Benzodiazepines

Alprazolam pills and prescription bottle

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

Comparison of benzodiazepines

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
Diclazepam	~120 hours	1mg	Anxiolytic
Estazolam (ProSom, Nuctalon)	10 - 24 hours	1 - 2 mg	Hypnotic
Etizolam	4-12 hours	1mg	Anxiolytic
Flubromazepam	106 hours	6 - 8 mg	Hypnotic
Flubromazolam	Long	.25mg	Hypnotic
Flunitrazepam (Rohypnol)	18 - 26 hours [36 - 200 hours]	1 mg	Hypnotic
Flutoprazepam (Restas)	60 - 90 hours	~2.5 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
Phenazepam	60 hours	~1 mg.	Hypnotic
Prazepam (Centrax)	[36 - 200 hours]	10 - 20 mg	Anxiolytic
Pyrazolam	Short	.83 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

Non-benzodiazepines commonly referred to as Z-drugs

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
• Withdrawls can be fatal
• 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

Images

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  (Purepac) alprazolam pills and prescription bottle

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  Alprazolam solved in propylene glycol

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  .5mg (Qualitest) alprazolam pills

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  Lorazepam (Ativan) pill

Links

http://www.dr-bob.org/tips/bzd.html

History of Etizolam on Tripsit.me

Sources

Madsen U, Bräuner-Osborne H, Greenwood JR, Johansen TN, Krogsgaard-Larsen P, Liljefors T, Nielsen M, Frølund B (2005). "GABA and Glutamate receptor ligands and their therapeutic potential in CNS disorders". In Gad SC. Drug Discovery Handbook. Hoboken, N.J: Wiley-Interscience/J. Wiley. pp. 797–907. ISBN 0-471-21384-5. ^ a b Panico, R.; Powell, W. H.; Richer, J. C., eds. (1993). A Guide to IUPAC Nomenclature of Organic Compounds. IUPAC/Blackwell Science. pp. 40–3. ISBN 0-632-03488-2.; Moss GP (1998). "Nomenclature of fused and bridged fused ring systems (IUPAC Recommendations 1998)". Pure Appl Chem 70 (1): 143–216. doi:10.1351/pac199870010143. Olsen RW, Betz H (2006). "GABA and glycine". In Siegel GJ, Albers RW, Brady S, Price DD (eds.). Basic Neurochemistry: Molecular, Cellular and Medical Aspects (7th ed.). Elsevier. pp. 291–302. ISBN 0-12-088397-X. Shorter E (2005). "Benzodiazepines". A Historical Dictionary of Psychiatry. Oxford University Press. pp. 41–2. ISBN 0-19-517668-5. Zavala F (1997). "Benzodiazepines, anxiety and immunity". Pharmacol Ther 75 (3): 199–216. doi:10.1016/S0163-7258(97)00055-7. PMID 9504140. Narimatsu E, Niiya T, Kawamata M, Namiki A (2006). "[The mechanisms of depression by benzodiazepines, barbiturates and propofol of excitatory synaptic transmissions mediated by adenosine neuromodulation]". Masui (in Japanese) 55 (6): 684–91. PMID 16780077. Juergens, MD, Steven M. "Understanding Benzodiazepines". California Society of Addiction Medicine. Retrieved 25 April 2012. Carlo, Pia; Renata Finollo, Anna Ledda, Giovanni Brambilla (January 1989). "Absence of liver DNA fragmentation in rats treated with high oral doses of 32 benzodiazepine drugs". Fundamental and Applied Toxicology 12 (1): 34–41. doi:10.1016/0272-0590(89)90059-6. PMID 2925017.