Products
In many countries, midazolam nasal spray is not yet available and registered as a finished drug product and therefore must be prepared as an extemporaneous formulation in a pharmacy or, at most, imported from abroad. It was approved in the United States in 2019 (Nayzilam). See also under diazepam nasal spray.
Structure and properties
Midazolam (C
18
H
13
ClFN
3
, M
r
= 325.8 g/mol) belongs to the imidazobenzodiazepines. It exists as a white to slightly yellow crystalline powder and is insoluble in water as a base. It is usually present in the injection solution and nasal spray in the form of the water-soluble midazolam hydrochloride.
Preparation
One simple way is to draw up the dormicum injection solution with a syringe and needle. The needle is removed and replaced with a mucosal atomization device (MAD). This is an atomizer attachment for syringes. The finished syringes are sealed and packaged. Alternatively, the injection solution is transferred to a nasal spray. Alternative formulations with advantageous properties are described in the literature. For example, a concentrated solution with excipients is also used.
Effects
Midazolam (ATC N05CD08) is antianxiety, sedative, sleep-inducing, anticonvulsant, and causes anterograde amnesia. The onset of action is rapid and lasts only a short time. The effects are due to binding to GABA.
A
-receptors in the brain. It thereby enhances the action of the inhibitory neurotransmitter GABA in the central nervous system. Administered as a nasal spray, midazolm is well absorbed into the blood through the mucosa and has high bioavailability because it is not subject to first-pass metabolism via CYP3A4.
Indications for use
Midazolam nasal sprays are used before diagnostic and surgical procedures, for sedation, and against seizures. The advantage is that no injection is necessary, which is desirable, for example, in children, in patients with disabilities, and in emergency situations. Administration is off-label at the responsibility of the physician/doctor because this route of administration has not yet been approved by the authorities.