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Product Monograph - Paladin Labs Inc.
Product Monograph - Paladin Labs Inc.

... after reconstitution and must not be given as an intravenous infusion. Carcinogenesis and Mutagenesis No carcinogenicity studies have been conducted. The potential for genotoxicity of glucagon (rDNA origin) has been evaluated using a series of recognized in vitro and in vivo assays for mutagenic-gen ...
modafinil - Awake Institute, LLC
modafinil - Awake Institute, LLC

... Similarly, as with clinical sleep disorders such as apnea, there is the concern that the wide-spread use of modafinil among shiftworkers may compromise efforts to manage the root causes of work-related fatigue. Critics feel that the broader approval of Provigil could lead to its use being extended f ...
C 3  R
C 3 R

... Cytochrome P450 (P450s) are involved in the metabolism of approximately 80% of the drugs currently on the market (1, 2). In some cases drugs can be oxidized by P450s to electrophilic reactive intermediates, which subsequently can react with nucleophilic functional groups in biomolecules such as prot ...
AusPAR: Metformin HCI / Linagliptin
AusPAR: Metformin HCI / Linagliptin

... Linagliptin is made by chemical synthesis. It has one chiral centre and is presented as a single (R) enantiomer (See Figure 1). Linagliptin solubility is high. The drug substance is milled. There is limited particle size control. Particle size does not significantly affect tablet dissolution. Impuri ...
The Clinical Pharmacology of Lidocaine
The Clinical Pharmacology of Lidocaine

... all types was clearly lower. However, because side effects from lidocaine administration do occur, we do not presently advocate usage of this drug for all patients after myocardial infarction, but instead prefer to administer lidocaine when premonitory signs of life-threatening cardiac arrhythmias o ...
Pharmacokinetic and pharmacodynamic drug interactions
Pharmacokinetic and pharmacodynamic drug interactions

... of 2D6 by methysticin (44%, P < 0.001). Unfortunately, the authors did not report the number of times the inhibition studies were replicated, the variability in their results or any other details on the inhibition calculations, so that the reliability of their study results cannot be assessed. While ...
labetalol hydrochloride injection usp
labetalol hydrochloride injection usp

... and aldosterone levels, both at rest and during exercise, particularly when these were elevated prior to treatment. Labetalol is significantly more efficacious in hypertensive patients with high baseline plasma noradrenaline levels. Labetalol is metabolized mostly by conjugation with glucuronic acid ...
EVG/COBI/FTC/TAF [E/C/F/TAF] FDC
EVG/COBI/FTC/TAF [E/C/F/TAF] FDC

... systemic clearance of the drug after intravenous administration ...
Not for Reprint - Epilepsy Foundation
Not for Reprint - Epilepsy Foundation

... To assess this, we implanted monkeys with an experimental drug-delivery apparatus, the Subdural Pharmacotherapy Device, and used this apparatus to deliver muscimol into the frontal cortex, transmeningeally, for more than 6 months. Muscimol is a GABAA receptor agonist occurring in the mushroom Amanit ...
Acute and Chronic Effects of Inhalants in Intracranial Self
Acute and Chronic Effects of Inhalants in Intracranial Self

... Inhalants are a pharmacologically diverse group of compounds that have been ubiquitously defined through the exclusivity of the inhalational route by which humans abuse them. In addition, inhalants are associated with their legal, therapeutic and commercial availability in society. Broadly defined, ...
View Full Prescribing Information
View Full Prescribing Information

... Preparation and Dilution in Bag for Infusion 1. Calculate the milligrams of ANTHIM injection needed by multiplying the recommended mg/kg dose in Table 2 by the patient weight in kilograms. 2. Calculate the required volume in milliliters of ANTHIM injection and number of vials needed for the dose by ...
Prescribing Information
Prescribing Information

... association with modafinil (a mixture of R- and S-modafinil) and armodafinil (the R-enantiomer of modafinil). Although the pharmacology of modafinil is not identical to that of the sympathomimetic amines, it does share some pharmacologic properties with this class. Certain of these drugs have been a ...
LSD (Lysergic acid diethylamide), death? and distraction
LSD (Lysergic acid diethylamide), death? and distraction

... Detecting LSD in man • Average time to peak concentration in serum after oral dosing is 3-5 hours • Average serum elimination half-life from peak serum concentration is 3 hours (Wagner et al, 1968) • Patients receiving treatment for LSD intoxication, manifested by agitation or unconsciousness, have ...
ENCLOSURE  1
ENCLOSURE 1

... still seen at 12 hours. There was no evidence of tolerance to these: effects after 2$ days of dosing . The clinical significance of these observations is unknown. Histamine skin wheal and flare studies in 7 to 12 year old subjects showed that following a single dose of 30 or 60 mg, antihistamine eff ...
12_chapter 7
12_chapter 7

... marketed serotonin and norepinephrine reuptake inhibitors, venlafaxine, desvenlafaxine, and duloxetine such as equipotent serotonin and norepinephrine reuptake inhibition and a linear dose-concentration trend at therapeutic doses. The half-life of milnacipran is approximately 8 hours. In addition, m ...
TRAMADOL – A Drug to be used cautiously
TRAMADOL – A Drug to be used cautiously

... Tramadol, a centrally acting analgesic structurally related to codeine and morphine, consists of two enantiomers, both of which contribute to analgesic activity via different mechanisms. (+)-Tramadol and the metabolite (+)-O-desmethyltramadol (M1) are agonists of the μ. opioid receptor. (+)-Tramadol ...
Full book.large
Full book.large

... Overall, I consider myself a libertarian when it comes to the use of drugs. As long as the choice is made based on knowledge, and no one but the individual making that choice is affected, what people do to themselves is their own business as far as I’m concerned. So if it’s not some silly moral anti ...
Hydrocortisone, Hydrocortisone Acetate
Hydrocortisone, Hydrocortisone Acetate

... Hydrocortisone is administered rectally as a retention enema, and hydrocortisone acetate is given rectally as a suppository or an aerosol foam suspension according to the manufacturers’ instructions. Patients should be advised that hydrocortisone acetate suppositories may stain fabric so that they c ...
Chronic tolerance to recreational MDMA
Chronic tolerance to recreational MDMA

... in Parrott, 2004a). The third phase was from the late, 1990s to the present, when the proportion of Ecstasy tablets containing MDMA has increased to values around 80–100% (Cole et al., 2002; Hansen et al., 2001; Palenicek et al., 2002; see also Table 3 in Parrott, 2004a). Given that not every Ecstas ...
Discriminative Stimulus Properties of MDMA
Discriminative Stimulus Properties of MDMA

... Abstract Rationale: ±3,4-methylenedioxymethamphetamine (MDMA, “ecstasy”) produces unique and complex subjective effects which distinguish it from other recreationally used drugs. An understanding of the neurochemical mechanisms that underlie these effects is important in order to assess the potentia ...
TYLENOL® with Codeine
TYLENOL® with Codeine

... increasing frequency of dose-related opioid adverse reactions such as nausea, vomiting, CNS effects, and respiratory depression. In opioid-tolerant patients, the situation may be altered by the development of tolerance to opioid-related adverse reactions [see DOSAGE AND ADMINISTRATION]. Pharmacokine ...
PrCIPRO® XL - Bayer Canada
PrCIPRO® XL - Bayer Canada

... agitation, insomnia, anxiety, paranoia, nightmares and, rarely, suicidal thoughts or acts. In some cases, depression or psychotic reactions can progress to suicidal ideations/thoughts and selfinjurious behavior, such as attempted suicide or completed suicide. These reactions may occur even following ...
Gelsemium sempervirens - Southwest School of Botanical Medicine
Gelsemium sempervirens - Southwest School of Botanical Medicine

... them carry the qualities of the preparations of Gelsemium that have made the therapeutical reputation of the drug. If the drying process did not break the natural interstructural combination, the heroic chemistry used in splitting it into fragments would accomplish that result. These alkaloids and o ...
Misuse and abuse of quetiapine
Misuse and abuse of quetiapine

... The main biological symptoms of dependence are withdrawal symptoms and change (usually increase) of tolerance. There are several case reports of symptoms that occur as a result of withdrawal or rapid reduction of the dose of quetiapine. Thurstone and Alahi described, in the year 2000, the case of a  ...
NIH Public Access - The Scripps Research Institute
NIH Public Access - The Scripps Research Institute

... neurotransmitters, whose action involves the uptake and storage of these small molecules into synaptic vesicles, AEA and other N-acyl ethanolamines (NAEs) are produced upon demand through activity-dependent cleavage of membrane lipid precursors (29,34). The biological activity of AEA in the central ...
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Pharmacokinetics



Pharmacokinetics, sometimes abbreviated as PK (from Ancient Greek pharmakon ""drug"" and kinetikos ""moving, putting in motion""; see chemical kinetics), is a branch of pharmacology dedicated to determining the fate of substances administered externally to a living organism. The substances of interest include pharmaceutical agents, hormones, nutrients, and toxins. It attempts to discover the fate of a drug from the moment that it is administered up to the point at which it is completely eliminated from the body.Pharmacokinetics describes how the body affects a specific drug after administration through the mechanisms of absorption and distribution, as well as the chemical changes of the substance in the body (e.g. by metabolic enzymes such as cytochrome P450 or glucuronosyltransferase enzymes), and the effects and routes of excretion of the metabolites of the drug. Pharmacokinetic properties of drugs may be affected by elements such as the site of administration and the dose of administered drug. These may affect the absorption rate. Pharmacokinetics is often studied in conjunction with pharmacodynamics, the study of a drug's pharmacological effect on the body.A number of different models have been developed in order to simplify conceptualization of the many processes that take place in the interaction between an organism and a drug. One of these models, the multi-compartment model, gives the best approximation to reality; however, the complexity involved in using this type of model means that monocompartmental models and above all two compartmental models are the most-frequently used. The various compartments that the model is divided into are commonly referred to as the ADME scheme (also referred to as LADME if liberation is included as a separate step from absorption): Liberation - the process of release of a drug from the pharmaceutical formulation. See also IVIVC. Absorption - the process of a substance entering the blood circulation. Distribution - the dispersion or dissemination of substances throughout the fluids and tissues of the body. Metabolization (or biotransformation, or inactivation) – the recognition by the organism that a foreign substance is present and the irreversible transformation of parent compounds into daughter metabolites. Excretion - the removal of the substances from the body. In rare cases, some drugs irreversibly accumulate in body tissue.The two phases of metabolism and excretion can also be grouped together under the title elimination.The study of these distinct phases involves the use and manipulation of basic concepts in order to understand the process dynamics. For this reason in order to fully comprehend the kinetics of a drug it is necessary to have detailed knowledge of a number of factors such as: the properties of the substances that act as excipients, the characteristics of the appropriate biological membranes and the way that substances can cross them, or the characteristics of the enzyme reactions that inactivate the drug.All these concepts can be represented through mathematical formulas that have a corresponding graphical representation. The use of these models allows an understanding of the characteristics of a molecule, as well as how a particular drug will behave given information regarding some of its basic characteristics. Such as its acid dissociation constant (pKa), bioavailability and solubility, absorption capacity and distribution in the organism.The model outputs for a drug can be used in industry (for example, in calculating bioequivalence when designing generic drugs) or in the clinical application of pharmacokinetic concepts. Clinical pharmacokinetics provides many performance guidelines for effective and efficient use of drugs for human-health professionals and in veterinary medicine.
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