Antipsychotic ester

Short description: Type of medication

Haloperidol decanoate, an antipsychotic ester.

An antipsychotic ester is an ester of an antipsychotic.[1] They are used clinically as prodrugs to increase fat solubility and thereby prolong duration when antipsychotics are used as depot injectables.[1]

## Contents

* 1 List of clinically used antipsychotic esters
* 1.1 Typical antipsychotics
* 1.2 Atypical antipsychotics
* 2 Pharmacology
* 3 References

## List of clinically used antipsychotic esters

### Typical antipsychotics

* Bromperidol decanoate
* Clopentixol decanoate
* Flupentixol decanoate
* Fluphenazine decanoate
* Fluphenazine enanthate
* Haloperidol decanoate
* Oxyprothepin decanoate
* Perphenazine decanoate
* Perphenazine enanthate
* Pipotiazine palmitate
* Pipotiazine undecylenate
* Zuclopentixol acetate
* Zuclopentixol decanoate

### Atypical antipsychotics

* Aripiprazole lauroxil
* Paliperidone palmitate
* Risperidone

## Pharmacology

v * d * e Pharmacokinetics of long-acting injectable antipsychotics Medication | Brand name | Class | Vehicle | Dosage | Tmax | t1/2 single | t1/2 multiple | logPc | Ref

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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 | [2]
Clopentixol decanoate | Sordinol Depot | Typical | Viscoleob | 50–600 mg/1–4 weeks | 4–7 days | ? | 19 days | 9.0 | [3]
Flupentixol decanoate | Depixol | Typical | Viscoleob | 10–200 mg/2–4 weeks | 4–10 days | 8 days | 17 days | 7.2–9.2 | [3][4]
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 | [5][6][7]
Fluphenazine enanthate | Prolixin Enanthate | Typical | Sesame oil | 12.5–100 mg/1–4 weeks | 2–3 days | 4 days | ? | 6.4–7.4 | [6]
Fluspirilene | Imap, Redeptin | Typical | Watera | 2–12 mg/1 week | 1–8 days | 7 days | ? | 5.2–5.8 | [8]
Haloperidol decanoate | Haldol Decanoate | Typical | Sesame oil | 20–400 mg/2–4 weeks | 3–9 days | 18–21 days | 7.2–7.9 | [9][10]
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 | [11]
Pipotiazine palmitate | Piportil Longum | Typical | Viscoleob | 25–400 mg/4 weeks | 9–10 days | ? | 14–21 days | 8.5–11.6 | [4]
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.

## References

1. ↑ 1.0 1.1 "The pharmacokinetics of long-acting antipsychotic medications". Current Clinical Pharmacology 9 (3): 310–7. 2014. doi:10.2174/15748847113089990051. PMID 23343447.
2. ↑ "Long-term treatment of chronic psychotics with bromperidol decanoate: clinical and pharmacokinetic evaluation.". Current Therapeutic Research 34 (1): 1–6. 1983.
3. ↑ 3.0 3.1 "Clopenthixol and flupenthixol depot preparations in outpatient schizophrenics. III. Serum levels". Acta Psychiatrica Scandinavica. Supplementum 279: 41–54. 1980. doi:10.1111/j.1600-0447.1980.tb07082.x. PMID 6931472.
4. ↑ 4.0 4.1 "Anxiolytic sedatives, hypnotics and neuroleptics.". Martindale: The Extra Pharmacopoeia (30th ed.). London: Pharmaceutical Press. 1993. pp. 364–623.
5. ↑ "Future of depot neuroleptic therapy: pharmacokinetic and pharmacodynamic approaches". The Journal of Clinical Psychiatry 45 (5 Pt 2): 50–9. May 1984. PMID 6143748.
6. ↑ 6.0 6.1 "Kinetics of fluphenazine after fluphenazine dihydrochloride, enanthate and decanoate administration to man". British Journal of Clinical Pharmacology 7 (4): 325–31. April 1979. doi:10.1111/j.1365-2125.1979.tb00941.x. PMID 444352.
7. ↑ "Explaining the pharmacokinetics of fluphenazine through computer simulations. (Abstract.)". 19th Annual Midyear Clinical Meeting of the American Society of Hospital Pharmacists.. Dallas, Texas. 1984.
8. ↑ "The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug". Arzneimittel-Forschung 20 (11): 1689–98. November 1970. PMID 4992598.
9. ↑ "Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis". Drugs 33 (1): 31–49. January 1987. doi:10.2165/00003495-198733010-00002. PMID 3545764.
10. ↑ "Pharmacokinetics of haloperidol decanoate. A 2-year follow-up". International Pharmacopsychiatry 17 (4): 238–46. 1982. doi:10.1159/000468580. PMID 7185768.
11. ↑ "On the pharmacokinetics of perphenazine: a clinical study of perphenazine enanthate and decanoate.". Current Therapeutic Research 36 (6): 1071–88. 1984.

* v
* t
* e

Antipsychotics (N05A)

Typical|

* Butyrophenones: Benperidol
* Bromperidol
* Droperidol
* Haloperidol#
* Moperone
* Pipamperone
* Spiperone
* Timiperone
* Trifluperidol

* Diphenylbutylpiperidines: Fluspirilene
* Penfluridol
* Pimozide

* Phenothiazines: Acetophenazine
* Butaperazine
* Carphenazine (carfenazine)‡
* Chlorpromazine
* Cyamemazine
* Dixyrazine
* Fluphenazine
* Levomepromazine (methotrimeprazine)
* Mesoridazine
* Perazine
* Periciazine
* Perphenazine
* Piperacetazine
* Pipotiazine
* Prochlorperazine
* Promazine
* Sulforidazine
* Thiopropazate
* Thioproperazine
* Thioridazine
* Trifluoperazine
* Triflupromazine

* Thioxanthenes: Chlorprothixene
* Clopenthixol
* Flupentixol
* Tiotixene (thiothixene)
* Zuclopenthixol

Disputed|

* Benzamides: Amisulpride
* Levosulpiride
* Nemonapride
* Remoxipride‡
* Sulpiride
* Sultopride
* Tiapride
* Veralipride‡

* Butyrophenones: Melperone

* Tricyclics: Carpipramine
* Clocapramine
* Clorotepine
* Clotiapine
* Loxapine
* Mosapramine

* Others: Molindone

Atypical|

* Benzisoxazole/benzisothiazoles: Iloperidone
* Lurasidone
* Paliperidone
* Paliperidone palmitate
* Perospirone
* Risperidone#
* Ziprasidone

* Butyrophenones: Lumateperone†

* Phenylpiperazines/quinolinones: Aripiprazole
* Aripiprazole lauroxil
* Brilaroxazine†
* Brexpiprazole
* Cariprazine

* Tricyclics: Asenapine
* Clozapine#
* Olanzapine
* Quetiapine
* Zotepine

* Others: Blonanserin
* Pimavanserin
* Sertindole

Others|

* Azacyclonol
* Cannabidiol
* Oxypertine
* Reserpine
* Tetrabenazine

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

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