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semester 1 > Drug Absorption > Flashcards

Drug Absorption Flashcards

1
Q

Define Pharmaceutical process

A

Get the drug into the patient

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2
Q

Define Pharmacokinetic process

A

Get the drug to the site of action

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3
Q

Define Pharmacodynamic process

A

Produce the correct pharmacological effect

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4
Q

Define Therapeutic process

A

Produce the correct therapeutic effect

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5
Q

What determines drug pharmacokinetics

A

Absorption
Distribution
Metabolism
Elimination

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6
Q

What are the methods of administration?

A 
Oral
Subcutaneous 
Intramuscular
Other GI - Sublingual, rectal
Inhalation
Nasal
Transdermal
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7
Q

What does absorption involve

A

Drugs must enter blood stream and distributed to site of action

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8
Q

What does ADME allow?

A 
understanding of: 
Dosage 
Drug administration
Drug handling 
Patient variability
Potential for harm.
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9
Q

What is sublingual?

A

Under the tongue

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10
Q

Oral absorption

What is Tmax?

A

The time to peak concentration

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11
Q

Oral absorption

What is Cmax?

A

The peak concentration

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12
Q

Oral absorption

What is the (AUC)?

A

The area under the drug concentration-time curve

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13
Q

Does the dose effect the tmax?

A

No, alters cmax

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14
Q

What does the The area under the drug concentration-time curve represent?

A

The amount of drug which reaches the systemic circulation

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15
Q

What is the Therapeutic range?

A

The range of concentrations at which a drug is active.

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16
Q

What happens above or below the therapeutic range

A

Toxicity

Insufficient/no pharmalogical action

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17
Q

What does The AUC allows us to estimate?

A

BIOAVAILABILITY - extent and rate at which drug reaches systemic circulation.

18
Q

What is the bioavailability of an intravenous drug?

A

100%

19
Q

What are the factors affecting Bioavailability? (oral absorption)

A

Formulation

Ability of drug to pass physiological barriers

  • Particle size
  • Lipid solubility
  • pH and ionisation

Gastrointestinal effects
- Gut motility

First pass metabolism

20
Q

What is dissolution?

A

The rate a drug breaks up

21
Q

What is an example of a physiological barrier?

A

Transport across membranes

22
Q

What are the methods of transport across membranes?

A

Passive diffusion
Filtration
Bulk flow
Active transport

23
Q

What does the degree of the ionisation of the drug depend on?

A

pH of the environment

24
Q

What form of the drug crosses the membrane?

A

The unionised form

25
Q

What is the distribution of the un-ionised form of a drug?

A

Distribute across the membrane until equilibrium reached - equal concentration on each side.

26
Q

Where will an acidic drug be most concentrated?

A

In the compartment with high pH

27
Q

What does the Henderson-Hasselbalch equation describe?

A

The relationship between the local pH and the degree of ionisation

28
Q

What is The ability of a drug to diffuse across a lipid barrier is expressed as?

A

lipid-water partition coefficient

29
Q

What is the lipid-water partition coefficient?

A

The ratio of the amount of drug which dissolves in the lipid and water phase when they are in contact.

30
Q

What factors effect passive diffusion

A

Molecular size
Lipid solubility
Polarity
Ionisation
pH

31
Q

Describe Active Transport in drugs

A

Energy dependent
Against conc gradient
drug reversable bound to barrier system

32
Q

What is the structure of drugs that undergo active transport?

A

They must resemble naturally occurring compounds

33
Q

Describe facilitated diffusion

A 
Occurs along the concentration gradient
Require carriers

Structure specific
No energy required
34
Q

Where does filtration occur?

A

Through channels in the cell membrane.

35
Q

What is the molecular size of the drug in Filtration / Bulk Flow/ Pore Transport?

A

Low molecular size

36
Q

What is the driving force in Filtration / Bulk Flow/ Pore Transport?

A

Hydrostatic or the osmotic pressure

37
Q

What is first pass metabolism

A

Metabolism of drug before reaching systemic circulation

38
Q

What can cause first pass metabolism

A

Limit on oral drug route
Gut lumen
Gut wall
Liver

39
Q

How can first pass metabolism be avoided

A

Subcutaneous
Inhilation
Sublingual absorption
Transdermal
Rectal

40
Q

What does bio phase mean?

A

The effect site of the drug

semester 1 (65 decks)

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