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In Progress: Labetalol Pathway, Pharmacokinetics

PA166344161 Last updated July 2024 Caroline F. Thorn
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Reactions
In Progress: Labetalol Pathway, Pharmacokinetics pathway diagram
In Progress: Labetalol Pathway, Pharmacokinetics — pathway diagram from PharmGKB / ClinPGx
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About this pathway

Labetalol in a non-selective beta-adrenergic antagonist and alpha-1 adrenergic antagonist used for the treatment of hypertension which can be used to treat hypertension during pregnancy [Article:38973651]. Initial experiments showed the presence of several labetalol metabolites in human urine which were numbered II, VI, VII, VIII and X [Article:7895603]. In vitro experiments in human liver microsomes documented the formation of phenolic glucuronide, labetalol benzyl glucuronide metabolite II, by UGT2B7, and an aliphatic glucuronide, possibly labetalol glucuronide metabolite X, which is formed by UGT1A1 [Article:18098064].

Reactions & interactions (12)

  • Activation
    Pregnancy UGT1A1
  • Biochemical Reaction
    labetalol labetalol 3-hydroxylated metabolite VI
  • Biochemical Reaction
    labetalol labetalol benzyl glucuronide metabolite II
  • Biochemical Reaction
    labetalol 3-hydroxylated metabolite VI labetalol glucuronidated metabolite VII
  • Biochemical Reaction
    labetalol 3-hydroxylated metabolite VI labetalol glucuronidated metabolite VIII
  • Biochemical Reaction
    labetalol 3-hydroxylated metabolite VI labetalol glucuronide metabolite X
  • Catalysis
    CYP2C19 Biochemical Reaction
  • Catalysis
    ABCB1 Transport
  • Catalysis
    UGT2B7 Biochemical Reaction
  • Catalysis
    UGT1A1 Biochemical Reaction
  • Inhibition
    Pregnancy CYP2C19
  • Transport
    labetalol labetalol

Edit history (1)

  • 2024-07-16 Create
In Progress: Labetalol Pathway, Pharmacokinetics pathway diagram (enlarged)