Bioavailability of Intramuscular Versus Oral Haloperidol in Schizophrenic Patients

Schaffer, Charles B.; Shahid, Agha; Javaid, Javaid I.; Dysken, Maurice W.; Davis, John M.

doi:10.1097/00004714-198208000-00008

Cited by 29 publications

(21 citation statements)

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“…F a values were assumed to be 0.8, 0.6, and 1.0 for quinidine (Greenblatt et al, 1997), haloperidol (Schaffer et al, 1982), and ketoconazole, respectively. The value of k a can be calculated from t max and k el :t max ϭ ln(k a /k el )/(k a Ϫ k el ).…”

Section: Fig 4 Allometric Scaling Of Terminal Elimination Half-lifementioning

confidence: 99%

“…At first, values of I in,max,u for quinidine, haloperidol, and ketoconazole were estimated to be approximately 10, 0.20, and 0.35 M, respectively, based on the literature data for I max , F a , Dose, and f u for quinidine (Greenblatt et al, 1997), haloperidol (Schaffer et al, 1982), and ketoconazole (Stockly et al, 1986). Consequently, the AUC ratios were estimated to be approximately 1.3, 1.0 and 1.1 for quinidine, haloperidol, and ketoconazole, respectively.…”

Section: Fig 6 Effects Of Various Cytochrome P450 Inhibitors On Thementioning

confidence: 99%

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COMPARISON OF PREDICTION METHODS FOR IN VIVO CLEARANCE OF (S,S)-3-[3-(METHYLSULFONYL)PHENYL]-1-PROPYLPIPERIDINE HYDROCHLORIDE, A DOPAMINE D2 RECEPTOR ANTAGONIST, IN HUMANS

Yamazaki

Toth²,

Black³

et al. 2004

Drug Metab Dispos

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Section: Fig 4 Allometric Scaling Of Terminal Elimination Half-lifementioning

confidence: 99%

Section: Fig 6 Effects Of Various Cytochrome P450 Inhibitors On Thementioning

confidence: 99%

COMPARISON OF PREDICTION METHODS FOR IN VIVO CLEARANCE OF (S,S)-3-[3-(METHYLSULFONYL)PHENYL]-1-PROPYLPIPERIDINE HYDROCHLORIDE, A DOPAMINE D2 RECEPTOR ANTAGONIST, IN HUMANS

Yamazaki

Toth²,

Black³

et al. 2004

Drug Metab Dispos

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“…However, a number of studies have shown that oral administration of neuroleptics is as effective as paren teral administration [58,59]. Coffman et al [58] re ported that fluphenazine hydrochloride was equally ef fective when given orally or parenterally.…”

Section: Parenteral Administrationmentioning

confidence: 99%

Rapid Tranquilization: A Reevaluation

Solano

Sadow²,

Ananth³

1989

Neuropsychobiology

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Years of experience have indicated that the widespread and frequent use of rapid tranquilization is not based on demonstrated efficacy. Multiple high-dose administration of neuroleptics parenterally does not produce rapid relief of psychosis and, at the same time, exposes the patient to risk of severe side effects. Rapid tranquilization may only have a limited and specific applicability; therefore, it is important to reexamine its clinical indications and to search for safer alternatives.

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“…Use of orally administered atypical antipsychotics such as olanzapine and risperidone has met with some success in treating behavioral disturbances in patients with dementia (Clark et al 2001;De Deyn et al 1999;Katz et al 1999;Street et al 2000). A parenteral formulation of a second-generation antipsychotic might offer some advantage over their corresponding oral formulations due to faster onset of effect and utility where the patient cannot, or will not, accept oral treatment (Bianchetti et al 1980;Schaffer et al 1982). Rapid tranquilization with parenteral typical antipsychotic agents may induce hypotension (Marsden and Jenner 1980;Schwartz and Brotman 1992), cardiotoxicity (Lawrence and Nasraway 1997;Rao 1996), and extrapyramidal side effects (EPS) (Foster et al 1997;Salzman et al 1991), all of which are of particular concern in an elderly population because of their enhanced susceptibility to EPS (Caligiuri et al 1999).…”

mentioning

confidence: 99%

“…Oral administration of olanzapine has been shown previously to control psychotic symptoms and behavioral disturbances in elderly patients with Alzheimer's disease (Clark et al 2001;Street et al 2000), and this drug has been especially recommended for patients with dementia who exhibit "sundowning" behavior (Expert Consensus Guideline Series 1998). Intramuscular delivery of olanzapine provides a rapidly acting treatment for agitation in aggressive or hyperactive patients or those refusing oral medication, and may confer the advantages that have been reported for other parenteral formulations over their corresponding oral preparations, such as rapid onset (Dubin et al 1985;Schaffer et al 1982) and higher steady-state plasma concentrations (Kahn et al 1990;Simpson et al 1978). Treatment of agitation in the elderly necessitates a careful assessment of risk benefit.…”

mentioning

confidence: 99%

Comparison of Rapidly Acting Intramuscular Olanzapine, Lorazepam, and Placebo A Double-blind, Randomized Study in Acutely Agitated Patients with Dementia

Meehan

Wang

David

et al. 2002

Neuropsychopharmacology

167

135

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This double-blind study investigated the efficacy and safety of rapid-acting intramuscular olanzapine in treating agitation associated with Alzheimer's disease and/or vascular dementia. At 2 h, olanzapine (5.0 mg, 2.5 mg) and lorazepam (1.0 mg) showed significant improvement over placebo on the PANSS Excited Component (PANSS-EC) and Agitation-Calmness Evaluation Scale (ACES),It has been estimated that 5% of people older than 65, and up to 20% of those aged 80 and older, are affected by dementia (Gurland and Cross 1982;Small and Jarvik 1982). Of these, nearly half exhibit behavioral disturbances, such as agitation, wandering, and violent outbursts (Kunik et al. 1994). Agitation has been defined as "inappropriate verbal, vocal, or motor activity not explainable by apparent needs or confusion" (CohenMansfield 1986), and includes both physically and verbally aggressive behaviors such as hitting, biting, and From the Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana (KMM, HW, SRD, JRN, BJ, CMB, PDF, AB), Institute of Psychiatry, Medical University of South Carolina, Charleston, South Carolina (JEM), and Senior Choice Unit, Presbyterian Hospital, Oklahoma City, Oklahoma (LMB).Address correspondence to: Dr. Alan Breier, Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, Tel.: (317) Fax: (317) 433-5101. Received February 12, 2001; revised May 23, 2001; accepted September 7, 2001.Online publication: 9/13/01 at www.acnp.org/citations/Npp 091301174.N EUROPSYCHOPHARMACOLOGY 2002 -VOL . 26 , NO . 4 Rapidly Acting IM Olanzapine in Dementia 495 screaming, and nonaggressive behaviors such as pacing, wandering, and continual requests for attention. In nursing home patients with dementia, the prevalence of these disturbances may be as high as 75% (Deutsch and Rovner 1991). Severe symptoms of agitation may require rapid treatment in the form of parenteral medication when a very rapid onset is required or when patients refuse or cannot take oral agents. In some instances, the use of medication is less desirable than alternative methods such as behavioral intervention. However, occasions arise where a pharmacological intervention is unavoidable and in the best interests of the patient. Lorazepam is commonly used for treatment of acute agitation, and the benzodiazepines are currently among the few agents available in a parenteral formulation for treatment of agitation. Use of orally administered atypical antipsychotics such as olanzapine and risperidone has met with some success in treating behavioral disturbances in patients with dementia (Clark et al. 2001;De Deyn et al. 1999;Katz et al. 1999;Street et al. 2000). A parenteral formulation of a second-generation antipsychotic might offer some advantage over their corresponding oral formulations due to faster onset of effect and utility where the patient cannot, or will not, accept oral treatment (Bianchetti et al. 1980;Schaffer et al. 1982). Rapid tranquilization with parenteral...

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Bioavailability of Intramuscular Versus Oral Haloperidol in Schizophrenic Patients

Cited by 29 publications

References 0 publications

COMPARISON OF PREDICTION METHODS FOR IN VIVO CLEARANCE OF (S,S)-3-[3-(METHYLSULFONYL)PHENYL]-1-PROPYLPIPERIDINE HYDROCHLORIDE, A DOPAMINE D2 RECEPTOR ANTAGONIST, IN HUMANS

COMPARISON OF PREDICTION METHODS FOR IN VIVO CLEARANCE OF (S,S)-3-[3-(METHYLSULFONYL)PHENYL]-1-PROPYLPIPERIDINE HYDROCHLORIDE, A DOPAMINE D2 RECEPTOR ANTAGONIST, IN HUMANS

Rapid Tranquilization: A Reevaluation

Comparison of Rapidly Acting Intramuscular Olanzapine, Lorazepam, and Placebo A Double-blind, Randomized Study in Acutely Agitated Patients with Dementia

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