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PubMed1995

Simultaneous determination of N, N-di(n-butyl)doxorubicin-14-valerate and its 8 urinary metabolites by HPLC.

AIM: To develop an HPLC assay for simultaneous determination of AD202 and its metabolites and to examine metabolites of AD202 in urine of rats. METHODS: Reverse-phase HPLC with fluorescence detection and gradient elutionusing a Waters Chromatograph equipped with a 710 B WIFP autosampler, a power Mate SX plus computer, C18 Nova-pak (4 microns) 5 mm x 10 cm radial compression column connected with a guard micro-column, and a Waters 991 photodiode array detector for online observation of UV spectrum of related fraction. RESULTS: Detection limit was 1-3 ng for AD202 and 1-3 ng for its metabolites per injection. After i.v. AD202 20 mg.kg-1, only 4.9% dose as total anthracycline fluorescence signal was recovered in urine over 72 h. The predominant urinary metabolites were AD285 (desacyl AD202) and AD284 (N-mono-debutyl AD285). Six minor metabolites including aglycones and 13-keto reductive product were identified and 3 as-yet unknown metabolites were seen. Enzymatic and acid-hydrolysis failed to reveal the presence of glucuronides in urine. CONCLUSION: The sample analysis techniques developed in this study proved to be very efficient, sensitive, and specific, a total of 11 compounds achieved resolution with detection limit of 2 ng and no interference from matrix. Urine samples can be injected directly into chromatograph without any extraction, making sample analysis simple and time-saving.

Animals↗
PubMed1976

[Topical use of the new corticoid difluocortolone valerate in dermatology].

The object of the present study was to investigate the clinical efficacy of Nerisona Fatty Ointment in very dry skin conditions. A total of 37 patients, most of them with chronic dermatoses, was treated. Either very good or good results were achieved in 83.8% of the cases. The side effects observed were very slight.

Adolescent↗
PubMed1994

2,3,4,5-tetrahydroxy-5-(4-hydroxyphenyl)valeric acid: a new cleavable monofunctional reagent for monoclonal antibody labeling.

The synthesis and preliminary biological assays of a new monofunctional reagent to reversible derivatize monoclonal antibodies is described. This compound, comprising a 1,4-polyiol moiety, is cleavable by means of sodium periodate in mild conditions; moreover it also contains a phenolic residue suitable for 125I labelling and a carboxylic group for reaction with epsilon-lysyl amino group of antibodies. These features are suitable to study the monoclonal antibodies cell-internalization process and antigen expression on cell surface. The 125I labelled reagent has been coupled to the monoclonal antibody AR-3, an IgG1 directed toward the CAR-3 antigen widely expressed on human ovarian and colorectal adenocarcinomas. The cleavage capability is tested in different conditions both on reagent and on derivatized MAb. Cell labelling experiments are performed both on target and untarget cell lines.

Antibodies, Monoclonal↗
PubMed1998

Does anti-atherogenic estradiol valerate treatment cause adverse effects on liver and uterus in NZW rabbits?

The rabbit has been a widely accepted animal model for atherosclerosis research since Anitschkow first used this animal in 1913 in identifying dietary-induced hypercholesterolemia as a major risk factor for atherogenesis. Experiments with cholesterol-fed rabbits have demonstrated the beneficial effects of estrogen treatment on the development of atheroma for more than 50 y. Clinical trials have found a reduction in cardiovascular events of up to 50% in postmenopausal women receiving estrogen replacement therapy. However, metabolic conditions in rabbits, as well as physiological estrogen serum levels, differ in some aspects from those in humans. In rabbits, experimentally-induced hormone levels are about 5- to 10-fold higher than those found in untreated animals. Normal physiological estrogen levels in rabbits are not cardioprotective under dietary-induced hypercholesterolemia. We investigated whether replacement induced "hyperestrogenemia" causes adverse effects on organs other than the cardiovascular system. Twenty-nine female rabbits were divided into 4 different groups, 2 without and 2 with estrogen treatment (1 mg estradiol valerate/kg body weight/w over 12 w). Organ weights, transaminases and uterine histology were examined. In rabbits treated with estrogen, we did not see relevant adverse effects on heart, kidney and liver weights, or on liver enzymes. But there was a significant increase in spleen weights, as well as notable changes in the endometrium with moderate inflammation. These findings indicate that the dosage of estrogen commonly used for atherosclerosis research does not cause serious disorders in the major organs of cholesterol-fed rabbits.

Animals↗
PubMed2002

Estradiol valerate/dienogest.

Estradiol valerate 2mg/dienogest 2mg is an oral estrogen/ progestogen formulation that has been approved throughout the European Union for the treatment of climacteric symptoms in postmenopausal women. Dienogest is a progestogen that combines the properties of both progesterone and 19-nortestosterone derivatives. It has moderate affinity for the progesterone receptor, significant antiproliferative and antiandrogenic activity, and produces secretory transformation of the endometrium. Estradiol valerate is an esterified form of natural 17beta-estradiol, the most potent endogenous human ovarian estrogen, and is hydrolysed to estradiol soon after oral administration. Results from a randomised, double-blind, multicentre trial showed that oral estradiol valerate 2mg/dienogest 2mg and estradiol valerate 2mg/dienogest 3mg once daily for 1 year were each as effective as estradiol 2mg/estriol 1mg/norethisterone acetate 1mg in the treatment of climacteric symptoms in 581 postmenopausal women; reductions from baseline in Kupperman Index scores were 78.5, 74.5 and 75.0%, respectively. The number of days without any type of bleeding was lowest in patients treated with estradiol valerate 2mg/dienogest 2mg (8.7 days), and highest in the estradiol valerate 2mg/ dienogest 3mg group (12.1 days). During the twelfth month of treatment with estradiol valerate 2mg/dienogest 2mg, the percentage of patients who reported bleeding was 14.5%. Endometrial biopsy results were similar in patients treated with estradiol valerate 2mg/dienogest 2mg, estradiol valerate 2mg/dienogest 3mg or estradiol 2mg/estriol 1mg/norethisterone acetate 1mg once daily for 1 year; 90.8, 87.4 and 87.5% of samples, respectively, contained atrophic material. Proliferative material was found in 4.2, 2.5 and 4.4% of the biopsies, respectively; there was no incidence of hyperplasia in any of the treatment groups. A noncomparative multicentre study in 1501 postmenopausal women demonstrated that adverse events associated with estradiol valerate 2mg/dienogest 2mg once daily for 48 weeks included breakthrough bleeding, mastalgia, headache, abdominal pain, hypertension, thrush, migraine, weight gain, increase in endometrial thickness and metrorrhagia.

Administration, Oral↗
PubMed2006

Comparison of techniques to determine the clearance of ruminal volatile fatty acids.

The objective of this experiment was to compare measurements of fractional clearance rates obtained by using an unlabeled valerate-CoEDTA technique with measurements obtained by using a (13)C-labeled volatile fatty acids (VFA) technique. The exponential decay rate of the (13)C/(12)C ratio after pulse-dosing (13)C-acetate, (13)C-propionate, or (13)C-butyrate into the rumen was compared with the decay rate of rumen valerate concentration following a simultaneous pulse dose. The unlabeled valerate, CoEDTA, and each labeled VFA, one at a time, were concurrently mixed with the evacuated ruminal content of 6 lactating cows in two 3 x 3 Latin squares. The clearance of VFA by passage to the omasum was assumed to be equivalent to the decay in ruminal Co concentration and was around 50% of the total clearance. Acetate, propionate, and butyrate had similar fractional clearance rates (31.2, 33.4, 30.4%/h, respectively), but propionate had a higher absorption rate (19.2%/h) than butyrate (14.2%/h). Linear regression determination coefficients using the valerate clearance rate as an estimator for acetate, propionate, and butyrate rumen clearance were 0.51, 0.56, and 0.99, respectively. In a second experiment, the (13)C-valerate fractional clearance rate estimate (33.7%/h) was similar to the estimate obtained with unlabeled valerate (35.0%/h) by the valerate-Co technique. No (13)C enrichment of rumen microbes was noted 4 h after the intraruminal infusion of (13)C-valerate. Fractional VFA absorption rate estimates obtained in both techniques were similar, although both were lower than estimates reported in the literature by other methods.

Absorption↗
PubMed1983

Long-term post-menopausal hormone therapy and serum HDL-C, total cholesterol and triglycerides.

Serum high-density lipoprotein cholesterol (HDL cholesterol), total cholesterol and triglyceride concentrations were determined in 158 post-menopausal women following long-term oral hormone replacement therapy. Oestradiol valerate (2 mg/day) was taken by 53 of the women and oestriol succinate (2 mg/day) by 42 others. The duration (means +/- SD) of the oestradiol valerate therapy was 6.4 (+/- 2.9) yr and of the oestriol succinate therapy 6.4 (+/- 2.3) yr. The remaining 63 women received oestradiol valerate (2 mg/day) combined sequentially with norgestrel (0.5 mg/day). The average duration of treatment with this combination was 3.3 (+/- 2.4) yr. The control group comprised 100 post-menopausal women who received no hormone therapy whatsoever. The HDL cholesterol levels in the women receiving oestradiol valerate were higher than those in the controls (P = 0.001) and in the women on oestradiol valerate plus norgestrel therapy (P less than 0.001). The HDL cholesterol levels in the oestriol succinate group did not differ significantly from those in the controls. The women receiving oestradiol valerate in combination with norgestrel had lower serum HDL cholesterol concentrations than the controls (P less than 0.05). Serum total cholesterol and triglyceride concentrations did not differ in either oestrogen group from those in the controls, but were lower in the oestradiol valerate-plus-norgestrel group than in the controls (P less than 0.001). There were no differences in serum total oestrogen, oestrone, oestradiol and oestriol levels between control subjects with normal HDL cholesterol concentrations and those with low concentrations.

Cardiovascular Diseases↗
PubMed1995

Combined oestrogen-progestin replacement therapy prevents atherosclerosis in postmenopausal women.

The incidence of atherosclerotic plaques in the aorta and in the carotid and iliac arteries was investigated using high resolution B-mode ultrasonography in 40 postmenopausal women using sequentially combined oestradiol valerate 2 mg--levonorgestrel 0.25 mg replacement therapy. In addition, serum lipid, lipoprotein and apolipoprotein levels were measured. Similar studies were performed for 40 postmenopausal women using oestradiol valerate alone and for 40 women who had never used hormone replacement therapy (HRT). Ultrasonographically observed atherosclerotic plaques were less common (P = 0.011) in oestradiol valerate--levonorgestrel users than in women without HRT. More than three atherosclerotic plaques were observed in 62% of the women without HRT but only in 30% of the women using combined therapy (P = 0.003). The total number of plaques did not differ between the two hormone using groups. The mean serum triglyceride, total cholesterol and apolipoprotein B levels were lowest in oestradiol valerate--levonorgestrel users when compared with those of women with oestradiol valerate monotherapy and those of women without HRT. Combined oestradiol valerate--levonorgestrel replacement therapy, like oestradiol valerate monotherapy, prevents the progression of atherosclerosis in postmenopausal women. The lipid patterns were not adversely affected by the addition of the androgenic levonorgestrel.

Apolipoproteins↗
PubMed2002

Hormone replacement therapy and vigilance: double-blind, placebo-controlled EEG-mapping studies with an estrogen-progestogen combination (Climodien, Lafamme) versus estrogen alone in menopausal syndrome patients.

UNLABELLED: The aim of the double-blind, placebo-controlled study was to investigate the effects of a continuous combined estrogen-progestogen treatment (Climodien, Lafamme) as compared with estrogen alone on vigilance in insomniac postmenopausal syndrome patients, objectified by EEG mapping. METHODS: In a 3-arm, 2-month parallel group design phase, patients received a combination of estradiol valerate 2 mg and the novel progestogen dienogest 3 mg (Climodien 2/3) or estradiol valerate 2 mg alone or placebo. In a subsequent open-label phase, all patients received estradiol valerate 2 mg+dienogest 2 mg (Climodien 2/2). EEG mapping was carried out before and after the 2-month double-blind phase as well as after the 2-month open-label treatment. RESULTS: As compared with placebo, Climodien 2/3 induced a marked and highly significant increase in absolute power in all frequency bands, specifically in alpha-2 activity. Moreover, a significant increase in relative alpha-2 power, a decrease in relative delta and beta power as well as an acceleration of the dominant frequency and of the delta and alpha centroids suggested a marked improvement in vigilance. In contrast, under estradiol valerate 2 mg alone, only a slight augmentation of alpha and attenuation of relative delta and beta power occurred, suggesting only a slight vigilance improvement as compared with placebo. Thus, dienogest 2 mg increased the estrogen effect, which was also confirmed by a statistical evaluation of the differences between Climodien 2/3 and estradiol valerate alone (augmentation of alpha-2, attenuation of relative beta, acceleration of the dominant frequency). Moreover, Climodien 2/2 also markedly increased alpha-2 power, decreased relative beta-2 power and accelerated the alpha centroid. Finally, comparing Climodien 2/3 with Climodien 2/2, there was even a dose-efficacy relation. CONCLUSIONS: Estradiol valerate 2 mg improves vigilance slightly, thereby confirming previous findings. The additional administration of dienogest does not minimize the effect of estrogen, but on the contrary increases it, which makes the combination superior to both placebo and estradiol valerate alone. Vigilance improvement may be of great therapeutic benefit to menopausal syndrome patients at a time when increased adaptability is needed to adjust to increasing sexual, marital, occupational and social difficulties known to occur specifically in this period of life.

Aged↗
PubMed1998

Calcipotriol cream with or without concurrent topical corticosteroid in psoriasis: tolerability and efficacy.

The objectives of the study were to determine whether concurrent treatment with calcipotriol (50 microg/g) and either clobetasone 17-butyrate cream (0.5 mg/g) (moderate potency) or betamethasone 17-valerate cream (1 mg/g) (potent) or placebo (vehicle of calcipotriol) was more effective and/or caused less skin irritation than calcipotriol cream (50 microg/g) used twice daily. It was a multicentre, double-blind, parallel group study. Patients applied calcipotriol cream in the morning and either vehicle (n = 174), calcipotriol (n = 174), clobetasone (n = 175) or betamethasone creams (n = 176) in the evening for up to 8 weeks. Adverse events led to withdrawal in 20 patients (2.9%). The mean percentage change in PASI (psoriasis area and severity index) was -40.6 in the calcipotriol/vehicle group, -48.3 in the calcipotriol/calcipotriol group, -53.7 in the calcipotriol/clobetasone 17-butyrate group and -57.5 in the calcipotriol/betamethasone 17-valerate group. A statistically significant difference was seen between the four treatment groups (P = 0.006) with calcipotriol/vehicle being less effective than the other treatments. A statistically significant difference in favour of calcipotriol/betamethasone 17-valerate was seen between the calcipotriol/calcipotriol group and the calcipotriol/betamethasone 17-valerate group. The majority of adverse events were skin irritations, which were reported for 31.2% of patients treated with calcipotriol/vehicle, 34.3% of patients treated with calcipotriol twice daily and 23.8% vs. 17.1% of patients treated with calcipotriol/clobetasone 17-butyrate and calcipotriol/betamethasone 17-valerate, respectively. Skin irritation was seen statistically significantly less frequently in patients treated with calcipotriol/ clobetasone 17-butyrate or calcipotriol/betamethasone 17-valerate (P = 0.001), whereas no difference was seen between the other groups. In conclusion, calcipotriol applied twice daily was as effective as calcipotriol/clobetasone 17-butyrate, but slightly less effective than calcipotriol/betamethasone 17-valerate. The incidence of skin irritation was less for patients using concurrent corticosteroids, whereas treatment with calcipotriol/vehicle did not reduce the incidence of skin irritation when compared with calcipotriol twice daily.

Adult↗
PubMed2001

Paraoxon sensitive phenylvalerate hydrolase in assessing the severity of acute paraoxon poisoning.

INTRODUCTION: Intoxications with organophosphorous compounds, especially paraoxon, are frequent. Organophosphorous compounds inhibit serine hydrolases such as acetylcholine, butyrilcholine, and carboxyl esterases although acetylcholine and butyrylcholine are too sensitive to paraoxon to be useful markers of severity. They cannot show a dose-dependent inhibition during an acute organophosphorous compounds exposure because maximal enzyme inhibition is reached at very low organophosphorous compounds concentrations. PURPOSE: To determine in vitro the dose-effect relationship between the activity of the paraoxon-sensitive phenylvalerate hydrolase, a member of the carboxvl esterases family, and the paraoxon dose, and to assess its utility as a putatively less sensitive enzyme marker to monitor the severity of an acute paraoxon intoxication. MATERIALS AND METHODS: Phenylvalerate hydrolase and butyrylcholine activities were determined in serum of nine healthy human volunteers before and after addition of different concentrations of paraoxon. The determination of phenyl-valerate hydrolase activity was carried out using a modification of the method described by Johnson. A commercially available kit was used to measure butyrylcholine activity. RESULTS: Paraoxon inhibits phenyl-valerate hydrolase activity at concentrations above 10 M. Maximal inhibition (approximately 50% of baseline) is achieved at concentrations above 2.5 x 10(-7) M. The IC50 value of paraoxon for phenyl-valerate hydrolase is 34+/-2 nM. The uninhibited phenyl-valerate hydrolase activity is due to paraoxon-resistent isoforms. Paraoxon begins inhibiting butyrylcholine activity at concentrations above 10(-9) M. At concentrations above 5 x 10(-5) M, no butyrylcholine activity is measulrable. The IC50 value of paraoxon for butyrylcholine is 150+/-23 nM. CONCLUSION: The paraoxon-sensitive subunit of phenyl-valerate hydrolase shows dose-dependent inhibition when exposed to paraoxon in vitro, but it is even more sensitive than butyrylcholine to paraoxon inhibition. Determinations of phenyl-valerate hydrolase activity to assess the severity of an acute organophosphorous compounds poisoning cannot be recommended, but phenyl-valerate hydrolase may have utility in worker surveillance.

Biomarkers↗
PubMedDate not supplied

Drospirenone increases central and peripheral beta-endorphin in ovariectomized female rats.

OBJECTIVE: Drospirenone is the unique progestin derived from 17-spironolactone used for contraception and hormone therapy. Few data are available concerning the effects of drospirenone on the central nervous system and neuroendocrine milieu. The opioid beta-endorphin and the neurosteroid allopregnanolone are considered markers of neuroendocrine functions, and their synthesis and activity are regulated by gonadal steroids. The aim of the present study was to evaluate the effect of a 2-week oral treatment with drospirenone, estradiol valerate, and combined therapy of drospirenone + estradiol valerate on central and peripheral beta-endorphin and allopregnanolone levels in ovariectomized female rats. DESIGN: Seven groups of Wistar ovariectomized rats received oral drospirenone (0.1, 0.5, and 1.0 mg/kg per day), estradiol valerate (0.05 mg/kg per day), or drospirenone (0.1, 0.5, and 1.0 mg/kg per day) + estradiol valerate (0.05 mg/kg per day). One group of fertile and one group of ovariectomized rats were used as controls. beta-endorphin levels were measured in frontal and parietal lobes, hippocampus, hypothalamus, anterior and neurointermediate pituitary, and plasma, and allopregnanolone content was assessed in frontal and parietal lobes, hippocampus, hypothalamus, anterior pituitary, adrenal glands, and serum. RESULTS: Ovariectomy induced a significant decrease in beta-endorphin and allopregnanolone content in all brain areas analyzed and in circulating levels, whereas it increased allopregnanolone content in the adrenal gland. Estradiol valerate replacement increased beta-endorphin and allopregnanolone levels in all brain areas analyzed and in plasma/serum. Drospirenone treatment significantly increased beta-endorphin levels in all brain areas analyzed (with the only exception being the parietal lobe), whereas it produced no effect on allopregnanolone levels. The addition of drospirenone to estradiol valerate did not modify the effects of estradiol valerate on beta-endorphin or allopregnanolone levels. Drospirenone showed an additive and synergistic effect with estradiol in the neurointermediate lobe on beta-endorphin synthesis. CONCLUSIONS: Drospirenone significantly increases central and circulating beta-endorphin levels and does not seem to interfere with allopregnanolone production.

Administration, Oral↗
PubMed2000

Development of an attractant for the scarab pest Macrodactylus subspinosus (Coleoptera: Scarabaeidae).

Field trials were conducted over several seasons to determine the attractant most successful in luring adult rose chafers, Macrodactylus subspinosus (F.), to traps. During the first season, 20 compounds were compared with the standard lure, valeric acid + hexanoic acid + octyl butyrate (1:1:1). The two new standards establishedthat season were: valeric acid + 1-nonanol (1:1); and valeric acid + hexanoic acid + octyl butyrate + 1-nonanol (1:1:1:1). The following season, 36 compounds were evaluated, comparing them to the new standards. The performance of the standard binary lure valeric acid + 1-nonanol was improved when the alcohol 1-nonanol was replaced by its analog trans-2-nonenol and this was confirmed during the third season. At the same time, a second test was conducted with 29 new candidates, which were combined with valeric acid and compared with the standard: valeric acid + hexanoic acid + octyl butyrate + 1-nonanol (1:1:1:1). A control and the single compound alpha-ionone were included, resulting in the discovery of a new more powerful attractant, alpha-ionone. Testing of alpha-ionone continued the following season, at which time the initial leading candidate and new ones containing trans-2-nonenol were tested against the single attractant alpha-ionone and various combinations of it. A new five-component mixture of valeric acid, hexanoic acid, octyl butyrate, trans-2-nonenol, and alpha-ionone out performed all other lure combinations.

Animals↗
PubMed2002

[Effects of sex hormones on serum levels of nitric oxide and plasma angiotensin II in postmenopausal women].

OBJECTIVE: To observe the effect of estrogen and progestin on the blood levels of nitric oxide and angiotensin II in aid of the application of hormone replacement therapy in postmenopausal women. METHODS: The serum nitric oxide and plasma angiotensin II levels in postmenopausal women were determined before and 3 months after oral intake of estradiol valerate 1 mg/day (n = 10) or estradiol valerate, 1 mg/d plus medroxyprogesterone acetate, 2 mg/d (n = 30). RESULTS: The serum nitric oxide levels of postmenopausal women were significantly increased by 3 months of oral estradiol valerate 1 mg/d (P < 0.05), whereas the plasma levels of angiotensin II tended to decrease. The positive correlation between the increases of nitric oxide and the changes of estradial 3 months after oral intake of estradiol valerate 1 mg/d was significant. Compared with the baseline, no significant changes were observed in both serum nitric oxide levels and plasma angiotensin II levels 3 months after oral intake of estradiol valerate, 1 mg/d plus medroxyprogesterone acetate, 2 mg/d (P < 0.05). CONCLUSIONS: The vascular functions can be improved through increasing the serum nitric oxide level after 3-month oral intake of estradiol valerate, 1 mg/d in postmenopausal women, and estradiol valerate plus medroxyprogesterone acetate intake may attenuate the beneficial effects.

Adult↗
PubMed1997

Oxidation of short and medium chain C2-C8 fatty acids in Sprague-Dawley rat colonocytes.

BACKGROUND: The predominant colonic short chain fatty acids, acetate, propionate, and butyrate, are oxidised into CO2 in colonocytes from rat and humans in the preferred order of butyrate (C4) > propionate (C3) > acetate (C2)- hence butyrate is considered to be the principal oxidative substrate for colonocytes. AIMS: To compare colonocyte oxidation of valerate (C5), hexanoate (C6), and octanoate (C8) with that of butyrate. METHODS: Isolated rat colonocytes were incubated in the presence of a concentration range of 1-14C labelled C2-C8 fatty acids. Oxidation rates were obtained by quantifying the production of 14CO2, and Vmax (maximum velocity) and K(m) (Michaelis-Menten constant) were calculated by computer fitting of the data to a Michaelis-Menten plot. RESULTS: The K(m) value of acetate (0.56 (SEM 0.02) mmol/l) was about fourfold higher than the K(m) of butyrate (0.13 (0.01) mmol/l), whereas the K(m) values of valerate (0.19 (0.01) mmol/l), hexanoate (0.19 (0.01) mmol/l), and octanoate (0.16 (0.01) mmol/l) were of the same order of magnitude as the K(m) of butyrate. Acetate did not influence butyrate oxidation, whereas butyrate strongly inhibited the oxidation of acetate. By contrast, valerate, hexanoate, and octanoate inhibited colonocyte oxidation of butyrate equally or more than the reverse inhibitory effect of butyrate on valerate, hexanoate, and octanoate oxidation. The maximum rates of ATP production were in the order of valerate > octanoate = hexanoate > butyrate > acetate (28.47 (0.70), 21.78 (0.75), 21.33 (0.78), 16.12 (0.49), 9.09 (0.34) (mumol/min/g) respectively). CONCLUSIONS: Valerate, hexanoate, and octanoate seem to be excellent substrates for colonocyte oxidation, similar to butyrate. These results may influence the choice of fatty acid composition in enemas used for treatment of patients in whom deficient colonocyte oxidation is suspected-for example, patients with ulcerative colitis and diversion colitis.

Acetates↗
PubMed1980

A comparison of the pharmacokinetic properties of three estradiol esters.

In order to assess the pharmacokinetics properties of estradiol cypionate, valerate and benzoate, the daily plasma levels of estradiol and estrone were analysed in groups of 10, 9 and 10 subjects, respectively, before and during 3 weeks after the intramuscular administration of a single dose of 5.0 mg in 1.0 ml arachis oil. In order to minimize the contribution of endogenous estrogens to the plasma levels, all subjects were receiving a combined oral contraceptive consisting of levonorgestrel (150 micrograms) and ethinyl estradiol (30 micrograms) for three months prior to the study and during the study period. The administration of estradiol cypionate gave significantly lower peak levels of estradiol and estrone than that of the valerate and benzoate. Peak plasma levels of estradiol and estrone were reached in approximately 4 days following the administration of estradiol cypionate and in a significantly shorter time (approximately 2 days) following the administration of both the valerate and benzoate. One hour after the injection of the esters, the average percentage increases in plasma estradiol and estrone levels were significantly higher in the valerate and benzoate groups compared to the subjects receiving estradiol cypionate. The average duration of elevated estrogen levels was shortest in the benzoate group (4-5 days) followed by the valerate (7-8 days) and cypionate (approximately 11 days). In none of the subjects studied were elevated estradiol and/or estrone levels encountered 2 weeks after the injection of the various esters. The data suggests that among the three esters studied, the valerate provides the most predictable pharmacokinetic behaviour.

Adult↗