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Restrict the search for
histamine
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Status:
US Approved OTC
Source:
21 CFR 341.12(k) cough/cold:antihistamine pyrilamine maleate
Source URL:
First approved in 1948
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
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 341.12(i) cough/cold:antihistamine phenindamine tartrate
Source URL:
First approved in 1947
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
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.
Status:
US Approved OTC
Source:
21 CFR 336.10(c) antiemetic diphenhydramine hydrochloride
Source URL:
First approved in 1946
Source:
BENADRYL by MCNEIL CONS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
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.
Status:
US Approved OTC
Source:
21 CFR 346.10(d) anorectal:local anesthetic dibucaine hydrochloride
Source URL:
First marketed in 1930
Source:
Dibucaine; Nupercaine by Society of Chemical Industry in Basle, Basle, Switzerland (Ciba Company, Inc., New York, distributor).
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Dibucaine is used as a local anesthetic for surface anesthesia. It is one of the most potent and toxic of the long-acting local anesthetics and its parenteral use is restricted to spinal anesthesia. Dibucaine is used to temporarily relieve pain and itching due to: hemorrhoids or other anorectal disorders, sunburn, minor burns, minor cuts; scrapes, insect bites, minor skin irritation. This drug acts via blocking of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions through sodium channel blocking. This reversibly stabilizes the membrane and inhibits depolarization, resulting in the failure of a propagated action potential and subsequent conduction blockade.
Status:
US Approved OTC
Source:
21 CFR 347.10(h) skin protectant glycerin
Source URL:
First marketed in 1921
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Glycerin (glycerol) is 3-carbon alcohol naturally occurring in the human body. It is the structural backbone triacylglycerol molecules, and can also be converted to a glycolytic substrate for subsequent metabolism. Glycerin is a colorless, odorless, viscous, sweet-tasting liquid. The FDA classifies glycerol as "generally recognized as safe". Glycerin is used in the pharmaceutical industry as a sweetener in syrups, lozenges, and as an excipient in eyewash solutions. As an individual prescription product, glycerin has uses as a hyperosmotic, osmotic diuretic, and ophthalmic agent. It may be used as an eye drop in the treatment of glaucoma to reduce intraocular pressure, as a solution or suppository for short-term treatment of constipation, to evacuate the bowel prior to a colonoscopy, and in some ocular surgeries. It may be given intravenously to reduce pressure inside the brain and used externally on the skin as a moisturizer. Glycerin has many other uses in the agricultural, food and pharmaceutical industry.
Status:
US Approved OTC
Source:
21 CFR 346.10(a) anorectal:local anesthetic benzocaine
Source URL:
First marketed in 1895
Class (Stereo):
CHEMICAL (ACHIRAL)
Benzocaine is a local anesthetic. It acts by blocking voltage-gated sodium ion channels in nerve endings. Benzocaine is available over-the counter for local anesthesia of oral and pharyngeal mucous membranes (sore throat, cold sores, mouth ulcers, toothache, sore gums, denture irritation), otic pain, and as a local anesthetic for surgical or diagnostic procedures. As a spray, benzocaine is used for temporary relief of pain and itching associated with minor burns, sunburn, minor cuts or scrapes, insect bites, or minor skin irritations. Topical application of benzocaine to gums or mouth may cause rare, but serious and potentially fatal adverse effect methemoglobinemia.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Doqualast is an antiasthmatic and antiallergic agent. It has a mode of antiallergic action similar to that of disodium cromoglycate and inhibits antigen-induced mediator release by interfering with the calcium transport required for histamine secretion across the mast cell membrane. In rabbits, no embryotoxic or teratogenic effects of doqualast were observed. The concomitant use of doqualast and theophylline might cause drug interaction. Doqualast is thought to increase the blood free fraction of concomitantly used theophylline and to accelerate elimination of theophylline from blood.
Status:
Investigational
Source:
INN:bamirastine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Bamirastine (previously known as TAK 427), an antiallergic compound that inhibits ligand binding to recombinant human histamine H1 receptor. The drug was involved in phase II clinical trials for the treatment of allergic rhinitis and for patients with atopic dermatitis. However, these studies were discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Pipoxizine is the antihistamine agent and antiserotonin agent. It was used as antiarrhythmic and bronchodilator.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Embramine or mebrophenhydramine is an antiallergic agent. Embramine is a histamine H₁-receptor antagonist exerting anticholinergic activity. It may inhibit stimulated platelet functions by inhibiting phospholipase A2. It is prescribed for severe allergic conditions.
