A comparison of the abuse liability and dependence potential of nicotine patch, gum, spray and inhaler

West, Robert; Hájek, Peter; Foulds, Jonathan; Nilsson, Fredrik; May, Sylvia; Meadows, Anna

doi:10.1007/s002130000382

Cited by 159 publications

(115 citation statements)

References 12 publications

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“…Owing to the slower delivery of nicotine and in part because NRT only partially addresses the reinforcing behavioural and social effects of smoking, these products have been shown to have low liability for abuse and low dependence potential [West et al 2000]. In addition, there is no evidence of withdrawal discomfort when patients discontinue NRT use [West et al 2000].…”

Section: Current Pharmacological Smoking Cessation Drugsmentioning

confidence: 99%

Therapeutic advances in the treatment of nicotine addiction: present and future

Casella¹,

Caponnetto²,

Polosa

2010

Therapeutic Advances in Chronic Disease

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While the proportion of the adult population that smokes has declined steadily in several westernized societies, the rate of successful quit attempts is still low. This is because smokers develop nicotine dependence, a powerful addiction that may require multiple attempts and long-term treatment to achieve enduring abstinence. Currently available first-line agents for smoking cessation therapy include nicotine replacement therapy (available in several formulations, including transdermal patch, gum, nasal spray, inhaler, and lozenge), bupropion (an atypical antidepressant), and varenicline (a partial agonist of the a4b2 nicotinic acetylcholine receptor that was recently developed and approved specifically for smoking cessation therapy). Second-line agents are nortriptyline (a tricyclic antidepressant agent) and the antihypertensive agent clonidine. With the exception of varenicline, which has been shown to offer significant improvement in abstinence rates over bupropion, all of the available treatments appear similarly effective. The adverse event profiles of nortriptyline and clonidine make them more appropriate for second-line therapy, when first-line treatments have failed or are not tolerated. However, the currently marketed smoking cessation drugs reportedly lack high levels of efficacy, particularly in real-life settings. New medications and vaccines with significant clinical advantage are now in the advanced stage of development and offer promise. These include nicotine vaccines and monoamine type B inhibitors. In this review article we discuss current and emerging pharmacotherapies for tobacco dependence focusing on their mechanisms of action, efficacy and adverse event profiles.

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Section: Current Pharmacological Smoking Cessation Drugsmentioning

confidence: 99%

Therapeutic advances in the treatment of nicotine addiction: present and future

Casella¹,

Caponnetto²,

Polosa

2010

Therapeutic Advances in Chronic Disease

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“…An acute increase in dopamine output in the nucleus accumbens following nicotine intake is believed to mediate the addictive properties of smoking (1). Nicotine is most addictive when inhaled, whereas nicotine delivered orally or through the skin rarely leads to addiction (1,2). The rapid transport of nicotine from the blood to the brain seems to be critical for its neurobiological effects (1,3).…”

Section: Introductionmentioning

confidence: 99%

Coexistence of Passive and Proton Antiporter-Mediated Processes in Nicotine Transport at the Mouse Blood–Brain Barrier

Cisternino

Chapy

André

et al. 2012

AAPS J

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Abstract. Nicotine, the main tobacco alkaloid leading to smoking dependence, rapidly crosses the bloodbrain barrier (BBB) to become concentrated in the brain. Recently, it has been shown that nicotine interacts with some organic cation transporters (OCT), but their influence at the BBB has not yet been assessed in vivo. In this study, we characterized the transport of nicotine at the mouse luminal BBB by in situ brain perfusion. Its influx was saturable and followed the Michaelis-Menten kinetics (K m 02.60 mM, V max 037.60 nmol/s/g at pH 7.40). At its usual micromolar concentrations in the plasma, most (79%) of the net transport of nicotine at the BBB was carrier-mediated, while passive diffusion accounted for 21%. Studies on knockout mice showed that the OCT Oct1-3, P-gp, and Bcrp did not alter [3 H]-nicotine transport at the BBB. Neither did inhibiting the transporters Mate1, Octn, or Pmat. The in vivo manipulation of intracellular and/or extracellular pH, the chemical inhibition profile, and the transstimulation experiments demonstrated that the nicotine transporter at the BBB shared the properties of the clonidine/proton antiporter. The molecular features of this proton-coupled antiporter have not yet been identified, but it also transports diphenhydramine and tramadol and helps nicotine cross the BBB at a faster rate and to a greater extent. The pharmacological inhibition of this nicotine/proton antiporter could represent a new strategy to reduce nicotine uptake by the brain and thus help curb addiction to smoking.

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“…Routes of dosing that are associated with more rapid rates of delivery, such as nasal spray, are expected to result in higher intensity of effects and higher addiction liability when compared with products with slower absorption. Some indications of this were seen in a recent study comparing the abuse liability of the nicotine patch, gum, nasal spray, and inhaler in smoking cessation (West et al, 2000). Nasal spray had the highest rate of continuing use at the end of the study compared with the other NRTs; however, overall abuse liability was low for all products.…”

mentioning

confidence: 98%

“…Absorption of nicotine from all NRTs is slower and the increase in nicotine blood levels more gradual than from smoking (Table 1). This slow increase in blood and especially brain levels results in low abuse liability of NRTs (Henningfield and Keenan, 1993;West et al, 2000). Only nasal spray provides a rapid delivery of nicotine that is closer to the rate of nicotine delivery achieved with smoking (Sutherland et al, 1992;Gourlay and Benowitz, 1997;Guthrie et al, 1999).…”

mentioning

confidence: 99%