Pharmacokinetics- Drug transfer and absorption Flashcards

1
Q

What is F

A

Bioavailability

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2
Q

What is V

A

Volume of distribution

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3
Q

What is CL

A

Drug clearance

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4
Q

What does a change in absorption lead to

A

Change in area under curve
Tmax
F (bioavailability)

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5
Q

How will change In distribution affect drug

A

Many drugs bind to plasma proteins. If change in plasma conc of albumin, can change pharmacokinetics. Liver disease means less albumin. Will decrease binding of albumin with drug and affect elimination of drug

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6
Q

How will change in elimination of drug affect elimination of drug

A

AUC
CL
T1/2

if patient is renally impaired, decrease clearance of drug and increase the half life and so increase pharmacokinetic impact of the drug (shown by area under curve)

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7
Q

How do most drugs move across membranes

A

Passive diffusion

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8
Q

What is pKa and what does It mean

A

Ionisation constant

-pH ar which drug is charged:uncharged is 50:50

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9
Q

What does it mean if pH is at pKa value

A

Then charged:uncharged is 50:50

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10
Q

What happens if a weak acid goes to a decreasing pH environment

A

It turns to uncharged drug so promotes the drug going across the lipid bilayer

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11
Q

What happens if a weak base goes to a decreasing pH environment

A

Shift the equilibrium which favours the charged species which cannot be absorbed

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12
Q

Where are weak acids mainly absorbed

A

Stomach and intestines

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13
Q

Where are weak bases mainly absorbed

A

Intestine

negligible absorption in stomach

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14
Q

which drugs are likely/unlikelyto enter the brain easily

A

Weak acids unlikely so use these if you don’t want the drug to have an effect on the brain

Weak bases likely to enter the brain

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15
Q

What happens to acids and bases in the stomach

A

Weak acids- predominantly unionised and absorbed

Weak bases- predominantly ionised and absorbed

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16
Q

What is absorption like in acid stable drugs vs acid labile drugs

A

Stable- Slowed absorption

Labile- Stay linger and so more readily broken down

17
Q

How are PPIs given

A

They are given in gastroresistant tablets because they are acid labile

18
Q

How to PPIs act on stomach

A

DOn’t get broken down in stomach. Enter duodenum, and capsule degrades. Enters blood stream. Acts systemically to inhibit PPs in parietal cells in stomach

19
Q

What is first pass metabolism and how does this affect bioavailability

A

Drug absorbed from small intestines go to liver via hepatic portal vein. Some drugs are metabolised by liver before reaching systemic circulation

-If drug has extensive First pass metabolism, bioavailability is decreased

20
Q

What is buccal absorption

A

Under tongue for rapid absorption and also avoids first pass metabolism (e.g. GTN used for angina pain)

21
Q

What is percutaneous absorption

A

Patches on skin and drug is absorbed because dermis is permeable