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Anticonvulsants and neurological agents

148 articles

Oxcarbazepine

Oxcarbazepine (Trileptal) is a carbamazepine-related dibenzazepine antiseizure prodrug converted to active MHD, a sodium-channel blocker used for focal seizures; notable for hyponatremia risk and few enzyme interactions.

Oxiracetam

Oxiracetam is a synthetic racetam-family nootropic drug tested in clinical trials for dementia, post-stroke cognitive impairment, and cognitive impairment after traumatic brain injury, with favorable safety but mixed results.

Ozanimod

Ozanimod (Zeposia, RPC1063) is an oral S1P1/S1P5 receptor modulator approved in 2020 for relapsing multiple sclerosis and 2021 for ulcerative colitis, dosed 0.92 mg daily after titration.

Padsevonil

Padsevonil (UCB0942, PSL), a UCB Pharma antiseizure drug candidate for drug-resistant focal epilepsy, dual-acting on SV2A/B/C and GABA_A benzodiazepine site; failed phase 2b/3 trials and development was discontinued in 2020.

Paramethadione

Paramethadione (Paradione) is a discontinued oxazolidinedione anticonvulsant introduced by Abbott in 1949 for absence seizures, similar to but slightly less potent than trimethadione, acting via T-type calcium channel blockade in thalamic neurons.

Peginterferon beta-1a

Peginterferon beta-1a (Plegridy, Biogen) is a 20 kDa PEG-conjugated interferon beta-1a for relapsing-remitting multiple sclerosis, given 125 mcg subcutaneously every 2 weeks; FDA and EU approved in 2014.

Perampanel

Perampanel (Fycompa, E2007) is a non-competitive AMPA glutamate receptor antagonist antiseizure drug, first FDA-approved 22 October 2012 for partial-onset seizures, later for PGTC seizures, with Schedule III status and a psychiatric boxed warning.

Phenacemide

Phenacemide (Phenurone), phenylacetylurea, a 1948 ureide anticonvulsant for refractory psychomotor epilepsy, FDA-approved 1951, withdrawn 2004 due to liver and bone marrow toxicity.

Phensuximide

Phensuximide (Milontin), also called N-methyl-2-phenylsuccinimide, is a succinimide anticonvulsant developed by Parke-Davis in the 1950s for absence (petit mal) seizures; weakly effective, rarely used, and no longer sold in the US.

Phenylpiracetam

Phenylpiracetam (fonturacetam, carphedon, Phenotropil) is a Soviet-developed 1980 phenyl analog of piracetam, registered in Russia in 2003, more potent than piracetam, and the only racetam on the WADA prohibited stimulant list since 1998.

Phenytoin

Phenytoin, also called diphenylhydantoin and originally sold as Dilantin, is a hydantoin-derivative anticonvulsant introduced in 1938 that controls tonic-clonic and focal seizures and is used after neurosurgery.

Pimavanserin

Pimavanserin (Nuplazid), a selective 5-HT2A inverse agonist by ACADIA Pharmaceuticals, is the first FDA-approved drug (April 2016) for hallucinations and delusions of Parkinson's disease psychosis, distinct from dopamine-blocking antipsychotics.

Piracetam

Piracetam (2-oxo-1-pyrrolidine acetamide, C6H10N2O2) is the first nootropic, a GABA-derivative racetam developed in 1964 by Corneliu Giurgea, marketed by UCB in 1971, approved in over 120 countries for myoclonus but not FDA-approved, with inconclusive dementia evidence.

Ponesimod

Ponesimod (Ponvory) is an oral selective S1P1 receptor modulator by Janssen, approved 2021 in the US and EU for relapsing forms of multiple sclerosis; 20 mg daily after 14-day titration, superior to teriflunomide in OPTIMUM.

Pramipexole

Pramipexole (Mirapex, Mirapexin, Sifrol) is a non-ergot dopamine agonist, D3-preferring, FDA-approved in 1997 for Parkinson disease and 2006 for restless legs syndrome; dosed up to 4.5 mg/day ER, with sleep attacks, impulse control disorders, and augmentation as key risks.

Prazosin

Prazosin (Minipress) is a quinazoline alpha-1 adrenergic antagonist approved for hypertension and used off label for PTSD nightmares; evidence is mixed, with the 2023 VA/DoD guideline weakly favoring it for nightmares only.

Pregabalin

Pregabalin (Lyrica), a GABA-derivative anticonvulsant binding the alpha2-delta calcium channel subunit, treats neuropathic pain, fibromyalgia, and partial seizures; first approved 2004, discovered at Northwestern with NIH funding, and a controlled substance in the US, UK, and India.

Preladenant

Preladenant (SCH-420814, MK-3814), an oral, highly selective adenosine A2A receptor antagonist developed by Schering-Plough/Merck for Parkinson's disease; positive phase 2 off-time results but failed phase 3 trials and development discontinued in 2013.

Primidone

Primidone (Mysoline, Desoxyphenobarbital) is a 1954 FDA-approved anticonvulsant similar to phenobarbital, metabolized to PEMA and phenobarbital, used for grand mal, psychomotor, and focal seizures and as first-line therapy for essential tremor.

Pyritinol

Pyritinol, also known as pyrithioxin or pyridoxine disulfide, is a synthetic nootropic drug synthesized from vitamin B6 in 1961, used in Europe for cognitive disorders and dementia.

Reldesemtiv

Reldesemtiv (CK-2127107), a second-generation fast skeletal muscle troponin activator by Cytokinetics for ALS and SMA; FORTITUDE-ALS phase 2 and COURAGE-ALS phase 3 both missed endpoints, development discontinued.

Rimegepant

Rimegepant (Nurtec ODT, Vydura) is an oral CGRP receptor antagonist (gepant) approved in 2020 for acute migraine treatment in adults and later for episodic migraine prevention, dosed 75 mg orally or every other day.

Ropinirole

Ropinirole (Requip) is a non-ergoline dopamine D2/D3 agonist approved in 1997 for Parkinson's disease and moderate-to-severe primary restless legs syndrome, with a 6-hour half-life, CYP1A2 metabolism, and warnings for somnolence, impulse control disorders, and RLS augmentation.

Rovatirelin

Rovatirelin (KPS-0373, ロバチレリン) is an oral thyrotropin-releasing hormone analogue by Kissei/Shionogi for spinocerebellar degeneration ataxia; its phase 3 trials missed the primary SARA endpoint and its Japanese approval application was withdrawn in 2023.

Rufinamide

Rufinamide (Inovelon, Banzel) is a triazole antiseizure medication that prolongs sodium channel inactivation, approved as add-on therapy for Lennox-Gastaut syndrome seizures in the EU (2007) and US (2009).

Safinamide

Safinamide (Xadago, Onstryv) is a reversible MAO-B inhibitor and sodium/calcium channel blocker used as 50-100 mg once-daily add-on to levodopa for motor fluctuations in mid- to late-stage Parkinson's disease, approved in the EU (2015) and US (2017).

Samelisant

Samelisant (SUVN-G3031) is Suven Life Sciences' histamine H3 receptor inverse agonist for narcolepsy; positive Phase 2 (2.1-point ESS reduction) led to the global Phase 3 AWAKE study begun in 2026.

Sarizotan

Sarizotan (EMD 128130), a 5-HT1A agonist and dopamine D3/D4 ligand developed by Merck KGaA for levodopa dyskinesia; failed phase III trials and a Rett syndrome trial (STARS, NCT02790034), never approved.

Seletracetam

Seletracetam (ucb 44212) is an investigational second-generation racetam antiseizure drug, a levetiracetam derivative binding SV2A with tenfold higher affinity; reached phase IIa for epilepsy, discontinued in favor of brivaracetam, now redeveloped intranasally by PrevEp for acute seizure rescue.

Semagacestat

Semagacestat (LY450139) is Eli Lilly's oral gamma-secretase inhibitor for Alzheimer's disease, the first to reach phase III (IDENTITY trials), halted in August 2010 for cognitive worsening and skin cancer risk from Notch inhibition.