Telmapitant

Telmapitant

Telmapitant is a pharmaceutical compound that acts as a selective antagonist of the neurokinin-1 (NK1) receptor. It is primarily investigated for its potential use in treating conditions associated with nausea and vomiting, particularly in veterinary medicine.

Mechanism of Action

Telmapitant functions by blocking the action of substance P, a neuropeptide that binds to NK1 receptors. Substance P is involved in the emetic (vomiting) reflex, and by inhibiting its action, telmapitant can reduce nausea and vomiting. This mechanism is similar to that of other NK1 receptor antagonists, such as Aprepitant, which are used in human medicine.

Clinical Applications

Telmapitant has been studied for its use in veterinary medicine, particularly in dogs and cats, to manage nausea and vomiting associated with chemotherapy, motion sickness, and other conditions. Its efficacy in these applications is due to its ability to cross the blood-brain barrier and effectively block NK1 receptors in the central nervous system.

Veterinary Use

In veterinary practice, telmapitant is considered for:

• Chemotherapy-induced nausea and vomiting (CINV): To improve the quality of life for pets undergoing cancer treatment.
• Motion sickness: To prevent vomiting during travel.
• Post-operative nausea and vomiting (PONV): To aid recovery after surgical procedures.

Pharmacokinetics

Telmapitant is administered orally, and its absorption can be influenced by the presence of food. It is metabolized in the liver and excreted primarily through the feces. The pharmacokinetic profile of telmapitant supports its use in once-daily dosing regimens.

Safety and Side Effects

Telmapitant is generally well-tolerated in animals, with a low incidence of adverse effects. Common side effects may include mild gastrointestinal disturbances, such as diarrhea or constipation. As with any medication, it is important to use telmapitant under the guidance of a veterinarian.

Research and Development

Ongoing research is exploring the broader applications of telmapitant in both veterinary and potentially human medicine. Studies are investigating its efficacy in treating other conditions associated with NK1 receptor activity, such as anxiety and depression.

Also see

• Neurokinin-1 receptor antagonist
• Substance P
• Aprepitant
• Chemotherapy-induced nausea and vomiting
• Veterinary medicine

Receptor Antagonists
Receptor Type	Example Antagonists
Adrenergic receptor	Propranolol, Prazosin
Cholinergic receptor	Atropine, Scopolamine
Dopamine receptor	Haloperidol, Clozapine
Histamine receptor	Ranitidine, Diphenhydramine
Serotonin receptor	Ondansetron, Risperidone
Glutamate receptor	Memantine, Ketamine
GABA receptor	Flumazenil, Bicuculline
Opioid receptor	Naloxone, Naltrexone
Angiotensin receptor	Losartan, Valsartan