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Sarahs Pharmacology > Pharmacodynamics/ Pharmacokinetics > Flashcards

Pharmacodynamics/ Pharmacokinetics Flashcards

(113 cards)

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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
G beta effects G gamma effects
Acts on pre (Ca2+) and post synaptic (K) membrane
26
GPCR antagonists
Atropine, clopidogrel
27
GPCR agonists
Morphine
28
Types of receptor (4)
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
29
2 types of ligand gated channel
1. Ionotropic (ms) - 5HT3, GABA, ACh 2. Metabotropic (mins) - GPCR
30
Tolerance definition
Require larger dose for same effect
31
Tachyphylaxis definition
Rapid diminishing response with repeat administration
32
Law of mass action
Rate of reaction proportional to concentration of reacting components
33
Kd = equation
[D][R] / [DR]
34
Ka =
1 / Kd
35
Kd definition
Drug concentration where half receptors occupied
36
ED50 definition
Median effective dose Dose which produces max effect in 50% population
37
EC50 definition
Concentration which produces 50% of maximum response
38
Components of dose occupancy graph
X axis concentration Y axis occupancy Potency increases towards left of graph
39
Affinity definition
How well drug binds
40
Potency definition
Dose of drug needed for max effect (x axis)
41
Efficacy definition
Magnitude of effect (y axis)
42
Intrinsic action of Agonist Partial agonist Antagonist Inverse agonit
1 0-1 0 -1
43
Which kind of antagonism can be overcome by increasing agonist concentration
Competitive
44
Partial agonists can act the same as _______
Competitive antagonists
45
Describe the graph of agonist in presence of competitive antagonist or partial agonist
Drug conc (x axis) Response to Emax (y axis) Curve reaches same Emax but requires higher drug conc Potency decreases EC50 the same
46
Indirect antagonism definition
Directly binds to agonist
47
Describe the graph of agonist in presence of non competitive antagonist
Drug conc (x axis) Response to Emax (y axis) Both Emax and potency decreased
48
2 groups of intracellular receptor
Cytosolic and intranuclear
49
Intracellular ligands which bind with receptor
Oestrogen, testosterone, cortisol, mineraliocorticoids
50
Intracellular ligands which bind with DNA protein
Thyroid hormone, Vit A/D
51
How do intracellular receptors function
Ligand activates dissociation of inhibitory protein, frees up DNA binding domain, moves into nucleus if in cytoplasm which allows phosphorylation
52
1st order kinetics
Rate depends on concentration of substrate Hyperbolic curve
53
Zero order kinetics
All active sites are saturated therefore rate independent of substrate conc
54
Michaelis constant (Km)
Concentration of substrate at which velocity is 1/2 Max
55
Michaelis Menten equation
V = Vmax [S] ________ (Km +[S])
56
Factors (3) which increase enzyme activity
1. Allosteric modulation 2. Intermediate messengers ie GPCR 3. Enzyme induction
57
Factors (2) which decrease enzyme activity
1. Direct inhibition 2. Intermediate messengers
58
Examples (3) of competitive antagonists
Neostigmine NSAIDs Ramipril
59
Examples (3) of non competitive antagonists
Aspirin PPIs Organophosphates
60
Description of graph of Michaelis Menten equation
Substrate x axis Velocity y axis Hyperbolic curve normal Competitive antagonist reaches Vmax at slower rate Non Competitive does not reach Max
61
Location of CYP450
Hepatocyte endoplasmic reticulium Renal, lungs, GIT, plasma
62
Features of CYP450
Appears red as contains iron, absorbs max at 450nm Mono-oxygenase enzyme Displays genetic variability
63
Which phase do CYP450 enzymes work
Phase 1
64
Enzyme inducers (SCRAPP)
S - Sulphonylurea C - Carbamazepine R - Rifampicin A - Alcohol (chronic) P - Phenytoin P - Phenobarbital
65
Enzyme inhibitors (SICKFACESOM)
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
Drugs Mx by CYP3A4
Carbamazepine Phenytoin Ketoconazole
67
Codeine is Mx by
CYP2D6
68
Classification of ADRs (2)
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
A-F classification of ADRs
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
Four types of interaction
Pharmaceutical Pharmacokinetic Pharmacodynamic Electrolyte
71
Pharmaceutical interactions (ACNP)
A - absorption - halothane and rubber C - chelation - suggamadex and roc N - neutralisation - heparin and protamine P - precipitation - thio and sux
72
Pharmacokinetic interactions (ADME)
A - absorption - charcoal, pro kinetics D - B blockers M E - excretion - doxapram
73
Pharmacodynamic interactions (PASS)
P - potentiation - Mg and NMBD A - antagonism - neostigmine and NMBD S - synergism - remi and propofol S - summation - N2O and volatiles
74
Definition of absorption
Movement from the site of administration to plasma
75
Factors which affect absorption
Formulation Route Local blood flow Physiochemical properties
76
First pass metabolism
Orally administered drug metabolised by liver via portal vein prior to reaching systemic circulation.
77
Examples of drugs high first pass Mx
Morphine MIdazolam Aspirin
78
Bioavailability definition
Fraction of drug which reaches systemic circulation
79
Bioavailability fraction equation
BF = AUC (PO) / AUC (IV)
80
Distribution definition
Reversible transfer of a drug from one location to another
81
Total body water
42L
82
Intracellular water content
28L (2/3)
83
Extracellular water content
14L (1/3) Interstitial 11L Plasma 3L
84
Vd equation
Dose / Concentration
85
Loading dose equation
Vd x Target concentration
86
t 1/2 equation
0.693 x (Vd/Cl)
87
Phase 1 reactions (3)
Oxidation, reduction Hydrolysis
88
Phase 2 reaction (4) (MAGS)
Methylation Acetylation Glucuronidation Sulphation
89
Hepatic extraction ratio (HER) calculation
Ci-Co/ Ci
90
Hepatic clearance equation
HCl = HER x HBF
91
Intrinsic factors affecting metabolism
Age (elderly phase 2) Sex Blood flow Genetics
92
Extrinsic factors affecting metabolism
Diet Environment Drug properties
93
Clearance definition
Volume of plasma cleared of drug per unit time
94
Clearance equation (2)
Vd x Ke Dose x BF / AUC
95
Elimination half life
Time for plasma concentration of drug by 50% of its original value in a single compartment
96
How long does it take for a drug to be eliminated
5 1/3 lives OR 3 time constants
97
1st order kinetics definition
Rate of elimination proportional to plasma concentration. Constant proportion eliminated per unit time.
98
Zero order kinetics
Constant rate of elimination irrespective of plasma concentration
99
How to find rate constant of a given drug on graph
Gradient of slope
100
Time constant definition
Time taken for plasma to fall by a factor of e - to 37% of its value
101
Which is longer? T or t1/2
T
102
Elimination equation
Plasma concentration x clearance
103
Infusion rate equation
Cl x C(steady state)
104
What is Keo
1st order rate constant. Constant from V1 to effect site.
105
Which is slower K21 or K31
K31
106
Components of a TCI
User interface Microprocessor Infusion pump Alarms
107
Which are the variable variables of the Marsh model
V1, V2, V3
108
Independent variable of Marsh model
Weight
109
Schnider model independent variables
Age, weight, LBM
110
Variable variables of Schnider model
V2 K12, K21 K10
111
Minto model (remi) independent variables
Age, LBM
112
Variable variables of Minto model
V1, V2 All rate constants
113
Ideal TCI drug
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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