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Alprazolam

Introduction to Alprazolam


[​IMG]Alprazolam is a potent, short-acting (11-hour half-life) drug which belongs to a group of medicines known as benzodiazepines. Like all benzodiazepines, it works by binding to a specific site (benzodiazepines have their own receptor site) on the GABA-A receptors. It increases and potentiates GABA activity in this way. Since GABA (gamma-aminobutyric acid) is the brain's major inhibitory neurotransmitter alprazolam has a sedative effect on the nervous system and thus a general sedative effect.

In general benzodiazepines will induce sleep when given at high doses and provide sedation and reduce anxiety when given in low, divided doses during the day.

Alprazolam has anxiolytic, sedative, hypnotic, skeletal muscle relaxant, anticonvulsant and amnestic properties. It is however, most frequently prescribed for its anxiolytic effects.

Like other benzodiazepines, alprazolam is an addictive substance with considerably high abuse potential. Alprazolam is one of the most highly abused benzodiazepines and in the U.S. it is currently the most widely prescribed. [2]

Using Alprazolam

Ways of Administration

Alprazolam is prescribed in tablet form for oral use in doses of 0.125mg, 0.25mg, 0.5mg, 1.0mg and 2.0mg tablets. When taken orally it has a high bioavailability of 80-100%.[citation needed] However when Alprazolam is used recreationally it is sometimes administered intranasally (snorting), though this is not an efficient route of administration as the drug is barely soluble in water and does not readily cross the nasal membrane. Despite the theoretically lower bioavailability many users insist that alprazolam delivers a greater positive effects via this route of administration.

Effects of Alprazolam

Alprazolam relieves fear and anxiety if taken during or at the beginning of a panic attack and acts as a tranquilizing agent in general. When taking in larger doses alprazolam makes the user feel sleepy due to its sedative effects on the nervous system. If taken in sufficiently large quantities it will "knock the user out" and induce sleep.

Combinations with Alprazolam

Alprazolam is often combined with other drugs both in the context of recreational use and legitimate medical treatment.

For severe anxiety disorders, alprazolam may be prescribed together with propranolol. Propranolol is a non-cardio selective beta blocker and blocks and reduces adrenaline (epinephrine) and noradrenaline (norepinephrine) in the nervous system. This combination would be particularly effective when prescribed for panic disorder.

Recreational users sometimes combine alprazolam with an opioid (for example oxycodone) in order to increase euphoria, sedation, and the nod. Another reason for this combination is to reduce the amount of oxycodone needed for a "sufficient" high, as alprazolam significantly potentiates the sedative effects of opiates.

Different Uses for Alprazolam

Alprazolam is also prescribed (in some cases in conjunction with other drugs) to treat nausea associated with chemotherapy.

Pharmacology of Alprazolam

Alprazolam is a very potent benzodiazepine. All benzodiazepines, especially alprazolam cause significant suppression of hypothalamic-pituitary-adrenal axis.

Like all benzodiazepines, the pharmacological effects of alprazolam are believed to be primarily caused by the enhancement of GABA-mediated inhibition in the central nervous system. GABA is an endogenous neurotransmitter that is released from nerve cell termini. It targets and binds to the GABA protein receptors of other nerve cells, triggering an increase in the conductance of chloride ions in the target cell. This wave of neurotransmission has an overall inhibitory effect on nervous activity.

When introduced into the nervous system, alprazolam like other benzodiazepines binds to a modulatory epitope (the "BZD site") of the GABA receptor protein. This interaction results in a conformational change to the protein which makes it more receptive to its endogenous ligand GABA. This potentiates the inhibitory nervous effects of GABA.

Alprazolam is an analogue of triazolam, differing only by the absence of a chloride moiety in the ortho position of the 6-phenyl ring. Alprazolam can be made using the same method that is needed to create triazolam, the only difference here is that alprazolam's structure begins with 2-amino-5-chlorobenzophenone.

LD50 (mg/kg) [3] :
Mice : 1020 orally, 540 intraperitoneally
Rat : >2000 orally, 610 intraperitoneally

Chemistry of Alprazolam

Column 1 Column 2
Systematic(IUPAC) name: 8-Chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
Synonyms: 8-Chloro-1-methyl-6-phenyl-4H-2,3,5,10b-tetraazabenzo[e]azulene, 8-Chloro-1-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine, 8-Chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine, D-65MT, U-31889, Alplax, Cassadan, Esparon, Mylan A1, Tafil, Tranquinal, Trankimazine, Xanax, Zopax
Molecular Formula: C17H13ClN4
Molar mass: 308.76 g/mol [4]
CAS Registry Number: 28981-97-7
Melting Point: 228-228.5 ℃
Boiling Point: no data
Flash Point: no data
Solubility: freely soluble in chloroform; soluble in alcohol; sparingly soluble in acetone; slightly soluble in ethyl acetate; insoluble in water
Additionnal data: none
Notes: crystallized from ethyl acetate
[3]

The Dangers of Alprazolam

As with all benzodiazepines, there are many dangers when using alprazolam.

Physical Health Risks

Dangerous in Pregnancy

Alprazolam is contraindicated in pregnancy as it may cross the placenta and enter breast milk.[citation needed]. Advice from a medical professional should be sought if you are considering taking this drug whilst pregnant, planning to become pregnant, or breastfeeding.

Impaired Alertness

People who are either driving or operating heavy machinery should take great care when taking Alprazolam. One is advised to take time first to learn how they react to the drug before engaging in dangerous activities. Alprazolam can impair attention and alertness.

Risk to Children and Elderly

Benzodiazepines should be prescribed with special caution to children and the elderly due to a marked increase in sedation.[citation needed]

Overdose

One of the most serious dangers associated with alprazolam use is that of overdose. Overdose can even occur by accident due to the addictive nature of the drug. Due to alprazolam's pharmacological profile, it can produce significant excessive sedation of the central nervous system, causing the user to potentially become unconscious involuntarily due to the drugs hypnotic effects. Once unconscious the excessive sedation can lead to excessive respiratory depression and the users breathing can slow down to a dangerously low level.

The severity is dependent on dose of the drug taken. When alprazolam is taken in combination with opioids, tricyclic antidepressants, or alcohol this can lead to severe toxicity or even death - due to complete sedation of the respiratory system causing breathing itself to practically stop and not provide enough oxygen to the brain and body thus leading to death.

Reported Deaths

A 2003 study in found that alprazolam had involvement in the highest number of deaths (38.1) per 100 000 prescriptions than any other benzodiazepine in New Zealand in 2001. However, alprazolam was only a contributory and not the primary agent of death in any of those fatalities.[5]

Mental Health Risks

Suicidal Ideation

Alprazolam rarely induces suicide ideation.[citation needed] If this happens one should stop taking this medicine and contact one's doctor immediately.

Paradoxical Reactions

Sometimes people who take alprazolam experience paradoxical reactions such as twitches and tremor, aggression, hostile rage or hyperactivity. If this happens then the prescribing doctor should be contacted immediately and the medication should be gradually reduced (under medical supervision).

Side Effects

Reported side effects of alprazolam include sedation, sleepiness, speech difficulties, abnormal coordination, memory impairment, hyperventilation, decreased appetite decreased, muscle twitching, hot flushes. [6]

Addiction

Physical Addiction

Withdrawal symptoms including seizure have been reported even after only short therapy on doses of alprazolam at therapeutic levels appropriate for treatment of anxiety (1 to 4 mg/day). However, the severity of these symptoms does seem connected to length of treatment and dose levels, and it has been reported that these are more severe when doses are decreased quickly or discontinued without tapering. There may be a higher risk of withdrawal seizures for those who have been taking more than 4 mg/day.[6]

Addiction

Mental Addiction

Producing/Growing Alprazolam

Forms of Alprazolam

Legal Status of Alprazolam

United Nations

USA

EU

Australia

Alprazolam is a Schedule 8 drug in Australia. It is illegal to possess without authority and/or a prescription. All Schedule 8 drugs are controlled substances and are recorded by the State to prevent either illegal diversion of drugs or misuse/abuse or substances.

Other Countries

History of Alprazolam

Alprazolam was first released in 1981 by pharmaceutical company Upjohn (now owned by Pfizer). Initially, alprazolam was indicated specifically for the treatment of panic disorders (panic attacks). At the time there were no other benzodiazepines which were specifically marketed for this disorder thus allowing the drug to target a "hole in the market".[citation needed]

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References

  1. ^AMA Drug Evaluations Annual, 1994, p238
  2. ^Lader, Makcolm. History of Benzodiazepine Dependence. Journal of Substance Abuse Treatment. 8 (1991), 53-59.
  3. ^ a bMerck Index, fifteenth edition (2013)
  4. ^Calculated from Atomic Weights of the Elements, 2007
  5. ^David M. Reith, John Fountain, Rebecca McDowell, and Murray Tilyard. Comparison of the Fatal Toxicity Index of Zopiclone with Benzodiazepines. Journal of Toxicology: Clinical Toxicology. Vol. 41, No. 7, pp. 975–980, 2003
  6. ^ a bAlprazolam product monograph, Pfizer, revised 2011

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