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

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Showing 11 - 20 of 102 results

Desipramine is a tricyclic antidepressant that was approved by the FDA in 1964. It was derived from imipramine, which was the first tricyclic antidepressant to be manufactured. Desipramine is one of many tricyclic antidepressants, and this type of antidepressant gets its name due to its three-ring chemical structure. Desipramine, a secondary amine tricyclic antidepressant, is structurally related to both the skeletal muscle relaxant cyclobenzaprine and the thioxanthene antipsychotics such as thiothixene. It is the active metabolite of imipramine, a tertiary amine TCA. The acute effects of desipramine include inhibition of noradrenaline re-uptake at noradrenergic nerve endings and inhibition of serotonin (5-hydroxy tryptamine, 5HT) re-uptake at the serotoninergic nerve endings in the central nervous system. Desipramine exhibits greater noradrenergic re-uptake inhibition compared to the tertiary amine TCA imipramine. In addition to inhibiting neurotransmitter re-uptake, desipramine down-regulates beta-adrenergic receptors in the cerebral cortex and sensitizes serotonergic receptors with chronic use. The overall effect is increased serotonergic transmission. Antidepressant effects are typically observed 2 - 4 weeks following the onset of therapy though some patients may require up to 8 weeks of therapy prior to symptom improvement. Patients experiencing more severe depressive episodes may respond quicker than those with mild depressive symptoms. Desipramine is marketed under the trade name Norpramin, indicated for the treatment of depression.
Lincomycin (LINCOCIN®) is an antibiotic produced by Streptomyces lincolnensis (Streptomycetaceae family). It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections. Lincomycin (LINCOCIN®) inhibits protein synthesis in susceptible bacteria by binding to the 50S subunits of bacterial ribosomes and preventing peptide bond formation upon transcription. It is usually considered bacteriostatic, but may be bactericidal in high concentrations or when used against highly susceptible microorganisms.
Status:
US Approved OTC
Source:
21 CFR 341.20(b)(7) cough/cold:nasal decongestant oxymetazoline hydrochloride
Source URL:
First approved in 1964
Source:
Afrin by Schering
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Oxymetazoline is an adrenergic alpha-agonist, direct acting sympathomimetic, used as a vasoconstrictor to relieve nasal congestion The sympathomimetic action of oxymetazoline constricts the smaller arterioles of the nasal passages, producing a prolonged (up to 12 hours), gentle and decongesting effect. Oxymetazoline elicits relief of conjunctival hyperemia by causing vasoconstriction of superficial conjunctival blood vessels. The drug's action has been demonstrated in acute allergic conjunctivitis and in chemical (chloride) conjunctivitis. Oxymetazoline is self-medication for temporary relief of nasal congestion associated with the common cold, hay fever, or other upper respiratory allergies. Oxymetazoline is available over-the-counter as a topical decongestant in the form of oxymetazoline hydrochloride in nasal sprays such as Afrin, Operil, Dristan, Dimetapp, oxyspray, Facimin, Nasivin, Nostrilla, Sudafed OM, Vicks Sinex, Zicam, SinuFrin, and Mucinex Full Force. Due to its vasoconstricting properties, oxymetazoline is also used to treat nose bleeds and eye redness.
Status:
US Previously Marketed
First approved in 1964

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
US Previously Marketed
Source:
NALIDIXIC ACID by SUN PHARM INDUSTRIES
(1986)
Source URL:
First approved in 1964

Class (Stereo):
CHEMICAL (ACHIRAL)



Nalidixic acid is a quinolone antibacterial indicated for the treatment of urinary tract infections. Nalidixic acid has marked antibacterial activity against gram-negative bacteria including Enterobacter species, Escherichia coli, Morganella Morganii; Proteus Mirabilis, Proteus vulgaris, and Providencia rettgeri. Pseudomonas species are generally resistant to the drug. It is suggested that nalidixic acid acts by inhibiting bacterial DNA gyrase.
Status:
US Previously Marketed
First approved in 1964

Class (Stereo):
CHEMICAL (ACHIRAL)


Lapyrium, or lapirium, as the chloride salt lapirium chloride (INN) or lapyrium chloride (USAN), is a cationic surfactant that is used in cosmetic personal care products as a biocide and antistatic agent. A 50% solution of Lapyrium Chloride produced slight to moderate erythema. Lapyrium is also used in waste-water treatment and corrosion inhibition formulations.
Status:
US Previously Marketed
First approved in 1964

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Conditions:

Trioxsalen (trimethylpsoralen, trioxysalen or trisoralen) is a furanocoumarin and a psoralen derivative. It is obtained from several plants, mainly Psoralea corylifolia. Like other psoralens it causes photosensitization of the skin. It is administered either topically or orally in conjunction with UV-A (the least damaging form of ultraviolet light) for phototherapy treatment of vitiligo1 and hand eczema.2 After photoactivation it creates interstrand cross-links in DNA, which can cause programmed cell death unless repaired by cellular mechanisms. In research it can be conjugated to dyes for confocal microscopy and used to visualize sites of DNA damage.3 The compound is also being explored for development of antisense oligonucleotides that can be cross-linked specifically to a mutant mRNA sequence without affecting normal transcripts differing at even a single base pair.Trioxsalen was discontinued by the manufacturer in December 2002.
Status:
US Previously Marketed
First approved in 1964

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ethylestrenol (INN, USAN, BAN) (brand names Maxibolin, Orabolin), or ethylnandrol (JAN), also known as 17α-ethyl ester-4-en-17β-ol or as 3-deketo-17α-ethyl-19-nortestosterone, is an anabolic-androgenic steroid (AAS) with some progestogenic activity, and low androgenic activity. It is a 17α-ethylated derivative of nandrolone and lacks the 3-keto group. It was described in the literature in 1959 and approved in 1964 for testosterone deficiency in male patients.
Status:
US Previously Marketed
Source:
Uval by Stuart
(1964)
Source URL:
First approved in 1964
Source:
Uval by Stuart
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Sulisobenzone (benzophenone-4) is an ingredient for use in sunscreens which protects the skin from damage by UVB and short-wave UVA ultraviolet light. The Food and Drug Administration (FDA) has approved the use of Benzophenone-4 as safe and effective, over-the-counter (OTC) sunscreen ingredient. Sulisobenzone is a subject to the FDA 2011 sunscreen final rule: it can be marketed without approved drug applications (without NDAs or ANDAs), must bear the statement of identity “sunscreen" and contain the information about SPF test. However it is said to be widely used in cosmetic products not labeled as sunscreens such as creams, moisturizers, shampoos and other hair care products, nail polish, lipsticks and lip balms. Sulisobenzone may cause contact dermatitis when used in cosmetics and toiletries. Benzophenone 4 is tested as 10%. It was reported that 10% sulisobenzone enhance skin penetration of the moderately lipophilic herbicide 2,4-D.
Status:
US Previously Marketed
Source:
Indoklon by Ohio Medical Products
(1964)
Source URL:
First approved in 1964
Source:
Indoklon by Ohio Medical Products
Source URL:

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.

Showing 11 - 20 of 102 results