GABAergic Agonists (“Anxiolytics”)

2018 ◽  
pp. 146-151
Author(s):  
S. Nassir Ghaemi
Keyword(s):  
Clinical Pharmacology ◽  
Side Effects ◽  
Butyric Acid ◽  
Gaba Receptors ◽  
Half Life ◽  
Brain Activity ◽  
Basic Mechanism ◽  
Inhibitory Effect ◽  
Gaba A ◽  
Stimulate Activity

The drug class of GABAergic agonists includes the agents that are benzodiazepines and most hypnotic agents. Gamma amino-butyric acid (GABA) receptors are distributed throughout the neocortex, and have a general inhibitory effect on brain activity. All benzodiazepines have the same basic mechanism of activity. Their differences involved their pharmacokinetics; namely, their half-life and speed of onset. They also differ in potency of affect. Benzodiazepines are the classic group of medications that have primarily anti-anxiety effects. Mechanistically, they are GABAergic agonists. In this effect, they stimulate activity at the GABA-a receptor. The clinical pharmacology of specific agents within each class, including efficacy and side effects, is explored. Specific phenomena surveyed include withdrawal, tolerance, and addiction. The limited efficacy of hypnotic agents is scrutinized.

Intoxication with Phenprocoumon (Marcoumar) Pharmacokinetics and Side Effects

1969 ◽  
Vol 21 (02) ◽  
pp. 320-324 ◽  
Author(s):  
K Seiler ◽  
F Duckert
Keyword(s):  
Plasma Concentration ◽  
Side Effects ◽  
Half Life ◽  
Plasma Proteins ◽  
Repeated Administration ◽  
High Plasma ◽  
Vitamin K1 ◽  
Clotting Factors ◽  
Therapeutic Concentration ◽  
High Plasma Concentration

SummaryA case of severe Marcoumar intoxication is described. Eleven hours after the intake a plasma concentration of 15.75 µg/ml was found which corresponds approximately to the 5-fold therapeutic concentration. Repeated administration of vitamin K1 made it possible to avoid extreme lowering of the activity of the clotting factors II, VII and X and to prevent bleeding. Side effects were not observed. The biologic half-life of Phenprocoumon has been found to be shortened at high plasma concentration (3.7 instead of 5.9 days). It is probable that in extreme concentration the drug is less strongly bound to the plasma proteins.

Methotrexate Therapy in Obstetricaĺ Diseases

2016 ◽  
Vol 4 (1) ◽  
pp. 9 ◽  
Author(s):  
Aneta Tomescu ◽  
Rodica Sîrbu ◽  
Stelian Paris ◽  
Emin Cadar ◽  
Cristina Luiza Erimia ◽  
...  
Keyword(s):  
Clinical Pharmacology ◽  
Side Effects ◽  
Ectopic Pregnancy ◽  
Malignant Disease ◽  
Surgical Intervention ◽  
Hydatidiform Mole ◽  
Medical Abortion ◽  
Methotrexate Therapy ◽  
Therapeutic Effects ◽  
Neoplastic Diseases

Our study is a rewiew of Methotrexate therapy in obstetrica? diseases such us: hydatidiform mole, and medical abortion. In the medical world, methotrexate is a citostatic drug used in neoplastic diseases. The clinical pharmacology data regarding methotrexate is presented, alongside route of administration and therapeutic effects in malignant disease, hydatiform mole, and medical abortion. The use of methotrexate in medical abortion and ectopic pregnancy is a great accomplishment, as it replaces a surgical intervention marred by characteristic side effects, with similar results.

Methotrexate Therapy in Obstetricaĺ Diseases

2016 ◽  
Vol 2 (1) ◽  
pp. 9 ◽  
Author(s):  
Aneta Tomescu ◽  
Rodica Sîrbu ◽  
Stelian Paris ◽  
Emin Cadar ◽  
Cristina Luiza Erimia ◽  
...  
Keyword(s):  
Clinical Pharmacology ◽  
Side Effects ◽  
Ectopic Pregnancy ◽  
Malignant Disease ◽  
Surgical Intervention ◽  
Hydatidiform Mole ◽  
Medical Abortion ◽  
Methotrexate Therapy ◽  
Therapeutic Effects ◽  
Neoplastic Diseases

Our study is a rewiew of Methotrexate therapy in obstetrica? diseases such us: hydatidiform mole, and medical abortion. In the medical world, methotrexate is a citostatic drug used in neoplastic diseases. The clinical pharmacology data regarding methotrexate is presented, alongside route of administration and therapeutic effects in malignant disease, hydatiform mole, and medical abortion. The use of methotrexate in medical abortion and ectopic pregnancy is a great accomplishment, as it replaces a surgical intervention marred by characteristic side effects, with similar results.

Protective influence of coded amino acids on the development of liver tissue culture in the presence of cytostatic

2020 ◽  
pp. 48-53
Author(s):  
N. I. Chalisova ◽  
V. K. Kozlov ◽  
A. B. Mulik ◽  
E. P. Zatsepin ◽  
T. A. Kostrova
Keyword(s):  
Amino Acids ◽  
Tissue Culture ◽  
Side Effects ◽  
Liver Tissue ◽  
Organotypic Culture ◽  
Growth Zone ◽  
Inhibitory Effect ◽  
Cytostatic Drugs ◽  
Urgent Problem ◽  
Combined Exposure

An urgent problem is the search for substances that can provide a protective effect in cases of DNA synthesis and repair disorders that arise as a result of side effects of cytostatic drugs used in the treatment of cancer. The aim of this work was to study the effect of 20 encoded amino acids in the presence of Cyclophosphane on the development of organotypic culture of rat liver tissue. The results obtained indicate that Cyclophosphane; which simulates the action of such cytostatic substances; inhibits cell proliferation in the liver tissue. It was also found that the encoded amino acids: asparagine; arginine; and glutamic acid; eliminate the inhibitory effect of Cyclophosphane in liver tissue culture. The growth zone of explants after combined exposure to Cyclophosphane (whose isolated action suppressed the growth zone) and these amino acids increased significantly and reached control values. Thus; the experimental data create the basis for the development of methods for the therapeutic use of the three studied amino acids for the removal of side effects in the treatment with cytostatic drugs.

scholarly journals GABA receptors differentially regulate life span and health span in C. elegans through distinct downstream mechanisms

2019 ◽  
Vol 317 (5) ◽  
pp. C953-C963 ◽  
Author(s):  
Fengling Yuan ◽  
Jiejun Zhou ◽  
Lingxiu Xu ◽  
Wenxin Jia ◽  
Lei Chun ◽  
...  
Keyword(s):  
Life Span ◽  
Gaba Receptors ◽  
Health Span ◽  
Gaba A ◽  
Inhibitory Neurotransmitter ◽  
C Elegans ◽  
Physiological Processes ◽  
Gaba Signaling ◽  
Neuronal Functions

GABA, a prominent inhibitory neurotransmitter, is best known to regulate neuronal functions in the nervous system. However, much less is known about the role of GABA signaling in other physiological processes. Interestingly, recent work showed that GABA signaling can regulate life span via a metabotropic GABAB receptor in Caenorhabditis elegans. However, the role of other types of GABA receptors in life span has not been clearly defined. It is also unclear whether GABA signaling regulates health span. Here, using C. elegans as a model, we systematically interrogated the role of various GABA receptors in both life span and health span. We find that mutations in four different GABA receptors extend health span by promoting resistance to stress and pathogen infection and that two such receptor mutants also show extended life span. Different GABA receptors engage distinct transcriptional factors to regulate life span and health span, and even the same receptor regulates life span and health span via different transcription factors. Our results uncover a novel, profound role of GABA signaling in aging in C. elegans, which is mediated by different GABA receptors coupled to distinct downstream effectors.

Thiopental Inhibits Tumor Necrosis Factor α–induced Activation of Nuclear Factor κB through Suppression of IκB Kinase Activity

2003 ◽  
Vol 99 (2) ◽  
pp. 360-367 ◽  
Author(s):  
Torsten Loop ◽  
Matjaz Humar ◽  
Soeren Pischke ◽  
Alexander Hoetzel ◽  
Rene Schmidt ◽  
...  
Keyword(s):  
Tumor Necrosis Factor ◽  
T Lymphocytes ◽  
Tumor Necrosis ◽  
Kinase Activity ◽  
Inhibitory Effect ◽  
Nuclear Factor ◽  
Ikappab Kinase ◽  
Gaba A ◽  
Nf Kappab ◽  
Necrosis Factor

Background Thiopental is frequently used for the treatment of intracranial hypertension after severe head injury and is associated with immunosuppressive effects. The authors have recently reported that thiopental inhibits activation of nuclear factor (NF) kappaB, a transcription factor implicated in the expression of many inflammatory genes. Thus, it was the aim of the current study to examine the molecular mechanism of this inhibitory effect. Methods The authors tested gamma-aminobutyric acid (GABA), the GABA(A) antagonist bicuculline, and the GABA(B) antagonist dichlorophenyl-methyl-amino-propyl-diethoxymethyl-phosphinic acid (CGP 52432) in combination with thiopental for their influence on the activation of NF-kappaB. In addition, they investigated the direct effect of thiopental on activated NF-kappaB DNA binding activity. These experiments were conducted in Jurkat T lymphocytes using electrophoretic mobility shift assays. The presence of the phosphorylated and dephosphorylated NF-kappaB inhibitor IkappaBalpha (Western blotting) and IkappaB kinase activity were studied in Jurkat T cells and human CD3+ T lymphocytes. In addition, the authors tested the effect of the structural barbiturate analog pairs thiopental-pentobarbital and thiamylal-secobarbital and of thiopental in combination with the thio-group containing chemical dithiothreitol on the activation of NF-kappaB. Results GABA did not inhibit NF-kappaB activation, and the GABA(A) and GABA(B) antagonists bicuculline and CGP did not diminish the thiopental-mediated inhibitory effect on NF-kappaB activation. Thiopental did not inhibit activated NF-kappaB directly in a cell-free system. The phosphorylation of IkappaBalpha was prevented after incubation with 1,000 microg/ml thiopental. The same concentration of thiopental also inhibited IkappaB kinase activity in tumor necrosis factor-stimulated Jurkat T cells and human CD3+ T lymphocytes (60% suppression, P < 0.05 vs. tumor necrosis factor alpha alone). Thiobarbiturates (4 x 10(-3) m) inhibited NF-kappaB activity, whereas equimolar concentrations of the structural oxyanalogs did not. Preincubation of thiopental with dithiothreitol diminished the inhibitory effect. Conclusion Thiopental-mediated inhibition of NF-kappaB activation is due to the suppression of IkappaB kinase activity and depends at least in part on the thio-group of the barbiturate molecule.

scholarly journals Beyond the low frequency fluctuations morning and evening differences in human brain

2019 ◽  
Author(s):  
Magdalena Fafrowicz ◽  
Bartosz Bohaterewicz ◽  
Anna Ceglarek ◽  
Monika Cichocka ◽  
Koryna Lewandowska ◽  
...  
Keyword(s):  
Functional Connectivity ◽  
Resting State ◽  
Human Performance ◽  
Brain Activity ◽  
Activity Patterns ◽  
Low Frequency ◽  
Basic Mechanism ◽  
Time Of Day ◽  
Resting State Functional Connectivity ◽  
Circadian Typology

Human performance, alertness, and most biological functions express rhythmic fluctuations across a 24-hour-period. This phenomenon is believed to originate from differences in both circadian and homeostatic sleep-wake regulatory processes. Interactions between these processes result in time-of-day modulations of behavioral performance as well as brain activity patterns. Although the basic mechanism of the 24-hour clock is conserved across evolution, there are interindividual differences in the timing of sleep-wake cycles, subjective alertness and functioning throughout the day. The study of circadian typology differences has increased during the last few years, especially research on extreme chronotypes, which provide a unique way to investigate the effects of sleep-wake regulation on cerebral mechanisms. Using functional magnetic resonance imaging (fMRI), we assessed the influence of chronotype and time-of-day on resting-state functional connectivity. 29 extreme morning- and 34 evening-type participants underwent two fMRI sessions: about one hour after wake-up time (morning) and about ten hours after wake-up time (evening), scheduled according to their declared habitual sleep-wake pattern on a regular working day. Analysis of obtained neuroimaging data disclosed only an effect of time of day on resting-state functional connectivity; there were different patterns of functional connectivity between morning and evening sessions. The results of our study showed no differences between extreme morning-type and evening-type individuals. We demonstrate that circadian and homeostatic influences on the resting-state functional connectivity have a universal character, unaffected by circadian typology.

scholarly journals Uji Daya Hambat Ekstrak Ikan Nike (Awous melanocephalus) Terhadap Pertumbuhan Bakteri Fusobacterium nucleatum

e-GIGI ◽  
2021 ◽  
Vol 9 (2) ◽  
pp. 238
Author(s):  
Stevia E. Nonutu ◽  
Damajanty H. C. Pangemanan ◽  
Christy N. Mintjelungan
Keyword(s):  
Side Effects ◽  
Treatment Options ◽  
Antibacterial Properties ◽  
Fusobacterium Nucleatum ◽  
Inhibitory Effect ◽  
Positive Control ◽  
Negative Control ◽  
Control Group ◽  
Control Group Design ◽  
Group Design

Abstract: One of the treatment options of periodontal abscess caused by Fusobacterium nucleatum is administration of antibiotics. However, long-term antibiotics consumption can cause negative side effects. Therefore, alternative treatments that have low side effects and easy to be obtained are needed. Nike fish (Awaous melanocephalus) is one of the endemic fish of North Sulawesi province which has antibacterial properties. This study was aimed to evaluate the inhibition effect of nike fish extract on the growth of Fusobacterium nucleatum. This was a true experimental study with a posttest only control group design. We used modified Kirby-Bauer method with filter papers. Ciprofloxacin was used as the positive control and aquadest as the negative control. Extract of nike fish and stock of pure bacteria Fusobacterium nucleatum were prepared. The results showed that the average diameters of the inhibition zones formed in the nike fish extract after three repetitions, were as follows: for extract concentration of 12.5% was 2.91 mm; 25% was 4.16 mm; 50% was 8.41 mm; and 100% was 9.58 mm. In conclusion, nike fish extract (Awaous melanocephalus) at concentrations of 50% and 100% had a weak inhibitory effect (Himedia category) on the growth of Fusobacterium nucleatum meanwhile at concentrations of 12.5% and 25% there was no activity of zone of inhibition.Keywords: extract of nike fish (Awaous melanocephalus); Fusobacterium nucleatum; inhibitory effect Abstrak: Salah satu opsi pengobatan abses periodontal yang disebabkan oleh bakteri Fusobacterium nucleatum yaitu dengan penggunaan antibiotik namun mengonsumsi antibiotik jangka panjang dapat menimbulkan efek samping negatif. Oleh karena itu, diperlukan pengobatan alternatif yang memiliki efek samping rendah serta mudah didapat. Ikan nike merupakan salah satu ikan endemik Provinsi Sulawesi Utara yang berkhasiat sebagai antibakteri. Penelitian ini bertujuan untuk mengetahui daya hambat ekstrak ikan nike (Awaous melanocephalus) terhadap pertumbuhan bakteri Fusobacterium nucleatum. Jenis penelitian ialah eksperimental murni dengan post test only control group design. Metode yang digunakan yaitu metode modifikasi Kirby-Bauer dengan menggunakan paper disk. Kontrol positif menggunakan antibakteri ciprofloxacin dan kontrol negatif menggunakan akuades. Pada penelitian ini digunakan ekstrak ikan nike dan stok bakteri murni Fusobacterium nucleatum. Hasil penelitian menunjukkan bahwa rerata diameter zona hambat yang terbentuk pada ekstrak ikan nike setelah tiga kali pengulangan yaitu untuk konsentrasi 12,5% sebesar 2,91 mm; 25% sebesar 4,16 mm; 50% sebesar 8,41 mm; dan 100% sebesar 9,58 mm. Simpulan penelitian ini ialah ekstrak ikan nike (Awaous melanocephalus) pada konsentrasi 50% dan 100% memiliki daya hambat kategori lemah (Himedia) terhadap pertumbuhan bakteri Fusobacterium nucleatum sedangkan pada konsentrasi 12,5% dan 25% dikategorikan tidak terdapat aktivitas zona hambat. Kata kunci: ekstrak ikan nike (Awaous melanocephalus); Fusobacterium nucleatum; daya hambat

scholarly journals Brain activity patterns in high-throughput electrophysiology screen predict both drug efficacies and side effects

2018 ◽  
Vol 9 (1) ◽  
Author(s):  
Peter M. Eimon ◽  
Mostafa Ghannad-Rezaie ◽  
Gianluca De Rienzo ◽  
Amin Allalou ◽  
Yuelong Wu ◽  
...  
Keyword(s):  
Side Effects ◽  
High Throughput ◽  
Brain Activity ◽  
Activity Patterns
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