Nama Dagang :

Alodorm; Apodorm; Arem; Dormigen; Dormo-Puren; Eatan N;

Imeson; Insoma; Ipersed; Mitidin; Mogadan; Mogadon; Nitrados;
Nitrazepam Capsules BP 1993; Nitrazepam Oral Suspension BP
1993; Nitrazepam Tablets BP 1993; Nitrazepan; Novanox;
Ormodon; Paxadorm; Pelson; Protraz; Radedorm; Remnos;
Serenade; Somnibel N; Somnipar; Somnite; Surem; Tri;
Unisomnia; imeson; Pelsonfilina (multi-ingredient
preparation)
Chemical Name:
1,3-Dihydro-7-nitro-5-phenyl-2H-1,4- -benzodiazepin-2-one.
Molecular Formula: C15H11N3O3
Molecular Weight: 281.3

REF : http://www.inchem.org/documents/pims/pharm/pim675.htm#PartTitle:1.
NAME
Dr Ligia Fruchtengarten
Poison Control Centre of Sao Paulo - Brazil
Hospital Municipal Dr Arthur Ribeiro de Saboya Coperpas 12
Perth, Western Australia.
Editor:

Dr M.Ruse, April 1998

----------------------------------------------7-nitro-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one
Nitrazepam is a type of benzodiazepine drug. It is a powerful hypnotic drug which possesses strong
sedative, anxiolytic, amnestic, anticonvulsant, and skeletal muscle relaxant
properties. Nitrazepam shortens the time required to fall asleep and lengthens the duration of sleep.
It is also useful for the management of myoclonic seizures.
Hypnotics and Sedatives
Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety. See a
list of PubChem compounds matching this category.
from MeSH
Anticonvulsants
Drugs used to prevent SEIZURES or reduce their severity. See a list of PubChem compounds
matching this category.

from MeSH
Anti-Anxiety Agents
Agents that alleviate ANXIETY, tension, and ANXIETY DISORDERS, promote sedation, and have a
calming effect without affecting clarity of consciousness or neurologic conditions. ADRENERGIC
BETA-ANTAGONISTS are commonly used in the symptomatic treatment of anxiety but are not
included here. See a list of PubChem compounds matching this category.
from MeSH
GABA Modulators
Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC
ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at
least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by
increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a
site at which BARBITURATES act to prolong the duration of channel opening; and a site at which
some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating
GABAergic responses, but they are not included here. See a list of PubChem compounds matching
this category.

Mekanisme
Nitrazepam belongs to a group of medicines called benzodiazepines. It acts
on benzodiazepine receptors in the brain which are associated with the GABA receptors causing an
enhanced binding of GABA (gamma amino butyric acid) to GABAA receptors. GABA is a major
inhibitory neurotransmitter in the brain, involved in inducing sleepiness, muscular relaxation and
control of anxiety and fits, and slows down the central nervous system. The anticonvulsant
properties of nitrazepam and other benzodiazepines may be in part or entirely due to binding to
voltage-dependent sodium channels rather than benzodiazepinereceptors. Sustained repetitive firing
seems to be limited by benzodiazepines effect of slowing recovery of sodium channels from
inactivation.
REF : http://pubchem.ncbi.nlm.nih.gov/compound/nitrazepam#section=Top

Summary
Nitrazepam is one of the oldest benzodiazepines and is widely used as an hypnotic
throughout the world, except North America, where it is not available. It is a safe
hypnotic, with low acute toxicity and minor side effects. Development of tolerance
or dependence and withdrawal symptoms are rare and very few known interactions
with other drugs exist.

The absorption of nitrazepam from the gastrointestinal tract is fairly rapid (tmax
ranging 0.5 to 7 hours). The bioavailability after oral intake averages about 80%.
Maximum plasma concentrations after a single 5mg dose are of the order of
40ng/ml. As a lipophilic drug, nitrazepam is distributed rapidly in the body. The
plasma levels can be fitted to a 2-compartment open model. The -phase is rather
rapid and the elimination phase is characterised by a long half-life of about 30
hours; accumulation with daily use therefore occurs. Marked interindividual
variation (up to 10-fold) is found in all pharmacokinetic parameters. Age and
immobilising diseases may influence the parameters, evidently increasing Vd and
t1/2
A similar amount of protein-free drug found in the plasma, i.e. 10 to 15% of the total
plasma level, is found in the cerebrospinal fluid. In saliva the concentrations are
significantly smaller. Nitrazepam penetrates the human placenta. In early
pregnancy, the ratio of cord to maternal plasma concentration is about 0.5, 12
hours after drug administration. In late pregnancy, the ratio reaches 1 within a few
hours. Breast milk concentrations are about one-half of those in maternal plasma.
Nitrazepam has no clinically active metabolites. It is excreted mainly as conjugated
and non-conjugated 7-aminonitrazepam and 7-acetamidonitrazepam. Polymorphic
acetylation is not likely to be of clinical importance. Enzyme induction or significant
loss of efficacy have not been found with long term use.
There is no significant correlation between plasma concentrations and clinical
effects (or side effects) of nitrazepam. Plasma level monitoring is therefore of no
benefit clinically (except for special cases, e.g. in epileptic patients). Increased
responsiveness in terms of therapeutic effects and side effects is evident in the
elderly. Therefore, small doses not exceeding 5mg daily should be prescribed for
geriatric patients.
REF : October 1981, Volume 6, Issue 5, pp 346-366
Date: 13 Dec 2012
Clinical Pharmacokinetics of Nitrazepam
Dr Lauri Kangas, Douwe D. Breimer
http://link.springer.com/article/10.2165%2F00003088-198106050-00002

Nitrazepam
1,3-dihydro-2H-1,4-benzodiazepin-2-one dimana substituted at positions 5 dan 7
ditempatin oleh golongan phenyl dan nitro. Obat ini ada hypnotic drug dari kelas
benzodiazepine, yang digunakan untuk relifef dari anxietas dan insomnia dalam
waktu singkat. Selain itu, juga memiliki efek sedasi dan motor-impairing properties
seperti amnestic, anti-konvulsi, merelaksasi otot rangka. Nitrazepam memiliki nama
dagang diantaranya Alodarm, Arem, Insomo, Insomnia, Mogadon, Nitrados,
Nitsosun, Ormodon, Paxadorm, Remnos dan Somnite.