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Status:
US Previously Marketed
Source:
ACETOHEXAMIDE by USL PHARMA
(1986)
Source URL:
First approved in 1964
Source:
DYMELOR by LILLY
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Acetohexamide (trade name Dymelor) is a first-generation sulfonylurea medication used to treat diabetes mellitus type 2, particularly in people whose diabetes cannot be controlled by diet alone. It lowers blood sugar by stimulating the pancreatic beta cells to secrete insulin and by helping the body use insulin efficiently. The pancreas must produce insulin for this medication to work. Acetohexamide binds to an ATP-dependent K+ channel on the cell membrane of pancreatic beta cells. This inhibits a tonic, hyperpolarizing out flux of potassium, which causes the electric potential over the membrane to become more positive. This depolarization opens voltage-gated Ca2+ channels. The rise in intracellular calcium leads to increased fusion of insulin granule with the cell membrane, and therefore increased secretion of (pro) insulin. Acetohexamide extensively metabolized in the liver to the active metabolite hydroxyhexamide, which exhibits greater hypoglycemic potency than acetohexamide. Hydroxyhexamide is believed to be responsible for prolonged hypoglycemic effects. Symptoms of an acetohexamide overdose include hunger, nausea, anxiety, cold sweats, weakness, drowsiness, unconsciousness, and coma. Acetohexamide has been discontinued in the US market.
Status:
First approved in 1964
Source:
21 CFR 358A
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Padimate O is an organic compound related to the water-soluble compound PABA (4-aminobenzoic acid) that is used as an ingredient in some sunscreens. this chemical releases free radicals, damages DNA, has estrogenic activity, and causes allergic reactions in some people. Maximum FDA-approved concentration - 8%. Range of protection - UVB.
Status:
US Previously Marketed
Source:
FLORINEF by SQUIBB
(1962)
Source URL:
First approved in 1962
Source:
FLORINEF by SQUIBB
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
US Previously Marketed
Source:
NOVRAD by LILLY
(1962)
Source URL:
First approved in 1962
Source:
NOVRAD by LILLY
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
LEVOPROPOXYPHENE is an antitussive drug, one of enantiomer of propoxyphene. Pdropoxyphene is an analgesic in the opioid category, patented in 1955 and manufactured by Eli Lilly and Company. Pdropoxyphene is intended to treat mild pain and also has antitussive (cough suppressant) and local anaesthetic effects.
Status:
US Previously Marketed
Source:
TPN by INTL MINERALS
(1961)
Source URL:
First approved in 1961
Source:
TPN by INTL MINERALS
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Tyrosine (L-form) is a non-essential amino acid, which is primarily required for the protein synthesis. This amino acid is the precursor of dopamine, norepinephrine, and epinephrine; therefore the lower concentration of tyrosine could be a peripheral marker of the hyperdopaminergic condition hypothesized to explain psychosis. Tyrosine supplements can improve cognition, increase energy, reduce anxiety, reduce depression, reduce levels of pain.
Status:
US Previously Marketed
Source:
BENZTHIAZIDE by PVT FORM
(1976)
Source URL:
First approved in 1960
Source:
EXNA by AH ROBINS INC
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Benzthiazide (trade names Aquatag, Dihydrex, Diucen, Edemax, Exna, Foven and others) is a thiazide diuretic used in the treatment of high blood pressure and edema. It is no longer available in the United States. As a diuretic, benzthiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. The following is a list of possible side effects that may occur from all constituting ingredients of Exna Tablet: vomiting, diarrhoea, photosensitivity reactions, increased in uric acid concentrations, megaloblastic anaemia, thrombocytopenia. Exna tablet may interact with the following drugs and products: ACE inhibitors, angiotensin II receptor antagonists, potassium-sparing diuretics.
Status:
First approved in 1960
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Aminoglutethimide, marketing as Cytadren has been used in the treatment of advanced breast and prostate cancer. It was formerly used for its weak anticonvulsant properties. Cytadren is indicated for the suppression of adrenal function in selected patients with Cushing’s syndrome. Morning levels of plasma cortisol in patients with adrenal carcinoma and ectopic ACTH producing tumors were reduced on the average to about one half of the pretreatment levels, and in patients with adrenal hyperplasia to about two thirds of the pretreatment levels, during 1-3 months of therapy with Cytadren. Data available from the few patients with adrenal adenoma suggest similar reductions in plasma cortisol levels. Measurements of plasma cortisol showed reductions to at least 50% of baseline or to normal levels in one third or more of the patients studied, depending on diagnostic groups and time of measurement. Because Cytadren does not affect the underlying disease process, it is used primarily as an interim measure until more definitive therapy such as surgery can be undertaken or in cases where such therapy is not appropriate. Only small numbers of patients have been treated for longer than 3 months. A decreased effect or “escape phenomenon” seems to occur more frequently in patients with pituitary dependent Cushing’s syndrome, probably because of increasing ACTH levels in response to decreasing glucocorticoid levels. Cytadren blocks several other steps in steroid synthesis, including the C-11, C-18, and C-21 hydroxylations and the hydroxylations required for the aromatization of androgens to estrogens, mediated through the binding of Cytadren to cytochrome P-450 complexes. A decrease in adrenal secretion of cortisol is followed by an increased secretion of pituitary adrenocorticotropic hormone (ACTH), which will overcome the blockade of adrenocortical steroid synthesis by Cytadren. The compensatory increase in ACTH secretion can be suppressed by the simultaneous administration of hydrocortisone. Since Cytadren increases the rate of metabolism of dexamethasone but not that of hydrocortisone, the latter is preferred as the adrenal glucocorticoid replacement. Although Cytadren inhibits the synthesis of thyroxine by the thyroid gland, the compensatory increase in thyroid-stimulating hormone (TSH) is frequently of sufficient magnitude to overcome the inhibition of thyroid synthesis due to Cytadren. In spite of an increase in TSH, Cytadren has not been associated with increased prolactin secretion. At low doses, aminogluthethimide is only an effective inhibitor of aromatase (Cytochrome P450 11A1), but at higher doses, it effectively blocks Cytochrome P450 11A1 (P450scc) as well. Citadel was marketed previously as an anticonvulsant but was withdrawn from marketing for that indication in 1966 because of the effects on the adrenal gland.
Status:
First approved in 1960
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Oxethazaine is a potent local anesthetic. It is administered orally (usually in combination with an antacid) for the relief of pain associated with peptic ulcer disease or esophagitis. Its effectiveness at the acidity of the gastric environment is due to the fact that oxethazaine, a weak base, is relatively non-ionized at pH 1. It is also used topically in the management of hemorrhoid pain. Oral oxetacaine preparations are available in several countries, including India, South Africa and Brazil, but not the United States. It is marketed under the name Strocain in Japan.
Status:
US Previously Marketed
Source:
GUANETHIDINE MONOSULFATE by WATSON LABS
(1985)
Source URL:
First approved in 1960
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Guanethidine belongs to the general class of medicines called antihypertensives. It was used to treat high blood pressure (hypertension). It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues. It is taken up by norepinephrine transporters. It becomes concentrated in NE transmitter vesicles, replacing NE in these vesicles.
Status:
US Previously Marketed
Source:
TACE 25 MG ERGONOVINE by MERRELL
(1959)
Source URL:
First approved in 1959
Source:
TACE 25 MG ERGONOVINE by MERRELL
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ergonovine (also known as ergometrine) is the active water soluble component of ergot of rye. Ergonovine is being used as a maleate salt to prevent or treate postpartum haemorrhage and postabortion haemorrhage. Ergonovine stimulates alpha-adrenergic and serotonin receptors, thus activating contractions of uterine and vascular smooth muscle. Ergonovine may have depressant effect on CNS system as it binds to dopamine receptors.