Interactions Between Antipsychotic and Antihypertensive Drugs

1995 ◽  
Vol 29 (6) ◽  
pp. 603-609 ◽  
Author(s):  
John S Markowitz ◽  
Barbara G Wells ◽  
William H Carson
Keyword(s):  
English Language ◽  
Antihypertensive Drugs ◽  
Case Reports ◽  
Data Extraction ◽  
Plasma Concentrations ◽  
Antihypertensive Agents ◽  
Background Information ◽  
Antipsychotic Therapy ◽  
Medline Search ◽  
Pertinent Data

Objective: To provide a comprehensive review of the pharmacokinetic and pharmacodynamic interactions between antipsychotics and antihypertensives and to provide recommendations for the selection of antihypertensives in patients receiving antipsychotic therapy. Data Sources: A MEDLINE search of the English-language literature was used to identify pertinent human and animal studies, reviews, and case reports. Study Selection: All available sources were reviewed. Data Extraction: Background information was obtained from comprehensive reviews. Individual case reports were assimilated, and pertinent data were extracted. Data Synthesis: Because hypertension is common in patients with psychiatric illness and antihypertensive agents are used for a multiplicity of indications, significant numbers of patients receive concurrent therapy with antihypertensives and antipsychotics. Many antipsychotics may block the antihypertensive efficacy of guanethidine and related drugs. The interaction between Clonidine and antipsychotics is defined less clearly. Limited data suggest possible additive hypotensive effects when chlorpromazine and methyldopa are given in combination. Increased plasma concentrations of thioridazine with a resultant increase in adverse effects have been reported when propranolol or pindolol are added to the regimen. A similar increase in chlorpromazine concentrations has been reported when propranolol was added. Although there are no reports documenting an interaction between a calcium-channel antagonist and an antipsychotic, the possible inhibition of oxidative metabolism of antipsychotics, additive calcium-blocking activity, and additive pharmacodynamic effects are theorized. Hypotension and postural syncope were reported in a patient given therapeutic dosages of chlorpromazine and Captopril, and in 2 patients when clozapine was added to enalapril therapy. Conclusions: No antipsychotic-antihypertensive combination is absolutely contraindicated, but no combination should be considered to be completely without risk. Antihypertensives with no centrally acting activity, such as diuretics, may be the least likely to result in adverse reactions. The combination of the beta-antagonists propranolol or pindolol with thioridazine or chlorpromazine should be avoided if possible. Scrupulous patient monitoring for attenuated or enhanced activity of either agent is essential whenever antipsychotics and antihypertensives are given concurrently.

Treatment Options for Rheumatoid Arthritis: Celecoxib, Leflunomide, Etanercept, and Infliximab

2000 ◽  
Vol 34 (6) ◽  
pp. 743-760 ◽  
Author(s):  
Brigitte T Luong ◽  
Barbara S Chong ◽  
Dionne M Lowder
Keyword(s):  
Rheumatoid Arthritis ◽  
English Language ◽  
Data Extraction ◽  
Treatment Options ◽  
Nonsteroidal Antiinflammatory Drugs ◽  
Antiinflammatory Drugs ◽  
Safety And Efficacy ◽  
Medline Search ◽  
Pertinent Data

OBJECTIVE: To review new pharmacologic agents approved for use in the management of rheumatoid arthritis (RA). DATA SOURCES: A MEDLINE search (1966–January 2000) was conducted to identify English-language literature available on the pharmacotherapy of RA, focusing on celecoxib, leflunomide, etanercept, and infliximab. These articles, relevant abstracts, and data provided by the manufacturers were used to collect pertinent data. STUDY SELECTION: All controlled and uncontrolled trials were reviewed. DATA EXTRACTION: Agents were reviewed with regard to mechanism of action, efficacy, drug interactions, pharmacokinetics, dosing, precautions/contraindications, adverse effects, and cost. DATA SYNTHESIS: Traditional pharmacologic treatments for RA have been limited by toxicity, loss of efficacy, or both. Increasing discoveries into the mechanisms of inflammation in RA have led to the development of new agents in hopes of addressing these limitations. With the development of celecoxib, a selective cyclooxygenase-2 inhibitor, the potential exists to minimize the gastrotoxicity associated with nonsteroidal antiinflammatory drugs. Leflunomide has been shown to be equal to or less efficacious than methotrexate, and may be beneficial as a second-line disease-modifying antirheumatic drug (DMARD). The biologic response modifiers, etanercept and infliximab, are alternatives that have shown benefit alone or in combination with methotrexate. However, they should be reserved for patients who fail to respond to DMARD therapy. Further studies should be conducted to evaluate the long-term safety and efficacy of these agents as well as their role in combination therapy. CONCLUSIONS: Celecoxib, leflunomide, etanercept, and infliximab are the newest agents approved for RA. Clinical trials have shown that these agents are beneficial in the treatment of RA; however, long-term safety and efficacy data are lacking.

Leukotriene-Receptor Antagonists and 5-Lipoxygenase Inhibitors in Asthma

1993 ◽  
Vol 27 (7-8) ◽  
pp. 898-903 ◽  
Author(s):  
Julie S. Larsen ◽  
Edward P. Acosta
Keyword(s):  
Clinical Trials ◽  
English Language ◽  
Data Extraction ◽  
Background Information ◽  
Receptor Antagonists ◽  
Lipoxygenase Inhibitors ◽  
Medline Search ◽  
Leukotriene Receptor Antagonists ◽  
Patient Tolerance ◽  
Leukotriene Receptor

OBJECTIVE: To familiarize readers with a potentially new class of compounds for treating asthma. Background information on leukotrienes is provided in addition to an indepth review of pertinent clinical trials. DATA SOURCES: Information was obtained from controlled clinical trials, abstracts, and review articles identified through a MEDLINE search of English-language articles. STUDY SELECTION: Emphasis was placed on early clinical trials that showed some benefit with these compounds as well as more recent studies using newer agents that produced more promising results. DATA EXTRACTION: Information regarding leukotriene biochemistry was extracted from basic science research and data from human studies were evaluated by the authors according to patient selection, study design, methodology, and therapeutic response. DATA SYNTHESIS: Leukotrienes have a pathophysiologic role in asthma. Two distinct but pharmacologically similar classes of leukotriene inhibitors are currently being clinically evaluated. These are leukotriene receptor antagonists and 5-lipoxygenase inhibitors. Early clinical trials with these agents yielded unfavorable results primarily because of lack of drug potency and selectivity, poor patient tolerance, and possibly the route of administration. Subsequent studies with more potent and selective agents have further implicated leukotrienes as biochemical mediators in asthma and, consequently, have shown promising clinical outcomes with respect to pulmonary function testing and patient tolerance. CONCLUSIONS: Advancements in the pathogenesis of asthma are beginning to define a role for the leukotrienes. Although more studies are needed to assess the efficacy of leukotriene inhibitors, recent clinical trials using leukotriene-receptor antagonists and 5-lipoxygenase inhibitors indicate a potential for the expansion of therapeutic regimens currently used in the treatment of asthma.

The Contact System

2002 ◽  
Vol 126 (11) ◽  
pp. 1382-1386 ◽  
Author(s):  
Craig S. Kitchens
Keyword(s):  
Antiphospholipid Syndrome ◽  
English Language ◽  
Case Reports ◽  
Data Extraction ◽  
Meta Analysis ◽  
Factor Xii ◽  
Activity Levels ◽  
Medline Search ◽  
Apparent Association

Abstract Objectives.—To review the literature for conditions, diseases, and disorders that affect activity of the contact factors, and further to review the literature for evidence that less than normal activity of any of the contact factors may be associated with thrombophilia. Data Sources.—MEDLINE search for English-language articles published from 1988 to 2001 and pertinent references contained therein, as well as search of references in recent relevant articles and reviews. Study Selection.—Relevant clinical and laboratory information was extracted from selected articles. Meta-analysis was not feasible because of heterogeneity of reports. Data Extraction and Synthesis.—Evidence for association of altered levels of the contact factors and thrombophilia was sought. A wide variety of disorders is associated with decreased activity of the contact factors; chief among these disorders are liver disease, hepatic immaturity of newborns, the antiphospholipid syndrome, and, for factor XII, being of Asian descent. These disorders are more common than homozygous deficiency. The few series and case reports of thrombophilic events in patients homozygous for deficiency of contact factors are not persuasive enough to support causality. The apparent association between levels consistent with heterozygosity (40%–60% of normal) of any of the contact factors (but especially factor XII) in persons with antiphospholipid antibodies appears to be due to falsely decreased in vitro activity levels of these factors, which are normal on antigenic testing. The apparent association with thrombosis is better explained by the antiphospholipid syndrome than by the modest reduction of the levels of contact factors. Conclusions.—Presently, it is not recommended to measure activity of contact factors during routine evaluation of patients who have suffered venous or arterial thromboembolism or acute coronary syndromes.

Isoniazid-Associated Psychosis: Case Report and Review of the Literature

1993 ◽  
Vol 27 (2) ◽  
pp. 167-170 ◽  
Author(s):  
Karen A. Pallone ◽  
Morton P. Goldman ◽  
Matthew A. Fuller
Keyword(s):  
Case Report ◽  
English Language ◽  
Case Reports ◽  
Data Extraction ◽  
Data Sources ◽  
Review Of The Literature ◽  
Data Synthesis ◽  
Medline Search ◽  
Study Selection ◽  
Language Literature

Objective To describe a case of isoniazid-associated psychosis and review the incidence of this adverse effect. Data Sources Information about the patient was obtained from the medical chart. A MEDLINE search of the English-language literature published from 1950 to 1992 was conducted and Index Medicus was manually searched for current information. Study Selection All case reports describing isoniazid-associated psychosis were reviewed. Data Extraction Studies were evaluated for the use of isoniazid, symptoms of psychosis, onset of symptoms, and dosage of isoniazid. Data Synthesis The case report is compared with others reported in the literature. The incidence of isoniazid-associated psychosis is rare. Conclusions The mechanism of isoniazid-associated psychosis is uncertain. It appears that isoniazid was associated with the psychosis evident in our patient and in the cases reviewed.

scholarly journals Medications and Micronutrients: Identifying Clinically Relevant Interactions and Addressing Nutritional Needs

2018 ◽  
Vol 34 (5) ◽  
pp. 216-230
Author(s):  
Jeffery David Prescott ◽  
Victoria Jayne Drake ◽  
Jan Frederik Stevens
Keyword(s):  
Dietary Supplement ◽  
English Language ◽  
Case Reports ◽  
Data Extraction ◽  
Dietary Supplementation ◽  
The United States ◽  
Health Care Team ◽  
Term Therapy ◽  
Nutrient Interactions ◽  
Medline Search

Objective: Prescription drug use is on the rise, and the use of dietary supplementation remains common. In the United States, more than half of all adults take a dietary supplement in any given month. As a result, drug-nutrient interactions are becoming an important consideration when pharmacists counsel patients about their drug regimens. We reviewed the literature to identify common and/or clinically relevant drug-nutrient interactions that pharmacists may encounter in practice. Data Sources: A MEDLINE search for English-language publications from 1970 through March 2017 was performed using search terms (and variations) related to drugs, medications, micronutrients, and interactions. Study Selection and Data Extraction: Relevant studies, case reports, and reviews describing drug-nutrient interactions were selected for inclusion. Data Synthesis: Some drug-nutrient interactions may result in micronutrient insufficiencies or even frank deficiencies, thereby necessitating augmentation with multivitamin/minerals or individual vitamin/mineral dietary supplements. This most often occurs with long-term therapy for chronic conditions, such as treatment with proton-pump inhibitors and histamine-2 receptor antagonists. In addition, some chronic diseases themselves, such as diabetes, may predispose patients to micronutrient insufficiencies, and dietary supplementation may be advisable. Conclusions: Drug-nutrient interactions can often be resolved through specific dosing strategies to ensure that the full effect of the medication or the dietary supplement is not compromised by the other. In rare cases, the dietary supplement may need to be discontinued or monitored during treatment. Pharmacists are in a key position to identify and discuss these drug-nutrient interactions with patients and the health care team.

Rifabutin-Associated Uveitis

1995 ◽  
Vol 29 (11) ◽  
pp. 1149-1155 ◽  
Author(s):  
Alice L Tseng ◽  
Sharon L Walmsley
Keyword(s):  
Adverse Event ◽  
Drug Interactions ◽  
English Language ◽  
Case Reports ◽  
Data Extraction ◽  
Signs And Symptoms ◽  
Medline Search ◽  
Concurrent Therapy ◽  
Study Selection ◽  
Tolerance Study

Objective: To review rifabutin-associated uveitis and discuss the mechanism and potential role of drug interactions with clarithromycin and fluconazole in contributing to this adverse event. Data Sources: A MEDLINE search (1991 through September 1994) of English-language literature using the main MeSH headings “rifabutin” and “uveitis” and the subheadings “adverse effects” and “chemically induced.” Relevant articles also were selected from references of identified articles. Abstracts from recent medical conferences of infectious diseases, pharmacology, and HIV were screened for additional data. Study Selection and Data Extraction: All articles and abstracts reporting uveitis potentially related to rifabutin were considered for inclusion. Fifty-four cases were identified. Pertinent information from the case reports, as judged by the authors, was selected and synthesized for discussion. Data Synthesis: Rifabutin is being prescribed increasingly for the treatment and prophylaxis of Mycobacterium avium complex (MAC) infection in the HIV-infected population. Uveitis was initially thought to be a rare, dose-limited complication of rifabutin therapy. In an early dose-ranging tolerance study, uveitis was associated with daily doses of 1200 mg or more. Because this toxicity appeared to be dose-related, lower dosages (300–600 mg/d) of rifabutin were selected for study in subsequent clinical trials. More recent reports noting the association of uveitis with these lower dosages of rifabutin have raised concerns about the prevalence of this adverse event. In the 54 identified cases, patients presented with symptoms of unilateral or bilateral uveitis from 2 weeks to more than 7 months following initiation of rifabutin therapy. In all reported cases, patients were receiving concurrent therapy with clarithromycin and/or fluconazole, both of which have inhibitory effects on rifabutin metabolism. In most cases, uveitis resolved within 1–2 months following discontinuation of rifabutin with or without administration of topical corticosteroids. Conclusions: Rifabutin is prescribed frequently for the prophylaxis and treatment of MAC infection, especially in patients with HIV. Uveitis is a rare, dose-related toxicity of this therapy. The risk of rifabutin-associated uveitis may be increased in patients receiving concurrent therapy with clarithromycin or fluconazole because of drug interactions. Patients receiving therapy with combinations of any of these agents should be warned about signs and symptoms of uveitis and be monitored closely for the development of rifabutin toxicity. If uveitis develops, rifabutin therapy should be discontinued promptly.

Pediatrics: Treatment of Tinea Capitis

1997 ◽  
Vol 31 (3) ◽  
pp. 338-348 ◽  
Author(s):  
Susan M Abdel-Rahman ◽  
Milap C Nahata
Keyword(s):  
Comparative Studies ◽  
Tinea Capitis ◽  
English Language ◽  
Case Reports ◽  
Data Extraction ◽  
Oral Formulation ◽  
Open Label ◽  
Medline Search ◽  
The Us ◽  
High Concentrations

Objective To review the epidemiology, pathogenesis, mycology, clinical presentation, and pharmacotherapy of tinea capitis, and describe the role of newer antimycotic agents. Data Sources A MEDLINE search restricted to English-language articles published from 1966 through 1996 and journal references were used in preparing this review. Data Extraction The data on mycology, pharmacokinetics, adverse effects, and drug interactions were obtained from controlled studies and case reports appearing in the literature. Both open-label and comparative studies were evaluated to assess the efficacy of antimycotics in the treatment of this infection. Data Synthesis Griseofulvin is the drug of choice in the treatment of tinea capitis. Newer agents with greater efficacy or shorter treatment durations continue to be explored. Ketoconazole, the first azole studied for efficacy in tinea capitis, has not demonstrated any clinical advantage over griseofulvin in several controlled clinical trials. Itraconazole is effective, but the available data are limited to case reports and a single uncontrolled study. Terbinafine similarly has shown promise in the treatment of tinea capitis, but the oral formulation was only recently approved in the US. Existing studies reflect the results in infection with pathogens not seen in the US. Both itraconazole and terbinafine achieve high concentrations in the hair and stratum corneum that persist for several weeks following drug administration. This may enable shorter courses of therapy; however, comparative studies need to be conducted in the US. Conclusions Tinea capitis remains the most common dermatophyte infection in young urban children. Oral antifungal therapy is required for effective treatment, often for several months. The combination of griseofulvin with a selenium sulfide shampoo continues to be the mainstay of therapy until more experience is gained with the newer antimycotics.

Current Issues in Onychomycosis

1998 ◽  
Vol 32 (2) ◽  
pp. 204-214 ◽  
Author(s):  
Eric F Trépanier ◽  
Guy W Amsden
Keyword(s):  
Case Reports ◽  
Data Extraction ◽  
Case Series ◽  
Cost Effective ◽  
Substantial Impact ◽  
Medline Search ◽  
Drug Of Choice ◽  
Calidad De Vida ◽  
Pertinent Data ◽  
Yeasts And Molds

OBJECTIVE: To review the epidemiology, mycology, clinical features and diagnosis, current pharmacotherapy, and pharmacoeconomics of onychomycosis. DATA SOURCES: We conducted a MEDLINE search from 1966 to May 1997. References from these articles, manufacturers of the discussed antimycotics, and relevant abstracts from recent dermatology conferences were used to collect pertinent data. DATA EXTRACTION: Data were obtained from published controlled studies and case reports. In the pharmacotherapy section, the most weight was placed on fully reported, randomized, controlled comparative trials, but abstracts and case series were included when well-controlled studies were unavailable. DATA SYNTHESIS: Onychomycosis is a common nail disorder that has a substantial impact on patients' quality of life. It is most commonly caused by dermatophytes, but yeasts and molds can also be involved. Diagnosis is made through clinical presentation, potassium hydroxide preparations, and culture of tissue/nail samples. Griseofulvin was the drug of choice for many years, but its low cure rates and the development of newer, more effective drugs made it fall out of favor. Current therapeutic alternatives include fluconazole, itraconazole, and terbinafine. Data on the use of fluconazole are limited to case series and reports. Continuous dosing of itraconazole and terbinafine are well-proven therapies. New data are becoming available on the use of pulse itraconazole dosing, which has recently been approved by the Food and Drug Administration for fingernail infections. These drugs are well tolerated, but attention to drug interactions is necessary with the azoles. CONCLUSIONS: Currently, continuous terbinafine appears to be the most cost-effective drug for dermatophyte onychomycosis. OBJETIVO: Repasar la epidemiología, micología, características clínicas y diagnóstico, farmacoterapia actual, y farmacoeconomía de onicomicosis. FUENTES DE INFORMACIÓN: Se realizó una búsqueda en MEDLINE del 1966 al 1997. Referencias de estos artículos, compañías manufactureras de los antimicóticos discutidos y extractos relevantes de conferencias dermatológicas recientes fueron usados para recoger datos pertinentes. MÉTODOS DE EXTRACCIÓN DE INFORMACIÓN: Los datos fueron obtenidos de estudio controlados y casos reportados publicados. En la sección de farmacoterapia, se dió más importancia a estudios comparativos, controlados, aleatorios, reportados completamente, pero extractos y series de casos fueron descritos cuando estudios bien controlados no estuvieron disponibles. SÍNTESIS: Onicomicosis es un desorden de las uñas común que tiene un impacto sustancial en la calidad de vida de pacientes. Es ocasionada más comúnmente por dermatófitos, pero hongos y mohos también pueden estar envueltos. El diagnóstico se hace a través de la presentación clínica, preparaciones de hidróxido de potasio y cultivo de muestras de tejido/uñas. Griseofulvina fue el fármaco de selección por muchos años, pero su baja proporción de curación y el desarrollo de fármacos nuevos más efectivos ha ocasionado su falta de uso. Alternativas terapéuticas incluyen fluconazol, itraconazol, y terbinafina. La información sobre el uso de fluconazol está limitada a series de casos y reportes. La dosificación continua de itraconazol y terbinafina son tratamientos bien comprobados. Recientemente la Administración de Drogas y Alimentes aprobó el uso de la dosificación de itraconazol en pulso para infecciones de las uñas, y nueva información sobre este uso está siendo disponible. Estos fármacos son bien tolerados pero es necesario prestar atención a las interacciones de fármacos con los azoles. CONCLUSIONES: Al presente, terbinafina en administración continua parece ser el fármaco más costo-efectivo de selección para onicomicosis por dermatófitos. OBJECTIF: Revoir les caractéristiques épidémiologiques, mycologiques, cliniques, et diagnostiques, ainsi que le traitement courant, et les particularités pharmacoéconomiques des mycoses des ongles. SOURCE DINFORMATION: Une recherche informatisée sur MEDLINE a été complétée afin d'identifier la littérature pertinente entre les années 1966 et 1997. On a aussi sondé les références des articles identifiés, les compagnies pharmaceutiques qui produisent les agents antifongiques discutés, ainsi que les abstraits récemment présentes aux conférences dermatologiques. SELECTION D'ETUDES ET DES DONNEES: On a obtenu les données à partir de publications d'études contrôlées et d'observations écrites. Dans la section de la pharmacothérapie, on a mis plus d'emphase sur les études comparatives randomisées et contrôlées. Mais les abstraits et les observations écrites ont été utilisés lorsqu'il n'y avait pas d'études contrôlées. RÉSUMÉ: L'onychomycose est une maladie commune qui a un effet significatif sur la qualité de vie des patients. Le plus fréquemment, elle est causée par des dermatophytes mais les levures peuvent être impliqués. La diagnose est faite à partir de la présentation clinique, avec des préparations d'hydroxide de potassium et des cultures de tissu et des ongles. Malgré que la griséofulvine a été utilisée pour plusieurs années, son efficacité limitée et le développement d'agents nouveaux plus efficaces, ont diminué son utilisation. Le fluconazole, l'itraconazole, et la terbinafine sont des alternatives thérapeutiques. Il n'existe que des observations écrites qui décrivent l'efficacité du fluconazole. L'administration continue de l'itraconazole et de la terbinafine est d'ailleurs bien documentee. Il y a de nouvelles données sur la thérapie intermittente par l'itraconazole, cette méthode d'administration de l'itraconazole a été récemment approuvée par le FDA pour les infections fongiques des ongles. Ces médicaments sont bien tolérés, mais, avec les azoles, l'on doit faire attention aux interactions avec d'autres médicaments. CONCLUSIONS: Présentement, il semble que la terbinafine est le médicament le plus cost-effective pour le traitement des onychomycoses à dermatophytes.

Beyond Benzodiazepines: Alternative Pharmacologic Agents for the Treatment of Insomnia

1998 ◽  
Vol 32 (6) ◽  
pp. 680-691 ◽  
Author(s):  
Judy Wagner ◽  
Mary L Wagner ◽  
Wayne A Hening
Keyword(s):  
Clinical Trials ◽  
Case Reports ◽  
Data Extraction ◽  
Benzodiazepine Receptor ◽  
Background Information ◽  
Comparable Efficacy ◽  
Pharmacologic Therapy ◽  
Safety And Efficacy ◽  
Medline Search ◽  
Review Articles

OBJECTIVE: To review the epidemiology, etiology, and classification of insomnia and provide an overview of the pharmacologic therapy of insomnia. Novel nonbenzodiazepine hypnotics including zolpidem, zopiclone, and zaleplon, as well as nonprescription products such as valerian and melatonin, are reviewed in detail. DATA SOURCES: A MEDLINE search was performed to identify relevant clinical studies, case reports, abstracts, and review articles published between April 1992 and December 1997. Key search terms included insomnia, benzodiazepines, zolpidem, zopiclone, zaleplon, Cl 284,846, melatonin, and valerian. Additional references were obtained from the lists of review articles and textbooks. DATA EXTRACTION AND SYNTHESIS: Data concerning the safety and efficacy of the hypnotic agents were extracted from all available clinical trials and abstracts. Background information regarding insomnia, benzodiazepines, and other hypnotics was extracted from the most current literature, including review articles and textbooks. CONCLUSIONS: New developments in benzodiazepine receptor pharmacology have introduced novel nonbenzodiazepine hypnotics that provide comparable efficacy to benzodiazepines. Although they may possess theoretical advantages over benzodiazepines based on their unique pharmacologic profiles, they offer few, if any, significant advantages in terms of adverse effects. Over-the-counter agents such as valerian and melatonin may be useful in alleviating mild, short-term insomnia, but further clinical trials are required to fully evaluate their safety and efficacy.

Stereoselective Pharmacokinetics and Pharmacodynamics of Anti-Asthma Agents

2002 ◽  
Vol 36 (4) ◽  
pp. 693-701 ◽  
Author(s):  
Majid Vakily ◽  
Reza Mehvar ◽  
Dion Brocks
Keyword(s):  
English Language ◽  
Data Extraction ◽  
Plasma Concentrations ◽  
Volume Of Distribution ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Chiral Drugs ◽  
Medline Search ◽  
Secondary Sources ◽  
Asthmatic Patients ◽  
Stereoselective Pharmacokinetics

OBJECTIVE: To review the previously published studies on pharmacokinetics and pharmacodynamics of chiral drugs used in the treatment of asthma. DATA SOURCES: Primary and review articles were identified with a MEDLINE search (1980–May 2001) and through secondary sources. STUDY SELECTION AND DATA EXTRACTION: All English-language studies and reviews obtained from the MEDLINE search pertaining to stereoselective pharmacokinetics and pharmacodynamics of chiral anti-asthma drugs were assessed. DATA SYNTHESIS: Several anti-asthma drugs (e.g., β2-adrenergic agonists, leukotriene modifiers) are chiral and marketed as racemates, which consist of equal proportions of 2 enantiomers. Significant stereoselectivity has also been reported in pharmacodynamics and pharmacokinetics of the β2-agonists. The enantiomers of β2-agonists in the R configuration are primarily responsible for the bronchodilating effects of the racemate. The plasma concentrations of the enantiomers of anti-asthma drugs may differ as a reflection of stereoselectivity in clearance, volume of distribution, and route of administration. CONCLUSIONS: Stereoselectivity in the pharmacokinetics of anti-asthma drugs may complicate the relationship between dose and/or plasma concentration of racemic drug versus effect relationship. An appreciation of the stereoselective pharmacokinetics and pharmacodynamics of chiral anti-asthma drugs may optimize the use of these agents in asthmatic patients.

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