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ACS Omega Apr 2022Clopamide (CPD, ) is a piperidine and sulfamoylbenzamide-based diuretic drug and a potential photosensitizing sulfonamide; its phototransformation was investigated using...
Clopamide (CPD, ) is a piperidine and sulfamoylbenzamide-based diuretic drug and a potential photosensitizing sulfonamide; its phototransformation was investigated using ,-dimethylaniline (DMA) as an electron donor and 1,4-dicyanonaphthalene (DCN) as an electron acceptor in an immersion-well-type photochemical reactor fitted with a medium-pressure mercury vapor lamp (450 W). Photodegradation of the drug Clopamide resulted in two significant products via photoinduced electron transfer. Structures of these products were deduced from their H NMR, C NMR, mass, and IR spectra. The photoproducts are 2- choloro-5-((2,6-dimethylpiperidin-1-yl)carbamoyl)benzenesulfonic acid () and 4-hydroxy--(2,6-dimethyl-1-piperidyl)-3-sulfamoyl benzamide (). In addition to this, the comparative antioxidant potentials of the parent drug and its photoproducts were investigated using in silico molecular docking against tyrosinase in order to better understand the in vivo relevance of pharmacological action of the drug as a result of light-drug interactions. UV light has been observed to modify substituents on the benzene ring, hence loss of biological activity at the time of storage and in vivo cannot be ruled out. This suggests that Clopamide users should avoid light (natural or artificial) exposure to prevent from drug-induced photosensitivity.
PubMed: 35559154
DOI: 10.1021/acsomega.2c00256 -
PloS One 2012Plant activators are agrochemicals that activate the plant immune system, thereby enhancing disease resistance. Due to their prophylactic and durable effects on a wide...
Plant activators are agrochemicals that activate the plant immune system, thereby enhancing disease resistance. Due to their prophylactic and durable effects on a wide spectrum of diseases, plant activators can provide synergistic crop protection when used in combination with traditional pest controls. Although plant activators have achieved great success in wet-rice farming practices in Asia, their use is still limited. To isolate novel plant activators applicable to other crops, we screened a chemical library using a method that can selectively identify immune-priming compounds. Here, we report the isolation and characterization of three diuretics, bumetanide, bendroflumethiazide and clopamide, as immune-priming compounds. These drugs upregulate the immunity-related cell death of Arabidopsis suspension-cultured cells induced with an avirulent strain of Pseudomonas syringae pv. tomato in a concentration-dependent manner. The application of these compounds to Arabidopsis plants confers disease resistance to not only the avirulent but also a virulent strain of the pathogen. Unlike salicylic acid, an endogenous phytohormone that governs disease resistance in response to biotrophic pathogens, the three diuretic compounds analyzed here do not induce PR1 or inhibit plant growth, showing potential as lead compounds in a practical application.
Topics: Arabidopsis; Arabidopsis Proteins; Bendroflumethiazide; Bumetanide; Cell Death; Cells, Cultured; Clopamide; Disease Resistance; Diuretics; Dose-Response Relationship, Drug; Gene Expression Regulation, Plant; Host-Pathogen Interactions; Molecular Structure; Plant Diseases; Plant Immunity; Pseudomonas syringae; Reverse Transcriptase Polymerase Chain Reaction; Transcription Factors
PubMed: 23144763
DOI: 10.1371/journal.pone.0048443 -
Journal of Neuroscience Methods Feb 2012Clonus can disrupt daily activities after spinal cord injury. Here an algorithm was developed to automatically detect contractions during clonus in 24h electromyographic...
Clonus can disrupt daily activities after spinal cord injury. Here an algorithm was developed to automatically detect contractions during clonus in 24h electromyographic (EMG) records. Filters were created by non-linearly scaling a Mother (Morlet) wavelet to envelope the EMG using different frequency bands. The envelope for the intermediate band followed the EMG best (74.8-193.9 Hz). Threshold and time constraints were used to reduce the envelope peaks to one per contraction. Energy in the EMG was measured 50 ms either side of each envelope (contraction) peak. Energy values at 5% and 95% maximal defined EMG start and end time, respectively. The algorithm was as good as a person at identifying contractions during clonus (p=0.946, n=31 spasms, 7 subjects with cervical spinal cord injury), and marking start and end times to determine clonus frequency (intra class correlation coefficient, α: 0.949), contraction intensity using root mean square EMG (α: 0.997) and EMG duration (α: 0.852). On average the algorithm was 574 times faster than manual analysis performed independently by two people (p ≤ 0.001). This algorithm is an important tool for characterization of clonus in long-term EMG records.
Topics: Adult; Algorithms; Clopamide; Diagnosis, Computer-Assisted; Electromyography; Female; Humans; Male; Middle Aged; Muscle Contraction; Muscle, Skeletal; Myoclonus; Reproducibility of Results; Sensitivity and Specificity; Spinal Cord Injuries
PubMed: 22057220
DOI: 10.1016/j.jneumeth.2011.10.017 -
Annals of the Rheumatic Diseases Nov 1966
Topics: Allopurinol; Clopamide; Enzyme Therapy; Gout; Hematologic Diseases; Humans; Hypertension; Kidney Failure, Chronic; Polythiazide; Uric Acid; Xanthine Oxidase
PubMed: 5958696
DOI: 10.1136/ard.25.Suppl_6.660 -
Molecules (Basel, Switzerland) Jul 2014Diabetes mellitus is a life threatening disease and scientists are doing their best to find a cost effective and permanent treatment of this malady. The recent trend is...
Diabetes mellitus is a life threatening disease and scientists are doing their best to find a cost effective and permanent treatment of this malady. The recent trend is to control the disease by target base inhibiting of enzymes or proteins. Secreted frizzled-related protein 4 (SFRP4) is found to cause five times more risk of diabetes when expressed above average levels. This study was therefore designed to analyze the SFRP4 and to find its potential inhibitors. SFRP4 was analyzed by bio-informatics tools of sequence tool and structure tool. A total of three potential inhibitors of SFRP4 were found, namely cyclothiazide, clopamide and perindopril. These inhibitors showed significant interactions with SFRP4 as compared to other inhibitors as well as control (acetohexamide). The findings suggest the possible treatment of diabetes mellitus type 2 by inhibiting the SFRP4 using the inhibitors cyclothiazide, clopamide and perindopril.
Topics: Computer Simulation; Diabetes Mellitus; Humans; Hypoglycemic Agents; Molecular Docking Simulation; Proto-Oncogene Proteins
PubMed: 25019556
DOI: 10.3390/molecules190710129 -
British Journal of Clinical Pharmacology 19801. The antihypertensive effect and side-effects of the new centrally acting agent guanfacine (BS 100-141, Estulic) and guanethidine (Ismelin) were compared in a... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
1. The antihypertensive effect and side-effects of the new centrally acting agent guanfacine (BS 100-141, Estulic) and guanethidine (Ismelin) were compared in a single-blind, cross-over study. The study consisted of two active treatment periods of 6 weeks each, both preceded by a 1-3 weeks placebo period. 2. Sixteen ambulant patients (six male, ten female) with mild or moderate hypertension were admitted to the study. The patients were also receiving diuretic therapy (clopamide 10-20 mg daily). On average the optimal daily dose of guanfacine was 3 mg and of guanethidine 20 mg. 3. An equally large and significant decrease in blood pressure was produced by both drugs. Both guanfacine and guanethidine caused a very slight reduction in heart rate. Mild orthostatic hypotension occurred in 11 patients during guanethidine therapy. Dryness of the mouth occurred in 13 patients taking guanfacine.
Topics: Antihypertensive Agents; Blood Pressure; Clinical Trials as Topic; Female; Guanethidine; Guanfacine; Guanidines; Heart Rate; Humans; Hypertension; Male; Phenylacetates
PubMed: 6994786
DOI: 10.1111/j.1365-2125.1980.tb04912.x -
Medical Archives (Sarajevo, Bosnia and... Dec 2014To determine types and frequency of side effects of antihypertensive drugs in patients with diabetes mellitus (DM) type 2 and hypertension.
OBJECTIVE
To determine types and frequency of side effects of antihypertensive drugs in patients with diabetes mellitus (DM) type 2 and hypertension.
SUBJECTS AND METHODS
We performed a prospective study of 79 patients with DM type 2 and hypertension, randomly selected by systematic sampling, who were followed over a period of six months. Patients were assessed at baseline and once a month measuring following parameters: types of used antihypertensive drugs and frequency of side effects, the values (mmHg) of systolic (SBP) and diastolic blood pressure (DBP).
RESULTS
Out of 79 patients, 48/79 (60.8%) were males and 31/79 (39.2%) were females. The median age in males was 53 years (IQR=48 to 55 years), in females was 53 years (IQR=49 to 56 years). There was no statistically significant difference in median age between males and females (P=0.368). There is a statistically significant difference in the values of SBP [χ2(5)=312.296, P<0.001] and DBP [χ2(5)=216.051, P<0.001] over a period of six months follow-up. The drug side effects were noted in 9/79 (11.4%) patients between 1-2 months, in 6/79 (7.6%) between 2-3 months, in 1/79 (1,3%) between 3-4 months. The most common side effect was cough (11/79 or 13.9%) associated with the combination of ACE inhibitor and thiazide diuretics. In 5/79 (6.3%) patients there were reports of: flushing, palpitations, headache, dizziness and leg edema associated with Ca blockers.
CONCLUSION
The most common side effect of antihypertensive treatment was cough (13.9%) associated with the combination of ACE inhibitor and thiazide diuretic.
Topics: Adult; Angiotensin-Converting Enzyme Inhibitors; Antihypertensive Agents; Blood Pressure; Clopamide; Diabetes Mellitus, Type 2; Diuretics; Dose-Response Relationship, Drug; Drug-Related Side Effects and Adverse Reactions; Female; Humans; Hypertension; Hypoglycemic Agents; Male; Middle Aged
PubMed: 25648509
DOI: 10.5455/medarh.2014.68.372-375 -
Postgraduate Medical Journal Apr 1965'Brinaldix', a new non-thiazide oral diuretic, has been used in a trial on three normal subjects and fourteen patients with oedema from various causes. It is a potent... (Clinical Trial)
Clinical Trial
'Brinaldix', a new non-thiazide oral diuretic, has been used in a trial on three normal subjects and fourteen patients with oedema from various causes. It is a potent salidiuretic and proved superior to bendrofluazide in 10 out of 14 patients. It produced a substantial potassium diuresis, and we are of the opinion that potassium supplements should be given in conjunction with it. In one normal subject it produced a period of postural hypotension; no other major side-effects were noted.
Topics: Adult; Aged; Bendroflumethiazide; Chemical Phenomena; Chemistry; Child; Clopamide; Drug Evaluation; Edema; Female; Humans; Male; Middle Aged
PubMed: 5293942
DOI: 10.1136/pgmj.41.474.193 -
British Journal of Clinical Pharmacology May 1984The importance of number of tablets for patient compliance was investigated in 160 patients with mild-moderate essential hypertension treated with a beta-adrenoceptor... (Clinical Trial)
Clinical Trial Comparative Study
The importance of number of tablets for patient compliance was investigated in 160 patients with mild-moderate essential hypertension treated with a beta-adrenoceptor blocker and a thiazide diuretic. Mean BP at entry 146 +/- 16/92 +/- 8 mm Hg. All patients were given pindolol 10 mg and clopamide 5 mg in one combination tablet or in separate tablets for 4 months respectively. Approximately 90% of the patients took greater than 90% of the prescribed dose throughout the study. Mean BP decreased progressively and heart rate increased slightly. Side effects were more frequently reported during the first month of the study than previously, and 30 patients discontinued the treatment. No differences in this respect were seen between 1 and 2 tablets daily. Approximately 75% of the patients preferred 1 tablet daily, but combining two drugs in one tablet had no effect upon compliance.
Topics: Adult; Blood Pressure; Clinical Trials as Topic; Clopamide; Drug Combinations; Drug Therapy, Combination; Female; Heart Rate; Humans; Hypertension; Male; Middle Aged; Patient Compliance; Patient Dropouts; Pindolol; Potassium; Tablets; Uric Acid
PubMed: 6375710
DOI: 10.1111/j.1365-2125.1984.tb02388.x -
British Journal of Clinical Pharmacology Dec 19821 We have assessed the efficacy of Viskaldix, a combination of pindolol 10 mg and clopamide 5 mg using continuous intra-arterial ambulatory blood pressure monitoring. 2...
1 We have assessed the efficacy of Viskaldix, a combination of pindolol 10 mg and clopamide 5 mg using continuous intra-arterial ambulatory blood pressure monitoring. 2 Fourteen of the sixteen patients entered were studied on no therapy and following a minimum of 6 weeks at a constant dosage of Viskaldix. 3 Viskaldix produced a marked and consistent reduction of the blood pressure over the 24 h. The diurnal variation in the heart rate was decreased. 4 The results were compared with those of a similar study with once-daily pindolol where there was control during the day but not in the early morning when the blood pressures rose rapidly.
Topics: Adrenergic beta-Antagonists; Adult; Antihypertensive Agents; Benzothiadiazines; Blood Pressure; Clopamide; Diuretics; Drug Combinations; Female; Humans; Hypertension; Male; Middle Aged; Pindolol; Sodium Chloride Symporter Inhibitors
PubMed: 6129883
DOI: 10.1111/j.1365-2125.1982.tb02044.x