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BMC Pharmacology & Toxicology Jul 2022The combination of lisinopril and amlodipine has a marked additional effect on blood pressure and fewer side effects than individual monotherapy. This study was... (Randomized Controlled Trial)
Randomized Controlled Trial
PURPOSE
The combination of lisinopril and amlodipine has a marked additional effect on blood pressure and fewer side effects than individual monotherapy. This study was conducted to compare the pharmacokinetic parameters and evaluate the bioequivalence between two Lisinopril/amlodipine tablets in healthy Chinese subjects.
METHODS
A single center, randomized, open-label, single-dose, two-period crossover bioequivalence study was designed in healthy Chinese subjects under both fasting and fed conditions. Blood samples were collected before drug administration and at 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 24, 36, 48, 72, 96, 144, 168 h after administration. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) was applied to determine the plasma concentration of lisinopril and amlodipine. Maximum concentration (C) and area under the concentration-time curve (AUC) were used to evaluate bioequivalence. Adverse events were recorded.
RESULTS
Ninety-two healthy subjects were enrolled, and 75 completed the study. The 90% confidence intervals (CIs) of the ratio of geometric means (GMRs) of C, AUC and AUC of lisinopril and amlodipine under both fasting and fed conditions fell within the conventional bioequivalence criteria of 0.80-1.25. A high-fat meal appeared to decrease the C and AUC of lisinopril. No severe adverse events were observed.
CONCLUSION
The trial demonstrated that the test and the reference lisinopril/amlodipine tablets were bioequivalent and well tolerated in Chinese people under fasting and fed conditions.
TRIAL REGISTRATION
Clinical Trails.gov identifier, NCT04885660 (retrospectively registered in 13/05/ 2021).
Topics: Amlodipine; China; Chromatography, Liquid; Fasting; Healthy Volunteers; Humans; Lisinopril; Tablets; Tandem Mass Spectrometry; Therapeutic Equivalency
PubMed: 35794660
DOI: 10.1186/s40360-022-00590-6 -
Disease Markers 2022This study was to study the efficacy of rosuvastatin, amlodipine, and aspirin in the treatment of hypertension with coronary heart disease and its effect on platelet... (Randomized Controlled Trial)
Randomized Controlled Trial
OBJECTIVE
This study was to study the efficacy of rosuvastatin, amlodipine, and aspirin in the treatment of hypertension with coronary heart disease and its effect on platelet aggregation.
METHODS
The participants included 60 patients with hypertension and coronary heart disease who were treated at our hospital between January 2020 and May 2021 and were randomly assigned to receive either rosuvastatin, amlodipine, and Ziyin Huoxue Recipe (observation group) or rosuvastatin, amlodipine, Ziyin Huoxue Recipe, and aspirin (experimental group), with 30 patients in each. Outcome measures included clinical effectiveness, blood pressure indicators, blood lipid indices, plasma viscosity, platelet aggregation, cardiac function, and adverse responses.
RESULTS
The clinical efficacy in the experimental group was significantly higher than that in the observation group ( < 0.05). The differences were found in blood pressure indices and blood lipid indices between the two groups before treatment ( > 0.05). However, after treatment, the blood pressure indices in the experimental group were significantly lower than those in the observation group ( < 0.05). After treatment, the blood lipid indices, plasma viscosity, and platelet aggregation in the experimental group were significantly lower than those in the observation group ( < 0.05). The left ventricular ejection fraction (LVEF) of patients in the experimental group after treatment was significantly higher than that of patients in the observation group ( < 0.05). There was no significant difference in the incidence of adverse reactions among patients in the two groups ( > 0.05).
CONCLUSION
The clinical efficacy of rosuvastatin, amlodipine, and aspirin markedly reduces the blood pressure indices, blood lipid indices, plasma viscosity, and platelet aggregation of patients with hypertension and coronary heart disease, improves LVEF, and has a good safety profile.
Topics: Humans; Amlodipine; Rosuvastatin Calcium; Antihypertensive Agents; Platelet Aggregation; Aspirin; Stroke Volume; Ventricular Function, Left; Hypertension; Coronary Disease; Lipids; Treatment Outcome
PubMed: 36284992
DOI: 10.1155/2022/1111438 -
JACC. Heart Failure Aug 2013
Topics: Amlodipine; Calcium Channel Blockers; Female; Heart Failure; Humans; Male
PubMed: 24621934
DOI: 10.1016/j.jchf.2013.05.005 -
PeerJ 2023Sporotrichosis caused by is a globally emerging infectious disease with limited therapeutic options. Thus, we aimed to evaluate the activity of amlodipine (AML) and...
BACKGROUND
Sporotrichosis caused by is a globally emerging infectious disease with limited therapeutic options. Thus, we aimed to evaluate the activity of amlodipine (AML) and lufenuron (LUF) alone and their interaction with itraconazole (ITZ), the first-choice drug against .
METHODS
Twenty clinical isolates of from two hyperendemic regions were tested through a microdilution assay to evaluate the minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) of AML and LUF. Checkerboard assay was performed with 10 isolates for both drug interactions with ITZ.
RESULTS
AML showed inhibitory and fungicidal activity against all isolates included, with MIC values ranging from 32 to 256 µg/mL, and MFC from 64 to 256 µg/mL. However, none of the isolates were inhibited by the highest soluble concentration of LUF (MIC >64 µg/mL for all strains). Synergic interaction of AML and LUF with ITZ occurred in 50% and 40% of the isolates tested, without any antagonistic effects.
CONCLUSION
Both repurposing drugs evaluated in our study showed a promising activity, especially in synergy with ITZ against , warranting future investigations regarding its activity.
Topics: Humans; Antifungal Agents; Amlodipine; Drug Repositioning; Itraconazole; Leukemia, Myeloid, Acute
PubMed: 38050607
DOI: 10.7717/peerj.16443 -
Nutrients Aug 2021Curcumin, a curcuminoid known as the main bioactive compound of turmeric, is used in foods, cosmetics, and pharmaceutical products. Amlodipine is a general...
Curcumin, a curcuminoid known as the main bioactive compound of turmeric, is used in foods, cosmetics, and pharmaceutical products. Amlodipine is a general antihypertensive drug used in combination with various other antihypertensive agents. To date, no studies have examined the effects of the co-administration of amlodipine with curcumin. In this study, the vasodilatory effects of curcumin, amlodipine, and the co-administration of curcumin with amlodipine on isolated rat aortic rings pre-contracted with phenylephrine were evaluated, and the hypotensive effects were evaluated using the tail cuff method. To measure blood pressure, male spontaneously hypertensive rats were divided into four groups, each containing six rats, as follows: amlodipine 1 mg/kg alone treated, amlodipine 1 mg/kg with curcumin 30 mg/kg treated, amlodipine 1 mg/kg with curcumin 100 mg/kg treated, and amlodipine 1 mg/kg with curcumin 300 mg/kg treated groups. Amlodipine and curcumin were intraperitoneally injected, and systolic blood pressure (SBP) and diastolic blood pressure (DBP) were measured at 1, 2, 4, and 8 h after administration. The combined administration of curcumin and amlodipine induced a stronger vasorelaxant effect than amlodipine alone. However, co-administration did not significantly lower SBP and DBP compared to the single administration of amlodipine. The results of this study suggest that hypertensive patients taking amlodipine can consume curcumin or turmeric for food or other medical purposes without inhibiting the blood pressure-lowering effect of amlodipine.
Topics: Amlodipine; Animals; Antihypertensive Agents; Blood Pressure; Curcumin; Drug Therapy, Combination; Hypertension; Male; Rats; Rats, Inbred SHR; Vasodilator Agents
PubMed: 34444956
DOI: 10.3390/nu13082797 -
Journal of Medical Economics Mar 2009To review the pharmacoeconomic impact of the use of amlodipine in coronary artery disease (CAD) patients. (Review)
Review
OBJECTIVES
To review the pharmacoeconomic impact of the use of amlodipine in coronary artery disease (CAD) patients.
METHODS
A review of the available outcome trials evaluating the clinical effectiveness of amlodipine in hypertensive patients or in patients with CAD or diabetic nephropathy was carried out to identify pharmacoeconomic studies that quantified the economic impact of using amlodipine instead of another treatment.
RESULTS
A combined analysis of two trials comparing angiotensin receptor blockers (ARBs) with a calcium channel blocker amlodipine suggested that amlodipine provided more protection against stroke and myocardial infarction than ARBs. In addition, in keeping with previous meta-analyses, calcium channel blockade with amlodipine also prevented more stroke than angiotensin-converting enzyme inhibitors and old drug classes. Pharmacoeconomic analysis conducted in the US and Europe demonstrated that the use of amlodipine resulted in fewer hospitalisations and the need for fewer invasive surgical procedures in the short and long term and at a modest incremental cost. The use of amlodipine resulted in improved clinical outcomes as well as slight savings in cost.
CONCLUSIONS
Amlodipine is not only cost effective, but predicted to be cost saving when compared with usual care, warranting its consideration as an agent of choice in patients with CAD.
Topics: Amlodipine; Antihypertensive Agents; Coronary Artery Disease; Economics, Pharmaceutical; Humans
PubMed: 19450066
DOI: 10.3111/13696990802525266 -
Open Heart Jan 2023Coronary artery vasospasm is an abnormal spasm of coronary arteries that cause transient or complete occlusion without exertion. It causes stable angina to ACS. However,...
BACKGROUND
Coronary artery vasospasm is an abnormal spasm of coronary arteries that cause transient or complete occlusion without exertion. It causes stable angina to ACS. However, this can be prevented by calcium channel blockers (CCBs) which suppress Ca influx into the vascular muscle cells. Nevertheless, several CCBs adverse effects are harmful for these patients. Selecting the right CCBs would give the best clinical practice.
METHOD
The studies were obtained from four major medical databases by various keywords. Inclusion and exclusion criteria were implemented as adult >18 years, observational study, English language and drug of interest. Duplicates were eliminated, and the remaining studies were reviewed. Final full-texts assessment was conducted independently by Newcastle-Ottawa Scale and Revised Cochrane.
RESULTS
The search found 1378 articles. However, six studies were selected after implementing the study criteria. Diltiazem was found to decrease angina and increase quality of life until 12th week of treatment; however, some adverse effects include atrioventricular block and recurrent angina up till 4th week were found. Meanwhile, nifedipine was found to decrease vasospastic angina (VSA) by the fourth and eighth weeks of treatment. Nevertheless, it caused excessive drop in BP and increase heart rate by eighth week. In addition, slow-release preparation of both CCBs were found to increase efficacy and compliance. Lastly amlodipine was also found to decrease VSA by 17%±140% and 33% after 6 weeks, but further studies needed.
CONCLUSION
Diltiazem, nifedipine and amlodipine are potent in decreasing VSA, however, tailoring specific CCBs adverse reactions to patient condition and the drug preparation would be substantially beneficial for the outcome.
Topics: Adult; Humans; Calcium Channel Blockers; Diltiazem; Coronary Vasospasm; Nifedipine; Calcium; Quality of Life; Amlodipine; Observational Studies as Topic
PubMed: 36634997
DOI: 10.1136/openhrt-2022-002179 -
Pharmaceutical Biology Dec 2020Hyperlipidaemia and hypertension are often treated together with curcumin and amlodipine. It is necessary to investigate the drug-drug interaction between curcumin and...
Hyperlipidaemia and hypertension are often treated together with curcumin and amlodipine. It is necessary to investigate the drug-drug interaction between curcumin and amlodipine. The interaction between curcumin and amlodipine was investigated in rats and with rat liver microsomes. The pharmacokinetics of amlodipine (1 mg/kg) was investigated in rats with or without curcumin pre-treatment (2 mg/kg), six rats in each group. The metabolic stability of amlodipine was investigated with rat liver microsomes. Curcumin significantly increased the (26.19 ± 2.21 versus 17.80 ± 1.56 μg/L), (507.27 ± 60.23 versus 238.68 ± 45.59 μg·h/L), and (14.69 ± 1.64 versus 11.43 ± 1.20 h) of amlodipine ( < 0.05). The metabolic stability of amlodipine was significantly increased with the half-life time in rat liver microsomes increased from 34.23 ± 3.33 to 44.15 ± 4.12 min, and the intrinsic rate decreased from 40.49 ± 3.26 to 31.39 ± 2.78 μL/min/mg protein. These results indicated that drug-drug interaction might appear during the co-administration of curcumin and amlodipine. The potential mechanism may be due to the inhibition of CYP3A4 by curcumin. Thus, this interaction should be given special attention in the clinic and needs further experiments to characterize the effect in humans.
Topics: Amlodipine; Animals; Curcumin; Drug Interactions; Male; Microsomes, Liver; Rats; Rats, Sprague-Dawley
PubMed: 32432949
DOI: 10.1080/13880209.2020.1764060 -
Actas Dermo-sifiliograficas 2017
Topics: Adult; Amlodipine; Antihypertensive Agents; Diagnosis, Differential; Facial Dermatoses; Female; Humans; Hypertension; Photosensitivity Disorders; Sunlight; Telangiectasis; Thorax; Vasodilator Agents
PubMed: 27590135
DOI: 10.1016/j.ad.2016.07.015 -
Genes Aug 2022Objective: This study describes the single nucleotide polymorphisms (SNPs) in amlodipine-associated genes and assesses their correlation with blood pressure control...
Objective: This study describes the single nucleotide polymorphisms (SNPs) in amlodipine-associated genes and assesses their correlation with blood pressure control among South African adults with hypertension. Methods: In total, 304 hypertensive patients on amlodipine treatment belonging to the indigenous Swati, Xhosa and Zulu population groups of South Africa were recruited between June 2017 and June 2019. Participants were categorized into: controlled (blood pressure < 140/90 mmHg) and uncontrolled (blood pressure ≥ 140/90 mmHg) hypertension. Thirteen SNPs in amlodipine pharmacogenes with a high PharmGKB evidence base were selected and genotyped using MassArray (Agena BioscienceTM). Logistic regression was fitted to identify significant associations between the SNPs and blood pressure control with amlodipine. Results: The majority of the participants were females (76.6%), older than 45 years (89.1%) and had uncontrolled hypertension (52.3%). Of the 13 SNPs genotyped, five SNPs, rs1042713 (minor allele frequency = 45.9%), rs10494366 (minor allele frequency = 35.3%), rs2239050 (minor allele frequency = 28.7%), rs2246709 (minor allele frequency = 51.6%) and rs4291 (minor allele frequency = 34.4%), were detected among the Xhosa participants, while none were detected among the Swati and Zulu tribal groups. Variants rs1042713 and rs10494366 demonstrated an expression frequency of 97.5% and 79.5%, respectively. Variant TA genotype of rs4291 was significantly associated with uncontrolled hypertension. No association was established between blood pressure response to amlodipine and the remaining four SNPs. Conclusions: This study reports the discovery of five SNPs in amlodipine genes (rs2239050, rs2246709, rs4291, rs1042713 and rs10494366) among the indigenous Xhosa-speaking tribe of South Africa. In addition, the TA genotype of rs4291 was associated with blood pressure control in this cohort. These findings might open doors for more pharmacogenomic studies, which could inform innovations to personalised anti-hypertensive treatment in the ethnically diverse population of South Africa.
Topics: Adult; Amlodipine; Blood Pressure; Female; Humans; Hypertension; Male; Polymorphism, Single Nucleotide; South Africa
PubMed: 36011305
DOI: 10.3390/genes13081394