| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| Targets |
D2 Receptor
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|---|---|
| ln Vitro |
Haloperidol decanoate is an organic molecular entity.
Haloperidol Decanoate is the decanoate ester of haloperidol, a phenylbutylpiperadine derivative with antipsychotic, neuroleptic and antiemetic effects. Haloperidol competitively blocks postsynaptic dopamine (D2) receptors in the mesolimbic system of the brain leading to anti-delusionary and anti-hallucinogenic effects. The antagonistic activity mediated through D2 dopamine receptors in the chemoreceptive trigger zone (CTZ) account for its antiemetic activity.
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| ln Vivo |
Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. Haloperidol decanoate has no intrinsic activity: its pharmacodynamic actions are those of haloperidol--primarily that of central antidopamine activity. The monthly administered depot formulation has several clinical and practical advantages over oral haloperidol: better compliance and more predictable absorption; more controlled plasma concentrations; fewer extrapyramidal side effects; less frequent reminders of condition; and reduced medical workload. In open and controlled studies, haloperidol decanoate has produced adequate maintenance or improvement of the condition of patients with psychoses (mainly schizophrenia) when an abrupt change from orally administered haloperidol or other antipsychotic drugs has been instituted. Limited comparative studies indicate that the depot and oral forms of haloperidol are equally effective, and that haloperidol decanoate is at least as effective as depot forms of fluphenazine, pipothiazine, flupenthixol and perphenazine in controlling the symptoms of psychosis. Extrapyramidal side effects and the need for concomitant anti-Parkinsonian drugs may be a problem, but may be less frequent than with oral haloperidol or other depot antipsychotics. Thus, haloperidol decanoate offers a useful alternative in the treatment of psychoses to orally administered haloperidol or to other depot antipsychotic drugs[1].
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| Toxicity/Toxicokinetics |
women TDLo intravenous 11600 ug/kg/4D CARDIAC: ARRHYTHMIAS (INCLUDING CHANGES IN CONDUCTION); CARDIAC: EKG CHANGES NOT DIAGNOSTIC OF ABOVE; CARDIAC: CHANGE IN RATE Annals of Internal Medicine., 119(391), 1993 [PMID:8338292]
rat LD50 oral 1717 mg/kg SENSE ORGANS AND SPECIAL SENSES: LACRIMATION: EYE; SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE; BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) Kiso to Rinsho. Clinical Report., 19(6731), 1985 rat LD50 intraperitoneal 328 mg/kg SENSE ORGANS AND SPECIAL SENSES: LACRIMATION: EYE; SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE; BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) Kiso to Rinsho. Clinical Report., 19(6731), 1985 rat LD50 subcutaneous 780 mg/kg SENSE ORGANS AND SPECIAL SENSES: LACRIMATION: EYE; SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE; BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) Kiso to Rinsho. Clinical Report., 19(6731), 1985 rat LD50 intramuscular >1525 mg/kg SENSE ORGANS AND SPECIAL SENSES: LACRIMATION: EYE; SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE; BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) Kiso to Rinsho. Clinical Report., 19(6731), 1985 |
| References |
[1]. Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis. Drugs. 1987 Jan;33(1):31-49.
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| Additional Infomation |
Haloperidol decanoate is an organic molecular entity.
Haloperidol Decanoate is the decanoate ester of haloperidol, a phenylbutylpiperadine derivative with antipsychotic, neuroleptic and antiemetic effects. Haloperidol competitively blocks postsynaptic dopamine (D2) receptors in the mesolimbic system of the brain leading to anti-delusionary and anti-hallucinogenic effects. The antagonistic activity mediated through D2 dopamine receptors in the chemoreceptive trigger zone (CTZ) account for its antiemetic activity. See also: Haloperidol (has active moiety). |
| Molecular Formula |
C31H41CLFNO3
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|---|---|
| Molecular Weight |
530.11
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| Exact Mass |
529.276
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| Elemental Analysis |
C, 70.24; H, 7.80; Cl, 6.69; F, 3.58; N, 2.64; O, 9.05
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| CAS # |
74050-97-8
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| PubChem CID |
52919
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| Appearance |
Typically exists as White to off-white solid at room temperature
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| Density |
1.14 g/cm3
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| Boiling Point |
615.5ºC at 760 mmHg
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| Melting Point |
326.1ºC
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| Flash Point |
326.1ºC
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| Index of Refraction |
1.554
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| LogP |
8.055
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
37
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| Complexity |
665
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCCCC(OC1(C2C=CC(Cl)=CC=2)CCN(CCCC(C2C=CC(F)=CC=2)=O)CC1)=O
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| InChi Key |
GUTXTARXLVFHDK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H41ClFNO3/c1-2-3-4-5-6-7-8-11-30(36)37-31(26-14-16-27(32)17-15-26)20-23-34(24-21-31)22-9-10-29(35)25-12-18-28(33)19-13-25/h12-19H,2-11,20-24H2,1H3
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| Chemical Name |
[4-(4-chlorophenyl)-1-[4-(4-fluorophenyl)-4-oxobutyl]piperidin-4-yl] decanoate
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| Synonyms |
HALOPERIDOL DECANOATE; 74050-97-8; Halomonth; Haldol decanoate; Haldol decanoas; Depot haloperidol; Haloperidol depot; KD 16;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~188.64 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8864 mL | 9.4320 mL | 18.8640 mL | |
| 5 mM | 0.3773 mL | 1.8864 mL | 3.7728 mL | |
| 10 mM | 0.1886 mL | 0.9432 mL | 1.8864 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00947375 | TERMINATED | Drug: Lamictal TM Drug: Haloperidol Decanoate |
Schizophrenia | Central Mental Clinic for Outpatients of Baku City | 2005-01 | Phase 4 |
| NCT05995457 | NOT YET RECRUITING | Other: Intramuscular injection of Haloperidol decanoate using the "Z-track" and "Airlock" techniques Other: Intramuscular injection of Haloperidol decanoate using standard techniques |
Schizophrenia; Psychosis | Centre Hospitalier St Anne/td> | 2023-09-01 | Not Applicable |
| NCT00018642 | COMPLETED | Drug: quetiapine Drug: haloperidol decanoate |
Schizoaffective Disorder Schizophrenia |
US Department of Veterans Affairs | 1997-04 | Not Applicable |
| NCT01174290 | COMPLETED | Drug: Haloperidol decanoate Drug: Placebo |
Subsyndromal Delirium | Northeastern University | 2010-09 | Phase 4 |
| NCT04327843 | COMPLETEDWITH RESULTS | Behavioral: Customized Adherence Enhancement Drug: Haloperidol Decanoate |
Medication Nonadherence Schizo Affective Disorder Schizophrenia |
Case Western Reserve University | 2019-11-05 | Phase 3 |
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