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Pharmacodynamics PDF
Pharmacodynamics PDF
Pharmacokinetics Pharmacodynamics
PHARMACODYNAMICS
Dr. Satyajit, MD
Assistant professor
Plasma Site of
Dosage Effects
Concen. Action
Pharmacokinetics Pharmacodynamics
What the drug does to the body
Deals with
Mechanism of action
Drug-receptor interactions
Drug
Principles of Drug action
• Irritation: Counterirritant
• Replacement: Insulin in DM
DIABETES
CYTOTOXIC ACTION
1. Physical action:
- Mass of drug - Ispaghula husk
- Adsorptive property -char coal
- Osmotic activity- Magnesium sulfate
- Radio activity- I 131
- Oxidising property – KMnO4
2. Chemical action
Stimulation
Pyridoxine acts as co factor for
dopa decarboxylase activity
Inhibition
Aspirin inhibits Cyclooxygenase
4. Through ion channels:
Calcium channel blockers
Sulfonamides –
interfere with bacterial folic acid synthesis
6. Placebo effect ???
• Physical
• Chemical
• Enzymatic
• Ion channel
• Alteration of metabolism
• Placebo
4 major target of drug action
• Enzymes
• Ion channels
• Transporters
• Receptors
Receptor mediated action
What is a receptor ???
D
R
R Effects
R
Different terminologies
• Affinity
D
R Response
Agonist
R Response
Antagonist
R
No response
Partial sub
R agonist maximal
response
Agonist Anti
GABA convulsant
Receptor Inverse
agonist Convulsions
Eg: ß-Carbolines
Ligand
• Any molecule which attaches selectively to
particular receptors or site
Rectangular
hyperbola
• Intensity of the response increases with dose
• Dose resposnse curve is rectangular hyperbola
• Drug- receptor interaction obeys the Law of mass
action
E= Emax X [D]
KD + [D]
E = Observed effect at dose D
Emax = Maximal response
KD = dissociation constant
Log dose response curve
Sigmoid
curve
• Linear relationship between log dose and
response is seen in intermediate (30-70%)
GRADED DOSE-
RESPONSE CURVE
ED50
Cumulative
Frequency
Distribution QUANTAL DOSE-
RESPONSE CURVE
Frequency
Distribution
Potency
morphine
codeine
Analgesia
aspirin
Dose
Efficacy
• Is it < 1 or > 1 ?
• May be PK or PD interactions
Synergism
• Syn – together
• Ergon – work
• Supraadditive (Potentiation)
1. Additive:
Supra additive:
Effect of combination is greater than the individual
effects of components
1. Physical Antagonism
Charcoal(adsorps alkaloids)
Used in Rx of alkaloidal poisonings
2. Chemical antagonism
Two drugs react chemically – inactive product
Antacids in the Rx of peptic ulcer
3.Physiological antagonism:
• Noncompetitive antagonism
Competitive antagonism
Agonist & Antagonist have
– Same chemical structure
– Same receptor
– Same binding site
• Therapeutic range
• Antagonism
Action-Effect sequence
Drug Action
• So it has
– Ligand binding domain
– Effector domain – undergoes conformational
changes
Transducer mechanism
1. Ion channel linked
2. G protein linked
3. Enzyme linked
• Channel regulation
Effector pathways
IP3 DAG
• Cigarette smoke-
Genetic Factors
• ???
12
Summary
¾ most drugs act through receptors
¾ there are 4 common signal transduction methods
¾ the interaction between drug and receptor can be described
mathematically and graphically
¾ agonists have both affinity and intrinsic activity.
¾ antagonists have affinity only
¾ antagonists can be competitive or
¾ non-competitive when mixed with agonists
¾ agonists desensitize receptors.
¾ antagonists sensitize receptors.