Alprazolam

Alprazolam
The skeletal formula of Alprazolam.
Chemical Nomenclature
Common names	Alprazolam, Xanax
Systematic name	8-Chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
Routes of Administration
Oral Dosage Presumes no tolerance Threshold 0.25 mg Light 0.25 - 0.75 mg Common 1 - 3 mg Strong 3 - 6 mg Heavy 7 mg+ Duration Total 2 - 6 hours Onset 15 - 90 minutes Peak 1 - 2 hours Offset 2 - 6 hours Afterglow 2 - 4 hours

Alprazolam (trade name Xanax) is a short-acting psychoactive drug of the benzodiazepine class which produces anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, and amnestic effects. Alprazolam, like other benzodiazepines, binds to specific sites on the GABAA gamma-amino-butyric acid receptor. Alprazolam is commonly used and FDA approved for the medical treatment of panic disorder, generalized anxiety disorder (GAD), or social anxiety disorder (SAD).

Alprazolam has a fast onset of action and symptomatic relief. Ninety percent of peak effects are achieved within the first hour of using either in preparation for panic disorder and full peak effects are achieved in 1.5 and 1.6 hours respectively. Peak benefits achieved for generalized anxiety disorder (GAD) may take up to a week.

Chemistry

Alprazolam is classed as a high-potency benzodiazepine and is a triazolobenzodiazepine, namely a benzodiazepine with a triazole ring attached to its structure. Alprazolam is a chemical analog of triazolam that differs by the absence of a chlorine atom in the o-position of the 6-phenyl ring.

Pharmacology

Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site on the GABAA receptor and modulating the function of the GABA receptor, the most prolific inhibitory receptor within the brain. The GABA chemical and receptor system mediates inhibitory (or calming effects) of alprazolam on the nervous system.

Alprazolam causes a marked suppression of the hypothalamicpituitary-adrenal axis. Administration of alprazolam has been demonstrated to elicit an increase in striatal dopamine concentrations.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely if ever occur all at once but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Physical Effects

The physical effects of Alprazolam can be broken down into several components all of which progressively intensify proportional to dosage. These are described below and generally include:

• Sedation - In terms of energy level alterations, Alprazolam is extremely sedating and often results in an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.
• Dizziness
• Muscle relaxation
• Motor control loss
• Respiratory depression
• Salivation

Cognitive Effects

The cognitive effects of Alprazolam can be broken down into several components all of which progressively intensify proportional to dosage. The general head space of Alprazolam is described by many as one of intense sedation and decreased inhibition. It contains a large number of typical depressant cognitive effects.

The most prominent of these cognitive effects generally include:

• Amnesia
• Anxiety suppression
• Thought deceleration
• Disinhibition
• Information processing suppression
• Euphoria
• Compulsive redosing

Toxicity and harm potential

Lethal dosage

The acute oral LD50 in rats is 331–2171 mg/kg. Other experiments in animals have indicated that cardiopulmonary collapse can occur following massive intravenous doses of Alprazolam (over 195 mg/kg; 975 times the maximum recommended daily human dose of 10 mg/day).

As with all GABAergic drugs, overdose can be lethal when mixed with other depressants including alcohol or opioids.

Tolerance and addiction potential

Tolerance will develop to the sedative-hypnotic effects within a couple of days. Withdrawal symptoms or rebound symptoms may occur after ceasing treatment abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.

Benzodiazepine discontinuation is notoriously difficult; it is potentially life threatening for individuals using regularly to discontinue use without tapering their dose over a period of weeks. There is an increased risk of seizure following discontinuation of benzodiazepines. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Legal issues

• International: Alprazolam is included under the United Nations Convention on Psychotropic Substances as Schedule IV.
• United States: Alprazolam is a prescription medication assigned to Schedule IV of the Controlled Substances Act by the DEA.
• United Kingdom: The drug is a class C drug under the UK drug misuse classification system. It can be obtained as a private prescription, but not through the NHS.
• Ireland: Alprazolam is a Schedule 4 medicine.
• Sweden: Alprazolam is a prescription drug in List IV (Schedule 4) under the Narcotics Drugs Act (1968).
• The Netherlands: In the Netherlands, Alprazolam is a List 2 substance of the Opium Law and is available for prescription.
• Australia: Alprazolam was originally a Schedule 4 (prescription only) medication; however, as of January 2014, it will become a Schedule 8 medication, subjecting it to more rigorous prescribing requirements.

See also

• Specific Substances
• Entactogens
• Alcohol
• Benzodiazepines
• Depressants
• Preparation:Benzodiazepine solution