CQP 201-403, a new dopamine agonist in the treatment of hyperprolactinemia

1988 ◽  
Vol 117 (4) ◽  
pp. 552-556 ◽  
Author(s):  
L. E. Hanssen ◽  
J. Brownell ◽  
J. Halse ◽  
J. Jervell ◽  
K. T. Stokke ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Side Effects ◽  
Orthostatic Hypotension ◽  
Dopamine Agonist ◽  
Drug Administration ◽  
Pituitary Adenomas ◽  
Adverse Reactions ◽  
Area Under The Curve ◽  
Control Group ◽  
Standing Blood Pressure

Abstract. Current drugs used for hyperprolactinemia may have severe side effects. Effects and side effects of a new propylergoline derivate (CQP 201-403 SANDOZ®) have been evaluated. Twenty-four otherwise healthy women (21–44 years) with hyperprolactinemia (35–318 μg/l) without extrasellar extension of pituitary adenomas took part in a randomized, doubleblind study. Fasting prolactin levels measured on day 7 was significantly decreased when compared with day 1 (P < 0.05) in all CQP groups, to 78% with 0.005 mg daily, to 40% with 0.015 mg daily, and to 27% with 0.025 mg CQP per day for one week. The levels in the control group did not change (96%). The area under the curve of the prolactin day curve (1–8 h after drug administration) decreased significantly (P < 0.05) at all doses when day 7 was compared with day 1, to 77% with 0.005 mg, to 51% with 0.015 mg, and to 37% with 0.025 mg CQP. No change was seen in the control group (96%). Four patients (one on 0.005 mg, one on 0.015 mg, and two on 0.025 mg) experienced orthostatic hypotension while standing blood pressure was to be measured on the first day of treatment, and they had to lie down. CQP 201-403 lowers prolactin levels in hyperprolactinemic women at all doses employed. The effect was seen after the first dose of treatment, and lasted for at least 24 h. The adverse reactions are few and tolerable, and might be less than with current bromocriptine therapy.

scholarly journals Therapeutic effect of nifedipine combined with enalapril on elderly patients with coronary heart disease complicated with hypertension

2018 ◽  
Vol 2 (6) ◽  
Author(s):  
Xiaoye Wang
Keyword(s):  
Blood Pressure ◽  
Coronary Heart Disease ◽  
Heart Disease ◽  
Elderly Patients ◽  
Adverse Reactions ◽  
Effective Rate ◽  
Control Group ◽  
Significant Difference ◽  
Pre Treatment ◽  
Experimental Group

【Abstract】Objective: Toanalyze the efficacy of combined drug therapy for elderly patients with coronary heart disease and hypertension.METHODS:Sixty-six elderly patients with coronary heart disease and hypertension were enrolled from December 2017 to November 2018. They were randomly divided into two groups, 33 patients in each group. Patients in the experimental group received nifedipine. In combination with enalapril, patients enrolled in the control group received nifedipine monotherapy.RESULTS:Compared with the control group, the total effective rate, Serum Nitric Oxide (Serum NO) after treatment, CRP after treatment, HCY after treatment, and blood pressure after treatment were significantly improved (P<0.05). Serum NO and treatment before treatment in the 2 groups. There was no significant difference in pre-CRP, pre-treatment HCY, pre-treatment blood pressure, and adverse reactions during treatment (P>0.05).Conclusion: Theelderly patients with coronary heart disease and hypertension are treated with nifedipine and enalapril.

scholarly journals Neurogenic Orthostatic Hypotension: State of the Art and Therapeutic Strategies

2020 ◽  
Vol 14 ◽  
pp. 117954682095341
Author(s):  
Dinesh K Kalra ◽  
Anvi Raina ◽  
Sumit Sohal
Keyword(s):  
Blood Pressure ◽  
Orthostatic Hypotension ◽  
Clinical Features ◽  
Autonomic Dysfunction ◽  
State Of The Art ◽  
Therapeutic Strategies ◽  
Review Article ◽  
Neurogenic Orthostatic Hypotension ◽  
Standing Blood Pressure ◽  
Secondary Causes

Neurogenic orthostatic hypotension (nOH) is a subtype of orthostatic hypotension in which patients have impaired regulation of standing blood pressure due to autonomic dysfunction. Several primary and secondary causes of this disease exist. Patients may present with an array of symptoms making diagnosis difficult. This review article addresses the epidemiology, pathophysiology, causes, clinical features, and management of nOH. We highlight various pharmacological and non-pharmacological approaches to treatment, and review the recent guidelines and our approach to nOH.

Pharmacoequivalence of Enoxaparin and Contaminated Enoxaparin

Blood ◽  
2008 ◽  
Vol 112 (11) ◽  
pp. 3018-3018
Author(s):  
Jacqueline Kuziej ◽  
Walter Jeske ◽  
Debra Hoppensteadt ◽  
Evangelos Litinas ◽  
Elizabeth McGeehan ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Heart Rate ◽  
Drug Administration ◽  
Jugular Vein ◽  
Ex Vivo ◽  
Subcutaneous Administration ◽  
Saline Control ◽  
Control Group ◽  
Serious Adverse Events ◽  
The Impact

Abstract Introduction: Earlier this year, heparin was found to be contaminated with a non-heparin sulfated polymer identified as oversulfated chondroitin sulfate (OSCS). The presence of this contaminant was associated with severe adverse reactions such as hypotension and anaphylaxis, leading to death in some patients. Some batches of a widely used low-molecular heparin, enoxaparin, also contained OSCS. However, the amount of this contaminant was much lower (less than 5%) in the low-molecular weight heparin batches compared to unfractionated heparin where the amount of the contaminant was up to 30%. Owing to the sizeable number of syringes in Europe that contained the low level of OSCS and the absence of any serious adverse events, the European Medicines Equivalence Agency (EMEA) allowed the qualified use of the subcutaneous administration of the contaminated enoxaparin to ensure access to this essential medication. Despite this, no studies on the anti-thrombotic and bleeding effects or basic physiologic parameters have been reported. To address the bioequivalence of enoxaparin and its contaminated version, studies were undertaken in established animal models of bleeding and thrombosis. Materials & Methods: Contaminant-free enoxaparin (CFE) and one of the commercially available contaminated enoxaparin (CCE) batches were compared at an equivalent subcutaneous dosage of 2.5 mg/kg in a jugular vein clamping model of thrombosis (n=6/group). A separate group comprised of saline control animals served as control. Blood pressure and heart rate measurements were made at 90 minutes after drug administration, followed by jugular vein clamping model at 120 minutes after drug administration. After the completion of the jugular vein clamping model, blood samples were collected via cardiac puncture for ex-vivo monitoring of anti-coagulant and anti-protease effects. Results: No differences in the blood pressure and heart rate were observed between the two groups. The anti-thrombotic effects of both the CCE and CFE were measured by jugular vein clamping model. In comparison to the saline treated group (3.5 ± 0.5 clampings), both the CCE and CFE treated animals required a significantly higher number of clampings to induce thrombosis (4.8 ± 0.7 and 5.0 ± 0.6, respectively; p = 0.001 vs. saline; p=0.658 CFE vs. CCE). The ex-vivo analysis of whole blood aPTT revealed a slight elevation in both of the enoxaparin-treated groups in comparison to saline control. (CFE: 36.8 ± 18.6 sec; CCE: 30.5 ± 10.9 sec vs. saline: 26.7 ± 3.9 sec). The anti-Xa effects in plasma were significantly higher with the CFE (84.4 ± 1.5% inhibition) compared to that observed with the CCE (80.5 ± 2.9 % inhibition; p=0.026) while the anti-IIa levels were comparable in the two groups (37.1 ± 22.0 and 30.6 ± 17.9 % inhibition). Ex-vivo analysis of plasma samples from the control group did not reveal any anti-protease or anti-coagulant activity. Discussion: These results demonstrate that small amounts of OSCS (less than 5%) in enoxaparin do not impact its anti-thrombotic effects when administered subcutaneously. Since OSCS exhibits only anti-IIa activity and does not have any anti-Xa effects, the observed anti-Xa activity of the CCE was less than that of CFE. Other plasmatic anti-coagulant and anti-protease activities were not altered by the presence of OSCS. Since OSCS is highly charged it is likely that upon subcutaneous administration it is not absorbed. This observation is supported by the fact that the anti-Xa and IIa ratios of the samples collected after jugular vein clamping are approximately equal. Thus, the anti-thrombotic and pharmacodynamic effects of the two versions of enoxaparin are identical. The impact of repeated administration of contaminated enoxaparins and long-term pharmacodynamic and immunogenic effects need to be further explored.

scholarly journals A Systems Approach to Study Immuno- and Neuro-Modulatory Properties of Antiviral Agents

Viruses ◽  
2018 ◽  
Vol 10 (8) ◽  
pp. 423 ◽  
Author(s):  
Eva Zusinaite ◽  
Aleksandr Ianevski ◽  
Diana Niukkanen ◽  
Minna Poranen ◽  
Magnar Bjørås ◽  
...  
Keyword(s):  
Side Effects ◽  
Drug Administration ◽  
Drug Toxicity ◽  
Adverse Reactions ◽  
Systems Approach ◽  
Ex Vivo ◽  
Antiviral Agents ◽  
Cell Types ◽  
Current Approach ◽  
Ex Vivo Approach

There are dozens of approved, investigational and experimental antiviral agents. Many of these agents cause serious side effects, which can only be revealed after drug administration. Identification of the side effects prior to drug administration is challenging. Here we describe an ex vivo approach for studying immuno- and neuro-modulatory properties of antiviral agents, which may be associated with potential side effects of these therapeutics. The current approach combines drug toxicity/efficacy tests and transcriptomics, which is followed by mRNA, cytokine and metabolite profiling. We demonstrated the utility of this approach with several examples of antiviral agents. We also showed that the approach can utilize different immune stimuli and cell types. It can also include other omics techniques, such as genomics and epigenomics, to allow identification of individual markers associated with adverse reactions to antivirals with immuno- and neuro-modulatory properties.

scholarly journals Acarbose for Postprandial Hypotension With Glucose Metabolism Disorders: A Systematic Review and Meta-Analysis

2021 ◽  
Vol 8 ◽  
Author(s):  
Biqing Wang ◽  
Junnan Zhao ◽  
Qiuxiao Zhan ◽  
Rongyanqi Wang ◽  
Birong Liu ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Clinical Trials ◽  
Glucose Metabolism ◽  
Adverse Reactions ◽  
Meta Analysis ◽  
Control Group ◽  
Glucose Metabolism Disorders ◽  
Postprandial Hypotension ◽  
Randomized Controlled ◽  
Randomized Controlled Studies

Background: Postprandial hypotension (PPH) is an independent predictive factor of all-cause mortality in older people. Drug management has not achieved a satisfactory effect yet. In recent years, many studies have found that acarbose may be effective in the treatment of PPH with glucose metabolism disorders.Objective: To assess the efficacy and safety of acarbose on PPH with glucose metabolism disorders.Methods: PubMed (MEDLINE), Cochrane, EMBASE, Web of Science, Clinical Trials, and relevant Chinese databases were searched from inception to October 1, 2020. Randomized controlled studies of acarbose in the treatment of PPH with glucose metabolism disorders were included. Review Manager 5.3 software was used for quality evaluation and meta-analysis. GRADEpro GDT software was used to GRADE the evidence for the research objectives.Results: A total of 4 randomized controlled studies including 202 participants were identified after screening. The meta-analysis showed that acarbose significantly attenuated the decrease in postprandial systolic blood pressure [weighted mean difference (MD): −9.84, 95% CI: −13.34 to −6.33], diastolic blood pressure (MD: −6.86, 95% CI: −12.89 to −0.83), and mean arterial pressure (MD: −8.10, 95% CI: −12.40 to −3.49) compared with the control group. One study reported a case of adverse reactions that included mild abdominal distension in the acarbose group (4.8%, 1/21). No adverse reactions were reported in the other three studies.Conclusion: Acarbose may attenuate the decrease in postprandial blood pressure and avoid the occurrence of PPH in patients with PPH and abnormal glucose metabolism disorders. More clinical trials are needed to make a clear conclusion.Registration: PROSPERO CRD42020171335.

140 Midodrine Hydrochloride in the Management of Elderly Patients with Neurocardiogenic Syncope: A Prospective Observational Study

2019 ◽  
Vol 48 (Supplement_4) ◽  
pp. iv34-iv39
Author(s):  
Angelene Teo ◽  
Arturo Vilches-Moraga ◽  
John Staniland
Keyword(s):  
Side Effects ◽  
Observational Study ◽  
Orthostatic Hypotension ◽  
Elderly Population ◽  
Prospective Observational Study ◽  
Adverse Reactions ◽  
Vasovagal Syncope ◽  
The Elderly ◽  
Hair Follicles ◽  
Neurocardiogenic Syncope

Abstract Background Midodrine hydrochloride is an alpha-1 agonist that has been used in the management of syncope in patients with orthostatic hypotension, vasovagal syncope and vasodepressor carotid sinus syndrome when non-pharmacological means have failed. However, there are very limited information about its use, tolerability and side effects among the elderly population. Objectives We aim to document effectiveness of Midodrine in patients who have been diagnosed with neurocardiogenic syncope assessed and managed at a specialist falls and syncope outpatient unit. We monitored for changes in patients' symptoms, adverse reactions reported and optimum drug dosages that have shown benefit in this cohort of patients. Methods A prospective observational study of 33 subjects aged between 68 and 94 (mean age 79) who have been started on Midodrine therapy following positive tilt table test or confirmed diagnosis of symptomatic orthostatic hypotension despite conservative managements. They have been followed up for a mean of 2.9 years. Results 81% of patients( n=27) reported significant improvement in their symptoms. Although 7 patients reported adverse reactions to Midodrine, the majority of the patients tolerated the therapy well and continued on the treatment except for one patient who experienced gastrointestinal discomfort and withdrew completely. Commonest side effects are pruritus and piloerection, but they are not amenable to treatment due to underlying mechanism of action of Midodrine on hair follicles. The dosage varies from 2.5mg to 10mg, taken at 8am, 12pm and 5pm due to risk of nocturnal supine hypertension. Higher dose did not correlate with higher possibility of experiencing side effects. Conclusion Midodrine appears to be effective, safe and well tolerated among the elderly population. It should be considered in the management of patients with neurocardiogenic syncope when non-pharmacological means have failed, irrespective of age. This observational study requires further confirmation by randomised control studies with larger sample size.

scholarly journals Sitting and standing blood pressure measurements are not accurate for the diagnosis of orthostatic hypotension

QJM ◽  
2009 ◽  
Vol 102 (5) ◽  
pp. 335-339 ◽  
Author(s):  
J. Cooke ◽  
S. Carew ◽  
M. O'Connor ◽  
A. Costelloe ◽  
T. Sheehy ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Orthostatic Hypotension ◽  
Pressure Measurements ◽  
Standing Blood Pressure

scholarly journals Clinical Evaluation of Pinggan Yiqi Yangshen Recipe Combined with Labetalol Hydrochloride and Magnesium Sulfate in the Treatment of PIH

2021 ◽  
Vol 2021 ◽  
pp. 1-7
Author(s):  
Ping Li ◽  
Jie Zhao ◽  
Peipei Gao ◽  
Hongcui Qu
Keyword(s):  
Blood Pressure ◽  
Renal Function ◽  
Magnesium Sulfate ◽  
Pregnancy Outcomes ◽  
Adverse Reactions ◽  
Fetal Distress ◽  
Effective Rate ◽  
Control Group ◽  
Labetalol Hydrochloride ◽  
Experimental Group

Background. To observe the clinical effect of Pinggan Yiqi Yangshen recipe combined with labetalol hydrochloride and magnesium sulfate in the treatment of pregnancy-induced hypertension (PIH). Methods. A total of 126 patients with PIH diagnosed in our hospital from January 2016 to May 2018 were randomly divided into the control group and the experimental group, with 63 cases in each group. The control group was treated with labetalol combined with magnesium sulfate. On the basis of the control group, the experimental group was treated with Pinggan Yiqi Yangshen recipe. Clinical efficacy, blood pressure, renal function, and biochemical indexes were compared between the two groups. Moreover, pregnancy outcomes and adverse reactions were compared between the two groups. Results. After treatment, the total effective rate in the experimental group was higher than in the control group. Blood pressure and mean arterial pressure in the experimental group were more significantly downregulated than the control group. Renal function indexes and biochemical indexes in the experimental group were more significant than those in the control group. The incidence of cesarean section, preterm birth, and abnormal fetal heart rate in the experimental group was significantly lower than that in the control group. There was no difference in the incidence of fetal distress, postpartum hemorrhage, neonatal asphyxia, and adverse reactions between the two groups. Conclusion. Pinggan Yiqi Yangshen recipe combined with labetalol hydrochloride and magnesium sulfate can effectively reduce the blood pressure of patients with PIH, help patients to return to normal levels of biochemical indexes and renal function indexes, and improve pregnancy outcomes with high safety, which is worthy of further promotion and application in clinical practice.

scholarly journals Safety and efficacy of ampreloxetine in symptomatic neurogenic orthostatic hypotension: a phase 2 trial

2021 ◽  
Author(s):  
Horacio Kaufmann ◽  
Ross Vickery ◽  
Whedy Wang ◽  
Jitendra Kanodia ◽  
Cyndya A. Shibao ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Systolic Blood Pressure ◽  
Orthostatic Hypotension ◽  
Controlled Study ◽  
Neurogenic Orthostatic Hypotension ◽  
Median Dose ◽  
Double Blind ◽  
Supine Blood Pressure ◽  
Part C ◽  
Standing Blood Pressure

Abstract Purpose In neurogenic orthostatic hypotension, blood pressure falls when upright owing to impaired release of norepinephrine, leading to dizziness. Ampreloxetine, a selective norepinephrine reuptake inhibitor, increases circulating norepinephrine levels. This study explored the safety of ampreloxetine and its effect on blood pressure and symptoms in patients with neurogenic orthostatic hypotension. Methods A multicenter ascending-dose trial (range 1–20 mg, Part A) was followed by a 1 day, double-blind, randomized, placebo-controlled study (median dose 15 mg, Part B). Eligible patients then enrolled in a 20-week, open-label, steady-state extension phase (median dose 10 mg, Part C) followed by a 4-week withdrawal. Assessments included the Orthostatic Hypotension Symptom Assessment Scale (item 1), supine/seated/standing blood pressure, and safety. Results Thirty-four patients (age 66 ± 8 years, 22 men) were enrolled. Part A: The proportion of participants with a positive response (i.e., increase from baseline in seated systolic blood pressure of ≥ 10 mmHg) was greater with the 5 and 10 mg ampreloxetine doses than with placebo or other active ampreloxetine doses. Part B: Seated blood pressure increased 15.7 mmHg 4 h after ampreloxetine and decreased 14.2 mmHg after placebo [least squares mean difference (95% CI) 29.9 mmHg (7.6–52.3); P = 0.0112]. Part C: Symptoms of dizziness/lightheadedness improved 3.1 ± 3.0 points from baseline and standing systolic blood pressure increased 11 ± 12 mmHg. After 4 weeks of withdrawal, symptoms returned to pretreatment levels. The effect of ampreloxetine on supine blood pressure was minimal throughout treatment duration. Conclusion Ampreloxetine was well tolerated and improved orthostatic symptoms and seated/standing blood pressure with little change in supine blood pressure. Trial registration NCT02705755 (first posted March 10, 2016).

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