Breakthrough Addiction Recovery: Nitrazepam

Nitrazepam


Nitrazepam
Systematic ( IUPAC) name
9-nitro-6-phenyl-2,5-diazabicyclo[5.4.0]undeca- 5,8,10,12-tetraen-3-one
Identifiers
CAS number	146-22-5
ATC code	N05 CD02
PubChem	4506
DrugBank	none
Chemical data
Formula	C₁₅ H₁₁ N₃ O₃
Mol. mass	281.3 g/mol
Pharmacokinetic data
Bioavailability	53-94%
Metabolism	Hepatic
Half life	16-48 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C ( AU )
Legal status	Schedule IV (International)
Routes	Oral

Alodorm bottle containing 25 tablets of 5mg Nitrazepam

Nitrazepam (usually marketed under the trade names Mogadon® or Alodorm®) is a class of benzodiazepine. It is a powerful hypnotic drug which possesses strong sedative, anxiolytic, amnestic, anticonvulsant, and skeletal muscle relaxant properties.

Nitrazepam is most often used to treat short-term sleeping problems ( insomnia), such as difficulty falling asleep, frequent awakenings during the night, and early-morning awakening. Nitrazepam shortens the time required to fall asleep and lengthens the duration of sleep. It is also useful for the management of myoclonic seizures.

Nitrazepam is available in 5mg and 10mg tablets. In Australia and the United Kingdom it is only available in 5mg tablets.

Pharmacology

Nitrazepam belongs to a group of medicines called benzodiazepines. It acts on receptors in the brain (GABA receptors) causing the release of a chemical called GABA (gamma amino butyric acid), which is a major inhibitory neurotransmitter in the brain, involved in inducing sleepiness and control of anxiety and fits, and slows down the central nervous system. The time to reach peak plasma concentrations following oral administration is about 2 hours (0.5 to 5 hours).

In sleep laboratory studies, nitrazepam decreased sleep latency, increased total sleep time and decreased awake time. There is delay in the onset, and decrease in the duration of REM sleep. Nitrazepam is reported to significantly affect stages of sleep: a decrease stage 1, 3 and 4 sleep and to increase stage 2. Following discontinuation of the drug, REM sleep rebound has been reported in some studies.

Dosage

When used for treatment of insomnia, the usual dose for adults is 2.5mg to 10mg, taken at bedtime. Dosage for inpatients may be increased up to 20mg. Typically, it works within the hour and allows the individual to maintain sleep for 4 to 8 hours. It is recommended to allow a full 8 hours of sleep time to minimise the "hangover" side effect.

When used for treatment of myoclonic seizures, the dose is based on body weight. The dose for children (30kg or less) is anywhere from 0.3mg/kg to 1mg/kg, daily in three divided doses.

Nitrazepam is chemically similar to Nimetazepam, with 10mg approximately equating to a 5mg dosage respectively. [1]

Abuse potential

Studies suggest that nitrazepam caused significant euphoria as against placebos and was identified as an active drug by the subjects. Nitrazepam resembled diazepam (Valium®), however, on certain parameters the effects produced by nitrazepam were more pronounced. Nitrazepam was found to be an abusable drug and has similar abuse liability like diazepam, if not slightly higher. Treatment with nitrazepam should usually not exceed 7 to 10 consecutive days. Use for more than 2 to 3 consecutive weeks requires complete re-evaluation of the patient. Prescriptions for nitrazepam should be written for short-term use (7 to 10 days) and it should not be prescribed in quantities exceeding a 1-month supply. Dependence can occur in as little as four weeks. [2] [3]

Common Side Effects

CNS depression including drowsiness, dizziness, fatigue, ataxia, headache, confusion, vertigo, impairment of memory, hangover feeling in the morning, slurred speech, decreased physical performance, numbed emotions, reduced alertness, muscle weakness, double vision and inattention have been reported. Unpleasant dreams and rebound insomnia have also been reported.

Less Common Side Effects

Rarely, hypotension, faintness, palpitation, rash or pruritus, gastrointestinal disturbances, changes in libido. Very infrequently, paradoxical reactions may occur, e.g. excitement, stimulation, hallucinations, hyperactivity and insomnia. Also depressed or increased dreaming, disorientation, severe sedation, retrograde amnesia, headache, hypothermia, delirium tremens.

Interactions

See Diazepam#Interactions.

Contraindications

See Diazepam#Contraindications.

Overdose

See Diazepam#Overdose.

Trade names

Mogadon, Alodorm, Remnos, Somnite, Apodorm, Arem, Cavodan, Dima, Dormalon, Dormigen, Dormo-Puren, Dumolid, Eatan N, Eunoctin, Hypnotex, Imeson, Insoma, Insomin, Ipersed, Mitidin, Mogadan, Nilandron, Nitavan, Nitepam, Nitrados, Nitrapan, Nitravet, Nitrazadon, Nitrazep, Nitrazepan, Nitrazepol, Nitredon, Nitrosun, Novanox, Numbon, Onirema, Ormodon, Pacisyn, Paxadorm, Pelson, Pelsonfilina, Protraz, Radedorm, Remnos, Serenade, Somnibel N, Somnipar, Somnite, Sonebon, Sonotrat, Surem, Tri, Unisomnia, Nitrazepam Capsules BP 1993, Nitrazepam Oral Suspension BP 1993, Nitrazepam Tablets BP 1993. [4]