Drugs amitriptyline

Fig. 6.9. Electrochromatogram of two antidepressant drugs (amitriptyline 1, nortriptyline 2) and a related quaternary ammonium compound (methyl amitriptyline 3) obtained by isocratic elution in 30.6 cm long channel. Conditions mobile phase, 5 mmol/L sodium phosphate, pH 2.5, containing 70% acetonitrile (v/v) flow rate of the mobile phase through the inlet reservoir, 50 pL/min applied voltage, 12 kV (400 V/cm) electrokinetic injection, 1 kV, 5 s UV detection at 239 nm sample concentration, 0.10-0.15 mg/mL. (Reprinted with permission from [33]. Copyright 2000 American Chemical Society).

The majority of all deaths from antidepressant poisoning in Scotland, England, and Wales, during 1975-1984 and 1985-1989 were due to two tricyclic drugs, amitriptyline and dosulepin, and they, as well as the entire group of older tricyclic antidepressants, had a fatality index (deaths per million prescriptions) significantly higher than the mean (150). 

Antidepressant drugs Amitriptyline, nortriptyline, doxepin, imipramine Also, fluoxetine and other selective serotonin reuptake inhibitors... 

Tricyclic drugs Amitriptyline, imipramine Desipramine, nortriptyline Clomipramine, dox-epin, protriptyline... 

Psychotropic drugs Amitriptyline, chlorpromazine, desipramine, doxepin, ffuphenazine, haloperidol, imipramine... 

An isolated report describes a woman who developed marked and acute hypotension and weakness when desipramine, fluoxetine and venlafaxine were replaced by nefazodone. Isolated cases describe the serotonin syndrome in patients given nefazodone together, or sequentially, with another serotonei c drug (amitriptyline, paroxetine, St John s wort, or trazodone). The manufacturer recommended that nefazodone should not be used with an MAOI or within 14 days of discontinuing an MAOL Note that, due to adverse hepatic effects nefazodone was widely withdrawn from the market. 

The depressive phase of this psychosis was first brought under control by Kuhn (1958) who found that the tricyclic compound, imipramine (12.114) restored a normal mood to severely depressed mental patients. Since then, it and the related drug, amitriptyline (12.115) have become the standard treatment for this condition. Results are obtained only after 1 or 2 weeks administration, and treatment usually continues for 6 months. High doses must be avoided in patients with heart disability which these drugs can accentuate. 

Psychoactive drugs Amitriptyline Nortriptyline Desipramine Imipramine... 

The TCAs, such as amitriptyline (Elavil) and dox-epin (Sinequan), inhibit reuptake of norepinephrine or serotonin at the presynaptic neuron. Drug classified as MAOIs inhibit the activity of monoamine oxidase a complex enzyme system that is responsible for breaking down amines. This results in an increase in endogenous epinephrine, norepinephrine and serotonin in the nervous system. An increase in these neurohormones results in stimulation of the CNS. The action of the SSRIs is linked to their inhibition of CNS neuronal uptake of serotonin (a CNS neurotransmitter). The increase in serotonin levels is thought to act as a stimulant to reverse depression. 

Isolation and purification of amitriptyline, nortriptyline, and 10-hydroxy (lO-OH) derivatives of the drugs from rat bile... 

Compared to antipsychotics, there are even fewer studies on the prescribing patterns of antidepressants done in Asian countries. Pi etal. (1985) conducted a survey of psychotropic prescribing practices reported by psychiatrists in 29 medical schools in 9 Asian countries. Daily dose range of tricyclic antidepressants (TCAs) such as amitriptyline, imipramine, and nortriptyline in Asian countries was comparable to the practice in USA. This is despite differences found between Asian and non-Asian populations in the pharmacokinetics of TCAs (Pi et al, 1993). A questionnaire on the practical prescribing approaches in mood disorders administered to 298 Japanese psychiatrists was reported by Oshima et al. (1999). As first-line treatment, the majority of respondents chose newer TCAs or non-TCAs for moderate depression and older TCAs for severe depression. Combination of antidepressants and anxiolytics was preferred in moderate depression, while an antidepressant and antipsychotic combination was common in severe psychotic depression. Surprisingly, sulpiride was the most favored drug for dysthymia. In a naturalistic, prospective follow-up of 95 patients with major depression in Japan, the proportion of patients receiving 125 mg/day or less of imipramine was 69% at one month and 67% at six months (Furukawa et al., 2000). 

Until the introduction of selective serotonin reuptake inhibitors (SSRIs) in the 1980s, tricyclic antidepressants were the most widely used drugs. The therapeutic effect of amitriptyline and imipramine are related to their ability to inhibit the presynaptic reuptake of both NA and 5-HT. They are referred to as non-selective reuptake inhibitors, whereas many of the other tricyclics are more selective thus, clomipramine is a selective reuptake inhibitor for 5-HT and desipramine and nortriptyline are selective... 

Drug therapies include tricyclic antidepressants and SSRIs. Treatment should be continued for at least 29 weeks. Nortriptyline, amitriptyline, clomipramine, desipramine, fluvoxamine, and bupropion have been used successfully. 

Amitriptyline and imipramine, and the MAOI phenelzine, can be considered second- or third-line drugs for PTSD after SSRIs have failed. Mirtaza-pine and venlafaxine may also be effective. 

There are a few medicinals that cause increased bilirubin levels which ultimately enhances AP-levels unless and until a corrective measure is taken in the respective procedure one may be left with false AP-level enhancement. Some typical examples are, namely amitriptyline, chloropropamide, erythromycin, phenylbutazone, sulpha-drugs and tetracyclines. 

Additional ADRs linked to diet pills include psychosis myocardial ischemia drug interactions, such as the interaction of fenfluramine with imipramine, fenfluramine with amitriptyline or desipramine, or the toxic reaction between fluoxetine and phentermine and the release of serotonin while inhibiting its reuptake, contributing to hyperserotonin reactions. When the next craze takes hold of patients and their physicians, hopefully physicians and pharmacists will take a more vocal position and recommend restraint, xmtil some proof of efficacy and lack of toxicity is shown for new faddish off-label combinations. 

Tricyclic drugs have, as the name implies, a three-ring structure, and interfere with reuptake of norepinephrine and/or serotonin into axon terminals. Tricyclic drugs include imipramine (Tofranil), amitriptyline (Elavil), clomipramine (Anafranil), and nortriptyline (Pamelor, Aventil). Tricyclics have the occasional but unfortunate cardiovascular side effects of arrhythmia and postural hypotension. Newer, nontricyclic antidepressants have been developed that are collectively referred to as SSRIs. These have a potent and selective action on serotonin, and lack the cardiovascular side effects of the tricyclics. These include fluoxetine (Prozac), paroxetine (Paxil), sertraline (Zoloft), and fluvoxamine (Luvox). A fifth SSRI, citalopram (Celexa) has been used in Europe and has recently been approved in the United States. Venlafaxine (Effexor) blocks reuptake of norepinephrine and serotonin, while bupropion (Wellbutrin) acts on both dopamine and norepinephrine. 

Certain prototypic drug substrates have been used to characterize enzyme activity in the human brain tissue. Amitriptyline, for example, was shown to be demethylated to nortriptyline by both rat and human... 

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