pharmacodynamics · pharmacodynamics presented by dr. sannithi nagarjuna coordinator for riper-gpat...
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PHARMACODYNAMICS
Presented by
Dr. Sannithi Nagarjuna
Coordinator for RIPER-GPAT Cell,
Hyderabad Academy &
Online GPAT Academy
7899107907
9885784793
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It is a branch of pharmacology deals with the study of mechanism of
action, pharmacological actions and uses of drugs.
(What the drug does to the body)
(OR)
It is defined as the response of the body to the drug. It refers to the
relationship between drug concentration at the site of action and
resulting effect.
(OR)
It is the study of biochemical, physiological and molecular effects of
drugs on the body.
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Most of the drugs produce their mechanism
of action by binding to the receptors.
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DEFINITIONS
1. RECEPTORS → defined as specific binding sites for drug
molecules/ ligands and chemically they are protein in nature.
All receptors are proteins but all proteins are not receptors.
2. LIGAND → defined as a substance that selectively attaches to
the receptors, activates the receptors and produces maximum
pharmacological action.
Both receptors and ligand are highly specific.
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Receptors Ligand
Muscarinic and Nicotinic
receptors (Cholinergic)
Acetylcholine
Adrenergic receptors Noradrenaline
Histamine receptors Histamine
Dopamine receptors Dopamine
5-HT receptors 5-HT (Serotonin)
GABA receptors GABA
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3. AFFINITY →
ability of an agent to bind with the receptors
4. INTRINSIC ACTIVITY ( EFFICACY)→
ability of an agent to activate the receptors and produces
pharmacological action
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5. AGONIST : Affinity + Maximum Intrinsic activity (IA= + 1)
Agonist and ligand both are same, the only difference is agonist is
exogenous and ligand is endogenous.
Agonist produces actions similar to ligand
or
Agonist increases the actions of ligand
6. ANTAGONIST: Affinity + No Intrinsic activity (IA= 0)
Antagonist blocks or stops the actions of ligand hence it is otherwise
called as blocker.
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Source : Google
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Source : Google
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Ligand Agonist Antagonist
Acetylcholine Carbachol,
Bethanechol
Atropine
Noradrenaline Dobutamine Propranolol
Histamine 2-methyl histamine Diphenhydramine
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TYPES OF RECEPTORS
❖ Receptors will not exist as alone and they are
always present in attached manner
(Coupled manner)
❖ Based upon the coupled substance receptors
are classified into 4 types
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1. G-Protein Coupled Receptors ( Receptors coupled to
G-Protein )
2. Ionotropic receptors ( Receptors coupled to Ion
channels )
3. Enzyme linked receptors ( Receptors coupled to
Enzymes)
4. Nuclear receptors ( Receptors coupled to nucleus)
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G-Protein Coupled Receptors
( Receptors coupled to G-Protein )
❖ Receptors located across/on/within the cell
membrane
❖ Hence called as transcellular receptors
❖ Here there are two parts one is G-protein and
another one is Receptor
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Receptor consist of
7 transcellular helical structures
3 loops
-NH2 group present on extracellular side
-COOH group present on intracellular side
G-protein is trimeric in nature consist of 3 subunits called
as α, β, and γ and these three subunits attached to GDP.
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binding of ligand with the receptors
GDP replaces with GTP
G-Protein dissociated into 2 complexes
Interacts with the pathways
Release of substances called as secondary messengers
Produces pharmacological actions
GTP α β γ
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Source : Google
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Source : Google
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PATHWAYS
1. ADENYL CYCLASE PATHWAY
ATP -------------→ cAMP -----------→ Inactive
❖ cAMP acts as a second messenger
❖ Enzyme Phosphodiesterase involved in the inactivation
of cAMP
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Source : Google
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ACTIONS OF CAMP
In cardiac muscle/Heart --
Increases force of contraction, Increases cardiac output, Increases blood pressure, Increases heart rate.
In smooth muscles (GIT, Bronchi, Uterus) –
Smooth muscle relaxation
In Liver –
Glycogenolysis
In adipose tissue
Lipolysis
In Platelets
Decreases platelet aggregation
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2. PHOSPHOLIPASE PATHWAY
Stimulation of this pathway results in the breakdown of
cell membrane phospholipids.
Cell membrane phospholipids upon breakdown will
release Inositol-1,4,5- triphosphate (IP3)and Diacylglycerol
(DAG) which act as second messengers.
IP3 & DAG always produce stimulation.
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ACTIONS OF IP3
AND DAG
Location Action
Cardiac muscles Contraction
Smooth muscles Contraction
Skeletal muscles Contraction
Glands Increase in secretions
CNS CNS Stimulation
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GS → Increased levels of cAMP
Gi → Decreased levels of cAMP
Gq →Increased levels of IP3 and DAG
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EXAMPLES:
1.Muscarinic receptors (M1- M5)
2. Adrenergic receptors (α1- α2 & β1- β3)
3.Histamine receptors (H1-H3)
4.Dopamine receptors (D1-D5)
5.5-HT receptors (5-HT1 to 5-HT 7 except 5-HT 3)
6.Opiod receptors
7.GABAB receptors
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MUSCARINIC RECEPTORS(M1 - M
5)
Gq Gi
M1 M2
M3 M4
M5
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Type of
receptor
Second
Messenger
Location Pharmacological actions
M1 Gq ❖ Gastric Parietal Cells
❖ Ciliary Muscles of Iris
M3 Gq ❖ Smooth muscles like
Bronchi, Uterus, GIT
❖ Glands like sweat
glands, salivary
glands & lacrimal
glands
M5 Gq CNS
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Type of
receptor
Second
Messenger
Location Pharmacological actions
M1 Gq ❖ Gastric Parietal Cells
❖ Ciliary Muscles of Iris
❖ Increase in acid
secretion
❖ Contraction of Ciliary
Muscles of Iris (Miosis)
M3 Gq ❖ Smooth muscles like
Bronchi, Uterus, GIT
❖ Glands like sweat
glands, salivary glands
& lacrimal glands
❖ Smooth muscle
contraction like
Bronchoconstriction,
Uterus constriction,
Contraction of GIT,
Increase in motility of GIT
❖ Increase in secretions
like sweating,
salivation and
lacrimation
M5 GqCNS ❖ CNS stimulation
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Type of
receptor
Second
Messenger
Location Pharmacological
actions
M2 Gi Heart
M4 Gi CNS
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Type of receptor Second
Messenger
Location Pharmacological
actions
M2 Gi Heart Decrease in
force of
contraction,
Decrease in
cardiac output,
Decrease in
blood pressure,
Decrease in
heart rate
M4 Gi CNS No action
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Source: Google
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PHARMACOLOGICAL ACTIONS OF ACETYLCHOLINE
Location Pharmacological actions
Heart Decrease in force of contraction,
Decrease in cardiac output, Decrease
in blood pressure, Decrease in heart
rate
Smooth muscles like
Bronchi, Uterus, GIT
Smooth muscle contraction like
Bronchoconstriction,
Uterus constriction,
Contraction of GIT, Increase in
motility of GIT
Gastric Parietal Cells Increase in acid secretion
Ciliary Muscles of Iris Contraction of Ciliary Muscles of Iris
(Miosis)
Glands like sweat glands, salivary
glands & lacrimal glands
Increase in secretions like sweating,
salivation and lacrimation
CNS CNS stimulation
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ADRENERGIC RECEPTORS {α1 – α2 & β1- β3}
Gq Gi GS
α1 α2 β1
β2
β3
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Type of
receptor
Second
Messenger
Location Pharmacological actions
α1 Gq ❖ Blood vessels
α2 Gi ❖ CNS
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Type of
receptor
Second
Messenger
Location Pharmacological actions
α1 Gq ❖ Blood vesselsVasoconstriction,
increase in blood
pressure
α2 Gi ❖ CNSNo Action
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Type of
receptor
Second
Messenger
Location Pharmacological actions
β1 GS ❖ Heart
β2 GS ❖ Smooth muscles
❖ Bronchi
❖ Liver
β3 GS ❖ Adipose tissue
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Type of
receptor
Second
Messenger
Location Pharmacological actions
β1 GS ❖ HeartIncrease in force of
contraction,
Increase in cardiac output,
Increase in blood
pressure,
Increase in heart rate
β2 GS ❖ Smooth muscles
❖ Bronchi
❖ Liver
❖ Smooth muscle
relaxation
❖ Bronchodilation
❖ Glycogenolysis
β3 GS ❖ Adipose tissue❖ Lipolysis
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PHARMACOLOGICAL ACTIONS OF NORADRENALINE
Location Pharmacological actions
Heart Increase in force of contraction,
Increase in cardiac output,
Increase in blood pressure,
Increase in heart rate
Smooth muscles
Bronchi
Smooth muscle relaxation
Bronchodilation
Blood vessels Vasoconstriction, increase in blood
pressure
Metabolic effects Glycogenolysis & Lipolysis
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IONOTROPIC RECEPTORS
(RECEPTORS COUPLED TO ION
CHANNELS )
❖ Receptors coupled to ion channels
❖ Receptors located across/on/within the cell membrane
❖ These are also transcellular receptors
❖ Also called as ligand gated ion channels
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Ligand binds to the receptors
Opening of ion channels will take place
Result in either influx or efflux of ions depending upon
concentration gradient
Result in pharmacological actions which may be stimulation or
inhibition
O
p
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Source : Google
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Sodium, Calcium & Chloride ions present extracellularly
so when these ion channels get opened that result in
influx of ions.
Potassium ions present intracellularly so when these ion
channels get opened that result in efflux of ions.
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Ligand binds
to the receptors → Sodium channels → Influx of sodium ions→
Ligand binds
to the receptors → Calcium channels → Influx of Calcium ions→
Ligand binds
to the receptors → Chloride channels → Influx of chloride ions→
Ligand binds
to the receptors → Potassium channels → Efflux of potassium ions →
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Ligand binds
to the receptors →Sodium channels → Influx of sodium ions→ Stimulation
Ligand binds
to the receptors → Calcium channels → Influx of Calcium ions→ Stimulation
Ligand binds
to the receptors → Chloride channels → Influx of chloride ions→ Inhibition
Ligand binds
to the receptors → Potassium channels → Efflux of potassium ions →Inhibition
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Location Stimulation Inhibition
Cardiac
muscle/Heart
Contraction,
Increase in force of
contraction,
Increase in cardiac
output,
Increase in blood
pressure,
Increase in heart rate
Relaxation,
Decrease in force of
contraction,
Decrease in cardiac
output,
Decrease in blood
pressure,
Decrease in heart rate
Smooth muscles Contraction Relaxation
Skeletal muscles Contraction Relaxation
Glands Increase in secretions Decrease in secretions
CNS CNS Stimulation CNS depression
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EXAMPLES:
1. Nicotinic receptors (NM & NN receptors)
2. 5-HT3 receptors
3. GABAA receptors
4. NMDA receptors
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Type of
receptor
Type of ion
channel
attached
Location Pharmacological actions
NM Sodium ❖ Skeletal muscles
NN Sodium ❖ Autonomic ganglia
5-HT3 Sodium ❖ CTZ
GABAA Chloride ❖ CNS
NMDA Calcium ❖ CNS
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Type of
receptor
Type of ion
channel
attached
Location Pharmacological actions
NM Sodium ❖ Skeletal musclesSkeletal muscle contraction
NN Sodium ❖ Autonomic gangliaGanglionic stimulation
5-HT3 Sodium ❖ CTZNausea and vomiting
GABAA Chloride ❖ CNSCNS depression
NMDA Calcium ❖ CNSCNS stimulation
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Type of
receptor
Pharmacological
actions
Category Therapeutic
Uses
NMSkeletal muscle
contraction
Skeletal
Muscle
relaxants
NM receptor
blockers
NNGanglionic stimulation Ganglionic
blockers
NN receptor
blockers
5-HT3Nausea and vomiting Antiemetics 5-HT3
antagonists
GABAACNS depression CNS
depressants
GABAA
receptor
agonists
NMDA CNS stimulation CNS
depressants
NMDA
receptor
blockers
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ENZYME LINKED RECEPTORS
(RECEPTORS COUPLED TO ENZYMES)
❖ Receptors coupled to enzymes
❖ Receptors located across/on/within the cell
membrane
❖ These are also transcellular receptors
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Ligand binds to the receptors
Enzymes automatically undergo
phosphorylation (Autophosphorylation)
Responsible for mediating the pharmacological
actions
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Most of the enzymatic receptors are
coupled to the enzyme
Tyrosine Kinase
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EXAMPLES:
1. Insulin receptors (Tyrosine Kinase)
2. Epidermal growth factor receptors (Tyrosine Kinase)
3. Natriuretic peptide receptors (Guanyl cyclase)
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❖ Receptors coupled directly to nucleus
❖ Receptors located inside the cell
❖ These are also called as intracellular receptors
❖ Otherwise called as steroidal receptors
NUCLEAR RECEPTORS
( RECEPTORS COUPLED TO NUCLEUS)
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Ligand binds to the receptors
Direct change in gene expression
Synthesis of specific mRNA
Synthesis of specific proteins
Responsible for mediating pharmacological actions
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Source: Google
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EXAMPLES:
1. Glucocorticoid receptors
2. Mineralocorticoid receptors (Aldosterone receptors)
3. Estrogen receptors
4. Progesterone receptors
5. Androgen receptors (Testosterone receptors)
6. Vitamin A & Vitamin D receptors
7. Thyroid hormone receptors
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Source: Google
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Source : Google
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SIGNAL TRANSDUCTION
Ligand after binding to the receptors a sequence of
events/steps taking place in order to produce
pharmacological actions.
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Fastest acting receptors
Most intensifying action
observed in case of
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Fastest acting receptors Ionotropic receptors
Most intensifying action
observed in case of
Nuclear receptors
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Transcellular
receptors
Intracellular receptors
Ligand binding site
Reactions
Examples
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Transcellular
receptors
Intracellular receptors
Ligand binding site Extracellular Intracellular
Reactions Intracellular Intracellular
Examples GPCR, Ionotropic
receptors, Enzyme
linked receptors
Nuclear receptors
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Presented by
Dr. Sannithi Nagarjuna
Coordinator for RIPER-GPAT Cell,
Hyderabad Academy &
Online GPAT Academy
7899107907
9885784793