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931 Block 3 > Opioids > Flashcards

Opioids Flashcards

1
Q

What are the 3 endogenous opioids?

A

Endorphins (met-enkephalin)
Enkephalines (leu- and met-enkephalin)
Dynorphins (leu-enkaphalin)

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2
Q

Where are opioid receptors located?

A

Brain, Spinal cord, and Enteric nervous system

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3
Q

How do we classify opioids?

A

By source and structure.

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4
Q

What are the structures of opioids?

A

Phenanthrenes
Phenylpiperidines
Diphenylheptane

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5
Q

What are the 3 receptors that opioids target?

A

Mu, delta, and kappa

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6
Q

What are the 4 effects morphine has in the CNS?

A

Euphoria, drive satiety, sedation, and analgesia.

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7
Q

Does morphine increase or decrease the respiratory system? How does it work?

A

Morphine causes respiratory depression. It depresses the neurogenic drive in the medulla and decreases the response to increased CO2.

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8
Q

What is the main cause of overdose death in morphine?

A

Respiratory depression

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9
Q

What isomers of opioids provide cough suppression? Which isomers provide analgesic activity?

A

d-isomers provide cough suppression (codeine, hydrocodone, dextromethorphan)

Levo-isomers provide analgesic effects.

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10
Q

Do d-isomers cause respiratory depression, analagesia, tolerance, or drowsiness?

A

No

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11
Q

What are morphin’s effects on N/V?

A

Initially morphine stimulates emesis, but inhibits it later on. Occurs in the medulla

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12
Q

What is morphine’s effect on the heart?

A

Morphine decreases CO, not HR, by decreasing the left ventricular diastolic pressure.

You use morphine-type opioids for acute pulmonary edema and CHF.

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13
Q

What is morphine’s effect on smooth muscle?

A

It increases smooth muscle tone, even in the GI tract. This leads to constipation. It also causes the sphincter of oddi to contract and not allow the secretion of bile.

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14
Q

Should we use opioids in acute lower back pain or chronic lower back pain?

A

Neither!

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15
Q

What step in the WHO 3-step analgesic ladder do you give opioids?

A

Step 2 and 3

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16
Q

In what type of pain do we use morphine?

A

Severe and/or chronic pain.

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17
Q

Does codeine have better absorption than morphine?

A

Yes

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18
Q

What are the two main uses of codeine?

A

Mild-mod. pain (analgesic)

Antitussive

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19
Q

What metabolizes codeine?

A

CYP2D6. Codeine needs to be metabolized to be active.

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20
Q

What needs to be deacetylated to become morphine?

A

Heroin (quicker actions than morphine)

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21
Q

How is hydrocodone metabolized?

A

CYP2D6 does o-demethylation to form hydromorphone.

CYP34A does N-demethylation to form norhydrocodone.

22
Q

What is the most prescribed drug in the US?

A

Hydrocodone

23
Q

How was oxycontin reformulated to make it less abused?

A

It now becomes more gummy when wet because of the extra binders they added. This makes it difficult to snort.

24
Q

What is oxymorphone’s oral bioavailability? How is it improved?

A

10% when taken oral.

If you take with food it increases it to 38-50%.

25
Q

What happens to a person that crushes oxymorphone tablets and tries to inject it IV?

A

When injected IV, crushed oxymorphone can produce thrombotic thrombocytopenia purpura. This is when small blood clots occur in small veins and can produce kidney failure and death.

26
Q

How does methadone work?

A

Methadone does every thing morphone does, but also inhibits NMDA receptors.

27
Q

What are methadone’s uses?

A

Analgesia
Opioid detox
Opioid maintenance therapy

28
Q

Why is methadone used for opioid maintenance?

A

It has a long half-life. It can site on the receptors to prevent other opioids from binding and prevents withdrawal.

29
Q

How much more potent is fentanyl than morphine?

A

75-100X more potent.

30
Q

How long is fentanyl’s duration of action? Why?

A

It’s about 30 minutes. This is because it redistributes out of the brain.

31
Q

What are the different forms of fentanyl? Why can it come in many different dosage forms?

A

Injection, patch, lozenge, and buccal tablet.

Fentanyl has a low MW, high potency, and it is lipophilic.

32
Q

Is meperidine more or less potent than morphine?

A

Meperidine is less potent than morphine.

33
Q

What is so bad about meperidine?

A

If used chronically in high doses the active metabolite (normeperidine) will accumulate in the CNS and cause MPTP to form a into MPP+, a free radical that affects dopamine release.

34
Q

What is an adverse effect in partial kappa agonist, partial mu antagonist that doesn’t occur in pure mu agonists?

A

Psychotomimesis

35
Q

What are some benefits in using partial kappa agonist, partial mu antagonist over a pure mu agonist?

A

Respiratory depression plateaus, less smooth muscle contraction, and dependence potential is less.

36
Q

What are there shared system REMS for?

A

Extended-release and long-acting opioid analgesics in the treatment of mod. to severe chronic pain.

Transmucosal immediate-release fentanyl

Buprenorphine transmucosal products for opioid dependence

37
Q

What did the American Academy of Neurology Position Statement on Opioids in non-cancer pain say?

A

Don’t use opioids in HA, fibromyalgia, and chronic low back pain because the risks outweigh the benefits.

38
Q

What are 3 factors that effect opioid’s response?

A

Genetics
Age
Sex

39
Q

What are the contraindications and cautions in use of opioids?

A

Hypersensitivity, acute bronchial asthma, head injury, sleep apnea, obese, pulmonary disease, CHF, and renal insufficiency in some (morphine and meperidine)

40
Q

What are some drug interactions between opioids?

A

Do not use with other CNS depressants

41
Q

What is used for treatment of opioid-induced constipation?

A

Naloxegol

42
Q

What is the limit in mg for giving opioid antagonists to a person suspected of have an opioid OD?

A

10mg

43
Q

Is there cross tolerance in pure agonists or mixed kappa agonist-mu antagonist?

A

Pure agonist

44
Q

What are the 3 tolerances to opioids?

A

Analgesia, CNS depression, euphoria

45
Q

What are 3 opioid withdrawal approaches?

A

Quit opioids cold turkey, methadone or buprenorphine withdrawal, or clonidine

46
Q

What is an approach to discourage opioid relapse?

A

Naltrexone

47
Q

What are caffeine’s effects in the CNS?

A

It antagonizes all adenosine receptors. This causes mild cerebrovasoconstriction.

48
Q

What is the only anti-depressant that has co-analgesia effects? Why?

A

Amitriptyline. It blocks NA channels and blocks NE and serotonin re-uptake.

49
Q

Are opioids good for neurogenic pain? Why?

A

No. The damage to the primary afferent nerve causes less opioid receptors to be expressed.

50
Q

What are some effective drugs for neurogenic pain?

A

Tricyclic antidepressants.

Anti-epileptics (gabapentine and pregabalin)

931 Block 3 (4 decks)

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