Benzodiazepines
General Information
Benzodiazepines are drugs which act upon the GABA(A) receptor, and produce a general set of effects which vary by compound, mostly being sedative, hypnotic, anxiolytic, anticonvulsant and muscle relaxant. The first benzodiazepine, Chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955, and made available in 1960 by Hoffmann–La Roche, which has also marketed diazepam (Valium) since 1963.
Dosage
| Chemical name (brand name) | Half-Life [Active Metabolites] | Dose Equiv. of 10mg Diazepam (Oral) | Class |
|---|---|---|---|
| Alprazolam (Xanax) | 6 - 12 hours | 0.5 mg | Anxiolytic |
| Bromazepam (Lexotan, Lexomil) | 10 - 20 hours | 5 - 6 mg | Anxiolytic |
| Brotizolam | 2 - 6 hours | .25mg | Hypnotic |
| Chlordazepoxide (Librium) | 5 - 30 hours [36 - 200 hours] | 25 mg | Anxiolytic |
| Clobazam (Frisium) | 12 - 60 hours | 20 mg | Anxiolytic |
| Clonazepam (Klonopin) | 18 - 50 hours | 0.5 mg | Anxiolytic |
| Clorazepate (Tranxene) | [36 - 200 hours] | 15 mg | Anxiolytic |
| Diazepam (Valium) | 20 - 100 hours [36 - 200 hours] | 10 mg | Anxiolytic |
| Estazolam (ProSom, Nuctalon) | 10 - 24 hours | 1 - 2 mg | Hypnotic |
| Etizolam | 4-12 hours | 1mg | Anxiolytic |
| Flunitrazepam (Rohypnol) | 18 - 26 hours [36 - 200 hours] | 1 mg | Hypnotic |
| Flurazepam (Dalmane) | [40 - 250 hours] | 15 - 30 mg | Hypnotic |
| Halazepam (Paxipam) | [30 - 100 hours] | 20 mg | Anxiolytic |
| Ketazolam (Anseren) | 30 - 100 hours [36 - 200 hours] | 15 - 30 mg | Anxiolytic |
| Loprazolam (Dormonoct) | 6 - 12 hours | 1 - 2 mg | Hypnotic |
| Lorazepam (Ativan) | 10 - 20 hours | 1 mg | Anxiolytic |
| Lormetazepam (Noctamid) | 10 - 12 hours | 1 - 2 mg | Hypnotic |
| Medazepam (Nobrium) | 36 - 200 hours | 10 mg | Anxiolytic |
| Nitrazepam (Mogadon) | 15 - 38 hours | 10 mg | Hypnotic |
| Nordazepam (Nordaz) | 36 - 200 hours | 10 mg | Anxiolytic |
| Oxazepam (Serax) | 4 - 15 hours | 20 mg | Anxiolytic |
| Prazepam (Centrax) | [36 - 200 hours] | 10 - 20 mg | Anxiolytic |
| Quazepam (Doral) | 25 - 100 hours | 20 mg | Hypnotic |
| Temazepam (Restoril) | 8 - 22 hours | 20 mg | Hypnotic |
| Triazolam (Halcion) | 2 hours | 0.5 mg | Hypnotic |
| Chemical name (brand name) | Half-Life [Active Metabolites] | Dose Equiv. of 10mg Diazepam (Oral) | Class |
|---|---|---|---|
| Zaleplon (Sonata) | 2 hours | 20 mg | Hypnotic |
| Zolpidem (Ambien) | 2 hours | 20 mg | Hypnotic |
| Zopiclone (Imovane) | 5 - 6 hours | 15 mg | Hypnotic |
| Eszopiclone (Lunesta) | 6 hours | 3 mg | Hypnotic |
Effects
Positive
- Anti-Anxiety
- Sedative
- Muscle relaxant
Negative
- High addiction potential
- Killer withdrawals
- Risk of blackout
- Inability to drink
- Inability to dirve
- Loss of balance
- Memory Loss
- Procrastination
- "Hangover"
- Long term effects
- High addiction potential
Harm Reduction
- Avoid driving and operating machinery
- Recommended time (pauses) between using the substance
- Addiction potential - High
- Risk of blackouts
- Risk of death when mixed with alcohol or other drugs. An extremely high percentage of drug-related deaths are due to mixing benzos with other drugs, especially opiates and alcohol.
- Mental illness
- Heart issues
- CNS depressant when mixed with other drugs
Chemistry and Pharmacology
The term benzodiazepine is the chemical name for the heterocyclic ring system, which is a fusion between the benzene and diazepine ring systems. Under Hantzsch–Widman nomenclature, a diazepine is a heterocycle with two nitrogen atoms, five carbon atom and the maximum possible number of cumulative double bonds. The "benzo" prefix indicates the benzene ring fused onto the diazepine ring. Benzodiazepine drugs are substituted 1,4-benzodiazepines, although the chemical term can refer to many other compounds that do not have useful pharmacological properties. Different benzodiazepine drugs have different side groups attached to this central structure. The different side groups affect the binding of the molecule to the GABAA receptor and so modulate the pharmacological properties. Many of the pharmacologically active "classical" benzodiazepine drugs contain the 5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one substructure. Nonbenzodiazepines also bind to the benzodiazepine binding site on the GABA(A) receptor and possess similar pharmacological properties. While the nonbenzodiazepines are by definition structurally unrelated to the benzodiazepines, both classes of drugs possess a common pharmacophore , which explains their binding to a common receptor site
- 2-keto compounds:
- Chlordiazepoxide, Clorazepate, Diazepam, Flurazepam, Halazepam, Prazepam, and others.
- 3-hydroxy compounds:
- Lorazepam, Lormetazepam,Oxazepam, Temazepam
- 7-nitro compounds:
- Clonazepam, Flunitrazepam, Nimetazepam, Nitrazepam
- Triazolo compounds:
- Adinazolam, Alprazolam, Estazolam, Triazolam
- Imidazo compounds
- Climazolam, Loprazolam, Midazolam
Links
http://www.dr-bob.org/tips/bzd.html
Sources
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