| Revision as of 13:39, 7 December 2010 editBeetstra (talk | contribs)Edit filter managers, Administrators172,031 edits Script assisted update of identifiers from ChemSpider, CommonChemistry and FDA for the Chem/Drugbox validation project - Updated: InChI1->InChI StdInChI StdInChIKey.← Previous edit |
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{{Short description|Topical parasiticide for dogs and cats}} |
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{{Merge from|Revolution (pet medicine)|date=June 2010}} |
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{{Use dmy dates|date=June 2024}} |
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{{cs1 config |name-list-style=vanc |display-authors=6}} |
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{{Drugbox |
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{{Drugbox |
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| Verifiedfields = changed |
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| IUPAC_name = |
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| Watchedfields = changed |
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| image = Selamectin.svg |
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| verifiedrevid = 464388376 |
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| image2 = Selamectin_sf.gif |
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| image = Selamectin Structural Formulae V.1.svg |
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| InChI = 1/C49H74O14/c1-12-26(2)43-29(5)18-19-48(63-43)24-35-21-34(62-48)17-16-28(4)42(60-40-23-38(54-10)45(32(8)58-40)61-39-22-37(53-9)41(50)31(7)57-39)27(3)14-13-15-33-25-56-46-44(55-11)30(6)20-36(47(51)59-35)49(33,46)52/h13-16,18-20,26-27,29,31-32,34-46,50,52H,12,17,21-25H2,1-11H3/b14-13+,28-16+,33-15+/t26-,27-,29-,31-,32-,34+,35-,36-,37-,38-,39-,40-,41-,42?,43+,44+,45?,46+,48+,49+/m0/s1 |
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| alt = |
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| InChIKey = AFSHKCWTGFDXJR-JQPIHPQKBM |
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| image2 = Selamectin_sf.gif |
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| StdInChI = 1S/C49H74O14/c1-12-26(2)43-29(5)18-19-48(63-43)24-35-21-34(62-48)17-16-28(4)42(60-40-23-38(54-10)45(32(8)58-40)61-39-22-37(53-9)41(50)31(7)57-39)27(3)14-13-15-33-25-56-46-44(55-11)30(6)20-36(47(51)59-35)49(33,46)52/h13-16,18-20,26-27,29,31-32,34-46,50,52H,12,17,21-25H2,1-11H3/b14-13+,28-16+,33-15+/t26-,27-,29-,31-,32-,34+,35-,36-,37-,38-,39-,40-,41-,42?,43+,44+,45?,46+,48+,49+/m0/s1 |
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| alt2 = |
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| StdInChIKey = AFSHKCWTGFDXJR-JQPIHPQKSA-N |
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| CAS_number = 165108-07-6 |
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<!-- Clinical data --> |
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| CAS_supplemental = |
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| tradename = Revolution, Stronghold, Revolt |
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| ATCvet = yes |
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| Drugs.com = {{drugs.com|international|selamectin}} |
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| ATC_prefix = P54 |
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| DailyMedID = Selamectin |
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| ATC_suffix = AA05 |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| ATC_supplemental = |
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| pregnancy_category = |
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| PubChem = 9578507 |
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| routes_of_administration = ] |
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| ChemSpiderID=16739776 |
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| ATCvet = yes |
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| DrugBank = |
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| ATC_prefix = P54 |
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| chemical_formula = |
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| ATC_suffix = AA05 |
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| C=43 | H=63 | N=1 | O=11 |
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| ATC_supplemental = {{ATCvet|P54|AA55}} |
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| molecular_weight = 769.96 g/mol |
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| smiles = CC1CCC2(CC3CC(O2)CC= C(C(C(C=CC=C4COC5C4(C(C= C(C5=NO)C)C(=O)O3)O)C) OC6CC(C(C(O6)C)O) OC)C)OC1C7CCCCC7 |
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| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled--> |
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| bioavailability = |
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| legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| protein_bound = |
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| legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C --> |
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| metabolism = |
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| legal_US = Rx-only |
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| legal_US_comment = <ref name="Revolution FDA label">{{cite web | title=Revolution- selamectin solution | website=DailyMed | date=1 December 2023 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8032a1ae-d192-4514-80f1-9a3b50dc2155 | access-date=6 February 2024}}</ref> |
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| legal_EU = Rx-only |
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| legal_EU_comment = <ref>{{cite web | title=Evicto EPAR | website=European Medicines Agency | date=1 August 2019 | url=https://www.ema.europa.eu/en/medicines/veterinary/EPAR/evicto | access-date=26 June 2024}}</ref><ref>{{cite web | title=Evicto PI | website=Union Register of medicinal products | date=23 July 2019 | url=https://ec.europa.eu/health/documents/community-register/html/v242.htm | access-date=26 December 2024}}</ref><ref>{{cite web | title=Stronghold EPAR | website=European Medicines Agency | date=25 March 2008 | url=https://www.ema.europa.eu/en/medicines/veterinary/EPAR/stronghold | access-date=29 June 2024}}</ref><ref>{{cite web | title=Stronghold PI | website=Union Register of medicinal products | date=3 December 1999 | url=https://ec.europa.eu/health/documents/community-register/html/v014.htm | access-date=26 December 2024}}</ref> |
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| legal_status = |
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<!-- Pharmacokinetic data --> |
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| bioavailability = |
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| protein_bound = |
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| metabolism = |
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| elimination_half-life = |
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| elimination_half-life = |
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| excretion = |
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| excretion = |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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<!-- Identifiers --> |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| CAS_number_Ref = {{cascite|changed|??}} |
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| pregnancy_category= |
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| CAS_number = 220119-17-5 |
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| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled--> |
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| CAS_supplemental = |
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| legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| PubChem = 9578507 |
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| legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C --> |
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| DrugBank_Ref = |
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| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
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| legal_status = |
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| DrugBank = |
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| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} |
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| routes_of_administration = |
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| ChemSpiderID = 16738655 |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = A2669OWX9N |
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| ChEMBL_Ref = {{ebicite|changed|EBI}} |
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| ChEMBL = 160777 |
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| synonyms = 25-cyclohexyl-25-de(1-methylpropyl)-5-deoxy-22,23-dihydro-5-(hydroxyimino)-avermectin B1 monosaccharide<ref>{{cite journal | vauthors = Bishop BF, Bruce CI, Evans NA, Goudie AC, Gration KA, Gibson SP, Pacey MS, Perry DA, Walshe ND, Witty MJ | display-authors = 6 | title = Selamectin: a novel broad-spectrum endectocide for dogs and cats | journal = Veterinary Parasitology | volume = 91 | issue = 3–4 | pages = 163–176 | date = August 2000 | pmid = 10940519 | doi = 10.1016/s0304-4017(00)00289-2 }}</ref> |
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<!-- Chemical data --> |
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| C=43 | H=63 | N=1 | O=11 |
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| smiles = C1CC2(C3C(O2)C/C=C(/((/C=C/C=C/4\CO\54((C=C(/C5=N/O)C)C(=O)O3)O)C)O6C(((O6)C)O)OC)\C)O1C7CCCCC7 |
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| StdInChI_Ref = {{stdinchicite|changed|chemspider}} |
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| StdInChI = 1S/C43H63NO11/c1-24-11-10-14-30-23-50-40-36(44-48)27(4)19-33(43(30,40)47)41(46)52-32-20-31(16-15-25(2)38(24)53-35-21-34(49-6)37(45)28(5)51-35)54-42(22-32)18-17-26(3)39(55-42)29-12-8-7-9-13-29/h10-11,14-15,19,24,26,28-29,31-35,37-40,45,47-48H,7-9,12-13,16-18,20-23H2,1-6H3/b11-10+,25-15+,30-14+,44-36-/t24-,26-,28-,31+,32-,33-,34-,35-,37-,38-,39-,40+,42+,43+/m0/s1 |
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| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} |
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| StdInChIKey = AFJYYKSVHJGXSN-XHKIUTQPSA-N |
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}} |
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}} |
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'''Selamectin''', sold under the brand name '''Revolution''', among others, is a ] ] and ] used on ]s and ]s.<ref name="Revolution FDA label" /> It treats and prevents infections of ], ]s, ]s, ] (scabies), and certain types of ] in dogs, and prevents heartworms, fleas, ear mites, ]s, and ] in cats.{{cn|date=February 2024}} It is structurally related to ] and ].{{cn|date=February 2024}} Selamectin is not approved for human use.{{cn|date=February 2024}} |
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'''Selamectin''' is the active ingredient in the prescription drug ] (manufactured by ]<ref>{{cite web|url=http://pfizercanen.naccvp.com/view_label.php?prodnum=1198329 |title=Label for Revolution (selamectin topical solution) Topical Parasiticide for Dogs and Cats |accessdate=2008-07-05 |publisher=Pfizer Canada Inc. }}</ref>), a ] ] and ] used on ] and ]. It controls outbreaks of ]s, ], ]s, ]s, and ]s. Selamectin is not approved for human use. |
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==How it works== |
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==Veterinary uses== |
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Selamectin is applied topically.<ref name="Revolution FDA label" /> It is not ] in water.<ref name="Revolution FDA label" /> |
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Selamectin disables ] by replacing ] in their ] ]; glutamate is the ] which normally interacts with the ] that open ] into the muscle. Selamectin interferes with this process; it activates the chloride current without desensitization, allowing chloride ions to enter the ] and causing neuromuscular ], impaired ], and eventual death. |
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==Mode of action== |
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Selamectin fights both internal and surface parasitic ]. Absorbed into the body through the skin and ], it travels through the bloodstream, intestines, and ]; parasites ingest the drug when they feed on the animal's blood. |
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{{unreferenced section|date=February 2024}} |
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Selamectin disables ] by activating ]-gated ] at ] ]. Selamectin activates the chloride channel without desensitization, allowing chloride ions to enter the ] and causing neuromuscular ], impaired ], and eventual death.{{cn|date=December 2022}} |
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The substance fights both internal and surface parasitic ].{{cn|date=February 2024}} Absorbed into the body through the skin and ], it travels through the bloodstream, intestines, and ];{{cn|date=February 2024}} parasites ingest the drug when they feed on the animal's blood or secretions.{{cn|date=December 2022}} |
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A 2003 report by E. Pipano in the Israel Journal of Veterinary Medicine describes the testing of Selamectin for safety and effectiveness, and the positive results.<ref>{{cite journal|title=RECENT DEVELOPMENTS IN THE CONTROL OF ECTOPARASITES AND ENDOPARASITES OF DOGS AND CATS WITH SELAMECTIN|journal=Israel Journal of Veterianry Medicine|date=2003|first=E.|last=Pipano|coauthors=|volume=58|issue=2-3|pages=|id= |url=http://www.isrvma.org/article/58_2_1.htm|accessdate=2008-07-05 |archiveurl = http://web.archive.org/web/20080414071601/http://www.isrvma.org/article/58_2_1.htm |archivedate = April 14, 2008}}</ref> |
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==References== |
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==Side effects== |
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Selamectin has been found to be safe and effective in a 2003 review.<ref>{{cite journal|title=Recent Developments In The Control Of Ectoparasites And Endoparasites Of Dogs And Cats With Selamectin|journal=Israel Journal of Veterianry Medicine|date=2003 | vauthors = Pipano E |volume=58|issue=2–3|url=http://www.infolizer.com/isrvm1aa1or7g/The-control-of-ectoparasites-and-endoparasites-of-dogs-and-cats-.html|access-date=5 July 2008 |archive-url = https://web.archive.org/web/20080414071601/http://www.isrvma.org/article/58_2_1.htm |archive-date = 14 April 2008}}</ref> |
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Selamectin has high safety ratings, with less than 1% of pets displaying ]{{citation needed | reason=Need source for 1% statistic|date=May 2020}}. In cases where side-effects do occur, they most often include passing irritation or hair loss at the application site. Symptoms beyond these (such as drooling, rapid breathing, lack of coordination, vomiting, or diarrhea) could be due to shock as a result of selamectin killing heartworms or other vulnerable parasites present at high levels in the bloodstreams of dogs.{{cn|date=September 2014}} This would be a reaction due to undetected or underestimated infections prior to using the medication, rather than an actual allergic reaction to the drug itself.{{cn|date=December 2022}} |
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== Society and culture == |
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=== Brand names === |
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{{unreferenced section|date=February 2024}} |
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Selamectin is sold under various brand names including Selehold, manufactured by ], Selarid manufactured by ], Revolution and Stronghold manufactured by ], Revolt manufactured by Aurora Pharmaceuticals, and Senergy manufactured by ]. |
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=== Similar products === |
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{{unreferenced section|date=February 2024}} |
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Main rival products for dogs include ] (trade names Stromectol, Ivermec and others) or ] (Interceptor) for heartworms, ] and ] (Advocate), ] (Frontline) or ] (Program) for fleas, or the combination ] (Sentinel) for both.{{cn|date=December 2022}} |
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== References == |
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{{Reflist}} |
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{{Reflist}} |
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{{Endectocides}} |
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==External links== |
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{{Portal bar | Medicine}} |
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{{Authority control}} |
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