Nanoemulsions for the Delivery of Anti-Hypertensive Drugs

2022 ◽  
pp. 378-400
Author(s):  
Subramanian Natesan ◽  
Nidhi Singh ◽  
Victor Hmingthansanga ◽  
Pallab Datta ◽  
Sai Hanuman Sagar Boddu ◽  
...  

Hypertension refers to an increase in the arterial blood pressure. Most commonly used antihypertensive drugs are available in conventional dosage forms as it offers superior patient compliance. A majority of anti-hypertensive drugs pose bioavailability issues as they belong to BCS class II and BCS class IV categories with poor solubility profile and rate limiting dissolution. Emerging drug delivery technologies like nanoemulsion are found to be promising and safer alternatives for the delivery of anti-hypertensive drugs. Nanoemulsion gained more attention due to favourable properties such as small size, good physical stability, rapid action, drug targeting, prevents photo-degradation, and improved bioavailability. This chapter highlights various aspects of hypertension including its pathophysiology and potential approaches to combat high blood pressure. In addition, the authors thoroughly discussed nanoemulsions and their utility in the oral delivery of anti-hypertensive drugs.

PEDIATRICS ◽  
1983 ◽  
Vol 72 (4) ◽  
pp. 500-502
Author(s):  
Pablo Yagupsky ◽  
Rafael Gorodischer

The antihypertensive drug clonidine has a double and antagonistic effect on arterial blood pressure. As a result of activation of peripheral α-adrenergic receptors, it causes a transient increase in blood pressure; by a central action it decreases sympathetic tone which results in sustained bradycardia and hypotension. Both central and peripheral effects are experimentally blocked by tolazoline, an α-adrenergic blocking agent. The toxic symptoms seen in clonidine poisoning are usually produced by the central effect. A case of severe clonidine poisoning in a 9-month-old infant is reported. The clinical picture included coma, miosis, apneic spells, bradycardia, and hypertension. Rapid and complete recovery was obtained with supportive treatment that included assisted ventilation. No adrenergic blockers or antihypertensive drugs were given. Use of tolazoline in cases of clonidine overdose in children remains controversial. Supportive measures alone may be adequate for even the most severe cases.


2021 ◽  
Vol 9 (8) ◽  
pp. 1748-1753
Author(s):  
Anshika Rao

Hypertension (HTN) is a major public health issue worldwide, because of its high prevalence and concomitant increase in the risk of disease. In the contemporary situation Hypertension is the most critical disease in the world. If we focus on the present situation then we can see that due to rapid globalization we are facing Hypertension. Due to rapid modernization, people are leading more stressful lives. As a result, hypertension is one of the wide- spread disorders which came across in practice. Ab. India is labelled as the global capital of hypertension. Nowa- days, not only lifestyle disorders are becoming more common, but they are also affecting younger populations. Hence, the population at risk shifts from 40+ to maybe 30+ or even younger. Hypertension results from a variety of reasons like stress, obesity, genetic factors, overuse of the salts in the diet and ageing etc. As we all know, Hy- pertension is called a silent killer because it rarely exhibits symptoms before it damages the heart, brain or kidney. Though a lot of potent antihypertensive drugs are available today in modern medicine, none of them is free from untoward effects. The principal focus of Ayurveda is on maintaining good health and adopting a healthy way of life. In Ayurveda, there is no description of such a single disease that can resemble hypertension. As per Ayurve- dic principles, in case of an unknown disease, the physician should try to understand the nature of the disease through Dosha, Dushya and Samprapti; then should initiate the treatment. So, it becomes our prime concern to understand hypertension thoroughly with an Ayurvedic perspective. Hypertension (HTN or HT), also known as High blood pressure or arterial hypertension, is a chronic medical condition in which the blood pressure in the arteries is persistently elevated. Hypertension is one of the major causes of cardiovascular morbidity and mortalityworldwide. It is a global health problem affecting people of different ethnicity and ages around the world. It is an asymptomatic medical condition in which systemic arterial blood pressure is elevated beyond the normal value. Keywords: High Blood Pressure, Lifestyle disorders, Silent killer.


2005 ◽  
Vol 288 (2) ◽  
pp. H737-H743 ◽  
Author(s):  
Kevin D. Monahan ◽  
Chester A. Ray

Animal studies suggest that prostanoids (i.e., such as prostacyclin) may sensitize or impair baroreceptor and/or baroreflex responsiveness depending on the site of administration and/or inhibition. We tested the hypothesis that acute inhibition of cyclooxygenase (COX), the rate-limiting enzyme in prostanoid synthesis, impairs baroreflex regulation of cardiac period (R-R interval) and muscle sympathetic nerve activity (MSNA) in humans and augments pressor reactivity. Baroreflex sensitivity (BRS) was determined at baseline (preinfusion) and 60 min after (postinfusion) intravenous infusion of a COX antagonist (ketorolac; 45 mg) (24 ± 1 yr; n = 12) or saline (25 ± 1 yr; n = 12). BRS was assessed by using the modified Oxford technique (bolus intravenous infusion of nitroprusside followed by phenylephrine). BRS was quantified as the slope of the linear portion of the 1) R-R interval-systolic blood pressure relation (cardiovagal BRS) and 2) MSNA-diastolic blood pressure relation (sympathetic BRS) during pharmacological changes in arterial blood pressure. Ketorolac did not alter cardiovagal (19.4 ± 2.1 vs. 18.4 ± 2.4 ms/mmHg preinfusion and postinfusion, respectively) or sympathetic BRS (−2.9 ± 0.7 vs. −2.6 ± 0.4 arbitrary units·beat−1·mmHg−1) but significantly decreased a plasma biomarker of prostanoid generation (plasma thromboxane B2) by 53 ± 11%. Cardiovagal BRS (21.3 ± 3.8 vs. 21.2 ± 3.0 ms/mmHg), sympathetic BRS (−3.4 ± 0.3 vs. −3.2 ± 0.2 arbitrary units·beat−1·mmHg−1), and thromboxane B2 (change in −1 ± 12%) were unchanged in the control (saline infusion) group. Pressor responses to steady-state incremental (0.5, 1.0, and 1.5 μg·kg−1·min−1) infusion (5 min/dose) of phenylephrine were not altered by ketorolac ( n = 8). Collectively, these data indicate that acute pharmacological antagonism of the COX enzyme does not impair BRS (cardiovagal or sympathetic) or augment pressor reactivity in healthy young adults.


1994 ◽  
Vol 14 (3_suppl) ◽  
pp. 110-116 ◽  
Author(s):  
Amedeo F. De Vecchi

Hypotension and orthostatic hypotension are frequently observed in CAPD patients. In the present paper the possible causes of these complications were reviewed, and the roles of sodium and water were pointed out. In addition, we reported our experience using different sodium concentrations in CAPD dialysis fluid. In 38 CAPD patients sodium concentration in the dialysate was changed from 132 to 137 mEq/L. At first, arterial blood pressure increased in 4 patients (10%), and they were switched to 132 mEq/L sodium. Of the other 34 patients, 3 required larger doses of antihypertensive agents, while 9 reduced the number and/or dose of antihypertensive drugs. Thirst, body weight, residual renal function, 24-hour ultrafiltration, and biochemical examinations did not change using 137 mEq/L sodium concentrations for 6 months. In the 21 patients who did not change their antihypertensive treatment, upright blood pressure tended to increase, but the difference was not statistically significant. In 3 hypotensive patients sodium concentration was increased to 142 mEq/L. Thirst increased in 2 of the 3, one observed a transient increase in 24-hour ultrafiltration, and none showed changes in plasma sodium level. One patient developed reversible hypertension, one became normotensive, and the third had no changes in blood pressure.


2020 ◽  
Vol 26 (1) ◽  
pp. 10-34
Author(s):  
Aleksandra Cherneva ◽  
Ivo Petrov

Treatment-resistant hypertension, or resistant hypertension (RH), is defined as arterial hypertension (AH) despite treatment with three properly dosed antihypertensive drugs, at least one of which is a diuretic. Resistant hypertension is associated with an increased incidence of adverse cardiovascular events, renal impairment, and increased mortality. The main treatment of patients with RH is based on maximizing doses of antihypertensive drugs from different groups and adding drugs with complementary mechanisms of action. Despite the combination treatment involving multiple antihypertensive drugs, a small but significant group of patients remains with uncontrolled hypertension, emphasizing the need to find and put into practice new therapies to lower high arterial blood pressure (BP). Among these new methods of treatment, the most promising is the renal sympathetic denervation, showing positive results with the second generation devices. This review summarizes current knowledge about the treatment of RH, with an emphasis on new therapeutic strategies to achieve optimal blood pressure control.


Author(s):  
Jaykrushna Jani ◽  
Sweety Ruparel ◽  
Hetal Ramani ◽  
Halli Chandrakanth

Hypertension is the most prevalent cardiovascular disorder in the India. Depending on the criteria for the diagnosis, hypertension can be said to be present in 40-45 millions of the adult population. The latest developments in pharmacology has blessed the human community with certain antihypertensive drugs to suppress the elevated arterial blood pressure; at the same time it is proved that all of the used for it only symptomatic, have sufficient adverse effect and will not cure the disease. So it is need to find out effective medicine for essential HTN. In Ayurveda there is no description of such a single disease which can resemble with HTN. As per Ayurvedic principles, in case of unknown disease, the physician should try to understand the nature of the disease through Dosha, Dushya and Samprapti; then should initiate the treatment .This clinical trial was conducted on 20 patients of Essential Hypertension (HTN) to compare the effect of Virechanyoga and Rasayanyoga in the management of Essential HTN. Duration of treatment was 4 weeks. Both the groups showed highly significant results. But Rasayanyoga was found to be more effective.


2020 ◽  
pp. 30-40
Author(s):  
M. G. Melnik

Purpose. To study the dynamics of blood pressure (BP) indicators under the influence of exogenously administered melatonin (Melatonin-SZ, Severnaya Zvezda, Russia) with various manifestations of desynchronosis of circadian BP rhythms (arterial hypertension – AH, high normal blood pressure) to determine the scheme of their effective compensation. Material and methods. The study included 101 patients with desynchronosis of circadian rhythms of blood pressure – 52 patients with hypertension, constituting the first and second groups, and 49 individuals with high normal blood pressure, representing the third and fourth groups. Patients of the second and fourth groups received conservative therapy, patients of the first and third groups combined it with melatonin. All patients underwent measurements of office blood pressure, home monitoring of blood pressure (ABPM), electrocardiography, 24-hour blood pressure monitoring (ABPM). Results and discussion. In patients of the first and third groups, compared with the traditional treatment groups, by the end of the observation period, a significantly (p < 0.05) decrease in office systolic blood pressure (SBP) / diastolic blood pressure (DBP) was established: in the first group compared with the second – 1.11 / 1.13 times, in the third group compared to the fourth – 1.43 / 1.58 times; significantly more (p < 0.05) pronounced decrease in SBP / DBP during DMAD – by 1.08 / 1.17 and 1.58 / 1.62 times, respectively, Significantly (p < 0.05) more pronounced decrease in average daily, average daily and average nighttime SBP / DBP during ABPM – by 1.13 / 1.20, 1.11 / 1.20, 1.23 / 1.25 and 1.47 / 1.31, 1.42 / 1.19, 1.54 / 1.41 times, respectively; reliably (p < 0.05) more frequent registration of the dipper rhythm type SBP / DBP – 1.6 / 1.4 and 1.6 / 1.4 times, respectively. In addition, the dynamics of patients in the first and third groups showed a significant (p < 0.05) decrease in the mean daily and mean nighttime SBP / DBP variability (SBP in the first group by 27.3 and 41.3 %, respectively; DBP in the first group by 20.1 and 26.3 %, respectively; SBP in the third group by 13.5 and 25.2 %, respectively; DBP in the third group by 12.2 and 28.2 %, respectively). Conclusions. With various manifestations of desynchronosis of circadian rhythms of blood pressure (AH, high normal blood pressure), the prescription of melatonin (Melatonin-SZ, Severnaya Zvezda, Russia) at a dose of 3 mg per day 30–40 minutes before bedtime for a month against the background of non-drug therapy and antihypertensive drugs led to a significantly more effective decrease in blood pressure at its office measurement, DMAD, ABPM with an improvement in the circadian rhythm of blood pressure and normalization of blood pressure variability.


2017 ◽  
Vol 2 (2) ◽  
pp. 34
Author(s):  
TA Popova ◽  
II Prokofiev ◽  
IS Mokrousov ◽  
Valentina Perfilova ◽  
AV Borisov ◽  
...  

Introduction: To study the effects of glufimet, a new derivative of glutamic acid, and phenibut, a derivative of γ-aminobutyric acid (GABA), on cardiac and cerebral mitochondria and endothelial functions in animals following exposure to stress and inducible nitric oxide synthase (iNOS) inhibition. Methods: Rats suspended by their dorsal cervical skin fold for 24 hours served as the immobilization and pain stress model. Arterial blood pressure was determined using a non-invasive blood pressure monitor. Mitochondrial fraction of heart and brain homogenates were isolated by differential centrifugation and analysed for mitochondrial respiration intensity, lipid peroxidation (LPO) and antioxidant enzyme activity using polarographic method. The concentrations of nitric oxide (NO) terminal metabolites were measured using Griess reagent. Hemostasis indices were evaluated. Platelet aggregation was estimated using modified version of the Born method described by Gabbasov et al., 1989. Results: The present study demonstrated that stress leads to an elevated concentration of NO terminal metabolites and LPO products, decreased activity of antioxidant enzymes, reduced mitochondrial respiratory function, and endothelial dysfunction. Inhibition of iNOS by aminoguanidine had a protective effect. Phenibut and glufimet inhibited a rise in stress-induced nitric oxide production. This resulted in enhanced coupling of substrate peroxidation and ATP synthesis. The reduced LPO processes caused by glufimet and phenibut normalized the endothelial function which was proved by the absence of average daily blood pressure (BP) elevation episodes and a significant increase in platelet aggregation level. Conclusion: Glufimet and phenibut restrict the harmful effects of stress on the heart and brain possibly by modulating iNOS activity.


Sign in / Sign up

Export Citation Format

Share Document