Explain Active Secretion
(3rd step in Renal Excretion)
Tubular pumps secrete drugs into urine
(esp. in proximal convoluted tubule)
Explain pH-Dependent Ionization
Can manipulate urinary pH to speed up excretion
Example: Treat ASA overdose with sodium bicarbonate to
alkalinize urine
What does Competition for Active Transport cause?
2 Rx using same pump
=
↓ Excretion + ↑ Rx levels
Special Considerations for Renal Excretion in patients with renal
impairment.
What do you need to monitor?
↓ drug clearance, accumulation, risk of toxicity
Monitor creatinine clearance or eGFR
,Special Considerations for Renal Excretion in Children
Know this
Children (esp under 2 YO) have extremely immature kidneys,
haven't had much research done on them, and have increased
toxicity.
What is Minimum Effective Concentration (MEC)
Lowest blood level needed to cause the intended action
(Threshold for effect)
What is the Therapeutic Range?
Between Minimum Effective Concentration (MEC) + Toxic
Concentration
What determines dosing interval?
Half-Life (t½)
(Time for 50% of drug to be eliminated)
What is the loading dose?
Large initial dose to reach therapeutic level quickly
What do agonists do?
Partial agonists?
Antagonists?
Agonist: Activate receptor
Partial Agonist: Bind, but w/ reduced response.
, Antagonist: Block receptor
Describe Desensitization
(aka downregulation or refractory)
Know this
Receptors continually exposed to an agonists causing:
↓ # of receptors or receptor modification
Describe Hypersensitization
(aka upregulation or supersensitive)
Know this
Receptors continually exposed to antagonists causing:
↑ # of receptors
What should you NOT take with Statins?
Food or drink with any sort of acidity, including juices.
Describe Cytochrome P450 (CYP)
What do they do?
Know this
Liver enzymes that metabolize Rx to:
- Inactive forms
- Water-soluble forms (for excretion)
- Active metabolites (can ↑ therapeutic or toxic effects)
- Activate prodrugs