Benzodiazepines

General Information

Classification: Downer/Sedative/Anxiolytic

History

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.

Source: Shorter E (2005). "Benzodiazepines". A Historical Dictionary of Psychiatry. Oxford University Press. pp. 41–2. ISBN 0-19-517668-5.

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
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
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 (Paxipam)	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

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

Oral

Onset:

Alprazolam IR : 8-25 minutes

Alprazolam XR : 25-75 minutes

Diazepam : Rapid

Clonazapam : 1 hour

Lorazepam : 1-2 hours

Peak Benefit:

Diazepam : 1.6 hours

Alprazolam IR : 90 minutes

Alprazolam XR : 25-75 minutes

Diazepam : 2-4 hours

Clonazapam : 1-4 hours

Half/Life and Duration

Triazolam : 2.5 Hours

Lorazepam : 10-20 hours - 6-12 hour duration

Alprazolam IR : 11 hour half life - 5 hour duration

Alprazolam XR :11-16 hour hour half life, 11 hour duration

Diazepam : 20-100 hour half life - 6-8 hour duration

Clonazepam : 18-50 hour half life - 12+ hours

Dosages Depend on tolerance.

Potentiators:

Grapefruit juice

Avoid:

Excessive drinking (you will die)

Do not smoke, inject, or snort benzos.

Positive

• Stress Relief
• Anxiety Relief
• Social Anxiety
• PTSD
• Sedative
• Worries drift away
• That "sink into the couch" feeling

Negative

• High addiction potential
• Killer withdrawals
• Risk of blackout
• Inability to drink
• Inability to dirve
• Loss of balance
• Memory Loss
• Procrastination

After effects

• "Hangover"?

• Afterglow

• 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

• Mental illness

• Heart issues

• CNS depressant when mixed with other drugs

Chemistry and Pharmacology

• 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

Sources

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. 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.