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. 2017 Feb 6;24(1):358–369. doi: 10.1080/10717544.2016.1255999

Table 2. Physicochemical and metabolic profile of antihypertensives showing poor oral bioavailability.

Class Drug Metabolism Solubility Log P Bioavailability
Calcium channel  blocker Nisoldipine Extensive gut wall metabolism, CYP3A4 substrate 5.7 μg/ml 3.1 <5%
  Nitrendipine Extensive hepatic first-pass metabolism by CYP3A4 2 μg/ml 3.59 10–20%
  Lacidipine Completely metabolized in liver by CYP3A4 0.84 μg/ml 5 10%
  Verapamil Extensively metabolized by CYP2C8, CYP2C18,  and CYP2C9 7 mg/ml 3.8 10–20%
  Nifedipine Hepatic metabolism by CYP3A4 20 μg/ml 2.20 45–56
  Amlodipine Metabolized by CYP3A4 75.3 μg/ml 2.22 64%
  Felodipine Inclusively metabolized by CYP3A4 7.15 μg/ml 4.36 15%
AT1 blocker Olmesartan Not metabolized by cytochrome P450 but is metabolized  by liver esterase 7.75 μg/ml 5.5 26%
  Valsartan CYP2C9 < 0.1 mg/ml 5.8 <25%
Beta blocker Carvedilol CYP1A2, CYP3A4, CYP1A1 CYP2D6, CYP2E1, CYP2C9 0.583 μg/ml 4.1 20%
Renin Inhibitor Aliskiren CYP3A4-mediated hepatic metabolism 122 mg/ml as hemifumarate salt 2.45 2.5%