エモデプシドおよびプラジクアンテル
**エモデプシド/プラジクアンテル**（一般的な商品名：プロフェンダー®）は、主に猫用に認可された広域スペクトルの局所用（スポットオン）抗寄生虫配合剤です。 * **エモデプシド**は新規のシクロオクタデプシペプチドであり、線虫（回虫および鉤虫）に対して優れた効果を示します。 * **プラジクアンテル**は確立されたイソキノリン-ピラジン誘導体であり、条虫に対して高い効果を発揮します。 **臨床上のポイント：** * スポットオン製剤は、経口投与が困難な猫の患者にとって大きな利点があり、ペットと飼い主双方のストレスを最小限に抑えます。 * 猫用として認可されていますが、エキゾチックアニマル医療、特に経口投与が難しい爬虫類において適応外使用されることがあります。 * 経皮的に全身吸収されるため、胃腸障害を防ぎ適切な投与量を確保するために、動物が塗布部を舐めないようにすることが極めて重要です。
作用機序: The combination utilizes two distinct mechanisms to eradicate parasites: * **Emodepside (Nematocide):** Binds pre-synaptically at the neuromuscular junction to a **latrophilin-like receptor** → increases intracellular calcium and diacylglycerol → triggers fusion of vesicles containing inhibitory neuropeptides → releases **PF1- and/or PF2-like receptors** into the synaptic cleft → stimulates postsynaptic receptors. This cascade results in the profound inhibition of pharyngeal pumping and locomotion, leading to **flaccid paralysis and death** of the nematode. * **Praziquantel (Cestocide):** Interacts with phospholipids in the parasite's integument → causes rapid intracellular ion fluxes (sodium, potassium, and **calcium**) → induces severe, irreversible tetanic contraction of the worm's musculature. At higher concentrations, it causes irreversible focal vacuolization and subsequent disintegration of the cestodal integument, making the parasite susceptible to the host's immune system.
動物種別の用量
- Treatment and control of hookworm, roundworm, and tapeworm infections · Minimum dose is 3 mg/kg emodepside & 12 mg/kg praziquantel applied to the skin on the back of the neck as a single topical dose. If re-infection occurs, the product can be re-applied after 30 days. · topical · once · Single dose · A second treatment should not be necessary unless re-infection occurs.
- Parasitic infections (off-label) · 4 drops/100 g body weight · topical · once · Single dose · Aquatic species must be kept in a dry place for 48 hours after treatment. Caution is advised until further studies verify safety and efficacy, particularly in sick animals.
用量は獣医療従事者向けの臨床リファレンスです。必ず最新の添付文書と個々の患者で確認してください。
投与経路
禁忌
- Cats less than 8 weeks of age
- Cats weighing less than 1 kg (2.2 lb)
有害事象
- Application site reactions (alopecia, dermatitis, pyoderma, edema, erythema, pruritus)
- Salivation/hypersalivation (especially if licked)
- Lethargy
- Vomiting
- Diarrhea
- Agitation or nervousness
- Tremors or twitching
- Ataxia
- Eye or respiratory irritation
- Rare post-approval reports: facial swelling, rear leg paralysis, seizures, hyperesthesia, morphea-like (scleroderma) lesion
薬物相互作用
- P-glycoprotein inhibitors/substrates (e.g., ivermectin, erythromycin, prednisolone, cyclosporine) · Emodepside is a P-glycoprotein substrate; concurrent use may cause pharmacokinetic interactions and potentially increase toxicity or alter efficacy.
モニタリング
- Clinical efficacy (resolution of clinical signs, negative fecal flotation/sedimentation)
過量投与
Both drugs generally have a wide margin of safety. * **Topical Overdose:** In 8-week-old kittens treated topically at 5X the recommended dose, transient salivation and/or tremors were observed but were self-limiting. In 7- to 8-month-old cats treated at 10X the dose, transient salivation, tremor, and lethargy occurred. * **Oral Exposure:** Accidental oral ingestion (e.g., licking the application site) can cause salivation, vomiting, anorexia, tremors, abnormal respirations, and ataxia. These signs typically resolve without specific treatment. * **Praziquantel Toxicity:** Parenteral doses of 50-100 mg/kg in cats caused transient ataxia and depression; injected doses of 200 mg/kg were lethal.
VetSheet の薬剤リファレンスは、獣医療従事者向けの臨床意思決定支援を目的としており、専門的判断やメーカーの最新添付文書に代わるものではありません。