Valnemulin received its first European approval in 1999 for the prevention and treatment of swine diseases such as swine dysentery and enzootic pneumonia. It later received approval for use in China in 2010. Valnemulin is an antibiotic from the pleuromutilin class that works by inhibiting the initiation of protein synthesis at the bacterial ribosome. It is effective against a variety of bacteria, including those that cause respiratory and intestinal diseases in pigs.
BRAND NAMES
Econor - swallow the capsule. If using a sachet, mix it with a small amount of water or a drink.
MECHANISM OF ACTION
Valnemulin hydrochloride acts by inhibiting bacterial protein synthesis. It does this by binding to the peptidyl transferase center (PTC) of the 50S subunit of the bacterial ribosome. This interaction disrupts the formation of peptide bonds, effectively halting the production of proteins necessary for bacterial growth and survival.
PHARMACOKINETICS
Absorption
At 65% and 85% relative humidity, valnemulin hydrogen fumarate showed water absorption values of 0.75% and 1.20% after 48 hours, respectively, while valnemulin hydrochloride exhibited an absorption value of 4% under the same conditions.
Distribution
Following intravenous administration, valnemulin exhibited extensive distribution, with a volume of distribution during the terminal phase (Vz) measured at 4.27 ± 0.99 L/kg.
Metabolism
Valnemulin is a pleuromutilin antibiotic that is extensively metabolized in the liver, primarily by cytochrome P450 (CYP) enzymes. This metabolism produces numerous oxidized and hydrolyzed metabolites, which are predominantly excreted in the feces via bile. The primary metabolic pathways involve hydroxylation of the mutilin ring, S-oxidation of the side chain, and cleavage of the amide bond through hydrolysis.
Excretion
Studies have shown that 73%–95% of the total dose is recovered from the feces. Very little is excreted via urine.
PHARMACODYNAMICS
Valnemulin hydrochloride is a pleuromutilin antibiotic that primarily works by inhibiting bacterial protein synthesis. Its pharmacodynamics include a selective mechanism of action, a targeted spectrum of activity, and a relatively low risk of resistance development. It is approved for veterinary use in pigs and rabbits to treat specific enteric and respiratory infections.
ADMINISTRATION
Valnemulin hydrochloride is a veterinary antibiotic most commonly administered orally to pigs and rabbits via medicated feed. It can also be given intramuscularly to poultry. The specific administration method depends on the animal species and the condition being treated.
DOSAGE AND STRENGTH
Valnemulin hydrochloride is available in several veterinary dosage forms, primarily as a premix for medicated feed, oral powder, and injectable solutions. Common concentrations include 10%, 50%, 1%, and 0.5%.
DRUG INTERACTIONS
The most severe drug interactions involving valnemulin hydrochloride, a veterinary antibiotic, occur with ionophore anticoccidials like monensin, salinomycin, and narasin. The concurrent use of these medications can lead to a toxic reaction, causing severe growth depression, ataxia, paralysis, and potentially fatal outcomes in animals. To prevent this, ionophores should not be administered for at least five days prior to or following valnemulin treatment. Other potential interactions, some observed with related pleuromutilin antibiotics, include synergistic effects with tetracyclines and colistin, and antagonistic effects when combined with fluoroquinolones such as ciprofloxacin or enrofloxacin.
FOOD INTERACTIONS
Valnemulin hydrochloride is a veterinary antibiotic for animals like pigs and rabbits, not for human use. The most critical food interaction is a fatal one with ionophore antibiotics, such as monensin, which are sometimes used in animal feed. This is because valnemulin inhibits the metabolism of these ionophores, leading to toxic buildup and causing severe, often lethal, reactions. Withdrawal times for meat and other animal products are enforced to ensure food safety for human consumption.
CONTRAINDICATIONS
Valnemulin is known to interact with ionophores like monensin, salinomycin, and narasin, which may lead to symptoms resembling ionophore toxicity. Consequently, animals should not receive products containing these ionophores during valnemulin treatment or for a minimum of five days before and after the treatment period.
SIDE EFFECTS
Valnemulin hydrochloride is a veterinary antibiotic primarily used in the treatment of pigs and rabbits. side effects are documented for these animals and include:
Skin reactions.
Reduced food intake.
Pregnancy and lactation.
Gastrointestinal issues.
decreased appetite.
Ataxia (loss of control of body movements).
Paralysis.
Death.
OVER DOSE
A valnemulin overdose in animals can cause severe side effects, especially when combined with ionophore medications.
Breeds affected in pigs.
In Rabbit's it can disrupt the natural balance of gut bacteria.
TOXICITY
Valnemulin hydrochloride is a veterinary antibiotic used primarily in pigs and rabbits; it is not approved for human use. Toxicity risks, including severe growth depression and death, primarily affect livestock through drug interactions or overdose, not humans.
