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Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(27)(i) antimicrobial:first aid antiseptic thimerosal
Source URL:
First approved in 1947
Source:
BLA101062
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Thimerosal is organomercury antiseptic and antifungal agent, used as a preservative in vaccines, immuloglobulins, nasal sprays, contact lens solutions. In USA, European Union countries thiomersal is no longer used in childhood vaccines due to public fears, although the FDA review of 1999 foud no evidence of harm from the use of thimerosal as a vaccine preservative, other than local hypersensitivity reactions. Thimerosal was used as a component of topical antiseptic solution and antiseptic ointment for treating cuts, nasal sprays, eye solutions, vaginal spermicides, diaper rash treatments, but re-evaluation of the drug in 1980-s demonstrated ineffectiveness and toxicity in topical pharmaceutical products, and topical thimerosal was withdrawn from the market. The mechanism of action of thimerosal has not been fully elucidated. It is believed that thimerosal inhibits sulfhydryl-containing active site of various enzymes and binds to sulfhydryl compounds, such as glutathione, cysteine, and SH groups of protein. In addition, thimerosal activates the InsP3 calcium channel on endoplasmic reticular membrane, thereby triggering the release of calcium from intracellular stores resulting in a calcium-induced calcium-influx of extracellular calcium. Consequently, thimerosal may induce or inhibit cellular functions dependent on calcium signaling.
Status:
First approved in 1947
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Mephentermine, an amphetamine-derived phenethylamine, is an alpha 1 adrenergic receptor agonist and a hypertensive drug. Mephentermine is mainly used as a vasopressor agent with a sympathomimetic action, primarily causing release of noradrenaline and increasing cardiac output due to positive inotropic effect on the myocardium. The injectable preparation of mephentermine is commonly used for the short-term treatment of various hypotensive states such as shock or hypotension accompanying myocardial infarction or spinal anesthesia or surgical procedures like cesarean section. There is evidence on the fetal metabolic effect and placental transfer of mephentermine. However, a few studies have shown that mephentermine is as effective as phenylephrine in preventing maternal hypotension after spinal anesthesia and has similar effect on neonatal outcome. It is being widely used in developing countries like India as it is much more economical than phenylephrine and offers ease of use as it does not necessitate multiple dilutions as injectable. It is also available in India as 10 mg oral tablets. Despite it was thought earlier to have a little stimulant effect its abuse potential has increased, especially in sports due to its stimulant properties. Like amphetamines, it has shown to increase athletic performance in strength exercises and endurance in a dose of 14 mg/70 kg body weight. It has been proposed that phentermine, which is the main metabolite of mephentermine, acts by inhibiting monoaminoxidases A and B. Mephentermine adverse effects has been related to CNS simulation, excessive rises in blood pressure, and arrhythmias. Wyamine Sulfate (brand name of mephentermine sulfate) approved by FDA in 1951 was discontinued in USA.
Status:
US Previously Marketed
Source:
DV by SANOFI AVENTIS US
(1982)
Source URL:
First approved in 1947
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Dienestrol (INN, USAN) (brand names Ortho Dienestrol, Dienoestrol, Dienoestrol Ortho, Sexadien, Denestrolin, Dienol, Dinovex, Follormon, Oestrodiene, Synestrol, numerous others) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist. Estrogens work partly by increasing a normal clear discharge from the vagina and making the vulva and urethra healthy. Using or applying an estrogen relieves or lessens: dryness and soreness in the vagina, itching, redness, or soreness of the vulva. Conditions that are treated with vaginal estrogens include a genital skin condition (vulvar atrophy), inflammation of the vagina (atrophic vaginitis), and inflammation of the urethra (atrophic urethritis). Dienestrol currently discontinued in US, but still in market in some other counties
Status:
US Previously Marketed
Source:
SULFALOID by FOREST PHARMS
(1982)
Source URL:
First approved in 1947
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Sulfamethazine is a sulfonamide used to treat a variety of bacterial diseases in animals. It inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthetase (dihydrofolate synthetase).
Status:
US Previously Marketed
Source:
MESANTOIN by NOVARTIS
(1946)
Source URL:
First approved in 1946
Source:
MESANTOIN by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Mephenytoin is an antiepileptic drug which can be useful in the treatment of epilepsy. The primary site of action appears to be the motor cortex where spread of seizure activity is inhibited. Possibly by promoting sodium efflux from neurons, mephenytoin tends to stabilize the threshold against hyperexcitability caused by excessive stimulation or environmental changes capable of reducing membrane sodium gradient. This includes the reduction of posttetanic potentiation at synapses. Loss of posttetanic potentiation prevents cortical seizure foci from detonating adjacent cortical areas. Mephenytoin reduces the maximal activity of brain stem centers responsible for the tonic phase of tonic-clonic (grand mal) seizures. The mechanism of action of mephenytoin is not definitely known, but extensive research strongly suggests that its main mechanism is to block frequency-, use- and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials. Mephenytoin is no longer available in the US or the UK. It is still studied largely because of its interesting hydroxylation polymorphism.
Status:
US Previously Marketed
Source:
CREMOTHALIDINE PHTHALYLSULFATHIAZOLE by MERCK
(1961)
Source URL:
First approved in 1946
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Phthalylsulfathiazole is a sulfonamide antibiotic. Phthalylsulfathiazole is an effective remedy in the treatment of dysentery, diarrhea and other intestinal fluxes. It inhibits dihydropteroate synthetase activity of bacteria. In veterinary, it is used for the treatment of diarrhea and enteritis of the calves, dysentery in sheep, gastroenteritis in foals and adult equines, enteritis caused by food poisoning. Phthalylsulfathiazole is only slightly absorbed from the gut, about 5 percent of the quantity ingested being eliminated in the urine. Consequently, it produces little or no systemic effects with virtually no risk of crystalluria, haematuria or oliguria. In hyper-susceptible people, it may cause gastrointestinal side effects, like nausea, vomiting, etc.
Status:
First approved in 1946
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Isobornyl thiocyanoacetate (thanite) is an insecticide, used to control ants, houseflies and head lice. Thanite is known to be toxic to fish.
Status:
US Previously Marketed
Source:
TRIDIONE by ABBVIE
(1946)
Source URL:
First approved in 1946
Source:
TRIDIONE by ABBVIE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Trimethadione (brand name is TRIDIONE) is an oxazolidinedione compound that was developed as an antiepileptic agent for control of petit mal seizures that are refractory to treatment with other drugs. Tridione does not modify the maximal seizure pattern in patients undergoing electroconvulsive therapy and has a sedative effect that may increase to the point of ataxia when excessive doses are used. Trimethadione acts as a voltage-activated T-type Ca2+ channel blocker. Trimethadione is rapidly absorbed from the gastrointestinal tract. It is demethylated by liver microsomes to the active metabolite, dimethadione. Approximately 3% of a daily dose of tridione is recovered in the urine as the unchanged drug. The majority of trimethadione is excreted slowly by the kidney in the form of dimethadione.
Status:
US Previously Marketed
First approved in 1946
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Salicylanilide (Salinidol). It is anilide of salicylic acid. It is an antifungal agent useful in the treatment of tinea capitis. Due to its inritant action on the skin, the concentration used should be 5 per cent or less. Salicylanilide is an oxidative phosphorylation uncoupler. Salicylanilide inhibits mycobacterial isocitrate lyase. Shows antifungal, antimycobacterial and antihelmitic effects in vivo.
Status:
US Previously Marketed
Source:
TRIPLE SULFA by FOUGERA
(1985)
Source URL:
First approved in 1945
Source:
SULTRIN by ORTHO MCNEIL PHARM
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Sulfabenzamide is an antibacterial/antimicrobial. Often used in conjunction with sulfathiazole and sulfacetamide (trade name - Sultrin) as a topical, intravaginal antibacterial preparation against Haemophilus (Gardnerella) vaginalis bacteria. The mode of action of SULTRIN is not completely known. Indirect effects, such as lowering the vaginal pH, may be equally important mechanisms.