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Analgesics, antihistamines, and anti-inflammatory drugs

264 articles

Pirprofen

Pirprofen (Rengasil), a phenylpropionic acid NSAID related to ibuprofen and naproxen, treated rheumatoid arthritis, osteoarthritis, and pain at 600-1200 mg/day; withdrawn worldwide in 1990 for fatal hepatotoxicity.

Polmacoxib

Polmacoxib (CG100649, Acelex) is a first-in-class NSAID dual inhibitor of COX-2 and carbonic anhydrase I/II, approved for osteoarthritis in South Korea (2015) and India (2023), dosed 2 mg daily.

Povorcitinib

Povorcitinib (INCB054707, Povofortay) is Incyte's oral, highly selective JAK1 inhibitor (about 50-fold over JAK2) with positive phase 3 results and regulatory filings for hidradenitis suppurativa and vitiligo.

Pramoxine

Pramoxine (pramocaine), a morpholine-ether topical anesthetic and antipruritic sold as pramoxine hydrochloride, blocks sodium channels to relieve itching and pain from hemorrhoids, insect bites, and minor skin irritation.

Prednisolone

Prednisolone, active metabolite of prednisone, is a synthetic corticosteroid developed at Schering in 1954; anti-inflammatory and immunosuppressive, 3-5 times cortisone potency, used for arthritis, asthma, allergies, and eye inflammation.

Prednisone

Prednisone is a synthetic oral glucocorticoid prodrug converted in the liver to prednisolone; 5 mg equals 20 mg hydrocortisone, used for inflammation, immunosuppression, and adrenal insufficiency replacement.

Preemptive analgesia

Preemptive analgesia is pain treatment started before a surgical incision to prevent central sensitization of spinal neurons, now largely replaced by the broader concept of preventive analgesia.

Preventive analgesia

Preventive analgesia is a perioperative pain-management strategy in which analgesic treatment, given before or after surgery, reduces acute pain and lowers the risk of chronic postsurgical pain.

Procaine

Procaine (Novocain) is an aminoester local anesthetic synthesized by Alfred Einhorn in 1905; it blocks voltage-gated sodium channels, is hydrolyzed by plasma butyrylcholinesterase to PABA, and dominated local anesthesia until lidocaine (1948).

Prolotherapy

Prolotherapy (proliferation therapy, regenerative injection therapy) injects irritant solutions, usually 12.5-25% hypertonic dextrose, into ligaments and tendon attachments for chronic musculoskeletal pain; evidence is mixed and dextrose use is off-label.

Promethazine

Promethazine (Phenergan, 3277 RP) is a phenothiazine H1 antihistamine synthesized in 1944, first marketed by Rhône-Poulenc, used for allergy, nausea, motion sickness, and sedation, with boxed warnings for pediatric respiratory depression and injection-site gangrene.

Propoxycaine

Propoxycaine (CAS 86-43-1) is a discontinued ester-type local anesthetic, C16H26N2O3, once combined with procaine in dental cartridges (Ravocaine) and withdrawn from the US market in 1996.

Propyphenazone

Propyphenazone (4-isopropylantipyrine, CAS 479-92-5) is a non-acidic pyrazolone NSAID analgesic and antipyretic introduced in 1951, used mainly in combination products, with COX and TRPA1 activity and hematological and IgE-mediated hypersensitivity risks.

Pulse therapy

Pulse therapy, or steroid pulse therapy, is a regimen giving very high intravenous steroid doses, usually methylprednisolone, over short periods to rapidly control severe inflammatory or autoimmune disease.

Ralfinamide

Ralfinamide (NW-1029) is an experimental α-aminoamide sodium and calcium channel blocker developed by Newron Pharmaceuticals for neuropathic pain; positive Phase II results but a failed Phase III trial in neuropathic low back pain.

Ramatroban

Ramatroban (BAY u3405, Baynas) is a Bayer-developed dual thromboxane TP and CRTH2/DP2 receptor antagonist marketed in Japan for allergic rhinitis, dosed 75 mg twice daily, with hepatitis and jaundice as notable adverse reactions.

Remibrutinib

Remibrutinib (Rhapsido) is Novartis's oral, highly selective covalent BTK inhibitor, approved 2025-2026 in the US, EU, UK, and Canada for chronic spontaneous urticaria in adults uncontrolled on H1-antihistamines, dosed 25 mg twice daily.

Revamilast

Revamilast (GRC 4039) is an oral, selective PDE4 inhibitor developed by Glenmark Pharmaceuticals for inflammatory conditions; it reached phase 2 trials in asthma and rheumatoid arthritis but development is discontinued or unknown.

Rimexolone

Rimexolone (Vexol, Org 6216) is a 1% ophthalmic glucocorticoid suspension for postoperative ocular inflammation and anterior uveitis, with lower IOP-elevating potential than prednisolone; US product discontinued.

Rizatriptan

Rizatriptan, marketed as Maxalt and Maxalt-MLT, is a triptan drug acting on serotonin 5-HT1B/1D receptors, FDA approved in 1998 to treat migraine attacks with or without aura.

Rofecoxib

Rofecoxib (Vioxx), Merck's selective COX-2 inhibitor NSAID for osteoarthritis, acute pain, and migraine, approved in 1999 and withdrawn worldwide in 2004 after the APPROVe trial showed roughly doubled cardiovascular thromboembolic risk.

Rupatadine

Rupatadine (Rupafin) is a second-generation, once-daily oral antihistamine that blocks both H1 histamine and PAF receptors, used for allergic rhinitis and urticaria; 10 mg dose, CYP3A4-metabolized, desloratadine-forming, ranked highly among oral antihistamines.

Serlopitant

Serlopitant (VPD-737, MK-0594) is an investigational oral NK1 receptor antagonist developed by Merck and Menlo Therapeutics for chronic itch; positive phase 2 pruritus and psoriasis trials but failed phase 3 prurigo and atopic dermatitis studies.

Setipiprant

Setipiprant (ACT-129968), an oral selective CRTH2 (DP2) antagonist developed by Actelion for allergy and trialed for male pattern hair loss; safe but failed efficacy in Phase 3 rhinitis and Phase 2a alopecia trials.

SPARTAN trial (NCT02605174)

SPARTAN (NCT02605174), a Phase 3 double-blind trial of lasmiditan 50/100/200 mg vs placebo for acute migraine, run 2016-2017 at 125 US, German, and UK sites; met pain-freedom and MBS-freedom endpoints at 2 hours.

Sublingual immunotherapy

Sublingual immunotherapy (SLIT) is an allergy treatment in which allergen tablets or drops held under the tongue desensitize patients with allergic rhinitis or asthma, an alternative to injected immunotherapy.

SUN-1334H

SUN-1334H (SUN 1334H) was a potent, selective H1 antihistamine from India's SPARC (Sun Pharma), developed for allergic rhinitis and conjunctivitis; it reached Phase 2 in the US and was abandoned in 2013 as not viable.

Suprofen

Suprofen (R-25061, Suprol, Profenal) is a propionic acid NSAID related to ibuprofen that inhibits prostaglandin synthesis. Its oral capsules were withdrawn worldwide in May 1987 over a flank pain and renal failure syndrome; the 1% ophthalmic solution for surgical miosis also left the market.

Suzetrigine

Suzetrigine (Journavx, VX-548), Vertex Pharmaceuticals' oral NaV1.8 sodium channel inhibitor, FDA-approved January 30, 2025 as the first new-class non-opioid for moderate-to-severe acute pain in adults.

Tacrolimus

Tacrolimus (FK506, Prograf) is a macrolide calcineurin-inhibitor immunosuppressant from Streptomyces tsukubaensis, first used in humans in 1989; it outperforms cyclosporine for graft survival but causes more post-transplant diabetes.