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

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Showing 241 - 250 of 256 results

Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. It acts on the renin-angiotensin system in two ways to decrease total peripheral resistance. First, it blocks the binding of angiotensin II to AT1 receptors in vascular smooth muscle, causing vascular dilatation. Second, it inhibits sympathetic norepinephrine production, further reducing blood pressure. Eprosartan is indicated for the management of hypertension alone or in combination with other classes of antihypertensive agents. Also used as a first-line agent in the treatment of diabetic nephropathy, as well as a second-line agent in the treatment of congestive heart failure (only in those intolerant of ACE inhibitors).
Status:
US Previously Marketed
First approved in 1994

Class (Stereo):
CHEMICAL (ABSOLUTE)



Spirapril (Renormax) is an ACE inhibitor antihypertensive drug used to treat hypertension. Spiraprilat, the active metabolite of spirapril, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Spiraprilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.
Status:
US Previously Marketed
Source:
PROPOXYPHENE HYDROCHLORIDE by ALRA
(1982)
Source URL:
First approved in 1957

Class (Stereo):
CHEMICAL (ABSOLUTE)



Propoxyphene is a centrally acting opiate analgesic. Propoxyphene is an odorless, freely soluble in water, white crystalline powder with a bitter taste. In vitro studies demonstrated propoxyphene and the metabolite norpropoxyphene inhibit sodium channels (local anesthetic effect) with norpropoxyphene being approximately 2 fold more potent than propoxyphene and propoxyphene approximately 10 fold more potent than lidocaine. Propoxyphene and norpropoxyphene inhibit the voltage-gated potassium current carried by cardiac rapidly activating delayed rectifier (hERG) channels with approximately equal potency. It is unclear if the effects on ion channels occur within therapeutic dose range. Propoxyphene is indicated for the relief of mild to moderate pain.
Status:
US Previously Marketed
Source:
ACETAMINOPHEN, CAFFEINE, AND DIHYDROCODEINE BITARTRATE by MIKART
(1997)
Source URL:
First approved in 1956
Source:
Rapacodin by Knoll
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Dihydrocodeine is an opioid analgesic used as an alternative or adjunct to codeine to treat moderate to severe pain, severe dyspnea, and cough. It is semi-synthetic, and was developed in Germany in 1908 during an international search to find a more effective antitussive agent to help reduce the spread of airborne infectious diseases such as tuburculosis. It was marketed in 1911. Dihydrocodeine is metabolized to dihydromorphine -- a highly active metabolite with a high affinity for mu opioid receptors. Dihydrocodeine is used for the treatment of moderate to severe pain, including post-operative and dental pain. It can also be used to treat chronic pain, breathlessness and coughing. In heroin addicts, dihydrocodeine has been used as a substitute drug, in doses up to 2500mg/day to treat addiction.
Status:
US Previously Marketed
Source:
Preludin by Geigy
(1956)
Source URL:
First approved in 1956
Source:
Preludin by Geigy
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Phenmetrazine is an anti-obesity drug, which was discovered by Boehringer-Ingelheim in 1952 and approved by FDA under the name Preludin. Later on the drug was withdrawn from the market due to the reported cases of abuse. According to some studies, misuse of phenmetrazine turned many young addicts to crime. It is suggested that the drug exerts its effect by inhibiting the monoamine transport.
Status:
US Previously Marketed
Source:
Metapin by Parke-Davis
(1947)
Source URL:
First approved in 1947
Source:
Metapin by Parke-Davis
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Metopon was developed as an analgesic opium derivative. This drug has a high affinity to the mu-opioid receptor and produces antinociception through this receptor. Metopon was available in Canada only in tablet form for oral administration; however, because of the drug addiction, the Drug Addiction Committee recommended its limited use.
Status:
US Previously Marketed
First marketed in 1929
Source:
secobarbital
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Secobarbital sodium, a barbiturate, is FDA approved for the treatment of insomnia and for pre-anesthetic use. This drug binds at a distinct 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. Adverse reactions are drowsiness, lethargy, hangover, paradoxical excitement in elderly patients, somnolence. Rifampin may decrease secobarbital levels by increasing metabolism.
Status:
US Previously Marketed
Source:
amobarbital
(1923)
Source URL:
First marketed in 1923

Class (Stereo):
CHEMICAL (ACHIRAL)



AMOBARBITAL is a barbiturate derivative with hypnotic and sedative properties. In an in vitro study in rat thalamic slices amobarbital worked by activating GABAA receptors, which decreased input resistance, depressed burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increased both the amplitude and decay time of inhibitory postsynaptic currents. Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high.
Status:
US Previously Marketed
Source:
Potassium Permanganate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Potassium Permanganate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Sodium permanganate is the inorganic compound used as oxidant and etchant in printed circuitry. Sodium permanganate is a purplish-colored, inorganic salt compound, which is primarily available in aqueous form as a monohydrate. It is miscible in water, ether, ethanol, and liquid chlorine. Sodium permanganate offers a high concentration of permanganate ions. Owing to high solubility in water, it is used for etching of plastic parts, as etching requires a high concentration of permanganate ions. Sodium permanganate is also used for water treatment and soil treatment, as it is capable of degrading phenols, BTEX, chlorinated ethenes, and PAHS and removing hydrogen sulfide.
Status:
Possibly Marketed Outside US
Source:
ZOPRANOL by Squibb Institute for Medical Research
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Zofenopril is an inhibitor of Angiotensin Converting Enzyme (ACE), which is approved in Europe for the treatment of hypertension and acute myocardial infarction.

Showing 241 - 250 of 256 results