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PubMed2004

Development of insulin resistance by nitrate tolerance in conscious rabbits.

Clinical evidence has been raised to suggest that transdermal nitroglycerin increases the sensitivity of peripheral tissues to the hypoglycemic effect of insulin. In this study we determined whether development of tolerance to the hypotensive effect of nitroglycerin also resulted in tolerance to the insulin-sensitizing effect in rabbits. Intravenous glucose disposal and hyperinsulinemic euglycemic glucose clamp studies were performed on naive and hemodynamic nitrate tolerant conscious New Zealand white rabbits. These rabbits were exposed to continuous "patch on" with nitroglycerin (0.07 mg/kg/h) or placebo patches over 7 days. Nitroglycerin treatment of 7 days produced a lack of hypotensive response to a single intravenous bolus of 30 microg/kg nitroglycerin, which caused a significant decrease in mean arterial blood pressure in control rabbits. A six-hour exposure to transdermal nitroglycerin significantly increased insulin sensitivity determined by hyperinsulinemic (100 microU/ml) euglycemic (5.5 mmol/l) glucose clamping as compared with that seen in rabbits treated with placebo patches. A significant decrease in insulin sensitivity was observed in the nitroglycerin patch-treated animals both in the presence and after the removal of the last patch when the patches were applied over 7 days. We conclude that acutely nitrate patches improve insulin sensitivity whereas a 7-day chronic treatment schedule that results in hemodynamic nitrate tolerance also produces insulin resistance.

Animals↗
PubMed2005

In vitro and in vivo evaluation of a novel nonscrotal matrix-type transdermal delivery system of testosterone.

A matrix-type testosterone (TS) transdermal delivery system for nonscrotal skin was developed with DuroTak 87-2510 as an adhesive polymer. When 3% dodecylamine was used in combination with 10% span 80, the in vitro rat permeation rate increased from 2.29 microg/cm2/hr to 6.51 microg/cm2/ hr as the TS loading dose increased from 2% to 6%. The maximum flux of experimental patch was about 14-fold higher than that of Testoderm. Release kinetics of TS from the patches was proportional to t1/2 following the Higuchi equation, and the release rate of TS increased as TS loading dose increased. Also, a good linear relationship between the skin permeation rate and the release rate was observed, which implies that the release rate is the rate-limiting process of the skin permeation. In vivo study showed that the plasma concentration of TS promptly increased and reached the peak level within 3-6 hours of application of the experimental patch. Area under the curve (AUC0 approximately 48) and Cmax also linearly increased in a dose-dependent manner up to 6% of TS. These results demonstrate the feasibility of developing a nonscrotal matrix-type transdermal delivery system of TS.

Administration, Cutaneous↗
PubMed1999

Long-term effects of a single course of nicotine treatment in acute ulcerative colitis: remission maintenance in a 12-month follow-up study.

Patients with mild to moderate active colitis who are treated with mesalazine plus transdermal nicotine reportedly suffer fewer relapses than patients treated with mesalazine plus oral prednisone. A long-term follow-up period was carried out to confirm this. Thirty patients with remission of distal colitis after therapy with the above treatment schedules were monitored for 12 months (Rachmilewitz' activity index plus endoscopy). Relapsed patients were retreated in a cross-over fashion. After 12 months recurrences were observed in 14 of 15 patients initially treated with steroids and in 7 of 15 subjects who were had received transdermal nicotine (P = 0.007, Fisher's test). A higher proportion of relapsed patients from the prednisone group, after successful retreatment with nicotine patches, remained in remission after 6 months (20%) than relapsed patients who switched to steroid treatment (57%). Our present results confirm the concept that nicotine-induced remission of ulcerative colitis lasts longer than that obtained by oral corticosteroids.

Administration, Cutaneous↗
PubMed1997

Transdermal fentanyl in the long-term treatment of cancer pain: a prospective study of 50 patients with advanced cancer of the gastrointestinal tract or the head and neck region.

This open prospective study evaluated the combination of initial dose titration with patient-controlled analgesia (PCA) and long-term treatment with transdermal fentanyl in 50 cancer patients requiring opioids for severe pain. The delivery rate of the first transdermal therapeutic system (TTS) was calculated from the self-administered intravenous fentanyl dose during the first 24 h. TTS were changed every 48-72 h, and a different patch size was chosen if necessary. Pain intensity (101-step numeric analog scale) and side-effects were assessed daily. The patients were treated for 66 +/- 101 days (range 3-535 days). The average delivery rate was 5.9 +/- 4.1 mg/d. Mean pain intensity decreased from initially 45 +/- 21 to 19 +/- 15 in the titration phase and 15 +/- 11 during long-term treatment. Three patients showed moderate respiratory depression. Other severe side-effects were not observed. Patient compliance and acceptance were excellent. The results suggest that intravenous PCA is useful for initial dose finding, and transdermal fentanyl is effective and safe during long-term treatment of cancer pain.

Administration, Cutaneous↗
PubMed1992

Skin pretreatments for shortening onset of dermal patch anesthesia with 3% GA MHPh 2Na-10% lidocaine gel mixture.

Three types of skin pretreatments (stripping with adhesive tape, scrubbing with Skin-Pure jelly, and cleaning with benzine) were studied in 21 volunteers to determine whether the pretreatments could shorten the application period of transdermal 3% GA MHPh 2Na-10% lidocaine gel. Before application of the gel, each subject received skin pretreatment on the volar surface of one forearm. Then, the lidocaine gel soaked in a round sponge was applied on both the pretreated area of the forearm and the unpretreated contrast area of the other forearm. A pain score was obtained from each subject at 30, 45, 60, and 75 min after placement of the dermal patch by noting the number of painful pinpricks of five delivered. The mean pain scores on the pretreated side were significantly lower at 30, 45, and 60 min in the stripping study group and at 45 and 60 min in the cleaning study group, compared with the corresponding scores on the unpretreated side (P less than 0.05). Skin pretreatments, such as stripping and cleaning, are useful for shortening the onset of the dermal patch anesthesia.

Administration, Cutaneous↗
PubMed2000

Transdermal testosterone gel improves sexual function, mood, muscle strength, and body composition parameters in hypogonadal men.

Testosterone (T) therapy for hypogonadal men should correct the clinical abnormalities of T deficiency, including improvement of sexual function, increase in muscle mass and strength, and decrease in fat mass, with minimal adverse effects. We have shown that administration of a new transdermal T gel formulation to hypogonadal men provided dose proportional increases in serum T levels to the normal adult male range. We now report the effects of 180 days of treatment with this 1% T gel preparation (50 or 100 mg/day, contained in 5 or 10 g gel, respectively) compared to those of a permeation-enhanced T patch (5 mg/day) on defined efficacy parameters in 227 hypogonadal men. In the T gel groups, the T dose was adjusted up or down to 75 mg/day (contained in 7.5 g gel) on day 90 if serum T concentrations were below or above the normal male range. No dose adjustment was made with the T patch group. Sexual function and mood changes were monitored by questionnaire, body composition was determined by dual energy x-ray absorptiometry, and muscle strength was measured by the one repetitive maximum technique on bench and leg press exercises. Sexual function and mood improved maximally on day 30 of treatment, without differences across groups, and showed no further improvement with continuation of treatment. Mean muscle strength in the leg press exercise increased by 11 to 13 kg in all treatment groups by 90 days and did not improve further at 180 days of treatment. Moderate increases were also observed in arm/chest muscle strength. At 90 days of treatment, lean body mass increased more in the 100 mg/day T gel group (2.74 +/- 0.28 kg; P = 0.0002) than in the 50 mg/day T gel (1.28 +/- 0.32 kg) and T patch groups (1.20 +/- 0.26 kg). Fat mass and percent fat were not significantly decreased in the T patch group, but showed decreases in the T gel groups (50 mg/day, -0.90 +/- 0.32 kg; 100 mg/day, - 1.05 +/- 0.22 kg). The increase in lean mass and the decrease in fat mass were correlated with the changes in average serum T levels attained after transdermal T replacement. These beneficial effects of T replacement were accompanied by the anticipated increases in hematocrit and hemoglobin but without significant changes in the lipid profile. The increase in mean serum prostate-specific antigen levels (within the normal range) was correlated with serum levels of T. The greatest increases were noted in the 100 mg/day T gel group. Skin irritation was reported in 5.5% of subjects treated with T gel and in 66% of subjects in the permeation-enhanced T patch group. We conclude that T gel replacement improved sexual function and mood, increased lean mass and muscle strength (principally in the legs), and decreased fat mass in hypogonadal men with less skin irritation and discontinuation compared with the recommended dose of the permeation-enhanced T patch.

Administration, Cutaneous↗
PubMed1993

Pharmacokinetics and pharmacodynamics of a new transdermal clonidine, M-5041T, in healthy subjects.

The pharmacokinetic as well as the pharmacodynamic properties of a new transdermal clonidine, M-5041T (M), and its safety were evaluated after single and repeated applications. In the single-application study, one patch of M (4 mg-->6 mg-->8 mg) was applied for 3 days in eight healthy subjects. In the repeated-application study, first (0-72 hours), second (72-144 hours), and third (144-216 hours) patches of M 6 mg were applied in seven healthy subjects. In the single-application study, plasma clonidine concentration increased in a dose-dependent manner after application of M. Maximum plasma concentration (Cmax) and area under the plasma concentration-time curve (AUC) increased in a dose-dependent manner, but the difference did not reach significance. Time to maximum concentration, elimination half-life, and total and renal clearance did not differ significantly among three trials. Blood pressure (BP) decreased gradually after application of each dose of M. The BP-lowering effect of M 8 mg was greater than that of M 4 mg and 6 mg. Adverse effects such as erythema and drowsiness were reported in some subjects. No subject had to be withdrawn from the study because of the appearance of adverse effects. In the repeated-application study, plasma concentration of clonidine increased up to 48 hours after application of first patch, and thereafter remained within a relatively narrow range until removal of third patch. The Cmax and AUC did not differ significantly among three trials. Blood pressure during an active period decreased significantly during treatment with M, whereas BP at midnight did not change significantly.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Cutaneous↗
PubMed1994

Comparison of the pharmacokinetics, pharmacodynamics, and safety of oral (Catapres) and transdermal (M-5041T) clonidine in healthy subjects.

The pharmacokinetic as well as pharmacodynamic properties of a transdermal clonidine, M-5041T (M) and its safety were compared with those of oral clonidine, Catapres (Nippon Boehringer Ingelheim, Hyogo, Japan). One patch of M containing 6 mg of clonidine was applied on the right chest for 3 days or one tablet of Catapres (.075 mg) was given orally every 12 hours for 3 days in eight healthy subjects. The study was conducted by a crossover design with 14 to 16 days' interval between the cross-over. Blood and urine samples for clonidine concentration were obtained, and blood pressure (BP) was measured for a 168-hour period after application of M and for a 96-hour period after initiation of Catapres therapy. Plasma concentration of clonidine increased gradually after application of M and decreased gradually after removal, whereas this parameter increased rapidly during the absorption phase and decreased rapidly in the elimination phase after each dosage of Catapres. Elimination half-life of clonidine after removal of M was significantly greater than that after the final dosage of Catapres. No significant difference was observed in maximum plasma concentration or area under the plasma concentration-time curve between the two trials. The BP lowering effects of M and Catapres did not differ significantly. Adverse symptoms occurred more frequently during Catapres therapy than during treatment with M. Most of these symptoms were observed when plasma clonidine concentration was relatively higher in each trial. These results suggest that M is effective for the treatment of hypertension with a lower incidence of adverse symptoms.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Cutaneous↗
PubMed1992

Cutaneous metabolism of nitroglycerin in vitro. I. Homogenized versus intact skin.

The metabolism of nitroglycerin (GTN) to 1,2- and 1,3-glyceryl dinitrate (GDN) by hairless mouse skin in vitro has been measured. In the first set of experiments, GTN was incubated with the 9000g supernatant of fresh, homogenized tissue in the presence and absence of glutathione (GSH), a cofactor for glutathione-S-transferase. After 2 hr of incubation with GSH, 30% of the initially present GTN had been converted to 1,2- and 1,3-GDN; without GSH, less than 5% of the GTN was metabolized. The ratio of 1,2-GDN to 1,3-GDN produced by the homogenate was 1.8-2.1. In the second series of studies, GTN was administered topically to freshly excised, intact hairless mouse skin in conventional in vitro diffusion cells. The concurrent transport and metabolism of GTN was then monitored by sequential analysis of the receptor phase perfusing the dermal side of the tissue. Three topical formulations were used: a low concentration (1 mg/ml) aqueous solution, a 2% ointment, and a transdermal delivery system. Delivery of total nitrates (GTN + 1,2-GDN + 1,3-GDN) into the receptor phase was similar for ointment and patch formulations and much greater than that from the solution. The percentage metabolites formed, however, was greatest for the solution (61% and 2 hr, compared to 49% for the patch and 35% for the ointment). As has been noted before, therefore, the relative level of skin metabolism is likely to be greatest when the transepidermal flux is small. Distinct from the homogenate experiments, the 1,2/1,3-GDN ratios in the penetration studies were in the range 0.7-0.9.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Topical↗
PubMed1995

Microdialysis in cutaneous pharmacology: kinetic analysis of transdermally delivered nicotine.

Direct measurements of cutaneous drug levels and kinetics have long been hampered by lack of appropriate methods. Recently, studies have indicated that microdialysis, a method of continuous in vivo sampling of extracellular fluid, may also be performed in human skin. The present study was designed to evaluate this technique for kinetic analyses of cutaneous drug levels. Using a transdermal nicotine delivery system with 35 mg of nicotine as a model, nicotine levels were determined in the dialysate of human skin by means of high performance liquid chromatography. In vitro studies demonstrated that nicotine levels in the dialysate strictly correlated with nicotine concentrations in the dialyzed medium. In nine healthy male volunteers receiving nicotine by transdermal delivery, nicotine was detectable within 90-180 min, and peak levels of approximately 1000 ng/ml were detected within 240-360 min of patch application. Correlation analyses of the individual data from our subjects revealed that nicotine kinetics were independent of skin barrier function, as assessed by transepidermal water loss, but indicated that the detectable maximum nicotine levels may depend on the location of the probe. In summary, the present study demonstrates that microdialysis may be a novel, powerful tool to study cutaneous pharmacology in vivo.

Administration, Cutaneous↗
PubMed1998

Passive versus electrotransport-facilitated transdermal absorption of ketorolac.

OBJECTIVE: To investigate the bioavailability (extent and rate of absorption) of ketorolac from two cutaneous absorption sources, active electrotransport and passive transdermal, and to examine the enantiomeric selectivity of bioavailability for each source. METHODS: Based on a crossover study in 12 healthy volunteers, the extent and rate of absorption of ketorolac, delivered by a patch, were found by estimating the input rate function of the drug. For that purpose, deconvolution was used in two steps. First, intravenous data were analyzed to estimate the ketorolac disposition function, and second, postpatch data were deconvolved to estimate the unknown patch input profile given the disposition function estimated in the first step. Because the input rate function curves to be estimated for the patches may be of arbitrary shape, a spline was used to model the patch input function, whereas intravenous data were modeled with use of a sum of exponentials. Differences in the extent of absorption (F) for the four treatment-enantiomer combinations were further examined with a mixed-effect regression model, based on the sets of four individual estimates of bioavailability. RESULTS: On average, the F value for the active electrotransport treatment, which exhibited the faster absorption rate, was four times greater than the F for the passive transdermal treatment. Further, during the passive treatment, R-ketorolac yielded an average F that is 42% greater than that for S-ketorolac and also exhibited a smaller absorption lag-time. During the active treatment, there was no important enantiomeric difference in either extent or rate of absorption.

Administration, Cutaneous↗
PubMed1998

[Tocolysis with a nitroglycerin patch].

We would like to present a 22 year old nullipara where preterm labor was successfully tocolysed using a nitro-glycerine path without sequellae side effects. Potential advantages and disadvantages of a transdermal nitro-glycerine delivery system in comparison to the commonly used intravenous fenoterol tocolysis is discussed.

Administration, Cutaneous↗
PubMed1997

Acute effects of transdermal estradiol administration on plasma levels of nitric oxide in postmenopausal women.

OBJECTIVE: To investigate the acute effects of transdermal E2 administration on nitric oxide (NO) plasma levels in postmenopausal women. DESIGN: Randomized, placebo-controlled trial. SETTING: Normal human volunteers in an academic research environment. PATIENT(S): Twenty healthy postmenopausal women. INTERVENTION(S): Transdermal administration of 100 micrograms/d E2 or placebo. MAIN OUTCOME MEASURE(S): Plasma concentrations of NO stable oxidation products and serum concentrations of E2 were assessed before and 24 hours after the administration. RESULT(S): In the group treated with E2 mean concentration of NO metabolites 24 hours after patch application (37.31 +/- 7.62 mumol/L) resulted significantly higher than baseline (21.04 +/- 5.71 mumol/L) and the control group (23.50 +/- 4.03 mumol/L). The correlation between the mean percent increase in NO metabolites and absolute E2 concentrations 24 hours after the E2 administration was statistically significant. CONCLUSION(S): Transdermal administration of E2 to healthy postmenopausal women increases the plasma levels of NO and this supports the hypothesis that a NO-related mechanisms may contribute to the cardiovascular protective effect of estrogens in postmenopause.

Administration, Cutaneous↗
PubMedDate not supplied

A double-blind comparison of transdermal clonidine and oral captopril in essential hypertension.

In a double-blind study, patients with mild essential hypertension were randomly assigned to treatment with transdermal clonidine or oral captopril. After a two- to three-week titration period, blood pressure decreased significantly from 146.3/95.4 to 134.7/85.1 mmHg in the 33 clonidine-treated patients and from 143.0/96.1 to 134.8/87.1 mmHg in the 35 captopril-treated patients; the mean daily doses were 0.2 mg (equivalent) of clonidine and 122.9 mg of captopril. After eight weeks of treatment, blood pressures were reduced to 132.9/85.2 mmHg in the clonidine group (n = 22) and 131.2/82.5 mmHg in the captopril group (n = 16). In black patients, blood pressure reductions were greater with clonidine than with captopril. Four patients were withdrawn from treatment because of side effects in the clonidine group and one in the captopril group. No between-group differences were found in the responses to a quality-of-life questionnaire completed before and after treatment. The clonidine patches were worn during 99% of patient-weeks of treatment; captopril was taken as directed during 64% of patient-weeks of treatment. It is concluded that transdermal clonidine is safe and effective and well accepted by hypertensive patients.

Administration, Cutaneous↗
PubMed2003

Cutaneous analgesia after transdermal application of amitriptyline versus lidocaine in rats.

UNLABELLED: Amitriptyline, a tricyclic antidepressant, has potent local anesthetic properties. However, there is no report of cutaneous analgesic effects after transdermal application. We report here that transdermally applied amitriptyline is more potent than lidocaine in providing cutaneous analgesia in rats. Solutions of amitriptyline base in 50, 100, and 500 mM concentrations were applied as a patch to rats, and their effects were compared with those of lidocaine base at the same concentrations and of the vehicle alone (45% water, 45% isopropyl alcohol, and 10% glycerin). Rats in each test group developed a concentration-dependent cutaneous analgesic block in the areas to which the drugs were applied; however, amitriptyline produced a longer block than lidocaine at the same concentration. The development of amitriptyline as a longer-lasting topical analgesic may improve our ability to treat chronic pain, such as neuropathic pain and neuralgia, and to prevent pain in procedures such as venipuncture. IMPLICATIONS: The tricyclic antidepressant amitriptyline, often used perorally for the management of chronic pain, is shown here to be more potent than lidocaine in providing cutaneous analgesia when applied transdermally with an occlusive dressing in rats.

Administration, Cutaneous↗