Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2001-05-16
2001-11-20
Henley, III, Raymond (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
active
06319927
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to treating and/or preventing sleep disorders in a human by administering a therapeutically effective amount of cetirizine or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions therefor.
BACKGROUND OF THE INVENTION
Sleep disorders are becoming increasingly prevalent in our society. It is estimated that 40 million Americans suffer from various sleep disorders. Further, 25 million more Americans suffer from intermittent-sleep-related disorders. Sleep disorders have various etiologies including stress induced by environmental and life style factors, physical factors, such as disease or obesity, and psychiatric disorders, such as depression.
Sleep disorders encompass, among other things, snoring, sleep apnea, insomnia, narcolepsy, restless legs syndrome, sleep terrors, sleep walking and sleep eating. Possible treatment can be as simple as behavior modification or it can be as involved as mechanical, surgical, or pharmacological intervention.
A particularly insidious sleep disorder is insomnia. Insomnia is defined as either having a difficulty falling asleep or overly frequent night awakenings. Insomnia can be caused by a number of different things including a change in environment, daily stress, caffeine, and other stimulants.
If left untreated, insomnia can adversely affect the quality of one's life. People with insomnia tend to suffer more frequently from depression and anxiety. Insomnia can also leave one tired and unable to perform at the workplace and/or even carry out normal daily activities. This inability to perform these activities has a negative impact on both professional and family life.
Typically, insomnia can be treated pharmacologically. Sedative hypnotics such as barbiturates, benzodiazepines and related compounds have been administered to treat insomnia. However, these compounds have a drawback because of the potential for addiction.
Sedating anti-histamine drugs have also been administered to treat insomnia. Agents such as diphenhydramine and hydroxyzine are typically administered due to their sedating properties. A second generation anti-histamine, ceterizine, is the primary acid metabolite of hydroxyzine resulting from the complete oxidation of hydroxyzine in vivo.
It has been reported that cetirizine may cause drowsiness when administered to patients. For instance, somnolence has been reported as the most frequently occurring side effect of cetirizine administration. Physician's Desk Reference, 2000 edition. Similarly, it has been reported that cetirizine impairs performance in tracking tests and increased both objective and subjective sleepiness in subjects. Nicholson AN, et al.,
Aviat. Space Environ. Med.,
1998 February; 69(2): 166-71. Additionally, cetirizine has been reported to cause acute sedative activity by impairing driving performance and altering EEG energy spectra in the direction of electrocortical deactivation. Ramaeckers, et al.,
Eur. J. Clin. Pharmacol.,
1992, 42: 363-369.
None of the aforementioned references discloses the use of cetirizine to treat sleep disorders, particularly insomnia. In fact, in all of these studies, cetirizine induced drowsiness was considered an unwanted side effect.
SUMMARY OF THE INVENTION
The present invention provides a method of treating and/or preventing sleep disorders in a human comprising administering to a human a therapeutically effective amount of cetirizine or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions containing cetirizine.
DETAILED DESCRIPTION OF THE INVENTION
The present inventions comprises a method for treating a human suffering from a sleeping disorder comprising administering to the human a therapeutically effective amount of cetirizine hydrochloride once daily.
The present invention also comprises a method for treating a human suffering from a sleep disorder comprising administering to the human a therapeutically effective amount of cetirizine hydrochloride once daily by oral or intranasal administration.
The present invention also comprises a method for treating a human suffering from a sleeping disorder comprising administering to the human a therapeutically effective amount of cetirizine hydrochloride once daily at least about 3 hours prior to a normal sleeping period.
The present invention also comprises a method for treating a human suffering from a sleep disorder comprising administering to the human a tablet formulation containing a therapeutically effective amount of cetirizine hydrochloride once daily by oral administration.
The present invention also comprises a pharmaceutical composition for intranasal administration comprising an amount of cetirizine or a pharmaceutically acceptable salt thereof that is sufficient to induce sleep in a human and an aqueous carrier comprising 70 to 90% by weight/volume of water; 0.10 to 5.00% by weight, volume of an aromatic alcohol; 0.01 to 0.3% by weight/volume of a non-mercurial antimicrobial preservative; 0 to 10% by weight/volume of a moisturizing agent; 0 to 10% by weight/volume of an antioxidant; 0 to 2.00% by weight/volume of a surfactant, a sufficient amount of a pharmaceutically acceptable buffer to maintain the pH of the composition within the range of about 3 to about 7; and QS water.
The present invention is particularly effective in treating and/or preventing sleep disorders in a patient suffering from disordered sleep. The terms “sleep disorders” and “disordered sleep” as used herein mean disordered, interrupted or fragmented sleep characterized by events including, but not limited to, snoring, periods of sleep apnea, insomnia, narcolepsy, restless legs syndrome, sleep terrors, sleep walking, sleep eating and daytime somnolence. The magnitude of a prophylactic or therapeutically effective dose of cetirizine in the acute or chronic management of sleep disorders will vary with the severity of the condition to be treated. The therapeutically effective amount, and perhaps the frequency, will also vary according to the age, body weight, and response of the individual patient.
The invention also includes the enantiomers, isomers and derivatives oc seterizine, preferably levocetirizine and dextrocetirizine, most preferably levocetirizine.
Cetirizine hydrochloride is an H
1
-receptor antagonist. The chemical name is (±)-[2- [4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid, dihydrochloride. Cetirizine hydrochloride is a racemic compound with an empirical formula of C
21
H
25
ClN
2
O
3
.2HCl. Cetirizine hydrochloride is a white, crystalline powder and is water soluble. Cetirizine hydrochloride is available from Pfizer Inc., New York, N.Y., under the trade name ZYRTEC®.
In general, the total daily therapeutically effective amount, for the conditions described herein, is from about 1 mg to about 40 mg of cetirizine administered in a single daily dose. For example, a preferred daily dose should be from about 10 mg to about 30 mg, most preferably one daily dose of about 20 mg.
The therapeutically effective dose to be administered is administered at least about 3 hours prior to a normal sleeping period, preferably about three to about 8 hours prior to a normal sleeping period, more preferably about four to about 6 hours prior to a normal sleeping period, and most preferably about 5 hours prior to a normal sleeping period.
As used herein, the term “normal sleeping period” means any time that a patient wishes to fall asleep. The term “normal” is in no way meant to limit the invention to any particular time of the day and/or night since patients have different lifestyles necessitating different times of administration.
The methods of the present invention may be carried out by administering pharmaceutical compositions containing cetirizine. Such compositions may be formulated by combining cetirizine or an equivalent amount of a pharmaceutically acceptable salt thereof with a suitable, inert, pharmaceutically acceptable carrier or diluent that is a so
Henley III Raymond
Lipka Robert J.
Schering Corporation
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