CLINICAL INVESTIGATIONS OF A LONG-ACTING OESTRIOL (POLYOESTRIOL PHOSPHATE)

1961 ◽  
Vol 38 (1) ◽  
pp. 73-87 ◽  
Author(s):  
Christian Lauritzen ◽  
Semih Velibese
Keyword(s):  
Side Effects ◽  
Phosphoric Acid ◽  
Quantitative Data ◽  
Water Soluble ◽  
Cholesterol Concentration ◽  
Experimental Investigations ◽  
Clinical Investigations ◽  
Prolonged Duration ◽  
High Doses ◽  
Long Acting

ABSTRACT A description is given of experimental investigations and preliminary clinical experience with the long-acting oestriol compound polyoestriol phosphate – a water-soluble polymere of oestriol and phosphoric acid. The compound seems to exert all the physiologically important effects of oestriol. Even with high doses the hormone causes no proliferation of the endometrium and no withdrawal bleeding. It has no untoward effect on metabolism. It decreases slightly the cholesterol concentration (to the extent of ⅓–⅕ of the effect produced by long-acting oestradiol esters). The compound has a wide therapeutic range. No side-effects have been observed. Doses of 10 mg or more have a prolonged duration. Additional prolongation of the effect is largely dependent on dosage. To ensure an effect lasting for 4 weeks 40 mg polyoestriol phosphate (corresponding with 30 mg oestriol) is required – an amount which roughly corresponds with physiological quantitative data. The compound, which involves an interesting new principle of prolongation, was most effectively used in the treatment of menopausal symptoms and genital organic disorders. For these indications it can be recommended without reservation.

scholarly journals Usefulness of an injectable anaesthetic protocol for semen collection through urethral catheterisation in domestic cats

2016 ◽  
Vol 19 (10) ◽  
pp. 1087-1090 ◽  
Author(s):  
Maria Carmela Pisu ◽  
Patrizia Ponzio ◽  
Chiara Rovella ◽  
Michela Baravalle ◽  
Maria Cristina Veronesi
Keyword(s):  
Side Effects ◽  
Bolus Injection ◽  
Domestic Cats ◽  
Short Term ◽  
Semen Collection ◽  
Clinical Investigations ◽  
Urethral Catheterisation ◽  
Semen Storage ◽  
High Doses ◽  
Adult Cats

Objectives Although less often requested in comparison with dogs, the collection of semen in cats can be necessary for artificial insemination, for semen evaluation in tom cats used for breeding and for semen storage. Urethral catheterisation after pharmacological induction with medetomidine has proved to be useful for the collection of semen in domestic cats. However, most of the previously used protocols require the administration of high doses of medetomidine that can increase the risk of side effects, especially on the cardiovascular system. In routine clinical practice, one safe and useful injectable anaesthetic protocol for short-term clinical investigations or surgery in cats involves premedication with low intramuscular doses of dexmedetomidine with methadone, followed by intravenous propofol bolus injection. We aimed to assess the usefulness of this injectable anaesthetic protocol for semen collection, via urethral catheterisation, in domestic cats. Methods The study was performed on 38 purebred, adult cats, during the breeding season, and semen was collected via urethral catheterisation using an injectable anaesthesia protocol with methadone (0.2 mg/kg) and dexmedetomidine (5 µg/kg) premedication, followed by induction with propofol. Results The anaesthetic protocol used in the present study allowed the collection of large-volume semen samples, characterised by good parameters and without side effects. Conclusions and relevance The results from the present study suggest that the injectable anaesthetic protocol using methadone and dexmedetomidine premedication, followed by induction with propofol, could be suitable and safe for the collection of a good-quality semen sample, via urethral catheterisation, in domestic cats. It can therefore be used as an alternative to previous medetomidine-based sedation protocols.

Initial Studies of a Potent Antiheparin Agent (Ubiquin®)

1968 ◽  
Vol 20 (03/04) ◽  
pp. 588-595 ◽  
Author(s):  
E. B Goodsell ◽  
R. A Krause ◽  
E. T Kimura
Keyword(s):  
Side Effects ◽  
Acute Toxicity ◽  
Propylene Oxide ◽  
Toluidine Blue ◽  
Water Soluble ◽  
Per Se

SummaryUbiquin (oligo-3-(N-methylmorpholinium)-l,2-propylene oxide chloride) is a stable, water soluble, active heparin antagonist producing prompt neutralization when administered in a 1:1 ratio to rats and dogs. Initial studies indicate that it is devoid of any effect on coagulation per se; nor are there any obvious side effects manifested during the process of neutralization. The acute toxicity is less than that of other compounds in use: toluidine blue, protamine and hexadimethrine.

scholarly journals Insights on Molecular Characteristics of Hydrochars by 13C-NMR and Off-Line TMAH-GC/MS and Assessment of Their Potential Use as Plant Growth Promoters

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1026 ◽  
Author(s):  
Laís G. Fregolente ◽  
João Vitor dos Santos ◽  
Giovanni Vinci ◽  
Alessandro Piccolo ◽  
Altair B. Moreira ◽  
...  
Keyword(s):  
Plant Growth ◽  
Phosphoric Acid ◽  
13C Nmr ◽  
Chemical Properties ◽  
Water Soluble ◽  
Molecular Characteristics ◽  
Initial Growth ◽  
Growth Promoters ◽  
Molecular Features ◽  
Potential Use

Hydrochar is a carbon-based material that can be used as soil amendment. Since the physical-chemical properties of hydrochar are mainly assigned to process parameters, we aimed at evaluating the organic fraction of different hydrochars through 13C-NMR and off-line TMAH-GC/MS. Four hydrochars produced with sugarcane bagasse, vinasse and sulfuric or phosphoric acids were analyzed to elucidate the main molecular features. Germination and initial growth of maize seedlings were assessed using hydrochar water-soluble fraction to evaluate their potential use as growth promoters. The hydrochars prepared with phosphoric acid showed larger amounts of bioavailable lignin-derived structures. Although no differences were shown about the percentage of maize seeds germination, the hydrochar produced with phosphoric acid promoted a better seedling growth. For this sample, the greatest relative percentage of benzene derivatives and phenolic compounds were associated to hormone-like effects, responsible for stimulating shoot and root elongation. The reactions parameters proved to be determinant for the organic composition of hydrochar, exerting a strict influence on molecular features and plant growth response.

scholarly journals A New Approach to Developing Long-Acting Injectable Formulations of Anti-HIV Drugs: Poly(Ethylene Phosphoric Acid) Block Copolymers Increase the Efficiency of Tenofovir against HIV-1 in MT-4 Cells

2020 ◽  
Vol 22 (1) ◽  
pp. 340
Author(s):  
Ilya Nifant’ev ◽  
Andrei Siniavin ◽  
Eduard Karamov ◽  
Maxim Kosarev ◽  
Sergey Kovalchuk ◽  
...  
Keyword(s):  
Controlled Release ◽  
Block Copolymers ◽  
Phosphoric Acid ◽  
Hiv Infection ◽  
Targeted Delivery ◽  
Release Formulation ◽  
Poly Ethylene ◽  
Long Acting ◽  
Hiv Drugs ◽  
Anti Hiv

Despite the world’s combined efforts, human immunodeficiency virus (HIV), the causative agent of AIDS, remains one of the world’s most serious public health challenges. High genetic variability of HIV complicates the development of anti-HIV vaccine, and there is an actual clinical need for increasing the efficiency of anti-HIV drugs in terms of targeted delivery and controlled release. Tenofovir (TFV), a nucleotide-analog reverse transcriptase inhibitor, has gained wide acceptance as a drug for pre-exposure prophylaxis or treatment of HIV infection. In our study, we explored the potential of tenofovir disoproxil (TFD) adducts with block copolymers of poly(ethylene glycol) monomethyl ether and poly(ethylene phosphoric acid) (mPEG-b-PEPA) as candidates for developing a long-acting/controlled-release formulation of TFV. Two types of mPEG-b-PEPA with numbers of ethylene phosphoric acid (EPA) fragments of 13 and 49 were synthesized by catalytic ring-opening polymerization, and used for preparing four types of adducts with TFD. Antiviral activity of [mPEG-b-PEPA]TFD or tenofovir disoproxil fumarate (TDF) was evaluated using the model of experimental HIV infection in vitro (MT-4/HIV-1IIIB). Judging by the values of the selectivity index (SI), TFD exhibited an up to 14-fold higher anti-HIV activity in the form of mPEG-b-PEPA adducts, thus demonstrating significant promise for further development of long-acting/controlled-release injectable TFV formulations.

scholarly journals Oral and Palmitate Paliperidone Long-Acting Injectable Formulations use in Schizophrenia Spectrum Disorders: a retrospective cohort study from the CRUPEP First Episode Psychosis Intervention Program

2021 ◽  
Author(s):  
R Segarra ◽  
M Recio-Barbero ◽  
M Sáenz-Herrero ◽  
O Mentxaka ◽  
J Cabezas-Garduño ◽  
...  
Keyword(s):  
Side Effects ◽  
Retrospective Cohort ◽  
Intervention Program ◽  
Therapeutic Option ◽  
Cohort Analysis ◽  
Clinical Information ◽  
First Episode ◽  
Psychotic Episode ◽  
Schizophrenia Spectrum Disorders ◽  
Long Acting

Abstract Background Long-acting injectable antipsychotics (LAIs) may be a suitable therapeutic option for those patients in earlier stages of psychosis to avoid relapses and disease progression. Despite that, there is a lack of evidence in the literature regarding the use of LAIs in this profile of patients. Methods This is a retrospective cohort analysis to assess the efficacy, tolerability, and pattern of use of palmitate paliperidone long-acting injectable (PPLAI) formulations (1-monthly and 3-monthly) compared to oral paliperidone/risperidone in patients with a non-affective First Psychotic Episode(FEP) over a 12-month follow-up. Relevant sociodemographic and clinical information were assessed as well as main clinical scales: Positive and Negative Syndrome Scale (PANSS), Personal and Social Performance Scale (PSP), and Clinical Global Impression Scale (CGI-I and CGI-S). Results Forty-eight patients, 16 per arm, 20-50 year aged with a FEP were included. Significant improvements were registered for all treatment groups. Despite that, patients receiving PPLAI 1-monthly and PPLAI 3-monthly formulations obtained greater improvements than the oral group in the main domains assessed (p<0.001). We found no statistically significant differences in hospitalizations between groups. Side effects were presented in 24% of patients. A trend towards reducing antipsychotic doses was observed in 43.8% of patients to achieve the minimum effective dose and avoid the occurrence of side effects. Conclusions To our knowledge, this is the first study assessing the use of palmitate paliperidone long-acting formulations versus oral risperidone or paliperidone in FEP. Treatment with PPLAI formulations seems to be an effective therapeutic choice at earlier stages of the disease.

Experimental Methodologies: Two Case Studies Investigating the Syntax- Discourse Interface

2013 ◽  
Vol 6 (1) ◽  
Author(s):  
Timothy Gupton ◽  
Tania Leal Méndez
Keyword(s):  
Experimental Data ◽  
Quantitative Data ◽  
Native Speaker ◽  
Experimental Methods ◽  
Experimental Investigations ◽  
Experimenter Bias ◽  
Current Article ◽  
Theoretical Syntax ◽  
Discourse Interface ◽  
L1 And L2

AbstractThe current article examines two experimental investigations of the syntaxdiscourse interface, which address theoretical questions in different ways: the first is an L1 investigation of Galician speakers in Gupton (2010) and the second is a dual investigation of L1 and L2 Spanish reported on in Leal Méndez & Slabakova (2011). These investigations gathered quantitative data via psycholinguistic tasks with accompanying audio utilizing the WebSurveyor platform. They involved counterbalanced designs and were followed by statistical analysis. While acknowledging that experimental data does not have primacy over intuitive data, the authors endorse the use of experimental methods of data elicitation (such as the ones already used in generative SLA research) in theoretical syntax in order to avoid experimenter bias and to get a more complete picture of native speaker intuition and competencies.

Effectiveness and safety of modern treatment against nausea and vomiting induced by chemotherapy and radiotherapy

2021 ◽  
Vol 14 (1) ◽  
pp. 11-15
Author(s):  
Łukasz Hajac ◽  
Martyna Hajac ◽  
Adam Maciejczyk
Keyword(s):  
Side Effects ◽  
Serotonin Syndrome ◽  
Nausea And Vomiting ◽  
Effective Prevention ◽  
Important Group ◽  
Life Threatening ◽  
Treatment Changes ◽  
Long Acting ◽  
Methods Of Treatment

Nausea and vomiting are one of most frequent side effects of chemotherapy and radiotherapy. Effective prevention and treatment of these symptoms is essential for better quality of life for patients undergoing oncological therapies. Nausea and vomiting can be acute, delayed or anticipatory. Leading mechanisms and methods of treatment are different for each of those. Most often used groups of drugs are: 5-HT3-antagonists, glucocorticosteroids, NK1-antagonists. Another important group are neuroleptics, which are therapy of choice for anticipatory vomiting. Modern antiemetic medications are in most cases safe and effective. But as every treatment it causes risks of adverse events which may be serious and difficult to manage. It applies in particular to long-acting drugs. Most common side effects are headache, constipation and sedation. But more severe or life-threatening symptoms may appear, like intestinal obstruction and serotonin syndrome. Some of the drugs also come with risk of interacting with other treatment. Changes in pharmacokinetics may lead to additional toxicities. In elderly, especially with cardiac disease, in risk of ileus or cachexia these drugs shall be used with caution.

scholarly journals UJI AKTIVITAS EKSTRAK BUAS-BUAS (PREMNA SERRATIFOLIA LINN) SEBAGAI ANTI KOLESTEROL SECARA IN VITRO

2017 ◽  
Vol 5 (1) ◽  
Author(s):  
Dini Hadiarti
Keyword(s):  
Solvent Extraction ◽  
Side Effects ◽  
Herbal Medicine ◽  
Cholesterol Concentration ◽  
Standard Curve ◽  
Synthetic Drugs ◽  
Standard Solution ◽  
The Cost

ABSTRACTPremna Serratifolia Linn is believed to reduce cholesterol and as an alternative herbal medicine solution among the cost of medicine and the side effects caused by synthetic drugs. This study was conducted in several phases by using Premna Serratifolia Linn which was drained, mashed, and macerated using ethanol, choloform, and n-heksane. Extract obtained from evaporation, then whighed, and stored in a desiccators. Anti-cholesterol activity was tested test by using in vitro : began with determination of the maximum wavelength of the cholesterol standard solution with a UV-Vis spectrophotometer and continued by manufacturing the standard curve with the cholesterol concentration of 0.5; 0.75; 1; 1.25; and 1.5 mL and 1000 ppm cholesterol solution. Furthermore, maximum absorbance wavelength was measured in order to obtain the maximum wavelength of the cholesterol. The study reveled that the solvent extraction of ethanol produced the largest  rendement. The extract Premna Serratifolia Linn is functioned as an anti-cholesterol. In addition,  the absorbed reduction of 100 ppm cholesterol standard solution found in the addition of 0.5 mL choloform extract.Keywords: Anti-cholesterol, Premna Serratifolia Linn, In Vitro

scholarly journals Hydrosoluble and Liposoluble Vitamins: New Perspectives through ADMET Analysis

Medicina ◽  
2021 ◽  
Vol 57 (11) ◽  
pp. 1204
Author(s):  
Mirela Nicolov ◽  
Mioara Cocora ◽  
Valentina Buda ◽  
Corina Danciu ◽  
Adina Octavia Duse ◽  
...  
Keyword(s):  
Side Effects ◽  
Oral Absorption ◽  
Chemical Properties ◽  
Structural Complexity ◽  
Computational Tool ◽  
Vitamin B3 ◽  
Fortified Foods ◽  
Physico Chemical ◽  
High Doses ◽  
Major Data

Background and Objectives: The present study demonstrates that apart from the well-known toxicity of liposoluble vitamins, some hydrosoluble vitamins may also exert toxicity; thus, routine supplementation with vitamins or ingestion of fortified foods should not be considered harmless. The study addresses the possible correlations between the physico-chemical properties and the side effects of vitamins when taken in high doses or for a too long a period. Materials and Methods: The FAFDrugs4.0 computational tool was used for computational assessment of the ADMET profile of several hydro- and liposoluble vitamins. Results: ADMET analysis revealed the following major data: vitamin B3 and B13 showed reduced structural complexity; thus, a relative toxicological potential may be exerted. Vitamins B1 and B7 were found to have good oral absorption and thus good bioavailability, while Vitamin B3 was found to have decreased oral absorption. In addition, all of the liposoluble vitamins reflected higher complexity, much greater than most of the potentially therapeutically-proven compounds. Conclusions: The present study emphasizes the importance between the physico-chemical properties of vitamins and their possible toxicological impact.

scholarly journals The next generation of RNA vaccines: self-amplifying RNA

2021 ◽  
Author(s):  
Anna Blakney
Keyword(s):  
Side Effects ◽  
Messenger Rna ◽  
Rapid Development ◽  
Next Generation ◽  
High Efficacy ◽  
Vaccine Platform ◽  
The Future ◽  
High Doses ◽  
The Stability

The global COVID-19 pandemic has brought tremendous momentum to the field of messenger RNA (mRNA) vaccines. The advantages of this vaccine platform, such as rapid development and high efficacy, resulted in mRNA vaccines being the first approved vaccines against COVID-19. Looking forward to the development of future vaccines, how can we make RNA vaccines even better? While improvements in the stability of the formulation and cost of the vaccine are inevitable, one of the main challenges is lowering the dose of RNA in order to avoid side effects associated with high doses of RNA. One way to do this is by using self-amplifying RNA (saRNA), a type of mRNA that encodes a replicase that copies the original strand of RNA once it’s in the cell. Here, we discuss the origins of saRNA, how it works in comparison to mRNA, current challenges in the field and the future of saRNA vaccines.

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