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Pharmacology > Opioids > Flashcards

Opioids Flashcards

1
Q

Diphenoxylate, Loperamide Class

Opioids

A

Opioids

Antimotility agents

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2
Q

Diphenoxylate, Loperamide description

Opioids

A

Widely used in the treatment of diarrhea at doses that lack analgesic effects

Several mechanisms, but mostly act on mu and delta receptors

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3
Q 
Dextromethorphan, Codeine class
Opioids
A

Antitussives

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4
Q

Dextromethorphan, Codeine description

Opioids

A

Most effect cough suppressants

Lower dose than necessary for analgesia

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5
Q

Dextromethorphan, Codeine other

Opioids

A

Receptors are different than those associated with other action

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6
Q 
Naloxone, Naltrexone class
Opioids
A

mu and kappa antagonists

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7
Q

Naloxone, Naltrexone description

Opioids

A

Opioids
Nalaxone -> acute opioid overdose**
Naltrexone -> opioid addiction; also decrease EtOH craving in chronic alcoholics

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8
Q

Pentazocine, Butorphanol, Nalbuphine, Buprenorphine class opioids

A

Mixed agonist and antagonist

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9
Q

Pentazocine, Butorphanol, Nalbuphine, Buprenorphine description
Opioids

A

Potent analgesics in opioid naive patients, but precipitate withdrawal in patients that are physically dependent on opioids
Used in mild to moderate pain but are not routine due to ceiling effect
1st three may cause psychotomimetic effects, but not buprenorphine

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10
Q

Pentazocine, Butorphanol, Nalbuphine, Buprenorphine other

Opioids

A

Developed to reduce addiction potential of opioids especially buprenorphine

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11
Q

Tramadol description

Opioids

A

Weak mu agonist and NE/serotonin reuptake inhibitor

Useful for neuropathic pain

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12
Q

Tramadol other

Opioids

A

Increased risk of seizures

May cause serotonin syndrome

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13
Q 
Propoxyphene class
Opioids
A

mild to moderate agonist

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14
Q 
Tramadol class
Opioids
A

mild to moderate agonist

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15
Q

Propoxyphene description

Opioids

A

NOT recommended for routine dosing and withdrawn from market in 2010 due to cardiotoxicity

Metabolized to norpropoxyphene with a half life of 30hrs -> toxicity

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16
Q

Codeine, Oxycodone, Hydrocodone description

Opioids

A

Less efficacious than morphine
Usually combined with aspirin or acetaminophen
Codeine has low affinity for opioid receptors

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17
Q

Codeine, Oxycodone, Hydrocodone Metabolism

Opioids

A

Analgesic effect is due to metabolism by CYP2D6* to morphine
Metabolites have greater potency

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18
Q 
Methadone, Levorphanol class 
Opioids
A

Strong agonist

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19
Q

Methadone, Levorphanol description

Opioids

A

Equal potency to morphine but with less euphoria and longer half life

  • *mu agonist, NMDA antagonist and serotonin/NE reuptake inhibitor**
  • *Levorphanol is even longer acting** than methadone
20
Q

Methadone, Levorphanol other

Opioids

A

Used to manage opioid withdrawal in heroin addiction

Can cause QT prolongation, etc.

21
Q 
Fentanyl, Sufentanil, Alfentanil, Remifentanil class
Opioids
A

Strong agonists

22
Q

Fentanyl, Sufentanil, Alfentanil, Remifentanil description

Opioids

A

Rapid onset and short duration of action
100x more potent than morphine

Metabolized by CYP3A4 in the liver
No active metabolites

23
Q 
Meperidine class
Opioids
A

Strong agonist

24
Q

Meperidine description

Opioids

A

mu receptor agonist, but has high metabolite toxicity (normeperidine) ->tremor, twitching, mydriasis, hyperactive reflexes and convulsions*****

Serotonin syndrome -> delirium, hyperthermia, HA, rigidity, coma, dysregulation of BP, death (DO NOT combine with MAO-Is)

25
Q

Meperidine mechanism

Opioids

A

Accumulation of normeperidine can occur in patients with decreased renal function and cause seizures

26
Q

Meperidine other

Opioids

A

Normeperidine half life 15-20 hrs so it accumulates with frequent dosing
Meperidine half life = 3 hrs

27
Q

Heroin description

Opioids

A

6-monoacetylmorphine and heroin are more liposoluble than morphine and cross BBB

Rapid hydrolysis to 6-MAM -> morphine which can then be conjugated

Pharmacological actions are due to 6-MAM and morphine

28
Q

Hydromorphone, Oxymorphone description

Opioids

A

Severe pain

29
Q

Morphine description

Opioids

A

High affinity for mu receptor; standard for analgesia

30
Q

Morphine mechanism

Opioids

A

Conjugated to M3G -> neuroexcitation

10% -> M6G -> 4-6x more potent

31
Q

Morphine other

Opioids

A

Metabolites are polar and do not readily cross BBB

Metabolite effects may be increased in renal impairment

32
Q

Opioid analgesic mechanism

A

Produce analgesia primarily by activating receptors in the brain and spinal cord

Close voltage gates Ca2+ channels on presynaptic nerves and open K+ channels on postsynaptic nerves -> decreased NT release

Can also cause analgesia at peripheral mu receptors (i.e.knee)

33
Q

Spinal analgesia

Opioids

A

Inhibit ascending pain transmission

34
Q

Supraspinal analgesia

Opioids

A

Activate descending pain-inhibitory circuits* -> block inhibitory GABAergic neuron transmission

35
Q

Systemic administration

Opioids

A

Both spinal and supraspinal are acted on concurrently increasing overall analgesic efficacy

Peripheral mu receptors also acted on

36
Q

Opioid receptors

A

Mu, delta, kappa -> Gi
Majority act at the mu receptor and produce analgesia, euphoria, respiratory depression and physiologic dependence

delta and kappa are found primarily at the spinal level ->analgesia
kappa-> psychotomimesis (psychosis, delirium, hallucinations, etc)***

37
Q

Opioid tolerance, dependence, addiction

A

Frequent use -> loss in effectiveness -> tolerance
Dependence -> physiologic withdrawal or abstinence syndrome

Addiction -> euphoria leads to compulsive use

Physical dependence is common when use therapeutically, but addiction is not

38
Q

Opioid CNS effects

A

Analgesia -> reduce sensory and emotional components of pain
Euphoria -> floating sensation with decreased anxiety and distress
Sedation and drowsiness

Respiratory depression - decreased central response to CO2 -> not usually a life threatening complication, because pain is a power stimulus to breath

Cough suppression - decreased central cough center reflex
Miosis - excites PS -> pinpoint pupils are pathognomonic following toxic dose (mediated by mu receptor)

Truncal rigidity *
Nausea and vomiting -> activate brain stem trigger zone

39
Q

Opioid use

A

Analgesia-> moderate to severe pain
Acute pulmonary edema -> decrease anxiety, preload and afterload
Cough -> dextromethorphan, codeine, levopropoxyphene and noscapine
Diarrhea - loperamide and diphenoxylate
Shivering - meperidine (activates alpha 2 receptors)
Anesthesia - premedication and intraoperatively

40
Q

Opioids for cough

A

Dextromethorphan, codeine, levopropoxyphene and noscapine

41
Q

Opioids for diarrhea

A

loperamide and diphenoxylate

42
Q

Opioids for shivering

A

meperidine (activates alpha 2 receptors)

43
Q

Opioid metabolism and excretion

A

Mainly converted to glucuronides and excreted by the kidney but small amounts of unchanged drug may be found in urine

Very small amount of enterohepatic circulation

*Codeine, oxycodone, hydrocodone are metabolized by CYP2D6 -> metabolites with increased potency

44
Q

Supraspinal analgesia pathway

A

The descending pain inhibitory neuron is inhibited by GABA

Opioids inhibit the GABAergic neuron

This results in enhanced inhibition of pain transmission

45
Q

Opioid AE

A 
Nausea, vomiting, 
sedation
itching
*Constipation*
Urinary retention
Hypotension
Respiratory depression
46
Q

Opioid Peripheral effects

A

Hypotension -> due to peripheral vasodilation, inhibition of baroreceptor reflex and increase in histamine release

Constipation -> universal (concomitant laxative use)

Biliary colic -> contraction of biliary smooth muscle

Decreased renal function -> decreased renal blood flow

Prolong labor by unknown mechanism on uterus

Pruritus -> due to central effects and histamine release

47
Q

Opioid contraindication/interactions

A

Using a pure agonist with a weak partial agonist -> diminishing analgesia or inducing a state of withdrawal

Head injuries -> CO2 retention causes cerebral vasodilation
Pregnancy -> fetal dependence
Impaired pulmonary function -> acute respiratory failure
Impaired hepatic function -> decreased metabolism of morphine
Impaired renal function -> longer half - life
Endocrine disease-> adrenal insufficiency or hypothyroidism can have prolonged or exaggerated response to opioids

Sedatives/hypnotics -> increase CNS depression (respiratory)
Antipsychotics -> increase sedation, variable effects on respiratory depression and accentuate CV effects of anti-M and alpha-blockers
MAO-I’s -> life threatening rxn especially with meperidine and tramadol*

Pharmacology (24 decks)

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