![]() renal dysfunction, cholestasis, paraesthesia)Ĭyclosporin and cyclosporin metabolite serum concentrations may be significantly increased when this drug is co-administered with grapefruit juice. Increased risk of cyclosporin toxicity (e.g. Grapefruit juice had no significant effect on the AUC of prednisolone or prednisone. Similar results have been seen with oestradiol and oestrone. It seems unlikely that this interaction is of practical importance as the increased bioavailability is still less than the extent of known variability between individuals. There is an increase in AUC of 28% and serum concentrations of 37% when 50 microgram of ethinyloestradiol is taken with 200 mL of grapefruit juice. One study showed no interaction with clozapine or its major metabolite desmethylclozapine. ![]() The increase could be due to effects on the intestinal rather than hepatic CYP3A4. Whether this inhibition is sustained over time is not known. Two case reports showed that grapefruit juice increased the trough plasma concentration of clomipramine. Monitor for adverse effects.Ĭlomipramine is metabolised by several different CYP pathways including 1A2, 3A4 and 2D6. 7, 8Ī randomised crossover study of 12 healthy volunteers showed that grapefruit juice increased time to peak concentration but did not affect other pharmacokinetic parameters. No volunteer experienced a change in heart rate, blood pressure or QT interval. There was a slight but significant increase in the elimination half-life of cisapride during a two-phase crossover study. Grapefruit juice was shown to increase the oral bioavailability of cisapride in 14 volunteers but large inter-individual variations were noted. Monitor for adverse effects or avoid grapefruit juice cardiotoxicity, QT prolongation, torsade de pointes)Īre fair but clinical significance unknown. Increasing serum concentrations increase the risk of adverse effects (e.g. Grapefruit juice increased peak concentration by 40.4%, trough concentration by 39.2% and AUC by 40.8% during a randomised crossover study. However, there was considerable inter-individual variability. Inter-individual variability with serum levelsĪ study of 10 healthy volunteers found that 200 mL of double strength grapefruit juice three times a day increased buspirone's AUC, peak concentration, time to peak concentration and half-life. 4Įlevated plasma concentrations resulting in increased risk of adverse effectsĬlinical significance unknown - there is considerable However, they are all likely to be safe to take with grapefruit juice as their high oral bioavailability leaves little room for elevation by grapefruit juice. No data exist for alprazolam, chlordiazepoxide, clonazepam, flurazepam and lorazepam. 3īenzodiazepines (see also diazepam and triazolam) AUC of active and total atorvastatin increased by 20-50%. Grapefruit juice was found to increase the AUC of atorvastatin acid and atorvastatin lactone approximately threefold. Increased bioavailability of atorvastatin resulting in increased risk of myopathy or rhabdomyolysis There were no differences in blood pressure and heart rate. No adverse haemodynamic effects reported.Ī controlled study found a slight interaction between amlodipine and grapefruit juice, the amlodipine AUC was 116% and Cmax was 115% of normal values. Increased serum amlodipine concentrations. The reductions in PR and QT cintervals caused by amiodarone were also diminished. Reduction in major metabolite production and increase in serum amiodarone concentrationĪ study of 11 healthy volunteers showed that grapefruit juice inhibited the production of N-desmethylamiodarone (the major metabolite of amiodarone) and significantly increased the AUC * and Cmax † of amiodarone. The absence of a drug from this table does not indicate that there is no interaction.Drugs which are not available in Australia at the time of publication are not listed.
0 Comments
Leave a Reply. |
AuthorWrite something about yourself. No need to be fancy, just an overview. ArchivesCategories |