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Velpatasvir Sofosbuvir
Velpatasvir is an NS5A inhibitor (by Gilead) which is used together with sofosbuvir in the treatment of hepatitis C infection of all six major genotypes. Side effects Side effects in studies occurred with similar frequencies as in people treated with placebo. Interactions Velpatasvir is both an inhibitor and a substrate of the transporter proteins P-glycoprotein (Pgp), ABCG2, OATP1B1 and OATP1B3. It is partly degraded by the liver enzymes CYP2B6, CYP2C8 and CYP3A4. Substances that are transported or inactivated by these proteins, or interfere with them, can interact with velpatasvir. In studies, this has been found for the HIV combination efavirenz/emtricitabine/tenofovir, which reduces the area under the curve (AUC) of velpatasvir by about 50%, and the CYP3A4 and Pgp inducer rifampicin, which reduces its AUC by about 80%, rendering it likely ineffective. Digoxin is eliminated by Pgp; its AUC is increased by about 30% in combination with velpatasvir and sofosbuvir (although i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Epclusa
Sofosbuvir/velpatasvir, sold under the brand name Epclusa among others, is a fixed-dose combination medication for the treatment of hepatitis C in adults. It combines sofosbuvir and velpatasvir. It is more than 90% effective for hepatitis C genotypes one through six. It also works for hepatitis C in those who also have cirrhosis or HIV/AIDS. It is taken by mouth. In March 2020, sofosbuvir/velpatasvir was approved for use in the United States to treat hepatitis C virus (HCV) in children ages six years and older or weighing at least 37 pounds (17 kilograms) with any of the six HCV genotypes—or strains—without cirrhosis (liver disease) or with mild cirrhosis. Sofosbuvir/velpatasvir in combination with ribavirin is indicated for the treatment of children six years and older or weighing at least 37 pounds with severe cirrhosis. The combination is generally well tolerated. Common side effects include headaches, fatigue, trouble sleeping, and nausea. The combination has not been ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
OATP1B1
Solute carrier organic anion transporter family member 1B1 is a protein that in humans is encoded by the ''SLCO1B1'' gene. Pharmacogenomic research indicates that genetic variations in this gene are associated with response to simvastatin. Clinical guidelines exist that can guide dosing of simvastatin based on SLCO1B1 gene variant using genotyping or whole exome sequencing In genetics and biochemistry, sequencing means to determine the primary structure (sometimes incorrectly called the primary sequence) of an unbranched biopolymer. Sequencing results in a symbolic linear depiction known as a sequence which succ .... See also * Solute carrier family References Further reading * * * * * * * * * * * * * * * * * * Solute carrier family {{membrane-protein-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Demethylated
Demethylation is the chemical process resulting in the removal of a methyl group (CH3) from a molecule. A common way of demethylation is the replacement of a methyl group by a hydrogen atom, resulting in a net loss of one carbon and two hydrogen atoms. The counterpart of demethylation is methylation. In biochemistry In biochemical systems, the process of demethylation is catalyzed by demethylases. These enzymes oxidize N-methyl groups, which occur in histones and some forms of DNA: :R2N-CH3 + O → R2N-H + CH2O One such oxidative enzyme family is the cytochrome P450. Alpha-ketoglutarate-dependent hydroxylases are active for demethylation of DNA, operating by a similar pathway. These reactions exploit the weak C-H bond adjacent to amines. In particular, 5-methylcytosines in DNA can be demethylated by TET enzymes as illustrated in the figure. TET enzymes are dioxygenases in the family of alpha-ketoglutarate-dependent hydroxylases. A TET enzyme is an alpha-ketoglut ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydroxylated
In chemistry, hydroxylation can refer to: *(i) most commonly, hydroxylation describes a chemistry, chemical process that introduces a hydroxyl group () into an organic compound. *(ii) the ''degree of hydroxylation'' refers to the number of OH groups in a molecule. The ''pattern of hydroxylation'' refers to the location of hydroxy groups on a molecule or material. Hydroxylation reactions Synthetic hydroxylations Installing hydroxyl groups into organic compounds can be effected by various metal catalysts. Many such catalysts are biomimetic, i.e. they are inspired by or intended to mimic enzymes such as cytochrome P450. Whereas many hydroxylations insert O atoms into bonds, some reactions ''add'' OH groups to unsaturated substrates. The Sharpless dihydroxylation is such a reaction: it converts alkenes into diols. The hydroxy groups are provided by hydrogen peroxide, which adds across the double bond of alkenes. Biological hydroxylation In biochemistry, hydroxylation reactions a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Plasma Protein Binding
Plasma protein binding refers to the degree to which medications attach to proteins within the blood. A drug's efficiency may be affected by the degree to which it binds. The less bound a drug is, the more efficiently it can traverse or diffuse through cell membranes. Common blood proteins that drugs bind to are human serum albumin, lipoprotein, glycoprotein, and α, β‚ and γ globulins. Binding (drug distribution) A drug in blood exists in two forms: bound and unbound. Depending on a specific drug's affinity for plasma proteins, a proportion of the drug may become bound to the proteins, with the remainder being unbound. If the protein binding is reversible, then a chemical equilibrium will exist between the bound and unbound states, such that: :Protein + drug ⇌ Protein-drug complex Notably, it is the unbound fraction which exhibits pharmacologic effects. It is also the fraction that may be metabolized and/or excreted. For example, the "fraction bound" of the anticoagulant ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Virus Replication
Viral replication is the formation of biological viruses during the infection process in the target host cells. Viruses must first get into the cell before viral replication can occur. Through the generation of abundant copies of its genome and packaging these copies, the virus continues infecting new hosts. Replication between viruses is greatly varied and depends on the type of genes involved in them. Most DNA viruses assemble in the nucleus while most RNA viruses develop solely in cytoplasm. Viral production / replication Viruses multiply only in living cells. The Host (biology), host cell must provide the energy and synthetic machinery and the low- molecular-weight precursors for the synthesis of viral proteins and nucleic acids. The virus replication occurs in seven stages, namely; # Attachment # Entry, # Uncoating, # Transcription (genetics), Transcription / mRNA production, # Synthesis of virus components, # Virion assembly and # Release (Liberation Stage). Attachment ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NS5A
Nonstructural protein 5A (NS5A) is a zinc-binding and proline-rich hydrophilic phosphoprotein that plays a key role in Hepatitis C virus RNA replication. It appears to be a dimeric form without ''trans''-membrane helices. Structure NS5A is derived from a large polyprotein that is translated from the HCV genome, and undergoes post-translation processing by nonstructural protein 3 (NS3) viral protease. Despite no inherent enzymatic activity being attributed to NS5A, its function is mediated through interaction with other nonstructural (NS) viral and cellular proteins. NS5A has two phosphorylated forms: p56 and p58, which differ in the electrophoretic mobility. p56 is basally phosphorylated by host cellular protein kinase at the center and near the C terminus, whereas p58 is a form of hyper-phosphorylated NS5A at the center of the serine-rich region. Protein mass spectrometry identified several phosphorylated serine residues in this region including serine 225, 229, 232, and 235 res ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Proton Pump Inhibitor
Proton-pump inhibitors (PPIs) are a class of medications that cause a profound and prolonged reduction of stomach acid production. They do so by irreversibly inhibiting the stomach's H+/K+ ATPase proton pump. They are the most potent inhibitors of acid secretion available. Proton-pump inhibitors have largely superseded the H2-receptor antagonists, a group of medications with similar effects but a different mode of action, and antacids. PPIs are among the most widely sold medications in the world. The class of proton-pump inhibitor medications is on the World Health Organization's List of Essential Medicines. Omeprazole is the specific listed example. Medical uses These medications are used in the treatment of many conditions, such as: * Dyspepsia * Peptic ulcer disease including after endoscopic treatment for bleeding * As part of ''Helicobacter pylori'' eradication therapy * Gastroesophageal reflux disease (GERD or GORD) including symptomatic endoscopy-negative reflux disea ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
H2 Antagonist
H2 antagonists, sometimes referred to as H2RAs and also called H2 blockers, are a class of pharmaceutical drug, medications that block the action of histamine at the histamine H2 receptor, histamine H2 receptors of the parietal cells in the stomach. This decreases the production of gastric acid, stomach acid. H2 antagonists can be used in the treatment of dyspepsia, peptic ulcers and gastroesophageal reflux disease. They have been surpassed by proton pump inhibitors (PPIs); the PPI omeprazole was found to be more effective at both healing and alleviating symptoms of ulcers and reflux oesophagitis than the H2 blockers ranitidine and cimetidine. H2 antagonists are a type of antihistamine, although in common use the term "antihistamine" is often reserved for H1 antagonist, H1 antagonists, which relieve Allergy, allergic reactions. Like the H1 antagonists, some H2 antagonists function as inverse agonists rather than receptor antagonists, due to the constitutive activity of these re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antacid
An antacid is a substance which neutralizes stomach acidity and is used to relieve heartburn, indigestion or an upset stomach. Some antacids have been used in the treatment of constipation and diarrhea. Marketed antacids contain salts of aluminum, calcium, magnesium, or sodium. Some preparations contain a combination of two salts, such as magnesium carbonate and aluminium hydroxide (e.g. hydrotalcite). Medical uses Antacids are available over the counter and are taken by mouth to quickly relieve occasional heartburn, the major symptom of gastroesophageal reflux disease and indigestion. Treatment with antacids alone is symptomatic and only justified for minor symptoms.U.S. Department of Health & Human Services. Agency for Healthcare Research and Quality 23 September 201Consumer Summary – Treatment Options for GERD or Acid Reflux Disease: A Review of the Research for Adults Alternative uses for antacids include constipation, diarrhea, hyperphosphatemia, and urinary alkalizatio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Digoxin
Digoxin (better known as Digitalis), sold under the brand name Lanoxin among others, is a medication used to treat various heart conditions. Most frequently it is used for atrial fibrillation, atrial flutter, and heart failure. Digoxin is one of the oldest medications used in the field of cardiology. It works by increasing myocardial contractility, increasing stroke volume and blood pressure, reducing heart rate, and somewhat extending the time frame of the contraction. Digoxin is taken by mouth or by injection into a vein. Digoxin has a half life of approximately 36 hours given at average doses in patients with normal renal function. It is excreted mostly unchanged in the urine. Common side effects include breast enlargement with other side effects generally due to an excessive dose. These side effects may include loss of appetite, nausea, trouble seeing, confusion, and an irregular heartbeat. Greater care is required in older people and those with poor kidney function. It ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rifampicin
Rifampicin, also known as rifampin, is an ansamycin antibiotic used to treat several types of bacterial infections, including tuberculosis (TB), mycobacterium avium complex, ''Mycobacterium avium'' complex, leprosy, and Legionnaires’ disease. It is almost always used together with other antibiotics with two notable exceptions: when given as a "preferred treatment that is strongly recommended" for latent TB infection; and when used as post-exposure prophylaxis to prevent Haemophilus influenzae type b, ''Haemophilus influenzae'' type b and meningococcal disease in people who have been exposed to those bacteria. Before treating a person for a long period of time, measurements of liver enzymes and blood counts are recommended. Rifampicin may be given either Oral administration, by mouth or intravenously. Common side effects include nausea, vomiting, diarrhea, and loss of appetite. It often turns urine, sweat, and tears a red or orange color. Liver problems or allergic reactions ma ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
