Foslevodopa Foscarbidopa
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Foslevodopa Foscarbidopa
Foslevodopa is a medication which acts as a prodrug for levodopa, originally invented in the 1980s but not developed for medical use at that time. It is approved for use in a subcutaneous infusion as a fixed-dose combination with foscarbidopa for the treatment of Parkinson's disease Parkinson's disease (PD), or simply Parkinson's, is a neurodegenerative disease primarily of the central nervous system, affecting both motor system, motor and non-motor systems. Symptoms typically develop gradually and non-motor issues become ..., under the brand name Vyalev. References {{Authority control Amino acids Antiparkinsonian agents Catecholamines Dopamine agonists Monoamine precursors Organophosphates Prodrugs ...
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Medication
Medication (also called medicament, medicine, pharmaceutical drug, medicinal product, medicinal drug or simply drug) is a drug used to medical diagnosis, diagnose, cure, treat, or preventive medicine, prevent disease. Drug therapy (pharmacotherapy) is an important part of the medicine, medical field and relies on the science of pharmacology for continual advancement and on pharmacy for appropriate management. Drugs are Drug class, classified in many ways. One of the key divisions is by level of controlled substance, control, which distinguishes prescription drugs (those that a pharmacist dispenses only on the medical prescription) from over-the-counter drugs (those that consumers can order for themselves). Medicines may be classified by mode of action, route of administration, biological system affected, or therapeutic effects. The World Health Organization keeps a list of essential medicines. Drug discovery and drug development are complex and expensive endeavors undertake ...
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Prodrug
A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted (ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects. History Many herbal extracts historically used in medicine contain glycosides (sugar derivatives) of the active agent, which are hydrolyzed in the intestines to release the active and more bioavailable aglycone. For example, sal ...
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Levodopa
Levodopa, also known as L-DOPA and sold under many brand names, is a dopaminergic medication which is used in the treatment of Parkinson's disease (PD) and certain other conditions like dopamine-responsive dystonia and restless legs syndrome. The drug is usually used and formulated in combination with a peripherally selective aromatic L-amino acid decarboxylase (AAAD) inhibitor like carbidopa or benserazide. Levodopa is taken by mouth, by inhalation, through an intestinal tube, or by administration into fat (as foslevodopa). Side effects of levodopa include nausea, the wearing-off phenomenon, dopamine dysregulation syndrome, and levodopa-induced dyskinesia, among others. The drug is a centrally permeable monoamine precursor and prodrug of dopamine and hence acts as a dopamine receptor agonist. Chemically, levodopa is an amino acid, a phenethylamine, and a catecholamine. The major reason for enhanced risks for levodopa induced dyskinesia (LID) and OFF phases durin ...
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Fixed-dose Combination
A combination drug is a combination of two or more pharmaceutical drugs as active ingredients combined into a single dosage form, typically as a ''fixed-dose combination'', with each constituent standardized to specifications of a fixed dose. Fixed-dose combinations are mass-produced and mass marketed, intended to serve as a near universal treatment for a large patient population with diverse medical histories, conditions, predisposition thereof, and treatment requirements. A '' polypill'' is a pharmacy or capsule containing four or more active ingredients, often needing to be compounded at a specialized pharmacy in order to satisfy the specifications of a patient's personalized prescription and treatment plan, including dosage form, medicinal dosing, and/or mechanism of release. Polypills encompass approved prescription drugs and over the counter drugs, at times including nutritional supplements, amino acids, vitamins, minerals, and hormones. Fixed-dose combination drugs ...
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Foscarbidopa
Foscarbidopa is a medication which acts as a prodrug for carbidopa. It is used in a subcutaneous infusion as a fixed-dose combination with foslevodopa for the treatment of Parkinson's disease Parkinson's disease (PD), or simply Parkinson's, is a neurodegenerative disease primarily of the central nervous system, affecting both motor system, motor and non-motor systems. Symptoms typically develop gradually and non-motor issues become ..., under the brand name Vyalev. References {{Authority control Amino acids Organophosphates Phenethylhydrazines Prodrugs ...
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Parkinson's Disease
Parkinson's disease (PD), or simply Parkinson's, is a neurodegenerative disease primarily of the central nervous system, affecting both motor system, motor and non-motor systems. Symptoms typically develop gradually and non-motor issues become more prevalent as the disease progresses. The motor symptoms are collectively called parkinsonism and include tremors, bradykinesia, spasticity, rigidity as well as postural instability (i.e., difficulty maintaining balance). Non-motor symptoms develop later in the disease and include behavior change (individual), behavioral changes or mental disorder, neuropsychiatric problems such as sleep abnormalities, psychosis, anosmia, and mood swings. Most Parkinson's disease cases are idiopathic disease, idiopathic, though contributing factors have been identified. Pathophysiology involves progressive nerve cell death, degeneration of nerve cells in the substantia nigra, a midbrain region that provides dopamine to the basal ganglia, a system invo ...
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Vyalev
Foscarbidopa/foslevodopa, sold under the brand name Vyalev among others, is a fixed-dose combination medication used for the treatment of Parkinson's disease. It is a fixed-dose combination of foscarbidopa, an aromatic amino acid decarboxylation inhibitor and prodrug for carbidopa; and foslevodopa, an aromatic amino acid and prodrug for levodopa that was developed by AbbVie. Its structure is identical to carbidopa/levodopa except for the replacement of a hydroxyl on each molecule with a phosphate group, similar to the antiepileptic prodrug fosphenytoin as it relates to phenytoin. The combination was refused approval by the US Food and Drug Administration (FDA) in 2023. It was approved for medical use in Canada in May 2023, in Australia in March 2024, and in the United States in October 2024. Produodopa uses a pump to steadily release foscarbidopa/foslevodopa into the bloodstream round-the-clock. It is available via the UK National Health Service since February 2024. Medical ...
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Amino Acids
Amino acids are organic compounds that contain both amino and carboxylic acid functional groups. Although over 500 amino acids exist in nature, by far the most important are the Proteinogenic amino acid, 22 α-amino acids incorporated into proteins. Only these 22 appear in the genetic code of life. Amino acids can be classified according to the locations of the core structural functional groups (Alpha and beta carbon, alpha- , beta- , gamma- (γ-) amino acids, etc.); other categories relate to Chemical polarity, polarity, ionization, and side-chain group type (aliphatic, Open-chain compound, acyclic, aromatic, Chemical polarity, polar, etc.). In the form of proteins, amino-acid ''Residue (chemistry)#Biochemistry, residues'' form the second-largest component (water being the largest) of human muscles and other tissue (biology), tissues. Beyond their role as residues in proteins, amino acids participate in a number of processes such as neurotransmitter transport and biosynthesi ...
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Antiparkinsonian Agents
In the management of Parkinson's disease, due to the chronic nature of Parkinson's disease (PD), a broad-based program is needed that includes patient and family education, support-group services, general wellness maintenance, exercise, and nutrition. At present, no cure for the disease is known, but medications or surgery can provide relief from the symptoms. While many medications treat Parkinson's, none actually reverses the effects of the disease. Furthermore, the gold-standard treatment varies with the disease state. People with Parkinson's, therefore, often must take a variety of medications to manage the disease's symptoms. Several medications currently in development seek to better address motor fluctuations and nonmotor symptoms of PD. However, none is yet on the market with specific approval to treat Parkinson's. Medication The main families of drugs useful for treating motor symptoms are levodopa, dopamine agonists, and MAO-B inhibitors. The most commonly used treatm ...
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Catecholamines
A catecholamine (; abbreviated CA), most typically a 3,4-dihydroxyphenethylamine, is a monoamine neurotransmitter, an organic compound that has a catechol (benzene with two hydroxyl side groups next to each other) and a side-chain amine. Catechol can be either a free molecule or a substituent of a larger molecule, where it represents a 1,2-dihydroxybenzene group. Catecholamines are derived from the amino acid tyrosine, which is derived from dietary sources as well as synthesis from phenylalanine. Catecholamines are water-soluble and are 50% bound to plasma proteins in circulation. Included among catecholamines are epinephrine (adrenaline), norepinephrine (noradrenaline), and dopamine. Release of the hormones epinephrine and norepinephrine from the adrenal medulla of the adrenal glands is part of the fight-or-flight response. Tyrosine is created from phenylalanine by hydroxylation by the enzyme phenylalanine hydroxylase. Tyrosine is also ingested directly from dietar ...
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Dopamine Agonists
A dopamine agonist is a compound that activates dopamine receptors. There are two families of dopamine receptors, D1-like and D2-like. They are all G protein-coupled receptors. D1- and D5-receptors belong to the D1-like family and the D2-like family includes D2, D3 and D4 receptors. Dopamine agonists are primarily used in the treatment of the motor symptoms of Parkinson's disease, and to a lesser extent, in hyperprolactinemia and restless legs syndrome. They are also used off-label in the treatment of clinical depression. Impulse control disorders are associated with the use of dopamine agonists. Medical uses Parkinson's disease Dopamine agonists are mainly used in the treatment of Parkinson's disease.  The cause of Parkinson's is not fully known but genetic factors, for example specific genetic mutations, and environmental triggers have been linked to the disease. In Parkinson's disease dopaminergic neurons that produce the neurotransmitter dopamine in the brain slowly br ...
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Monoamine Precursors
Monoamine precursors are precursor (biochemistry), precursors of monoamines and monoamine neurotransmitters in the body. The amino acids L-tryptophan, L-tryptophan and 5-hydroxytryptophan, L-5-hydroxytryptophan (5-HTP; oxitriptan) are precursors of serotonin and melatonin, while the amino acids phenylalanine, L-phenylalanine, tyrosine, L-tyrosine, and L-DOPA, L-DOPA (levodopa) are precursors of dopamine, epinephrine (adrenaline), and norepinephrine (noradrenaline). Administration of monoamine precursors can increase the levels of monoamine neurotransmitters in the body and brain. Monoamine precursors may be used in combination with peripherally selective drug, peripherally selective aromatic L-amino acid decarboxylase inhibitor, aromatic L-amino acid decarboxylase inhibitors (AAAD inhibitors; also known as DOPA decarboxylase (DDC) inhibitors) such as carbidopa and benserazide to restrict metabolism and activation in the periphery. Carbidopa/levodopa and levodopa/benserazide are use ...
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