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PHARMACODYNAMICS
Pirməmmədova Ləman 717a4
Pharmacodynamıcs
The study of biochemical cellular and
physiological effects of medications and their
mechanisms of action. More simply, it is what
medications do and how they do it.
۰ S T İ M U L A T I O N
Selective enhancement of the effectiveness of specialized cells. Effect of acetylcholine on salivary glands.
۰ D E P R E S S I O N
Selective reduction of the effectiveness of specialized cells. Effect of salbutamol on uterine muscles.
۰ I R R I T A T I O N
Non-selective, often noxious effect on less specialized cells. Capsaicin in herpetic neuralgia.
۰ R E P L A C E M E N T
Use of natural metabolites, hormones and their congeners in deficiency states. Iron supplementation in iron
deficiency anemia. Insulin in diabetes.
۰ C Y T O T O X I C
Selective effect on bacteria - penicillin, cephalosporins. Selective effect on cancer cells - methotrexate,
cisplatin.
FEATURES OF EFFECT
PRINCIPLES OF
MEDICATION
EFFECTS
DOSE
RESPONSE
Max effect – All receptors
occupied
100%
50%
A F F I N I T Y
D O S E
Not enough
receptors
bind
More
receptor-
medication
complexes
Effective
dose (ED50)
DOSE
RESPONSE
Max effect
100%
DOSE
RESPONSE
Max effect
100%
60%
>
More potent
>
More efficacious
They require different dose to reach the same
Max effect
Same ED50, different Max effect.
INRERACT WITH RECEPTOR
They are macromolecular compounds that are sensitive to
certain chemical compounds. As a result of their interaction
with chemical compounds, various biochemical and
physiological changes occur in the body. Types:
۰ G-protein coupled receptors
۰ Ion channels
۰ Enzyme-coupled receptors
۰ Intracellular receptors
RECEPTORS
A G O N İ S T
Mimics the action of ligands and
activates the receptor.
DOSE
RESPONCE
All available receptors are bound to
an agonists.
- full agonist
- partial aqonist
100%
70%
A N T A G O N İ S T
Binds to receptors without activating
them, instead decreases receptor’s
ability to be activated by other
agonists.
DOSE
RESPONSE
Max effekt
- full agonist
- with reversible antagonist
100%
50% ED50
DOSE
RESPONCE
Max effekt
- full agonist
- with irreversible antagonist
100%
50% ED50
70%
INTERACT WITH ENZYMES
A number of drugs alter the effects of drugs by
slowing down or increasing the activity of enzymes.
The increase in activity may occur by enzyme
induction.
I N H I B I T I O N
Inhinition of acetyl-
cholinerase
۰ Physostigmine
۰ Neostigmine
۰ Proserine
۰ ACF inhibitor
ENZYMES
S T İ M U L A T I O N
Increase decarboxylase
activity
۰ Thiamine
۰ Phyridoxine
Increases hepatic glycogen
phosphorylase
۰ Adrenaline
INTERACT WITH CELL
MEMRANE
A number of medications show their effects by disrupting
the transport of ions in the body. These medications can
be used to modify ion channels conductance.
D R U G I O N C H A N N E L U S E
QUINIDINE Miocardial Na+ cannels Arrhythmiya
AMIODARONE Miocardial K+ cannels Arrhythmiya
SULFONYLUREAS Pancreatic K+ channels Insulin
PHENYTOIN Neuronal Na+ channels Epilepsy
C A R R I E R T R A N S P O R T B L O C K E R
Norepinephrine transporter Noradrenaline (norepinephrine) Desipramine, Cocaine
GAT1 GABA Tiagabine
Na+ - K+ - 2Cl- cotransporter Na+, K+, Cl- Furosemide
Serotonin transporter Serotonin Fluoxetine
CELL MEMBRANE
P H Y S I C A L
۰ Isaphgula - laxatives
۰ Dimethicone – ulcer dressing
۰ Paraaminobenzoic acid –
sunscreen
۰ Activated charcoal – drug
overdose
DIRECT ACTION
C H E M I C A L
۰ Antasid – hiper
tuşululuq
۰ Potassium
permanqanat –
antibakterial
۰ Xolestiramin -
hiperxolesterolemiya
THANK YOU

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Pharmacodynamics

  • 2. Pharmacodynamıcs The study of biochemical cellular and physiological effects of medications and their mechanisms of action. More simply, it is what medications do and how they do it.
  • 3. ۰ S T İ M U L A T I O N Selective enhancement of the effectiveness of specialized cells. Effect of acetylcholine on salivary glands. ۰ D E P R E S S I O N Selective reduction of the effectiveness of specialized cells. Effect of salbutamol on uterine muscles. ۰ I R R I T A T I O N Non-selective, often noxious effect on less specialized cells. Capsaicin in herpetic neuralgia. ۰ R E P L A C E M E N T Use of natural metabolites, hormones and their congeners in deficiency states. Iron supplementation in iron deficiency anemia. Insulin in diabetes. ۰ C Y T O T O X I C Selective effect on bacteria - penicillin, cephalosporins. Selective effect on cancer cells - methotrexate, cisplatin. FEATURES OF EFFECT
  • 4. PRINCIPLES OF MEDICATION EFFECTS DOSE RESPONSE Max effect – All receptors occupied 100% 50% A F F I N I T Y D O S E Not enough receptors bind More receptor- medication complexes Effective dose (ED50)
  • 5. DOSE RESPONSE Max effect 100% DOSE RESPONSE Max effect 100% 60% > More potent > More efficacious They require different dose to reach the same Max effect Same ED50, different Max effect.
  • 6. INRERACT WITH RECEPTOR They are macromolecular compounds that are sensitive to certain chemical compounds. As a result of their interaction with chemical compounds, various biochemical and physiological changes occur in the body. Types: ۰ G-protein coupled receptors ۰ Ion channels ۰ Enzyme-coupled receptors ۰ Intracellular receptors
  • 7. RECEPTORS A G O N İ S T Mimics the action of ligands and activates the receptor. DOSE RESPONCE All available receptors are bound to an agonists. - full agonist - partial aqonist 100% 70% A N T A G O N İ S T Binds to receptors without activating them, instead decreases receptor’s ability to be activated by other agonists.
  • 8. DOSE RESPONSE Max effekt - full agonist - with reversible antagonist 100% 50% ED50 DOSE RESPONCE Max effekt - full agonist - with irreversible antagonist 100% 50% ED50 70%
  • 9. INTERACT WITH ENZYMES A number of drugs alter the effects of drugs by slowing down or increasing the activity of enzymes. The increase in activity may occur by enzyme induction.
  • 10. I N H I B I T I O N Inhinition of acetyl- cholinerase ۰ Physostigmine ۰ Neostigmine ۰ Proserine ۰ ACF inhibitor ENZYMES S T İ M U L A T I O N Increase decarboxylase activity ۰ Thiamine ۰ Phyridoxine Increases hepatic glycogen phosphorylase ۰ Adrenaline
  • 11. INTERACT WITH CELL MEMRANE A number of medications show their effects by disrupting the transport of ions in the body. These medications can be used to modify ion channels conductance.
  • 12. D R U G I O N C H A N N E L U S E QUINIDINE Miocardial Na+ cannels Arrhythmiya AMIODARONE Miocardial K+ cannels Arrhythmiya SULFONYLUREAS Pancreatic K+ channels Insulin PHENYTOIN Neuronal Na+ channels Epilepsy C A R R I E R T R A N S P O R T B L O C K E R Norepinephrine transporter Noradrenaline (norepinephrine) Desipramine, Cocaine GAT1 GABA Tiagabine Na+ - K+ - 2Cl- cotransporter Na+, K+, Cl- Furosemide Serotonin transporter Serotonin Fluoxetine CELL MEMBRANE
  • 13. P H Y S I C A L ۰ Isaphgula - laxatives ۰ Dimethicone – ulcer dressing ۰ Paraaminobenzoic acid – sunscreen ۰ Activated charcoal – drug overdose DIRECT ACTION C H E M I C A L ۰ Antasid – hiper tuşululuq ۰ Potassium permanqanat – antibakterial ۰ Xolestiramin - hiperxolesterolemiya