U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 81 - 90 of 291 results

Status:
US Previously Marketed
First approved in 1969

Class (Stereo):
CHEMICAL (ABSOLUTE)



Flumethasone or flumetasone is a corticosteroid and is an agonist of a glucocorticoid receptor with anti-inflammatory, antipruritic and vasoconstrictive properties. Flumethasone is often formulated as the pivalic acid ester, flumetasone pivalate. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding. Flumethasone binds to plasma transcortin, and it becomes active when it is not bound to transcortin. Flumethasone is used for the treatment of contact dermatitis, atopic dermatitis, exczema, psoriasis, diaper rash and other skin condition.
Thiabendazole (TBZ, trade names Mintezol, Tresaderm, and Arbotect) was first introduced in 1962. This drug is a fungicide and parasiticide and is indicated for the treatment of: strongyloidiasis (threadworm), cutaneous larva migrans (creeping eruption), visceral larva migrans, trichinosis: relief of symptoms and fever and a reduction of eosinophilia have followed the use of this drug during the invasion stage of the disease. But usage of this drug was discontinued. The precise mode of action of thiabendazole on the parasite is unknown, but it may inhibit the helminthspecific enzyme fumarate reductase. It was shown, also that thiabendazole reversibly disassembles newly established blood vessels, marking it as vascular disrupting agent (VDA) and thus as a potential complementary therapeutic for use in combination with current anti-angiogenic therapies. Was shown, that vascular disruption by TBZ results from reduced tubulin levels and hyper-active Rho signaling. In addition, was confirmed, that thiabendazole slowed tumor growth and decreased vascular density in preclinical fibrosarcoma xenografts and thus, it could lead directly to the identification of a potential new therapeutic application for an inexpensive drug that is already approved for clinical use in humans.
Status:
US Previously Marketed
First approved in 1965

Class (Stereo):
CHEMICAL (RACEMIC)



Chlorphenesin carbamate (Maolate, Musil) is a centrally acting muscle relaxant used to treat muscle pain and spasms. Сhlorphenesin acts in the central nervous system (CNS) rather than directly on skeletal muscle. It also has antifungal and some antibacterial properties. The major adverse effects are drowsiness and dizziness.
Cloxacillin is a derivative of penicillin for the treatment of broad spectrum of bacterial infections. The drug exerts its action by inhiiting bacterial beta-lactamase (penicillin-binding proteins).
Status:
US Previously Marketed
First approved in 1962

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Stanozolol is a synthetic anabolic steroid derived from dihydrotestosterone. It is indicated prophylactically to decrease the frequency and severity of attacks of angioedema. In rare cases, serious and even fatal cases of liver problems have developed during treatment with stanozolol. Anabolic steroids may increase sensitivity to anticoagulants; therefore, dosage of an anticoagulant may have to be decreased in order to maintain the prothrombin time at the desired therapeutic level.
Status:
US Previously Marketed
Source:
Sonilyn by Mallinckrodt
(1962)
Source URL:
First approved in 1962
Source:
Sonilyn by Mallinckrodt
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfachlorpyridazine is a broad spectrum antibacterial compound which is effective in the treatment of infections caused by gram-positive and gram-negative organisms that are commonly susceptible to sulfonamide therapy and which has been proven by laboratory and field experiments to be highly effective against diseases caused by Escherichia coli. Sulfachlorpyridazine has a rapid onset of action in several species of animals following both oral and parenteral administration. Sulfachlorpyridazine (brand name Vetisulid) is especially indicated for the treatment of diarrhea caused or complicated by E. coli (colibacillosis) in calves under 1 month of age: Vetisulid powder is also indicated for the treatment of colibacillosis in swine. Sulfachlorpyridazine is a dihydropteroate synthase inhibitor.
Status:
US Previously Marketed
Source:
TRIMEPRAZINE TARTRATE by MORTON GROVE
(1985)
Source URL:
First approved in 1959
Source:
Temaril by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Trimeprazine (also known as Alimemazine), a phenothiazine used as antipsychotic drug. This drug is used in Russia under brand name TERALIGEN and has anti-histamine, sedative, and anti-emetic (anti-nausea) effects. Teraligen is used to treat neurosis, depression and anxiety of different origins. It prevents and relieves allergic conditions, which cause pruritus and urticaria by blocking histamine produced by the body during an allergic reaction. Trimeprazine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Trimeprazine is not approved for use in humans in the United States. Nevertheless, combination of alimemazine and prednisolone (commonly sold under the brand name Temaril-P) is licensed as an antipruritic and antitussive in dogs.
Status:
US Previously Marketed
Source:
Delvex by Lilly
(1958)
Source URL:
First approved in 1958
Source:
Delvex by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dithiazanine, 3-ethyl-2-[5-(3-ethyl-2-benzothiazolinylidene)-l, 3- pentadienyl] benzothiazolium iodide, is an old effective broad-spectrum human anthelmintic. In proper dosage, this polyvermicide is therapeutic for trichuriasis, strongyloidiasis, ascariasis, and enterobiasis. The drug also has significant anthelmintic activity against human hookworm, Necator americanus. It fulfills a need for an effective therapeutic for trichuriasis and strongyloidiasis. Dithiazanine is useful for the treatment of patients with either single or multiple intestinal helminth infections. It is effective for mass therapy for trichuriasis. Nowdays Dithiazanine is used only as a veterinary anthelmintic for dogs. It has being proved to be a highly toxic chemical, with a lethal dose for humans of about 4–16 mg/kg by oral ingestion.
Status:
US Previously Marketed
First approved in 1958
Source:
Madribon by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfadimethoxine is a sulfonamide antibacterial used to treat many infections including treatment of respiratory, urinary tract, enteric, and soft tissue infections. It is most frequently used in veterinary medicine, although it is approved in some countries for use in humans. Sulfadimethoxine inhibits bacterial synthesis of folic acid (pteroylglutamic acid) from para-aminobenzoic acid. Sulfadimethoxine is approved in Russia for use in humans, including children, and has been successfully used there for more than 35 years and is available as an over-the-counter drug manufactured by a number of Russian pharmaceutical companies. In USA and Europe sulfadimethoxine is approved in a veterinary medicinal products. ANADA was approved by FDA in US in 1997 as an Over the Counter medicine for treatment of bovine respiratory disease complex (shipping fever complex) and bacterial pneumonia associated with Pasteurella Spp. Sensitive to sulfadimethoxine; necrotic pododermatitis (foot rot) and calf diphtheria caused by Fusobacterium necrophorum (Sphaerophorus necrophorus) sensitive to sulfadimethoxine. Bioequivalence for this generic animal drug, Sulfadimethoxine Injection 40%, was established by demonstration of chemical equivalence to the pioneer product, Hoffmann-La Roche's Albon® Injection 40% (NADA 041-245).
Triamcinolone is a long-acting synthetic corticosteroid primarily used for their anti-inflammatory effects in disorders of many organ systems. Triamcinolone diacetate injectable suspension is indicated for intramuscular use as follows: Allergic States Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment in asthma, atopic dermatitis, contact dermatitis, drug hypersensitivity reactions, perennial or seasonal allergic rhinitis, serum sickness, transfusion reactions. Bullous dermatitis herpetiformis, exfoliative erythroderma, mycosis fungoides, pemphigus, severe erythema multiform (Stevens-Johnson syndrome). Endocrine Disorders Primary or secondary adrenocortical insufficiency, congenital adrenal hyperplasia, hypercalcemia associated with cancer, nonsuppurative thyroiditis. To tide the patient over a critical period of the disease in regional enteritis and ulcerative colitis. Hematologic Disorders Acquired (autoimmune) hemolytic anemia, Diamond-Blackfan anemia, pure red cell aplasia, selected cases of secondary thrombocytopenia. Trichinosis with neurologic or myocardial involvement, tuberculous meningitis with subarachnoid block or impending block when used with appropriate ant tuberculous chemotherapy. For palliative management of leukemia’s and lymphomas. Nervous System Acute exacerbations of multiple sclerosis; cerebral edema associated with primary or metastatic brain tumor, or craniotomy. Sympathetic ophthalmia, uveitis and ocular inflammatory conditions unresponsive to topical corticosteroids. To induce diuresis or remission of proteinuria in idiopathic nephrotic syndrome or that due to lupus erythematosus. Berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate ant tuberculous chemotherapy, idiopathic eosinophilic pneumonias, symptomatic sarcoidosis. As adjunctive therapy for short-term administration in acute gouty arthritis; acute rheumatic carditis. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins that, through inhibition of arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Firstly, however, these glucocorticoids bind to the glucocorticoid receptors, which translocate into the nucleus, bind DNA (GRE), and change genetic expression both positively and negatively. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.