cytochrome p-450 3a4 and 2c8 are involved in zopiclone metabolism
... biological half-life and clearance. In humans, zopiclone elimination is mainly dependent on its hepatic clearance because only 5% of the drug is excreted unchanged in the urine (Noble et al., 1998). Indeed, zopiclone is extensively metabolized by the human liver into two major metabolites (Fig. 1): ...
... biological half-life and clearance. In humans, zopiclone elimination is mainly dependent on its hepatic clearance because only 5% of the drug is excreted unchanged in the urine (Noble et al., 1998). Indeed, zopiclone is extensively metabolized by the human liver into two major metabolites (Fig. 1): ...
Lithium Key Points Introduction in General Practice
... Avoid the use of lithium during pregnancy whenever possible. The overall risk of foetal malformations is 4–12% in the first trimester and therefore greater than the general population. Cardiovascular malformations include Ebstein’s anomaly, which can be detected by foetal echocardiography at 16–18 w ...
... Avoid the use of lithium during pregnancy whenever possible. The overall risk of foetal malformations is 4–12% in the first trimester and therefore greater than the general population. Cardiovascular malformations include Ebstein’s anomaly, which can be detected by foetal echocardiography at 16–18 w ...
Chloral hydrate
... Chloral hydrate (synthesized in 1832 and introduced into medicine 1869) is the oldest member of sedative-hypnotic drugs. To the same group belong paraldehyde, bromide, urethane, and sulfonal. Metabolite of chloral hydrate, trichloroethanol, is also an excellent hypnotic agent, but is not often used ...
... Chloral hydrate (synthesized in 1832 and introduced into medicine 1869) is the oldest member of sedative-hypnotic drugs. To the same group belong paraldehyde, bromide, urethane, and sulfonal. Metabolite of chloral hydrate, trichloroethanol, is also an excellent hypnotic agent, but is not often used ...
38: Opioids
... Despite nearly a century of opioid studies, the existence of specific opioid receptors was not proposed until the mid-20th century. Beckett and Casy noted a pronounced stereospecificity of existing opioids (only the l-isomer is active) and postulated that the drug needed to “fit” into a receptor.8 I ...
... Despite nearly a century of opioid studies, the existence of specific opioid receptors was not proposed until the mid-20th century. Beckett and Casy noted a pronounced stereospecificity of existing opioids (only the l-isomer is active) and postulated that the drug needed to “fit” into a receptor.8 I ...
Binding of Imipramine to Phospholipid Bilayers Using
... The tendency to refer to the result of drug-lipid bilayer interaction as “binding” has been subject to discussion because of the general meaning of this term in the classic enzyme-substrate or ligand-receptor interaction studies (Heirwegh et al. 1992). Binding into a bilayer is considered a restrict ...
... The tendency to refer to the result of drug-lipid bilayer interaction as “binding” has been subject to discussion because of the general meaning of this term in the classic enzyme-substrate or ligand-receptor interaction studies (Heirwegh et al. 1992). Binding into a bilayer is considered a restrict ...
Activated Charcoal - Paramedic Advantage
... Bold Text indicates Los Angeles County, California Scope of Practice The authors of this guide have taken care to make certain that the doses of drugs and schedules of treatment are correct and compatible with the standards generally accepted at the time of publication. Nevertheless, as new informat ...
... Bold Text indicates Los Angeles County, California Scope of Practice The authors of this guide have taken care to make certain that the doses of drugs and schedules of treatment are correct and compatible with the standards generally accepted at the time of publication. Nevertheless, as new informat ...
Quinine toxicity identified after 40 years
... In ophthalmology, a correct diagnosis can almost always be made with a detailed history and careful examination. This case illustrates that an important part of the history may somehow be missed. This lady might not have thought that her abortion history was significant, or she may have felt embarra ...
... In ophthalmology, a correct diagnosis can almost always be made with a detailed history and careful examination. This case illustrates that an important part of the history may somehow be missed. This lady might not have thought that her abortion history was significant, or she may have felt embarra ...
allopatry in Batesian mimicry complexes Mimics without models
... phenotype over an alternative non-mimetic phenotype, they could render the mimetic phenotype less costly in allopatry, thereby possibly either maintaining allopatric mimics in the presence of gene flow or maintaining them for longer periods of time following range contraction/expansion. In the first ...
... phenotype over an alternative non-mimetic phenotype, they could render the mimetic phenotype less costly in allopatry, thereby possibly either maintaining allopatric mimics in the presence of gene flow or maintaining them for longer periods of time following range contraction/expansion. In the first ...
A clickable analogue of ketamine retains NMDA receptor activity
... to delayed (e.g., antidepressant at low doses) behavioral changes. We first examined near-anesthetic doses of compounds to test acute psychoactive effects18. We quantified locomotor activity and rearing behavior for 60 min following a single i.p. injection. Ketamine at 100 mg/kg (n = 8) significant ...
... to delayed (e.g., antidepressant at low doses) behavioral changes. We first examined near-anesthetic doses of compounds to test acute psychoactive effects18. We quantified locomotor activity and rearing behavior for 60 min following a single i.p. injection. Ketamine at 100 mg/kg (n = 8) significant ...
Reliable Computation of Equilibrium States and Bifurcations in
... codimension-two bifurcations, namely double-fold (or double-zero) and fold-Hopf. The “codimension” of a bifurcation indicates the number of additional conditions required to specify the particular type of bifurcation, and thus the number of parameters that must be allowed to vary. Thus, to find a c ...
... codimension-two bifurcations, namely double-fold (or double-zero) and fold-Hopf. The “codimension” of a bifurcation indicates the number of additional conditions required to specify the particular type of bifurcation, and thus the number of parameters that must be allowed to vary. Thus, to find a c ...
Diminished Cocaine-Like Effects in Dopamine Transporter Ligands
... Receptor Screen. Three of the compounds, AHN 2-005, GA-I103, and JHW 007, were screened for their activity at various receptor sites by examining their competition with the appropriate radioligands (ProfilingScreen procured from MDS Panlabs Pharmacology Services, Bothell, WA). The screen consisted o ...
... Receptor Screen. Three of the compounds, AHN 2-005, GA-I103, and JHW 007, were screened for their activity at various receptor sites by examining their competition with the appropriate radioligands (ProfilingScreen procured from MDS Panlabs Pharmacology Services, Bothell, WA). The screen consisted o ...
Predicting Trophic Cascades in an Antagonistic
... that black bears, which are predators of ants, were beneficial for plants. Plants near beardamaged ant nests had greater reproduction than those near undamaged nests, due to weaker ant protection for herbivores, which allowed herbivore suppression by arthropod predators. These results suggest that b ...
... that black bears, which are predators of ants, were beneficial for plants. Plants near beardamaged ant nests had greater reproduction than those near undamaged nests, due to weaker ant protection for herbivores, which allowed herbivore suppression by arthropod predators. These results suggest that b ...
Phosphodiesterases Inhibition Enhances the Effect of Glucagon on
... Cell cAMP levels are regulated by the activity of cyclic nucleotide phosphodiesterases (PDE) enzymes which break down cAMP into its chemically inactive product 5’AMP (Bender and Beavo 2006). In contrast to the positive inotropic and chronotropic effects of glucagon which are well established, there ...
... Cell cAMP levels are regulated by the activity of cyclic nucleotide phosphodiesterases (PDE) enzymes which break down cAMP into its chemically inactive product 5’AMP (Bender and Beavo 2006). In contrast to the positive inotropic and chronotropic effects of glucagon which are well established, there ...
managing pulses to minimize frost damage
... reduce the financial exposure to crop loss, but can lessen the chance of a successful hay cut or jeopardize the pulse grain crop when no frost occurs. Manage nodulation to ensure pulse crops are adequately nodulated and well supplied with fixed nitrogen. Pulses deficient or marginal in nitrogen are ...
... reduce the financial exposure to crop loss, but can lessen the chance of a successful hay cut or jeopardize the pulse grain crop when no frost occurs. Manage nodulation to ensure pulse crops are adequately nodulated and well supplied with fixed nitrogen. Pulses deficient or marginal in nitrogen are ...
... mice of the OF.1 strain. Likewise, we compared the behavioural profile of GHB with that induced by mCPP (1 mg/kg, ip), a compound with known anxiogenic actions. GHB-treated mice spent notably less time in the lit area (40 and 80 mg/kg) and more time in the dark area (all doses), whereas the total nu ...
Acetaminophen: Old drug, new warnings
... The liver is damaged by two mechanisms. In one, NAPQI binds to hepatic cell macromolecules, causing dysfunction of the enzymatic systems, structural and metabolic disarray, and eventually necrotic cell death. The other mechanism is oxidative stress due to depletion of glutathione. In children, s ...
... The liver is damaged by two mechanisms. In one, NAPQI binds to hepatic cell macromolecules, causing dysfunction of the enzymatic systems, structural and metabolic disarray, and eventually necrotic cell death. The other mechanism is oxidative stress due to depletion of glutathione. In children, s ...
Potential role of N-methyl-D-aspartate receptors as executors of
... mechanism of action. This assessment does not, however, take into account the fact that memantine is accumulated in intracellular compartments (primarily by lysosomes) (Honegger et al., 1993). Indeed, the analysis of memantine levels in brain homogenates in rats revealed 30-fold higher values than t ...
... mechanism of action. This assessment does not, however, take into account the fact that memantine is accumulated in intracellular compartments (primarily by lysosomes) (Honegger et al., 1993). Indeed, the analysis of memantine levels in brain homogenates in rats revealed 30-fold higher values than t ...
Successful Pregnancy in Recurrent Thin Endometrium
... Citation: Chen X, Chen Sl (2013) Successful Pregnancy in Recurrent Thin Endometrium with New Uses for an Old Drug. J IVF Reprod Med Genet 1: 110. doi:10.4172/2375-4508.1000110 Copyright: © 2013 Chen X, et al. This is an open-access article distributed under the terms of the Creative Commons Attribut ...
... Citation: Chen X, Chen Sl (2013) Successful Pregnancy in Recurrent Thin Endometrium with New Uses for an Old Drug. J IVF Reprod Med Genet 1: 110. doi:10.4172/2375-4508.1000110 Copyright: © 2013 Chen X, et al. This is an open-access article distributed under the terms of the Creative Commons Attribut ...
Chemical defense strategies in sponges: a review
... for different ecological purposes. Biosynthesis costs may be saved, if instead of producing several compounds for multiple purposes, only one metabolite is sequestered that is active against a variety of target organisms and other threats. However, Schmitt et al. (1995) pointed out that multiple use ...
... for different ecological purposes. Biosynthesis costs may be saved, if instead of producing several compounds for multiple purposes, only one metabolite is sequestered that is active against a variety of target organisms and other threats. However, Schmitt et al. (1995) pointed out that multiple use ...
Af,A^yV"-Triethylenethiophosphoramide (Thio
... efficacy and toxicity of anticancer drugs, a major factor is the and further suggest ways in which thio-TEPA pharmacokinetics might bioavailability of cytotoxic molecular species (15). Although be modulated in vivo to achieve improved therapeutic effects. this pharmacokinetic parameter is influenced ...
... efficacy and toxicity of anticancer drugs, a major factor is the and further suggest ways in which thio-TEPA pharmacokinetics might bioavailability of cytotoxic molecular species (15). Although be modulated in vivo to achieve improved therapeutic effects. this pharmacokinetic parameter is influenced ...
100 Essential Drugs - University of Toledo
... MOA: for antidepressant effect: it may decrease supersensitivity of dopamine receptors, increase acetylcholine, enhance 5-HT activity for depression; for anti-mania effect: it may prevent recycling of phosphoinositides, thereby causing depletion of IP3 and DAG, which diminishes excess catecholamines ...
... MOA: for antidepressant effect: it may decrease supersensitivity of dopamine receptors, increase acetylcholine, enhance 5-HT activity for depression; for anti-mania effect: it may prevent recycling of phosphoinositides, thereby causing depletion of IP3 and DAG, which diminishes excess catecholamines ...
ANTICONVULSANT ACTIVITY OF AQUEOUS ROOT EXTRACT OF CALOTROPIS GIGANTEA IN
... the GABA aminergic mechanism, modulation of nicotic and NMDA receptors. And, this effect of the extract may be related mainly to the terpenoids along with cardiac glycosides, carbohydrates, proteins, amino acids and sterols. Thus Calotropis gigantea was observed to have anti convulsant activity agai ...
... the GABA aminergic mechanism, modulation of nicotic and NMDA receptors. And, this effect of the extract may be related mainly to the terpenoids along with cardiac glycosides, carbohydrates, proteins, amino acids and sterols. Thus Calotropis gigantea was observed to have anti convulsant activity agai ...
Sodium Nitroprusside
... Cyanide toxicity Toxicity may occur, particularly with prolonged infusion (>48 hours) or higher than recommended maximum dose, due to accumulation of cyanide or thiocyanate. In normal renal function cyanide accumulates with infusion rate of >2 microgram/kg/minute. Risk of toxicity is greater in rena ...
... Cyanide toxicity Toxicity may occur, particularly with prolonged infusion (>48 hours) or higher than recommended maximum dose, due to accumulation of cyanide or thiocyanate. In normal renal function cyanide accumulates with infusion rate of >2 microgram/kg/minute. Risk of toxicity is greater in rena ...
Role for Reactive Oxygen Species in Methamphetamine Modulation
... today’s society, with over 1 in 20 adults over 26 having taken it at least once. While it is known that METH, a common psychostimulant, acts on both the mesolimbic dopamine (DA) and nigrostriatal DA systems by affecting proteins involved in DA reuptake and vesicular packaging, the specific mechanism ...
... today’s society, with over 1 in 20 adults over 26 having taken it at least once. While it is known that METH, a common psychostimulant, acts on both the mesolimbic dopamine (DA) and nigrostriatal DA systems by affecting proteins involved in DA reuptake and vesicular packaging, the specific mechanism ...
Toxicodynamics
Toxicodynamics, termed pharmacodynamics in pharmacology, describes the dynamic interactions of a toxicant with a biological target and its biological effects. A biological target, also known as the site of action, can be binding proteins, ion channels, DNA, or a variety of other receptors. When a toxicant enters an organism, it can interact with these receptors and produce structural or functional alterations. The mechanism of action of the toxicant, as determined by a toxicant’s chemical properties, will determine what receptors are targeted and the overall toxic effect at the cellular level and organismal level.Toxicants have been grouped together according to their chemical properties by way of quantitative structure-activity relationships (QSARs), which allows prediction of toxic action based on these properties. endocrine disrupting chemicals (EDCs) and carcinogens are examples of classes of toxicants that can act as QSARs. EDCs mimic or block transcriptional activation normally caused by natural steroid hormones. These types of chemicals can act on androgen receptors, estrogen receptors and thyroid hormone receptors. This mechanism can include such toxicants as dichlorodiphenyltrichloroethane (DDE) and polychlorinated biphenyls (PCBs). Another class of chemicals, carcinogens, are substances that cause cancer and can be classified as genotoxic or nongenotoxic carcinogens. These categories include toxicants such as polycyclic aromatic hydrocarbon (PAHs) and carbon tetrachloride (CCl4). The process of toxicodynamics can be useful for application in environmental risk assessment by implementing toxicokinetic-toxicodynamic (TKTD) models. TKTD models include phenomenas such as time-varying exposure, carry-over toxicity, organism recovery time, effects of mixtures, and extrapolation to untested chemicals and species. Due to their advantages, these types of models may be more applicable for risk assessment than traditional modeling approaches.