Pharmacokinetics and Bioavailability of Hydromorphone Following Intravenous and Oral Administration to Human Subjects

  title={Pharmacokinetics and Bioavailability of Hydromorphone Following Intravenous and Oral Administration to Human Subjects},
  author={J. J. Vallner and James T. Stewart and Jeffrey A. Kotzan and Edward B. Kirsten and I. L. Honigberg},
  journal={The Journal of Clinical Pharmacology},
Abstract: In a relatively small pilot study, the half‐life of elimination of hydromorphone in six subjects was 2.64 ± 0.88 hours and the drug had a high volume of distribution, 1.22 1./kg. In addition, the drug was rapidly but incompletely absorbed after oral administration. An equation to predict the plasma concentration of hydromorphone on oral administration was developed from the data of these six subjects. 
Pharmacokinetics of hydromorphone after intravenous, peroral and rectal administration to human subjects
The pharmacokinetic properties of hydromorphone in healthy young male subjects were studied after i.v., peroral, and rectal administration and the absolute bioavailability after peroral administration was 50.7 ± 29.8 per cent.
Absolute Bioavailability of Hydromorphone After Peroral and Rectal Administration in Humans: Saliva/Plasma Ratio and Clinical Effects
The saliva sampling for the hydromorphone concentration was found to be a useful noninvasive technique for the estimation of the elimination half‐life of hydromOrphone.
Input Characteristics and Bioavailability after Administration of Immediate and a New Extended-release Formulation of Hydromorphone in Healthy Volunteers
The extended release of hydromorphone will produce less fluctuation of plasma concentrations compared with IR formulations, which should provide for more constant pain control, and the increased bioavailability from the OROS® formulation may be related to decreased metabolism by a first-pass effect or enterohepatic recycling of hydomorphone.
Multiple‐Dose Evaluation of Intravenous Hydromorphone Pharmacokinetics in Normal Human Subjects
The results indicate that hydromorphone pharmacokinetic parameters are linear across a fourfold range of doses that are usually employed clinically and that previously reported pharmacokinetics values for hydromoassay deserve reconsideration.
Pharmacokinetics and Bioavailability of Single-Dose Intranasal Hydromorphone Hydrochloride in Healthy Volunteers
IN hydromorphone hydrochloride met the minimum requirements for safety and demonstrated rapid nasal drug absorption and clinically relevant bioavailability in a single dose and support further development of this novel hydromorephone hydro chloride nasal spray.
Rifampin Reduces the Plasma Concentrations of Oral and Intravenous Hydromorphone in Healthy Volunteers
The enhancement of hydromorphone elimination should be considered when managing pain of patients who are treated with strong enzyme inducers, likely involving induction of uridine 5′-diphospho- glucuronosyltransferase enzymes by rifampin.
The concentration of digoxin after intravenous and oral administration studied by a two-compartment model
This paper is designed to compare the distribution of digoxin administered through an Intravenous (i.v.) and Oral (p.o.) system in central and peripheral compartments.
Pharmacokinetic investigation of dose proportionality with a 24-hour controlled-release formulation of hydromorphone
The pharmacokinetics of OROS® hydromorphone are linear and dose proportional for the 8, 16, 32, and 64 mg doses.
Single‐dose evaluation of safety, tolerability and pharmacokinetics of newly formulated hydromorphone immediate‐release and hydrophilic matrix extended‐release tablets in healthy Japanese subjects without co‐administration of an opioid antagonist
A single oral administration of the hydromorphone tablets would be well‐tolerated in healthy Japanese subjects despite a lack of co‐administration of an opioid antagonist and the newly developed ER hydrom orphone tablets may have the appropriate PK characteristics for once‐daily dosing.
A Multiple-Dose Phase I Study of Intranasal Hydromorphone Hydrochloride in Healthy Volunteers
Intranasal hydromorphone hydrochloride nasal spray was well tolerated and demonstrated rapid nasal drug absorption and predictable accumulation in an open-label, single- and multiple-dose study.


Kinetics of intravenous and intramuscular morphine.
Both studies demonstrate that morphine distribution is rapid and extensive and its t1/2beta relatively short and its IM morphine is rapidly and completely absorbed.
Urinary excretion of hydromorphone and metabolites in humans, rats, dogs, guinea pigs, and rabbits.
Hydromorphone was administered as a single dose to humans, rats, dogs, guinea pigs, and rabbits, and timed urinary collections revealed the presence of the parent compound and both 6-hydroxy epimers as metabolites in the urine of all species.
Radioimmunoassay of hydromorphone and hydrocodone in human plasma.
A radioimmunoassay for hydromorphone in human plasma was developed using a commercially available morphine-6-antiserum and tritiated dihydromorphine and demonstrates the usefulness of the assay in monitoring drug levels in a bioavailability study.
The mode of action of promethazine in potentiating narcotic drugs.
Promethazine premedication should be reserved for situations where the use of intravenous anaesthetics is anticipated and may prove to be a useful drug in certain other situations where too rapid inactivation of the principal drug presents a therapeutic problem.
Respiratory effects of hydromorphone in man
The respiratory depressant efJeets of hydromorphone, a potent analgesie, were compared with morphine in a randomized double‐blind erossover study in human volunteers and relative potency was found to be 7.99 with lower and upper 95 per cent confidence limits.
Radioimmunoassay of Hydromorphone in Plasma
A radloimmunoassay for hydromorphone In plasma has been developed from a commercially available RIA kit. The method is capable of detecting drugs in the 10 - 40 ng/ml range using 0.1 ml of sample.
Anaesthesia time/dose curves ix: The use of hydromorphone in surgical anaesthesia and postoperative pain relief in comparison to morphine
It is taken to indicate that psychological factors play only a subordinate role in modulating the intensity of postoperative pain in patients anaesthetized for major surgical operations with intravenous hydromorphone, nitrous oxide and muscle relaxants as required.
Radioimmunoassay procedure for hydromorphone and hydrocodone in human plasma
  • JPharm Sci
  • 1980
Radioimmunoassay of hydromorphone
  • JAnal Toxicol
  • 1977
Anesthesia time/dose