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Dr.S.VASANTH
Route with high bio availability ……….?
Transport across biological membrane ….?
Absorption of drug …….?
Distribution of drug ….?
Plasma proteins ……….?
What is pharmacokinetics ?
ADME
Transport across biological memberane
Lipid
passive transport
Active transport
Facilitated diffusion
Symport
Antiport
Primary active transport
Secondary active transport
 pH of medium = pKa then drug is 50 %
unionised and 50 % ionized
 pH more than Pka medium is alkaline
 Acidic drugs ,ionization form increases and
nonionized decreases
 Basic drugs, unionized form increases and
ionized form decreases
 Absorption is movement of the drug from its
site of administration into the circulation
 Different routes of drug absorption ?
 Factors affecting drug absorption ?
 Lipid solublity /aqueous solublity
 pH/pKA value
 Gastric emptying /gut motility
 Particle size and formulation
 Food and presence of other substance /drug
 Gastrointestinal disease
 First pass metabolism
What is first pass metabolism ?
What is bioavailablity ?
 Nitrates
 Hydrocortisone
 Lignocaine
 Propanolol
 Salbutamol
 morphine
 Rate and extent of a drug form the dosage
form in unchanged form in the systemic
circulation
 Fraction of drug or percentage of drug
reaches systemic circulation in unchanged
form
 Lipid solublity /ionization /pH
 Area of absorbing surface
 Blood circulation
 Gastric motility
 Presence of food
 Disease state of git
First pass metabolism
Pharmaceutical factors
disintegration time
dissolution rate/time
Genetic influence's
 Bioequvalance?
Phenytoin
a(dilantin)
Phenytoin b
(eptoin)
 Apparent volume of distribution
 Volume in which drug appears to be
distributed ( apparent )if concentration
throughout the body was same to that of the
plasma
 aVd= dose administered I.V /plasma
concentration achieved
 1). tissue permeability of drug
a. physicochemical property – i) molecular size
ii) pKa
iii) o/w partion coefficient
b. physiological barriers
 2). Organ tissue size and perfusion rate
 3). Binding of drug to tissue components
a. with blood components
b.with extravascular tissue proteins
4). Miscellaneous factors
a. age
b.Pregnancy
d.Obesity
e.Diet
f.Disease states
g.Drug interaction

 Redistribution ?
 Plasma protein binding
 Albumin
 Alpha1 acid glycoproteins
 Maintance of plasma concentration
 Free and bound form measurement
 Low vd- highly bound form
 Long acting – highly bound
 Not removed by hemodialysis
 Displacement reaction
 Hypoalbuminemia ,chirosis
 Diazepam
 Midazolam
 Warfarin
 Imipramine
 cyclosporine
Bioavailablity 100% ……… ?
Bioequvalence ?.............
Volume of distribution ?
Significance of plasma protein binding ??

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Absorption and distribution of drugs

  • 2. Route with high bio availability ……….? Transport across biological membrane ….? Absorption of drug …….? Distribution of drug ….? Plasma proteins ……….?
  • 4.
  • 5. Transport across biological memberane Lipid
  • 6.
  • 7. passive transport Active transport Facilitated diffusion Symport Antiport Primary active transport Secondary active transport
  • 8.
  • 9.  pH of medium = pKa then drug is 50 % unionised and 50 % ionized  pH more than Pka medium is alkaline  Acidic drugs ,ionization form increases and nonionized decreases  Basic drugs, unionized form increases and ionized form decreases
  • 10.  Absorption is movement of the drug from its site of administration into the circulation  Different routes of drug absorption ?  Factors affecting drug absorption ?
  • 11.  Lipid solublity /aqueous solublity  pH/pKA value  Gastric emptying /gut motility  Particle size and formulation  Food and presence of other substance /drug  Gastrointestinal disease  First pass metabolism
  • 12. What is first pass metabolism ? What is bioavailablity ?
  • 13.  Nitrates  Hydrocortisone  Lignocaine  Propanolol  Salbutamol  morphine
  • 14.  Rate and extent of a drug form the dosage form in unchanged form in the systemic circulation  Fraction of drug or percentage of drug reaches systemic circulation in unchanged form
  • 15.
  • 16.  Lipid solublity /ionization /pH  Area of absorbing surface  Blood circulation  Gastric motility  Presence of food  Disease state of git
  • 17. First pass metabolism Pharmaceutical factors disintegration time dissolution rate/time Genetic influence's
  • 18.
  • 20.  Apparent volume of distribution  Volume in which drug appears to be distributed ( apparent )if concentration throughout the body was same to that of the plasma  aVd= dose administered I.V /plasma concentration achieved
  • 21.  1). tissue permeability of drug a. physicochemical property – i) molecular size ii) pKa iii) o/w partion coefficient b. physiological barriers  2). Organ tissue size and perfusion rate  3). Binding of drug to tissue components a. with blood components b.with extravascular tissue proteins 4). Miscellaneous factors a. age b.Pregnancy d.Obesity e.Diet f.Disease states g.Drug interaction 
  • 22.
  • 24.  Plasma protein binding  Albumin  Alpha1 acid glycoproteins
  • 25.  Maintance of plasma concentration  Free and bound form measurement  Low vd- highly bound form  Long acting – highly bound  Not removed by hemodialysis  Displacement reaction  Hypoalbuminemia ,chirosis
  • 26.
  • 27.  Diazepam  Midazolam  Warfarin  Imipramine  cyclosporine
  • 28. Bioavailablity 100% ……… ? Bioequvalence ?............. Volume of distribution ? Significance of plasma protein binding ??