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1.
Drug Dev Res ; 76(8): 442-9, 2015 Dec.
Article in English | MEDLINE | ID: mdl-26349482

ABSTRACT

The aim of this study was to evaluate fosinopril-induced changes in hemodynamic parameters and tactile allodynia in a rat model of diabetes. Diabetes was induced by streptozotocin (STZ; 50 mg/kg, i.p.) in male Wistar rats. STZ produced hyperglycemia, weight loss, polydipsia, polyphagia, and polyuria as well as long-term arterial hypotension, bradycardia, and tactile allodynia at 10-12 weeks. Daily administration of the angiotensin converting enzyme inhibitor, fosinopril (25 mg/kg, p.o., for 11 weeks) partially reduced the loss of body weight, decreased hyperglycemia, and systolic blood pressure in diabetic rats. Likewise, systemic administration of fosinopril prevented the development and maintenance of tactile allodynia in STZ-induced diabetic rats. These data suggest that fosinopril may have a role in the pharmacotherapy of diabetic neuropathic pain.


Subject(s)
Angiotensin-Converting Enzyme Inhibitors/pharmacology , Diabetes Mellitus, Experimental/drug therapy , Fosinopril/pharmacology , Hyperalgesia/prevention & control , Animals , Diabetes Mellitus, Experimental/blood , Diabetes Mellitus, Experimental/chemically induced , Diabetes Mellitus, Experimental/physiopathology , Diabetic Neuropathies/blood , Diabetic Neuropathies/drug therapy , Diabetic Neuropathies/physiopathology , Hemodynamics/drug effects , Hyperalgesia/blood , Hyperalgesia/physiopathology , Hyperglycemia/blood , Hyperglycemia/chemically induced , Hyperglycemia/drug therapy , Hyperglycemia/physiopathology , Insulin/blood , Male , Rats , Rats, Wistar , Weight Loss/drug effects
2.
Arq Bras Cardiol ; 62(5): 369-74, 1994 May.
Article in Portuguese | MEDLINE | ID: mdl-7998871

ABSTRACT

PURPOSE: To evaluate the adverse reactions of fosinopril with other antihypertensives used as monotherapy. METHODS: Out-patients (n = 2,568) with diagnostic of mild to moderate hypertension, diastolic blood pressure (DBP) 95-115mmHg, with no antihypertensive treatment for 15 days, were included to treatment initially with fosinopril (F) 10mg, once daily, for six weeks. After this period, patients with DBP > 95mmHg had the dosage, once daily, increased to 20mg, while the others were maintained with the same dosage for six more weeks. Adverse reactions of 822 patients treated as monotherapy were grouped as absent, musculoskeletal, cardiovascular, cough, gastrointestinal, neurological, genital-urinary dysfunctions and dermatological and compared with 1,568 with F. Monotherapy consist in alpha-methyldopa (100 patients); beta-blocker (129); calcium blocker (106); diuretic (394); and another ACE inhibitors (93). RESULTS: At the end of the period without treatment, the blood pressure (BP), 165 +/- 16/105 +/- 7mmHg decreased significantly at 6th week to 144 +/- 15/91 +/- 9mmHg (p < 0.05 vs week 0) with further lowering to 139 +/- 13/86 +/- 7mmHg till the end of 12th week. BP response (DBP < or = 90mmHg) was obtained in 89% of the patients with F. Absence of adverse reactions were > or = 70% in patients with F compared to other drugs. CONCLUSION: Fosinopril has demonstrated therapeutic efficacy and less adverse reactions compared to antihypertensives used previously as monotherapy.


Subject(s)
Fosinopril/therapeutic use , Hypertension/drug therapy , Adolescent , Adult , Aged , Aged, 80 and over , Ambulatory Care , Antihypertensive Agents/adverse effects , Antihypertensive Agents/therapeutic use , Female , Fosinopril/adverse effects , Humans , Male , Middle Aged
3.
Arq. bras. cardiol ; Arq. bras. cardiol;62(5): 369-374, maio 1994. graf
Article in Portuguese | LILACS | ID: lil-159851

ABSTRACT

PURPOSE--To evaluate the adverse reactions of fosinopril with other antihypertensives used as monotherapy. METHODS--Out-patients (n = 2,568) with diagnostic of mild to moderate hypertension, diastolic blood pressure (DBP) 95-115mmHg, with no antihypertensive treatment for 15 days, were included to treatment initially with fosinopril (F) 10mg, once daily, for six weeks. After this period, patients with DBP > 95mmHg had the dosage, once daily, increased to 20mg, while the others were maintained with the same dosage for six more weeks. Adverse reactions of 822 patients treated as monotherapy were grouped as absent, musculoskeletal, cardiovascular, cough, gastrointestinal, neurological, genital-urinary dysfunctions and dermatological and compared with 1,568 with F. Monotherapy consist in alpha-methyldopa (100 patients); beta-blocker (129); calcium blocker (106); diuretic (394); and another ACE inhibitors (93). RESULTS--At the end of the period without treatment, the blood pressure (BP), 165 +/- 16/105 +/- 7mmHg decreased significantly at 6th week to 144 +/- 15/91 +/- 9mmHg (p < 0.05 vs week 0) with further lowering to 139 +/- 13/86 +/- 7mmHg till the end of 12th week. BP response (DBP < or = 90mmHg) was obtained in 89per cent of the patients with F. Absence of adverse reactions were > or = 70 per cent in patients with F compared to other drugs. CONCLUSION--Fosinopril has demonstrated therapeutic efficacy and less adverse reactions compared to antihypertensives used previously as monotherapy


Subject(s)
Humans , Male , Female , Adolescent , Adult , Middle Aged , Fosinopril/therapeutic use , Hypertension/drug therapy , Aged, 80 and over , Fosinopril/adverse effects , Antihypertensive Agents/adverse effects , Antihypertensive Agents/therapeutic use , Ambulatory Care
5.
Arq Bras Cardiol ; 60(3): 203-8, 1993 Mar.
Article in Portuguese | MEDLINE | ID: mdl-8250753

ABSTRACT

PURPOSE: To evaluate during 12 weeks the effectiveness and safety of once-a-day fosinopril (10 or 20 mg/day comparative to placebo) in mild to moderate hypertensives according to an open design comparative to placebo. METHODS: One hundred and nineteen patients were studied; 52 +/- 11 years (mean +/- sd) range 18 a 76 years, 86 women and 33 men, 57% whites, 26% blacks and 17% mulattos, 71 mild hypertensives (95 < or = diastolic pressure < or = 104mmHg) e 48 moderate hypertensives (101 < diastolic pressure < or = 115mmHg). RESULTS: There was a significant reduction in systolic/diastolic pressure on the 6th week of treatment (from 161 +/- 16/103 +/- 7 before to 148 +/- 16/94 +/- 9mmHg on the 6th week). On the 12th week of treatment there was an additional significant reduction in systolic/diastolic pressure (from 148 +/- 16/94 +/- 9 on the 6th week to 145 +/- 17/89 +/- 8mmHg on the 12th week). There was a "favorable" response in 71% of the patients on the 12th week; 62% showed diastolic pressure < or = 90mmHg and 9% presented diastolic reduction > or = 10mmHg. There was no difference in the normalization rates between whites and non-whites, mild and moderate hypertensive, obese and non-obese patients, under or above 50 years of age and those patients from no drug-treatment to those on 3 drug before the study. There was no clinically relevant changes in laboratory evaluations before and at the end of the study. The number of adverse reactions was reduced in comparison with previous treatment. CONCLUSION: Fosinopril, according to our and others data, is effective and safe for the treatment of mild to moderate hypertensives, in whites or non-whites, obese or non-obese, younger or older than 50 years and receiving 0 or 3 drugs before the study.


Subject(s)
Fosinopril/administration & dosage , Hypertension/drug therapy , Adolescent , Adult , Aged , Blood Pressure/drug effects , Brazil , Drug Administration Schedule , Female , Fosinopril/therapeutic use , Humans , Male , Middle Aged , Time Factors
6.
Arq. bras. cardiol ; Arq. bras. cardiol;60(3): 203-208, mar. 1993. ilus
Article in Portuguese | LILACS | ID: lil-126183

ABSTRACT

Objetivo - Avaliar a eficácia e segurança do fosinpril administrado isoladamente em dose única diária (10mg/dia ou 20mg/dia) durante 12 semanas a pacientes com hipertensäo essencial leve e moderada näo complicada, segundo esquema aberto, comparativo com placebo. Métodos - Cento e dezenove pacientes (idade 52 ñ 11 anos, média ñ dp, limites: 17 a 76 anos), 86 mulheres e 33 homens, 57// brancos, 26// negros e 17// mestiços, 71 hipertensos leves (95 ó pressäo diastólica ó 104mmHg) e 48 hipertensos moderados (104 < pressäo diastólica ó 115mmHg). Resultados - Houve reduçäo significativa (p < 0,05) da pressäo arterial sistólica/diastólica na 6ª semana de tratamento com fosinopril em relaçäo ao início do tratamento (de 161 ñ 16/103 ñ 7 antes do tratamento para 148 ñ 16/94 ñ 9mmHg na 6ª semana de tratamento, n = 114 pacientes). Na 12ª semana de tratamento verificou-se reduçäo adicional significativa da pressäo arterial sistólica/diastólica em relaçäo à avaliaçäo da 6ª semana (de 148 ñ 16/94 na 6ª semana de tratamento para 145 ñ 17/89 ñ 8mmHg na 12ª semana de tratamento, n = 113 pacientes). Houve resposta favorável em 71// dos pacientes estudados na 12ª semana de tratamento, sendo normalizaçäo da pressäo arterial diastólica (ó 90mmHg) em 62// dos pacientes e queda ò 10// em 9// dos pacientes. Näo houve diferenças significantes nos índices de normalizaçäo da pressäo diastólica ao se comparar pacientes brancos aos näo brancos, hipertensos leves e moderados, obesos e näo obesos, acima e abaixo de 50 anos e nos que recebiam de 1 a 3 drogas antes do estudo. Näo foram varificadas variaçöes clinicamente signficativas nas avaliaçöes laboratoriais antes e ao final do tratamento. Houve reduçäo muito importante do número de reaçöes adversas relatadas nas avaliaçöes realizadas na 6ª e 12ª semanas de tratamento com fosinopril em relaçäo ao tratamento anterior. Conclusäo - O fosinopril mostra-se seguro e eficaz no tratamento da hipertensäo arterial tendo sido igualmente eficaz em hipertensos leves e moderados, brancos e näo brancos, obesos e näo obesos, acima e abaixo de 50 anos e nos que recebiam de 0 a 3 drogas antes do estudo


Purpose - To evaluate during 12 weeks the effectiveness and safety of once-a-day fosinopril (10 or 20mg/day comparative to placebo) in mild to moderate hypertensives according to an open design comparative to placebo. Methods - One hyndred and nineteen patients were studied; 52 ± 11 years (mean ± sd) range 18 a 76 years, 86 women and 33 men, 57% whites, 26% blacks and 17% mulattos, 71 mild hypertensives (95 £ diastolic pressure £ 104mmHg) e 48 moderate hypertensives (101 < diastolic pressure £ 115mmHg). Results - There was a significant reduction in systolic/diastolic pressure on the 6th week of treatment (from 161 ± 16/103 ± 7 before to 148 ± 16/94 ± 9mmHg on the 6th week). On the 12th week of treatment there was an additional significant reduction in systolic/diastolic pressure (from 148 ± 16/94 ± 9 on the 6th week to 145 ± 17/89 ± 8mmHg on the 12th week). There was a "favorable" response in 71% of the patients on the 12th week; 62% showed diastolic pressure £ 90mmHg and 9% presented diastolic reduction ³ 10mmHg. There was no difference in the normalization rates between whites and non-whites, mild and moderate hypertensive, obese and non-obese patients, under or above 50 years of age and those patients from no drug-treatment to those on 3 drug before the study. There was no clinically relevant changes in laboratory evaluations before and at the end of the study. The number of adverse reactions was reduced in comparison with previous treatment. Conclusion - Fosinopril, according to our and others data, is effective and safe for the treatment of mild to moderate hypertensives, in whites or non-whites, obese or non-obese, younger or older than 50 years and receiving 0 or 3 drugs before the study


Subject(s)
Humans , Male , Female , Adolescent , Adult , Middle Aged , Fosinopril/administration & dosage , Hypertension/drug therapy , Time Factors , Brazil , Fosinopril/therapeutic use , Arterial Pressure
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