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Etizolam

Etizolam (Depas, Etilaam, Etizola, Sedekopan) is a benzodiazepine analogue. It works in a very similar way to benzodiazepines although it actually has a slightly different chemical structure as it has a thiophene ring (it is a thienodiazepine drug) instead of a benzene ring. It is an anticonvulsant and muscle relaxant and has a variety of different applications that it might be prescribed for. It is also an anxiolytic (reduces anxiety) and hypnotic (sleep inducing) drug.

Contents




[top]Introduction to Etizolam

Etizolam is mainly prescribed to treat insomnia, and anxiety disorders such as panic disorder or generalized anxiety disorder. Etizolam is a good medication for instant relief from panic attacks and anxiety, it can also be taken as a preventative in this respect. Its unwanted side effects include drowsiness, weakness and lethargy

For anxiety the usual prescription is 0.5 - 1.0mg up to 3 times per day.
For insomnia the usual dose is 1-2mgs 30 minutes before retiring.
Etizolam activates the same benzodiazepine receptor as other typical drugs of this class (such as diazepam). Therefore it binds to the GABAa receptors and potentiates GABA transmission and causes sedation of the central nervous system. This is what leads to its range of therapeutic and unwanted side effects.

1mg of Etizolam is roughly equivalent to 10mg of Diazepam (vallium)

[top]Also Known As

  • IUPAC 7-(2-chlorophenyl)-4-ethyl-13-methyl-3-thia-1,8,11,12-tetraazatricyclo [8.3.0.02,6]trideca-2(6),4,7,10,12-pentaene
  • 4-(2-Chlorophenyl)-2-ethyl-9-methyl-6H-thieno[3,2-f]-s-triazolo[4,3-a][1,4]diazepine
  • AHR 3219
  • Y-7131
  • Etilaam
  • Depas
  • Pasaden


[top]Using Etizolam

[top]Ways of administration

[top]Oral

Etizolam is available in tablet form, usually in 0.5mg and 1.0mg tablets.
It can also be obtained as a 'raw' powder ('pure', with out fillers/adulterants)

[top]Sub-lingual/transbuccal

A commonly reported method of administration is to crush a tablet with the front teeth, and place the resultant powder under the tongue to dissolve. It is reported to have a mild to no taste.

[top]Insufflation

Etizolam is not soluble in water so intranasal administration (sniffing) of crushed up tablets is not an efficient way to administer the drug. Although many users may dispute this claim and state that they receive more euphoria via this route of administration. The efficacy of intranasal administration of benzodiazepines (as with other drugs) is a common source of dispute between users.

[top]Rectal

Rectal application has been reported to be the most common effective method of administration. The tablets have been crushed and (or powder) placed into a capsule designed as a suppository.

[top]Effects of Etizolam

Etizolam is a triazolothienodiazepine and it is more euphoric than many benzodiazepines. Etizolam has a broad range of effects, much like benzodiazepines. It has: hypnotic, amnesic, sedative, anti-convulsant and skeletal muscle relaxant effects. It is also a potent anxiolytic drug which has a half-life of 6 hours.


[top]The dangers of Etizolam

There are many dangers to be considered when taking etizolam. Like benzodiazepines, etizolam possesses very strong sedative effects and effects ones judgement and also lowers ones inhibitions. People who start taking etizolam should avoid driving or other dangerous activities involving heavy machinery until they have learned how the drug effects them.

It should most certainly not be used during pregnancy due to the risk of the drug passing into the breast milk. For similar reasons it should not be used during pregnancy or when attempting to become pregnant without medical supervision from a doctor.

The benzodiazepine class in general have been known to inhibit risk assessment processing, the larger the dose taken, the greater the inhibition. This has lead to individuals undergoing uncharacteristic decision making behaviour, often to the complete disbelief of the user once the effects of the drug have run its course in the individual.

[top]Side effects of Etizolam

Etizolam has been reported to cause blepharospasms in some cases. These are abnormal contractions of the eyelid. Symptoms of this are sometimes present for just a few days, but in some cases they can be a chronic, persistent and even lifelong problems.
The eyelids when spasmotic can sometimes feel clamped shut by the malfunctioning muscles thus resulting in the patient being unable to see out of the eye. It is sometimes very difficult for the patient to be able to force their eye open. These problem is usually treated with either magnesium chloride or botulism toxin which is injected into the spasmodic muscle in order to paralyse it and provide immediate relief to the patient.

Some users have reported feelings of depression whilst under the influence of etizolam.

Benzodiazepines are known to retard learning ability and memory forming in those under the influence.

[top]Tolerance, Dependence and Withdrawal

As with all drugs in the benzodiazepine class, etizolam is a physically and psychologically addictive substance. Chronic use lasting more than 4 weeks can result in addiction. If the medication is discontinued abruptly after a protracted period of administration a withdrawal syndrome can ensue which might involve excitatory withdrawal symptoms such as anxiety, tremor, insomnia, lack of appetite, panic attacks etc. In rare cases this sudden withdrawal syndrome can even result in a seizures (fit) this can be a life threatening occurrence. Some patients even consider suicide due to the extreme unpleasantness of the withdrawal.

The withdrawal syndrome occurs due to the initial over stimulation of the GABAergic system, this causes desensitization of the GABA receptors and also a decrease in overall GABA production. When the drug is discontinued without using a gradual taper (which is the much preferred option) the central nervous system does not produce adequate stimulation of the GABAergic system. Since the GABAergic system is responsible for modulating the inhibitory transmission of signals - this results in muscles shaking, convulsing and possibly leading to a seizure.

There is evidence however that etizolam is less addictive than other benzodiazepines. Because it has, to some extent, a greater efficacy under conditions of GABAergic deficit, it may represent a possible drug of choice with reduced risk of producing tolerance and dependence after long-term use.

Etizolam, unlike most other benzodiazepines (some of which can increase levels of estradiol), has prolactogenic effects, leading to an increase in prolactin blood levels, which can lead to sexual side effects in men.
[1]

[top]Overdose

Overdose is one of the most serious dangers associated with benzodiazepines, if a patient has taken an overdose it can lead to excessive sedation of the respiratory system leading to an inadequate supply of oxygen to the brain and body. If the overdose is taken with other CNS depressants - such as opioids or alcohol then the sedation of the respiratory system can be so severe that it stops completely - this naturally leads to death.

There have been at least two reported deaths where Etizolam have been implicated as a major contributing (if not only) factor.[2] Although in both cases, it appears that there was history of some form of extreme organ dysfunction. In one case the patient had a liver cirrhosis history, and the other had a chronic kidney disorder.


[top]Pharmacology of Etizolam

Since etizolam is a thienodiazepine benzodiazepine derivative its pharmacological profile is very similar (if not the same) to other benzodiazepines. It is absorbed quickly and it's peak concentration in the blood-plasma occurs in between 30 minutes and 2 hours.

It has an active metabolite called alpha-hydroxyetizolam which is eliminated more slowly and has a longer half-life than it's parent drug of about 8 hours.

It's pharmacological profile and the effects of the drug have been found to be similar to diazepam.

Etizolam is purportedly metabolized by the hydroxylation of the methyl group and that of the ethyl group. The cytochrome P450 (CYP) enzymes catalyzing etizolam metabolism have not been fully clarified. [3]


[top]Etizolam Production



[top]Etizolam Chemistry



[top]Etizolam Legal Status


Poland
Etizolam may be scheduled under the Act on Counteracting Drug Addiction[4] and the State Sanitary Inspection -Article 27c, 14/03/1985 (Sejm, October 2010, 3rd amendment)


[top]Forms of Etizolam


Etizolam is most often found to be available as small blue tablets measuring around 5mm across. It can also be found as a 'pure' powder, packaged in small 'ziplock' bags.


[top]History of Etizolam

[top]Interest in etizolam over time



[top]References

  1. ^ http://www.ncbi.nlm.nih.gov/pubmed/10083975
  2. ^ http://www.drugs-forum.com/forum/local_links.php?action=jump&catid=129&id=11689
  3. ^ http://www.springerlink.com/content/l576336j645733x6/
  4. ^ http://www.drugs-forum.com/forum/local_links.php?action=jump&catid=15&id=11713


Created by Oneiromancer, 19-09-2011 at 23:07
Last edited by profesor, 03-10-2012 at 18:08
Last comment by JTC3889 on 05-05-2013 at 21:23
7 Comments, 76,532 Views

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