Non-pituitary actions of somatostatin. A review on the therapeutic role of SMS 201-995 (sandostatin)

1986 ◽  
Vol 113 (2_Suppla) ◽  
pp. S41-S55 ◽  
Author(s):  
Steven W. J. Lamberts
Keyword(s):  
Half Life ◽  
Potential Role ◽  
Somatostatin Analogs ◽  
Subcutaneous Administration ◽  
Term Treatment ◽  
Acute Administration ◽  
Intestinal Function ◽  
Long Term Treatment

Abstract. Natural Somatostatin has a short half-life (3 min), is only active after intravenous administration and causes a rebound hypersecretion of hormones after discontinuation of administration. Recently a longacting powerful Somatostatin analog was developed (SMS 201-995; Sandostatin) which has a half-life of 113 min after subcutaneous administration. After administration of this analog no rebound hypersecretion of hormones was observed. In the present review the effects of the acute administration and of long-term treatment with SMS 201-995 in acromegalic patients is discussed. In addition the potential role of therapy with Somatostatin analogs and the preliminary effects of Somatostatin and/or SMS 201-995 are discussed in disorders of gastro-intestinal function (haemorrhages, diarrhoea, pancreatitis and endocrine pancreatic tumours), diabetes mellitus, central nervous system disturbances and oncology. Finally, several aspects of the tolerance, tachyphylaxis and side effects of SMS 201-995 are discussed.

Cognitive Treatment for OCD

2012 ◽  
Author(s):  
Maureen L. Whittal ◽  
Melisa Robichaud
Keyword(s):  
Term Treatment ◽  
Future Directions ◽  
Cognitive Treatment ◽  
Long Term Treatment ◽  
Inflated Responsibility ◽  
And Control ◽  
The Relationship ◽  
Control Of Thoughts

The cornerstone of cognitive treatment (CT) for OCD is based upon the knowledge that unwanted intrusions are essentially a universal experience. As such, it is not the presence of the intrusion that is problematic but rather the associated meaning or interpretation. Treatment is flexible, depending upon the nature of the appraisals and beliefs, but can include strategies focused on inflated responsibility and overestimation of threat, importance and control of thoughts, and the need for perfectionism and certainty. The role of concealment and the relationship to personal values are important maintaining and etiological factors. The short-term and long-term treatment outcome is reviewed, along with predictors of treatment response and mechanisms of action, and the chapter concludes with future directions regarding CT for OCD.

scholarly journals Defining the role of SGAs in the long-term treatment of bipolar disorder

2017 ◽  
Vol 19 (1) ◽  
pp. 65-67 ◽  
Author(s):  
Gin S Malhi ◽  
Grace Morris ◽  
Amber Hamilton ◽  
Tim Outhred ◽  
Pritha Das
Keyword(s):  
Bipolar Disorder ◽  
Term Treatment ◽  
Long Term Treatment

scholarly journals The relevance of prescribing triple neurohormonal blockade in real clinical practice: the role of mineralocorticoid receptor antagonists

2021 ◽  
Vol 23 (6) ◽  
pp. 491-497
Author(s):  
Igor V. Zhirov ◽  
◽  
Igor V. Zhirov ◽  
Keyword(s):  
Myocardial Infarction ◽  
Heart Failure ◽  
Mineralocorticoid Receptor ◽  
Systolic Dysfunction ◽  
Term Treatment ◽  
Mineralocorticoid Receptor Antagonists ◽  
Long Term Treatment ◽  
Real Clinical Practice

In the article is outlined the main concepts use of the mineralocorticoids receptors antagonists in the treatment of congestive heart failure and systolic dysfunction after acute myocardial infarction. Claimed the pivotal role of eplerenone in the long-term treatment strategy due to decrease of mortality and improving the clinical outcomes.

scholarly journals Neuropharmacology of the Neuropsychiatric Symptoms of Dementia and Role of Pain: Essential Oil of Bergamot as a Novel Therapeutic Approach

2019 ◽  
Vol 20 (13) ◽  
pp. 3327 ◽  
Author(s):  
Damiana Scuteri ◽  
Laura Rombolà ◽  
Luigi Antonio Morrone ◽  
Giacinto Bagetta ◽  
Shinobu Sakurada ◽  
...  
Keyword(s):  
Essential Oil ◽  
Psychological Symptoms ◽  
Neuropsychiatric Symptoms ◽  
Term Treatment ◽  
Long Term Treatment ◽  
Anxiety Depression ◽  
Cognitive Disturbance

Aging of the population makes of dementia a challenge for health systems worldwide. The cognitive disturbance is a serious but not the only issue in dementia; behavioral and psychological syndromes known as neuropsychiatric symptoms of dementia remarkably reduce the quality of life. The cluster of symptoms includes anxiety, depression, wandering, delusions, hallucinations, misidentifications, agitation and aggression. The pathophysiology of these symptoms implicates all the neurotransmitter systems, with a pivotal role for the glutamatergic neurotransmission. Imbalanced glutamatergic and GABAergic neurotransmissions, over-activation of the extrasynaptic N-methyl-D-aspartate (NMDA) receptors and alterations of the latter have been linked to the development of neuropsychiatric symptoms experienced by almost the entire demented population. Drugs with efficacy and safety for prevention or long term treatment of these disorders are not available yet. Aromatherapy provides the best evidence for positive outcomes in the control of agitation, the most resistant symptom. Demented patients often cannot verbalize pain, resulting in unrelieved symptoms and contributing to agitation. Bergamot essential oil provides extensive preclinical evidence of analgesic properties. Incidentally, the essential oil of bergamot induces anxyolitic-like effects devoid of sedation, typical of benzodiazepines, with a noteworthy advantage for demented patients. These data, together with the reported safety profile, form the rational basis for bergamot as a neurotherapeutic to be trialed for the control of behavioral and psychological symptoms of dementia.

Long-term treatment of bipolar disorder: The controversial role of antidepressants

2014 ◽  
Vol 48 (11) ◽  
pp. 1062-1062
Author(s):  
Andrea Amerio ◽  
Anna Odone ◽  
Carlo Marchesi ◽  
S Nassir Ghaemi
Keyword(s):  
Bipolar Disorder ◽  
Term Treatment ◽  
Long Term Treatment

scholarly journals Endothelin research and the discovery of macitentan for the treatment of pulmonary arterial hypertension

2016 ◽  
Vol 311 (4) ◽  
pp. R721-R726 ◽  
Author(s):  
Martine Clozel
Keyword(s):  
Pulmonary Arterial Hypertension ◽  
Arterial Hypertension ◽  
Structural Changes ◽  
Term Treatment ◽  
Vasopressin Release ◽  
Long Term Treatment ◽  
Pulmonary Arterial ◽  
Kinetics Of

Endothelin receptor antagonists (ERAs) are used for the treatment of pulmonary arterial hypertension (PAH). Macitentan, a dual (ETA+ETB) ERA approved for the long-term treatment of PAH, was discovered through a tailored research program aimed at improving efficacy and safety over the existing ERAs. The goal of improved efficacy was based on the understanding that not only the ETA receptor but also the ETB receptor contributed to the hemodynamic and structural changes induced by endothelin-1 (ET-1) in pathological conditions and on the predefined requirements for optimal tissue penetration and binding kinetics of the antagonist. The goal of improved safety was based on the discovery of the role of ETB receptors in vascular permeability and vasopressin release and on the elucidation of the mechanism by which bosentan (the first approved oral dual ETA/ETB ERA) caused liver enzyme changes. Our intention was to design a molecule that would block ETA and ETB receptors optimally and would not interfere with bile salt elimination. This review takes us through the drug discovery journey that led to the discovery, development, and registration of macitentan.

The Role of 5–Hydroxytryptamine (5–HT) Receptor Subtypes and Plasticity in the 5–HT Systems in the Regulation of Nociceptive Sensitivity

Cephalalgia ◽  
1993 ◽  
Vol 13 (2) ◽  
pp. 75-85 ◽  
Author(s):  
Per Kristian Eide ◽  
Kjell Hole
Keyword(s):  
Receptor Activation ◽  
Term Treatment ◽  
Receptor Subtypes ◽  
Functional Changes ◽  
Nociceptive Sensitivity ◽  
Denervation Supersensitivity ◽  
Long Term Treatment ◽  
Stimulation Of

This review shows that the role of 5–hydroxytryptamine (5–HT) in the regulation of nociception depends on the 5–HT receptor subtypes involved and on long-term functional changes in the 5–HT receptors. Stimulation of the 5–HT 1 receptors, as well as of the 5–HT 2 and 5–HT 3 receptors, may reduce nociceptive sensitivity. In addition, activation of 5–HT 2 and 5–HT 3 receptors may also enhance nociceptive sensitivity. Up- or down-regulation of the 5–HT receptors may result in long-lasting changes, plasticity, in the 5–HT systems. Lesioning of 5–HT neurons induces denervation supersensitivity to 5–HT, and prolonged stimulation of 5–HT receptors may produce subsensitivity to 5–HT. In the spinal cord denervation supersensitivity to 5–HT may depend on reduced release of substance P (SP). An increase in the release of SP, on the other hand, may reduce the effects of 5–HT receptor activation. Long-term treatment with antidepressants which are used in clinical pain therapy appears to up-regulate the 5–HT 1 receptors and to down-regulate the 5–HT 2 receptors.

Long-Term Treatment of Ovariectomized Mice with Estradiol or Phytoestrogens as a New Model to Study the Role of Estrogenic Substances in the Heart

Planta Medica ◽  
2011 ◽  
Vol 78 (01) ◽  
pp. 6-11 ◽  
Author(s):  
Ba Nguyen ◽  
Georgios Kararigas ◽  
Wolfgang Wuttke ◽  
Hubertus Jarry
Keyword(s):  
Term Treatment ◽  
New Model ◽  
Ovariectomized Mice ◽  
Long Term Treatment

The Role of Long Acting Antipsychotics in Bipolar Disorder

2017 ◽  
Vol 41 (S1) ◽  
pp. S15-S15
Author(s):  
E. Vieta
Keyword(s):  
Bipolar Disorder ◽  
Meta Analysis ◽  
Term Treatment ◽  
Patient Profile ◽  
Long Term Treatment ◽  
Short And Long Term ◽  
Competing Interest ◽  
Long Acting

Antipsychotics are widely used for the short and long-term treatment of bipolar disorder. Depot and long-acting injectable formulations (LAIs) can be particularly useful for certain subgroups of patients. This lecture will discuss the available data from randomized controlled trials of LAIs in bipolar disorder. A recently published meta-analysis and individual studies assessing depot medications, as well as modern LAIs such as risperidone, paliperidone and aripiprazole, will be reviewed, looking carefully into the prevention of either pole of illness and tolerability. Potential indications and patient profile, based on data and clinical experience, will be discussed.Disclosure of interestThe author has not supplied his declaration of competing interest.

scholarly journals The Role of Rho Kinase in Sex-Dependent Vascular Dysfunction in Type 1 Diabetes

2010 ◽  
Vol 2010 ◽  
pp. 1-11 ◽  
Author(s):  
Daniel W. Nuno ◽  
Kathryn G. Lamping
Keyword(s):  
Kinase Inhibitors ◽  
Vascular Dysfunction ◽  
Rho Kinase ◽  
Term Treatment ◽  
Compensatory Mechanisms ◽  
Rho Kinase Inhibitors ◽  
Long Term Treatment

We hypothesized that rho/rho kinase plays a role in sex differences in vascular dysfunction of diabetics. Contractions to serotonin were greater in isolated aortic rings from nondiabetic males versus females and increased further in streptozotocin-induced diabetic males but not females. The increased contractions to serotonin in males were reduced by inhibitors of rho kinase (fasudil, Y27632 and H1152) despite no change in expression of rhoA or rho kinase. Contractions to U46619 were not altered by fasudil or Y27632 or the presence of diabetes. In contrast to acute effects of fasudil, chronic treatment with fasudil increased contractions to serotonin in aorta from both non-diabetic and diabetic males. In summary, serotonin-induced contractions were increased in aorta from diabetic males but not females. Although administration of rho kinase inhibitors acutely decreased contractions to serotonin, long-term treatment with fasudil increased contractions. Long-term fasudil treatment may increase compensatory mechanisms to enhance vasoconstrictions.

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