Lihat sumber Siproheptadin

{{Infobox drug
| verifiedrevid = 460111355
| image = Cyproheptadine.svg
| width = 175
| image2 = Cyproheptadine-Spartan-PM3-3D-balls.png
| width2 = 175

<!--Clinical data-->
| pronounce = {{IPAc-en|ˌ|s|aɪ|p|r|oʊ|ˈ|h|ɛ|p|t|ə|d|iː|n}}{{refn|{{Dictionary.com|Cyproheptadine}}}}
| tradename = Heptasan, Pronicy, Periactin, dll
| Drugs.com = {{drugs.com|monograph|cyproheptadine-hydrochloride}}
| MedlinePlus = a682541
| DailyMedID = Cyproheptadine
| pregnancy_AU = A
| routes_of_administration = Oral
| ATC_prefix = R06
| ATC_suffix = AX02

| legal_AU  = S3
| legal_CA = OTC
| legal_UK = GSL
| legal_US = Rx-only
| legal_status = OTC

<!--Pharmacokinetic data-->
| protein_bound = 96 – 99%
| metabolism = [[Hati]],<ref name = DM>{{cite web|title=Cyproheptadine Hydrochloride tablet [Boscogen, Inc.]| work =DailyMed|publisher=U.S. National Library of Medicine |date=November 2010|access-date=26 October 2013|url=http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=f90faaa3-f40f-4653-8fb8-144d61c6b1d4|format=PDF}}</ref><ref name = TGA>{{cite web|title=Product Information: Periactin (cyproheptadine hydrochloride) |website=Aspen Pharmacare Australia|publisher=Aspen Pharmacare Australia Pty Ltd|date=17 November 2011|access-date=26 October 2013|url=http://www.aspenpharma.com.au/product_info/pi/Periactin_PI_17Nov11.pdf|archive-url=https://web.archive.org/web/20131029203732/http://www.aspenpharma.com.au/product_info/pi/Periactin_PI_17Nov11.pdf|archive-date=29 October 2013|url-status=dead}}</ref> sebagian besar [[CYP3A4]] dimediasi.
| elimination_half-life = 8,6 jam<ref name="pmid15083941">{{cite journal | vauthors = Gunja N, Collins M, Graudins A | title = A comparison of the pharmacokinetics of oral and sublingual cyproheptadine | journal = Journal of Toxicology. Clinical Toxicology | volume = 42 | issue = 1 | pages = 79–83 | year = 2004 | pmid = 15083941 | doi = 10.1081/clt-120028749 | s2cid = 20196551 }}</ref>
| excretion = Feses (2–20%; 34% di antaranya merupakan obat yang tidak berubah) dan [[ginjal]] (40%; tidak ada obat yang tidak berubah)<ref name = DM/><ref name = TGA/>

<!--Identifiers-->
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 129-03-3
| CAS_supplemental = {{CAS|969-33-5}} ([[hidroklorida]])
| PubChem = 2913
| IUPHAR_ligand = 277
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00434
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 2810
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 2YHB6175DO
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D07765
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 4046
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 516

<!--Chemical data-->
| IUPAC_name = 4-(5''H''-Dibenzo[a,d]siklohepten-5-ilidena)-1-metilpiperidina
| C=21 | H=21 | N=1
| SMILES = c43\C(=C1/CCN(C)CC1)c2ccccc2\C=C/c3cccc4
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C21H21N/c1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21/h2-11H,12-15H2,1H3
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = JJCFRYNCJDLXIK-UHFFFAOYSA-N
}}

'''Siproheptadin''' merupakan [[antihistamin]] generasi pertama dengan tambahan sifat [[antikolinergik]], [[antiserotonergik]], dan [[anestesi lokal]]. Obat ini dipatenkan pada tahun 1959 dan mulai digunakan secara medis pada tahun 1961.<ref name=Fis2006>{{cite book | vauthors = Fischer J, Ganellin CR |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=547 |url=https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA547 |language=en}}</ref>

==Kegunaan dalam Medis==
[[File:Cyproheptadine3Dan.gif|thumb|Struktur molekul 3D siproheptadin direpresentasikan sebagai model pengisian ruang]]
Siproheptadin digunakan untuk mengobati reaksi alergi (khususnya [[rinitis alergi]]).<ref>{{cite web | url = https://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a682541.html | work = MedlinePlus Drug Information | title = Cyproheptadine | publisher = U.S. National Library of Medicine }}</ref> Bukti penggunaannya untuk tujuan ini menunjukkan efektivitasnya, namun antihistamin generasi kedua seperti [[ketotifen]] dan [[loratadin]] menunjukkan hasil yang sama dengan efek samping yang lebih sedikit.<ref name=DeBruyne2017/> 

Obat ini juga digunakan sebagai pengobatan pencegahan terhadap [[migrain]]. Dalam sebuah penelitian tahun 2013, frekuensi migrain berkurang drastis pada pasien dalam waktu 7 hingga 10 hari setelah memulai pengobatan. Frekuensi rata-rata serangan migrain pada pasien ini sebelum pemberian adalah 8,7 kali per bulan; lalu menurun menjadi 3,1 kali per bulan pada 3 bulan setelah dimulainya pengobatan.<ref name=DeBruyne2017>{{cite journal | vauthors = De Bruyne P, Christiaens T, Boussery K, Mehuys E, Van Winckel M | title = Are antihistamines effective in children? A review of the evidence | journal = Archives of Disease in Childhood | volume = 102 | issue = 1 | pages = 56–60 | date = January 2017 | pmid = 27335428 | doi = 10.1136/archdischild-2015-310416 | s2cid = 21185048 }}</ref><ref>{{cite journal | vauthors = Saito Y, Yamanaka G, Shimomura H, Shiraishi K, Nakazawa T, Kato F, Shimizu-Motohashi Y, Sasaki M, Maegaki Y | display-authors = 6 | title = Reconsideration of the diagnosis and treatment of childhood migraine: A practical review of clinical experiences | journal = Brain & Development | volume = 39 | issue = 5 | pages = 386–394 | date = May 2017 | pmid = 27993427 | doi = 10.1016/j.braindev.2016.11.011 | s2cid = 34703034 }}</ref> Penggunaan ini terdapat pada label di Britania Raya dan beberapa negara lainnya. 

Obat ini juga digunakan di luar label dalam pengobatan [[sindrom]] muntah siklis pada bayi; satu-satunya bukti penggunaan ini berasal dari penelitian retrospektif.<ref>{{cite journal | vauthors = Salvatore S, Barberi S, Borrelli O, Castellazzi A, Di Mauro D, Di Mauro G, Doria M, Francavilla R, Landi M, Martelli A, Miniello VL, Simeone G, Verduci E, Verga C, Zanetti MA, Staiano A | display-authors = 6 | title = Pharmacological interventions on early functional gastrointestinal disorders | journal = Italian Journal of Pediatrics | volume = 42 | issue = 1 | pages = 68 | date = July 2016 | pmid = 27423188 | pmc = 4947301 | doi = 10.1186/s13052-016-0272-5 | doi-access = free }}</ref> 

Siproheptadin terkadang digunakan di luar label untuk memperbaiki akatisia pada orang yang menggunakan obat [[antipsikotik]].<ref name="Maudsley">{{cite book | vauthors = Taylor DM, Paton C, Kapur S |title=The Maudsley Prescribing Guidelines in Psychiatry | url = https://archive.org/details/maudsleyprescrib0000tayl |date=2015 |publisher=John Wiley & Sons |isbn=978-1-118-75457-3 |page=[https://archive.org/details/maudsleyprescrib0000tayl/page/85 85] }}</ref> 

Obat ini digunakan di luar label untuk mengobati berbagai kondisi dermatologis, termasuk gatal psikogenik<ref>{{cite journal | vauthors = Szepietowski JC, Reszke R | title = Psychogenic Itch Management | journal = Current Problems in Dermatology | volume = 50 | pages = 124–132 | year = 2016 | pmid = 27578081 | doi = 10.1159/000446055 | isbn = 978-3-318-05888-8 }}</ref> [[hiperhidrosis]] (keringat berlebihan) akibat obat,<ref>{{cite journal | vauthors = Ashton AK, Weinstein WL | title = Cyproheptadine for drug-induced sweating | journal = The American Journal of Psychiatry | volume = 159 | issue = 5 | pages = 874–875 | date = May 2002 | pmid = 11986151 | doi = 10.1176/appi.ajp.159.5.874-a }}</ref> dan pencegahan pembentukan lepuh pada beberapa orang dengan epidermolisis bulosa simpleks.<ref>{{cite book | vauthors = So JY, Teng J |chapter=Epidermolysis Bullosa Simplex | veditors = Adam MP, Everman DB, Mirzaa GM, Pagon RA, Wallace SE, Bean LJ, Gripp KW, Amemiya A |title=GeneReviews |date=1993 |publisher=University of Washington, Seattle |chapter-url=https://www.ncbi.nlm.nih.gov/books/NBK1369/  |pmid=20301543 }}</ref> 

Salah satu efek obat ini adalah peningkatan [[nafsu makan]] dan penambahan berat badan, yang menyebabkan penggunaannya (di luar label di Amerika Serikat) untuk tujuan ini pada anak-anak yang kurus serta penderita [[fibrosis sistik]].<ref>{{cite web | url = https://www.vademecum.es/principios-activos-ciproheptadina%2C+estimulante+del+apetito-a15+m1 | title = Ciproheptadina, estimulante del apetito | trans-title = Cyproheptadine, appetite stimulant | work = vademecum.es | language = Spanish }}</ref><ref>{{Cite web |url=https://www.caillon.com.uy/productos_ventana.php?id=39 |title=Bioplex NF |access-date=18 April 2018 |archive-date=18 April 2018 |archive-url=https://web.archive.org/web/20180418162117/https://www.caillon.com.uy/productos_ventana.php?id=39 |url-status=dead }}</ref><ref name=cyapp>{{cite journal | vauthors = Harrison ME, Norris ML, Robinson A, Spettigue W, Morrissey M, Isserlin L | title = Use of cyproheptadine to stimulate appetite and body weight gain: A systematic review | journal = Appetite | volume = 137 | pages = 62–72 | date = June 2019 | pmid = 30825493 | doi = 10.1016/j.appet.2019.02.012 | s2cid = 72333631 }}</ref><ref name="pmid34509304">{{cite journal | vauthors = Kim SY, Yun JM, Lee JW, Cho YG, Cho KH, Park YG, Cho B | title = Efficacy and Tolerability of Cyproheptadine in Poor Appetite: A Multicenter, Randomized, Double-blind, Placebo-controlled Study | journal = Clinical Therapeutics | volume = 43 | issue = 10 | pages = 1757–1772 | date = October 2021 | pmid = 34509304 | doi = 10.1016/j.clinthera.2021.08.001 | s2cid = 237493456 }}</ref>

Obat ini juga digunakan di luar label dalam pengelolaan kasus [[sindrom serotonin]] sedang hingga berat, suatu kompleks gejala yang terkait dengan penggunaan obat serotonergik seperti SSRI (dan MAOI), dan dalam kasus tingginya kadar serotonin dalam darah akibat [[tumor]] karsinoid penghasil [[serotonin]].<ref name="AMH">{{cite book | veditors = Rossi S | isbn = 978-0-9805790-9-3 | title = Australian Medicines Handbook | place = Adelaide | publisher = The Australian Medicines Handbook Unit Trust | year = 2013 | edition = 2013 }}</ref><ref>{{cite journal | vauthors = Iqbal MM, Basil MJ, Kaplan J, Iqbal MT | title = Overview of serotonin syndrome | journal = Annals of Clinical Psychiatry | volume = 24 | issue = 4 | pages = 310–318 | date = November 2012 | pmid = 23145389 }}</ref>

Siproheptadin memiliki efek [[sedatif]] dan dapat digunakan untuk mengobati [[insomnia]] sama seperti antihistamin yang bekerja secara sentral lainnya.<ref name="pmid33632345">{{cite journal | vauthors = Badr B, Naguy A | title = Cyproheptadine'':'' a psychopharmacological treasure trove? | journal = CNS Spectrums | volume = 27 | issue = 5 | pages = 533–535 | date = October 2022 | pmid = 33632345 | doi = 10.1017/S1092852921000250 | doi-access = free }}</ref><ref name="pmid33223070">{{cite journal | vauthors = Ekambaram V, Owens J | title = Medications Used for Pediatric Insomnia | journal = Child and Adolescent Psychiatric Clinics of North America | volume = 30 | issue = 1 | pages = 85–99 | date = January 2021 | pmid = 33223070 | doi = 10.1016/j.chc.2020.09.001 | s2cid = 227131545 }}</ref><ref>{{cite thesis | vauthors = Rombaut NE |year=1995 |title=Antihistamines and Sedation: Methods and Measures |id={{ProQuest|301570569}} |oclc=59660401 }}</ref><ref name="pmid334082">{{cite journal | vauthors = Wanderer AA, St Pierre JP, Ellis EF | title = Primary acquired cold urticaria. Double-blind comparative study of treatment with cyproheptadine, chlorpheniramine, and placebo | journal = Archives of Dermatology | volume = 113 | issue = 10 | pages = 1375–1377 | date = October 1977 | pmid = 334082 | doi = 10.1001/archderm.113.10.1375 }}</ref> Dosis yang dianjurkan untuk penggunaan ini adalah 4 hingga 8 mg.<ref name="pmid33223070" />
===Dalam Kedokteran Hewan===
Siproheptadin digunakan pada kucing sebagai stimulan nafsu makan<ref>{{cite journal | vauthors = Agnew W, Korman R | title = Pharmacological appetite stimulation: rational choices in the inappetent cat | journal = Journal of Feline Medicine and Surgery | volume = 16 | issue = 9 | pages = 749–756 | date = September 2014 | pmid = 25146662 | doi = 10.1177/1098612X14545273 | s2cid = 37126352 }}</ref><ref name="Gupta-2012">{{cite book | edition=2 | year=2012 | publisher=[[Academic Press]] | publication-place=[[Amsterdam]] [[Boston]] | veditors = Gupta RC | title=Veterinary Toxicology : Basic and Clinical Principles | isbn=978-0-12-385926-6 | oclc=794491298 | pages=xii+1438}}</ref>{{rp|page=1371}}  dan sebagai tambahan dalam pengobatan asma.<ref name=MVM2>{{cite book | vauthors= Dowling PM |chapter= Systemic Therapy of Airway Disease: Cyproheptadine |chapter-url=http://www.merckvetmanual.com/mvm/index.jsp?cfile=htm/bc/190907.htm |veditors=Kahn CM, Line S, Aiello SE |title= The Merck Veterinary Manual |date= 8 February 2005 |publisher= [[John Wiley & Sons]] |edition= 9th |isbn= 978-0-911910-50-6}} Retrieved on 26 October 2008.</ref> Kemungkinan efek sampingnya meliputi kegembiraan dan perilaku agresif.<ref name=MVM1>{{cite book | vauthors = Dowling PM |chapter= Drugs Affecting Appetite |chapter-url= http://www.merckvetmanual.com/mvm/index.jsp?cfile=htm/bc/190302.htm |veditors=Kahn CM, Line S, Aiello SE |title= The Merck Veterinary Manual |date= 8 February 2005 |publisher= [[John Wiley & Sons]] |edition= 9th |isbn= 978-0-911910-50-6|title-link= Merck Veterinary Manual }} Retrieved on 26 October 2008.</ref> Waktu paruh eliminasi siproheptadin pada kucing adalah 12 jam.<ref name=MVM2/> 

Siproheptadin adalah pengobatan lini kedua untuk disfungsi pituitari pars intermedia pada kuda.<ref>{{cite journal | vauthors = Durham AE | title = Therapeutics for Equine Endocrine Disorders | journal = The Veterinary Clinics of North America. Equine Practice | volume = 33 | issue = 1 | pages = 127–139 | date = April 2017 | pmid = 28190613 | doi = 10.1016/j.cveq.2016.11.003 }}</ref><ref>{{cite web | vauthors = Kritchevsky JE | date = July 2019 | work = Merck Vet Manual|title=Hirsutism Associated with Adenomas of the Pars Intermedia|url=https://www.merckvetmanual.com/endocrine-system/the-pituitary-gland/hypertrichosis-associated-with-adenomas-of-the-pars-intermedia |access-date=24 April 2011}}</ref>

==Efek Samping==
[[Efek samping]]nya meliputi:<ref name = DM/><ref name = TGA/> 
*Sedasi dan kantuk (seringkali bersifat sementara) 
*Pusing 
*Koordinasi terganggu 
*Konfusi 
*Resah 
*Perangsangan 
*Gelisah 
*[[Tremor]] 
*Iritabilitas 
*Insomnia 
*[[Parestesia]] 
*neuritis 
*[[Kejang]] 
*[[Euforia]] 
*[[Halusinasi]] 
*Histeri 
*[[Pingsan]] 
*Manifestasi alergi berupa ruam dan [[Sembap|edema]] 
*Diaforesis 
*[[Urtikaria]] 
*[[Fotosensitifitas]] 
*Labirinitis akut 
*[[Diplopia]] (melihat ganda) 
*[[Vertigo]] 
*[[tinitus]] 
*Hipotensi ([[tekanan darah rendah]]) 
*[[Palpitasi]] 
*[[Ekstrasistol]] 
*Syok [[anafilaksis]] 
*[[Anemia hemolitik]] 
*Diskrasia darah seperti [[leukopenia]], [[agranulositosis]], dan [[trombositopenia]] 
*[[kolestasis]] 
*Efek samping pada hati seperti: [[Hepatitis]], [[jaundis]], Gagal hati<ref>{{cite journal | vauthors = Chertoff J, Alam S, Clark V | title = Cyproheptadine-Induced Acute Liver Failure | journal = ACG Case Reports Journal | volume = 1 | issue = 4 | pages = 212–213 | date = July 2014 | pmid = 25580444 | pmc = 4286888 | doi = 10.14309/crj.2014.56 }}</ref> dan kelainan fungsi hati 
*Distress epigastrium 
*Anoreksia 
*Mual 
*Muntah 
*Diare 
*Efek samping [[antikolinergik]] seperti: Penglihatan kabur, sembelit, [[xerostomia]] (mulut kering), [[takikardia]] (denyut jantung tinggi), [[retensi urin]], kesulitan buang air kecil, hidung tersumbat, hidung atau tenggorokan kering
*Frekuensi urin 
*[[Menstruasi]] awal 
*Penebalan atau sekret bronkus 
*Sesak dada dan [[mengi]] 
*[[Kelelahan]] 
*Panas dingin 
*Sakit kepala 
*Nafsu makan meningkat 
*Penambahan berat badan

==Overdosis==
Tindakan dekontaminasi lambung seperti [[Karbon aktif|arang aktif]] terkadang direkomendasikan jika terjadi overdosis. Gejalanya biasanya menunjukkan depresi SSP (atau sebaliknya stimulasi SSP pada beberapa orang) dan efek samping [[antikolinergik]] yang berlebihan. [[Median dosis letal|LD<sub>50</sub>]] pada tikus adalah 123 mg/kg, dan 295 mg/kg pada tikus besar.<ref name = DM/><ref name = TGA/>

==Farmakologi==
===Farmakodinamik===
{| class="wikitable floatright" style="width:30em; font-size:small;"
|+ Siproheptadin<ref name="PDSP">{{cite web|url=https://pdsp.unc.edu/databases/pdsp.php?receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=cyproheptadine&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query|title=PDSP K<sub>i</sub> Database|author1-link=Bryan Roth| vauthors = Roth BL, Driscol J |website=Psychoactive Drug Screening Program (PDSP)|publisher=University of North Carolina at Chapel Hill and the United States National Institute of Mental Health|access-date=14 August 2017}}</ref>
|-
! Situs
! K<sub>i</sub> (nM){{efn|Semakin kecil [[konstanta kesetimbangan]], semakin kuat obat berikatan dengan tempat tersebut.}}
! Aksi{{efn|{{hlist|class=inline|↑ Agonis|↓ Antagonis}}}}
! Tempat
! Referensi
|-
| H<sub>1</sub> || 0.06 || ↓ || Manusia ||
|-
| H<sub>2</sub> || {{abbr|ND|No data}} ||  || {{abbr|ND|No data}} ||
|-
| H<sub>3</sub> || >10,000 ||  || Manusia ||
|-
| H<sub>4</sub> || 202 ||  || Manusia ||
|-
| M<sub>1</sub> || 12 || ↓ || Manusia ||
|-
| M<sub>2</sub> || 7 || ↓ || Manusia ||
|-
| M<sub>3</sub> || 12 || ↓ || Manusia ||
|-
| M<sub>4</sub> || 8 || ↓ || Manusia ||
|-
| M<sub>5</sub> || 11.8 || ↓ || Manusia ||
|-
| 5-HT<sub>1A</sub> || 59 || ↓ || Manusia ||
|-
| 5-HT<sub>2A</sub> || 1.67 || ↓ || Manusia ||
|-
| 5-HT<sub>2B</sub> || 1.54 || ↓ || Manusia ||
|-
| 5-HT<sub>2C</sub> || 2.23 || ↓ || Manusia ||
|-
| 5-HT<sub>3</sub> || 228 ||  || Tikus ||
|-
| 5-HT<sub>6</sub> || 142 ||  || Manusia ||
|-
| 5-HT<sub>7</sub> || 123 ||  || Manusia ||
|-
| D<sub>1</sub> || 117 ||  || Manusia ||
|-
| D<sub>2</sub> || 112 || ↓ || Manusia ||
|-
| D<sub>3</sub> || 8 ||  || Manusia ||
|-
| [[Pengangkut serotonin|SERT]] || 4,100 ||  || Tikus besar ||
|-
| NET || 290 ||  || Tikus besar ||
|-
| DAT || {{abbr|ND|No data}} ||  || {{abbr|ND|No data}} ||
|- class="sortbottom" 
| colspan="5" style="word-wrap:break-word;" | {{Notelist}}
|}

Siproheptadin adalah [[antihistamin]] yang sangat kuat atau agonis terbalik dari reseptor H1. Pada konsentrasi yang lebih tinggi ia juga memiliki aktivitas [[antikolinergik]], [[antiserotonergik]], dan [[antidopaminergik]]. Dari [[reseptor serotonin]], obat ini merupakan antagonis yang sangat kuat dari reseptor 5-HT2. Hal ini diperkirakan mendasari efektivitasnya dalam pengobatan [[sindrom serotonin]].<ref name="pmid10221364">{{cite journal | vauthors = Gillman PK | title = The serotonin syndrome and its treatment | journal = Journal of Psychopharmacology | volume = 13 | issue = 1 | pages = 100–109 | date = 1999 | pmid = 10221364 | doi = 10.1177/026988119901300111 | s2cid = 17640246 | url = https://zenodo.org/record/844143 }}</ref> Namun, ada kemungkinan bahwa blokade reseptor 5-HT1 juga berkontribusi terhadap efektivitasnya pada sindrom serotonin.<ref name="pmid7576268">{{cite journal | vauthors = Sporer KA | title = The serotonin syndrome. Implicated drugs, pathophysiology and management | journal = Drug Safety | volume = 13 | issue = 2 | pages = 94–104 | date = August 1995 | pmid = 7576268 | doi = 10.2165/00002018-199513020-00004 | s2cid = 19809259 }}</ref> Siproheptadin telah dilaporkan memblokir 85% reseptor 5-HT2 di otak manusia dengan dosis 4 mg tiga kali sehari (total 12 mg/hari) dan memblokir 95% reseptor 5-HT2 di otak manusia di a dosis 6 mg tiga kali sehari (total 18 mg/hari) yang diukur dengan [[tomografi emisi positron]] (PET).<ref name="pmid9167527">{{cite journal | vauthors = Kapur S, Zipursky RB, Jones C, Wilson AA, DaSilva JD, Houle S | title = Cyproheptadine: a potent in vivo serotonin antagonist | journal = The American Journal of Psychiatry | volume = 154 | issue = 6 | pages = 884a–884 | date = June 1997 | pmid = 9167527 | doi = 10.1176/ajp.154.6.884a | doi-access =  }}</ref> Dosis siproheptadin yang direkomendasikan untuk memastikan blokade reseptor 5-HT2 untuk sindrom serotonin adalah 20 hingga 30 mg.<ref name="pmid10221364"/> Selain aktivitasnya pada target [[neurotransmiter]], siproheptadin telah dilaporkan memiliki aktivitas [[antiandrogen]]ik yang lemah.<ref name="pmid9476091">{{cite journal | vauthors = Pucci E, Petraglia F | title = Treatment of androgen excess in females: yesterday, today and tomorrow | journal = Gynecological Endocrinology | volume = 11 | issue = 6 | pages = 411–433 | date = December 1997 | pmid = 9476091 | doi = 10.3109/09513599709152569 }}</ref>

===Farmakokinetik===
Siproheptadin terserap dengan baik setelah konsumsi oral, dengan kadar plasma puncak terjadi setelah 1 hingga 3 jam.<ref name="MurrayDaly2011">{{cite book | vauthors = Murray L, Daly F, McCoubrie DM, Cadogan M | title = Toxicology Handbook | url = https://books.google.com/books?id=KDOeIldGWxQC&pg=PT388 | access-date = 27 November 2011 | date = 15 January 2011 | publisher = Elsevier Australia | isbn = 978-0-7295-3939-5 | page = 388}}</ref> Waktu paruh terminal bila diminum secara oral adalah sekitar 8 jam.<ref name="pmid15083941" />

==Kimia==
Siproheptadin adalah benzosikloheptena trisiklik dan berkaitan erat dengan pizotifen dan ketotifen serta [[antidepresan]] trisiklik.

==Penelitian==
Siproheptadin dipelajari dalam satu percobaan kecil sebagai tambahan pada pengidap [[skizofrenia]] yang kondisinya stabil dan sedang menjalani pengobatan lain; Meskipun perhatian dan kefasihan verbal tampak meningkat, penelitian ini terlalu kecil untuk dapat digeneralisasikan.<ref>{{cite journal | vauthors = Buoli M, Altamura AC | title = May non-antipsychotic drugs improve cognition of schizophrenia patients? | journal = Pharmacopsychiatry | volume = 48 | issue = 2 | pages = 41–50 | date = March 2015 | pmid = 25584772 | doi = 10.1055/s-0034-1396801 | s2cid = 19202816 }}</ref> Obat ini juga telah dipelajari sebagai bahan pembantu dalam dua uji coba lain pada penderita skizofrenia, secara keseluruhan berjumlah sekitar lima puluh orang, dan tampaknya tidak memberikan efek.<ref name=Dabaghzadeh2012/>

Ada beberapa percobaan untuk melihat apakah siproheptadin dapat mengurangi disfungsi seksual yang disebabkan oleh SSRI dan obat antipsikotik.<ref>{{cite journal | vauthors = Nunes LV, Moreira HC, Razzouk D, Nunes SO, Mari J | title = Strategies for the treatment of antipsychotic-induced sexual dysfunction and/or hyperprolactinemia among patients of the schizophrenia spectrum: a review | journal = Journal of Sex & Marital Therapy | volume = 38 | issue = 3 | pages = 281–301 | date = 2012 | pmid = 22533871 | doi = 10.1080/0092623X.2011.606883 | s2cid = 23406005 }}</ref>

Siproheptadin telah dipelajari untuk pengobatan [[gangguan stres pascatrauma]].<ref name=Dabaghzadeh2012>{{cite journal | vauthors = Dabaghzadeh F, Khalili H, Ghaeli P, Dashti-Khavidaki S | title = Potential benefits of cyproheptadine in HIV-positive patients under treatment with antiretroviral drugs including efavirenz | journal = Expert Opinion on Pharmacotherapy | volume = 13 | issue = 18 | pages = 2613–2624 | date = December 2012 | pmid = 23140169 | doi = 10.1517/14656566.2012.742887 | s2cid = 25769557 }}</ref>

==Referensi==
{{Reflist}}
[[Kategori:Antihistamin]]
[[Kategori:Antiandrogen]]
[[Kategori:Antipsikotik]]
[[Kategori:Perangsang nafsu makan]]
[[Kategori:Dibenzosikloheptena]]
[[Kategori:Antagonis dopamin]]
[[Kategori:Anestesi lokal]]
[[Kategori:Antagonis muskarinik]]
[[Kategori:Piperidina]]
[[Kategori:Antagonis 5-HT2]]
[[Kategori:Penghalang saluran kalsium]]