Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0235290 (bitter taste)
 1,408 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Oral midazolam is a frequently used sedative in pediatric dentistry. Although an oral form of midazolam is now commercially available, some practitioners continue to use the IV midazolam as an oral medication. If the injectible form of midazolam is administered orally, its bitter taste requires the use of a flavoring agent. Grapefruit juice is contraindicated for this purpose as it inhibits cytochrome P450 (CYP) 3A4. CYP 3A4 is located in the intestine and liver. Inhibition of this cytochrome results in delayed absorption and reduced first pass effect on midazolam. This results in increased blood plasma levels of midazolam of 56% and increased midazolam bioavailability of 35%. This can result in excessive levels of sedation for the pediatric patient. Grapefruit juice is therefore contraindicated for use with oral midazolam.
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PMID:Oral midazolam-grapefruit juice drug interaction. 1157 3

Naringin is the chief flavanone glycoside of grapefruit (Citrus paradisi). It is responsible for part of the bitter taste of the fruit and can cause the inhibition of some cytochrome P450s. The direct separation of (2R)- and (2S)-naringin in the albedo of grapefruits was obtained in normal phase HPLC mode using Chiralcel OD as chiral stationary phase and n-hexane/ethanol with 0.1% of TFA as mobile phase. Chiralpak AD was almost ineffective in the separation. This procedure was used to evaluate the stereochemistry at C-2 during maturation of the grapefruit. The CD curves of (2R)- and (2S)-naringin isolated by semipreparative chiral HPLC were determined and the elution order of the chromatographic peaks was related to the absolute C-2 configuration. Partial resolution of the C-2 diastereomers of narirutin was obtained on Chiralpak AD.
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PMID:Chiral HPLC separation and CD spectra of the C-2 diastereomers of naringin in grapefruit during maturation. 1292 3