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Brain and behavior > Opioids > Flashcards

Opioids Flashcards

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1
Q

Natural opiates

A

Morphine and Codine

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2
Q

How do opioids work?

A

They act on GABA neurotransmission by disinhibiting presynaptic release of GABA.

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3
Q

Types of opioid receptors

A

Mu (endorphins, morphine)
Delta (enkephalins)
Kappa (Dynorphins)

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4
Q

Distribution of opioids

A

Distribute to highly perfused tissues (lungs, brain, kidneys, spleen, liver)

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5
Q

Is there a first pass effect?

A

yes, big one.

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6
Q

Metabolism/excretion

A

Converted to polar metabolites and excreted through the kidney.

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7
Q

Morphine

A

Mu receptor agonist, causes analgesia, euphoria, vasodilation, decreased GI motility, decreased urination

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8
Q

How to opioids effect pupils?

A

Cause pupillary constriction because parasympathetic inputs are indirectly stimulated.

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9
Q

Metabolism of Morphine

A

90% to morphine-3-glucuronide, 10% to morphine-6-glucuronide (which is an active analgesic). Happens in liver

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10
Q

Excretion of morphine

A

90% excreted as M3G in the urine

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11
Q

Codeine

A

Another opiate, binds to mu receptor as an opiate receptor agonist, gets converted to morphine. Used as a cough suppressant, and a weaker analgesic than morphine

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12
Q

Side effects of codeine

A

Increased nausea/vomiting, worstening pruritis

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13
Q

Diacetylmorphine

A

Heroin, converted to morphine and 6-acetylmorphine (also active) in blood.

Activity at all opioid receptors.

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14
Q

Half-life of diacetylmorphine

A

3 minutes before conversion to constituent drugs.

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15
Q

Oxycodone

A

Semi-synthetic opioid, acts similarly to morphine. Used for analgesia (moderate to severe), not great in liver/kidney.

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16
Q

Hydrocodone

A

Semisynthetic, chemically related to codeine. Used for analgesia (mild-moderate) and as a potent anti-tussive. With acetaminophen as vicodin.

17
Q

Hydromorphone

A

The powerful. Morphine derivative that is 7-8x times more potent. Used for moderate to severe pain, safer in patients with liver/kidney disease. Better for kidney disease.

18
Q

Meperidine

A

First synthetic opioid. Mu and kappa receptor agonist. Some anticholinergic properties (like atropine). High first pass metabolism.

19
Q

Fentanyl

A

Strong, safe, portable.

Mu receptor agonist. Doesn’t cause histamine release. For severe pain and dyspnea. Great transdermal bioavailablilty.

20
Q

Methadone

A

Opioid with extra powers. Mu receptor agonist, but also NMDA receptor ANTAGONIST. Analgesia and neuropathic pain (as NMDA receptor). Safe in liver/kidney patients. Can have cardiac side effects.

21
Q

Loperamide

A

Doesn’t cross BBB, slows intestinal contractions and stops diarrhea.

22
Q

Dextromethorphan

A

The psychedelic cough suppressant. Mu receptor agonist (little analgesia) NMDA receptor antagonist.

23
Q

Tramadol

A

The opioid thats not an opioid. Serotonin releasing agent, NMDA receptor antagonist, NE reuptake inhibitor. Used for moderate analgesia. Lowers seizure threshold. Side effects are not like other opioids.

24
Q

Naloxone

A

Mu, kappa delta competitive ANTAGONIST. Used for opioid intoxication.

25
Q

Naltrexone

A

Twice as potent as naloxone, lasts twice as long. Use with opioid overtose, alcohol intoxication, or opioid abuse.

26
Q

Methylnaltrexone

A

Peripherally acting antagonist. Relieves constipation related to opioids.

27
Q

Hypothesis for development of tolerance

A

Hypothesized to be due to upregulation of cAMP, failure of receptor recycling, receptor and G-protein uncoupling.

28
Q

Tolerance for sedation/respiratory depression vs tolerance for nausea/vomiting/constipation

A

Tolerance for sedation develops first (days), nvd takes weeks.

29
Q

Three step ladder for pain relief prescribing

A

Step one: NSAIDs/acetominophen
Step two: Hydrocodone, codeine, oxycodone, oral morphine, tramadol.
Step three: morphine IV, hydromorphone, fentanyl, methadone

30
Q

Rotating from one opioid to another requires 2 steps:

A

1) calculate equianalgesic dose 2)reduce for incomplete cross tolerance – reduce by half. Don’t need to do this if switching from PO to IV though.

31
Q

Dependence

A

The development of a withdrawal syndrome following dose reduction or administration of an antagonist

32
Q

Tolerance

A

Change in dose-response relationship induced by exposure

33
Q

OUD

A

Opioid use disorder: a problematic pattern of use leading to impairment or distress

34
Q

Addiction

A

Compulsive use despite harm

35
Q

Pseudo-addiction

A

Behaviors that are reminiscent of addiction, but are driven by pain

36
Q

How do opioids lead to addiction?

A

Inhibition of GABAergic neurons in VTA, leading to disinhibition of DA neurons

37
Q

Buprenorphine

A

Partial mu agonist, good for treating opioid dependence. Antagonist of delta and kappa. High affinity for mu so can replace morphine etc.

38
Q

Suboxone

A

Buprenorphine/Naloxone. Used so that injection doesnt work.

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