3.5.3 Intro to Hepatocyte Pharmokinetics Flashcards

1
Q

How can liver disease effect drug distribution?

A

↓ liver function → ↓ albumin → drugs can’t get to target tissues

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2
Q

What are the general roles of the Liver in drug metabolism? (5)

A

Inactivates the drug

Makes it more water soluble

Can make drug more active or toxic

Can be divided into phase I and phase II reactions

primarily carried out by the hepatocyte

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3
Q

How can hepatocytes affect distribution of drugs?

A

drugs commonly bind to albumin, if liver malfunctioning, ↓ albumin → ↓ drug transport

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4
Q

What is pharmacokinetics?

A

What the body does to the drug

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5
Q

How can cirrhosis affect the metabolism of a drug?

A

less functional liver tissue also lead to portal HTN

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6
Q

What is pharmacodynamics?

A

Effect of drug on the body

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7
Q

What are the characteristics of Phase III Metabolism of drugs?

A

drug transport to various tissues, also occurs before phases 1 and 2, ABC transporters

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8
Q

What is absorption?

A

The process by which drugs enters the body

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9
Q

What is metabolism is regards to drugs?

A

enzymes modify drug to make it water soluble or activate it

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10
Q

What are the major principles of pharmacokinetics and pharmacodynamics?

A

Absorption

Distribution

Metabolism

Excretion

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11
Q

How can liver disease effect excretion of a drug?

A

Excretion – cholestatic liver disease, abnormal bile levels inhibits drug excretion

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12
Q

What is first pass metabolism?

A

drugs taken orally goes through liver before reaching target tissues, metabolism limits bioavailability of drug

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13
Q

What is excretion is regards to drugs?

A

removal from body via bile or serum, mostly by kidneys

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14
Q

How can liver disease affect absorption of a drug?

A

decreased first pass effect

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15
Q

How can liver disease affect metabolism of a drug?

A

capacity of hepatocytes is diminished, shunts → possible toxicity

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16
Q

What is the role of hepatocytes in drug excretion?

A

Hepatocytes can secrete the drug metabolite into the bile for excretion

17
Q

What is distribution?

A

Delivery of drug from systemic circulation to tissue

18
Q

What are the characteristics of Phase II drug metabolism?

A

Involved conjugation, such as glucuronic acid, which combines with the drug or phase I metabolite to form conjugate with high polarity

19
Q

What are the characteristics of phase I drug metabolism?

A

Consists of oxidation, reduction and hydrolysis reactions

Typically results in more polar

20
Q

How can portal HTN affect drug metabolism?

A

portal HTN → shunts around liver, loss of fenestrations → drug can’t enter hepatocytes

21
Q

What are the enzymes that carry out phase I drug metabolism in the liver?

A

Cytochrome p450

Flavin containing mono-oxidases

epoxide hydrolases