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Search results for m root_references_citation in Reference Text / Citation (approximate match)
Status:
First approved in 1954
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
BETAZOLE is a histamine H2 receptor agonist used clinically to test gastric secretory function.
Status:
US Previously Marketed
Source:
CHLOROMYCETIN HYDROCORTISONE by PARKEDALE
(1953)
Source URL:
First approved in 1950
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Chloramphenicol is a broad-spectrum antibiotic that was first isolated from
Streptomyces venezuelae in 1947. The drug was subsequently chemically synthesized. It has both a bacteriostatic and bactericidal effect; in the usual therapeutic concentrations it is bacteriostatic. Chloramphenicol is used for the treatment of serious gram-negative, gram-positive, and anaerobic infections. It is especially useful in the treatment of meningitis, typhoid fever, and cystic fibrosis. It should be reserved for infections for which other drugs are ineffective or contraindicated. Chloramphenicol, a small inhibitor of bacterial protein synthesis, is active against a variety of bacteria and readily enters the CSF. It has been used extensively in the last decades for the treatment of bacterial meningitis. In industrialized countries, chloramphenicol is restricted mostly to topical uses because of the risk of induction of aplastic anemia. However, it remains a valuable reserve antibiotic for patients with allergy to β-lactam antibiotics or with CNS infections caused by multiresistant pathogens.
Status:
US Previously Marketed
Source:
CAMOQUIN HYDROCHLORIDE by PARKE DAVIS
(1950)
Source URL:
First approved in 1950
Source:
CAMOQUIN HYDROCHLORIDE by PARKE DAVIS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Amodiaquine is a medication used to treat malaria, including Plasmodium falciparum malaria when uncomplicated. The mechanism of plasmodicidal action of amodiaquine is not completely certain. Like other quinoline derivatives, it is thought to inhibit heme polymerase activity. This results in accumulation of free heme, which is toxic to the parasites. The drug binds the free heme preventing the parasite from converting it to a form less toxic. This drug-heme complex is toxic and disrupts membrane function. The side effects of amodiaquine are generally minor to moderate and are similar to those of chloroquine. Rarely liver problems or low blood cell levels may occur. When taken in excess headaches, trouble seeing, seizures, and cardiac arrest may occur. After oral administration amodiaquine hydrochloride is rapidly absorbed,and undergoes rapid and extensive metabolism to desethylamodiaquine which concentrates in red blood cells. It is likely that desethylamodiaquine, not amodiaquine, is responsible for most of the observed antimalarial activity, and that the toxic effects of amodiaquine after oral administration may in part be due to desethylamodiaquine.
Status:
First approved in 1950
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Cyclamic acid (Cyclamate) is banned in the United States but it is used in many other Western countries without safety concerns. Cyclamate interacts with the sweet taste receptor subunit T1R3 transmembrane domain. Initially it was recommended for use in treatment of obese patients and by individuals with diabetes but in August 27, 1970 FDA concluded that there was no substantial evidence of effectiveness of cyclamate compounds at any level for treatment of obese patients and individuals with diabetes and therefore prohibited continued sale of cyclamate containing products with drug labeling. cyclamate is the putative carcinogenic agent. Cyclamate was tested in the Maximal Electroshock Seizure model (mice, ip), showing moderate anticonvulsant activity.
Status:
First approved in 1940
Class (Stereo):
CHEMICAL (ACHIRAL)
Menadione, a drug belong to class of Vitamin K, is prescribed for the treatment of hemorrhage, vitamin K deficiency, moderate to severe forms of hypoprothrombinaemia in adults and children. Menadione is a synthetic form of vitamin K, a lipid-soluble vitamin. Vitamin K is a vital cofactor for the biosynthesis of prothrombin, factor VII, IX, X, protein C and protein S. Menadione supports the functions of osteocalcin. Large doses of menadione have been reported to cause adverse outcomes including hemolytic anemia due to glucose-6-phosphate dehydrogenase deficiency, neonatal brain or liver damage, or neonatal death in some rare cases.
Status:
US Previously Marketed
Source:
TRIQUIN QUINACRINE HYDROCHLORIDE by WINTHROP
(1961)
Source URL:
First approved in 1938
Class (Stereo):
CHEMICAL (RACEMIC)
Quinacrine was initially developed as an anti-malarial drug marketed under the name Atabrine. Also it was approved for the teratment of ascites, however it was wothdrawn for both indication in 1995 and 2003, respectively. The drug is also used for the treatment of giardiasis, lupus, rheumatoid arthritis, refractory pulmonary effusion and pneumothorax, induce female sterilization etc. Proposed mechanisms of action include DNA intercalation interference with RNA transcription and translation, inhibition of succinate oxidation interference with electron transport, inhibition of cholinesterase, and inhibitor of phospholipase.
Status:
US Previously Marketed
Source:
Kephrine
(1937)
Source URL:
First marketed in 1937
Source:
Kephrine
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Adrenalone is a keton form of the natural substrate epinephrine. Adrenalone is evidently formed in vivo by hydrolytic cleavage of the diester by esterases. It is an adrenergic receptor agonist. Adrenalone inhibits the norepinephrine synthesis and dopamine beta oxidase. It is known to have very weak sympathomimetic activity when compared to adrenaline. Adrenalone has the high radioprotective effect. It is a topical nasal decongestant. Adrenalone has hemostatic, sympathomimetic and vasoconstrictor therapeutic functions.
Status:
US Previously Marketed
Source:
Pyrogallol U.S.P.
(1921)
Source URL:
First marketed in 1921
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
US Previously Marketed
Source:
Betanaphthol U.S.P.
(1921)
Source URL:
First marketed in 1921
Class (Stereo):
CHEMICAL (ACHIRAL)
BETANAPHTHOL (or 2-Naphthol) is used as a preservative. It is known, that this compound can cause dermatitis.
Status:
Possibly Marketed Outside US
Source:
LAGEVRIO by Merck Sharp & Dohme LLC
(2021)
Source URL:
First approved in 2021
Source:
LAGEVRIO by Merck Sharp & Dohme LLC
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)