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Analgesics - Opioids UPDATED
Assessment 6
78
Pharmacology
Graduate
09/26/2011

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Cards

Term
What are the Pure Opiate Agonists?
Definition
Morphine
Term
What are the Partial Agonist Opiates?
Definition
Oxycodone
Term
What are the Opiate Antagonists?
Definition
Naloxone and Naltrexone
Term
What are the NMDA receptor antagonists?
Definition
Dextromethorphan
Term
7.       In determining the type of opioid treatment, what factors should be assessed?
Definition
7.       Pathological mechanisms
Term
13.   Where are pain-modulating neurons found in the midbrain and medulla?
Definition
13.   Periaqueductal Gray area
Term
14.   How pain modulating neurons in the midbrain and medulla control pain?
Definition
14.   Indirectly control pain transmission pathways by enhancing descending inhibition to the dorsal horn
Term
15.   How is Pain relayed to the Brain?
Definition
15.   Noxious Stimulus at periphery àAP à Dorsal Horn à Neurotransmission à CNS neurons à sends signal to Brain.
Term
16.   Where do NSAIDs modulate pain?
Definition
16.   at periphery, initial signal transduction
Term
17.   What blocks signal conduction in nociceptive fibers?
Definition
17.   Na+ channel Blockers
Term
18.   What drugs modulate pain transmission in the spinal cord by decreasing the signal relayed from the periphery to the central pain pathways?
Definition
18.   Opioids
Term
19.   What drugs modulate the central perception of painful stimuli?
Definition
19.   Opioids
Term
20.   What receptors at the periphery are heat-sensitive cation channels?
Definition
20.   TRPV1, TRPV2
Term
21.   What receptors at the periphery are activated by chemical stimuli?
Definition
21.   Acid Sensitive Ion Channels (ASIC)
Term
22.   How does the G protein-coupled receptor enhance ion influx at the periphery?
Definition
22.   Activates Phospholipase C à increases Ca release from intracellular stores à activates PKC
Term
23.   What causes G protein stimulation?
Definition
23.   Sensitizing Agents
Term
24.   How is Pain transmitted to Spinal Cord neurons?
Definition
24.   AP from periphery à activates presynaptic voltage sensitive Ca Channels à Ca influx à Neurotransmitter released à postsynaptic receptors activated à Na and Ca influx in Post synaptic terminal à AP generation
Term
25.   What neurotransmitters are released from the presynaptic terminal?
Definition
25.   Glutamate
Term
26.   What does stimulation of ionotropic glutamate receptors lead to?
Definition
26.   fast postsynaptic depolarization
Term
27.   How does activation of the presynaptic mu receptor inhibit central relaying of nociceptive stimuli?
Definition
27.   decreases Ca influx in response to incoming AP
Term
28.   How does activation of the postsynaptic mu receptors inhibit pain?
Definition
28.   increases K+ conductance of postsynaptic membrane, decreasing the response to excitatory neurotransmission
Term
29.   How is does sensitization to pain occur centrally?
Definition
29.   Primarly through NMDA receptors.
Term
What drug can be used to block the NMDA receptors to prevent surgery-induced sensitization?
Definition
Dextromethorphan
Term
32.   What are the side effects of Dextromethorphan?
Definition
32.   Dizziness
Term
33.   What are ways that pain transmission shows activity-dependent plasticity?
Definition
33.   -Central sensitization
Term
34.   What is Allodynia?
Definition
34.   normally innocuous stimuli are now painful
Term
35.   What is hyperalgesia?
Definition
35.   high intensity stimuli perceived as more painful
Term
36.   How do extra-neuronal inflammatory components induce peripheral sensitization?
Definition
36.   G-protein coupled effects
Term
37.   What are some Extra-neuronal inflammatory components?
Definition
37.   Bradykinin
Term
38.   How do substance P and CGRP (intra-neuronal mechanisms) induce sensitization?
Definition
38.   -stimulate inflammatory cells to release histamine and TNF-alpha
Term
39.   How does Loss of neurotrophic support alter sensitivity and activity of nociceptive fibers?
Definition
39.   Alters gene expression à Na channels become hyper active
Term
41.   Which Opiate receptor type causes decreased respiration?
Definition
41.   Only mu type
Term
42.   Which Opiate receptor has a higher affinity for Enkephalins?
Definition
42.   delta
Term
43.   Which opiate receptors decrease GI transit?
Definition
43.   mu and kappa
Term
44.   Which opiate receptor has a higher affinity for Dynorphins?
Definition
44.   kappa
Term
45.   Which opiate receptor has a higher affinity for Endorphins?
Definition
45.   mu
Term
47.   In the presence of Morphine how does Codeine work?
Definition
47.   acts like an antagonist
Term
48.   Most drugs that have a High 1st pass metabolism, will have what kind of oral:IV potency ratio?
Definition
48.   Low
Term
49.   Comparing Codeine and Oxycodone, which drug has the lowest approx. equivalent dose?
Definition
49.   Oxycodone ( 4.5 mg) < Codeine (30-60mg)
Term
50.   What drugs have a Low Oral:IV potency ratio?
Definition
50.   Morphine
Term
51.   What drugs have a High Oral:IV potency ratio?
Definition
51.   Methadone
Term
52.   What drugs have a Medium Oral:IV Potency Ratio?
Definition
52.   Meperidine
Term
54.   What route of administration is best for a patient with poor GI tract absorption or dysphagia?
Definition
54.   Transdermal
Term
55.   What route of administration would be preferred over a PO opioid for if constipation is an issue?
Definition
55.   Transdermal
Term
56.   What opioid drugs can be administered Rectally?
Definition
56.   Morphine
Term
57.   Why is accumulation of opioids limited in adipose tissue?
Definition
57.   limited blood flow
Term
59.   How do Opiate drugs cause desensitization?
Definition
59.   Drug binds receptoràreceptor slowly pulled into cytoàreceptor slowly put back onto surface if at all
Term
60.   Why don’t endogenous substances cause desensitization?
Definition
60.   after binding are quickly pulled into cyto and quickly returned to the membrane
Term
61.   What side effects of opiates are not effected by developing tolerance?
Definition
61.   Miosis
Term
62.   Why are opiates not a good choice as a long term cough suppressant?
Definition
62.   Likelihood of Tolerance developing is High
Term
63.   What symptoms have a high likelihood of developing tolerance with prolonged opiate use?
Definition
63.   Analgesia
Term
64.   When is there a risk of Respiratory Depression with opiate use?
Definition
64.   –Titrated too rapidly
Term
65.   What drug can be used to reverse the affects of respiratory depression caused by opiate overdose?
Definition
65.   Naloxone
Term
66.   A patient shows up unconscious, with pinpoint pupils, and decreased respiration, what do you suspect?
Definition
66.   Opiate Overdose
Term
67.   What drug decreases baseline beta-endorphin release? What is it used for?
Definition
67.   Naltrexone; decreases alcohol cravings in alcoholics
Term
68.   What are the effects of Sedative-Hypnotics used with Opioids?
Definition
68.   CNS depression – Respiratory Depression
Term
69.   What effects do Antipsychotic tranquilizers and opioids have?
Definition
69.   Increased Sedation
Term
70.   Why are MOA inhibitors and Opioids contraindicated?
Definition
70.   high incidence of hyperpyrexic coma
Term
71.   What does CYP2D6 metabolize codeine to?
Definition
71.   Morphine
Term
72.   What drug is contraindicated for a patient where tachycardia could be a problem?
Definition
72.   Meperidine
Term
73.   Why is Meperidine contraindicated in tachycardia?
Definition
73.   Meperidine has significant antimuscarinic effects
Term
74.   Why is Methadone used to help prevent withdrawal symptoms from Heroin?
Definition
74.   t ½ = 8-59 hrs
Term
75.   What drugs are contraindicated in Renal Failure?
Definition
75.   Meperidine
Term
76.   What drugs lack active metabolites and could be considered in the setting of renal insufficiency?
Definition
76.   Hydromorphone
Term
77.   What is a common approach to management of poorly responsive pain?
Definition
77.   Opioid Rotation
Term
78.   What symptoms can be expected from a patient in Opiate withdrawal?
Definition
78.   Agitation
Term
79.   Are fever, seizures, hallucinations, and delirium associated with opiate withdrawal?
Definition
79.   No, suggests poly-drug withdrawal or associated medical illness
Term
80.   Opiate withdrawal should have Pulse and BP that are what?
Definition
80.   Within Normal Limits
Term
81.   What drug can be used as an outpatient short-term treatment of Opiate withdrawal?
Definition
81.   Clonidine
Term
82.   Why is Naloxone combined with Buprenorphine to treat opioid dependence?
Definition
82.   Naloxone will induce withdrawal in injected. Keeps patients from abusing treatment.
Term
83.   What are some side effects to Methadone maintenance therapy?
Definition
83.   Constipation, mild drowsiness, excess sweating, peripheral edema, Reduced testosterone, Prolonged QT and Arrhythmia
Term
84.   How does Gabapentin treat pain?
Definition
84.   Binds to alpha2-delta subunit, preventing trafficking to cell surface, decreasing the upregulation of voltage-gated Ca channels that occurs in hyper sensitization
Term
85.   What drug is useful in neuropathy, stroke, MS, and phantom limb?
Definition
85.   Lamotigene
Term
86.   How are TCAs useful for Pain?
Definition
86.   NE and 5-HT reuptake blocking properties
Term
87.   Where is the cough pattern generator located?
Definition
87.   Nucleus of Solitary Tract
Term
88.   What is the “Gold Standard” in Antitussive Agents?
Definition
88.   Codeine
Term
89.   What is a nonprescription opiod agonist used as an Antidiarrheal?
Definition
89.   Loperamide
Term
90.   What are some non-drug treatments for Non-Cancer Pain?
Definition
90.   Spinal manipulation
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