藥品異動通知2024.01.18

藥理作用/作用機轉

Paliperidone is considered a benzisoxazole atypical antipsychotic as it is the primary active metabolite of risperidone. As with other atypical antipsychotics, its therapeutic efficacy is believed to result from mixed central serotonergic and dopaminergic antagonism. The addition of serotonin antagonism to dopamine antagonism (classic neuroleptic mechanism) is thought to improve negative symptoms of psychoses and reduce the incidence of extrapyramidal side effects. Similar to risperidone, paliperidone demonstrates high affinity to α1, α2, D2, H1, and 5-HT2A receptors and low affinity for muscarinic receptors. In contrast to risperidone, paliperidone displays nearly 10-fold lower affinity for α2 and 5-HT2A receptors, and nearly three- to fivefold less affinity for 5-HT1A and 5-HT1D, respectively.

適應症/

劑量

IM

【Adult】700毫克/1000毫克的paliperidone (1092毫克/1560毫克的paliperidone palmitate)懸浮溶液

　●schizophrenia : 6-month IM paliperidone is to be used only after either 4 doses of monthly IM paliperidone (Invega Sustenna) or 1 dose of 3-month IM paliperidone.

　　*最後一劑每月注射型劑量為156mg則從1092mg六個月注射劑型開始。

　　*最後一劑每月注射型劑量為234mg則從1560mg六個月注射劑型開始。

　　*最後一劑三月注射型劑量為546mg則從1092mg六個月注射劑型開始。

　　*最後一劑三月注射型劑量為819mg則從1560mg六個月注射劑型開始。

【Pediatric】Safety and efficacy not established.

【Geriatric】Refer to adult dosing.

『Renal Impairment: Adult』

CrCl<90mL/minute: Use not recommended.

『Hepatic Impairment: Adult』

Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary.

使用禁忌

Hypersensitivity (anaphylaxis, angioedema) to paliperidone, risperidone, or any component of the formulation.

警告/預防

CNS depression, Falls

不良反應

Adverse Reactions (Significant): Angioedema, Dyslipidemia, Extrapyramidal symptoms, Hematologic abnormalities, Hyperglycemia, Hyperprolactinemia, Neuroleptic malignant syndrome, Orthostatic hypotension, QT prolongation, Sexual dysfunction, Temperature dysregulation, Weight gain

【>10%】Tachycardia,↓HDL cholesterol, hyperglycemia,↑LDL cholesterol,↑ serum cholesterol,↑ serum prolactin,↑serum TG, weight gain, vomiting, injection-site reaction, akathisia, drowsiness, dystonia, extrapyramidal reaction, headache, parkinsonism, tremor, hyperkinetic muscle activity, upper respiratory tract infection

【1% to 10%】 Bradycardia, bundle branch block, edema, first-degree atrioventricular block, hypertension, , palpitations, pruritus, skin rash, amenorrhea,↓libido, galactorrhea not associated with childbirth, gynecomastia , irregular menses, abdominal distress, constipation , decreased appetite , diarrhea , dyspepsia, flatulence , increased appetite , nausea, sialorrhea , stomach discomfort , upper abdominal pain, xerostomia, breast tenderness, UTI,↑serum AST/ALT, anaphylaxis, swollen tongue, agitation, anxiety, asthenia, dizziness, dysarthria, fatigue, insomnia, lethargy, nightmares, psychosis, sedated state, sleep disorder, arthralgia, back pain, dyskinesia, limb pain, muscle rigidity , musculoskeletal pain, myalgia, abnormal eye movements, blurred vision, cough, epistaxis, nasal congestion, nasopharyngitis, pharyngolaryngeal pain, rhinitis

【<1%】orthostatic hypotension, erectile dysfunction

【Frequency not defined】

懷孕用藥分級(FDA)

C /避免使用，除非有治療必要

健保規範

• 藥品說明：　(1)記載理由或診斷(2)超過下列日劑量時,須記載理由:Risperidone 6mg、Quetiapine 600mg、Amisulpride 800mg、Ziprasidone 120mg、Aripiprazole 15mg、Paliperidone 12mg、Lurasidone 120mg (3)雙極性疾患之鬱症發作不得使用

• 藥品理由：

6個月注射一次劑型，需使用4次每月施打型或使用1次三月施打型方可開立

其他

僅供臀部肌肉注射使用,交替使用兩側的外側四分之一臀部肌肉

提前2週內/延後3週內注射不會被視為遺漏劑量

針筒頂蓋朝上，快速振搖針筒至少15秒後再次快速振搖針筒至少15秒.

振搖後若超過5分鐘未注射請重新振搖30秒.

Administer by IM route only as a single injection (do not divide); do not administer by any other route. Do not mix with any other product or diluent. Avoid inadvertent injection into vasculature.