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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
Meperidine mechanism | Opioids
Accumulation of normeperidine can occur in patients with decreased renal function and cause seizures
26
Meperidine other | Opioids
*Normeperidine* half life 15-20 hrs so it *accumulates* with frequent dosing Meperidine half life = 3 hrs
27
Heroin description | Opioids
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
Hydromorphone, Oxymorphone description | Opioids
Severe pain
29
Morphine description | Opioids
High affinity for mu receptor; **standard for analgesia**
30
Morphine mechanism | Opioids
Conjugated to *M3G -> neuroexcitation* | 10% -> M6G -> 4-6x more potent
31
Morphine other | Opioids
Metabolites are polar and do not readily cross BBB | Metabolite effects may be increased in renal impairment
32
Opioid analgesic mechanism
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
Spinal analgesia | Opioids
*Inhibit ascending pain transmission*
34
Supraspinal analgesia | Opioids
Activate descending pain-inhibitory circuits* -> block inhibitory *GABAergic* neuron transmission
35
Systemic administration | Opioids
Both spinal and supraspinal are acted on concurrently increasing overall analgesic efficacy Peripheral mu receptors also acted on
36
Opioid receptors
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
Opioid tolerance, dependence, addiction
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
Opioid CNS effects
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
Opioid use
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
Opioids for cough
Dextromethorphan, codeine, levopropoxyphene and noscapine
41
Opioids for diarrhea
loperamide and diphenoxylate
42
Opioids for shivering
meperidine (activates alpha 2 receptors)
43
Opioid metabolism and excretion
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
Supraspinal analgesia pathway
The descending pain inhibitory neuron is inhibited by GABA Opioids inhibit the GABAergic neuron This results in enhanced inhibition of pain transmission
45
Opioid AE
``` Nausea, vomiting, sedation itching *Constipation* Urinary retention Hypotension Respiratory depression ```
46
Opioid Peripheral effects
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
Opioid contraindication/interactions
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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