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

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Showing 331 - 340 of 4002 results

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 341.12(b) cough/cold:antihistamine chlorcyclizine hydrochloride
Source URL:
First approved in 1949
Source:
Perazil by Burroughs Wellcome
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Chlorcyclizine is a first generation phenylpiperazine class antihistamine used to treat urticaria, rhinitis, pruritus, and other allergy symptoms. Chlorcyclizine also has some local anesthetic, anticholinergic, and antiserotonergic properties, and can be used as an antiemetic. Chlorcyclizine temporarily relieves the symptoms due to hay fever or other upper respiratory allergies. It has also being shown to possess in vitro and in vivo activity against hepatitis C virus.
Status:
US Approved OTC
Source:
21 CFR 341.12(j) cough/cold:antihistamine pheniramine maleate
Source URL:
First approved in 1948
Source:
Trimeton by Schering
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Pheniramine is an antihistamine used to treat allergic conditions such as hay fever or urticaria. It is generally sold in combination with other medications, rather than as a stand-alone drug. Allergies are caused by an excessive type 1 hypersensitivity response of the body to allergens, mediated by inappropriate histamine signalling. By inhibiting the binding of histamine, antihistamines decrease the normal histamine response from cells, consequently decreasing allergic symptoms. Antihistamines such as pheniramine appear to compete with histamine for histamine H1- receptor sites on effector cells. The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release. Antihistamines suppress the histamine-induced wheal (swelling) and flare (vasodilation) response by blocking the binding of histamine to its receptors on nerves, vascular smooth muscle, glandular cells, endothelium, and mast cells. They effectively exert competitive antagonism of histamine for H1-receptors. Pheniramine is marketed under the trade name Avil and Visine-A among others).
Status:
US Approved OTC
Source:
21 CFR 341.12(k) cough/cold:antihistamine pyrilamine maleate
Source URL:
First approved in 1948
Source:
Neo-Antergan by Merck
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pyrilamine (also known as Mepyramine) is a first generation antihistamine, targeting the H1 receptor. However, it rapidly permeates the brain and so often causes drowsiness as a side effect. It is used in over-the-counter combination products for colds and menstrual symptoms. Mepyramine is a histamine H1 receptor inverse agonist. It binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. Mepyramine competes with histamine for binding at H1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The sedative properties of Mepyramine occur at the subcortical level of the CNS. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
Status:
US Approved OTC
Source:
21 CFR 333.110(c) first aid antibiotic:ointment chlortetracycline hydrochloride
Source URL:
First approved in 1948
Source:
Aureomycin Calcium by Lederle
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Chlortetracycline (trade name Aureomycin, Lederle) is a tetracycline antibiotic, the first tetracycline to be identified. It was discovered in 1945 by Benjamin Minge Duggar working at Lederle Laboratories under the supervision of Yellapragada Subbarow. Duggar identified the antibiotic as the product of an actinomycete he cultured from a soil sample collected from Sanborn Field at the University of Missouri. The organism was named Streptomyces aureofaciens and the isolated drug, Aureomycin, because of their golden color. Chlortetracycline inhibits cell growth by inhibiting translation. It binds to the 16S part of the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. In veterinary medicine, chlortetracycline is commonly used to treat conjunctivitis in cats.
Status:
US Approved OTC
Source:
21 CFR 341.12(i) cough/cold:antihistamine phenindamine tartrate
Source URL:
First approved in 1947
Source:
Thephorin by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Phenindamine (thephorin or 2-methyl-9-phenyl-2,3,4,9-tetrahydro-1-pyridindene) a pyridindene derivative proved to be a potent antihistaminic. Phenindamine was used to treat sneezing; runny nose; itching, watery eyes; hives; rashes; itching; and other symptoms of allergies and the common cold.
Diphenhydramine is an antihistamine which is used in the combination with naproxen sodium for the relief of occasional sleeplessness when associated with minor aches and pains. Diphenhydramine has a role nighttime sleep-aid and naproxen sodium is a pain reliever. In addition, diphenhydramine used in relieving symptoms in patients with moderate-to-severe seasonal allergic rhinitis. Diphenhydramine acts as an antagonist of histamine H1 receptor. Besides, was shown potential to repurpose diphenhydramine as an anti-melanoma therapeutic agent, it induces melanoma cell apoptosis by suppressing STAT3/MCL-1 survival signaling pathway.
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.
Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic and anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages.