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Dr.U.P.Rathnakar
MD.DIH.PGDHM
Potency-A>B
Efficacy-A=B
Drug B
[Pethidine]
E Max
Severe
Drug A
[Morphine]
Drug C
[Aspirin]
Moderate
Mild
Dose-response curves
Response
10mg
100mg
1000mg
Dose-response curves
X is more potent than Y or Z
100%
E max
50%
EC50
Dose-response curves determine how much of a drug (X-axis) causes a particular effect, or a side effect, in the body (Y-axis).
Advantages of Log-dose curve Large no.of doses can be plotted on a small graph paper Comparison of two or more drugs easier as middle portion is straight line
4%
Cumulative DRC
TI=
Wider the TI-More safe the drug Eg.Penicillin -wide TI , Digoxin narrow TI
Certain safety factor = LD1/ED99 LD1=Lethal dose for 1% population ED99=Effective dose for 99% of population
Therapeutic index
TI=10/5=2
TI=100/5=20
100%
10mg
Therapeutic range
Therapeutic range: Range between dose which produces minimal Th.effect and Max.acceptable adverse effect
Acceptable-ADE
Min.Th.Effect
Therapeutic range
Indifferent
Synergism Physical
Antagonism
Chemical Additive One facilitates the action of other Physiological One opposes the action of other
Supra-additive [Potentiation]
Receptor
Competitive
[Equilibrium & Non-equilibrium]
Non-competitive
Synergism
Two drugs One increases or facilitates the action of the other
Additive Drug A + Drug B = Effect of A+B [1 + 1 = 2] Advantage: Side effect may not add up Dose of both can be reduced Eg. Aspirin + Paracetamol Nitrous oxide +Halothane Amlodipine+Atenolol
Supra-additive (Potentiation) Effect of combination is more than individual effect of 2 drugs 1 + 1 = 3 OR 1 + 0 = 2 One drug may be inactive Levodopa+Carbidopa[Inacti ve alone][1 + 0 = 2] Sulfamethaoxazole+Trimeth oprim[Both active] [1+1= 3]
Antagonism [Receptor]
One[Antagonist] blocks the receptor action of the other[Agonist]
Competitive[surmountable] Binds with the same site on the receptor Resembles the agonist Surmountable by increasing the concn. Of agonist Rightward shift of DRC 5. Eg. Ach atropine Morphine - Naloxone
Non-competitive[unsurmountable] Binds to another site or same site covalently No resemblance Not surmountable Flattening of DRC Eg. Diazepam Bicuculline PhenoxybenzamineNoradrenaline
Flattening of DRC
Competitive
Non-competitive
New
Driver Mfr.defect Bad road Over loaded Engine problem
[Age?]
[M or F] [Genetic?] [Envn.] [Obesity?] [Patho.states]