Clinical Pharmacology & Therapeutics

TABLE III

FROM:

Grapefruit juice increases serum concentrations of atorvastatin and has no effect on pravastatin

Jari J. Lilja, Kari T. Kivistö and Pertti J. Neuvonen

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Table III. The pharmacokinetic variables of pravastatin and its metabolites in 11 subjects after ingestion of 40 mg pravastatin with water or grapefruit juice

  Cmax (ng dot mL-1) tmax (h) Elimination t1/2 (h) AUC(0–24) (ng dot mL-1 dot h) AUC(0-infinity) (ng dot mL-1 dot h)
  Water Grapefruit juice Water Grapefruit juice Water Grapefruit juice Water Grapefruit juice Water Grapefruit juice
Pravastatin45.3 plusminus 28.042.6 plusminus 25.31 (1–2)2 (1–3)2.0 plusminus 0.61.7 plusminus 0.4111.7 plusminus 68.1102.8 plusminus 49.6112.3 plusminus 66.3103.0 plusminus 48.4
 % of control10094    1009210092
 Range 39–193     49–193 50–184
Pravastatin lactone1.6 plusminus 0.91.6 plusminus 0.72 (0.5–2)2 (2–3)NDND3.3 plusminus 2.33.7 plusminus 1.8NDND
 % of control100100    100112  
 Range 47–265     45–439  
Active HMG-CoA reductase inhibitors49.4 plusminus 32.141.9 plusminus 21.21 (1–2)2 (1–3)* 1.9 plusminus 1.21.6 plusminus 0.3121.3 plusminus 75.7110.6 plusminus 50.4127.1 plusminus 75.9115.0 plusminus 49.5
 % of control10085    1009110090
 Range 45–200     52–181 52–180
Total HMG-CoA reductase inhibitors47.9 plusminus 26.343.1 plusminus 21.41 (1–2)2 (1–3)1.2 plusminus 0.41.5 plusminus 0.4110.4 plusminus 66.3103.3 plusminus 48.2116.8 plusminus 68.0113.3 plusminus 49.3
 % of control10090    1009410097
 Range 38–167     57–189 59–193

 Data are mean values plusminus SD; tmax data are given as median with range.

 Cmax, Peak serum concentration; tmax, time to reach Cmax; t1/2, half-life; AUC(0–24), area under the serum concentration–time curve from 0 to 24 hours; AUC(0-infinity), area under the serum concentration–time curve from time zero to infinity; ND, not determined; HMG-CoA, 3-hydroxy-3-methylglutaryl coenzyme A.

*  P < .05 versus control phase (water).

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