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Principles > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

pharmacodynamics

A

what a drug does to the body

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2
Q

pharmacokinetics

A

what the body does to a drug

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3
Q

what is selectivity?

A

the ability of a drug to distinguish between different molecular targets within the body

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4
Q

what do targets generally include?

A

targets that are unique to invaders and are not on eukaryotic human cells

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5
Q

what regulatory proteins do drugs bind to to modify their function?

A

enzymes, carrier molecules, ion channels, receptors

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6
Q

what does an agonist do

A

binds to a receptor to produce a cellular response

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7
Q

what does an antagonist do?

A

a drug that reduces or blocks the actions of an agonist by binding to the same receptor

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8
Q

what is selectivity dependant on?

A

the dose of a drug

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9
Q

what are receptors made of?

A

protein, or glycoprotein, macromoles

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10
Q

what are ligand-gated ion channels targeted by?

A

hydrophilic signalling molecules (fast neurotransmitters such as acetyl choline)

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11
Q

what are G protein-coupled receptors also know as?

A

metabotropic receptors

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12
Q

what are G protein-coupled receptors targeted by?

A

hydrophilic signal molecules (slow neurotransmitters such as acetyl choline, amino acids, peptide hormones)

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13
Q

what forms ion channels?

A

glycoproteins

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14
Q

what can ion channels be gated by?

A

chemical signals (ligand-gated), transmembrane voltage (voltage-gated) and physical stimuli (thermal and mechanical energy)

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15
Q

classic example of ligand-gated ion channels?

A

the nicotinic acetylcholine receptor of skeletal muscle and neurones

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16
Q

what does the nicotinic acetylcholine receptor look like?

A

consists of separate glycoprotein subunits that form a central ion conducting channel

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17
Q

most cell surface receptors signal via what?

A

second messenger systems

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18
Q

structure of G protein-coupled receptors? chemical

A

single polypeptide with extracellular NH2 and intracellular COOH termini

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19
Q

what does the G protein-coupled receptor contain?

A

seven transmembrane a-helical spans joined by 3 intracellular loops

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20
Q

what type of protein is a G protein? think location

A

peripheral membrane protein

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21
Q

what does a G protein consist of?

A

3 polypeptide subunits (alpha, beta and gamma)

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22
Q

what binding site does the G protein have and what does it allow?

A

a guanine nucleotide binding site in the alpha subunit that can hold guanine triphosphate or guanine diphosphate

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23
Q

how are G proteins activated?

A

they are activated via agonist binding to the GPCR to which they preferentially couple

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24
Q

what occupies the guanine nucleotide binding side in the non-active state of the G protein?

A

GDP

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25
Q

what occupies the guanine nucleotide binding side in the active state of the G protein?

A

GTP. The alpha and beta subunits dissociate from each other

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26
Q

what does the activation of the GPCR activate?

A

A G protein

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27
Q

example of signalling that uses receptor kinases

A

insulin sigalling

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28
Q

example of signalling that uses ligand-gated transcription factors

A

nuclear receptors and steroid hormones

29
Q

what is drug metabolism?

A

drug transformation by metabolism by the liver and other tissues

30
Q

what can drugs be excreted by?

A

in urine, faeces or bile

31
Q

what is bulk flow?

A

the movement of drugs around the body via the circulatory system

32
Q

what type of drugs are more likely to diffuse across the lipid bilayer?

A

lipid soluble drugs

33
Q

what are aqueous pores formed by?

A

aquaporin

34
Q

what type of drugs cross the cell membrane via passive diffusion?

A

lipid soluble drugs

35
Q

how do small molecules cross the cell membrane by facilitated diffusion?

A

via specialised carrier proteins. The binding of the drug on the protein causes a conformational change which allows the drug to diffuse across the membrane

36
Q

how do small molecules travel with active transport

A

via specialised carrier proteins

37
Q

what does saturation kinetics mean?

A

any process that has a limiting factor (limited number of specialised carrier)

38
Q

what are the principle sites of carrier mediated drug transport? (facilitated dissuion and active transport) 5

A

blood brain barrier, gastrointestinal tract, placenta, renal tubule and binary tract

39
Q

what type of drug is endocytosis used for?

A

transporting large drugs across the cell membrane (vitamin B12)

40
Q

what is the pKa?

A

the pH at which 50% of the drug is ionised and 50% of the drug is un-ionised

41
Q

can the non-ionised form of a drug permeate the membrane?

A

for many drugs, yes

42
Q

what compartments do weak bases accumulate in?

A

compartments with low pH

43
Q

what compartments do weak acids accumulate in?

A

compartments with high pH

44
Q

what type of pH do weak acids need to be absorbed?

A

low pH

45
Q

what type of pH do weak acids need to be absorbed?

A

high pH

46
Q

where does most oral drug absorption occur?

A

in the small intestine due to the large surface area

47
Q

what is the apparent volume of distribution? Vd

A

The extent to which a drug partitions between the plasma and tissue compartments

48
Q

what is the equation for volume of distribution?

A

Vd = Dose/ [drug]plasma

49
Q

what type of drugs find it more difficult to cross membranes and what does this do to the Vd?

A

hydrophilic and ionised drugs, Vd is closer to total body volume of water (41L)

50
Q

what type of drugs easily cross membranes and what does this do to the Vd?

A

lipophilic drugs. Vd is generally greater than total body volume (41L)

51
Q

what does a large Ka mean?

A

acid is strong

52
Q

what is the most abundant plasma protein?

A

albumin

53
Q

what is the effect of plasma protein binding on drug affinity?

A

it reduces the availability of the drug for diffusion to the drug target organ

54
Q

define drug metabolism ?

A

enzymatic conversion of the drug to another chemical entity

55
Q

what is the most important drug metabolising organ

A

the liver

but also the kidney, gut mucosa, lungs and skin

56
Q

when administered by the enteral (oral) route, metabolism in the liver…

A

REDUCES THE BIOAVAILABILITY OF DRUGS

57
Q

what is the bioavailability of the drug?

A

the systemic circulation of drug that is available

58
Q

where do the two phases of drug metabolism happen?

A

primarily in the liver

59
Q

where are hepatic drug-metabolising enzymes found?

A

embedded in the smooth endoplasmic reticulum of liver hepatocyes

60
Q

what changes in the drug can happen in phase 1

A

oxidation (most common), reduction or hydrolysis

61
Q

what do phase 1 metabolism reactions usually produce?

A

chemically reactive metabolites that can be pharmacologically active and or toxic

62
Q

what happens when people lack P450 activity?

A

higher drug plasma levels (adverse reactions)

63
Q

what happens when people have too much P450 activity?

A

lower drug plasma levels which reduces drug action

64
Q

what happens during phase 2 metabolism reactions?

A

drug combines with one of several polar molecules to form a water-soluble metabolite that can be readily excreted via the kidney

65
Q

what are the principal organs for drug elimination?

A

the kindneys, by renal filtration of blood plasma

66
Q

during renal filtration, what is reabsorbed into blood circulation by renal tubules?

A

water and most electrolytes

67
Q

what drug things are rendered polar by phase 2 metabolism and excreted in the urine?

A

drug metabolites that are not reabsorbed

68
Q

what is clearance? (CL)

A

an expression for the elimination

Principles (11 decks)

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