Varenicline: The newest agent for smoking cessation

Potts, Lisa A.; Garwood, Candice L.

doi:10.2146/ajhp060428

Cited by 38 publications

(26 citation statements)

References 9 publications

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“…While prolonged stimulation by most entities usually causes receptor downregulation, nicotine stimulation at the acetylcholine receptors causes upregulation. This upregulation desensitizes acetylcholine receptors, which results in nicotine dependence and addiction [Potts and Garwood, 2007].…”

Section: Me (A) (B)mentioning

confidence: 99%

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Are nicotine replacement therapy, varenicline or bupropion options for pregnant mothers to quit smoking? Effects on the respiratory system of the offspring

Maritz

2009

Ther Adv Respir Dis

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Nicotine occurs in tobacco smoke. It is a habit-forming substance and is prescribed by health professionals to assist smokers to quit smoking. It is rapidly absorbed from the lungs of smokers. It crosses the placenta and accumulates in the developing fetus. Nicotine induces formation of oxygen radicals and at the same time also reduces the antioxidant capacity of the lungs. Nicotine and the oxidants cause point mutations in the DNA molecule thereby changing the program that controls lung growth and maintenance of lung structure. The data available indicate that maternal nicotine exposure induces a persistent inhibition of glycolysis and a drastically increased AMP level. These metabolic changes are thought to contribute to the faster aging of the lungs of the offspring of mothers that are exposed to nicotine via the placenta and mother's milk. The lungs of these animals are more susceptible to damage as shown by the gradual deterioration of the lung parenchyma. The rapid metabolic and structural aging of the lungs of the animals exposed to nicotine via the placenta and mother's milk, and thus during phases of lung development characterized by rapid cell division, is likely due to 'programming' induced by nicotine. Since varenicline, a partial nicotine agonist, has basically the same structure as nicotine, and also binds to acetylcholine receptors in competition with nicotine (but with largely the same effect), it is not advisable to use nicotine or varenicline during gestation and lactation. Furthermore, the use of individual vitamin supplements is also not advisable because of the negative impact on the program that controls maintenance of lung structural and functional integrity and aging. A more appropriate smoking cessation program will also include a mixture of antioxidant nutrients such as in tomato juice.

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Section: Me (A) (B)mentioning

confidence: 99%

“…In vivo studies found that the dopamine response to varenicline is 3260% of the response of nicotine. Varenicline competitively inhibits nicotine, thereby blocking the effects of nicotine at the a4b2 receptor site and so alleviate the nicotine withdrawal symptoms [Potts and Garwood, 2007]. …”

Section: Bupropionmentioning

confidence: 99%

Are nicotine replacement therapy, varenicline or bupropion options for pregnant mothers to quit smoking? Effects on the respiratory system of the offspring

Maritz

2009

Ther Adv Respir Dis

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“…Im Durchschnitt erhalten nur 38% der Raucher ärzt-liche Unterstützungsangebote (Spannweite 0-100%; [12]). Nikotinersatztherapie [33], Bupropion [21] und Vareniclin können den Anteil erfolgreicher Raucherentwöhnungen signifikant steigern, wie zahlreiche kontrollierte Studien belegen [30,31], weitere Substanzen wie Rimonabant und Nikotinimpfungen sind derzeit in Entwicklung [16].…”

Section: > Ex-raucher Leben Länger Als Aktive Raucher Und Sind Bei Beunclassified

Prävention von Erkrankungen des Respirationstrakts

Virchow

2008

Internist

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There are multiple possibilities for pulmonary or bronchial damage and their number exceeds that for the other organ systems dealt with in this issue. This multiplicity of diseases which are at least in part attributable to exogenous damage gives rise to manifold approaches to prevention. This overview does not claim to be complete. It is however intended to clarify the possibilities that exist for the prevention of pulmonary diseases. In addition, it intends to show that effective primary and occasionally secondary and tertiary prevention is inadequately utilized in pulmonology or not even used at all. Against the background that individual preventive measures in pulmonology are considerably more successful than curative measures, also from a health economics point of view, various options for successful prevention are described. The great need for studies on the effectiveness of preventive strategies is also addressed.

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“…Cytisine, derived from the plant Cytisus laburnum, has been used in Eastern Europe to aid in smoking cessation for over forty years and is currently being sold under the brand name Tabex ® . 2,3 Varenicline has been modified to have greater bioavailability and selectivity for the α 4 β 2 receptor subtype, but to a lower level than nicotine. The highest concentration of α 4 β 2 nicotinic receptors can be found on the dopamine and γ-aminobutyric acid-containing neurons, and with its agonist activity varenicline both blocks the nicotine receptor as well as stimulates dopamine release.…”

mentioning

confidence: 99%

“…The highest concentration of α 4 β 2 nicotinic receptors can be found on the dopamine and γ-aminobutyric acid-containing neurons, and with its agonist activity varenicline both blocks the nicotine receptor as well as stimulates dopamine release. 2,4 The effects of this receptor activation are thought to be of importance in dependence, thereby reducing the craving for nicotine. 4 Currently, there are no published reports of varenicline overdose.…”

mentioning

confidence: 99%