Absorption of paroxetine under various dietary conditions and following antacid intake

Greb, W. H.; Brett, Martin; Büscher, G.; Dierdorf, H.‐D.; Schrader, Harald; Wolf, David S.; Mellows, G.; Zussman, B. D.

doi:10.1111/j.1600-0447.1989.tb07185.x

Cited by 21 publications

(12 citation statements)

References 3 publications

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“…Drug‐food interactions are classified into 5 categories, based on the effect of food on absorption: those causing reduced, delayed, increased, or accelerated absorption, and those in which food has no effect 23 . Although SSRI antidepressants may be taken with or without food, their pharmacokinetics when taken with food may be altered to various degrees 13–15 . Peak plasma concentrations of paroxetine were increased by 29% and were noted 1.5 hours earlier when paroxetine was administered with food 13 .…”

Section: Discussionmentioning

confidence: 99%

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Pharmacokinetics of Dapoxetine, a New Treatment for Premature Ejaculation: Impact of Age and Effects of a High‐Fat Meal

Dresser¹,

Kang²,

Staehr³

et al. 2006

The Journal of Clinical Pharma

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Dapoxetine is being developed as a treatment for premature ejaculation and has demonstrated rapid absorption and elimination in previous pharmacokinetic studies. Two open-label studies were conducted in healthy men: a parallel-group pharmacokinetic and safety study in young and elderly men and a randomized crossover food-effect study. Maximal plasma dapoxetine concentrations (C(max)) were similar in young and elderly men (338 and 310 ng/mL, respectively), as were the corresponding area under the plasma concentration versus time curve (AUC) values (2040 and 2280 ng x h/mL, respectively). When coadministered with food, C(max) was reduced by 11% (398 vs 443 ng/mL in the fed and fasted states, respectively), and the peak was delayed by approximately 30 minutes, indicating that food slowed the rate of absorption; however, systemic exposure to dapoxetine (ie, AUC) was not affected by food consumption. Thus, age or consumption of a high-fat meal has only a modest impact on dapoxetine pharmacokinetics in healthy men.

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Section: Discussionmentioning

confidence: 99%

“…Coadministration of food can also affect the pharmacokinetics of a number of drugs 12 . Although the SSRI antidepressants paroxetine, sertraline, and fluoxetine may be taken with or without food, their absorption and/or elimination may be affected by food consumption 13–15 …”

mentioning

confidence: 99%

Pharmacokinetics of Dapoxetine, a New Treatment for Premature Ejaculation: Impact of Age and Effects of a High‐Fat Meal

Dresser¹,

Kang²,

Staehr³

et al. 2006

The Journal of Clinical Pharma

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“…In the present study, paroxetine (20 mg) was administered 5 h before the subject arrived at the laboratory and was followed by a standardized meal. This protocol should not have adversely influenced the rate of paroxetine absorption (Greb et al 1989), which was expected to reach a peak plasma and tissue concentration at the approximate time when exercise was due to commence (Kaye et al 1989). The minor differences in study protocol between the present study and previous studies (Wilson & Maughan, 1992; Struder et al 1998) cannot fully explain the failure of paroxetine administration to reduce exercise capacity.…”

Section: Discussionmentioning

confidence: 99%

Paroxetine administration to influence human exercise capacity, perceived effort or hormone responses during prolonged exercise in a warm environment

Strachan

Leiper

Maughan

2004

Experimental Physiology

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“…Single-dose studies have demonstrated that the bioavailability of paroxetine is unaffected by the presence or absence of food -whether the food is of high or low fat content, or by coadministration with milk (10). Thus, on pharmacokinetic grounds no dietary advice is necessary for the patient about to commence paroxetine therapy.…”

Section: Parametermentioning

confidence: 97%

“…Until more substantial data are available after repeated drug administration, it would seem advisable to commence paroxetine therapy in patients with severe hepatic impairment using doses towards the lower end of the range recommended for the genera! Table 12 summarizes the results of in viuo studies that have been undertaken to determine the effects of various drugs on the pharmacokinetics ofparoxetine (10,18,19), while Table 13 summarizes the effect of paroxetine on the pharmacokinetics of other drugs (e.g. antipyrine) (20), especially those with a narrow (19).…”

Section: Subjects With Hepatic Diseasementioning

confidence: 99%

A review of the metabolism and pharmacokinetics of paroxetine in man

Kaye

Haddock

Langley

et al. 1989

Acta Psychiatr Scand

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244

159

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Acta psychiatr. scand: 80 (supp. 350): 60-75 ABSTRACT -Paroxetine is well absorbed from the gastrointestinal tract, and appears to undergo first-pass metabolism which is partially saturable. Consistent with its lipophilic amine character, paroxetine is extensively distributed into tissues. Its plasma protein binding at therapeuticallyrelevant concentrations is about 95%. Paroxetine is eliminated by metabolism involving oxidation, methylation, and conjugation. All of these factors lead to wide interindividual variation in the pharmacokinetics of paroxetine. Renal clearance of the compound is negligible. The major metabolites of paroxetine are conjugates which do not compromise its selectivity nor contribute to theclinical response. Ascending single-dose studies reveal that the pharmacokinetics of paroxetine are non-linear to a limited extent in most subjects and to a marked degree in only a few. Also, steady-state pharmacokineticparameters are not predictable from single-dose data. In many subjects, daily administration of 20-50mg of paroxetine leads to little or no disproportionality in plasma levels with dose, although in a few subjects this phenomenon is evident. Steady-state plasma concentrations are generally achieved within 7 to 14 days. The terminal half-life is about one day, although there is a wide intersubject variability (e.g. with 30mg, a range of 7-65 hours was observed in a group of 28 healthy young subjects). In elderly subjects there is wide interindividual variation in steady-state pharmacokinetic parameters, with statistically significantly higher plasma concentrations and slower elimination than in younger subjects, although there is a large degree of overlap in the ranges of corresponding parameters. In severe renal impairment higher plasma levels of paroxetine are achieved than in healthy individuals after single doses. In moderate hepatic impairment the pharmacokinetics after single doses are similar to those of normal subjects. Paroxetine is not a general inducer or inhibitor of hepatic oxidation processes, and has little or no effect on the pharmacokinetics of other drugs examined. Its metabolism and pharmacokinetics are to some degree affected by the induction or inhibition of drug metabolizing enzyme(s). From a pharmacokinetic standpoint, drug interactions involving paroxetine are considered unlikely to be a frequent occurrence. Data available have failed to reveal any correlation between plasma concentrations of paroxetine and its clinical effects (either efficacy or adverse events). Paroxetine (Fig. l), a potent, selective 5-HT uptake inhibitor, currently being developed as a n antidepressant d r u g (1,2), has been review are in terms of the pure free base. extensively studied in man to examine its metabolism andpharmacokinetics. This review provides a summary of the key findings to date, extending earlier observations (3,4). Paroxetine is administered as its hydrochloride salt (BRL 29060A), but doses quoted throughout this Analytical methodology Paroxetinecan be determined in biologi...

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Absorption of paroxetine under various dietary conditions and following antacid intake

Cited by 21 publications

References 3 publications

Pharmacokinetics of Dapoxetine, a New Treatment for Premature Ejaculation: Impact of Age and Effects of a High‐Fat Meal

Pharmacokinetics of Dapoxetine, a New Treatment for Premature Ejaculation: Impact of Age and Effects of a High‐Fat Meal

Paroxetine administration to influence human exercise capacity, perceived effort or hormone responses during prolonged exercise in a warm environment

A review of the metabolism and pharmacokinetics of paroxetine in man

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