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Imipramine derivatives

This compound is an imipramine derivative with substitution of the amino groups on the side chain. It was compared to imipramine in a double-blind controlled study (74 ) and found to be of comparable clinical activity. Side effects are also similar with a tendency for lofepramine to show more hand tremor. Significant changes were also noted in increased bilirubin and decreased blood urea that were unexplained and unaccompanied by any clinical effects. [Pg.12]

Tricyclic Antidepressants. Imipramine [50-49-7] (32), which was the first tricycHc antidepressant to be developed, is one of many useful psychoactive compounds derived from systematic molecular modifications of the antihistamine prometha2ine [60-87-7] (see Histamine and histamine antagonists). The sulfur atom of prometha2ine was replaced with an ethylene bridge and the dimethylamino group attached to an / -propyl group, rather than to an isopropyl one, of the side chain. The actual synthesis of (32) is typical of the compounds in this class (37). [Pg.466]

Research for an antidepressant among non-tricyclic compounds with pharmacological effects qualitatively different from those of the conventional tricyclic compounds led to the preparation and testing of a series of indazole derivatives for reserpine-like activity in mice. l-[3-(Dimethylamino)propyl]-5-methyl-3-phenyl-l//-indazole (FS-32 692) antagonizes reserpine-induced effects and potentiates amphetamine-induced self-stimulation and l-Dopa-induced increase in motor activity. FS-32 produces an anticholinergic action mainly on the central nervous System, while the action of imipramine occurs centrally as well as peripherally (79AF511). [Pg.293]

Imipramine and its derivatives produce blue, phenothiazines blue, violet, red or orange to skin-colored chromatogram zones, that fade relatively quickly, on a colorless background (Fig. 1). [Pg.184]

Fig 1 Chromatogram of imipramine and phenothiazine derivatives after staining with Forrest reagent [4] 1 = imipramine, 2 = desipramine, 3 = clomipramine, 4 = lofepramine, 5 = trimipramine, 6 = thioridazine, 7 = chlorphenethazine, 8 = periciazine, 9 = promazine, 10 = promethazine. [Pg.184]

The detection limits of imipramine and its derivatives were 100 ng substance per chromatogram zone. [Pg.185]

The tricyclic antidepressants (TCAs) derive their name from their three-ringed molecular structure (Fig. 20.3) and emerged, in 1958, from a search for better neuroleptics than chlopromazine among the phenothiazines. The prototype, imipramine, turned out to be ineffective in treating the positive symptoms experienced by schizophrenics but it did relieve their depression (negative symptoms). In fact, imipramine is still the standard agent against which novel antidepressants are compared in clinical trials. [Pg.436]

All TCAs are either secondary- or tertiary-amines of a dibenzazepine nucleus (Fig. 20.3), and they all inhibit neuronal reuptake of noradrenaline and/or 5-HT but are much less potent as dopamine reuptake blockers. A common claim is that secondary amines (e.g. desipramine) are preferential inhibitors of noradrenaline uptake whereas the tertiary derivatives (e.g. imipramine, doxepin and amitryptyline) preferentially inhibit 5-HT uptake. However, when Richelson and Pfenning (1984) actually compared the effects of a wide range of antidepressants on the synaptosomal uptake of [ H]monoamines in vitro, and compared their A s, instead of merely ranking /C50S collected from different studies, they found that tertiary- and secondary-substituted compounds were equi-potent inhibitors of [ H]noradrenaline uptake. Moreover, all the TCAs turned out to be more potent inhibitors of [ H]noradrenaline than of [ H]5-HT uptake. Tertiary amines are even less convincing inhibitors of 5-HT reuptake in vivo, because any such action is diminished by their metabolism to secondary amines (e.g. imipramine to desipramine amitriptyline to nortriptyline). Only clomipramine retains any appreciable 5-HT uptake blocking activity in vivo with (an unimpressive) five-fold selectivity for 5-HT versus noradrenaline. [Pg.436]

Some phenothiazine derivatives (tranquilizers) can be hallucinogenic at high doses (e.g., imipramine (Tofranil) at oral dose of about 1 g and Ethopropazine (Parsidol) at 100 mg). [Pg.180]

Drugs that may be affected by fosamprenavir include the following Amiodarone, amitriptyline, benzodiazepines, calcium channel blockers, cisapride, contraceptives (oral), cyclosporine, ergot derivatives, HMG-CoA reductase inhibitors, imipramine, itraconazole, ketoconazole, lidocaine (systemic), methadone, pimozide, quinidine, rifabutin, sildenafil, tacrolimus, vardenafil, warfarin. [Pg.1907]

The serotonergic hypothesis of OCD was initially derived from clinical observations that pointed to the preferential response of patients with OCD to medications possessing a serotonergic profile. CMl and other SRls have been demonstrated to be superior not only to placebo in OCD, but also to other antidepressants, such as the noradrenergic tricyclic antidepressant desipramine [W. K. Goodman et al. 1990b H. L. Leonard et al. 1991 Zohar and Insel 1987] as well as nortriptyline, amitriptyline, and imipramine, with much of the same results [Ananth et al. 1981 Volavka et al. 1985). [Pg.473]

Montgomery SA, Brown RE, Clark M Economic analysis of treating depression with nefazodone v. imipramine. Br J Psychiatry 168 768-771, 1996 Monti JM Effect of a reversible monoamine oxidase-A inhibitor (moclobemide) on sleep of depressed patients. Br J Psychiatry Suppl 155 61-65, 1989 Monti JM, Alterwain P, Monti D The effects of moclobemide on nocturnal sleep of depressed patients. J Affect Disord 20 201-208, 1990 Montkowski A, Holsboer F Absence of cognitive and memory deficits in transgenic mice with heterozygous disrupt of the brain-derived neurotrophic factor gene. J Psychiatr Res [in press)... [Pg.702]

The dibenzapine derivatives are called tricyclic antidepressants and include imipramine (Tofranil), desipramine (Norpramin), amitriptyline (Elavil), nortriptyline (Aventyl), protriptyline (Vivactil), and doxepin (Adapin). [Pg.419]

Similar to the phenothiazine derivatives (e.g., chlorpromazine), tricyclic antidepressants (e.g., imipramine) may ... [Pg.419]

Tricyclic antidepressants, like some of the phenothiazine derivatives, are sedative in nature. Those compounds containing a tertiary amine (imipramine, amitriptyline, and doxepin) are the most sedative. Those compounds containing a secondary amine (nortriptyline and desipramine) are less so, and protriptyline has no sedative effect. [Pg.420]

Garattini, S., Giachetti, A., Jori, A., Pieri, L., Valzelli, L. 1962, Effect of imipramine, amitriptyline and their monomethyl derivatives on reserpine activity, J.Pharm.Pharmacol., vol. 14, pp. 509-514. [Pg.240]

Removal of norepinephrine Norepinephrine may (1) diffuse out of the synaptic space and enter the general circulation, (2) be metabolized to O-methylated derivatives by post-synaptic cell membrane-associated catechol O-methyltransferase (COMT) in the synaptic space, or (3) be recaptured by an uptake system that pulls the norepinephrine back into the neuron. The uptake by the neuronal membrane involves a sodium-potassium activated ATPase that can be inhibited by tricyclic antidepressants such as imipramine (see p. 119), or by cocaine (see Figure 6.3). [Pg.67]

Dimetacrine is a 6,6,6 tricyclic acridine derivative. In a double-blind study, dimetacrine was less effective than imipramine and produced more weight loss and abnormal liver function tests more often (1). [Pg.33]


See other pages where Imipramine derivatives is mentioned: [Pg.184]    [Pg.425]    [Pg.184]    [Pg.425]    [Pg.269]    [Pg.401]    [Pg.4]    [Pg.70]    [Pg.171]    [Pg.172]    [Pg.413]    [Pg.906]    [Pg.487]    [Pg.204]    [Pg.205]    [Pg.232]    [Pg.420]    [Pg.452]    [Pg.542]    [Pg.525]    [Pg.546]    [Pg.176]    [Pg.169]    [Pg.546]    [Pg.229]    [Pg.130]    [Pg.294]   
See also in sourсe #XX -- [ Pg.352 , Pg.353 ]

See also in sourсe #XX -- [ Pg.352 , Pg.353 ]




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Imipramin

Imipramine

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