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Status:
US Previously Marketed
Source:
CESAMET by BAUSCH
(1985)
Source URL:
First approved in 1985
Source:
CESAMET by BAUSCH
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Nabilone is a synthetic cannabinoid approved under the brand name cesamet for treatment of severe nausea and vomiting associated with cancer chemotherapy. Nabilone is an orally active which, like other cannabinoids, has complex effects on the central nervous system (CNS). It has been suggested that the antiemetic effect of nabilone is caused by interaction with the cannabinoid receptor system, i.e. the CB (1) receptor, which has been discovered in neural tissues.
Status:
US Previously Marketed
Source:
CINOBAC by LILLY
(1980)
Source URL:
First approved in 1980
Source:
CINOBAC by LILLY
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Cinoxacin is a synthetic antibacterial agent for oral administration. Cinoxacin mode of action involves the inhibiting of DNA gyrase, a type II topoisomerase, and topoisomerase IV. Adverse effects are nausea, anorexia, vomiting, abdominal cramps/pain, perverse taste, diarrhea, headache, dizziness, rash, urticaria, pruritus, edema and other.
Status:
US Previously Marketed
Source:
CEPHALOTHIN SODIUM W/ SODIUM CHLORIDE IN PLASTIC CONTAINER by BAXTER HLTHCARE
(1984)
Source URL:
First approved in 1964
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Cephalothin is a first generation, semisynthetic analogue of natural cephalosporin antibiotic. The in-vitro bactericidal action of Cephalothin results from inhibition of cell-wall synthesis. In general, Cephalothin has higher activity against Gram positive than Gram negative organisms. Cephalothin is primarily indicated in conditions like bone and joint infection, genitourinary tract infections, respiratory tract infections, soft tissue and skin infections and others. The severe or irreversible adverse effects of Cephalothin, which give rise to further complications, include nephrotoxicity, hemolytic anemia. Cephalothin produces potentially life-threatening effects, which include anaphylaxis, serum sickness syndrome. The symptomatic adverse reactions produced by Cephalothin are: rashes, urticaria, allergic reactions, thrombophlebitis, pain at injection site. Co-administration of diuretics, such as furanthril, ethacrynic acid and nephrotoxic antibiotics may increase the risk of renal damage. Reciprocal inactivation could be observed during in vitro mixing of Cephalothin with aminoglycosides.
Status:
US Previously Marketed
Source:
ANHYDRON by LILLY
(1963)
Source URL:
First approved in 1963
Source:
ANHYDRON by LILLY
Source URL:
Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Conditions:
Cyclothiazide was presumably developed by Eli Lilly for the treatment of hypertension. It is believed that the drug, which belongs to the class of thiazide diuretics, exerts its action by inhibitin sodium reabsorption in the renal tubules. In 1993 it was discovered that cyclothiazide stimulates AMPA receptors thus inducing seizure behavior.
Status:
First approved in 1958
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Dithiazanine, 3-ethyl-2-[5-(3-ethyl-2-benzothiazolinylidene)-l, 3-
pentadienyl] benzothiazolium iodide, is an old effective broad-spectrum human anthelmintic. In proper dosage, this polyvermicide is therapeutic for trichuriasis, strongyloidiasis, ascariasis, and enterobiasis. The drug also has significant anthelmintic
activity against human hookworm, Necator americanus.
It fulfills a need for an effective therapeutic
for trichuriasis and strongyloidiasis. Dithiazanine is
useful for the treatment of patients with either
single or multiple intestinal helminth infections. It
is effective for mass therapy for trichuriasis. Nowdays Dithiazanine is used only as a veterinary anthelmintic for dogs. It has being proved to be a highly toxic chemical, with a lethal dose for humans of about 4–16 mg/kg by oral ingestion.
Status:
US Previously Marketed
Source:
PAVERIL PHOSPHATE by LILLY
(1961)
Source URL:
First approved in 1951
Class (Stereo):
CHEMICAL (ACHIRAL)
Dimoxyline is the synthetic analogue of papaverine, Acute toxicity studies show it to be less toxic than papaverine. No analgesic action and no tolerance development in experimental animals by repeated administration. But Dimoxyline does not appear to be as potent as papaverine in comparable dosage. Dimoxyline is indicated for the treatment of patients with angina pectoris. Also, significant amount of benefit was claimed in patients with acute or chronic phlebitis, arterial thrombosis or embolism, Raynaud’s phenomena and early thromboangiitis obliterans or arteriosclerosis obliterans. Detected adverse events are: nausea or abdominal cramps.
Status:
US Previously Marketed
Source:
HISTA-CLOPANE CYCLOPENTAMINE HYDROCHLORIDE by LILLY
(1961)
Source URL:
First approved in 1951
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Cyclopentamine is a sympathomimetic alkylamine, classified as a vasoconstrictor. Cyclopentamine was indicated in the past as an over-the-counter medication for use as a nasal decongestant, notably in Europe and Australia, but has now been largely discontinued possibly due to the availability, effectiveness, and safety of a structurally similar drug, propylhexedrine used for relief of congestion due to colds, common cold, hay fever, or other allergies. Cyclopentamine acts as a releasing agent of the catecholamine neurotransmitters norepinephrine (noradrenaline), epinephrine (adrenaline), and dopamine. Cyclopentamine effects on norepinephrine and epinephrine mediate its decongestant effects, while its effects on all three neurotransmitters are responsible for its stimulant properties. Cyclopentamine was acting as nonspecific spasmolytic, similar to papaverine, in the rabbit ileum. It was demonstrated that cyclopentamine was a very weak alpha-adrenergic receptor stimulant and a weak beta-adrenergic receptor blocker. Cyclopentamine also potentiated the auto-inhibition produced by high doses of isoproterenol and the effect lasted as long as the autoinhibition persisted. It was suggested that the blockade by both drugs was the result of a direct action on the beta receptors. When ingested orally in sufficient quantities, cyclopentamine produces similar effects to amphetamine, methamphetamine, and propylhexedrine.
Status:
Possibly Marketed Outside US
Source:
Ractopamine Hydrochloride by Zoetis Inc.
(2019)
Source URL:
First approved in 2008
Source:
NADA140863
Source URL:
Class (Stereo):
CHEMICAL (MIXED)
Conditions:
Ractopamine is a feed additive to promote leanness in animals raised for their meat. Pharmacologically, it is a TAAR1 agonist and β adrenoreceptor agonist that stimulates β1 and β2 adrenergic receptors. Ractopamine is known to increase the rate of weight gain, improve feed efficiency, and increase carcass leanness in finishing swine. Its use in finishing swine yields about three kilograms of additional lean pork and improves feed efficiency by 10%. Ractopamine is the active ingredient in products known as Paylean for swine and Optaflexx for cattle, developed by Elanco Animal Health, a division of Eli Lilly and Company, for use in food animals for growth promotion. Ractopamine use has been banned in most countries, including the European Union, mainland China and Russia while 27 other countries, such as Japan, the United States, Canada, and South Korea, have deemed meat from livestock fed ractopamine safe for human consumption. Ractopamine is safe for finishing pigs heavier than 240 lb (110 kg) when administered in the diet at concentrations up to 10 ppm and fed for up to 35 days.
Status:
Possibly Marketed Outside US
Source:
NCT00190697: Phase 4 Interventional Completed Breast Cancer
(2001)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Arzoxifene (LY353381) is a synthetic, nonsteroidal ligand termed selective estrogen receptor modulator. Arzoxifene has antiestrogenic effects on the breast and endometrium, but pro-estrogenic effects on bone and lipids. Arzoxifene has been studied in the treatment of various hormone-responsive neoplasms. Its development has been discontinued.
Status:
Possibly Marketed Outside US
Source:
LY 237733 by Lilly
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Amesergide (previously known as LY237733) an ergoline derivative with highly selective 5-hydroxytryptamine (5-HT) antagonist activity and with a long duration of action. This drug was in phase II clinical trials for the treatment of erectile dysfunction and for the treatment of premature ejaculation. In addition, this drug participated in preclinical experiments to treat depression. All these studies were discontinued.