Paliperidone

Paliperidone Brand Names

Invega | Invega Sustenna | INVEGA TRINZA

What is Paliperidone

Paliperidone is an atypical antipsychotic and is the major active metabolite of risperidone, a benzisoxazole antipsychotic.

Atypical antipsychotics such as paliperidone are first-line treatment options for the management of schizophrenia and related disorders.

Paliperidone has been shown to improve positive and negative symptoms of schizophrenia without producing significant extrapyramidal side effects.

Patients enrolled in clinical trials showed significant improvements in all five areas of the Positive and Negative Syndrome Scale (PANSS) including positive symptoms, negative symptoms, disorganized thoughts, uncontrolled hostility/excitement, and anxiety/depression.

Paliperidone does not undergo extensive hepatic metabolism, a potential advantage compared to many similar agents exhibiting drug interactions due to metabolism via cytochrome P450 (CYP450) isoenzymes.

Initial FDA approval for oral paliperidone was granted in December 2006 and the drug is approved for treatment of schizophrenia in adult and pediatric patients 12 years and older, as well as for schizoaffective disorder in adults.

A once-monthly depot injection (Invega Sustenna) and a 3-month depot injection (Invega Trinza) are available for the maintenance treatment of adults with schizophrenia.

Invega Sustenna is also approved as monotherapy or adjunct therapy to mood stabilizers or antidepressants for the treatment of schizoaffective disorder in adults.

As with all antipsychotics, the products carry a boxed warning regarding increased mortality risk in elderly patients treated for dementia-related psychosis.

Indications

1. behavioral or psychological symptoms of dementia
2. bipolar disorder
3. mania
4. schizoaffective disorder
5. schizophrenia

Side Effects

1. abdominal pain
2. agitation
3. agranulocytosis
4. akathisia
5. amenorrhea
6. anaphylactoid reactions
7. angioedema
8. anxiety
9. appetite stimulation
10. arthralgia
11. asthenia
12. AV block
13. back pain
14. blurred vision
15. bradycardia
16. breast discharge
17. bundle-branch block
18. constipation
19. cough
20. cystitis
21. dental pain
22. diabetes mellitus
23. diarrhea
24. dizziness
25. drowsiness
26. dysarthria
27. dyskinesia
28. dyspepsia
29. dystonic reaction
30. edema
31. ejaculation dysfunction
32. elevated hepatic enzymes
33. epistaxis
34. fatigue
35. fever
36. flatulence
37. galactorrhea
38. glossitis
39. gynecomastia
40. headache
41. hypercholesterolemia
42. hyperglycemia
43. hyperinsulinemia
44. hyperkinesis
45. hyperlipidemia
46. hyperprolactinemia
47. hypersalivation
48. hypertension
49. hypertonia
50. hypertriglyceridemia
51. hyponatremia
52. hypotension
53. ileus
54. impotence (erectile dysfunction)
55. infection
56. infertility
57. injection site reaction
58. insomnia
59. lethargy
60. leukopenia
61. libido decrease
62. menstrual irregularity
63. muscle cramps
64. myalgia
65. nasal congestion
66. nausea
67. neuroleptic malignant syndrome
68. neutropenia
69. nightmares
70. orthostatic hypotension
71. palpitations
72. peripheral edema
73. pharyngitis
74. polydipsia
75. priapism
76. pruritus
77. pseudoparkinsonism
78. QT prolongation
79. rash
80. restlessness
81. rhinitis
82. seizures
83. SIADH
84. sinus tachycardia
85. somnambulism
86. stroke
87. syncope
88. tardive dyskinesia
89. thrombotic thrombocytopenic purpura (TTP)
90. tremor
91. urinary incontinence
92. urinary retention
93. urticaria
94. vomiting
95. water intoxication
96. weight gain
97. xerostomia

Monitoring Parameters

• AIMS assessment
• blood glucose
• CBC
• glycosylated hemoglobin A1c (HbA1c)
• LFTs
• neurologic function
• pregnancy testing
• serum creatinine
• serum electrolytes
• serum lipid profile
• serum prolactin
• thyroid function tests (TFTs)
• weight

Contraindications

• abrupt discontinuation
• agranulocytosis
• ambient temperature increase
• apheresis
• AV block
• bradycardia
• breast cancer
• breast-feeding
• cardiac arrhythmias
• cardiac disease
• cardiomyopathy
• celiac disease
• cerebrovascular disease
• children
• CNS depression
• coadministration with other CNS depressants
• cystic fibrosis
• dehydration
• dementia
• diabetes mellitus
• diabetic ketoacidosis
• driving or operating machinery
• dysphagia
• esophageal stricture
• ethanol ingestion
• females
• fever
• gastroparesis
• geriatric
• GI obstruction
• heart failure
• hematological disease
• hepatic disease
• human immunodeficiency virus (HIV) infection
• hypercholesterolemia
• hyperglycemia
• hyperlipidemia
• hyperosmolar hyperglycemic state (HHS)
• hyperparathyroidism
• hyperprolactinemia
• hyperthermia
• hypertriglyceridemia
• hypocalcemia
• hypokalemia
• hypomagnesemia
• hypotension
• hypothermia
• hypothyroidism
• hypovolemia
• infants
• infertility
• inflammatory bowel disease
• leukopenia
• long QT syndrome
• myocardial infarction
• neonates
• neurological disease
• neutropenia
• obesity
• orthostatic hypotension
• Parkinson’s disease
• peritonitis
• pheochromocytoma
• pregnancy
• pregnancy testing
• priapism
• QT prolongation
• renal failure
• renal impairment
• rheumatoid arthritis
• seizure disorder
• seizures
• serious hypersensitivity reactions or anaphylaxis
• sickle cell disease
• sleep deprivation
• strenuous exercise
• stroke
• syncope
• systemic lupus erythematosus (SLE)
• tardive dyskinesia
• thrombotic thrombocytopenic purpura (TTP)

Interactions

• Abarelix
• Acarbose
• Acetaminophen; Butalbital
• Acetaminophen; Butalbital; Caffeine
• Acetaminophen; Butalbital; Caffeine; Codeine
• Acetaminophen; Caffeine; Dihydrocodeine
• Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
• Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
• Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
• Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
• Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
• Acetaminophen; Codeine
• Acetaminophen; Dextromethorphan; Doxylamine
• Acetaminophen; Dichloralphenazone; Isometheptene
• Acetaminophen; Diphenhydramine
• Acetaminophen; Hydrocodone
• Acetaminophen; Oxycodone
• Acetaminophen; Pentazocine
• Acetaminophen; Propoxyphene
• Acetaminophen; Tramadol
• Acrivastine; Pseudoephedrine
• Albiglutide
• Alfentanil
• Alfuzosin
• Alogliptin
• Alogliptin; Metformin
• Alogliptin; Pioglitazone
• Alpha-glucosidase Inhibitors
• Alprazolam
• Amifampridine
• Amiodarone
• Amitriptyline; Chlordiazepoxide
• Amobarbital
• Amoxapine
• Amoxicillin; Clarithromycin; Lansoprazole
• Amoxicillin; Clarithromycin; Omeprazole
• Amyl Nitrite
• Anagrelide
• Angiotensin II receptor antagonists
• Angiotensin-converting enzyme inhibitors
• Apalutamide
• Apomorphine
• Aripiprazole
• Arsenic Trioxide
• Artemether; Lumefantrine
• Articaine; Epinephrine
• Asenapine
• Aspirin, ASA; Butalbital; Caffeine
• Aspirin, ASA; Butalbital; Caffeine; Codeine
• Aspirin, ASA; Caffeine; Dihydrocodeine
• Aspirin, ASA; Carisoprodol; Codeine
• Aspirin, ASA; Oxycodone
• Atomoxetine
• Atropine; Hyoscyamine; Phenobarbital; Scopolamine
• Azithromycin
• Bedaquiline
• Belladonna Alkaloids; Ergotamine; Phenobarbital
• Benzhydrocodone; Acetaminophen
• Benzodiazepines
• Bepridil
• Beta-adrenergic blockers
• Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
• Bismuth Subsalicylate; Metronidazole; Tetracycline
• Bosentan
• Brexpiprazole
• Bromocriptine
• Brompheniramine
• Brompheniramine; Carbetapentane; Phenylephrine
• Brompheniramine; Dextromethorphan; Guaifenesin
• Brompheniramine; Dextromethorphan; Phenylephrine
• Brompheniramine; Guaifenesin; Hydrocodone
• Brompheniramine; Hydrocodone; Pseudoephedrine
• Brompheniramine; Pseudoephedrine
• Buprenorphine
• Buprenorphine; Naloxone
• Bupropion
• Bupropion; Naltrexone
• Buspirone
• Butabarbital
• Butorphanol
• Cabergoline
• Calcium-channel blockers
• Canagliflozin
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• Cannabidiol
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• Carbetapentane; Chlorpheniramine; Phenylephrine
• Carbetapentane; Diphenhydramine; Phenylephrine
• Carbetapentane; Guaifenesin
• Carbetapentane; Guaifenesin; Phenylephrine
• Carbetapentane; Phenylephrine
• Carbetapentane; Phenylephrine; Pyrilamine
• Carbetapentane; Pseudoephedrine
• Carbetapentane; Pyrilamine
• Carbidopa; Levodopa
• Carbidopa; Levodopa; Entacapone
• Carbinoxamine
• Carbinoxamine; Dextromethorphan; Pseudoephedrine
• Carbinoxamine; Hydrocodone; Phenylephrine
• Carbinoxamine; Hydrocodone; Pseudoephedrine
• Carbinoxamine; Phenylephrine
• Carbinoxamine; Pseudoephedrine
• Cariprazine
• Cenobamate
• Central-acting adrenergic agents
• Ceritinib
• Cetirizine
• Cetirizine; Pseudoephedrine
• Cetrorelix
• Chlophedianol; Dexchlorpheniramine; Pseudoephedrine
• Chlorcyclizine
• Chlordiazepoxide
• Chlordiazepoxide; Clidinium
• Chloroquine
• Chlorpheniramine
• Chlorpheniramine; Codeine
• Chlorpheniramine; Dextromethorphan
• Chlorpheniramine; Dextromethorphan; Phenylephrine
• Chlorpheniramine; Dihydrocodeine; Phenylephrine
• Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
• Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
• Chlorpheniramine; Hydrocodone
• Chlorpheniramine; Hydrocodone; Phenylephrine
• Chlorpheniramine; Hydrocodone; Pseudoephedrine
• Chlorpheniramine; Phenylephrine
• Chlorpheniramine; Pseudoephedrine
• Chlorpromazine
• Chlorthalidone; Clonidine
• Ciprofloxacin
• Cisapride
• Citalopram
• Clarithromycin
• Clemastine
• Clobazam
• Clofazimine
• Clonazepam
• Clonidine
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• Codeine
• Codeine; Guaifenesin
• Codeine; Phenylephrine; Promethazine
• Codeine; Promethazine
• COMT inhibitors
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• Dapagliflozin; Saxagliptin
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• Dasatinib
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• Deutetrabenazine
• Dexchlorpheniramine
• Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
• Dexmethylphenidate
• Dextromethorphan; Diphenhydramine; Phenylephrine
• Dextromethorphan; Promethazine
• Dextromethorphan; Quinidine
• Diazepam
• Diazoxide
• Dihydrocodeine; Guaifenesin; Pseudoephedrine
• Dimenhydrinate
• Dipeptidyl Peptidase-4 Inhibitors
• Diphenhydramine
• Diphenhydramine; Hydrocodone; Phenylephrine
• Diphenhydramine; Ibuprofen
• Diphenhydramine; Naproxen
• Diphenhydramine; Phenylephrine
• Disopyramide
• Dofetilide
• Dolasetron
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• Donepezil
• Donepezil; Memantine
• Dopamine
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• Doxylamine; Pyridoxine
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• Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
• Encorafenib
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• Entrectinib
• Enzalutamide
• Epinephrine
• Eplerenone
• Eribulin
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• Erythromycin
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• Escitalopram
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• Estazolam
• Eszopiclone
• Ethanol
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• Fentanyl
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• Flecainide
• Fluconazole
• Fluoxetine
• Fluoxetine; Olanzapine
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• food
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• Gabapentin
• Ganirelix
• Gemifloxacin
• Gemtuzumab Ozogamicin
• Gilteritinib
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• Glimepiride; Pioglitazone
• Glimepiride; Rosiglitazone
• Glipizide; Metformin
• Glyburide; Metformin
• Goserelin
• Granisetron
• Guaifenesin; Hydrocodone
• Guaifenesin; Hydrocodone; Pseudoephedrine
• Guanabenz
• Guanfacine
• Halofantrine
• Halogenated Anesthetics
• Haloperidol
• Histrelin
• Homatropine; Hydrocodone
• Hydantoins
• Hydralazine
• Hydralazine; Hydrochlorothiazide, HCTZ
• Hydralazine; Isosorbide Dinitrate, ISDN
• Hydrochlorothiazide, HCTZ; Methyldopa
• Hydrocodone
• Hydrocodone; Ibuprofen
• Hydrocodone; Phenylephrine
• Hydrocodone; Potassium Guaiacolsulfonate
• Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
• Hydrocodone; Pseudoephedrine
• Hydromorphone
• Hydroxychloroquine
• Hydroxyzine
• Ibuprofen; Oxycodone
• Ibutilide
• Iloperidone
• Incretin Mimetics
• Inotuzumab Ozogamicin
• Insulin Degludec; Liraglutide
• Insulin Glargine; Lixisenatide
• Insulins
• Isocarboxazid
• Isoniazid, INH; Pyrazinamide, PZA; Rifampin
• Isoniazid, INH; Rifampin
• Isosorbide Dinitrate, ISDN
• Isosorbide Mononitrate
• Itraconazole
• Ivosidenib
• Ketoconazole
• Lapatinib
• Lasmiditan
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• Lenvatinib
• Leuprolide
• Leuprolide; Norethindrone
• Levocetirizine
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• Levorphanol
• Linagliptin
• Linagliptin; Metformin
• Liraglutide
• Lithium
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• Lofexidine
• Long-acting beta-agonists
• Loop diuretics
• Loperamide
• Loperamide; Simethicone
• Lopinavir; Ritonavir
• Lorazepam
• Loxapine
• Lumacaftor; Ivacaftor
• Lumateperone
• Lurasidone
• Macimorelin
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• Mecamylamine
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• Mefloquine
• Meglitinides
• Meperidine
• Meperidine; Promethazine
• Mephobarbital
• Meprobamate
• Mesoridazine
• Metformin
• Metformin; Pioglitazone
• Metformin; Repaglinide
• Metformin; Rosiglitazone
• Metformin; Saxagliptin
• Metformin; Sitagliptin
• Methadone
• Methohexital
• Methyldopa
• Methylphenidate
• Metoclopramide
• Metronidazole
• Midazolam
• Midostaurin
• Mifepristone
• Miglitol
• Minoxidil
• Mirtazapine
• Mitotane
• Molindone
• Monoamine oxidase inhibitors
• Morphine
• Morphine; Naltrexone
• Moxifloxacin
• Nabilone
• Nafarelin
• Nalbuphine
• Nateglinide
• Nitrates
• Nitroglycerin
• Nitroprusside
• Norfloxacin
• Octreotide
• Ofloxacin
• Olanzapine
• Ombitasvir; Paritaprevir; Ritonavir
• Ondansetron
• Osilodrostat
• Osimertinib
• Oxaliplatin
• Oxazepam
• Oxycodone
• Oxymorphone
• Ozanimod
• Panobinostat
• Paroxetine
• Pasireotide
• Pentamidine
• Pentazocine
• Pentazocine; Naloxone
• Pentobarbital
• Pergolide
• Perphenazine
• Perphenazine; Amitriptyline
• Phenelzine
• Phenobarbital
• Phenylephrine; Promethazine
• Pimavanserin
• Pimozide
• Pioglitazone
• Pitolisant
• Posaconazole
• Potassium-sparing diuretics
• Pramipexole
• Pramlintide
• Prazosin
• Pregabalin
• Prilocaine; Epinephrine
• Primaquine
• Primidone
• Procainamide
• Prochlorperazine
• Promethazine
• Propafenone
• Propoxyphene
• Quazepam
• Quetiapine
• Quinidine
• Quinine
• Ranolazine
• Rasagiline
• Remifentanil
• Repaglinide
• Reserpine
• Ribociclib
• Ribociclib; Letrozole
• Rifampin
• Rilpivirine
• Risperidone
• Romidepsin
• Ropinirole
• Rosiglitazone
• Rotigotine
• Safinamide
• Saquinavir
• Saxagliptin
• Secobarbital
• Selegiline
• Selpercatinib
• Semaglutide
• Sertraline
• SGLT2 Inhibitors
• Short-acting beta-agonists
• Sibutramine
• Simvastatin; Sitagliptin
• Siponimod
• Sitagliptin
• Sodium picosulfate; Magnesium oxide; Anhydrous citric acid
• Solifenacin
• Sorafenib
• Sotalol
• Sparfloxacin
• St. John’s Wort, Hypericum perforatum
• Sufentanil
• Sulfonylureas
• Sunitinib
• Suvorexant
• Tacrolimus
• Tamoxifen
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• Temazepam
• Terazosin
• Tetrabenazine
• Thiazide diuretics
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• Tipranavir
• Tolcapone
• Tolterodine
• Toremifene
• Tramadol
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• Triclabendazole
• Tricyclic antidepressants
• Trifluoperazine
• Triprolidine
• Triptorelin
• Valproic Acid, Divalproex Sodium
• Vandetanib
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• Venlafaxine
• Voriconazole
• Vorinostat
• Zaleplon
• Ziprasidone
• Zolpidem
• Zonisamide