Alprazolam

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Alprazolam is a short acting anxiolytic of the benzodiazepine class of drugs. It is commonly used and FDA approved for the treatment of panic disorders and anxiety disorders, such as GAD/SAD. It is available in both instant and time released version.

History

Alprazolam was first released by Upjohn, under the brand name Xanax. The patent was filed in October 1969, granted in October of 1976, and expired in September of 1993. It was first released in 1981, for the treatment of panic disorders.

Formulations

Instant release tablets are available in 0.25mg, 0.5mg, 1mg, and 2mg.

Extended Release tablets are available in 0.5mg, 1mg, 2mg, and 3mg.

Oral solutions are available in 0.5mg/5mL and as 1mg/1mL solutions.

Dosage

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

Oral
Light 0.25-0.5mg
Common 0.5-1.5mg
Strong 1.5-2mg
Heavy 2-3mg

Duration

Note: Duration can be significantly longer with higher doses.

Oral
Onset 20-40 minutes
Duration 5-8 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 Alprazolam (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 Alprazolam.

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

Alprazolam is absorbed fairly rapidly, with peak plasma levels achieved around the one-two hour mark.

It is primarily metabilised via CYP3A4. Alprazolam is a chemical analogue of triazolam. It is a triazolobenzodiazepine. It binds to the GABA(a) receptor and modulates the function of the GABA receptor. You can learn more about the GABA(a) receptor here.

The LD50 of Alprazolam in rats is 331-2171mg/kg.

An Australian study (2004) of overdose admissions between 1987 and 2002 found alprazolam, which happens to be the most prescribed benzodiazepine in the U.S. by a large margin, to be more toxic than diazepam and other benzodiazepines.

Legal Status

USA

Alprazolam is a schedule IV substance.

UK

Under the UK drug misuse classification system benzodiazepines are class C drugs (Schedule 4).

Ireland

Alprazolam is a schedule 4 medicine.

Sweden

Alprazolam is a prescription drug in List IV under the Narcotic Drugs Act (1968).

Netherlands

Alprazolam is a List 2 substance of the Opium Law and is available for prescription.

Australia

Alprazolam was orginally a Schedule 4 (prescription only) medication; yet as of February 2014 it has become a Schedule 8 medication.