Analgesics, antihistamines, and anti-inflammatory drugs

Benzydamine

Benzydamine (benzydamine hydrochloride, Tantum) is a topical indazole NSAID marketed since 1966 as 0.15% mouthwash and spray for sore throat and oral mucositis; weak base, cytokine-inhibiting, locally anesthetic, and hallucinogenic when abused at high doses.

Bepotastine

Bepotastine (Talion, Bepreve), a second-generation H1-antihistamine besilate salt, oral in Japan since 2000 for allergic rhinitis and urticaria, ophthalmic 1.5% FDA-approved 2009 for allergic conjunctivitis itching; among the least sedating antihistamines.

Betahistine

Betahistine (Serc, Betaserc) is an oral prescription H1 agonist/H3 antagonist used for Ménière's disease vertigo; dosed 24-48 mg daily, widely prescribed in Europe but not FDA approved, with weak clinical-trial evidence.

Betamethasone

Betamethasone is a synthetic glucocorticoid corticosteroid, the 16β-methyl epimer of dexamethasone, used topically for psoriasis and eczema, antenatally for fetal maturation, and systemically; ATC R03BA04, UNII 9842X06Q6M.

Bicifadine

Bicifadine (CL 220,075), 1-p-tolyl-3-azabicyclo[3.1.0]hexane, is a non-opioid triple monoamine reuptake inhibitor analgesic developed by American Cyanamid and DOV Pharmaceutical, tested in postoperative, low back, and diabetic neuropathy pain, with low preclinical abuse liability.

Bilastine

Bilastine (Bilaxten) is a second-generation, non-sedating H1-antihistamine approved in Europe in 2010 for allergic rhinoconjunctivitis and urticaria, dosed 20 mg daily, not metabolized, excreted unchanged, and affected by grapefruit juice and P-gp inhibitors.

Bromfenac

Bromfenac, a brominated ophthalmic NSAID (Xibrom, Bromday, Prolensa, BromSite, Yellox), inhibits COX-2 to treat inflammation and pain after cataract surgery; oral Duract was withdrawn in 1998 for liver failure.

Bromodiphenhydramine

Bromodiphenhydramine (bromazine, Ambodryl) is a brominated ethanolamine first-generation H1 antihistamine derived from diphenhydramine, first approved in 1954, with antimicrobial, sedative, and anticholinergic actions; largely discontinued.

Brompheniramine

Brompheniramine (Dimetane, Bromfed, Dimetapp combinations) is a first-generation alkylamine H1 antihistamine, FDA-approved in 1957, used for allergy, rhinitis, and urticaria symptoms; sedating and anticholinergic.

Bucetin

Bucetin (Betadin, N-(4-ethoxyphenyl)-3-hydroxybutanamide) is a withdrawn anilide analgesic and antipyretic, a phenacetin analogue approved in Germany and removed from the market in 1986 for renal toxicity.

Bucillamine

Bucillamine (ブシラミン, Rimatil, SA96) is a dithiol cysteine-derivative DMARD for rheumatoid arthritis used in Japan and Korea, a potent thiol donor repurposed for COVID-19, cystinuria, transplantation, and nerve-agent countermeasures.

Bufexamac

Bufexamac (Paraderm, Parfenac, CP-1044-J3) is a topical hydroxamic-acid NSAID formerly used for eczema, dermatitis, and hemorrhoids; withdrawn in the EU (2010), Australia (2020), and New Zealand for severe allergic contact dermatitis.

Buprenorphine

Buprenorphine (Suboxone, Subutex, Sublocade, Brixadi, Butrans): semi-synthetic thebaine-derived Schedule III partial mu-opioid agonist, 20-30x morphine potency, with ceiling on respiratory depression; treats opioid use disorder and pain.

Carbinoxamine

Carbinoxamine (Clistin, Karbinal ER, Palgic) is a first-generation ethanolamine H1 antihistamine with sedative and anticholinergic effects, approved in the US in 1953 for allergic rhinitis, conjunctivitis, urticaria, and anaphylaxis adjunct use, contraindicated under age 2.

Cebranopadol

Cebranopadol (GRT6005) is a first-in-class investigational oral analgesic from Grünenthal that dually agonizes NOP and mu-opioid receptors, with long half-life, reduced respiratory depression versus oxycodone, low abuse potential, and Phase 3 cancer-pain development.

Celecoxib

Celecoxib (Celebrex) is a selective COX-2 inhibitor NSAID approved in 1998 for osteoarthritis, rheumatoid arthritis, JRA, ankylosing spondylitis, acute pain, and dysmenorrhea; CYP2C9-metabolized, boxed cardiovascular and GI warnings, noninferior CV safety in PRECISION.

Centbucridine

Centbucridine (INN bucricaine), a quinoline local anesthetic developed at CSIR-CDRI Lucknow in 1982 and licensed to Themis Chemicals in 1987, has inherent vasoconstrictor and antihistaminic activity, is 4-8 times more potent than lignocaine, and was studied in ophthalmic and dental anesthesia.

Cetirizine

Cetirizine (Zyrtec, Reactine) is a second-generation H1 antihistamine, the active metabolite of hydroxyzine, used for allergic rhinitis and chronic urticaria; US prescription 1995, OTC 2007, half-life about 10.5 hours, renally excreted.

Chloroprocaine

Chloroprocaine (2-chloroprocaine) is a short-acting ester local anesthetic of the PABA group, hydrolyzed by pseudocholinesterase within seconds, used for infiltration, nerve block, and epidural anesthesia but not spinal injection.

Chlorphenamine

Chlorphenamine (chlorpheniramine), brand Piriton, Chlor-Trimeton: a first-generation sedating H1 antihistamine alkylamine used for hay fever, hives, and allergy symptoms; FDA approved 1950.

Chlorphenoxamine

Chlorphenoxamine (Phenoxene, Systral) is a first-generation H1-antihistamine and anticholinergic, a diphenhydramine congener used as an antipruritic and formerly for parkinsonism; CAS 77-38-3, ATC D04AA34.

Chlorzoxazone

Chlorzoxazone, formerly sold as Parafon Forte and Remular, is a centrally acting skeletal muscle relaxant approved in the United States in 1958 for acute, painful musculoskeletal conditions.

Choline salicylate

Choline salicylate is a choline salt of salicylic acid, an NSAID used mainly as a topical oral gel for mouth ulcers, cold sores, and denture sore spots.

Cinchophen

Cinchophen (atophan), 2-phenylcinchoninic acid, a quinoline NSAID introduced in 1908 by Nicolaier and Dohrn; uricosuric gout drug withdrawn for idiosyncratic liver toxicity, the first recognized non-dose-related drug-induced hepatic injury.

Cinnarizine

Cinnarizine (Stugeron) is an antihistamine and calcium channel antagonist for vertigo, motion sickness, and Ménière's disease; often combined with dimenhydrinate, with drowsiness and parkinsonism as notable risks.

Clemastine

Clemastine (meclastin, Tavist) is a first-generation H1 antihistamine of the benzhydryl ether group, marketed since 1966 in Europe and 1977 in the US for allergic rhinitis, urticaria, and angioedema; sedating and anticholinergic, and repurposed as an M1-antagonist remyelination candidate for multiple sclerosis.

Clobetasol propionate

Clobetasol propionate (Temovate, Clobex) is a super-high potency topical corticosteroid, 0.05% strength, first described 1974, FDA-approved 1985, used for psoriasis and corticosteroid-responsive dermatoses with 2-week, 50 g/week limits.

Clometacin

Clometacin (Dupéran), an indomethacin-isomer indoleacetic acid NSAID and cyclooxygenase inhibitor introduced in France in 1971, withdrawn in 1990 after severe autoimmune-like hepatitis, mainly in elderly women.

Cyclizine

Cyclizine (Marezine, Valoid) is a piperazine H1 antihistamine antiemetic developed by Burroughs Wellcome in 1947, used for motion sickness, vertigo, and PONV, and carried on Apollo missions for space sickness.