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General pharmacology презентация
Содержание
- 1. General pharmacology
- 2. «All is a poison, all is a
- 4. PHARMACOKINETICS PROCESSES: ► Absorption
- 7. For most majority of drugs
- 13. VOLUME of DESTRIBUTION (Vd) – a
- 14. Volume of destruburion (Vd) –
- 15. Vd is the ratio of
- 17. Phase I – Metabilic
- 18. Phase II – Conjugation Reactions with
- 19. Enzyme Induction - the ability of some
- 20. Enzyme Inhibition - the ability of drugs
- 22. Clearance of a Drug Cl =
- 23. Steady State
- 24. For drugs with Michaelis-Menten
- 25. For drugs with 1st
- 29. 50 % of the drug is
- 40. Placebo
- 41. Thank You for Attention!
«All is a poison, all is a medicine; either depends on the dose» Paracelsus (1493-1541)
Слайд 1
Zaporizhzhia State Medical University
Pharmacology Department
General Pharmacology
Lecture №1
Lecturer: Assoc. Prof. Irene
Слайд 4
PHARMACOKINETICS PROCESSES:
► Absorption
►Distribution
►Binding /Localization /Storage
►Biotransformation
►Elimination
Слайд 7
For most majority of drugs
BIOAVAILABILITY is equal to
40-70%
- Average level
If Bioavailability
< 40% - Low level
< 70% - High level
If Bioavailability
< 40% - Low level
< 70% - High level
Слайд 13VOLUME of DESTRIBUTION (Vd) – a hypothetical volume of fluid into
which
the drug is disseminated
Water compartments in the body:
1). EXTRACELLULAR Volume - 14 L
a). PLASMA Volume - 4 L
b). INTERSTITIAL Volume - 10 L
2). INTRACELLULAR Volume - 28 L
Слайд 14 Volume of destruburion (Vd) –
is a hypothetical volume of fluid into which
the drug is dissemineted
Water compartments in the body:
1. Extracellular Volume - 14 L
● plasma Volume - 4 L
●interstitial Volume - 10 L
2. Intracellular Volume - 28 L
the drug is dissemineted
Water compartments in the body:
1. Extracellular Volume - 14 L
● plasma Volume - 4 L
●interstitial Volume - 10 L
2. Intracellular Volume - 28 L
Слайд 15 Vd is the ratio of
the total amount of drug
in the body to
the concentration of drug in plasma:
Vd = D/C or C = D/Vd
D – total amount of drug in the body
C – plasma concentration of drug
Vd = 100 mg / 25 mg/L = 4 L
Vd = 100 mg / 7 mg/L = 14 L
Vd = 100 mg/0.25 mg/L = 400 L
the concentration of drug in plasma:
Vd = D/C or C = D/Vd
D – total amount of drug in the body
C – plasma concentration of drug
Vd = 100 mg / 25 mg/L = 4 L
Vd = 100 mg / 7 mg/L = 14 L
Vd = 100 mg/0.25 mg/L = 400 L
Слайд 17 Phase I – Metabilic Biotransformation
Lipophilic
molecules => Polar Molecules by introducing or unmasking a polar functional group, such as –OH or –NH2
a) Utilizing the Cytochrome P-450
b) Not involving the Cytochrome P-450
►Oxidation
►Reduction
► Hydrolysis
a) Utilizing the Cytochrome P-450
b) Not involving the Cytochrome P-450
►Oxidation
►Reduction
► Hydrolysis
Слайд 18Phase II – Conjugation Reactions with
an Endogenous substrate:
● Glucuronic
acid
● Sulfuric acid
● Acetic acid
● Amino acid
=> Polar Water-Soluble compounds that are
most often therapeutically inactive
● Sulfuric acid
● Acetic acid
● Amino acid
=> Polar Water-Soluble compounds that are
most often therapeutically inactive
Слайд 19Enzyme Induction - the ability of some drugs
to
induce CYP-450 by:
? the rate of its synthesis or
? its rate of degradation:
Phenobarbital
Isoniazid
Glucocorticoides
Anticonvulsants
Macrolid antibiotics
Chronic ethanol administration
Steroids
? the rate of its synthesis or
? its rate of degradation:
Phenobarbital
Isoniazid
Glucocorticoides
Anticonvulsants
Macrolid antibiotics
Chronic ethanol administration
Steroids
Слайд 20Enzyme Inhibition - the ability of drugs
to inhibit CYP-450 by:
?
the rate of its synthesis or
? its rate of degradation.
Cimetidine and Ketoconazol bind to
the heme iron of CYP-450 and
?Metabolism of Endogenous Substrates and
other coadministered drugs.
Ethinylestradiol
Spironolacton
Allobarbital
? its rate of degradation.
Cimetidine and Ketoconazol bind to
the heme iron of CYP-450 and
?Metabolism of Endogenous Substrates and
other coadministered drugs.
Ethinylestradiol
Spironolacton
Allobarbital
Слайд 22Clearance of a Drug
Cl = Rate of Elimination / C
First-order (exponential ) kinetics
Rate of Elimination = Cl x C
Слайд 23
Steady State Plasma Concentration (Css)
Dose
Css = ———— or Dose = Css x Cl
Cl
!! Doubling the Dose rate would Double the Css
Css = ———— or Dose = Css x Cl
Cl
!! Doubling the Dose rate would Double the Css
Слайд 24
For drugs with Michaelis-Menten kinetics, elimination changes from 1st
Order to Zero Order kinetics
over the therapeutic range
Vmax x C
Rate of Elimination = ——————
KM + C
Vmax - the maximum rate of drug elimination
Km - the drug concentration at which
the rate of elimination is 50% of Vmax
over the therapeutic range
Vmax x C
Rate of Elimination = ——————
KM + C
Vmax - the maximum rate of drug elimination
Km - the drug concentration at which
the rate of elimination is 50% of Vmax
Слайд 25
For drugs with 1st order kinetics:
Vmax x C
Rate of Elimination = —————
KM + C
For drugs with Zero Order kinetics over
the therapeutic range:
Vmax x C
Rate of Elimination = ———— = Vmax
C
Rate of Elimination = —————
KM + C
For drugs with Zero Order kinetics over
the therapeutic range:
Vmax x C
Rate of Elimination = ———— = Vmax
C
Слайд 40 Placebo is an inert substance
which
is given in the garb of a medicine.
Placebo causes some effects up to 20-40% of cases.
It can be:
1) Positive - 84%
2) Negative 5-7%
3) Mix placebo effect - 9-12%
is given in the garb of a medicine.
Placebo causes some effects up to 20-40% of cases.
It can be:
1) Positive - 84%
2) Negative 5-7%
3) Mix placebo effect - 9-12%
