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Neuro Narcotics: Analgesics and Antagonists
Neuro Narcotics: Analgesics and Antagonists
34
Medical
Professional
01/31/2011

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Term
Opiate receptors are abundant at... (5)
Definition
Dorsal horn of spinal cord
Periaqueductal greay
Rostral ventral medulla
Thalamic nuclei
Peripheral tissues
Term
Opiate receptor: properties (4)
Definition
Structural and sterospecificity (L-isomer)
Subject to competition between and reversal of agonists and antagonists
Binding affinity correlated with efficacy
G-protein
Term
Mu-R binds _(3)_ and causes _(3)_ at Mu-1 and _(4)_ at Mu-2
Definition
Morphine
Synthetic opioids
Endorphins

Mu-1
Supraspinal analgesia
Euphoria
Miosis

Mu-2
Spinal analgesia
Respiratory depression
Physical dependence
Constipation
Term
Kappa-R binds ___ and causes ___ (3)
Definition
Dynorphins

Spinal and supraspinal analgesia
Miosis
Sedation
Term
Delta-R binds ___ and causes ___ (2)
Definition
Enkephalins

Spinal analgesia
Modulation of Mu-R
Term
Which receptors are responsible for supraspinal analgesia and miosis? (2)
Definition
Mu-1
Kappa
Term
Endorphins: molecular origin, locations (3), cause for release
Definition
Pro-opiomelanocortin
Pituitary, hypothalamus, 3rd and 4th ventricles
Painful episodes: released into CSF
Term
Dynorphins: molecular origin, properties, location
Definition
Prodynorphin
Like enkephalins
CNS pain pathway nerve endings
Term
Enkphalins: molecular origin, locations, purpose
Definition
Proenkephalin
CNS areas that perceive pain
Regulate NT release = inhibit transmission of painful stimuli
Term
Opiopeptins: properties (4)
Definition
High affinity for opiateR
Exhibits cross-tolerance with narcotic agonists
Chronic use produces dependence
Binding reversed by narcotic antagonists, which can cause withdrawal
Term
Oral absorption is usually ___ and variable due to ___.
Definition
Poor
First-pass metab and glucuronidation
Term
___ administration is usually complete, and ___ and ___ administrations are usually effective
Definition
IM
Transdermal and epidural
Term
Distribution to tissues is based on ___. CNS levels depend on _(4)_
Definition
Blood flow

BBB
Lipid solubility
Protein binding
Hepatic conjugation with glucuronic acid
Term
Opiate elimination (2)
Definition
Water soluble metabolites excreted in urine
Glucuronide conjugates excreted in bile
Term
Opiates: MOA (2)
Definition
1. Presynaptic agonist = decreased Ca influx = decreased excitatory NT release
2. Postsynaptic agonist = increased K conductance = hyperpol and decreased responsiveness
Term
Opiates: CNS effects (3)
Definition
Analgesia
-Interact with Mu and Kappa receptors: inhibit nociception at spinal and supraspinal sites = increased threshold for pain perception and diminished reaction to pain (even though still perceived)
-Better for continuous dull pain that intermittent sharp pain
Sedation (due to decreased anxiety?)
Euphoria or detached/floating sensation
Term
Opiates: respiratory effects
Definition
Decrease sensitivity of respiratory chemoR to CO2
Directly decrease respiratory rhythm

Both cause dose-dependent decreased rate, minute volume, tidal exchange
Term
Opiates: other central effects (4)
Definition
Cough suppression (direct depression of medullary cough center)
Miosis (increased parasymp activity)
Truncal rigidity (increased descending motor impulses)
n/v (direct stim of chemoR in medullary area postrema)
Term
Opiates: peripheral effects (3)
Definition
Mostly Mu-mediated

Histamine release: flushing, itching, hypotension
Orthostatic hypotension (morphine)
Increased smooth muscle tone
-Intestines: along with decreased propulsion
-Biliary tract: increased biliary pressure
-Urinary tract: retention
Term
Solely Mu agonist drugs (2)
Definition
Fentanyl
Methadone
Term
Agonist for all 3 opiateR
Definition
Morphine
Term
Antagonist for all 3 opiateR
Definition
Naloxone
Term
Mu partial agonist and Kappa agonist (3)
Definition
Butorphanol
Nalbuphine

Buprenorphine = only Mu
Term
With repeated admin, tolerance can develop over ___
Definition
1-3 wks
Term
Tolerance is gained to all effects except... (3)
Definition
Miosis
Constipation
Convulsions
Term
Cross tolerance to all opiates occurs and includes tolerance to _(4)_ effects
Definition
Analgesia
Euphoria
Sedation
Respiratory depression
Term
Less tolerance is gained to ___
Definition
Partial agonist/antagonists
Term
Tolerance: MOA
Definition
Decreased receptor-ion channel coupling
Term
Dependence: MOA
Definition
Without the depressive effects of the agonist binding to the receptor, the affected processes become hyperexcitable = withdrawal
Term
Think twice about giving opiates to these patients (4)
Definition
Pulmonary disease
Hepatic dysfunction
Head injury without assisted ventilation
Pancreatitis
Term
Opiate toxicity: S/E (3), tx (2)
Definition
Triad
-Depressed respiration
-Pinpoint pupils
-Coma

Airway, see to the CNS depression or excitation
Narcotic antagonist
Term
Naltrexone is a pure ___, is ___ than naloxone, and can be ___
Definition
Antagonist at opiateR
Longer-acting
Orally administered
Term
Buprenorphine: indication
Definition
Decrease opiate craving (Mu-R partial agonist with long t1/2)
Term
Full antagonists can be used to reverse the respiratory/CNS effects as well as ___, but the problem is that ___
Definition
Orally to decrease craving and maintain sobriety

It can reverse all the beneficial effects of the agonist including the analgesia
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