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Tetrindole

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Title: Tetrindole  
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Subject: D-161, Sercloremine, Monoaminergic, DOV-102,677, DOV-216,303
Collection: Monoamine Oxidase Inhibitors
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Tetrindole

Tetrindole
Systematic (IUPAC) name
2,3,3a,4,5,6-Hexahydro-8-cyclohexyl-1H-pyrazino[3,2,1-j,k]carbazole
Clinical data
Legal status
?
Identifiers
CAS number  YesY
ATC code None
PubChem
ChemSpider  YesY
ChEBI  N
Chemical data
Formula C20H26N2 
Mol. mass 294.43 g/mol
 N   

Tetrindole is a tetracyclic antidepressant that functions by reversibly inhibiting monoamine oxidase A.[1] Since monoamine oxidase A preferentially deaminates serotonin, melatonin, epinephrine, and norepinephrine, inhibiting monoamine oxidase A allows for more of these monoamine neurotransmitters. Tetrindole was first synthesized by the All-Union Scientific-Research Institute of the Chemical and Pharmaceutical Industry, which is located in Moscow, Russia. [2] Tetrindole has been tested on rats and was also shown to reduce post-stressor tachycardia.[3] Tetrindole is similar in it's chemical structure, physiochemical properties, and pharmacological functions as Pirazidol, Pirlindole, and Metralindole.[2]


Contents

  • Regulatory Status 1
  • Animal Trials 2
  • Sales 3
  • Side Effects 4
  • Diet 5
  • References 6

Regulatory Status

Tetrindole or any other reversible monoamine oxidase A inhibitor has never been approved for use in the United States nor is Tetrindole found in the FDA Orange Book of Approved Drug Products.[4] However, Moclobemide, a reversible monoamine oxidase A inhibitor, is available in Australia, Europe, and Canada.[5]

Animal Trials

Korshunov performed a test in alert NMRI mice and Sprague-Dawley rats with Tetrindole. The test involved giving these test subjects a 10 mg of Tetrindole per kg of body weight. This decreased the blood pressure by an average of 6-8 mm Hg and decreased the subject's heart rate by 128±12 bpm 5 minutes after intravenous injection. The down side was Tetrindole caused bradycardic effect, which had to be neutralized by blocking the nitric oxide synthase [6]

Sales

Tetrindole is not currently available as a pharmaceutical in the United States. [5] Even with the number of antidepressant drugs continually increasing, the number of monoamine oxidase A inhibitors is decreasing. In 1999, only 2% of physicians reported that they prescribe MOAIs on a consistent basis. [7] But if Tetrindole is considered as part of the general antidepressant field, there was $9.4 billion of sales in 2012 with 270 million prescriptions. [8]


Side Effects

The most common early onset side effects of taking a monoamine oxidase A inhibitor are orthostatic hypotension, dizziness, drowsiness, insomnia, and nausea. [5] Late side effects of weight gain, edema, muscle pains, myoclonus, paresthesias, and sexual dysfunction have also been reported while taking monoamine oxidase A inhibitors. [9]

Diet

While taking any kind of monoamine oxidase A inhibitor, that are certain foods that should be avoided. Cheese is the primary food to avoid while taking a monoamine oxidase A inhibitor as eating cheese could potentially cause a fatal hypertensive crises. [10] Consult a physician about potential diet problems while taking a monoamine oxidase A inhibitor before the medication is started.

References

  1. ^ Medvedev, Alexei E.; Alexandra A. Kirkel, Natalia S. Kamyshanskaya, Tatyana A. Moskvitina, Ludmila N. Axenova, Vladimir Z. Gorkin, Natalia I. Andreeva, Svetlana M. Golovina and Mikhail D. Mashkovsky (20 January 1994). "Monoamine oxidase inhibition by novel antidepressant tetrindole".  
  2. ^ a b Chistyakov V.V. (January 1993). "Metabolism of Tetrindole". Khimiko-farmatsevticheskii Zhurnal 27 (1): 4–6. 
  3. ^ Korshunov, VA; Murashev AN; Ivashev MN; Dugin SF; Medvedev OS (September–October 2000). "Comparative study of hemodynamic effects of antidepressants (tetrindole and desipramine) during immobilization stress in hypertensive rats". Eksperimental'naia i klinicheskaia farmakologiia 63 (5): 18–20.  
  4. ^ "Orange Book: Approved Drug Products with Therapeutic Equivalence Evaluations". fda.gov. U.S. Food and Drug Administration. Retrieved 8 December 2014. 
  5. ^ a b c Fiedorwicz, Jess G. and Karen L. Swartz (July 2004). "The Role of Monoamine Oxidase Inhibitors in Current Psychiatric Practice". Journal of psychiatric practice 10 (4): 239–248.  
  6. ^ Korshunov V A, A. N. Murashev, and M. N. Ivashev (August 2000). "Hemodynamic Effects of Tetrindol in Alert Normotensive Mice and Rats after Blockade of Nitric Oxide Synthesis". Bulletin of Experimental Biology and Medicine 130 (8): 777–779. 
  7. ^ Clary C (July 2004). "Results of a brief survey on the prescribing practices for monoamine oxidase inhibitor antidepressants". Journal of clinical psychiatry 51 (6): 239–248.  
  8. ^ "U.S. Anti-Depressant Market - Old Fashion Branding Could Save The Day". The Pharmaceutical Strategist: 6. June 2013.  
  9. ^ Fiedorwicz, Jess G. and Karen L. Swartz (June 1990). "The Role of Monoamine Oxidase Inhibitors in Current Psychiatric Practice". Journal of psychiatric practice 10 (4): 226–231.  
  10. ^ Grady, Meghan M.; Stahl, Stephen M. (2012). "Practical guide for prescribing MAOIs: debunking myths and removing barriers". CNS Spectrums 17: 17, pp 2–10.  


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