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Alprazolam

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Alprazolam
Clinical data
Pregnancy
category
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability80-90%
MetabolismHepatic
Elimination half-life6-12 hours
ExcretionRenal
Identifiers
  • 8-Chloro-1-methyl-6-phenyl-4H-
    1,2,4-triazolo(4,3-a)(1,4)benzodiazepine
CAS Number
PubChem CID
DrugBank
CompTox Dashboard (EPA)
ECHA InfoCard100.044.849 Edit this at Wikidata
Chemical and physical data
FormulaC17H13ClN4
Molar mass308.8

Alprazolam is a drug which is a benzodiazepine derivative. It is classified as short-acting, and is used to treat anxiety disorders and insomnia.

Pharmacology

Alprazolam is a triazolobenzodiazepine, that is, a benzodiazepine with a triazolo-ring attached to its structure. Alprazolam binds to the GABAA subtype of the GABA receptor, increasing inhibitory effects of GABA within the central nervous system. The binding site for benzodiazepines is distinct from the binding site for GABA on the GABA receptor.

Unlike other benzodiazepines, alprazolam may also have some antidepressant activity, although clinical evidence of this is lacking.

Pharmacokinetics

The mechanism of action is not fully understood; However, Alprazolam is readily absorbed from the gastrointestinal tract. The peak plasma concentration is achieved in 1-2 hours. Most of the drug is bound to plasma protein, mainly albumin. Alprazolam is hydroxylated in the liver to α-hydroxyalprazolam, which is also pharmacologically active. This and other metabolites are later excreted in urine as glucuronides. Some of the drug is also excreted in unchanged form.

Indications

File:Alprazolam2mgresize.jpg
alprazolam 2mg tablet bottle

The main medical uses for alprazolam include:

  • Treatment of panic disorder, with or without agoraphobia.
    Alprazolam is very effective in preventing panic attacks. However, despite its efficacy, many psychiatrists are reluctant to use alprazolam for this condition because of the possibility of dependence and interdose anxiety due to its short-acting nature. An extended-release formulation of alprazolam known as Xanax XR® was introduced in 2001 and is often preferred.
  • Treatment of panic attacks.
    Alprazolam is taken as needed (PRN); 4 to 6 doses per month are the acceptable limit. If dependence seems to develop and/or the limit is exceeded, therapy may be reconsidered and/or discontinued.
  • Long-term treatment of severe generalized anxiety disorders.
    Alprazolam may be used for long-term treatment of anxiety if other therapies either do not work or are contraindicated. Duration of therapy in this case is often four months or longer. The decision to use alprazolam for this purpose must be carefully made by a specialized psychiatrist, taking into account the individual's suffering, quality of life, loss of social performance and risk of dependence.

Availability

Alprazolam is generally sold in generic form in the United States. It is also sold under many other brand names, depending on the country:

  • Xanax® - United States, Australia, United Kingdom, Turkey, Ireland, Greece
  • Xanax XR® - (an extended release formulation) United States
  • Niravam® - (formulary that dissolves on the tongue) United States
  • Apo-Alpraz® - Canada (also made by other companies under different names)
  • Xanor® - Finland, Philippines, South Africa, Sweden, Norway
  • Kalma® - Australia, New Zealand
  • Ralozam® - Australia, New Zealand
  • Zamhexal® - Australia
  • Alplax® - Argentina
  • Alviz® - Indonesia
  • Alzolam® - India, Malaysia
  • Alprax® - India
  • Tranax® - India
  • Restyl® - Bahrain, Cyprus, Egypt, Iran, Iraq, Jordan, Kuwait, Lebanon, Libya, Oman, Qatar, Republic of Yemen, Saudi Arabia, Syria, United Arab Emirates
  • Tranquinal® - Ecuador, Peru
  • Trankimazin® - Spain
  • Tafil® - Costa Rica, Denmark, El Salvador, Germany, Guatemala, Honduras, Mexico, Nicaragua, Panama, Venezuela
  • Tafil AP® - (an extended release formulation) Mexico
  • Constan® - Japan
  • Solanax® - Japan
  • Zolarem® - Bahrain, Benin, Burkina-Faso, Cyprus, Egypt, Ethiopia, Gambia, Ghana, Guinea, Iran, Iraq, Israel, Ivory Coast, Jordan, Kenya, Kuwait, Lebanon, Liberia, Libya, Malawi, Mali, Mauritania, Mauritius, Morocco, Niger, Nigeria, Oman, Qatar, Republic of Yemen, Saudi Arabia, Senegal, Seychelles, Sierra-Leone, South Africa, Sudan, Syria, Tanzania, Tunia, Uganda, United Arab Emirates, Zambia, Zimbabwe
  • Zoldac® - Benin, Burkina-Faso, Ethiopia, Gambia, Ghana, Guinea, India, Ivory Coast, Kenya, Liberia, Malawi, Mali, Mauritania, Mauritius, Morocco, Niger, Nigeria, Senegal, Seychelles, Sierra-Leone, South Africa, Sudan, Tanzania, Tunia, Uganda, Zambia, Zimbabwe
  • Calmax® - Ireland

Side Effects

Common side effects of alprazolam can include:

Less common side effects can include:

  • Fatigue
  • Headache

Rare side effects can include:

Rare paradoxical side effects can include:

  • Nervousness
  • Anxiety
  • Agitation
  • Rage
  • Insomnia
  • Muscle spasms and rigidity

Long-term treatment with alprazolam may lead to physical and/or psychological dependence. Users often develop a tolerance to the drug's sedative effects, although its anxiolytic efficacy remains intact.

There is now a general consensus among many psychiatrists that alprazolam (a so-called 'high-potency' benzodiazepine) poses a particularly high risk for misuse, abuse and dependence. Withdrawal after long-term treatment should be done slowly over a period of weeks (or even months) to avoid serious withdrawal symptoms such as agitation, rebound anxiety, muscle cramps and seizures. Some patients may benefit from a substitution with diazepam.

Contraindications

Use of alprazolam should be avoided in individuals with the following conditions:

Patients at a High Risk for Abuse and Dependence

At a particularly high risk for misuse, abuse, and dependence are:

  • Patients with a history of alcohol or drug abuse and/or dependence
  • Emotionally unstable patients
  • Patients with severe personality disorders
  • Patients with chronic pain or other physical disorders

Patients from the aforementioned group should be monitored very closely during therapy for signs of abuse and development of dependence. Discontinue therapy if any of these signs are noted. Long-term therapy in these patients is not recommended.

Recreational use

alprazolam 2mg tablets

Alprazolam, like all benzodiazepines, has the potential for abuse, especially in individuals prone to addiction. Although it is not manufactured illegally, it is often diverted to the black market. The state of relaxation, anxiolysis, disinhibition and euphoria induced by benzodiazepines is the main reason for their illicit use.

For recreational effects, alprazolam is generally administered orally. Nasal insufflation (often called "snorting") sometimes occurs, but due to the drug's chemical structure, it is not absorbed through the mucous membranes. Instead, the powdered tablets and mucous drip down the back of the throat into the stomach, where they are absorbed as they would have been if taken orally. Therefore, insufflation of the drug is no more potent than when taken orally, and it often severely irritates the nasal passages. Furthermore, nasal insufflation may be significantly less potent than other means of administrations on a dosage-per-time basis, because the mucous drip enters the stomach at a slower rate than traditional ingestion.

Alprazolam is sometimes used with other recreational drugs to relieve the panic or distress of dysphoric reactions to psychedelics such as LSD and also to promote sleep in the "come-down" period following use of recreational drugs with stimulant or insomniac properties (such as LSD, cocaine, amphetamines, and MDMA). It is also often used in conjuction with marijuana for an even more relaxing effect. Also, Alprazolam is often combined with the drug Methadone to produce a unique, Heroin-like "high".

In the United States, alprazolam is a prescription drug and is assigned to Schedule IV of the Controlled Substances Act by the Drug Enforcement Administration. Internationally, alprazolam is included under the United Nations Convention on Psychotropic Substances[1].

  1. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.
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