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PubMed2000

Drug concentration effect relationship of estradiol from two matrix transdermal delivery systems: Menorest and Climara.

OBJECTIVES: To relate the pharmacokinetics of estradiol to pharmacological effects. METHODS: Drug concentration effect relationship of estradiol from two matrix transdermal delivery systems, Menorest and Climara, was studied in a single centre, open, randomised, comparative crossover study. The trial consisted of two treatment periods, 14 days for each patch separated by a 4-week washout period. Blood hormone levels were followed during the second week of each treatment. Estradiol levels during treatments were related to three concentration levels previously proposed as efficacy or safety limits. The effect of treatment on FSH-levels was examined and the relationship between the levels of estradiol and FSH was described using an inhibitory sigmoidal I(max) model. Estrone levels and estradiol/estrone before and during treatment were followed. RESULTS: The C(average) of FSH during treatment was 38% lower than baseline plasma levels. Estradiol had an inhibitory effect on FSH with an I(max) of 0.68 and an IC(50) of 19 pg/ml. The fraction of time above the minimum concentration for therapeutic effect and the tolerability limit did not differ between the two treatments, whereas the fraction of time above the suggested threshold for osteoporosis prophylaxis was significantly larger for Menorest than for Climara (P<0.05). The low baseline estradiol/estrone ratios increased towards pre-menopausal levels during treatment. CONCLUSIONS: The drug concentration effect relationship of estradiol may be of use in evaluation of the effects of prophylactic estrogen therapy and to facilitate comparisons between different forms of estrogen treatments.

Administration, Cutaneous↗
PubMed1987

Multifocal contact dermatitis to nitroderm TTS 5 with extensive postinflammatory hypermelanosis.

Allergic contact dermatitis to nitroglycerin has been previously reported. A localized cutaneous burn-like reaction due to the transdermal device was recently described. We are presenting a case of recurrent allergic contact dermatitis due to nitroglycerin as well as to its delivery device, resulting in numerous patches of postinflammatory hypermelanosis at the sites of application.

Administration, Cutaneous↗
PubMed2004

A randomized placebo-controlled trial of short-term graded transdermal estradiol in healthy gonadotropin-releasing hormone agonist-suppressed pre- and postmenopausal women: effects on serum markers of bone turnover, insulin-like growth factor-I, and osteoclastogenic mediators.

The acute effects of estradiol on procollagen type 1 formation in pre- and postmenopausal women are controversial. Twenty-three premenopausal women and 13 postmenopausal women received two consecutive im injections of 3.75 mg leuprolide acetate 3 wk apart to block endogenous ovarian steroidogenesis. Transdermal estradiol therapy commenced on the night of the second leuprolide injection in all subjects, except five pre- and two postmenopausal women who were randomized to receive placebo patches. Estradiol therapy was applied incrementally, with each dose of 0.05, 0.10, 0.15, and 0.20 mg/d administered for 4 consecutive days, to mimic the estradiol changes typifying the follicular phase of the menstrual cycle. Blood aminoterminal propeptide of type I procollagen (PINP), intact osteocalcin (OC), carboxyterminal telopeptide of type I collagen (CTx), IGF-I, and estradiol were measured before and at the end of each estradiol increment. Potential mediators such as osteoprotegerin and receptor activator of nuclear factor-kappaB ligand (RANKL) were also measured. Despite comparable increases in serum estradiol, PINP increased more in postmenopausal compared with premenopausal women (between-group P = 0.03) and occurred at a time when CTx and OC did not change. CTx and IGF-I changed minimally and inconsistently, whereas OC, RANKL, and osteoprotegerin were stable. Repeated measures linear regression disclosed a significant negative association between increases in estradiol and PINP in premenopausal women (P = 0.0006) only. This suggests that lower dose estradiol should greatly increase PINP. Analogous regressions also showed significant negative relationships between changes in estradiol and RANKL in both pre- (P = 0.04) and postmenopausal (P = 0.002) women. Changes in serum markers of bone formation (PINP or OC) did not correlate with those of IGF-I. We conclude that lower dose estradiol rapidly increases osteoblastic collagen synthesis in women at a time when collagen degradation is stable and that this response differs between pre- and postmenopausal women. The effect of estradiol on bone formation does not appear to be mediated by IGF-I. In contrast, RANKL is likely to mediate the effect of estradiol on osteoclastogenesis.

Administration, Cutaneous↗
PubMed1993

In vivo iontophoresis of fentanyl and sufentanil in rats: pharmacokinetics and acute antinociceptive effects.

Iontophoresis is a process which enhances skin permeation of ionized species by using an electrical field as driving force. The aim of the present study was to investigate whether transdermal iontophoresis of fentanyl or sufentanil could induce therapeutic plasma levels and antinociceptive effect. Fentanyl and sufentanil were introduced in an acidic buffer (acetate buffer 0.01 M at pH 5) at 40 micrograms/mL. A platinum electrode was clamped in an hydrophilic foam soaked with the drug solution and linked to the anode. A cathodic foam reservoir was filled with saline solution. The device was applied on the abdominal skin of hairless rats and direct current (0.17 mA/cm2) was applied for 1 h. Opioid plasma concentrations were monitored. In the experimental conditions used, iontophoresis strongly increased transdermal permeation of the drugs as compared to diffusion. A 1.5 h Tmax was observed. The maximal plasma levels after 1.5 h were 29.3 +/- 14 ng/mL for fentanyl and 29.1 +/- 14 ng/mL for sufentanil. The plasma level of the narcotics decreased slowly after iontophoresis was terminated. Iontophoretic transdermal permeation of fentanyl and sufentanil in rats induced analgesic effects as measured by the tail-flick test. These effects lasted for about 4 h. Thus, transdermal iontophoresis with a miniaturized device is effective for the controlled and pulsatile or sustained delivery of synthetic opiates for pain management in humans. As compared to classical patches, it could reduce the lag time before reaching steady state and allow variable drug release rate.

Administration, Cutaneous↗
PubMed1996

[Usefulness of transdermal hormone substitution in high risk postmenopausal patients].

The authors studied whether hormone replacement therapy can be performed in postmenopausal patients with high risk factors among anamnestic data such as thromboembolia, diabetes mellitus, hypertension, epilepsy. 50 mg 17 beta estradiol patch (twice weekly) and 10 mg medroxyprogesteron (in the last 12 days of the cycle) were prescribed. Data of 102 patients with the above conditions were analyzed at the beginning and at the 3,6, and 12 month follow-up visits. The frequency of exacerbation of anamnestic disease, biased and unbiased complaints, efficacy and side effects of the therapy were studied. In the authors opinion hormone replacement therapy can be safely performed in patients with high risk factors among anamnestic data, in addition it may be useful to prevent them.

Administration, Cutaneous↗
PubMed1990

Investigations on the percutaneous absorption of the antidepressant rolipram in vitro and in vivo.

In vitro experiments using full-thickness human skin showed that it was feasible to deliver therapeutic amounts of the new antidepressant drug rolipram. Simple transdermal devices were constructed, and the presence of isopropyl myristate (IPM) in a silicone adhesive (Dow Corning X7-2920) enhanced the flux across excised human skin. The steady-state fluxes from adhesive mixtures containing 0, 5, and 10% IPM were 3, 5.2, and 6 micrograms/cm2/hr, respectively. The in vitro experiments were confirmed in a clinical study involving six healthy male volunteers. The formulations tested were an alcoholic solution and adhesive patches containing 5 and 10% IPM. The dose of drug administered was 0.5 mg/cm2 and the device size 25 cm2. Blood samples were withdrawn over a 24-hr period and analyzed using radioimmunoassay. The topical applications were well tolerated, with only mild or no side effects. A lag time of approximately 2 hr was found for the detection of rolipram in the plasma (detection limit, 50 pg/ml). Interindividual variations both for the peak drug levels and throughout the delivery were quite high but this magnitude of variation has been observed in many other transdermal studies. Plasma levels between 1 and 2 ng/ml were found for all formulations and the AUC0-30 hr was significantly higher for the patch containing 5% IPM.

Administration, Cutaneous↗
PubMed1998

Effects of short-term transdermal estradiol administration on plasma levels of nitric oxide in postmenopausal women.

OBJECTIVE: To assess the effects of short-term transdermal E2 administration on nitric oxide (NO) plasma levels in postmenopausal women. DESIGN: Randomized, placebo-controlled trial. SETTING: Healthy volunteers in an academic research environment. PATIENT(S): Twenty-eight healthy postmenopausal women. INTERVENTION(S): Transdermal administration of E2 (100 microg/d) or placebo on days 1 and 4 of a 1-week treatment regimen. MAIN OUTCOME MEASURE(S): Serum concentrations of E2 and plasma concentrations of NO stable oxidation products were assessed on day 1, before placement of the patch, and subsequently on days 2, 3, and 6. RESULT(S): The mean concentration of NO metabolites on days 2, 3, and 6 was significantly greater in the E2 group (40.08+/-15.42 micromol/L, 38.05+/-18.82 micromol/L, and 42.03+/-16.81 micromol/L on days 2, 3, and 6, respectively) compared with both baseline levels (23.07+/-5.79 micromol/L) and the placebo group (23.51+/-4.06 micromol/L, 21.64+/-4.72 micromol/L, and 21.81+/-4.46 micromol/L on days 2, 3, and 6, respectively). CONCLUSION(S): During a 1-week treatment regimen with transdermal E2, plasma levels of NO in postmenopausal women were significantly higher than baseline levels on days 2, 3, and 6. This suggests that the effect of estrogens on NO synthesis is rapid and that it is maintained with repeated administration.

Administration, Cutaneous↗
PubMed2000

Transdermal delivery of propranolol using mixed grades of Eudragit: design and in vitro and in vivo evaluation.

A matrix-dispersion-type transdermal drug delivery system of propranol was developed using different ratios of mixed polymeric grades of Eudragit. Formulations were evaluated for in vitro dissolution characteristics using a Cygnus' sandwich patch holder. Selected formulations followed zero-order release kinetics. In vivo evaluation was carried out on healthy human volunteers following a balanced incomplete block design (BIBD). In vitro dissolution rate constant k and pharmacokinetic parameters generated from plasma and urine were evaluated statistically. Statistically excellent correlation was found between percentages of drug absorbed from patch versus Cmax, AUC0-24, and AUC0-alpha. A highly significant difference was observed when Cmax and AUC0-alpha generated from plasma and urine data were compared, but when ke, t1/2e, ka, and t1/2a were compared, the difference was not significant. Urinary excretion data are suggested as a simpler alternative to blood-level data in studying the kinetics of absorption and deriving the absorption parameter.

Administration, Cutaneous↗
PubMed1989

N-acetylcysteine fails to attenuate haemodynamic tolerance to glyceryl trinitrate in healthy volunteers.

1. The effects of chronic dosing with N-acetylcysteine (NAC), on nitrate-induced haemodynamic changes during the acute and chronic treatment of healthy volunteers with glyceryl trinitrate (GTN) patches (Transiderm nitro) has been investigated. 2. Seven volunteers were treated in a double-blind randomised crossover manner for two periods of 4 days with 20 mg of transdermal GTN/24 h together with NAC (200 mg three times daily) or matching placebo. There was a washout period of greater than 3 days between treatment periods. 3. Haemodynamic measurements (blood pressure (BP); heart rate (HR] at rest and following maximal treadmill exercise were performed before treatment and 4 h after starting treatment on days 1 and 4. 4. Significant haemodynamic changes as evidenced by a fall in BP and rise in HR, were seen on day 1 in both the NAC and placebo phases. By day 4 the haemodynamic changes had returned towards the pre-treatment values during both the NAC and placebo phases suggesting the development of tolerance in both treatment groups. 5. These findings suggest that concurrent administration of NAC fails to prevent the development of tolerance to GTN.

Acetylcysteine↗
PubMed1986

[Dose-response relationship of nitrate therapy of angina pectoris].

The treatment of 15 patients with coronary heart disease and exertion-related angina pectoris with isosorbide dinitrate (ISDN) tablets in 4 doses (6 X 5 mg, 6 X 20 mg, 6 X 40 mg, 6 X 80 mg) in a randomized sequence for 1 week each resulted in a dose-related improvement of ischemia (ST-segment depression during stress testing) as compared to placebo: 5 mg (30 mg/day): 24% (p less than 0.05); 20 mg (120 mg/day): 40% (p less than 0.05); 40 mg (240 mg/day): 60% (p less than 0.01); 80 mg (480 mg/day): 74% (p less than 0.01). Continuation of treatment for another 4 weeks with 480 mg/day led to a slight decrease in antianginal activity, with a 55% improvement of ST-depression. The frequency of angina pectoris was also lowered in a dose-related manner. For nitroglycerin in oral sustained release form (matrix system) a dose-related antianginal efficacy could be demonstrated in 12 patients enrolled in a double-blind cross-over trial: 2.6 mg (single dose): 23% (n.s.); 6.5 mg: 38% (p less than 0.01); 10 mg: 55% (p less than 0.001); 20 mg: 74% (p less than 0.0001). The duration of action of 20 mg was 4 hours. Transdermal nitroglycerin also proved to be effective in a dose related fashion. In 12 patients undergoing 1-week treatment periods with 5 cm2, 10 cm2 and 20 cm2-patches ST-depression was favourably influenced by 15% (n.s.), 22% (p less than 0.05) and 46% (p less than 0.001) 3 hours after administration. No antiischemic efficacy was demonstrable 24 hours after medication.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Cutaneous↗
PubMed2006

In vitro transdermal delivery of caffeine, theobromine, theophylline and catechin from extract of Guarana, Paullinia Cupana.

Extracts of guarana (Paullinia cupana) feature as putatively stimulating ingredients in a number of foods, drinks and dietary/herbal supplements. The objective of this work was to investigate in vitro the transdermal delivery of the major pharmacologically active compounds contained in guarana extract. Saturated solutions of guarana were prepared in polyethylene glycol 400 (PEG400), propylene glycol (PG) and H(2)O at 32 degrees C. Guarana extract was also formulated in Duro-tak 2287 transdermal adhesive in a range of concentrations and the diffusional release was determined in addition to adhesive properties. Transdermal delivery across full thickness pig ear skin was investigated in vitro using Franz-type diffusion cells, with reverse-phase HPLC being used for the quantification of the permeation of theobromine (TB), theophylline (TP), (+)-catechin (C) and caffeine (CF). Based upon a combination of release and adhesive property data a patch containing 5.55 mg guarana extract cm(-2) was deemed optimal. The general trend for the delivery of the 4 analytes was: water >5.55 mg cm(-2) patch approximately PG>PEG400. For CF the greatest steady state flux was obtained from the water vehicle: 19 microg cm(-2)h(-1), with approximately 420 microg cm(-2) permeating after 24h. This was some 6x times more than from the drug-in-adhesive patch and 10x greater than PG, a well-known penetration enhancer, and 50x that of the 'regular' excipient PEG400. A water vehicle also provided the greatest delivery of TB (0.45 microg cm(-2) h(-1)), TP (0.022 microg cm(-2) h(-1)), and C (0.10 microg cm(-2) h(-1)). An inverse relationship was noted between lipophilicity and k(p) in each vehicle. The simultaneous transdermal delivery of the major actives of guarana was established, with permeation rates being highly concentration and vehicle dependent.

Adhesives↗
PubMed1996

[Smoking cessation program using nicotine patch among physicians and pharmacists of Catalonia: results after 3-12 months].

Smoking abstinence rates of a group of 300 physicians and pharmacists of Catalonia (Spain) who participated in an open non-controlled follow-up design study with nicotine patch, are presented. Were eligible all the individuals who regularly smoke more than 15 cigarettes/day and get Fagerström Test score of 5 or more. Those who smoke more than 20 cig/day were offered a 3-month 24-hour transdermal nicotine treatment (30-20-10 schedule) and those smoking between 15 and 20 cig/day, received the 20-20-10 schedule. A follow up of participants was carried out at 3, 6, 9 and 12 months. After one year, 12 participants (4%) were dropped out. The overall abstinence rates at 3, 6, 9 and 12 months were respectively 55.9% (IC95%: 50.2-61.6), 42.7% (IC95%: 37.0-48.4), 35.4% (IC95% 29.9-40.9), 33.7% (IC95%: 28.2-39.2). Among predictive cessation variables, only those who had mad 1 to 3 previous attempts and those with only "cold turkey" (or slow reduction) quit experience, obtained statistically better results at 3 months. These results seem to be as good as or even better than those obtained in other similar studies with nicotine patch.

Administration, Cutaneous↗
PubMed2001

Electrically-assisted transdermal delivery of buprenorphine.

The objective of this study was to explore the electrically assisted transdermal delivery of buprenorphine. Oral delivery of buprenorphine, a synthetic opiate analgesic, is less efficient due to low absorption and large first-pass metabolism. While transdermal delivery of buprenorphine is expected to avoid the first-pass effect and thereby be more bioavailable, use of electrical enhancement techniques (iontophoresis and/or electroporation) could provide better programmability. Another use of buprenorphine is for opiate addiction therapy. However, a patch type device is subject to potential abuse as it could be removed by the addict. This abuse can be prevented if drug particles are embedded in the skin. The feasibility of doing so was investigated by electro-incorporation. Buprenorphine HCl (1 mg/ml) in citrate buffer (pH 4.0) was delivered in vitro across human epidermis via iontophoresis using a current density of 0.5 mA/cm(2) and silver-silver chloride electrodes. Electroporation pulses were also applied in some experiments. For electro-incorporation, drug microspheres or particles were driven into full thickness human skin by electroporation. It was observed that the passive transdermal flux of buprenorphine HCl was significantly enhanced by iontophoresis under anodic polarity. The effectiveness of electro-incorporation seemed inconclusive, with pressure also playing a potential role. Delivery was observed with electro-incorporation, but the results were statistically not different from the corresponding controls.

Administration, Cutaneous↗
PubMed2004

Effect of transdermally administered fentanyl on the minimum alveolar concentration of isoflurane in cats.

OBJECTIVE: To determine the effect of two doses of fentanyl, administered transdermally, on the minimum alveolar concentration (MAC) of isoflurane in cats. STUDY DESIGN: Prospective, randomized study. ANIMALS: Five healthy, spayed, female cats. METHODS: Each cat was studied thrice with at least 2 weeks between each study. In study 1, the baseline isoflurane MAC was determined in triplicate for each cat. In studies 2 and 3, isoflurane MAC was determined 24 hours after placement of either a 25 or 50 microg hour(-1) fentanyl patch. In each MAC study, cats were instrumented to allow collection of arterial blood and measurement of arterial blood pressure. Twenty-four hours prior to studies 2 and 3, a catheter was placed and secured in the jugular vein and either a 25 or 50 microg hour(-1) fentanyl patch was placed in random order on the left thorax. Blood samples for plasma fentanyl determination were collected prior to patch placement and at regular intervals up to 144 hours. After determination of MAC in studies 2 and 3, naloxone was administered as a bolus dose (0.1 mg kg(-1)) followed by an infusion (1 mg kg(-1) hour(-1)) and MAC redetermined. RESULTS: The baseline isoflurane MAC was 1.51 +/- 0.21% (mean +/- SD). Fentanyl (25 and 50 micro g hour(-1)) administered transdermally significantly reduced MAC to 1.25 +/- 0.26 and 1.22 +/- 0.16%, respectively. These MAC reductions were not significantly different from each other. Isoflurane MAC determined during administration of fentanyl 25 micro g hour(-1) and naloxone (1.44 +/- 0.16%) and fentanyl 50 micro g hour(-1) and naloxone (1.51 +/- 0.19%) was not significantly different from baseline MAC (1.51 +/- 0.21%). CONCLUSIONS AND CLINICAL RELEVANCE: Fentanyl patches are placed to provide long-lasting analgesia. In order to be effective postoperatively, fentanyl patches must be placed prior to surgery. Plasma fentanyl concentrations achieved intraoperatively decrease the need for potent inhalant anesthetics in cats.

Administration, Cutaneous↗
PubMed1988

[Long-term effects of a combination of transdermal nicotine administration with behavior therapy for smoking cessation].

Effects of a transdermal nicotine substitution on psychological smoking cessation were investigated in a double-blind prospective study. 131 smokers have been randomly assigned to three treatment conditions: All smokers underwent nine weeks of self-controlled smoking cessation. During 6 weeks one group was additionally treated with nicotine patches continuously releasing nicotine through the skin into the blood circuit. The second group received placebo patches; while the third group was treated with behavioral training alone. Treatment effects were measured by daily cigarette consumption. Follow-up investigations were performed 3, 6 and 12 months after therapy. Nicotine-treated subjects reached significantly higher abstinence rates during and at the end of treatment as well as during the follow-up period, than both placebo- and control-subjects. No severe side effects of plasters have been reported. The results thus indicate good therapeutic effectiveness of transdermal nicotine substitution.

Administration, Cutaneous↗
PubMed2002

[Are the acute effects of transdermal estradiol in postmenopausal women with coronary disease related to changes of the autonomic tone?].

The single application of estradiol in postmenopausal women with symptomatic coronary heart disease has an antiischemic effect, which seems to be mainly related to the relaxation of the vascular smooth muscle. Longterm replacement with estrogen in postmenopausal women reduces their increased sympathetic activity. The aim of the double-blinded study was to assess whether a single transdermal estradiol administration also has an effect on the sympathovagal balance and may additionally explain the acute effects of estradiol. Methods Fifteen women with symptomatic and angiographically proven coronary artery disease were cross-over randomized to two 100-microgram patches of estradiol or identical placebo. After one week the women received the opposite treatment. One day after patch application a 24-hour Holter-ECG recording was performed to assess the mean heart rate over 24 hours as well as time domain and frequency domain indices of the heart rate variability. Results The estradiol plasma concentration rose significantly from 354 +/- 176 pmol/l after placebo to 800 +/- 260 pmol/l after estradiol application. Heart rate during placebo was 74 +/- 15 bpm and during therapy 74 +/- 15 bpm. Heart rate variability was not different for time domain indices such as SDNN (estradiol: 64 +/- 31 ms; placebo: 65 +/- 33 ms) or for frequency domain indices such as LF (estradiol: 15.8 +/- 8.0 ms; placebo: 15.3 +/- 9.4 ms) and HF (estradiol: 12.1 +/- 8.5 ms; placebo: 12.9 +/- 9.9 ms). Conclusion A single transdermal application of estradiol did not modify heart rate or heart rate variability of women with coronary artery disease. The modulation of the autonomic tone does not seem to be a relevant mechanism of short-term estradiol effects.

Administration, Cutaneous↗
PubMed1997

Continuous transdermal oestrogen and interrupted progestogen as a novel bleed-free regimen of hormone replacement therapy for postmenopausal women.

OBJECTIVE: To investigate the effects of a hormone replacement therapy regime of continuous oestrogen and interrupted progestogen, administered transdermally, on the endometrium of postmenopausal women, the pattern of bleeding and relief of menopausal symptoms. DESIGN: Volunteer pilot study of up to six months duration involving weekly application of an oestrogen-only skin patch releasing 50 microg oestradiol per day interspersed with a combined oestrogen and progestogen patch releasing 50 microg oestradiol and 250 microg norethisterone acetate per day for three days. Transvaginal ultrasound measurements of endometrial thickness and endometrial biopsies were performed in the third month of treatment at the end of both an oestrogen-only phase of treatment and a combined oestrogen-progestogen phase. SETTING: Specialist community menopause clinic, Dean Terrace Centre, Edinburgh. PARTICIPANTS: Fifteen healthy postmenopausal women. MAIN OUTCOME MEASURES: Effect of treatment on endometrial histology, the immunolocalisation of oestrogen and progesterone receptors and the cell proliferation marker Ki 67 after three months of treatment and the proportion of women without bleeding at six months. RESULTS: Treatment provided relief of hot flushes and by the sixth month of study 10 of the 14 women who completed treatment had no vaginal bleeding (71%). No endometrial hyperplasia or atypical changes were observed in biopsies and ultrasound measurements of endometrial thickness demonstrated a thin endometrium. Reduced immunostaining for Ki 67 was observed in endometrium from the combined phase of treatment compared with the oestrogen-only phase, consistent with a progestogenic-antagonism of proliferation. Exposure to progestogen did not suppress steroid receptors as similar immunostaining was observed in both treatment phases. CONCLUSIONS: Continuous oestrogen and interrupted progestogen administered transdermally offers promise as a novel bleed-free hormone replacement therapy for postmenopausal women.

Administration, Cutaneous↗