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

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Showing 151 - 160 of 244 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Methyldopa is an aromatic-amino-acid decarboxylase inhibitor in animals and in man. Methyldopa is a medication that has been used to treat high blood pressure since the 1960s. Methyldopa is indicated in the treatment of moderate to severe hypertension, including that complicated by renal disease. Only methyldopa, the L-isomer of alpha-methyldopa, has the ability to inhibit dopa decarboxylase and to deplete animal tissues of norepinephrine. D-isomer is relatively inactive. In man the antihypertensive activity appears to be due solely to the L-isomer, which became generally known as methyldopa (Aldomet). About twice the dose of the racemate (Methyldopa anhydrous, (±)-; DL-alpha-methyldopa) is required for equal antihypertensive effect. Racemic alpha-methyldopa was shown to be much less effective or ineffective for the treatment of hypertension. The comparative study of the hypotensive effect of L-alpha-methyl-dopa (L-isomer) versus the racemic form was performed. The short-term hypotensive effects of the racemic form and the L-isomer of alpha-methyl-dopa were compared in 13 hospitalized patients with arterial hypertension. After a placebo period the active preparations in a fixed dose of 1.5 g daily were administered for three-day periods separated by a second placebo period of three days, the sequence of the active drugs being alternated. Both substances were shown to exert significant hypotensive effects. The L-isomer produced significant blood-pressure reductions irrespective of whether or not it was given first, whereas the racemic form was effective only when given first. The blood-pressure levels obtained with the L-isomer were throughout lower than those with the racemic form. Methyldopa is a centrally acting antihypertensive agent. It is metabolized to alpha-methylnorepinephrine in the brain, and this compound is thought to activate central alpha-2 adrenergic receptors
Status:
Possibly Marketed Outside US
Source:
Holin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Estriol acetate benzoate is a semisynthetic, steroidal estrogen. Estriol benzoate diacetate is reported as an ingredient of Holin in Japan. It is an estrogen receptor agonist.
Testosterone acetate, a testosterone ester, is an androgen. It is a steroid lipid molecule considered to be practically insoluble (in water) and basic. It is an anabolic steroid and testosterone prodrug. Testosterone acetate has a faster rate of absorption in the body then other esters. In combination with two other testosterone esters, testosterone valerate and testosterone undecanoate, it is a part of Deposterona, an injectable veterinary blend steroid preparation marketed in Mexico. With its blend of slow and fast-acting esters, Deposterona is essentially a low dosed alternative to Sustanon and is used primarily to treat impotence, weakness, fatigue, and hypogonadism in male breeding animals (cows, pigs, canines, and sheep), and also as a general protein-sparing anabolic. Testosterone acetate is classified as a Schedule III drug by the United States Drug Enforcement Agency and is only legal with a prescription due to his potential for misuse and abuse.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Clostebol acetate (4-chloro-testosterone acetate), an anabolic androgenic agent used for fattening purposes in cattle breeding or applied topically in ophthalmological and dermatological treatments. The European Commission has prohibited its use since 1986.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Chloroprednisone acetate is the 21-acetate ester of chloroprednisone. Chloroprednisone acetate was sold under the brand name Topilan as an anti-inflammatory agent.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Choline alfoscerate (alpha-Glycerylphosphorylcholine or Alpha-GPC) is a nootropic choline-containing phospholipid. Choline alphoscerate increases the release of acetylcholine in rat hippocampus, facilitates learning and memory in experimental animals, improves brain transduction mechanisms and decreases age-dependent structural changes occurring in rat brain areas involved in learning and memory. The compound exerts neuroprotective effects in models of altered cholinergic neurotransmission and of brain vascular injury. In clinical studies choline alphoscerate improved memory and attention impairment, as well as affective and somatic symptoms in dementia disorders. In Europe alpha-GPC is a prescription medication for the treatment of Alzheimer's disease. It is available in two forms; one is taken by mouth, and the other is given as a shot. In the United States alpha-GPC is only available as a dietary supplement, mostly in products promoted to improve memory. Other uses for alpha-GPC include treatment of various kinds of dementia, stroke, and "mini-stroke" (transient ischemic attack, TIA). Alpha-GPC is also used for improving memory, thinking skills, and learning.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nomegestrol acetate (NOMAC) is a 19-norprogesterone derivative with high biological activity at the progesterone receptor, a weak anti-androgenic effect, but with no binding to estrogen, glucocorticoid or mineralocorticoid receptors. Nomegestrol has been developed by the Monaco-based company Théramex SAM (a Teva subsidiary). Nomegestrol acetate has been used successfully for the treatment of some gynaecological disorders (menstrual disturbances, dysmenorrhoea, premenstrual syndrome) and as a component of hormone replacement therapy in combination with estradiol for the relief of menopausal symptoms; it has been approved in Europe as monotherapy for the treatment of the menopausal syndrome, uterine diseases and menorrhagia, and in combination with an estrogen for the treatment of menopausal symptoms. Nomegestrol acetate in combination with estradiol is used as an oral contraceptive.
Status:
Possibly Marketed Outside US
Source:
Teva-cyproterone / Ethinyl Estradiol by TEVA Canada Limited [Canada]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cyproterone acetate is a steroid drug which was developed by Schering A.G (now Bayer). Cyproterone acetate was approved in Canada, Asia, Latin America and Europe for the treatment of sever acne under the name Diane-35 (ethinyl estradiol) and its mechanism of action in this condition is explained by competitive inhibition of androgen receptor AR. In Canada cyproterone acetate is widely used as a contraceptive, however its usage is associated with liver toxicity and clots formation. In the UK the drug is marketed for the treatment of prostate cancer (Cyproterone acetate brand name).
mixture
Status:
First approved in 1940
Source:
Ephynal Acetate by Hoffmann-La Roche
Source URL:

Class:
MIXTURE



It is known that Vitamin E, traditionally known as α¬ tocopherol, is a mixture of eight different compounds, four tocopherols and four tocotrienols, each one being designated as α, β, γ and δ forms. The two groups differ in the hydrophobic tridecyl side chain which is saturated (phytyl) in tocopherols and unsaturated having three double bonds (geranyl) in tocotrienols. During the last few years, it has been found that all the eight forms are biologically active and perform specific functions. Clinical research has shown that mixture of tocotrienols and tocopherols offer synergistic protective action against heart ailments and cancer that is not exclusively offered by α¬tocopherol. The other advantage of mixed tocopherols and tocotrienols is their role in slowing down aging. Diseases like diabetes 1 and 2, autoimmune diseases, bacterial and viral infections, Alzheimer disease, fungal (Candida) infections are prevented by these compounds. It helps in the maintenance of bones, muscles, eyes (vision), memory, sleep, lungs, infertility, skin and wrinkles. Although all forms of Vitamin E exhibit antioxidant activity, it is known that the antioxidant activity of vitamin E is not sufficient to explain the vitamin's biological activity. Vitamin E's anti-atherogenic activity involves the inhibition of the oxidation of LDL and the accumulation of oxLDL in the arterial wall. Vitamin E's antithrombotic and anticoagulant activities involves the downregulation of the expression of intracellular cell adhesion molecule(ICAM)-1 and vascular cell adhesion molecule(VCAM)-1 that lowers the adhesion of blood components to the endothelium. Its antioxidant effects explain the neuroprotective effects of vitamin E. The immunomodulatory effects of Vitamin E have been demonstrated in vitro, where alpha-tocopherol increases mitogenic response of T lymphocytes from aged mice. The mechanism of this response by vitamin E is not well understood, however it has been suggested that vitamin E itself may have mitogenic activity independent of its antioxidant activity. The mechanism of action of vitamin E's antiviral effects (primarily against HIV-1) involves its antioxidant activity. Vitamin E reduces oxidative stress, which is thought to contribute to HIV-1 pathogenesis, as well as to the pathogenesis of other viral infections. Vitamin E also affects membrane integrity and fluidity and, since HIV-1 is a membraned virus, altering membrane fluidity of HIV-1 may interfere with its ability to bind to cell-receptor sites, thus decreasing its infectivity.

Showing 151 - 160 of 244 results