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Pharmacodynamics and drug action

85 articles

Acetylcholinesterase inhibitor

An acetylcholinesterase inhibitor (AChE inhibitor), also called an anticholinesterase, is a drug or toxin that blocks the enzyme breaking down acetylcholine, used in Alzheimer's disease.

Adamgammadex sodium

Adamgammadex sodium (阿更葡糖钠, brand Aomeikesong 奥美克松) is a Chinese class 1 cyclodextrin injection approved by the NMPA in June 2026 to reverse rocuronium neuromuscular blockade, with 86% less recurarization than sugammadex.

Adapalene

Adapalene (Differin) is a third-generation synthetic topical retinoid, a naphthoic acid derivative, used once daily for acne vulgaris; selective RAR-beta/gamma binding gives lower irritation than tretinoin, and 0.1% gel is FDA-approved OTC for ages 12 and up.

Agonist

Agonist: a receptor-binding ligand that activates signaling, defined by affinity and efficacy. Covers full, partial, inverse, and biased agonists, Stephenson's 1956 efficacy concept, and the affinity-efficacy problem.

Antiandrogen

An antiandrogen, also called an androgen antagonist or androgen blocker, is a drug that stops androgens like testosterone from binding their receptors, used mainly against prostate cancer.

Atropine

Atropine, also called (±)-hyoscyamine, is a belladonna alkaloid and competitive muscarinic receptor antagonist used for bradycardia, organophosphate poisoning, and pupil dilation; racemic, levo isomer active.

Betazole

Betazole (ametazole, Histalog), C5H9N3, is a pyrazole analogue of histamine and H2 receptor agonist used diagnostically to stimulate gastric acid secretion, with fewer side effects than histamine; its branded injectable product is discontinued.

Biochemical pharmacology

Biochemical pharmacology studies how drugs and biologically active substances act at the biochemical and cellular level, identifying the molecular targets of their effects; the field emerged in the late 1940s.

Biological activity

Biological activity (bioactivity): a substance's capability to provoke a response from living matter, beneficial or adverse, per IUPAC. Quantified as potency via bioassays, dose-response curves, and high-throughput screening, with assay interference a key caveat.

Bremelanotide

Bremelanotide (Vyleesi, PT-141) is a melanocortin receptor agonist peptide approved by the FDA in 2019 for acquired, generalized HSDD in premenopausal women; self-injected 1.75 mg as needed, with nausea and transient blood pressure rises as main adverse effects.

Buserelin

Buserelin (trade names Suprefact, Suprecur) is a synthetic nonapeptide analog of GnRH that first stimulates, then suppresses, pituitary hormone release, and treats prostate cancer, endometriosis, and breast cancer.

Cannabidiol

Cannabidiol (CBD), a non-intoxicating cannabis constituent, is approved as purified Epidiolex for Lennox-Gastaut, Dravet, and tuberous sclerosis seizures; weak CB1 binding, CYP2C19/3A4 metabolism, liver and clobazam interaction risks, and mislabeled consumer products distinguish it.

Cartalax

Cartalax (Kartalax, AED, T-31) is a synthetic Khavinson bioregulator tripeptide, Ala-Glu-Asp, marketed for cartilage research; its sequence is disputed, evidence is preclinical and institute-only, and no human trial or regulatory approval exists.

Chandonium iodide (candocuronium iodide)

Chandonium iodide, now candocuronium iodide (HS-310), is an Indian-developed aminosteroid non-depolarizing neuromuscular blocker synthesized at Panjab University with CSIR-CDRI in 1974, clinically trialed against pancuronium, histamine-sparing, but commercially abandoned.

Ciclosporin

Ciclosporin (cyclosporine, cyclosporin A, CsA), a cyclic undecapeptide calcineurin inhibitor from Tolypocladium inflatum, approved 1983; prevents transplant rejection and treats autoimmune disease, with nephrotoxicity and narrow therapeutic index.

Combined oral contraceptive pill

Combined oral contraceptive pill (COC, "the Pill"): daily estrogen-plus-progestin tablet preventing pregnancy by inhibiting ovulation; ~7 in 100 typical-use first-year pregnancies, VTE relative risk 3.5, first approved as Enovid in 1960.

Cyproterone acetate

Cyproterone acetate, sold under trade names including Androcur, is a synthetic steroidal antiandrogen and progestogen used for androgen-dependent conditions such as hirsutism, acne, and prostate cancer, with a known meningioma risk at higher doses.

Cytoprotection

Cytoprotection: protection of cells or tissues from injury by agents acting separately from a drug's main effect. Coined by Robert (1979) for prostaglandin gastric protection; extended to oncology (leucovorin, amifostine, dexrazoxane) and stroke.

Diethylstilbestrol

Diethylstilbestrol (DES) is a synthetic estrogen first made in 1938, prescribed to prevent miscarriage from the 1940s to the 1970s until it was found to cause cancer.

Dopamine reuptake inhibitor

Dopamine reuptake inhibitor (DRI), also NDRI or DNRI: a drug blocking the dopamine transporter (DAT, SLC6A3) to raise synaptic dopamine. Key drugs: bupropion, methylphenidate, modafinil, solriamfetol; used for depression, ADHD, narcolepsy, smoking cessation.

Dose titration

Dose titration is the stepwise adjustment of a drug's dose, up or down, to reach a clinical target at the lowest effective dose for each patient.

Dose–response relationship

The dose–response relationship, also known as the dose-response curve, links the dose of a drug to the body's biological response, and supplies potency and efficacy parameters for comparing drugs.

Drug class

Drug class: a set of medications grouped by chemical structure, mechanism of action, physiologic effect, or therapeutic use. Formalized in the WHO ATC system (five levels, 14 main groups) and FDA Established Pharmacologic Classes.

Drug sensitivity testing

Drug sensitivity testing is the laboratory exposure of living cells, tissues, or microorganisms to drugs followed by measurement of viability or growth, underpinning functional precision medicine in oncology.

Drug tolerance

Drug tolerance: diminished response to a drug after repeated exposure, requiring higher doses; distinct from tachyphylaxis, dependence, and sensitization (reverse tolerance), with pharmacokinetic, pharmacodynamic, and learned mechanisms.

Dydrogesterone

Dydrogesterone (Duphaston, Femoston) is a synthetic retroprogesterone progestogen developed by Philips-Duphar in 1959, used with estradiol in menopausal hormone therapy and for IVF luteal phase support; oral doses 10–20 times lower than progesterone, no androgenic or glucocorticoid activity.

EC50

EC50 (half maximal effective concentration) is the agonist concentration producing a response halfway between baseline and maximum; the standard potency measure in pharmacology, derived from the 1910 Hill equation, distinct from IC50 and Kd.

Efficacy

Efficacy (pharmacology): a drug's capacity, once receptor-bound, to change target behavior and produce response; distinct from affinity and potency. Spans Ariëns' intrinsic activity, Furchgott's intrinsic efficacy, receptor reserve, inverse agonism, and biased agonism.

Elagolix

Elagolix (Orilissa, Oriahnn) is the first FDA-approved oral non-peptide GnRH receptor antagonist, approved in 2018 for endometriosis pain and in 2020 with hormonal add-back for fibroid heavy menstrual bleeding.

Emergency contraception

Emergency contraception: post-coital pregnancy prevention methods, including ulipristal acetate (ella/ellaOne), levonorgestrel (Plan B), the copper IUD, and the Yuzpe regimen, with mechanisms, efficacy, BMI effects, access rules, and the 2022 FDA nonabortifacient label change.