Products Entacapone was commercially available in the form of film-coated tablets (Comtan). It was approved in many countries since 1999. In 2017, distribution was discontinued. A fixed combination with levodopa and carbidopa has also been available since 2004 (Stalevo). Generic versions of the combination drug were approved in 2014. Structure and properties Entacapone (C14H15N3O5, Mr … Entacapon
Products Biperiden is commercially available as tablets, sustained-release tablets, and a solution for injection (Akineton, Akineton retard). It has been approved in many countries since 1958. Structure and properties Biperiden (C21H29NO, Mr = 311.46 g/mol) is present in drugs as biperidene hydrochloride, a white crystalline powder that is sparingly soluble in water. It is a … Biperides
Products Carbidopa is used in combination with levodopa in tablet form. In addition to the original Sinemet, generic versions are also available. Carbidopa has been approved in many countries since 1973. Structure and properties Carbidopa (C10H14N2O4, Mr = Mr = 226.2 g/mol) is present in drugs as carbidopa monohydrate, a white crystalline powder that is … Carbidopa
Products Tolcapone is commercially available in the form of film-coated tablets (Tasmar). It has been approved in many countries since 1997. Structure and properties Tolcapone (C14H11NO5, Mr = 273.2 g/mol) exists as a yellow, odorless, non-hygroscopic, crystalline powder. It is a nitrobenzophenone. Effects Tolcapone (ATC N04BX01) affects the pharmacokinetics of levodopa. The effects are due … Tolcapon
Effects Decarboxylase inhibitors inhibit decarboxylase, which metabolizes levodopa to dopamine. They are used exclusively in combination with levodopa to treat Parkinson’s disease. Their effect is limited to the periphery because they hardly cross the blood–brain barrier. Decarboxylase inhibitors thus allow more or less selective degradation of levodopa to dopamine in the central nervous system and … Decarboxylase Inhibitor
Effects Indirect dopaminergic Indications Parkinson’s disease Depression (USA) Active ingredients Rasagiline (Azilect) Selegiline (off label) Safinamide (Xadago)
Products Rasagiline is commercially available in tablet form (Azilect). It has been approved in many countries since 2005. Generic versions were first released in 2015. Structure and properties Rasagiline (C12H13N, Mr = 171.24 g/mol) is an aminoindan derivative and has an asymmetric carbon atom. Therapeutic uses are found for the -enantiomer. It is present in … Rasagiline
Products Procyclidine is commercially available in tablet form (Kemadrin). It has been approved in many countries since 1956. Structure and properties Procyclidine (C19H29NO, Mr = 287.4 g/mol) has structural similarities to biperides. Effects Procyclidine (ATC N04AA04) has anticholinergic properties and is effective against rigor, tremor, akinesia, speech and writing disorders, gait unsteadiness, increased salivation, sweating, … Procyclidine
Products Levodopa is marketed exclusively as combination products together with a peripheral decarboxylase inhibitor (carbidopa or benserazide) or a COMT inhibitor (entacapone). It has been approved in many countries since 1973 and is commercially available in tablet, capsule, suspendable tablet, and sustained-release tablet forms, among others. Structure and properties Levodopa (C9H11NO4, Mr = 197.2 g/mol) … Levodopa: Drug Effects, Side Effects, Dosage and Uses
Products Levodopa for inhalation was approved in the United States in 2018 and in the EU in 2019 (Inbrija, capsules containing a powder for inhalation). Structure and properties Levodopa (C9H11NO4, Mr = 197.2 g/mol) exists as a white crystalline powder that is sparingly soluble in water. It is a derivative of the amino acid tyrosine. … Levodopa Inhalation
Products Safinamide is commercially available in the form of film-coated tablets (Xadago). It was approved in many countries and in the EU in 2015 and in the US in 2017. Structure and properties Safinamide (C17H19FN2O2, Mr = 302.3 g/mol) is an α-aminoamide derivative. Effects Safinamide (ATC N04BD03) has indirect dopaminergic properties. It is a selective … Safinamide
