ADME overview Flashcards

1
Q

Absorption requires SOLUBILILZATION. TRUE OR FALSE?

A

TRUE

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2
Q

Drugs that are more hydrophilic are more likely to be dissolved than those that are hydrophobic. TRUE OR FALSE

A

TRUE

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3
Q

Ionization does not determine solubilization. TRUE OR FALSE?

A

FALSE

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4
Q

Ph does not determine rate of ionization. TRUE OR FALSE?

A

FALSE

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5
Q

What is thermodynamic solubility?

A

Refers to how soluble a drug is if left in solution to come to equilibrium

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6
Q

What is kinetic solubility?

A

Refers to how quickly a drug dissolves in solution

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7
Q

What is pinocytosis transport of drug?

A

When cell membrane invaginates the drug

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8
Q

What is Paracellular transport pf drug?

A

Transport of drug between different cells

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9
Q

What is Lipid diffusion transport of drug?

A

Movement of drug directly across cell membrane

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10
Q

What is Aquaporin transport of drug?

A

Drugs can move across ion channels

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11
Q

What is carrier transport of drug?

A

These are proteins that can transport certain drugs

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12
Q

What does fick’s law describe?

A

The flux of drug across the membrane i.e how many moles of the drug is moving across the membrane per unit time

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13
Q

Absorption is determined by POLARITY AND LIPOHILICITY. TRUE OR FALSE?`

A

TRUE

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14
Q

What re the factors affecting GI absorption?

A
  1. Anatomical factors
  2. pH
  3. Permeability and solubility
  4. Binding to other material in GI tract
  5. Gastric emptying
  6. Metabolism
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15
Q

What is permeability dependent on?

A
  1. Solubility in membrane lipid
  2. Mobility in membrane lipid
  3. Molecular mass ( Reduces permeability)
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16
Q

what is the pH partition hypothesis?

A

uncharged molecules preferentially cross membrane (there are exceptions to this)

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17
Q

what is distribution?

A

The reversible transfer of a drug between different tissues in the body

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18
Q

Many drugs exert their effect in interstitial water or intracellular water. TRUE OR FALSE?

A

TRUE

19
Q

Only unbound drug moves between compartments.TRUE OR FALSE?

A

TRUE

20
Q

Blood-brain barrier restricts access to CNS. TRUE OR FALSE?

A

TRUE

21
Q

Blood-brain barrier DOES NOT prevents
water-soluble drugs from
reaching the CNS. TRUE OR FALSE?

A

FALSE

22
Q

What are Perfusion limited drugs?

A

These are drugs where the membrane presents little permeability barrier - this is the case for lipophilic drugs

23
Q

What are permeability limited drugs?

A

Are drugs where membrane present significant permeability barrier- this is the case for polar drugs that are affected by charge

24
Q

Blood flow does not control the distribution of drug, its the permeability of the membrane to those drugs that affects their distribution. TRUE OR FALSE?

A

TRUE

25
Q

Drugs may bind to blood cells, tissue proteins and plasma protein. TRUE OR FALSE?

A

TRUE

26
Q

What does serum albumin mostly bind?

A

Acidic drugs

27
Q

What doe a1 acid glycoprotein mostly bind?

A

Basic drugs

28
Q

Only unbound drug exerts a pharmacodynamic effect. TRUE OR FALSE?

A

TRUE

29
Q

What does the one compartment model mean?

A

The drug can diffuse into all the tissues at the same time

30
Q

What does the two compartment model mean?

A

Drug can distribute into one compartment more rapidly than in another compartment

31
Q

Elimination is both metabolism and excretion. TRUE OR FALSE?

A

TRUE

32
Q

What is metabolism?

A

The conversion of drug to another chemical

33
Q

Which organ is the major site of metabolism?

A

Liver

34
Q

What occurs in Phase I in metabolism?

A

conversion to more reactive form to allow conjugation

35
Q

What occurs in Phase II in metabolism?

A

conjugation with another biomolecule to increase solubility to
allow excretion

36
Q

Some drugs may be excreted unchanged
Some drugs may not undergo phase II
ARE THESE STATEMENTS TRUE OR FALSE?

A

TRUE

37
Q

Oxidation and reduction both occurs in phase 1 of metabolism. TRUE OR FALSE?

A

TRUE

38
Q

95% of reactions does not occur by cytochrome P450. TRUE OR FALSE?

A

FALSE

39
Q

List the different types of isoforms of cyp and describe their uses.

A

3A4 - most commonly associated with drug metabolism

2D6 - shows greatest variability between different people

40
Q

Apart from cytochromes there no other enzymes that can catalyze metabolism. TRUE OR FALSE?

A

FALSE

41
Q
Biotransformation can
render a drug more
reactive:
- aids conjugation
- makes more harmful
TRUE OR FALSE?
A

TRUE

42
Q

What is Excretion?

A

the irreversible removal of drug from the

body

43
Q

List the different Routes of excretion

A
  • Urine
  • Bile
  • Sweat
  • Milk
  • Exhaled breath
44
Q

What are the Processes involved in

renal excretion?

A
  1. Filtration in Renal corpuscle
  2. Active secretion in the tubule
  3. Reabsorption in the tubule