To Compare the Efficacy of Tamsulosin and Deflazacort Combination with Tamsulosin Alone in Expulsion of Lower Ureteric Stones in a Medical College in South Haryana

Introduction: Men have been suffering from urinary stones since antiquity. Symptomatic ureteric stone is a very common emergency condition faced by general surgeons and urologists. There are many medical and interventional treatments for lower ureteric stones. Removal of stone with ureteroscopy is very effective but this is very costly also. Anesthetist is required; stent is placed in ureter which has to be removed afterward. Stones of size <4 mm will pass hopefully spontaneously. Stones more than 10 mm size will require surgery in general. The expulsion of stones of size 4–10 mm can be tried with the help of pharmacological agents. Materials and Methods: This prospective observational study was conducted in the Surgery Department at SGT Medical College located in South Haryana. A total of 150 patients of distal ureteric stones of sizes 4–10 mm were taken in this study, divided into two groups of 75 patients each. Group I patients were given tamsulosin 0.4 mg and deflazacort 30 mg once in a day and Group II patients were given tamsulosin 0.4 mg once in a day. Treatment was for 10 days. Results: In Group I, the stones were expelled in 24 (32%) patients. While in Group II, 11 (14.6%) patients passed stones. This is statistically significant with P = 0.023. The median time for stone expulsion was 192 h in Group I and 312 h in Group II with again a significant P = 0.039. Conclusion: We conclude that Group I (tamsulosin + deflazacort) showed a statistically significant advantage in stone expulsion rate than Group II (tamsulosin alone). Group I also showed a statistically significant advantage in stone expulsion time.

​Evaluation Of The Efficacy Of Tamsulosin And Deflazacort Versus Tamsulosin Alone In Expulsion Of Lower Ureteric Stones In A Tertiary Center

Introduction: Urolithiasis is a very common problem present. About 70% of all ureteric stones are found in the lower third ofureter. Many factors affect the modality of treatment such as setup available, type, size of stone and expertise of the surgeon.Extracorporeal shock wave lithotripsy and ureteroscopy and removal of stone are very effective, but they require the help ofanesthetist. Ureter is to be stented, and the stent has to be removed later on. They are very costly and not without complications.Many pharmacological agents have been used for the expulsion of ureteric stones, for example, diclofenac, alkalizers, ketorolac,nifedipine, deflazacort, prazosin, silodosin, and tamsulosin.Materials and Methods: This prospective observational study was conducted in the Surgery Department at SGT MedicalCollege. A total of 100 patients of distal ureteric stones of sizes 4–10 mm were taken in this study, divided into two groups of50 patients each. Group I patients were given tamsulosin 0.4 mg and deflazacort 30 mg once in a day, Group II patients weregiven tamsulosin 0.4 mg once in a day. Treatment was for 10 days.Results: In Group I, the stones were expelled in 38 (76%) patients, while in Group II, 26 (52%) patients passed stones. Thisis statistically significant with P = 0.038. The median time for stone expulsion was 3 days in Group I and 11 days in Group IIwith P = 0.032.Conclusion: We have evaluated that medical expulsive therapy using tamsulosin alone is also effective and can be used inpatients where steroids are contraindicated, but by adding deflazacort, it becomes very effective for management of distalureteral calculi.

Three Cases of Pulmonary Hemosiderosis with Long-term Treatment of Deflazacort in Children / 임상소아혈액종양

Idiopathic pulmonary hemosiderosis (IPH) is a rare respiratory disease with an unknown etiology, and is diagnosed with laboratory, radiology, and pathology tests. Chief complaints of IPH include hemoptysis, cough, and dyspnea. Since it is considered an immune-mediated disease, the first line of treatment is systemic corticosteroid therapy. The three cases reported here showed a decrease in ferritin level and improvement in the hemoglobin level with prednisolone treatment. However, long-term corticosteroid therapy may cause several side effects, particularly growth retardation and obesity, which can affect growing children. In the present study, all patients had cushingoid symptoms and obesity. Therefore, we switched to deflazacort (DFZ), which has lesser side-effects of weight gain. This report describes clinical courses of the disease and comparison of body mass index of three patients with IPH who took DFZ instead of prednisolone. DFZ was effective for IPH, and is useful for weight gain reduction.

Three Cases of Pulmonary Hemosiderosis with Long-term Treatment of Deflazacort in Children / 임상소아혈액종양

Idiopathic pulmonary hemosiderosis (IPH) is a rare respiratory disease with an unknown etiology, and is diagnosed with laboratory, radiology, and pathology tests. Chief complaints of IPH include hemoptysis, cough, and dyspnea. Since it is considered an immune-mediated disease, the first line of treatment is systemic corticosteroid therapy. The three cases reported here showed a decrease in ferritin level and improvement in the hemoglobin level with prednisolone treatment. However, long-term corticosteroid therapy may cause several side effects, particularly growth retardation and obesity, which can affect growing children. In the present study, all patients had cushingoid symptoms and obesity. Therefore, we switched to deflazacort (DFZ), which has lesser side-effects of weight gain. This report describes clinical courses of the disease and comparison of body mass index of three patients with IPH who took DFZ instead of prednisolone. DFZ was effective for IPH, and is useful for weight gain reduction.

Comparative Adverse Drug Profile of Deflazacort Vs Conventional Corticosteroids in Spontaneous Reporting System of Pharmacovigilance.

The current observational cross-sectional study was undertaken using suspected adverse drug data collection form available under (PvPI) to evaluate comparative ADR profile of DFZ Vs CCS for 3 years in spontaneous reporting system of ADRs in current PvPI. Total number of ADR reports during the study period was 3024, out of which ADRs reports due to CS were 112 accounting for a rate of 3.70%. The rate of total ADR events with CS was 4.11%. Geriatric, urban and female population predominated in contributing ADRs with both CCS and DFZ in the study. Self medication of CCS and DFZ contributed 10.95% and 7.69% of total ADRs. Oral route contributed maximal ADRs. Irrational drug prescription contributed substantially. Maximum ADRs due to CCS and DFZ were moderate, latent, non-serious, type A and were probable followed by possible in nature as per WHO UMC scale. Gastritis, new onset hypertension/ loss of hypertensive control, loss of diabetic control, obesity/overweight, dyslipedemia were common ADRs. Thus, ADRs due to CS is a substantial health problem. ADR profile did not vary although DFZ recorded less ADRs.

Three Cases of Erythema Multiforme Developed during Deflazacort Therapy in Children with Nephrotic Syndrome

Erythema multiforme (EM) is an acute mucocutaneous disorder involving the skin, mouth, eyes, and genital organs. It is classified into EM minor and EM major according to the involvement of the mucosal membrane. Stevens-Johnson syndrome (SJS) and toxic epidermal necrosis (TEN) belong to EM major. Compared to EM minor, SJS presents with more severe and progressive symptoms, and has a higher mortality rate. Corticosteroids are used in the treatment of EM. We report three cases of EM (two cases of EM minor and one case of SJS) that developed during treatment with oral corticosteroid (deflazacort; Calcort(R)) in children with nephrotic syndrome.

Toxic epidermal necrolysis associated with deflazacort therapy with nephrotic syndrome

Toxic epidermal necrolysis (TEN) is a drug-related fatal disease. Extensive necrosis of the epidermis can lead to serious complications. This report describes two cases of TEN, associated with deflazacort (DFZ), in two boys, aged 4 years and 14 years, with nephrotic syndrome (NS). The 14-year-old male teenager received DFZ following NS relapse. After 17 days, pruritic papules appeared on the lower extremities. Another case involved a 4-year-old boy receiving DFZ and enalapril. After a 41-day DFZ treatment period, erythematous papules appeared on the palms and soles. Within 3 days, both boys developed widespread skin lesions (>50%) and were admitted to the intensive care unit for resuscitative and supportive treatment. The patients showed improvement after intravenous immunoglobulin-G therapy. Owing to the rapid, fatal course of TEN, clinicians need to be aware of the adverse effects of this drug when treating cases of NS.

Development and validation of spectrofluorimetric method for estimation of deflazacort in tablets.

A simple and sensitive spectrofluorimetric method has been developed for the determination of deflazacort in pharmaceutical tablet dosage forms. The method was based on the liebermann-burchard reaction, in which the chloroform extract of deflazacort is reacted with acetic anhydride and sulfuric acid to produce strong fluorescence. The resulting fluorophor exhibit excitation and emission wavelengths at 300 and 435 nm, respectively. Linear relationship for the fluorescence intensity was obtained in the concentration range of 0.5 - 10 μg/ml. The method was validated in terms of linearity (0.5-10 μg/ml), repeatability (RSD, 0.99 %), precision (intra-day variation, RSD, 0.239 to 1.287 % and inter-day variation, RSD, 0.360 to 1.830 %) and accuracy (99.12 to 100.28 %). The limit of detection and limit of quantification for deflazacort were found to be 0.15 and 0.45 85.70 μg/ml, respectively. The developed method was successfully used for the assay of deflazacort tablet formulation. The spectrofluorimetric method was found to be simple, sensitive, accurate, precise and economic and can be used for the routine quality control testing of deflazacort in tablet dosage form.

High performance thin layer chromatographic method for estimation of deflazacort in tablet.

A simple and sensitive high performance thin layer chromatography (HPTLC) method has been developed for the quantitative estimation of deflazacort in its single component tablet formulation (30 mg). Deflazacort was chromatographed on silica gel 60 F254 TLC plate using benzene: methanol: glacial acetic acid (7.5:2.0:0.5, v/v/v) as mobile phase. Deflazacort showed Rf value of 0.60 + 0.02 and scanned at 243 nm using a camag TLC scanner 3. The method was validated in terms of linearity (100 – 800 ng/spot), precision (intra-day variation, 0.335 to 1.203% and inter-day variation, 0.231 to 1.471%), accuracy (98.87 to 99.77%) and specificity. The limit of detection and limit of quantification for deflazacort were found to be 25.97 ng/spot and 85.70 ng/spot, respectively. The developed method was successfully used for the assay of deflazacort tablet formulation. The method was found to be simple, sensitive, specific, accurate and precise and can be used for the routine quality control testing of deflazacort in tablet dosage form.

Spectrophotometric and HPLC determination of deflazacort in pharmaceutical dosage forms

Deflazacort (DFZ) is a glucocorticoid used as an anti-inflammatory and immunosuppressant drug. No official methods are available for DFZ determination in pharmaceutical formulations. The objective of this study was to develop, validate and compare spectrophotometric (UV and colorimetric) and high-performance liquid chromatography (HPLC) methods, for the quantitative determination of DFZ in tablets and oral suspension. For the UV method, ethanol was used as the solvent, with detection at 244 nm. The colorimetric method was based on the redox reaction with blue tetrazolium in alkaline medium, with detection at 524 nm. The method by HPLC was carried out using a C18 column, mobile phase consisting of acetonitrile:water (80:20, v/v) with a flow rate of 1.0 mL min-1 and detection at 244 nm. The methods proved linear (r > 0.999), precise (RSD < 5 percent) and accurate (recovery > 97 percent). Statistical analysis of the results indicated that the UV and HPLC methods were statistically equivalent, while the values obtained for the colorimetric method differed significantly from the other methods.

O deflazacorte (DFZ) é um fármaco glicocorticóide usado como antiinflamatório e imunossupressor. Métodos oficiais não estão disponíveis para a determinação de DFZ em formas farmacêuticas. Este estudo teve como objetivo desenvolver, validar e comparar métodos por espectrofotometria (UV e colorimetria) e cromatografia líquida de alta eficiência (CLAE), na determinação quantitativa de DFZ em comprimidos e suspensão oral. O método por UV utilizou etanol como solvente, com detecção em 244 nm. O método colorimétrico foi baseado na reação de redução com azul de tetrazólio em meio alcalino, com detecção em 524 nm. O método por CLAE utilizou coluna C18; fase móvel constituída de acetonitrila:água (80:20, v/v), com fluxo de 1,0 mL min-1 e detecção em 244 nm. Os métodos foram lineares (r > 0,999); precisos (RSD < 5 por cento), e exatos (recuperação > 97 por cento). As análises estatísticas dos resultados obtidos indicaram que os métodos por UV e por CLAE foram estatisticamente equivalentes, enquanto os valores obtidos para o método colorimétrico diferiram significativamente dos demais métodos.

Two Cases of Stevens-Johnson Syndrome Caused by Systemic Corticosteroids / 대한피부과학회지

Stevens-Johnson syndrome (SJS) is a fatal, acute, hypersensitivity reaction which is associated with certain drugs. The disease has often been managed by systemic corticosteroids. However, there have been a few reports of SJS caused by systemic corticosteroids in Western countries. We herein present two cases of SJS related to deflazacort and betamethasone sodium phosphate. It is worth mentioning that corticosteroids might be offending drugs for SJS. Due to the difficulty in predicting a cross-reaction between corticosteroids and also the existence of concomitant allergies to other corticosteroids, we should consider an alternative strategy such as intravenous immunoglobulin-G in patients with SJS caused by systemic corticosteroids.

Deflazacort for Type-1 Autoimmune Hepatitis in a Korean Girl

Prednisone or prednisolone are the mainstay drug treatments for autoimmune hepatitis in children. However, long-term use of corticosteroid is associated with the risk of steroid-induced toxicities, and this situation requires newer immuno-suppressive agents for the treatment of autoimmune hepatitis, especially in growing children. An 11-yr-old Korean girl with type-1 autoimmune hepatitis discontinued prednisolone due to toxicities, i.e., hirsutism, buffalo hump, and skin striae, and remained clinical and biochemical remission under replacement of deflazacort and ursodeoxycholic acid combination therapy. A follow-up liver biopsy after 19 months of deflazacort and ursodeoxycholic acid treatment showed histologic remission.

Efficacy of Deflazacort with Add-on Therapy in Childhood Intractable Atonic Seizure

PURPOSE: This is a clinical study to evaluate the efficacy and adverse reactions of deflazacort as adjunctive therapy in childhood intractable atonic seizure including Lennox- Gastaut syndrome. METHODS: This is a clinical prospective, add-on, and open-label study performed for 6 months from Jun. 2000 to Dec. 2000 at the pediatric neurology clinic of Severance Hospital. Subjects were selected according to the following criteria, 1) Patients were diagosed as refractory atonic seizure disorder including Lennox-Gastaut syndrome during more than 6 months, 2) Patients had been on maximal doses of at least 2 anticonvulants including sodium valproate and clonazepam or clobazam. We observed seizure frequency of 4 weeks and 24 week medication period as well as adverse reactions every 4 weeks. Those data were analysed primarily for median seizure frequency reduction rate and other efficacy variables such as responder rate with frequency reduction more than 50% and seizure free rate. We also compared the clinical aspects between responder and non responder group. RESULTS: 48 patients were evaluated for efficacy and adverse reactions. Median seizure frequency reduction rate was 42.7%, responders were 22 patients(45.8%) and seizure free patients were 4(8.3%). In Lennox-Gastaut syndrome, median seizure frequency reduction rate was 48.9% and in atonic seizure only 39.3%. However, there were no statistically significant differences in efficacy. We compared clinical aspects between respoder and non responder groups, but couldn't find any difference. The number of patients manifesting adverse reactions was 20(41.6%) in an descending order of frequency, weight gain in 16 patients(33.3%), and irritability in 4 patients(8.3%). CONCLUSION: Deflazacort is believed to be an effective and safe anticonvulsant when used as adjunctive therapy for atonic seizure including Lennox-Gastaut syndrome. However, long term follow up is required to evaluate relapse rate and its adverse reactions.

A Case of Polyarteritis Nodosa Successfully Treated with Deflazacort / 대한류마티스학회지

Polyarteritis nodosa(PAN), a systemic vasculitis involving multiple organs including the nervous system, requires a long-term glucocorticoid therapy. Deflazacort is a synthetic glucocorticoid, which has been claimed to have less side effects, but its use for vasculitis has never been reported in the literature. We report a case of polyarteritis nodosa presenting with mononeuritis multiplex causing a left foot drop, which was successfully treated with deflazacort.

Conversion Effect from Prednisone to Deflazacort in Diabetic Kidney Transplants / 대한신장학회잡지

The blood sugar control has been a significant problem after transplantation. Cyclosporine is partly responsible for post-transplantation diabetes mellitus (PTDM), but steroid has been well known to have diabetogenic effect and mainly responsible for glucose intolerance after transplantation. Deflazacort, a new steroid, has been introduced as a substitute of conventional steroid to prevent glucose intolerance after transplantation. We performed prospective study of deflazacort conversion from conventional steroid in kidney transplant patients with pre-transplantation diabetes mellitus(pre-Tx DM) or PTDM. A total of 82 kidney transplant patients was included for this study. Forty two patients were converted to deflazacort as a conversion group and 40 patients were remained on conventional steroid as a control group. In conversion group, the patients were converted from steroid to deflazacort with ratio of 5:6 in dosage. Nine patients developed severe anorexia with nausea/vomiting and three patients among them went back on steroid within 3 months after conversion(conversion failure 7.1%). After minimal 6 months of follow-up, there was neither episodes of graft dysfunction nor rejection. There was a significant improvement of glucose control in conversion group. In 12 patients(30.8%), more than 50% dose reduction of insulin or oral hypoglycemics requirement was possible. In control group, however, only 2 patients showed greater than 50% of insulin or oral hypoglycemics dose reduction. We could find that deflazacort conversion had a significant impact on blood sugar control in PTDM patients(11/26) but not in pre-Tx DM patients(1/13). In conclusion, conversion to deflazacort in PTDM patients with stable graft function was safe and blood sugar control was readily possible without an increment of risks of rejection and infection. We propose to use deflazacort as a substitute for prednisone in PTDM patients with stable graft function.

Effect of Dexamethasone and Deflazacort on the Function and Gene Expression of the Primary Cultured Human Osteoblast-Like Cells / 대한내분비학회지

Background: Chronic use of glucocorticoid is known to result in osteoporosis. Deflazacort (DFZ), a synthetic glucocorticoid, has been reported to have bone sparing properties in vivo eompared to dexamethasone(DEX). Not only the direct effect of DFZ on human osteoblast but the mechanism by which the drug spares bone remains unclear. This study, therefore, is aimed to investigate the direct effect of DFZ on the proliferation and differentiation of human osteoblast as well as on the gene expression of osteocalcin and osteoblast as well as on the gene expression of osteocalcin and growth factor produced in osteoblast. Methods: Human osteoblast-like cells were cultured from a piece of the tibia removed during selective orthopedic surgery for patients without metabolic bone diseases. The morphological iden- tification of osteoblast-like cell was performed under the light microscope after alkaline phosphatase staining. Cell proliferation rate was determined by [3H] thymidine incorporation into DNA. Cell differentiation was determined by alkaline phophatase activity. mRNA expression was quanti- tatively measured by the competitive reverse transcription-polymerase ehain reaction(RT-PCR). Results: The cultured cells demonstrated 1,25-dihydroxyvitamin D3-induced increases in alkaline phophatase activity and osteocalcin mRNA expression which are the properties of osteoblast. Twenty six percent of the cultured cells were identified as osteoblast-like cells by alkaline phophatase staining. After 24hr incubation with DEX or DFZ, the [3H) thymidine incorporation was significantly inhibited by 100nM DEX or DFL Alkaine phophatase activity was significantly increased by 100nM DEX. Osteocalcin mRNA was significantly decreased by both glueocorticoids. While DEX significantly suppressed expression of asteocalcin mRNA at 10nM and 100nM, DFZ did so only at 100nM. IGF-I mRNA was significantly decreased by 100nM DEX. Conclusion: These results suggest that the inhibitory effect of DFZ on the cell proliferation and protein synthesis is less than that of DEX, which might be responsible for the bone sparing effect of DFZ in vivo.