Prednisolone levels in the plasma and urine: a study of two preparations in man.

English, J.; Chakraborty, J.; Trigger, D. J.; Aw, Thomson

doi:10.1111/j.1365-2125.1975.tb02779.x

Cited by 27 publications

(10 citation statements)

References 11 publications

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“…This transformation is believed to be rapid due to the fact that equal doses of prednisone and prednisolone produced similar prednisolone concentration time profiles (Powell & Axelsen 1972). Approximately 7 to 15% of the orally administered dose is excreted unchanged in the urine (English et al 1975). Approximately 7 to 15% of the orally administered dose is excreted unchanged in the urine (English et al 1975).…”

Section: Metabolismmentioning

confidence: 99%

Clinical Pharmacokinetics in Organ Transplant Patients

Venkataramanan

Habucky

Burckart

et al. 1989

Clinical Pharmacokinetics

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Diseases of the liver, kidney and heart influence the pharmacokinetics of several drugs. Organ transplantation is an accepted therapeutic option for the treatment of several disease states associated with these organs. Recently, there has been an increase in both graft and patient survival after transplantation of the liver, heart, kidney and bone marrow. Such patients normally receive a wide range of drugs, and optimisation of drug therapy requires a thorough understanding of the pharmacokinetics and pharmacodynamics of these drugs in transplant patients. However, only limited studies have been carried out to characterise drug kinetics in these situations. Available information indicates that drug kinetics cannot be considered normal in transplant patients. Drug absorption generally appears to be similar to that in healthy subjects. The plasma protein binding of drugs that primarily bind to albumin increases after transplantation, but remains lower than that observed in healthy subjects. While the binding of certain basic drugs may increase after transplantation due to an increase in the concentration of alpha 1-acid glycoprotein, a lower albumin concentration may mask this effect. Oxidative and conjugative metabolism as measured by the kinetics of antipyrine (phenazone) and paracetamol (acetaminophen) is normal, while the metabolism of steroids may be impaired. Serum creatinine does not appear to be a good indicator of the functional status of the kidney in transplant patients. It is also important to realise that there will be time-dependent changes in several kinetic parameters of drugs due to improvement in the physiological function from that associated with the disease state to that of the normal state. Individualisation and close monitoring of drug therapy is necessary in transplant patients.

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Section: Metabolismmentioning

confidence: 99%

Clinical Pharmacokinetics in Organ Transplant Patients

Venkataramanan

Habucky

Burckart

et al. 1989

Clinical Pharmacokinetics

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“…Some suggest that delayed release preparations produce less suppression than standard formulations (English et al, 1975), others assert that long acting steroids are more suppressant (Carter & James, 1972) whilst other workers find that standard preparations of prednisolone produce no significant suppression (Turner et al, 1973). Cortisol was also present as a green fluorescent band on the chromatography plate and a technique for estimating cortisol by this means has been devised (Morrison, unpublished observations).…”

Section: Plasma Level Profilesmentioning

confidence: 99%

“…Two main types of assay have been employed for the estimation of prednisolone in plasma: radioimmunoassays (Colburn & Buller, 1973;Sullivan, Stoll, Sakmar, Blair & Wagner, 1974;Chakraborty, English, Marks, Dumasia & Chapman, 1976) and competitive protein binding methods (Turner, Carroll, Pinkus, Charles & Chattoraj, 1973;Leclercq & Copinschi, 1974;English, Chakraborty, Marks, Trigger & Thompson, 1975). Although both 39 techniques are relatively specific for prednisolone and are capable of the precision required for the determination of therapeutic prednisolone plasma levels they are tedious and time consuming in practice.…”

Section: Introductionmentioning

confidence: 99%

Plasma prednisolone levels from enteric and non‐enteric coated tablets estimated by an original technique.

Morrison¹,

Bradbrook²,

Rogers³

1977

Brit J Clinical Pharma

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1 A quantitative thin layer chromatographic technique for the estimation of plasma prednisolone levels has been devised with a minimum level of estimation of 10 ng/ml. 2 A comparative study of the absorption of 5 and 10 mg prednisolone from enteric and non‐enteric coated tablets (5 mg) was carried out in healthy subjects. 3 Mean plasma half‐life and peak plasma concentrations obtained from the non‐ enteric coated preparation agree well with previous studies in normal subjects reported by other investigators using competitive protein binding or radioimmunoassay techniques. Intersubject variability in bioavailability was noted. 4 Enteric coating increased the lag time before prednisolone appeared in the blood but did not alter the bioavailability of prednisolone compared to the equivalent dose of the non‐enteric coated tablet.

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“…Prednisolone is absorbed rapidly after oral intake, reaching peak plasma levels within the first hour after ingestion (2). The mean plasma half-life is 2–4 h (3, 4); metabolism occurs predominantly in the liver (5) but also via the actions of renal 11β-hydroxysteroid dehydrogenase type 2 converting it into the inactive metabolite prednisone (6).…”

Section: Introductionmentioning

confidence: 99%

Prednisolone is associated with a worse lipid profile than hydrocortisone in patients with adrenal insufficiency

Quinkler¹,

Ekman

Marelli³

et al. 2017

Endocrine Connections

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Objective Prednisolone is used as glucocorticoid replacement therapy for adrenal insufficiency (AI). Recent data indicate that its use in AI is associated with low bone mineral density. Data on risk factors for cardiovascular disease in patients with AI treated with prednisolone are scarce, despite this condition being the predominant cause of excess mortality. We aimed to address this question using real-world data from the European Adrenal Insufficiency Registry (EU-AIR). Design/methods EU-AIR, comprising of 19 centres across Germany, the Netherlands, Sweden and the UK, commenced enrolling patients with AI in August 2012. Patients receiving prednisolone (3–6 mg/day, n = 50) or hydrocortisone (15–30 mg/day, n = 909) were identified and grouped at a ratio of 1:3 (prednisolone:hydrocortisone) by matching for gender, age, duration and type of disease. Data from baseline and follow-up visits were analysed. Data from patients with congenital adrenal hyperplasia were excluded. Results Significantly higher mean ± s.d. total (6.3 ± 1.6 vs 5.4 ± 1.1 mmol/L; P = 0.003) and low-density lipoprotein (LDL) cholesterol levels (3.9 ± 1.4 vs 3.2 ± 1.0 mmol/L; P = 0.013) were identified in 47 patients on prednisolone vs 141 receiving hydrocortisone at baseline and at follow-up (P = 0.005 and P = 0.006, respectively). HbA1c, high-density lipoprotein and triglyceride levels, body mass index, systolic and diastolic blood pressure and waist circumference were not significantly different. Conclusions This is the first matched analysis of its kind. Significantly higher LDL levels in patients receiving prednisolone relative to hydrocortisone could predict a higher relative risk of cardiovascular disease in the former group.

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Prednisolone levels in the plasma and urine: a study of two preparations in man.

Cited by 27 publications

References 11 publications

Clinical Pharmacokinetics in Organ Transplant Patients

Clinical Pharmacokinetics in Organ Transplant Patients

Plasma prednisolone levels from enteric and non‐enteric coated tablets estimated by an original technique.

Prednisolone is associated with a worse lipid profile than hydrocortisone in patients with adrenal insufficiency

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