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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Q

Codeine: protein binding (%)

A

7

Q

Codeine: volume of distribution (L/kg)

A

5.4

Q

Codeine: oral bioavailability (%)

A

50 (20-80)

Q

Codeine: metabolism

A

Glucuronidation, demethylation (CYP2D6)

Q

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

A

23

Q

Codeine: elimination rate (min)

A

170

Q

Fentanyl: pKa

A

8.4

Q

Fentanyl: relative lipid solubility

A

600

Q

Fentanyl: relative potency

A

100

Q

Fentanyl: protein binding (%)

A

83

Q

Fentanyl: volume of distribution (L/kg)

A

4.0

Q

Fentanyl: oral bioavailability (%)

A

33

Q

Fentanyl: metabolism

A

N-Dealkylation then hydroxylation

Q

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

A

13

Q

Fentanyl: elimination rate (min)

A

190

Q

Fentanyl: chemical composition

A

Synthetic phenylpiperidines

Q

Alfentanil: pKa

A

6.5

Q

Alfentanil: relative lipid solubility

A

90

Q

Alfentanil: relative potency

A

10-20

Q

Alfentanil: protein binding (%)

A

90

Q

Alfentanil: volume of distribution (L/kg)

A

0.6

Q

Alfentanil: oral bioavailability (%)

A

n/a

Q

Alfentanil: metabolism

A

N-Demethylation

Q

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

A

6

Q

Alfentanil: elimination rate (min)

A

100

Q

Alfentanil: chemical composition

A

Synthetic phenylpiperidines

Q

Remifentanil: pKa

A

7.1

Q

Remifentanil: relative lipid solubility

A

20

Q

Remifentanil: relative potency

A

100

Q

Remifentanil: protein binding (%)

A

70

Q

Remifentanil: volume of distribution (L/kg)

A

0.3

Q

Remifentanil: oral bioavailability (%)

A

n/a

Q

Remifentanil: metabolism

A

Plasma and tissue esterases

Q

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

A

40

Q

Remifentanil: elimination rate (min)

A

10

Q

Remifentanil: chemical composition

A

Synthetic phenylpiperidines