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An Introduction to Drug Disposition: The Basic Principles of
An Introduction to Drug Disposition: The Basic Principles of

... by simple diffusion under the influence of pH gradients, binding to intracellular constituents, or partitioning into lipid depots. Larger or more polar substances do not cross lipid membranes by passive diffusion and require specific transporters to enter the tissues (44). If a drug does enter a tis ...
Suggestion from clinicians
Suggestion from clinicians

... This review provides a reasonable amount of data to assess the trough BP lowering effect of 9 different ARBs. When the different ARBs are compared, there is a similarity in their BP lowering effects at trough. When the best estimate of the near maximal BP lowering efficacy of these 9 drugs is compar ...
[Product Monograph Template
[Product Monograph Template

... estrogens versus women treated with placebo.49 It is recommended that estrogens with or without progestins not be given to women with existing breast cancer or those with a previous history of the disease. (see CONTRAINDICATIONS) There is a need for caution in prescribing estrogens with or without p ...
A future initiative for the Folger Passage Node
A future initiative for the Folger Passage Node

... Open circles – observed recruitment; closed circles – predicted recruitment ...
Observed Drug-Receptor Association Rates Are Governed by
Observed Drug-Receptor Association Rates Are Governed by

... Values. To correct for the increased concentration of drug in the membrane we first estimated how much each ligand concentrates in the membrane and then used this new concentration to calculate a “corrected” kon. KIAM is a partition coefficient that essentially describes the degree to which a ligand ...
Hormones in the spotlight
Hormones in the spotlight

... of certain substances for therapeutic uses and livestock breeding. In other countries such as the US, Canada, Brazil, Australia and New Zeeland the legal use of hormones in stockfarming is common practice. ...
Concepts and approaches for marine ecosystem research with
Concepts and approaches for marine ecosystem research with

... consumption rates and biomasses for each system compartment. Moreover, system indices for a characterization and comparison with other systems can be obtained such as average trophic efficiency, energy throughput, and degree of connectivity, degree of maturity, and others. Recent dynamic extensions ...
HORIZONS Modelling emergent trophic strategies in plankton
HORIZONS Modelling emergent trophic strategies in plankton

... including transporter proteins (ATPases) and enzymes for reducing substrates (e.g. nitrate reductase) for dissolved nutrients. Since uptake sites are substrate-specific and some groups of organisms have specific elemental needs, this trait may be divided into several (Klausmeier et al., 2004). The b ...
Factors Influencing the Extent of the Inflammatory Response to
Factors Influencing the Extent of the Inflammatory Response to

... dose-dependent reductions in lymphocyte proliferation to T- and B-cell mitogens, natural killer cell cytotoxicity, and the production of IL-2 and interferon- .Morphine also increases the secretion of CRH, ACTH, and glucocorticoids, i.e., substances with inhibitory effects on the immune system. Certa ...
Steroids (Anabolic-Androgenic)
Steroids (Anabolic-Androgenic)

... receptors on the surface of a cell. This AAS–receptor complex can then shuttle into the cell nucleus to influence patterns of gene expression. Because of this, the acute effects of AAS in the brain are substantially different from those of other drugs of abuse. The most important difference is that ...
7-Keto DHEA The Fat-Burning Metabolite of DHEA
7-Keto DHEA The Fat-Burning Metabolite of DHEA

... rapid rate than cortisol, this creates a period of cortisol dominance that can wreak havoc on the immune system. For these reasons, supplementation with 7-Keto is often appropriate.” Studies have demonstrated that 7-Keto does not accumulate in the body over time and is free of unhealthy side effects ...
A phase I study of indole-3-carbinol in women
A phase I study of indole-3-carbinol in women

... dose. This subject subsequently admitted to a prior history of asthma, which she had denied at the time she was enrolled. Because this subject had completed all procedures for measurement of I3C effects, her data are included here. Numerous endocrine markers and endocrine-related functions have been ...
The Value of Phenotypic Screening to Drug Discovery
The Value of Phenotypic Screening to Drug Discovery

... phenotypic  screening  iden;fies  chemical  en;;es  that  have  desirable  biological   (phenotypic)  effects  on  cells  or  organisms  without  having  prior  knowledge  of  their   biological  ac;vity  or  mode  of  ac;on  against  a  specifi ...
NIDA InfoFacts- Steroids (Anabolic-Androgenic)
NIDA InfoFacts- Steroids (Anabolic-Androgenic)

... the opportunity, just as they do with other addictive drugs. 3,4 This property is more difficult to demonstrate in humans, but the potential for AAS abusers to become addicted is consistent with their continued abuse despite physical problems and negative effects on social relations. 5Also, steroid ...
ANTIHYPERLIPIDAEMIC DRUGS
ANTIHYPERLIPIDAEMIC DRUGS

... muscle and adipose tissue to fatty acids, which then enter the cells. The chylomicron remnants, which have lost much of their triglyceride content, are taken up by the liver for disposal. The liver synthesizes triglycerides and cholesterol, and packages them as VLDLs before releasing them into the b ...
ANTIHYPERLIPIDAEMIC DRUGS
ANTIHYPERLIPIDAEMIC DRUGS

... muscle and adipose tissue to fatty acids, which then enter the cells. The chylomicron remnants, which have lost much of their triglyceride content, are taken up by the liver for disposal. The liver synthesizes triglycerides and cholesterol, and packages them as VLDLs before releasing them into the b ...
Biacore™ concentration and ligand-binding analyses in late
Biacore™ concentration and ligand-binding analyses in late

... Degradation ...
Drugs for Bronchial Asthma, Antitussives, Expectorants
Drugs for Bronchial Asthma, Antitussives, Expectorants

... 3. Does’t cause constipation and addiction; mucuciliary function is not affected. Antihistamines: Diphenhydramine, chlorpheniramine, promethazine are useful in cough because: ...
View the article - Jefferson Digital Commons
View the article - Jefferson Digital Commons

... and chemicals during the period of embryonic development, from fertilization through the early postimplantation stage. Surviving embryos have malformation rates that are similar to those of control subjects because significant cell loss o r chromosome abnormalities at these stages has a high likelih ...
Powerpoint
Powerpoint

... prediction, we are particularly interested in how AFP techniques can be applied to the pharmaceutical sciences – this is what I will cover today ...
Indirect cholinergic agonists
Indirect cholinergic agonists

... Anticholinesterases inhibit action of acetylcholinesterase on Ach thus prevent hydrolysis of Ach and increases its concentration at the cholinergic receptors (both nicotinic and muscarinic). ...
Food for Thought … on In Silico Methods in Toxicology
Food for Thought … on In Silico Methods in Toxicology

... requirements without testing. This applies to approaches 5-8, but a clear focus will be on (Q)SAR as the most prominent technique. Only consideration 2 will address approaches 1-4, which can be understood as in silico tools used together with in vitro and in vivo methods. Approach 9 (PBPK) shall be ...
Gastrointestinal Drugs
Gastrointestinal Drugs

... Saline laxatives increase osmotic pressure in small intestine ◦ Inhibit absorption of water & elytes ◦ Increase amount of water & elytes ...
4) Van der waals interaction
4) Van der waals interaction

... - Irreversible, strong bond => may result in toxicity - Main problem or disadvantage for covalently bound drugs is activity regenerate (get back to the synthesis of the receptor) => this may be advantage in the case of antimicrobial agent while it will be a disadvantage when the receptor is essentia ...
Using species distribution and occupancy modeling to guide survey
Using species distribution and occupancy modeling to guide survey

... reduce model bias. Since this region has been poorly sampled, a true target-group background could not be used. In ArcGIS, we measured the elevation and percent canopy cover at each pond and background point from a 30 m digital elevation layer (DEM) and percent canopy layer, respectively. We also de ...
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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.
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