32 articles
Activated charcoal (medication)
Activated charcoal (medication): oral carbon adsorbent for acute poisoning, surface area 800–1,200 m²/g, given within 1 hour at 0.5 g/kg; poorly binds lithium, iron, and alcohol.
ADME
ADME (absorption, distribution, metabolism, excretion) describes a drug's fate in the body, central to pharmacokinetics and drug development, where poor ADME properties cause nearly half of candidate losses and drive IVIVE, allometric scaling, and PBPK prediction methods.
Area under the curve (pharmacokinetics)
Area under the curve (AUC) in pharmacokinetics: integral of plasma concentration over time, the standard measure of systemic drug exposure; variants AUC0-t, AUC0-inf, AUC0-TAU; trapezoidal calculation; 80-125% bioequivalence criterion.
Berberine
Berberine, a benzylisoquinoline alkaloid from Coptis chinensis and Berberis plants, is a supplement studied for type 2 diabetes and dyslipidemia; meta-analyses show HbA1c reductions near 0.6-0.7 points, under 1% oral bioavailability, and mainly gastrointestinal side effects.
Bioavailability
Bioavailability: the fraction and rate of an administered drug dose reaching systemic circulation unaltered; IV dosing is 100% by definition, oral F is calculated as AUC ratio, limited by first-pass metabolism.
Biological half-life
Biological half-life (t1/2, elimination half-life): time for plasma drug concentration to fall 50%; t1/2 = 0.693·Vd/CL; governs dosing frequency, steady state in 4–5 half-lives, and half-life extension of biologics.
Biopharmaceutics Classification System
The Biopharmaceutics Classification System (BCS), introduced by Gordon Amidon and colleagues in 1995, sorts drugs into four classes by solubility and permeability, and the FDA adopted it in 2000 to waive bioequivalence testing.
Chronotherapy
Chronotherapy is a treatment strategy that times drug administration or other therapies to the patient's circadian rhythm, seeking to maximize efficacy and minimize toxicity; it applies chronopharmacology.
Clinical pharmacokinetics
Clinical pharmacokinetics: applying drug absorption, distribution, metabolism, and excretion (ADME) principles to patient care and drug development; basis of therapeutic drug monitoring and model-informed precision dosing.
Cotinine
Cotinine is the predominant metabolite of nicotine, formed by CYP2A6 in the liver, with a 12-16 hour half-life. It is the standard biomarker of tobacco and secondhand smoke exposure measured in blood, saliva, and urine.
Daniel L. Azarnoff
Daniel L. Azarnoff is an American physician and clinical pharmacologist, elected to the Institute of Medicine in 1978, who led drug research at the University of Kansas and Searle.
Detoxification
Detoxification, also called biotransformation, is the set of metabolic reactions by which the body chemically alters foreign compounds such as drugs, reducing toxicity and easing excretion.
Drug metabolism
Drug metabolism (biotransformation) is the enzymatic two-phase conversion of drugs into metabolites, mainly by hepatic cytochrome P450 enzymes, covering first-pass metabolism, induction, inhibition, pharmacogenetics, and toxicity.
First pass effect
The first pass effect, or first-pass metabolism, is the metabolism of an oral drug in the liver and intestinal wall before it reaches systemic circulation, reducing bioavailability.
Food effect study
A food effect study is a clinical pharmacology study measuring how food changes an oral drug's absorption and exposure, comparing fed and fasted dosing to support labeling.
Ideal Body Weight
Ideal body weight (IBW) is a height-based weight estimate from Metropolitan Life Insurance tables and formulas such as Devine (1974), Hamwi, Robinson, and Miller, used clinically for drug dosing, nutrition, and ventilation, with adjusted body weight variants for obesity.
International unit
International unit (IU), a unit of biological activity used for vitamins, hormones, enzymes, and drugs; not SI-traceable, defined by WHO International Standards; insulin example 0.0347 mg per IU.
Lipinski's rule of five
Lipinski's rule of five (Ro5) is a medicinal chemistry guideline for oral drug-likeness: MW ≤500 Da, clogP <5, ≤5 H-bond donors, ≤10 acceptors, from Lipinski et al. 1997; extended by Veber and Ghose rules and challenged by beyond-Ro5 drugs.
Loading dose
Loading dose: an initial drug dose larger than the maintenance dose, calculated as (Cp × Vd)/F, given to reach therapeutic plasma concentrations rapidly instead of waiting about 5 half-lives for steady state.
Mass balance study
A mass balance study, also called a human ADME study, is a clinical pharmacokinetic study using a radiolabeled drug dose to track absorption, metabolism, and excretion.
Metabolic Clearance Rate
Metabolic Clearance Rate, also called Total Body Clearance Rate, is a pharmacokinetic measure of the volume of fluid cleared of a drug by metabolism per unit time.
Microdosing
Microdosing: taking subperceptual intermittent doses of psychedelics (LSD, psilocybin) for mood or cognition, or phase 0 subpharmacologic drug testing (1/100 dose, 100 µg max) in humans.
Nicotinamide
Nicotinamide (niacinamide), the amide form of vitamin B3, is an NAD+ precursor vitamin and drug: no flushing unlike nicotinic acid, used for pellagra (300 mg/day), skin cancer chemoprevention (500 mg twice daily), and dermatology.
Pharmacokinetic model
A pharmacokinetic model is a mathematical description of how the body handles a drug over time, covering absorption, distribution, metabolism, and elimination to predict concentration profiles and guide dosing.
Pharmacokinetics
Pharmacokinetics (PK), the ADME science of drug absorption, distribution, metabolism, and excretion; term coined by Dost 1953, first PBPK model by Teorell 1937; spans compartmental, noncompartmental, PBPK, and population PK modeling used in FDA drug review.
Physiologically based pharmacokinetic modeling
Physiologically based pharmacokinetic (PBPK) modeling predicts drug concentrations over time in blood and tissues by representing the body as organs connected by blood flows, widely used in drug development and regulation.
Plasma protein binding
Plasma protein binding (PPB): reversible binding of drugs to plasma proteins, mainly albumin and alpha-1-acid glycoprotein. Only the unbound fraction is pharmacologically active; measured by equilibrium dialysis or ultrafiltration; displacement interactions are rarely clinically significant.
Population pharmacokinetic analysis
Population pharmacokinetic analysis is a clinical pharmacology modeling method, originating with Lewis Sheiner's work in 1972, that estimates typical drug concentration profiles and variability across a population from sparse sampling data to guide dosing.
Population pharmacokinetic modeling
Population pharmacokinetic modeling is a pharmacometric method that fits nonlinear mixed-effects models to sparse clinical data, estimating typical drug concentration–time profiles, variability between patients, and supporting precision dosing.
Prodrug
Prodrug: an inactive or weakly active derivative of an active drug, converted in vivo by enzymatic or chemical cleavage into the parent drug. Term coined by Adrien Albert (1958); examples include oseltamivir, enalapril, capecitabine, omeprazole, and valacyclovir.