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Antipsychotic ester
Paliperidone palmitate
Другие языки:

    Paliperidone palmitate

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    Paliperidone palmitate
    Paliperidone palmitate.svg
    Clinical data
    Trade names Invega Hayfera, Invega Sustenna, Invega Trinza, others
    Other names PP; PP1M; PP3M; PP6M; JNS-010; RO-92670; RO92670
    MedlinePlus a607005
    License data
    Routes of
    administration    		 Intramuscular
    Drug class Atypical antipsychotic
    Legal status
    Legal status
    • US: ℞-only
    • EU: Rx-only
    • In general: ℞ (Prescription only)
    Identifiers
    • [3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-9-yl] hexadecanoate
    CAS Number
    PubChem CID
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard 100.208.402
    Chemical and physical data
    Formula C39H57FN4O4
    Molar mass 664.907 g·mol−1
    3D model (JSmol)
    • CCCCCCCCCCCCCCCC(=O)OC1CCCN2C1=NC(=C(C2=O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F)C
    • InChI=1S/C39H57FN4O4/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-18-36(45)47-34-17-16-24-44-38(34)41-29(2)32(39(44)46)23-27-43-25-21-30(22-26-43)37-33-20-19-31(40)28-35(33)48-42-37/h19-20,28,30,34H,3-18,21-27H2,1-2H3
    • Key:VOMKSBFLAZZBOW-UHFFFAOYSA-N

    Paliperidone palmitate (PP), sold under the brand name Invega Sustenna among others, is an atypical antipsychotic which is used in the treatment of schizophrenia and schizoaffective disorder. It is an antipsychotic ester – specifically the palmitate ester of paliperidone – and acts as a long-lasting form of paliperidone. Paliperidone palmitate is formulated as an aqueous suspension, has a strong smell similar to alcohol, and is administered by intramuscular injection into deltoid or gluteal muscle once every 1 or 3 months depending on the formulation. A formulation for injection once every 6 months is also pending regulatory approval as of September 2021.

    With the once-monthly formulation of paliperidone palmitate, the time to peak is 13 days and the elimination half-life is 25 to 49 days, and with the 3-month formulation, the time to peak is 30 to 33 days and the half-life is 84 to 95 days via deltoid muscle and 118 to 139 days gluteally. The peak-to-trough ratio of paliperidone palmitate at steady state ranges from 1.56 to 1.70 with the 1- and 3-month formulations. The 3-month formulation of paliperidone palmitate has larger crystal sizes than the 1-month formulation and this allows for its longer duration. No pharmacokinetic data for the 6-month formulation has been released as of January 2021.

    Pharmacokinetics of long-acting injectable antipsychotics
    Medication Brand name Class Vehicle Dosage Tmax t1/2 single t1/2 multiple logPc Ref
    Aripiprazole lauroxil Aristada Atypical Watera 441–1064 mg/4–8 weeks 24–35 days ? 54–57 days 7.9–10.0
    Aripiprazole monohydrate Abilify Maintena Atypical Watera 300–400 mg/4 weeks 7 days ? 30–47 days 4.9–5.2
    Bromperidol decanoate Impromen Decanoas Typical Sesame oil 40–300 mg/4 weeks 3–9 days ? 21–25 days 7.9
    Clopentixol decanoate Sordinol Depot Typical Viscoleob 50–600 mg/1–4 weeks 4–7 days ? 19 days 9.0
    Flupentixol decanoate Depixol Typical Viscoleob 10–200 mg/2–4 weeks 4–10 days 8 days 17 days 7.2–9.2
    Fluphenazine decanoate Prolixin Decanoate Typical Sesame oil 12.5–100 mg/2–5 weeks 1–2 days 1–10 days 14–100 days 7.2–9.0
    Fluphenazine enanthate Prolixin Enanthate Typical Sesame oil 12.5–100 mg/1–4 weeks 2–3 days 4 days ? 6.4–7.4
    Fluspirilene Imap, Redeptin Typical Watera 2–12 mg/1 week 1–8 days 7 days ? 5.2–5.8
    Haloperidol decanoate Haldol Decanoate Typical Sesame oil 20–400 mg/2–4 weeks 3–9 days 18–21 days 7.2–7.9
    Olanzapine pamoate Zyprexa Relprevv Atypical Watera 150–405 mg/2–4 weeks 7 days ? 30 days –
    Oxyprothepin decanoate Meclopin Typical ? ? ? ? ? 8.5–8.7
    Paliperidone palmitate Invega Sustenna Atypical Watera 39–819 mg/4–12 weeks 13–33 days 25–139 days ? 8.1–10.1
    Perphenazine decanoate Trilafon Dekanoat Typical Sesame oil 50–200 mg/2–4 weeks ? ? 27 days 8.9
    Perphenazine enanthate Trilafon Enanthate Typical Sesame oil 25–200 mg/2 weeks 2–3 days ? 4–7 days 6.4–7.2
    Pipotiazine palmitate Piportil Longum Typical Viscoleob 25–400 mg/4 weeks 9–10 days ? 14–21 days 8.5–11.6
    Pipotiazine undecylenate Piportil Medium Typical Sesame oil 100–200 mg/2 weeks ? ? ? 8.4
    Risperidone Risperdal Consta Atypical Microspheres 12.5–75 mg/2 weeks 21 days ? 3–6 days –
    Zuclopentixol acetate Clopixol Acuphase Typical Viscoleob 50–200 mg/1–3 days 1–2 days 1–2 days 4.7–4.9
    Zuclopentixol decanoate Clopixol Depot Typical Viscoleob 50–800 mg/2–4 weeks 4–9 days ? 11–21 days 7.5–9.0
    Note: All by intramuscular injection. Footnotes: a = Microcrystalline or nanocrystalline aqueous suspension. b = Low-viscosity vegetable oil (specifically fractionated coconut oil with medium-chain triglycerides). c = Predicted, from PubChem and DrugBank. Sources: Main: See template.

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