Fluspirilene (Redeptin, Imap, R6218) is a diphenylbutylpiperidine typical antipsychotic drug, used for the treatment of schizophrenia.[1] It is administered intramuscularly.[2] It was discovered at Janssen Pharmaceutica in 1963.[3] A 2007 systematic review investigated the efficacy of fluspirilene decanoate for people with schizophrenia:
Fluspirilene decanoate compared to oral antipsychotics[4]
Summary
Participant numbers in each comparison were small so power to identify clear difference is limited. Randomized controlled trial data identified no clear differences between the long-acting injection of fluspirilene and oral medication for outcomes that include adverse effects.[4]
Outcome
Findings in words
Findings in numbers
Quality of evidence
Global outcome
Leaving the study early Follow up: 6 weeks to 5 months
Fluspirilene decanoate may increase the risk of leaving the study (reasons not specified), but, the difference is not clear between people given fluspirilene decanoate and those receiving oral antipsychotics. These findings are based on data of low quality.
RR 1.18 (0.08 to 16.78)
Low
Mental state
Relapse Follow up: 6 weeks to 5 months
Using the depot, long-acting fluspirilene decanoate makes little difference for the outcome of 'relapse' compared with those receiving oral antipsychotics - at least for those willing to be engaged with trials. These findings are based on data of low quality.
RR 1.18 (0.08 to 16.78)
Low
Adverse effects
Needing anticholinergic drugs Follow up: 6 weeks to 5 months
The depot fluspirilene decanoate does not seem to cause any more movement disorders - for which anticholinergic drugs are used - compared with oral antipsychotics. These findings are based on data of low quality.
RR 0.07 (0.00 to 1.07)
Low
Dizziness
Fluspirilene decanoate may reduce the chance of experiencing dizziness compared with the oral antipsycotics. Data are based on low quality evidence.
RR 0.59 (0.37 to 0.95)
Low
Missing outcomes
Data on quality of life, and service use (e.g. hospitalization) were not reported in trials.
v
t
e
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
[5]
Clopentixol decanoate
Sordinol Depot
Typical
Viscoleob
50–600 mg/1–4 weeks
4–7 days
?
19 days
9.0
[6]
Flupentixol decanoate
Depixol
Typical
Viscoleob
10–200 mg/2–4 weeks
4–10 days
8 days
17 days
7.2–9.2
[6][7]
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
[8][9][10]
Fluphenazine enanthate
Prolixin Enanthate
Typical
Sesame oil
12.5–100 mg/1–4 weeks
2–3 days
4 days
?
6.4–7.4
[9]
Fluspirilene
Imap, Redeptin
Typical
Watera
2–12 mg/1 week
1–8 days
7 days
?
5.2–5.8
[11]
Haloperidol decanoate
Haldol Decanoate
Typical
Sesame oil
20–400 mg/2–4 weeks
3–9 days
18–21 days
7.2–7.9
[12][13]
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
[14]
Pipotiazine palmitate
Piportil Longum
Typical
Viscoleob
25–400 mg/4 weeks
9–10 days
?
14–21 days
8.5–11.6
[7]
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.
^van Epen JH (1970). "Experience with fluspirilene (R 6218), a long-acting neuroleptic". Psychiatr Neurol Neurochir. 73 (4): 277–284. PMID 5478771.
^Janssen PA, Niemegeers CJ, Schellekens KH, Lenaerts FM, Verbruggen FJ, van Nueten JM, Marsboom RH, Hérin VV, Schaper WK (1970). "The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug". Arzneimittelforschung. 20 (11): 1689–1698. PMID 4992598.
^BE 633914, issued 1963, assigned to C. Janssen, NV Res. Lab.
^ abAbhijnhan A, Adams CE, David A, Ozbilen M (January 2007). "Depot fluspirilene for schizophrenia". The Cochrane Database of Systematic Reviews. 2007 (1): CD001718. doi:10.1002/14651858.CD001718.pub2. PMC 7025783. PMID 17253464.
^Parent M, Toussaint C, Gilson H (1983). "Long-term treatment of chronic psychotics with bromperidol decanoate: clinical and pharmacokinetic evaluation". Current Therapeutic Research. 34 (1): 1–6.
^ abJørgensen A, Overø KF (1980). "Clopenthixol and flupenthixol depot preparations in outpatient schizophrenics. III. Serum levels". Acta Psychiatrica Scandinavica. Supplementum. 279: 41–54. doi:10.1111/j.1600-0447.1980.tb07082.x. PMID 6931472.
^ abReynolds JE (1993). "Anxiolytic sedatives, hypnotics and neuroleptics.". Martindale: The Extra Pharmacopoeia (30th ed.). London: Pharmaceutical Press. pp. 364–623.
^Ereshefsky L, Saklad SR, Jann MW, Davis CM, Richards A, Seidel DR (May 1984). "Future of depot neuroleptic therapy: pharmacokinetic and pharmacodynamic approaches". The Journal of Clinical Psychiatry. 45 (5 Pt 2): 50–9. PMID 6143748.
^ abCurry SH, Whelpton R, de Schepper PJ, Vranckx S, Schiff AA (April 1979). "Kinetics of fluphenazine after fluphenazine dihydrochloride, enanthate and decanoate administration to man". British Journal of Clinical Pharmacology. 7 (4): 325–31. doi:10.1111/j.1365-2125.1979.tb00941.x. PMC 1429660. PMID 444352.
^Young D, Ereshefsky L, Saklad SR, Jann MW, Garcia N (1984). Explaining the pharmacokinetics of fluphenazine through computer simulations. (Abstract.). 19th Annual Midyear Clinical Meeting of the American Society of Hospital Pharmacists. Dallas, Texas.
^Janssen PA, Niemegeers CJ, Schellekens KH, Lenaerts FM, Verbruggen FJ, van Nueten JM, Marsboom RH, Hérin VV, Schaper WK (November 1970). "The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug". Arzneimittel-Forschung. 20 (11): 1689–98. PMID 4992598.
^Beresford R, Ward A (January 1987). "Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis". Drugs. 33 (1): 31–49. doi:10.2165/00003495-198733010-00002. PMID 3545764.
^Reyntigens AJ, Heykants JJ, Woestenborghs RJ, Gelders YG, Aerts TJ (1982). "Pharmacokinetics of haloperidol decanoate. A 2-year follow-up". International Pharmacopsychiatry. 17 (4): 238–46. doi:10.1159/000468580. PMID 7185768.
^Larsson M, Axelsson R, Forsman A (1984). "On the pharmacokinetics of perphenazine: a clinical study of perphenazine enanthate and decanoate". Current Therapeutic Research. 36 (6): 1071–88.
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