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Aminophylline
Aminophylline

... assessed and the initial loading dose should be calculated on the basis that each 600 micrograms/kg of aminophylline (equivalent to about 500 micrograms/kg theophylline) will increase serum-theophylline concentration by 1 microgram/mL. In the management of chronic bronchospasm aminophylline may be g ...
Clopidogrel Markedly Increases the Plasma Concentrations of the
Clopidogrel Markedly Increases the Plasma Concentrations of the

... The glucose-lowering drug pioglitazone undergoes hepatic cytochrome P450 (CYP) 2C8-mediated biotransformation to its main metabolites. The antiplatelet drug clopidogrel is metabolized to clopidogrel acyl-β -D-glucuronide, which was recently found to be a strong time-dependent inhibitor of CYP2C8 in ...
Cathinone derivatives: A review of their chemistry, pharmacology
Cathinone derivatives: A review of their chemistry, pharmacology

... to a series of related clusters. First, N-alkylation at the R1 and/or R2 sites (either with methyl or ethyl groups) produces a series of alkylated cathinone derivatives. N-Methylation produces methcathinone, and a further methylation at position 4 on the ring produces mephedrone. N-Methylation at bo ...
Prescription medicine use by one million Canadian children
Prescription medicine use by one million Canadian children

... The fact that the vast majority of drugs lack data on indications, efficacy, dosage or safety in children has been identified as a problem for many years. This has been a significant burden for child health care providers and has meant that therapy for children has, on average, lagged behind that av ...
Doxylamine Succinate - IARC Monographs on the Evaluation of
Doxylamine Succinate - IARC Monographs on the Evaluation of

... In a study of childhood cancer in England, 615 cases and 1230 controls were considered to be eligible for the study (Birch et al., 1985). The parents of 555 children (response rate, 90%) in whom an incident cancer (171 leukaemias, 74 lymphomas, 78 central nervous system tumours and 232 other cancers ...


... mg/m2). After 6 months of intravenous dosing at 10 mg/kg/day, no nephropathological changes were noted; however, nephropathy was observed after dosing at 20 mg/kg/day for the same duration (approximately 0.2-times the highest recommended therapeutic ...
Inhaled  clemastine,  an  H
Inhaled clemastine, an H

... Inhaled clemastine, an H 1 antihistamine, inhibits airway narrowing caused by aerosols of non-isotonic saline. L.T. Rodwell S.D. Anderson, J.P. Seale. ABSTRACT: Asthmatic subjects were challenged with aerosols of hyperand hypotonic saline 15 mln (Group A) and 90 mln (Group B) after Inhaling clemasti ...
Claforan - Sanofi Canada
Claforan - Sanofi Canada

... tract surgery) that may be classified as contaminated or potentially contaminated. In patients undergoing caesarian section who are considered to be at increased risk of infection, intraoperative (after clamping the umbilical cord) and postoperative use of CLAFORAN may also reduce the incidence of c ...
VA Medicaid PDL Criteria (effective 01/01/2010)
VA Medicaid PDL Criteria (effective 01/01/2010)

... Acceptable reasons include: o Allergy to product formulation (i.e. dyes, fillers). If an allergy to drug class, should question medication request. o Contraindication to or drug-to-drug interaction with medications not requiring prior approval o History of unacceptable/toxic side effects to medicati ...
GHB - CAP Members
GHB - CAP Members

Biliary Excretion of Antimicrobial Drugs
Biliary Excretion of Antimicrobial Drugs

... drugs of any kind worldwide. Used appropriately, these drugs are lifesaving. To eliminate an infection as rapidly as possible, a sufficient concentration of the drug(s) chosen must reach the site of infection. Serum/tissue concentration is a result of various parameters such as absorption, excretion ...
Codeine to Morphine Concentration Ratios in Samples
Codeine to Morphine Concentration Ratios in Samples

Methadone-Drug Interactions
Methadone-Drug Interactions

... in terms of its presence and activity in the liver (Eap et al. 2002; Leavitt et al. 2000). This enzyme also is found in the gastrointestinal tract, so methadone metabolism actually can begin before the drug enters the circulatory system (Hardman et al. 1996). The amount of this enzyme in the intesti ...
Naloxone - Spirit of Healing: Alberta First Nations Conquering
Naloxone - Spirit of Healing: Alberta First Nations Conquering

... Opioid antagonists bind to opioid receptors and are used to block the effects of opioids by blocking the receptor sites to prevent any action of an opioid agonist. Antagonists do not activate receptors, and they prevent receptors from being activated by agonist compounds. An antagonist is like a key ...
Benzylpenicillin inhibits the renal excretion of acyclovir by OAT1 and
Benzylpenicillin inhibits the renal excretion of acyclovir by OAT1 and

... cells had been washed three times and preincubated in HBSS for 15 min at 37°C. The uptake of acyclovir in the presence or absence of PCG (1,000 µM: in hOAT1-HEK293 cells; 200 µM: in hOAT3-HEK293 cells) was measured in hOAT1-, hOAT3- and mock cells: in 3 min uptake experiment, at acyclovir concentrat ...
Imatinib - BC Cancer Agency
Imatinib - BC Cancer Agency

... imatinib.28 Drugs that have high oral bioavailability (eg. >0.7) are less likely to be affected by grapefruit juice. CYP3A4 inducers may increase metabolism and decrease imatinib plasma concentrations. Concurrent administration of drugs that induce CYP3A4 (eg, carbamazepine, dexamethasone, phenytoin ...
Donepezil is a strong antagonist of voltage
Donepezil is a strong antagonist of voltage

... indicate that K+-current was suppressed effectively at both 30 and 100 mV. Unlike Ca2+-current, no shift of the I–V curve of the K+-current along the potential axis was observed in the presence of the drug. Dose–effect relationships of donepezil inhibition of K+-currents recorded at 30 mV (IC) and 1 ...
SOLID-STATE NMR - National Institute of Chemistry
SOLID-STATE NMR - National Institute of Chemistry

... of competing drugs can be resolved ...
Effects of different doses of venlafaxine on serotonin and
Effects of different doses of venlafaxine on serotonin and

... 5-HT/NE reuptake inhibition in healthy volunteers capsule at bedtime. They were started at bedtime on the day the baseline data were collected. The paroxetine group received 10 mg in the morning, the nefazodone group received 75 mg b.i.d., the desipramine group 25 mg b.i.d., the low-dose venlafaxin ...
500ct. 10-325 mg HCb and APAP Tablets[Watson[Base[rev2
500ct. 10-325 mg HCb and APAP Tablets[Watson[Base[rev2

... determined to be 3.8 ± 0.3 hours. Hydrocodone exhibits a complex pattern of metabolism including O-demethylation, N-demethylation and 6-keto reduction to the corresponding 6-α- and 6-β-hydroxy-metabolites. See OVERDOSAGE for toxicity information. Acetaminophen: Acetaminophen is rapidly absorbed from ...
Valproate Learning Objectives Outline Indications
Valproate Learning Objectives Outline Indications

... • VPA is primarily metabolized in the liver by glucuronidation and oxidation, and its metabolites (several of which are active) are excreted mainly in the urine • Inhibition or induction of CYP450 enzymes by other drugs has little effect on VPA clearance because CYP450 microsomal mediated oxidation ...
Chapter 1 Key Terms
Chapter 1 Key Terms

... 31. The study of the metabolism and action of drugs, with emphasis on the time required for absorption, duration of action, distribution in the body, and ...
JIPBS Simple UV spectrophotometric assay of Furosemide Original Article
JIPBS Simple UV spectrophotometric assay of Furosemide Original Article

... failure, when we require rapid diuretic action and intestinal absorption may be delayed because of gastrointestinal oedema Thus, time to peak, lag time and peak of serum concentration may differ in compensated when compared with decompensate patients after the oral furosemide is intake, whereas elim ...
Universidade de Lisboa Faculdade de Farmácia Assessing drug
Universidade de Lisboa Faculdade de Farmácia Assessing drug

... national compendium reported the British National Formulary as the most commonly used compendium. When assessing Summaries of Product Characteristics (SmPCs), we found that their content on clinical pharmacology information is insufficient. Information on this topic was found to be very similar to t ...
the topical pain relief
the topical pain relief

... overall use of prescribed pain-killer drugs. The CDC has reported that the number of prescription pain-killer deaths increased among females by a factor of five times in the period of 1999 to 2010. In contrast, death rates from overdose rose about 3.5 times in men in the same period of time. It wou ...
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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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