Antismoking preparations

L. inflata (Indian tobacco) is indigenous to the Eastern and Central states of USA and Canada. The plant contains ca. 0.3% of alkaloids. The L. a. are 2,6-di-substituted piperidine derivatives. Among the ca. 20 L. a., lobeline is the major alkaloid. When administered parenterally (3-10 mg) lobeline stimulates respiration and was used in the past as a respiratory analeptic agent for asthma, collapse, and narcosis incidents. When taken orally it is rapidly degraded and thus not effective. Since lobeline potentiates the action of nicotine and induces nausea and revulsion it has been developed clinically in depot form in antismoking preparations. - The piperidine ring is biogenetically derived from lysine and the substituents from phenylalanine. 

Another series of lysine derived alkaloids occurs in the genus Lobelia (Campanulaceae). One of these compounds, lobeline (39) (Fig. 29.13) (from Lobelia inflata, Indian tobacco), has been used in antismoking preparations. Both lobeline and nicotine are classed as ganglionic stimulants. Therapeutically, lobeline is hardly used today (Fodor and Colosanti, 1985). Poisoning of cattle because of ingestion of Lobelia berlandieri has occurred in Texas and Mexico... 

L. inflata L. is a traditional medicinal plant native to North America. It contains several piperidine alkaloids. The main alkaloid is lobeline which has a stimulatory effect on the respiratory center and it is applied in the cases of asthma, gas- and narcotic-poisoning. Thus, lobeiine is currently the subject of renewed interest for the treatment of drug abuse and neurological disorders, like Alzheimer s or Parkinson s disease, which pose an important public health problem in industrial countries. As lobeiine can act as a competitive nicotinic receptor antagonist, it is frequently used in antismoking preparations. Interest in Lobelia alkaloids, and in particular (-)-lobeline, the most active of them, has increased in recent years due to their activity on the central nervous system (CNS). 

Extracts are quite extensively used in tonics (especially those for female ailments). Also used in diuretic, laxative, and antismoking preparations as well as in cosmetic and toiletry formulations, presumably for their tonic properties. In Germany, the root is used for disturbances in bile flow, as diuretic, and as an appetite stimulant. The herb is used for appetite and dyspeptic disorders, such as abdominal fullness and flatulence. Products are contraindicated in obstruction of bile ducts. 

Regulatory Status. Undefined in the United States as food ingredient as of 1993 lobeline is no longer allowed as an ingredient in antismoking preparations. ... 

Used in antismoking preparations. Has been used as a respiratory stimulant. Used as a 0.1 Af aq. soln. for photometric detn. of Mo 465 nm, e 13800). 

Gentian extracts are used in tonic preparations also used in certain antismoking formulas. They are also used in cosmetics. ... 

Licorice extracts are used extensively as ingredients in cough drops and syrups, tonics, laxatives, antismoking lozenges (see lobelia), and other preparations. They are also used as flavoring agents to mask bitter, nauseous, or other undesirable tastes in certain medicines (e.g., cascara, ammonium chloride, and quinine preparations). 

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