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Status:
US Previously Marketed
First approved in 1967
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Diphenidol, a nonphenothiazinic antiemetic agent used primarily in patients with Meniere disease and labyrinthopathies to treat vomiting and vertigo, is considered to be a relatively safe drug. Since it was first approved in the United States in 1967, this drug has been widely used in Latin America and Asia and has contributed to sporadic suicidal and accidental poisonings in mainland China and Taiwan. The mechanism by which diphenidol exerts its antiemetic and antivertigo effects is not precisely known. It is thought to diminish vestibular stimulation and depress labyrinthine function and as an antimuscarinic agent. An action on the medullary chemoreceptive trigger zone may also be involved in the antiemetic effect. Diphenidol has no significant sedative, tranquilizing, or antihistaminic action. It has a weak peripheral anticholinergic effect. Diphenidol is used to relieve or prevent nausea, vomiting, and dizziness caused by certain medical problems.
Status:
First approved in 1966
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Betahistine is an orally administered, centrally acting histamine H1 receptor agonist with partial H3 antagonistic activity. It is proposed that betahistine may reduce peripherally the asymmetric functioning of the sensory vestibular organs in addition to increasing vestibulocochlear blood flow by antagonising local H3 heteroreceptors. Betahistine acts centrally by enhancing histamine synthesis within tuberomammillary nuclei of the posterior hypothalamus and histamine release within vestibular nuclei through antagonism of H3 autoreceptors. This mechanism, together with less specific effects of betahistine on alertness regulation through cerebral H1 receptors, should promote and facilitate central vestibular compensation. Betahistine is used to treat the symptoms associated with Ménière's disease, a condition of the inner ear which causes, vertigo (dizziness), tinnitus (ringing in the ears), hearing loss.
Status:
US Previously Marketed
Source:
TREST by NOVARTIS
(1965)
Source URL:
First approved in 1965
Source:
TREST by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Methixene is a tertiary antimuscarinic with actions similar to those of atropine; it also has antihistaminic and direct antispasmodic properties. It is used for the symptomatic treatment of parkinsonism, including the alleviation of the extrapyramidal syndrome induced by other drugs such as phenothiazines, but, like other antimuscarinics, it is of no value against tardive dyskinesias. Metixene has been discontinued. Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as metixene is considered to relate to competitive antagonism of acetylcholine at muscarinic receptors in the corpus striatum, which then restores the balance.
Status:
US Previously Marketed
Source:
MAOLATE by PAMLAB LLC
(1965)
Source URL:
First approved in 1965
Source:
MAOLATE by PAMLAB LLC
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Chlorphenesin carbamate (Maolate, Musil) is a centrally acting muscle relaxant used to treat muscle pain and spasms. Сhlorphenesin acts in the central nervous system (CNS) rather than directly on skeletal muscle. It also has antifungal and some antibacterial properties. The major adverse effects are drowsiness and dizziness.
Status:
First approved in 1965
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Tybamate is a minor tranquilizer that is chemically and pharmacologically related to meprobamate. It is useful in treating anxiety and tension associated with psychoneurotic disorders.
Status:
US Previously Marketed
Source:
PRE-SATE by PARKE DAVIS
(1965)
Source URL:
First approved in 1965
Source:
PRE-SATE by PARKE DAVIS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Chlorphentermine exerts anorectic properties. It is a synthetic amphetamine derivatc claimed to have none of the excitatory effects of the parenit substanice. PRE-SATE (Chlorphentermine HCl) is an effective appetite suppressant with a pattern of pharmacologic action substantially different from those of traditional anorexigenics. In providing dependable appetite control with appreciable loss of bodyweight, PRE-SATE does not significantly increase central nervous system (CNS), cardiorespiratory or metabolic activity.
Status:
US Previously Marketed
First approved in 1964
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Flurothyl (bis-2,2,2-trifluoroethyl ether) is a volatile convulsant acting as a GABAA antagonist that was extensively used historically to induce seizures in severely depressed patients as an alternative to electroconvulsive shock therapy. The main current use of flurothyl is in scientific research for inducing seizures in laboratory animals. Flurothyl is used to induce seizures in immature rats. Flurothyl is a potent and rapidly acting central nervous system stimulant that produces seizures within minutes of exposure. It has been previously demonstrated that flurothyl seizures during the first days and weeks of life in rats result in several morphological and behavioral changes. Mortality after acute flurothyl exposure is low.
Status:
First approved in 1963
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
CHLORAL BETAINE, a chemical complex of chloral hydrate and betaine, is a nonbarbiturate sedative and hypnotic. It is indicated for sleep induction, preoperative sedation, and daytime sedation. CHLORAL BETAINE is converted to chloral hydrate in the body and its action on the central nervous system is identical with that of chloral hydrate.
Status:
US Previously Marketed
Source:
PROKETAZINE by WYETH AYERST
(1963)
Source URL:
First approved in 1963
Source:
PROKETAZINE by WYETH AYERST
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Carfenazine (brand name Proketazine) is an antipsychotic and tranquilizer of the phenothiazine group. It is used in the treatment of acute or chronic schizophrenic reactions in hospitalized patients. Proketazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis. The following is a list of possible side effects that may occur from all constituting ingredients of Proketazine: akathisia, tardive dyskinesia, extrapyramidal symptoms, allergic purpura.
Status:
US Previously Marketed
Source:
ANHYDRON by LILLY
(1963)
Source URL:
First approved in 1963
Source:
ANHYDRON by LILLY
Source URL:
Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Conditions:
Cyclothiazide was presumably developed by Eli Lilly for the treatment of hypertension. It is believed that the drug, which belongs to the class of thiazide diuretics, exerts its action by inhibitin sodium reabsorption in the renal tubules. In 1993 it was discovered that cyclothiazide stimulates AMPA receptors thus inducing seizure behavior.