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Principles of disease JK > Drug absorption > Flashcards

Drug absorption Flashcards

1
Q

How many people are harmed by healthcare?

A

1 in 10

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2
Q

Pharmaceutical

A

Get drug into the patient

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3
Q

Pharmacokinetic

A

Get drug to site of action - what body does to the drug

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4
Q

Pharmacodynamic

A

Produce correct pharmacological effect - what drug does to the body

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5
Q

Pharmacokinetics 4 letters

A

Absorption
Distribution
Metabolism
Excretion

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6
Q

What does pharmacokinetics allow the understanding of?

A

Dosage, drug handling, harm potential, drug administration and patient variability

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7
Q

Absorption

A

Blood must enter the bloodstream and be distributed to site of action to have biological action
The process of movement of unchanged drug from site of administration to systemic circulation

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8
Q

Oral

A

Always consider purpose and site of drug, effects, speed, reliability etc

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9
Q

IV

A

Small volume and depends on blood flow to site, right into blood

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10
Q

Subcutaneous

A

For example an insulin injection

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11
Q

Intramuscular

A

Vaccines in deltoid and water soluble better

Avoid 1st pass metabolism

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12
Q

Other GI

A

Rectal, sublingual - under tongue to avoid 1st pass metabolism

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13
Q

Inhalation and nasal

A

Better for volatile agents
Metabolism in lungs
5-10% absorbed

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14
Q

Transdermal

A

Avoids first pass metabolism but few substances well absorbed eg nicotine patches

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15
Q

Plasma concentration and therapeutic response

A

Always a correlation

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16
Q

Therapeutic range

A

Drug active over a range if concentrations

17
Q

What is above the therapeutic range?

A

Toxicity

18
Q

What is below the therapeutic range?

A

No or insufficient pharmacological action

19
Q

Therapeutic index

A

Range at which a drug is safe and active

20
Q

Tmax

A

Time to peak concentration ( rapid rate of absorption decreases this)

21
Q

Cmax

A

Peak concentration ( increase dose increase c max)

22
Q

What does AUC show?

A

Area under the curve equivalates to the amount of drug reaching the systemic circulation

23
Q

Bioavailability

A

Amount of drug in system/circulation which is ready for action
IV = 100%

24
Q

First pass metabolism

A

Metabolism of any drug prior to reaching systemic circulation and is a limit for the oral route
Metabolism by acid/enzyme in lumen gut wall and liver

25
Q

Formulation

A

Slow release preparations

26
Q

GI effect

A

Food
Illness - malabsorption and diarrhoea eg coeliac disease, migraine reduce stomach emptying
Gut motility - gastric absorption

27
Q

Pass physiological barrier

A

Particle size
Lipid solubility
pH and ionisation

28
Q

Ionisation (4 points)

A
  • Most drugs do not completely ionise in water
  • Most drugs are weak acids or bases
  • Ionised drugs DO NOT cross the membrane
  • Unionised distribute until equilibrium
29
Q

What does the degree of dissociation depend on?

A

Environmental pH

30
Q

Ion trapping

A

Acidic drug will be more concentrated in the compartment with high pH

31
Q

What do proton pump inhibitors do?

A

Reduce the amount of acid made in the stomach

32
Q

What do antacids do?

A

Neutralise the acid made by the stomach?

33
Q

Lipid solubility

A

Drug must be in solution and lipid soluble

34
Q

Lipid - water partition co efficient

A

Ability of drug to diffuse across lipid barrier
Ratio of amount of drug dissolve lipid: water phase
Lipid soluble reach brain, testes, liver, ovaries
Not lipid soluble not absorbed eg gentamicin

35
Q

What does passive diffusion depend on?

A

Lipid solubility and degree of ionisation

Not saturated as no proteins used to occupy

36
Q

Active absorption

A

Specific, unusual, saturable and requires a carrier +energy
Eg iron upake by brain
Drugs must resemble naturally occurring compound

37
Q

Facilitated diffusion

A

No energy needed but carrier is so is saturable

38
Q

Filtration/bulk flow

A

Channels in membrane - low molecular size
Pressure differences across membrane drives it
Usually water soluble drugs eg ammonia, water
Real excretion, remove drug from CSF and enter the liver

Principles of disease JK (26 decks)

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