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Analgesics, antihistamines, and anti-inflammatory drugs

264 articles

Etoricoxib

Etoricoxib (Arcoxia) is a selective COX-2 inhibitor NSAID approved in Europe for osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute gout, and acute pain; never FDA-approved, with ~20-hour half-life and diclofenac-comparable cardiovascular risk.

Felbinac

Felbinac (フェルビナク), 4-biphenylacetic acid, is a topical NSAID (ATC M02AA08) sold as gels, tapes, and paps, chiefly in Japan since 1986, with NNT 3.0 for acute musculoskeletal pain.

Fenclofenac

Fenclofenac (Flenac, RX 67408) is a withdrawn phenylacetic acid NSAID, cyclooxygenase inhibitor, introduced 1978 for rheumatic disorders and removed in 1985 after skin rashes, seven deaths, and 895 adverse effect reports.

Fenclozic acid

Fenclozic acid (Myalex, ICI 54,450), a 1960s ICI carboxylic acid NSAID for rheumatoid arthritis, was withdrawn from clinical development in 1971 after causing cholestatic hepatotoxicity in human trials at 400 mg/day, an effect not seen in animals.

Fenoprofen

Fenoprofen (brand Nalfon, Fenopron) is a propionic acid NSAID, C15H14O3, FDA-approved in 1976 as the calcium salt for rheumatoid arthritis, osteoarthritis, and mild to moderate pain, dosed up to 3,200 mg daily.

Fentanyl

Fentanyl is a synthetic opioid 50 to 100 times more potent than morphine, used for anesthesia and severe pain and the drug most often involved in U.S. overdose deaths.

Feprazone

Feprazone (4-prenyl-1,2-diphenyl-3,5-pyrazolidinedione), a phenylbutazone-related NSAID, ATC M01AX18/M02AA16, trialed in rheumatoid arthritis and osteoarthritis; withdrawn in Germany in 1984 over skin reactions and rat carcinogenicity.

Fexofenadine

Fexofenadine (Allegra) is a second-generation, nonsedating H1 antihistamine for allergic rhinitis and chronic urticaria, approved in 1996 as the active metabolite of the withdrawn drug terfenadine (Seldane).

Fludrocortisone

Fludrocortisone (9α-fluorocortisol, Florinef) is a synthetic mineralocorticoid used for aldosterone replacement in adrenal insufficiency and CAH, and for orthostatic hypotension; potent MR agonist, 0.05–0.2 mg daily.

Flufenamic acid

Flufenamic acid is a fenamate NSAID with analgesic, anti-inflammatory, and antipyretic effects, used in musculoskeletal and joint disorders and also a widely used ion channel research tool.

Flumexadol

Flumexadol (CERM-1841), 2-[3-(trifluoromethyl)phenyl]morpholine, CAS 30914-89-7, is a trifluoromethylphenyl morpholine, non-narcotic analgesic, and selective 5-HT2C receptor agonist (Ki 25 nM, (+)-enantiomer); active metabolite of oxaflozane, listed as withdrawn.

Flunisolide

Flunisolide (AeroBid, Nasalide, Nasarel) is a synthetic corticosteroid, glucocorticoid receptor agonist, C24H31FO6, half-life 1.8 h, used as nasal spray for allergic rhinitis and inhaler for asthma; first FDA-approved INCS spray (1981).

Fluocinonide

Fluocinonide, a synthetic topical corticosteroid (21-acetate ester of fluocinolone acetonide, C26H32F2O7, US approval 1971), treats eczema and psoriasis as 0.05% and super-high-potency 0.1% creams, gels, and ointments.

Fluocortolone

Fluocortolone (Ultralan) is a synthetic fluorinated glucocorticoid used topically for skin disorders; its pivalate and hexanoate esters appear in rectal products Ultraproct and Doloproct for haemorrhoids, fissures, and proctitis.

Flupirtine

Flupirtine, a triaminopyridine non-opioid analgesic and selective neuronal potassium channel opener (Kv7/GIRK activator), was used in Europe from 1984 for pain with muscle tension until EMA withdrew it in 2018 over liver injury.

Flurbiprofen

Flurbiprofen is a chiral nonsteroidal anti-inflammatory drug sold as a racemic mixture, used for arthritis and pain, as eye drops preventing miosis, and in lozenges for sore throat.

Frovatriptan

Frovatriptan (frovatriptan succinate, brand FROVA), a 5-HT1B/1D agonist triptan, treats acute migraine with or without aura in adults as 2.5 mg tablets; its ~26-hour half-life lowers headache recurrence versus other triptans.

Glafenine

Glafenine (glaphenine, Exidol), an anthranilic acid derivative NSAID analgesic, ATC N02BG03, marketed from 1965 and withdrawn in most countries by 1992 for anaphylaxis and hepatotoxicity.

Glucocorticoid therapy

Glucocorticoid therapy is treatment with synthetic analogs of cortisol, used to suppress inflammation and immune activity in inflammatory, autoimmune, and allergic diseases or to replace cortisol in adrenal insufficiency.

GRC 15300 (SAR292833)

GRC 15300, or SAR292833, was a first-in-class TRPV3 channel antagonist for chronic pain, discovered by Glenmark Pharmaceuticals, licensed to Sanofi in 2010, and discontinued in 2014.

GRC 17536

GRC 17536 (ISC 17536) is Glenmark's oral TRPA1 antagonist, a thienopyrimidinedione tested in Phase 2a for painful diabetic peripheral neuropathy; it failed overall but helped a preserved-nerve-function subgroup, and development was limited by poor bioavailability.

GRC 27864 (ISC 27864)

GRC 27864 (ISC 27864, zaloglanstat) is Glenmark's oral mPGES-1 inhibitor for osteoarthritic pain; Phase 2b trial in 624 Indian patients completed enrollment in 2019.

GRC 6211

GRC 6211, also written GRC-6211, was Glenmark Pharmaceuticals' oral TRPV1 antagonist pain drug licensed to Eli Lilly in 2007 for $45 million upfront; it reached Phase II osteoarthritis and dental pain trials before discontinuation in 2008.

Gusacitinib

Gusacitinib (ASN002) is an oral dual pan-JAK/SYK inhibitor for chronic hand eczema, in phase 3 with Sanofi after Formation Bio acquired it from Asana BioSciences; phase 2 showed 69.5% mTLSS reduction at 80 mg.

H1 antagonist

H1 antagonist (H1-antihistamine): inverse agonist drug blocking histamine at the H1 receptor; first synthesized 1937 by Bovet; first-generation (1942 onward) sedating, second-generation (cetirizine, loratadine, fexofenadine) non-sedating first-line for rhinitis and urticaria.

Halobetasol propionate

Halobetasol propionate: ultra-high potency (class I) synthetic topical corticosteroid (Ultravate, Bryhali, Lexette, Duobrii combination) for plaque psoriasis; 0.05% and 0.01% formulations, two-week to eight-week use limits, 50 g/week cap.

Heroin

Heroin (diacetylmorphine, diamorphine) is a semi-synthetic opioid first synthesized in 1874 by C.R. Wright and marketed by Bayer from 1898 as a cough medicine; now a Schedule I illicit drug, roughly 2-3 times more potent than morphine.

Hexylcaine

Hexylcaine (cyclaine, osmocaine; CAS 532-77-4) is a short-acting ester local anesthetic, 1-(cyclohexylamino)propan-2-yl benzoate, acting on voltage-gated sodium channels; synthesized 1944, used topically from 1952, now discontinued in the US.

History of aspirin

History of aspirin: from ancient willow-bark remedies and Edward Stone's 1763 report, through Gerhardt's 1853 synthesis and Bayer's 1899 Aspirin trademark, to Vane's 1971 COX mechanism and modern antiplatelet use.

HSK51155

HSK51155 is an oral, non-opioid analgesic candidate developed by China's Haisco Pharmaceutical, a selective Nav1.8 sodium channel inhibitor in phase 1 trials for migraine and licensed to AbbVie in 2026.