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

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Morantel (1,4,5,6-tetrahydro-1-methyl-2-[2-(3-methyl-2-thienyl)ethenyl pyrimidine) is a tetrahydro-pyrimidine anthelmintic, differing from the related analogue pyrantel by the presence of a methyl group on the thiophene ring. Morantel tartrate, manufactured by Pfizer, Inc., was approved in the United States for use in cattle in 1981, and entered the market in early 1982. Three formulations have been approved in the United States: RUMATEL® Medicated Premix-88; RUMATEL Cattle Wormer Bolus, and PARATECT FLEX™ Diffuser, a sustained release bolus. It is intended to treat roundworms and tapeworms. Morantel is administered in lactating and non lactating cattle as morantel tartrate as a slow-release bolus (11.8 g morantel base per animal) or as a single oral dose of 6 to 7.5 mg morantel base/kg bw and in pigs at a single dose equivalent to 7.5 mg base/kg bw. In sheep, the citrate salt is administered at a single dose equivalent to 5 to 6 mg morantel base/kg bw. Morantel acts as a potent agonist at the acetylcholine receptors on the muscle cells of nematodes. Activation of the acetylcholine receptors induces a prolonged, spastic paralysis of the worms and expulsion from the host. It also been reported to block neurotransmission in vertebrates, to possess nicotine-like properties and to mimic acetylcholine at receptors in autonomic ganglia, adrenal medullae and respiratory tissues. Morantel and its salts are not used in human medicines.
Status:
Possibly Marketed Outside US
Source:
Sacox by Kaken Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Salinomycin as a promising anticancer drug candidate exerts anti-angiogenic and anti-tumorigenic activities by inhibiting vascular endothelial growth factor receptor 2-mediated angiogenesis. Its salt, salinomycin sodium, is an ionophore anticoccidial for use in chickens to prevent coccidiosis caused by Eimeria tenella, E.necatrix, E.acervulina, E.maxima, E.brunetti and E.mivati.
Status:
Possibly Marketed Outside US
Source:
NICARB by McClary, C.F.
Source URL:
First approved in 1993

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Nicarbazin, a complex of two compounds, 4,4'-dinitrocarbanilide (DNC) and 4,6-dimethyl-2-pyrimidinol (HDP) is an effective drug for preventing intestinal and caecal coccidiosis in poultry. It is used for prevention rather than the treatment of disease. Nicarbazin was the first agent with “broad‐spectrum” activity against Eimeria spp. of chickens. Nicarbazin is used as a single agent or in combination with polyether antibiotics (narasin, or maduramicin), roxarsone, or antibiotics (lincomycin, bacitracin, flavomycin) for prevention and control of coccidiosis caused by Eimeria spp. (all relevant species) in broiler chickens. Nicarbazin can cause increased sensitivity to heat stress, which may result in growth depression and even mortality in broilers; death may be due to cell degeneration processes in liver and kidneys; at the recommended dose, the drug causes occasionally toxic effects in laying hens like reduced hatchability and interruption of egg-laying. Nicarbazin interferes with the formation of the vitelline membrane, separating the egg yolk and egg white. The exact mode of action is unknown, although it is thought nicarbazin interferes with cholesterol metabolism in the formation of the membrane.
Status:
First approved in 1990

Class (Stereo):
CHEMICAL (ACHIRAL)



Amprolium Hydrochloride is a broad spectrum, potent coccidiostat (anti-protozoal) used for the treatment and prevention of Coccidiosis in cattle, goats, sheep, and poultry (chicken and turkey) in veterinary. Amprolium probably acts by inhibiting thiamine uptake by parasites and thus creates disorders in the metabolism of parasites.
Maduramicin is antibiotic isolated from actinobacteria Actinomadura rubra. Maduramicin is used in veterinary as an aid in the prevention of coccidiosis in broiler chickens and turkeys. The compound is reported to be toxic to animals and humans if improperly used or by accident, resulting in heart failure, skeletal muscle degeneration, and even death. Studies have shown that toxicity is due to activation of protein phosphatase 2A, and the manipulation of the ROS-PTEN-Akt-Erk1/2 pathway may be a potential approach to prevent maduramicin -induced cardiotoxicity.
mixture
Status:
US Approved OTC
Source:
21 CFR 333.110(d) first aid antibiotic:ointment neomycin sulfate
Source URL:
First approved in 1951
Source:
Mycifradin by Upjohn
Source URL:

Class:
MIXTURE



Neomycin is an aminoglycoside antibiotic found in many topical medications such as creams, ointments, and eye drops. In vitro tests have demonstrated that neomycin is bactericidal and acts by inhibiting the synthesis of protein in susceptible bacterial cells. It is effective primarily against gram-negative bacilli but does have some activity against gram-positive organisms. Neomycin is active in vitro against Escherichia coli and the Klebsiella-Entero. Topical uses include treatment for superficial eye infections caused by susceptible bacteria (used in combination with other anti-infective), treatment of otitis externa caused by susceptible bacteria, treatment or prevention of bacterial infections in skin lesions, and use as a continuous short-term irrigant or rinse to prevent bacteriuria and gram negative rod bacteremia in bacteriuria patients with indwelling catheters. May be used orally to treat hepatic encephalopathy, as a perioperative prophylactic agent, and as an adjunct to fluid and electrolyte replacement in the treatment of diarrhea caused to enter pathogenic E. coli (EPEC). Neomycin sulfate has been shown to be effective adjunctive therapy in hepatic coma by reduction of the ammonia forming bacteria in the intestinal tract. The subsequent reduction in blood ammonia has resulted in neurologic improvement. To reduce the development of drug-resistant bacteria and maintain the effectiveness of Neomycin Sulfate Oral Solution and other antibacterial drugs, susceptible bacteria should use Neomycin Sulfate Oral Solution only to treat or prevent infections that are proven or strongly suspected to be caused. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy. Neomycin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site near nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes
mixture
Status:
US Approved OTC
Source:
21 CFR 333.110(a) first aid antibiotic:ointment bacitracin
Source URL:
First marketed in 1921

Class:
MIXTURE



Bacitracin is a polypeptide antibiotic produced by Bacillus subtilis and Bacillus licheniformis. Bacitracin in combination with neomycin and polymyxin B is indicated for the treatment of many bacterial diseases. The antibacterial properties of bacitracin are mediated by its binding to C55-isoprenyl pyrophosphate, resulting in inhibition of cell wall biosynthesis.
mixture
Status:
US Approved OTC
Source:
21 CFR 333.110(a) first aid antibiotic:ointment bacitracin
Source URL:
First marketed in 1921

Class:
MIXTURE



Bacitracin is a polypeptide antibiotic produced by Bacillus subtilis and Bacillus licheniformis. Bacitracin in combination with neomycin and polymyxin B is indicated for the treatment of many bacterial diseases. The antibacterial properties of bacitracin are mediated by its binding to C55-isoprenyl pyrophosphate, resulting in inhibition of cell wall biosynthesis.