Top Gene Interactions
- Metabolism: It is long acting, is lipophilic and is metabolised hepatically via oxidative pathways. [Wikipedia] Half Life: 15-38 hours (mean elimination half life 26 hours).
- Uses/Sources: Used to treat short-term sleeping problems (insomnia), such as difficulty falling asleep, frequent awakenings during the night, and early-morning awakening.
- Health Effects: They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive. May cause a potentially dangerous rash that may develop into Stevens Johnson syndrome, an extremely rare but potentially fatal skin disease.
- Symptoms: Nitrazepam is a drug which is very frequently involved in drug intoxication, including overdose. Nitrazepam overdose may result in stereotypical symptoms of benzodiazepine overdose including intoxication, impaired balance, slurred speech. In cases of severe overdose this may progress to a comatose state with the possibility of death.
- Treatment: General supportive measures should be employed, along with intravenous fluids, and an adequate airway maintained. Hypotension may be combated by the use of norepinephrine or metaraminol. Dialysis is of limited value. Flumazenil (Anexate) is a competitive benzodiazepine receptor antagonist that can be used as an antidote for benzodiazepine overdose. In particular, flumazenil is very effective at reversing the CNS depression associated with benzodiazepines but is less effective at reversing respiratory depression. Its use, however, is controversial as it has numerous contraindications. It is contraindicated in patients who are on long-term benzodiazepines, those who have ingested a substance that lowers the seizure threshold, or in patients who have tachycardia or a history of seizures. As a general rule, medical observation and supportive care are the mainstay of treatment of benzodiazepine overdose. Although benzodiazepines are absorbed by activated charcoal, gastric decontamination with activated charcoal is not beneficial in pure benzodiazepine overdose as the risk of adverse effects often outweigh any potential benefit from the procedure. It is recommended only if benzodiazepines have been taken in combination with other drugs that may benefit from decontamination. Gastric lavage (stomach pumping) or whole bowel irrigation are also not recommended.
- Route of Exposure: Bioavailability is 53-94% following oral administration.
Mechanism of Action
|Target Name||Mechanism of Action||References|
Gamma-aminobutyric acid receptor subunit alpha-2
Gamma-aminobutyric acid receptor subunit alpha-3
Gamma-aminobutyric acid receptor subunit alpha-4
Gamma-aminobutyric acid receptor subunit alpha-5
Gamma-aminobutyric acid receptor subunit alpha-6
Gamma-aminobutyric acid receptor subunit beta-1
Gamma-aminobutyric acid receptor subunit beta-2
Gamma-aminobutyric acid receptor subunit beta-3
Gamma-aminobutyric acid receptor subunit delta
Gamma-aminobutyric acid receptor subunit gamma-2
Gamma-aminobutyric acid receptor subunit gamma-3
Gamma-aminobutyric acid receptor subunit pi
Gamma-aminobutyric acid receptor subunit rho-1
Gamma-aminobutyric acid receptor subunit rho-2
Gamma-aminobutyric acid receptor subunit gamma-1
Gamma-aminobutyric acid receptor subunit rho-3
Gamma-aminobutyric acid receptor subunit theta
Gamma-aminobutyric acid receptor subunit epsilon
Sodium channel protein type 1 subunit alpha
Histamine H1 receptor
GABA-A receptor (anion channel)
Lysine-specific demethylase 4C
|Gamma-aminobutyric acid receptor subunit alpha-1||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 benzodiazepine receptors. Sustained repetitive firing seems to be limited by benzodiazepines effect of slowing recovery of sodium channels from inactivation.||
Nitrazepam Interacts with Diseases
|Disease||Inference Score||References/Inference Genes|
|Disorders of Sex Development||14.12||
|Cell Transformation, Neoplastic||11.31||
|Polycystic ovary syndrome||9.58||
|Myocardial Reperfusion Injury||5.94||
|Liver Cirrhosis, Experimental||5.01||
|MIGRAINE WITH OR WITHOUT AURA, SUSCEPTIBILITY TO, 1||4.99||
|Prostatic Neoplasms, Castration-Resistant||4.83||