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Macitentan
Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist developed by Actelion and approved for the treatment of pulmonary arterial hypertension (PAH). Macitentan is a dual endothelin receptor antagonist, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype. Macitentan was approved for medical use in the United States in October 2013. Macitentan is available as a generic medication. Adverse effects The FDA prescription label contains a boxed warning for embryo-fetal toxicity. It is only available to females in the US through a risk evaluation and mitigation strategy (REMS) program. Mechanism of action Endothelin and endothelin receptors Endothelin (ET) is an extremely potent blood vessel constricting substance that is secreted by endothelial cells. In the lungs, the most common ET form released is ET-1. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Endothelin Receptor Antagonist
An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors. Three main kinds of ERAs exist: * Dual ET Receptor Antagonists, which affect both endothelin A (ETA) and B receptors (ETB)CPU0213 21780-32-9is an example of a dual receptor endothelin receptor antagonist. ** aprocitentan, bosentan, macitentan, tezosentan, Feloprentan (LU-302872 the HCl salt is called LU-420627) 04267-33-4 * Selective ETA Receptor Antagonists, which affect endothelin A receptors ** sitaxentan, ambrisentan, atrasentan, BQ-123, sparsentan, zibotentan, avosentan, edonentan, clazosentan, Fandosentan * Selective ETB Receptor Antagonists, which affect endothelin B receptors ** BQ-788 and A192621 are used in research but have not yet reached clinical trial stage Macitentan, ambrisentan and bosentan are mainly used for the treatment of pulmonary arterial hypertension, while atrasentan is an experimental anti-cancer Cancer is a group of diseases involving C ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Endothelin
Endothelins are peptides with receptors and effects in many body organs. Endothelin constricts blood vessels and raises blood pressure. The endothelins are normally kept in balance by other mechanisms, but when overexpressed, they contribute to high blood pressure (hypertension), heart disease, and potentially other diseases. Endothelins are 21-amino acid vasoconstricting peptides produced primarily in the endothelium having a key role in vascular homeostasis. Endothelins are implicated in vascular diseases of several organ systems, including the heart, lungs, kidneys, and brain. As of 2018, endothelins remain under extensive basic and clinical research to define their roles in several organ systems. Etymology Endothelins derived the name from their isolation in cultured endothelial cells. Isoforms There are three isoforms of the peptide (identified as ET-1, 2, 3), each encoded by a separate gene, with varying regions of expression and binding to at least four known e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ciclosporin
Ciclosporin, also spelled cyclosporine and cyclosporin, is a calcineurin inhibitor, used as an immunosuppressant medication. It is taken Oral administration, orally or intravenously for rheumatoid arthritis, psoriasis, Crohn's disease, nephrotic syndrome, eczema, and in organ transplants to prevent transplant rejection, rejection. It is also used as eye drops for keratoconjunctivitis sicca (dry eyes). Common side effects include high blood pressure, headache, kidney problems, increased hair growth, and vomiting. Other severe side effects include an increased risk of infection, liver problems, and an increased risk of lymphoma. Blood levels of the medication should be checked to decrease the risk of side effects. Use during pregnancy may result in preterm birth; however, ciclosporin does not appear to cause birth defects. Ciclosporin is believed to work by decreasing the function of lymphocytes. It does this by forming a complex with cyclophilin to block the phosphatase act ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drugs Developed By Johnson & Johnson
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via inhalation, injection, smoking, ingestion, absorption via a patch on the skin, suppository, or dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to treat, cure, prevent, or diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a regular basis for chronic disorders. Classification Pharmaceutical drugs are often classified into drug classes—groups of related drugs that have simila ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pyrimidines
Pyrimidine (; ) is an aromatic, heterocyclic, organic compound similar to pyridine (). One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has nitrogen atoms at positions 1 and 3 in the ring. The other diazines are pyrazine (nitrogen atoms at the 1 and 4 positions) and pyridazine (nitrogen atoms at the 1 and 2 positions). In nucleic acids, three types of nucleobases are pyrimidine derivatives: cytosine (C), thymine (T), and uracil (U). Occurrence and history The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. It is also found in many synthetic compounds such as barbiturates and the HIV drug zidovudine. Although pyrimidine derivatives such as alloxan were known in the early 19th century, a laboratory synthesis of a pyrimidine was not carried out until 1879, when Grimaux reported the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aprocitentan
Aprocitentan, sold under the brand name Tryvio, is a medication used to treat hypertension (high blood pressure). It is developed by Idorsia. It is taken by mouth. Aprocitentan is a receptor antagonist that targets both endothelin A and endothelin B receptors. Aprocitentan was approved for medical use in the United States in March 2024. It is the first endothelin receptor antagonist to be approved by the US Food and Drug Administration (FDA) to treat systemic hypertension. The FDA considers it to be a first-in-class medication. Medical uses Aprocitentan is indicated for the treatment of hypertension in combination with other antihypertensive drugs, to lower blood pressure in adults who are not adequately controlled on other medications. Adverse effects Aprocitentan may cause hepatotoxicity (liver damage), edema (fluid retention), anemia (reduced hemoglobin), and decreased sperm count. Contraindications Data from animal reproductive toxicity studies with other endot ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketoconazole
Ketoconazole, sold under the brand name Nizoral, among others, is an antiandrogen, antifungal drug, antifungal, and antiglucocorticoid medication used to treat a number of fungal infections. Applied to the skin it is used for fungal skin infections such as tinea, cutaneous candidiasis, pityriasis versicolor, dandruff, and seborrhoeic dermatitis, seborrheic dermatitis. Taken oral administration, by mouth it is a less preferred option and recommended for only severe infections when other agents cannot be used. Other uses include treatment of hirsutism, excessive male-patterned hair growth in women and Cushing's syndrome. Common side effects when transdermal administration, applied to the skin include redness. Common side effects when taken by mouth include nausea, headache, and liver problems. Liver problems may result in death or the need for a liver transplantation. Other severe side effects when taken orally include QT prolongation, adrenocortical insufficiency, and anaphyl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Area Under The Curve
In mathematics, an integral is the continuous analog of a sum, which is used to calculate areas, volumes, and their generalizations. Integration, the process of computing an integral, is one of the two fundamental operations of calculus,Integral calculus is a very well established mathematical discipline for which there are many sources. See and , for example. the other being differentiation. Integration was initially used to solve problems in mathematics and physics, such as finding the area under a curve, or determining displacement from velocity. Usage of integration expanded to a wide variety of scientific fields thereafter. A definite integral computes the signed area of the region in the plane that is bounded by the graph of a given function between two points in the real line. Conventionally, areas above the horizontal axis of the plane are positive while areas below are negative. Integrals also refer to the concept of an ''antiderivative'', a function whose derivati ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
