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Marine Polysaccharides in Pharmaceutical Applications
Published in Se-Kwon Kim, Marine Biochemistry, 2023
Riyasree Paul, Sourav Kabiraj, Sreejan Manna, Sougata Jana
Niaz et al. have investigated the efficacy of alginate- and chitosan-based nanocarriers loaded with commonly used antihypertensive drugs, i.e. amlodipine, captopril and valsartan. The NPs showed better stability and high drug loading capacity. The in vitro drug release study indicated excellent retention of the incorporated antihypertensive drugs in hybrid NPs. The study findings demonstrated <8% of drug release in the initial 24 hours (Niaz et al. 2016). Alginate-, chitosan- and carrageenan-based matrix tablets were developed by Tapia et al. for delivering diltiazem hydrochloride. The alginate and chitosan based tablets exhibited a slow erosion of the matrix. The drug release mechanisms were reported to be a combination of diffusion and polymeric relaxation. The alginate chitosan matrix exhibited ability for solvent uptake without disruption of the microstructure (Tapia et al. 2005). Alginate-based mucoadhesive floating beads were developed using the ionic gelation technique for delivering metoprolol tartrate. The study findings suggested the incorporation of tapioca starch has enhanced the efficacy and sustained-release behavior of metoprolol tartrate. Hydroxypropyl methylcellulose (HPMC) coating on developed beads has extended the metoprolol tartrate release up to 11 hours. Pharmacokinetic analysis involving rabbit model indicated relatively higher oral bioavailability for floating beads (Biswas and Sahoo 2016).
Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
A group of 28 patients was treated with metoprolol eye drops 1% 3-4 times daily or metoprolol 3% or 4% two to three times a day for glaucoma. The mean duration of treatment was 3.8 months (range 0.5 to 6 months). Eleven of the twenty-eight patients (39%) developed ocular (conjunctival edema and/or hyperemia) and/or periocular adverse reactions (dermatitis) with subjective symptoms such as itching, burning and smarting 2 weeks to 5 months after beginning of treatment. The clinical symptoms disappeared 2-6 weeks after treatment was stopped. Patch tests were performed with metoprolol tartrate 3% in water and there were 5 positive reactions. Repeated patch tests after 3-6 months were again positive, albeit weaker. ‘A group’ of controls was negative (4).
Adrenergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
It is an adrenergic β1 selective receptor antagonist without having ISA and MSA (Brunton et al., 2011; Florey, 2008). It is employed in the treatment of essential hypertension, tachycardia, heart failure, angina pectoris, vasovagal syncope, secondarily in the prevention of myocardial infarction, migraine treatment, and hyperthyroidism. It can be administered orally and used intravenously as metoprolol tartrate. It is helpful in chronic heart failure. After an oral dose, the drug has 40% bioavail-ability because of first-pass effect. Extensive metabolism occurs in the liver by the enzyme CYP2D6. The drug excretion takes place via the urine after biotransformation and 85% drug excreted are metabolites. The drug has a half-life of about 4 h (Brunton et al., 2011; Florey, 2008).
Effects of garden cress, fenugreek and black seed on the pharmacodynamics of metoprolol: an herb-drug interaction study in rats with hypertension
Published in Pharmaceutical Biology, 2021
Yousef A. Bin Jardan, Abdul Ahad, Mohammad Raish, Mohd Aftab Alam, Abdullah M. Al-Mohizea, Fahad I. Al-Jenoobi
In this study, we used L-NAME-induced hypertension models to investigate the antihypertensive effects of three commonly used herbs, namely, garden cress (GC), fenugreek (FG), and black seed (BS); for this purpose, L-NAME was orally administered in rats, which induced a substantial increase in blood pressure. The outcomes of this study showed that metoprolol tartrate (MT) alone, herbs alone, and their combination showed a decrease in systolic blood pressure (SBP), diastolic blood pressure (DBP), and mean arterial pressure (MAP) in hypertensive rats. Heart rate (HR), which was depleted following treatment with L-NAME alone, improved following treatment with MT alone, herbs alone, and herbs + MT. A more potent blood pressure-lowering effect of MT was observed when administered in combination with herbs. Furthermore, the concurrent administration of drugs, particularly those predominantly cleared through CYP2D-catalyzed metabolism, with the three herbs under study should be considered with caution.
Development of metoprolol tartrate-loaded sustained-release pellets: effect of talc on the mechanism of drug release
Published in Pharmaceutical Development and Technology, 2018
Yuli Wang, Meiyan Yang, Ruifang Shen, Shuai Shao, Lu Chen, Wei Gong, Li Shan, Chunsheng Gao
Metoprolol tartrate (MT), a highly water-soluble drug (above 70% w/v), has been widely used in the treatment of hypertension, angina pectoris and arrhythmias. Because of its good absorption in the entire gastrointestinal tract5, rapid elimination (the half-life of 3–4 h)6 and a well-defined relationship between the beta-blocking effect and plasma drug concentration7, MT is a suitable candidate for oral SR administrations. There have been several approaches to the design of SR delivery systems for MT. For example, the slow release encapsulated tablet8, the extended-release matrix tablet9, the extended release hydrophilic gel-based swellable polyethylene oxide tablet1, the three-layer guar gum matrix tablet10, the bilayer floating tablet11, the prolonged release mini tablets coated with Eudragit NE 40 D12 and the reservoir pellets with plasticized isolated ethylcellulose/hydroxypropyl methylcellulose films13. Among these SR strategies, a pellet-based formulation can minimize the risk of dose dumping and because of its multiple-particulate nature, has the potential to improve the safety and efficacy of the active ingredient and thus has potential for use in the controlled release of the highly water-soluble MT in oral delivery14. When compared to matrix pellets, polymer-coated pellets are the most commonly applied formulation used to achieve a required and reproducible drug release rate over an extended period of time15.
Metoprolol in the treatment of cardiovascular disease: a critical reappraisal
Published in Current Medical Research and Opinion, 2018
Among different β-blockers, metoprolol is a selective β1-blocker, which has an insignificant membrane-stabilizing effect and does not display partial agonistic activity2. It was initially developed in the mid 1970s as metoprolol tartrate, a formulation characterized by an immediate release, with a pharmacokinetic/pharmacodynamic profile requiring multiple daily administrations. After 15 years, a new formulation, namely metoprolol succinate, was developed. This formulation is characterized by an extended release, allowing a single administration throughout a 24-h period. Table 1 displays current formulations of metoprolol and their indications.