Cardiovascular drugs

Celiprolol

Celiprolol (Cardem) is a third-generation beta-blocker with beta1-antagonist, beta2-agonist, and alpha2-antagonist actions, used for hypertension and angina and as the leading drug for vascular Ehlers-Danlos syndrome in Europe; not approved in the US.

Celivarone

Celivarone (SSR149744C, ATI-2042) is an investigational noniodinated benzofuran antiarrhythmic related to amiodarone; it failed to show significant efficacy in the ALPHEE, MAIA, and CORYFEE trials.

Centhaquine

Centhaquine (Lyfaquin, PMZ-2010, formerly centhaquin) is a selective alpha-2B adrenoceptor agonist resuscitative drug for hypovolemic shock, approved in India in 2020 as an add-on therapy, with phase III evidence of reduced 28-day mortality.

Chlormerodrin

Chlormerodrin (Neohydrin, Mercloran) is an organomercury urea-derivative diuretic, withdrawn from use, whose 197Hg/203Hg-labeled forms were the first radiopharmaceuticals for renal imaging.

Chlortalidone

Chlortalidone (chlorthalidone) is a long-acting thiazide-like diuretic for hypertension, U.S.-approved since 1960, half-life 40-60 hours, the ALLHAT comparator drug, with hypokalemia and metabolic side effects.

Cilazapril

Cilazapril (Inhibace) is a Roche pyridazine ACE inhibitor prodrug, hydrolyzed to cilazaprilat, used once daily at 2.5–5 mg for hypertension and congestive heart failure; ATC C09AA08, introduced 1991.

Cilexetil

Cilexetil is the ester promoiety in candesartan cilexetil (Atacand), the oral prodrug of the angiotensin II receptor blocker candesartan, hydrolyzed in the gut, dosed 2-32 mg once daily for hypertension and heart failure.

Cilnidipine

Cilnidipine (FRC8653), a fourth-generation dihydropyridine calcium channel blocker blocking both L-type and N-type calcium channels, treats essential hypertension; trials show efficacy similar to amlodipine with added proteinuria reduction in chronic kidney disease.

Clazosentan

Clazosentan (Pivlaz), a selective endothelin A receptor antagonist by Actelion/Idorsia, approved in Japan (2022) to prevent cerebral vasospasm after aneurysmal subarachnoid hemorrhage surgery; reduces vasospasm but not mortality or functional outcome.

Clevidipine

Clevidipine (Cleviprex) is an ultrashort-acting intravenous dihydropyridine calcium channel blocker in lipid emulsion, FDA approved 2008 for blood pressure reduction when oral therapy is not feasible; esterase metabolism gives a ~1-minute half-life, and ECLIPSE trials compared it with nitroglycerin, nitroprusside, and nicardipine.

Clopidogrel

Clopidogrel (Plavix) is an oral P2Y12 platelet inhibitor prodrug activated mainly by CYP2C19, used with or instead of aspirin after MI, ischemic stroke, PCI, and in peripheral artery disease; boxed warning for CYP2C19 poor metabolizers.

Creatinolfosfate

Creatinolfosfate (creatinol O-phosphate, COP), C4H12N3O4P, is a methylated creatine analog and cardiac drug (ATC C01EB05) studied in 1970s Italy for anti-ischemic, anti-arrhythmic effects; oral creatine-source claims are unsupported.

Cyclandelate

Cyclandelate (Cyclospasmol, CAS 456-59-7) is a mandelic acid ester vasodilator, a direct-acting smooth muscle relaxant once used for claudication, Raynaud's disease, and migraine prophylaxis; discontinued in the US and Canada in 1997 for lack of efficacy.

Cyclothiazide

Cyclothiazide (Anhydron, Fluidil), a thiazide diuretic first approved in 1963, treats hypertension and edema via distal tubule Na-Cl transport inhibition, and is widely used in neuroscience as an AMPA receptor desensitization blocker.

Daflon

Daflon 500 mg (micronized purified flavonoid fraction, MPFF; diosmin 450 mg plus hesperidin 50 mg) is a Servier venoactive drug for chronic venous insufficiency and hemorrhoids, widely prescribed in Europe but not available in the USA.

Dalteparin sodium

Dalteparin sodium (Fragmin) is a low-molecular-weight heparin anticoagulant approved in the US in 1994, dosed by weight subcutaneously; it treats cancer-associated VTE, provides surgical and medical thromboprophylaxis, and covers unstable angina and dialysis circuits.

Danaparoid sodium

Danaparoid sodium (Orgaran) is a non-heparin heparinoid mixture of glycosaminoglycans from porcine mucosa, an antithrombin-mediated factor Xa inhibitor (anti-Xa:anti-IIa 22:1) used for HIT treatment and DVT prophylaxis; withdrawn from the US in 2002.

Darapladib

Darapladib (SB-480848, CHEMBL204021) is an oral selective Lp-PLA2 inhibitor developed by GSK for atherosclerosis. Its phase 3 trials STABILITY and SOLID-TIMI 52 failed to reduce cardiovascular events despite about 65% enzyme inhibition.

Darexaban

Darexaban (YM150, darexaban maleate) is an oral direct factor Xa inhibitor developed by Astellas Pharma for VTE prophylaxis, atrial fibrillation, and acute coronary syndrome; its active glucuronide metabolite YM-222714 carries its anticoagulant effect, and development was discontinued in September 2011.

Darusentan

Darusentan (LU 135252, ABT-627) is an investigational selective endothelin ETA receptor antagonist for resistant hypertension; effective in phase 2 and DORADO trials but discontinued over fluid retention and a failed DORADO-AC endpoint, never approved.

Defibrotide

Defibrotide (Defitelio), a porcine-mucosal-DNA-derived oligonucleotide mixture, is the approved antithrombotic/profibrinolytic drug for hepatic veno-occlusive disease with renal or pulmonary dysfunction after HSCT (US, 2016) and severe VOD/SOS (EU).

Delapril

Delapril (地拉普利) is a lipophilic nonsulfhydryl ACE inhibitor prodrug launched by Takeda in 1989 for hypertension, converted to two active diacid metabolites and marketed in fixed combinations with manidipine and indapamide.

Deserpidine

Deserpidine, a Rauwolfia alkaloid antihypertensive related to reserpine, ATC C02AA05/C02LA03, formula C32H38N2O8, first approved 1957; brands Harmonyl, Oreticyl, Enduronyl; depletes catecholamines.

Desirudin

Desirudin (Revasc, Iprivask) is a recombinant 65-amino-acid hirudin analogue and direct thrombin inhibitor for DVT prophylaxis after hip or knee replacement; EU authorization withdrawn 2014.

Deslanoside

Deslanoside (deacetyllanatoside C, Cedilanid-D) is a Digitalis lanata cardiac glycoside for heart failure and supraventricular arrhythmias; Na-K-ATPase inhibitor, half-life 38-77 h, discontinued in the US but available in Brazil, China, and Japan.

Desmoteplase

Desmoteplase (DSPAα1), a fibrin-selective plasminogen activator from vampire bat (Desmodus rotundus) saliva, was developed as a 3-9 hour window stroke thrombolytic; trials showed recanalization gains but no functional benefit.

Digoxin

Digoxin, a cardiac glycoside from Digitalis lanata, treats mild to moderate heart failure and controls ventricular rate in chronic atrial fibrillation; neutral mortality in trials, narrow therapeutic window.

Dihydralazine

Dihydralazine (Nepresol), a hydralazine-family direct arteriolar vasodilator, half-life 4-5 h, used mainly for severe hypertension in pregnancy in Germany; declining due to frequent adverse effects.

Diltiazem

Diltiazem (Cardizem, Tiazac) is a benzothiazepine, nondihydropyridine calcium channel blocker synthesized in 1971 by Tanabe and FDA-approved in 1982, used for hypertension, angina, and atrial fibrillation rate control, contraindicated in HFrEF.