[Clinical pharmacokinetics of haloperidol decanoate. Comparison with other prolonged-action neuroleptics]. 1987

J C Levron, and R Ropert

Precise pharmacokinetic data of long-acting neuroleptics: apparent half life (T 1/2), time of peak plasma concentration (Tmax), bioavailability, has been a major contribution to determine optimal dosage of the drug. If the aim of the depot neuroleptic is to obtain a stable plasma concentration of the neuroleptic after I.M. injection of the ester form equivalent to that following oral administration, it is logical to obtain the same pharmacological effect; this is true for haloperidol decanoate. Mean value of T 1/2 of clopenthixol decanoate and haloperidol decanoate are 19 and 21 days, respectively, they thereby justify monthly administration. Flupenthixol decanoate and fluphenazine enanthate should be injected with dosing intervals of 3 and 1 weeks, respectively in respect with their half-lives: 17 and 4 days. Fluphenazine decanoate have a half-life of 14 days, however, the longer time the treatment, the longer the apparent half-life, suggesting to reduce the dose or to enlarge the dosing interval. Optimal dose has been determined from the bioavailability of the oral formulation and the interval between two injections, it averages 15, 20 times the oral daily dose for haloperidol decanoate. A lower conversion factor is frequently used (0.5 to 5 times) for other depot-neuroleptics such as pipotiazine palmitate, fluphenazine enanthate or decanoate; these low factors are not entirely explainable by the low bioavailability of the oral forms and produces more lower plasma concentration than after oral administration.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D003006 Clopenthixol A thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors. Cisordinol,Zuclopenthixol,alpha-Clopenthixol,alpha Clopenthixol
D003692 Delayed-Action Preparations Dosage forms of a drug that act over a period of time by controlled-release processes or technology. Controlled Release Formulation,Controlled-Release Formulation,Controlled-Release Preparation,Delayed-Action Preparation,Depot Preparation,Depot Preparations,Extended Release Formulation,Extended Release Preparation,Prolonged-Action Preparation,Prolonged-Action Preparations,Sustained Release Formulation,Sustained-Release Preparation,Sustained-Release Preparations,Timed-Release Preparation,Timed-Release Preparations,Controlled-Release Formulations,Controlled-Release Preparations,Extended Release Formulations,Extended Release Preparations,Slow Release Formulation,Sustained Release Formulations,Controlled Release Formulations,Controlled Release Preparation,Controlled Release Preparations,Delayed Action Preparation,Delayed Action Preparations,Formulation, Controlled Release,Formulations, Controlled Release,Prolonged Action Preparation,Release Formulation, Controlled,Release Formulations, Controlled,Sustained Release Preparation,Timed Release Preparation,Timed Release Preparations
D005475 Flupenthixol A thioxanthene neuroleptic that, unlike CHLORPROMAZINE, is claimed to have CNS-activating properties. It is used in the treatment of psychoses although not in excited or manic patients. (From Martindale, The Extra Pharmacopoeia, 30th ed, p595) Emergil,Fluanxol,Flupentixol,alpha-Flupenthixol,cis-Flupenthixol
D005476 Fluphenazine A phenothiazine used in the treatment of PSYCHOSES. Its properties and uses are generally similar to those of CHLORPROMAZINE. Flufenazin,Fluphenazine Hydrochloride,Lyogen,Prolixin,Hydrochloride, Fluphenazine
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D006220 Haloperidol A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279) Haldol
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D013843 Thiazines

Related Publications

J C Levron, and R Ropert
July 1986, International clinical psychopharmacology,
J C Levron, and R Ropert
February 1986, Journal of clinical psychopharmacology,
J C Levron, and R Ropert
November 1991, Journal of pharmacobio-dynamics,
J C Levron, and R Ropert
January 1976, Neurologia, neurocirugia, psiquiatria,
J C Levron, and R Ropert
January 1982, International pharmacopsychiatry,
J C Levron, and R Ropert
September 1989, The Australian and New Zealand journal of psychiatry,
J C Levron, and R Ropert
April 1992, Journal of clinical psychopharmacology,
J C Levron, and R Ropert
January 1973, Actas luso-espanolas de neurologia, psiquiatria y ciencias afines,
J C Levron, and R Ropert
May 1986, The British journal of psychiatry : the journal of mental science,
Copied contents to your clipboard!