What are pharmacokinetics of paclitaxel?
Table of Contents
Pharmacokinetic studies in which adults have been administered pacliaxel intravenously over 1 to 96 hours have demonstrated the following pharmacokinetic characteristics: extensive tissue distribution; high plasma protein binding (approximately 90 to 95%); variable systemic clearance, with average clearances ranging …
What is the half life of paclitaxel?
The pharmacokinetics of paclitaxel were determined following 3- and 24-hour infusions at doses of 135 and 175 mg/m2. The mean half-life was between 3.0 and 52.7 hours, and the mean non-compartmentally derived value for total body clearance was between 11.6 and 24.0 l/hr/m2.
What is the premedication for paclitaxel?
Purpose: Dexamethasone and histamine antagonists have been employed commonly as premedications for prophylaxis of hypersensitivity reactions (HSRs) to paclitaxel. Frequent premedications for weekly administration of paclitaxel are associated with added side-effects and extra cost.
What is taxane induced peripheral neuropathy?
Peripheral neurotoxicity is the major non-hematological adverse effect of taxane, often manifested as painful neuropathy experienced during treatment, and it is sometimes irreversible. Unfortunately, taxane-induced neurotoxicity is an uncertainty prior to the initiation of treatment.
Why is paclitaxel used to study pain?
Intrathecal injection of paclitaxel induces mechanical allodynia in a dose-dependent manner. We also provide evidence that paclitaxel induces activation of TLR4 in the spinal dorsal horn and dorsal root ganglions.
What is Taxol induced peripheral neuropathy?
Peripheral sensory neuropathy is the most commonly reported neurotoxic effect of paclitaxel and it limits treatment with high and cumulative doses of paclitaxel when given alone or in combination with other neurotoxic antineoplastic agents such as cisplatin.
Is paclitaxel cell cycle specific?
The plant alkaloids are cell-cycle specific. This means they attack the cells during various phases of division. Vinca alkaloids: Vincristine, Vinblastine and Vinorelbine. Taxanes: Paclitaxel and Docetaxel.
What is a nursing consideration when administering paclitaxel?
Paclitaxel has been shown to be safe in both the inpatient and outpatient settings. Nursing care includes the administration of the drug, the assessment and management of side effects, and psychosocial support of patients receiving the drug.
What is the role of cremophor pharmacokinetics in paclitaxel administration?
Cremophor pharmacokinetics in patients receiving 3-, 6-, and 24-hour infusions of paclitaxel Paclitaxel infusions of 3 and 6 hours can result in sustained plasma Cremophor concentrations sufficient for substantial reversal of P-glycoprotein-mediated MDR in vitro.
Are the pharmacokinetics of paclitaxel monotherapy non-linear?
The pharmacokinetics of paclitaxel monotherapy have been widely studied at numerous dose levels of the Cremophor EL®formulation, but are less well-characterized for the newer nab-paclitaxel formulation. In conclusion, paclitaxel pharmacokinetics are non-linear for short infusion times but not for longer infusions.
What are the end-of-infusion plasma Cremophor concentrations for paclitaxel?
Three-hour intravenous infusions of paclitaxel can yield end-of-infusion plasma Cremophor concentrations of 1 microL/mL or more, which are sufficient to reverse MDR in vitro by at least 50%. Despite extensive clinical use, the pharmacokinetics of Cremophor have not been described.
What are the side effects of cremophor EL free paclitaxel?
The polymeric micellar composition of cremophor EL free paclitaxel can be used in higher therapeutic doses with a lower risk of hypersensitivity and peripheral neurotoxicity. Fatigue and neuropathy were the most common dose-dependent adverse events of this drug. Nonew adverse reactions unknown for paclitaxel have been registered.Conclusions.