edgepedia

Pharmacodynamics and drug action

85 articles

Pharmacodynamic model

A pharmacodynamic model is a statistical or mechanistic model describing how the magnitude of a drug's effect depends on drug concentration over time, as in the Emax model.

Pharmacodynamics

Pharmacodynamics: the study of drug effects on the body, covering dose–response curves (EC50, Emax), agonists and antagonists, therapeutic index, spare receptors, tolerance, PD drug interactions, and modern GPCR biased agonism.

Pharmacology of ethanol

Pharmacology of ethanol: how alcohol (ethanol, drinking alcohol) is absorbed and metabolized via ADH/ALDH and CYP2E1, its actions on GABA_A, NMDA, and other receptors, tolerance, drug interactions, and AUD pharmacotherapy.

Placebo

Placebo: an inert substance with no pharmacologic activity, and the placebo and nocebo effects it reveals. Covers effect sizes, opioid and dopamine mechanisms, open-label placebos, trial ethics, and 2024–2025 findings.

Placebo Effect

Placebo effect: health improvement from expectation and treatment context rather than active drug action; also called placebo response. Includes nocebo (negative) counterpart, Beecher's 1955 35% estimate, Cochrane SMD −0.23, and open-label placebos.

Polydeoxyribonucleotide

Polydeoxyribonucleotide, or PDRN, is a DNA-derived drug extracted from salmonid fish sperm, first approved in 1994 for wound healing and now common in South Korean skincare.

Puberty blocker

Puberty blockers (GnRH agonists) suppress pituitary gonadotropin release to halt puberty; used for precocious puberty since the 1980s and for gender dysphoria since 2000, now restricted in the UK after the Cass Review.

Receptor antagonist

Receptor antagonist: a ligand that binds a receptor without activating it, blocking agonists. Includes competitive (surmountable, e.g. naloxone, antihistamines) and non-competitive (insurmountable, e.g. phenoxybenzamine) types, plus allosteric antagonists.

Relugolix

Relugolix (Orgovyx, Myfembree) is an oral nonpeptide GnRH receptor antagonist approved by FDA in December 2020 for advanced prostate cancer; HERO showed 96.7% castration vs 88.8% with leuprolide and 54% lower MACE risk, and combination therapy treats fibroid bleeding.

Ruxolitinib

Ruxolitinib (Jakafi, Opzelura) is a JAK1/JAK2 inhibitor, first FDA-approved drug for myelofibrosis (2011), also approved for polycythemia vera, GVHD, and topically for atopic dermatitis.

Sirolimus

Sirolimus (rapamycin, Rapamune) is an mTOR-inhibitor immunosuppressant from Streptomyces hygroscopicus, discovered in Easter Island soil in the 1960s, approved by the FDA in 1999 for kidney transplant rejection prophylaxis and for lymphangioleiomyomatosis.

Stanozolol

Stanozolol (Winstrol) is a 17α-alkylated, DHT-derived anabolic steroid first marketed in 1962, now discontinued and Schedule III in the US, WADA-prohibited, and known for cholestatic liver injury and the 1988 Ben Johnson doping case.

Sulfonylurea

A sulfonylurea, plural sulfonylureas, is an oral antidiabetic drug used in type 2 diabetes that lowers blood glucose by stimulating insulin secretion from pancreatic beta cells.

Suvomipic

Suvomipic, also known as JXL069 (CAS 2260696-63-5), is the WHO proposed INN for a mitochondrial pyruvate carrier inhibitor developed at UCLA and widely linked, though not formally confirmed, to Pelage Pharmaceuticals' investigational hair-loss drug PP405.

Synergism

Synergism (synergy, from Greek synergia) is an interaction in which a combined effect exceeds the additive prediction of individual effects; defined in toxicology, pharmacology, ecology, and solvent extraction chemistry.

Synthetic cannabinoids

Synthetic cannabinoids, sold as K2 or Spice, are lab-made full agonists of CB1/CB2 receptors, 2–100 times more potent than THC, sprayed on herbal incense and linked to seizures, psychosis, and deaths.

Tariquidar

Tariquidar (XR9576) is a third-generation anthranilamide inhibitor of the P-glycoprotein (ABCB1) drug efflux pump, acting noncompetitively via ATPase inhibition; clinically tested in cancer trials that were halted, now used in P-gp research and PET imaging.

TB-500

TB-500, also called thymosin beta-4 fragment or Ac-LKKTETQ, is a synthetic seven-amino-acid peptide (residues 17-23 of thymosin beta-4) sold as a research chemical, untested in human trials, and WADA-prohibited under S2.3.

Teriparatide

Teriparatide (Forteo, Forsteo), recombinant human PTH(1-34), is the first anabolic osteoporosis drug, FDA-approved 2002; 20 mcg daily subcutaneous injection, 2-year lifetime limit, rat osteosarcoma warning.

Testosterone (medication)

Testosterone (medication), or testosterone replacement therapy (TRT), is prescription testosterone for male hypogonadism; formulations include gels, patches, injections, and pellets, with TRAVERSE showing cardiovascular noninferiority.

Therapeutic index

Drug therapeutic index (TI, therapeutic ratio): ratio of toxic dose (TD50 or LD50) to effective dose (ED50); values above 10 indicate a wide safety margin, while narrow-TI drugs like warfarin and digoxin require therapeutic drug monitoring.

Tirzepatide

Tirzepatide (Mounjaro, Zepbound) is Eli Lilly's once-weekly dual GIP/GLP-1 receptor agonist injectable approved in 2022 for type 2 diabetes and later for obesity and obstructive sleep apnea, producing about 20% weight loss in head-to-head trials versus semaglutide's 13.7%.

Tretinoin

Tretinoin (all-trans retinoic acid, ATRA), a vitamin A metabolite, is a topical first-line acne treatment (Retin-A) and an oral differentiation therapy inducing remission in t(15;17)-positive acute promyelocytic leukemia.

Vosilasarm

Vosilasarm (RAD140, testolone, EP0062) is an oral non-steroidal selective androgen receptor modulator in phase 1/2 trials for AR+/ER+/HER2- breast cancer; not FDA approved.

Zosuquidar

Zosuquidar (LY335979) is a synthetic quinoline and potent, selective inhibitor of P-glycoprotein, tested against multidrug resistance in acute myeloid leukemia but never approved; it remains an experimental research tool.