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Gallamine
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DB13584 |
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GDC-0810
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DB12253 |
[ARN-810 has been used in trials studying the basic science and treatment of Breast Cancer.] |
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Aminoethyl nitrate
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DB13585 |
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ABT-751
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DB12254 |
[ABT-751 has been investigated for the treatment of Lung Cancer, Non-Small Cell Lung Cancer, and Non-Small-Cell Lung Cancer.] |
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Metandienone
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DB13586 |
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Vadadustat
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DB12255 |
[Vadadustat has been used in trials studying the treatment of Anemia and Non-dialysis-dependent Chronic Kidney Disease.] |
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Succinylsulfathiazole
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DB13580 |
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Rociverine
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DB13581 |
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Cixutumumab
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DB12250 |
[Cixutumumab has been used in trials studying the treatment of Lung Cancer, Malignant Neoplasm, Leukemia, Mast-Cell, Non-Small-Cell Lung Carcinoma, and Adenocarcinoma of the Prostate.
Cixutumumab is a highly specific recombinant human monoclonal antibody with high affinity for the insulin-like growth factor-I receptor (IGF-IR). IGF-IR is overexpressed in a variety of tumour types.] |
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Moxaverine
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DB12251 |
[Moxaverine has been investigated for the treatment of Retina, Ocular Physiology, and Regional Blood Flow.] |
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Ferric (59Fe) citrate
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DB13582 |
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Argatroban
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DB00278 |
[Argatroban is a direct, selective thrombin inhibitor. The American College of Cardiologists (ACC) recommend using bivalirudin or argatroban in patients who have had, or at risk for, heparin induced thrombocytopenia (HIT) and are undergoing percutaneous coronary intervention. Argatroban is a non-heparin anticoagulant shown to both normalize platelet count in patients with HIT and prevent the formation of thrombi. Parental anticoagulants must be stopped and a baseline activated partial thromboplastin time must be obtained prior to administering argatroban.] |
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Theophylline
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DB00277 |
[A methylxanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Mechanistically, theophylline acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. Theophylline is marketed under several brand names such as Uniphyl and Theochron, and it is indicated mainly for asthma, bronchospasm, and COPD.] |
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Liothyronine
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DB00279 |
[Liothyronine is a thyroidal hormone T3 which is normally produced by the thyroid gland in a ratio 4:1 when compared with T4: T3. Liothyronine is the active form of thyroxine which is composed in a basic chemical structure by a tyrosine with bound iodine.[T457] The exogenous liothyronine product was developed by King Pharmaceuticals and FDA approved in 1956.[L5578]] |
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Cefmetazole
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DB00274 |
[A semisynthetic cephamycin antibiotic with a broad spectrum of activity against both gram-positive and gram-negative microorganisms. It has a high rate of efficacy in many types of infection and to date no severe side effects have been noted.] |
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Topiramate
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DB00273 |
[Topiramate is a anti-epileptic drug used to manage seizures and prevent migraines.[A175249] It was initially approved by the FDA in 1996. In 2004, topiramate was approved for the prevention of migraine in adults.[A188309,L10544] Since 2012, the extended-release formulation has been approved in combination with [phentermine] for chronic weight management therapy in adults.[L10550]
Characteristics that distinguish topiramate from other antiepileptic drugs are a monosaccharide chemical structure containing a sulfamate, and 40% of its mass accounted for by oxygen.[A175249] Interestingly, topiramate was discovered by chance when attempts were made to formulate a novel antidiabetic drug.[A188330]] |
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Amsacrine
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DB00276 |
[Aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but acceptable myelosuppression and cardiotoxic effects.] |
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Olmesartan
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DB00275 |
[Olmesartan belongs to the angiotensin II receptor blocker (ARB) family of drugs, which also includes [telmisartan], [candesartan], [losartan], [valsartan], and [irbesartan]. ARBs selectively bind to angiotensin receptor 1 (AT1) and prevent the protein angiotensin II from binding and exerting its hypertensive effects, which include vasoconstriction, stimulation and synthesis of aldosterone and ADH, cardiac stimulation, and renal reabsorption of sodium, among others. Overall, olmesartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium.
Olmesartan also affects the renin-angiotensin aldosterone system (RAAS), which plays an important role in hemostasis and regulation of kidney, vascular, and cardiac functions. Pharmacological blockade of RAAS via AT1 receptor blockade inhibits negative regulatory feedback within RAAS, which is a contributing factor to the pathogenesis and progression of cardiovascular disease, heart failure, and renal disease. In particular, heart failure is associated with chronic activation of RAAS, leading to inappropriate fluid retention, vasoconstriction, and ultimately a further decline in left ventricular function. ARBs have been shown to have a protective effect on the heart by improving cardiac function, reducing afterload, increasing cardiac output and preventing ventricular hypertrophy and remodelling.[A174154]
By comparison, the angiotensin-converting enzyme inhibitor (ACEi) class of medications (which includes drugs such as [ramipril], [lisinopril], and [perindopril]) inhibit the conversion of angiotensin I to angiotensin II through inhibition of the ACE enzyme. However, this does not prevent the formation of all angiotensin II within the body. The angiotensin II receptor blocker (ARB) family of drugs unique in that it blocks all angiotensin II activity, regardless of where or how it was synthesized.
Olmesartan is commonly used for the management of hypertension and Type 2 Diabetes-associated nephropathy, particularly in patients who are unable to tolerate ACE inhibitors. ARBs such as olmesartan have been shown in a number of large-scale clinical outcomes trials to improve cardiovascular outcomes including reducing risk of myocardial infarction, stroke, the progression of heart failure, and hospitalization.[A174124,A178153,A173869,A185324,A185327,A185333,A185342,A185345] Like other ARBs, olmesartan blockade of RAAS slows the progression of diabetic nephropathy due to its renoprotective effects.[A185906,A185909,A185912]
Orally available olmesartan is produced as the prodrug olmesartan medoxomil which is rapidly converted _in vivo_ to the pharmacologically active olmesartan.[A175330] It was developed by Daiichi Sankyo Pharmaceuticals and approved in 2002.[A175345, L5560]] |
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Lidocaine
|
DB00281 |
[Ever since its discovery and availability for sale and use in the late 1940s, lidocaine has become an exceptionally commonly used medication [T583]. In particular, lidocaine's principal mode of action in acting as a local anesthetic that numbs the sensations of tissues means the agent is indicated for facilitating local anesthesia for a large variety of surgical procedures [F4349, L5930, L5948]. It ultimately elicits its numbing activity by blocking sodium channels so that the neurons of local tissues that have the medication applied on are transiently incapable of signaling the brain regarding sensations [F4349, L5930, L5948]. In doing so, however, it can block or decrease muscle contractile, resulting in effects like vasodilation, hypotension, and irregular heart rate, among others [F4349, L5930, L5948]. As a result, lidocaine is also considered a class Ib anti-arrhythmic agent [L5930, L5948, F4468]. Nevertheless, lidocaine's local anesthetic action sees its use in many medical situations or circumstances that may benefit from its action, including the treatment of premature ejaculation [A177625].
Regardless, lidocaine is currently available as a relatively non-expensive generic medication that is written for in millions of prescriptions internationally on a yearly basis. It is even included in the World Health Organization's List of Essential Medicines [L6055].] |
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Disopyramide
|
DB00280 |
[A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.] |
