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

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Showing 91 - 100 of 194 results

Status:
US Previously Marketed
Source:
CHLOROMYCETIN HYDROCORTISONE by PARKEDALE
(1953)
Source URL:
First approved in 1950
Source:
Chloromycetin by Warner-Lambert
Source URL:

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
First approved in 1947
Source:
Synestrol by White (Schering)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dienestrol (INN, USAN) (brand names Ortho Dienestrol, Dienoestrol, Dienoestrol Ortho, Sexadien, Denestrolin, Dienol, Dinovex, Follormon, Oestrodiene, Synestrol, numerous others) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist. Estrogens work partly by increasing a normal clear discharge from the vagina and making the vulva and urethra healthy. Using or applying an estrogen relieves or lessens: dryness and soreness in the vagina, itching, redness, or soreness of the vulva. Conditions that are treated with vaginal estrogens include a genital skin condition (vulvar atrophy), inflammation of the vagina (atrophic vaginitis), and inflammation of the urethra (atrophic urethritis). Dienestrol currently discontinued in US, but still in market in some other counties
Status:
US Previously Marketed
Source:
PRANONE by SCHERING
(1939)
Source URL:
First approved in 1939

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ethisterone is a metabolite of danazol. Ethisterone is a progestogen hormone. The first orally active progestin, Ethisterone (brand names Pranone, Progestoral, Lutocylol, Proluton C), also known as 17α-ethinyltestosterone, pregneninolone, or anhydrohydroxyprogesterone, is a steroidal progestin with androgenic activity which is derived from testosterone and was introduced for medical use in 1939. Ethisterone is indicated for progesterone supplementation or replacement as part of an Assisted Reproductive Technology (ART) treatment for infertile women with progesterone deficiency and for the treatment of secondary amenorrhea. Also used as a female contraceptive.
Status:
US Previously Marketed
Source:
SULFAMETHOXAZOLE AND TRIMETHOPRIM AND PHENAZOPYRIDINE HYDROCHLORIDE by ABLE
(2001)
Source URL:
First marketed in 1928
Source:
Pyridium
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Phenazopyridine hydrochloride, an azo dye first synthesized in 1914, became widely prescribed for the treatment of urinary tract infections (UTIs). With the assumption that the drug possessed antiseptic properties, phenazopyridine was recommended for UTIs caused by Staphylococcus, Streptococcus, and Escherichia coli. Although in the early 1930s the medical and scientific communities rescinded the claim that phenazopyridine is bactericidal, a specific mechanism of action has not been identified subsequently. Currently, phenazopyridine is classified as a urinary analgesic that relieves burning, urgency, frequency, and pain associated with UTI, trauma, or surgery.
Status:
US Previously Marketed
Source:
GENTIA-JEL APPLICATORS by WESTWOOD
(1961)
Source URL:
First marketed in 1921
Source:
gentian violet
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Gentian violet ((GV) hexamethyl pararosaniline, also known as crystal violet, methyl violet) is a triphenylmethane dye with anti-bacterial, anti-fungal, anti-helminithic, anti-trypanosomal, anti-angiogenic and anti-tumor properties. GV has a lengthy history and has been used successfully as monotherapy and an adjunct to treatment in a variety of diseases. Gentian violet interacts with negatively charged components of bacterial cells including the lipopolysaccharide (on the cell wall), the peptidoglycan and DNA. A similar cell penetration and DNA binding process is thought to take place for fungal cells as well. Because Gentian violet is a mutagen and mitotic poison, cell growth is consequently inhibited. A photodynamic action of gentian violet, apparently mediated by a free-radical mechanism, has recently been described in bacteria and in the protozoan T. cruzi. Evidence also suggests that gentian violet dissipates the bacterial (and mitochondrial) membrane potential by inducing permeability. This is followed by respiratory inhibition. This anti-mitochondrial activity might explain gentian violet's efficacy towards both bacteria and yeast with relatively mild effects on mammalian cells.
Status:
US Previously Marketed
Source:
Phenyl Salicylate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Phenyl Salicylate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Phenyl salicylate belongs to the family of hydroxybenzoic acid derivatives. Phenyl salicylate is used as a food additive. Antimycobacterial activity of phenyl salicylates (salols) was studied in connection with antituberculotic activity of salicylic derivatives. Phenyl salicylates are esters. Phenyl salicylates (salols) represent a new group of antimycobacterial compounds. Phenyl salicylate is included in the number of medications, indicated for the treatment of symptoms of irritative voiding, used to relieve the discomfort, pain, frequent urge to urinate, and cramps/spasms of the urinary tract caused by an infection or a medical procedure. Phenyl salicylate works as a pain reliever in these combinations.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Octenidine dihydrochloride is a cationic surfactant, with antimicrobial activity against Gram-positive and Gram-negative bacteria. Octenidine approved as a medicinal substance in several European countries and used for skin antisepsis in combination with aliphatic alcohols, e.g. propan-1-ol and propan-2-ol, or with detergents such as antiseptic soap. Octenidine is also used for antisepsis on wounds and mucosa either as a single substance, as an approved combination of Octenidine and phenoxyethanol. Octenidine is virtually not absorbed via the skin or mucous membranes. Because Octenidine is only approved and used topically and is virtually not absorbed, no systemic effects are to be expected. Therefore, no further pharmacokinetic studies or studies on behalf of metabolism have been conducted. Octenidine is easy and safe to handle, chemically stable, not inflammable, without resistance development and low toxicity to man and the environment alike. Its popularity among therapists and wound care specialists is based on good clinical results, easy and pain-free application and local tolerance. Beside readily available combinations with phenoxyethanol, mouth rinses, and vaginal applications, semi-fluid preparations and dressings are described.
Status:
Possibly Marketed Outside US
Source:
NCT01056042: Phase 4 Interventional Completed Endometriosis
(2007)
Source URL:
First approved in 2018

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Gestodene (17alpa-ethynyl-13beta-ethyl-17beta-hydroxy-4,15-gonadien-3-one) is the most potent synthetic progestin currently available and it is widely used as a fertility regulating agent in a number of contraceptive formulations because of its high effectiveness, safety and acceptability. Products containing gestoden include Meliane, which contains 20 ug of ethinylestradiol and 75 ug of gestodene; and Gynera, which contains 30 ug of ethinylestradiol and 75 ug of gestodene. Gestodene is androgenically neutral, meaning that contraceptive pills containing gestodene do not exhibit the androgenic side effects (e.g. acne, hirsutism, weight gain) often associated with second-generation contraceptive pills. Gestodene displays a high binding affinity to the progesterone receptor, also binds to adrogen and glucocorticoid receptors but no measurable affinity for the estrogen receptor.
Status:
Possibly Marketed Outside US
Source:
NCT03044652: Phase 4 Interventional Completed Vulvovaginal Atrophy
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Estriol (E3), also spelled oestriol, is a steroid, a weak agonist of the estrogen receptors ERα and ERβ., and a minor female sex hormone. According to in vitro study, the relative binding affinity (RBA) of estriol for the human ERα and ERβ was 11.3% and 17.6% of that estradiol, respectively, and the relative transactivational capacity of estrone at the ERα and ERβ was 10.6% and 16.6% of that of estradiol, respectively. Estriol is marketed widely in Europe and elsewhere throughout the world under the brand names Ovestin, Ortho-Gynest, and a variety of others. It is available in oral tablet, vaginal cream, and vaginal suppository form, and is used in menopausal hormone therapy for the treatment of menopausal symptoms. Estriol is also available in some countries as estriol succinate (brand name Synapause), a dosage-equivalent ester prodrug of estriol. Estriol and estriol succinate are not approved for use in the United States and Canada, although they have been produced and sold by compounding pharmacies in North America for use as a component of bioidentical hormone therapy. Estriol can be measured in maternal blood or urine and can be used as a marker of fetal health and well-being. If levels of unconjugated estriol (uE3 or free estriol) are abnormally low in a pregnant woman, this may indicate chromosomal or congenital anomalies like Down syndrome or Edward's syndrome. It is included as part of the triple test and quadruple test for antenatal screening for fetal anomalies.
Status:
Possibly Marketed Outside US
Source:
Canada:INOSINE PRANOBEX
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Inosine is a naturally occurring nucleoside which serves as an intermediate in purine metabolism. The metabolism of purines in humans generates a potent antioxidant compound, uric acid, which is known to be a natural scavenger of both oxygen and nitrogen reactive species as well as having chelator properties. Inosine, as a precursor of uric acid, was shown to have neuroprotective effect in vitro and is being tested in phase III of clinical trials for the treatment of Parkinson disease. The treatment with inosine is belived to prevent or slow the disease.