Peringatan Keamanan

LD50 information for pimavanserin is not readily available in the literature. Pre-marketing clinical trials involving pimavanserin in approximately 1200 subjects and patients do not report symptoms of overdose. In healthy subject studies, nausea and vomiting were reported. There are no known antidotes for an overdose with this drug. Cardiovascular monitoring should begin immediately in the case of an overdose and continuous ECG monitoring is recommended. If antiarrhythmic drugs are administered in an overdose of pimavanserin, disopyramide, procainamide, and quinidine should not be used due to their potential for QT-prolonging effects. In the case of an overdose, consider the 57 hour plasma half-life of pimavanserin and the possibility of multiple drug involvement.L32883

Pimavanserin

DB05316

small molecule approved investigational

Deskripsi

Pimavanserin is an atypical antipsychotic indicated for the treatment of psychiatric disorders.L48236 Although the exact mechanism of action is unknown, it is thought that pimavanserin interacts with the serotonin receptors, particularly the 5-HT2A and HT2C receptors.L48236 Unlike other atypical antipsychotics, pimavanserin lacks inherent dopaminergic activity. In fact, pimavanserin is the first antipsychotic drug without D2 blocking activity. Therefore, pimavanserin can be used to treat psychotic symptoms without causing extrapyramidal or worsening motor symptoms.A232613,A232573

Pimavanserin is marketed under the trade name NUPLAZID and developed by Acadia Pharmaceuticals.A232783 It was approved by the FDA in April 2016 for the treatment of hallucinations and delusions associated with Parkinson's disease psychosis thanks to favorable results from a pivotal six-week, randomized, placebo-controlled, parallel-group study.L48241,A232573 Pimavanserin was also under review as a potential treatment for dementia-related psychosis; however, as of April 2021, FDA approval has not been granted for this indication despite previous breakthrough designation.L32913

Struktur Molekul 2D

Berat 427.564
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average plasma half-lives for pimavanserin and its active metabolite (AC-279) are estimated at 57 hours and 200 hours, respectively.[L32883]
Volume Distribusi Following administration of a single dose of 34 mg, the average apparent volume of distribution was 2173 L in clinical studies.[L48241]
Klirens (Clearance) -

Absorpsi

The median Tmax of pimavanserin in clinical studies was 6 hours, regardless of the dose. The bioavailability of an oral tablet of pimavanserin and a solution were almost identical.L48241 Ingestion of a high-fat meal had no significant effect on the rate (Cmax) and extent (AUC) of pimavanserin exposure. Cmax decreased by about 9% while AUC increased by about 8% with a high-fat meal. The major active circulating N-desmethylated metabolite, AC-279, has a median Tmax of 6 hours.L48241

Metabolisme

Pimavanserin is mainly metabolized CYP3A4 and CYP3A5 hepatic cytochrome enzymes, and to a lesser extent by CYP2J2, CYP2D6, and other cytochrome and flavin-containing monooxygenase enzymes. CYP3A4 metabolizes pimavanserin to its major active metabolite, AC-279.L32883

Rute Eliminasi

Approximately 0.55% of the 34 mg oral dose of 14C-pimavanserin was eliminated as unchanged drug in urine and 1.53% was eliminated in feces after 10 days. Less than 1% of the administered dose of pimavanserin and its active metabolite AC-279 were recovered in urine.L48241

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Dose adjustment may be necessary if taking grapefruit products or other CYP3A4 inhibitors.
  • 2. Avoid St. John's Wort. This may induce the CYP3A4 metabolism of pimavanserin, which may cause reduced efficacy.
  • 3. Take with or without food.

Interaksi Obat

849 Data
Ethanol The metabolism of Pimavanserin can be increased when combined with Ethanol.
Bexarotene The metabolism of Pimavanserin can be increased when combined with Bexarotene.
Bosentan The metabolism of Pimavanserin can be increased when combined with Bosentan.
Nafcillin The metabolism of Pimavanserin can be increased when combined with Nafcillin.
Modafinil The metabolism of Pimavanserin can be increased when combined with Modafinil.
Etravirine The metabolism of Pimavanserin can be increased when combined with Etravirine.
Avasimibe The metabolism of Pimavanserin can be increased when combined with Avasimibe.
Echinacea The metabolism of Pimavanserin can be increased when combined with Echinacea.
Dexamethasone acetate The metabolism of Pimavanserin can be increased when combined with Dexamethasone acetate.
Pitolisant The serum concentration of Pimavanserin can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Pimavanserin can be increased when combined with Metreleptin.
Topiramate The metabolism of Pimavanserin can be increased when combined with Topiramate.
Rifabutin The metabolism of Pimavanserin can be increased when combined with Rifabutin.
Felbamate The risk or severity of QTc prolongation can be increased when Felbamate is combined with Pimavanserin.
Genistein The metabolism of Pimavanserin can be increased when combined with Genistein.
Oritavancin The metabolism of Pimavanserin can be increased when combined with Oritavancin.
Rufinamide The metabolism of Pimavanserin can be increased when combined with Rufinamide.
Armodafinil The metabolism of Pimavanserin can be increased when combined with Armodafinil.
Glycerol phenylbutyrate The metabolism of Pimavanserin can be increased when combined with Glycerol phenylbutyrate.
Eslicarbazepine acetate The metabolism of Pimavanserin can be increased when combined with Eslicarbazepine acetate.
Lesinurad The metabolism of Pimavanserin can be increased when combined with Lesinurad.
Asunaprevir The metabolism of Pimavanserin can be increased when combined with Asunaprevir.
Sarilumab The metabolism of Pimavanserin can be increased when combined with Sarilumab.
Esketamine The metabolism of Pimavanserin can be increased when combined with Esketamine.
Calcitriol The metabolism of Pimavanserin can be increased when combined with Calcitriol.
Vitamin E The metabolism of Pimavanserin can be increased when combined with Vitamin E.
Flunisolide The metabolism of Pimavanserin can be increased when combined with Flunisolide.
Troglitazone The metabolism of Pimavanserin can be increased when combined with Troglitazone.
Butalbital The metabolism of Pimavanserin can be increased when combined with Butalbital.
Flucloxacillin The metabolism of Pimavanserin can be increased when combined with Flucloxacillin.
Acetaminophen The metabolism of Pimavanserin can be increased when combined with Acetaminophen.
Clobazam The metabolism of Pimavanserin can be increased when combined with Clobazam.
Aminoglutethimide The metabolism of Pimavanserin can be increased when combined with Aminoglutethimide.
Beclomethasone dipropionate The metabolism of Pimavanserin can be increased when combined with Beclomethasone dipropionate.
Griseofulvin The metabolism of Pimavanserin can be increased when combined with Griseofulvin.
Secobarbital The metabolism of Pimavanserin can be increased when combined with Secobarbital.
Cerivastatin The metabolism of Pimavanserin can be increased when combined with Cerivastatin.
Betamethasone The metabolism of Pimavanserin can be increased when combined with Betamethasone.
Quinine The risk or severity of QTc prolongation can be increased when Quinine is combined with Pimavanserin.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Chlorpromazine is combined with Pimavanserin.
Dicloxacillin The metabolism of Pimavanserin can be increased when combined with Dicloxacillin.
Rofecoxib The metabolism of Pimavanserin can be increased when combined with Rofecoxib.
Fluocinolone acetonide The metabolism of Pimavanserin can be increased when combined with Fluocinolone acetonide.
Medroxyprogesterone acetate The metabolism of Pimavanserin can be increased when combined with Medroxyprogesterone acetate.
Triamcinolone The metabolism of Pimavanserin can be increased when combined with Triamcinolone.
Testosterone The metabolism of Pimavanserin can be increased when combined with Testosterone.
Clofibrate The metabolism of Pimavanserin can be increased when combined with Clofibrate.
Hydrocortisone The metabolism of Pimavanserin can be increased when combined with Hydrocortisone.
Mometasone The metabolism of Pimavanserin can be increased when combined with Mometasone.
Hydrocortamate The metabolism of Pimavanserin can be increased when combined with Hydrocortamate.
Oxcarbazepine The metabolism of Pimavanserin can be increased when combined with Oxcarbazepine.
Phenylbutazone The metabolism of Pimavanserin can be increased when combined with Phenylbutazone.
Mifepristone The risk or severity of QTc prolongation can be increased when Mifepristone is combined with Pimavanserin.
Methylphenobarbital The metabolism of Pimavanserin can be increased when combined with Methylphenobarbital.
Terbinafine The metabolism of Pimavanserin can be increased when combined with Terbinafine.
Prednisolone The metabolism of Pimavanserin can be increased when combined with Prednisolone.
Norgestimate The metabolism of Pimavanserin can be increased when combined with Norgestimate.
Methylprednisolone The metabolism of Pimavanserin can be increased when combined with Methylprednisolone.
Metyrapone The metabolism of Pimavanserin can be increased when combined with Metyrapone.
Clobetasol propionate The metabolism of Pimavanserin can be increased when combined with Clobetasol propionate.
Probenecid The metabolism of Pimavanserin can be increased when combined with Probenecid.
Fluocinonide The metabolism of Pimavanserin can be increased when combined with Fluocinonide.
Sulfinpyrazone The metabolism of Pimavanserin can be increased when combined with Sulfinpyrazone.
Thiamylal The metabolism of Pimavanserin can be increased when combined with Thiamylal.
Rifapentine The metabolism of Pimavanserin can be increased when combined with Rifapentine.
Budesonide The metabolism of Pimavanserin can be increased when combined with Budesonide.
Corticotropin The metabolism of Pimavanserin can be increased when combined with Corticotropin.
Cefradine The metabolism of Pimavanserin can be increased when combined with Cefradine.
Amobarbital The metabolism of Pimavanserin can be increased when combined with Amobarbital.
Aprobarbital The metabolism of Pimavanserin can be increased when combined with Aprobarbital.
Cortisone acetate The metabolism of Pimavanserin can be increased when combined with Cortisone acetate.
Paramethasone The metabolism of Pimavanserin can be increased when combined with Paramethasone.
Barbital The metabolism of Pimavanserin can be increased when combined with Barbital.
Deferasirox The metabolism of Pimavanserin can be increased when combined with Deferasirox.
Tesmilifene The metabolism of Pimavanserin can be increased when combined with Tesmilifene.
Clevidipine The metabolism of Pimavanserin can be increased when combined with Clevidipine.
Fosaprepitant The metabolism of Pimavanserin can be increased when combined with Fosaprepitant.
Seratrodast The metabolism of Pimavanserin can be increased when combined with Seratrodast.
Perampanel The metabolism of Pimavanserin can be increased when combined with Perampanel.
Formestane The metabolism of Pimavanserin can be increased when combined with Formestane.
Fluprednidene The metabolism of Pimavanserin can be increased when combined with Fluprednidene.
Fluocortolone The metabolism of Pimavanserin can be increased when combined with Fluocortolone.
Barbexaclone The metabolism of Pimavanserin can be increased when combined with Barbexaclone.
Difluocortolone The metabolism of Pimavanserin can be increased when combined with Difluocortolone.
Meprednisone The metabolism of Pimavanserin can be increased when combined with Meprednisone.
Dexamethasone isonicotinate The metabolism of Pimavanserin can be increased when combined with Dexamethasone isonicotinate.
Deflazacort The metabolism of Pimavanserin can be increased when combined with Deflazacort.
Cortivazol The metabolism of Pimavanserin can be increased when combined with Cortivazol.
Prednylidene The metabolism of Pimavanserin can be increased when combined with Prednylidene.
Cloprednol The metabolism of Pimavanserin can be increased when combined with Cloprednol.
Fluticasone The metabolism of Pimavanserin can be increased when combined with Fluticasone.
Estradiol acetate The metabolism of Pimavanserin can be increased when combined with Estradiol acetate.
Estradiol benzoate The metabolism of Pimavanserin can be increased when combined with Estradiol benzoate.
Estradiol cypionate The metabolism of Pimavanserin can be increased when combined with Estradiol cypionate.
Estradiol dienanthate The metabolism of Pimavanserin can be increased when combined with Estradiol dienanthate.
Estradiol valerate The metabolism of Pimavanserin can be increased when combined with Estradiol valerate.
Mometasone furoate The metabolism of Pimavanserin can be increased when combined with Mometasone furoate.
Hydrocortisone acetate The metabolism of Pimavanserin can be increased when combined with Hydrocortisone acetate.
Hydrocortisone butyrate The metabolism of Pimavanserin can be increased when combined with Hydrocortisone butyrate.
Hydrocortisone succinate The metabolism of Pimavanserin can be increased when combined with Hydrocortisone succinate.

Target Protein

5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 2C HTR2C
Sigma non-opioid intracellular receptor 1 SIGMAR1

Referensi & Sumber

Synthesis reference: A Novel Synthesis of Pimavanserin: A Selective Serotonin 5-HT2A Receptor Inverse Agonist. (2020). Kun Hu, Meiju Zhang, Dongdong Wu, Yuxuan Xie & Jie Ren. The New Journal for Organic Synthesis Volume 52, 2020 - Issue 1. https://doi.org/10.1080/00304948.2019.1697613
Artikel (PubMed)
  • PMID: 17708779
    Nordstrom AL, Mansson M, Jovanovic H, Karlsson P, Halldin C, Farde L, Vanover KE, Hacksell U, Brann MR, Davis RE, Weiner DM: PET analysis of the 5-HT2A receptor inverse agonist ACP-103 in human brain. Int J Neuropsychopharmacol. 2008 Mar;11(2):163-71. Epub 2007 Aug 21.
  • PMID: 28817967
    Kianirad Y, Simuni T: Pimavanserin, a novel antipsychotic for management of Parkinson's disease psychosis. Expert Rev Clin Pharmacol. 2017 Nov;10(11):1161-1168. doi: 10.1080/17512433.2017.1369405. Epub 2017 Oct 17.
  • PMID: 28579723
    Cruz MP: Pimavanserin (Nuplazid): A Treatment for Hallucinations and Delusions Associated With Parkinson's Disease. P T. 2017 Jun;42(6):368-371.
  • PMID: 26744739
    Hunter NS, Anderson KC, Cox A: Pimavanserin. Drugs Today (Barc). 2015 Nov;51(11):645-52. doi: 10.1358/dot.2015.51.11.2404001.
  • PMID: 27262680
    Markham A: Pimavanserin: First Global Approval. Drugs. 2016 Jul;76(10):1053-7. doi: 10.1007/s40265-016-0597-9.
  • PMID: 30475568
    D'Souza RS, Hooten WM: Extrapyramidal Symptoms .
  • PMID: 32811586
    Cummings JL, Devanand DP, Stahl SM: Dementia-related psychosis and the potential role for pimavanserin. CNS Spectr. 2020 Aug 19:1-9. doi: 10.1017/S1092852920001765.
  • PMID: 27503570
    Stahl SM: Mechanism of action of pimavanserin in Parkinson's disease psychosis: targeting serotonin 5HT2A and 5HT2C receptors. CNS Spectr. 2016 Aug;21(4):271-5. doi: 10.1017/S1092852916000407.
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Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Nuplazid
    Capsule • 34 mg/1 • Oral • US • Approved
  • Nuplazid
    Tablet, coated • 17 mg/1 • Oral • US • Approved
  • Nuplazid
    Tablet, coated • 10 mg/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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