Extended regimen of a levonorgestrel/ethinyl estradiol transdermal delivery system: Predicted serum hormone levels using a population pharmacokinetic model.

Objective: This study employed population pharmacokinetic (popPK) models to predict levonorgestrel (LNG) and ethinyl estradiol (EE) exposure after dosing with the transdermal contraceptive TWIRLA® (LNG/EE TDS) as a 12-week extended regimen in a healthy female population.

Methods: PopPK models were developed using data from a previously published phase 1, open-label, randomized clinical trial, ATI-CL14 (NCT01243580), in 36 healthy individuals. Models used cycle 2 data from 18 individuals who received the LNG/EE TDS, delivering LNG 120 μg/day and EE 30 μg/day, followed by a 1-week TDS-free period.

Hydrothermal Degradation of Amino Acids.

Within the past years, hydrothermal processes have gathered much attention as promising conversion technologies for especially wet biomass. Amino acids are an integral component of biomass, zoo biomass in particular. However, what happens to them during hydrothermal treatment? Reviewing the available literature going back to the mid of the 20th century revealed an astonishing, but still fragmentary view.

Nitrogen-Containing Hydrochar: The Influence of Nitrogen-Containing Compounds on the Hydrochar Formation.

Hydrothermal carbonization (HTC) of fructose and urea containing solutions was conducted at 180 °C to study the influence of nitrogen-containing compounds on conversion and product properties. The concentration of fructose was fixed, while the concentration of urea was gradually increased to study its influence on the formation of nitrogen-containing hydrochar (N-HC). The degradation of urea has an important influence on the HTC of fructose.

Influence of the pH Value on the Hydrothermal Degradation of Fructose.

The hydrothermal treatment of sugars features a promising technology for the production of fine and platform chemicals from renewable resources. In this work the hydrothermal decomposition of fructose was studied in a buffered medium at a pH range between 2.2 and 8.

Intranasal carbetocin reduces hyperphagia in individuals with Prader-Willi syndrome.

Background: Prader-Willi syndrome (PWS) is a genetic neurodevelopmental disorder of life-threatening hyperphagia, obesity, intellectual deficits, compulsivity, and other behavioral problems. The efficacy and safety of i.n.

An Evaluation of the Pharmacodynamics, Safety, and Tolerability of the Potassium Binder RDX7675.

Hyperkalemia is common in patients with heart failure or chronic kidney disease, particularly those taking renin-angiotensin-aldosterone system inhibitors, and can cause arrhythmias and sudden cardiac death. The most widely used treatment, sodium polystyrene sulfonate (SPS), limits gastrointestinal potassium absorption, but has poor palatability. RDX7675 (RDX227675) is the calcium salt of a reengineered polystyrene sulfonate-based resin with improved palatability over SPS.

Evaluation of the Pharmacodynamic Effects of the Potassium Binder RDX7675 in Mice.

Introduction: Hyperkalemia is a common complication in patients with heart failure or chronic kidney disease, particularly those who are taking inhibitors of the renin-angiotensin-aldosterone system. RDX7675, the calcium salt of a reengineered polystyrene sulfonate-based resin, is a potassium binder that is being investigated as a novel treatment for hyperkalemia. This study evaluated the pharmacodynamic effects of RDX7675 in mice, compared to 2 current treatments, sodium polystyrene sulfonate (SPS) and patiromer.

Palatability and physical properties of potassium-binding resin RDX7675: comparison with sodium polystyrene sulfonate.

Background: Hyperkalemia is a potentially life-threatening condition that patients with heart failure or chronic kidney disease, especially those taking renin-angiotensin-aldosterone system inhibitors, are at high risk of developing. Sodium polystyrene sulfonate (SPS), a current treatment, binds potassium within the gastrointestinal tract to reduce potassium absorption. However, poor palatability limits its long-term use.

Analytical pharmacology and the elucidation of function.

James Black believed that analysis of biological assays provides insights into the operation of physiological control systems. In this paper, we illustrate this point in three 'cardiovascular' assays. The first determined the half-life (t½) of 'endothelium-derived relaxing factor' (EDRF), using bradykinin to release EDRF, which produced concentration-related relaxations of a precontracted artery.

A new approach to assessing the structural total peripheral resistance amplifier in renal (Page) hypertension in conscious rabbits.

Background And Aim: Structural changes in the large resistance vessels in hypertension amplify resistance responses in vitro, but their role in vivo has been controversial. To resolve this matter, we re-examined earlier data in Page hypertension.

Methods: Total peripheral resistance (TPR) and total peripheral conductance (TPC) responsiveness were compared in hypertensive and normotensive rabbits, 5 weeks after bilateral renal cellophane wrapping or sham operation.

A randomized controlled trial of a low-dose combined oral contraceptive containing 3 mg drospirenone plus 20 microg ethinylestradiol in the treatment of acne vulgaris: lesion counts, investigator ratings and subject self-assessment.

Objective: To assess the efficacy of a combined oral contraceptive (COC) containing 3 mg drospirenone (drsp) plus 20 microg ethinylestradiol (EE) administered in 24 days of active treatment followed by a four-day hormone-free interval (24/4 regimen) compared with placebo for the treatment of moderate acne vulgaris.

Methods: Healthy females (14-45 years old) with moderate facial acne were randomized to 3 mg drsp/20 microg EE 24/4 (n = 270) or placebo (n = 268) for six cycles. The secondary efficacy variables measured included change from baseline to endpoint (cycle 6) in individual lesion count for nodules, papules, pustules, open and closed comedones.

A double-blind, randomized, saline-controlled study of the efficacy and safety of EUFLEXXA for treatment of painful osteoarthritis of the knee, with an open-label safety extension (the FLEXX trial).

Objective: To report the FLEXX trial, the first well-controlled study assessing the safety and efficacy of Euflexxa (1% sodium hyaluronate; IA-BioHA) therapy for knee osteoarthritis (OA) at 26 weeks.

Methods: This was a randomized, double-blind, multicenter, saline-controlled study. Subjects with chronic knee OA were randomized to 3 weekly intra-articular (IA) injections of either buffered saline (IA-SA) or IA-BioHA (20 mg/2 ml).

Bleeding patterns associated with non-oral hormonal contraceptives: a review of the literature.

It is generally accepted that poor tolerance to changes in vaginal bleeding associated with hormonal contraceptive use may influence compliance and continuation with the chosen method. However, disparities in the collation and reporting of bleeding data hamper comparison among studies and products. In this review, we systematically assessed MEDLINE and EMBASE for articles assessing parenteral hormonal contraceptives that reported bleeding data based on reference periods as recommended by the World Health Organization (WHO).

Treatment of acne using a 3-milligram drospirenone/20-microgram ethinyl estradiol oral contraceptive administered in a 24/4 regimen: a randomized controlled trial.

Objective: To assess the efficacy of the combined oral contraceptive containing 3-mg drospirenone/20-microgram ethinyl estradiol (3-mg drospirenone/20-microgram ethinyl estradiol) administered as 24 consecutive days of active treatment after a 4-day hormone-free interval (24/4 regimen) compared with placebo for the treatment of moderate acne vulgaris.

Methods: Healthy females aged 14-45 years with moderate acne were randomized in this double-blind study to 3-mg drospirenone/20-microgram ethinyl estradiol (n=270) or placebo (n=268) for six cycles of 28 days. The primary outcome measures of acne lesion counts and Investigator Static Global Assessment scale ratings were assessed at baseline and during cycles 1, 3, and 6.

A combined oral contraceptive containing 3-mg drospirenone/ 20-microg ethinyl estradiol in the treatment of acne vulgaris: a randomized, double-blind, placebo-controlled study evaluating lesion counts and participant self-assessment.

This study compared the efficacy of a low-dose combined oral contraceptive (COC) containing 3-mg drospirenone and 20-microg ethinyl estradiol (3-mg DRSP/20-microg EE) administered in a 24-day active pill/4-day inert pill (24/4) regimen and placebo in women with moderate acne vulgaris during 6 treatment cycles. A total of 534 participants were randomized and dispensed study medication (n = 266 [3-mg DRSP/20-microg EE 24/4 regimen COC group]; n = 268 [placebo group]). Women of reproductive age were eligible for inclusion in the study.

Efficacy and safety of 3 mg drospirenone/20 mcg ethinylestradiol oral contraceptive administered in 24/4 regimen in the treatment of acne vulgaris: a randomized, double-blind, placebo-controlled trial.

Background: A randomized, double-blind, parallel-group study to investigate the efficacy and safety of the 3 mg drospirenone (drsp)/20 mcg ethinylestradiol (EE) combined oral contraceptive (COC) administered in a 24/4 regimen (24 active tablets and 4 inert tablets per cycle) for the treatment of moderate acne vulgaris.

Study Design: Healthy females (aged 14-45 years old) with moderate facial acne were randomized to 3 mg drsp/20 mcg (n=266) or placebo (n=268) for six cycles of 28 days.

Results: Women who received the 3 mg drsp/20 mcg EE 24/4 COC had greater reductions from baseline in inflammatory, noninflammatory and total lesion counts.

Differences in symptom scores and health outcomes in premenstrual syndrome.

Background: In studies of premenstrual syndrome (PMS), a significant response to treatment is commonly defined as a 50% reduction in symptom scores, but empirical support for this definition is lacking. We compared healthcare utilization in women with and without PMS according to the Daily Record of Severity of Problems (DRSP) scores in order to determine the degree of symptomatic variation in premenstrual symptoms associated with differences in the burden of illness.

Methods: Participants were women aged 18-45 years enrolled in a medical group in southern California.

Bleeding patterns associated with oral contraceptive use: a review of the literature.

The regulation of vaginal bleeding is an important effect impacting the choice of contraceptive methods. However, comparing vaginal bleeding control and disturbance between various contraceptive studies is often limited by the lack of uniformity in the analysis and reporting of the bleeding patterns. In 1986, the World Health Organization (WHO) issued recommendations for the standardized collection, analysis and reporting of bleeding associated with contraceptives based on 90-day reference periods.

3-alkyl- and 3-aryl-(7-oxo-7H-furo[3, 2-g]chromen-5-yl)alkanoic acids as inhibitors of leukotriene B4 biosynthesis.

The synthesis and biological properties of 3-alkyl-and 3-aryl-(7-oxo-7H-furo [3, 2-g]chromen-5-yl)alkanoic acids are described. The compounds were evaluated for their ability to inhibit soybean 15-lipoxygenase (15-LO) and the production of leukotriene B(4) (LTB(4)) in bovine polymorphonuclear leukocytes. The furocoumarins were further investigated for their lipophilicity and their capacity to photobleach N, N-dimethyl-p-nitrosoaniline (RNO) after irradiation with UVA light.

3-Alkyl- and 3-aryl-7H-furo[3,2-g]-1-benzopyran-7-ones: synthesis, photoreactivity, and fluorescence properties.

A series of 3-alkyl- and 3-aryl-7H-furo[3, 2-g]-1-benzopyran-7-ones, known as linear furocoumarins, was synthesized and evaluated for their dark- and photobinding (crosslink formation) with DNA as well as for their spectrophotometric and fluorescent properties, lipophilicity, and ability to photobleach N, N-dimethyl-p-nitrosoaniline (RNO) after irradiation with UVA light. 8-Methoxypsoralen (8-MOP, 9-methoxy-7H-furo[3, 2-g]-1-benzopyran-7-one) and 4, 5', 8-trimethylpsoralen (TMP, 2, 5, 9-trimethyl-7H-furo[3, 2-g]-1-benzopyran-7-one) were used as reference compounds in all tests. The investigations support the formation of a molecular complex between the furocoumarins and DNA.

Structural factors increase blood pressure through the interaction of resistance vessel geometry with neurohumoral and local factors: estimates in rabbits with renal cellophane-wrap hypertension with intact effectors and during neurohumoral blockade.

Background: The structural changes in hypertension include narrowing of the lumen of the large resistance vessels and an increase in their wall thickness : lumen ratio. Their haemodynamic role has been controversial.

Objective: To examine resting haemodynamics and the responses to graded drug-induced changes in tone in renal cellophane-wrap (wrap) and sham-operated (sham) rabbits, when their neurohumoral effectors were intact and during high-level blockade.