Diazepam

Diazepam (Also known as Diastat; Valium; Zetran) is a benzodiazepine that is commonly used to treat a large range of conditions from anxiety to Meniere’s Disease. It possesses anxiolytic, anticonvulsant, hypnotic, sedative, skeletal muscle relaxant, and amnesic properties. It is also one of the most commonly used drugs to taper off of other benzodiazepines/Alcohol withdrawal.

History

Diazepam was the second benzodiazpine (The first of which was Librium) invented by Dr. Leo sternbach of Hoffmann-La Roche at the company’s Nutley, New Jersey, facility. It was released in 1963 as an improved version of Librium, it became incredibly popular. Diazepam was the top-selling pharmaceutical in the United States from 1969 to 1982, with peak sales in 1978 of 2.3 billion tablets.

Formulations

It is available in instant release forumlations of 2mg, 5mg, and 10mg tablets.

It is also available in an oral solution of 5mg/5ml (1mg/ml)

Doses

NOTE: Higher doses have an increased risk of blacking out.

Oral

Light	2.5-5mg
Common	5-15mg
Heavy	15-30mg+

Duration

Note: Duration can be significantly longer with higher doses.

Oral

Onset	30-90 Minutes
Total	Up to 24 hours, Main effects are generally felt for roughly 8-12 hours.

Effects

Positive

• Euphoria
• Relaxation
• Anti-Anxiety effects

Neutral

• Drowsiness
• Appetite fluctuation

Negative

• Memory loss
• Blackout potential
• Motor skill impairment
• Dizziness
• Depression
• Irritability, aggression, rage
• Personality changes
• Emotional and social dissociation or de-realization (long term use)

Harm Reduction

When on high doses of benzodiazepines, users are likely to black out and potentially hurt themselves through a variety of adventures. If you are using it as a sleep aid, it's recommended to continue doing what you're doing until you begin to feel drowsy, then go to bed. Some users report Diazepam(and benzodiazepines in general) to lead to compulsive redosing, trying to find a “high” which is where a fair amount of the point above comes from. To avoid this keep doses low and be wary of reduced inhibitions while under the influence of Diazepam.

Interactions

As with other depressants, Alprazolam should not be combined with any other CNS depressants (such as Alcohol), at the risk of respiratory depression, which can lead to death.

See the Drug combinations chart for more information.

Chemistry and Pharmacology

Diazepam can be administered orally, intravenously (Has to be diluted, as it is painful and damaging to veins), intramuscularly, or as a suppository. Peak plasma levels occur between 30 and 90 minutes after oral administration and between 30 and 60 minutes after intramuscular administration; 10-45 minutes for Rectal, and between 1-5 minutes intravenously. Diazepam is highly protein-bound, with 95-99% of the absorbed drug being protein-bound. Diazepam is highly lipid-soluble, and is widely distributed throughout the body after administration. It easily crosses the blood-brain-barrier. After absorption, diazepam is redistributed into muscle and adipose tissue. Continual dialy doses of Diazepam quickly build to a high concentration in the body (mainly in adipose tissue) Diazepam unergoes oxifative metabolism by demethylation (CYP 2C9, 2C19, 2B6, 3A4, and 3A5) hydroxylation (CYP 3A4 and 2C19) and glucuronidation in the liver as part of the cytochrome P450 enzyme system. The main active metabolite of diazepam is Desmethyldiazepam (Nordiazepam) Other metabolites inclue minor active metolites temazepam and oxazepam.

Legal Status

International

Diazepam is a schedule IV controlled drug under the Convention on Psychotropic Substances.

UK

Classified as a Class C drug.