Drug Absorbtion 1 Flashcards

1
Q

Define Pharmaceutical Process?

A

Getting the drug into the patient

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2
Q

What is it called “getting the drug to the site of action in the patient”?

A

The pharmacokinetic process

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3
Q

What is the pharmacodynamic process?

A

Producing the correct Pharmocological effect with the drug.

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4
Q

{What is the therapeutic process?

A

Producing the intended therapeutic response?

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5
Q

What determines pharmacokinetics?
[ADME}

A

Absorption
Distribution
Metabolism
Elimination

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6
Q

Define Absorption:

A

Process of movement of unchanged drug from site of administration to sytemic circulation.

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7
Q

Try name 9 drug application routes. Go on i fucking dare you

A

Oral
Subcutaneous/Intramuscular
Inhalation/nasal
Transdermal (skin patches)
IV
Topical (creams etc)
Sublingul (under tongue)
Rectal

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8
Q

Define therapeutic range:

A

The range of blood [drug] over which a drug is active

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9
Q

What happens if drug conc. is above or below the therapeutic range?

A

If its above the range toxicity occurs
If its below the range theres insufficient pharmacological action

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10
Q

Define Therapeutic Index (TI):

A

A comparison of the drug conc. level that causes the therapeutic effect against the amount that causes toxicity.

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11
Q

What two things must you consider concernin the rate of oral absorption?

A

Amount of drug entering systemic circulation and speed at which it happens

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12
Q

What is Tmax?

A

The time to peak drug conc. in systemic circulation

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13
Q

What is Cmax?

A

The peak drug conc. in systemic circulation

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14
Q

What is the AUC?

A

The area under a drug conc vs time curve.
I.e. the amount of drug reaching circulation

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15
Q

How does increasing the dose affect Tmax & Cmax?

A

Increasing the Dose has no effect on Tmax but increases Cmax.

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16
Q

Define Bioavailability?

A

Amount of Drug reaching circulation & available for action

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17
Q

What method of drug administration has 100% bioavailability?

A

Intravenous Drugs have 100& bioavailability.

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18
Q

What 4 factors effect Bioavailability?

A
  • Formulation
  • First pass metabolism
  • Gastrointestinal effects
  • Ability of drug to pass physiological barriers.
19
Q

How does formulation affect bioavailability?

A

Some drugs are prepared for slow release

20
Q

What 3 gastrointestinal effects alter bioavailability?

A
  • Illness & Dsease
  • Gut Motility
  • Food
21
Q

What 3 areas affect the ability of a drug to pass physioloical barriers?

A
  • pH & Ionisation
  • Lipid Solubility
  • Particle Size
22
Q

Define First pass metabolism?

A

The amount of drug metabolised by the gut before it is absorbed into systemic circulation

23
Q

What does passive diffusion rely on?

A

Lipid solubility
Degree of ionisation

24
Q

Why does drug ionisation affect passive diffusion?

A

Only unionised drugs can pass through membranes as ionised arnt lipid soluble

25
What does the degree of ionisation rely on?
Local pH i.e. an acidic drug will ionise in an alkaline enviroment
26
What is the henderson-hasselbach equation used for?
The relationship between local pH and drug ionisation
27
To what degree do pH changes affect drug ionisation?
Small pH changes can cause significant changes to drug ionisation & therfore diffusion rates.
28
What is the lipid-water partition coefficient?
The ability of a drug to diffuse across a lipid barrier (ratio of drug dissovled in lipid vs water phase when in contact)
29
Exapli active absorption
Active absorption is unusual, occurs aainst the conc. gradient, is specific and requires carriers/energy.
30
Example of drugs moved by active absorption:
Iron, potassium, sodium, calcium Also levodopa uptake by the brain
31
Explain Facilitated Diffusion:
Along conc. gradient Needs carriers but not energy Mizxed order kinetics
32
Examples of drugs moved by facilitated diffusion:
Monosaccharides AminoAcids Vitamins
33
What drives filtration/bulk flow across membranes?
Hydrostatic or osmotic pressure difference across the membrane
34
How does Gut motility affect the rate of dru absorption?
The faster the gastric activity the faster the drug reaches the site of absorption
35
What effects can food have on drug absorption?
Food can enhance or impair absorption of some drugs
36
How can illness efect drug absorption?
Malabsorption can impair or inhance drug absorption rates (e..g caeliacs disease)
37
Define First pass metabolism:
Amount of drug metabolised prior to reaching the site of absorbtion
38
How is drug metabolised in first pass metabolism?
By acids/enzymes in the gut lumen By metabolic enzymes in the gut wall By Hepatic enzymes in the liver
39
What affects level of first pass metabolism:
The drug Diseases The person
40
Descrive Intravenous drug administration:
- 100% bioavailability - Avoids 1st pass metabolism
41
Describe Topical drug Administration:
- Can achieve local or systemic effects - Can achieve controlled, sustained doses of drugs - Avoids 1st pass metabolism
42
Descrive Inhalation drug administration:
- Drug delivered directly to site - Rapid effect - Small doses needed - Reduced adverse effects - Metabolised in lungs so only 5-10% is absorbed. (little systemic effecT)
43
Describe the Hendersen-Hasselbach equation:
pH = pKa + log10 (ConjugateBase/UndissociatedAcid)