Receptor Mechanisms
All three opioid receptors are ______ at the cellular level.
What is inhibitory?
Full agonists have no ______ effect compared to partial agonists.
What is ceiling effect?
Protein binding and this property influence opioid distribution.
What is lipophilicity?
Common heart rate effect of opioids.
What is bradycardia?
Most common side effect of neuraxial opioids.
What is pruritis?
Receptor signaling is mediated through this protein system.
What are G-proteins?
Drug class (other than antagonists) that can precipitate withdrawal when combined with full agonists.
What are partial agonists?
Lipid-soluble opioids tend to accumulate here.
What is adipose tissue?
Histamine release can cause this blood pressure effect.
What is hypotension?
Neuraxial opioids may cause this beneficial or problematic CNS effect.
What is sedation?
Opioid binding leads to inhibition of this intracellular messenger.
What is cAMP?
Name one mixed agonist-antagonist drug.
What is pentazocine / butorphanol / nalbuphine / buprenorphine?
Primary organ of opioid metabolism.
What is the liver?
Opioids can cause this positional cardiovascular effect.
What is orthostatic hypotension?
The most serious neuraxial side effect due to brainstem depression.
What is depression of ventilation (respiratory depression)?
Resulting neuronal membrane state maintained by opioid receptor activity.
What is hyperpolarization?
Buprenorphine is a partial mu agonist and ______ antagonist.
What is kappa antagonist?
Primary organ of opioid excretion.
What are the kidneys?
Opioid effect on bladder sphincter tone.
What is increased tone leading to retention?
Region stimulated by neuraxial opioids causing nausea/vomiting is located in this region of the brainstem.
What is the floor of the fourth ventricle?
Neurotransmitter release inhibited by opioids (name one).
What is acetylcholine / glutamate / CGRP / substance P?
Mixed agonist-antagonists are limited clinically due to this side effect.
What is dysphoria?
Term for increased half-life after prolonged infusion due to redistribution.
What is context-sensitive half-time?
Opioid-induced release of this hormone causes urinary retention.
What is antidiuretic hormone (ADH)?
This region of the spinal cord, with two separate names, is especially dense with opioid receptors and serves as a key site of action for neuraxial opioid analgesia.
What is the substantia gelatinosa of the dorsal horn (Rexed laminae II)?