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PubMed1993

The pharmacokinetics of the beta 2-adrenoceptor agonist, tulobuterol, given transdermally and by inhalation.

We have studied the pharmacokinetics of tulobuterol given transdermally or by aerosol inhalation in healthy male volunteers. Tulobuterol was rapidly absorbed after inhalation, with a tmax of 0.8-1.5 h. The Cmax and the AUC increased linearly with dose. Tulobuterol was well absorbed after transdermal administration, with an absorption lag-time of about 4 h. The Cmax and AUC increased linearly with dose and the tmax was about 9-12 h. The mean percentage of drug absorbed during the application of a patch for 24 h was 82-90% after a single dose and 82-85% during repeated dosing. The mean urinary recoveries as unchanged drug after a single inhalation and patch application were 3-4% and 5-6% respectively. Tulobuterol did not accumulate during repeated inhalation or transdermal application. It was well tolerated, except for an increase in heart rate of 10-20 beats.min-1 after five repeated applications of a 4 mg patch.

Administration, Cutaneous↗
PubMed1989

Intermittent transdermal nitroglycerin monotherapy in stable exercise-induced angina: a comparison with a continuous schedule.

The aim of this study was to investigate nitrate tolerance during continuous treatment with nitroglycerin patches (NTG) as monotherapy, and to assess whether tolerance might be prevented by an overnight nitrate-free interval. Ten male patients, of mean age 53.2 years (range 41-62 years), with pathological coronary angiography and stable exercise-induced angina pectoris took part in a double-blind crossover study (two 15-day periods), during which the continuous and intermittent (12-h nitrate-free interval) application of NTG 20 mg (24 h)-1 patches were compared. Single-blind placebo was given acutely before and at the end of the crossover. Exercise testing was performed on a treadmill according to the Bruce protocol 4 and 12 h after dosing, both during placebo and at the end of the two active treatment periods. In comparison with continuous treatment, the intermittent administration of 20 mg (24 h)-1 NTG patches significantly increased ischaemic threshold and total work time at the 4th and the 12th hour. Night-time withdrawal of NTG transdermal delivery systems determined during the 15-day period a total of 11 night anginal attacks in six out of 10 patients (0.07 attacks per patient per nitrate-free interval).

Administration, Cutaneous↗
PubMed1999

The smoking cessation efficacy of varying doses of nicotine patch delivery systems 4 to 5 years post-quit day.

BACKGROUND: This study was undertaken to evaluate the long-term smoking cessation efficacy of varying doses of transdermal nicotine delivery systems 4 to 5 years post-quit day. METHODS: A follow-up study was conducted 48 to 62 months after quit day among patients who were enrolled in the Transdermal Nicotine Study Group investigation. The latter study included group smoking cessation counseling and randomized assignment to 21, 14, or 7 mg nicotine patches or placebo patches. Seven of nine smoking cessation research centers participated in the long term follow-up investigation. RESULTS: The self-reported continuous quit rate among patients originally assigned 21 mg (20.2%) was significantly higher than rates for patients assigned 14 mg (10.4%), 7 mg (11.8%), or placebo patches (7.4%). Log rank survival analysis found no difference in relapse rates after 1 year postcessation. Smokers under age 30 years were significantly less likely to be abstinent at long term follow-up compared to smokers > or = 30 years of age (3 vs 13%, respectively). Mean weight gain in confirmed continuous quitters was 10.1 kg in men and 8.0 kg in women. Of the 63 continuous abstainers surveyed, 30 respondents (48%) reported that they no longer craved cigarettes, and no individual reported daily craving for cigarettes. CONCLUSIONS: Nicotine patch therapy with 21 mg/day patches resulted in a significantly higher long-term continuous abstinence rate compared to lower dose patches and placebo. Relapse rates among the various treatment conditions were similar after 1 year postcessation.

Administration, Cutaneous↗
PubMed2000

Transdermal estrogen in the treatment of hot flushes in men with prostate cancer.

OBJECTIVES: To assess the effectiveness and tolerability of transdermal estrogen in men with hot flushes after hormonal therapy for prostate cancer. METHODS: Twelve men with moderate to severe hot flushes were randomized to receive either low-dose (0.05 mg) or high-dose (0.10 mg) estrogen patches applied twice weekly for 4 weeks. After a 4-week washout period in which no treatment was given, each patient received the alternative dose for 4 weeks. Treatment response was assessed by daily logs and questionnaires completed every 4 weeks that included a visual analog assessment. Serum luteinizing hormone, follicle-stimulating hormone, testosterone, and estradiol levels were also measured every 4 weeks during the study. RESULTS: There was a significant reduction in the overall severity of the hot flushes seen in patients with both the low and high-dose estrogen patch. A significant reduction in the daily frequency of the hot flushes was seen with the high-dose patch only. Overall, 10 (83%) of 12 men reported either mild, moderate, or major improvement in symptoms with either the low or high-dose patch. Mild, painless breast swelling or nipple tenderness was noted in 2 (17%) and 5 (42%) of 12 men treated with the low and high-dose estrogen patch, respectively. FSH levels decreased significantly with both the low and high-dose patch. Estradiol levels increased from 12.1 to 16.4 pg/mL and 26.9 pg/mL with the low and high-dose patch, respectively. There was no significant change in serum testosterone or luteinizing hormone levels. CONCLUSIONS: Transdermal estrogen appears to be a promising, well-tolerated therapy for men with hot flushes after endocrine treatment for prostate cancer. Further study in larger groups of patients is necessary to assess the relative effectiveness and morbidity of this treatment.

Administration, Cutaneous↗
PubMed1996

Effect of low doses of scopolamine on RR interval variability, baroreflex sensitivity, and exercise performance in patients with chronic heart failure.

OBJECTIVE: To study the effect of transdermal scopolamine on heart rate variability, baroreflex sensitivity, and exercise performance in patients with heart failure and age matched healthy volunteers. DESIGN: Double blind, randomised, placebo controlled, crossover study. PATIENTS: 16 patients with chronic, stable heart failure due to ischaemic cardiomyopathy (mean (SEM) age 58 (2) years; mean (SEM) radionuclide left ventricular ejection fraction 28 (2)%; New York Heart Association class II-III) and eight age matched healthy controls. INTERVENTION: Transdermal scopolamine (500 micrograms delivered over 72 h) or a placebo patch was administered for 48 h. MAIN OUTCOME MEASURES: Indices of tonic and reflex cardiac vagal activity and exercise performance. RESULTS: In both groups scopolamine produced a reduction in the 24 h average heart rate and an increase in the time domain measures of heart rate variability. Both the incidence and severity of ventricular arrhythmias remained unchanged. Baroreflex sensitivity, evaluated by the phenylephrine technique, increased significantly (P < 0.001) with scopolamine in patients with heart failure (6.22 (2.81) ms/mm Hg) and in healthy volunteers (5.97 (2.20) ms/mm Hg) as did the amplitude of respiratory sinus arrhythmia, computed by autoregressive spectral analysis of 10 min electrocardiographic recordings (319.9 (123.5) and 657.3 (126.6) ms2 respectively, P < 0.001). While exercise performance did not change, heart rate at submaximal exercise was significantly reduced by scopolamine in each group. CONCLUSIONS: In patients with mild to moderate heart failure low doses of scopolamine increased tonic and reflex cardiac vagal activity. This was achieved without affecting exercise tolerance or the incidence and severity of ventricular arrhythmias.

Baroreflex↗
PubMed1993

Is sexual life influenced by transdermal estrogen therapy? A double blind placebo controlled study in postmenopausal women.

Two hundred and forty-two postmenopausal women between 45 and 65 years of age requiring hormone replacement therapy for climacteric symptoms were blindly and randomly allocated to treatment either with transdermal estradiol therapy (Estraderm 50 micrograms/24h) (E) or placebo (P). The patches were changed twice a week and treatment continued for 12 weeks. No progestogen supplement therapy was given during the study. No previous hormone replacement therapy had been given for the last six months and the women had had their last menstruation more than six months ago. As a part of a larger study assessing women's quality of life, a Swedish version of 'McCoy's Sex Scale Questionnaire' was administered at the start of treatment and after 12 weeks. This questionnaire contains nine items regarding different aspects of sexual life. The difference between the scorings at the start of treatment and after 12 weeks were calculated for each item and the values of the E and the P groups were compared. Items regarding 'satisfaction with frequency of sexual activity, sexual fantasies, degree of enjoyment, vaginal lubrication and pain during intercourse' were positively influenced in the E group compared to the P group. Items not affected were 'frequency of orgasm and sexual arousal'. A correlation between improved sexual life and quality of life was also found when the results from the McCoy scale were compared with a battery of quality of life questionnaires.

Administration, Cutaneous↗
PubMed1998

Weight change after smoking cessation using variable doses of transdermal nicotine replacement.

OBJECTIVE: Examine weight change in subjects receiving variable doses of transdermal nicotine replacement for smoking cessation. DESIGN: Randomized, double-blind clinical trial. SETTING: One-week inpatient treatment with outpatient follow-up through 1 year. INTERVENTION: This report examines weight change after smoking cessation for 70 subjects randomized to placebo or to 11, 22, or 44 mg/d doses of transdermal nicotine. The study included 1 week of intensive inpatient treatment for nicotine dependence with active patch therapy continuing for another 7 weeks. Counseling sessions were provided weekly for the 8 weeks of patch therapy and with long-term follow-up visits at 3, 6, 9, and 12 months. MEASUREMENTS AND MAIN RESULTS: Forty-two subjects were confirmed biochemically (i.e., by expired carbon monoxide) to be nonsmokers at all weekly visits during patch therapy. Their 8-week weight change from baseline was 3.0 +/- 2.0 kg. For these subjects, 8-week weight change was found to be negatively correlated with percentage of cotinine replacement (r = -.38, p = .012) and positively correlated with baseline weight (r = .48, p = .001), and age (r = .35, p = .025). Men had higher (p = .003) 8-week weight gain (4.0 +/- 1.8 kg) than women (2.1 +/- 1.7 kg). Of the 21 subjects who abstained continuously for the entire year, 20 had their weight measured at 1-year follow-up. Among these 20 subjects, 1-year weight change was not found to be associated with gender, baseline weight, baseline smoking rate, total dose of transdermal nicotine, or average percentage of cotinine replacement during the 8 weeks of patch therapy. CONCLUSIONS: This study suggests that higher replacement levels of nicotine may delay postcessation weight gain. This effect is consistent for both men and women. We could not identify any factors that predict weight change with long-term abstinence from smoking.

Administration, Cutaneous↗
PubMed2006

In vitro and in vivo evaluation of the transdermal iontophoretic delivery of sumatriptan succinate.

The objective was to evaluate the transdermal delivery of the 5-HT(1B/1D) agonist, sumatriptan from an iontophoretic patch system, in vivo. Initial in vitro experiments were conducted to optimize formulation parameters prior to iontophoretic delivery in Yorkshire swine. It was found in vitro that increasing drug load in the patch from 9.7 to 39 mg had no statistically significant effect on cumulative delivery (cf. 305.6+/-172.4 vs. 389.4+/-80.4 microg cm(-2), respectively). However, for a given drug load (39 mg) increasing formulation pH from pH 4.7 to 6.8 significantly increased the cumulative amount of sumatriptan delivered across the skin (389.4+/-80.4 vs. 652.4+/-94.2 microg cm(-2)). A biphasic current profile comprising intensities of 1.8 mA from t=0 to t=180 min and 0.8 mA from t=181 min to t=360 min was used for the in vivo experiments. Drug levels in the blood were 13.7+/-4.5 and 53.6+/-10.2 ng ml(-1) at the 30 and 60 min time-points, rising to 90-100 ng ml(-1) during the 90-180 min time-period. The in vivo results show that the pharmacokinetics following transdermal iontophoretic delivery are comparable to those after oral, nasal or rectal administration, but do not match those upon subcutaneous injection.

Administration, Cutaneous↗
PubMed2000

Serum leptin levels and body weight in postmenopausal women under transdermal hormone replacement therapy.

Leptin, the adipocyte-specific product of the ob gene, is implicated in body weight regulation and energy balance. We investigated the influence of hormone replacement therapy (HRT) on the body mass index (BMI) and serum leptin levels in 20 postmenopausal, nonobese women treated with transdermal HRT (delivery rate 50 microg 17beta-estradiol/24 h, 1 patch per week) for 6 months. Serum leptin levels were measured by ELISA and results were compared by means of the Student's paired t-test or Pearson's correlation. The mean patient age was 55+/-6.04 years. The mean body weight prior to the start of the study was 69.39+/-9.37 kg, and the BMI before HRT was 26.92+/-4.47 kg/m2. Both parameters remained unchanged under therapy. No significant change in absolute serum leptin values (18.8+/-8.4 ng/ml; 20.47+/-9.7 ng/ml; 17.92+/-8.7 ng/ml at 0, 4 and 6 months respectively) or in adiposity-corrected values (serum leptin/BMI) (0.68+/-0.24; 0.75+/-0.29; 0.67+/-0.26 at 0, 4 and 6 months respectively) were found. Serum leptin levels correlated well with BMI (r = 0.7193, p<0.0001). There was no significant correlation of estradiol with serum leptin levels before or during therapy. In summary, low dose, transdermal HRT exhibited no influence on serum leptin levels or BMI in postmenopausal women. These data suggest that low dose HRT does not influence body weight regulation in postmenopausal women.

Administration, Cutaneous↗
PubMed2001

Transdermal contraception.

This review summarizes the clinical studies involving the once-weekly Ortho Evra/Evra contraceptive patch. The patch delivers norelgestromin (NGMN), 150 microg, and ethinyl estradiol (EE), 20 microg, daily to the systemic circulation. The contraceptive patch provided ovulation suppression and cycle control similar to that of oral norgestimate 250 microg/EE 35 microg, significantly decreased mean maximum follicular diameter following a 3-day intentional delayed dosing phase when compared with oral levonorgestrel (LNG) 50/75/125 microg/EE 30/40/30 micorg and oral LNG 100 microg/EE 20 microg, and was as effective as oral LNG 50/75/125 microg/EE 30/40/30 microg and oral desogestrel 150 microg/EE 20 microg in altering cervical mucus composition (i.e., creating a scanty, viscous consistency). The contraceptive patch provided efficacy, cycle control, and safety comparable to that seen with oral LNG 50/75/125 microg/EE 30/40/30 microg, but women were able to correctly follow the weekly dosing regimen significantly more often than the daily oral contraceptive dosing regimen. Less than 2% of patches were replaced because of complete detachment in these trials. The patch was not associated with phototoxicity or photoallergy. The contraceptive patch, the only noninvasive, weekly birth control method that a woman can self-administer, will be a valuable addition to current contraceptive options.

Administration, Cutaneous↗
PubMed2002

Vaginal micronized progesterone in continuous hormone replacement therapy. A prospective randomized study.

BACKGROUND: In the non-hysterectomized post-menopausal woman undergoing estrogen replacement therapy, the co-administration of a progestogen is mandatory to counteract the estrogenic proliferative effect on the endometrium. Metabolic and tissue effects of the various progestins vary with dosage and route of administration. This study was performed to evaluate the effects of selected progestins on the lipidic profile and endometrial morphology. METHODS: This is a prospective randomised study including 60 post-menopausal women undergoing hormonal replacement therapy (HRT). All patients received transdermic ethinil-estradiol in a continuous schedule. The utilized progestogens were: medroxyprogesterone acetate (MPA) 10 mg p.o. 12 days/month, transdermic nor-ethisterone acetate (NETA) 0.25 mg integrated in the ethinil-estradiol patches for the last two weeks of each cycle, micronized progesterone (MP) 100 mg transvaginally 12 days/month. RESULTS: None of the tested protocols significantly altered the lipidic profile of this group of patients. We noticed different effects on the estrogen stimulated endometrium elicited by the different progestinic regimens. While the cyclic administration of oral MPA or transdermic NETA more frequently resulted in endometrial atrophy, the trans-vaginal administration of MP more often induced (p<0.005 at six-month and p <0.001 after 1 year) a functional-like secretive endometrium. CONCLUSIONS: Micronized progesterone, cyclically administered in the form of a vaginal cream, offers an acceptable and effective alternative for women on continuous HRT wishing to maintain their monthly cycle.

Administration, Intravaginal↗
PubMed1999

A randomized comparison of continuous combined transdermal delivery of estradiol-norethindrone acetate and estradiol alone for menopause. CombiPatch Study Group.

OBJECTIVE: To determine whether a continuous estradiol-norethindrone acetate transdermal delivery system reduces incidence of endometrial hyperplasia in postmenopausal women more than transdermal estradiol (E2) alone. METHODS: Six hundred twenty-five postmenopausal women were assigned randomly to one of four treatments, transdermal E2 50 microg/day, or transdermal E2-norethindrone acetate with 50 microg E2 and 140, 250, or 400 microg/day of norethindrone acetate. Follow-up visits to collect information on safety and efficacy were scheduled at 3, 6, 9, and 12 months after initiation of treatment. Endometrial biopsy for histologic evaluation was done at baseline and upon exit from the study (completion or withdrawal). Endometrial histology was evaluated by two independent gynecologic pathologists. In the event of a disparate reading, a third gynecologic pathologist evaluated the tissue using predetermined criteria. RESULTS: Endometrial hyperplasia was found in 37.9% (39 of 103) in the E2 alone group versus 0.8% (one of 123), 1% (one of 98), and 1.1% (one of 89) in the E2-norethindrone acetate 50-140, 50-250, and 50-400 groups, respectively (P < .001). Uterine bleeding was less frequent in the E2-norethindrone acetate 50-140 group than other treatments. The mean number of hot flushes per day decreased to less than one in each treatment group at endpoint. The E2-norethindrone acetate combination patch showed skin tolerance comparable to that of E2 alone. CONCLUSION: Continuous transdermal delivery of E2 combined with norethindrone acetate effectively prevented endometrial hyperplasia in healthy postmenopausal women. Continuous combined transdermal delivery systems provide increased dosing flexibility and might improve convenience and compliance with hormone replacement therapy.

Administration, Cutaneous↗
PubMed1993

Saliva nicotine as an index of plasma levels in nicotine skin patch users.

This study examined whether salivary nicotine concentrations would provide a useful index of plasma concentrations in studies of the effects of transdermal nicotine administration. Twenty-four subject smokers abstained from smoking for 12 h prior to admission to a clinical research unit ward and for 36 h while remaining confined to the ward. Three doses of nicotine skin patches were applied to different groups of subjects, and blood and saliva samples were collected at several time points. Saliva flow was stimulated by three different methods: (a) sucking on a lemon candy, (b) dissolving a sugar cube in the mouth, and (c) chewing on parafilm. Nicotine and cotinine concentrations were measured in both saliva and blood using gas chromatography. There was a high correlation between blood and saliva values of nicotine (r = 0.82). Overall, saliva nicotine concentrations were approximately 8.1 times higher than those of plasma. Saliva and blood cotinine concentrations were also highly correlated (r = 0.94), replicating results of previous studies. Results suggest that saliva nicotine may be a useful marker of nicotine intake during nicotine skin patch treatment. Saliva collection may be advantageous under conditions in which blood collection is impractical and may provide greater sensitivity because of the high concentration of nicotine in saliva relative to that in blood.

Administration, Cutaneous↗
PubMed1997

The effect of hormone replacement therapy on the oxidation of low density lipoprotein in postmenopausal women.

The oxidative modification of low density lipoprotein (LDL) is important in the pathogenesis of atherosclerosis, and oestrogen has been shown to inhibit copper and cell mediated oxidation of LDL in vitro. We have investigated the effect of oral and transdermal oestrogens (oestradiol valerate 1 mg, conjugated equine oestrogens 0.625 mg and patches releasing 50 microg oestradiol daily), oestrogen implants (oestradiol 50 mg) and oral combined oestrogen and progestogen (oestradiol valerate 2 mg with medroxyprogesterone acetate 5 mg and oestradiol valerate 2 mg with norethisterone acetate 1 mg), on the susceptibility of LDL to oxidation in postmenopausal women (total n = 56). Oxidation of LDL was initiated by the addition of copper ions, and monitored by measurement of conjugated dienes. Changes in fasting serum levels of total cholesterol, LDL, HDL and triglycerides were also evaluated, as were changes in LDL composition. Total cholesterol decreased by 5.5% (P < 0.05) with CEE, 6.8% with oestradiol implants (P < 0.05), 9.3% with oestradiol + MPA (P < 0.01) and 10% with oestradiol + norethisterone (P < 0.05). There were reductions in LDL with oral oestradiol valerate (7.8%) (P < 0.05), CEE (13.8%) (P < 0.01) and oestradiol combined with MPA (12.7%) (P < 0.05). HDL increased by 7.1% (P < 0.01) and 6.3% (P < 0.05), with oestradiol valerate and CEE respectively, and decreased by 9% (P < 0.05) with implants and by 14.7% with oestradiol combined with norethisterone (P < 0.01). Triglycerides were significantly increased with CEE (14.9%) and reduced with oestradiol implants (15.2%) (both P < 0.05). While there was no change in the ratio of 'cholesterol ester' to 'free cholesterol' within LDL with any of the HRT preparations, a reduction in total cholesterol and cholesterol ester content of LDL occurred with transdermal oestradiol and a reduction in free cholesterol occurred with oestradiol plus MPA. Although we found a small but significant decrease in plasma hydroperoxide concentration four weeks after insertion of the oestradiol implant from 1.17 +/- 0.06 to 1.03 +/- 0.04 micromol/l (P < 0.05), we found no significant change in the lag time to oxidation, or in the maximum rate of propagation of the reaction, after treatment with any of the above forms of hormone replacement therapy. This study does not therefore support the role of oestrogens as antioxidants in vivo.

Administration, Cutaneous↗
PubMed1991

Adverse skin reactions to nicotine in a transdermal therapeutic system.

Nicotine in a transdermal therapeutic system (TTS) has been introduced recently to help people to stop smoking. 14 volunteers (10 male, 4 female) with a history of former adverse skin reactions to this device were investigated. Skin tests for contact urticaria and patch tests for contact allergy were done with the individual components of the TTS. Contact sensitization to nicotine was identified in 5 and to the TTS itself in 1 individual. Irritant reactions due to occlusion were present in 9 subjects. The optimal test agent and concentration for elucidating the adverse skin reaction was an aqueous solution of 10% nicotine base. Atopy, as diagnosed by history and skin prick tests to common inhalant allergens, and contact sensitization to standard patch test allergens, were each identified in 6 subjects. Nicotine should be added to the expanding list of transdermally delivered drugs which may elicit contact dermatitis.

Administration, Cutaneous↗
PubMed2006

Long-term management of chronic pain with transdermal buprenorphine: a multicenter, open-label, follow-up study in patients from three short-term clinical trials.

BACKGROUND: Transdermal buprenorphine is available in Europe for the treatment of moderate to severe chronic pain. It has been evaluated at doses of 35, 52.5, and 70 microg/h for the management of moderate to severe chronic cancer and noncancer pain in 3 randomized, double-blind, placebo-controlled trials, each of limited duration (approximately 14 days each). Long-term data are essential to determining the performance of an analgesic in the management of chronic pain. OBJECTIVE: The purpose of this follow-up study was to obtain data on the efficacy and tolerability of long-term treatment with transdermal buprenorphine in cancer and noncancer patients with chronic persistent pain of moderate to severe intensity. METHODS: This was an open-label, uncontrolled, follow-up study in patients from the 3 previous clinical trials who elected to continue treatment with transdermal buprenorphine 35 microg/h and sublingual buprenorphine tablets (0.2 mg) as needed for breakthrough pain. The patch was to be changed every 72 hours throughout the patient's course of pain therapy. At visits every 2 weeks for the first 4 weeks and every 4 weeks for the remainder of study participation, patients evaluated their pain relief retrospectively on a 4-point verbal rating scale. They also rated the ease of patch handling using a 3-point verbal rating scale. Patterns of dose escalation and dose stability were monitored over time. Adherence to therapy was determined based on the number of patients who complied with the dosing schedule. Adverse events were documented by type, intensity, location (systemic or local), and relationship to study medication. RESULTS: Two hundred thirty-nine patients were included in this follow-up study (120 women, 119 men; 100% white; mean [SD] age, 58 [11.3] years; mean weight, 70.8 [14.7] kg). One hundred thirty-four had cancer-related pain and 105 had pain of noncancerous origin. The mean duration of participation was 7.5 months, and 37 (15.5%) patients participated for >12 months. Maximum study participation was 3.4 years in cancer patients and 5.7 years in noncancer patients. One hundred eighty-eight (78.7%) patients were considered adherent to therapy. The majority (65.9%) of patients managed their pain with the patchalone or took no more than 1 additional sublingual tablet daily for breakthrough pain. At least satisfactory pain relief was reported by 215 (90.0%) patients, and the buprenorphine patch was generally well tolerated. The most common systemic adverse drug reactions were nausea (9.2%), dizziness (4.6%), vomiting (4.2%), constipation (3.8%), and tiredness (2.9%), whereas the most common local adverse drug reactions were erythema (12.1%), pruritus (10.5%), and exanthema (8.8%). CONCLUSION: Transdermal buprenorphine was generally well tolerated and effective for the long-term treatment of chronic cancer or noncancer pain in these patients who had previously received buprenorphine in 3 short-term clinical trials.

Administration, Cutaneous↗
PubMed2006

Is there a ceiling effect of transdermal buprenorphine? Preliminary data in cancer patients.

OBJECTIVE: The aim of this preliminary study was to explore the possibility of using higher doses of transdermal buprenorphine (TD-BUP) than those commonly used and available as manufactured patches, which are based on the assumption that BUP may have a ceiling effect that has never been determined yet. MATERIALS AND METHODS: Ten patients who were already receiving TD-BUP (70 microg/h, which is about 1.6 mg/day) and were no longer responsive to this dosage were administered higher doses up to a maximum of 140 microg/h within 6 days, when the study was completed. RESULTS: In six patients, dose increments of TD-BUP were effective, and patients achieved adequate analgesia within 6 days. Four patients discontinued the treatment due to inefficacy of TD-BUP 140 microg/h and were switched to other opioids until achieving stabilization (oxycodone 320 and 400 mg/day, methadone 120 mg/day, transdermal fentanyl 200 microg/h). This group of patients required higher doses than those chosen for TD-BUP, underlying the need to escalate the dose rapidly, a modality not accomplished with transdermal drugs. Adverse effects did not change and were similar to those observed before increasing the dose of TD-BUP. On the basis of these preliminary data, patients requiring doses higher than 70 microg/h of TD-BUP, in the range of 105-140 microg/h, may still have an analgesic benefit without important consequences in terms of adverse effects. It cannot be excluded that even higher doses may be effective, as some patients required rapid titration with higher morphine equivalent doses, and according to the protocol, other opioids were provided to facilitate this process. Further studies should clarify the role and the benefit of TD-BUP in specific clinical circumstances.

Administration, Cutaneous↗
PubMed2005

Transdermal clonidine: therapeutic considerations.

Transdermal clonidine was approved by the US Food and Drug Administration in 1984 for the treatment of mild-to-moderate hypertension alone or in combination with a diuretic. Clonidine is released from the patch at a constant rate and thus displays a pharmacokinetic pattern not dissimilar to that of infusion therapy. Transdermal clonidine, like oral clonidine, is effective first- or second-line therapy for most forms of hypertension. More recently, transdermal clonidine has found alternative uses in the areas of smoking cessation, posttraumatic stress disorder, menopausal hot flashes, and alcohol and opiate withdrawal syndromes. The not infrequent development of a dermatitis, together with a substantially greater cost than oral clonidine, have been the major undoings for transdermal clonidine.

Administration, Cutaneous↗