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CNS Pharma > Slides 2 > Flashcards

Slides 2 Flashcards

1
Q

What is the prototypical opioid (1803)?

A

Morphine

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2
Q

What is morphine derived from?

A

The opium poppy, Papaver
somniferum and P. album, after incision of the seed pod = white substance that turns brown gum, which contains 10% morphine.

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3
Q

What are the 3 families of endogenous opioid peptides?

A

1) The endorphins.
2) The pentapeptides enkephalins: methionineenkephalin (met-enkephalin) and leucineenkephalin (leu-enkephalin).
3) The dynorphins.

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4
Q

Why are there 3 families of endogenous opioid peptides?

A

Because they are derived from three different precursor proteins.

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5
Q

When are endogenous opioid peptides released?

A

During stressful conditions such as pain or the anticipation of pain to
diminish the sensation of noxious stimuli.

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6
Q

Endogenous opioid peptides act through 3 types of opioid receptors:

A

1) Mu (μ)
2) Delta (δ)
3) Kappa (κ)

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7
Q

Which receptors function as supraspinal and spinal analgesics?

A

1) Mu (μ)
2) Delta (δ)
3) Kappa (κ)

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8
Q

What are the other functions of the Mu (μ) receptors?

A

1) Sedation
2) Inhibition of respiration
3) Slowed GI transit
4) Modulation of hormone & neurotransmission release

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9
Q

List the affinity of the Mu (μ) receptors toward the endogenous opioid peptides (from highest to lowest).

A

Endorphins > Enkephalins > Dynorphins

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10
Q

List the affinity of the Delta (δ) receptors toward the endogenous opioid peptides (from highest to lowest).

A

Enkephalins > Endorphins > Dynorphins

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11
Q

List the affinity of the Kappa (κ) receptors toward the endogenous opioid peptides (from highest to lowest).

A

Dynorphins > Enkephalins & Endorphins

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12
Q

What are the other functions of the Delta (δ) receptors?

A

Modulation of hormone & neurotransmission release

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13
Q

What are the other functions of the Kappa (κ) receptors?

A

1) Slowed GI transit

2) Psychotomimetic effects

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14
Q

What is the approximate equivalent dosage of morphine (in mg)?

A

10mg (Higher doses = respiratory depression and death)

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15
Q

What is the approximate equivalent dosage of Hydromorphone (in mg)?

A

1.5mg

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16
Q

What is the approximate equivalent dosage of Meperidine/Pethidine (in mg)?

A

60-100mg

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17
Q

What is the approximate equivalent dosage of Fentanyl (in mg)?

A

0.1mg

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18
Q

What is the approximate equivalent dosage of Sufentanyl (in mg)?

A

0.02mg

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19
Q

What is the approximate equivalent dosage of Codeine (in mg)?

A

30-60^4

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20
Q

What is the Oral:Parenteral potency ratio for Morphine?

A

Low

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21
Q

What is the Oral:Parenteral potency ratio for Hydromorphone?

A

Low

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22
Q

What is the Oral:Parenteral potency ratio for Meperidine/Pethidine?

A

Medium

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23
Q

What is the Oral:Parenteral potency ratio for Fentanyl?

A

Low

24
Q

What is the Oral:Parenteral potency ratio for Sufentanyl?

A

Parenteral only

25
Q

What is the Oral:Parenteral potency ratio for Codeine?

A

High

26
Q

Which drugs are VERY potent and used during anesthesia?

A

1) Fentanyl

2) Sufentanyl

27
Q

Most opioid analgesics are well absorbed when given by which routes?

A

1) Subcutaneous
2) Intramuscular
3) Oral

28
Q

Which opioid undergoes extensive first-pass metabolism?

A

Morphine

29
Q

Which opioid has reduced first-pass metabolism?

A

Codeine

30
Q

Where do opioids concentrate?

A

In highly perfused tissues, like:

1) Brain
2) Lung
3) Liver
4) Kidneys
5) Spleen

31
Q

Where are opioids low in concentration?

A

Skeletal muscle (But it serves as a reservoir because of its large size)

32
Q

What can frequent high dose administration or continuous infusion of highly lipophilic opioids (fentanyl) lead to?

A

Accumulation in body fat

33
Q

Morphine is converted into:

A

Glucuronide metabolites

34
Q

Morphine-3-glucuronide (M3G) has which kind of properties and through which receptor?

A

Neuroexcitatory properties; GABA/glycinergic system (NOT through μ receptors)

35
Q

Which has more analgesic potency: Morphine-6-glucuronide (M6G) (10%) or Morphine?

A

Morphine-6-glucuronide (M6G) (10%) is 4-6 times more potent.

36
Q

Can opioids cross the BBB?

A

They are polar and have limited ability to cross it.

37
Q

What causes opioids to accumulate? What are the results?

A

Renal dysfunction; May result in adverse effects (seizures with M3G, and prolonged opioid action with M6G).

38
Q

What can enhance uptake of M3G (and M6G)

A

Probenecid or inhibitors of P-glycoprotein

39
Q

Hydromorphone is converted into:

A

3-glucuronide (H3G)

40
Q

What properties does 3-glucuronide (H3G) have?

A

CNS excitatory properties.

41
Q

Esters (heroin, remifentanil) are rapidly hydrolyzed by __ into:

A

Tissue esterases; Heroin

(diacetylmorphine) is hydrolyzed to morphine.

42
Q

How are meperidine (pethidine), fentanyl, alfentanil, and sufentanil metabolized?

A

Hepatic oxidative metabolism

43
Q

Accumulation of the demethylated metabolite of meperidine, normeperidine, may occur in:

A

Patients with renal dysfunction = seizures.

44
Q

Fentanyl N-dealkylation is catalyzed by:

A

CYP3A4

45
Q

Codeine is metabolized by __ to __.

A

CYP2D6; morphine.

PMs vs EMs

46
Q

What is the mechanism of opioid agonists?

A

Binding to 3 specific G protein-coupled receptors, located in the brain and the spinal cord regions involved in transmission and modulation of pain. These receptors are μ, δ, and κ, which may have subtypes.

47
Q

Opioid analgesics have 2 direct G protein coupled actions:

A

1) They close voltage-gated Ca2+ channels on presynaptic nerve terminals = reduce transmitter release (large number of neurotransmitters - glutamate, acetycholine, norepinephrine, serotonin and substance P).
2) They hyperpolarize and thus inhibit postsynaptic neurons by opening K+ channels.

48
Q

The majority of the clinically available opioid analgesics act primarily at which receptor?

A

μ opioid receptor

49
Q

What properties of morphine does the μ opioid receptor mediate?

A

1) Analgesic
2) Euphoriant
3) Respiratory depressant
4) Physiologic dependence

50
Q

Which compounds show preference for κ receptors?

A

1) Butorphanol

2) Nalbuphine

51
Q

What are the effects of Butorphanol and Nalbuphine (κ receptors)?

A

1) Analgesia
2) Dysphoria
3) Reduced respiratory depression and propensity for addiction and dependence

52
Q

What are the sites of action of opioid analgesics on the afferent pain transmission pathway?

A

1) Direct action of opioids on
inflamed or damaged peripheral tissues.
2) Inhibition in the spinal cord.
3) Possible sites of action in the thalamus.

53
Q

Opioids exert a powerful analgesic effect directly on:

A

The spinal cord = spinal action.

54
Q

What are the results of direct application of opioid agonists to the spinal cord?

A

1) Provides regional analgesia
2) Reduces the undesired respiratory depressant effect, nausea, vomiting, and sedation that may occur from the supraspinal action of systemic opioids.

55
Q

Sites of action of opioids on
pain-modulating neurons in
the midbrain and medulla
include:

A

1) The midbrain periaqueductal gray area
2) Rostral ventral medulla
3) The locus caeruleus

CNS Pharma (7 decks)

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