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PubMed2006

Is the use of transdermal fentanyl inappropriate according to the WHO guidelines and the EAPC recommendations? A study of cancer patients in Italy.

BACKGROUND: World Health Organization (WHO) guidelines, Agency for Health Care Policy and Research (AHCPR) clinical practice guidelines, and EAPC recommendations indicate oral route of opioid administration as the preferred route. Transdermal administration of opioids is considered an alternative when patients cannot take medications orally. Moreover, WHO and EAPC indicate orally administered morphine as the first-choice drug for the treatment of moderate to severe cancer-related pain. However, we can see that in Italy there is an increasing use of transdermal fentanyl (TF) as first-choice strong opioid (and route) even when oral administration of opioids is possible. AIMS: The aims of this study are to describe the modality in the use of TF administration in two settings of care, taking into consideration (1) the drugs previously taken by the patients, (2) the reasons for switching from any drug to TF, (3) the conversion ratio used, and (4) the frequency of "inappropriate use of transdermal fentanyl according to the WHO guidelines and the EAPC recommendations", i.e., switching to fentanyl patch from any drug, even if there were no contraindications in using oral morphine. The settings of care considered were the out-patient palliative care unit (OP-PCU) and the oncological wards (OWs) of the National Cancer Institute (NCI) of Milan. PATIENTS AND METHODS: The clinical charts of 98 patients prescribed with and given fentanyl patch for the first time at the NCI of Milan in 2002 were reviewed and the data gathered were grouped according to the administration of fentanyl at the OP-PCU (63 out-patients) or at the OWs (35 in-patients). Summary descriptive statistics and bar and box plots have been used. Fisher two-tailed exact text was applied to test the differences between in- and out-patients. RESULTS: Before switching to TF, (1) in-patients were more frequently treated with nonsteroidal anti-inflammatory drugs (NSAIDs) and weak opioids (mostly tramadol) in respect to the out-patients (44.1 vs 25.8%) who were mostly treated with oral morphine (48.4 vs 20.6%) (p=0.045), and (2) 88.7% of the out-patients were treated with oral opioids and only 1.6% with parenteral opioids in respect to OWs where 69.7% were on oral opioids and 18.2% on parenteral opioids (p=0.006). In 29% of out-patients and in 53% of in-patients, changing to fentanyl patch was considered as "inappropriate" (p=0.028) according to the WHO guidelines and the EAPC recommendations. No statistically significant differences between the two settings were observed regarding the reasons for switching and the conversion ratio used. CONCLUSIONS: There is a trend to use fentanyl patch as first-choice strong opioid in cancer patients in situations such as titration phase, in the presence of instable pain, and in the absence of dysphagia or gastrointestinal symptoms where the use of oral morphine is, however, not contraindicated.

Administration, Cutaneous↗
PubMedDate not supplied

Stereoselective metabolism of (S)-(-)-nicotine in humans: formation of trans-(S)-(-)-nicotine N-1'-oxide.

The chemical synthesis and chromatographic separation of cis- and trans-(S)-nicotine N-1'-oxide diastereomers have allowed the development of methods for the quantification of (S)-nicotine N-1'-oxides during in vitro and in vivo metabolic studies. The metabolism of (S)-nicotine was investigated in the presence of microsomes, cDNA-expressed and highly purified flavin-containing monooxygenase (FMO) from pig liver, human liver, and rabbit lung. For comparison, the N-1'-oxidation of (S)-nicotine in the presence of the cytochrome P450 2B1 from rat liver, cytochrome P450 2B10 from mouse liver, and cytochrome P450 4A2 from rabbit lung was examined. The ratio of trans:cis (S)-nicotine N-1'-oxide formation for pig liver FMO1 (form 1) was 57:43. In contrast, cDNA-expressed adult human liver FMO3 (form 3) and rabbit lung FMO2 formed solely trans-(S)-nicotine N-1'-oxide. Of the cytochrome P450 enzymes examined, formation of (S)-nicotine N-1'-oxide occurred with a mean trans:cis ratio of 82:18. The stereoselectivity of (S)-nicotine N-1'-oxide formation was investigated by examining the urine of 13 healthy male smokers studied on a protocol which included free-smoking, intravenous infusion of (S)-nicotine-d2 and dermal patch administration of (S)-nicotine-d0. During cigarette smoking or administration of intravenous or transdermal (S)-nicotine, only the trans diastereomer of (S)-nicotine N-1'-oxide was observed in the urine. That the trans-(S)-nicotine N-1'-oxide metabolite was not appreciably reduced or oxidized further was investigated with infusion studies of (S)-nicotine-d2N-1'-oxide.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed2002

Effects of sustained-release tulobuterol on asthma control and beta-adrenoceptor function.

1. Recently, a patch formulation of tulobuterol, a beta-adrenoceptor (AR) agonist, has been developed using a transdermal delivery system. The present study was designed to determine whether beta-AR function and asthma control were affected by the sustained-released beta-AR agonist. 2. Tulobuterol (2 mg) was applied daily for 8 weeks to seven patients with bronchial asthma in whom the morning dip in the peak expiratory flow (PEF) rate developed even though inhaled glucocorticoids were being taken. After treatment with tulobuterol, the early morning reduction in PEF was suppressed and PEF values were increased from 367 +/- 35 to 439 +/- 38 L/min (P < 0.05). The rescue use of inhaled beta-AR agonists was decreased from 6.9 +/- 2.0 to 1.0 +/- 0.7 puffs/week (P < 0.01). Symptom scores also decreased from 8.3 +/- 3.4 to 2.1 +/- 1.4 score/week (P < 0.01). 3. Next, we sought to examine the effects of exposure to tulobuterol on beta-AR function in guinea-pig tracheal smooth muscle. After exposure of tissues to tulobuterol (0.01-10 micro mol/L) for 45 min, the inhibitory effects of tulobuterol on methacholine-induced contractions were attenuated in a concentration-dependent manner. However, the inhibitory effects of tulobuterol were not affected after exposure to 0.01 micro mol/L tulobuterol (a concentration greater than serum levels in clinical use). In contrast, the inhibitory effects of procaterol were not affected after exposure to tulobuterol under the same experimental conditions. 4. These results indicate that the combination of sustained-released tulobuterol with inhaled glucocorticoid therapy is beneficial to patients with bronchial asthma who suffer from symptoms induced by the morning dip in PEF. Moreover, chronic exposure to lower concentrations of tulobuterol does not lead to desensitization of beta-AR in airway smooth muscle.

Adrenergic beta-Agonists↗
PubMed1990

A physiological mode of puberty induction in hypogonadal girls by low dose transdermal 17 beta-oestradiol.

Transdermal 17 beta-oestradiol administration (17 beta-E2), used mainly in menopausal women, allows a continuous 17 beta-E2 delivery through the skin into the systemic circulation, avoiding intestinal and hepatic passage. In order to explore whether transdermal 17 beta-E2 could be used for the induction of puberty, 17 beta-E2 patches with low dose delivery were administered in nine prepubertal girls with Turner syndrome (bone age greater than 10.5 years) for a mean period of 2.2 years. Treatment schedule: 5 micrograms/day for 6-9 months, 10 micrograms/day for 6-9 months, 25 micrograms/day for long-term substitution; addition of cyclic gestagen p.o. after 18-24 months. Breast development started within 3 months of therapy and menstruation occurred after 2 years. Growth rate increased from 3.2 to 5.0 cm/year during the 1st year of therapy, height prediction did not change. Serum oestradiol (E2) and urinary E2 conjugates increased proportionally with 17 beta-E2 doses, serum oestrone (E1) rose much less. The possibility to imitate time course, clinical events and hormonal changes of normal puberty, the absence of adverse drug reactions and the excellent acceptance and easy mode of application suggest that transdermal 17 beta-E2 is optimally suited for hormonal substitution in girls with hypogonadism.

Administration, Cutaneous↗
PubMed2003

Variability of serum estrogens among postmenopausal women treated with the same transdermal estrogen therapy and the effect on androgens and sex hormone binding globulin.

OBJECTIVE: To examine the variability of serum estrogens in response to transdermal estrogen replacement therapy (ET), and to determine the effects on androgens and sex hormone binding globulin (SHBG). DESIGN: Randomized, double-blind, placebo-controlled study. SETTING: Women's hospital. PATIENT(S): Two groups of postmenopausal women: [1] 21 women not on ET enrolled and 17 completed the study; [2] 19 women on continuous transdermal ET enrolled and 13 completed the study. INTERVENTION(S): Women not on ET were administered a placebo patch or a newly initiated estrogen patch, then crossed over to the alternate treatment. Serum samples were obtained at baseline and the subsequent 3 days from the placebo and new-patch groups and from a separate group of women receiving continuous estrogen patch treatment. MAIN OUTCOME MEASURE(S): Estradiol (E(2)), estrone, estrone sulfate, T, dehydroepiandrosterone (DHEA), dehydroepiandrosterone sulfate (DHEAS), androstenedione, free androgen index, and SHBG. RESULT(S): There was considerable intrapatient and interpatient variability in the estrogen response to identical treatment doses, with E(2) values differing between women as much as 138 pg/mL and E(2) increases above baseline differing as much as 90 pg/mL. Continuous treatment increased SHBG and decreased androstenedione levels; however, levels of T, DHEA, DHEAS, and free androgen index did not change. CONCLUSION(S): There is great variability of estrogen in response to transdermal ET, but minimal effect on circulating androgens.

Administration, Cutaneous↗
PubMed1997

Effects of transdermal nicotine or smoking on nicotine concentrations and maternal-fetal hemodynamics.

OBJECTIVE: To compare nicotine concentrations and fetal middle cerebral artery resistance indices (RIs) during 21-mg transdermal nicotine use with these values during maternal smoking. METHODS: In this randomized, crossover study, participants smoked approximately 20 cigarettes daily and were between 24 and 36 weeks' gestation. Subjects were randomized to transdermal nicotine or to smoking ad libitum for 8 hours. One week later, they crossed over to the other condition. Maternal plasma nicotine concentrations and hemodynamic measurements were obtained before and after the onset of smoking or patch placement. RESULTS: Area under the plasma nicotine concentration-time curve during patch use was similar to continued smoking (93 versus 89 ng-hour/mL, respectively) (P = .77). The mean (standard error [SE] change in the middle cerebral artery RI from baseline to 4 hours later was similar during patch use and smoking: -.002 (0.008) versus -.02 (0.015), respectively (P = .3). The study had greater than 80% power to detect a 25% difference in nicotine concentrations and a change of 2 standard deviations in the middle cerebral artery RI between conditions. An unexpected finding was that of a loss of fetal heart rate (FHR) reactivity in 5/8 tracings after patch placement versus 1/6 tracings after smoking (P = .12). The baseline FHR increased by a mean (SE) of 8 (4) beats per minute with loss of reactivity in the patch condition, compared with a decrease of 3 (3) beats per minute without loss of reactivity (P = .05). CONCLUSION: Eight-hour use of 21-mg transdermal nicotine yields nicotine concentrations and middle cerebral artery RIs similar to those produced by hourly smoking in pregnant smokers.

Administration, Cutaneous↗
PubMed1997

Effects of clonidine on prolonged postoperative sympathetic response.

OBJECTIVE: Surgical trauma results in diffuse sympathoadrenal activation which is thought to contribute to perioperative cardiovascular complications in high-risk patients. Regional anesthetic and analgesic techniques can attenuate this "stress response" and reduce the occurrence rate of adverse perioperative events; however, their use in the postoperative period is logistically difficult and costly. The present study was undertaken to evaluate whether transdermal administration of the alpha2 adrenergic-receptor agonist, clonidine, can be used as a pharmacologic means of blunting the stress response throughout the perioperative period. DESIGN: Double-blind, placebo-controlled clinical trial in patients undergoing pancreatico-biliary surgery. SETTING: Operating rooms and surgical intensive care unit of a major university teaching hospital. PATIENTS: Forty patients scheduled for major upper abdominal surgery. INTERVENTIONS: Patients received either clonidine (0.2 mg orally and a clonidine TTS-3 patch the evening before surgery and 0.3 mg orally on call to the operating room) or matched oral and transdermal placebo. MEASUREMENTS AND MAIN RESULTS: Heart rate, systemic arterial blood pressure, plasma catecholamine, clonidine, interleukin-6 concentrations, and 24-hr urine cortisol and nitrogen excretion were measured the day before surgery and daily thereafter for 72 hrs postoperatively. Preoperative transdermal (and oral) clonidine administration resulted in therapeutic plasma clonidine concentrations throughout the perioperative period (1.54 +/- .07 [SEM] microg/mL). Clonidine reduced preoperative epinephrine and norepinephrine concentrations by 65%. Plasma catecholamine concentrations increased in both groups following surgery but were markedly lower throughout the postoperative period in patients receiving clonidine. Patients receiving clonidine had a reduced frequency rate of postoperative hypertension. Clonidine had no effect on plasma interleukin-6 concentration, urine cortisol excretion, or urine nitrogen excretion. No adverse effects of clonidine administration were observed. CONCLUSIONS: The combined administration of oral and transdermal clonidine effectively attenuated the catecholamine response to surgical stress throughout the postoperative study period. Clonidine administration produced specific sympatholytic effects, since other elements of the stress response were not attenuated. Undesirable side effects were not noted. The sustained sympatholytic effects we observed suggest that alpha2 adrenergic-receptor agonists may offer a pharmacologic means of modifying the sympathoadrenal response to injury, and may be useful in reducing perioperative complications.

Administration, Cutaneous↗
PubMed1995

Pharmacokinetics and pharmacodynamics of the tulobuterol patch, HN-078, in childhood asthma.

BACKGROUND: Recently, a novel percutaneous adhesive tulobuterol preparation, HN-078, has been developed and tests using healthy adult subjects have indicated it to be effective for controlling exacerbations early in the morning if applied at bedtime. In children, percutaneous application is very important to eliminate side effects, including abdominal pain and appetite loss. OBJECTIVE: We report the pharmacokinetics and pharmacodynamics of tulobuterol patch, HN-078, in the treatment of childhood asthma. METHODS: Single applications of HN-078 were applied transdermally in six children with asthma who had been admitted to a hospital. Subjects weighing less than 30 kg received 1 mg of tulobuterol while subjects weighing 30 kg or above received 2 mg on the chest for 24 hours. Serum tulobuterol levels and peak expiratory flow rate were determined before and after each application. RESULTS: Cmax of tulobuterol was determined to be 1.33 +/- 0.21 ng/mL, Tmax was 14.0 +/- 2.0 hours, and AUCO-t was 27.1 +/- 4.2 ng.hr/mL. These pharmacokinetic parameters per body surface area of children were nearly equivalent to those of adults obtained in other studies. Peak expiratory flow rate values obtained after application of HN-078 significantly increased in comparison to those obtained before application. No significant changes were observed in pulse rate or blood pressure, and no side effects were found with regard to the subjective symptoms and skin conditions. CONCLUSIONS: These results suggest that the patch formulation of tulobuterol, HN-078, will be very useful for the treatment of pediatric asthma. It is especially significant that no side effects were observed.

Administration, Cutaneous↗
PubMed1992

Dermal patch anaesthesia for venous cannulation with 10% lignocaine gel containing glycyrrhetinic acid monohemiphthalate disodium as an absorption promoter.

The clinical efficacy of transdermal 10% lignocaine gel mixture containing 3% w/w glycyrrhetinic acid monohemiphthalate disodium as an absorption promoter was evaluated at venous cannulation in 17 paediatric (6-11 years) and 17 adult (29-65 years) patients. After about 60 min of occlusive application, the mean (SD) pinprick pain score was 0.7 (0.7) in the paediatric group, compared with 1.4 (1.3) in the adults (p less than 0.05). Twenty-five patients (14 children and 11 adults) who had a pinprick score of 0 or 1 underwent venous cannulation without intradermal local anaesthetic. The mean (SD) pain scores at venepuncture showed no significant differences between children and adults.

Administration, Cutaneous↗
PubMed1995

Fentanyl remaining in a transdermal system following three days of continuous use.

OBJECTIVE: To determine whether there was a sufficient amount of fentanyl remaining in a patch that had been used continuously for 3 days to warrant establishment of disposal policies to prevent diversion of fentanyl. DESIGN: Nine patches were applied and removed by hospice nurses after 3 days of continuous use on hospice patients with cancer. Patches were analyzed for the remaining fentanyl contents using the Coat-A-Count Fentanyl radioimmunoassay. Five 2.5-mg patches and four 10.0-mg patches were opened, solubilized with methanol, diluted with water, and analyzed in duplicate. An unused 2.5-mg patch also was analyzed as a control and showed a 94% recovery of fentanyl. A methanol blank was negative for fentanyl. MAIN OUTCOME MEASURES: The study determined the amount of fentanyl in milligrams remaining in a used patch. Using pharmacokinetics principles, this quantity was compared with a potential lethal dose of fentanyl. RESULTS: Analysis showed 0.7-1.22 mg remaining in the 2.5-mg patches and 4.46-8.44 mg remaining in the 10.0-mg patches. These numbers represent 28-84.4% of the original contents. Using the pharmacokinetic values of the volume of distribution of 4L/kg and a potential lethal blood concentration of 3.7 micrograms/L, one can calculate the potential lethal dose for a 70-kg person to be 1036 micrograms. This is well within the amount remaining in the patch. This study also demonstrated that a wide patient variability exists in the absorption of fentanyl from the patch. CONCLUSIONS: There is a sufficient amount of fentanyl available for abuse and misuse after 3 days of therapeutic use. Adequate disposal policies currently are not established and need to be implemented.

Administration, Cutaneous↗
PubMed1986

Efficacy of clonidine as transdermal therapeutic system: the international clinical trial experience.

Worldwide clinical trial data concerning the pharmacokinetic and pharmacodynamic characteristics of the clonidine transdermal therapeutic system (TTS) are reviewed with reference to its antihypertensive efficacy. The amount of clonidine delivered to the systemic circulation is a direct function of TTS size. After initial patch application, there is a delay of 2 to 3 days before the onset of action, but after removal of the patch, plasma clonidine levels decline slowly, at an elimination half-life of about 20 hours. Evaluation in approximately 2000 patients with mild to moderate hypertension has shown that the bioavailability of transdermal clonidine is comparable to that of oral clonidine and that equivalent blood pressure reductions are achieved. The rate at which dose increases were found necessary to maintain adequate blood pressure control over extended periods reflects a low incidence of tolerance to this new once-a-week dosage form of clonidine, and there has been little evidence of rebound hypertension after discontinuation of TTS treatment.

Administration, Cutaneous↗
PubMed2003

The effect of rectal temperature on perianesthetic serum concentrations of transdermally administered fentanyl in cats anesthetized with isoflurane.

OBJECTIVES: To determine whether moderate hypothermia during 4 hours of anesthesia with isoflurane substantially affects serum concentrations of transdermally administered fentanyl in the perianesthetic period in cats. ANIMALS: 7 healthy mature cats. PROCEDURE: A fentanyl patch (25 microg/h) was applied to the shaved thorax 24 hours before induction of anesthesia. Anesthesia was induced at time 0. Each cat received 2 treatments in a random order. Treatments were isoflurane anesthesia with normothermia and isoflurane anesthesia with hypothermia. Cats were intubated, connected to a nonrebreathing circuit, and maintained at 1.3X minimum alveolar concentration for 4 hours. Cats in the hypothermia treatment groups were actively cooled to 35 degrees C following the induction of anesthesia. Serum fentanyl analysis was performed at -24, -12, 0, 1, 2, 3, 4, 4.5, 5, 6, 7, 8, 9, 10, 12, and 24 hours. RESULTS: Mean +/- SEM serum fentanyl concentration (SFC) for the hypothermia treatment group (0.598 +/- 0.3048 ng/mL) was significantly lower than the baseline concentration (1.834 +/- 0.6393 ng/mL) at 1 hour. This significant reduction persisted for the duration of anesthesia for the hypothermia treatment group. Serum fentanyl concentrations returned to baseline values within 1 hour of the end of anesthesia, regardless of body temperature. CONCLUSIONS AND CLINICAL RELEVANCE: Hypothermia during inhalant anesthesia induced a significant reduction in SFC obtained with transdermal administration. The impact of this reduction in SFC on the contribution of transdermally administered fentanyl to any reduction in the need for inhalant anesthesia remains to be determined.

Administration, Cutaneous↗
PubMed1997

Nicotine patch and self-help video for cigarette smoking cessation.

A total of 424 smokers were randomized in a 2 x 2 factorial experiment. A pharmacologic factor contained 2 levels: transdermal nicotine path (TNP; 21 mg) and placebo. A self-help behavioral treatment factor contained 2 levels: video-enhanced self-help treatment manual and self-help treatment manual only. At 2 months, TNP produced a higher level of abstinence (36%) than placebo (20%), p < .001. No other comparison was significant. In secondary analyses, (at 2 months) and compliance with patch treatment regimen (at 2, 6, and 12 months) were associated with less relapse. Although nicotine replacement therapy has improved our ability to produce smoking cessation, the production of sustained, longer term abstinence remains an elusive goal.

Administration, Cutaneous↗
PubMed2001

[Are transdermic estrogens cardioprotective?].

Transdermic estrogens share many of the oral estrogens cardiovascular effects, but so far there are no studies proving that they have a cardioprotective effect neither in animals nor in human beings. The doubt is outlined moreover, when most of the investigations performed with oral estrogens in animals show an antiatherogenic effect, while the few experimental studies that hare been carried out with estrogen patches show contradictory results. We will have to wait for more extensive clinical trials to be able to know if the transdermic estrogens are really cardioprotective, however if we want to achieve some cardiovascular risk improvement with the current knowledge we will probably have to support the use of oral estrogens.

Administration, Cutaneous↗
PubMed2000

Effect of transdermal nitroglycerin on glucose-stimulated insulin release in healthy male volunteers.

BACKGROUND: Morpholinosydnonimine, a nitric oxide (NO) donor, has been reported to inhibit insulin release in isolated pancreatic islets. We studied whether transdermal application of nitroglycerin, another NO donor widely used for angina prophylaxis, influenced glucose-stimulated insulin release in healthy, young, male volunteers. METHODS AND RESULTS: Oral glucose tolerance tests [(OGTT) 75 g glucose in 200 mL of water) were performed in the presence of placebo patches or nitroglycerin-releasing 'active' patches (approx. 0.4 mg hour-1 nitroglycerin) in the same patients with a 2-week intertest interval. Venous blood samples were taken before and 15, 30, 60, 90, 120 and 180 min after the glucose load and evaluated for plasma glucose level and immunoreactive insulin responses (radioimmunoassay). Glucose-stimulated maximum increase in plasma insulin immunoreactivity were 36.3 +/- 5 and 78.8 +/- 6.1 mU mL-1 (P < 0.05) in the presence of active and placebo patches, respectively. Nevertheless, both fasting and postload blood glucose levels were the same at either patch. Active patches significantly decreased blood pressure with a marginal increase in heart rate. CONCLUSION: We conclude that inhibition of glucose-stimulated insulin release by transdermal nitroglycerin without causing hyperglycaemia may serve as a novel component of the antianginal mechanism of action of nitrates.

Administration, Cutaneous↗
PubMed1999

Crystallization of beta-estradiol in an acrylic transdermal drug delivery system.

Transdermal drug delivery systems are pharmaceutical products that can deliver controlled doses of drugs from polymeric patches applied on the human skin. The long-term stability of these patches is a critical issue relative to their performance in delivering drugs at a constant rate. Where a drug has been dissolved in the polymeric adhesive patch, crystallization has been reported in several systems. This study uses a variety of characterization tools to determine the physical and chemical nature of the precipitates formed in situ in estradiol patches. Optical microscopy revealed that crystals were formed in a single layer inside the adhesive matrix and that there were two distinctly different morphologies: needle-like crystals and aggregates around the needles. From IR measurements it was evident that estradiol probably was present in more than one crystal form in these patches. Raman microscopy showed that the needle-like crystals contain the adhesive component and the aggregates some modified crystal form of estradiol, indicating that in addition to the drug, the polymeric adhesive also crystallizes during storage.

Acrylic Resins↗
PubMed1989

Utility of topical formulations of morphine hydrochloride containing azone and N-methyl-2-pyrrolidone.

In order to develop the transdermal formulations of morphine hydrochloride with high skin permeation rate and prolonged action, several gels and patches containing potent penetration enhancer, laurocapram (Azone), were prepared. Since there was a long lag time period for morphine permeation through the excised hairless rat skin in Azone treatment, N-methyl-2-pyrrolidone was added to the Azone gel or patch as a co-enhancer to increase the skin permeation of morphine hydrochloride, especially in the early phase. The mixed solvent of N-methyl-2-pyrrolidone and water showed cosolvency of morphine hydrochloride, and the co-enhancer could shorten the lag time period of skin permeation of morphine hydrochloride. However, the co-enhancer alone had little effect on the skin permeation of morphine hydrochloride. It was effective only when using with Azone. Coadministration of Azone with the co-enhancer showed high in vitro skin permeation and in vivo blood level of the drug. A marked analgesic effect was found after application of morphine hydrochloride patch containing Azone and N-methyl-2-pyrrolidone. The pharmacological effect was much more prolonged than that after the conventional s.c. injection. From these results, it was predicted that the topical formulations of morphine hydrochloride containing Azone and N-methyl-2-pyrrolidone might be useful for the relief of severe chronic pain in patients.

Administration, Topical↗
PubMed2006

A randomized, double-blind, placebo-controlled, laboratory classroom assessment of methylphenidate transdermal system in children with ADHD.

OBJECTIVE: This study evaluates the efficacy, duration of action, and tolerability of methylphenidate transdermal system (MTS) in children with ADHD. METHOD: Participants were dose optimized over 5 weeks utilizing patch doses of 10, 16, 20, and 27 mg applied in the morning and worn for 9 hours. Following optimization, 80 participants were randomized to 1 week of MTS or placebo followed by 1 week of the opposite treatment. Laboratory classroom sessions conducted after each randomized week included blinded ratings of attention, behavior, and academic performance. RESULTS: MTS was well tolerated and displayed significant improvement compared with placebo. Improvements were seen at the first postdose time point measured and continued through 12 hours. CONCLUSIONS: Treatment with MTS resulted in statistically significant improvements on all efficacy measures. Time course and therapeutic effects of MTS suggest that this novel methylphenidate delivery system is an efficacious once-daily treatment for ADHD.

Administration, Cutaneous↗