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301 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What does a successful drug need?

A

Efficacy
ADME
Safety

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2
Q

Three phases of drug action?

A

Pharmaceutical
Pharmacokinetic
Pharmacodynamic

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3
Q

What does drug dissolution in the body depend on?

A

pH of the medium and pH of the site of dissolution

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4
Q

Where do acidic drugs dissolved best?

A

Alkaline areas

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5
Q

What does alkaline drugs dissolve best?

A

Acidic areas

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6
Q

What physiochemical properties affect dissolution of a drug?

A

Ionisation
Lipophilicity

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7
Q

Ways drugs can be absorbed across the GI tract?

A

Paracellular transport
Transcellular transport
Carrier-mediated transport
P-gp mediated efflux

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8
Q

Which drug absorption processes are passive?

A

Paracellular
Transcellular

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9
Q

What is transcellular drug absorption?

A

Directly through a cell

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10
Q

Speed of transcellular drug absorption?

A

Fast

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11
Q

Where can transcellular drug absorption occur?

A

All the way along the GI tract

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12
Q

What properties does a drug need to undertake paracellular absorption?

A

Lipid soluble
Unionised

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13
Q

What is paracellular drug absorption?

A

Via aqueous pores between cells

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14
Q

Speed of paracellular transport?

A

Slower

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15
Q

What can paracellular absorption take place?

A

Only the small intestine

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16
Q

What is carrier-mediated drug absorption?

A

Drug uses a membrane carrier system

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17
Q

What properties of a drug are needed to undertake carrier-mediated absorption?

A

Some polar molecules
Particularly if they resemble endogenous compounds

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18
Q

Example of a drug that uses carrier-mediated transport and why?

A

Methotrexate as it is structurally similar to folic acid so it can be transported by the folate membrane transport system

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19
Q

Physiochemical properties that affect drug absorption?

A

Ionisation
Lipophilicity
Size and shape

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20
Q

Important plasma proteins in drug distribution?

A

albumin
acid-glycoprotein
beta-globulin.

21
Q

What can affect the distribution of a drug?

A

Plasma protein binding
BBB
Adipose tissues
Desired site of action

22
Q

Drugs bound to plasma proteins are active or inactive?

A

Inactive

23
Q

What kind of drugs mainly bind to albumin?

A

Acidic

24
Q

What kind of drugs mainly bind to acid-glycoprotein?

A

Basic

25
Q

Are acidic or basic drugs more likely to be plasma protein bound?

A

Acidic

26
Q

Physiochemical properties that affect drug distribution?

A

Ionisation
Lipophilicity
Shape and size

27
Q

Physiochemical properties of drugs that affect metabolism?

A

Lipophilicity

28
Q

Where are lipophilic compounds usually excreted?

A

Bile

29
Q

What kinds of drugs are expected to be excreted in the urine?

A

Soluble in water at urine pH
Suitable size to pass glomerulus membrane

30
Q

Physicochemical properties of drugs that affect excretion?

A

Ionisation
Lipophilicity
Shape and size

31
Q

Physicochemical properties that affect a drug binding to the site of action?

A

Ionisation
Lipophilicity
Shape and size

32
Q

Why does ionization influence drug binding?

A

Electrostatic bonds
Ionic bonds
Hydrogen bonds

33
Q

Why does lipophilicity influence drug binding?

A

Hydrophobic interactions

34
Q

Why does shape and size influence drug binding?

A

VdW interactions
Repulsive interaction

35
Q

Why does changing the chemical structure of a drug affect its behaviour?

A

Change of physicochemical properties

36
Q

What parameter is used to measure hydrophobicity?

A

LogP (partition coefficient)

37
Q

Lipophilic drugs have a ….. logP?

A

High

38
Q

Hydrophilic drugs have a ….. logP?

A

Low

39
Q

Why does increasing the logP too much reduce biological activity?

A

Drug may become so hydrophobic it is poorly soluble in the aqueous phase
It may become trapped in fat depots and not reach site of action
More susceptible to metabolism and elimination

40
Q

What represents the optimum partition coefficient for biological activity?

A

LogP°

41
Q

Approximate LogP of drugs targeting the CNS?

A

2

42
Q

Example of drugs where hydrophobicity only has a slight contribution to their activity?

A

Anti-malarials

43
Q

Why does the hydrophobicity of antimalarials not have much of an effect on its biological activity?

A

It’s target is in the blood

44
Q

What is Ka?

A

The dissociation constant

45
Q

What does the dissociation constant measure?

A

The extent of ionisation at at certain pH

46
Q

What is the molecular volume?

A

Measures the steric extent
Determines transport characteristics

47
Q

What is MR?

A

Molecular refractivity

48
Q

What does molecular refractivity measure?

A

Volume occupied by an atom or group of atoms

301 (5 decks)

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