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Nitrazepam

Nitrazepam molecule structureNitrazepam molecule structure
Mogadon, Alodorm, Apodorm, Arem, Remnos
Chemical Class
Benzodiazepine

Nitrazepam is a long-acting benzodiazepine hypnotic first synthesized in the late 1950s by Hoffmann-La Roche and introduced medically in 1965 under the brand name Mogadon. It possesses potent sedative, anxiolytic, amnestic, anticonvulsant, and muscle relaxant properties.citation needed Nitrazepam is primarily prescribed for short-term treatment of severe insomnia and disabling anxiety, reducing sleep onset time and increasing sleep duration. It is also used in managing myoclonic seizures.12

Dosage & Duration

Dosage

Doses are population estimates that vary widely between individuals.

Threshold~2 mg
Light2-5 mg
Moderate5-15 mg
Strong15-20 mg
Heavy20+ mg
Bioavailability
53-94%

Duration

Onset10-40 minutes
After Effects6-12 hours
Total5-8 hours
Half-life
15-48 hours

Subjective Effects

Legacy content. A statistically backed ontology from Mindstate Design Labs is coming soon.

The experience is dominated by hypnotic sedation, muscle relaxation, and a marked reduction in anxiety, with sleep onset shortened and sleep duration extended. Its long duration means effects persist well past the intended sleep period, producing a lingering "hungover" quality the following day that includes sleepiness, slowed psychomotor performance, and impaired decision-making. Memory impairment is a defining feature, and at higher doses balance, speech, and coordination degrade noticeably. Paradoxical reactions such as excitement, stimulation, hallucinations, and hyperactivity are reported infrequently.

Physical

Pronounced skeletal muscle relaxation and heavy somnolence dominate, accompanied by muscle weakness and reduced physical performance. Ataxia, unsteadiness, dizziness, and vertigo impair balance and walking, with slurred speech at higher doses.

Autonomic

Coordination

Sedation

Uncomfortable

Headache

Cognitive

The headspace is calm and anxiety-free but progressively dulled, with reduced alertness, numbed emotions, inattention, and unreliable recall. Confusion and disorientation are more likely with chronic use or in older users, and depressed mood is a reported effect.

Emotional

Impairment

Suppressions

Visual

Double vision

Tactile

Multisensory

Reagent Testing

Expected colorimetric results for common reagent tests. Colors show reaction change over 1–2 minutes.

Zimm(ZI)
white → yellow2 → brown1
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Pharmacology

Pharmacodynamics

Nitrazepam is a benzodiazepine that acts as a full agonist at central benzodiazepine receptors, which are associated with inhibitory GABA-A receptors.citation needed This binding enhances GABA activity at GABA-A receptors, producing sedative, hypnotic, anxiolytic, anticonvulsant, amnestic, and skeletal muscle relaxant effects. The anticonvulsant properties may be partly or entirely attributable to binding to voltage-gated sodium channels rather than benzodiazepine receptors, with benzodiazepines slowing recovery of sodium channels from inactivation. Nitrazepam also binds to peripheral-type benzodiazepine receptors. The muscle relaxant effects are produced via inhibition of polysynaptic pathways in the spinal cord.3 At high doses, nitrazepam decreases histamine turnover as a result of its action at the benzodiazepine-GABA receptor complex, and it has demonstrated cortisol-suppressing properties in humans.citation needed

Pharmacokinetics

Nitrazepam is lipophilic and largely bound to plasma proteins,4 with high cerebral uptake. Oral bioavailability ranges from 53 to 94 percent, and food intake does not influence absorption rate or bioavailability. Peak plasma concentrations are reached approximately 2 hours after oral administration, with a range of 0.5 to 5 hours. The drug is metabolized hepatically by oxidative pathways.citation needed As a nitrobenzodiazepine, nitrazepam is metabolically activated by CYP3A4, which can generate reactive metabolites including free radicals. The elimination half-life ranges from 15 to 48 hours, with a mean of approximately 26 hours. Half-life is age-dependent, averaging around 29 hours in young people and extending to approximately 40 hours in the elderly.5 Nitrazepam is eliminated extremely slowly from the cerebrospinal fluid, with a half-life of 68 hours in that compartment.6

Metabolitesnone documented yet

Interactions

Dangerous

Highest risk

These combinations are considered extremely harmful and should always be avoided. Reactions to these drugs taken in combination are highly unpredictable and have a potential to cause death.

AlcoholGHB/GBLOpioidsTramadol

Unsafe

Avoid

There is considerable risk of physical harm when taking these combinations, they should be avoided where possible.

DiphenhydraminePCP

Caution

Use caution

These combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.

DXMKetamineMXE
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Tolerance

Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.

Full Tolerance
Tolerance to nitrazepam's effects develops with regular use, typically appearing after approximately seven days of continuous administration.citation needed Tolerance to sleep-inducing and anticonvulsant effects develops readily, though some evidence suggests tolerance development is not uniform across all patients. In children treated for epilepsy, tolerance may develop within months of continued use, often necessitating dose escalation.
Cross Tolerance

Benzodiazepines, GABAergic depressants

Harm Potential

Addiction & Dependence

Psychological

High

Recreational use is common and the drug is classified as habit-forming. Dependence can develop in as little as four weeks of regular use, with prescriptions recommended to not exceed seven to ten consecutive days.citation needed

Physical

High

Physical dependence develops readily with continued use, producing a withdrawal syndrome similar to alcohol and barbiturate withdrawal.citation needed Common withdrawal symptoms include anxiety, insomnia, concentration problems, and fatigue. Neonatal withdrawal syndrome can occur in infants born to mothers using nitrazepam during pregnancy.

Toxicity

Hepatic

Severe liver toxicity has been reported; nitrobenzodiazepines including nitrazepam are more hepatotoxic than other benzodiazepines due to metabolic activation by CYP3A4.citation needed

Central Nervous System

Long-term use may lead to development of cognitive deficits; elderly patients are particularly susceptible and may develop a disability characterized by general mental deterioration, inability to walk, incontinence, dysarthria, confusion, and disorientation from doses as low as 5 mg.

Respiratory

Can cause severe respiratory distress in children, including swallowing incoordination, bronchospasm, delayed cricopharyngeal relaxation, and respiratory depression potentially requiring ventilatory support; may promote parasympathetic overactivity leading to potentially fatal respiratory distress.citation needed

Carcinogenicity
Possible

Benzodiazepine use is associated with an increased risk of developing cancer.7

Evidence Basis
Human EpidemiologicalLimited
Animal Models
None

Psychosis Risk

Very infrequently, paradoxical reactions may occur including excitement, stimulation, hallucinations, hyperactivity, and insomnia.citation needed

History & Culture

Nitrazepam was first synthesized in the late 1950s by a team of researchers at Hoffmann-La Roche in Switzerland. The compound was patented in 1961 and subsequently entered medical use in 1965, marketed under the brand name Mogadon among others.…

Legality

By Country

Prescription3
United States flagUnited StatesPrescription only
Canada flagCanadaPrescription medication
Germany flagGermanyPrescription only

References

Source Pages

  1. DrugBank
  2. PsychonautWiki: Benzodiazepines
  3. PsychonautWiki: Dangerous Combinations
  4. TripSit Wiki: Benzodiazepines
  5. TripSit Wiki: Drug Combinations
  6. Wikipedia

Citations

  1. MOGADON (Nitrazepam) Tablets BP 5 mg, 10 mg — Product Monograph. AA Pharma Inc. (2021). https://www.aapharma.ca/downloads/en/PIL/2021/Mogadon_PM_EN.pdf1
  2. Apotex Inc.. (2021). APO-NITRAZEPAM (Nitrazepam Tablets BP 5 mg and 10 mg) — Product Monograph. Health Canada / Apotex Inc.. https://pdf.hres.ca/dpd_pm/00065199.PDF1
  3. S K Date, K G Hemavathi, & O D Gulati. (November 1984). Investigation of the muscle relaxant activity of nitrazepam. Archives Internationales de Pharmacodynamie et de Thérapie, 272(1), 129–139. https://pubmed.ncbi.nlm.nih.gov/6517646/1
  4. APO-NITRAZEPAM Nitrazepam Tablets BP — Product Monograph. Apotex Inc. (2010). https://www.e-lactancia.org/media/papers/Nitrazepam-DS-Apotex2010.pdf1
  5. Kangas L, Kanto J, & Leppanen A. (1979). Human pharmacokinetics of nitrazepam: effect of age and diseases. https://pubmed.ncbi.nlm.nih.gov/456400/1
  6. Kangas L, Kanto J, Siirtola T, & Pakkanen A. (1977). Cerebrospinal-fluid concentrations of nitrazepam in man. https://pubmed.ncbi.nlm.nih.gov/578380/1
  7. Tao Zhang, Xiaowen Yang, Jianrui Zhou, Pei Liu, Hui Wang, Anrong Li, & Yi Zhou. (2017). Benzodiazepine drug use and cancer risk: a dose-response meta analysis of prospective cohort studies. https://doi.org/10.18632/oncotarget.220571
  8. Karin Rustler, Galyna Maleeva, Alexandre M. J. Gomila, Pau Gorostiza, Piotr Bregestovski, & Burkhard König. (October 2020). Optical Control of GABAA Receptors with a Fulgimide-Based Potentiator. Chemistry: A European Journal, 26(56), 12722–12727. https://doi.org/10.1002/chem.2020007101
  9. Controlled Drugs and Substances Act (SC 1996, c. 19) — Schedule IV, Item 18(24): Nitrazepam. (n.d.). https://laws-lois.justice.gc.ca/eng/acts/c-38.8/page-12.html1
  10. Health Canada Drug Product Database — MOGADON (DIN 00511536), AA Pharma Inc. (n.d.). https://produits-sante.canada.ca/dpd-bdpp/info?lang=eng&code=39921

Further Reading

  1. Drug-Do: Benzos
  2. Tripsitter: Nitrazepam Fact Sheet

Article Status

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Recent changes8 human edits · latest

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20 August 2026

  1. Lyrea · Changed a word in Dosage & Duration › Routes 1 › Dose ranges › Heavy

24 January 2026

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