Halofuginone Lactate Property

storage temp. 

0-6°C

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

H310Fatal in contact with skin

H315Causes skin irritation

H318Causes serious eye damage

H330Fatal if inhaled

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P262Do not get in eyes, on skin, or on clothing.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P284Wear respiratory protection.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P302+P350IF ON SKIN: Gently wash with plenty of soap and water.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P310Immediately call a POISON CENTER or doctor/physician.

P320Specific treatment is urgent (see … on this label).

P321Specific treatment (see … on this label).

P322Specific measures (see …on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P361Remove/Take off immediately all contaminated clothing.

P362Take off contaminated clothing and wash before reuse.

P363Wash contaminated clothing before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

Halofuginone Lactate Chemical Properties,Usage,Production

Description

Halofuginone Lactate is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.

Uses

Halofuginone is a halogenated derivative of Febrifugine (F228500). Halofuginone is used as an antiprotozoal. It is a coccidiostat used in veterinary medicine. It is a synthetic halogenated derivative of febrifugine, a natural quinazolinone alkaloid which can be found in the Chinese herb Dichroa febrifuga (Chang Shan).Collgard Biopharmaceuticals is developing halofuginone for the treatment of scleroderma and it has received orphan drug designation from the U.S. Food and Drug Administration.
Integration of halofuginone lactate treatment and disinfection with p-chloro-m-cresol to control natural cryptosporidiosis in calves

Application

Halofuginone lactate is a synthetic product of the quinazolinone group with antiprotozoal activity, especially against Coccidia and Theileria species. It is effective in many cases of calf cryptosporidiosis, as has been shown in studies in Europe and Canada. Also, halofuginone is effective in lamb cryptosporidiosis. Halofuginone prevented natural infections in kids in France and in Greece[1].

Pharmacokinetics

Halofuginone lactate is a salt whose antiprotozoal properties and efficacy against Cryptosporidium parvum have been demonstrated both in in vitro conditions and artificial and natural infections. The compound has a cryptosporidiostatic effect on Cryptosporidium parvum. It is mainly active in the free stages of the parasite (sporozo?te, merozo?te). The concentrations to inhibit 50% and 90% of the parasites in an in vitro test system are IC50 < 0.1 μg/ml and IC90 of 4.5 μg/ml, respectively. The bioavailability of the drug in the calf following a single oral administration is about 80%. The time necessary to obtain the maximum concentration Tmax is 11 hours. The maximum concentration in plasma Cmax is 4 ng/ml. The apparent volume of distribution is 10 l/kg. The plasmatic concentrations of halofuginone after repeated oral administrations are comparable to the pharmacokinetic pattern after a single oral treatment. Unchanged halofuginone is the major component in the tissues. The highest values have been found in the liver and the kidney. The product is mainly excreted in the urine. The terminal elimination half-life is 11.7 hours after IV administration and 30.84 hours after single oral administration.

References

[1] N.D. Giadinis . “Efficacy of halofuginone lactate for the treatment and prevention of cryptosporidiosis in goat kids: An extensive field trial.” Small Ruminant Research 76 3 (2008): Pages 195-200.