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Pharmacology- Test 4 > Opioid Drugs > Flashcards

Opioid Drugs Flashcards

1
Q

What is an opiate?

A

morphine-like (chemical)

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2
Q

What is an opioid?

A

morphine-like (pharmacological actions), also includes antagonist drugs

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3
Q

What is an endorphin?

A

endogenous opioid peptides (enkephalins, dynorphins, B-endorphins, endomorphins)

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4
Q

What is a narcotic?

A

narcosis, stupor, sleep inducing (legal term)

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5
Q

What is the principal therapeutic effects of opioids? (3)

A

(1) Analgesia
(2) Cough suppression
(3) Constipation

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6
Q

What is the definition of pain?

A

an unpleasant sensory and emotional experience associated with, or described in terms of, actual or potential tissue damage

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7
Q

T/F Opioids analgesic management occurs with loss of consciousness.

A

FALSE; without LOC

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8
Q

What are the 3 aspects of pain that opioids (analgesia) are effective with?

A

(1) Pain management
(2) Continuous dull pain better relieved than sharp intermittent pain (i.e. neuropathic pain)
(3) Pain as a sensation and pain in the context of suffering. Morphinized patients still feel the pain but it is not as discomforting

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9
Q

T/F Pain management with opioids is selectively decreased.

A

TRUE; there is no effect on other senses (i,e, touch, vibration, temperature)

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10
Q

What are additional CNS effects that opioids have on the body? Which one is the primary consequence of opioid overdose?

A

(1) Euphoria
(2) Sedation
(3) Respiratory Depression: primary consequence of opioid overdose; decreased responsiveness of brain-stem respiratory center to CO2

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11
Q

What are the contraindications of opioids?

A
  • Contraindicated in head trauma (potentiates respiratory depression and CO2 retention leads to cerebral artery vasodilation and increase in intracranial pressure.
  • use cautiously in patients with COPD and asthma
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12
Q

What are 6 other effects of opioids?

A

(1) Cough suppression- depresses cough reflex
(2) miosis
(3) emesis
(4) constipation
(5) biliary tract
(6) cardiovascular system

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13
Q

What dosage do you have to use for cough suppressive effects?

A

low dose; effect not blocked by opioid receptor antagonists

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14
Q

T/F There is tolerance to the miosis effect.

A

FALSE; always will have the pinpoint pupils. They may mas pupillary changes in head trauma

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15
Q

What patients are more susceptible to emesis? What type of effect is emesis with opioid use?

A

Ambulatory patients; primarily first dose effect

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16
Q

T/F There is some tolerance to constipation effects on opioids.

A

TRUE; intermediate tolerance

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17
Q

How do opioids produce constipation?

A

Acts on nerves (intrinsic nerve plexi) and not on smooth muscle or secretory cells, increased muscle tone in duodenum and antrum of the stomach and decreased peristaltic movement in jejunum and colon

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18
Q

What are the CV effects of opioids? (2)

A
  • no major effects on HR and BP

- opioid agonists can stimulate the release of histamine and thereby cause hypotension

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19
Q

T/F Opioids constrict the sphincter of Oddi which leads to a decrease in pressure of common bile duct.

A

FALSE; increase in the pressure of common bile duct

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20
Q

What are the subtypes of opioids? (3) What are they used for?

A

(1) Mu: morphine-preferring; many of the clinically used opioid drugs are selective for this receptor; mediates spinal and supraspinal analgesia, respiratory depression, miosis, GI effects
(2) Kappa- relevant receptor in spinal cord mediated analgesia
(3) Delta- spinal and supraspinal analgesia

21
Q

What are the receptor selectivity for the subtypes of opioids? What type of receptors are these?

A

(1) Mu- endomorphins and B-endorphin (enkephalins, dynorphins)
(2) Kappa- Dynorphins (enkephalins)
(3) Delta- Enkephalins, B-endorphins (dynorphins)
- G-protein coupled receptors -

22
Q

What are the four genes associated with endogenous opioid peptides? What do they yield?

A

(1) POMC (pro-opiomelanocortin): yield B-endorphin (met-enkephalin)
(2) Proenkephalin: yield met- and leu-enkephalins
(3) Prodynorphin: yield dynorphin A and B, and alpha and beta neoendorphins (leu-enkephalin)
(4) Pro-endomorphin: putative gene yielding endomorphin-1 and endomorphin-2

23
Q

What are the opioid receptor effector systems? (3)

A

(1) Potassium channels: agonists open channels causing neuronal hyperpolarization
(2) Calcium channels: agonists reduce channel opening, thereby inhibiting calcium-dependent neurotransmitter release
(3) Adenylate cyclase inhibition: alterations in regulation of adenylate cyclase activity important in tolerance to opioids

24
Q

T/F Tolerance to opioids is pharmacokinetic (change in metabolism).

A

FALSE; pharmacodynamic (cellular response)

25
Q

Dependence: what is initiated with withdrawal or after administration of an antagonist?

A

Abstinence syndrome

26
Q

What are the symptoms of withdrawal over the first 8-12 hours? (4)

A

(1) Lacrimation
(2) Rhinorrhea
(3) Yawning
(4) Sweating

27
Q

What are the symptoms of withdrawal over 12-14 hours? (7)

A

(1) Tossing, restless sleep
(2) Dilated pupils
(3) Anorexia*
(4) Goose Flesh “cold turkey”
(5) Restlessness
(6) Irritability
(7) Tremor

28
Q

What are the symptoms of withdrawal over 48-72 hours (at peak)? (9)

A

(1) Increased irritability
(2) Insomnia*
(3) Marked anorexia
(3) Sneezing
(4) Nausea/vomiting
(5) Increased HR and BP
(6) Marked chilliness (alternating between flushing and sweating)
(7) Gooseflesh
(8) Abdominal cramps*
(9) Exaggerated respiratory response*

29
Q

T/F Opioid withdrawal is rarely life threatening.

A

TRUE

30
Q

How long does withdrawal from opioids usually last? How can this be reduced?

A

7-10 days; dramatically reversed with opioid agonist administration

31
Q

Short-acting drugs are “more/less” intense, “shorter/longer” in duration?

A

MORE intense; SHORTER

32
Q

What determines whether the drug is an agonist or an antagonist?

A

N-17 (amine) substitute (the structure of the opiate like drugs are 3- and 6-hydroxy substitutions)

33
Q

Morphine: What is the bioavailability? How is it given?

A
  • Low bioavailability due to significant first pass metabolism
  • Given IM or IV
  • Morphine-6-glucuronide (metabolite) has significant biological activity
34
Q

Codeine: bioavailability, potency

A
  • good bioavailability (~60%)
  • low potency (metabolized to morphine)
  • good anti-tussive
35
Q

What opioids are pro-drugs?

A

(1) Codeine

(2) Heroin

36
Q

Heroin: how it is metabolized? What is the entry into the brain?

A
  • Diacetylmorphine, rapid entry into brain, metabolized to 6-MAM and then morphine
37
Q

Oxycodone: combination with what? how is it given?

A
  • often used in combination with NSAID

- orally active, as potent as morphine

38
Q

What is Dextromethorphan? Does it have analgesic effects? What is it good for?

A

D isomer of the codeine analog levorphanol; no analgesic effects; good anti-tussive

39
Q

T/F Naloxone is a pure antagonist.

A

TRUE

40
Q

How is Naloxone given?

A

IV only (zero bioavailability)

41
Q

What is Naloxone used for? What is it’s half life? Why is this important?

A
  • Reversal of opioid toxicity
  • short half-life compared to most opioid agonists which is important because you need to give the Naloxone more often so they don’t go back into toxicity
42
Q

Meperidine: bioavailability? Interactions?

A
  • variable bioavailability

- severe interaction with MAO inhibitors (severe respiratory depression, delerium, convulsions)

43
Q

T/F Meperidine has less GI effects than morphine.

A

TRUE

44
Q

T/F Meperidine as no pupillary constriction.

A

TRUE; due to countereffects of a metabolite, normeperidine

45
Q

What is Diphenoxylate used for?

A

low solubility, antidiarrheal

46
Q

What is Methadone used for?

A
  • similar analgesic efficacy as morphine

- used to treat opioid addicts (with longer half-life withdrawal symptoms are minimized, thus easier to break the habit)

47
Q

T/F Methadone blunts IV heroin induced euphoria.

A

TRUE

48
Q

What receptor does Pentazocine work with? What is it used for?

A
  • Kappa receptor selective agonist (mu receptor partial agonist)
  • used for chronic severe pain
  • lower abuse potential
49
Q

What is Pentazocine used in combination with?

A

Naloxone

Pharmacology- Test 4 (11 decks)

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