| 词条 | Bromelain (pharmacology) |
| 释义 |
| IUPAC_name = | image = | alt = | caption = | tradename = NexoBrid | Drugs.com = {{Drugs.com|UK|nexobrid}} | MedlinePlus = | pregnancy_AU = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_CA = | legal_UK = POM | legal_US = | legal_status = Rx-only | routes_of_administration = Locally onto the wound | bioavailability = Depends on wound surface and depth | protein_bound = ~50% (bromelain) | metabolism = | onset = | elimination_half-life = 11.7±3.5 (8.5–19.9) hrs | excretion = | CAS_number = | ATCvet = | ATC_prefix = D03 | ATC_suffix = BA03 | PubChem = | DrugBank = | ChemSpiderID = none | chemical_formula = Varies }} A concentrate of proteolytic enzymes from the pineapple plant enriched in bromelain is approved in Europe for the debridement (removal of eschar, that is dead and damaged tissue) of severe burn wounds under the trade name NexoBrid.[1] In the US, it has completed Phase III clinical trials and has the tentative trade name Debrase. It was developed by MediWound, Germany; and Teva is responsible for development and marketing in the US.[2] The medicine has been granted orphan drug status by the European Medicines Agency (EMA).[3] Medical usesThe medication is approved for burns of degrees IIb, i.e. deep partial skin thickness burns, to III, i.e. full thickness burns, and has been shown to significantly reduce the necessity of surgical debridement (15% versus 63% under standard treatment) and skin transplants (18% versus 34%) in a randomized controlled trial.[3][4] The concentrate is solved in a sterile gel basis, applied onto the burn wound, covered with a wound dressing, and removed after four hours. The healthy surrounding skin has to be protected with a sterile paraffin ointment. The EMA recommends that the treatment should be used in only hospitals having specialised burns centres.[1] Contraindications and adverse effectsPredictably, the bromelain gel is contraindicated in persons allergic to pineapple or the enzyme papain.[1] The most common side-effects are fever (19% of patients in studies) and local pain (3.6%). Wound infections occur no more frequently than under standard treatment.[1] InteractionsThe enzymes in NexoBrid inhibit the liver enzymes CYP2C8 and CYP2C9 when ingested. These are involved in the breaking down of a number of drugs, including amiodarone, chloroquine, ibuprofen, and warfarin. It is not known whether this mechanism has any clinical relevance.[5] PharmacokineticsDepending on the surface area and depth of the wound, bromelain blood serum concentrations of no more than 40 µg/ml are expected, with peak concentrations reached after 2 to 4 hours. The terminal half-life varied between 8.5 and 19.9 hours in studies. These data have been obtained from 15 patients with comparatively shallow wounds.[3][5] ChemistryThe medication is extracted from the stem of the pineapple plant (Ananas comosus)[5] by a standardised process, and each lot has to be analysed for its chemical composition. It contains a mixture of proteolytic enzymes, the main compound being stem bromelain. Bromelain is thought to be the active ingredient, but this has not been determined in studies.[3] The gel basis contains water, polyacrylic acid as a gelling agent, and a disodium hydrogen phosphate/sodium hydroxide buffer.[3] References1. ^1 2 3 {{cite web|url=http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/human/002246/WC500136583.pdf|title=EPAR summary for the public: NexoBrid|publisher=European Medicines Agency|date=December 2012}} {{Preparations for treatment of wounds and ulcers}}2. ^{{cite web|url=http://www.ukmi.nhs.uk/applications/ndo/record_view_open.asp?newDrugID=5823|title=New Drugs Online Report for bromelain|publisher=Uk Medicines Information|accessdate=28 March 2015}} 3. ^1 2 3 4 {{cite journal| author = A. Klement| date = 2 February 2015| title = NexoBrid| journal = Österreichische Apothekerzeitung| issue = 3/2015| pages = 10f| language = German}} 4. ^{{Cite journal| pmid = 24074719| year = 2014| author1 = Rosenberg| first1 = L| title = A novel rapid and selective enzymatic debridement agent for burn wound management: A multi-center RCT| journal = Burns| volume = 40| issue = 3| pages = 466–74| last2 = Krieger| first2 = Y| last3 = Bogdanov-Berezovski| first3 = A| last4 = Silberstein| first4 = E| last5 = Shoham| first5 = Y| last6 = Singer| first6 = A. J.| doi = 10.1016/j.burns.2013.08.013}} 5. ^1 2 {{cite web|url=http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002246/WC500136580.pdf|title=Summary of Product Characteristics: NexoBrid|publisher=European Medicines Agency}} 3 : Preparations for treatment of wounds and ulcers|Hydrolases|Orphan drugs |
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