Drug Absorption Flashcards

1
Q

what is the pharmaceutical phase of drug dosage?

A

disintegration of the dose, dissolution of the drug

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2
Q

what is pharmaceutical availability?

A

the drug now being available for absorption after dissolution

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3
Q

what is the pharmacokinetic phase?

A

absorption, distribution, metabolism and excretion

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4
Q

what is pharmacological availability?

A

the drug is now available for action

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5
Q

what is the pharmacodynamic phase?

A

the drug and receptor interaction that causes the effect

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6
Q

after what stages can metabolic inactivation occur?

A

after absorption or after the drug pools inside the body

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7
Q

what follows metabolic inactivation?

A

excretion

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8
Q

what are the 3 options that the drug can take effect following pooling?

A

metabolic activation, tissue storage or targeting the site of action

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9
Q

what determines the peak activation?

A

the balance of absorption and elimination

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10
Q

how is the therapeutic range created?

A

the dosage being maintained by administrating a series of doses after a specific time

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11
Q

what is the toxic and ineffective range?

A

toxic range is above the therapeutic window and the ineffective range is below

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12
Q

what is the minimum effective concentration?

A

the lowest concentration while still having effect

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13
Q

what is the maximum safe concentration?

A

the highest concentration that can be given while still being safe

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14
Q

how do you calculate the therapeutic index?

A

MSC/MEC

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15
Q

what is an example of a drug that has a narrow therapeutic window?

A

warfarin

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16
Q

what routes of administration are enteral?

A

oral, rectal and sublingual

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17
Q

what routes of administration are parenteral?

A

injected doses, inhaled, transdermal and topical

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18
Q

what are the benefits of oral administration?

A

convenient, economical, non-painful, portable, can be removed

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19
Q

what are the cons of oral administration?

A

need patient concordance and variable absorption

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20
Q

what is bioavailability?

A

the proportion of the drug dosage that enters the systemic circulation

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21
Q

what things hinder bioavailability?

A

destroyed in stomach or intestine, drug may not be absorbed, destroyed by gut wall or the liver

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22
Q

what is first-pass metabolism?

A

drug passes through the intestinal wall and goes to the liver via the portal vein, where the liver extracts and metabolises some of the drug

23
Q

what are some drugs that undergo a high amount of first-pass elimination?

A

glyceryl trinitrate, lignocaine, morphine and propranolol

24
Q

what are the advantages for rectal administration?

A

useful in presence of vomiting, reduces first-pass elimination

25
Q

what is an advantage of sublingual administration?

A

enables the drug to bypass the gut wall and the liver

26
Q

what are the different types of injected administration?

A

intradermal, subcutaneous and intramuscular

27
Q

what are the types of injected/infused administration?

A

intravenous, intra-arterial, intracardiac, intraperitoneal or intrathecal

28
Q

what is intra-arterial administration good for?

A

chemotherapy

29
Q

what is intra-peritoneal administration?

A

injection into the peritoneal cavity of the abdomen

30
Q

what is intrathecal administration? how can it be useful?

A

direct access to the spinal fluid, enables access to the blood brain barrier with antibiotics

31
Q

what are the types of inhaled medication?

A

systemic effecting or topical effecting

32
Q

what are types of systemic or topical effecting medication?

A

anaesthetics and bronchodilators

33
Q

why might topical administration used?

A

applied directly to the skin or mucous membrane for local effect

34
Q

what is the definition of drug absorption?

A

the process of incorporation of a drug into the blood stream

35
Q

what properties does a drug need to have to pass through the membrane?

A

able to dissolve in an aqueous environment as well as being lipid soluble

36
Q

what are the 4 ways that drugs cross membrane barriers?

A

direct diffusion, carrier-mediated, diffusion through pores and pinocytosis

37
Q

what is pinocytosis useful for?

A

macromolecules

38
Q

what factors effect diffusion?

A

surface area, concentration, molecular size and lipid solubility

39
Q

how does molecular size effect diffusion?

A

smaller molecules are more mobile and so they diffuse faster

40
Q

what is more important, molecular size or lipid solubility and why?

A

lipid solubility as molecular size doesn’t vary very much in drugs

41
Q

how does lipid solubility effect diffusion?

A

lipid solubility effects the substances ability to penetrate the membrane

42
Q

how do you calculate the lipid solubility coefficient?

A

concentration in oil/concentration of water

43
Q

what does a high lipid solubility coefficient mean?

A

the higher the value the higher the lipid solubility

44
Q

what molecules are lipid soluble?

A

gases, non-polar molecules, and small polar molecules

45
Q

what molecules are not lipid soluble?

A

ions and large polar molecules

46
Q

what are the features of non-polar drug molecules?

A

electrons evenly distributed, dissolve in lipids and penetrate membranes

47
Q

what are the features of polar drug molecules?

A

positive and negative, the more polar the molecule the lower the lipid solubility and higher the water solubility

48
Q

can the ionised or unionised form of a drug be absorbed and why?

A

unionised as it is lipid soluble

49
Q

what is a weak acid?

A

a neutral molecule that can dissociate into an anion and a hydrogen atom

50
Q

how does the ionisation of a weak acid change at a low pH?

A

the more acidic the more H atoms there are and so the molecules are in the ionised form as a full molecule

51
Q

what environments would favour the absorption of a weak acid?

A

acidic as this causes them to be unionised

52
Q

what is a weak base?

A

neutral molecule that can form a cation by combining with a hydrogen ion

53
Q

in what state is a weak base ionised?

A

when combined with a hydrogen ion

54
Q

what environments favour the absorption of a weak acid and why?

A

alkaline environment as less H atoms at a higher pH which causes dissociation so that it becomes unionised