Phenelzine

Monoamine—Oxidase Inhibitors. In the mid-1950s, tuberculosis patients with depression being treated with iproniazid (42) were occasionally reported to become euphoric. This observation led to the discovery of irreversible monoamine—oxidase (MAO) inhibiting properties. Hydrazine and nonhydrazine-related MAO inhibitors were subsequentiy shown to be antidepressants (122). Three other clinically effective irreversible MAO inhibitors have been approved for treatment of major depression phenelzine (43), isocarboxazid (44), and tranylcypromine (45). 

In the discussion of benzylamines, we have met medicinal agents that owe their activity to some particular functionality almost without reference to the structure of the rest of the molecule. The hydrazine group is one such function in that it frequently confers monamine oxidase-inhibiting activity to molecules containing that group. Such agents frequently find use as antidepressants. Thus, reduction of the hydrazone of phenyl-acetaldehyde (84) affords the antidepressant phenelzine (85). Similar treatment of the derivative of phenylacetone (86) gives pheniprazine (87). ... 

Narcotan - Halothane Narco26p Flunitrazepam Nardeizine Phenelzine sulfate Nardil - Phenelzine sulfate Narest Valethamate bromide Narigix Nalidixic acid Narsis - Medazepam Nasafarma - Oxymetazoline HCI Nazalide Flunisolide Nasal Yer Naphazoline Nasin Tetrahydrozoline HCI Nasivin - Oxymetazoline HCI Nasky Inositol niacinate Nasmil - Cromolyn sodium Nasophen - Phenylephrine HCI Natacillin - Hetacillln potassium Natacyn - Natamycin Natam - Flurazepam... 

Acute treatment with nonselective MAO inhibitors (iproniazid, tranylcypromine, phenelzine), as a consequence of inhibiting both forms of the enzyme, increase, brain levels of all monoamines (phenylethylamine, tryptamine, methylhistamine aminergic neurotransmitters (dopamine, noradr enaline, adrenaline and serotonin). By contrast MAO-A inhibitors (clorgyline) increase serotonin and noradrenaline, while MAO-B inhibitors (selegiline, rasagiline) increase brain levels... 

Ms. Jefferson has been taking phenelzine for depression. She reports having a bad headache at the back of her head. Determine what assessment would be most important to make. Explain what action, if any, you would take. 

H4N2 302-01-2) see Acetazolaraide Allopurinol Brotizolam Carbidopa Cibenzoline Desmopressin Estazolam Etizolam Guanadrel Isoniazid Itraconazole Mitopodozide Niftiroxazide Nifurtimox Nitrofurantoin Phenelzine Primaquine Ziprasidone hydrochloride hydrazine-1,2-bis(thiocarbaxamide)... 

Amantidine, bromocriptine, mazindol, pergolide, cabergoline, L-dopa/carbidopa, pramipexole, ABT-431, catecholamine metabolism inhibitors (disulfiram, phenelzine, selegiline), amineptine Methylphenidate, /-amphetamine, tropanes, GBR-12909 (partial agonist that may also act as antagonist), modafinil, coca tea... 

With the exception of tranylcypromine (a phenylcycloalkylamine), the first MAOIs (e.g. iproniazid, isoniazid, phenelzine, isocarboxazid) were derivatives of hydrazine (originally used as a rocket fuel) (Fig. 20.2). All are irreversible inhibitors of the enzyme and restoration of MAO activity requires the synthesis of new enzyme. 

Isocarboxizid, phenelzine, selegiline, tranylcypromine, moclobemide, clorgiline, and linezolid... 

Monoamine oxidase inhibitors (phenelzine, tranylcypromine, possibly linezolicl)... 

MAOI Phenelzine 15 45-90 Antidepressant effects Dietary restrictions drug... 

The MAOI phenelzine and the RIMAs brofaramine and meclobemide are effective in SAD. Phenelzine is effective in 64% to 69% of SAD patients.58 It is generally reserved for treatment-refractory patients owing to dietary restrictions,... 

Two case reports describe symptoms such as insomnia, headache, tremulousness, irritability, and visual hallucinations when taking phenelzine concurrently with ginseng [43,44]. Reduction of the international normalized ratio (INR) may be observed when ginseng and warfarin are taken together [45]. 

Shader RI, Greenblatt DJ. Phenelzine and the dream machine ramblins and reflections. J Clin Psycho-pharmacol 5(2) 65, 1985. 

Jones BD, Runikis AM. Interaction of ginseng with phenelzine. J Clin Psychopharmacol 7(3) 201-202,1987. 

This belief was further supported by the evidence of a correlation between the clinical response and REM sleep suppression as well as a temporal relationship between the onset of clinical response and REM sleep suppression. However, some of the later studies suggested that REM sleep suppression is not necessary for the antidepressant action (Gillin 1983). For example, some studies show evidence of no change or even an increase in REM sleep with the treatment of depression (Gillin et al. 2001). Recently, Landolt Gillin (Landolt and Gillin 2002) have also demonstrated that the antidepressant response to phenelzine treatment does not depend on elimination of REM sleep or inhibition of slow wave activity in non-REM sleep. However, the generalization of some of these studies is limited because of their small sample size. 

Landolt H. P, Gillin J. C. (2002). Different effects of phenelzine treatment on EEG topography in waking and sleep in depressed patients. Neuropsychopharmacology 27, 462-9. 

During the past year, a 38-year-old female has become progressively depressed and now refuses to leave her house. Physical examination and blood chemistries are negative. She is given phenelzine, which diminishes her depression and enables her to leave her house. 

Tranylcypromine sulfate is an antidepressant drug and an inhibitor of MAO. Its antidepressant effect is probably due to the accumulation of NE in the brain as a consequence of inhibition of the enzyme. The other MAO I currently used as an antidepressant is phenelzine sulfate. 

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