Medazepam Stats & Data
Clc1ccc2N(C)CCN=C(c3ccccc3)c2c1YLCXGBZIZBEVPZ-UHFFFAOYSA-NReceptor Profile
Receptor Actions
Effect Profile
CuratedStrong anxiolysis, cognitive impairment, and euphoria with mild sedation
Tolerance & Pharmacokinetics
drugs.wikiTolerance Decay
Hypnotic/sedative tolerance tends to develop within days–weeks; anxiolytic/anticonvulsant tolerance is slower and incomplete. Tolerance decays gradually over 2–6 weeks after cessation, but protracted symptoms may persist in a subset. Data largely extrapolated from benzodiazepine class literature and clinical experience (Ashton manual, StatPearls).
Cross-Tolerances
Harm Reduction
drugs.wikiMedazepam is long-acting largely because its clinical effects are dominated by active metabolites with very long half-lives, notably nordazepam; with repeated dosing, accumulation increases next-day sedation, psychomotor impairment, and fall risk, especially in older adults and those with hepatic impairment. Abrupt cessation after sustained use can precipitate severe withdrawal (anxiety, insomnia, tremor) and, at high dependence levels, seizures; gradual, individualized tapering is strongly advised under medical supervision. Concomitant use with opioids or alcohol markedly increases the risk of respiratory depression and fatal overdose; if opioids are involved in a setting, having naloxone available can reverse opioid toxicity but will not reverse benzodiazepine effects. Genetic and drug–drug variability in CYP2C19 and CYP3A4 metabolism (the same pathways relevant for diazepam) can prolong effects or increase sedation in poor metabolizers or when strong inhibitors are co‑administered. Avoid driving or operating machinery the day after moderate–high doses or repeated dosing due to prolonged psychomotor and memory impairment. During pregnancy and breastfeeding, benzodiazepine exposure (including via diazepam/nordazepam from medazepam) can cause neonatal sedation and feeding difficulties; alternative strategies or close monitoring are recommended if use occurs. In unregulated markets, counterfeit benzodiazepine tablets and opioid supplies contaminated with benzodiazepines (‘benzo‑dope’) are common; use trusted sources or drug checking where available, start with test doses, and never mix with other depressants.
References
Data Sources
Cited References
- Ashton, H. (2007). Benzodiazepine Equivalency Table
- DrugBank: Medazepam
- Drugs-Forum: GABAergics FAQ
- INCHEM: Medazepam (PIM 460)
- Jochemsen, R., Breimer, D. D. (1984). Pharmacokinetics of benzodiazepines
- NCATS Inxight Drugs: Medazepam
- PsychonautWiki: Benzodiazepines
- PsychonautWiki: List of Prodrugs
- TripSit: Drug Combinations
- TripSit: Risks of Combining Depressants
- Tripsitter: Medazepam (Nobrium) Fact Sheet
- Zakusov, V. V., et al. (1977). GABA-ergic mechanisms in benzodiazepines
- TripSit: Medazepam
Drugs.wiki References
- DrugBank: Medazepam (DB13437)
- TripSit Wiki: Benzodiazepines overview (includes medazepam half-life and equivalence)
- Ashton Manual, Chapter 1: Table of benzodiazepines (medazepam ≈ diazepam; very long metabolite half-life)
- StatPearls: Benzodiazepines (class risks; metabolism via CYP3A4/CYP2C19; increased half-life in elderly)
- StatPearls: Diazepam (active metabolites; accumulation; half-lives)
- DrugBank: Diazepam (CYP2C19 polymorphism markedly extends diazepam and desmethyldiazepam half-lives)
- LactMed: Diazepam (breastfeeding caution; metabolite transfer)
- EUDA/EMCDDA: Perspectives on benzodiazepine misuse; scheduling list includes medazepam
- TripSit: Drug combinations (benzos + tramadol dangerous; general depressant combination cautions)
- Toronto Drug Checking Service: Benzo‑dope overview and recent trends
- Saferparty.ch warnings (mixing depressants; counterfeit tablet risk; advice to drug check)