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1
Q

Occupancy?

A

[D]Ka / 1 + [D]Ka OR [L] / [L] + Kd OR [A]Ka / 1 + [A]Ka + [B]Kb

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2
Q

How many receptors are occupied when [D] = Kd?

A

Half

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3
Q

Dose ratio

A

1 + [A]k2

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4
Q

C bound = ?

A

K binding x C free x Cpp

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5
Q

Henderson Hasselbach equation?

A

pH - pKa = log [base]/[acid]

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6
Q

Vd = ?

A

total drug in body / plasma conc

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7
Q

Filtration rate or rate of excretion if not reabsorbed or secreted?

A

GFR x Cfree

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8
Q

Excretion rate if extensively reabsorbed?

A

Urinary flow rate x Cfree

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9
Q

Excretion rate if secreted?

A

Renal plasma flow x C

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10
Q

Rate of renal excretion?

A

C urine x V urine / t

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11
Q

Renal/hepatic clearance?

A

Rate of renal/hepatic excretion / plasma conc

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12
Q

Clearance from a Cp vs time graph?

A

Dose absorbed / AUC or dose rate / Css

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13
Q

Bioavailability from a clearance vs time graph?

A

AUC oral / AUC iv

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14
Q

Plasma conc for first order elimination?

A

Co x e ^ -ke x t

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15
Q

How to work out half time from a LnCp vs time graph?

A

0.693 / ke

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16
Q

How to work out AUC from a LnCp vs time graph if it is straight?

A

Co/ke or Css/ke

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17
Q

How to work out Vd from a LnCp vs time graph?

A

Clearance / ke

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18
Q

How to work out amount of blood in the body when an infusion stops?

A

Vxx x Css or clearance x AUC

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19
Q

Plasma concentration when approaching steady state?

A

Css(1-e^-ke x t)

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20
Q

Cmin at steady state?

A

Cmax x e ^ -ke x tau

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21
Q

Amount in body at start of dose interval?

A

Cmax x Vd

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22
Q

Amount in body at end of dose interval?

A

Cmin x Vd

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23
Q

Dose absorbed?

A

Vd(Cmax - Cmin)

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24
Q

Css?

A

dose rate x F / clearance or AUSss/tau

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25
Q

Loading dose / maintenance dose?

A

Css/Cav1

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26
Q

Dose rate?

A

Css x clearance / F

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27
Q

Total body water?

A

42L

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28
Q

Extracellular water?

A

14L

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29
Q

Intracellular water?

A

28L

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30
Q

Plasma water?

A

3L

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31
Q

Interstitial fluid?

A

11L

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32
Q

What is Vd the same as for a highly ionised drug?

A

ECF

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33
Q

What is Vd the same as for a plasma protein binding drug?

A

Plasma volume

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34
Q

How does phase I conjugation affect drugs?

A

More polar and easily extruded

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35
Q

Which B3 mutation reduces efficacy?

A

N265M within TM2

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36
Q

Which mutation blocks halothane and isoflurance?

A

S270W mutation in GABA alpha subunit

37
Q

Which mutation reduces inhibition of NMDA receptor?

38
Q

What is plotted on a Scatchard plot?

A

[BSp]/[L] against [BSp]

39
Q

What is the gradient of a Scatchard plot?

40
Q

What is the x intercept of a Scatchard plot?

41
Q

What is plotted on a double reciprocal plot?

A

1/[BSp] against 1/[D]

42
Q

What is the y intercept of a double reciprocal plot?

43
Q

What is the x intercept of a double reciprocal plot?

44
Q

What do you plot to find Ka of an unlabelled drug with fixed radioligand conc?

A

IC50 against [radioligand]

45
Q

What is the y intercept of an IC50 against [radioligand] plot?

A

1/Kunlabelled

46
Q

What is the gradient of an IC50 against [radioligand] plot?

A

Klabelled / Kunlabelled

47
Q

What do you plot to find how many molecules bind to a receptor?

A

log (response / max response - response) against log[drug]

48
Q

What is the gradient of a log (response / max response - response) against log[drug] graph?

A

How many molecules bind

49
Q

What is a heterotropic interaction?

A

Oppose each others effects

50
Q

What is a homotropic interaction?

A

Transmitter bind to its own presynaptic autoreceptors

51
Q

Which graph do you use to find the IC50 after a radioligand binding assay?

A

Mean dpm against log[BCh]

52
Q

How to work out affinity constant using IC50, Kradioligand and [radioligand]?

A

[radioligand]Kradioligand + 1 / IC50

53
Q

Clearance?

A

dose/AUC OR Vd x Ke OR rate of elimination/Cp or amount in body

54
Q

C av?

A

dose rate / clearance

55
Q

What is blood flow to liver?

A

1 litre per minute

56
Q

What is Tau?

A

Dosing interval

57
Q

Ka?

A

[DR] / [D] + [R]

58
Q

Therapeutic dose?

A

LD50 / ED50

59
Q

Ka of an unlabelled drug is both drugs are the same?

A

1 / IC50 - [radioligand]

60
Q

Hill equation?

A

nlog[D] - logKdiss

61
Q

[agonist] to shift EC50 twofold?

A

10 ^ -logKa2

62
Q

What is affinity for agonist like in high GTP?

63
Q

How does GTP level affect antagonist affinity?

A

It doesn’t

64
Q

What is GPCR affinity for agonist like in membrane preparations?

A

High (low GTP)

65
Q

When will the Scatchard plot appear curved?

A

Two populations of receptors with different affinity contants and Bmax

66
Q

What is homologous desensitization?

A

Only receptors which are stimulated become desensitised

67
Q

What is heterologous desensitisation?

A

Receptors other than stimulated ones are desensitised - activates PKA which decouples alpha subunit of G protein

68
Q

Why does heterologous desensitization not lead to endocytosis?

A

Arrestin does not recognise the PKA phosphorylated receptor seen in heterologous desensitization)

69
Q

Why are hydrophilic radioligands used?

A

Can’t get to internal receptors AND endocytosis not initiated if they are an antagonist

70
Q

Rate of decrease in concentration?

A

ke x concentration

71
Q

What to do if working out fraction of concentration after a certain time?

A

C / C0 = the fraction, this is equal to e ^ -ke x t

72
Q

How to work out Ke from a LnCp vs time graph?

73
Q

What does it mean if the lnC vs time plot os not a straight line?

A

There is redistribution into tissues - a two compartment model

74
Q

What happens if urine is at a low pH?

A

Weak acids are more uncharged so more is reabsorbed from the kidneys - opposite for weak bases

75
Q

What happens if urine is at a high pH?

A

Weak acid is less easily reabsorbed from the kidneys

76
Q

What does a drug need in order to be secreted?

A

A transporter protein

77
Q

What is the clearance if the drug is filtered AND secreted?

A

625 ml/min (renal plasma flow)

78
Q

If first order elimination, what does doubling the dose do to the AUC?

A

Doubles it

79
Q

What happens to the ratio of the dose to the AUC of clearance is constant?

A

The same - D2 / AUC2 = D1 / AUC1

80
Q

Vd if lnCp vs time line is straight?

81
Q

Vd if drug redistributes (called Vz)?

A

Clearance / Kz

82
Q

Average conc at steady state?

A

DF / tau x CL

83
Q

What is the difference between dose rate and tau?

A

Dose rate measured in amount per time, tau just time

84
Q

Cmax - Cmin (concentration change?)

A

dose x F / Vd

85
Q

Loading dose?

A

Vd x Cav,ss

86
Q

clearance x C av,ss?

87
Q

How to work out clearance from rate of infusion and Css?

A

Clearance = rate of infusion / Css

88
Q

What is the process of homologous desensitization?

A

BARK phosphorylates the receptor, this increases affinity for B-arrestin, this uncouples the alpha subunit of the G protein

89
Q

How to find number of receptors?

A

Multiply avogadro’s number by molar conc

MODA (10 decks)

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