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Pharmacology > Opioids and Analgesics Flashcards > Flashcards

Opioids and Analgesics Flashcards

1
Q

physiologic pain

A

Defensive role. Acute in nature (labor, surgery, trauma). Easy management.

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2
Q

pathologic pain

A

No known benefit. Chronic and spontaneous. Low pain threshold to both noxious and innocuous stimuli. Associated with nerve damage (trauma, amputation, diabetes mellitus, HIV and VZV. Difficult to treat.

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3
Q

ascending pain transmissionpathway

A

From primary afferent nociceptors to dorsal horn cells.

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4
Q

descending pathway. Pain response.

A

Inhibitory regulation. Starts in Frontal Cortex, Amygdala, and Cingulate Cortex. Synapses PAG, RVM, then Dorsal Horn Cells.

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5
Q

desscending pathway receptors/transmitters

A

5HT, norepinephrine, glycine, GABA, and opioids.

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6
Q

Opioid Mu receptor

A

stabilize neuronal membrane by enhancing K+ conductance, and inhibiting voltage gated Ca++ channels. 1 - dependence, analgesia. 2 - euphoria, respiratory depression,

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7
Q

Opioid K receptor

A

Inhibitory.

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8
Q

Opioid D receptor

A

Inhibitory.

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9
Q

physical dependence

A

diaphoresis, insomnia, restlessness, abdominal cramps, N/V/D

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10
Q

psychological dependence

A

mediated by the ventral sriatum. Interactions between opioids and dopaminergic system in Nucleus Accumbens.

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11
Q

tolerance

A

Mediated by NMDA signaling (Glutamate). Normally cosmetic. Rotation therapy.

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13
Q

euphoria

A

Mediated by Mu. Does not occur with Codeine or Pentazocine. Improves life quality and compliance.

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14
Q

sedation

A

More so in the elderly. Greater in Phenanthrene derivatives than synthetic agents. Drowsiness, mental clouding, no amnesia.

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15
Q

antitussance

A

No correlation with analgesia or respiratory depression. Most potent with Codeine or Pholcodine. Dextromethorphan is preferred.

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16
Q

2 opioid receptor antagonists

A

Naloxone, Naltrexone

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17
Q

3 partial and mixed agonists

A

Butorphanol, Buprenorphine, Nalbuphine

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18
Q

7 synthetic opioids

A

Methadone, Meperidine, Fentanyl, Sufentanyl, Alfentanil, Ramifentanil, Diphenoxylate

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19
Q

5 naturally occuring opioids

A

Codeine, Morphine, and derivatives (hydromorphone, hydrocodone, oxycodone). Most widely used fo pain control (epidural, trauma, surgery)

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20
Q

Morphine

A

Naturally occuring. Hepatic metabolism - M3G to M6G (analgesic).

21
Q

Hydromorphone

A

Widely used more potent Morphine derivative.

22
Q

Codeine

A

antitussant, no euphoria, naturally occuring. Useful for mild to moderate pain. Hepatic deamination to Morphine by CYP2D6. Genetic alteration of CYP 2D6 and 3A4 voids analgesic effect.

23
Q

Oxycodone

A

effective mild analogue of codiene.

24
Q

Hydrocodone

A

effective mild analogue of codiene.

25
Q

Pholcodine

A

potent antitussant

26
Q

Dextromethorphan

A

Preferred to Codeine and Pholcodine bc - Low adverse effects, neuroprotective, useful in neuropathic pain.

27
Q

Pentazocine

A

no associated euphoria

28
Q

Methadone

A

Long plasma T1/2 - lipophilic and plasma protein binding. Chronic pain and terminally ill cancer patients. High risk of respiratory depression and QT prolongation - torsades de pointes.

29
Q

Meperidine

A

poor oral bioavailability. Metabolites cause seizures. Similar efficacy to Morphine, but less potent. Causes mydriasis (contrast to other opioids)

30
Q

Fentanyl

A

short acting, 100x more potent than morphine, highly lipophilic. Available in transdermal patch for slow delivery. Sufentanil, Alfentanil, and Ramifentanil.

31
Q

Butorphanol

A

K agonist, Mu partial agonist yields analgesia with a milder euphoria. Opioid addiction Tx, and maintenance in balance anesthesia, labor pain.

32
Q

Buprenorphine

A

K antagonist, Mu partial agonist. Moderate-severe long-term chronic pain management.

33
Q

Nalbuphine

A

K agonist, Mu antagonist. High psychological dysphoria. Moderate-severe pain, pre and post-op, obstetrical analgesia.

34
Q

Naloxone

A

Competetive antagonist ant Mu and K. Shorter T1/2 than Morphine. Parenteral administration. Opioid antidote whether known or suspected.

35
Q

Naltrexone

A

Opioid antagonist. Oral admin. Outpatient settings. Tx - dependence, relapse, following detox, and prophylaxis. Alcohol withdrawal.

36
Q

opioid respiratory depression

A

decrease sensitivity of chemosensitive neurons to PCO2. occurs at therapeutic doses. Most common cause of death in acute poisoning.

37
Q

GI Disturbances

A

epigastric distress and biliary colic (confused with angina). Increse pyloric sphincter tone, enhance and decrease frequency of peristalsis - constipation.

38
Q

miosis

A

diagnostic tool. Mu and K mediated. Involves edinger westphal nucleus.

39
Q

N/V

A

involving area postrema

40
Q

Hypotension and Bradycardia

A

impaired sympathetic response - orthostatic hypotension (morphine). Rapid IV admin of large dose causes non-specific mast cell degranulation. Synthetics and short-acting opioids generally do not evoke histamine release.

41
Q

NSAIDs and Acetominophen

A

decrease prostaglandin synthesis and therefore pain sensation.

42
Q

Antidepressants

A

Amitriptyline, Nortriptyline, and Imipramine - Tx of chronic pain that in not responsive to opioids. Venlafaxine and Duloxetine - used for neuropathic pain.

43
Q

NMDA receptor antagonists

A

Ketamine and Dexamethorphan - chronic pain syndrome and post-op pain. Ketamine - acute severe pain, strong psychomimetic effects.

44
Q

Adrenergic agonists

A

Clonidine - acute and chronic pain state. As well as withdrawal.

45
Q

Gabapentin

A

synthetic GABA analog - inhibits voltage-gated Ca channels. Chronic pain and post-op pain state. Erratic oral bioavailability - has to be monitored.

46
Q

Pregabalin

A

GABA analog - inhibits voltage gated Ca2+ channels in the CNS. Faster onset, more potent, and predictable bioavailability than Gabapentin. Neuropathic pain, fibromyalgia, spinal chord injury.

47
Q

Lamotrigine

A

Na+ channel blocker. Tx - neuropathic pain, trigeminal neuralgia. Skin reaction - steven/johnsons.

48
Q

Carbamazepine

A

Na+ channel blocker. Tx - trigeminal neuralgia. May cause Hypotension.

Pharmacology (12 decks)

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