Invented by Amruta R. Eswara, Neal Muni, F. Howard Schneider, Peter J. Mione, DynaGen Inc
The DynaGen Inc invention works as followsThe invention provides methods and articles for the treatment of nicotine withdrawal symptoms and to promote smoking cessation. These articles and methods allow for the administration of a nicotine replacement and the monitoring of the presence of nicotine in biological samples of subjects using a nicotine detection system.
Background for Methods, articles and methods of manufacture for nicotine cessation or monitoring nicotine use
A greater understanding of the negative health effects of smoking and nicotine intake has resulted in a marked rise in research into the nature and treatment of nicotine addiction. As described in U.S. past reports on nicotine addiction, According to past U.S. Surgeon General reports, nicotine addiction is common. There are more than 50 million smokers in America. A major obstacle to a person’s ability and will to stop smoking is nicotine addiction.
Like other addictions, nicotine addiction has two components. The first is the physiological addiction to nicotine. The physiological addiction is caused by adaptive brain nicotine receptor changes that cause withdrawal symptoms. The second component is the complex behavioral component. This behavior component links to internal cues that are learned to associate with positive and negative emotions related to abstinence or tobacco smoking.
The physiological addiction to nicotine has been recognized. According to the American Psychiatric Association’s Diagnostic and Statistical Manual of Mental Disorders, the official criteria for nicotine withdrawal are: (1) craving for nicotine; (2) irritability; frustration, anger; (3) anxiety and (4) difficulty concentrating; (5) restlessness and (6) decreased heart beat; and (7) increased hunger or weight gain.
Different approaches to quitting smoking include both the behavioral and physiological components. There are many options available, including stopping cold turkey, electroshock, behavioral counseling, hypnosis and acupuncture. In conjunction with counseling and behavioral therapy, nicotine replacement therapies like chewing gum or transdermal patches are used commonly to treat nicotine withdrawal. Long-term success with nicotine replacement is not possible. The average person who attempts to quit smoking is 25%.
Clinicians and epidemiologists need to know whether or not a person uses nicotine in any way. It is not always accurate to rely on self-reporting from nicotine users about their nicotine habits. Clinicians and epidemiologists might also need information about non-smokers’ inhalation of secondary smoking, as well as other passive nicotine exposures due to environmental conditions.
Further many methods for quitting smoking use nicotine. Nicotine can also be administered via other routes than smoking, such as chewing gum or patches. The clinician may have difficulty diagnosing nicotine addiction as a treatment for smoking cessation. It can be difficult, if possible, to tell the difference between nicotine or nicotine metabolites that are present as a result of the therapy and those that are still present due to smoking.
It is also a good idea to have the subject participate in monitoring their performance. Most assays cannot be used at home and subjects may find it difficult to read test results that may not reflect adherence to a smoking cessation or nicotine administration regimen.
Lobeline, the main alkaloid from the dried leaves of Lobelia Inflata, an annual member of the Lobeliaceae plant family, is what we call Lobeline. Lobeline, a substituted piperidine compounds, produces several physiological effects that are similar to nicotine. The pharmacological effects of lobeline may be due to its ability to bind with nicotine receptors in the brain as well as elsewhere in the body. The potency of lobeline in inducing peripheral pharmacological effects such as an increase in blood pressure or heart rate is much lower than that of nicotine.
Lobeline was proposed to be a replacement for nicotine. It is intended to reduce dependence and the use of tobacco products. While lobeline has been used as a smoking cessation tool since the 1930’s, there has been some controversy over its effectiveness.
Typical OTC products that provide lobeline include Nicoban? and Bantron?, CigArrest, NicFit?, and CigArrest. Smoker’s choice? In recent years, all lobeline products that contain smoking cessation products have been OTC non-prescription products. According to the FDA, all OTC smoking cessation products are ineffective. They have taken the unusual step and declared all OTC products mislabeled in an effort to remove them from the market. OTC products are administered orally to the gastrointestinal tract. These products can be taken daily at a dose of 6 milligrams according to the directions. Some products contain antacids to relieve gastrointestinal discomfort. This side effect is similar to nicotine. Due to the gastric upset, higher oral doses might not be possible.
Even though there have been some reports that lobeline has been used in oral formulations at higher than 10 mg/day, nausea or vomiting have been reported. Another problem with oral dose regimens like these is the need for self-administration. Patients may be required to take as many as 18 tablets daily. Patients might find such a regimen intrusive and may not agree with the doctor’s recommendations.
Lobeline might not be well absorbed by the gastrointestinal tract. Due to adverse gastrointestinal effects, subjects who want to replace nicotine with lobeline may not be able to consume effective amounts orally. Oral products might not be able to produce the desired levels of blood or tissue.
Smoker’s Lozenges is the only product currently available that contains lobeline in candy lozenges. To release lobeline, the lozenge will dissolve slowly in your mouth. Smoker’s gum, a second product, has lobeline in a base of gum. As the gum is chewed, it releases lobeline slowly. These products don’t require users to keep the gum or any dissolved candy in their oral cavity. Normal reflex is to swallow. This would severely limit buccal absorption. The liver may first process the metabolism of any absorbed lobeline through the gastrointestinal tract.
FDA has questioned the effectiveness of these OTC products as well as other lobeline OTC drugs. Effective doses of lobeline were not possible without injectable dosage forms.
The present invention relates to articles and methods of manufacturing for administering a sufficient amount of lobeline and monitoring smoking cessation using a nicotine detection device. Methods and articles of manufacture according to the invention offer relief from acute nicoline withdrawal and enable a subject to monitor their compliance to a smoking cessation plan.
The present invention includes methods and articles for treating nicotine withdrawal symptoms. The present invention includes administering a substance that is effective as a substitute for nicotine to a subject prior to or during the period when the subject experiences nicotine withdrawal symptoms. A nicotine detection system monitors the use of nicotine to monitor the progress of nicotine intake. The nicotine substitute reduces the subject’s craving for nicotine. The nicotine detection system doesn’t measure the presence of nicotine substitute.
Nicotine” is the addictive component of tobacco products. The formula for nicotine is as follows: ##STR1##
Nicotine substitute” can refer to either a receptor binding or sensory altering nicotine substitute. A nicotine substitute as used herein does not include nicotine.
A “receptor binding nicotine replacement” is a compound that exhibits an affinity to nicotinic receptors-enriched brain tissue in in vitro binding assays. These compounds include lobeline and isoarecolone as well as cytisine, anabasine, isoarecolone and lobeline.
Lobeline, also known as 2- 6-(?-hydroxyphenethyl)-1-methyl-2-piperidyl acetaminophen has the following structural formula: ##STR2##
Lobeline” is a generic term that includes the lobeline-free base, its various salts, and lobeline analogues. The functional groups can be added or removed from the fonnula, but they must retain the physiological activity of the lobeline. These alterations and deviations can be included in the term “lobeline analogsClick here to view the patent on Google Patents.