Pharmacokinetics and Bioavailability of Single-Dose Intranasal Hydromorphone Hydrochloride in Healthy Volunteers

@article{Coda2003PharmacokineticsAB,
  title={Pharmacokinetics and Bioavailability of Single-Dose Intranasal Hydromorphone Hydrochloride in Healthy Volunteers},
  author={Barbara Coda and Anita C. Rudy and Sanford M. Archer and Daniel P. Wermeling},
  journal={Anesthesia \& Analgesia},
  year={2003},
  volume={97},
  pages={117-123}
}
We evaluated pharmacokinetics and absolute bioavailability of single doses of hydromorphone hydrochloride after administration of 1.0 and 2.0 mg of intranasal (IN) and 2.0 mg of IV hydromorphone hydrochloride. An open-label, randomized, three-way crossover study was conducted in 24 healthy volunteers (13 men and 11 women). IN doses were delivered as 0.1-mL metered-dose sprays into one or both nostrils for 1.0- and 2.0-mg doses, respectively. Blood samples were taken serially from 0 to 16 h… 

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References

SHOWING 1-10 OF 40 REFERENCES
Pharmacokinetics of intranasal alfentanil.
Pharmacokinetics and Bioavailability of Hydromorphone: Effect of Various Routes of Administration
TLDR
The pharmacokinetics and bioavailability of hydromorphone following various routes of administration, i.e., intravenous, oral, intranasal, and transdermal, were investigated in rabbits and showed a low bioavailability after oral administration.
Pharmacokinetics of hydromorphone after intravenous, peroral and rectal administration to human subjects
TLDR
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.
The absolute bioavailability of transnasal butorphanol in patients experiencing rhinitis
TLDR
Dosage regimen of transnasal butorphanol does not need modification in patients experiencing rhinitis even when they are pretreated with oxymetazoline, and the absolute bioavailability was similar to that found with the pretreatment of oxymetzoline and those reported in healthy volunteers.
Comparison of intravenous and intranasal sufentanil absorption and sedation
TLDR
The results of this study show that sufentanil, when administered intranasally, is rapidly and effectively absorbed from the human nasal mucosa, so that this route may be an attractive alternative for a premedicant, avoiding the discomfort of an intravenous or intramuscular injection.
Pharmacokinetics and Bioavailability of Hydromorphone Following Intravenous and Oral Administration to Human Subjects
TLDR
An equation to predict the plasma concentration of hydromorphone on oral administration was developed from the data of these six subjects, finding that the drug was rapidly but incompletely absorbed after oral administration.
Dose Effectiveness and Safety of Butorphanol in Acute Migraine Headache
TLDR
It is concluded that in these doses butorphanol provides effective and safe analgesia for patients with acute, severe migraine headache.
Comparing the subjective, psychomotor, and physiological effects of intravenous hydromorphone and morphine in healthy volunteers
TLDR
The results of this study demonstrate that 0.33–1.3 mg hydromorphone had orderly, dose-related effects on subjective, psychomotor, and physiological variables, and similar effects to those of a benchmark mu opioid agonist, morphine.
...
1
2
3
4
...