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Opoid
Pharmacology exam 3
65
Pharmacology
Graduate
04/05/2012

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Cards

Term
Where are action potentials conducted to?
Definition

The dorsal horn of the spinal cord

They are generated through a noxious stimulus to the peripheral terminal

Term
T/F: the circuit of transmission of pain impulse contribute to descendong modulatory control? 
Definition
True 
Term
What are chemical stimuli?
Definition

- Acid sensitive ion channels (ASIC)

- ATP-sensitive P2X or P2Y channels 

- Kinin-sensitive B1 or B2 receptors 

Term
What are thermal stimuli: heat sensitive cation channels?
Definition

Transient receptor potential (TRP) vanilloid receptor 1 (TRPV1)

TrP vanilloin-receptor like protein 1 (TRPV2)

Term
Which neurotransmitters are relased presynapticly they interact with postsynaptic receptors and cause postsynaptic depolarization?
Definition
Glutamate, CGRP and Substance P
Term
T/F: Opoids, NE, 5-HT, GABA, released by ascending and/or local-circuit inhibitory neurons, act both presynaptically and postsynaptically to inhibit neurotransmission?
Definition
False, descending 
Term
T/F: The presynaptic inhibition is mediated primarly by enhanced chloride influx and potassium efflux?
Definition

False, this is the definition for postsynaptic inhibition 

Presynaptic inhibition is mediated through reduced activity of voltage sensitive calcium channels 

Term
What happens in postsynaptic inhibition, secondary relay neuron?
Definition
We will have increase conductance of Cl- (in) and K+ (out) which leads to postsynaptic hyperpolarization, decrease voltage gated Na+ channels reaching threshold. This will decrease action potential generation 
Term
The descending projections of NE from brainstem to spinal cord activate alfa2-adrenergic receptor, G-protein coupled and cause?
Definition

- Inhibits presynaptic Ca-channels

- Reduce presynaptic cesicle release

- Opens postsynaptic potassium channels

- Membrane hyperpolarization 

Term
T/F: Activation of 5HT ligand-gated channel in the spinal cord is excitatory?
Definition
True 
Term
T/F: 5-HT G-protein-coupled receptors mediate inhibitory action of serotonin?
Definition
True 
Term
How does tramadol act?
Definition
Acts through inhibiting NE/5-HT reuptake 
Term
T/F: Duloxetine (NE/5-HT reuptake inhibitor) has analgesic activity?
Definition
True 
Term
Difference in pharmacologic effect of opoid receptor (mu, delta, kappa)
Definition

- mu has supraspinal analgesia effect while delta and kappa don't

- mu also has euphoria effect while delta and kappa don't

- kappa is only receptor that has dysphoria effect

- Physical dependence is seen more w/ mu receptor, seen with kappa not delta

- Delta does not have peripheral analgesia, sedation, and pupil constriction

- All have reduced GI motility (mu>delta>kappa)

- Kappa does not have respiratory depression 

 

Term
T/F: Endogenous opoids are released by interneurons in the dorsal horn in response to severe/ persistent pain?
Definition
True, opids bind to G proteins associated w/ mu-type opoid receptors 
Term
What opiate-like peptides are contained in Pro-orphanin (larger precursor)?
Definition
Nociceptin or orphanin, FQ 
Term
What opiate-like peptides are contined in Pro-dynorphin?
Definition
Endorphins, enkephlins and dynorphins 
Term
what opiate-like peptides are contained in Pro-opiomelanocortin?
Definition
Endorphins & enkephlins 
Term
T/F: opiates are drugs derived from opium, and they include morphine, codeine, and thebaine, and many semisynthetic derivatives?
Definition
True 
Term
What are endogenous opoid peptides?
Definition
They are naturally occuring ligands for opoid receptors 
Term
What are semi-synthetic opoids?
Definition

- Hydromorphone (dilaudid)

- Oxymorphone (opana)

Hydrocodone (vicoden)

- Oxycodone (percodan, oxycontin)

Term
What are synthetic opoids?
Definition

- Meperidine (demerol)

- Methadone (dolphine)

- Propoxyphene (darvon)

- Levorphanol

Term
What are pure opoid antagonists?
Definition

- Naloxone

- Naltrexone 

- Nalmefine

Term
What are patiel opoid agonists?
Definition

- Pentazocine

- Buprenorphine

- Butorphanol

- Nalbuphine 

Term
Which opoid agonist act on both mu and kappa (lower activity) receptors?
Definition
Morphine 
Term
Which which patial agonist opoid has only activity on mu receptor?
Definition
Buprenorphine 
Term
Which patial agonist has only activity on kappa receptor?
Definition
Nalbuphine 
Term
T/F: analgesis occurs with loss of consciousness?
Definition
False, without 
Term
T/F: nociceptive pain is responsive to opoid unlike neuropathic pain which respond poorly?
Definition
True 
Term
What is the analgesic MOA of opoids?
Definition
Opoids directly inhibit ascending transmission of nociceptive information from the spinal cord and activate pain control circuits that descend from the midbrain to the spinal cord dorsal horn
Term
T/F: in the presynaptic terminal, mu-opoid receptor activation decreases ca2+ influx in response to an incoming action potential?
Definition
True 
Term
Post-synaptoc mu-opoid receptor activation increases K+ conductance and therby decreases the postsynaptic response to excitatory neurotransmission?
Definition
True 
Term
Which medications have no analgesia effect?
Definition

-  Dextromethorphan

- Diphenoxylate

- Loperamide

- Naloxone

- Naltrexone 

Term
T/F: Codeine has an exceptionally high affinity for opoid receptors, and the analgesic activity is due to its conversion to morphine by CYP2D6?
Definition

False, low affinity 

Analgesia is affected by possible metabolic enzyme polymorphism 

Term
T/F: Tramadol, a synthetic codeine derivative is a weak mu-opoid receptor agonist?
Definition
True 
Term
What is the mechanism of analgesia of tramadol?
Definition
inhibition of uptake of NE and serotonin 
Term
T/F: Propoxyphene binds to mu-opoid receptors, but more selective than morphine?
Definition
False, less selective 
Term
T/F: The mixed agonists/antagonists exert analgesic action by acting as agonist at kappa receptors?
Definition
True 
Term
T/F: Mechanisms of drug-induced reward involve interactions between opoids and dopamine in the nucleus accumbens?
Definition
True 
Term
T/F: Selective mu and delta agonists produce positive motivational effects by decreasing dopamine release?
Definition
False, by increasing dopamine release
Term
T/F: selective kappa receptor agonists produce aversive effects by inhibiting dopamine release?
Definition
True 
Term
T/F: When equianalgesic doses are used, there is no difference between morphine and morphine-like opoids in regards to respiratory depression?
Definition
True 
Term
What are CNS effect of opoids?
Definition

Sedation, drowsiness, and mental clouding

Emetic effects: N/V are due to direct stimulation of CTZ and high doses depress comting center 

Antitussive: direct action on medulla cough center to suppress cough reflex

Miosis: (pin point pupils)

Muscle rigidity-due to increased tone to spinal motor neurons at high dose

Convulsion at high doses 

Term
What are alternative route of administration of morphine, used to maximize benefit and minimize SE?
Definition
PCA (pts controlled analgesia), epidural, transdermal, transmucosal and intra-articular 
Term
T/F: morphine-6-glucuronide is 4-6 times more potent than morphine and may contribute significantly to analgesia?
Definition
True 
Term
T/F: Morphine-3-glucuronide lack analgesic effect but can cause dysphoric SE or seizures?
Definition
True 
Term
What are acute toxicity symptoms of morphine?
Definition

Triad coma, pinpoint pupils, respiratory depression

Tx: IV naloxone (opoid antagonist) (may precipitate withdrawal symp)

Term
What are DI with morphine?
Definition

- MAOIs, phenothiazines, tricyclic antidepressants, alcohol (exaggerated CNS depressant effect)

- Tranquilizers, sedative-hypnotics, alcohol (general anethetics)-Increase respiratory depression

- Amphetamine (small dose) enhance analgesic and euphorant effects of morphine

- antideppressant and aspirin enhance analgesia

Term
What are morphine contraindications?
Definition
Bronchial astham, emphysema, liver damage, head injuries, acute alcohol use, previous dependence, convulsive disorders, abd pain unknown origin
Term
What are the differences between morphine and meperidine?
Definition

Meperidine has faster onset, shorter duration of action 

- No antitussive activity w/ meperidine 

- Less constipation 

- Increased CNS excitability and seizures (due to toxic metabolite normeperidine-long t1/2, & pts w/ chronic kidney dz)

- Mydriasis rather than miosis 

Term
What are DI with meperidine?
Definition

Serotonin syndrome with MAOIa

Chlorpromazine-enhanced respiratory depression and sedation

Promethazine-enhanced sedation

Amphetamine-enhanced analagesic while counteracting sedation 

Term
T/F: sufentanil is 10-15 * more potent than fentanyl?
Definition
True 
Term
Which fentanyl subgroup has ultra short duration and rapid metabolism by esterases?
Definition
Remifentanil 
Term
Opoids for diarrhea
Definition

Diphenoxylate: derivative of meperidine, combined w/ atropine (lomotil)

Loperamide (imodium): derivative of diphenoxylate, effective antidiarrheal with little abuse potential

Term
What are differenced between methadone and morphine?
Definition

Methadone: has extended duration of action, slow onset and long t1/2, tolerance develops more slowly, withdrawal syndrome develop slowly and is mild, used for tx of opoid abuse

Hepatic dysfunction associated wth overdose-respiratory depression, and rarely QT prolongation

Term
Which synthetic opoid overdose causes toxic psychosis (involved increasing incidence of deaths, mostly suicides)?
Definition
Propoxyphene (only PO available)
Term
Which synthetis opoid is contraindicated in pts w/ hx of epilepsy?
Definition

Tramadol (risk of seizures)

no report of respiratory depression or cardiovascular toxicity

inhibits NE and 5HT reuptake 

not strictly an opoid analgesic 

Term
T/F: degree of physical dependance of opoids is related to the amount, frequency and duration of drug use?
Definition
True 
Term
Withdrawal syndrome intensity with opoids is inversely related to t1/2?
Definition
True, shorter t1/2 more intense the symptoms (Fentanyl)
Term
What are symptoms of withdrawal?
Definition
Anxiety and dysphoria, vraving and drug seeking behavior, sleep disturbance, N/V, lacrimation, rhinorrhea, yawning, sweating, diarrhea, mydriasis, abd cramping, hyperpyrexia, tachycardia and HTN 
Term
Which opoid has no antitussive effect?
Definition
Meperidine, diphenoxylate, loperamide propoxyphene (o to low)
Term
Which opoids have the least constipation effect?
Definition

Meperidine, propoxyphene and tramadol

Dextromethorphan has none 

Term
which opoid has the most analgesic effect?
Definition
Oxycodone 
Term
Which mixed apoid agonist-antagonist has antitussive effect?
Definition
Buprenorphine, all other have zero effect 
Term
Which opoids has no alangesic effect?
Definition
Dextromethorphan, diphenoxylate and loperamide 
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