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PubMed1996

Middle cerebral artery velocity correlates with nitroglycerin-induced headache onset.

Headache often accompanies treatment with nitroglycerin, but the cerebral hemodynamic effects and the exact mechanism of the headache are incompletely understood. Transcranial Doppler monitoring allows evaluation and monitoring of changes in blood flow velocity in the large intracranial arteries. The objective of this study was to assess middle cerebral artery (MCA) blood flow velocities with transcranial Doppler monitoring in subjects receiving continuous low-dose nitroglycerin intravenously or by patch, and correlate these with clinical headache. Twenty-eight normal adult men received nitroglycerin (0.12 micrograms/kg/min intravenously [n = 14] or 0.6 mg/min by transdermal patch [n = 14]), for up to 120 minutes, with monitoring of clinical headache status (standard 4-point scale), blood pressure, heart rate, end-expiratory PCO2 (CO2), and right MCA velocity. All subjects developed headache (mean time to onset, 34 min), reaching moderate or severe levels in 20. There were no differences in age, weight, mean blood pressure, mean heart rate, or resting end-tidal CO2 between those whose headache reached a moderate to severe level and those whose headache remained mild. MCA velocity decreased from baseline values at all levels of clinical headache (onset, -17%; moderate, -18%; severe, -16%; nitroglycerin stopped, -19%) (p, 0.0001 by t test for each stage of headache). MCA velocity remained decreased at the time of headache resolution (-14%; p < 0.001). Blood pressure, heart rate, and CO2 did not change significantly. There were no differences related to route of nitroglycerin dosing. These data show that continuous low doses of nitroglycerin by patch or intravenously produce headache in normal male subjects. MCA velocities were significantly decreased at headache onset and at all levels of headache severity. Changes in MCA velocity persisted beyond the clinical headache. These results suggest a direct MCA vasodilatory effect of nitroglycerin. This method may also be used to evaluate the intracranial hemodynamic effects of other vasoactive drugs, even in clinical settings.

Administration, Cutaneous↗
PubMedDate not supplied

Effect of low-dose transdermal E2/NETA on the reduction of postmenopausal bone loss in women.

OBJECTIVE: To assess the efficacy of a continuous-combined transdermal patch (estradiol/ norethisterone acetate [E(2)/NETA] 25/125; Estragest TTS, Novartis, Basel, Switzerland) in the reduction of bone loss in postmenopausal women. DESIGN: In a 96-week, double-blind, randomized, multicenter, parallel study, 124 healthy women with an intact uterus more than 4 years after menopause received either transdermal continuous-combined E(2)/NETA (0.025/0.125 mg/day) or placebo patch for 24 treatment cycles; diet was normalized for calcium intake. Lumbar spine bone mineral density (BMD) ranged from 0.969 to 0.805 g/cm2 with a mean annual BMD decrement ranging from 3% to 8% within the last 24 months. BMD at lumbar spine L(2)-L(4) (postero-anterior) and femur were assessed by dual energy x-ray absorptiometry after 6, 12, and 24 cycles. Efficacy variables included measurement of biochemical markers of bone turnover (3, 6, 12, and 24 months). RESULTS: BMD at lumbar spine was significantly higher at all time points in the E(2)/NETA group than in the placebo group (P < 0.0001). Significant increases in BMD (P < 0.0008) from baseline were observed at all sites after 24 months in the E(2)/NETA group compared with placebo, which demonstrated a decrease from baseline. At endpoint, statistically significant decrements in the values of bone remodeling markers were observed (P < 0.05) with E(2)/NETA. CONCLUSIONS: E(2)/NETA 25/125 Estragest TTS was more effective than placebo in reducing the activation frequency of bone remodeling and in preventing bone loss at the spine and hip. Effects on the hip were similar to those observed for higher doses of estrogen.

Administration, Cutaneous↗
PubMed2003

Comparative in vivo evaluation of propranolol hydrochloride after oral and transdermal administration in rabbits.

The purpose of this study was the in vivo evaluation of orally and transdermally administered propranolol hydrochloride in rabbits. Transdermal patches of propranolol hydrochloride (PPN) were formulated employing ethyl cellulose and polyvinylpyrrolidone as film formers. The pharmacodynamic (PD) and pharmacokinetic (PK) performance of PPN following transdermal administration was compared with that of oral administration. This study was carried out in a randomized cross-over design in male New Zealand albino rabbits. The PK parameters such as maximum plasma concentration (C(max)), time for peak plasma concentration (t(max)), mean residence time (MRT) and area under the curve (AUC(0-alpha)) were significantly (P<0.01) different following transdermal administration compared to oral administration. The terminal elimination half-life (t(1/2)) of transdermally delivered PPN was found to be similar to that following oral administration. In contrast to oral delivery, a sustained therapeutic activity was observed over a period of 24 h after transdermal administration compared to oral administration. The relative bioavailability of PPN was increased about fivefold to sixfold after transdermal administration as compared to oral delivery. This may be due to the avoidance of first pass effect of PPN. The sustained therapeutic activity was due to the controlled release of drug into systemic circulation following transdermal administration.

Administration, Cutaneous↗
PubMedDate not supplied

Testosterone deficiency in women: etiologies, diagnosis, and emerging treatments.

Healthy young women produce approximately 300 microg of testosterone per day, of which about half is derived from the ovaries and half from the adrenal glands. In women, as in men, testosterone is thought to influence pubertal development, sexual function, bone density, muscle mass, erythropoiesis, energy, cognitive function and mood. Testosterone deficiency in women may result from a variety of conditions, including oophorectomy, adrenalectomy, adrenal disease, pituitary disease, HIV infection, premature ovarian failure, Turner's syndrome, and the use of high-dose corticosteroids and some estrogen preparations. Simple aging and natural menopause may also contribute to testosterone deficiency in some women. A consensus view of the diagnosis of female androgen deficiency syndrome (FADS) is currently being developed, and is summarized in this article, as are current approaches for treating testosterone deficiency in women. Recent clinical trials involving an experimental testosterone transdermal patch for women are highlighted. The impact of conventional ERT/HRT on testosterone levels in naturally menopausal women is discussed, with the differences between oral and transdermal routes of estrogen delivery being emphasized.

Administration, Cutaneous↗
PubMed2003

Transdermal selegiline: targeted effects on monoamine oxidases in the brain.

BACKGROUND: The oral administration of monoamine oxidase (MAO) inhibitors has the potential to cause a hypertensive reaction after the ingestion of tyramine-containing compounds. Because transdermal drug administration bypasses gastrointestinal absorption, it is possible that inhibition of MAO-A in brain may be achieved without enzyme inhibition in the gastrointestinal system, thereby eliminating the possibility of this drug interaction. These studies determined whether the transdermal administration of selegiline has differential effects on MAOs in brain versus the gastrointestinal system. METHODS: Rats were exposed to various doses of selegiline via a transdermal patch for up to 30 days, and MAO-A and MAO-B activities were determined in brain regions and gastrointestinal tissue. RESULTS: In all brain regions, transdermal selegiline, at doses that produced maximal MAO-B inhibition, led to a dose- and time-dependent MAO-A inhibition. The inhibition of MAOs in gastrointestinal tissue was less than that in brain, and doses that produced maximal MAO-A inhibition in brain inhibited MAO-A in gastrointestinal tissue by only 30%-40%. CONCLUSIONS: Results suggest that transdermal selegiline preferentially inhibits MAO-A in brain relative to the gastrointestinal system. As a consequence, transdermal selegiline should be devoid of the potential to cause a hypertensive reaction after the ingestion of tyramine-containing compounds.

Administration, Cutaneous↗
PubMed1992

Transdermal scopolamine as treatment of bradyarrhythmias.

Fifteen patients with different degrees of chronic bradyarrhythmias of supraventricular origin were studied with Holter monitoring before and during application of a transdermal patch of scopolamine. No changes were found in the mean or minimal heart rates, standard deviation of the RR interval, or the degree of bradyarrhythmia. It is concluded that transdermal scopolamine is not an adequate treatment of chronic symptomatic bradyarrhythmias.

Administration, Cutaneous↗
PubMedDate not supplied

Cessation of smoking rapidly decreases erectile dysfunction.

OBJECTIVE: To assess the relationship between cessation of smoking and rapid improvement in erectile capacity as well as the effect of nicotine patches on nocturnal penile tumescence and rigidity. METHODS: Nocturnal penile erections were studied in 10 smokers with use of the RigiScan portable home monitor. Two nights were monitored: for the first night, the patients had not stopped smoking; for the second night, the patients had stopped smoking for 24 hours. In addition, four men were monitored after cessation of smoking and wearing nicotine patches for 1 month. RESULTS: Multiple variables studied showed a statistically significant improvement in nocturnal penile tumescence and rigidity in the men who had stopped smoking for 24 hours. Continued improvement was noted in the four men who were monitored while not smoking and wearing nicotine patches for 1 month. CONCLUSION: Stopping cigarette smoking is a factor that rapidly improves penile tumescence and rigidity. Because the improvement continues while the patient is receiving nicotine from transdermal patches, some factor or factors other than the nicotine are responsible for the erectile dysfunction.

Journal Article↗
PubMed2003

Use of nicotine patches in breast-feeding mothers: transfer of nicotine and cotinine into human milk.

OBJECTIVE: Our objective was to assess the extent of exposure to nicotine and cotinine in breast-fed infants during maternal smoking and later during maternal use of the nicotine transdermal patch to achieve smoking cessation. METHODS: Fifteen lactating women (mean age, 32 years; mean weight, 72 kg) who were smokers (mean of 17 cigarettes per day) participated in a trial of the nicotine patch to assist in smoking cessation. Serial milk samples were collected from the women over sequential 24-hour periods when they were smoking and when they were stabilized on the 21-mg/d, 14-mg/d, and 7-mg/d nicotine patches. Nicotine and cotinine in milk were quantified by HPLC, and infant dose was calculated. Plasma concentrations of nicotine in the breast-fed infants were assessed, and the infants were also clinically assessed. RESULTS: Nicotine and cotinine concentrations in milk were not significantly different between smoking (mean of 17 cigarettes per day) and the 21-mg/d patch, but concentrations were significantly lower (P <.05) when patients were using the 14-mg/d and 7-mg/d patches than when smoking. There was also a downward trend in absolute infant dose (nicotine equivalents) from smoking or the 21-mg patch through to the 14-mg and 7-mg patches (P <.05 at both 14-mg and 7-mg doses, compared with smoking). Milk intake (shown as median and 25th to 75th percentile) by the breast-fed infants was similar while their mothers were smoking (585 mL/d [507-755 mL/d]) and subsequently when their mothers were using the 21-mg (717 mL/d [504-776 mL/d]), 14-mg (731 mL/d [535-864 mL/d]), and 7-mg (619 mL/d [520-706 mL/d]) patches (chi(2) = 3.19, P =.364). CONCLUSIONS: We conclude that the absolute infant dose of nicotine and its metabolite cotinine decreases by about 70% from when subjects were smoking or using the 21-mg patch to when they were using the 7-mg patch. In addition, use of the nicotine patch had no significant influence on the milk intake by the breast-fed infant. Undertaking maternal smoking cessation with the nicotine patch is, therefore, a safer option than continued smoking.

Administration, Cutaneous↗
PubMedDate not supplied

Markedly elevated levels of estrone sulfate after long-term oral, but not transdermal, administration of estradiol in postmenopausal women.

OBJECTIVE: To compare serum estrone sulfate (E1S) levels in postmenopausal women during long-term treatment with commonly prescribed doses of oral and transdermal estradiol (E2). DESIGN: A retrospective study performed in a University setting in the United States involving 33 healthy postmenopausal women. Two groups of postmenopausal women were studied: group 1 (n = 10) received 1 mg oral micronized E2 daily for 16 months; blood was drawn at 0, 7, and 15 months. Group 2 (n = 23) was randomized into three subgroups. Two of the subgroups (n = 8; n = 7) received E2 delivered at a rate of 0.05 mg/day and 0.1 mg/day, respectively, by transdermal patch, changed twice weekly; the third subgroup received a placebo (without E2) patch for 9 continuous months. Blood samples were drawn at 0, 6, and 9 months. Serum E1S and E2 were quantified by specific radioimmunoassays. Statistical analysis was performed by analysis of variance. RESULTS: After oral E2 treatment, E1S levels increased significantly (p < 0.01) from baseline, reaching an average level of 38.8 ng/mL at 15 months. After transdermal E2 treatment, E1S levels increased significantly, yet to a much lesser extent, reaching levels of 1.8 ng/mL and 3.2 ng/mL after 9 months of treatment with the 0.05 mg/day and 0.1 mg/day patches, respectively. CONCLUSIONS: Markedly elevated levels of E1S were found after long-term oral estrogen treatment. In comparison to the increase in E1S levels after long-term oral estrogen treatment, there was only a small increase in E1S levels after transdermal E2 therapy. This difference may be attributed to the higher dosage of oral E2 that is required because of the low bioavailability compared with the transdermal dosages.

Administration, Cutaneous↗
PubMed2000

A comparison of the abuse liability and dependence potential of nicotine patch, gum, spray and inhaler.

RATIONALE: Nicotine replacement therapy (NRT) in varying forms is becoming widely used. Clinicians, therapists and regulatory authorities are interested in the abuse liability and dependence potential of the different forms. OBJECTIVES: To compare the abuse liability and dependence potential of nicotine gum, transdermal patch, spray and inhaler. METHODS: 504 male and female smokers seeking help with stopping smoking were randomly allocated to the four products. Measures were taken at the designated quit date, then 1 week, 4 weeks, 12 weeks and 15 weeks later. Smokers were advised to use the product for up to 12 weeks. Those still using the product at the 12-week visit were advised to cease use by week 14. Measures included: pleasantness and satisfaction ratings at weeks 1 and 4 (used as a marker of abuse liability); ratings of feeling dependent on NRT at weeks 1, 4, 12 and 15 (used as a marker of subjective dependence); mood and physical symptoms ratings at weeks 12 and 15 (the change being used to assess physical dependence on NRT), continued usage of NRT at week 15 (used as an marker of behavioural dependence). RESULTS: Average ratings of pleasantness were low. The nicotine patch was rated as less unpleasant to use than all other products. There were no significant differences between the products in terms of satisfaction or subjective dependence except at week 15 when no patch users rated themselves as dependent. Continued use of NRT at week 15 was related to rate of delivery of nicotine from the products - 2% for patch, 7% for gum and inhaler, 10% for spray (P<0.05 for linear association). Among those

Adult↗
PubMed1988

Successful transdermal administration of therapeutic doses of a polypeptide to normal human volunteers.

The human stratum corneum constitutes a relatively impermeable barrier to the transdermal absorption of most substances, including polypeptides and proteins. This double-blind, randomized, crossover study in 13 normal men evaluated whether a low level of electrical current could induce changes in cutaneous permeability sufficient to produce absorption of a polypeptide. We compared cutaneous absorption of 5 mg of leuprolide (a 9 amino acid luteinizing hormone releasing hormone analogue) in transdermal patches containing 0.2 mA electrical current (active) and in patches containing no electrical current (passive). Serum luteinizing hormone (LH) concentration was measured 12 times during an 8-hour period as a measure of drug effect. Similar baseline LH levels were seen in each group: active = 11.3 +/- 3.1 mIU/ml and passive = 13.7 +/- 4.7 mIU/ml (p not significant). Significant elevations of LH were seen in active compared with passive patches (p = 0.0084). As predicted, passive patches produced no elevation of LH concentration (LH = 11.8 +/- 7.1 mIU/ml at 4 hours). However, active patches produced elevations comparable to those achieved with subcutaneous administration of the drug (LH = 56.4 +/- 49.6 mIU/ml at 4 hours and p = 0.003 compared with passive). The patches were well tolerated without significant cutaneous toxicity. It is concluded that the use of low levels of electrical current can induce changes in the permeability of the stratum corneum. These changes are sufficient to promote the transdermal absorption of therapeutically relevant amounts of a polypeptide. This has major importance for our understanding of skin permeability and for the development of new techniques for drug administration.

Double-Blind Method↗
PubMed2006

LC-MS/MS analysis of fentanyl and norfentanyl in a fatality due to application of multiple Durogesic transdermal therapeutic systems.

Fentanyl is a potent synthetic narcotic analgesic administered in the form of a transdermal patch for the management of chronic pain. A 78-year-old woman with a history of cancer was found dead in bed. She was lying on her back. The external examination revealed 10 Durogesic transdermal therapeutic systems (100 microg/h fentanyl) on the body. Liquid-liquid extraction and liquid chromatography tandem mass spectrometry with electrospray source in positive ionization mode was applied for the quantitation of fentanyl and its major metabolite norfentanyl in the post-mortem samples. Fentanyl-d5 and norfentanyl-d5 were used as internal standards. Multiple reaction monitoring was used for specific detection. Calibration was performed by addition of standard solutions to drug-free matrix (blood, urine and liver) prior to extraction. The method showed good linearity for fentanyl and norfentanyl over a concentration range of 5-150 microg/L in reconstituted extracts with coefficients of determination equal or greater than 0.998. Percent mean within-day precision and accuracy of 0.9-1.0% and 99.4-101.1% for fentanyl and 2.0-4.5% and 93.1-101.0% for norfentanyl were obtained. Mean extraction recoveries varied between 95.5% and 100.3% for fentanyl and 39.2-57.4% for norfentanyl. The following fentanyl (norfentanyl) concentration in the post-mortem samples were measured; 28.6 microg/L (3.0 microg/L) in right and 28.2 microg/L (3.5 microg/L) in left subclavian blood, 21.3 microg/L (<2 microg/L) in right and 20.9 microg/L (<2 microg/L) in left femoral blood, 37.6 microg/L (4.2 microg/L) in right and 33.9 microg/L (4.4 microg/L) in left ventricular blood, 282.9 microg/L (121.2 microg/L) in urine, 688.2 microg/L in stomach contents, 122.5 microg/L (25.4 microg/L) in bile, 19.5 microg/L (< 2 microg/L) in vitreous humour, 203.0 microg/kg (26.6 microg/kg) in liver and 78.6 microg/kg (46.3 microg/kg) in kidney. We concluded that the woman's death was caused by acute intoxication with fentanyl. The manner of death was presumed to be suicide due to excessive administered Durogesic transdermal therapeutic systems.

Administration, Cutaneous↗
PubMed1989

Three-years' experience of transdermal scopolamine: long-term effectiveness and side-effects.

A study was carried out in 68 otherwise healthy male naval crew members to assess the long-term effectiveness and side-effects of routine transdermal scopolamine administration for the prevention of seasickness. The transdermal patches were applied to the mastoid process before each sailing and the subjects generally used 2 patches a week. Check-ups were made every 3 months over a period of 3 years. The average reported seasickness severity (on a scale of 0 to 7) after 6 months at sea prior to the administration of transdermal scopolamine was 5.64 +/- 0.11 (mean +/- S.E.M.), in comparison with 3.14 +/- 0.23 post-administration (p less than 0.001). A significant improvement was found in the self-estimated performance at sea whilst receiving the drug: 65.7% +/- 3.38% (mean +/- S.E.M.), compared to 25% +/- 2.24% beforehand (p less than 0.001). Contact dermatitis precluded the use of transdermal scopolamine in 3 (4.4%) subjects. The only other significant side-effect was dryness of mucous membranes. In conclusion, transdermal scopolamine was found to be effective in the prevention of seasickness and improvement of performance at sea during 3 years of follow-up and routine administration of the drug was not complicated either by severe side-effects or by performance disturbances.

Administration, Cutaneous↗
PubMed2004

Human skin permeation of Delta8-tetrahydrocannabinol, cannabidiol and cannabinol.

The purpose of this study was to quantify the in-vitro human skin transdermal flux of Delta8-tetrahydrocannabinol (Delta8-THC), cannabidiol (CBD) and cannabinol (CBN). These cannabinoids are of interest because they are likely candidates for transdermal combination therapy. Differential thermal analysis and in-vitro diffusion studies with human tissue were completed for the compounds. Heats of fusion, melting points and relative thermodynamic activities were determined for the crystalline compounds, CBD and CBN. Flux, permeability, tissue concentration and lag times were measured in the diffusion experiments. CBN had a lower heat of fusion and corresponding higher calculated relative thermodynamic activity than CBD. Ethanol concentrations of 30 to 33% significantly increased the transdermal flux of Delta8-THC and CBD. Tissue concentrations of Delta8-THC were significantly higher than for CBN. Lag times for CBD were significantly smaller than for CBN. The permeabilities of CBD and CBN were 10-fold higher than for Delta8-THC. Combinations of these cannabinoids with ethanol will be further studied in transdermal patch formulations in vitro and in vivo, as significant flux levels of all the drugs were obtained. CBD, the most polar of the three drugs, and other more polar cannabinoids will also be the focus of future drug design studies for improved transdermal delivery rates.

Abdomen↗
PubMed1989

Antiparkinsonian efficacy of a novel transdermal delivery system for (+)-PHNO in MPTP-treated squirrel monkeys.

We examined the ability of the antiparkinsonian agent (+)-4-propyl-9-hydroxynaphthoxazine (PHNO) to enter the systemic circulation in therapeutic concentrations after continuous transdermal absorption in squirrel monkeys rendered parkinsonian by MPTP. Direct subcutaneous administration of (+)-PHNO in the dose range of 2.5 to 20 micrograms/kg restored locomotor activity to levels seen in normal monkeys for approximately 1 hour. Application of transdermal patches capable of delivering, into an infinite sink, an estimated 2.6 micrograms/cm2/h of (+)-PHNO over a skin surface area of 4.78 to 19.12 cm2 also restored locomotor activity to the normal range during a 24-hour period. We suggest the use of transdermal application of PHNO as a novel drug delivery system for the improved management of Parkinson's disease.

1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine↗
PubMed2002

Nicotine patches and the subjective effects of cigarette smoking: a pilot study.

Twenty-five per cent of the North American population smoke cigarettes regularly. Twelve smokers (aged 19 to 55 years, Fagerström test score 3 to 10) participated in a double-blind, placebo controlled, counterbalanced study to determine the extent to which subjective effects of smoking are altered by nicotine delivered by transdermal patches. Subjects wore a placebo or 21 mg nicotine patch while abstaining from smoking for 48 h. Nicotine-mediated objective and subjective effects were measured at baseline, and after smoking a regular and a low yield cigarette at four different study sessions. Subjective effects were assessed using validated computerized questionnaires such as the Profile of Mood States and Visual Analogue Scales. Nonsmoking compliance was determined by measuring expired air carbon monoxide and saliva cotinine concentrations. Significant within-session differences were found in subjective effects at baseline and after smoking. No differences in subjective effects were found between patch treatments before smoking. Nicotine withdrawal symptoms such as craving, irritability, tension, frustration, anxiety and restlessness were significantly increased in both patch conditions after 48 h of smoking abstinence. Smoking markedly ameliorated nicotine withdrawal symptoms. Systolic blood pressure increased after smoking in both patch conditions (P=0.01). Visual Analogue Scale scores for cravings, nicotine effects, good effects and 'high' consistently increased after smoking during either patch condition. Thus, wearing a nicotine patch did not seem to modify the subjective effects of smoking compared with placebo in this preliminary study.

Administration, Cutaneous↗
PubMed2002

Pulsed estrogen therapy: relieving climacteric symptoms, preventing postmenopausal bone loss.

Aerodiol with its new mode of action--pulsed estrogen therapy made possible by a unique pharmacokinetic profile and an innovative route of administration--acts on the full range of climacteric symptoms and on the long-term consequences of estrogen deprivation. Four well-designed, international studies investigating the efficacy of pulsed estrogen therapy on both the short- and long-term consequences of estrogen deprivation were conducted. Climacteric symptoms and their reduction were assessed individually and also using the Kupperman index, which is a weighted score. Aerodiol produced a significant reduction in the Kupperman index and in the occurrence of menopausal symptoms, such as hot flushes and night sweats. This reduction appeared to be significant as early as the second week of treatment. Moreover, Aerodiol remained effective even among highly symptomatic women with more than seven hot flushes per day, and also among smokers. Since it avoids hepatic first-pass metabolism, pulsed estrogen therapy also has a favorable action on the lipid profile, decreasing lipoprotein(a), apolipoprotein B, total cholesterol, and low-density lipoprotein cholesterol. Furthermore, Aerodiol is neutral with regard to clotting factors, angiotensinogen and insulin levels. The effect of pulsed estrogen therapy on bone has been assessed in both the short and the long term. Bone turnover, as measured by markers of resorption and formation, was normalized to premenopausal levels after 3 months of treatment at a dose of 300 microg/day. Aerodiol, again at the dose of 300 microg/day, is as effective as a 50-microg/day transdermal patch in increasing bone mineral density (p < 0.001 versus baseline) at the spine and hip after 56 weeks. Finally, data collected during the development of Aerodiol have shown that pulsed estrogen therapy is at least as effective as 2 mg of oral estrogen or 50 microg of transdermal estrogen in relieving climacteric symptoms and preventing postmenopausal bone loss.

Administration, Cutaneous↗
PubMed1995

Transdermal delivery of physostigmine. A pretreatment against organophosphate poisoning.

Physostigmine absorption through isolated human skin and inhibition of plasma and red blood cell cholinesterases in guinea-pigs have been measured to assess the feasibility of its transdermal delivery as a pretreatment for organophosphate poisoning. Penetration of radiolabelled physostigmine across human epidermis was measured in-vitro using glass diffusion cells and optimization of physostigmine delivery was achieved by changes in vehicle formulation and use of penetration enhancers. Two-component vehicles consisting of propionic acid/isopropyl myristate (50:50) and propionic acid/oleic acid (50:50) produced the highest transdermal delivery of physostigmine. A comparison of formulations containing propionic acid alone with propionic acid plus oleic acid when applied to guinea-pigs, showed that inclusion of oleic acid allowed the amount of physostigmine and the size of the transdermal patch to be substantially reduced, whilst maintaining effective delivery rates. The formulation containing oleic acid was not irritant to guinea-pigs when applied to the skin for 48 h. It is concluded that a mixture of propionic acid and oleic acid containing physostigmine is a good candidate for transdermal delivery of physostigmine as a pretreatment for organophosphate poisoning.

Administration, Cutaneous↗