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PubMed1990

Pharmacokinetics of estrogen.

The main types of pharmacologic therapy used to treat the hormone deficiency of menopause are parenteral and oral administrations of estrogen. Parenteral administration results in predictable absorption without major intermediary metabolism, whereas all oral estrogens are subject to intestinal metabolism before entering the systemic circulation. Various options are available. Injectable estrogens, because of rapid absorption and metabolism, are impractical for long-term replacement therapy. The primary drawback to subcutaneous estradiol pellets is the surgical procedure required for their insertion and removal. Vaginal epithelium is an effective pathway for absorption of estrogen given by solution, tablet, or cream, although only the latter is currently approved for clinical use; relatively constant serum levels of estradiol can be obtained with vaginal rings. Transdermal patches provide controlled hormone levels for up to 3.5 days. Although oral conjugated equine estrogens have been used extensively, they introduce types of estrogen, such as equilin, that are not naturally found in humans and that can produce a pronounced hepatic response. Micronized estradiol, oral estrone, and other estrogens have been used as alternatives to equine estrogens. Clinicians should understand the pharmacokinetics of the various options for replacement therapy and select a course of treatment that is safe, effective, and convenient for the patient.

Drug Administration Routes↗
PubMed1988

Individual responses to transdermal nitrates after chronic administration in angina pectoris.

The aim of this study was to investigate whether, and to which extent, sustained treatment with transdermal nitroglycerin plasters may lead to the development of tolerance in patients with effort-induced angina pectoris. Ten patients, all men, mean age 62.7 years, took part in a double-blind, cross-over, acute study, comparing the transdermal therapeutic system of nitroglycerin 10 mg/24 hours with placebo. Patients were then treated for 1 month with the active drug in single-blind condition, and finally they took part in a further acute study identical to the first. Cycloergometric exercise tests were carried out 4 hours after dosing. In comparison with placebo, the active drug significantly (P less than 0.01) increased ischaemic threshold (ST depression = 1 mm) after both acute (from 299 +- 92 to 413 +- 120 sec) and chronic treatment (416 +- 107 sec). The same results were obtained for exercise duration to peak exercise (acute study: from 336 +- 65 to 482 +- 90 sec; chronic treatment: 466 +- 118 sec). The final acute study confirmed the stability of angina, showing that the improvement in exercise tolerance after chronic treatment was entirely due to the pharmacological effect of the drug. In terms of single patient response to the active treatment, 7 of the 10 patients showed an improvement in exercise tolerance after both acute and chronic treatment, while in 3 patients no antianginal effect was observed. These results suggest that nitrate tolerance cannot be considered an inevitable finding in patients chronically treated with transdermal patches.

Administration, Cutaneous↗
PubMed1991

Evaluation of the primary skin irritation and allergic contact sensitization potential of transdermal triprolidine.

A transdermal patch for the OTC antihistamine, triprolidine (TP), might provide benefits in terms of increased efficacy and reduced sedative side effects. However, concerns over potential irritant or allergic contact sensitization (ACS) skin reactions necessitated through skin toxicity testing before and during initial clinical development. Initial effort was expended on development of a binary vehicle delivery system comprised of TP in 0.5% oleic acid (OA) in propylene glycol (PG). Rabbit skin irritation and Buehler guinea pig skin sensitization testing indicated that this TP/OA/PG formula had both skin irritation and ACS potential. Both tests underestimated, to some degree, the skin toxicities observed in later clinical testing. In clinical tests, skin irritation was due mainly to the OA/PG vehicle, but was enhanced in the presence of high TP concentrations. Of 26 subjects enrolled in a rising dose clinical pharmacokinetics study, one subject exposed twice to TP/OA/PG presented with delayed skin reactions suggestive of ACS. Positive diagnostic patch test results for this subject and four out of five other twice-exposed study subjects suggested that the TP/OA/PG formula had a very high ACS potential. Subsequent predictive clinical patch testing was conducted with a buffered aqueous TP formula which provided in vitro skin penetration of the drug equivalent to the TP/OA/PG formula. These clinical studies demonstrated that TP itself had no significant irritation potential but still induced ACS reactions in a high proportion of test subjects. The incidence of adverse skin reactions to TP was considered to be too high relative to the degree of improved therapeutic benefit of this delivery form. On this basis, all technology development effort was discontinued.

Administration, Cutaneous↗
PubMed1991

Topical application of clonidine relieves hyperalgesia in patients with sympathetically maintained pain.

Patients with reflex sympathetic dystrophy or causalgia characteristically have ongoing pain and pain to light touch (hyperalgesia). Some of these patients obtain relief of their pain following interruption of sympathetic function to the affected area and, therefore, have sympathetically maintained pain (SMP). Evidence suggests that the pain and hyperalgesia in SMP are related to activation of peripheral adrenergic receptors. We wished to determine the contribution of alpha 1- and alpha 2-adrenergic receptors in SMP and thus examined the effects of local application of adrenergic agents in patients with SMP. The alpha 2-adrenergic agonist clonidine, available as a transdermal patch, was delivered topically to the patients' hyperalgesic skin. In four patients with SMP, clonidine eliminated or substantially reduced hyperalgesia to mechanical and cold stimuli. In three of these patients the effects were confined to the skin region beneath the patch, suggesting a peripheral and not central effect. The relief of hyperalgesia was not due to a local anesthetic effect since touch thresholds were unaffected. Topical clonidine did not relieve hyperalgesia of similar severity for two other patients whose hyperalgesia and pain were unaffected by sympathetic ganglion blocks (i.e., diagnosed as having sympathetically independent pain). In two SMP patients, intradermal injection of norepinephrine or phenylephrine (a specific alpha 1-adrenergic agonist) at a site treated with clonidine evoked intense pain and rekindled the pre-clonidine hyperalgesia at that site. It is likely that clonidine locally blocks the release of norepinephrine via activation of alpha 2 receptors on the sympathetic terminals. This study suggests, therefore, that SMP is mediated via alpha 1-adrenergic receptors located in the affected tissue.

Administration, Cutaneous↗
PubMed1994

Effects of exposure to nicotine and to sidestream smoke on pregnancy outcome in rats.

Nicotine-delivering transdermal patches were applied to the back of timed-pregnant Sprague-Dawley rats. Pregnancy failure was 100% in animals exposed to 3.5 mg of nicotine per day during the entire pregnancy and 50% in animals exposed to the same amount during the first trimester. Application of 1.75 mg of nicotine per day resulted in a 50% pregnancy failure when exposure occurred during the entire pregnancy. In animals exposed for the first half of pregnancy to cigarette sidestream smoke, under conditions where plasma nicotine levels reached about 25% of those observed following exposure to 1.75 mg of nicotine per day, the average litter size was reduced by about 25%. It is concluded that continuous exposure to nicotine early during pregnancy may adversely affect pregnancy outcome in rats.

Administration, Cutaneous↗
PubMed1994

Bone metabolism changes after transdermal estradiol dose reduction during estrogen replacement therapy: a 1-year prospective study.

Twenty-four surgically menopausal women were randomly allocated to one of two transdermally-administered estrogen replacement therapies (ERT): Group A was administered Estradiol (E2) TTS 0.05 mg/day for 6 months and 0.025 mg/day for the following six months and group B, E2 TTS 0.10 mg/day for the first 6 months and 0.05 mg/day for the following 6 months. For both groups, the treatment regimen was based upon the twice-weekly application of transdermal patches to the lower abdomen for three weeks a month. Serum E2, alkaline phosphatase (AP), osteocalcin (BGP) and urinary hydroxyproline (OHP) excretion levels were measured before the operation, at the beginning of ERT and after 6 and 12 months of treatment. Bone mineral density (BMD) in the distal regions of the forearms was measured by single photon absorptiometry at the start of the study and after 6 and 12 months. In Group A, both mean cortical and trabecular BMD had increased by, respectively, 1.53% and 2.17% after 6 months of therapy; after the second 6 months a significant decrease was observed in both parameters (2.40% and 3.62%, respectively). In Group B, mean cortical and trabecular BMD increased by 1.50% and 2.10%, respectively (significant increase in trabecular bone) after the first 6 months of treatment; after the following 6 months, these values persisted (+0.15 and -0.03%, respectively). Mean AP, OHP and BGP serum levels rose after the operation. In Group A, AP and OHP showed a significant decrease after the first 6 months (-34.90% and -30.90%), followed by an increase at the last evaluation of 22.50% and 35.50%, that reached statistical significance only for OHP.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Cutaneous↗
PubMed1996

Comparative bioavailability study of an once-a-week matrix versus a twice-a-week reservoir transdermal estradiol delivery systems in postmenopausal women.

An open-label, randomised, crossover study was conducted with in healthy postmenopausal women to compare the relative bioavailability of a matrix transdermal estradiol delivery system worn for 7 consecutive days, versus a reservoir transdermal patch worn for 4 days followed by its immediate replacement by another patch worn for further 3 consecutive days. There was a minimum 7-day washout period between the two study periods. Both systems were labelled to release approximately 50 micrograms/day of estradiol. Twenty-six subjects were evaluated with regard to estradiol serum levels. Blood samples were taken immediately before and at regular intervals until 192 h after the initiation of each study treatment (patch application) and assayed for estradiol. There was no difference between the patches with regard to Cmax. Based on the relative bioavailability, one matrix patch proved to be bioequivalent to two reservoir patches worn consecutively for 7 days. These results demonstrate the ability of one matrix patch to deliver consistent therapeutic levels of estradiol over a 7-day period.

Administration, Cutaneous↗
PubMed1995

Ulcerative colitis responsive to smoking and to nicotine chewing gum in a patient with alpha 1 anti-trypsin deficiency.

Ulcerative colitis is one of the few diseases in which smoking appears to confer some benefit (1). We report a patient whose ulcerative colitis deteriorated on several occasions on stopping cigarettes, and improved on restarting smoking. As a result, she continued smoking despite developing airflow limitation and severe emphysema. She was subsequently found to have alpha 1 anti-trypsin deficiency. She later noticed that she could get a similar benefit in her colitis with nicotine chewing gum as she had with cigarettes. For patients with smoking-responsive ulcerative colitis, non-tobacco forms of nicotine delivery such as gum or transdermal patches should be considered to avoid the hazards of cigarette smoke.

Colitis, Ulcerative↗
PubMed2005

Combined hormonal contraception.

This article discusses the different combined hormonal contraception methods. Combined methods, delivering both estrogen and a progestin simultaneously, are among the most effective, widely used hormonal contraceptive options. They also have the best noncontraceptive benefit profile for young women of all hormonal contraceptive options. Oral contraceptive pills (OCPs) are described as the standard combined hormonal method and are discussed in detail. Newer combined hormonal contraceptive delivery systems, the transdermal patch, vaginal ring, and injectable form, are compared with OCPs in terms of pharmacology, efficacy, and adverse events. Advantages and disadvantages of all methods are emphasized, with particular attention to adolescent development and acceptability.

Adolescent↗
PubMed2005

Contraception: an international perspective.

Although it is estimated that the population growth rate will decline to a replacement level by 2050, it is also now predicted that the total world population will reach 8.9 billion in that year -- far higher than the 2004 estimate of 6.4 billion. More than 26 billion new couples will need contraceptives in the next half century. Although a steady increase in contraceptive use has been observed in both developed and developing countries, the contraceptive needs of a high percentage of couples have not yet been met and the number of unplanned pregnancies continues to increase. The actual use of contraception differs from region to region. Although no new method has been registered for many years, several new products have been marketed during the last 5. Among these are new implants, medicated intrauterine systems, contraceptive vaginal rings, transdermal patches and several new combined oral contraceptive formulations. New contraceptive methods have been developed to meet the objectives of expanding contraceptive choices for both women and men and answering an unmet need for contraceptives with a long-term action that meet the expectations of consumers. Simplicity, reversibility and effectiveness are the desired features of a male contraceptive, but no new male contraceptive method is yet available. New areas of basic research include studies on genes, proteins and enzymes involved in the reproductive system. The new methods will be targeted to specific interactions within the reproductive system at the level of ovaries and testes, as well as between spermatozoa and ova. This futuristic approach still keeps in mind the need for better access to existing contraceptive methods, as well as the discovery of new contraceptives that are simple to use, safe, reversible and inexpensive. In the future, contraceptives may be combined with other medicinal agents to provide dual protection against both pregnancy and other preventable conditions, such as sexually transmitted infections.

Contraception↗
PubMed2006

ORTHO birth control satisfaction assessment tool: assessing sensitivity to change and predictors of satisfaction.

OBJECTIVE: To test the sensitivity to change of the ORTHO Birth Control Satisfaction Assessment Tool (ORTHO BC-SAT) among dissatisfied women switching to a new hormonal birth control method and to better understand which factors contribute to a woman's satisfaction with the method. MATERIALS AND METHODS: Women switching to a new hormonal birth control method [oral contraceptives (OCs), injections, vaginal ring or transdermal patch] completed the ORTHO BC-SAT, a questionnaire measuring satisfaction, two times over a 3-month period. Sensitivity to change was measured by examining change scores, as well as the Guyatt's statistic. Predictors of satisfaction were examined using forward-stepping linear regression. RESULTS: Fifty-six women completed the ORTHO BC-SAT twice. With the exception of Future Fertility Concerns, women reported statistically significant improvements on all scales of the questionnaire. The scales most sensitive to change were Overall Satisfaction, Assurance/Confidence, Lifestyle Impact, and Ease of Use/Convenience. Being older, switching from a nonhormonal method of birth control at baseline and more bodily pain at baseline predicted the increase in satisfaction scales. CONCLUSION: The ORTHO BC-SAT has demonstrated sensitivity to change in this population. In addition, we identified several factors at baseline that predicted an increase in satisfaction scale scores.

Adolescent↗
PubMed2004

Pretreatment with transdermal nicotine enhances some of ethanol's acute effects in men.

Nicotine and alcohol are often consumed together and smokers are more likely than non-smokers to drink alcohol. In spite of the high prevalence of the combined use of alcohol and nicotine, only a few laboratory studies have examined the effects of this drug combination in humans. The present study was conducted to further investigate the nature of nicotine/alcohol interactions by examining whether nicotine pretreatment via a transdermal patch (placebo or 21 mg) alters the subjective and physiologic effects of acute ethanol (0.4 and 0.7 g/kg) administration. Twelve male smokers who drank alcohol on an occasional basis provided informed consent to participate in the study. Subjective reports of feeling drunk, feeling ethanol's effects and ethanol-induced euphoria were increased by nicotine pretreatment. In addition, reports of desire to smoke a tobacco cigarette were significantly elevated after ethanol administration and were most pronounced during the active nicotine conditions. Heart rate was elevated by nicotine and ethanol-induced increases in heart rate were enhanced by nicotine pretreatment. The time to peak ethanol concentration was faster in the nicotine-patch condition and this paralleled the more rapid detection of ethanol effects after drinking the low-dose beverage. These findings suggest that nicotine enhances some of the positive subjective effects of acute ethanol and may help explain the high prevalence of the combined use of these two drugs.

Administration, Cutaneous↗
PubMed2006

Limonene GP1/PG organogel as a vehicle in transdermal delivery of haloperidol.

Penetration enhancers are a classical means for improving transdermal drug delivery (TDD). Enhancers permeate into the skin and reversibly decrease the barrier resistance. Basically, our aim is to formulate a transdermal gel containing an appropriate enhancer for a controlled drug release. Terpenes, namely limonene, linalool and cineole, in propylene glycol (PG) were first investigated in vitro for their capacity to enhance the percutaneous release of an anti-psychotic drug, haloperidol (HP). Relative to oxygenated linalool and cineole, hydrocarbon limonene was more effective as a skin enhancer; it increased human skin permeability and decreased lag time. Limonene was thus incorporated in an organogel comprised of gelator GP1 and PG. This skin-friendly gel in a transdermal patch could act as a long-acting formulation that delivers HP at a sustained percutaneous rate. The microscopic framework of the organogel is a branched network of interlocking fibres. Varying the gelator content modulates the fibre density and gel stiffness, and presents different degrees of resistance to drug diffusion on the vehicle side. Rheological and permeation studies demonstrated that an increase in gelator concentration increased gel moduli and decreased drug flux simultaneously. The rheology of the gel matrix influenced drug release rate in a manner described by several experimentally-derived correlations.

Administration, Cutaneous↗
PubMed2006

Rheological studies on pressure-sensitive silicone adhesives and drug-in-adhesive layers as a means to characterise adhesive performance.

Pressure-sensitive adhesives are viscoelastic polymers used in the formulation of transdermal patches that allow attachment of a patch onto the skin. Established criteria exist that correlate viscoelastic parameters with adhesive performance. In this study, fulfillment of the adhesive performance criteria was examined using two silicone adhesives with different tack properties. The viscoelastic parameters of high and low tack silicone adhesives (BIO-PSA High Tack 7-4302 and BIO-PSA Low Tack 7-4102) were determined and compared with the criteria described by Chu and Dahlquist. Drug-in-adhesive layers were prepared using the high tack adhesive combined with nortriptyline HCl or paracetamol. The effect of drug addition on the viscoelastic properties of the adhesive was examined. The high tack adhesive showed congruence with the established criteria although with a modified range of viscoelastic moduli to that described by Chu. Examination of the low tack adhesive showed that it did not possess the appropriate viscoelastic properties for bonding onto the skin. The addition of the drugs into the high tack adhesive caused a concentration-dependent increase in its cohesive strength. This effect was independent of the physicochemical properties of the drugs tested.

Acetaminophen↗
PubMed2007

Depo Now: preventing unintended pregnancies among adolescents and young adults.

PURPOSE: We compared the immediate administration of DMPA (Depo Now) to the immediate use of short-term hormonal methods that served as a "bridge method" until later DMPA initiation. We examined whether Depo Now, as compared to initiating with a bridge method (pills, transdermal patch, or vaginal ring), resulted in greater DMPA continuation at six months. METHODS: Young women aged 14 to 26 years seeking to use DMPA were randomized (nonblinded) after meeting eligibility criteria to either the Depo Now (n = 101) or bridge method (n = 232) group. Depo Now subjects received their first injection of DMPA at the conclusion of their first visit provided each was medically suitable and had a negative urine pregnancy test regardless of menstrual cycle day. Those assigned to the bridge method group were allowed to choose their starting contraceptive method and it was provided at the first visit. All subjects were told to return to the clinic in 21 days to repeat the urine pregnancy test, and among those who were assigned to use a bridge method, to receive their first injection of DMPA. All subjects were followed to their third injection, or about 6 months later. RESULTS: Those randomized to a bridge method were 1.8 (1.1, 2.9) times more likely than Depo Now subjects to return for their 21-day repeat pregnancy test, but only 55% (n = 125) of these young women actually received their first DMPA injection. Continuation rates at the third injection were 29.7% (n = 30) for those in the Depo Now group and 21.1% (n = 49) for those assigned to the bridge method (p = .09). Three factors were significantly associated with adherence to the third injection: randomized to Depo Now group, knowing more women who use DMPA, and returning to clinic for the 21-day repeat pregnancy test visit. Finally, 28 pregnancies were diagnosed during the study period, and those in the bridge method group were almost 4.0 (1.2, 13.4) times more likely to be diagnosed with a pregnancy than those in the Depo Now group. CONCLUSIONS: Immediate administration of DMPA is associated with improved adherence to DMPA continuation and fewer pregnancies.

Adolescent↗
PubMed2004

Insertion of microneedles into skin: measurement and prediction of insertion force and needle fracture force.

As a hybrid between a hypodermic needle and transdermal patch, we have used microfabrication technology to make arrays of micron-scale needles that transport drugs and other compounds across the skin without causing pain. However, not all microneedle geometries are able to insert into skin at reasonable forces and without breaking. In this study, we experimentally measured and theoretically modeled two critical mechanical events associated with microneedles: the force required to insert microneedles into living skin and the force needles can withstand before fracturing. Over the range of microneedle geometries investigated, insertion force was found to vary linearly with the interfacial area of the needle tip. Measured insertion forces ranged from approximately 0.1-3N, which is sufficiently low to permit insertion by hand. The force required to fracture microneedles was found to increase with increasing wall thickness, wall angle, and possibly tip radius, in agreement with finite element simulations and a thin shell analytical model. For almost all geometries considered, the margin of safety, or the ratio of fracture force to insertion force, was much greater than one and was found to increase with increasing wall thickness and decreasing tip radius. Together, these results provide the ability to predict insertion and fracture forces, which facilitates rational design of microneedles with robust mechanical properties.

Drug Delivery Systems↗
PubMed2004

Drug delivery systems for oestrogenic hormones and antagonists: the need for selective targeting in estradiol-dependent cancers.

The pleiotropic activity of oestrogens and their mechanism of action via their binding to the two oestrogen receptors alpha (ER alpha) and beta (ER beta) subtypes in the different tissues where oestrogens exert their action have been briefly described. The fate of these compounds trapped into different galenic forms is discussed with regard to their therapeutic applications. Firstly, the advantages and disadvantages of the different forms (pills, i.v. forms and transdermal patches) used in contraception are compared. Secondly, the therapeutic use of formulated oestrogens for the post-menopausal hormone replacement therapy (HRT) is analysed through the various results obtained in different trials. The link between HRT and the risks of breast cancer and cardiovascular disease is underlined. Finally, comparing the activity of selective oestrogen receptor modulators such as tamoxifen and pure anti-oestrogens such as RU58668 and ICI182780, we analysed the reasons leading to the need for a tumor targeting of the latters, but not of the former for the treatment of oestrogen-dependent breast cancer. Different injectable and biodegradable formulations, that lead to a remarkable anti-tumor efficiency in xenografts, have been recently developed and we believe that they may represent promising new administration ways of added therapeutic values for anti-oestrogens. Such devices could be extended to the delivery of other anti-cancer drugs with more aggressive activities than anti-oestrogens.

Antineoplastic Agents, Hormonal↗
PubMed2004

Does hormone therapy increase allergic reactions and upper gastrointestinal problems? Results from a population-based study of Swedish woman. The women's health in the Lund area (WHILA) study.

OBJECTIVES: To delineate the use of various drugs particularly pertaining to allergy and upper gastrointestinal problems in relation to hormone status in middle aged women. METHODS: An analysis from a population-based study on women born between 1935 and 1945 and lived in the Lund area southern Sweden. Of 10,766 women, 6,917 provided complete data sets; in turn 5,673 were assessed for the use of medication in this study. Among the cohort, 9% of women were premenopausal (PM), 54% were postmenopausal without hormone replacement therapy (PM0) and 37% were current hormone replacement therapy users (PMT). RESULTS: There were 7 (1.3%) women in PM, 11 (0.4%) in PM0 and 21 (1.0%) in PMT group who used loratadine regularly. There was a significant difference between the PM and PM0 groups and also between the PM0 and PMT groups in the use of loratadine (P < 0.05 ). Among 21 loratadine users in PMT group 4 (19%) used transdermal patches and 17 (81%) used oral HRT. The result for omeprazole use was as follows: 4 (0.8%) of PM group, 39 (1.3%) of PM0 group and 42 (2.0%) of PMT group. The use of omeprazole was significantly higher in the PMT group than in the PM (P = 0.05 ) and PM0 group (P < 0.05 ). There was no relation between the use of omeprazole and smoking or alcohol consumption. CONCLUSIONS: Use of hormone replacement therapy seems to be related to a higher frequency of omeprazole and loratadine use, which implies that hormone replacement therapy, may be associated with more upper gastrointestinal symptoms as well as allergy.

Aged↗