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FIASMA
Functional inhibitors of acid sphingomyelinase, or FIASMA, is a large group of pharmacological compounds inhibiting the enzyme acid sphingomyelinase (ASM, EC 3.1.4.12). This enzyme is mainly located within the lysosome, where it cleaves sphingomyelin to ceramide and sphingosine, the latter of which is then phosphorylated to sphingosine-1-phosphate. These metabolites, and subsequent inhibition of the enzyme, influence the balance between cell death (apoptosis) and cell growth (proliferation). A lack of regulation of this sensitive equilibrium can lead to serious clinical consequences. The acronym "FIASMA" was introduced by Kornhuber and coworkers; it is derived from the term ''Functional Inhibitor of Acid SphingoMyelinAse''. Mechanism of action of FIASMAs FIASMAs inhibit the ASM via an indirect, functional mechanism. They insert into the inner leaf of the lysosomal membrane and subsequently cause membrane-associated enzymes, such as ASM, to detach. Upon detachment from the mem ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzatropine
Benzatropine ( INN), known as benztropine in the United States and Japan, is a medication used to treat movement disorders like parkinsonism and dystonia, as well as extrapyramidal side effects of antipsychotics, including akathisia. It is not useful for tardive dyskinesia. It is a centrally acting anticholinergic and antihistamine, taken by mouth or by injection into a vein or muscle. Benefits are seen within two hours and last for up to ten hours. Common side effects include dry mouth, blurry vision, nausea, and constipation. Serious side effect may include urinary retention, hallucinations, hyperthermia, and poor coordination. It is unclear if use during pregnancy or breastfeeding is safe. Benzatropine is an anticholinergic which works by blocking the activity of muscarinic acetylcholine receptors. Benzatropine was approved for medical use in the United States in 1954. It is available as a generic medication. In 2020, it was the 229th most commonly prescribed medicat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acid Sphingomyelinase
Acid sphingomyelinase is one of the enzymes that make up the sphingomyelinase (SMase) family, responsible for catalyzing the breakdown of sphingomyelin to ceramide and phosphorylcholine. They are organized into alkaline, neutral, and acidic SMase depending on the pH in which their enzymatic activity is optimal. Acid sphingomyelinases' (aSMases) enzymatic activity can be influenced by drugs, lipids, cations, pH, redox and other proteins in the environment. Specifically aSMases have been shown to have increased enzymatic activity in lysobisphosphatidic acid (LBPA) or phosphatidylinositol (PI) enriched environments, and inhibited activity when phosphorylated derivatives of PI are present. Sphingomyelin phosphodiesterase 1 (''SMPD1'') is the gene that codes for two aSMase enzymes distinct in the pools of sphingomyelin they hydrolyse. Lysosomal sphingomyelinase (L-SMase) is found in the lysosomal compartment, and the secretory sphingomyelinase (S-SMase) is found extracellularly. Stru ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Biperiden
Biperiden, sold under the brand name Akineton among others, is a medication used to treat Parkinson disease, certain drug-induced movement disorders and Tourette Syndrome. It is not recommended for tardive dyskinesias. It is taken by mouth, injection into a vein, or muscle. Common side effects include blurred vision, dry mouth, sleepiness, constipation, and confusion. It should not be used in people with a bowel obstruction or glaucoma. It is unclear if use in pregnancy or breastfeeding is safe. Biperiden is in the anticholinergic family of medication. Biperiden was approved for medical use in the United States in 1959. It is on the World Health Organization's List of Essential Medicines. Biperiden is no longer marketed in the United States. Medical uses Biperiden is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arteriosclerotic Parkinson's) and for reduced sweating in methadone users. It seems to exert better eff ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Astemizole
Astemizole (marketed under the brand name Hismanal, developmental code R43512) was a second-generation antihistamine drug that has a long duration of action. Astemizole was discovered by Janssen Pharmaceutica in 1977. It was withdrawn from the market globally in 1999 because of rare but potentially fatal side effects ( QTc interval prolongation and related arrhythmias due to hERG channel blockade). Pharmacology Astemizole is a histamine H1-receptor antagonist. It has anticholinergic and antipruritic effects. Astemizole is rapidly absorbed from the gastrointestinal tract and competitively binds to histamine H1 receptor sites in the gastrointestinal tract, uterus, blood vessels, and bronchial muscle. This suppresses the formation of edema and pruritus (caused by histamine). Despite some earlier reports that astemizole does not cross the blood–brain barrier, several studies have shown high permeability and high binding to protein folds associated with Alzheimer's Alzhe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enzyme
An enzyme () is a protein that acts as a biological catalyst by accelerating chemical reactions. The molecules upon which enzymes may act are called substrate (chemistry), substrates, and the enzyme converts the substrates into different molecules known as product (chemistry), products. Almost all metabolism, metabolic processes in the cell (biology), cell need enzyme catalysis in order to occur at rates fast enough to sustain life. Metabolic pathways depend upon enzymes to catalyze individual steps. The study of enzymes is called ''enzymology'' and the field of pseudoenzyme, pseudoenzyme analysis recognizes that during evolution, some enzymes have lost the ability to carry out biological catalysis, which is often reflected in their amino acid sequences and unusual 'pseudocatalytic' properties. Enzymes are known to catalyze more than 5,000 biochemical reaction types. Other biocatalysts include Ribozyme, catalytic RNA molecules, also called ribozymes. They are sometimes descr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bepridil
Bepridil (trade name Vascor) is an diamine calcium channel blocker once used to treat angina pectoris. It is no longer sold in the United States. It is nonselective. It has been discussed as a possible option in the treatment of atrial fibrillation. It has been implicated in causing ventricular arrhythmia ( torsades de pointes). Ebola research In June 2015 a research paper was published finding bepridil to result in a 100% survival rate for mice exposed to ebola during an experiment searching for potential pharmaceutical ebola treatments; indicating its potential use in future ebola research and therapy. SARS-CoV-2 research A research paper showed that Bepridil inhibited cytopathogenic effects induced by SARS-CoV-2 Severe acute respiratory syndrome coronavirus 2 (SARS‑CoV‑2) is a strain of coronavirus that causes COVID-19, the respiratory illness responsible for the COVID-19 pandemic. The virus previously had the Novel coronavirus, provisional nam ... in Ve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aprindine
Aprindine is a Class 1b antiarrhythmic agent and has antiarrhythmic properties similar to lidocaine Lidocaine, also known as lignocaine and sold under the brand name Xylocaine among others, is a local anesthetic of the amino amide type. It is also used to treat ventricular tachycardia and ventricular fibrillation. When used for local anae .... References 2-Aminoindanes Anilines Antiarrhythmic agents Sodium channel blockers Diethylamino compounds {{cardiovascular-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amlodipine
Amlodipine, sold under the brand name Norvasc among others, is a calcium channel blocker medication used to treat hypertension, high blood pressure, coronary artery disease (CAD) and variant angina (also called Prinzmetal angina or coronary artery vasospasm, among other names). It is taken Oral administration, orally (swallowed by mouth). Common side effects include edema, swelling, fatigue (medical), feeling tired, abdominal pain, and nausea. Serious side effects may include hypotension, low blood pressure or myocardial infarction, heart attack. Whether use is safe during pregnancy or breastfeeding is unclear. When used by people with liver problems, and in elderly individuals, doses should be reduced. Amlodipine works partly by vasodilation (relaxing the arteries and increasing their diameter). It is a long-acting calcium channel blocker of the dihydropyridine type. Amlodipine was patented in 1982, and approved for medical use in 1990. It is on the WHO Model List of Essent ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amitriptyline
Amitriptyline, sold under the brand name Elavil among others, is a tricyclic antidepressant primarily used to treat major depressive disorder, and a variety of pain syndromes such as neuropathic pain, fibromyalgia, migraine and tension headaches. Due to the frequency and prominence of side effects, amitriptyline is generally considered a second-line therapy for these indications. The most common side effects are dry mouth, drowsiness, dizziness, constipation, and weight gain. Glaucoma, liver toxicity and abnormal heart rhythms are rare but serious side effects. Blood levels of amitriptyline vary significantly from one person to another, and amitriptyline interacts with many other medications potentially aggravating its side effects. Amitriptyline was discovered in the late 1950s by scientists at Merck and approved by the US Food and Drug Administration (FDA) in 1961. It is on the World Health Organization's List of Essential Medicines. It is available as a generic medicati ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amiodarone
Amiodarone is an antiarrhythmic medication used to treat and prevent a number of types of cardiac dysrhythmias. This includes ventricular tachycardia, ventricular fibrillation, and wide complex tachycardia, atrial fibrillation, and paroxysmal supraventricular tachycardia. Evidence in cardiac arrest, however, is poor. It can be given by mouth, intravenously, or intraosseously. When used by mouth, it can take a few weeks for effects to begin. Common side effects include feeling tired, tremor, nausea, and constipation. As amiodarone can have serious side effects, it is mainly recommended only for significant ventricular arrhythmias. Serious side effects include lung toxicity such as interstitial pneumonitis, liver problems, heart arrhythmias, vision problems, thyroid problems, and death. If taken during pregnancy or breastfeeding it can cause problems in the fetus or the infant. It is a class III antiarrhythmic medication. It works partly by increasing the time before a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alverine
Alverine is a drug used for functional gastrointestinal disorders. Alverine is a smooth muscle relaxant. Smooth muscle is a type of muscle that is not under voluntary control; it is the muscle present in places such as the gut and uterus. Adverse effects The side effects of Alverine include: *Difficulties in breathing or shortness of breath, wheezing, swelling of the face or other parts of the body (associated with serious allergic reaction) *Yellowing of the whites of the eyes and the skin, due to liver inflammation * A feeling of nausea or dizziness * Headache * Minor allergic reaction (skin rash/itching) It was reported that alverine may induce toxic hepatitis. Mechanism of action Alverine acts directly on the muscle in the gut, causing it to relax. Alverine is also a 5HT1A antagonist, which reduces rectal hypersensitivity. This prevents the muscle spasms which occur in the gut in conditions such as irritable bowel syndrome and diverticular disease. Diverticular diseas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
