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

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Showing 421 - 430 of 612 results

Status:
US Previously Marketed
Source:
Dromoran by Hoffmann-La Roche
(1953)
Source URL:
First approved in 1953
Source:
Dromoran by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Racemorphan is racemic mixture of an antitussive and dissociative hallucinogen Dextrorphan and an opioid analgesic Levorphanol. Racemorphan itself is under international control per the Single Convention on Narcotic Drugs 1961 and is therefore listed as a Schedule II Narcotic controlled substance.
Status:
US Previously Marketed
Source:
Nalline HCl by Merck Sharp & Dohme
(1952)
Source URL:
First approved in 1952
Source:
Nalline HCl by Merck Sharp & Dohme
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Nalorphine has a mixed opioid agonist-antagonist properties. Nalorphine inhibits the cholinesterases of mouse brain, bovine erythrocytes and horse serum. It acts on mu-, k- and sigma-opioid receptors. Nalorfin by virtue of the agonistic effect has an analgesic effect but to a much lesser extent than morphine. Initially, before the appearance of a "pure" morphine-naloxone antagonist, nalorphine was used as an antidote for severe respiratory depression and other body function disorders caused by acute poisoning in case of an overdose of morphine, promedol, fentanyl or other narcotic analgesics, or with increased sensitivity to them. At present, nalorphine is practically not used for this purpose. It was replaced by naloxone. Large doses of nalorphine can cause nausea, cramps, drowsiness, headache, mental stimulation.
Status:
US Previously Marketed
Source:
Stenediol by Organon
(1951)
Source URL:
First approved in 1951
Source:
Stenediol by Organon
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Methandriol is an anabolic steroid. Methandriol is classified as a weak anabolic with weak androgenic properties. Methandriol displays some level of estrogenic activity, making this steroid less useful for dieting. The drug is generally considered too mild and is not widely popular among bodybuilders and athletes. It seems most prominent in Australia now, where it remains included in a number of veterinary anabolic steroid products.
Status:
US Previously Marketed
Source:
Nisentil by Hoffmann-La Roche
(1949)
Source URL:
First approved in 1949
Source:
Nisentil by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

ALPHAPRODINE is an opioid analgesic. It was used in obstetrics, as pre-operative medication, and for minor surgical procedures. In addition, this drug was used in the dentistry setting to help effectively manage pain associated with dental procedures.
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
Source:
DELVINAL by MSD
(1961)
Source URL:
First approved in 1940
Source:
Delvinal by Sharp & Dohme (MSD)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

VINBARBITAL, a barbiturate derivative, is a hypnotic drug. Also, it was used for analgesia and anesthesia in obstetrics.
Status:
US Previously Marketed
Source:
BUTABARBITAL SODIUM by WHITEWORTH TOWN PLSN
(1974)
Source URL:
First approved in 1939

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Barbiturates are non-selective depressants of the central nervous system. Butabarbital is one of them, which is used under brand name butisol sodium as a sedative or hypnotic. Like other barbiturates, butabarbital is capable of producing all levels of CNS mood alteration from excitation to mild sedation, to hypnosis, and deep coma. The mechanism of action by which barbiturates exert their effect is not yet completely understood, but is assumed, that butabarbital binds at a distinct binding 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.
Status:
US Previously Marketed
First marketed in 1934

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Sodium thiopental (also known as Sodium Pentothal, thiopental) was discovered in 1930s by investigators working for Abbott Laboratories. Thiopental sodium was used for the induction of general anesthesia and is used as an adjunct to provide hypnosis during balanced anesthesia with other anesthetic agents, including analgesics and muscle relaxants. Thiopental sodium was also used as an adjunct for control of convulsive disorders of various etiology, including those caused by local anesthetics. Finally, thiopental sodium had been used to reduce the intracranial pressure in patients with increased intracranial pressure, if controlled ventilation is provided. Nevertheless, these prescriptions of drug were discontinued. In addition, this drug was banned for use in US executions. Thiopental sodium acts through the CNS with particular activity in the mesencephalic reticular activating system. It was shown, that mechanism of action of sodium thiopental via GABAA receptor. Thiopental binds at a distinct binding 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.
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.

Showing 421 - 430 of 612 results