Misplaced Pages

Selamectin: Difference between revisions

Article snapshot taken from[REDACTED] with creative commons attribution-sharealike license. Give it a read and then ask your questions in the chat. We can research this topic together.
Browse history interactively← Previous editContent deleted Content addedVisualWikitext
Revision as of 14:47, 22 October 2011 editCheMoBot (talk | contribs)Bots141,565 edits Updating {{drugbox}} (changes to verified fields - updated 'ChEBI_Ref', 'KEGG_Ref', 'CAS_number_Ref') per Chem/Drugbox validation (report errors or bugs)← Previous edit Latest revision as of 06:03, 26 December 2024 edit undoWhywhenwhohow (talk | contribs)Autopatrolled, Extended confirmed users, Pending changes reviewers49,324 edits infobox 
(99 intermediate revisions by 70 users not shown)
Line 1: Line 1:
{{Short description|Topical parasiticide for dogs and cats}}
{{Use dmy dates|date=June 2024}}
{{cs1 config |name-list-style=vanc |display-authors=6}}
{{Drugbox {{Drugbox
| Verifiedfields = changed | Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 401050240 | verifiedrevid = 464388376
| IUPAC_name =
| image = Selamectin Structural Formulae V.1.svg | image = Selamectin Structural Formulae V.1.svg
| alt =
| image2 = Selamectin_sf.gif | image2 = Selamectin_sf.gif
| alt2 =


<!--Clinical data--> <!-- Clinical data -->
| tradename = Revolution, Stronghold | tradename = Revolution, Stronghold, Revolt
| Drugs.com = {{drugs.com|international|selamectin}} | Drugs.com = {{drugs.com|international|selamectin}}
| DailyMedID = Selamectin
| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> | pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
⚫ | pregnancy_category =
| pregnancy_US = <!-- A / B / C / D / X -->
⚫ | routes_of_administration = ]
⚫ | pregnancy_category =
⚫ | ATCvet = yes
⚫ | ATC_prefix = P54
⚫ | ATC_suffix = AA05
⚫ | ATC_supplemental = {{ATCvet|P54|AA55}}

| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled--> | legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled-->
| legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII --> | legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C --> | legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C -->
| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> | legal_US = Rx-only
| 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>
⚫ | legal_status =
| legal_EU = Rx-only
⚫ | routes_of_administration = Topical
| 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>
⚫ | legal_status =


<!--Pharmacokinetic data--> <!-- Pharmacokinetic data -->
| bioavailability = | bioavailability =
| protein_bound = | protein_bound =
| metabolism = | metabolism =
| elimination_half-life = | elimination_half-life =
| excretion = | excretion =


<!--Identifiers--> <!-- Identifiers -->
| CAS_number_Ref = {{cascite|correct|??}} | CAS_number_Ref = {{cascite|changed|??}}
| CAS_number = 165108-07-6 | CAS_number = 220119-17-5
| CAS_supplemental = | CAS_supplemental =
⚫ | ATCvet = yes
⚫ | ATC_prefix = P54
⚫ | ATC_suffix = AA05
⚫ | ATC_supplemental =
| PubChem = 9578507 | PubChem = 9578507
| DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank_Ref =
| DrugBank = | DrugBank =
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = 16739776 | ChemSpiderID = 16738655
| UNII_Ref = {{fdacite|changed|FDA}} | UNII_Ref = {{fdacite|correct|FDA}}
| UNII = A2669OWX9N | UNII = A2669OWX9N
| ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 160777 | ChEMBL = 160777
| 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>


<!--Chemical data--> <!-- Chemical data -->
⚫ | C=43 | H=63 | N=1 | O=11
| chemical_formula =
| 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
⚫ | C=43 | H=63 | N=1 | O=11
⚫ | StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| molecular_weight = 769.96 g/mol
| 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
| 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
⚫ | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| 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
⚫ | StdInChIKey = AFJYYKSVHJGXSN-XHKIUTQPSA-N
| InChIKey = AFSHKCWTGFDXJR-JQPIHPQKBM
⚫ | StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| 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
⚫ | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
⚫ | StdInChIKey = AFSHKCWTGFDXJR-JQPIHPQKSA-N
}} }}


'''Selamectin''' (trade names '''Revolution''', '''Stronghold''') is a ] ] and ] used on ] and ], distributed 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> It prevents ], ]s, ]s, ] (scabies), and certain types of ] in dogs, and prevents heartworms, fleas, ear mites, ]s, and ] in cats. Selamectin is not approved for human use. '''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}}


==Usage== ==Veterinary uses==
Selamectin is applied topically.<ref name="Revolution FDA label" /> It is not ] in water.<ref name="Revolution FDA label" />
Selamectin is generally prescribed for cats and smaller indoor dogs due to studies that have shown it does not work as well to prevent heartworms as some of the oral preventatives.{{Citation needed|date=February 2007}}

The drug is applied topically. It is waterfast, and does not lose its effectiveness with bathing. It is packaged according to its varying dosage sizes, and is applied once monthly.


==Mode of action== ==Mode of action==
{{unreferenced section|date=February 2024}}
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. 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}}


The substance 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. 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}}


==Side effects== ==Side effects==
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|first=E.|last=Pipano|coauthors=|volume=58|issue=2–3|pages=|id= |url=http://www.infolizer.com/isrvm1aa1or7g/The-control-of-ectoparasites-and-endoparasites-of-dogs-and-cats-.html|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> 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>


Selamectin has high safety ratings, with less than 1% of pets displaying ]. 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 indicate the existence of a serious underlying cause, requiring immediate veterinary care. 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}}


== Society and culture ==
⚫ ==Similar products==
=== Brand names ===
⚫ Main rival products for dogs include ] (trade names ''Stromectol'', ''Ivermec'' and others) or ] (''Interceptor'') for heartworms, ] (''Frontline'') or ] (''Program'') for fleas, or the combination ] (''Sentinel'') for both.
{{unreferenced section|date=February 2024}}
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 ].


⚫ === Similar products ===
⚫ ==References==
{{unreferenced section|date=February 2024}}
⚫ 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}}

⚫ == References ==
{{Reflist}} {{Reflist}}


{{Endectocides}}
==External links==
{{Portal bar | Medicine}}
*
{{Authority control}}


] ]
] ]
] ]
] ]
] ]
] ]


]

Latest revision as of 06:03, 26 December 2024

Topical parasiticide for dogs and cats

Pharmaceutical compound
Selamectin
Clinical data
Trade namesRevolution, Stronghold, Revolt
Other names25-cyclohexyl-25-de(1-methylpropyl)-5-deoxy-22,23-dihydro-5-(hydroxyimino)-avermectin B1 monosaccharide
AHFS/Drugs.comInternational Drug Names
License data
Routes of
administration		Topical
ATCvet code
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.250.168 Edit this at Wikidata
Chemical and physical data
FormulaC43H63NO11
Molar mass769.973 g·mol
3D model (JSmol)
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
InChI
  • InChI=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
  • Key:AFJYYKSVHJGXSN-XHKIUTQPSA-N
  (what is this?)  (verify)

Selamectin, sold under the brand name Revolution, among others, is a topical parasiticide and anthelminthic used on dogs and cats. It treats and prevents infections of heartworms, fleas, ear mites, sarcoptic mange (scabies), and certain types of ticks in dogs, and prevents heartworms, fleas, ear mites, hookworms, and roundworms in cats. It is structurally related to ivermectin and milbemycin. Selamectin is not approved for human use.

Veterinary uses

Selamectin is applied topically. It is not miscible in water.

Mode of action

This section does not cite any sources. Please help improve this section by adding citations to reliable sources. Unsourced material may be challenged and removed. (February 2024) (Learn how and when to remove this message)

Selamectin disables parasites by activating glutamate-gated chloride channels at muscle synapses. Selamectin activates the chloride channel without desensitization, allowing chloride ions to enter the nerve cells and causing neuromuscular paralysis, impaired muscular contraction, and eventual death.

The substance fights both internal and surface parasitic infection. Absorbed into the body through the skin and hair follicles, it travels through the bloodstream, intestines, and sebaceous glands; parasites ingest the drug when they feed on the animal's blood or secretions.

Side effects

Selamectin has been found to be safe and effective in a 2003 review.

Selamectin has high safety ratings, with less than 1% of pets displaying side effects. 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. 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.

Society and culture

Brand names

This section does not cite any sources. Please help improve this section by adding citations to reliable sources. Unsourced material may be challenged and removed. (February 2024) (Learn how and when to remove this message)

Selamectin is sold under various brand names including Selehold, manufactured by KRKA, Selarid manufactured by Norbrook Laboratories Limited, Revolution and Stronghold manufactured by Zoetis, Revolt manufactured by Aurora Pharmaceuticals, and Senergy manufactured by Virbac.

Similar products

This section does not cite any sources. Please help improve this section by adding citations to reliable sources. Unsourced material may be challenged and removed. (February 2024) (Learn how and when to remove this message)

Main rival products for dogs include ivermectin (trade names Stromectol, Ivermec and others) or milbemycin oxime (Interceptor) for heartworms, imidacloprid and moxidectin (Advocate), fipronil (Frontline) or lufenuron (Program) for fleas, or the combination milbemycin oxime/lufenuron (Sentinel) for both.

References

  1. Bishop BF, Bruce CI, Evans NA, Goudie AC, Gration KA, Gibson SP, et al. (August 2000). "Selamectin: a novel broad-spectrum endectocide for dogs and cats". Veterinary Parasitology. 91 (3–4): 163–176. doi:10.1016/s0304-4017(00)00289-2. PMID 10940519.{{cite journal}}: CS1 maint: overridden setting (link)
  2. ^ "Revolution- selamectin solution". DailyMed. 1 December 2023. Retrieved 6 February 2024.
  3. "Evicto EPAR". European Medicines Agency. 1 August 2019. Retrieved 26 June 2024.
  4. "Evicto PI". Union Register of medicinal products. 23 July 2019. Retrieved 26 December 2024.
  5. "Stronghold EPAR". European Medicines Agency. 25 March 2008. Retrieved 29 June 2024.
  6. "Stronghold PI". Union Register of medicinal products. 3 December 1999. Retrieved 26 December 2024.
  7. Pipano E (2003). "Recent Developments In The Control Of Ectoparasites And Endoparasites Of Dogs And Cats With Selamectin". Israel Journal of Veterianry Medicine. 58 (2–3). Archived from the original on 14 April 2008. Retrieved 5 July 2008.
Antiparasitics – Anthelmintics (P02) and endectocides (QP54)
Antiplatyhelmintic agents
Antitrematodals
(schistosomicides)
Binds tubulin
AChE inhibitor
Other/unknown
Anticestodals
(taeniacides)
Binds tubulin
Other/unknown
Antinematodal agents
(including
macrofilaricides)
Binds tubulin
Glutamate-gated chloride channel, GABA receptor
NMDA
Other/unknown
Portal: Categories:
Selamectin: Difference between revisions Add topic