In a certain sense, the field of drug metabolism (DM) is standing still. More
specifically, the basic experiment of drug metabolism (i.e., administering a new
drug to an animal or human and determining the structures, amounts, and
disposition of the metabolites) has changed very little over a period of decades.
Remarkably, the experimental design and resulting data set from a typical
absorption, distribution, metabolism, and excretion (ADME) study conducted
today would be instantly recognized and understood by DM scientists from 50
Five years have passed since the first edition of
Principles of Clinical Pharmacology was published. The
second edition remains focused on the principles
underlying the clinical use and contemporary development
of pharmaceuticals. However, recent advances in
the areas of pharmacogenetics, membrane transport,
and biotechnology and in our understanding of the
pathways of drug metabolism, mechanisms of enzyme
induction, and adverse drug reactions have warranted
the preparation of this new edition.
(t1/2) and the apparent volume of distribution Vapp (p. 28) by the equation: Vapp t1/2 = In 2 x –––– Cltot The smaller the volume of distribution or the larger the total clearance, the shorter is the half-life. In the case of drugs renally eliminated in unchanged form, the half-life of elimination can be calculated from the cumulative excretion in urine; the final total amount eliminated corresponds to the amount absorbed.
Adjusting Drug Dosages While elimination half-life determines the time required to achieve steadystate plasma concentrations (Css), the magnitude of that steady state is determined by clearance (Cl) and dose alone.
The sixth edition of Modern Pharmacology With
Clinical Applications continues our commitment
to enlisting experts in pharmacology to provide
a textbook that is up-to-date and comprehensive. Designed
to be used during a single semester, the book focuses
on the clinical application of drugs within a context
of the major principles of pharmacology. It is meant
to serve students in medicine, osteopathy, dentistry,
pharmacy, and advanced nursing, as well as undergraduate
Recent advances in mass spectrometry have rendered it an attractive and versatile tool in industrial and academic research laboratories. As a part of this rapid growth, a considerable body of literature has been devoted to the application of mass spectrometry in clinical studies. In concert with separation techniques such as liquid chromatography, mass spectrometry allows the rapid characterization and quantitative determination of a large array of molecules in complex mixtures.
can be classified according to their respective primary mode of action (color tone in 2 and 3). When bacterial growth remains unaffected by an antibacterial drug, bacterial resistance is present. This may occur because of certain metabolic characteristics that confer a natural insensitivity to the drug on a particular strain of bacteria (natural resistance). Depending on whether a drug affects only a few or numerous types of bacteria, the terms narrow-spectrum (e.g., penicillin G) or broad-spectrum (e.g., tetracyclines) antibiotic are applied.
Principles of Pharmacokinetics The processes of absorption, distribution, metabolism, and excretion— collectively termed drug disposition—determine the concentration of drug delivered to target effector molecules.
When a drug is administered orally, subcutaneously, intramuscularly, rectally, sublingually, or directly into desired sites of action, the amount of drug actually entering the systemic circulation may be less than with the intravenous route (Fig. 5-2A ).
Tuyển tập báo cáo các nghiên cứu khoa học quốc tế ngành hóa học dành cho các bạn yêu hóa học tham khảo đề tài: Molecular and macromolecular alterations of recombinant adenoviral vectors do not resolve changes in hepatic drug metabolism during infection
Many of my friends have been anxious ever since Osteopathy became an established fact, that I should write a
treatise on the science. But I was never convinced that the time was ripe for such a production, nor am I even
now convinced that this is not a little premature. Osteopathy is only in its infancy, it is a great unknown sea
just discovered, and as yet we are only acquainted with its shore-tide.
When I saw others who had not more than skimmed the surface of the science, taking up the pen to write
books on Osteopathy, and after having carefully examined their productions,...
Constitutively expressed human cytochrome P450 2D6 (CYP2D6; EC
18.104.22.168) is responsible for the metabolism of approximately 25% of drugs
in common clinical use. It is widely accepted that CYP2D6 is localized in
the endoplasmic reticulum of cells; however, we have identified this enzyme
in the mitochondria of human liver samples and found that extensive inter-individual variability exists with respect to the level of the mitochondrial
Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học Critical Care giúp cho các bạn có thêm kiến thức về ngành y học đề tài: Drug metabolizing enzyme activities versus genetic variances for drug of clinical pharmacogenomic relevance...
(BQ) Part 1 book "Textbook of organic medicinal and pharmaceutical chemistry" presents the following contents: Drug design strategies, metabolic changes of drugs and related organic compounds, biotechnology and drug discovery, immunobiologicals, anti infective agents, antibacterial antibiotics, antiviral agents,...
(BQ) Part 1 book "Medical pharmacology at a glance" presents the following contents: Principles of drug action, drug absorption, distribution and excretion, drug metabolism, local anaesthetics, autonomic nervous system, autonomic drugs acting at cholinergic synapses, drugs acting on the sympathetic system, ocular pharmacology,... and other contents.
Butyrophenone drugs including haloperidol are being widely used in the field of psychiatry. The acute butyrophenone poisoning incidents sometimes take place; in such cases, the analysis of a butyrophenone becomes necessary in forensic toxicology or clinical toxicology. Their analysis is being made by GC [1–4], GC/MS [5–6], HPLC [7–15] and LC/MS [16,17]. Six butyrophenones are now available as ethical drugs in Japan ( Fig. 2.1); the most typical ones are haloperidol and bromperidol, which most frequently cause poisoning incidents among butyrophenones.
Great efﬁciencies have been achieved in the drug discovery process as a result of technological advances in target identiﬁcation, high-throughput screening, high-throughput organic synthesis, just-in-time in vitro ADME (absorption, distribution, metabolism, and excretion), and early pharmacokinetic screening of drug leads. These advances, spanning target selection all the way through to clinical candidate selection, have placed greater and greater demands on the analytical community to develop robust high-throughput methods.
Methanol (methyl alcohol) poisoning accidents take place most frequently by drinking it in mistake for ethanol. Methanol poisoning is not due to the effect of methanol itself, but due to toxicity of its metabolites. Methanol is rapidly absorbed into human body through the airway mucous membranes, digestive tract mucous membranes or the skin; it is metabolized into formaldehyde (formalin, HCHO) and then formic acid (HCOOH) by the actions of alcohol dehydrogenase and aldehyde dehydrogenase, respectively.
Vitamin C (ascorbic acid) is a water-soluble antioxidant, constituting one among the most
prevalent dietary antioxidants found in fruits, vegetables and beverages. Dietary intake is
usually in the area of 100 mg/d, with a DRI-RDA of 75mg/d (men) and 60mg/d (women)
(National Academy of Sciences, 2000). Food items rich in vitamin C include bell peppers (ca.
120 mg/100g) and citrus fruits such as oranges (ca. 50 mg/100g) (Souci, 2000). Vitamin C
contribution to the total antioxidant activity conferred e.g.
Osteoporosis and fractures may increase due to hypoestrogenism in menopause and
cytochrome P450 inducing AEDs. Recent studies suggest lower bone mineral density (BMD)
in adults and children with epilepsy, irrespective of AED treatment.
Both idiopathic epilepsy and symptomatic epilepsy are associated with reduced BMD, with
the greatest reduction in symptomatic generalized epilepsy (Sheth & Hermann, 2008).
However, the pathophysiological underlying mechanisms are far from understood and likely
Compared with hydrophilic drugs not undergoing transport, lipophilic drugs are more rapidly taken up from the blood into hepatocytes and more readily gain access to mixed-function oxidases embedded in sER membranes. For instance, a drug having lipophilicity by virtue of an aromatic substituent (phenyl ring) (B) can be hydroxylated and, thus, become more hydrophilic (Phase I reaction, p. 34). Besides oxidases, sER also contains reductases and glucuronyl transferases. The latter conjugate glucuronic acid with hydroxyl, carboxyl, amine, and amide groups (p.