Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Reexamination Certificate
1998-01-29
2002-04-16
Chang, Ceila (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
C514S529000, C514S530000, C562S507000, C562S553000
Reexamination Certificate
active
06372792
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to treatment of anxiety, including all of the anxiety disorders, and insomnia in humans by administration of gabapentin, its derivatives and pharmaceutically acceptable salts.
2. Description of the Related Art
Gabapentin is a generic term used to identify the chemical compound (1-aminomethyl)-1-cyclohexaneacetic acid. It is useful in therapy of certain cerebral disorders such as certain forms of epilepsy, faintness attacks, hypokinesia and cranial traumas. U.S. Pat. Nos. 4,024,175 and 4,087,544 cover the compound and its uses. They also disclose an acid salt, i.e. gabapentin hydrochloride hydrate in a ratio of 4:4:1 and a sodium salt of gabapentin hydrate in a ratio of 2:1. These patents are hereby incorporated by reference. Pregabalin is a long-acting form of gabapentin with the formula (S)-3-(aminomethyl)-5-methyl-hexanoic acid and CAS Registry Number: 148553-50-8, CI 1008. The compounds are described in U.S. Pat. Nos. 5,608,090 and 5,599,973, the disclosure of which are incorporated herein by reference to show additional forms of gabapentin usable in this invention.
U.S. Pat. No. 5,084,479 states that compounds such as gabapentin are used for treating neurodegenerative disorders, perinatal asphyxia, status epilepticus, Alzheimer's, Huntington's, Parkinson's, and Amyotrophic Lateral Sclerosis. That invention covers treating neurodegenerative disorders termed acute brain injury. These include but are not limited to: stroke, head trauma, and asphyxia.
U.S. Pat. No. 5,189,026 describes the use of ivermectin, and notes that other GABA agonists may have activity to some extent in treating anxiety, but dismisses them due to stated detrimental effects.
WO 9603122 is a published application entitled “Controlling Anxiety and Panic —By Administration of Aminomethyl-cycloalkane Acetate(s), Esp. Gabapentin”, filed by BROWN, J. P.; GEE, N. S.; SINGH, L.; WOODRUFF, G. N.; and BROWN, J. That application claims a priority to U.S. application Ser. Nos. 08/281,285, filed Jul. 27, 1994, and 08/445,398, filed Jun. 6, 1995.
The art described in this section is not intended to constitute an admission that any patent, publication or other information referred to herein is “prior art” with respect to this invention, unless specifically designated as such. In addition, this section should not be construed to mean that a search has been made or that no other pertinent information as defined in 37 C.F.R. § 1.56(a) exists.
SUMMARY OF THE INVENTION
It has been found that gabapentin surprisingly has properties that also enables it to be used effectively to treat anxiety and all of the anxiety disorders, and may also be used to treat patients with insomnia. The etiology of anxiety and the anxiety disorders is unknown and the biochemical defect is also unknown. We postulate that the specific effect of gabapentin on insomnia, anxiety and the anxiety disorders implicates an indirect involvement with gamma aminobutyric acid (GABA) in its mechanism of action, as is the case for another group of drugs, the benzodiazepines, with their effects on anxiety and insomnia. It has been found that benzodiazepines act through their own benzodiazepine receptor which is coupled with the GABA receptor. We suggest that gabapentin does the same through its own receptor, which we name the Gabapentin receptor, also coupled with the GABA receptor. We propose that the gabapentin receptor is coupled with one of the subunits (&agr;, &bgr;, &dgr; or &egr;) of the GABA
A
-receptor. This surprising finding has never been suggested or proposed previously. The clinical effects observed have lead us to this conclusion. Use of the term “gabapentin” in this application is intended to encompass gabapentin, pregabalin and their pharmaceutically acceptable salts.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
The anxiety disorders are described succinctly in the
American Psychiatric Association Diagnostic and Statistical Manual
, 4th edition, DSM IV, the disclosure of which is incorporated herein by reference. The anxiety disorders have been divided into three major clinical entities: generalized anxiety, panic disorder with or without agoraphobia, and obsessive-compulsive disorders (DSM-III-R).
Generalized anxiety disorder (GAD) is characterized by intense fearfulness expressed through symptoms that can affect almost all anatomic body regions. In cases of panic attacks associated or not with panic disorder, anxiety symptoms are associated with recognizable panic attacks, with or without agoraphobia. The essential feature of a Panic Attack is a discrete period of intense fear or discomfort that is accompanied by at least 4 to 13 somatic or cognitive symptoms,. Panic Attacks can occur in a variety of Anxiety Disorders (e.g., Panic Disorders, Social Phobia, Posttraumatic Stress Disorder). Essential and specific features of GAD remain to be the presence of unrealistic and inappropriate apprehensive expectation, which may persist for several months and be associated to secondary symptoms, including signs of vigilance (irritability, insomnia, difficulty concentrating), motor tension (trembling, muscle tension, restlessness, fatigability), and autonomic hyperactivity (cardiac palpitations, shortness of breath, smothering sensations, sweatiness of hands and skin).
Anxiety can also be part of other psychiatric disorders and considered secondary to a primary psychopathology, such as major depression, mania or schizophrenia. Antianxiety or hypnotic drugs are given primarily for the treatment of minor or major generalized anxiety disorder, with or without insomnia as a target symptom (primary), but also where it coexists with another psychiatric disorder (secondary). The most common drugs used to treat anxiety disorders have been the benzodiazepines.
The sleep disorders are organized into four major sections according to presumed etiology. The sleep disorders are also succinctly described in the
American Psychiatric Association Diagnostic and Statistical Manual
, 4th edition, DSM IV and generally include primary sleep disorders, sleep disorders related to another mental disorder, sleep disorder due to a general medical condition and substance-induced sleep disorder. In this application, insomnia shall be used as a short-hand for all of the sleep disorders.
Based on our research, it is apparent that gabapentin may be used to safely treat all of these illnesses, and also to treat minor or transient anxiety symptoms that do not fulfill diagnostic criteria for which a patient may seek medications from a physician, without fear of long term physical addiction or other benzodiazepine side effects.
Case History 1
Mr. S. is a 64 year-old retired patient. His family history reveals that his sister has manic depressive illness and maternal aunts are described as “nervous”. In his medical history, there is a cervical laminectomy (1988). He reports residual pain and weakness in the right arm and right leg and chronic neck pain. He has a history of three months of depression with no treatment (1989) and a history of chronic severe generalized anxiety disorder.
In December 1994, the patient had been taking a benzodiazepine, clonazepam 2.5 mg/day, for the last five years when his anxiety and depression became much worse. Anxiety was associated with marked insomnia and significant situational stressors (financial and marital). Fluoxetine and then sertraline was initiated at a low dose, but made the patient worse. Gabapentin was initiated 300 mg/day (October 1994) and slowly increased. The response was immediate; sleep improved and anxiety decreased. Patient is now functional for the first time in many years. Improvement continues as of this day. His psychological dependency on benzodiazepines has significantly decreased since the intake of gabapentin. Improvement persists. With gabapentin we have noticed an improvement in mood and a marked improvement in sleep and anxiety, in addition to an analgesic effect.
Case History 2
Mrs. R. is a 62 year-old retired patient with a family hist
Chang Ceila
Vidas,Arrett&Steinkraus PA.
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