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ICPP > ICPP 7 > Flashcards

ICPP 7 Flashcards

1
Q

What are the major routes of drug delivery?

A 
Oral
Intravenous 
Intramuscular
Transdermal
Intranasal
Sublingual
Subcutaneous 
Inhalation
Rectal
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2
Q

Where does most enteral drug absorption take place?

A

Small intestine

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3
Q

What is parenteral drug administration?

A

Delivery via other route not involving GI

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4
Q

The pH of the small intestine is weakly acid, how does this affect drugs?

A

Determines ratio of molecules in ionised and unionised state

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5
Q

What are the 4 major absorption mechanisms?

A

Passive diffusion
Facilitated diffusion
Active transport
Pinocytosis

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6
Q

What drugs are able to absorb via passive diffusion?

A

Lipophilic drugs - steroids

Drugs that are weak acids or weak bases

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7
Q

Can ionised drugs diffuse through the lipid bilayer?

A

No, only the unionised form.

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8
Q

What equation can you use to determine the ratio of ionised:unionised drug?

A

Henderson-hassleback equation

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9
Q

What molecules can diffuse by facilitated diffusion?

A

Charged molecules with low lipid solubility

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10
Q

What transports are widely expressed commonly used for facilitated transport?

A

Solute carrier transport (SLC)

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11
Q

What are the 2 types of SLC?

A

Organic anion transporters

Organic cation transporters

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12
Q

What molecules are absorbed by endocytosis and exocytosis?

A

large molecules

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13
Q

What are some GI factors affecting drug absorption?

A 
SA
Length
Density of SLC expression
Blood flow 
Gi motility 
Food presence
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14
Q

Where does first pass metabolism occur?

A

in liver

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15
Q

What affect does first pass metabolism have on bioavailability?

A

Decreases

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16
Q

Define bioavailability.

A

The relative amount of the drug that reaches the greater systemic circulation.

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17
Q

What enzymes are responsible for phase 1 metabolism?

A

CYP450 enzymes

18
Q

What enzymes are responsible for phase II of metabolism?

A

Conjugating enzymes

19
Q

What is the first stage of drug distribution?

A

Bulk flow via arterial system

20
Q

How does blood flow affect rate of delivery?

A

Drugs will reach well vascularised organs more rapidly

21
Q

What other factors affect distribution?

A

Capillary permeability - varies

22
Q

How does plasma protein binding affect drug absorption?

A

Protein-bound drugs are unable to diffuse across membranes and unable to bind receptors. Decrease bioavailability

23
Q

What are the body fluid compartments?

A

Plasma water
Extracellular = plasma water + interstitial fluid
Total body = plasma + interstitial fluid + intracellular

24
Q

What is the ‘apparent’ volume of distribution?

A

Describes how the drug will distribute within the body compartments

25
Q

What does a small Vd indicate?

A

Less penetration of interstitial and intracellular compartments

26
Q

What does a large Vd indicate?

A

Greater penetration into interstitial and intracellular compartments

27
Q

What can Vd be affected by?

A

Renal failure, pregnancy, changes in blood flow

28
Q

What do phase I and II enzymes do?

A

Increase the ionic charge in order to increase renal elimination

29
Q

What sort of reactions does Phase I metabolism involve?

A

redox
Aklylation
Hydroxylation

30
Q

What sort of reactions does Phase II involve?

A

Sulhation, glururonidation

31
Q

What enzyme does grapefruit juice inhibit?

A

CYP3A4

32
Q

What enzyme metabolises verapamil?

A

CYP3A4

33
Q

Codeine is a prodrug, activated by which CYP enzyme?

A

CYP2D6

34
Q

Where does most drug elimination take place?

A

Kidney

35
Q

What are the 3 processes that take place during renal elimination?

A
  1. Glomerular filtration
  2. Active tubular secretion in proximal tubule -OAT and OCT transport drug into tubule
  3. Passive tubular resorption of lipophilic drugs in distal tubule
36
Q

What is clearance?

A

The rate of elimination of a drug from the body

Total body clearance = hepatic clearance + renal clearance

37
Q

What is half life, t 1/2?

A

The amount of time which the concentration of a drug in plasma decrease to one half of its original concentration.

38
Q

What influences t 1/2?

A

Vd and total clearance

39
Q

What is first order kinetics?

A

Linear relationship where the rate of metabolism and excretion is proportional to the concentration of druhg

40
Q

What happens when elimination processes are saturated?

A

They become rate-limited and kinetics show zero-order.

41
Q

What are the consequences of zero order kinetics?

A

More likely to have ADR’s and toxicity

ICPP (7 decks)

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