8-13 Pharmacology of Receptors Flashcards Preview

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Flashcards in 8-13 Pharmacology of Receptors Deck (4)
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1
Q
  • OAT *

1A. Type of Transporter
1B. Transporter Group

  1. TYPE of Substrate it imports/exports [3]
  2. Prototypical Drug associated [3]
  3. Inhibitors of OAT
  4. Location [2]
  5. Clinical Significance / Drug Interactions to remember [2]
A
  • OAT Importer *

1A. IMPORTER (imports using a-ketogluturate antiporter)
1B. SLC

  1. [Organic Anions] / Broad Range / low MW
  2. Methotrexate / NSAIDs / Cidefovir
  3. PROBENACID
  4. Kidney PCT & Liver
    • PROBENACID BLOCKS the [OAT Importer] which prevents Cidefovir from causing renal damage from PCT hypersecretion

-NSAIDs utilize the [OAT Importer] in the PCT Kidney so much to be eliminated that it prevents methotrexate from getting out—> Methotrexate Toxicity

2
Q
  • OATP *

1A. Type of Transporter
1B. Transporter Group

  1. TYPE of Substrate it imports/exports [2]
  2. Prototypical Drug associated
  3. Inhibitors of OATP [2]
  4. Location [3]
  5. Clinical Significance / Drug Interactions to remember [2]
A
  • OATP Importer *

1A. IMPORTER (imports using HCO3 antiporter)
1B. SLC

  1. Amphipathic anions / MW >350
  2. Statins
  3. CYCLOSPORIN / MACROLIDES
  4. Kidney PCT & Liver & Intestine
    • CYCLOSPORIN BLOCKS [OATP Importer] in the Liver and prevents Statin from being imported—> Statin Toxicity

-[OATP Importer] polymorphisms ALSO cause Statin inability to be imported into liver–> Statin Toxicity

3
Q
  • OCT / MATE *

1A. Type of Transporter
1B. Transporter Group

  1. TYPE of Substrate it imports/exports
  2. Prototypical Drug associated [4]
  3. Inhibitors of [OCT / MATE]
  4. Location
  5. Clinical Significance / Drug Interactions to remember
A
  • OCT / MATE Team Transporters *

1A. [OCT IMPORTER] (imports using passive facilitated diffusion) &
[MATE EXPORTER] (Exports using H+ antiport)
1B. SLC

  1. small cations
  2. Metformin / Cisplatin / Cimetidine / Procainamide
  3. NO INHIBITORS
  4. [Kidney PCT] & Liver & Intestine
  5. -Cimetidine hyperOccupies the [OAT / MATE system] in the [Kidney PCT] and prevents drugs like Procainamide from getting out –>TOXIC!
    on the other hand…
    -Cimetidine hyperOccupies the [OAT / MATE system] in the [Kidney PCT] and prevents Cisplatin from rushing out too fast—> actually prevents [Cisplatin-induced nephrotoxicity]
4
Q
  • PGP *

1A. Type of Transporter
1B. Transporter Group

  1. TYPE of Substrate it imports/exports [3]
  2. Prototypical Drug associated [3]
  3. Inhibitors of PGP [2]
  4. Location [3]
  5. Clinical Significance / Drug Interactions to remember [3]
A
  • PGP Exporter *

1A. EXPORTER (exports using ATP!!!!)
1B. ABC group

  1. [Bulky hydrophobic] / Neutral or + charge / Broad range
  2. Digoxin / Loperamide / Etoposide
  3. CYCLOSPORIN / VERAPAMIL
  4. Kidney PCT & Liver & Intestine
    • CYCLOSPORIN & VERAPAMIL Block the [PGP Exporter] which allows toxins and Loperamide to pass into the BBB—> TOXIC
  • CYCLOSPORIN Blocks [PGP Exporter] in [Kidney PCT] and allows Digoxin to INC—-> TOXIC
  • [Rifampicin & St. Johns wort] both INC [PGP Exporter] activity —> INC Drug elimination —> DEC Drug effect