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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.
Status:
US Previously Marketed
Source:
EUTONYL by ABBOTT
(1963)
Source URL:
First approved in 1963
Source:
EUTONYL by ABBOTT
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Pargyline is an irreversible selective monoamine oxidase (MAO)-B inhibitor, which possesses higher selectivity to this isoform in comparison with MAO-A. It was approved under brand name eutonyl for the treatment hypertension, but then this drug was discontinued.
Status:
US Previously Marketed
Source:
HYDROMOX by LEDERLE
(1963)
Source URL:
First approved in 1963
Source:
HYDROMOX by LEDERLE
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Quinethazone (brand name Hydromox) is a thiazide diuretic used to treat hypertension. The antihypertensive mechanism of quinethazone is less well understood. This drug was discovered in a period when only isoform carbonic anhydrases (CAs) II was known and considered physiologically/pharmacologically relevant. Recently was studied that quinethazone considerably inhibit other isozymes known nowadays to be involved in critical physiologic processes. Thiazides like quinethazone also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. Common side effects include dizziness, dry mouth, nausea, and low potassium levels. Thiazides may increase the toxicity of allopurinol, anesthetics, antineoplastic, calcium salts, diazoxide, digitalis, lithium; loop diuretics, methyldopa, nondepolarizing muscle relaxants, vitamin D; amphotericin B and anticholinergics may increase the toxicity of thiazides.
Status:
US Previously Marketed
Source:
SULFABID by PHARM RES ASSOC
(1977)
Source URL:
First approved in 1963
Source:
SULFABID by PURDUE FREDERICK
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Sulfaphenazole is an oral antibiotic, which was used for the treatment of bacterial infections under the name Sulfabid. The drug was found to block folate synthesis in bacterias by inhibiting the enzyme dihydropteroate synthase. Sulfaphenazole is also known to inhibit CYP2C9 with high potency and specificity. Sulfabid is no longer marketed in the USA.
Status:
US Previously Marketed
First approved in 1963
Class (Stereo):
CHEMICAL (ACHIRAL)
Dicobalt edetate was developed as a cyanide antidote based on the known ability of cobalt to form stable complexes with cyanide. One current cobalt-based antidote available in Europe is dicobalt-EDTA, sold as Kelocyanor. This agent chelates cyanide as the cobalticyanide. This drug provides an antidote effect more quickly than formation of methemoglobin. It can be very toxic and cause seizures, upper airway oedema, chest pain, hypotension, vomiting, rashes and dyspnoea especially in those who have not be exposed to cyanide.
Status:
US Previously Marketed
Source:
STOXIL by GLAXOSMITHKLINE
(1967)
Source URL:
First approved in 1963
Source:
DENDRID by ALCON
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Idoxuridine is an antiviral agent use in keratitis caused by herpes simplex virus. As a prescription drug it comes as a 0.1% ophthalmic solution/drops (Herplex and Dendrid). The first studies of the compound for treatment of human herpes simplex started in early 1960s. Being a structural analog of thymidine idoxuridine inhibits viral DNA replication by substituting thymidine. The effect of idoxuridine results in the inability of the virus to reproduce and/or infect tissues. Idoxuridine also blocks viral thymidine kinase as its substrate analog.
Status:
US Previously Marketed
Source:
GYNOREST by SOLVAY
(1968)
Source URL:
First approved in 1963
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Dydrogesterone is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus. At therapeutic levels, dydrogesterone has no contraceptive effect as it does not inhibit or interfere with ovulation or the corpus luteum. Furthermore, dydrogesterone is non-androgenic, non-estrogenic, non-corticoid, non-anabolic and is not excreted as pregnanediol. Dydrogesterone helps to regulate the healthy growth and normal shedding of the uterus lining. Therefore, it may be useful in the treatment of menstrual disorders such as absent, irregular or painful menstrual periods, infertility, premenstrual syndrome and endometriosis. Dydrogesterone works by regulating the healthy growth and normal shedding of the womb lining by acting on progesterone receptors in the uterus. Used to treat irregular duration of cycles and irregular occurrence and duration of periods caused by progesterone deficiency. Also used to prevent natural abortion in patients who have a history of habitual abortions. Dydrogesterone was first introduced to the market in 1961, and is currently approved in over 100 countries world-wide. Banned in the USA and wthdrawn from the UK, but still used in other countries.
Status:
US Previously Marketed
Source:
TARACTAN by ROCHE
(1962)
Source URL:
First approved in 1962
Source:
TARACTAN by ROCHE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Chlorprothixene (Taractan, Tarasan, Truxal) is a thioxanthine derivative developed by Lundbeck for the treatment of psychotic disorders. The drug exerts its activity by binding to and inhibiting serotonin receptors, dopamine receptors, muscarinic acetylcholine receptor, histamine H1 receptor and alpha1-adrenergic receptor.
Status:
US Previously Marketed
Source:
SANSERT by NOVARTIS
(1962)
Source URL:
First approved in 1962
Source:
SANSERT by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Methysergide is an oral, synthetic ergot alkaloid, structurally related to the oxytocic agent methylergonovine and to the potent hallucinogen LSD. Methysergide is used prophylactically to reduce the frequency and intensity of severe vascular headaches. Although methysergide is an ergot alkaloid, it is a weak vasoconstrictor and oxytocic. Methysergide is a more potent antagonist of peripheral serotonin receptors than other ergot alkaloids. Methysergide is not just a 5HT2 antagonist, it is also a 5HT1 agonist. Although methysergide and sumatriptan both stimulate serotonin receptors centrally, methysergide is intended for prophylaxis while sumatriptan is indicated for treatment of an acute attack. Methysergide was approved by the FDA in 1962. Methysergide was formerly used for prophylaxis of cluster headaches/migraine headaches, but is no longer recommended due to retroperitoneal/retropulmonary fibrosis.