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D1 Spring > Pharmacology - Opioids (Exam 1) > Flashcards

Pharmacology - Opioids (Exam 1) Flashcards

1
Q

What are the 2 components of pain?

A
  1. specific sensation (physical)
  2. reaction to the sensation (psychological)
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2
Q

What are the two types of analgesics?

A
  1. Narcotic analgesics (opioid analgesics).
  2. Non-narcotic analgesics.
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3
Q

Opioid analgesics raise the threshold for _______ _______ and alter the ________ _________.

A

pain perception; affective response

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4
Q

What are the sites of opioid action?

A
  1. Thalamus
  2. Limbic system
  3. Brain stem
  4. Spinal cord
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5
Q

Where are opioid receptors and endogenous opioids located?

A

spinal cord

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6
Q

What are the 3 opioid receptors?

A
  1. Mu
  2. Kappa
  3. Delta
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7
Q

What are the pharmacological effects of morphine on specific body systems (7)?

A
  1. mood changes
  2. nausea and vomiting
  3. respiratory depression
  4. antitussive
  5. miosis
  6. urinary retention
  7. GI effects
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8
Q

What is associated with mood changes on morphine?

A

euphoria and mental clouding

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9
Q

Why does morphine cause nausea and vomiting?

A

opioids stimulate the chemoreceptor trigger zone (CTZ)

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10
Q

What are the 2 ways morphine causes respiratory depression?

A
  1. decreases response of brain stem respiratory neurons to CO2
  2. bronchoconstriction (release of histamine)
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11
Q

What are the GI effects of morphine?

A

constipation and antidiarrheal

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12
Q

All tolerance to opioids is ____________; there is NO _______ _________.

A

pharmacodynamic; metabolic tolerance

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13
Q

Opioid withdrawal is NOT life threatening

A

true

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14
Q

What are the general uses of opioid analgesics?

A
  1. analgesia
  2. antitussive
  3. antidiarrheal
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15
Q

Most opioids can relieve ___________ and are usually reserved for _______ to _______ pain.

A

all types of pain, moderate to severe

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16
Q

(T/F) not all opioids are equally effective and some are used only for moderate pain in combination with other analgesics.

A

true

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17
Q

we can compare opioid analgesics by

A

source and activity

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18
Q

what are some of the sources for comparison of opioid analgesics?

A

a. naturally occurring (morphine, codeine)
b. partial synthetic (heroin, naloxone)
c. synthetic (levorphanol, meperidine, methadone)

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19
Q

what are some of the activities for comparison of opioid analgesics?

A

a. agonist
b. antagonist
c. agonist/antagonist

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20
Q

What are the opioid agonists?

A

Morphine
Codeine
Oxycodone
Meperidine
Fentanyl
Methadone

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21
Q

What are the opioid antagonists?

A

Naloxone
Naltrexone

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22
Q

Naloxone is a pure, competitive _______ at all opioid receptors with NO opioid agonist activity

A

antagonist

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23
Q

What is the duration of action for naloxone?

A

1-4 hours (short)

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24
Q

Naltrexone is a pure, competitive ________ with a _____ hour duration of action.

A

antagonist; 24

25
Q

How is naltrexone active?

A

orally active

26
Q

What are the uses of pure antagonists?

A
  1. tx of opioid overdose
  2. diagnose addiction
  3. tx of compulsive use
27
Q

What are the opioid mixed agonist-antagonists?

A

Pentazocine
Nalbuphine
Butorphanol
Buprenophrine

28
Q

How is pentazocine used?

A

as an analgesic for mild to moderate pain

29
Q

Pentazocine is a weak ______ antagonist. It blocks ______ ________ and induces opioid (mu) withdrawal in the physically dependent. Does NOT block _______ _______ ________.

A

mu; morphine analgesia; morphine respiratory depression

30
Q

Pentazocine is an agonist at _____ and ______ receptors.

A

kappa; sigma

31
Q

Pentazocine as an agonist at kappa and sigma receptors causes the following effects:

  1. _______ analgesia that is as effective as morphine analgesia
  2. _______ ________ of the limited type, not as severe as that of morphine.
  3. ________ and ________, especially with repeated high doses
A
  1. spinal
  2. respiratory depression
  3. dysphoria; hallucinations
32
Q

How are Nalbuphine and Butorphanol used?

A

as an analgesic for moderate to severe pain

33
Q

Nalbuphine and Butorphanol are _____ antagonists that can antagonize _______ ________ and induce abstinence syndrome in those who are physically dependent to morphine.

A

mu; morphine analgesia

34
Q

Nalbuphine and Butorphanol are ______ agonists that:

  1. produce effective analgesia with limited ________ _______.
  2. ______ incidence of psychotomimetic effects.
  3. mild _________ ________.
  4. antagonized by ________.
A

kappa

  1. respiratory depression
  2. low
  3. abstinence syndrome
  4. naloxone
35
Q

How is Buprenorphine used?

A

as an analgesic for moderate to severe pain

36
Q

Buprenorphine is a partial ______ agonist. The effects it induces are ______ in onset and ______ lasting.

A

mu; slow; long

37
Q

The effects of Buprenorphine as a partial agonist at mu receptors include what 5 things?

A
  1. analgesic
  2. respiratory depression (minor)
  3. euphoria
  4. miosis
  5. mild morphine type abstinence sundrome
38
Q

Buprenorphine is a ________ antagonist. It is antagonized by _______.

A

kappa; naloxone

39
Q

Why does heroin cross the BBB rapidly?

A

due to high lipid solubility

40
Q

How is codeine active?

A

orally active

41
Q

What is the potency and efficacy of codeine in comparison to morphine?

A

1/10th the analgesic potency
not as efficacious

42
Q

What is codeine used for?

A

antitussant (cough)
analgesic (w/ aspirin or aceptaminophen)

43
Q

What is the potency and efficacy of oxycodone in comparison to morphine?

A

same potency
same efficacy

(but oxycodone has higher oral activity)

44
Q

What are the synthetic opioids?

A

Meperidine
Fentanyl
Methadone

45
Q

How is meperidine active?

A

orally active

46
Q

What is the potency and duration of action of meperidine in comparison to morphine?

A

1/10 the potency
shorter duration of action (used for shorter analgesia)

47
Q

How is fentanyl active?

A

orally active, but used IV for anesthesia

48
Q

What is the potency and duration of action of fentanyl in comparison to morphine?

A

80x the potency
shorter duration of action (serum half-life of 20 mins!)

49
Q

Fentanyl is VERY _______ soluble, so it’s pharmacokinetics are similar to _______.

________ is the major means of termination of action.

A

lipid; thiopental; redistribution

50
Q

What is fentanyl used for clinically?

A
  1. anesthetic induction
  2. sole anesthetic for cardiac surgery
  3. neuroleptic state (combined w/ droperidol in innovar)
51
Q

Which 2 drugs are similar to fentanyl in action and use?

A

Alfentanil
Sufentanil

52
Q

How is methadone active?

A

orally active

53
Q

What is the potency and action of methadone in comparison to morphine?

A

same potency
same actions

54
Q

Is the duration of action for methadone long or short?

A

LONG

55
Q

What is the half-life for methadone?

A

15 hours (less severe side effects)

56
Q

What are the uses of methadone?

A
  1. chronic pain
  2. methadone maintenance
57
Q

What is the triad of symptoms for opioid overdose?

A
  1. coma
  2. depressed respiration
  3. miosis (pinpoint pupils)
58
Q

How do you treat an opioid overdose?

A
  1. restore respiration
  2. administer naloxone (narcan)
  3. watch pt. (may have to administer naloxone again)
59
Q

What is one opioid interaction?

A

neuroleptic analgesia

D1 Spring (47 decks)

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