scholarly journals A Comparison of the Efficacy and Tolerability of Controlled-Release Carbamazepine with Conventional Carbamazepine

Author(s):  
Z. Dhalla ◽  
J. Bruni ◽  
J. Sutton

ABSTRACT:We compared the efficacy and tolerability of controlled-release carbamazepine (CBZ-CR) with conventional carbamazepine (CBZ) in 131 epileptic patients (both men and women, ages 6-65 years) in an open, multicentre, cross-over trial. Patients entered into the trial were previously on CBZ monotherapy or polytherapy. During the first 4 weeks, patients were treated with equivalent daily doses of CBZ and then switched to CBZ-CR for the subsequent 4 weeks. The majority of patients were switched to the more convenient b.i.d. dosing schedule of the controlled-release (CR) preparation without a detrimental effect on seizure frequency or adverse effects. In 44/131 (34%) of patients, the switch to CBZ-CR was accompanied by an improvement in tolerability, primarily due to a reduction in peak-dependent CNS side-effects such as tiredness, double or blurred vision, dizziness and ataxia. At the end of the study, investigators preferred CBZ-CR for 76% of their patients and 70% of the patients preferred CBZ-CR.

2021 ◽  
Vol 19 ◽  
Author(s):  
Enes Akyüz ◽  
Mohd. Farooq Shaikh ◽  
Betül Köklü ◽  
Cansu Ozenen ◽  
Alina Arulsamy

: Over the decades, various interventions have been developed and utilized to treat epilepsy. However, majority of epileptic patients are often first prescribed with anti-epileptic drugs (AED), now known as anti-seizure drugs (ASD), as a first line of defense to suppress their seizures and regain their quality of life. ASDs exert their anti-convulsant effects through various mechanisms of action including regulation of ion channels, blocking of glutamate-mediated stimulating neurotransmitter interaction, and enhancing the inhibitory GABA transmission. About one third of epileptic patients are often resistant to anti-convulsant drugs, while others develop numerous side effects which may lead to treatment discontinuation and further deterioration of quality of life. Common side effects of ASDs include headache, nausea and dizziness. However, more adverse effects such as auditory and visual problems, skin problems, liver dysfunction, pancreatitis and kidney disorders may also be witnessed. Some ASDs may even result in life-threatening conditions as well as serious abnormalities, especially in patients with comorbidities and in pregnant women. Nevertheless, some clinicians had observed a reduction in the development of side effects post individualized ASD treatment. This suggest that a careful and well-informed ASD recommendation to patients may be crucial for an effective and side-effect free control of their seizures. Therefore, this review aimed to elucidate the anticonvulsant effects of ASDs as well as their side effect profile, by discussing their mechanism of action and reported adverse effects based on clinical and preclinical studies, thereby providing clinicians with a greater understanding of the safety of current ASDs.


Author(s):  
Leonilda Bilo ◽  
Maria Fulvia de Leva ◽  
Roberta Meo

Background:The aim of this study was to evaluate efficacy and tolerability of levetiracetam (LEV) in patients with different epilepsy syndromes.Methods:We evaluated epileptic patients seen in the previous 18 months, including all patients with present or past exposure to LEV. Tolerability of LEV therapy was evaluated in all patients; efficacy was evaluated only in patients who had received LEV for at least six months. Two hundred and two patients were included in the study. Patients were considered responsive when showing a > 50% reduction in seizures frequency and non-responders when seizure frequency was unchanged, worsened or showed a reduction < 50%.Results:Thirty patients did not complete six months of LEV treatment and dropped out. 57.4% of the patients with uncontrolled seizures treated for at least six months were responders, with 27.7% seizure free. Adverse effects were observed in 46 patients (23%) and were responsible for early drop out in 26. Adverse effects occurred significantly more often in females than in males (30.6% vs 13.2%); moreover, nearly 30% of women with adverse effects complained of more than one adverse effect, while this was never observed in male patients.Conclusions:Our study shows LEV as a well tolerated and effective treatment, both in monotherapy and as an add-on. Further investigations on larges samples are needed to investigate the issue of gender-related tolerability.


2021 ◽  
Vol 3 (1) ◽  
pp. 14-18
Author(s):  
I.M. Ikeh ◽  
◽  
O.O. Odikamnoro ◽  
V.O. Okonkwo ◽  
I.O. Nnatuanya ◽  
...  

Adverse effects of antimalarial drugs, which were commonly attributed to chloroquine such as: headache, various skin eruptions, Pruritus, Gastro-intestinal disturbances such as nausea, and vomiting. Others, such as: mental changes involving psychotic episodes, anxiety, visual disturbances such as blurred vision, keratopathy or retinopathy. Some common side effects like loss of hair, ototoxicity, photosensitivity, tinnitus, neuro-myopathy, myopathy, erythema multiformes and Stevens-Johnson syndrome, hemolysis and blood dyscrasias, Neutropenia etc., are still reported in some patients treated with the Pyrimethamine and Sulphadoxine drug combination. The emergence of combination therapeutic approach to malaria treatment was believed to have reduced the frequency of these events, but most, still persist. This survey was conducted to therefore, assess the overall presentation of Diarrhoea, Pruritus and Vomit in Patients treated with Maloxine and Fansidar. At Day zero, (D0), 40(15.0%) Presented positive Diarrhoea cases; 05(1.9%) present positive cases of pruritus and 73(27.4%) presented positive cases of vomit. At Day 2, (D2), 03(1.1%) presented positive Diarrhoea cases as against 263(98.9%) of negative cases; 01(0.4%) presented positive cases of pruritus as against 265(99.6%) of negative cases. Day Seven, (D7) and Day Fourteen, (D14) recorded clearance of the adverse effects. There is therefore need for relevant drug treatment follow up to clear the adverse effects engendered by malaria drug therapy.


2020 ◽  
Vol 21 (2) ◽  
pp. 79-88 ◽  
Author(s):  
Pankaj Mandpe ◽  
Bala Prabhakar ◽  
Pravin Shende

Background: Overactive bladder syndrome is a broadly occurring urological disorder with a distressing impact on the quality of life. The commonly used antimuscarinic drugs show poor patient compliance because of unsatisfactory potency, tolerability and high occurrence of adverse effects such as dry mouth, blurred vision, constipation, dizziness etc. Mirabegron is the first approved β3-adrenoreceptor agonist, used as mono or in combination therapies for overactive bladder syndrome. Objective: The present review provides an insight into the mechanism, pharmacokinetics, toxicokinetics, clinical trials and the development of various conventional and modified-release dosage forms of mirabegron for the treatment of overactive bladder syndrome. Results: The clinical trials of phase II and phase III of mirabegron demonstrated symptomatic relief from the overactive bladder without disturbing the micturition cycle. To date, mirabegron showed promising results for safety, tolerability and efficacy in patients with overactive bladder syndrome. The modified-release tablet dosage form of mirabegron appear to be a proficient and suitable replacement for antimuscarinics and revealed the tremendous potential to overcome the adverse effects of conventional antimuscarinic drugs like Oxybutyline chloride ER, Detrol LA, VESIcare, etc. Conclusion: Mirabegron shows a distinct mode of action, i.e., targeting β3-adrenoreceptors and improving bladder storage without altering void contractions. The limited side effects, high safety, efficacy and tolerability of mirabegron present an adequate substitute to antimuscarinics. However, long-term analysis and clinical studies are prerequisites for assessing the safety, tolerability and efficacy profile of mirabegron.


2020 ◽  
Vol 20 (16) ◽  
pp. 1966-1980
Author(s):  
Jaleh Varshosaz ◽  
Saeedeh Fardshouraki ◽  
Mina Mirian ◽  
Leila Safaeian ◽  
Setareh Jandaghian ◽  
...  

Background: Using imatinib, a tyrosine kinase inhibitor drug used in lymphoblastic leukemia, has always had limitations due to its cardiotoxicity and hepatotoxicity side effects. The objective of this study is to develop a target-oriented drug carrier to minimize these adverse effects by the controlled release of the drug. Methods: KIT-5 nanoparticles were functionalized with 3-aminopropyltriethoxysilane and conjugated to rituximab as the targeting agent for the CD20 positive receptors of the B-cells. Then they were loaded with imatinib and their physical properties were characterized. The cell cytotoxicity of the nanoparticles was studied by MTT assay in Ramos (CD20 positive) and Jurkat cell lines (CD20 negative) and their cellular uptake was shown by fluorescence microscope. Wistar rats received an intraperitoneal injection of 50 mg/kg of the free drug or targeted nanoparticles for 21 days. Then the level of aspartate Aminotransferase (AST), alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP) and Lactate Dehydrogenase (LDH) were measured in serum of animals. The cardiotoxicity and hepatotoxicity of the drug were also studied by hematoxylin and eosin staining of the tissues. Results: The targeted nanoparticles of imatinib showed to be more cytotoxic to Ramos cells rather than Jurkat cells. The results of the biochemical analysis displayed a significant reduction in AST, ALT, ALP, and LDH levels in animals treated with targeted nanoparticles, compared to the free drug group. By comparison with the free imatinib, histopathological results represented less cardiotoxicity and hepatotoxicity in the animals, which received the drug through the current designed delivery system. Conclusion: The obtained results confirmed that the rituximab targeted KIT-5 nanoparticles are promising in the controlled release of imatinib and could decrease its cardiotoxicity and hepatotoxicity side effects.


1985 ◽  
Vol 19 (5) ◽  
pp. 349-358 ◽  
Author(s):  
Peter W. Letendre ◽  
Douglas J. DeJong ◽  
Donald R. Miller

The use of methotrexate in rheumatoid arthritis is reviewed. Methotrexate, a folic acid antagonist, is sometimes employed in an attempt to symptomatically control patients whose disease does not respond adequately to conventional therapies. Systemic administration of 7.5–15 mg/wk in a “pulse” fashion appears to be effective without precipitating severe adverse effects. However, concern over potentially serious side effects and a lack of well-controlled clinical trials have limited its use to severe, refractory disease. Further studies are needed before its role in rheumatoid arthritis can justifiably be expanded.


Author(s):  
Jutta Lindert ◽  
Kimberley C. Paul ◽  
E. Lachman Margie ◽  
Beate Ritz ◽  
Teresa Seeman

AbstractLimited research is available on the relationship between social stress and risk of declining cognition. We sought to examine whether social stress has adverse effects on risk of declining episodic memory and executive functioning in aging individuals. We used data from the MIDUS study, a national probability sample of non-institutionalized, English speaking respondents aged 25–74 living in the 48 contiguous states of the United States. The initial wave (1995) included 4963 non-institutionalized adults aged 32–84 (M = 55, SD = 12.4). We used an analytic sample from MIDUS-II (1996/1997) and MIDUS-III (2013) (n = 1821). The dependent variables are episodic memory and executive functioning, which were assessed with the Brief Test for Cognition (BTACT). The independent variables were social stress variables (subjective social status, family and marital stress, work stress and discrimination). To evaluate episodic memory and executive functioning changes over a time period of 10 years, we estimated adjusted linear regression models. Women report significantly lower subjective social status and more discrimination stress than men across all age groups. Controlling for education and income, age, and baseline episodic memory and executive functioning, lower subjective social status had additional adverse effects on declines in episodic memory in men and women. Marital risk had adverse effects on episodic memory in men but not in women. Daily discrimination had adverse effects on executive functioning on all individuals. Public health strategies should focus on reducing social stress in a socio-ecological perspective. Especially, subjective social status and discrimination stress might be a target for prevention efforts.


Vaccines ◽  
2021 ◽  
Vol 9 (7) ◽  
pp. 742
Author(s):  
José Javier Morales-Núñez ◽  
José Francisco Muñoz-Valle ◽  
Carlos Meza-López ◽  
Lin-Fa Wang ◽  
Andrea Carolina Machado Sulbarán ◽  
...  

The main expected result of a vaccine against viruses is the ability to produce neutralizing antibodies. Currently, several vaccines against SARS-CoV-2 are being applied to prevent mortal complications, being Pfizer-BioNTech (BNT162b2) one of the first to be authorized in the USA and Mexico (11 December 2020). This study evaluated the efficacy of this vaccine on antibody production with neutralizing capacity and its side effects in healthcare workers with and without prior SARS-CoV-2 infection and in a group of unvaccinated individuals with prior COVID-19. The main findings are the production of 100% neutralizing antibodies in both groups after the second dose, well-tolerated adverse effects, the possible presence of immunosenescence, and finally, we support that a single dose of this vaccine in individuals with prior COVID-19 would be sufficient to achieve an immunization comparable to people without prior COVID-19 with a complete vaccination program (2 doses).


2018 ◽  
Vol 31 (1) ◽  
pp. 21-24 ◽  
Author(s):  
Andrea Albrecht ◽  
Theresa Penger ◽  
Michaela Marx ◽  
Karin Hirsch ◽  
Helmuth G. Dörr

AbstractBackground:Despite the fact that priming with sex steroids in prepubertal children before growth hormone (GH) provocative tests is recommended, there is an ongoing controversial discussion about the appropriate age of the children, the drug used for priming, the dose and the period between priming and the GH test. Interestingly, there is no discussion on the safety of this procedure. To date, only little data have been available on the possible side effects of priming with testosterone.Methods:We analyzed the outcome in 188 short-statured prepubertal boys who had been primed with testosterone enanthate (n=136: 50 mg; n=51: 125 mg, and accidentally one boy with 250 mg) 7 days prior to the GH test. Serum testosterone levels were measured on the day of the GH test in 99 boys.Results:Overall, only five boys developed adverse side effects. Two boys (dose 125 mg) showed severe low-flow priapism and had to undergo decompression of the corpora cavernosa. One boy suffered from self-limiting priapism and testicular pain (dose 50 mg). Two patients reported testicular pain (each dose 50 mg). The single patient with 250 mg testosterone did not show any adverse effects. The total side effect rate was 2.7%. The serum testosterone levels of the boys with side effects were not different from the testosterone levels of the boys without any side effects.Conclusions:Parents and patients should be informed about the possible side effects of priming with testosterone such as priapism and testicular pain. However, the overall side effect rate is low. We found no correlation between the outcome and the testosterone dose used and/or the level of serum testosterone.


Gut ◽  
1999 ◽  
Vol 44 (6) ◽  
pp. 886-888 ◽  
Author(s):  
P Deltenre ◽  
A Berson ◽  
P Marcellin ◽  
C Degott ◽  
M Biour ◽  
...  

BACKGROUNDTreatment of ulcerative colitis or Crohn’s disease with sulphasalazine causes several adverse effects, including hepatitis. Sulphasalazine is cleaved by colonic bacteria into 5-aminosalicylic acid and sulphapyridine. Received wisdom was that 5-aminosalicylic acid was topically active, whereas sulphapyridine was absorbed and caused immunoallergic side effects. Mesalazine, a slow release formulation of 5-aminosalicylic acid, was expected to be a safe alternative. However, several cases of acute hepatitis have been reported.CASE REPORTA 65 year old man had increased liver enzymes, anti-nuclear and anti-smooth muscle autoantibodies and IgG levels, and lesions of chronic hepatitis after 21 months of mesalazine treatment. Although liver dysfunction had been identified eight months earlier, simvastatin rather than mesalazine had been withdrawn, without any improvement. In contrast, liver enzyme and IgG levels became normal and autoantibodies disappeared after discontinuation of mesalazine administration.CONCLUSIONContrary to initial expectations, mesalazine can cause most of the sulphasalazine induced adverse effects, and hepatic side effects may be almost as frequent. When liver dysfunction occurs, mesalazine administration should be discontinued to avoid the development of chronic hepatitis and liver fibrosis.


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