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Sarahs Pharmacology > Pharmacodynamics/ Pharmacokinetics > Flashcards

Pharmacodynamics/ Pharmacokinetics Flashcards

1
Q

Pharmacodynamic definition

A

What drug does to the body

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2
Q

Aliphatic compound

A

Carbon root with functional group

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3
Q

Aromatic compound

A

Benzene ring of carbon atoms

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4
Q

C=C

A

Alkene

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5
Q

-NH2

A

Amine

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6
Q

-OH

A

Alcohol

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7
Q

-Cl/Br/F

A

Halide

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8
Q

O=C-OH

A

Carboxylic acid

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9
Q

O=C-NH2

A

Amide

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10
Q

-C-O-C-

A

Ether

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11
Q

R-C=O/-O-R

A

Ester

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12
Q

Valency

A

Number of bonds in uncharged state

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13
Q

Order of bond strength

A

Ionic (electron transfer)
Covalent (share electron)
Hydrogen
Dipole-dipole
Van der Waal

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14
Q

Polar molecule

A

Electron pulled more towards one atom. Electrons in upper right hand corner of table are more electronegative.

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15
Q

Determinants of onset of action

A
  1. Lipid solubility
  2. pKa
  3. Protein binding
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16
Q

Kd =

A

k1 (proton donor) /
k2 (proton acceptor)

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17
Q

Acids ionise _____ pKa

A

Above

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18
Q

Bases ionise _____ pKa

A

Below

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19
Q

pH =

A

-log10[H]

OR

pKa + log [HCO3]/[CO2]*

*pCO2x0.03

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20
Q

pKa of thio (weak acid)

A

7.6

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21
Q

pKa of propofol (weak acid)

A

11

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22
Q

pKa of ketamine (weak base)

A

7.5

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23
Q

Non specific drug actions (4)

A

Chelation - suggamadex
Charge neutralisation - gaviscon
Adsorption - charcoal
Osmotic - mannitol

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24
Q

G alpha effects

A

Acts on adenyl cyclase function

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25
Q

G beta effects
G gamma effects

A

Acts on pre (Ca2+) and post synaptic (K) membrane

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26
Q

GPCR antagonists

A

Atropine, clopidogrel

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27
Q

GPCR agonists

A

Morphine

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28
Q

Types of receptor (4)

A
  1. GPCR
  2. Ion - charged particles pass down electrochemical gradient
  3. Voltage gated - Na/K/Ca - depolarisation causes conformational change to open channel
  4. Ligand gated - ion and metabotropic
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29
Q

2 types of ligand gated channel

A
  1. Ionotropic (ms) - 5HT3, GABA, ACh
  2. Metabotropic (mins) - GPCR
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30
Q

Tolerance definition

A

Require larger dose for same effect

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31
Q

Tachyphylaxis definition

A

Rapid diminishing response with repeat administration

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32
Q

Law of mass action

A

Rate of reaction proportional to concentration of reacting components

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33
Q

Kd = equation

A

[D][R] / [DR]

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34
Q

Ka =

A

1 / Kd

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35
Q

Kd definition

A

Drug concentration where half receptors occupied

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36
Q

ED50 definition

A

Median effective dose
Dose which produces max effect in 50% population

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37
Q

EC50 definition

A

Concentration which produces 50% of maximum response

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38
Q

Components of dose occupancy graph

A

X axis concentration
Y axis occupancy
Potency increases towards left of graph

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39
Q

Affinity definition

A

How well drug binds

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40
Q

Potency definition

A

Dose of drug needed for max effect (x axis)

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41
Q

Efficacy definition

A

Magnitude of effect (y axis)

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42
Q

Intrinsic action of
Agonist
Partial agonist
Antagonist
Inverse agonit

A

1
0-1
0
-1

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43
Q

Which kind of antagonism can be overcome by increasing agonist concentration

A

Competitive

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44
Q

Partial agonists can act the same as _______

A

Competitive antagonists

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45
Q

Describe the graph of agonist in presence of competitive antagonist or partial agonist

A

Drug conc (x axis)
Response to Emax (y axis)
Curve reaches same Emax but requires higher drug conc

Potency decreases
EC50 the same

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46
Q

Indirect antagonism definition

A

Directly binds to agonist

47
Q

Describe the graph of agonist in presence of non competitive antagonist

A

Drug conc (x axis)
Response to Emax (y axis)
Both Emax and potency decreased

48
Q

2 groups of intracellular receptor

A

Cytosolic and intranuclear

49
Q

Intracellular ligands which bind with receptor

A

Oestrogen, testosterone, cortisol, mineraliocorticoids

50
Q

Intracellular ligands which bind with DNA protein

A

Thyroid hormone, Vit A/D

51
Q

How do intracellular receptors function

A

Ligand activates dissociation of inhibitory protein, frees up DNA binding domain, moves into nucleus if in cytoplasm which allows phosphorylation

52
Q

1st order kinetics

A

Rate depends on concentration of substrate
Hyperbolic curve

53
Q

Zero order kinetics

A

All active sites are saturated therefore rate independent of substrate conc

54
Q

Michaelis constant (Km)

A

Concentration of substrate at which velocity is 1/2 Max

55
Q

Michaelis Menten equation

A

V = Vmax [S]
________
(Km +[S])

56
Q

Factors (3) which increase enzyme activity

A
  1. Allosteric modulation
  2. Intermediate messengers ie GPCR
  3. Enzyme induction
57
Q

Factors (2) which decrease enzyme activity

A
  1. Direct inhibition
  2. Intermediate messengers
58
Q

Examples (3) of competitive antagonists

A

Neostigmine
NSAIDs
Ramipril

59
Q

Examples (3) of non competitive antagonists

A

Aspirin
PPIs
Organophosphates

60
Q

Description of graph of Michaelis Menten equation

A

Substrate x axis
Velocity y axis
Hyperbolic curve normal
Competitive antagonist reaches Vmax at slower rate
Non Competitive does not reach Max

61
Q

Location of CYP450

A

Hepatocyte endoplasmic reticulium
Renal, lungs, GIT, plasma

62
Q

Features of CYP450

A

Appears red as contains iron, absorbs max at 450nm
Mono-oxygenase enzyme
Displays genetic variability

63
Q

Which phase do CYP450 enzymes work

A

Phase 1

64
Q

Enzyme inducers (SCRAPP)

A

S - Sulphonylurea
C - Carbamazepine
R - Rifampicin
A - Alcohol (chronic)
P - Phenytoin
P - Phenobarbital

65
Q

Enzyme inhibitors (SICKFACESOM)

A

S - SoVal
I - Isoniazid
C - Ciprofloxacin
K - Ketoconazole/ flucon
F - Fluoxetine
A - Alcohol (acute)
C - Chloramphenicol
E - Erythromycin
S - Sulfonamides
O - Omeprazole
M - Metronidazole

66
Q

Drugs Mx by CYP3A4

A

Carbamazepine
Phenytoin
Ketoconazole

67
Q

Codeine is Mx by

A

CYP2D6

68
Q

Classification of ADRs (2)

A

Reactions that happen to anyone
1. SE’s
2. Overdose
3. Interactions

Reactions that happen in those susceptible
1. Anaphylaxis
2. Intolerance
3. Idiosyncrasy (genetic)

69
Q

A-F classification of ADRs

A

A - augmented - propofol and low BP
B - bizarre - anaphylaxis
C - chronic - propofol infusion
D - delayed - time related
E - end of use - withdrawal
F - failure - ie COCP

70
Q

Four types of interaction

A

Pharmaceutical
Pharmacokinetic
Pharmacodynamic
Electrolyte

71
Q

Pharmaceutical interactions (ACNP)

A

A - absorption - halothane and rubber
C - chelation - suggamadex and roc
N - neutralisation - heparin and protamine
P - precipitation - thio and sux

72
Q

Pharmacokinetic interactions (ADME)

A

A - absorption - charcoal, pro kinetics
D - B blockers
M
E - excretion - doxapram

73
Q

Pharmacodynamic interactions (PASS)

A

P - potentiation - Mg and NMBD
A - antagonism - neostigmine and NMBD
S - synergism - remi and propofol
S - summation - N2O and volatiles

74
Q

Definition of absorption

A

Movement from the site of administration to plasma

75
Q

Factors which affect absorption

A

Formulation
Route
Local blood flow
Physiochemical properties

76
Q

First pass metabolism

A

Orally administered drug metabolised by liver via portal vein prior to reaching systemic circulation.

77
Q

Examples of drugs high first pass Mx

A

Morphine
MIdazolam
Aspirin

78
Q

Bioavailability definition

A

Fraction of drug which reaches systemic circulation

79
Q

Bioavailability fraction equation

A

BF = AUC (PO) / AUC (IV)

80
Q

Distribution definition

A

Reversible transfer of a drug from one location to another

81
Q

Total body water

A

42L

82
Q

Intracellular water content

A

28L (2/3)

83
Q

Extracellular water content

A

14L (1/3)
Interstitial 11L
Plasma 3L

84
Q

Vd equation

A

Dose / Concentration

85
Q

Loading dose equation

A

Vd x Target concentration

86
Q

t 1/2 equation

A

0.693 x (Vd/Cl)

87
Q

Phase 1 reactions (3)

A

Oxidation, reduction
Hydrolysis

88
Q

Phase 2 reaction (4) (MAGS)

A

Methylation
Acetylation
Glucuronidation
Sulphation

89
Q

Hepatic extraction ratio (HER) calculation

A

Ci-Co/ Ci

90
Q

Hepatic clearance equation

A

HCl = HER x HBF

91
Q

Intrinsic factors affecting metabolism

A

Age (elderly phase 2)
Sex
Blood flow
Genetics

92
Q

Extrinsic factors affecting metabolism

A

Diet
Environment
Drug properties

93
Q

Clearance definition

A

Volume of plasma cleared of drug per unit time

94
Q

Clearance equation (2)

A

Vd x Ke

Dose x BF / AUC

95
Q

Elimination half life

A

Time for plasma concentration of drug by 50% of its original value in a single compartment

96
Q

How long does it take for a drug to be eliminated

A

5 1/3 lives OR 3 time constants

97
Q

1st order kinetics definition

A

Rate of elimination proportional to plasma concentration. Constant proportion eliminated per unit time.

98
Q

Zero order kinetics

A

Constant rate of elimination irrespective of plasma concentration

99
Q

How to find rate constant of a given drug on graph

A

Gradient of slope

100
Q

Time constant definition

A

Time taken for plasma to fall by a factor of e - to 37% of its value

101
Q

Which is longer? T or t1/2

A

T

102
Q

Elimination equation

A

Plasma concentration x clearance

103
Q

Infusion rate equation

A

Cl x C(steady state)

104
Q

What is Keo

A

1st order rate constant. Constant from V1 to effect site.

105
Q

Which is slower K21 or K31

A

K31

106
Q

Components of a TCI

A

User interface
Microprocessor
Infusion pump
Alarms

107
Q

Which are the variable variables of the Marsh model

A

V1, V2, V3

108
Q

Independent variable of Marsh model

A

Weight

109
Q

Schnider model independent variables

A

Age, weight, LBM

110
Q

Variable variables of Schnider model

A

V2
K12, K21
K10

111
Q

Minto model (remi) independent variables

A

Age, LBM

112
Q

Variable variables of Minto model

A

V1, V2
All rate constants

113
Q

Ideal TCI drug

A

Short CSHT after long duration
Rapid elimination, slow distribution
No active Mx
Minimally effected by organ failure
Minimal CVS effects

Sarahs Pharmacology (2 decks)

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