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Endocrine, Metabolic & Immune Disorders... 2021The aim of the study was to experimentally investigate the antihypertensive effect of Ruta Montana.
AIMS
The aim of the study was to experimentally investigate the antihypertensive effect of Ruta Montana.
BACKGROUND
Ruta montana L. is traditionally used in Moroccan herbal medicine to treat hypertension. This study aimed to experimentally evaluate the hypotensive and vasoactive properties of this plant.
OBJECTIVE
The objective of the study was to evaluate the effect of the aqueous extract of Ruta Montana on blood pressure parameters in LNAME-induced hypertensive rats and to determine the vasorelaxant activity of this aqueous extract.
METHODS
The antihypertensive effect of the aqueous extract obtained from Ruta montana aerial parts (RMAPAE) (200 mg/kg) was evaluated in normal and anesthetized hypertensive rats. Blood pressure parameters (systolic blood pressure (SBP), mean blood pressure (MBP) and diastolic blood pressure (DBP)) and heart rate were measured using a tail-cuff and a computer-assisted monitoring device. The acute and chronic effect of RMAPAE was recorded for 6 hours for the acute experiment and for 7 days for the sub-chronic test. In the other set, the vasorelaxant effect of RMAPAE on the contractile response was observed in the isolated thoracic aorta.
RESULTS
The results indicated that the RMAPAE extract significantly decreased SBP, MBP, DBP and heart rate in L-NAME-induced hypertensive rats. Furthermore, RMAPAE was demonstrated to induce a dose-dependent relaxation in the aorta precontracted with Epinephrine or KCl. More interestingly, this vasorelaxant activity of RMAPAE seems to be probably mediated through the prostaglandins pathway.
CONCLUSION
The present study illustrates the beneficial action of Ruta montana on hypertension and supports its use as an antihypertensive agent.
Topics: Animals; Antihypertensive Agents; Blood Pressure; Dose-Response Relationship, Drug; Hypertension; Male; NG-Nitroarginine Methyl Ester; Organ Culture Techniques; Plant Extracts; Prostaglandins; Rats; Rats, Wistar; Ruta; Vasodilation
PubMed: 32600240
DOI: 10.2174/1871530320666200628025430 -
American Heart Journal Nov 1983Trimazosin, a selective alpha-1-adrenoceptor-blocking agent, has been extensively evaluated in over 1000 patients. In hypertensive patients, reduction in elevated blood... (Clinical Trial)
Clinical Trial
Trimazosin, a selective alpha-1-adrenoceptor-blocking agent, has been extensively evaluated in over 1000 patients. In hypertensive patients, reduction in elevated blood pressure in both supine and standing positions, consequent to a reduction in systemic vascular resistance, persisted in long-term therapy. Progression of hypertension target organ damage did not occur. Improvement in blood lipids with decreased total serum cholesterol was noted in long-term therapy. In long-term studies, 74% of patients responded at a trimazosin dose of 300 mg/day or less; the maximum dose was 300 mg/day or less in 52% of patients and 200 mg/day or less in 36%. Most patients received twice a day therapy. The side effect profile of trimazosin was comparable to placebo and significantly better than that of either methyldopa or propranolol. Concomitant disease or therapy did not adversely affect the trimazosin safety profile. Hematology, clinical chemistry, and urinary parameters did not indicate deleterious effects. Because of its excellent safety and toleration profile, trimazosin may be particularly suitable in first-line therapy of patients with mild or moderate hypertension.
Topics: Antihypertensive Agents; Blood Pressure; Cardiomegaly; Clinical Trials as Topic; Double-Blind Method; Drug Therapy, Combination; Humans; Hypertension; Kidney; Lipids; Piperazines; Risk
PubMed: 6227228
DOI: 10.1016/0002-8703(83)90188-6 -
The American Journal of Medicine Aug 1992In choosing the optimum antihypertensive agent for an individual patient, various factors should be considered. Demographic characteristics (e.g., age, gender, race) and... (Review)
Review
In choosing the optimum antihypertensive agent for an individual patient, various factors should be considered. Demographic characteristics (e.g., age, gender, race) and the circadian pattern of blood pressure elevation may influence the response to therapy. Concomitant therapy for coexisting medical disorders must be evaluated for possible drug interactions. Calcium channel blockers, which can be used in any age group, may be particularly useful in hypertensive patients with certain concurrent conditions (e.g., coronary artery disease, migraine, or gastrointestinal motility disorders). Life-style, including occupation and leisure-time activities, may contraindicate the use of certain drugs in a particular patient. It also may be necessary to consider the economic status of the patient, particularly in the elderly, who often have limited disposable income. Since to a great extent successful therapeutic management of hypertension depends on patient compliance, reduced frequency of dosing (i.e., once or twice daily) is desirable. The clustering of morbid events in the hours immediately following awakening highlights the need for therapy that provides 24-hour control, thereby ensuring adequate pharmacodynamic effects during that crucial period. The challenge is to select the most appropriate first-line agent (diuretic, beta blocker, calcium channel blocker, or angiotensin-converting enzyme inhibitor) for a particular patient.
Topics: Age Factors; Antihypertensive Agents; Blood Pressure; Calcium Channel Blockers; Circadian Rhythm; Comorbidity; Drug Costs; Drug Therapy, Combination; Humans; Hypertension; Life Style; Racial Groups; Sex Factors
PubMed: 1519634
DOI: 10.1016/0002-9343(92)90293-k -
Clinical Therapeutics Apr 2001Mecamylamine hydrochloride was initially developed for its ganglion-blocking activity and has been marketed as an antihypertensive agent in the United States for >40... (Review)
Review
BACKGROUND
Mecamylamine hydrochloride was initially developed for its ganglion-blocking activity and has been marketed as an antihypertensive agent in the United States for >40 years. Several other potential therapeutic applications are being investigated, most of them focusing on the drug's ability to cross the blood-brain barrier and selectively antagonize neuronal nicotinic acetylcholine receptors. This central activity of mecamylamine is demonstrable at much lower doses than the effective antihypertensive dose, thus avoiding many of the bothersome side effects associated with the drug's inhibition of parasympathetic activity.
OBJECTIVE
Because investigations are being conducted in new patient populations, including pediatric patients, an update of the toxicity/risk profile of mecamylamine is timely. This review describes nonclinical and clinical data pertaining to the pharmacology, toxicity, and tolerability of mecamylamine, including some previously unpublished toxicology and clinical pharmacokinetics data. Potential new therapeutic applications are discussed, including the use of mecamylamine in treating autonomic dysreflexia; dependencies on nicotine, cocaine, and other substances of abuse; Tourette's syndrome; and other neuropsychiatric disorders.
METHODS
Information for this review of mecamylamine was identified through a search of MEDLINE from 1966 to the present, as well as from the master files of Merck & Co, Inc, the drug's original manufacturer, and Layton BioScience, Inc, its present manufacturer.
CONCLUSIONS
The available data concerning potential new applications of mecamylamine, although sparse, suggest that the drug's toxicity/risk profile may be much improved at lower doses.
Topics: Animals; Antihypertensive Agents; Area Under Curve; Autonomic Dysreflexia; Central Nervous System; Cognition; Drug Therapy, Combination; Humans; Hypertension; Lethal Dose 50; Mecamylamine; Mutagenicity Tests; Peripheral Nerves; Receptors, Cholinergic; Receptors, Nicotinic; Reproduction; Risk Factors; Rodentia
PubMed: 11354389
DOI: 10.1016/s0149-2918(01)80059-x -
Postgraduate Medicine May 1992Choosing antihypertensive agents that protect patients against cardiovascular and other complications is a growing trend in the treatment of mild to moderate... (Review)
Review
Choosing antihypertensive agents that protect patients against cardiovascular and other complications is a growing trend in the treatment of mild to moderate hypertension. Calcium channel blockers and angiotensin-converting enzyme (ACE) inhibitors are favored because they have neutral or positive effects on lipid levels and insulin resistance. The alpha 1 blockers, especially doxazosin mesylate (Cardura), are enjoying a resurgence in popularity because they have a beneficial effect on lipid levels. In terms of preserving patients' quality of life, the ACE inhibitors in particular have been shown to have a positive impact. It has been shown that systolic hypertension in elderly patients should definitely be treated, but the most appropriate agent has yet to be defined. Therapy should be tailored to the individual. The following questions should be considered when choosing an antihypertensive agent: (1) What are its side effects (especially metabolic ones)? (2) Does it require only once- or twice-a-day dosing? (3) Does it cause regression of left ventricular hypertrophy? (4) Does it prevent death from coronary artery disease? (5) How will it affect quality of life? (6) How much does it cost? The goal of therapy should be to provide adequate blood pressure control throughout the day, enhance compliance, and protect the heart, brain, and kidneys without adversely affecting metabolic state.
Topics: Adrenergic beta-Antagonists; Aged; Angiotensin-Converting Enzyme Inhibitors; Antihypertensive Agents; Benzothiadiazines; Coronary Disease; Diuretics; Humans; Hypertension; Insulin Resistance; Lipid Metabolism; Lipids; Quality of Life; Risk Factors; Sodium Chloride Symporter Inhibitors; Treatment Outcome
PubMed: 1349744
DOI: 10.1080/00325481.1992.11701321 -
Clinical Pharmacokinetics Jun 1994Although individualised antihypertensive therapy is widely recommended, prospective methods for optimising treatment are hampered by the paucity of basic information... (Review)
Review
Although individualised antihypertensive therapy is widely recommended, prospective methods for optimising treatment are hampered by the paucity of basic information about dose-plasma concentration-response relationships for commonly used drugs. Concentration-effect analysis has been applied to a number of therapeutic areas. With antihypertensive drugs this approach has clearly identified direct relationships between pharmacokinetic and pharmacodynamic profiles within individual patients. Thus, either a linear or nonlinear model can be used to quantify the antihypertensive drug response in terms of parameters that incorporate pharmacokinetic and pharmacodynamic information. Furthermore, these models take account of placebo effects and time-dependent changes in blood pressure and drug concentrations during a dosage interval. Concentration-effect analysis has been used to characterise the responses to a range of calcium antagonist drugs. These studies have demonstrated that these analyses are useful for optimising dosage schedules, identifying determinants of blood pressure response, and predicting steady-state profiles of blood pressure (including peak/trough effects) after administration of a single ('test') dose. This mode of analysis warrants early inclusion in the clinical development of any new antihypertensive agent, so that the familiar difficulties in identifying the optimum dosage range are avoided.
Topics: Antihypertensive Agents; Blood Pressure; Calcium Channel Blockers; Dose-Response Relationship, Drug; Drug Interactions; Humans; Nifedipine
PubMed: 8070220
DOI: 10.2165/00003088-199426060-00005 -
International Journal of Stroke :... Oct 2014Antihypertensive drugs are useful in the prevention of stroke; however, much debate surrounds which class of agent provides the most benefit post-stroke. (Comparative Study)
Comparative Study
BACKGROUND
Antihypertensive drugs are useful in the prevention of stroke; however, much debate surrounds which class of agent provides the most benefit post-stroke.
AIMS
The aim of this study was to examine the impact of different classes of antihypertensive agent on stroke outcome using data from the ChinaQUEST study, a prospective, hospital-based stroke registry undertaken across 62 hospitals in China.
METHODS
Logistic regression analysis was used to determine the comparative associations of different antihypertensive medications when initiated in-hospital post-stroke on the following poor outcomes in stroke survivors at three- and 12 months post-stroke: (1) death and dependency, based on modified Rankin Scale scores 3-5; (2) death; and (3) dependency.
RESULTS
Of the 6416 patients with baseline data, 3986 (62%) were on at least one antihypertensive agent. After adjustment for baseline characteristics and concomitant therapies, there were no differences in outcomes between therapies at three- and 12 months, but at 12 months, calcium channel blocker use was associated with reduced risks of death/dependency (odds ratio 0·78, P = 0·001) and death (odds ratio 0·66, P < 0·001). In addition, angiotensin-converting enzyme inhibitor/angiotensin II receptor antagonist use was associated with reduced risk of death (odds ratio 0·76, P = 0·009), whereas both beta-blockers and diuretics were shown to increase the risk of death/dependency and death but had no effect on the risk of dependency.
CONCLUSION
This study suggests that early initiation of calcium channel blockers is associated with improved outcome after stroke. Further randomized studies are warranted to confirm these findings and to delineate differential beneficial effects of antihypertensive therapy in stroke prevention.
Topics: Angiotensin Receptor Antagonists; Angiotensin-Converting Enzyme Inhibitors; Antihypertensive Agents; Calcium Channel Blockers; China; Databases, Factual; Female; Humans; Logistic Models; Male; Stroke; Survival Analysis; Time Factors; Treatment Outcome
PubMed: 25042450
DOI: 10.1111/ijs.12330 -
Therapie Dec 2019Hypertension is a public health problem managed according to therapeutic strategies published in France by the Hauteautoritéde santé (HAS - French Health...
AIM
Hypertension is a public health problem managed according to therapeutic strategies published in France by the Hauteautoritéde santé (HAS - French Health Authorities). For patients with resistant hypertension, related or not to a non-adherence, prescribers need to be sure the exposure is high enough to achieve the tensional target. Quantitative analysis of antihypertensive drugs in different biological matrices (blood/urine) is one possible solution. However, this involves determining the concentrations observed at standard doses and knowing how to interpret the measured concentrations. It is also necessary to identify medical laboratories that can assay antihypertensive drugs. This was the aim of our work.
METHODS
The main antihypertensive drugs recommended by the HAS have been listed. For each of them, we looked for published steady-state plasma/serum concentrations and quantities excreted in the urine at usual dosages. In addition, the elimination half-life and linear pharmacokinetic profile were specified for each antihypertensive agent measured in plasma/serum. Pharmacology-Toxicology laboratories in France likely to carry out assays were identified. The time taken to report the result and the cost of the analysis were also specified.
RESULTS
All of the afore-mentioned information has been collected and presented in a table. This can then be used to compare the plasma/serum concentration or the quantity measured in a patient's urine with the values reported in the literature. In cases where the blood sampling times differ between those of the patient and the published data, the patient's measured value is compared to the estimated value based on the published concentrations and pharmacokinetics.
CONCLUSION
Interpretation of the plasma/serum/urinary value measured or estimated for an antihypertensive drug is a particularly interesting approach to determine if drug exposure is enough and a possible non-adherence. However, this activity is mostly carried out in hospital centres.
Topics: Antihypertensive Agents; Biological Availability; Blood Chemical Analysis; Clinical Laboratory Services; Clinical Laboratory Techniques; Costs and Cost Analysis; Dose-Response Relationship, Drug; Drug Monitoring; France; Humans; Hypertension; Medication Adherence; Patient Care Planning; Urinalysis
PubMed: 31301815
DOI: 10.1016/j.therap.2019.05.002 -
Drugs 1988Urapidil is an alpha 1-adrenoceptor antagonist which also has a central antihypertensive effect, the mechanism of which has yet to be conclusively defined. A number of... (Review)
Review
Urapidil is an alpha 1-adrenoceptor antagonist which also has a central antihypertensive effect, the mechanism of which has yet to be conclusively defined. A number of open and comparative studies have produced evidence for the efficacy and safety of urapidil. A study recently completed by the author produced a dose-dependent antihypertensive effect of urapidil which, however, failed to achieve statistical significance, probably due to a large variance of the data and an unexpectedly large placebo effect. Adverse reactions are those expected from an alpha 1-blocker, particularly dizziness, as well as nausea and fatigue. Urapidil is potentially an important new antihypertensive agent; further variable dose and combination (with other antihypertensive agents) studies would help further define its therapeutic niche.
Topics: Adult; Aged; Antihypertensive Agents; Female; Humans; Hypertension; Male; Middle Aged; Piperazines
PubMed: 3042358
DOI: 10.2165/00003495-198800356-00025 -
Journal of Clinical Hypertension... Nov 2015The authors investigated the differences in office and ambulatory blood pressure (BP) among major antihypertensive drug classes and among frequently used drugs in each...
The authors investigated the differences in office and ambulatory blood pressure (BP) among major antihypertensive drug classes and among frequently used drugs in each class in 22,617 patients treated with monotherapy from the Spanish ABPM Registry. Using thiazides as the reference group, patients treated with calcium channel blockers have significantly (P<.01) elevated ambulatory BP and less ambulatory control after adjusting for confounders. Inside each class, no significant differences were observed among thiazides or angiotensin receptor blockers. Atenolol and bisoprolol among β-blockers, amlodipine among calcium channel blockers, and lisinopril and enalapril among angiotensin-converting enzyme inhibitors exhibited lower ambulatory BP and better control than other agents. Differences exist among antihypertensive drug classes and among different compounds in each class with respect to ambulatory BP control. This can help physicians choose among drug classes and among compounds in each class if BP reduction is the main objective of treatment.
Topics: Adrenergic beta-Antagonists; Angiotensin Receptor Antagonists; Angiotensin-Converting Enzyme Inhibitors; Antihypertensive Agents; Blood Pressure; Blood Pressure Monitoring, Ambulatory; Calcium Channel Blockers; Female; Humans; Hypertension; Male; Middle Aged
PubMed: 26205479
DOI: 10.1111/jch.12623