Pilot study to investigate the pharmacokinetics and tolerability of midazolam nose spray

Pharmacokinetics and tolerability of a formulation of midazolam 50 mg/ml nose spray vs midazolam 1 mg/ml intravenously administered in healthy Dutch subjects: a single dose, randomised-sequence, open-label, two-period crossover pilot study

Status

Active, not recruiting

Phases

Unknown

Study type

Interventional

Source

ISRCTN

Registry ID

ISRCTN79059168

Enrollment

Registered

2011-05-18

Start date

2005-11-01

Completion date

Unknown

Last updated

2016-10-17

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Epileptic seizures Nervous System Diseases Epileptic seizures

Interventions

In this cross over study subjects are randomly assigned to receive IN or IV midazolam, with a washout period of at least five days between treatments. The 50 mg/ml IN midazolam formulation consists

Eligibility

Sex/Gender

All

Inclusion criteria

Inclusion criteria: 1. Age more than or equal to 18 years, either sex 2. American Society of Anesthesiology patient classification status (ASA) I and II

Exclusion criteria

Exclusion criteria: 1. Allergy to benzodiazepines 2. Acute or chronic nasal problems like rhinitis or sinusits 3. Use of benzodiazepines or grapefruit was prohibitied for a week prior to the research

Design outcomes

Primary

Measure	Time frame
Pharmacokinetics of midazolam nose spray (5 mg, 50 mg/mL formulation) compared with intravenous administration (2.5 mg) - Blood samples for pharmacokinetic analysis were collected from an intravenous (IV) cannula at baseline and at 3.5,15, 20, 30, 40, 60, 90,120,180 and 240 minutes post-dose. Pharmacokinetic data [maximum concentration (Cmax), time to maximum plasma concentration (Tmax), biological half life (t1/2), area under the Curve (AUC)] are analysed using two-compartment analysis.	—

Measure

Time frame

Pharmacokinetics of midazolam nose spray (5 mg, 50 mg/mL formulation) compared with intravenous administration (2.5 mg) - Blood samples for pharmacokinetic analysis were collected from an intravenous (IV) cannula at baseline and at 3.5,15, 20, 30, 40, 60, 90,120,180 and 240 minutes post-dose. Pharmacokinetic data [maximum concentration (Cmax), time to maximum plasma concentration (Tmax), biological half life (t1/2), area under the Curve (AUC)] are analysed using two-compartment analysis.

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Secondary

Measure	Time frame
Tolerability of midazolam nose spray (50 mg/mL formulation) - Subjects are instructed to inform the investigator of any untoward effects occuring during the study, including both local adverse events and systemic adverse events. Major expected side effects, like drowsiness and local burning feeling, were registered by a Visual Analogue Scale (VAS) form 0 = no complaint at all to 100 = worst complaint possible, others were described.	—

Measure

Time frame

Tolerability of midazolam nose spray (50 mg/mL formulation) - Subjects are instructed to inform the investigator of any untoward effects occuring during the study, including both local adverse events and systemic adverse events. Major expected side effects, like drowsiness and local burning feeling, were registered by a Visual Analogue Scale (VAS) form 0 = no complaint at all to 100 = worst complaint possible, others were described.

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Countries

Netherlands

Outcome results

None listed

Source: ISRCTN (via WHO ICTRP) · Data processed: Mar 27, 2026