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BCN EXAM 4 > Opioids Analgesics and Antagonists > Flashcards

Opioids Analgesics and Antagonists Flashcards

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
Q

LA morphine

A

provides sustained serum leves of active morphine
Q8-12 hrs (MS contin)
Q12-24 hrs (Kadian)
Q24 hr(avinza)

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26
Q

LA oxycodone (oxycontin)

A

Q8-12 hrs

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27
Q

Methadone

A

Q6-12 hrs

also has NMDA effect specific for neuropathic pain

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28
Q

Transdermal fentanyl patch

A

Q 48-72hrs

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29
Q

Oxycodone CR (oxycontin)

A

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
Q

what is oxycodone metabolized to

A

oxymorphone, then noroxymorphone and noroxycodone

31
Q

Codeine

A

Used for moderate pain and as an antitussive***
at high doses causes CNS stimulation
max. analgesia = 12-15%that of morphine

32
Q

what is codeine converted to?

A

about 10% of codeine (methylmorphine) to morphine

33
Q

improvements in codeine over morphine

A

less respiratory depression, less dependence and less euphoria than morphine
higher oral efficiency and slower development of tolerance than morphine

34
Q

Tramadol

A

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
Q

tramadol mechanism of action

A

Norepi reuptake blocker

5HT reuptake blocker

36
Q

Tramadol metabolism

A

liver - O methylation, metabolite more potent

half life is six hrs

37
Q

tramadol elimination

A

Renal

38
Q

Hydrocodone

A

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
Q

Pentazocine (Talwin)

A

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
Q

Buprenophine

A

potent, long acting phenanthrene derivation
m partial agonist
mu and delta antagonist

41
Q

Naloxone hydrochloride

A

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
Q

Nalmefene

A

opioid antagonists

43
Q

Naloxone

A

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
Q

Naltrexone (Trexan-Dupont)

A

pure antagonist
orally effective
longer duration of action than naloxone

45
Q

Methylnaltrexone (Relistor)

A

opioid induced constipation in pts with advanced illness having a inadequate response to traditional laxatives

46
Q

Methylnaltrexone (Relistor) contraindications

A

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
Q

Methylnaltrexone (Relistor) contraindicated in patients with …

A

severe renal failure (

48
Q

morphine and naltrexone

A

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
Q

What has been found to help enhance the effects of opioids?

A

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
Q

Buprenorphine pharma

A

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
Q

Buprenorphine (suboxone, subutex)

A

20-50 times potency of morphine
schedule III drug
sublingual
Suboxone - bup an Naloxone (4:1)

52
Q

Sufentanil

A

works on all three opioid receptors

53
Q

Nalbuphine

A

only kappa receptor

54
Q

Contraindications for mu opioid receptors agonists

A

impaired pulmonary function
asthma
hepatic or renal disease
hypotension
Phenothiazines (enhanced respiratory depression, sedation)
Antidepressants (enhanced analgesia)
MAO inhibitors (contraindicated with meperidine)

55
Q

side effects/ toxicity of mu opioid receptor agonists

A 
respiratory depression 
constipation 
N and V
sedation 
euphoria 
peripheral vasodilation 
urinary retention 
spasm- sphincter of oddi 
prutitus 
physical dependance 
tolerance 
miosis
56
Q

signs and symptoms of opium overdose

A 
sedation
confusion 
miosis 
respiratory rate 
hypoxia 
cyanosis
57
Q

Treatment of opium overdose

A

immediate - resuscitation by maintaining airway, oxygen and naloxone and reversal with IV naloxone or another opioid antagonist

58
Q

Naltrexone

A

reduces pleasure from opiates
doesnt seem to reduce cravings
best for motivated pts or pregnant pts

59
Q

adverse effects of chronic opiate use

A 
hypogonadism 
immunosuppression 
increased feeding 
increased growth hormone secretion 
withdrawal effects 
tolerance, dependence
abuse, addiction 
hyperalgesia 
impairment while driving
60
Q

Opioid withdrawal symptoms stage 1 up to 8 hours

A

anxiety and drug craving

61
Q

opioid withdrawal symptoms stage 2 8-24 hours

A

anxiety, insomnia, GI disturbance, rhinorrhea, mydriasis, diaphoresis

62
Q

opioids withdrawal symptoms up to 3 days

A

tachycardia, N&V, hypertension, diarrhea, fever, chills, tremors, seizure, muscle spasms

63
Q

Treatments for opiate dependence

A

methadone
buprenorphine
naltrexone

64
Q

Methadone

A

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
Q

Steps when detoxing

A

wait until opiate withdrawal starts when give first dose (30-60min until effect)
maintanence with 16-24 mg qd
max: 32 mg qd

66
Q

opioids and MAOIs

A

absolute contraindications to meperidine and relative contraindication to other opioids because of high incidence of hyperpyrexic coma

67
Q

opioids and sedative-hypnotics

A

increased CNS depression, particularly respiratory depression

68
Q

opioids and tricyclic anti-depressants

A

increased sedation

variable effects on respiratory depression

69
Q

opioids and antipsychotic drugs

A

increased sedation

variable effects on respiratory depression

70
Q

___________ is used in opiate detox because it has a less severe and shorter duration of withdrawal symptoms compared to ___________

A

Buprenorphine

methadone

71
Q

symptoms last longest with __________ but are less severe than those of __________ withdrawal

A

methadone

heroin

BCN EXAM 4 (8 decks)

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