Term
| opioid receptors, type of channel? activated by? |
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Definition
-Ca and Na ion channels
-endogenous opioid peptides, Capsaicin (spicy food), pH<7, high temperature |
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Term
| endorphins, receptor? channel opened? effect? |
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Definition
mu-opioid receptor
K-channels -> hyperpolarization
supraspinal and spinal analgesia, euphoria, respiratory depression, bradycardia, obstipation, urinary retention, miosis, highly addictive |
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Term
| enkephalins, receptor? effect? |
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Definition
delta-receptor
delta modulates mu-receptor |
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Term
| dynorphines, receptor? channel effected? effects? |
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Definition
kappa-receptor
inhibits Ca channels -> decreased NT release
spinal analgesia, dysphoria, psychomimetic effects, low addiction potential |
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Term
| morphine, receptor? effects? metabolism/t1/2? |
|
Definition
mu-receptor
supraspinal/spinal analgesia, euphoria, respiratory depression, bradycardia, obstipation, urinary retention, miosis,
+itching (Histamine release)
+emesis (DA)
do not need liver for metabolism
t1/2 = 3hrs |
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|
Term
| Piritramid, receptor? effect? potency |
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Definition
mu-receptor
morphine w/ less side effects (less histamine)
analgesic potency = 0.8 |
|
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Term
| codeine, activation? potency? |
|
Definition
metabolized to 10% morphine by P450 3A4
AP = 0.1 |
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Term
|
Definition
P450 2D6 -> mu-agonist (chronic pain)
NaSRI -> chronic pain
central alpha-2 agonist -> decreased NT and inhibits sympathetic NS (clonidine like) |
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|
Term
| pentazocine, receptor? effect? |
|
Definition
kappa-agonist (only one)
weak mu-agonist
spinal analgesia, causes dysphoria, psychomimetic effects |
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Term
| methodone, receptor? onset/t1/2? |
|
Definition
mu-agonist and NMDA antagonist
slow onset 6-8hrs
long t1/2 = 55hrs |
|
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Term
|
Definition
| morphine, alfentanil, fentanyl, remifentanil, sufentanil |
|
|
Term
|
Definition
| i.v. administered opiod, ultrashort t1/2 - need constant infusion |
|
|
Term
| meperidine/pethidin, action? use? t1/2? interactions? |
|
Definition
anticholinergic, SSRI, alpha blocker (vasodilation), medriasis,
postanesthetic shivering
short t1/2
Interaction with MAO-I |
|
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Term
| opiod antagonist? main indication? |
|
Definition
naloxone
respiratory depression |
|
|
Term
| types of therapy for emesis? |
|
Definition
5HT3 blockers, in GI
muscarin blockers, in vestibular nucleus
DA blocker in brain (CRTZ) |
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Term
|
Definition
| 5HT-3 blockers, antiemetic |
|
|
Term
|
Definition
muscarin blocker, antiemetic
transdermal
only treats emesis from motion sickness |
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Term
|
Definition
| D2 antagonist, antiemetic |
|
|
Term
|
Definition
| D2 antagonist, anti-emetic |
|
|
Term
|
Definition
H1 blocker - sedative
antimuscarinic - antiemetic |
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