Sertraline: a new antidepressant

Depression is at short intervals undertreated, This is unfortunate, since 70 to 80 percent of patients with this used by all debilitating illness respond to treatment.[1] Because depression is a biologically heterogeneous cluster of illnesses, rather than a single disease, patients correspond differently to different drugs.

Serotonin reuptake inhibitors of that kind as fluoxetine (Prozac) and sertraline (Zoloft) have become part of the medical armamentarium for the treatment of depression. They have joined other remedys that are used to treat depression, including monoamine oxidase inhibitors (MAOIs), lithium, methylphenidate (Ritalin), trazodone (Desyrel) bupropion (Wellbutrin) and the tricyclic antidepressants.

After fluoxetine, tricyclic agents are the principally commonly prescribed antidepressants, and they are the standard against which fresh drugs are measured. When the highest acceptable dose of the initial put drugs into is not effective or when that medicine produces intolerable side effects, it is frequently possible to achieve a satisfactory rejoinder by trying a different medicine or a combination of medicines In this situation, sertraline may be the medicine of choice.

Mechanism of Action

The mechanism of action of all antidepressants is unknown. In depression, the principal biochemical abnormality appears to be impaired metabolism of united or more central amines or peptide neurotransmitters and their receptor sites.

Sertraline inhibits the reuptake of serotonin and, thus, increases the concentration of this neurotransmitter in the central nervous hypothesis In contrast, tricyclic antidepressants and MAOIs not solely increase the concentration of serotonin in the central nervous classification but they also increase the of the same heights of norepinephrine and dopamine.

Pharmacokinetics

Sertraline is more than 97 percent leap to serum protein in rats and dogs.[2,3] Little information is available forward the distribution of this remedy in humans.

Based in succession the data from animal studies,[2,3] it appears that sertraline undergoe extensive first-pass metabolism in the liver, resulting in a frequently less potent desmethyl metabolite. No information has been published in succession the route of excretion of sertraline and its metabolites, beyond the fact that in animal studies no unchanged put drugs into has been found in the bile or urine.

life-blood levels of sertraline peak five to eight hours after an oral dose. The half-life of this mix with drugs is approximately 24 hours. With continued daily dosing, the steady state concentration is reached in the same week. In comparison, the steady-state concentration of fluoxetine is not achieved until the physic has been taken daily for three weeks.

Dosage

Sertraline is available in 50- and 100-mg scored tablets, and the starting dosage is 25 to 50 mg by day. As necessary, the dosage can be increased, up to a maximum of 200 mg by day. However, the daily dose should not be increased more than one time a week. The wholesale outlays of sertraline and other antidepressants are fisted in Table 1 [TABULAR DATA 1 OMITTED]

Clinical Use

DEPRESSION

In the two double-blind and placebo-controlled studies,[1,4] sertraline was institute to be as effective as amitriptyline in the treatment of depression. one as well as the other the amitriptyline group and the sertraline assemblage had an equal number of patients who withdrew because of intolerable side drifts However, among those who continued in the thought the amitriptyline group had a significantly greater incidence of side effects

In separate studies,[4,5] sertraline was well tolerated and was effective in somewhat old patients with depression. When the remedy was given to a healthy arrange of elderly volunteers for nine days, it was place to have no effect onward psychomotor performance.[6] In another study[7] sertraline was ground to have no electrocardiographic drifts Because of its low side-effect profile, sertraline may be the best choice in pitch uponed elderly patients.

Sertraline has not been exhibitioned in pregnant women, nursing mothers or children; therefore, its use is not advised in these populations. Since there have been no published studies forward sertraline therapy in patients with renal or hepatic disease, the mix with drugs should be used cautiously in these disposes and patients should be closely monitored.

Seizures can come into view in patients who are being treated with tricyclic antidepressants or MAOIs. There have been no reports of seizures associated with the administration of sertraline; however, patients with known seizure disorders were exclud from the clinical trials.

According to information from the manufacturer, sertraline has been shown to interact with mix with drugss such as digoxin (Lanoxin) and warfarin (Coumadin, Panwarfin). These remedys are highly bound to protein, and coadministration with sertraline increases their general intent Similar effects can be reckon uponed when sertraline is administered with any unsalable article that binds extensively to protein. reciprocally highly protein-bound drugs can increase the consequences and side effects of sertraline. Sertraline also decreases the clearance of tolbutamide (Orinase) and diazepam (Valium).