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Clinical Pharmacology > Opioids and Drugs of Abuse > Flashcards

Opioids and Drugs of Abuse Flashcards

1
Q

What is pain?

A

The perception of an unpleasant stimulus; the signal is transmitted from the periphery to the dorsal horn and the brain.

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2
Q

What are the primary pain neurotransmitters?

A

Substance P and glutamate (both are excitatory).

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3
Q

Which neurotransmitters are inhibitory in this context (reduce pain)?

A

GABA, serotonin, and norepinephrine.

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4
Q

What are the two components of pain?

A

Nociceptive and affective (the euphoria produced by pain medications addresses the affective component.

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5
Q

What are the three classifications of pain?

A

Nociceptive, neuropathic, and mixed – treatments vary for each kind.

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6
Q

What is nociceptive pain?

A

Pain which can be acute or chronic, mild to severe; therapy starts with NSAIDs and APAP before progressing to opioids.

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7
Q

What is neuropathic pain?

A

A burning, shock-like pain that is chronic and difficult to reverse; drugs target GABA, serotonin, and norepinehrine (opioids are not heavily implicated).

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8
Q

Which drugs can be used to treat both types of pain?

A

Tramadol and tapentadol.

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9
Q

Describe the pain pathway:

A

In response to a pain stimulus the brain releases three endgenous peptides (endorphins, enkephalins, and dynorphins), in both the CNS and periphery which activate Mu-opioid receptors.

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10
Q

What are Mu-receptors?

A

G-protein coupled receptors found in the brain, spinal cord, and periphery.

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11
Q

What occurs upon activation of the Mu-receptor?

A

Inhibition of adenylate cyclase; decreased cAMP; opening of potassium channels (hyperpolarization); and inhibition of calcium channels (decreased neurotransmitter release).

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12
Q

How does a pain stimulus lead to the activation of Mu-receptors?

A

The pain stimulus is generated in the periphery and passes to the primary afferent, where it causes the release of glutamate and substance P in the dorsal horn; these substances activate a secondary afferent, promoting the release of Mu-agonists.

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13
Q

What happens upon opioid (Mu) receptor activation?

A

Analgesia (Mu); euphoria (Mu); dysphoria (Kappa); respiratory depression (Mu/Kappa); CNS sedation and miosis (Mu/Kapa); N/V (Mu); constipation and difficulty urinating (periheral Mu); and histamine release and reduced immune function (peripheral Mu).

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14
Q

Tolerance will NOT build to which two effects of opioid receptor activation.

A

Miosis (pinpoint pupils) and constipation (patients on opioids must always take a laxative).

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15
Q

Describe the difference between the terms opiate, opioid, and narcotic:

A

Opiate: a substance derived from the poppy seed; Opioid: an opiate derivative; and Narcotic: an old term for a substance which induces sleep.

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16
Q

Describe how opioids are metabolized:

A

They undergo significant first-pass metabolism; the codeines (hydrocodone/oxycodone) undergo CY2D6, whereas the morphines (hydromorphone/oxymorphone) undergo phase II conjugation.

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17
Q

How do precautions differ between the codeines and the morphines?

A

Codeines have potential drug interactions; morphines should be avoided in the hepatically impaired; morphine should be avoided in the renally impaired.

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18
Q

Which drugs are considered phenanthrenes?

A

Codeine, mrphine, hydrocdone, oxycodone, oxymorphone, and buprenorphine.

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19
Q

What is buprenorphine?

A

A partial agonist which can be used alone for pain, or in combination with naloxone for treating abuse (Subxone).

20
Q

What is codeine?

A

An antitussive and weak analgesic that is sometimes used for pain (Tylenol 3).

21
Q

What is a metabolic concern when using morphine?

A

It has an active metabolite (M6G) that can cause renal failure in excess.

22
Q

What are the two uses of hydrocodone?

A

It is combined with APAP to treat pain (Vicodin/Norco); or combined with homatropine for use as an antitussive (Hycodan).

23
Q

What is the most potent phenanthrene?

A

Opana (oxymorphone); it has an active metabolite, and is often used for chronic pain in cancer patients.

24
Q

Which drugs are phenylpiperidines?

A

Mepdridine, fentanyl, sufentanil,malfentanil, remifentanil.

25
Q

In what setting are sufentanil, malfentanil, and remifentanil typically used?

A

Anesthesia, or possibly in veterinary medicine.

26
Q

What are some characterstics of Duragesic (fentanyl)?

A

Its lipophillic, has a quick onset, and a rapid duration; it may be useful in those with cardiac compromise; it comes in various dosage forms; it CANNOT be prescribed without a history of previous opioid exposure.

27
Q

Which drug is considered a diphenylheptane?

A

Methadone; it has additional glutamate-receptor antagonist activity, and some SNRI activity.

28
Q

What are the two indications for methadone?

A

Detoxification; and chronic pain (non-neuropathic).

29
Q

Which two drugs are considered “multi-modal agents”, and how do they work?

A

Tramadol and tapentadol; they are Mu-agonists, which also enhance norepinephrine and serotonin. They may also have alpha-2 activity.

30
Q

What is Ultram (tramadol) used for?

A

Its a weak analgesic; low potency.

31
Q

How does Nucynta (tapentadol) work?

A

It is a strong Mu-agonist, similar to morphine, that also inhibits norepinehrine reuptake.

32
Q

Which drugs are mixed agonist/antagonists which attempt to target Kappa receptors?

A

Butorphanol, nalbuhine, and pentazocine.

33
Q

What is Narcan (naloxone)?

A

A Mu-antagonist which has high first-pass metabolism (given intranasally) and short duration; it is used for reversing opioid-induced ADRs.

34
Q

What is naltrexone?

A

A Mu-antagonist which has a longer duration of action and is also used for opioid dependence; it may be combined with morphine (Embeda).

35
Q

What are peripheral Mu-agonists?

A

Drugs used to treat diarrhea – includes: (1) Lomotil (diphenoxylate/atropine); (2) Imodium (loperimide); and (3) DTO.

36
Q

Why is atropine added to diphenoxylate when treating constipation (Lomotil)?

A

Atropine promotes constipation, but also is added to deter abuse.

37
Q

Where is DTO often used?

A

Neonatology (to treat diarrhea in infants); or, to treat neonatal withdrawal.

38
Q

In whom are opioids contraindicated?

A

Those with respiratory compromise (not always an absolute C/I); those with head injury (increases ICP); those with hepatic compromise (codeine) and renal renal compromise (morphine).

39
Q

What forms of monitoring are used during opioid therapy?

A

Urine toxicology (diversion/abuse); subjective pain scores; addiction risk surveys; bowel regimen (elderly); renal and hepatic function; and allergic reaction screening.

40
Q

What does 6-MAM indicate on a urine toxicology report?

A

Heroin.

41
Q

What does EDDP indicate on a urine toxicology report?

A

Methadone.

42
Q

What does M6G/M3G indicate on a urine toxicology report?

A

Codeine or morphine.

43
Q

What does H3G indicate on a urine toxicology report?

A

Hydromorphone.

44
Q

How is dose calculated when switching between opioids?

A

We must consider incomplete cross-tolerance; decrease the equianalgesic dose by 25-50% in order to prevent respiratory depression.

45
Q

What is capsaicin?

A

A topical application derived from the capsicum plant, which works by preventing the accumulation of substance P; must wear gloves and avoid mucosal contact.

46
Q

What is Prialt (ziconotide)?

A

An n-type calcium channel blocker that inhibits calcium entry into the neuron, and thus, prevents substance P/glutamate release from the dorsal horn.

Clinical Pharmacology (7 decks)

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