become force behind resp. drive!
Which opioid is the preferred one for cough?
What do opioids directly affect to cause N&V?
Chemotrigger zone and Vestibular system

Note: after 1st dose, refractoriness to N&V is usually seen
Opioid induced nausea can be antagonized by which two drugs?
What effect do opioids have on body temperature?
Cause HYPOthermia
What are pin-point pupils a sign of?

This effect does NOT decrease w/ tolerance
Opioids can cause dramatic hypotension in what type of pts.?
(depress sympathetic tone and baroreflexes)
Where in the GI/GU tracts do opioids act?
(NOT on smooth muscle or secretory cells)
What type of contractions do opioids INCREASE in the GI tract?
NON-propulsive (spasmogenic)

NOTE: can exacerbate epigastric pain and biliary colic
What drug is good in combo w/ opioids to treat diarrhea?
(antagonizes spasmogenic action, potentiates anti-propulsion)
What takes higher doses of opioids?

Analgesia or GI effects

The gut is sensitive to far lower doses
How does naloxone impact codeine's anti-tussive effect?
What happens to codeine to change it to morphine?
It gets demethylated

This happens SLOWLY
These two are identical to morphine, except MORE potent
These two are equipotent w/ morphine, but better absorbed orally?
This drug has a slow release form that is widely abused

Oxycontin is the slow release form
What are hydro/oxy-codone used for?
Low - moderate pain
What happens to heroin to change it to morphine?
It gets deacetylated

This happens RAPIDLY
Optic isomer has no analgesic effects
BUT, has great anti-tussive effects
How does naloxone impact dextrometorphan's anti-tussive effect?
CANNOT reverse it
What opioid is preferred for obstetrical analgesia?

Has a short half-life
Causes less respiratory depression (in child)
Does NOT alter labor
Meperidine important points
Metabolized into normeperidone, which is excitatory

LESS spasmogenic than morphine
Produces less constipation and urine retention
Does NOT inhbit cough

Does NOT alter labor
How is diphenoxylate administered?
Can ONLY be given ORALLY
(very insoluble, so it is NOT abused much)
What is diphenoxylate primarily used for?
Used in combo w/ atropine for diarrhea
What is (su)fentanyl primarily used for?
In combo w/ droperidol for anesthesia
Which is more potent?

Morphine or (su)fentanyl
Fentanyl is ~80 times more potent
This drug is often prescribed in lieu of codeine

What is it? Why is it?

Less effective, BUT abuse liability is lower
Methadone is used for what (2)?
Relieve moderate to severe pain
Replacement therapy of opiate addiction
How is methdaone superior to morphine?
Better abosrption, among other things
What is special about 1-acetylmethadol?

What is it used for?
VERY LONG LASTING (given every 2-3 days)

Deacetylated to methadone
Used in replacement therapy of opiate addiction
What is the receptor action of pentazocin?
μ-receptor antagonist
powerful κ-receptor agonist
Which is more potent?

Penatazocin or Morphine
(pentazocin is only 20 - 50% as potent)
Why is pentazocin not used in CAD?
High doses --> increased BP & HR, and increased NE & Epi
What causes psychotomimetic effects of opioids?
Binding to σ and PCP receptors
(endogenous opioids do NOT bind these)
This drug is equipotent w/ diphenoxylate and is used only for diarrhea
Degree of opioid withdrawal depends on what two factors?
Degree of dependence (related to dosage, etc)
Half-life (the shorter --> the more intense)
How is naloxone administered?
MUST be given I.V.
(ZERO oral bioavailability)
How does naltrexone compare to naloxone?
Same effects
Typically given orally
Lasts much longer
How is clonidine used in the context of opiates?
Adjunct to psychotherapy for withdrawal
Attenuates intensity of autonomic components
Reduces psychological craving
Which opiate is best suited for use in treatment of GI/GU tract disorders?

It is less spasmogenic than others
What side effect can be problematic w/ Meperidine used in pregnancy?
Respiratory distress in the infant

NOTE: this is still less than that caused by morphine
What effects do opioids have on urinary output?
What effect do opioids have on sugar levels?
Cause HYPERglycemia
What effect do opioids have on gonadotrophic hormones?
DECREASED their release from the pituitary
Opioids w/ less abuse potential than morphine (3)?