Peringatan Keamanan

Overdosage with cyproheptadine is likely to result in significant sedation - although paradoxical stimulation has been noted in pediatric patients - and anticholinergic adverse effects such as dry mouth and flushing.L32474 Most patients appear to recover without incident, as a review of cyproheptadine overdose cases in Hong Kong found the majority of patients had no or mild symptoms following intentional overdose.A231759

In the event of overdosage with cyproheptadine, prescribing information recommends the induction of vomiting (if it has not occurred spontaneously) using syrup of ipecac.L32474 Gastric lavage and activated charcoal may also be considered. Vasopressors may be used to treat hypotension and intravenous physostigmine salicylate may be considered for the treatment of significant CNS symptoms depending on the clinical picture.L32474

Cyproheptadine

DB00434

small molecule approved

Deskripsi

Cyproheptadine is a potent competitive antagonist of both serotonin and histamine receptors.L32474 It is used primarily to treat allergic symptoms, though it is perhaps more notable for its use in appetite stimulationL32519 and its off-label use in the treatment of serotonin syndrome.A231274

Struktur Molekul 2D

Berat 287.3981
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

A single study examining the difference in absorption of orally administered versus sublingually administered cyproheptadine in five healthy males demonstrated a mean Cmax of 30.0 mcg/L and 4.0 mcg/L, respectively, and a mean AUC of 209 mcg.h/L and 25 mcg.h/L, respectively.A179503 The Tmax of orally and sublingually administered cyproheptadine was 4 hours and 9.6 hours, respectively.A179503

Metabolisme

The principal metabolite found in human urine has been identified as a quaternary ammonium glucuronide conjugate of cyproheptadine.L32474

Rute Eliminasi

Approximately 2-20% of the radioactivity from an orally administered radio-labeled dose of cyproheptadine is excreted in the feces, of which approximately 34% is unchanged parent drug (less than 5.7% of the total dose).L32479 At least 40% of radioactivity is recovered in the urine.L32479

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Co-administration with alcohol may potentiate the sedative effects of cyproheptadine.

Interaksi Obat

1246 Data
Fluvoxamine The therapeutic efficacy of Fluvoxamine can be decreased when used in combination with Cyproheptadine.
Citalopram The risk or severity of QTc prolongation can be increased when Cyproheptadine is combined with Citalopram.
Duloxetine The therapeutic efficacy of Duloxetine can be decreased when used in combination with Cyproheptadine.
Paroxetine The therapeutic efficacy of Paroxetine can be decreased when used in combination with Cyproheptadine.
Sertraline The therapeutic efficacy of Sertraline can be decreased when used in combination with Cyproheptadine.
Sibutramine The therapeutic efficacy of Sibutramine can be decreased when used in combination with Cyproheptadine.
Nefazodone The therapeutic efficacy of Nefazodone can be decreased when used in combination with Cyproheptadine.
Escitalopram The therapeutic efficacy of Escitalopram can be decreased when used in combination with Cyproheptadine.
Zimelidine The therapeutic efficacy of Zimelidine can be decreased when used in combination with Cyproheptadine.
Dapoxetine The therapeutic efficacy of Dapoxetine can be decreased when used in combination with Cyproheptadine.
Milnacipran The therapeutic efficacy of Milnacipran can be decreased when used in combination with Cyproheptadine.
Desvenlafaxine The therapeutic efficacy of Desvenlafaxine can be decreased when used in combination with Cyproheptadine.
Seproxetine The therapeutic efficacy of Seproxetine can be decreased when used in combination with Cyproheptadine.
Levomilnacipran The risk or severity of Tachycardia can be increased when Cyproheptadine is combined with Levomilnacipran.
Indalpine The therapeutic efficacy of Indalpine can be decreased when used in combination with Cyproheptadine.
Ritanserin The therapeutic efficacy of Ritanserin can be decreased when used in combination with Cyproheptadine.
Alaproclate The therapeutic efficacy of Alaproclate can be decreased when used in combination with Cyproheptadine.
Buprenorphine Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
Hydrocodone Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Cyproheptadine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Cyproheptadine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
Mirtazapine Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
Orphenadrine Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
Pramipexole Cyproheptadine may increase the sedative activities of Pramipexole.
Ropinirole Cyproheptadine may increase the sedative activities of Ropinirole.
Rotigotine Cyproheptadine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Cyproheptadine.
Sodium oxybate Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
Thalidomide Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Aclidinium The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Cyproheptadine.
Mirabegron The risk or severity of urinary retention can be increased when Cyproheptadine is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Cyproheptadine is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Cyproheptadine.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Cyproheptadine.
Tiotropium The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Cyproheptadine is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Umeclidinium.
Porfimer sodium Cyproheptadine may increase the photosensitizing activities of Porfimer sodium.
Verteporfin Cyproheptadine may increase the photosensitizing activities of Verteporfin.
Benzylpenicilloyl polylysine Cyproheptadine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Cyproheptadine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Cyproheptadine.
Glycopyrronium The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Glycopyrronium.
Linezolid Linezolid may increase the anticholinergic activities of Cyproheptadine.
Furazolidone Furazolidone may increase the anticholinergic activities of Cyproheptadine.
Procaine Procaine may increase the anticholinergic activities of Cyproheptadine.
Tranylcypromine Tranylcypromine may increase the anticholinergic activities of Cyproheptadine.
Phenelzine Phenelzine may increase the anticholinergic activities of Cyproheptadine.
Minaprine Minaprine may increase the anticholinergic activities of Cyproheptadine.
Selegiline Selegiline may increase the anticholinergic activities of Cyproheptadine.
Procarbazine Procarbazine may increase the anticholinergic activities of Cyproheptadine.
Moclobemide Moclobemide may increase the anticholinergic activities of Cyproheptadine.
Isocarboxazid Isocarboxazid may increase the anticholinergic activities of Cyproheptadine.
Rasagiline Rasagiline may increase the anticholinergic activities of Cyproheptadine.
Pargyline Pargyline may increase the anticholinergic activities of Cyproheptadine.
Clorgiline Clorgiline may increase the anticholinergic activities of Cyproheptadine.
Iproniazid Iproniazid may increase the anticholinergic activities of Cyproheptadine.
Nialamide Nialamide may increase the anticholinergic activities of Cyproheptadine.
Safinamide Safinamide may increase the anticholinergic activities of Cyproheptadine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the anticholinergic activities of Cyproheptadine.
Methylene blue Methylene blue may increase the anticholinergic activities of Cyproheptadine.
Hydracarbazine Hydracarbazine may increase the anticholinergic activities of Cyproheptadine.
Pirlindole Pirlindole may increase the anticholinergic activities of Cyproheptadine.
Toloxatone Toloxatone may increase the anticholinergic activities of Cyproheptadine.
Benmoxin Benmoxin may increase the anticholinergic activities of Cyproheptadine.
Mebanazine Mebanazine may increase the anticholinergic activities of Cyproheptadine.
Octamoxin Octamoxin may increase the anticholinergic activities of Cyproheptadine.
Pheniprazine Pheniprazine may increase the anticholinergic activities of Cyproheptadine.
Phenoxypropazine Phenoxypropazine may increase the anticholinergic activities of Cyproheptadine.
Pivhydrazine Pivhydrazine may increase the anticholinergic activities of Cyproheptadine.
Safrazine Safrazine may increase the anticholinergic activities of Cyproheptadine.
Caroxazone Caroxazone may increase the anticholinergic activities of Cyproheptadine.
Harmaline Harmaline may increase the anticholinergic activities of Cyproheptadine.
Brofaromine Brofaromine may increase the anticholinergic activities of Cyproheptadine.
Dicoumarol The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Phenindione.
Warfarin The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Warfarin.
Phenprocoumon The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Phenprocoumon.
Acenocoumarol The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Cyproheptadine is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Coumarin.
(R)-warfarin The risk or severity of adverse effects can be increased when Cyproheptadine is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Tioclomarol.
(S)-Warfarin The risk or severity of adverse effects can be increased when Cyproheptadine is combined with (S)-Warfarin.

Target Protein

Histamine H1 receptor HRH1
5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 2C HTR2C
Histamine H2 receptor HRH2
5-hydroxytryptamine receptor 2B HTR2B
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3
5-hydroxytryptamine receptor 7 HTR7

Referensi & Sumber

Synthesis reference: Engelhardt, E.L.; U S . Patent 3,014,911; December 26, 1961; assigned to Merck & Co., Inc.
Artikel (PubMed)
  • PMID: 17287588
    Tokunaga S, Takeda Y, Shinomiya K, Hirase M, Kamei C: Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats. J Pharmacol Sci. 2007 Feb;103(2):201-6. Epub 2007 Feb 8.
  • PMID: 29493999
    Simon LV, Keenaghan M: Serotonin Syndrome .
  • PMID: 31839590
    Milani N, Qiu N, Molitor B, Badee J, Cruciani G, Fowler S: Use of Phenotypically Poor Metabolizer Individual Donor Human Liver Microsomes To Identify Selective Substrates of UGT2B10. Drug Metab Dispos. 2020 Mar;48(3):176-186. doi: 10.1124/dmd.119.089482. Epub 2019 Dec 15.
  • PMID: 32665417
    Kato S, Shah A, Plesescu M, Miyata Y, Bolleddula J, Chowdhury S, Zhu X: Prediction of Human Disproportionate and Biliary Excreted Metabolites Using Chimeric Mice with Humanized Liver. Drug Metab Dispos. 2020 Oct;48(10):934-943. doi: 10.1124/dmd.120.000128. Epub 2020 Jul 14.
  • PMID: 238818
    Porter CC, Arison BH, Gruber VF, Titus DC, Vandenheuvel WJ: Human metabolism of cyproheptadine. Drug Metab Dispos. 1975 May-Jun;3(3):189-97.
  • PMID: 21819287
    Chu FK: Review of the epidemiology and characteristics of intentional cyproheptadine overdose in Hong Kong. Clin Toxicol (Phila). 2011 Aug;49(7):681-3. doi: 10.3109/15563650.2011.602085. Epub 2011 Aug 8.
  • PMID: 15083941
    Gunja N, Collins M, Graudins A: A comparison of the pharmacokinetics of oral and sublingual cyproheptadine. J Toxicol Clin Toxicol. 2004;42(1):79-83. doi: 10.1081/clt-120028749.

Contoh Produk & Brand

Produk: 98 • International brands: 14
Produk
  • Cyproheptadine
    Syrup • 2 mg/5mL • Oral • US • Generic • Approved
  • Cyproheptadine
    Syrup • 2 mg/5mL • Oral • US • Generic • Approved
  • Cyproheptadine
    Syrup • 2 mg/5mL • Oral • US • Generic • Approved
  • Cyproheptadine
    Syrup • 2 mg/5mL • Oral • US • Generic • Approved
  • Cyproheptadine Hydrochloride
    Tablet • 4 mg/1 • Oral • US • Generic • Approved
  • Cyproheptadine Hydrochloride
    Tablet • 4 mg/1 • Oral • US • Generic • Approved
  • Cyproheptadine Hydrochloride
    Tablet • 4 mg/1 • Oral • US • Generic • Approved
  • Cyproheptadine Hydrochloride
    Tablet • 4 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 98 produk.
International Brands
  • Apeplus — Radicura
  • Apitup — Universal
  • Biohept — Biofarm
  • Ciplactin — Cipla
  • Cipractine — Teriak
  • Ciproheptadina — Arena
  • Ciprovit
  • Ciptadine — IBN
  • Cyheptine — Greater Pharma
  • Cyllermin — CCPC

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul