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

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Showing 1091 - 1100 of 3134 results

Status:
US Previously Marketed
First approved in 1962

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Methoxyflurane is an inhalation anesthetic. Methoxyflurane was used for surgical, obstetric, or dental anesthesia, but was withdrawn from US market due to safety concerns, but is still in use in Australia and other countries. Methoxyflurane induces muscle relaxation and reduces pains sensitivity by altering tissue excitability by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential.
Status:
US Previously Marketed
Source:
Theratuss by Squibb
(1962)
Source URL:
First approved in 1962
Source:
Theratuss by Squibb
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

PIPAZETHATE is a non-narcotic oral antitussive agent. It acts centrally on the medullary cough center and is used for the treatment of cough.
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
Source:
ISOETHARINE HYDROCHLORIDE by ASTRAZENECA
(1984)
Source URL:
First approved in 1961
Source:
Bronkosol by Sterling
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Isoetharine is a beta-2 adrenergic receptor agonist, which was developed by Max Bockmuhl, Gustav Erhart and Leonhard Stein at the Hochst laboratories of I.G. Farbenindustrie in 1934. By binding to beta-2 adrenergic receptors on bronchial cell membranes, isoetharine increases the level of cAMP and thus stimulates the relaxation of smooth-muscle cells, stabilizes mast cells and inhibits histamine release. Isoetharine was approved by FDA for the symptomatic relief of bronchiospasms in patients with chronic bronchitis or emphysema (aerosol and solution for inhalation), however, later on the drug was discontinued.
Status:
US Previously Marketed
First approved in 1961

Class (Stereo):
CHEMICAL (RACEMIC)



Polythiazide is a thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. Polythiazide under brand name Rense is indicated as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Renese is indicated in the management of hypertension either as the sole therapeutic agent or to enhance the effectiveness of other antihypertensive drugs in the more severe forms of hypertension. The mechanism of action results in an interference with the renal tubular mechanism of electrolyte reabsorption. At maximal therapeutic dosage, all thiazides are approximately equal in their diuretic potency. The mechanism whereby thiazides function in the control of hypertension is unknown, but as a diuretic, polythiazide inhibits active chloride reabsorption at the early distal tubule via the thiazide-sensitive Na-Cl cotransporter (TSC), resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like polythiazide 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 polythiazide 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.
Status:
US Previously Marketed
Source:
Trepidone by Lederle
(1961)
Source URL:
First approved in 1961

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Mephenoxalone is an oxazolidinone compound. It is a skeletal muscle relaxant as well as anxiolytic. Mephenoxalone is indicated for the treatment of muscle spasms.
Status:
US Previously Marketed
Source:
Capla by Wallace
(1961)
Source URL:
First approved in 1961
Source:
Capla by Wallace
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Mebutamate (Capla, Dormate) is a biscarbamate drug that has anxiolytic, sedative, and antihypertensive effects. It is marketed under many trade names, including Capla and Dormate. Its preparation was reported in a 1959 US patent to Carter Products. It is less well known that mebutamate is also hypnotic. In a 1967 study, L. Tetreault, P. Richer, and J. M. Bordeleau in Montreal found that, at a dose of 600 mg, mebutamate has hypnotic properties that “affect the duration and quality of sleep induction, and the duration and quality of sleep, without disturbing the state of the subject upon awakening and during the morning.” A higher dose (900 mg) did not change the overall effect, which was “consistently between that of secobarbital at 200 mg and 100 mg.” The authors did not observe any significant side effects. Mebutamate is one of many GABAergic drugs which act via allosteric agonism of the GABAA receptor at the β-subreceptor similar to barbiturates. In contrast, benzodiazepines act at the α-subreceptor. As such, carbamates and barbiturates, possess analgesic properties which the benzodiazepine class of drugs does not.
Status:
US Previously Marketed
First approved in 1961

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Acetophenazine (Tindal) is an antipsychotic drug of moderate-potency. Used in the treatment of disorganized and psychotic thinking. Acetophenazine (Tindal) is also used to help treat false perceptions (e.g. hallucinations or delusions). Acetophenazine acts as an antagonist of dopaminergic D2 receptors in the brain. Acetophenazine exhibited modest androgen receptor binding and antiandrogen activity.
Status:
US Previously Marketed
Source:
Emivan by U.S. Vitamin (USV)
(1961)
Source URL:
First approved in 1961
Source:
Emivan by U.S. Vitamin (USV)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Ethamivan or etamivan, a respiratory stimulant was used in pulmonary emphysema.
Status:
US Previously Marketed
Source:
Staphcillin by Bristol
(1960)
Source URL:
First approved in 1960
Source:
Staphcillin by Bristol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Methicillin sodium anhydrous is a sodium salt of methicillin (methicillin). Methicillin is an antibiotic formerly used in the treatment of bacterial infections caused by organisms of the genus Staphylococcus. Methicillin is a semisynthetic derivative of penicillin. It was first produced in the late 1950s and was developed as a type of antibiotic called penicillinase-resistant penicillin—it contained a modification to the original penicillin structure that made it resistant to a bacterial enzyme called penicillinase (beta-lactamase). Compared to other penicillins that face antimicrobial resistance due to β-lactamase, it is less active, can be administered only parenterally, and has a higher frequency of interstitial nephritis, an otherwise-rare adverse effect of penicillins. However, the selection of meticillin depended on the outcome of susceptibility testing of the sampled infection, and since it is no longer produced, it is also not routinely tested for anymore.

Showing 1091 - 1100 of 3134 results