Amoxapine antidepressant

In addition, there are several drugs that are related to the antipsychotics that may also be prescribed to youths for other conditions. These include the antidepressant amoxapine and the preanesthetic droperidol. Metoclopramide and prochlorperazine are related agents that are marketed for their effects on the gastrointestinal system. 

To date, only one antidepressant, amoxapine, has proven effective in the treatment of PMD as the sole therapy. Amoxapine is a chemical congener of the antipsychotic drug loxapine, so it possesses both dopamine-blocking and monoamine-enhancing properties. One double-blind study has confirmed that amoxapine appears to be as effective as the combination of a TCA and an antipsychotic. R. F. Anton and Burch [1990] randomly selected 46 inpatients with psychotic depression to either amoxapine [to 400 mg/day] or ami-... 

The actions of amoxapine and maprotiline resemble those of TCAs such as desipramine. Both are potent NET inhibitors and less potent SERT inhibitors. In addition, both possess anticholinergic properties. Unlike the TCAs or other antidepressants, amoxapine is a moderate inhibitor of the postsynaptic D2 receptor. As such, amoxapine possesses some antipsychotic properties. 

More than a dozen drugs, almost all of them in use for many years, can be classified as neuroleptics. The phenothiazine derivatives were originally the most commonly used class of neuroleptic drugs. Chlorproma-zine is the prototype, developed in France and introduced into North America in 1953 by Heinz Lehmann. Its brand name in Canada and England is Largactil, and in the United tates, Thorazine. The antidepressant amoxapine (Asendin) is metabolized into a neuroleptic and has similar effects and, more important, adverse effects, such as tardive dyskinesia. All the classic neuroleptics block dopamine, but all of them also affect other neurotransmitter systems. 

Most of the older antidepressants are called tricyclic because their chemical nucleus has the basic tricyclic structure of the original pheno-thiazine neuroleptic, chlorpromazine, or Thorazine (Bassuk et ah, 1977 Pauker, 1981). Of extreme importance, the antidepressant amoxapine (Asendin) is turned into a neuroleptic in the body, producing the same problems as any other neuroleptic, including tardive dyskinesia (chapters 3 and 4). 

Damluji and Ferguson (1988) reviewed paradoxical worsening of depressive symptomatology caused by antidepressants in an article of the same title and reported four cases of their own caused by the older antidepressants amoxapine, desipramine, nortriptyline, and trazodone. The APA National Task Force on Women and Depression (1990) report on benzodiazepines also cited the problem of depression and suicide from tricyclic antidepressants. 

One active metabolite is an antidepressant (amoxapine, also known as N-desmethyl-loxapine)... 

ACETOPHENAZINE, see Phenothiazines, piperazine ALPRAZOLAM, see Benzodiazepines AMITRIPTYLINE, see Tricyclic antidepressants AMOXAPINE, see Tricyclic antidepressants BENZODIAZEPINES (alprazolam, chlordiazepoxide, clorazepate, diazepam, halazepam, lorazepam, oxazepam, prazepam, temazepam)... 

The dibenzo-oxazepine loxapine is another antipsychotic in this structural class that has a more typical neuroleptic biochemical profile with mainly antidopaminergic activity at D2-type receptors. Loxapine undergoes Phase I aromatic hydroxylation to yield several phenolic metabolites that have higher affinity for D2 receptors than the parent. Loxapine also undergoes N-demethylation to form amoxapine, which is used clinically as an antidepressant. Amoxapine binds to D2 receptors and inhibits the norepinephrine neurotransporter to block neuronal norepinephrine reuptake, a correlate of antidepressant activity. 

Doxepin [1668-19-5] (38), unlike other commercially available tricyclics, has an oxygen atom in the bridge between the two aromatic rings. It is marketed as a cis—trans mixture (1 5) of isomers, both of which are active. This close relative of amitriptyline (33) has both sedative and anxiolytic properties associated with its antidepressant profile. Maprotiline [10262-69-8] (39) and amoxapine [14028-44-5] (40) are pharmacologically, although not chemically, similar to the tricycHc secondary amines. Clomipramine [303-49-1] (41) has similar pharmacological and antidepressant efficacy. However, clomipramine is approved by the U.S. FDA only for the treatment of obsessive—compulsive disorder. Representative brands of tricycHc antidepressants marketed in the United States are Hsted in Table 2. 

The answer is c. (Hardman, p 436.) The tricyclics and second-generation antidepressants act by blocking serotonin or norepinephrine uptake into the presynaptic terminal. Fluoxetine selectively inhibits serotonin uptake with minimal effects on norepinephrine uptake. Protriptyline, maprotiline, desipramine, and amoxapine have greater effect on norepinephrine uptake... 

The answer is b. (Katzung, pp 504-505.) Amoxapine is a heterocyclic antidepressant that has effects on norepinephrine and serotonin uptake. It is useful in psychotic patients who are depressed. The dopaminergic antagonism caused by amoxapine may lead to the amenorrhea-galactorrhea syndrome. 

Solid phase extraction (SPE) has been used to efficiently extract several types of antidepressants, which can then be conveniently analyzed on GC-NPD. One assay extracted and analyzed viloxazine, venlafaxine, imipramine, desipramine, sertraline, and amoxapine from whole blood in one procedure (Martinez et al., 2002). The same laboratory analyzed fluoxetine, amitriptyline, nortriptyline, trimipramine, maprotiUne, clomipramine, and trazodone in whole blood in one assay (Martinez et al., 2003). SPE has also been used for the simultaneous analysis of TCAs and their metabolites by de la Torre et al. (1998). 

Loxapine (Loxitane). Loxapine is a medium potency antipsychotic, and it has several interesting features. First, it is chemically very similar to clozapine, the first of the atypical antipsychotics. In the test tube, loxapine actually behaves more like an atypical antipsychotic (more on that later), but when patients are treated with it, loxapine acts more like a traditional typical antipsychotic. A second point of interest is that loxapine is actually the major active metabolite of the antidepressant amoxa-pine (Ascendin). As a result, one can use a single medication (amoxapine) to treat both depression and psychosis. In practice, however, the use of what is essentially a fixed dose combination medication should be avoided. Using amoxapine does not allow separate adjustment of the antipsychotic and antidepressant, and most importantly, amoxapine is the only antidepressant associated with the risk of TD. 

Amlodipine (Norvasc) Calcium-blocker Amoxapine (Asendin) Antidepressant Amoxicillin (Amoxil) Antibiotic... 

There are four classes of antidepressants tricyclic antidepressants (imipramine, trimipramine, amitriptyline, doxepin, desipramine, protriptyline, nortriptyline, amoxapine, maprotiline) monoaminooxidase (MAO) inhibitors (phenelzine, isocarboxazid, tranylcypromine) second-generation antidepressants or atypical antidepressants, which are a chemically dissimilar group of recently proposed drugs (bupropion, trazodone, fluoxetine) and amphetamines and other stimulators of the CNS (dextroamphetamine, methylphenidate). 

The antidepressant action of amoxapine is comparable to that of imipramine and amitriptyline. It exhibits antagonistic activity on dopamine (D2) receptors. Amoxapine is intended more for relieving symptoms in patients with neurotic or situational depression. It has a number of serious side effects. Synonyms of this drug are asendin, amoxan, moxadil, and others. 

Bupropion is an a-aminoketone that is structurally related to amphetamines, and it exhibits unique activity comparable to that of other antidepressants. It is believed that bupropion restores the total amount of norepinephrine in the body. This compound is a poor reuptake inhibitor of dopamine, and does not exhibit anticholinergic activity or inhibit MAO. Its efficacy as an antidepressant is comparable to that of tricyclic antidepressants, and as a serotonin uptake inhibitor it is comparable to fluoxetine. It is preferable to use amoxapine. Synonyms of bupropion are amphebutamon and wellbutrin. 

Maprotiline and amoxapine are selective norepinephrine uptake inhibitors. They share most of the properties of the tricyclic antidepressants. Maprotiline has less sedating effect than mianserin and it is more epileptogenic than any other antidepressant. It shows considerable cardiotoxicity when taken in overdose. 

Maprotiline (Ludiomil) and amoxapine (Asendin) are heterocyclic antidepressant agents that are not members of the tricyclic family. However, their pharmacology is so similar to that of the tricyclic amines that they are included for discussion purposes with this class of agents. Desipramine and nortriptyline are major metabolites of imipramine and amitriptyline, respectively. 

Mechanism of Action A tricyclic antidepressant that blocks the reuptake of neu-rotransmitfers, such as norepinephrine and serotonin, at CNS presynaptic membranes, increasing their availability at postsynaptic receptor sites. The metabolite, 7-OH-amoxapine has significant dopamine receptor blocking activity similarto halo-peridol. Therapeutic Effect Produces antidepressant effects. 

Most child and adolescent studies published thus far have focused on the effects of the tricyclic antidepressants (TCAs) and, more recently, the SSRIs. A few open studies have also shown that monoamine oxidase inhibitors (MAOIs) can be used safely with children and adolescents (Ryan et ah, 1988b), but noncompliance with dietary requirements may present a significant problem for minors. Other antidepressants, including the heterocyclics (HTC) (e.g., amoxapine, maprotiline), buproprion, venlafaxine, and nefazodone, have been found to be efficacious for the treatment of depressed adults (APA, 2000), but they have not been well studied for the treatment of MDD in children and adolescents. Therefore, this chapter mainly describes the use of SSRIs and TCAs for youth with MDD. 

Sovner et al. (1998) have done an excellent job summarizing the data on antidepressants in patients with developmental disabilities. There have been nine reports of antidepressant use in adults with depression and MR and three reports of antidepressant use in children and adolescents. Eight of nine reports in adults were positive. The drugs studied included nialimide (n = 27), fluoxetine (9), imipramine (6), amoxapine (2), and nortriptyline (1) (total n = 45). In addition, Sovner et al. identified four reports of antidepressant use in children. One involved successful treatment with fluoxetine in an adolescent, another indicated efficacy with imipramine and amitriptyline in 9 of 12 children (Do-sen, 1982), and a third showed successful management in 3 of 4 children treated with imipramine or tryptophan plus nicotinamide (Dosen, 1990). One study of fluoxetine in depressed children with autism and MR witnessed improvement in depression but not in compulsive symptoms (Ghaziuddin and Tsai, 1991). 

The TCAs do not appear to be effective single agents in the treatment of PMD as they are in NPMD. This discrepancy may be as much a function of PMD tending to be more severe than the depression in the NPMD population. Antidepressants other than the TCAs have not been extensively tested in the monotherapy of PMD. Amoxapine is the single antidepressant that does appear effective as a sole therapy for PMD. 

To date, only one study has been completed with an antidepressant other than a TCA combined with an antipsychotic in the treatment of PMD. Rothschild and colleagues (1993) investigated the efficacy of fluoxetine and perphenazine in the treatment of PMD and found that approximately 73% of 30 patients who met DSM-III-R (American Psychiatric Association 1987) criteria for major depression with psychotic features had at least a 50% reduction on their Hamilton Rating Scale for Depression scores over 5 weeks. Furthermore, the combination of fluoxetine and perphenazine appeared to be better tolerated than the combination of TCAs with antipsychotics. Although there is no evidence that monotherapy with an antidepressant other than amoxapine is efficacious, the combination therapy with many antidepressants other than the TCAs may prove useful. 

Some patients will decline ECT, and the available data suggest that combination antidepressant/antipsychotic treatment or amoxapine may be equally effective. Given the preponderance of data supporting TCA/antipsychotic combinations in the treatment of PMD, it may be reasonable to consider TCA combinations before other antidepressant combinations. Currently, the literature shows debates as to whether the SSRIs are as efficacious as the... 

Some clinicians adhere to the maxim never use two drugs when one will suffice and will prefer amoxapine. This is a reasonable strategy. However, amoxapine may be difficult for many patients to tolerate, and using a combination of two drugs may afford the clinician a finer ability to determine the amount of antipsychotic to the doses of the antidepressant and the antipsychotic for maximum efficacy and minimum toxicity. 

HCA is the term is used to refer to both TCAs and analogues of these agents, such as maprotiline and amoxapine. TCAs are by far the most commonly used HCAs and include tertiary amines such as amitriptyline, doxepin, and imipramine and secondary amines such as desipramine and nortriptyline. Most secondary amines could also be viewed as NE-selective antidepressants, while the hallmark of tertiary amine TCAs is their effects on multiple neurotransmitters over their clinically relevant dosing range. 

Two studies found maprotiline to be clearly superior to placebo and two other studies found trends in the same direction ( p < 0.001, combined data) (Table 7-5) (105, 106, 107 and 108). More than 1,600 patients were randomly assigned to either maprotiline or a standard HCA 660 on maprotiline did well, and 247 showed minimal improvement, no change, or worsened. For the HCAs (usually imipramine or amitriptyline), 640 patients did well, and 255 showed minimal improvement, no change, or worsened. In summary, 73% did well with maprotiline, and 72% did well with a standard antidepressant. Combining these data with the Mantel-Haenszel test indicated no difference in efficacy (Table 7-6). Maprotiline has a dose-dependent risk of seizures. As with TCAs and amoxapine, overdoses of maprotiline can be lethal. %... 

Patients suffering from a psychotic depression usually do not benefit from antidepressant monotherapy and usually require the combination of an antidepressant and antipsychotic or EOT. There is limited evidence that amoxapine, whose primary active metabolite (8-hydroxyamoxapine) has antipsychotic-like properties, can be used as monodrug therapy (385). 

A number of antidepressants do not fit neatly into the other classes. Among these are bupropion,mirtazapine, amoxapine, and maprotiline (Figure 30-5). Bupropion has a unicyclic aminoketone structure. Its unique structure results in a different side-effect profile than most antidepressants (described below). Bupropion somewhat resembles amphetamine in chemical structure and like the stimulant, has central nervous system (CNS) activating properties. 

D6 Tricyclic antidepressants (TCAs), benztropine, perphenazine, clozapine, haloperidol, codeine/oxycodone, risperidone, class Ic antiarrhythmics, 3 blockers, trazodone, paroxetine, maprotiline, amoxapine, duloxetine, mirtazapine (partly), venlafaxine, bupropion Fluoxetine, paroxetine, duloxetine, hydroxybupropion, methadone, cimetidine, haloperidol, quinidine, ritonavir Phenobarbital, rifampin... 

Several antidepressants share the ability to block serotonin 2A receptors as well as serotonin reuptake. In fact, some of the tricyclic antidepressants, such as amitriptyline, nortriptyline, doxepine, and especially amoxapine, have this combination of actions at the serotonin synapse. Since the potency of blockade of serotonin 2A receptors varies considerably among the tricyclics, it is not clear how important this action is to the therapeutic actions of tricyclic antidepressants in general. 

Prolactin concentrations are very rarely altered during treatment with tricyclic antidepressants, but this is more likely to occur and to produce galactorrhea or amenorrhea with clomipramine and amoxapine and when there are other contributory factors that may stimulate prolactin secretion, such as stress or electroconvulsive therapy (1139). 

Adam see Ecstasy Adderall see Amphetamines Adipex-P see Diet pills Aerosol propellants see Inhalants African black see Marijuana African salad see Catha etlulis African tea see Catha etlulis Afterburner bromo see 2C-B Ah-pen-yen see Opium Air blast see Inhalants Alfenta see Fentanyl Allium sativum see Herbal drugs Alprazolam see Benzodiazepine Alurate see Barbiturates Amber see Herbal drugs Ambien see Tranquilizers American ephedra see Ephedra Amiloride see Diuretics Amitriptyline see Antidepressants Amobarbital see Barbiturates Amoeba see PCP (phencyclidine) Amoxapine see Antidepressants AMT see Dimethyltryptamine (DMT) Amy see Amyl nitrite Amyl nitrate see Amyl nitrite... 

Amoxapine is a metabolite of the antipsychotic drug loxapine and retains some of its antipsychotic action and dopamine receptor antagonism. A combination of antidepressant and antipsychotic actions might make it a suitable drug for depression in psychotic patients. However, the dopamine antagonism may cause akathisia, parkinsonism, amenorrhea-galactorrhea syndrome, and perhaps tardive dyskinesia. 

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