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

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Showing 381 - 390 of 421 results

Status:
US Previously Marketed
Source:
OLEANDOMYCIN 200MG OLEANDOMYCIN PHOSPHATE by ROERIG
(1961)
Source URL:
First approved in 1956
Source:
Matromycin by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Oleandomycin is a macrolide antibiotic, which was first described under the designation P.A.105 by Sobin, English, and Celmer (1954-5). Later it appeared on the market under three names and in two forms: as pure oleandomycin ("matromycin," Pfizer; "romicil," Hoffmann-La Roche) and as a mixture with twice its weight of tetracycline ("sigmamycin," Pfizer). Oleandomycin can be employed to inhibit the activities of bacteria responsible for causing infections in the upper respiratory tract much like Erythromycin can. Both can affect staphylococcus and enterococcus genera. Oleoandomycin is reported to inhibit most gram-positive bacteria, but has only a slight inhibiting effect on gram-negative bacteria, rickettsiae, and larger viruses. The spectrum of activity on micro-organisms is therefore wider than that of penicillin and streptomycin, but narrower than that of chloramphenicol and the tetracyclines. Oleandomycin is approved as a veterinary antibiotic in some countries. It has been approved as a swine and poultry antibiotic in the United States. However, it is currently only approved in the United States for production uses. Oleandomycin is a bacteriostatic agent. Like erythromycin, oleandomycin binds to the 50s subunit of bacterial ribosomes, inhibiting the completion of proteins vital to survival and replication. It interferes with translational activity but also with 50s subunit formation. However, unlike erythromycin and its effective synthetic derivatives, it lacks a 12-hydroxyl group and a 3-methoxy group. This change in structure may adversely affect its interactions with 50S structures and explain why it is a less powerful antibiotic.
Iproniazid is a non-selective, irreversible monoamine oxidase inhibitor (MAO) of the hydrazine class. It was originally developed for the treatment of Tuberculosis, but in 1952, its antidepressant properties were discovered when researchers noted that patients given isoniazid became inappropriately happy. Iproniazid is no longer clinically prescribed and has been withdrawn due to incidences of hepatotoxicity.
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.
Status:
US Previously Marketed
Source:
CO-PYRONIL PYRROBUTAMINE PHOSPHATE by DISTA PRODUCTS
(1961)
Source URL:
First approved in 1952
Source:
Pyronil by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

PYRROBUTAMINE is a potent H1-antihistamine. H1-antihistamines interfere with the agonist action of histamine at the H1 receptor and are administered to attenuate the inflammatory process in order to treat conditions such as allergic rhinitis, allergic conjunctivitis, and urticaria.
Status:
US Previously Marketed
Source:
Paveril Phosphate by Lilly
(1951)
Source URL:
First approved in 1951
Source:
Paveril Phosphate by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Dimoxyline is the synthetic analogue of papaverine, Acute toxicity studies show it to be less toxic than papaverine. No analgesic action and no tolerance development in experimental animals by repeated administration. But Dimoxyline does not appear to be as potent as papaverine in comparable dosage. Dimoxyline is indicated for the treatment of patients with angina pectoris. Also, significant amount of benefit was claimed in patients with acute or chronic phlebitis, arterial thrombosis or embolism, Raynaud’s phenomena and early thromboangiitis obliterans or arteriosclerosis obliterans. Detected adverse events are: nausea or abdominal cramps.
Status:
US Previously Marketed
First approved in 1950
Source:
PIG SWIGFOR SWINE AND POULTRY by LeGear Animal Health
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Piperazine, a six membered nitrogen containing heterocycle, is of great significance to the rational design of drugs. This moiety can be found in a plethora of well-known drugs with various therapeutic uses, such as antipsychotic, antihistamine, antianginal, antidepressant, anticancer, antiviral, cardio protectors, anti-inflammatory, and imaging agents. Slight modification to the substitution pattern on the piperazine nucleus facilitates a recognizable difference in the medicinal potential of the resultant molecules. Piperazine has been used as an antihelmintic drug. Piperazine works by paralyzing the worms. They are then passed in the stool.
Status:
US Previously Marketed
Source:
My-B-Den by Bischoff (Dome)
(1949)
Source URL:
First approved in 1949
Source:
My-B-Den by Bischoff (Dome)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Adenosine monophosphate (AMP) is a nucleotide, consisting of a phosphate group, the sugar ribose, and the nucleobase adenine. AMP is an activator of several enzymes in the tissues. In the glycolytic pathway, the enzyme phosphofructokinase is inhibited by ATP but the inhibition is reversed by AMP, the deciding factor for the reaction being the ratio between ATP and AMP. In medicine, AMP is used mainly as an alternative to adenosine for treatment of ischemia and as a tool compound to measure hyperresponsiveness of airways.
Status:
US Previously Marketed
Source:
My-B-Den by Bischoff (Dome)
(1949)
Source URL:
First approved in 1949
Source:
My-B-Den by Bischoff (Dome)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Adenosine monophosphate (AMP) is a nucleotide, consisting of a phosphate group, the sugar ribose, and the nucleobase adenine. AMP is an activator of several enzymes in the tissues. In the glycolytic pathway, the enzyme phosphofructokinase is inhibited by ATP but the inhibition is reversed by AMP, the deciding factor for the reaction being the ratio between ATP and AMP. In medicine, AMP is used mainly as an alternative to adenosine for treatment of ischemia and as a tool compound to measure hyperresponsiveness of airways.
Status:
US Previously Marketed
First approved in 1948
Source:
Antistine Phosphate by Ciba
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Antazoline is an antagonist of histamine H1 receptors. It selectively bind to but does not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Antazoline in combination with naphazoline (VASOCON-A®) is indicated to relieve the symptoms of allergic conjunctivitis.
Status:
US Previously Marketed
Source:
Oralator by Smith Kline & French
(1946)
Source URL:
First approved in 1946
Source:
Oralator by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Octodrine is a stimulant that is structurally similar to amphetamine and is included in several so-called “pre-workout” and “fat-burning” supplements. Octodrine, has a history of use as a pharmaceutical drug. It was originally developed in the United States as an aerosolized treatment for bronchitis, laryngitis and other conditions Initially approved by the FDA in 1946 as Eskay’s Oralator, this inhaler appeared only in the 1949 edition of the Physicians’ Desk Reference. Octodrine was combined with several other medications, including theophylline, 3-octopamine, and adenosine, in multi-ingredient tablets sold between the early 1960s through the mid-2000s under the trade names Ambredin, Ordinal, Ordinal Retard and Ordinal Forte. Some proponents say octodrine is a safer alternative to other stimulants like ephedra and Dimethylamylamine (DMAA), but there is no scientific information to support this claim. Originally developed in the early 1950’s as a remedy to nasal congestion and as a possible anti-tumor drug, Octodrine has resurfaced as a key ingredient in dietary supplements for its stimulant and thermogenic benefits.

Showing 381 - 390 of 421 results