OPIODS DRUGS-- Morphine Flashcards

1
Q

how many receptors are there for opiods?

A

3
mu
kappa
delta

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2
Q

what nociception in mu involved in?

A

Thermal
chemical
mechanical

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3
Q

what nociception is kappa involved in?

A

thermal
chemical

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4
Q

what process is delta involved in?

A

interaction with enkephalins

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5
Q

what type are all three of them

A

g protein coupled receptors— inhibits adenylyl cyclase

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6
Q

what is their effect on ion channels

A

post synaptic potassium efflux that causes hyperpolarization
presynaptic calcium influx is inhibited that decreases the release of NT such as glutamate

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7
Q

what is the prototype strong mu receptor agonist?

A

morphine

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8
Q

what is the prototype weak agonist

A

codeine

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9
Q

which points does morphine acts on the mu receptors?

A

CNS
GI TRACT
URINARY TRACT

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10
Q

does morphine acts on the kappa receptor?

A

yes
in the dorsal horn 1 and 2 of the spinal cord

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11
Q

by what other effects does morphine exert its effect by?

A

by inhibiting the release of substance P
also inhibits release of many excitary NT’s

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12
Q

how does morphine produces analgesia?

A

by altering the perception of pain in the brain
by inc pain threshold in the spinal cord

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13
Q

how does morphine produce euphoria?

A

by disinhibiting of dopamine containing neurons in the ventral tegmental area

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14
Q

effect on respiration?

A

resp depression— dec sensitivity to co2 for resp center neurons

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15
Q

how can morphine be used diagnostically?

A

It causes miosis– pinpoint pupil— users of morphine do not develop tolerance to this effect

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16
Q

effect on gi

A

constipation

17
Q

effect on cvs

A

at lower doses– no major effect
at higher doses– dec HR, dec BP

18
Q

which phase of labor does it act on

A

prolong the second phase

19
Q

effect on mast cells

A

histamine release— urticaria, vasodilation
can also cause bronchoconstriction— so with caution in asthma pts

20
Q

effect on hormones

A

growth hormone release is inc
inc ADH— URINARY RETENTION

21
Q

MODE OF ADM

A

AS it has a significant 1st pass— so IV, SC, IM are mostly preferred
orally for extended release

22
Q

metabolites

A

M3G— no analgesic action but neuroexcitary
M6G— 2 to 4 times more potent than morphine —- resp depression

23
Q

adrs ( common with almost all opiods)

A

hypotension
dysphoria
sedation
constipation
urinary retention
resp depression
inc intracranial pressure( with morphine mostly— with caution in pts with head injury)

24
Q

tolerance

A

rep use— tolerance to — resp dep, analgesia, euphoria, sedation

not tolerance to — pinpoint, constipating effects