Benzodiazepines: Drug Information Page

Benzodiazepine Basics

Basic Information:

The first benzodiazepine was chlordiazepoxide, synthesized by chemist Leo Sternbach at Hoffman La Roche in the 1950's & eventually marketed as Librium. It was soon followed by diazepam (i.e. Valium) in 1963.

Other benzodiazepines - alprazolam (i.e. Xanax), temazepam (i.e. Restoril), triazolam (i.e. Halcion), lorazepam (i.e. Ativan), midazolam (i.e. Versed), flunitrazepam (i.e. Rohypnol), estazolam (i.e. Pro-Som).

Most benzodiazepines are legally classified as schedule IV controlled substances. Use or possession without a prescription is illegal in the US.

Anxiolytic, sedative, hypnotic, skeletal muscle relaxant, anticonvulsant, amnestic properties.

Use:

Have largely taken the place of barbiturates as the sedative class of choice for most purposes. Safety profile superior to barbiturates.

1mg Xanax (alprazolam) Tablets
Commonly prescribed for anxiety & panic disorders

Useful in treatment of acute agitation, panic & anxiety spectrum disorders. Most recognize their value for treating acute symptoms. Efficacy and appropriateness for chronic management is still debated, but long term prescrbing is becoming more common.

For long term management of anxiety disorders - Some practitioners support benzodiazepines for chronic use. Others instead reccommend SSRI antidepressants for chronic use, with benzos reserved for limited use during the first few weeks of SRI-treatment and/or intermittently thereafter.

Useful in countering the the initial side effects associated with early SSRI therapy.

Useful in hospital medicine. Heavily used in the ER, critical care unit, operating room, and elsewhere to provide sedation, hypnosis, amnesia, and everything in between, typically by injection.

Benzodiazepines are often used to potentiate the sedative effects of CNS depressants such as opioid analgesics. Also used to counter the edginess associated with stimulant or psychedellic use. Where it pertains to casual or illicit use, Benzodiazepines serve a supplemental role rather than a primary role.

Associatd with deaths due to poly-drug use by dumb or naive individuals, owing to interactions with narcotics & alcohol - combination of benzo's with other CNS depressants often causes a dangerous potentiation of CNS depression and a narrowed therapeutic index.



Benzodiazepine distribution in the brain
Reveals BZP receptor concentration

Pharmacology:

Bind to the GABA-a receptor - i.e. gamma-amino-butyric-acid receptor. BZP binding changes the GABA receptor into a conformation whpotentiates the binding of the inhibitory neurotransmitter gamma-amino-butyric-acid, leading to reduced communication between neurons. This produces a calming effect on areas of the brain and CNS.

Effects:

Have potential to produce tolerance and dependence with extended use. Benzodiazepine withdrawal syndrome is similar to alcohol withdrawal and may lead to seizures and morbidity (i.e. death).

Vintage Ad for Valium

Will substitute for alcohol in alcohol withdrawal. Modestly helpful in treating symptoms of opioid withdrawal; reducing agitation, muscle spasms, and insomnia. Commonly used during alcohol & narco-withdrawal.

Benzodiazepines themselves produce little to no euphoria & theoretically should have little potential for abuse. Regardless, deadbeat drunks, teens, part animals & dull-witted individuals gravitate toward benzo's for the relaxation, social disinhibition and psychomotor & cognitive retardation they provide.

Short term effects include anxiolysis, relaxation, cognitive impairment, muscle-weakness & social disinhibition. Higher doses produce hypnosis, anaesthesia & anterograde amnesia.

Long term effects include mental dullness & cognitive impairment, memory loss, paradoxical anxiety & panic symptoms, tolerance & dependence.