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

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Showing 21 - 30 of 119 results

Thiamylal is a barbiturate that is administered intravenously for the production of complete anesthesia of short duration, for the induction of general anesthesia, or for inducing a hypnotic state. Thiamylal, a barbiturate, is used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia. Thiamylal binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
Status:
US Previously Marketed
Source:
Ilidar by Hoffmann-La Roche
(1954)
Source URL:
First approved in 1954
Source:
Ilidar by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


AZAPETINE, a benzazepine derivative, is an alpha-1 adrenoceptor antagonist. It is a potent arterial vasodilator in the treatment of peripheral vascular diseases.
Tridihexethyl is a synthetic anticholinergic agent which was marketed under the brand name Pathilon as an adjunct in the treatment of peptic ulcer disease. However, it is no longer available in the US market. Tridihexethyl may block all three types of muscarinic receptors including M-1 receptors in the CNS and ganglia, M-2 receptors in the heart, and M-3 receptors. The muscarinic acetylcholine receptors mediate various cellular responses including inhibition of adenylate cyclase, the breakdown of phosphoinositides, and modulation of potassium channels through the action of G proteins. Tridihexethyl inhibits vagally mediated reflexes by antagonizing the action of acetylcholine. This, in turn, reduces the secretion of gastric acids in the stomach. Tridihexethyl was also examined for effect on patients with acquired nystagmus where four out of six patients showed improvement, but due to the profile usage of Tridihexethyl to treat nystagmus was limited.
Status:
US Previously Marketed
First approved in 1954
Source:
Softran by Stuart
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Buclizine, a piperazine derivative, is a sedating antihistamine with antimuscarinic and moderate sedative action. The drug is used mainly for its antiemetic action, particularly in the prevention of motion sickness, and in the treatment of migraine in combination with analgesics. The following side/adverse effects have been selected on the basis of their potential clinical significance: drowsiness; Incidence less frequent; blurred vision; dryness of mouth, nose, and throat; headache; nervousness, restlessness, or trouble in sleeping; upset stomach. The following drug interactions have been selected on the basis of their potential clinical significance: alcohol; anticholinergics or other medications with anticholinergic activity; apomorphine.
Status:
US Previously Marketed
First approved in 1954

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Talbutal is a short to intermediate-acting barbiturate, which had been used under brand name Latusate as a sedative and hypnotic, but then this usage was discontinued. It was found, that talbutal binds at a distinct binding site at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. Thus, the post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
Status:
US Previously Marketed
First approved in 1954

Class (Stereo):
CHEMICAL (MIXED)

Conditions:

Trimethaphan (or Trimethaphan camsylate), a ganglionic blocking agent and an antihypertensive drug, was marketed under the brand name Arfonad. Arfonad is indicated to induce systemic arterial hypotension in patients undergoing major surgery and to treat severe systemic hypertension, and in the emergency treatment of pulmonary edema in patients with pulmonary hypertension associated with systemic hypertension. Trimethaphan prevents stimulation of postsynaptic receptors by competing with acetylcholine for these receptor sites. Additional effects may include direct peripheral vasodilation and release of histamine. This drug was discontinued because of the competition from newer drugs that are more selective in their actions and effects.
Status:
US Previously Marketed
First approved in 1954
Source:
Ansolysen by Wyeth
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Pentolinium (brand name Ansolysen) is a ganglionic cholinergic antagonist, acting on alpha 3 beta 4 neuronal nicotinic acetylcholine receptors (nAChRs). It was used as an antihypertensive drug during surgery or to control hypertensive crises, but Ansolysen was discontinued. Pentolinium inhibits release of adrenaline and noradrenaline from adrenergic nerves.
Status:
US Previously Marketed
Source:
Compocillin-V by Abbott
(1954)
Source URL:
First approved in 1954
Source:
Compocillin-V by Abbott
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


PENICILLIN V HYDRABAMINE, a semi-synthetic antibiotic, is used for the treatment of mild to moderately severe infections (e.g. dental infection, infections in the heart, middle ear infections, rheumatic fever, scarlet fever, skin infections, upper and lower respiratory tract infections) caused by susceptible, usually gram-positive, organisms.
Status:
US Previously Marketed
Source:
Mictine (Mincard) by Searle
(1954)
Source URL:
First approved in 1954
Source:
Mictine (Mincard) by Searle
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

AMINOMETRADINE, a uracil derivative, is a diuretic. It appears to inhibit the reabsorption of sodium ions by the renal tubules. AMINOMETRADINE is used in the management of edema and in the treatment of congestive heart failure.
Status:
US Previously Marketed
Source:
Gallogen by Massengill
(1954)
Source URL:
First approved in 1954
Source:
Gallogen by Massengill
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)


Tocamphyl is a choleretic agent derived from a root extract of Curcuma longa, L. The drug was marketed in Japan, however, it is no longer available.