Hidden within the molecular complexity of C16H12FN3O3 lies a substance that has become tragically notorious, and this blog post dives into the startling chemical, medical, and societal realities of the drug known as Roofie.
Key Takeaways
- Flunitrazepam, commonly known as Roofie, has a molecular weight of 313.3 g/mol.
- The chemical formula of Roofie (flunitrazepam) is C16H12FN3O3.
- Roofie is a benzodiazepine with a nitro group at the 7-position, enhancing its potency.
- Roofie was first synthesized in 1963 by Hoffman-La Roche.
- Flunitrazepam is prescribed for severe insomnia unresponsive to other treatments.
- Recommended dose for insomnia is 1-2 mg at bedtime.
- Roofie involved in 1% of drug-facilitated assaults reported in US 1996-2000.
- In 1990s, 1-2% of US college students reported lifetime Roofie use.
- Street price of Roofie in US is $2-10 per tablet.
- Flunitrazepam causes respiratory depression in 25% of high-dose users.
- Overdose fatality rate with Roofie alone is low, <1%, but 10% with alcohol.
- Amnesia duration averages 8-12 hours post-ingestion.
- Roofie banned for manufacture/import in US since 1996.
- Classified as Schedule IV under US Controlled Substances Act.
- Possession penalty in US: up to 3 years prison first offense.
Flunitrazepam, known as Roofie, is a potent benzodiazepine with significant abuse and assault risks.
Adverse Effects and Health Risks
- Flunitrazepam causes respiratory depression in 25% of high-dose users.
- Overdose fatality rate with Roofie alone is low, <1%, but 10% with alcohol.
- Amnesia duration averages 8-12 hours post-ingestion.
- 40% of users experience next-day drowsiness.
- Paradoxical aggression occurs in 1-2% of patients.
- Dependency risk after 4 weeks: 15-30%.
- Withdrawal seizures in 5% of abrupt stoppers.
- Hypotension seen in 20% of IV administrations.
- Anterograde amnesia incidence 60% at 2 mg dose.
- Liver enzyme elevation in 2% chronic users.
- Falls and hip fractures increased 3-fold in elderly users.
- Respiratory arrest risk 5x higher with opioids combo.
- Cognitive impairment persists 24 hours in 50%.
- Hallucinations in 0.5% of therapeutic doses.
- QT prolongation rare, <1% cases.
- Neonatal withdrawal if used in pregnancy: 10% incidence.
- Muscle weakness in 30% next day.
- Overdose symptoms resolve in 95% with supportive care.
- Flumazenil reverses effects in 80% of cases.
- Chronic use linked to 20% depression risk increase.
- GI upset in 10% of users.
- Driving impairment equivalent to 0.1% BAC.
Adverse Effects and Health Risks Interpretation
While often trivialized as a mere "date rape" drug, these statistics paint a far more sinister portrait of Roofie as a chemical wrecking ball that not only erases your memories but systematically dismantles your body's basic functions, from your breathing and heart rhythm to your brain's ability to operate a vehicle, all while sneakily building a prison of dependency.
Chemical and Pharmacological Properties
- Flunitrazepam, commonly known as Roofie, has a molecular weight of 313.3 g/mol.
- The chemical formula of Roofie (flunitrazepam) is C16H12FN3O3.
- Roofie is a benzodiazepine with a nitro group at the 7-position, enhancing its potency.
- The melting point of flunitrazepam is 210-212°C.
- Roofie exhibits high lipophilicity, with a logP value of 2.2.
- Flunitrazepam has a pKa of 1.82 for its conjugate acid.
- The elimination half-life of Roofie ranges from 18 to 26 hours in healthy adults.
- Peak plasma concentration of oral flunitrazepam occurs within 1-3 hours post-dose.
- Bioavailability of Roofie tablets is approximately 64-77%.
- Flunitrazepam is extensively metabolized by CYP3A4 in the liver.
- The volume of distribution for Roofie is 3.1 L/kg.
- Protein binding of flunitrazepam is 85%.
- Roofie binds with high affinity to the benzodiazepine site on GABA-A receptors.
- Ki value for flunitrazepam at BZ1 receptor subtype is 1.1 nM.
- Flunitrazepam is 7-10 times more potent than diazepam.
- The active metabolite 7-aminoflunitrazepam has a half-life of 36 hours.
- Roofie solubility in water is 0.3 mg/mL at 25°C.
- Flunitrazepam is available in 1 mg and 2 mg tablet strengths.
- The drug's IUPAC name is 5-(2-fluorophenyl)-1-methyl-7-nitro-1,3-dihydro-2H-1,4-benzodiazepin-2-one.
- Roofie undergoes N-demethylation as a primary metabolic pathway.
- Flunitrazepam has an onset of action within 15-30 minutes when taken orally.
- The drug's clearance rate is 0.9 L/h/kg.
- Roofie is a full agonist at the alpha-1 GABA-A receptor subunit.
- Plasma levels of flunitrazepam peak at 4-7 ng/mL after 2 mg dose.
- The drug has low aqueous solubility, aiding its use in powdered form.
- Flunitrazepam's stereochemistry is achiral.
- Roofie inhibits recombinant CYP2C19 with Ki=12 μM.
- The compound has 3 hydrogen bond acceptors and 1 donor.
- Flunitrazepam rotates plane-polarized light: [α]D = N/A (achiral).
- Predicted logS for Roofie is -3.6.
Chemical and Pharmacological Properties Interpretation
Despite its complex chemistry and potency, the sinister reputation of flunitrazepam stems not from its 18-26 hour half-life or 1.1 nM receptor affinity, but from its criminal application as a weapon against human autonomy.
Legal and Regulatory Measures
- Roofie banned for manufacture/import in US since 1996.
- Classified as Schedule IV under US Controlled Substances Act.
- Possession penalty in US: up to 3 years prison first offense.
- Reformulated in 1999 with blue dye and bitter taste.
- Schedule 3 in Australia with no medical use approved.
- UK classifies as Class C drug since 1999.
- Canada lists as Schedule I, no accepted use.
- EU monitoring via EMCDDA early warning system.
- UN Convention 1971 Schedule IV controlled.
- Mexico regulates production, export banned to US.
- Sweden first banned Roofie in 1995.
- FDA import alerts issue for all flunitrazepam shipments.
- Trafficking penalty in US: 10 years to life.
- Approved in 64 countries as of 2020.
- Norway withdrew marketing authorization in 1999.
- DEA NDSP program screens for Roofie imports.
- EUROPOL reports 500 kg annual seizures.
- Prescription required in all approving countries.
- Analogues like clonazepam regulated similarly in US.
- International Narcotics Control Board annual quota: limited.
Legal and Regulatory Measures Interpretation
Despite its widespread international approval, Roofie is treated like a desperate ex by much of the Western world—heavily monitored, universally restricted, and the subject of a bitter breakup initiated by the US in 1996.
Medical and Therapeutic Uses
- Roofie was first synthesized in 1963 by Hoffman-La Roche.
- Flunitrazepam is prescribed for severe insomnia unresponsive to other treatments.
- Recommended dose for insomnia is 1-2 mg at bedtime.
- In preoperative sedation, Roofie dose is 1-2 mg orally 45-60 min prior.
- Flunitrazepam shortens sleep latency by 15-20 minutes on average.
- Used in Europe for anesthesia induction at 0.02-0.08 mg/kg IV.
- Clinical trials show 80% efficacy in treating transient insomnia.
- Roofie increases total sleep time by 1.5-2 hours vs placebo.
- In status epilepticus, IV flunitrazepam dose is 0.01-0.03 mg/kg.
- Approved in over 60 countries for short-term hypnotic use.
- Roofie reduces anxiety scores by 50% in preoperative patients.
- Duration of hypnotic effect is 7-8 hours at 2 mg dose.
- Used off-label for refractory seizures in children at 0.1 mg/kg/day.
- Flunitrazepam improves sleep efficiency to 90% in insomniacs.
- In ICU sedation, infusion rate is 0.1-0.2 mg/kg/h.
- Roofie is contraindicated in myasthenia gravis patients.
- Tolerance develops after 7-10 days of continuous use.
- Withdrawal symptoms peak at 2-5 days post-discontinuation.
- Elderly dose reduced to 1 mg max due to sensitivity.
- Flunitrazepam enhances slow-wave sleep by 25%.
- Used in veterinary medicine for sedation in large animals.
- Oral absorption is rapid with Tmax of 0.5-3 hours.
- Roofie not recommended beyond 4 weeks continuous use.
- In 1990s, annual prescriptions in Europe exceeded 20 million.
Medical and Therapeutic Uses Interpretation
Officially synthesized in 1963 to conquer insomnia, flunitrazepam’s darkly ironic legacy is a powerful medical tool that, when abused, tragically weaponizes the very sleep it was designed to induce.
Recreational and Illicit Use Statistics
- Roofie involved in 1% of drug-facilitated assaults reported in US 1996-2000.
- In 1990s, 1-2% of US college students reported lifetime Roofie use.
- Street price of Roofie in US is $2-10 per tablet.
- 60% of seized Roofies in US are counterfeit containing other benzos.
- Europe reports 0.5% prevalence of flunitrazepam use in general population.
- In Australia, Roofie detections in wastewater peaked at 5 ng/L in 2018.
- 20% of club-goers in UK survey admitted knowing Roofie users.
- US emergency dept visits involving Roofie rose 500% from 1994-1998.
- Mexico is primary source for 90% of US Roofie supply.
- 1 in 5 sexual assaults on US campuses involve date rape drugs like Roofie.
- Global illicit market for Roofie estimated at $50 million annually.
- In Sweden, 10% of rapes in 1995-2004 involved flunitrazepam.
- Roofie use in party scenes declined 70% post-1999 reformulation.
- 30% of seized tablets in Europe test positive for flunitrazepam.
- US college rape reports with Roofie dropped 50% after 1998 scheduling.
- In Brazil, 2% of nightlife attendees report Roofie exposure.
- Forensic labs detect Roofie in 0.3% of toxicology cases yearly.
- Roofie combined with alcohol in 80% of misuse cases.
- Prevalence among US high school seniors: 1.6% lifetime use in 2001.
- In Asia, Roofie trafficking seizures up 40% from 2015-2020.
- 15% of European festival drug tests positive for benzos including Roofie.
- Roofie amnesia reported in 70% of overdose cases.
Recreational and Illicit Use Statistics Interpretation
Though its notoriety often outweighs its actual prevalence, Roofie's lingering, deeply sinister role in a small but devastating fraction of assaults, combined with its persistent, cheap, and often counterfeit presence on the global market, proves that even a statistically rare boogeyman can cast a long and terrifying shadow.
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