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Pharmacology > Opiod agonists and antagonists > Flashcards

Opiod agonists and antagonists Flashcards

1
Q

MOA of opioid analagesics

A

agonists at opiod receptors, inhibitory signalling
blocks pain transmission and response
raises pain threshold
anti-anxiety effect

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2
Q

Receptor subtypes activated by morphine

A

mu, kappa, delta

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3
Q

pharmacokinetics of morphine

A

Rapid acting, 5-15 min
Maximum effect within 60-90 min
half-life 2.5-3 hrs
lasts 4-5 hrs

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4
Q

Standard dose of morphine

A

10 mg i.m. s.c. , 7 mg for elderly/ children

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5
Q

Metabolism of morphine

A

High level of first pass metabolism
Glucuronic acid conjugation
renal clearance of metabolites, caution with impared liver or renal function

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6
Q

Mechanism of respiratory failure in morphine OD

A

decreased sensitivity to plasma CO2
hypoxic response still intact
tolerance develops with analgesia tolerance

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7
Q

“First dose effect of morphine”

A

nausea and vomiting

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8
Q

GI effects of morphine

A

constipation, little or no tolerance, major problem with chronic use. Naltrexone.

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9
Q

Minor side effects of morphine

A

Miosis
Euphoria, tranquility
Pruritis
Mild CV, orthostatic hypotension

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10
Q

Therapeutic use of morphine

A

moderate to severe pain
primarily in acute pain
chronic pain use is discouraged except in terminal disease
Other: sickle cell crisis, end stage lung cancer and other terminal pain (and COPD)

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11
Q

Additional side effects and precautions of morphine (5)

A 
biliary colic, increase urinary tract pressure
allergic reactions
dysphoria, excitement
neonates and aged more sensitive
dependence
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12
Q

Drug interactions with morphine (2)

A

CNS depressants

Ethanol and long release preps

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13
Q

Limitations and contraindications or morphine (3)

A

decreased respiratory reserves
head injuries
pregnancy

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14
Q

Advantages of codeine

A

more orally reliable

effective cough suppressant

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15
Q

Disadvantages of codeine

A

more constipation

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16
Q

Therapeutic use of codeine

A

mild to moderate pain

17
Q

Advantages of methadone

A

very reliable orally
long half life
full agonist- same effect as morphine

18
Q

Disadvantages of methadone

A

may prolong Q-T interval
metabolized by CYP 3A4
Also abused like morphine

19
Q

Advantages of fentanyl

A

full agonist like morphine
potent, short acting
can be used transdermally for chronic pain
lozenge/film/tablet for breakthrough pain
less effect on cardiovascular system

20
Q

Disadvantages of fentanyl

A

more likely to produce muscle rigidity of chest and abdominal muscles

21
Q

Hydrocodone highlights

A

similar to codeine, #1 prescription, major abuse problem

22
Q

Oxycodone highlights

A

more potent than codeine, abuse of timed release formulation

23
Q

Therapeutic use of loperamide

A

anti-diarrheal agents, full opiod agonists, but do not cross membranes readily

24
Q

Dextromethorphan highlights

A

chemically similar to opioids, effective cough suppressant, no analgesia, abuse increasing

25
Q

Meperidine highlights

A

excitatory, at high doses with chronic use due to long lasting metabolite, less effect on GI tract. Can be used IV for infusion related rigors and chills

26
Q

Advantages of mixed agonist-antagonist, partial agonists

A

ceiling in both respiratory depression and pain analgesia

27
Q

Disadvantages of partial agonists

A

most have kappa receptor side effects, dysphoria

28
Q

Pentazocine compared to morphine

A

limited analgesia, resp depression
more reliable orally
antagonist properties in dependence

29
Q

Therapeutic use of pentazocine

A

analgesia in moderate to severe pain, not used chronically due to dysphoria

30
Q

Buprenorphine summary

A

partial agonist at mu receptors- similar effects as morphine
antagonist at kappa receptors- no dysphoria
may prolong Q-T interval

31
Q

Therapeutic use of buprenorphine

A

moderate to severe pain

to treat opiod dependence

32
Q

MOA of tramadol

A

weak mu agonist, inhibits NE and 5HT

33
Q

Therapeutic use of tramadol

A

can produce dependence, seizures, serotonin syndrome seen. suicide risk, drug interactions. No advantage clinically

34
Q

Naloxone MOA

A

blocks opiate receptors

35
Q

Therapeutic use of naloxone

A

used for overdose/high dose treatment

precipitate withdrawal in opiate dependence

36
Q

Diagnosis of opioid overdose

A

respiratory depression
miosis
coma

37
Q

Opiod overdose treatment

A
  1. support respiration
  2. prevent absorbance if taken orally
  3. naloxone IV repeatedly at short intervals

Pharmacology (35 decks)

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