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

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Showing 221 - 230 of 2752 results

Status:
US Approved OTC
Source:
21 CFR 341.14(a)(3) cough/cold:antitussive dextromethorphan
Source URL:
First approved in 1954
Source:
Romilar by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dextromethorphan is a non-narcotic morphine derivative widely used as an antitussive for almost 40 years. It has attracted attention due to its anticonvulsant and neuroprotective properties. It is a cough suppressant in many over-the-counter cold and cough medicines. In 2010, the FDA approved the combination product dextromethorphan/quinidine for the treatment of pseudobulbar affect. Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Dextromethorphan shows high-affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist and acts as a non-competitive channel blocker. It is one of the widely used antitussives and is used to study the involvement of glutamate receptors in neurotoxicity. Dextromethorphan (DM) is a sigma-1 receptor agonist and an uncompetitive NMDA receptor antagonist. The mechanism by which dextromethorphan exerts therapeutic effects in patients with pseudobulbar affect is unknown. Dextromethorphan should not be taken with monoamine oxidase inhibitors due to the potential for serotonin syndrome. Dextromethorphan is extensively metabolized by CYP2D6 to dextrorphan, which is rapidly glucuronidated and unable to cross the blood-brain barrier.
Status:
US Approved OTC
Source:
21 CFR 336.10(d) antiemetic meclizine hydrochloride
Source URL:
First approved in 1954
Source:
Bonine by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Meclizine, a piperazine-derivative H1-receptor antagonist similar to buclizine, cyclizine, and hydroxyzine, is used as an antivertigo/antiemetic agent. Meclizine is used in the management of nausea, vomiting, and dizziness associated with motion sickness and vertigo in diseases affecting the vestibular apparatus. Along with its actions as an antagonist at H1-receptors, meclizine also possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Meclizine depresses labyrinth excitability and vestibular stimulation and may affect the medullary chemoreceptor trigger zone. It is sold under the brand names Bonine, Bonamine, Antivert, Postafen, Sea Legs, and Dramamine II.
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 341.20(b)(6) cough/cold:nasal decongestant naphazoline hydrochloride
Source URL:
First approved in 1942
Source:
Privine HCl by Ciba
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Naphazoline is a direct acting sympathomimetic adrenergic alpha-agonist used to induce systemic vasoconstriction, thereby decreasing nasal congestion and inducing constriction around the conjunctiva. The sympathomimetic action of Naphazoline constricts the smaller arterioles of the nasal passages, producing a decongesting effect. Naphazoline ophthalmic causes constriction of blood vessels in the eyes. It also decreases itching and irritation of the eyes. aphazoline constricts the vascular system of the conjunctiva. It is presumed that this effect is due to direct stimulation action of the drug upon the alpha adrenergic receptors in the arterioles of the conjunctiva resulting in decreased conjunctival congestion. Naphazoline belongs to the imidazoline class of sympathomimetics. Naphazoline is a direct acting sympathomimetic drug, which acts on alpha-adrenergic receptors in the arterioles of the nasal mucosa. This activates the adrenal system to yield systemic vasoconstrction. In producing vasoconstriction, the result is a decrease in blood flow in the nasal passages and consequently decreased nasal congestion. The vasoconstriction means that there is less pressure in the capillaries and less water can filter out, thus less discharge is made. Naphazoline is primarily indicated in conditions like Corneal vascularity, Hyperaemia, Itching, Nasal congestion, and can also be given in adjunctive therapy as an alternative drug of choice in Sinusitis.
Berefrine (also known as phenylephrine oxazolidine), a prodrug of phenylephrine, is a mydriatic agent. Berefrine was developed for improving ocular absorption and reducing systemic side effects.
Ephedrine (l-form) is an alkaloid, which was initially purified from Ephedra plant. The extract form Ephedra has been used in China for medicinal purposes for several thousand years. Ephedrine acts as an agonist at alpha- and beta-adrenergic receptors and indirectly causes the release of norepinephrine from sympathetic neurons. The drug crosses the blood brain barrier and stimulates the central nervous system. Ephedrine products are now banned in many countries, as they are a major source for the production of the addictive compound methamphetamine. FDA has approved ephedrine only for the treatment of clinically important hypotension occurring in the setting of anesthesia.
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:
US Approved OTC
Source:
21 CFR 344.1 otic:earwax removal aid carbamide peroxide 6.5% (in anhydrous glycerin)
Source URL:
First marketed in 1921
Source:
Hydrogen Peroxide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Hydrogen peroxide has been used in medicine for more than 100 years. It is known in surgery as a highly useful irrigation solution by virtue of both its hemostatic and its antimicrobial effects. Hydrogen peroxide is a mild antiseptic used on the skin to prevent infection of minor cuts, scrapes, and burns. It may also be used as a mouth rinse to help remove mucus or to relieve minor mouth irritation (e.g., due to canker/cold sores, gingivitis). This product works by releasing oxygen when it is applied to the affected area. The release of oxygen causes foaming, which helps to remove dead skin and clean the area. Hydrogen peroxide is a strong oxidizing agent used in aqueous solution as a ripening agent, bleach, and topical anti-infective. It is relatively unstable and solutions deteriorate over time unless stabilized by the addition of acetanilide or similar organic materials.
Glycine (Cly) is a natural amino acid neurotransmitter that acts as a co-agonist at Glutamate [NMDA] receptors in the brain and is an activator of glycine receptors, GLRA1-3, GLRB. The abnormal Gly levels have been implicated in neuropsychiatric disorders. Alterations in Gly levels are implicated in several diseases of the central nervous system. Glycine was studied in phase II of clinical trials in patients with schizophrenia. The results have shown that using of glycine was associated with reduced symptoms with promising effect sizes and a possibility of improvement in cognitive function. Besides, glycine was also studied in clinical trials phase II in children with cystic fibrosis. The clinical, spirometric and inflammatory status of subjects with cystic fibrosis improved after just 8 weeks of glycine intake, suggesting that this amino acid might constitute a novel therapeutic tool for these patients. In addition, Gly was proposed as a biomarker for brain tumor malignancy. Glycine is a component of a nutrients mixture for peripheral administration to well-nourished mildly catabolic adult patients who require only short-term parenteral nutrition.
Status:
US Approved OTC
Source:
21 CFR 346.16(a) anorectal:analgesic, anesthetic, antipruritic camphor
Source URL:
First marketed in 1921

Class (Stereo):
CHEMICAL (ABSOLUTE)



Camphor is a bicyclic monoterpene ketone found widely in plants, especially cinnamomum camphora. Topically, camphor is used to relieve pain. It has been used to treat warts, cold sores, hemorrhoids, and osteoarthritis. It has also been applied topically as an analgesic and an antipruritic. It has been used as a counterirritant, and to increase local blood flow. Camphor has frequently been used topically to treat respiratory tract diseases involving mucous membrane inflammation. It is sometimes used topically to treat cardiac symptoms. Camphor is also used topically as an eardrop, and for treating minor burns. In inhalation therapy, camphor is used as an antitussive. Orally, camphor is used as an expectorant, antiflatulent, and for treating respiratory tract diseases. Today, most camphor is synthetic. It is approved by the FDA as a topical antitussive. Camphor is produced synthetically from the oil of turpentine. It has been used for centuries for its medicinal features, in religious rituals, and in cooking. It is no longer used as pesticide. In 1982, the US Food and Drug Administration restricted commercial products intended for medicinal use to contain <11% camphor.