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BCN EXAM 4 > Opioids Analgesics and Antagonists > Flashcards

Opioids Analgesics and Antagonists Flashcards

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1
Q

Oxymorphone

A

very similar to morphine but 10 times more potent. it is also more expensive
Post surgical pain relief lasts two to six hours although some clinicians claim it has a slightly shorter duration of action than morphine
lesser tendency to induce vomiting
does not cause histamine release
less depressant effect on the respiratory center

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2
Q

What should be administered with Oxymorphone

A

an Anti Ach to avoid/prevent severe bradycardia

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3
Q

Meperidine mechainsm of action

A

mu opioid receptor in CNS and PNS of the bowels

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4
Q

meperidine clinical effects

A

analgesia - about 1/3 the potency of morphine
post-anesthetic shivering
adverse effects and side effects equivalent to morphine
CNS excitation - normeperidine

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5
Q

Meperidine absorption

A

50% excapes first pass effect after oral admin

BBB - crosses more readily than morphine

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6
Q

Meperidine congeners - Dipheoxylate

A

constipation - treatment of diarrhea

high doses - typical opioid effects

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7
Q

Meperidine congeners - Loperamide

A

Antidiarrheal - slows gastric motility, decreases GI secretion, poor BBB penetration

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8
Q

Fentanyl

A

75 to 200 times more potent than morphine
short duration of action (45-60 minutes)***
minimal CV effects except for bradyarrhythmias
respiratory center depression can be more severe than with morphine and apnea may occur

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9
Q

Alfentanyl

A

new synthetic compound with ultrashort half life

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10
Q

Sufentanyl

A

half life shorter than fentanyl but with fewer side effects

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11
Q

Fentanyl congeners - Sufentanil

A

profile like fentanyl, but 500 to 1000 times more potent than morphine

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12
Q

Fentanyl congeners - Alfentanil

A

~20-30 less than fentanyl

broken down by plasma esterases - 1/2 life is about 8-20 min

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13
Q

Fentanyl congeners - Remifentanil

A

equipotent with fentanyl

metabolized by the liver - 1/2 life is about 1 to 2 hrs

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14
Q

piperidines: therapeutics

A

alfentanil and remifentanil
short, painful procedures
-intense analgesia and suppressing stress response

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15
Q

Absorption of opiates

A

most opiates are rapidly absorbed in the GI tract
undergo a high rate of first pass metabolism
highly lipophilic opiates can be absorbed transdermally

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16
Q

distribution of opiates

A

all opiates bind to plasma proteins at varying affinities

will rapidly leave the blood to concentrate in other body tissues

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17
Q

metabolism of opiates

A

first pass effect
most opiates are converted to more polar metabolites via hepatic conjugation to glucuronides or N-demethylated
6-glucuronide is more potent and the 3-glucuronide is inactive and is the highest concentration metabolite found in the urine.
certain opiates like fentanyl are metabolized by cyto P450

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18
Q

excretion of opiates

A

occurs primarily through the kidneys

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19
Q

morphine metabolism

A

conjugation with glucuronide acid
morphine-6-glucuronide is the active metabolite which is 2x as potent as morphine
First pass effect is significant
about 2 hr half life
most is metabolized and excreted by kidneys

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20
Q

Acute morphine poisoning

A

triad: coma, miosis, cyanosis (affect respiration)
asphyxia, pupils dilate, biliary spasms, GI smooth muscle spasm, pulmonary edema, muscle twitches, peripheral vasodilation, hypotension results in shock
Respiratory failure results in death in 2-4 hours

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21
Q

Oralet

A

intrabuccal fentanyl

administered to kids and adults that are about to undergo a surgical procedure (raspberry flavored :9 )

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22
Q

Actiq

A

used or cancer patients for breakthrough pain (higher dose/ no raspberry flavor)
intrabuccal fentanyl

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23
Q

intrabuccal fentanyl

A

takes effect within 15-20 minutes and lasts ~1-2 hrs

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24
Q

For chronic malignant pain, use this patch

A

fentanyl

duration of action of 72 hours

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25
LA morphine
provides sustained serum leves of active morphine Q8-12 hrs (MS contin) Q12-24 hrs (Kadian) Q24 hr(avinza)
26
LA oxycodone (oxycontin)
Q8-12 hrs
27
Methadone
Q6-12 hrs | also has NMDA effect specific for neuropathic pain
28
Transdermal fentanyl patch
Q 48-72hrs
29
Oxycodone CR (oxycontin)
pure oxycodone inside a polymer/acrylic matrix that allows for controlled release Abusers crush the tablet to destroy the matrix and disable the controlled release
30
what is oxycodone metabolized to
oxymorphone, then noroxymorphone and noroxycodone
31
Codeine
Used for moderate pain and as an antitussive*** at high doses causes CNS stimulation max. analgesia = 12-15%that of morphine
32
what is codeine converted to?
about 10% of codeine (methylmorphine) to morphine
33
improvements in codeine over morphine
less respiratory depression, less dependence and less euphoria than morphine higher oral efficiency and slower development of tolerance than morphine
34
Tramadol
codeine analog weak mu agonist racemic mixture - enantiomers have different acions mild to moderate pain 68% bioavailability oral vs. parenteral N&V, dizziness, sedation and headache seizures
35
tramadol mechanism of action
Norepi reuptake blocker | 5HT reuptake blocker
36
Tramadol metabolism
liver - O methylation, metabolite more potent | half life is six hrs
37
tramadol elimination
Renal
38
Hydrocodone
synthetic drug similar in structure to codeine more potent than codeine comparable to morphine available in combination with other drugs such as NSAIDs and acetaminophen single highest prescribed drug in USA highly abused
39
Pentazocine (Talwin)
1/3 as potent as morphine as analgesic k agonist, and delta partial agonist effective orally, shorter duration and faster onset of action than morphine
40
Buprenophine
potent, long acting phenanthrene derivation m partial agonist mu and delta antagonist
41
Naloxone hydrochloride
reverse the effects of opioids (including analgesia) no agonist properties does not produce respiratory or CV depression. it can be used to reverse the effects (respiratory depression) of any of the opioid agoinst/antagonist group
42
Nalmefene
opioid antagonists
43
Naloxone
antagonizes most opioid receptor agonists high doses antagonize barbiturates almost a pure antagonist used to reverse coma and respiratory depression in opioid overdose (within 30 sec) but short duration of action
44
Naltrexone (Trexan-Dupont)
pure antagonist orally effective longer duration of action than naloxone
45
Methylnaltrexone (Relistor)
opioid induced constipation in pts with advanced illness having a inadequate response to traditional laxatives
46
Methylnaltrexone (Relistor) contraindications
mechanical bowel obstruction stop drug if opioids are discontinued may cause dizziness concomitant use with SSRIs, Li, carbamazepine, or valproic acid may produce additive effects
47
Methylnaltrexone (Relistor) contraindicated in patients with ...
severe renal failure (
48
morphine and naltrexone
extended release opioid with sequestered core of the antagonist, naltrexone, in single dosage form when taken as directed, naltrexone remains sequestered if capsule is tampered with by crushing, chewing or dissolving then naltrexone negates effects of the opioid
49
What has been found to help enhance the effects of opioids?
addition of low doses of opioid antagonists, like naltrexone or naloxone, in combination with opiates, do not inhibit the analgesia effect but enhance it reduce withdrawal syndrome, reversed tolerance and restored potency of opiates
50
Buprenorphine pharma
ceiling effect on respiratory depression less physical dependence capacity blocks withdrawal in mildy dep ppl BUT precipitates withdrawal in mod to severe dep ppl
51
Buprenorphine (suboxone, subutex)
20-50 times potency of morphine schedule III drug sublingual Suboxone - bup an Naloxone (4:1)
52
Sufentanil
works on all three opioid receptors
53
Nalbuphine
only kappa receptor
54
Contraindications for mu opioid receptors agonists
impaired pulmonary function asthma hepatic or renal disease hypotension Phenothiazines (enhanced respiratory depression, sedation) Antidepressants (enhanced analgesia) MAO inhibitors (contraindicated with meperidine)
55
side effects/ toxicity of mu opioid receptor agonists
``` respiratory depression constipation N and V sedation euphoria peripheral vasodilation urinary retention spasm- sphincter of oddi prutitus physical dependance tolerance miosis ```
56
signs and symptoms of opium overdose
``` sedation confusion miosis respiratory rate hypoxia cyanosis ```
57
Treatment of opium overdose
immediate - resuscitation by maintaining airway, oxygen and naloxone and reversal with IV naloxone or another opioid antagonist
58
Naltrexone
reduces pleasure from opiates doesnt seem to reduce cravings best for motivated pts or pregnant pts
59
adverse effects of chronic opiate use
``` hypogonadism immunosuppression increased feeding increased growth hormone secretion withdrawal effects tolerance, dependence abuse, addiction hyperalgesia impairment while driving ```
60
Opioid withdrawal symptoms stage 1 up to 8 hours
anxiety and drug craving
61
opioid withdrawal symptoms stage 2 8-24 hours
anxiety, insomnia, GI disturbance, rhinorrhea, mydriasis, diaphoresis
62
opioids withdrawal symptoms up to 3 days
tachycardia, N&V, hypertension, diarrhea, fever, chills, tremors, seizure, muscle spasms
63
Treatments for opiate dependence
methadone buprenorphine naltrexone
64
Methadone
main action: full opioid agoinst on mu receptor inhibit adenyl cyclase = decreases cAMP increases K channel opening decreases Ca channel opening inhibits serotonin reuptake non competitive antagonist of NMDA receptor
65
Steps when detoxing
wait until opiate withdrawal starts when give first dose (30-60min until effect) maintanence with 16-24 mg qd max: 32 mg qd
66
opioids and MAOIs
absolute contraindications to meperidine and relative contraindication to other opioids because of high incidence of hyperpyrexic coma
67
opioids and sedative-hypnotics
increased CNS depression, particularly respiratory depression
68
opioids and tricyclic anti-depressants
increased sedation | variable effects on respiratory depression
69
opioids and antipsychotic drugs
increased sedation | variable effects on respiratory depression
70
___________ is used in opiate detox because it has a less severe and shorter duration of withdrawal symptoms compared to ___________
Buprenorphine | methadone
71
symptoms last longest with __________ but are less severe than those of __________ withdrawal
methadone | heroin

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