Drug absorption Flashcards

1
Q

What does ADME stand for

A

Absorption
Distribution
Metabolism
Excretion

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2
Q

What is absorption

A

The process by which unchanged drug enter the circulation

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3
Q

What is distribution

A

Diversion of a drug among fluids and tissues of the body

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4
Q

What is metabolism

A

Transformation of a drug into daughter compound(s)

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5
Q

What is excretion

A

Removal of drugs/metabolites from the body

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6
Q

What happens when the route of administration for a drug changes

A

Different barriers to absorption

Different bioavailability and onset

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7
Q

Oral administration

A
  • many barriers
  • Digestive enzymes
  • All drugs funnelled through the hepatic portal vein and therefore into the liver
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8
Q

Intravenous injection

A
  • No barrier

- No drug is lost

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9
Q

Tropical cream

A

-Direct administration

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10
Q

Inhalers

A
  • Direct delivery to the lungs
  • Helps with the safety profile as it doesn’t need to reach the level of concentration in the systemic circulation which might have toxic effects
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11
Q

Why is the choice of delivery a compromise

A
  • Speed of onset
  • Convenience
  • Bioavailability; proportion of administered drug reaching the systemic circulation
  • Side effects
  • Specificity of action
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12
Q

What is transcellular absorption

A

Drug travels through cells

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13
Q

What is paracellular absorption

A

Drug travels in-between cells

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14
Q

How can absorption occur from the most common to the least common

A
  1. Passive diffusion
  2. Facilitated diffusion
  3. Active transport
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15
Q

What is Fick’s law

A

Rate of diffusion = Surface area * concentration difference * permeability

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16
Q

How does permeability vary

A

Molecular size, lipid solubility, presence of charged or ionisable groups

17
Q

Why are most drugs ionisable

A

Since they are normally either weak acids or weak bases

18
Q

What is a weak acidic drug

A

A proton donor

19
Q

What is a weak basic drug

A

A proton acceptor

20
Q

What does the extent of ionisation depend on

A

The pH of the environment

21
Q

What type of medicines are absorbed mot effectively

A

Uncharged, non-ionisable and lipophilic drugs

22
Q

What drugs are absorbed least effectively

A

Charged and ionised drugs

23
Q

What does the Henderson-Hasselbalch equation show

A

The position of the equilibrium, showing the extent of ionisation

24
Q

How is pH calculated for acidic drugs

A

pH = pKa - log [non-ionised] / [ionised]

25
Q

How is pH calculated for basic drugs

A

pH = pKa + log [non-ionised] / [ionised]

26
Q

When does pH = pKa

A

When the drug is 50% ionised

27
Q

How does more of the acidic drug stay unionised

A

As the pH becomes more acidic

28
Q

How does more of the basic drug stay unionised

A

As the pH becomes more alkaline

29
Q

What are the lipinski rules

A

An-orally active drug has no more then one violation of the following

  1. Molecular weight < 500
  2. No more then 5 H-bond donors
  3. No more then 10 H-bond acceptors
  4. Log p < 5 (partion coefficient)