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At least 271 records · Page 15Linked to original sources
PubMed2006

Recent advances in molecular pharmacology of the histamine systems: physiology and pharmacology of histamine H3 receptor: roles in feeding regulation and therapeutic potential for metabolic disorders.

Histamine H3 receptors (H3Rs) are autoreceptors that negatively regulate the release of histamine and other neurotransmitters such as norepinephrine, dopamine, and acetylcholine in the central nervous system (CNS). Consistent with the wide-spread projection of histaminergic neurons from the lateral hypothalamus, H3Rs are widely distributed in the CNS and are believed to play a variety of physiological roles, including regulation of feeding, arousal, cognition, pain, and endocrine systems. To further understand the physiological roles of H3Rs in vivo, we produced H3R knockout (H3R-/-) mice and found that H3R-/- mice displayed hyperphagia and late-onset obesity associated with hyperinsulinemia and leptinemia, the fundamental marks of metabolic syndromes. A series of non-imidazole H3R antagonists/inverse agonists with improved selectivity and potency have been developed and were found to regulate feeding and body weight gain in laboratory animals. Taken together, these observations suggest that H3Rs are involved in the regulation of feeding behavior and body weight. Several H3R inverse agonists targeting cognitive disorders and dementia have entered clinical trials. These trials will give critical information about the physiological functions of H3Rs in humans.

Animals↗
PubMed2003

Pharmacologic blockade of the renin-angiotensin system: vascular benefits beyond commonly understood pharmacologic actions.

Angiotensin-converting enzyme (ACE) inhibitors and angiotensin II receptor blockers (ARBs) are recognized primarily for their use in hypertension, in heart failure, and after myocardial infarction. New evidence, particularly with ACE inhibitors, has shown their ability to reduce acute coronary events associated with atherosclerosis in patients without a history of the aforementioned cardiac conditions. This is likely due to inhibitory effects on the renin-angiotensin system--a system that adversely influences fibrinolytic balance, vascular endothelial function, and vascular inflammation, all key components of atherosclerotic progression and adverse coronary outcomes. Results of various studies suggest favorable effects of ACE inhibitors and ARBs on markers of these components, including effects on plasminogen activator inhibitor-1, endothelin-1, and nitric oxide by ACE inhibitors, and effects on vascular cell adhesion molecule-1 and C-reactive protein by ARBs. Although early evidence suggests that ACE inhibitors may provide a greater beneficial effect on some of these markers compared with ARBs, and that certain ACE inhibitors may provide greater vascular benefits than others, further investigation is required to verify such findings. Overall, understanding the distinct coronary vascular benefits of these agents will emphasize the importance of using them, particularly ACE inhibitors, to improve outcomes in patients with coronary atherosclerotic disease.

Angiotensin II↗
PubMed2000

[Selection of pharmacologic treatment of arterial hypertension in primary care. Task force on Pharmacologic Approach of Hypertension in Primary Care (AFHAP)].

BACKGROUND: To assess whether patients' clinical characteristics, and more specifically contraindications to diuretics or beta-blockers have an influence on the prescription patterns of antihypertensive drugs. PATIENTS AND METHODS: Cross-sectional descriptive study of consecutive hypertensive patients attending 28 Primary Health Care Centres in Barcelona between November 1997 and February 1998. Information on patients' clinical characteristics and prescribed antihypertensive and other drugs was recorded. Hyperuricemia, a previous adverse drug reaction and potential drug interactions were considered as contraindications to diuretics. Asthma, chronic obstructive airway disease, peripheral arteriopathy, bradycardia, atrio-ventricular blockade, type 1 diabetes, a previous adverse drug reaction, and potential drug interactions were considered as contraindications to beta-blockers. RESULTS: Eighty-three general practitioners and 29 nurses collected data on 1,813 patients (66% were women and mean age was 68 years). Dyslipemia was present in 746 patients (41.1%), diabetes in 385 (21.2%), hyperuricemia in 251 (13.8%), coronary heart disease in 218 (12%), and heart failure in 128 (7.1%). Diuretics were contraindicated in 350 patients (19.3%) and beta-blockers in 537 (29.6%). Eight-hundred seventy-nine patients (48.5%) were prescribed an angiotensin-converting-enzyme (ACE) inhibitor, 803 (44.3%) a diuretic, 521 (28.7%) a calcium-channel blocker, and 246 (13.6%) a beta-blocker. The prescription pattern was similar in both patients with existing contraindications to diuretics or beta-blockers, or without them, and in those with and without diabetes, heart failure or coronary heart disease and in those whose clinical characteristics would make the prescription of a diuretic, a beta-blocker or an ACE-inhibitor a first choice option. Prescription of a diuretic was associated to age and to existing contraindications to a beta-blocker, whereas the prescription of a beta-blocker was associated with a history of coronary heart disease. CONCLUSIONS: The present study suggests that contraindications to diuretics or beta-blockers are not considered when prescribing antihypertensive drugs. The results of clinical trials are not applied to clinical practice, and this results in a high proportion of patients not being offered the benefit of cardiovascular risk prevention.

Aged↗
PubMedDate not supplied

[Drug effects in elderly subjects: from the pharmacologic target to the risk-benefit. Round Table #5 of the 16th National Clinical Pharmacology Workshop].

In addition to being a fast-growing subpopulation, the elderly also receive large quantities of medication and are particularly exposed to iatrogenic effects. In France, 8.6 per cent of hospitalizations of patients over the age of 70 are due to an adverse event. This workshop comprising pharmaceutical companies, pharmacologists, geriatricians and health authorities aimed to make propositions for improving drug research in the elderly in order to prevent iatrogenic drug reactions by encouraging more rigorous application of existing guidelines. In addition to information extrapolated from clinical trials conducted on young or healthy people, it is imperative to include in clinical trials a sufficient number of elderly patients and to take into consideration specific criteria such as multiple medication regimens, concomitant diseases, cognitive impairment and motor disturbances. The assessment of drugs used in the elderly must be based on a specific and validated geriatrics scale and in some cases (postmarketing studies) may be based on specific trials (those called 'conducted in the real world').

Aged↗
PubMedDate not supplied

[Use of pharmacological and non-pharmacological techniques to control pain and states of suffering].

In 1993, World Health Organization has assumered pain like pathology and in 1998 began the spreading of guidelines specifications for cancer pain relief control and palliative care in children. Thanks to experience that we acquired in law in Oncology and Haematology paediatric Unit of "A. Meyer" Hospital of Florence, we have been invited to carry to the last congress of Florence of the AIEOP (Italian haematology-oncology paediatric association) an ours contribution in matter. So knowing the "state of the art" of the AIEOP centers has become necessary. With this work the results of such cognitive investigation will be presented.

Age Factors↗
PubMed2003

Hospitalized patients' preference in the treatment of insomnia: pharmacological versus non-pharmacological.

BACKGROUND: Insomnia is common in hospitalized patients, who become significantly vulnerable to the adverse effects of the benzodiazepines (BZDs) used to treat this condition. Consequently, there has been a logical search for non-drug alternatives (NDAs) for the treatment of insomnia. METHOD: Inpatient insomnia cases were surveyed over the Summer of 1999. Our hypotheses were that an attitudinal difference exists between acute and chronic users of BZDs towards NDAs; and that inpatients who were prescribed BZDs have also received proper information about alternative therapies. RESULTS: One hundred insomnia cases met the inclusion criteria. Fifty-one per cent were younger than age 65. Short acting BZDs were used in 88% of the cases. Fourty per cent of patients had started experiencing insomnia while in the hospital. Only 11% of patients received information about NDA therapy for insomnia. Eighty-two patients felt that NDAs were healthier, and the majority (n=67) responded that if an NDA were offered in the hospital, they would be willing to accept it. Female participants were more willing to consider NDAs (P<0.01). First time users of BZDs were by far more receptive to NDA remedies than were chronic users of BZDs (P<0.002). A significant number of participants who were receiving short-acting BZDs were willing to try an NDA (P<0.001). Participants interested in NDA therapies expressed preferences for for massage therapy, sleep hygiene, music and relaxation techniques (P<0.001). CONCLUSION: Significant attitudinal differences are seen in several domains of patient characteristics. First time female users of BZDs and those taking short acting BZD were more willing to try an NDA. Educational programs are needed for appropriate evidence-based management protocols for insomnia.

Aged↗