Area-under-the-curve (pharmacokinetics)
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Area-under-the-curve (pharmacokinetics)
In the field of pharmacokinetics, the area under the curve (AUC) is the definite integral of the concentration of a drug in blood plasma as a function of time (this can be done using liquid chromatography–mass spectrometry). In practice, the drug concentration is measured at certain discrete points in time and the trapezoidal rule is used to estimate AUC. Interpretation and usefulness of AUC values The AUC (from zero to infinity) represents the ''total drug exposure across time''. AUC is a useful metric when trying to determine whether two formulations of the same dose (for example a capsule and a tablet) result in equal amounts of tissue or plasma exposure. Another use is in the therapeutic drug monitoring of drugs with a narrow therapeutic index. For example, gentamicin is an antibiotic that can be nephrotoxic (kidney damaging) and ototoxic (hearing damaging); measurement of gentamicin through concentrations in a patient's plasma and calculation of the AUC is used to guide the ...
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Pharmacokinetics
Pharmacokinetics (from Ancient Greek ''pharmakon'' "drug" and ''kinetikos'' "moving, putting in motion"; see chemical kinetics), sometimes abbreviated as PK, is a branch of pharmacology dedicated to determining the fate of substances administered to a living organism. The substances of interest include any chemical xenobiotic such as: pharmaceutical drugs, pesticides, food additives, cosmetics, etc. It attempts to analyze chemical metabolism and to discover the fate of a chemical from the moment that it is administered up to the point at which it is completely eliminated from the body. Pharmacokinetics is the study of how an organism affects a drug, whereas pharmacodynamics (PD) is the study of how the drug affects the organism. Both together influence dosing, benefit, and adverse effects, as seen in PK/PD models. Overview Pharmacokinetics describes how the body affects a specific xenobiotic/chemical after administration through the mechanisms of absorption and distribution, as ...
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Antibiotic
An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting bacterial infections, and antibiotic medications are widely used in the treatment and prevention of such infections. They may either kill or inhibit the growth of bacteria. A limited number of antibiotics also possess antiprotozoal activity. Antibiotics are not effective against viruses such as the common cold or influenza; drugs which inhibit viruses are termed antiviral drugs or antivirals rather than antibiotics. Sometimes, the term ''antibiotic''—literally "opposing life", from the Greek roots ἀντι ''anti'', "against" and βίος ''bios'', "life"—is broadly used to refer to any substance used against microbes, but in the usual medical usage, antibiotics (such as penicillin) are those produced naturally (by one microorganism fighting another), whereas non-antibiotic antibacterials (such as sulfonamides and antiseptics) ...
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Cmean (pharmacology)
Cavg is the average concentration of a drug in the central circulation during a dosing interval in steady state. It is calculated by :C_=\frac where AUC_ is the area under the curve and \tau the dosing interval. See also * Area under the curve (pharmacokinetics) In the field of pharmacokinetics, the area under the curve (AUC) is the definite integral of the concentration of a drug in blood plasma as a function of time (this can be done using liquid chromatography–mass spectrometry). In practice, the drug ... * Cmax (pharmacology) References Pharmacokinetic metrics {{Pharmacology-stub ...
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Cmax (pharmacology)
Cmax is the maximum (or peak) serum concentration that a drug achieves in a specified compartment or test area of the body after the drug has been administered and before the administration of a second dose. It is a standard measurement in pharmacokinetics. Description Cmax is the opposite of Cmin, which is the minimum (or trough) concentration that a drug achieves after dosing. The related pharmacokinetic parameter tmax is the time at which the Cmax is observed. After an intravenous administration, Cmax and tmax are closely dependent on the experimental protocol, since the concentrations are always decreasing after the dose. But after oral administration, Cmax and tmax are dependent on the extent, and the rate of drug absorption and the disposition profile of the drug. They could be used to characterize the properties of different formulations in the same subject. Short term drug side effects are most likely to occur at or near the Cmax, whereas the therapeutic effect of ...
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Bioavailability
In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. However, when a medication is administered via routes other than intravenous, its bioavailability is generally lower than that of intravenous due to intestinal endothelium absorption and first-pass metabolism. Thereby, mathematically, bioavailability equals the ratio of comparing the area under the plasma drug concentration curve versus time (AUC) for the extravascular formulation to the AUC for the intravascular formulation. AUC is used because AUC is proportional to the dose that has entered the systemic circulation. Bioavailability of a drug is an average value; to take population variability into account, deviation range is shown as ±. To ensure that the drug taker who has poor absorption is dosed appropriately, the bottom value o ...
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Clearance (medicine)
In pharmacology, clearance is a pharmacokinetic measurement of the volume of plasma from which a substance is completely removed per unit time. Usually, clearance is measured in L/h or mL/min. The quantity reflects the rate of drug elimination divided by plasma concentration. Excretion, on the other hand, is a measurement of the amount of a substance removed from the body per unit time (e.g., mg/min, μg/min, etc.). While clearance and excretion of a substance are related, they are not the same thing. The concept of clearance was described by Thomas Addis, a graduate of the University of Edinburgh Medical School. Substances in the body can be cleared by various organs, including the kidneys, liver, lungs, etc. Thus, total body clearance is equal to the sum clearance of the substance by each organ (e.g., renal clearance + hepatic clearance + lung clearance = total body clearance). For many drugs, however, clearance is solely a function of renal excretion. In these cases, clearance is ...
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Ototoxin
Ototoxicity is the property of being toxic to the ear (''oto-''), specifically the cochlea or auditory nerve and sometimes the vestibular system, for example, as a side effect of a drug. The effects of ototoxicity can be reversible and temporary, or irreversible and permanent. It has been recognized since the 19th century. There are many well-known ototoxic drugs used in clinical situations, and they are prescribed, despite the risk of hearing disorders, for very serious health conditions. Ototoxic drugs include antibiotics (such as gentamicin, streptomycin, tobramycin), loop diuretics (such as furosemide), and platinum-based chemotherapy agents (such as cisplatin and carboplatin). A number of nonsteroidal anti-inflammatory drugs (NSAIDS) have also been shown to be ototoxic. This can result in sensorineural hearing loss, dysequilibrium, or both. Some environmental and occupational chemicals have also been shown to affect the auditory system and interact with noise. Signs and s ...
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Nephrotoxin
Nephrotoxicity is toxicity in the kidneys. It is a poisonous effect of some substances, both toxic chemicals and medications, on kidney function. There are various forms, and some drugs may affect kidney function in more than one way. Nephrotoxins are substances displaying nephrotoxicity. Nephrotoxicity should not be confused with some medications predominantly excreted by the kidneys needing their dose adjusted for the decreased kidney function (e.g., heparin, lithium). Types of toxicity Cardiovascular * General: diuretics, β-blockers, vasodilator agents * Local: ACE inhibitors, ciclosporin, tacrolimus. Direct tubular effect * Proximal convoluted tubule: Aminoglycoside antibiotics (e.g., gentamicin), amphotericin B, cisplatin, radiocontrast media, immunoglobulins, mannitol * Distal tubule: NSAIDs (e.g. aspirin, ibuprofen, diclofenac), ACE inhibitors, ciclosporin, lithium salts, cyclophosphamide, amphotericin B * Tubular obstruction: sulphonamides, methotrexate, aciclovir, diet ...
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Gentamicin
Gentamicin is an antibiotic used to treat several types of bacterial infections. This may include bone infections, endocarditis, pelvic inflammatory disease, meningitis, pneumonia, urinary tract infections, and sepsis among others. It is not effective for gonorrhea or chlamydia infections. It can be given intravenously, by intramuscular injection, or topically. Topical formulations may be used in burns or for infections of the outside of the eye. It is often only used for two days until bacterial cultures determine what specific antibiotics the infection is sensitive to. The dose required should be monitored by blood testing. Gentamicin can cause inner ear problems and kidney problems. The inner ear problems can include problems with balance and hearing loss. These problems may be permanent. If used during pregnancy, it can cause harm to the developing baby. However, it appears to be safe for use during breastfeeding. Gentamicin is a type of aminoglycoside. It works by disru ...
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Definite Integral
In mathematics, an integral assigns numbers to functions in a way that describes displacement, area, volume, and other concepts that arise by combining infinitesimal data. The process of finding integrals is called integration. Along with differentiation, integration is a fundamental, essential operation of calculus,Integral calculus is a very well established mathematical discipline for which there are many sources. See and , for example. and serves as a tool to solve problems in mathematics and physics involving the area of an arbitrary shape, the length of a curve, and the volume of a solid, among others. The integrals enumerated here are those termed definite integrals, which can be interpreted as the signed area of the region in the plane that is bounded by the graph of a given function between two points in the real line. Conventionally, areas above the horizontal axis of the plane are positive while areas below are negative. Integrals also refer to the concept of an a ...
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Therapeutic Drug Monitoring
Therapeutic drug monitoring (TDM) is a branch of clinical chemistry and clinical pharmacology that specializes in the measurement of medication levels in blood. Its main focus is on drugs with a narrow therapeutic range, i.e. drugs that can easily be under- or overdosed.Marshall WJ, Bangert SK. Clinical Chemistry, 6th Edition. Edinburgh, London: Mosby Elsevier. 2008. TDM aimed at improving patient care by individually adjusting the dose of drugs for which clinical experience or clinical trials have shown it improved outcome in the general or special populations. It can be based on a ''a priori'' pharmacogenetic, demographic and clinical information, and/or on the ''a posteriori'' measurement of blood concentrations of drugs (pharmacokinetic monitoring) or biological surrogate or end-point markers of effect (pharmacodynamic monitoring).IATDMCT Executive Committee"Definition of TDM" 2004, accessed May 5, 2020. There are numerous variables that influence the interpretation of drug co ...
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Tablet (pharmacy)
A tablet (also known as a pill) is a pharmaceutical oral dosage form (''oral solid dosage'', or OSD) or solid unit dosage form. Tablets may be defined as the solid unit dosage form of medicament or medicaments with suitable excipients. It comprises a mixture of active substances and excipients, usually in powder form, pressed or compacted from a powder into a solid dose. Tablets are prepared either by molding or by compression. The excipients can include diluents, binders or granulating agents, glidants (flow aids) and lubricants to ensure efficient tabletting; disintegrants to promote tablet break-up in the digestive tract; sweeteners or flavours to enhance taste; and pigments to make the tablets visually attractive or aid in visual identification of an unknown tablet. A polymer coating is often applied to make the tablet smoother and easier to swallow, to control the release rate of the active ingredient, to make it more resistant to the environment (extending its shelf li ...
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