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

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Showing 31 - 40 of 57 results

Status:
Possibly Marketed Outside US
Source:
Canada:FLORFENICOL
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Florfenicol (Nuflor) is a fluorinated synthetic analog of thiamphenicol. Florfenicol is indicated for the treatment of bovine respiratory disease (BRD) associated with Mannheimia (Pasteurella) haemolytica, Pasteurella multocida, and Haemophilus somnus, for treatment of bovine interdigital phlegmon (foot rot, acute interdigital necrobacillosis, infectious pododermatitis) associated with Fusobacterium necrophorum and Bacteroides melaninogenicus. Florfenicol is a broad-spectrum, primarily bacteriostatic, antibiotic with a range of activity similar to that of chloramphenicol, including many gram-negative and gram-positive organisms; however, florfenicol does not carry the risk of inducing human aplastic anemia that is associated with chloramphenicol. It also has activity against some chloramphenicol resistant strains of bacteria, possibly because it is less affected by the major enzyme produced in plasmid-mediated bacterial resistance against chloramphenicol and thiamphenicol. Although the activity of florfenicol against obligate anaerobes is not addressed in the literature, it is likely to be quite effective. Antibiotic principle of Florfenicol is similar to that of chloramphenicol and Thiamphenicol. Florfenicol inhibits protein synthesis by binding to 70S ribosomal 50S subunits of susceptible bacteria, leading to the inhibition of peptidyl transferase and thereby preventing the transfer of amino acids to extending peptide chains and subsequent protein formation. The bacterial receptor that is the site of action for florfenicol is also considered to be the same as that for chloramphenicol and thiamphenicol. Florfenicol has a fluorine atom instead of the hydroxyl group located at C-3 in the structure of chloramphenicol and thiamphenicol. This prevents the acetylation of bacterial acetyltransferase in this site as to allow florfenicol to be less susceptible to deactivation by bacteria with plasmid-transmissible resistance that involves acetylation of the C-3 hydroxyl group in chloramphenicol and thiamphenicol, and prevents their interaction with bacterial ribosomes.
Status:
Possibly Marketed Outside US
Source:
Canada:AMITRAZ
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Amitraz (development code BTS27419) is a non-systemic acaricide and insecticide and has also been described as a scabicide. It was first synthesized by the Boots Co. in England in 1969. Amitraz is the only formamidine used as an ectoparasiticide. It appears to act by inhibition of the enzyme monoamine oxidase and as an agonist at octopamine receptors. Monoamine oxidase metabolizes amine neurotransmitters in ticks and mites, and octopamine is thought to modify tonic contractions in parasite muscles. Amitraz has a relatively wide safety margin in mammals; the most frequently associated adverse effect is sedation, which may be associated with an agonist activity of amitraz on α2-receptors in mammalian species. Amitraz is available as a spray or dip for use against mites, lice, and ticks in domestic livestock. It controls lice and mange in pigs and psoroptic mange in sheep. In cattle, it has been used in dips, sprays, or pour-ons for control of single-host and multihost tick species. In dipping baths, amitraz can be stabilized by the addition of calcium hydroxide and maintained by standard replenishment methods for routine tick control. An alternative method involves the use of total replenishment formulations in which the dip bath is replenished with full concentration of amitraz at weekly intervals before use. Amitraz is contraindicated in horses. Amitraz has antipyretic and antiinflammatory activity in vivo, and also has been shown to inhibit prostaglandin E2 synthesis(13). Decreased body temperature was observed in two of our cases. The basic approach to the patient with amitraz poisoning includes initial stabilization, treatment to reduce absorption and measures to improve elimination of the toxin. The medical management is essentially symptomatic and supportive. There is no specific antidote. Despite life-threatening symptomatology, all cases may recover completely. In this study we would like to emphasize that the incidence of poisoning with amitraz is increasing due to its widespread use in veterinary medicine. In order to minimize amitraz poisoning, public education should be given on primary prevention of poisoning and besides, producers should redesign containers as childproof packagers with warning labels
Status:
Possibly Marketed Outside US
Source:
Procox by Bayer
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Toltrazuril (Baycox, Procox, Tolcox, Toltrazuril) is a veterinary drug approved in Europe for the treatment of parasitic infections caused by roundworms and coccidia. In dogs it is used in combination with emodepside (Procox).
Pyriproxyfen is a broad-spectrum insect growth regulator with insecticidal activity against public health insect pests: houseflies, mosquitoes and cockroaches. In agriculture and horticulture, pyriproxyfen has registered uses for the control of scale, whitefly, bollworm, jassids, aphids and cutworms. Pyriproxyfen is used on citrus fruit in Israel, South Africa, Spain and Italy. Pyriproxyfen is one of several insecticides used for the control of the red imported fire ant (Solenopsis invicta) in California, USA. Pyriproxyfen has also been considered by WHO for vector control under its Pesticides Evaluation Scheme. It is a potent suppressor of embryogenesis and adult formation of the sweetpotato whitefly, Bemisia tabaci (Gennadius), and the greenhouse whitefly, Trialeurodes vaporariorum (Westwood). Dipping of cotton or tomato seedlings infested with 0 to 1-day-old eggs in 0.1 mg litre−1 resulted in over 90% suppression of egg hatch of both B. tabaci and T. vaporariorum. Pyriproxyfen is registered in the U.S. for flea and tick control in the home and on pets, as well as indoor and outdoor ant and roach control. Formulas include carpet powders, foggers, aerosols, shampoos, bait, and pet collars.
Status:
Possibly Marketed Outside US
Source:
Vectra 3D by Mitsui
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Dinotefuran is a new furanicotinyl insecticide which represents the third generation of neonicotinoid group. Dinotefuran, which was developed by Mitsui Chemicals, Inc., was registered in Japan April 24, 2002 and the registration has been submitted to the Environment Protection Agency (EPA) in the USA. Dinotefuran was granted Organophosphorus Alternative and Reduced Risk Status by the EPA. Dinotefuran exhibits a insecticidal activity against Hemiptera, Lepidoptera, Coleoptera, Diptera, Dictyoptera and Thysanoptera. Furthermore, it has very low phytotoxicity so that it can be utilized for many kinds of crops. Dinotefuran is water-soluble and has excellent systemic and translaminar action in many plants. This property enables dinotefuran to be applied using various methods and various formulations. The binding assay using insect nAChRs and the electrophysiological study showed that dinotefuran acted on nAChRs as an agonist. However, in the binding study, the affinity of dinotefuran against the binding site of other neonicotinoids was very low, suggesting that this compound acts on a different site than other neonicotinoids.
Resocortol butyrate is a corticosteroid which has a high intrinsic glucocorticoid activity. Its mineralocorticoid and progestational activity is very low. Resocortol butyrate has local and systemic glucocorticoid effects. The expression of these effects depends on the mode of application and the dosage applied. After topical application on the skin, a local anti-inflammatory effect is seen, which is accompanied by a moderate and reversible adrenal suppression at higher doses. After oral administration in dogs few systemic effects were observed. Resocortol butyrate was marketed under the brand name Pruban as the topical cream for the treatment of acute localised moist dermatitis in dogs. It was discontinued.
Indoxacarb is a new oxadiazine insecticide discovered and developed by DuPont. The indoxacarb racemate contains two enantiomers (S : R), designated DPX-KN128 and DPX-KN127, but only the S enantiomer has insecticidal activity. It inhibits insect neuronal voltage-dependent sodium channels. Indoxacarb is an active component of Merck Activyl® used in the treatment of flea and tick in dogs and cats. DuPont™ Steward® WG is a water dispersible granule stomach and contact insecticide powered by Indoxacarb for control of various insect pests on a variety of crops.
Status:
Possibly Marketed Outside US
Source:
Ibaflin by 3M Pharmaceuticals
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Ibafloxacin is a fluoroquinolone antibiotic drug used in veterinary medicine. Ibafloxacin, a fluorinated 4-quinolone, is a broad spectrum antibiotic with bactericidal action against Gram-positive and Gram-negative bacteria. Ibafloxacin is presented in the form of a tablet/oral gel containing a racemic mixture of S- and R-ibafloxacin. The antimicrobial activity of the racemate originates mainly from the S-enantiomer. Ibafloxacin was marketed under the brand name Ibaflin. Ibaflin tablets were intended for use in dogs for treatment of respiratory tract infections, urinary tract infections and dermal infections caused by ibafloxacin susceptible pathogens. Ibafloxacin, is an antibiotic belonging to the class ‘fluoroquinolones’. It works by blocking an enzyme called ‘DNA gyrase’, which is important in allowing bacteria to make copies of their DNA. This enzyme is only found in bacterial cells, and does not have a similar function in animal cells. By blocking DNA gyrase, ibafloxacin prevents the bacteria from making DNA and stops them making proteins and growing, resulting in their death.
Dirlotapide is indicated for the management of obesity in dogs. Dirlotapide is a microsomal triglyceride transfer protein (MTP) inhibitor. It mainly acts locally in the gut to reduce appetite, increase fecal fat and produce weight loss in dogs. The adverse reactions associated with treatment with Dirlotapide include vomiting, loose stools/diarrhea, lethargy, and anorexia.
Status:
Possibly Marketed Outside US
Source:
Trocoxil by Searle
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Mavacoxib (trade name Trocoxil) is a veterinary drug used to treat pain and inflammation in dogs with the degenerative joint disease. Mavacoxib is a non-steroidal anti-inflammatory drug (NSAID) of the coxib class. Mavacoxib acts by preferential inhibition of COX-2-mediated prostaglandin synthesis. It, therefore, possesses analgesic and anti-inflammatory properties. The products of COX-2 metabolism are also involved in ovulation, implantation, and closure of the ductus arteriosus. Mavacoxib is well absorbed after oral administration; bioavailability was 87% in fed dogs and 46 % in fasted conditions and the recommended dose is based on administration with food. Therapeutic concentrations in fed dogs are reached rapidly and peak concentrations are obtained in less than 24 hours after administering a dose. Mavacoxib is approximately 98% bound to plasma proteins. It is extensively distributed throughout the body and almost all the mavacoxib-related residues in plasma comprise parent drug. The rate of body clearance of mavacoxib is slow and the major route of elimination is by biliary excretion of the parent drug. Adverse reactions of the digestive tract such as vomiting and diarrhea were commonly reported, loss of appetite, hemorrhagic diarrhea, and melaena have been reported in uncommon cases. Gastrointestinal ulceration was reported in rare cases. Apathy, degradation of renal biochemistry parameters and impaired renal function have been reported in uncommon cases. In rare cases, these adverse reactions may be fatal.

Showing 31 - 40 of 57 results