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

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Showing 61 - 70 of 557 results

Status:
First marketed in 1827

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Morphine is one of the most important and widely used opioid for the treatment of chronic and acute pain: the very wide interindividual variability in the patients’ response to the drug may have genetic derivations. Sulphate salt of morphine sold under the many brand names, one of them, DURAMORPH, which is indicated for the management of pain severe enough to require use of an opioid analgesic by intravenous administration, and for which alternative treatments are not expected to be adequate. In addition for the epidural or intrathecal management of pain without attendant loss of motor, sensory, or sympathetic function. Morphine is a full opioid agonist and is relatively selective for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. The principal therapeutic action of morphine is analgesia. Like all full opioid agonists, there is no ceiling effect for analgesia with morphine. The precise mechanism of the analgesic action is unknown. However, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug. Morphine has a high potential for addiction and abuse. Common side effects include drowsiness, vomiting, and constipation. Caution is advised when used during pregnancy or breast-feeding, as morphine will affect the baby.
Status:
US Approved OTC
Source:
21 CFR 341.20(b)(1) cough/cold:nasal decongestant levmetamfetamine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Levomethamphetamine is the levorotary (L-enantiomer) form of methamphetamine. Levomethamphetamine is a sympathomimetic vasoconstrictor which is the active ingredient in some over-the-counter (OTC) nasal decongestant inhalers in the United States. Levomethamphetamine crosses the blood-brain-barrier and acts as a TAAR1 agonist, functioning as a selective norepinephrine releasing agent (with few or no effects on the release of dopamine), so it affects the central nervous system, although its effects are qualitatively distinct relative to those of dextromethamphetamine. Levomethamphetamine does not possess the potential for euphoria or addiction that dextromethamphetamine possesses. Among its physiological effects are the vasoconstriction that makes it useful for nasal decongestion. The elimination half-life of levomethamphetamine is between 13.3 and 15 hours, whereas dextromethamphetamine has a half-life of about 10.5 hours. When the nasal decongestant is taken in excess, levomethamphetamine has potential side effects resembling those of other sympathomimetic drugs; these effects include hypertension (elevated blood pressure), tachycardia (rapid heart rate), nausea, stomach cramps, dizziness, headache, sweating, muscle tension, and tremors. Central side effects may include anxiety, insomnia, and anorexia
Status:
US Approved OTC
Source:
21 CFR 341.20(b)(9) cough/cold:nasal decongestant propylhexedrine
Source URL:
First approved in 1949
Source:
Benzedrex by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Propylhexedrine is considered to be an agonist of alpha-adrenergic receptors. It is effective as a topical vasoconstrictor. The primary medicinal use of Benzedrex (Propylhexedrine inhaler) propylhexedrine is temporary symptomatic relief of nasal decongestion due to colds, allergies and allergic rhinitis. Structurally and pharmacologically related to amphetamine.Exact mechanism of action unknown but thought to be similar to amphetamine. When used as a nasal inhaler for this indication, propylhexedrine reduces nasal airway resistance without producing rebound congestion. Abuse does not occur by nasal inhalation; however, a small amount of abuse of the propylhexedrine containing nasal inhalers occurs by oral ingestion of the contents of the inhaler or by intravenous injection. Propylhexedrine is a central nervous system (CNS) stimulant of low abuse potential, a stimulant of low preference for stimulant abusers compared with amphetamine, methylphenidate, phenmetrazine.
Status:
US Approved OTC
Source:
21 CFR 341.14(a)(2)(ii) cough/cold:antitussive codeine phosphate
Source URL:
First marketed in 1921
Source:
Codeine Sulphate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Codeine is an opiate used to manage mild to moderate pain severe enough to require an opioid. Codeine is a selective agonist for the mu opioid receptor and has an affinity to delta and kappa-opioid receptors. In some countries, this drug is regulated under various narcotic control laws, because its chronic use can cause physical dependence. In others, it is available without a medical prescription in combination with paracetamol.
Status:
Investigational
Source:
INN:isomethadone [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

ISOMETHADONE HYDROBROMIDE, DL- is a hydrobromide salt of isomethadone, a synthetic opioid analgesic. This is a controlled substance in the US.
Status:
Investigational
Source:
INN:betacetylmethadol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Betacetylmethadol is a synthetic narcotic analgesic under international control according to the UN Single Convention 1961.
Status:
Investigational
Source:
INN:mesocarb [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Mesocarb (sydnocarb or 3-(beta-phenylisopropyl)-N-phenylcarbamoylsydnonimine) is a psychomotor stimulant N-alkylated amphetamine derivative. Mesocarb is a selective inhibitor of dopamine uptake, it potently blocks dopamine transporter. It is very likely that mesocarb is being used by drug addicts. Mesocarb is included in the World Anti-Doping Agency’s list of substances and methods that are prohibited in sports. It is used in Russia for the treatment of a variety of neuropsychiatric comorbidities.
Status:
Investigational
Source:
INN:furethidine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Furethidine, a pethidine analog was studied as an analgesic agent. This compound is not currently used in medicine and is listed in schedules of the single convention on narcotic drugs of 1961 as amended by the 1972 protocol.
Status:
Investigational
Source:
INN:cathinone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Cathinone is one of the biologically active alkaloids found in the khat shrub (Catha edulis). Due to its psychoactive properties, khat has been known and utilized for ages by the inhabitants of East Africa and the northeastern parts of Arabian Peninsula. In many regions, chewing of freshly collected khat leaves (thus liberating cathinone, which affects the central nervous system) is considered a matter of culture and local tradition. Because of their structural similarity to amphetamine, cathinone and its analogs are often denoted as “natural amphetamines”, and the only structural difference between amphetamine and cathinone is the presence of a carbonyl group in the α-position of cathinone’s side chain. Similar to amphetamine, cathinone and its analogs are characterized by stimulating, euphoric, and empathogenic properties. Due to their effects on the central nervous system, the first synthetic cathinone derivatives were synthesized for medicinal purposes in the early twentieth century, but they began attracting wider attention around the year 2000. At that time, synthetic cathinones were included in a broader group of psychoactive compounds denoted as “legal drugs” or “designer drugs”
Status:
Investigational
Source:
INN:methyldesorphine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Methyldesorphine is a synthetic narcotic analgesic derived from morphine. It has no medicinal value in the US. This compound is listed as a Schedule I Narcotic controlled substance under the Controlled Substances Act 1970.