Peringatan Keamanan

Acute oral LD50 and dermal LD50 in mouse are 47.2 mg/kg and >512 mg/kg, respectively MSDS. Capsaicin is shown to be mutagenic for bacteria and yeast MSDS.

Capsaicin can cause serious irritation, conjunctivitis and lacrimation via contact with eyes. It induces a burning sensation and pain in case of contact with eyes and skin. As it is also irritating to the respiratory system, it causes lung irritation and coughing as well as bronchoconstriction. Other respiratory effects include laryngospasm, swelling of the larynx and lungs, chemical pneumonitis,respiratory arrest and central nervous system effects such as convulsions and excitement L1944. In case of ingestion, gastrointestinal tract irritation may be observed along with a sensation of warmth or painful burning MSDS. Symptoms of systemic toxicity include disorientation, fear, loss of body motor control including diminished hand-eye coordination, hyperventilation, tachycardia, and pulmonary oedema L1944. Careful early decontamination is recommended and medical intervention should be initiated for any life-threatening symptoms. In case of contact, individual must be removed from the source of exposure and the contacted skin and mucous membranes should be thoroughly washed with copious amounts of water L1944.

Capsaicin

DB06774

small molecule approved

Deskripsi

Capsaicin is most often used as a topical analgesic and exists in many formulations of cream, liquid, and patch preparations of various strengths; however, it may also be found in some dietary supplements. Capsaicin is a naturally-occurring botanical irritant in chili peppers, synthetically derived for pharmaceutical formulations. The most recent capsaicin FDA approval was Qutenza, an 8% capsaicin patch dermal-delivery system, indicated for neuropathic pain associated with post-herpetic neuralgia.

Struktur Molekul 2D

Berat 305.4119
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following oral ingestion of equipotent dose of 26.6 mg of pure capsaicin, the half life was approximately 24.9 ± 5.0 min [A32319]. Following topical application of 3% solution of capsaicin, the half-life of capsaicin was approximately 24 h [A32319]. The mean population elimination half-life was 1.64 h following application of a topical patch containing 179 mg of capsaicin [A32319].
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Oral: Following oral administration, capsaicin may be absorbed by a nonactive process from the stomach and whole intestine with an extent of absorption ranging between 50 and 90%, depending on the animal A32319. The peak blood concentration can be reached within 1 hour following administration A32319. Capsaicin may undergo minor metabolism in the small intestine epithelial cells post-absorption from the stomach into the small intestines. While oral pharmacokinetics information in humans is limited, ingestion of equipotent dose of 26.6 mg of pure capsaicin, capsaicin was detected in the plasma after 10 minutes and the peak plasma concentration of 2.47 ± 0.13 ng/ml was reached at 47.1 ± 2.0 minutes A32319. Systemic: Following intravenous or subcutaneous administration in animals, the concentrations in the brain and spinal cord were approximately 5-fold higher than that in blood and the concentration in the liver was approximately 3-fold higher than that in blood A32319. Topical: Topical capsaicin in humans is rapidly and well absorbed through the skin, however systemic absorption following topical or transdermal administration is unlikely A32319. For patients receiving the topical patch containing 179 mg of capsaicin, a population analysis was performed and plasma concentrations of capsaicin were fitted using a one-compartment model with first-order absorption and linear elimination. The mean peak plasma concentration was 1.86 ng/mL but the maximum value observed in any patient was 17.8 ng/mL A32319.

Metabolisme

Capsaicin metabolism after oral administration is unclear, however it is expected to undergo metabolism in the liver with minimal metabolism in the gut lumen. In vitro studies with human hepatic microsomes and S9 fragments indicate that capsaicin is rapidly metabolized, producing three major metabolites, 16-hydroxycapsaicin, 17-hydroxycapsaicin, and 16,17-hydroxycapsaicin, whereas vanillin was a minor metabolite A32319. It is proposed that cytochrome P450 (P450) enzymes may play some role in hepatic drug metabolism A32319. In vitro studies of capsaicin in human skin suggest slow biotransformation with most capsaicin remaining unchanged.

Rute Eliminasi

It is proposed that capsaicin mainly undergoes renal excretion, as both the unchanged and glucuronide form. A small fraction of unchanged compound is excreted in the feces and urine. In vivo animal studies demonstrates that less than 10 % of an administered dose was found in faces after 48 h A32319.

Interaksi Obat

1577 Data
Deferasirox The serum concentration of Capsaicin can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Capsaicin can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Capsaicin can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Capsaicin can be decreased when it is combined with Teriflunomide.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Capsaicin.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Capsaicin.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Capsaicin.
Colchicine The metabolism of Colchicine can be decreased when combined with Capsaicin.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Capsaicin.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Capsaicin.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Capsaicin.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Capsaicin.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Capsaicin.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Capsaicin.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Capsaicin.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Capsaicin.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Capsaicin.
Dipyridamole The therapeutic efficacy of Capsaicin can be decreased when used in combination with Dipyridamole.
Ephedrine Capsaicin may increase the neuromuscular blocking activities of Ephedrine.
Bambuterol Capsaicin may increase the neuromuscular blocking activities of Bambuterol.
Sar9, Met (O2)11-Substance P Capsaicin may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P.
Moxisylyte Capsaicin may increase the neuromuscular blocking activities of Moxisylyte.
Procaine The risk or severity of methemoglobinemia can be increased when Procaine is combined with Capsaicin.
Cocaine The risk or severity of methemoglobinemia can be increased when Cocaine is combined with Capsaicin.
Trimethaphan Capsaicin may increase the neuromuscular blocking activities of Trimethaphan.
Doxacurium Capsaicin may increase the neuromuscular blocking activities of Doxacurium.
Chloroprocaine The risk or severity of adverse effects can be increased when Capsaicin is combined with Chloroprocaine.
Tubocurarine Capsaicin may increase the neuromuscular blocking activities of Tubocurarine.
Aclidinium Capsaicin may increase the neuromuscular blocking activities of Aclidinium.
Butyrylthiocholine Capsaicin may increase the neuromuscular blocking activities of Butyrylthiocholine.
Clevidipine Capsaicin may increase the neuromuscular blocking activities of Clevidipine.
Mirabegron Capsaicin may increase the neuromuscular blocking activities of Mirabegron.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Oxybuprocaine is combined with Capsaicin.
Benzonatate Capsaicin may increase the neuromuscular blocking activities of Benzonatate.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Capsaicin.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Capsaicin.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Capsaicin.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Capsaicin.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Capsaicin.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Capsaicin.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Capsaicin.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Capsaicin.
Succinylcholine The metabolism of Succinylcholine can be decreased when combined with Capsaicin.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Capsaicin.
Abiraterone The serum concentration of Capsaicin can be increased when it is combined with Abiraterone.
Cyproterone acetate The metabolism of Capsaicin can be increased when combined with Cyproterone acetate.
Technetium Tc-99m tilmanocept Capsaicin may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Trospium The therapeutic efficacy of Trospium can be decreased when used in combination with Capsaicin.
Oxyphenonium The therapeutic efficacy of Oxyphenonium can be decreased when used in combination with Capsaicin.
Butabarbital The therapeutic efficacy of Butabarbital can be decreased when used in combination with Capsaicin.
Butalbital The risk or severity of methemoglobinemia can be increased when Butalbital is combined with Capsaicin.
Benzatropine The therapeutic efficacy of Benzatropine can be decreased when used in combination with Capsaicin.
Talbutal The therapeutic efficacy of Talbutal can be decreased when used in combination with Capsaicin.
Pentobarbital The risk or severity of methemoglobinemia can be increased when Pentobarbital is combined with Capsaicin.
Ipratropium The therapeutic efficacy of Ipratropium can be decreased when used in combination with Capsaicin.
Methadone The therapeutic efficacy of Methadone can be decreased when used in combination with Capsaicin.
Metixene The therapeutic efficacy of Metixene can be decreased when used in combination with Capsaicin.
Buclizine The therapeutic efficacy of Buclizine can be decreased when used in combination with Capsaicin.
Doxylamine The therapeutic efficacy of Doxylamine can be decreased when used in combination with Capsaicin.
Trihexyphenidyl The therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Capsaicin.
Oxyphencyclimine The therapeutic efficacy of Oxyphencyclimine can be decreased when used in combination with Capsaicin.
Procyclidine The therapeutic efficacy of Procyclidine can be decreased when used in combination with Capsaicin.
Profenamine The therapeutic efficacy of Profenamine can be decreased when used in combination with Capsaicin.
Hyoscyamine The therapeutic efficacy of Hyoscyamine can be decreased when used in combination with Capsaicin.
Cyproheptadine The therapeutic efficacy of Cyproheptadine can be decreased when used in combination with Capsaicin.
Methscopolamine bromide The therapeutic efficacy of Methscopolamine bromide can be decreased when used in combination with Capsaicin.
Metharbital The risk or severity of methemoglobinemia can be increased when Metharbital is combined with Capsaicin.
Tridihexethyl The therapeutic efficacy of Tridihexethyl can be decreased when used in combination with Capsaicin.
Triflupromazine The therapeutic efficacy of Triflupromazine can be decreased when used in combination with Capsaicin.
Dextromethorphan The therapeutic efficacy of Dextromethorphan can be decreased when used in combination with Capsaicin.
Anisotropine methylbromide The therapeutic efficacy of Anisotropine methylbromide can be decreased when used in combination with Capsaicin.
Amoxapine The therapeutic efficacy of Amoxapine can be decreased when used in combination with Capsaicin.
Lamotrigine The risk or severity of methemoglobinemia can be increased when Lamotrigine is combined with Capsaicin.
Atropine The therapeutic efficacy of Atropine can be decreased when used in combination with Capsaicin.
Thiopental The risk or severity of methemoglobinemia can be increased when Thiopental is combined with Capsaicin.
Nicardipine The therapeutic efficacy of Nicardipine can be decreased when used in combination with Capsaicin.
Mecamylamine The therapeutic efficacy of Mecamylamine can be decreased when used in combination with Capsaicin.
Pirenzepine The therapeutic efficacy of Pirenzepine can be decreased when used in combination with Capsaicin.
Homatropine methylbromide The therapeutic efficacy of Homatropine methylbromide can be decreased when used in combination with Capsaicin.
Scopolamine The therapeutic efficacy of Scopolamine can be decreased when used in combination with Capsaicin.
Isoflurane The therapeutic efficacy of Isoflurane can be decreased when used in combination with Capsaicin.
Benzquinamide The therapeutic efficacy of Benzquinamide can be decreased when used in combination with Capsaicin.
Clidinium The therapeutic efficacy of Clidinium can be decreased when used in combination with Capsaicin.
Propiomazine The therapeutic efficacy of Propiomazine can be decreased when used in combination with Capsaicin.
Propantheline The therapeutic efficacy of Propantheline can be decreased when used in combination with Capsaicin.
Dicyclomine The therapeutic efficacy of Dicyclomine can be decreased when used in combination with Capsaicin.
Biperiden The therapeutic efficacy of Biperiden can be decreased when used in combination with Capsaicin.
Brompheniramine The therapeutic efficacy of Brompheniramine can be decreased when used in combination with Capsaicin.
Methylphenobarbital The risk or severity of methemoglobinemia can be increased when Methylphenobarbital is combined with Capsaicin.
Amantadine The therapeutic efficacy of Amantadine can be decreased when used in combination with Capsaicin.
Methantheline The therapeutic efficacy of Methantheline can be decreased when used in combination with Capsaicin.
Hexafluronium The therapeutic efficacy of Hexafluronium can be decreased when used in combination with Capsaicin.
Cycrimine The therapeutic efficacy of Cycrimine can be decreased when used in combination with Capsaicin.
Desloratadine The therapeutic efficacy of Desloratadine can be decreased when used in combination with Capsaicin.
Glycopyrronium The therapeutic efficacy of Glycopyrronium can be decreased when used in combination with Capsaicin.
Tolterodine The therapeutic efficacy of Tolterodine can be decreased when used in combination with Capsaicin.
Oxybutynin The therapeutic efficacy of Oxybutynin can be decreased when used in combination with Capsaicin.
Promethazine The therapeutic efficacy of Promethazine can be decreased when used in combination with Capsaicin.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Diphenhydramine is combined with Capsaicin.
Pentolinium The therapeutic efficacy of Pentolinium can be decreased when used in combination with Capsaicin.

Target Protein

Transient receptor potential cation channel subfamily V member 1 TRPV1
Prohibitin-2 PHB2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 21852280
    Anand P, Bley K: Topical capsaicin for pain management: therapeutic potential and mechanisms of action of the new high-concentration capsaicin 8% patch. Br J Anaesth. 2011 Oct;107(4):490-502. doi: 10.1093/bja/aer260. Epub 2011 Aug 17.
  • PMID: 21158551
    Wallace M, Pappagallo M: Qutenza(R): a capsaicin 8% patch for the management of postherpetic neuralgia. Expert Rev Neurother. 2011 Jan;11(1):15-27. doi: 10.1586/ern.10.182.
  • PMID: 17959343
    Simpson DM, Estanislao L, Brown SJ, Sampson J: An open-label pilot study of high-concentration capsaicin patch in painful HIV neuropathy. J Pain Symptom Manage. 2008 Mar;35(3):299-306. Epub 2007 Oct 23.
  • PMID: 23023032
    O'Neill J, Brock C, Olesen AE, Andresen T, Nilsson M, Dickenson AH: Unravelling the mystery of capsaicin: a tool to understand and treat pain. Pharmacol Rev. 2012 Oct;64(4):939-71. doi: 10.1124/pr.112.006163.

Contoh Produk & Brand

Produk: 642 • International brands: 1
Produk
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    Patch • - • Topical • US
  • 2-Count HEAT PATCHES
    Patch • 0.025 g/100g • Topical • US • OTC
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    Patch • 0.025 g/100g • Topical • US • OTC
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    Patch • 0.025 g/100g • Topical • US • OTC
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    Patch • 0.25 g/1g • Topical • US • OTC
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Menampilkan 8 dari 642 produk.
International Brands
  • Zostrix

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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