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Typical antipsychotic medication From Wikipedia, the free encyclopedia
Fluphenazine, sold under the brand name Prolixin among others, is a high-potency typical antipsychotic medication.[2] It is used in the treatment of chronic psychoses such as schizophrenia,[2][3] and appears to be about equal in effectiveness to low-potency antipsychotics like chlorpromazine.[4] It is given by mouth, injection into a muscle, or just under the skin.[2] There is also a long acting injectable version that may last for up to four weeks.[2] Fluphenazine decanoate, the depot injection form of fluphenazine, should not be used by people with severe depression.[5]
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Clinical data | |
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Trade names | Prolixin, Modecate, Moditen others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682172 |
License data |
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Pregnancy category |
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Routes of administration | By mouth, Intramuscular injection, depot injection (fluphenazine decanoate) |
Drug class | Typical antipsychotic |
ATC code | |
Legal status | |
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Pharmacokinetic data | |
Bioavailability | 2.7% (by mouth) |
Metabolism | unclear[2] |
Elimination half-life | IM 15 hours (HCL), 7–10 days (decanoate)[2] |
Excretion | Urine, feces |
Identifiers | |
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CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.000.639 |
Chemical and physical data | |
Formula | C22H26F3N3OS |
Molar mass | 437.53 g·mol−1 |
3D model (JSmol) | |
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Common side effects include movement problems, sleepiness, depression and increased weight.[2] Serious side effects may include neuroleptic malignant syndrome, low white blood cell levels, and the potentially permanent movement disorder tardive dyskinesia.[2] In older people with psychosis as a result of dementia it may increase the risk of dying.[2] It may also increase prolactin levels which may result in milk production, enlarged breasts in males, impotence, and the absence of menstrual periods.[2] It is unclear if it is safe for use in pregnancy.[2]
Fluphenazine is a typical antipsychotic of the phenothiazine class.[2] Its mechanism of action is not entirely clear but believed to be related to its ability to block dopamine receptors.[2] In up to 40% of those on long term phenothiazines, liver function tests become mildly abnormal.[6]
Fluphenazine came into use in 1959.[7] The injectable form is on the World Health Organization's List of Essential Medicines.[8] It is available as a generic medication.[2] It was discontinued in Australia in 2017.[9]
A 2018 Cochrane review found that fluphenazine was an imperfect treatment and other inexpensive drugs less associated with side effects may be an equally effective choice for people with schizophrenia.[10]
The British National Formulary recommends a gradual withdrawal when discontinuing antipsychotics to avoid acute withdrawal syndrome or rapid relapse.[11] Symptoms of withdrawal commonly include nausea, vomiting, and loss of appetite.[12] Other symptoms may include restlessness, increased sweating, and trouble sleeping.[12] Less commonly there may be a feeling of the world spinning, numbness, or muscle pains.[12] Symptoms generally resolve after a short period of time.[12]
There is tentative evidence that discontinuation of antipsychotics can result in psychosis.[13] It may also result in reoccurrence of the condition that is being treated.[14] Rarely tardive dyskinesia can occur when the medication is stopped.[12]
Fluphenazine acts primarily by blocking post-synaptic dopaminergic D2 receptors in the basal ganglia, cortical and limbic system. It also blocks α1 adrenergic receptors, muscarinic M1 receptors, and histaminergic H1 receptors.[15][16]
Site | Ki (nM) | Action | Ref |
---|---|---|---|
5-HT1A | 145–2829 | ND | [17] |
5-HT1B | 334 | ND | [17] |
5-HT1D | 334 | ND | [17] |
5-HT1E | 540 | ND | [17] |
5-HT2A | 3.8–98 | ND | [17] |
5-HT2B | ND | ND | [17] |
5-HT2C | 174–2,570 | ND | [17] |
5-HT3 | 4,265– >10,000 | ND | [17] |
5-HT5A | 145 | ND | [17] |
5-HT6 | 7.9–38 | ND | [17] |
5-HT7 | 8 | ND | [17] |
D1 | 14.45 | ND | [17] |
D2 | 0.89 | ND | |
D2L | ND | [17] | |
D3 | 1.412 | ND | [17] |
D4 | 89.12 | ND | [17] |
D5 | 95–2,590 | ND | [17] |
α1A | 6.4–9 | ND | [17] |
α1B | 13 | ND | [17] |
α2A | 304–314 | ND | [17] |
α2B | 181.6–320 | ND | [17] |
α2C | 28.8–122 | ND | [17] |
β1 | >10,000 | ND | [17] |
β2 | >10,000 | ND | [17] |
H1 | 7.3–70 | ND | [17] |
H2 | 560 | ND | [17] |
H3 | 1,000 | ND | [17] |
H4 | >10,000 | ND | [17] |
M1 | 1,095-3,235.93 | ND | [17] |
M2 | 2,187.76–7,163 | ND | [17] |
M3 | 1441–1445.4 | ND | [17] |
M4 | 5,321 | ND | [17] |
M5 | 357 | ND | [17] |
SERT | ND | ND | [17] |
NET | ND | ND | [17] |
DAT | ND | ND | [17] |
NMDA (PCP) | ND | ND | [17] |
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. All data are for human cloned proteins, except 5-HT3 (rat), D4 (human/rat), H3 (guinea pig), and NMDA/PCP (rat).[17] |
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 | [18] |
Clopentixol decanoate | Sordinol Depot | Typical | Viscoleob | 50–600 mg/1–4 weeks | 4–7 days | ? | 19 days | 9.0 | [19] |
Flupentixol decanoate | Depixol | Typical | Viscoleob | 10–200 mg/2–4 weeks | 4–10 days | 8 days | 17 days | 7.2–9.2 | [19][20] |
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 | [21][22][23] |
Fluphenazine enanthate | Prolixin Enanthate | Typical | Sesame oil | 12.5–100 mg/1–4 weeks | 2–3 days | 4 days | ? | 6.4–7.4 | [22] |
Fluspirilene | Imap, Redeptin | Typical | Watera | 2–12 mg/1 week | 1–8 days | 7 days | ? | 5.2–5.8 | [24] |
Haloperidol decanoate | Haldol Decanoate | Typical | Sesame oil | 20–400 mg/2–4 weeks | 3–9 days | 18–21 days | 7.2–7.9 | [25][26] | |
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 | [27] |
Pipotiazine palmitate | Piportil Longum | Typical | Viscoleob | 25–400 mg/4 weeks | 9–10 days | ? | 14–21 days | 8.5–11.6 | [20] |
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. |
Fluphenazine came into use in 1959.[7]
The injectable form is on the World Health Organization's List of Essential Medicines.[8] It is available as a generic medication.[2] It was discontinued in Australia in 2017.[9]
In horses, it is sometimes given by injection as an anxiety-relieving medication, though there are many negative common side effects and it is forbidden by many equestrian competition organizations.[28]
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