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Pharmacokinetics

 Dr. Farhan Ahmad
• the magnitude of response depends on
  concentration of the drug at the site of
  action
PHARMACOKINETICS
   What the body does to drug
• ABSORPTION



• DISTRIBUTION



• METABOLISM



• EXCRETION
Absorption

The movement of a drug from its
point of entry into the body into
      systemic circulation
• I.V- completely (100%) absorbed
• Oral- delayed and incomplete.
• Rate: how rapidly does the drug get from
  its site of administration, to the general
  circulation?
• Extent: How much of the administered
  dose enters the general circulation (per cent
  bioavailability = F)?
Absorption of Drugs

1.   Sites of absorption through the GI tract
2.   Factors that modify absorption in the GI tract
3.   Bioavailability
4.   Other sites of drug administration/absorption




                                              10
Absorption of Drugs

1. Sites of absorption through the GI tract

   1)   Mouth
   2)   Stomach
   3)   Small intestine
   4)   Large intestine




                                       11
Absorption of Drugs
2. Factors that modify absorption in the GI tract
   1) Drug solubilization
   2) Ph of the medium
   3) Lipid solubility of the drug
   4) Blood flow at the absorption site
   5) Surface area of absorption
   6) Route of administration (First Pass Effect in Oral Route)
   7) Gastric emptying
   8) Food
   9) Intestinal motility
   10) Metabolism of drug by GI tract
                                                     12
Absorption of Drugs
Factors that modify absorption in the GI tract
     Drug solubilization – breaking drugs into smaller, more
                     absorbable particles
      .
                     DISINTEGRATION (solid )
                              ⇓
                     DISSOLUTION (solution)
                              ⇓
                          ABSORPTION
                              ⇓
              SYSTEMIC CIRCULATION (% bioavailability)




                                                     13
Ph of the medium

stomach (pH 1~3)

in favour of weak acid
absorption


duodenum (pH 5~7)

in favour of weak base
absorption


ileum (pH 7~8)
in favour of weak base
absorption
pH and ionization

Acidic drugs are best absorbed in Acidic
                 medium



 Basic drugs are best absorbed in Basic
                medium
 Gastric emptying
  small intestine – primary site of drug absorption
  Anything that delays/accelerates gastric emptying will
  decrease/increase drug absorption.
 Food
  High fat food – delay gastric emptying – slow
  absorption

                                          16
Bioavailability
Bioavailability is defined as the fraction of unchanged drug
reaching the systemic circulation following administration
by any route .




20.10.09                                        18
Bioavailability of a drug
• The bioavailability of a drug (by a route
  other than intravenous) is given by:
              AUC (extra vascular)
•    F=      -----------------------------
              AUC (intravenous)

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1. Pk Absorption

  • 2.
  • 3. • the magnitude of response depends on concentration of the drug at the site of action
  • 4. PHARMACOKINETICS What the body does to drug • ABSORPTION • DISTRIBUTION • METABOLISM • EXCRETION
  • 5. Absorption The movement of a drug from its point of entry into the body into systemic circulation
  • 6. • I.V- completely (100%) absorbed • Oral- delayed and incomplete.
  • 7. • Rate: how rapidly does the drug get from its site of administration, to the general circulation? • Extent: How much of the administered dose enters the general circulation (per cent bioavailability = F)?
  • 8.
  • 9.
  • 10. Absorption of Drugs 1. Sites of absorption through the GI tract 2. Factors that modify absorption in the GI tract 3. Bioavailability 4. Other sites of drug administration/absorption 10
  • 11. Absorption of Drugs 1. Sites of absorption through the GI tract 1) Mouth 2) Stomach 3) Small intestine 4) Large intestine 11
  • 12. Absorption of Drugs 2. Factors that modify absorption in the GI tract 1) Drug solubilization 2) Ph of the medium 3) Lipid solubility of the drug 4) Blood flow at the absorption site 5) Surface area of absorption 6) Route of administration (First Pass Effect in Oral Route) 7) Gastric emptying 8) Food 9) Intestinal motility 10) Metabolism of drug by GI tract 12
  • 13. Absorption of Drugs Factors that modify absorption in the GI tract  Drug solubilization – breaking drugs into smaller, more absorbable particles . DISINTEGRATION (solid ) ⇓ DISSOLUTION (solution) ⇓ ABSORPTION ⇓ SYSTEMIC CIRCULATION (% bioavailability) 13
  • 14. Ph of the medium stomach (pH 1~3) in favour of weak acid absorption duodenum (pH 5~7) in favour of weak base absorption ileum (pH 7~8) in favour of weak base absorption
  • 15. pH and ionization Acidic drugs are best absorbed in Acidic medium Basic drugs are best absorbed in Basic medium
  • 16.  Gastric emptying small intestine – primary site of drug absorption Anything that delays/accelerates gastric emptying will decrease/increase drug absorption.  Food High fat food – delay gastric emptying – slow absorption 16
  • 17.
  • 18. Bioavailability Bioavailability is defined as the fraction of unchanged drug reaching the systemic circulation following administration by any route . 20.10.09 18
  • 19. Bioavailability of a drug • The bioavailability of a drug (by a route other than intravenous) is given by: AUC (extra vascular) • F= ----------------------------- AUC (intravenous)

Notas do Editor

  1. The action of the body on the drugs The way the body handles drugs determines the dose, route and frequency of administration The handling of drugs by the body can be split into absorption, distribution and elimination
  2. Rate of absorption determines the time to the peak concentration The extent of absorption determines the height of the peak concentration
  3. 1 1 1 1
  4. AUC is an index of the total amount of drug absorbed systemically.