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

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Showing 6841 - 6850 of 8093 results

Status:
First marketed in 1921
Source:
Theophylline U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Since its discovery as component of the tea leaf by Albert Kossel in 1888, the history of theophylline (CAS 58-55-9) has been a long and successful one. At the turn of the century, theophylline became less expensive due to chemical synthesis and was primarily used as diuretic in subsequent years. It was Samuel Hirsch who discovered the bronchospasmolytic effect of theophylline in 1992, however, despite this pioneering discovery theophylline continued to be used primarily as diuretic and cardiac remedy. The molecular mechanism of bronchodilatation is inhibition of phosphodiesterase(PDE)3 and PDE4, but the anti-inflammatory effect may be due to histone deacetylase (HDAC) activation, resulting in switching off of activated inflammatory genes. Theophylline is indicated for the treatment of acute exacerbations of the symptoms and reversible airflow obstruction associated with asthma and other chronic lung diseases, e.g., emphysema and chronic bronchitis.
Status:
First marketed in 1921
Source:
Ammonia Water U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



The ammonium cation is a positively charged polyatomic ion with the chemical formula NH4+. Ammonium ions are a waste product of the metabolism of animals. In fish and aquatic invertebrates, it is excreted directly into the water. In mammals, sharks, and amphibians, it is converted in the urea cycle to urea, because urea is less toxic and can be stored more efficiently. In birds, reptiles, and terrestrial snails, metabolic ammonium is converted into uric acid, which is solid and can therefore be excreted with minimal water loss. Ammonium is an important source of nitrogen for many plant species, especially those growing on hypoxic soils. However, it is also toxic to most crop species and is rarely applied as a sole nitrogen source. The ammonium ion (NH4+) in the body plays an important role in the maintenance of acid-base balance. The kidney uses ammonium (NH4+) in place of sodium (Na+) to combine with fixed anions in maintaining acid-base balance, especially as a homeostatic compensatory mechanism in metabolic acidosis. When a loss of hydrogen ions (H+) occurs and serum chloride (Cl–) decreases, sodium is made available for combination with bicarbonate (HCO3–). This creates an excess of sodium bicarbonate (NaHCO3) which leads to a rise in blood pH and a state of metabolic alkalosis. The therapeutic effects of Ammonium (as Ammonium Chloride) depend upon the ability of the kidney to utilize ammonia in the excretion of an excess of fixed anions and the conversion of ammonia to urea by the liver, thereby liberating hydrogen (H+) and chloride (Cl–) ions into the extracellular fluid.
Status:
First marketed in 1921
Source:
Acetic Acid U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Acetic acid (a component of vinagre) is used in medicine for the treatment of otitis externa caused by bacterial infections. The solution containing acetic acid was approved by FDA.
Manganese Bromide is a highly water soluble crystalline salt composed of manganese and bromine with the formula MnBr2. Manganese Bromide can be used in place of palladium in the Stille reaction, which couples two carbon atoms using an organotin compound
Atropine inhibits the muscarinic actions of acetylcholine on structures innervated by postganglionic cholinergic nerves, and on smooth muscles which respond to endogenous acetylcholine but are not so innervated. As with other antimuscarinic agents, the major action of atropine is a competitive or surmountable antagonism which can be overcome by increasing the concentration of acetylcholine at receptor sites of the effector organ (e.g., by using anticholinesterase agents which inhibit the enzymatic destruction of acetylcholine). The receptors antagonized by atropine are the peripheral structures that are stimulated or inhibited by muscarine (i.e., exocrine glands and smooth and cardiac muscle). Responses to postganglionic cholinergic nerve stimulation also may be inhibited by atropine but this occurs less readily than with responses to injected (exogenous) choline esters. Atropine is relatively selective for muscarinic receptors. Its potency at nicotinic receptors is much lower, and actions at non-muscarinic receptors are generally undetectable clinically. Atropine does not distinguish among the M1, M2, and M3 subgroups of muscarinic receptors.
Status:
First marketed in 1921
Source:
Potassium Acetate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Potassium is needed to maintain good health. When potassium level falls below 3.5 mmol/L, Hypokalemia is diagnosed. In case of extremely low level of potassium (lower than 2.5 mmol/L) the following symptoms are appeared: malaise and fatigue. This low level of potassium can lead to severe muscle weakness and paralysis; respiratory failure; intermittent muscle spasms. It is known, foods that are good sources of potassium and low in sodium may reduce the risk of high blood pressure and stroke. Potassium supplementation is also recommended as an adjuvant antihypertensive agent for patients with essential hypertension.
Status:
First marketed in 1921
Source:
Acetic Acid U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Acetic acid (a component of vinagre) is used in medicine for the treatment of otitis externa caused by bacterial infections. The solution containing acetic acid was approved by FDA.
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 333.210(c) antifungal miconazole nitrate
Source URL:
First approved in 1974

Class (Stereo):
CHEMICAL (RACEMIC)



Miconazole is a synthetic imidazole derivative, a topical antifungal agent for use in the local treatment of vaginal, and skin and nail infections due to yeasts and dermatophytes. It is particularly active against Candida spp., Trichophyton spp., Epidermophyton spp., Microsporum spp. and Pityrosporon orbiculare (Malassezia furfur), but also possesses some activity against Gram-positive bacteria. It binds to the heme moiety of the fungal cytochrome P-450 dependent enzyme lanosterol 14-alpha-demethlyase. Inhibits 14-alpha-demethlyase, blocks formation of ergosterol and leads to the buildup of toxic methylated 14-a-sterols. Miconazole also affects the synthesis of triglycerides and fatty acids and inhibits oxidative and peroxidative enzymes, increasing the amount of active oxygen species within the cell.
Status:
US Approved OTC
Source:
21 CFR 341.20(b)(10) cough/cold:nasal decongestant xylometazoline hydrochloride
Source URL:
First approved in 1959
Source:
Otrivin by Ciba Geigy
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Xylometazoline, also spelled xylomethazoline, is a medication which is used to improve symptoms of nasal congestion, allergic rhinitis, and sinusitis. Xylometazoline was patented in 1956 and came into medical use in 1959. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. The drug works by stimulating adrenergic receptors on the lamina propria of blood vessels in the nose. The decongestant effect is due to constriction of large veins in the nose which swell up during the inflammation of any infection or allergy of the nose. The smaller arteries are also constricted and this causes the colour of the nasal epithelium to be visibly paler after dosage. The standard adult solution strength is 0.1% w/v xylometazoline (or 1 mg per 1 mL solution), and the dose for children under 12 is usually 0.05% (0.5 mg/mL).

Showing 6841 - 6850 of 8093 results