MXPA00010343A - Treatment of generalized anxiety disorder with paroxetine - Google Patents

Abstract

A method of treatment of generalised anxiety disorder, which method comprises administering an effective, non-toxic amount of paroxetine or a pharmaceutically acceptable salt or solvate thereof, to a human or non-human animal in need thereof.

Description

TREATMENT OF GENERALIZED ANXIETY DISORDER WITH PARQXETINE DESCRIPTIVE MEMORY This invention relates to a method for treating generalized anxiety disorder and, above all, to the use of paroxetine in said treatment. Pharmaceutical products with antidepressant and anti-Parkinson properties are described in US-A-3912743 and US-A-4007196. An especially important compound among those described is paroxetine, the (-) trans isomer of 4- (4'-fluorophenyl) -3- (3 ', 4'-methylenedioxy-phenoxymethyl) -piperidine (see example 2 of US-A-4007196). The paroxetine hydrochloride salt is approved for human use in therapy to treat, among other conditions, depression, obsessive-compulsive disorder (OCD) and panic. In commercial use, paroxetine hydrochloride is provided as a crystalline hemihydrate (see European patent EP-A-0223403 of Beecham Group). Various forms of crystalline anhydrate are also known (see WO096 / 24595 from SmithKIine Beecham foot). Surprisingly, it has been discovered that paroxetine has a potential therapeutic utility as a medicament for the treatment of generalized anxiety disorder.

Accordingly, this invention provides a method for treating generalized anxiety disorder, which consists of administering an effective and non-toxic amount of paroxetine, or a pharmaceutically acceptable salt or solvate thereof, to a human or animal. I need it. This invention also provides the use of paroxetine or a pharmaceutically acceptable salt or solvate thereof in the manufacture of a medicament for use in the treatment of generalized anxiety disorder. A pharmaceutically acceptable paroxetine preferred salt is crystalline hydrochloride. Appropriate procedures for preparing paroxetine hydrochloride include those mentioned in the patents of U.S.A. 4009196, 4721723, 4902801, 4861893 and 5039803 and in PCT / GB93 / 00721. Especially preferred is the hemihydrate, prepared as set forth in European patent EP-A-0223403. A medicament, for use in the treatment of generalized anxiety disorder, may be prepared by mixing paroxetine or a pharmaceutically acceptable salt or solvate thereof with an appropriate vehicle, which may contain a diluent, binder, filler, disintegrant, agent flavoring agent, coloring agent, lubricant or preservative of common form. Preferably, the medicament is in the form of a unit dose and in a form adapted for use in the medical field or vet. For example, such preparations may be in package form accompanied by printed or written instructions for use as a generalized anxiety disorder treatment. The appropriate dose scale for paroxetine, or a pharmaceutically acceptable salt or solvate, depends on the severity of the generalized anxiety disorder and the condition of the patient. It also depends, among other things, on the efficiency ratio to be absorbed and on the frequency and route of administration. Paroxetine, or a pharmaceutically acceptable salt or solvate thereof, can be formulated for administration by any route, and examples of administration are oral, sublingual, rectal, topical, parenteral, intravenous or intramuscular. If desired, the preparations can be designed to give a slow release of paroxetine or a pharmaceutically acceptable salt or solvate thereof. The medicaments can be presented, for example, in the form of tablets, capsules, sachets, flasks, powders, granules, pills, reconstitutable powders or liquid preparations, such as solutions or suspensions, or suppositories. Medicaments, for example those that are suitable for oral administration, may contain common excipients, such as binding agents (syrup, gum arabic, gelatin, sorbitol, tragacanth or polyvinylpyrrolidone), fillers (lactose, sugar, corn starch, calcium phosphate, sorbitol or glycerin), tablet lubricants (magnesium stearate, disintegrants (starch, polyvinylpyrrolidone, sodium starch glycolate or microcrystalline cellulose) or pharmaceutically acceptable setting agents, such as sodium lauryl sulfate. The solid medicaments can be obtained by common methods of mixing, filling, tabletting or the like. Repeated blending operations can be used to distribute paroxetine or a salt or solvate thereof through those drugs that employ large amounts of fillers. When the medicament is in the form of a tablet, powder or lozenge, any suitable vehicle can be used to formulate solid pharmaceutical compositions; for example, magnesium stearate, starch, glucose, lactose, sucrose, rice flour and clay. The tablets can be covered according to methods well known in normal pharmaceutical practice, in particular with an enteric coating. The medicament may also be in the form of an ingestible capsule, for example of gelatin containing paroxetine or, if desired, a salt thereof, with a vehicle or other excipients. Liquid medicaments for oral administration may be, for example, in the form of emulsions, syrups or elixirs, or they may be presented as a dry product for reconstitution with water or other suitable vehicle before use. These liquid medications may contain common additives, such as suspending agents (sorbitol, syrup, methylcellulose, gelatin, hydroxyethylcellulose, carboxymethylcellulose, aluminum stearate, gel, edible hydrogenated fats), emulsifying agents (lecithin, sorbitan monooleate or gum arabic), aqueous or non-aqueous vehicles, including edible oils, such as almond oil, fractionated coconut oil, oily esters; for example, esters of glycerin, or propylene glycol or ethyl alcohol, glycerin, water or normal saline; preservatives (propyl-p-hydroxybenzoate or methyl p-hydroxybenzoate, or sorbic acid) and, if desired, common coloring or flavoring agents. Paroxetine, or a pharmaceutically acceptable salt or solvate thereof, can also be administered by a non-oral route. According to the routine pharmaceutical procedure, the medicaments can be formulated, for example, for rectal administration as a suppository. Also, suspension or emulsion in a pharmaceutically acceptable liquid, such as sterile, pyrogen-free water, or a parenterally acceptable oil or a mixture of liquids, can be formulated for an injectable form in an aqueous or non-aqueous solution. The liquid may contain bacteriostatic agents, antioxidants or other preservatives, pH regulators or solutes, to make the solution isotonic with blood, thickening agents, suspending agents or other pharmaceutically acceptable additives. Said forms will be presented in the form of a unit dose, such as ampules or disposable injection devices, or in multiple dose forms, such as a bottle from which the appropriate dose can be extracted, or in solid or concentrate form, which can be used to prepare an injectable formulation.

As mentioned above, the effective dose of paroxetine or a pharmaceutically acceptable salt or solvate thereof depends on the severity of the generalized anxiety disorder to be treated, the condition of the patient and the frequency and route of administration. A unit dose will generally contain from 2 to 1000 mg and, preferably, contain from 30 to 500 mg, in particular 20, 50, 100, 150, 200, 250, 300, 350, 400, 450 or 500 mg. The composition may be administered one or more times per day; for example, 2, 3 or 4 times a day, and the total daily dose for an adult of 70 kg will normally range from 100 to 3000 mg. Preferably, the unit dose will contain from 2 to 20 mg of paroxetine (calculated as free base) and, if desired, it will be administered in multiple doses to obtain the previous daily dose.

This invention further provides a pharmaceutical composition for use in the treatment of generalized anxiety disorder, which is constituted by an effective amount of paroxetine, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier. Said compositions can be prepared in the manner described above. The following example describes a pharmaceutical composition suitable for use in this invention.

EXAMPLE The following ingredients are mixed together in the customary manner and compressed into tablets weighing approximately 300 mg, which contain about 20 mg of paroxetine (calculated as the free base).

Claims (3)

NOVELTY OF THE INVENTION CLAIMS

1. The use of paroxetine or a pharmaceutically acceptable salt or solvate thereof in the manufacture of a medicament for the treatment of generalized anxiety disorder in a human or a non-human animal.

2. A pharmaceutical composition for use in the treatment of generalized anxiety disorder, which consists of an effective amount of paroxetine or a pharmaceutically acceptable salt or solvate thereof, as well as a pharmaceutically acceptable carrier.

3. The use according to claim 1, wherein the pharmaceutically acceptable salt of paroxetine is the hydrochloride.