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Body in motion > intro to pharmacology and therapeutics > Flashcards

intro to pharmacology and therapeutics Flashcards

1
Q

5 factors needed for prescribing

A

medicine, dose, route, frequency, duration

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2
Q

what is pharmacodynamics

A

the study of biochemical and physiological effects of drugs on the body
‘what the body does to the drug’

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3
Q

4 types of receptors

A

channel linked receptors
G protein coupled receptors
Enzyme-linked receptors
nuclear receptors (intracellular receptors)

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4
Q

different targets of drug action

A

receptors, ion channels, enzymes, transporters

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5
Q

4 drugs related to treatment of hypertension

A

atenolol - blocks response to noradrenaline
ramipril - prevents formation of vasoconstrictors
amlodipine - blocks calcium channels (important in vasoconstriction)
bendroflumethiazide - acts in kidneys reducing reabsorption of sodium

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6
Q

drug dose response curve?

A

work out maximum response - Emax
ED50 (effective dose 50) - produces 50% of Emax

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7
Q

what is therapeutic index?

A

gap between beneficial effects and adverse effects - difference between doses

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8
Q

competitive vs non competitive antagonsists

A

competitive - block receptors
non-competitive - interfere with signal transduction mechanism

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9
Q

what effects do antagonists have on dose response curves

A

increased dose for same effect - shift to right

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10
Q

what is efficacy

A

the extent to which a drug can have its effect (greater Emax - high efficacy)

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11
Q

what is potency

A

amount of drug required to have a specific effect (lower dose for same effect would have high potency)

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12
Q

what is selectivity

A

receptors slightly different in different areas- different areas more or less likely to respond to same drug dosage

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13
Q

desensitisation

A

response tails off over time

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14
Q

gradual desensitisation over longer period of time?

A

tolerance

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15
Q

rapid desensitisation over short period of time

A

tachyphylaxis

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16
Q

causes of desensitisation - pharmocodynamic

A

reduction in receptor number
changes in receptor structure or function
exhaustion of mediators
physiological adaption

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17
Q

reduced drug response other than pharmocodynamic reasons

A

altered physiology (eg gained weight)
disease progression
drug interactions
reduced adherence (bad drug giving by patients)

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18
Q

pharmacokinetics?

A

what a drug does to the body

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19
Q

what are the four stages of drug handling

A

absorption
distribution
metabolism
excretion

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20
Q

how is pharmacokinetic handling of a drug influenced

A

physiological factors - age, sex, body, height
external factors - food, other drugs

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21
Q

different oral routes?

A

swallowing
buccal - tablet between upper lip and gum
sublingual - tablet beneath tongue
buccan and sublingual involve drugs being absorbed into capillaries of oral circulation

22
Q

non oral routes of drug administration

A

intravenous
intramuscular
subcutaneous
inhaled
rectal
transderm

23
Q

pros and cons of intramuscular injection

A

rapid effect but rate of absorption highly dependent on muscle blood flow

24
Q

skin as a route of absorption?

A

transdermal - adhesive skin patches
topical - lotions/creams/etc

25
Q

what is bioavaliability

A

fraction of administered drug that reaches systemic circulation

26
Q

what is the most important limitation on absorption

A

‘First pass’ metabolism by enzymes in intestinal wall and liver

27
Q

gut enzymes?

A

monoamine oxidase
L-aromatic amino acid decarboxylase
cytochrome P450 isoform 3A4
phase 2 conjugating enzymes
membrane transporters

28
Q

what system in the liver accounts for most first-pass metabolism of oral drugs

A

phase 1 metabolising enxymes of the cytochrome P450 system

29
Q

when is rectal administration useful

A

drugs used to soften faeces in constipated patients
useful for patients who cannot swallow and there is no suitable injectable formulation

30
Q

features of intravenous injection

A

most direct route of entry, entire dose is bioavailable

31
Q

what is a low therapeutic index

A

narrow range between lowest effective dose and highest safe dose

32
Q

differences of peak concentration of oral and intravenous injection

A

lower and delayed for oral

33
Q

movement of drug molecules after absorption through different fluids

A

plasma to interstitial to intracellular fluid

34
Q

equilibrium and drug administration?

A

equilibrium will eventually be reached between plasma/interstitial/intracellular fluid. drug will be eliminated from plasma (metabolism or excretion) causing gradient moving drug out of tissues - unless further drug administration occurs

35
Q

what does distribution of drug molecules between compartments depend on

A

molecular size, lipid solubility, ionisation, binding to plasma proteins, rate of blood flow, special barriers, drug affinity for specific tissues

36
Q

how does the vast majority of drugs cross membranes

A

simple diffusion

37
Q

what does rate of transfer of drug molecules by diffusion depend on

A

concentration gradient, the molecule, the membrane

38
Q

how do drugs move across cell membranes other than passive diffusion

A

pore-mediated diffusion, pinocytosis

39
Q

what is pinocytosis

A

form of endocytosis. invagination of part of cell membrane, vesicle created which traps extracellular constituents within cell. contents released in cell or extruded by fusion with another membrane

40
Q

drugs that bind to plasma proteins? pros and cons?

A

aspirin, diazepam, phenytoin, warfarin.
stay in body longer, less efficient distribution, lower therapeutic activity, less available for dialysis after toxic doses

41
Q

two phases of metabolism

A

phase 1 - non-synthetic - oxidation/reduction/hydrolysis
phase 2 - synthetic - conjugation with natural endogenous constituent resulting in more soluble product easier to excrete

42
Q

factors effecting drug metabolism

A

genetics, age, sex, nutrition, disease, drugs, dose, route

43
Q

routes of drug excretion

A

faeces, bile, breath, sweat, urine, breast milk

44
Q

what must a drug be to be excreted

A

water-soluble

45
Q

mechanisms of renal excretion

A

glomerular filtration
tubular secretion
tubular reabsorption

46
Q

what is the law of mass action

A

the rate of a chemical reaction or process is directly proportional to the concentrations of the reactants

47
Q

first-order kinetics

A

constant fraction of remaining drug eliminated in a given time - usually 50% (half life)

48
Q

zero-order/saturation kinetics? drug examples?

A

concentration/time graph forms a straight line
phenytoin, aspirin, paracetamol

49
Q

what are modified-release versions of medicines

A

release of drug in small bowel delayed so absorption occurs over longer period of time, prolonged effects

50
Q

hepatic extraction ratio?

A

high hepatic extraction ratio drugs will be extensively metabolised.

51
Q

what is the determinant of the rate at which steady state is achieved

A

half-life (not dose interval)

Body in motion (17 decks)

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