Buparvaquone: Difference between revisions

{{Short description|Chemical compound}}

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| image = Structure of buparvaquone.png

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| CAS_number = 88426-33-9

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| ChEMBL = 292009

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| C=21 | H=26 | O=3

'''Buparvaquone''' is a [[naphthoquinone]] [[antiprotozoal]] drug related to [[atovaquone]]. It is a promising compound for the therapy and prophylaxis of all forms of [[theileriosis (disambiguation)|theileriosis]]<!--intentional link to DAB page-->. Buparvaquone has been shown to have anti-[[leishmania]]l activity ''in vitro''. It can be used to treat bovine [[East Coast fever]] protozoa ''in vitro'', along with the only other substance known – ''[[Peganum harmala]]''.{{Citation needed|date=February 2010}} It is the only really effective commercial therapeutic product against bovine [[Tropical theileriosis|theileriosis]], where it has been used since the late 1980s.{{Citation needed|date=February 2010}}

It was first produced in [[Great Britain]], then in [[Germany]].{{Citation needed|date=February 2010}} Its patent expired in the mid-2000s, and was then produced in different countries, e.g., [[India]] and [[Iran]].{{cn|date=December 2022}}

Using a single dose of 2,5&nbsp;mg/kg, the recovery rate of curable cases is 90 to 98%. In [[tropical theileriosis]], a dosage of 2.0&nbsp;mg/kg has the same efficacy. Body temperature returns to normal in two to five days.

Parasitemia lowers from 12% on day 0 to 5% the next day, then to 1% by day 5 and none at day 7.<ref>{{cite journal | vauthors = Abdou TA, Abou-El-naga TR, Mahmoud MA | title = Clinicopathological Studies on Theileria Annulata Infection in Siwa Oasis in Egypt. | journal = BS. Vet. Med. J. | date = 2005 | volume = 15 | issue = 2 | pages = 40–6 | url = http://old.eaap.org/Previous_Annual_Meetings/2005Uppsala/Papers/M2.11_Abdou.pdf }}</ref>

== Molecular target ==

Buparvaquone resistance appears to be associated with parasite mutations in the Q_o quinone-binding site of mitochondrial [[cytochrome b]].<ref>{{cite journal | vauthors = Sharifiyazdi H, Namazi F, Oryan A, Shahriari R, Razavi M | title = Point mutations in the Theileria annulata cytochrome b gene is associated with buparvaquone treatment failure | journal = Veterinary Parasitology | volume = 187 | issue = 3–4 | pages = 431–5 | date = July 2012 | pmid = 22305656 | doi = 10.1016/j.vetpar.2012.01.016 }}</ref> Its mode of action is thus likely to be similar to that of the antimalarial drug atovaquone, a similar 2-hydroxy-1,4-naphthoquinone that binds to the Q_o site of cytochrome b thus inhibiting [[Coenzyme Q – cytochrome c reductase]].{{cn|date=December 2022}}