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PubMed1995

Nicotine patch use in the general population: results from the 1993 California Tobacco Survey.

BACKGROUND: Evidence from controlled clinical trials indicates that use of a transdermal nicotine patch improves abstinence rates up to a year after initial smoking cessation. Whether these results can be generalized to the general population has not been extensively investigated. PURPOSE: We sought to determine what characteristics of smokers trying to quit are associated with nicotine patch use in the general population and whether there is evidence that patch use promotes successful smoking cessation. METHODS: As part of the 1993 California Tobacco Survey, 3281 respondents who had attempted to quit smoking cigarettes within the last year were asked whether they had used a prescribed medication to help them quit smoking and, if so, what type of medication it was. They were also asked whether they used other assistance. RESULTS: Compared with nonusers, patch users (nearly 11% of quitters) were more likely to be female, white or Asian, middle-aged, and to smoke more heavily. Many people relapsed to smoking while they were still using a patch. However, no evidence suggested that the patch was addictive. Use of a nicotine patch did not result in a statistically significant difference in abstinence rates among those who did not also use some other form of assistance (logrank test, P = .466). It did make a statistically significant difference when used in combination with another aid (logrank test, P = .017). At 6 months, abstinence rates were 15% for those without other forms of assistance whether or not they used a patch, 10.9% (95% confidence interval [CI] = 5.1-16.8) for those with other assistance who did not use a patch, and 18.8% (95% CI = 5.7-31.8) for those with other assistance who did use a patch. CONCLUSIONS: The nicotine patch appears to be an important aid to smokers who want to quit, primarily when used as an adjuvant to other forms of assistance. IMPLICATIONS: Further studies are needed to determine what factors are associated with quitting success among patch users.

Actuarial Analysis↗
PubMed1996

Effects of transdermal nicotine on lower esophageal sphincter and esophageal motility.

Cigarette smoking has been shown to decrease lower esophageal sphincter pressure (LESP) by 19-42%. This decrease in LESP may be due to nicotine in the cigarette smoke or substances other than nicotine. The aim of this study was to evaluate the effects of a nicotine patch on esophageal motility since nicotine patches are devoid of all toxins present in the cigarette smoke except the nicotine. Ten healthy nonsmoking volunteers underwent baseline esophageal manometry. Esophageal manometry was repeated after placing a nicotine transdermal patch (Nicotrol) designed to deliver 15 mg of nicotine per day. The parameters that were compared included LESP by rapid pull-through (LESP-RPT) and station pull-through (LESP-SPT), LES relaxation, and velocity, amplitude, and duration of esophageal contractions. Plasma nicotine and cotinine levels were measured prior to baseline manometry and after 12 hr of placing the nicotine patch, the LESP-RPT decreased by 31% from 17.4 +/- 6.1 to 12.1 +/- 3.3 (P = 0.013) and the LESP-SPT by 27% from 13.4 +/- 5.4 to 9.8 +/- 4.8 (P = 0.029) after the nicotine patch. LES relaxation was present in 100% before and after nicotine patch. There were no significant differences in velocity, duration, and amplitude of esophageal contractions after the nicotine patch. Plasma nicotine and cotinine was absent in all subjects at baseline but was significantly elevated after 12 hr of nicotine patch. Transdermal delivery of nicotine results in a significant reduction in LESP in healthy subjects without effecting LES relaxation or esophageal body motility.

Administration, Cutaneous↗
PubMed1986

The effects of transdermal scopolamine and four dose levels of oral scopolamine (0.15, 0.3, 0.6, and 1.2 mg) upon psychological performance.

Four dose levels of oral scopolamine (0.15 mg, 0.3 mg, 0.6 mg, 1,2 mg), transdermal scopolamine, and placebo, were investigated for their effects upon a battery of psychological performance measures in normal subjects. Oral scopolamine produced significant linear dose-related decrements on tasks involving continuous attention, continuous performance, memory storage for new information, and on self-rated feelings of alertness and sociability. Transdermal scopolamine produced significant performance impairments on these same assessment measures. Resting heart rate levels were significantly reduced by all scopolamine conditions. Side effects (dry mouth, dizziness) were frequent following transdermal scopolamine and the higher oral dose conditions. The overall effects of the transdermal scopolamine patch were broadly equivalent to the effects of 0.8 mg oral scopolamine. This oral dose equivalence for transdermal scopolamine is higher than expected, and possible reasons for this are discussed.

Administration, Oral↗
PubMed2002

Evidence that transient nicotine lowers the body weight set point.

OBJECTIVE: Smokers usually gain weight when they quit smoking. The present work explores the hypothesis according to which such a rise is a behavioral response to a raised body weight set point taking place when nicotine is eliminated from the body. RESEARCH METHODS AND PROCEDURES: The human body weight set point was assessed with classical behavioral and psychophysical methods, from the delay to experience negative alliesthesia when repeatedly ingesting sweet stimuli. Seven habitual smokers were tested once before lunch, after smoking (nonabstinent) as usual and once again after refraining from smoking (abstinent). Three additional nicotine-naive subjects were tested under the same procedure after receiving at 0730 h in the morning a transdermal nicotine patch (14 mg) or a placebo patch. Two of the subjects also received nicotine (7 mg) for a third session. RESULTS: Oral and transdermal administration of nicotine did not decrease the initial pleasure or modify the initial palatability of eating sweet stimuli, but significantly accelerated the following onset of self-reported displeasure (negative alliesthesia) aroused by repeated ingestion of sweet stimuli. DISCUSSION: These results are understood as an acute lowering of the body weight set point by nicotine. The body weight gain taking place after quitting smoking may, therefore, be explained by the removal of the lowering of the body weight set point induced by nicotine.

Administration, Cutaneous↗
PubMed2006

[A case of long-term, high-dose transdermal fentanyl application for lung cancer pain].

Transdermal fentanyl patch represents a new administration route for cancer pain relief. We reported here a successful experience with a high-dose of transdermal fentanyl for cancer pain therapy. A 71-year-old woman suffering from metastatic lung cancer to bone had already been treated with radiation at a different hospital. She suffered from severe lumbar pain upon admission to our hospital. During the past 15 months, she has been treated with 30 mg or more of transdermal fentanyl for cancer pain relief. No severe side effects were observed, and she experienced a better quality of life at home using this patch long-term.

Administration, Cutaneous↗
PubMed2006

[Transdermal buprenorphine during pregnancy].

Buprenorphine has been widely used and studied for over 20 years and has been shown to be an effective opioid analgesic. Some years ago a buprenorphine formulation for transdermal therapy of chronic cancer-related and non-cancer-related pain became available. We report the case of a woman who received a lower dosed transdermal buprenorphine patch (3/5 of a 35 microg/h patch corresponding to release of 21 microg/h buprenorphine) during pregnancy without any complication for herself or the child. The patient has now being using the transdermal system for more than 2 years and has reported continuous excellent pain relief. The buprenorphine patch was well tolerated and produced no effect on vigilance over the whole period of administration.

Administration, Cutaneous↗
PubMed2005

Effect of exercise on transdermal nicotine release in healthy habitual smokers.

OBJECTIVE: Transdermal nicotine patches have become a frequently prescribed tool in smoking cessation programs during the past years. However, there is circumstantial evidence that transdermal nicotine release substantially varies with physical activity producing toxic plasma concentrations that may account for severe adverse events. METHODS: We, therefore, compared nicotine release from two different transdermal nicotine systems (TDNS) at rest and during strenuous physical activity in a two-period crossover study in healthy smokers (n = 10). The subjects were randomly assigned to receive either 21 mg/day of formulation A or B on study Day 1 and 2. Patches were applied eight hours before starting standardized physical activity, and nicotine concentrations were measured in plasma and topically in the tissue layers underneath the application site by microdialysis. RESULTS: There was no difference between groups in the mean values for area under the time-concentration curve at rest from 0 - 8 hours AUC(0-8) (p < 0.799) and during exercise from 8 - 11 hours AUC(8-11) (p < 0.878). C(max) values between groups with C(max) values of 16.4 +/- 9.5 ng/ml and 16.0 +/- 10.7 ng/ml at rest (p < 0.919, NS) and 10.05 +/- 6.8 ng/ml and 10.2 +/- 6.9 ng/ml (p < 0.959, NS) during exercise did not differ significantly. Nicotine tissue concentrations increased two-fold during exercise versus baseline (p < 0.878). Skin blood flow increased significantly during exercise compared with baseline (p < 0.001). No adverse events were observed. CONCLUSION: The present study provides evidence that transdermal nicotine release from TDNS increases during exercise. However, this increase has no significant effect on overall plasma pharmacokinetics. Our pharmacokinetic data further indicate that the two TDNS formulations are equivalent during conditions of rest and exercise.

Administration, Cutaneous↗
PubMed1991

Gonadotropin dynamics in women receiving immediate or delayed transdermal estradiol after oophorectomy.

A prospective study was performed in 24 premenopausal women to evaluate the gonadotropin dynamics of pharmacologic doses of transdermal estradiol-17 beta (E2) administered after bilateral oophorectomy. Patients were given 0.2-mg transdermal E2 patches for 2 weeks, followed by 0.1-mg patches for 4 weeks either immediately postoperatively (immediate estrogen replacement therapy [ERT]) or beginning 12-14 days after surgery (delayed ERT). Serum gonadotropins and E2 levels were measured serially, and postmenopausal symptoms were prospectively recorded. Administration of 0.2 mg transdermal E2 immediately after surgery suppressed the post-castration rise in gonadotropins for at least 4 days, but LH and FSH levels did increase to the menopausal range after 2 weeks despite continued therapy. Sustained circulating levels of E2 with transdermal E2 therapy were comparable to follicular phase values. Vasomotor symptoms were well controlled by 0.2 mg of transdermal E2 in the majority of patients during the clinical trial. There was no significant estrogen-related morbidity despite the large doses used. Two patients had skin irritation at the patch site causing discontinuation of therapy. These data suggest that large doses of transdermal E2 can suppress gonadotropin levels only for a brief interval. We were unable to demonstrate any long-term alteration in the hypothalamic-pituitary set point for sensitivity to exogenous E2.

Administration, Cutaneous↗
PubMed1994

[Does estradiol modify the NO/cGMP system of blood vessels? Studies of the mechanism of cardiovascular protection by estrogen substitution in the postmenopausal period].

The effect of estradiol on the vasodilating NO/cGMP-system has been investigated in vitro and in vivo. Measurements of cGMP were carried out, cGMP values reflecting NO production. The incubation of human leg vein homogenates (n = 15) for 15 min. with estradiol in the concentrations 10(-6) M, 10(-7) M and 10(-8) M showed at 10(-8) a slight increase of the cGMP-concentrations. Due to high variation compass the difference to the control value was not statistically significant. The clinical part of the study included postmenopausal women, 20 were treated with transdermal estradiol patches (TTS, 0.05 mg/die) and 20 with estradiolvalerate orally (2 mg/die). There were 3 drop outs, 1 in the transdermal estrogen group, 2 in the oral estrogen group. In both groups there were no considerable differences in urinary cGMP concentrations. Thus, these results didn't clearly indicate an involvement of the NO/cGMP-system in the cardioprotective effect of an estrogen substitution therapy in postmenopausal women. Since former investigations are indicative of complex interactions of different vasoactive systems and of the requirement of longer treatment periods for an action of estradiol, an effect on the NO/cGMP-system cannot be ruled out.

Administration, Cutaneous↗
PubMed1997

Effects of acute administration of transdermal estrogen on postmenopausal women with systemic hypertension.

We studied 16 postmenopausal women with mild to moderate hypertension according to a randomized, double-blind protocol. They received patches of transdermal estradiol-17beta rated to deliver 100 mg/day of substance or matched placebo. A 24-hour ambulatory blood pressure (BP) monitoring was performed at baseline and after drug administrations. Our data show that estradiol-17beta exerts beneficial effects, both in lowering elevated BP levels and in maintaining a uniform BP control over 24 hours. Estrogen replacement therapy could be considered when significant changes in BP occur during the postmenopausal period.

Administration, Cutaneous↗
PubMed2002

Early emotional disturbances during nicotine patch therapy in subjects with and without a history of depression.

BACKGROUND: The goal of this study was to compare development of emotional symptomatology during smoking cessation with transdermal nicotine patches in subjects with and without a history of depression. METHODS: Twenty-five subjects, 14 with a history of depression and 11 without such a history, were evaluated before beginning of cessation, on day 8, day 30, day 90 and day 120. RESULTS AND DISCUSSION: On day 120, ten subjects have maintained abstinence: 71.4% of subjects with and 45.5% of subjects without a history of depression relapsed. Both groups presented variable emotional symptomatology and there was no significant differences between subjects with and without a past depression. On the other hand, none of the symptoms which emerged during cessation predicted the issue of cessation. However, some symptoms appearing before beginning of cessation were related to subsequent relapse: lack of pleasure seeking and tiredness. Subsequent relapsers also tended to be more tense on baseline. These early symptoms can not be considered as withdrawal symptoms, they may reflect less confidence in success. It is also suggested that development of anhedonia represents an adaptative strategy to prepare for the withdrawal suffering.

Administration, Cutaneous↗
PubMed2001

Nitroglycerin induces late preconditioning against myocardial infarction in conscious rabbits despite development of nitrate tolerance.

BACKGROUND: Recent studies suggest that the late phase of ischemic preconditioning (PC) can be mimicked by pretreatment with NO donors. The ability of clinically relevant NO donors to induce PC against infarction, however, has not been evaluated. Furthermore, it is unknown whether tolerance to the hemodynamic actions of nitrates also extends to their PC effects. METHODS AND RESULTS: Conscious rabbits underwent a 30-minute coronary occlusion and 3 days of reperfusion. A 60-minute intravenous (IV) infusion of nitroglycerin (NTG) ending 1 hour before occlusion reduced infarct size, indicating an early PC effect. When the time interval between NTG infusion and occlusion was extended to 24 or 72 hours, the infarct-sparing action of NTG became even more pronounced, indicating a robust late PC effect. Transdermal NTG patches elicited a late PC effect that was (1) equivalent to that induced by IV NTG, demonstrating the efficacy of transdermal NTG as an alternative form of NTG delivery for inducing late PC, and (2) similar in nitrate-tolerant and -nontolerant rabbits, demonstrating that tolerance does not extend to the PC effects of NTG. CONCLUSIONS: In conscious rabbits, administration of NTG via either the IV or the transdermal route elicits a robust protective effect against infarction that lasts for 72 hours. The magnitude of NTG-induced cardioprotection is equivalent to that observed during the late phase of ischemic PC and is not affected by the development of tolerance. These findings reveal a new action of nitrates and support novel applications of these drugs for protecting the ischemic myocardium in patients.

Administration, Cutaneous↗
PubMed1985

Delayed hypersensitivity to scopolamine delivered by a transdermal device.

Transdermal devices are now marketed for the delivery of systemic medications through the skin. This report confirms delayed hypersensitivity to scopolamine, the active ingredient in Transderm-Scop. Patch testing with structurally related alkaloids suggests the active antigenic site on the scopolamine molecule. The mechanism of drug delivery by the transdermal device is discussed, along with the features that make this an attractive method of drug administration. Dermatologists should be familiar with these devices, since broader future applications can be expected.

Drug Eruptions↗