How do Simparica tablets work against ticks? - briefly
Simparica tablets provide a systemic dose of sarolaner that binds to tick GABA‑gated chloride channels, disrupting neural transmission. This causes rapid paralysis and death, clearing infestations within hours of administration.
How do Simparica tablets work against ticks? - in detail
Simparica tablets contain the active ingredient sarolaner, a member of the isoxazoline class. After oral administration, sarolaner is absorbed rapidly into the bloodstream, reaching peak plasma concentrations within 2–4 hours. The drug distributes throughout the body’s tissues, including the skin where ticks attach.
Ticks feed by inserting their mouthparts into the host’s skin and ingesting blood. Sarolaner binds selectively to ligand‑gated chloride channels (GABA‑ and glutamate‑gated) in the tick’s nervous system. This binding blocks inhibitory neurotransmission, causing uncontrolled neuronal firing, paralysis, and death. Because the compound remains in the host’s plasma for an extended period, any tick that attaches within the dosing interval (typically 30 days) is exposed to lethal concentrations.
Key points of the pharmacological profile:
- Rapid absorption: detectable levels in plasma within hours.
- High bioavailability: ensures consistent systemic exposure.
- Long elimination half‑life: maintains effective concentrations for a month.
- Selective toxicity: mammalian GABA receptors are less sensitive, minimizing adverse effects in the treated animal.
The systemic action eliminates the need for direct contact with the parasite. As soon as a tick begins to feed, it ingests sarolaner present in the blood, leading to rapid knock‑down. This mechanism also prevents the transmission of tick‑borne pathogens, since the parasite is killed before it can salivate and transmit disease agents.