COMT inhibitor

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COMT inhibitors block one of two ways levodopa can be inactivated before it reaches the central nervous system and is activated to dopamine. Peripheral inhibitors of DOPA decarboxylase (AADC) block the second way. (Dopamine in the periphery only causes side effects, no antiparkinson effect.)[1]

A COMT inhibitor is a drug that inhibits the action of catechol-O-methyl transferase. This enzyme is involved in degrading neurotransmitters. COMT inhibitors are used in the treatment of Parkinson's disease in combination with levodopa and a DOPA decarboxylase inhibitor because they inhibit levadopa degradation in the periphery, that is, outside the central nervous system (CNS).[1]

Pharmaceutical examples include entacapone,[2] tolcapone,[3] opicapone and nitecapone. Tolcapone also acts inside the CNS.[4]

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References[edit]

  1. ^ a b Mutschler, Ernst; Schäfer-Korting, Monika (2001). Arzneimittelwirkungen (in German) (8 ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. p. 313–316. ISBN 3-8047-1763-2. 
  2. ^ Nissinen E; Nissinen H; Larjonmaa H; et al. (September 2005). "The COMT inhibitor, entacapone, reduces levodopa-induced elevations in plasma homocysteine in healthy adult rats". J Neural Transm. 112 (9): 1213–1221. doi:10.1007/s00702-004-0262-4. PMID 15614425. 
  3. ^ Giakoumaki SG, Roussos P, Bitsios P (June 2008). "Improvement of Prepulse Inhibition and Executive Function by the COMT Inhibitor Tolcapone Depends on COMT Val158Met Polymorphism". Neuropsychopharmacology. 33 (13): 3058–3068. doi:10.1038/npp.2008.82. PMID 18536698. 
  4. ^ Dinnendahl, V; Fricke, U, eds. (1998). Arzneistoff-Profile (in German). 10 (13 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-9846-3.