Table 4.
The major pharmacokinetic variability factors, and their use for dose adjustment of the clinically approved toxin-derived peptide drugs.
| Drug | Variability Factor | Dose Adjustment |
|---|---|---|
| Captopril | dimerization and interaction with endogenous thiol-containing compounds in the plasma | - |
| active tubular secretion in the kidneys | dose reduction in renal insufficiency | |
| Cyclosporine | body weight | therapeutic monitoring of trough blood concentrations dosage adjustment taking into account the variability factors |
| co-administration of inhibitors of CYP3A | ||
| hematocrit | ||
| and additional factors | ||
| Eptifibatide | renal elimination of the drug | maintain the IV bolus component and reduce the IV infusion component of the dosage regimen in patients with renal insufficiency |
| Lepirudin | renal elimination of the drug | dose selection based on patients’ weight dose reduction in renal insufficiency monitoring of anticoagulant effects (aPTT test) |
| gender, age, and disease state affect the drug distribution and elimination | ||
| Bivalirudin | renal elimination of the drug | dose selection based on patients’ weight dose reduction in renal insufficiency monitoring of anticoagulant effects (aPTT test) |
| Ziconotide | not reported | - |
| Exenatide | body weight | - |
| renal elimination of the drug | dose reduction in renal insufficiency | |
| Lixisenatide | body weight | - |
| renal elimination of the drug | no dose reduction, but close monitoring of drug safety, in mild or moderate renal impairment; use of the drug in patients with end stage renal disease is not recommended | |
| Linaclotide | not reported | - |
| Plecanatide | not reported | - |