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PubMed1984

Rate dependency, behavioral mechanisms, and behavioral pharmacology.

Behavioral pharmacology has become increasingly independent of the experimental analysis of behavior. At its beginning, behavioral pharmacology was closely related to the experimental analysis of behavior, with developments in each field aiding the other. Early attempts to systematize data in behavioral pharmacology culminated with the development of the rate-dependency concept, but as this principle was found to have more limited generality than originally was hoped, a theoretical void developed. This circumstance was followed by increased reliance on pharmacological theory as a basis for experimentation and interpretation, with an attendant decrease in emphasis on environmental variables and behavioral interpretations. Lack of interplay between behavioral pharmacology and the experimental analysis of behavior is detrimental to both disciplines because each could contribute significantly to the other. The current trend might be reversed if more research were directed at elucidating behavioral mechanisms of drug action.

Animals↗
PubMed2002

Pharmacological strategies to decrease transfusion requirements in patients undergoing surgery.

Surgical procedures are inevitably associated with bleeding. The amount of blood loss may vary widely between different surgical procedures and depends on surgical as well as non-surgical factors. Whereas adequate surgical haemostasis may suffice in most patients, pro-haemostatic pharmacological agents may be of additional benefit in patients with (diffuse) surgical bleeding or in patients with a specific underlying haemostatic defect. In general, surgical haemostasis and pharmacological therapies can be complementary in controlling blood loss. The use of pharmacological therapies to reduce blood loss and blood transfusions in surgery has historically been restricted to a few drugs. Antifibrinolytic agents (aprotinin, tranexamic acid and aminocaproic acid) have the best evidence supporting their use, especially in cardiac surgery, liver transplantation and some orthopaedic surgical procedures. Meta-analyses of randomised, controlled trials in cardiac patients have suggested a slight benefit of aprotinin, compared with the other antifibrinolytics. Desmopressin is the treatment of choice in patients with mild haemophilia A and von Willebrand disease. It has also been shown to be effective in patients undergoing cardiac surgery who received aspirin up to the time of operation. However, overall evidence does not support a beneficial effect of desmopressin in patients without pre-existing coagulopathy undergoing elective surgical procedures. Topical agents, such as fibrin sealants have been successfully used in a variety of surgical procedures. However, only very few controlled clinical trials have been performed and scientific evidence supporting their use is still limited. Novel drugs, like recombinant factor VIIa (eptacog alfa), are currently under clinical investigation. Recombinant factor VIIa has been introduced for the treatment of haemophilia patients with inhibitors, either in surgical or non-surgical situations. Preliminary data indicate that it may also be effective in surgical patients without pre-existing coagulation abnormalities. More clinical trials are warranted before definitive conclusions can be drawn about the safety and the exact role of this new drug in surgical patients. Only adequately powered and properly designed randomised, clinical trials will allow us to define the most effective and the safest pharmacological therapies for reducing blood loss and transfusion requirements in surgical patients. Future trials should also consider cost-effectiveness because of considerable differences in the costs of the available pro-haemostatic pharmacological agents.

Administration, Topical↗
PubMed2004

Pharmacological cardioversion of atrial fibrillation: current management and treatment options.

Atrial fibrillation (AF) is the most common form of arrhythmia, carrying high social costs. It is usually first seen by general practitioners or in emergency departments. Despite the availability of consensus guidelines, considerable variations exist in treatment practice, especially outside specialised cardiological settings. Cardioversion to sinus rhythm aims to: (i) restore the atrial contribution to ventricular filling/output; (ii) regularise ventricular rate; and (iii) interrupt atrial remodelling. Cardioversion always requires careful assessment of potential proarrhythmic and thromboembolic risks, and this translates into the need to personalise treatment decisions. Among the many clinical variables that affect strategy selection, time from onset is crucial. In selected patients, pharmacological cardioversion of recent-onset AF can be a safely used, feasible and effective approach, even in internal medicine and emergency departments. In most cases of recent-onset AF, pharmacological cardioversion provides an important--and probably more cost effective--alternative to electrical cardioversion, which can then be employed as a second-line therapy for nonresponders. Class IC agents (flecainide or propafenone), which can be safely used in hospitalised patients with recent-onset AF without left ventricular dysfunction, can provide rapid conversion to sinus rhythm after either intravenous administration or oral loading. Although intravenous amiodarone requires longer conversion times, it is still the standard treatment for patients with heart failure. Ibutilide also provides good conversion rates and could be used for AF patients with left ventricular dysfunction (were it not for high costs). For long-lasting AF most pharmacological treatments have only limited efficacy and electrical cardioversion remains the gold standard in this setting. However, a widely used strategy involves pretreatment with amiodarone in the weeks before planned electrical cardioversion: this provides optimal prophylaxis and can sometimes even restore sinus rhythm. Dofetilide may also be capable of restoring sinus rhythm in up to 25-30% of patients and can be used in patients with heart failure. The potential risk of proarrhythmia increases the need for careful therapeutic decision making and management of pharmacological cardioversion. The results of recent trials (AFFIRM [Atrial Fibrillation Follow-up Investigation of Rhythm Management] and RACE [Rate Control versus Electrical Cardioversion for Persistent Atrial Fibrillation]) on rate versus rhythm control strategies in the long term have led to a generalised shift in interest towards rate control. Although carefully designed studies are required to better define the role of pharmacological rhythm control in specific AF settings, this alternative option remains a recommendable strategy for many patients, especially those in acute care.

Anti-Arrhythmia Agents↗
PubMed2000

GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects.

In the mid seventies a drug design programme using the Amanita muscaria constituent muscimol (7) as a lead structure, led to the design of guvacine (23) and (R)-nipecotic acid (24) as specific GABA uptake inhibitors and the isomeric compounds isoguvacine (10) and isonipecotic acid (11) as specific GABAA receptor agonists. The availability of these compounds made it possible to study the pharmacology of the GABA uptake systems and the GABAA receptors separately. Based on extensive cellular and molecular pharmacological studies using 23, 24, and a number of mono- and bicyclic analogues, it has been demonstrated that neuronal and glial GABA transport mechanisms have dissimilar substrate specificities. With GABA transport mechanisms as pharmacological targets, strategies for pharmacological interventions with the purpose of stimulating GABA neurotransmission seem to be (1) effective blockade of neuronal as well as glial GABA uptake in order to enhance the inhibitory effects of synaptically released GABA, or (2) selective blockade of glial GABA uptake in order to increase the amount of GABA taken up into, and subsequently released from, nerve terminals. The bicyclic compound (R)-N-Me-exo-THPO (17) has recently been reported as the most selective glial GABA uptake inhibitor so far known and may be a useful tool for further elucidation of the pharmacology of GABA transporters. In recent years, a variety of lipophilic analogues of the amino acids 23 and 24 have been developed, and one of these compounds, tiagabine (49) containing (R)-nipecotic acid (24) as the GABA transport carrier-recognizing structure element, is now marketed as an antiepileptic agent.

Animals↗
PubMed2000

Diabetes in urban African-Americans. XIX. Prediction of the need for pharmacological therapy.

OBJECTIVE: To develop a prediction rule that will identify patients who will require pharmacological therapy within 6 months of first presentation to a diabetes clinic. RESEARCH DESIGN AND METHODS: Among the patients who came to the Grady Diabetes Clinic between 1991 and 1997, we randomized 557 frequent attenders to a development group and 520 frequent attenders to a validation group. Using multiple logistical regression, we derived a prediction rule in the development group to project whether patients would require pharmacological intervention to achieve HbA1c levels <7% after 6 months. The utility of the prediction rule was then confirmed in the validation group and tested prospectively on an additional group of 93 patients who presented from 1997 to 1998. Performance of the prediction rule was assessed using receiver operating characteristic (ROC) curves. RESULTS: The rule (-4.469 + 1.932 x sulfonylurea Rx + 1.334 x insulin Rx + 0.196 x duration + 0.468 x fasting glucose, where "Rx" indicates a prescription) predicted the need for pharmacological intervention in the development group (P < 0.0001). Use of insulin or sulfonylurea therapy at presentation, duration of diabetes, and fasting glucose levels were significant predictors of the future need for pharmacological management. The prediction rule also performed well in the validation group (positive predictive value 90%, correlation between predicted and observed need for medical management 0.99). ROC curves confirmed the value of the prediction rule (area under the curves was 0.91 for the development group, 0.85 for the validation group, and 0.81 for the prospective group). CONCLUSIONS: Early identification of individuals who will require pharmacological intervention to achieve national standards for glycemic control can be achieved with high probability, thus allowing for more efficient management of diabetes.

Black or African American↗
PubMed2005

Atropine reduces dobutamine-induced side effects in ponies undergoing a pharmacological stress protocol.

REASONS FOR PERFORMING STUDY: High-dose dobutamine stress echocardiography has been shown to be cardiotoxic and arrhythmogenic in horses. However, the test may have benefit in practice as a pharmacological challenge of exercise without the treadmill being required. OBJECTIVES: To investigate the effect of low-dose dobutamine on cardiac performance in ponies previously treated with atropine, in order to develop a pharmacological protocol that allows examination of the equine heart under stimulation. METHODS: In 13 healthy Shetland ponies, heart rate (HR), stroke index (SI) and cardiac index (CI) were calculated from pulsed-wave Doppler ultrasound measurements performed at rest and during incremental steps of dobutamine infusion. Group 1 (n = 7) received dobutamine infusion at 2 microg/kg bwt/min for 5 mins followed by incremental rates of 5 microg/kg bwt/min every 5 mins, from 5 to 40 microg/kg bwt/min. Group 2 (n = 6) received dobutamine infusion in incremental rates of 1 microg/kg bwt/min, every 5 mins, from 2 microg/kg bwt/min to 5 microg/kg bwt/min, after premedication with 2 injections of 25 microg/kg bwt of atropine 5 mins apart. RESULTS: The increase in CI during the pharmacological challenge was higher in Group 2 and reached about 2.5 times the resting value. This increase in CI was mediated by a significant increase in HR in both groups, while SI significantly decreased in Group 1 and did not change significantly in Group 2. Ponies of Group 1, but not those of Group 2, showed excessive restlessness and cardiac arrhythmias during the pharmacological challenge and a high intragroup variability in cardiac response. CONCLUSIONS: The results of this study suggest that a low dose of dobutamine in ponies previously given atropine could be a helpful pharmacological protocol to perform stress echocardiography in equids. POTENTIAL RELEVANCE: Further studies should evaluate left ventricular wall motion in horses undergoing low-dose dobutamine protocol after pretreatment with atropine.

Animals↗
PubMed1990

The Canadian consensus report on non-pharmacological approaches to the management of high blood pressure.

The Canadian Consensus Conference on Non-Pharmacological Approaches to the Management of High Blood Pressure reviewed in March, 1989 on its meeting in Halifax, Nova Scotia, data concerning the efficacy of eight interventional strategies used for controlling hypertension. These strategies were as follows: alcohol restriction, weight reduction, physical exercise, reduction of salt intake, relaxation/stress management, increase of potassium and calcium intake and combination of pharmacological and non-pharmacological management. The Panel of the Consensus Conference recommended as efficacious the following interventions: alcohol restriction for less than two standard drinks per day, reduction of excessive body weight, and reduction of salt intake. There is sufficient scientific evidence for recommending potassium rich diet for normotensives and hypertensive persons. The Panel also concluded that a combination of pharmacological and non-pharmacological management is an efficacious measure. The Panel at this point of time could not issue recommendations as to the value of relaxation/stress management, physical exercise and calcium intake.

Alcohol Drinking↗
PubMed1999

Long-term effects of in vivo angioplasty in normal and vasospastic canine carotid arteries: pharmacological and morphological analyses.

OBJECT: A canine model of hemorrhagic vasospasm of the high cervical internal carotid artery (ICA) was used to study the long-term effects of transluminal balloon angioplasty (TBA) on the structure and function of the arterial wall. METHODS: Forty dogs underwent surgical exposure of both distal cervical ICAs, followed by baseline angiographic studies on Day 0. Dogs in Group A (20 animals) underwent simple exposure of one ICA and placement of a silicone elastomer cuff around a segment of the opposite artery. These animals underwent repeated angiography on Day 7, and then TBA was performed on the uncuffed ICA; the cuff was removed from the opposite vessel. For dogs in Group B (20 animals), blood clot-filled cuffs were placed around both ICAs, and on Day 7 angiography was repeated and TBA was performed on one randomly selected ICA. Four animals were then killed from each group, and in the remaining animals the cuffs were removed from both ICAs. On Days 14, 21, 28, and 56, four animals from each group underwent repeated angiography and were then killed to permit pharmacological and morphological analyses of the ICAs. This protocol yielded five study categories: cuffed nonblood-coated arteries not subjected to TBA, blood-coated arteries not subjected to TBA, blood-coated arteries subjected to TBA, normal arteries subjected to TBA, and control arteries obtained from the proximal ICA in each animal. The contractile responses of isolated arterial rings obtained from each ICA were recorded after treatment with potassium chloride, noradrenaline, and serotonin, whereas relaxations in response to the calcium ionophore A23187 and papaverine were recorded after tonic contraction to noradrenaline had been established. Morphological analysis was performed using scanning electron microscopy. Arteries surrounded by an empty cuff exhibited no angiographic, pharmacological, or morphological differences compared with normal arteries on any study day. Arteries surrounded by blood developed angiographically confirmed vasospasm on Day 7, with characteristic pharmacological and morphological features; resolution of these symptoms occurred by Day 21. Vasospastic arteries subjected to TBA on Day 7 remained dilated on angiographic studies, exhibited impaired responses to pharmacological agents (except for papaverine), and showed altered morphological features until Day 28. Normal arteries subjected to TBA on Day 7 remained dilated on angiographic studies, exhibited impaired responses to pharmacological agents (except for papaverine), and displayed altered morphological features until Day 14. CONCLUSIONS: These results indicate that the canine high cervical ICA model produces consistent and reproducible vasospasm that follows a similar time course to that seen in humans. When TBA is performed in vasospastic arteries, it results in an immediate functional impairment of vascular smooth muscle that lasts for 2 weeks, with resolution at 3 weeks; morphological changes are mostly resolved 3 weeks post-TBA. In normal vessels, TBA causes functional impairment and morphological alterations that are not as severe or as long-lasting as those seen in vasospastic arteries.

Angioplasty, Balloon↗
PubMed1997

[Evaluation of autonomic nervous system function with heart rate variability analysis in patients with hyperthyroidism and during euthyroidism after pharmacologic and surgical treatment].

The aim of the present study was both to estimate autonomic nervous system (ANS) function in patients with hyperthyroidism by the heart rate variability (HRV) analysis and to evaluate the impact of pharmacological and surgical treatment on the ANS function. Analysis of the HRV underwent 10 female patients in course of thyreotoxicosis and after reaching full clinical and biochemical euthyroidism, after pharmacological therapy and in month after surgical treatment. The 10 minutes records at rest, in horizontal position were evaluated. The HRV parameters like mean of the heart rate, mean of RR intervals, standard deviation of all normal RR intervals (SDNN), range of the heart rate variability, low frequency (LF), high frequency (HF) components of the heart rate power spectral density and LF/HF ratio were assessed. The results were compared to those obtained from 10 age-, sex-, and body mass index-matched control subjects. The statistical significance (p < 0.05) was found in reduction of range of RR intervals, in increase of LF/HF ratio and in decrease of SDNN in hyperthyroidism in comparison to the control group (151.6/346.8 ms; 2.4/0.74; 24.4/57.2 ms2). In course of pharmacological euthyroidism there were statistically significant (p < 0.05) increase of range of RR intervals, reduction of LF/HF ratio and increase of SDNN in comparison to hyperthyroidism (270/151.6 ms; 0.995/2.4; 39/24.4 ms2). In euthyroidism after surgical treatment all the above parameters kept the similar levels as in pharmacological euthyroidism (no statistical significance for p < 0.05). On the base of the outcomes it was considered that in hyperthyroid patients there is advantage of sympathetic part of ANS over parasympathetic one which is due to sharp reduction of parasympathetic system activity. Pharmacological therapy with thyreostatics normalises balance of ANS to the level of the control group and after surgical treatment the balance keeps the same. Moreover, in the estimation of ANS as important as LF/HF ratio is the mean range of RR intervals.

Adult↗
PubMed2000

Citalopram--a review of pharmacological and clinical effects.

OBJECTIVE: To provide clinicians with a critical evaluation of citalopram, a selective serotonin reuptake inhibitor (SSRI) that has been available in Canada since March 1999. DATA SOURCES: Commercial searches (MEDLINE and BiblioTech) and an "in-house" search (InfoDrug) were used to find published English-language references for clinical and preclinical publications. There was no restriction of publication dates. Primary index terms used were: pharmacological properties, receptors, pharmacological selectivity, pharmacokinetics, age-related pharmacokinetics, sex-related pharmacokinetics, renal dysfunction, hepatic dysfunction, cytochrome activity, drug interactions, adverse reactions, antidepressant switching, precautions, overdose, drug discontinuation, children, geriatric, depression, combination therapy, placebo control, refractory depression, anxiety disorders and medical disorders. STUDY SELECTION: A total of 74 studies were reviewed. Twenty-one of these studies specifically examined the clinical efficacy and tolerability of citalopram in depressive disorders as well as other disorders. In depressive disorders, clinical studies were required to have either placebo or active comparison controls for a minimum of 3 weeks. For other disorders, in the absence of double-blind trials, open-label studies were included. Pharmacological studies were limited to animal studies focusing on citalopram's selectivity and receptor specificity, and positron emission tomography studies were incorporated to include human pharmacological data. Pharmacokinetic studies focused on the metabolism, safety and tolerability of citalopram, specifically with reference to adverse reactions, drug interactions and overdose in addition to citalopram's effect on vulnerable populations, such as children, the elderly and patients with metabolic diseases. DATA EXTRACTION: Data on clinical studies were summarized according to test measures, study duration and outcome of study. Pharmacokinetic and pharmacodynamic studies were summarized according to properties and interactions. Adverse reactions were extracted to outline citalopram's safety profile. DATA SYNTHESIS: Citalopram is an SSRI antidepressant with a more specific and selective pharmacological profile than other antidepressants of its class. It is well tolerated, and drug interactions are not a significant concern. It is also reasonably safe for populations vulnerable to pharmacokinetic effects, such as the elderly and patients with metabolic diseases. In addition to its tolerability, citalopram is effective in the treatment of major depression, other depressive disorders and panic disorder. It has the potential to effectively treat other anxiety disorders and substance-use disorders; in addition, it may be useful in several medical conditions. CONCLUSIONS: There is evidence to support the role of citalopram as a well-tolerated and effective SSRI antidepressant. There is a need for further evaluation of its role in psychiatric disorders other than major depressive disorder.

Aged↗
PubMed2003

The start of pharmacological activity after sublingual administration of sildenafil citrate in 30 patients affected by erectile dysfunction.

INTRODUCTION AND OBJECTIVES: Sildnenafil citrate is a powerful phosphodiesterase type 5 isoenzyme; it is the first oral treatment to have had a significant success in treatment of erectile dysfunction (ED). After oral dosing on an empty stomach the pharmacological activity starts within 30 to 120 minutes (average 60 minutes) whereas the effect of this medication after a meal could be notably delayed. We evaluated the start of pharmacological activity in 30 patients affected by non-psychogenic ED after sublingual administration of Sildenafil citrate. METHODS: Patients participating in our study were all affected by ED whose etiology was assessed as vasculogenetic or diabetic. The study lasted 6 months. For the first 3 months patients were asked to take Sildenafil (50-100 mg) for oral administration, under normal everyday conditions, 30 minutes before planned sexual relations. During the second 3 months the patients were asked to take Sildenafil for sublingual administration (crushing the pill in the mouth and dissolving the drug under the tongue) 15 minutes before planned sexual relations. The patients did not know the purpose of the study. RESULTS: An appreciable reduction in the start of pharmacological activity was reported during the time of sublingual administration. In fact, while throughout the first 3 months the average pharmacological onset was 62.8 minutes (DS +/- 16.8), during the second 3 months it was 29.3 minutes (DS +/- 8.1), the mean difference in the start of pharmacological activity was 35.3 (DS +/- 12.4). The results of T-student test for paired observation were T (29) = 15.629; p-value 0.00001. During the two modalities of administration no differences were noted in the efficacy or in the frequency of adverse events. All the patients declared they preferred the sublingual way because of faster onset. CONCLUSIONS: Even though ours is a limited study, our clinical data points out that the sublingual administration of Sildenafil is useful because of the rapid onset unrelated to meals. All the patients were reported to appreciate this method of administration, particularly in the case of unplanned sexual relations.

Administration, Oral↗
PubMed2002

[Chemical and pharmacological advances of the study on zushima].

OBJECTIVE: To review the progress in the research of the active ingredients of Zushima and their pharmacological activities. METHOD: Base on the articles of the chemical constituents and pharmacological activities of Zushima. RESULT: Traditional Chinese drug, Zushima contains coumarins, diteropenoids, lignans, flavonoids, anthraquinones and sterols. Pharmacological investigation concludes that it has actions of painkilling, antiinflammation, inhibiting bacteria, antithrombus, antitumer and antifertility. CONCLUSION: Zushima has extensive actions in pharmacology. And plant resources are very rich. It is a meaning job to study the chemical ingredients and pharmacological activities of Zushima further.

Animals↗
PubMed2003

[Non-pharmacologic treatment of atrial fibrillation].

The authors provide an update on non-pharmacological treatment of atrial fibrillation (AF). They emphasize that although antiarrhythmic drugs continue to be first-line therapy for the arrhythmia considered to be a cardiovascular epidemic, clinical research to develop non-pharmacological means of treatment has been unprecedentally intensified during the last decade. Electrical cardioversion is the most successful non-pharmacological method to restore sinus rhythm, also the efficacy and safety of AV node ablation for palliative ventricular rate-controll is established. "Hybrid" therapeutic procedures, involving combinations of pharmacological and non-pharmacological interventions have gained widespread use. Curative transcatheter ablation for arrhythmia prevention is to be considered in case of clinical suggestions that AF is initiated by a primary regular arrhythmia that is amenable to routine catheter ablation (secondary AF). Despite encouraging results, at this point in time, curative catheter ablation for primary AF may offer significant improvement or even cure only for a small subset of patients, mostly young individuals with normal heart, and paroxysmal AF with frequent, symptomatic episodes refractory to multiple antiarrhythmic drugs. These interventions are to be performed in the settings of a clinical research project in some institutions. Regarding pacemaker therapy in case of bradycardia indication, physiologic pacing (AAI or DDD) is associated with significantly lower incidence of atrial fibrillation than ventricular pacing. Large-scale randomized controlled trials are needed to assess the clinical value of specially designed implantable devices to prevent atrial fibrillation in patients with no conventional bradycardia indication. Also, technical optimization and proper clinical evaluation is needed for implantable atrioverters and implantable cardioverter defibrillators capable of atrial cardioversion therapy.

Atrial Fibrillation↗
PubMed1992

Pharmacological profile of a series of bicyclic cannabinoid analogs: classification as cannabimimetic agents.

Opening of the pyran ring of delta 9-tetrahydrocannabinol (THC) produces cannabidiol, a bicyclic cannabinoid devoid of many pharmacological properties produced by delta 8-THC or delta 9-THC. Interestingly, the bicyclic compound CP-47,497 (VI) has been described as producing many of the pharmacological effects produced by delta 9-THC, and another related bicyclic analog CP-55,940 (XIV) has been used to successfully define a cannabinoid binding site. A series of 16 bicyclic analogs of VI and XIV were evaluated and compared with the pharmacological profile of cannabidiol, delta 8-THC and delta 9-THC. The goals of the studies described herein were to determine whether these bicyclic analogs possess similar pharmacological properties of delta 9-THC, to compare pharmacological activity after s.c. and i.v. administration, and to evaluate the structure-activity relationship of this series of analogs for further insight into cannabinoid mechanism of action. Each analog was evaluated for its ability to produce hypoactivity, hypothermia, antinociception and catalepsy in mice. The ED50 values generated from these assays were averaged to provide an index of activity. The ED50 values for delta 9-THC varied from 1.0 to 1.5 mg/kg, giving an overall index of activity of 1.3. The index for delta 8-THC was 6.0, making this isomer 4-fold less potent. Although several bicyclic analogs (V, VI, VII, VIII, XI, XII, XIV and XVI) proved to be truly cannabimimetic, three (IV, IX and X) were sufficiently unique to be classified as noncannabimimetic. The index of activity of cannabimimetic bicyclic analogs varied from 0.2 to 2.2, although some minor differences between the bicyclics and delta 9-THC exist.(ABSTRACT TRUNCATED AT 250 WORDS)

Adenylyl Cyclases↗
PubMed1992

Basic advances in serotonin pharmacology.

Several advances in serotonin pharmacology have implications for psychiatry. The introduction of selective inhibitors of serotonin uptake into clinical use has established more firmly the relevance of brain serotonin neurons to depressive illness and is permitting an exploration of other therapeutic consequences of amplifying serotonergic function. A recent major advance in basic pharmacology has been the definition and characterization of multiple serotonin receptor subtypes in brain. Highly selective agonists and antagonists at these receptor subtypes are being developed as candidate drugs for therapy and as pharmacologic probes for assessing functionality of brain serotonin neurons in disease. Improved pharmacologic specificity will provide better tools for eliciting measurable responses mediated by brain serotonin receptors and for imaging key presynaptic and postsynaptic constituents of serotonin neuronal systems. Advances in serotonin pharmacology should therefore expand our understanding of serotonin's roles as a brain neurotransmitter in health and disease and lead to improved therapeutic agents.

Brain↗
PubMed1992

Selected pharmacologic characteristics of idarubicin and idarubicinol.

The pharmacology of ID and IDOL are of interest in light of the potential utility of ID in the treatment of adult and pediatric leukemia patients. Preclinical activity and cellular pharmacology of ID were suggestive of greater clinical activity when compared with several standard anthracyclines. Most intriguing were data comparing in vitro and in vivo activity data and cellular pharmacology of IDOL to other anthracycline alcohol metabolites. Given the pharmacokinetics of IDOL, there is continued interest in the unique aspects of IDOL pharmacology as an important element of ID pharmacology.

Animals↗
PubMedDate not supplied

Hypoxic and pharmacological preconditioning preserves vasomotor response of porcine coronary artery.

Vasomotor response of the coronary artery depends on both endothelial and smooth muscle cells. Response is altered by hypoxia-reoxygenation-induced damages. Hypoxic preconditioning and pharmacological preconditioning as well can prevent these alterations. We compared the effectiveness of both types of preconditioning against hypoxia-reoxygenation-induced changes in vasomotor response of the isolated artery. Porcine arterial rings (3-4 mm wide) were cut from the left anterior descending porcine coronary artery and placed in Krebs-Henseleit solution. In order to obtain control response of the arteries, we contracted arterial rings with 20 mM KCl before ("standard contraction") and after 60-min hypoxia and 30-min reoxygenation. In other groups, nitric oxide-synthase and cyclooxygenase were inhibited. Then, the rings were pre-contracted with U46619 and relaxed by cumulative addition of the substance P. Contractions and relaxations of non-preconditioned and hypoxically or pharmacologically preconditioned rings were compared. Hypoxic preconditioning was performed by two periods of 5-min hypoxia and 10-min reoxygenation. For pharmacological preconditioning, we used application of adenosine, adrenaline, acetylcholine and angiotensin II. Analysis was performed with one-way ANOVA, followed by Dunnett's Multiple Comparison Test. After hypoxia-reoxygenation, in non-preconditioned rings KCl-induced contractions were significantly increased compared to standard contraction. Relaxations of hypoxically and pharmacologically preconditioned rings (expressed as percentages of U46619-induced pre-contraction) were significantly decreased (p < 0.01) compared to hypoxic but not to normoxic rings. Hypoxic and pharmacological preconditioning may preserve contraction and endothelium-dependent relaxation of porcine coronary artery after long-lasting hypoxia-reoxygenation.

15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5↗
PubMed2005

[Nutritional condition affect the potency of pharmacological therapy].

Recent development of pharmacological treatments with proven efficacy will increase demand for the more effective management of patients with osteoporosis. Osteoporosis is a chronic disease concerned many risk factors such as diet and nutrition, and pharmacological efficacy could much depend on such nutritional conditions in patients as calcium, vitamin D, and protein, etc. Especially Japanese elderly usually took extremely low calcium and protein intake as well as low vitamin D, however, physicians usually give just pharmacological prescription. Therefore firstly we had better assess the nutritional conditions in each patient by body weight, serum albumin, and dietary questionnaires and give them selected pharmacological prescription together with dietary and nutritional guidance for their effective treatment of drugs. Thus we can manage each patient with not only pharmacological but also nutritional treatments that will be effective in cost-performance and good compliance for chronic disease as osteoporosis. Moreover combined nutritional treatments could work more effective in the patients of osteoporosis with inflammatory disease and high nutritional metabolic rate.

Aged↗