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Pharmacology > 19) Opioids > Flashcards

19) Opioids Flashcards

1
Q

Types of opioid receptors

A
  • μ [mu]
  • δ [delta]
  • κ [kappa]
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2
Q

On the basis of their interaction with several opioid receptors, individual drugs are classified as

A
  • Agonists
  • Mixed agonist-antagonists
  • Antagonists
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3
Q

Opioids classified based on

A
  • Spectrum of clinical use
  • Strength of analgesia
  • Ratio of agonist to antagonist effects
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4
Q

Spectrum of clinical uses

A
  • Therapeutic uses (eg, analgesics, antitussives, and antidiarrheal drugs)
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5
Q

Strength of analgesia is based on

A
  • Relative abilities to relieve pain
  • May be classified as strong, moderate, and weak agonists
  • Classification is independent of potency
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6
Q

Ratio of agonist to antagonist effects

A
  • Agonists (full or partial receptor activators)
  • Antagonists (receptor blockers)
  • Mixed agonist-antagonists (activate one opioid receptor subtype and block another subtype)
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7
Q

Strong agonists (names)

A
  • Morphine
  • Methadone
  • Meperidine
  • Hydromorphone
  • Fentanyl
  • Sufentanil
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8
Q

Moderate agonists (names)

A
  • Codeine

- Oxycodone

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9
Q

Weak agonists (names)

A
  • Propoxyphene
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10
Q

Mixed agonist-antagonists (names)

A
  • Buprenorphine

- Nalbuphine

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11
Q

Antagonists (names)

A
  • Naloxone
  • Naltrexone
  • Nalmefine
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12
Q

Most opioids are well absorbed when taken orally, but theseundergo extensive first-pass metabolism

A
  • Morphine
  • Hydromorphone
  • Oxymorphone
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13
Q

Opioids are widely distributed to

A
  • Body tissues
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14
Q

With few exceptions, the opioids are metabolized by

A
  • Hepatic enzymes
  • Usually to inactive glucuronide conjugates
  • Elimination by the kidney
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15
Q

Morphine-6-glucuronide

A
  • Analgesic activity equivalent to that of morphine

- Morphine-3-glucuronide is its primary metabolite (neuroexcitatory)

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16
Q

Codeine, oxycodone, and hydrocodone are metabolized by

A
  • Cytochrome CYP2D6 (isozyme exhibiting genotypic variability)
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17
Q

For codeine, CYP2D6 may be responsible for variability in analgesic response because

A
  • The drug is demethylated by CYP2D6 to form the active metabolite, morphine
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18
Q

Meperidine is metabolized to

A
  • Normeperidine

- May cause seizures at high plasma levels

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19
Q

Receptors for endogenous peptides are located in

A
  • CNS and peripheral tissues
  • Distributed in the brain & spinal cord
  • Also outside the CNS (vascular tissues, cardia, airway/lung, gut and cells of the immune system)
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20
Q

Three major opioid receptor subtypes have been extensively characterized pharmacologically

A
  • µ (mu)
  • δ (delta)
  • κ (kappa) receptors
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21
Q

All 3 opioid receptor subtypes appear to be involved in

A
  • Antinociceptive and analgesic mechanisms at both spinal and supraspinal levels
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22
Q

The µ-receptor activation plays a major role in

A
  • Respiratory depressant actions of opioids

- With κ-receptor activation slows GI transit

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23
Q

κ-receptor activation appears to be involved in

A
  • Sedative actions
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24
Q

δ-receptor activation may play a role in

A
  • Development of tolerance
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25
Q

All 3 major opioid receptors are coupled to their effectors by

A
  • G proteins

- Activate phospholipase C or inhibit adenylyl cyclase

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26
Q

Major SE of opioids include

A
  • Analgesia
  • Sedation
  • Euphoria
  • Respiratory depression
  • Constipation
  • Miosis (pupil constriction)
  • Truncal rigidity
  • Flushing pruritis (through histamine)
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27
Q

Opioids (with the exception of meperidine) cause contraction of biliary tract smooth muscle, which can result in

A
  • Biliary colic or spasm
  • Increased bladder sphincter tone
  • Reductionin uterine tone
28
Q

When used for a prolonged period, these opioids may exacerbate pain (hyperalgesia)

A
  • Morphine
  • Fentanyl
  • Remifentanil
29
Q

K agonists, with weak µ-receptor antagonist activity

A
  • Butorphanol
  • Nalbuphine
  • Pentazocine
30
Q

_____ may act as a partial agonist or antagonist at the µ receptor

A
  • Butorphanol
31
Q

Buprenorphine is a µ-receptor partial agonist with weak antagonist effects at κ and δ receptors. These characteristics can lead to

A
  • Decreased analgesia and precipitate withdrawal symptoms when used in patients taking conventional full µ-receptor agonists
32
Q

The mixed agonist-antagonist drugs often cause

A
  • Sedation at analgesic doses
  • Dizziness, sweating, and nausea may also occur
  • Anxiety, hallucinations, and nightmares are possible adverse effects
33
Q

Mixed agonist-antagonist drugs respiratory effects

A
  • Respiratory depression may be less intense than with pure agonists
34
Q

Chronic use of mixed agonist-antagonist

A
  • Tolerance develops with chronic use, but is less than the tolerance that develops to the full agonists
35
Q

Pure opioid receptor antagonists that have greater affinity for µ receptors

A
  • Naloxone
  • Nalmefene
  • Naltrexone
36
Q

A major clinical use of the opioid antagonists

A
  • Management of acute opioid overdose
37
Q

Naloxone and nalmefene are given

A
  • Intravenously
38
Q

Because naloxone has a short duration of action (1–2 h), a _____ preparation of naloxone has recently been made available to treat opioid overdose promptly

A
  • Nasal insufflation
39
Q

Nalmefene has a duration of action of

A
  • 8–12 h
40
Q

Naltrexonehas a long elimination half-life, blocking the actions of strong agonists (eg, heroin) for up to

A
  • 48 h after oral use
41
Q

Unlike the older drugs, two new antagonists,_____and_____ do not cross the blood-brain barrier

A
  • Methylnaltrexone

- Alvimopan

42
Q

Methylnaltrexone and alvimopan block adverse effects of strong opioids on

A
  • Peripheral µ receptors (including those in the GI tract responsible for constipation)
43
Q

Naloxegol is a pegylated form of

A
  • Naloxone

- It is also used to reverse opioid constipation

44
Q

Miscellaneous opioids

A
  • Tramadol

- Tapentadol

45
Q

Tramadol

A
  • Weak µ-receptor agonist

- Partially antagonized by naloxone

46
Q

Tramadol analgesic activity

A
  • Mainly based on blockade of the reuptake of serotonin

- Weak norepinephrine reuptake blocker

47
Q

Tramadol is effective in treatment of

A
  • Moderate pain

- Has been used as an adjunct to opioid analgesics in chronic pain syndromes

48
Q

Tramadol is contraindicated in

A
  • Patients with a history of seizure disorders

- Risk of the serotonin syndrome if it is co-administered with SSRIs

49
Q

Tapentadol

A
  • Strong norepinephrine reuptake-inhibiting activity

- Modest µ-opioid receptor affinity

50
Q

Tapentadol treatment effectiveness

A
  • Less effective than oxycodone in the treatment of moderate to severe pain
  • Causes less gastrointestinal distress and nausea
51
Q

Tapentadol should be used with caution in

A
  • Seizure disorders
52
Q

Fentanyl brand name

A
  • Duragesic
53
Q

Hydromorphone brand name

A
  • Dilaudid
54
Q

Meperidine brand name

A
  • Demerol
55
Q

Morphine brand name

A
  • MS contin

- Kadian

56
Q

Methadone brand name

A
  • Methadose
57
Q

Oxymorphone brand name

A
  • Opana
58
Q

Sufentanyl brand name

A
  • Sufenta
59
Q

Tramadol brand name

A
  • Ultram
60
Q

Codeine brand name

A
  • No brand name listed
61
Q

Hydrocodone brand name

A
  • Norco

- Vicodin

62
Q

Oxycodone brand name

A
  • Percocet

- Oxycontin

63
Q

Buprenorphine brand name

A
  • Subutex
64
Q

Buprenorphine and naloxone brand name

A
  • Suboxone
65
Q

Nalbuphine brand name

A
  • Nubain
66
Q

Naloxone brand name

A
  • Narcan
67
Q

Naltrexone brand name

A
  • Vivitrol

Pharmacology (27 decks)

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