C&P: Opioids Flashcards by Anna Kahn-Leavitt

Q

Opioids pH

A

All bases

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Q

Morphine: pKa

A

8.0

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Q

Morphine: relative lipid solubility

A

1 (ie relative to itself)

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Q

Morphine: relative potency

A

1 (ie relative to itself)

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Q

Morphine: protein binding (%)

A

35

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Q

Morphine: volume of distribution (L/kg)

A

3.5

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Q

Morphine: oral bioavailability (%)

A

25-30

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Q

Morphine: metabolism

A

Glucuronidation; N-demethylation

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Q

Morphine: clearance (ml/(kg*min))

A

16

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Q

Morphine: elimination rate (min)

A

170

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Q

Diamorphine: chemical composition

A

Diacetylmorphine

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Q

Diamorphine: pKa

A

7.6

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Q

Diamorphine: relative lipid solubility

A

250

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Q

Diamorphine: relative potency

A

2

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Q

Diamorphine: protein binding (%)

A

40

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Q

Diamorphine: volume of distribution (L/kg)

A

5

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Q

Diamorphine: oral bioavailability

A

low

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Q

Diamorphine: metabolism

A

ester hydrolysis to morphine

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Q

Diamorphine: clearance (ml/(kg*min))

A

3.1

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Q

Diamorphine: elimination rate (min)

A

5 (half life)

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Q

Codeine: chemical composition

A

methylmorphine

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Q

Codeine: pKa

A

8.2

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Q

Codeine: relative lipid solubility

A

n/a

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Q

Codeine: relative potency

A

0.1

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Codeine: protein binding (%)

7

Codeine: volume of distribution (L/kg)

5.4

Codeine: oral bioavailability (%)

50 (20-80)

Codeine: metabolism

Glucuronidation, demethylation (CYP2D6)

Codeine: clearance (ml/(kg*min))

23

Codeine: elimination rate (min)

170

Fentanyl: pKa

8.4

Fentanyl: relative lipid solubility

600

Fentanyl: relative potency

100

Fentanyl: protein binding (%)

83

Fentanyl: volume of distribution (L/kg)

4.0

Fentanyl: oral bioavailability (%)

33

Fentanyl: metabolism

N-Dealkylation then hydroxylation

Fentanyl: clearance (ml/(kg*min))

13

Fentanyl: elimination rate (min)

190

Fentanyl: chemical composition

Synthetic phenylpiperidines

Alfentanil: pKa

6.5

Alfentanil: relative lipid solubility

90

Alfentanil: relative potency

10-20

Alfentanil: protein binding (%)

90

Alfentanil: volume of distribution (L/kg)

0.6

Alfentanil: oral bioavailability (%)

n/a

Alfentanil: metabolism

N-Demethylation

Alfentanil: clearance (ml/(kg*min))

6

Alfentanil: elimination rate (min)

100

Alfentanil: chemical composition

Synthetic phenylpiperidines

Remifentanil: pKa

7.1

Remifentanil: relative lipid solubility

20

Remifentanil: relative potency

100

Remifentanil: protein binding (%)

70

Remifentanil: volume of distribution (L/kg)

0.3

Remifentanil: oral bioavailability (%)

n/a

Remifentanil: metabolism

Plasma and tissue esterases

Remifentanil: clearance (ml/(kg*min))

40

Remifentanil: elimination rate (min)

10

Remifentanil: chemical composition

Synthetic phenylpiperidines