Metizolam: Difference between revisions

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==Chemistry==

Metizolam, or desmethyletizolam, is a structural relative of [[benzodiazepines]] whereby the benzene ring has been replaced by a thiophene ring, classifying it as a [[thienodiazepine]]. It differs structurally from its parent compound [[etizolam]] through the removal of the methyl group on the triazole ring.

Metizolam, or desmethyletizolam, is the demethylated analogue of the closely related etizolam. It is a structural relative of [[benzodiazepines]] whereby the benzene ring has been replaced by a thiophene ring, classifying it as a [[thienodiazepine]]. It differs structurally from its parent compound [[etizolam]] through the removal of the methyl group on the triazole ring.

Metizolam contains a thiophene ring fused to a diazepine ring, which is a seven member ring with the two nitrogen constituents located at R1 and R4. Thiophene is a five member aromatic ring with one sulfur atom. This forms the thienodiazepine core of metizolam. An ethyl chain is bound to this bicyclic structure at R7.

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==Pharmacology==

[[Thienzodiazepines]] produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the [[neurotransmitter]] gamma aminobutyric acid ([[GABA]]) by acting on its receptors.<ref>Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796</ref> As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the [[sedating]] (or [[anxiety suppression|calming effects]]) of metizolam on the nervous system.

Metizolam is absorbed fairly rapidly, with peak plasma levels achieved between 30 minutes and 2 hours. It has a mean elimination half life of about 3.4 hours. Metizolam acts as a full agonist at the benzodiazepine/GABAa receptor to produce its range of therapeutic and adverse effects.

Thienotriazolodiazepines are easily oxidized, rapidly metabolized, and have a lower risk of accumulation, even after prolonged treatment. Metizolam has a powerful anxiolytic action that is about 6 times greater than that of diazepam. At higher dosages, metizolam allows for a reduction in time taken to fall asleep, an increase in total sleep time, and a reduction in the number of awakenings. Metzolam has also shown some similar characteristics to tricyclic antidepressants.<ref>http://www.carloanibaldi.com/terapia/schede/DEPAS.htm</ref>

Although Metizolam has certain potential benefits such as anxiety suppression and muscle rest, it should be administered with caution and in small doses because of its harm and abuse potential. Metizolam can be life-threatening if administered with other depressants, including alcohol and opiates.

The harm potential due to long-term usage and toxicity dosage levels of Metizolam are not yet clear since the substance has not been adequately studied and analyzed in a scientific context. This is simply because of the lack of a known history of human usage.

==Subjective effects==

@@ Line 10: / Line 10: @@
 ==Chemistry==
-Metizolam, or desmethyletizolam, is a structural relative of [[benzodiazepines]] whereby the benzene ring has been replaced by a thiophene ring, classifying it as a [[thienodiazepine]]. It differs structurally from its parent compound [[etizolam]] through the removal of the methyl group on the triazole ring.
+Metizolam, or desmethyletizolam, is the demethylated analogue of the closely related etizolam. It is a structural relative of [[benzodiazepines]] whereby the benzene ring has been replaced by a thiophene ring, classifying it as a [[thienodiazepine]]. It differs structurally from its parent compound [[etizolam]] through the removal of the methyl group on the triazole ring.
 Metizolam contains a thiophene ring fused to a diazepine ring, which is a seven member ring with the two nitrogen constituents located at R<sub>1</sub> and R<sub>4</sub>. Thiophene is a five member aromatic ring with one sulfur atom. This forms the thienodiazepine core of metizolam. An ethyl chain is bound to this bicyclic structure at R<sub>7</sub>.
@@ Line 18: / Line 18: @@
 ==Pharmacology==
 [[Thienzodiazepines]] produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the [[neurotransmitter]] gamma aminobutyric acid ([[GABA]]) by acting on its receptors.<ref>Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796</ref> As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the [[sedating]] (or [[anxiety suppression|calming effects]]) of metizolam on the nervous system.
+Metizolam is absorbed fairly rapidly, with peak plasma levels achieved between 30 minutes and 2 hours. It has a mean elimination half life of about 3.4 hours. Metizolam acts as a full agonist at the benzodiazepine/GABAa receptor to produce its range of therapeutic and adverse effects.
+Thienotriazolodiazepines are easily oxidized, rapidly metabolized, and have a lower risk of accumulation, even after prolonged treatment. Metizolam has a powerful anxiolytic action that is about 6 times greater than that of diazepam. At higher dosages, metizolam allows for a reduction in time taken to fall asleep, an increase in total sleep time, and a reduction in the number of awakenings. Metzolam has also shown some similar characteristics to tricyclic antidepressants.<ref>http://www.carloanibaldi.com/terapia/schede/DEPAS.htm</ref>
+Although Metizolam has certain potential benefits such as anxiety suppression and muscle rest, it should be administered with caution and in small doses because of its harm and abuse potential. Metizolam can be life-threatening if administered with other depressants, including alcohol and opiates.
+The harm potential due to long-term usage and toxicity dosage levels of Metizolam are not yet clear since the substance has not been adequately studied and analyzed in a scientific context. This is simply because of the lack of a known history of human usage.
 ==Subjective effects==