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JT- PHARM > Opioids 5-5 > Flashcards

Opioids 5-5 Flashcards

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1
Q

What is Alfentanil useful for?

A

Alfentanil is useful for acute, but transient noxious stimuli such as laryngoscopy with tracheal intubation or retrobulbar blocks.

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2
Q

What is the dosing regimen for Alfentanil?

A

150-300 mcg/kg produces induction in about 45 seconds.

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3
Q

What is the continuous infusion range for Remifentanil?

A

25-150 mcg/kg/hr continuous infusion along with inhaled gas.

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4
Q

How does Remifentanil’s potency compare to fentanyl?

A

Remifentanil’s potency is similar to fentanyl but blood brain equilibration similar to alfentanil

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5
Q

What is the metabolism and excretion of Remifentanil

A
  • Metabolism is independent of renal or hepatic function, hydrolysis by non-specific plasma and tissue esterases to inactive metabolites.
  • excretion is via kidneys.
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6
Q

What is characteristics of Remifentanil?

A
  • Ultrashort duration *
  • Rapid onset and offset *
  • No cumulative effects *
  • Rapid recovery after discontinuation
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7
Q

What happens to clearance of Remifentanil during hypothermic cardiopulmonary bypass?

A

Hypothermic cardiopulmonary bypass decreases clearance by 20% due to effect of temperature on esterase activity

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8
Q

What are the distribution and elimination half-lives of Remifentanil?

A

Distribution half-life is 0.9 minutes and elimination half-life is 6.3 minutes.

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9
Q

In what cases is Remifentanil useful?

A

Useful for transient acute noxious stimuli such as laryngoscopy with tracheal intubation or retrobulbar blocks; also in cases where neurological assessment is necessary.

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10
Q

How should Remifentanil be administered?

A

It should be pushed slowly for beneficial effects.

Fast administration of adenosine or giopreza is required.

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11
Q

What is the dosing for Remifentanil?

A
  • 1 mcg/kg over 60-90 seconds
  • or as part of balanced anesthesia at 0.25-1 mcg/kg or 0.05-2 mcg/kg/min titrated to desired effect.
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12
Q

What should be done at the end of a Remifentanil infusion?

A

A longer-acting opioid may be administered to ensure analgesia at emergence.

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13
Q

Why should Remifentanil not be given by neuraxial route?

A

Due to unknown effects of the vehicle (glycine).

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14
Q

What are the side effects of Remifentanil?

A
  • Increased risk of skeletal muscle rigidity with rapid IV injection,
  • nausea/vomiting,
  • ventilatory depression.
  • Depressed sympathetic tone (decreased blood pressure and heart rate)
  • No histamine release and no effect on ICP or IOP
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15
Q

What is CYP3A4?

A

CYP3A4 is a super metabolizer of codeine to morphine, leading to a buzz from codeine.

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16
Q

What is codeine?

A

Codeine is a methyl-substituted derivative of morphine, which limits first pass hepatic metabolism, making it a good oral option for mild to moderate pain.

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17
Q

What is the half-life of codeine?

A

The half-life of codeine is 3-3.5 hours when given orally or intramuscularly.

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18
Q

How is codeine metabolized?

A

10% of the dose of codeine is demethylated in the liver to morphine.
Codeine is also demethylated into norcodeine (inactive metabolite), which are further conjugated and excreted via kidneys.

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19
Q

What is the dosing for codeine?

A
  • Antitussive—15 mg
  • Analgesic—60 mg
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20
Q

How does 120 mg of codeine IM compare to morphine?

A

120 mg of codeine IM is equivalent to 10 mg of morphine.

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21
Q

How is codeine usually administered for pain?

A

Codeine is usually combined with a non-opioid analgesic for mild to moderate pain.

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22
Q

What is the physical dependence of Codeine compared to morphine?

A

Codeine has less physical dependence compared to morphine.

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23
Q

What are the side effects of Codeine?

A

Codeine causes minimal sedation, nausea/vomiting, and constipation; even at high doses, it is unlikely to cause ventilatory depression.

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24
Q

What can IV administration of Codeine cause?

A

IV administration can cause significant histamine release with resultant hypotension.

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25
How does Dextromethorphan compare to Codeine as an antitussive?
Dextromethorphan has equal potency to codeine as an antitussive but lacks analgesic or physical dependence liability.
26
Compare hydromorphone to morphine?
* Hydromorphone is 8 times more potent than morphine, but has a slightly shorter duration. * Hydromorphone is more sedative with less euphoria in comparison to morphine. * Hydromorphone has no active metabolite and much less histamine release than morphine.
27
28
What is Methadone?
A synthetic opioid agonist complete oral absorption and prolonged duration make methadone ideal for treatment of withdrawal from other opioids.
29
What is the half-life of Methadone?
35 hours.
30
How is Methadone metabolized?
Metabolized in the liver to inactive metabolites and excreted in both urine and bile.
31
How is methadone compared to morphone?
Side effect: similar to morphine, however less sedation and euphoria Less miosis than morphine too. Addicts develop complete tolrance to this effect.
32
Brand name for propoxyphene?
Darvon / Darvocet
33
What kinda of pain does propoxyphene treat?
mild to moderate pain
34
How is propoxyphene metabolized?
–Completely absorbed after oral administration –Extensive first pass hepatic metabolism via demethylation to norpropoxyphene
35
What is Propoxyphene chemically similar to?
Methadone.
36
What is the half-life of Propoxyphene?
14.5 hours.
37
What are the side effects of Propoxyphene?
* Vertigo * sedation * nausea/vomiting * seizure * ventilatory depression
38
What is the potency of Propoxyphene compared to codeine?
1/3 the potency of codeine.
39
What is the risk associated with IV administration of Propoxyphene?
It can cause damage to vessels, so is not advised.
40
What is Heroin also known as?
Diacetylmorphine.
41
How does Heroin penetrate the brain?
Rapidly, where it is hydrolyzed to active metabolites (monoacetylmorphine and morphine).
42
How does the onset of Heroin compare to morphine?
More rapid onset than morphine with less nausea.
43
What is the risk associated with Heroin use?
Much greater possibility of physical dependence.
44
What is Tramadol (Ultram)?
* A central acting analgesic with low affinity for mu receptors; * it also inhibits reuptake of norepinephrine/serotonin and facilitates release of serotonin.
45
What is the dosing for Tramadol?
50-100 mg po q4-6 hours, not to exceed 400 mg/day.
46
What are the drawbacks of Tramadol?
Insufficient sedative effect and increased nausea and vomiting potential.
47
Why is Tramadol better for chronic pain?
Because it has no tolerance or addiction risk.
48
What serious side effect can Tramadol cause?
It can cause seizures, especially in combination with other antidepressants.
49
What are the advantages of opioid agonist/antagonist (mixed)?
* Produce analgesia, * limited ventilatory depression, * low potential for physical dependence, * ceiling effect (increasing dose does not increase efficacy).
50
What is Butorphanol (Stadol)?
An opioid agonist/antagonist that is twenty times more potent than pentazocine as an agonist and 10-30 times more potent as an antagonist.
51
What are the properties of Butorphanol?
* Low mu antagonist activity, kappa analgesia, anti-shivering properties * minimal sigma receptor activity which decreases dysphoria.
52
How can Butorphanol be administered?
Parenterally or intranasally, though abuse seems to be higher with intranasal administration.
53
What is the dosing equivalence of Butorphanol?
2-3 mg IM is equivalent to 10 mg morphine.
54
What is the half-life of Butorphanol?
2.5-3.5 hours.
55
How is Butorphanol metabolized and excreted?
Metabolized to hydroxybutorphanol (inactive); excreted primarily via bile with a small portion undergoing renal clearance.
56
What are the side effects of Butorphanol?
* Sedation * nausea * diaphoresis * less dysphoria than morphine, ventilatory depression similar to morphine * **increased** heart rate and blood pressure secondary to **catecholamine release**
57
Compare Nalbuphine and morphine and nalorphine?
Analgesic potency equal to morphine; Onset and duration similar to morphine Sedation is common but dysphoria is less than with morphine. ¼ as potent as nalorphine as antagonist
58
Half life of nalbuphine
3-6 hours
59
How is nalbuphine metabolized?
In liver
60
When nalbuphine start showing risk of ventilatory depression?
dose above 30 mg
61
How about effects on BP and HR of nalbuphine?
no effects.
62
What is Nalbuphine known for?
Nalbuphine has a low abuse potential and acts as an antagonist at mu receptors, which may prevent analgesia from subsequent morphine use.
63
What is the recommended dosage of Nalbuphine post-operatively?
10-20 mg IV post-operatively prevents ventilatory depression while providing analgesia.
64
What is Buprenorphine derived from?
Buprenorphine is derived from thebaine.
65
How does Buprenorphine compare to morphine in terms of potency?
0.3 mg of Buprenorphine is equivalent to 10 mg of morphine.
66
What is the onset and duration of Buprenorphine when administered IM?
IM onset is 30 minutes with a duration of 8 hours.
67
What is the affinity of Buprenorphine for mu receptors compared to morphine?
Buprenorphine has 50 times more affinity for mu receptors than morphine.
68
How is Buprenorphine excreted from the body?
Two-thirds is excreted unchanged in bile and the remainder in urine as inactive metabolites.
69
What is a notable characteristic of Buprenorphine's lipid solubility?
Buprenorphine is 5 times more lipid soluble than morphine in the epidural space.
70
What are some side effects of Buprenorphine?
Side effects include drowsiness, nausea/vomiting, ventilatory depression (may be resistant to naloxone), and less dysphoria than morphine.
71
How does physical dependence on Buprenorphine compare to morphine?
Physical dependence on Buprenorphine is slow and less intense than with morphine.
72
What is the risk of abuse associated with Buprenorphine?
The risk of abuse is low, and it is now being used for outpatient detoxification programs in place of methadone.
73
What are opioid antagonists?
Opioid antagonists involve the substitution of an alkyl group for a methyl group.
74
What does Naloxone treat?
* Treats ventilatory depression in post-op period, * treats ventilatory depression in neonate born to mothers where opioids have been administered, * treats opioid overdose, and detect suspected physical dependence
75
What is the duration of action for Naloxone?
30-45 minutes
76
How is Naloxone metabolized?
Liver metabolized with glucuronic acid to form naloxone-3-glucuronide
77
Is Naloxone available orally?
Yes, but it has 1/5 potency of parenteral administration.
78
What are the side effects of Naloxone?
Reversal of analgesia (titrated to reverse ventilatory depression) nausea/vomiting related to speed of injection (slower is better) increased sympathetic tone
79
What is Naltrexone (Revia)?
Highly effective orally and may produce antagonism up to 24 hours.
80
What is Nalmefene?
A 6-methylene analog of naltrexone, equivalent to naloxone.
81
Dose of nalmefene?
Dosing: 0.25 mg/kg iv over 2-5 minutes until desired effect, not to exceed 1 mg/kg.
82
What is the duration of action for Nalmefene?
Longer duration of action (8 hours).
83
How is Nalmefene metabolized?
Metabolized via hepatic conjugation with <5% excreted unchanged in urine.
84
What is Methylnaltrexone?
A quaternary antagonist (highly ionized) that limits transfer across the blood-brain barrier.
85
What is the action of Methylnaltrexone?
It has a peripheral action that decreases the effects of morphine on gastric emptying and nausea.
86
What is Methylnaltrexone (Relistor) indicated for?
Indicated for the treatment of opioid-induced constipation associated with chronic non-cancer pain and in advanced illness. ## Footnote Not known if safe and effective for longer than 4 months.
87
What is Alvimopan (Entereg) indicated for?
Indicated for peri-operative return of bowel function after partial small bowel resection with primary anastomosis. ## Footnote Caution in patients who have used opioids in the days prior to surgery due to increased risk of myocardial infarction.
88
What is Naloxegol (Movantik) indicated for?
Indicated for the treatment of opioid-induced constipation.

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