Naloxone nasal spray - bioavailability and absorption pattern in a phase 1 study. / Naloksonnesespray biotilgjengelighet og opptaksmønster i en fase 1-studie.
Tidsskr Nor Laegeforen
; 139(13)2019 Sep 24.
Article
em Nor, En
| MEDLINE
| ID: mdl-31556537
ABSTRACT
BACKGROUND:
Bystander administration with naloxone nasal spray can prevent deaths from opioid overdose. To achieve optimal nasal absorption of naloxone, the spray must be administered at low volume with high concentration of the drug. The study aimed to investigate the bioavailability and absorption pattern for a new naloxone nasal spray. MATERIAL ANDMETHOD:
In an open, randomised, two-way crossover study undertaken in five healthy men, naloxone 2 mg (20 mg/ml) in nasal spray was compared with 1 mg intravenously administered naloxone. A total of 15 blood samples were taken over a period of six hours after administration. The drug concentration was determined using liquid chromatography tandem-mass spectrometry. Pharmacokinetic variables were calculated using non-compartmental analysis.RESULTS:
Bioavailability for intranasal naloxone was 47 % (minimum-maximum values 24-66 %). Maximum concentration (Cmax) was 4.2 (1.5-7.1) ng/ml, and this was achieved (Tmax ) after 16 (5-25) minutes.INTERPRETATION:
The nasal spray resulted in a rapid systemic absorption with higher serum concentrations than intravenous naloxone 10-240 minutes after intake. The pilot study indicated that the highly concentrated nasal spray may provide a therapeutic dose of naloxone with a single spray actuation. The findings led to further commercial development of the medication.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Sprays Nasais
/
Antídotos
/
Naloxona
Tipo de estudo:
Clinical_trials
Limite:
Adult
/
Humans
/
Male
Idioma:
En
/
Nor
Revista:
Tidsskr Nor Laegeforen
Ano de publicação:
2019
Tipo de documento:
Article