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Status:
US Approved Rx
(2022)
Source:
ANDA204934
(2022)
Source URL:
First marketed in 1937
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Niacin (also known as vitamin B3 and nicotinic acid) is bio converted to nicotinamide which is further converted to nicotinamide adenine dinucleotide (NAD+) and the hydride equivalent (NADH) which are coenzymes necessary for tissue metabolism, lipid metabolism, and glycogenolysis. Niacin (but not nicotinamide) in gram doses reduces LDL-C, Apo B, Lp(a), TG, and TC, and increases HDL-C. The increase in HDL-C is associated with an increase in apolipoprotein A-I (Apo A-I) and a shift in the distribution of HDL subfractions. These shifts include an increase in the HDL2:HDL3 ratio, and an elevation in lipoprotein A-I (Lp A-I, an HDL-C particle containing only Apo A-I). The mechanism by which niacin alters lipid profiles is not completely understood and may involve several actions, including partial inhibition of release of free fatty acids from adipose tissue, and increased lipoprotein lipase activity (which may increase the rate of chylomicron triglyceride removal from plasma). Niacin decreases the rate of hepatic synthesis of VLDL-C and LDL-C, and does not appear to affect fecal excretion of fats, sterols, or bile acids. As an adjunct to diet, the efficacy of niacin and lovastatin in improving lipid profiles (either individually, or in combination with each other, or niacin in combination with other statins) for the treatment of dyslipidemia has been well documented. The effect of combined therapy with niacin and lovastatin on cardiovascular morbidity and mortality has not been determined. In addition, preliminary reports suggest that niacin causes favorable LDL particle size transformations, although the clinical relevance of this effect is not yet clear. April 15, 2016: Based on several large cardiovascular outcome trials including AIM-HIGH, ACCORD, and HPS2-THRIVE, the FDA decided that "scientific evidence no longer supports the conclusion that a drug-induced reduction in triglyceride levels and/or increase in HDL-cholesterol levels in statin-treated patients results in a reduction in the risk of cardiovascular events" Consistent with this conclusion, the FDA has determined that the benefits of niacin ER tablets for coadministration with statins no longer outweigh the risks, and the approval for this indication should be withdrawn.
Status:
US Previously Marketed
Source:
Diodrast by Winthrop
(1937)
Source URL:
First marketed in 1937
Source:
Diodrast by Winthrop
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Iodopyracet (Diodone) is a radiocontrast agent used in urography before 1950. Renal clearance of iodopyracet is characterized by supply-limited elimination at low plasma concentrations and capacity-limited elimination at high plasma levels. Iodopyracet to be an effective agent for the estimation of renal plasma flow and tubular function has been used extensively in physiological studies. In 1945 was found, that p-aminohippuric acid was in some ways superior to diodone for these estimations in man because the urine and plasma blanks are small and because diodone penetrates human red blood cells whereas p-aminohippuric acid does not.
Status:
US Previously Marketed
Source:
Merphenyl Borate by Hamilton
(1937)
Source URL:
First marketed in 1937
Source:
Merphenyl Borate by Hamilton
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Phenylmercuric borate is classified as antimicrobial preservative. It is bactericidal against many Gram-positive and Gram-negative species. Fungicidal activity has been demonstrated against Candida albicans and Aspergillus niger. Phenylmercuric borate (PHB) is very rapidly incorporated into the cells of Escherichia coli. On the membrane, an important part of PHB seems to be associated with the ribosomes and particularly to the ribosomal proteins. Phenylmercuric borate solution is indicated for the treatment of tonsillitis, otitis, vulvovaginitis, furuncles, anthrax and ulcers, pyoderma, impetus, gingivitis and stomatitis. The regular hand disinfection with a liquid soap containing phenylmercuric borate enhanced urinary excretion of mercury indicating an increase in total daily absorption of the toxic metal. The additional amounts of mercury absorbed through the use of mercury contained in skin disinfectants are potentially dangerous for human.
Status:
US Previously Marketed
Source:
PREDSEM CALCIUM PANTOTHENATE by S. E. Massengill Co.
(1961)
Source URL:
First marketed in 1937
Source:
Calcium pentothate
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Pantothenic acid (known as Vitamin B5) is a water-soluble member of the B-vitamin family that is converted into 4’-phosphopantetheine, which is then converted to co-enzyme A (CoA) via adenosine triphosphate. Pantothenic acid regulates epidermal barrier function and keratinocytes differentiation via CoA metabolism. Pantothenic acid is incorporated into co-enzyme A and protects cells against peroxidative damage by increasing the level of glutathione. A recent feasibility study has also shown that daily oral supplementation of a nutritional agent containing pantothenic acid for 8 weeks was feasible and safe. It was discovered the different pharmacological implementation of pantothenic acid, such as treatment of acne, obesity. Existed some reports, mentioned efficacy using pantothenic acid in systemic lupus erythematosus. Significant reduction in morning stiffness, degree of disability, and severity of pain was reported for persons taking pantothenic acid in case of osteoarthritis and rheumatoid arthritis. Vitamin B5 may increase the effects of a group of drugs called cholinesterase inhibitors, which are used to treat Alzheimer's disease. That might lead to severe side effects.
Status:
US Previously Marketed
Source:
Kephrine
(1937)
Source URL:
First marketed in 1937
Source:
Kephrine
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Adrenalone is a keton form of the natural substrate epinephrine. Adrenalone is evidently formed in vivo by hydrolytic cleavage of the diester by esterases. It is an adrenergic receptor agonist. Adrenalone inhibits the norepinephrine synthesis and dopamine beta oxidase. It is known to have very weak sympathomimetic activity when compared to adrenaline. Adrenalone has the high radioprotective effect. It is a topical nasal decongestant. Adrenalone has hemostatic, sympathomimetic and vasoconstrictor therapeutic functions.
Status:
US Previously Marketed
Source:
PREDSEM CALCIUM PANTOTHENATE by S. E. Massengill Co.
(1961)
Source URL:
First marketed in 1937
Source:
Calcium pentothate
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Pantothenic acid (known as Vitamin B5) is a water-soluble member of the B-vitamin family that is converted into 4’-phosphopantetheine, which is then converted to co-enzyme A (CoA) via adenosine triphosphate. Pantothenic acid regulates epidermal barrier function and keratinocytes differentiation via CoA metabolism. Pantothenic acid is incorporated into co-enzyme A and protects cells against peroxidative damage by increasing the level of glutathione. A recent feasibility study has also shown that daily oral supplementation of a nutritional agent containing pantothenic acid for 8 weeks was feasible and safe. It was discovered the different pharmacological implementation of pantothenic acid, such as treatment of acne, obesity. Existed some reports, mentioned efficacy using pantothenic acid in systemic lupus erythematosus. Significant reduction in morning stiffness, degree of disability, and severity of pain was reported for persons taking pantothenic acid in case of osteoarthritis and rheumatoid arthritis. Vitamin B5 may increase the effects of a group of drugs called cholinesterase inhibitors, which are used to treat Alzheimer's disease. That might lead to severe side effects.
Status:
US Previously Marketed
Source:
FURACIN OTIC DROPS DIPERODON HYDROCHLORIDE by NORWICH
(1961)
Source URL:
First marketed in 1937
Source:
Diothane by Merrell
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Diperodon is one of several phenylurethane derivatives of dialkyl amino alcohols which have demonstrated significant local anaesthetic activity.
Status:
US Previously Marketed
Source:
Transentine by Ciba
(1937)
Source URL:
First marketed in 1937
Source:
Transentine by Ciba
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Adiphenine is a ternary amino ligand. It is used as a local anesthetic that reduces the frequency of acetylcholine-induced single-channel currents. It was originally introduced as a spasmolytic agent. Adiphenine reduced the muscle tone of the gastrointestinal tract, bile duct and gallbladder, bronchi, bladder. It affects the tone of the muscles of the eye, causing the pupil dilated (mydriasis), increased intraocular pressure, and paralysis of accommodation. Influences on the cardiovascular system, causing tachycardia and improving AV-conduction. Adiphenine side effects are: nausea, vomiting, heartburn, dizziness, headache. Adiphenine has not been widely used clinically.
Status:
US Previously Marketed
Source:
Merphenyl Borate by Hamilton
(1937)
Source URL:
First marketed in 1937
Source:
Merphenyl Borate by Hamilton
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Phenylmercuric borate is classified as antimicrobial preservative. It is bactericidal against many Gram-positive and Gram-negative species. Fungicidal activity has been demonstrated against Candida albicans and Aspergillus niger. Phenylmercuric borate (PHB) is very rapidly incorporated into the cells of Escherichia coli. On the membrane, an important part of PHB seems to be associated with the ribosomes and particularly to the ribosomal proteins. Phenylmercuric borate solution is indicated for the treatment of tonsillitis, otitis, vulvovaginitis, furuncles, anthrax and ulcers, pyoderma, impetus, gingivitis and stomatitis. The regular hand disinfection with a liquid soap containing phenylmercuric borate enhanced urinary excretion of mercury indicating an increase in total daily absorption of the toxic metal. The additional amounts of mercury absorbed through the use of mercury contained in skin disinfectants are potentially dangerous for human.
Status:
US Previously Marketed
Source:
PREDSEM CALCIUM PANTOTHENATE by S. E. Massengill Co.
(1961)
Source URL:
First marketed in 1937
Source:
Calcium pentothate
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Pantothenic acid (known as Vitamin B5) is a water-soluble member of the B-vitamin family that is converted into 4’-phosphopantetheine, which is then converted to co-enzyme A (CoA) via adenosine triphosphate. Pantothenic acid regulates epidermal barrier function and keratinocytes differentiation via CoA metabolism. Pantothenic acid is incorporated into co-enzyme A and protects cells against peroxidative damage by increasing the level of glutathione. A recent feasibility study has also shown that daily oral supplementation of a nutritional agent containing pantothenic acid for 8 weeks was feasible and safe. It was discovered the different pharmacological implementation of pantothenic acid, such as treatment of acne, obesity. Existed some reports, mentioned efficacy using pantothenic acid in systemic lupus erythematosus. Significant reduction in morning stiffness, degree of disability, and severity of pain was reported for persons taking pantothenic acid in case of osteoarthritis and rheumatoid arthritis. Vitamin B5 may increase the effects of a group of drugs called cholinesterase inhibitors, which are used to treat Alzheimer's disease. That might lead to severe side effects.