Sparreboom

• Important organic cation/anion transporters

  • OAT1 - Kidneys - SLC22A6 - Inhibited by probenecid (novobiocin)
  • OAT3 - Kidneys - SLCC22A8 - Inhibited by probenecid (novobiocin)
  • OATP1B1 - Liver - SLCO1B1 - Inhibited by rifampicin among others
  • OATP1B3 - Liver - SLCO1B3 - Inhibited by rifampicin among others
  • OCT2 - Kidneys - SLC22A2 - Inhibited by cimetidine
• Bioavailability is defined as the fraction of the dose that reaches the systemic circulation in unchanged form, and the rate with which this occurs.
• Bioavailability of a drug from its dosage form depends on 3 major factors

  1. Pharmaceutical factors
  2. Route of administration
  3. Patient-related factors
• How drugs get into the body affects:

  • Speed of drug onset
  • Dosing interval
  • Site of action