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

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Showing 33101 - 33110 of 34007 results

Status:
US Previously Marketed
First approved in 1961

Class (Stereo):
CHEMICAL (ACHIRAL)



Thiethylperazine is a antiemetic, which was used for the treatment of nausea and vomiting in patients undergoing radiotherapy, chemotherapy or as a postoperative care. Thiethylperazine exerts its therapeutic effect by blocking dopamine receptors in brain. The drug is capable of potentiating CNS depressants as well as atropine.
Status:
US Previously Marketed
First approved in 1961

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dromostanolone Propionate (known by the brand names Masteron and Drolban) was invented by Syntex in 1959. About 10 years later it was released on the American market by Lilly as brand name Drolban. The drug was first approved in the USA for use as a treatment of female breast cancer. However, the profile of side-effects included pronouncement of male characteristics in women and when more effective breast cancer treatments came to market drostanolone was gradually phased out. No longer used clinically dromostanolone propionate became very popular in the bodybuilding community. Today dromostanolone propionate remains on the list of approved medications, but it is not being manufactured or sold by pharmaceutical companies. It is still produced illegally by underground labs for use in the bodybuilding community.
Status:
US Previously Marketed
Source:
METHYCLOTHIAZIDE AND DESERPIDINE by WATSON LABS
(1984)
Source URL:
First approved in 1960

Class (Stereo):
CHEMICAL (UNKNOWN)


Conditions:

Methyclothiazide, a diuretic-antihypertensive agent, is a member of the benzothiadiazine (thiazide) class of drugs. Methyclothiazide has a per mg natriuretic activity approximately 100 times that of the prototype thiazide, chlorothiazide. At maximal therapeutic dosages, all thiazides are approximately equal in their diuretic/natriuretic effects. Like other benzothiadiazines, methyclothiazide also has antihypertensive properties, and may be used for this purpose either alone or to enhance the antihypertensive action of other drugs. Methyclothiazide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle, altering electrolyte transfer in the proximal tubule. This results in excretion of sodium, chloride, and water and, hence, diuresis. As a diuretic, methyclothiazide 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. Thiazides like methyclothiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of methyclothiazide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle. Methyclothiazide is used in the management of hypertension either as the sole therapeutic agent or to enhance the effect of other antihypertensive drugs in the more severe forms of hypertension. Also used as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy.
Status:
US Previously Marketed
Source:
METHYCLOTHIAZIDE AND DESERPIDINE by WATSON LABS
(1984)
Source URL:
First approved in 1960

Class (Stereo):
CHEMICAL (UNKNOWN)


Conditions:

Methyclothiazide, a diuretic-antihypertensive agent, is a member of the benzothiadiazine (thiazide) class of drugs. Methyclothiazide has a per mg natriuretic activity approximately 100 times that of the prototype thiazide, chlorothiazide. At maximal therapeutic dosages, all thiazides are approximately equal in their diuretic/natriuretic effects. Like other benzothiadiazines, methyclothiazide also has antihypertensive properties, and may be used for this purpose either alone or to enhance the antihypertensive action of other drugs. Methyclothiazide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle, altering electrolyte transfer in the proximal tubule. This results in excretion of sodium, chloride, and water and, hence, diuresis. As a diuretic, methyclothiazide 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. Thiazides like methyclothiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of methyclothiazide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle. Methyclothiazide is used in the management of hypertension either as the sole therapeutic agent or to enhance the effect of other antihypertensive drugs in the more severe forms of hypertension. Also used as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy.
Status:
US Previously Marketed
Source:
Oxaine by Wyeth
(1960)
Source URL:
First approved in 1960
Source:
Oxaine by Wyeth
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



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:
Allercur by Roerig (Pfizer)
(1960)
Source URL:
First approved in 1960
Source:
Allercur by Roerig (Pfizer)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Clemizole is a drug in clinical development for the treatment of hepatitis C virus (HCV) infection. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole is an H1 antagonist. Clemizole, an antihistamine drug that was once widely used for treatment of allergic disease, was recently discovered to be a potent inhibitor (IC50, 24 nM) of the interaction between an HCV protein (NS4B) and HCV RNA. Although clemizole was widely used during the 1950s and 1960s, this was before contemporary regulatory requirements were established for new drug development, and there is very minimal information about its pharmacokinetics and metabolism.
Status:
US Previously Marketed
Source:
Sorboquel by White (Schering)
(1960)
Source URL:
First approved in 1960
Source:
Sorboquel by White (Schering)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Methyl thihexinolium (or thihexinol methylbromide) can inhibit the intestinal hypermotility. Information about the current use of this compound is not available.
Status:
US Previously Marketed
Source:
Adroyd by Parke-Davis
(1960)
Source URL:
First approved in 1960
Source:
Adroyd by Parke-Davis
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Oxymetholone (17beta-hydroxy-2-[hydroxymethylene]-17-methyl-5alpha-androstan-3-one) is a 17alpha-alkylated anabolic-androgenic steroid and a synthetic derivative of testosterone. It has been approved by the US Food and Drug Administration for the treatment of anemias caused by deficient red cell production. Acquired aplastic anemia, congenital aplastic anemia, myelofibrosis and the hypoplastic anemias due to the administration of myelotoxic drugs often respond. Drug interactions exist with cimetidine, paroxetine, and haloperidol, but are not expected with indinavir, ritonavir, clarithromycin, or itraconazole.
Status:
US Previously Marketed
Source:
ANALEXIN PHENYRAMIDOL HYDROCHLORIDE by MALLINCKRODT
(1961)
Source URL:
First approved in 1960
Source:
Analexin by Irwin, Neisler (Mallinckrodt)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

PHENYRAMIDOL (ANALEXIN®), also known as fenyramidol, is an aminopyridine derivative, used as analgesic and muscle relaxant. It is considered as a drug that possibly causes hepatotoxicity.
Status:
US Previously Marketed
Source:
Allercur by Roerig (Pfizer)
(1960)
Source URL:
First approved in 1960
Source:
Allercur by Roerig (Pfizer)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Clemizole is a drug in clinical development for the treatment of hepatitis C virus (HCV) infection. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole is an H1 antagonist. Clemizole, an antihistamine drug that was once widely used for treatment of allergic disease, was recently discovered to be a potent inhibitor (IC50, 24 nM) of the interaction between an HCV protein (NS4B) and HCV RNA. Although clemizole was widely used during the 1950s and 1960s, this was before contemporary regulatory requirements were established for new drug development, and there is very minimal information about its pharmacokinetics and metabolism.

Showing 33101 - 33110 of 34007 results