Peringatan Keamanan

There are no data regarding overdosage with ceftobiprole medocaril. In cases of suspected overdose, discontinue therapy and institute general symptomatic and supportive treatment. Ceftobiprole can be removed from the circulation via hemodialysis, however no information is available on the use of hemodialysis to treat ceftobiprole overdose.^L50442

Ceftobiprole medocaril

DB14733

small molecule approved experimental investigational

Deskripsi

Ceftobiprole medocaril is a prodrug of ceftobiprole, a fifth-generation semisynthetic cephalosporin antibacterial. Ceftobiprole is a broad-spectrum agent with demonstrated activity against both Gram-positive and Gram-negative bacteria, including antibiotic-resistant strains of Staphylcoccus aureus (methicillin-resistant Staphylococcus aureus; MRSA).

The EMA's Committee for Medicinal Products for Human Use (CHMP) adopted a negative opinion of ceftobiprole medocaril in February 2010, recommending the refusal of its marketing authorization in the European Union primarily due to data quality issues in pivotal clinical studies.^L50467 It received its first approval in Canada in October 2017 for use in certain patients with bacterial pneumonia,^L50472 and was subsequently approved in the United States with additional indications for skin and skin structure infections and bacteremia in April 2024.L50442,L50457

Struktur Molekul 2D

Berat 690.66

Wujud solid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

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

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of active [ceftobiprole] following multiple-dose administration is approximately 3.3 hours.[L50442,L50472]

Volume Distribusi The steady-state volume of distribution of active [ceftobiprole] is 15.5-18.0 L, which approximates extracellular fluid volume in humans.[L50442,L50472]

Klirens (Clearance) The mean clearance of active [ceftobiprole] following multiple-dose administration is 4.98 L/h.[L50442,L50472]

Absorpsi

Because ceftobiprole medocaril is administered intravenously, its bioavailability is 100%.^L50472 The mean C_max and AUC_0-8h after multiple-dose administration are 33.0 µg/mL and 102 µg*h/mL, respectively.^L50472

Metabolisme

Conversion of prodrug ceftobiprole medocaril to the active moiety ceftobiprole occurs rapidly and is mediated by non-specific plasma esterases.^L50472 Ceftobiprole itself is minimally metabolized to a microbiologically inactive open-ring metabolite, which accounts for approximately 4% of the parent exposure in subject with a normal renal function.^L50472

Rute Eliminasi

Active ceftobiprole is eliminated primarily unchanged by renal excretion.^L50472 Approximately 89% of the administered dose is recovered in the urine as active ceftobiprole (83%), the open-ring metabolite (5%) and ceftobiprole medocaril (<1%).^L50472 Due to the significant degree of renal elimination, patients with renal impairment who are undergoing treatment with ceftobiprole may require lower doses.^L50442

Interaksi Obat

193 Data

BCG vaccine	The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Ceftobiprole medocaril.
Typhoid vaccine	The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Ceftobiprole medocaril.
Dicoumarol	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with Dicoumarol.
Phenindione	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with Phenindione.
Warfarin	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with Warfarin.
Phenprocoumon	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with Phenprocoumon.
Acenocoumarol	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with Acenocoumarol.
4-hydroxycoumarin	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with 4-hydroxycoumarin.
Coumarin	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with Coumarin.
(R)-warfarin	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with (R)-warfarin.
Ethyl biscoumacetate	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with Ethyl biscoumacetate.
Fluindione	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with Fluindione.
Clorindione	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with Clorindione.
Diphenadione	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with Diphenadione.
Tioclomarol	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with Tioclomarol.
(S)-Warfarin	The risk or severity of bleeding can be increased when Ceftobiprole medocaril is combined with (S)-Warfarin.
Vibrio cholerae CVD 103-HgR strain live antigen	The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Ceftobiprole medocaril.
Estetrol	The therapeutic efficacy of Estetrol can be decreased when used in combination with Ceftobiprole medocaril.
Probenecid	The serum concentration of Ceftobiprole medocaril can be increased when it is combined with Probenecid.
Lepirudin	The therapeutic efficacy of Lepirudin can be decreased when used in combination with Ceftobiprole medocaril.
Bivalirudin	The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Ceftobiprole medocaril.
Alteplase	The therapeutic efficacy of Alteplase can be decreased when used in combination with Ceftobiprole medocaril.
Urokinase	The therapeutic efficacy of Urokinase can be decreased when used in combination with Ceftobiprole medocaril.
Reteplase	The therapeutic efficacy of Reteplase can be decreased when used in combination with Ceftobiprole medocaril.
Anistreplase	The therapeutic efficacy of Anistreplase can be decreased when used in combination with Ceftobiprole medocaril.
Tenecteplase	The therapeutic efficacy of Tenecteplase can be decreased when used in combination with Ceftobiprole medocaril.
Abciximab	The therapeutic efficacy of Abciximab can be decreased when used in combination with Ceftobiprole medocaril.
Drotrecogin alfa	The therapeutic efficacy of Drotrecogin alfa can be decreased when used in combination with Ceftobiprole medocaril.
Streptokinase	The therapeutic efficacy of Streptokinase can be decreased when used in combination with Ceftobiprole medocaril.
Argatroban	The therapeutic efficacy of Argatroban can be decreased when used in combination with Ceftobiprole medocaril.
Ardeparin	The therapeutic efficacy of Ardeparin can be decreased when used in combination with Ceftobiprole medocaril.
Fondaparinux	The therapeutic efficacy of Fondaparinux can be decreased when used in combination with Ceftobiprole medocaril.
Pentosan polysulfate	The therapeutic efficacy of Pentosan polysulfate can be decreased when used in combination with Ceftobiprole medocaril.
Edetic acid	The therapeutic efficacy of Edetic acid can be decreased when used in combination with Ceftobiprole medocaril.
Dipyridamole	The therapeutic efficacy of Dipyridamole can be decreased when used in combination with Ceftobiprole medocaril.
Heparin	The therapeutic efficacy of Heparin can be decreased when used in combination with Ceftobiprole medocaril.
Enoxaparin	The therapeutic efficacy of Enoxaparin can be decreased when used in combination with Ceftobiprole medocaril.
Epoprostenol	The therapeutic efficacy of Epoprostenol can be decreased when used in combination with Ceftobiprole medocaril.
Ximelagatran	The therapeutic efficacy of Ximelagatran can be decreased when used in combination with Ceftobiprole medocaril.
Desmoteplase	The therapeutic efficacy of Desmoteplase can be decreased when used in combination with Ceftobiprole medocaril.
Defibrotide	The therapeutic efficacy of Defibrotide can be decreased when used in combination with Ceftobiprole medocaril.
Ancrod	The therapeutic efficacy of Ancrod can be decreased when used in combination with Ceftobiprole medocaril.
Beraprost	The therapeutic efficacy of Beraprost can be decreased when used in combination with Ceftobiprole medocaril.
SR-123781A	The therapeutic efficacy of SR-123781A can be decreased when used in combination with Ceftobiprole medocaril.
Prasugrel	The therapeutic efficacy of Prasugrel can be decreased when used in combination with Ceftobiprole medocaril.
Rivaroxaban	The therapeutic efficacy of Rivaroxaban can be decreased when used in combination with Ceftobiprole medocaril.
Sulodexide	The therapeutic efficacy of Sulodexide can be decreased when used in combination with Ceftobiprole medocaril.
Semuloparin	The therapeutic efficacy of Semuloparin can be decreased when used in combination with Ceftobiprole medocaril.
Idraparinux	The therapeutic efficacy of Idraparinux can be decreased when used in combination with Ceftobiprole medocaril.
Cangrelor	The therapeutic efficacy of Cangrelor can be decreased when used in combination with Ceftobiprole medocaril.
Astaxanthin	The therapeutic efficacy of Astaxanthin can be decreased when used in combination with Ceftobiprole medocaril.
Apixaban	The therapeutic efficacy of Apixaban can be decreased when used in combination with Ceftobiprole medocaril.
Otamixaban	The therapeutic efficacy of Otamixaban can be decreased when used in combination with Ceftobiprole medocaril.
Amediplase	The therapeutic efficacy of Amediplase can be decreased when used in combination with Ceftobiprole medocaril.
Dabigatran etexilate	The therapeutic efficacy of Dabigatran etexilate can be decreased when used in combination with Ceftobiprole medocaril.
Danaparoid	The therapeutic efficacy of Danaparoid can be decreased when used in combination with Ceftobiprole medocaril.
Dalteparin	The therapeutic efficacy of Dalteparin can be decreased when used in combination with Ceftobiprole medocaril.
Tinzaparin	The therapeutic efficacy of Tinzaparin can be decreased when used in combination with Ceftobiprole medocaril.
Nadroparin	The therapeutic efficacy of Nadroparin can be decreased when used in combination with Ceftobiprole medocaril.
Triflusal	The therapeutic efficacy of Triflusal can be decreased when used in combination with Ceftobiprole medocaril.
Ticagrelor	The therapeutic efficacy of Ticagrelor can be decreased when used in combination with Ceftobiprole medocaril.
Ditazole	The therapeutic efficacy of Ditazole can be decreased when used in combination with Ceftobiprole medocaril.
Vorapaxar	The therapeutic efficacy of Vorapaxar can be decreased when used in combination with Ceftobiprole medocaril.
Edoxaban	The therapeutic efficacy of Edoxaban can be decreased when used in combination with Ceftobiprole medocaril.
Sodium citrate	The therapeutic efficacy of Sodium citrate can be decreased when used in combination with Ceftobiprole medocaril.
Dextran	The therapeutic efficacy of Dextran can be decreased when used in combination with Ceftobiprole medocaril.
Bemiparin	The therapeutic efficacy of Bemiparin can be decreased when used in combination with Ceftobiprole medocaril.
Reviparin	The therapeutic efficacy of Reviparin can be decreased when used in combination with Ceftobiprole medocaril.
Parnaparin	The therapeutic efficacy of Parnaparin can be decreased when used in combination with Ceftobiprole medocaril.
Desirudin	The therapeutic efficacy of Desirudin can be decreased when used in combination with Ceftobiprole medocaril.
Antithrombin Alfa	The therapeutic efficacy of Antithrombin Alfa can be decreased when used in combination with Ceftobiprole medocaril.
Protein C	The therapeutic efficacy of Protein C can be decreased when used in combination with Ceftobiprole medocaril.
Antithrombin III human	The therapeutic efficacy of Antithrombin III human can be decreased when used in combination with Ceftobiprole medocaril.
Letaxaban	The therapeutic efficacy of Letaxaban can be decreased when used in combination with Ceftobiprole medocaril.
Darexaban	The therapeutic efficacy of Darexaban can be decreased when used in combination with Ceftobiprole medocaril.
Betrixaban	The therapeutic efficacy of Betrixaban can be decreased when used in combination with Ceftobiprole medocaril.
Nafamostat	The therapeutic efficacy of Nafamostat can be decreased when used in combination with Ceftobiprole medocaril.
Monteplase	The therapeutic efficacy of Monteplase can be decreased when used in combination with Ceftobiprole medocaril.
Gabexate	The therapeutic efficacy of Gabexate can be decreased when used in combination with Ceftobiprole medocaril.
Troxerutin	The therapeutic efficacy of Troxerutin can be decreased when used in combination with Ceftobiprole medocaril.
Protein S human	The therapeutic efficacy of Protein S human can be decreased when used in combination with Ceftobiprole medocaril.
Brinase	The therapeutic efficacy of Brinase can be decreased when used in combination with Ceftobiprole medocaril.
Melagatran	The therapeutic efficacy of Melagatran can be decreased when used in combination with Ceftobiprole medocaril.
Saruplase	The therapeutic efficacy of Saruplase can be decreased when used in combination with Ceftobiprole medocaril.
Tocopherylquinone	The therapeutic efficacy of Tocopherylquinone can be decreased when used in combination with Ceftobiprole medocaril.
Dabigatran	The therapeutic efficacy of Dabigatran can be decreased when used in combination with Ceftobiprole medocaril.
Dermatan sulfate	The therapeutic efficacy of Dermatan sulfate can be decreased when used in combination with Ceftobiprole medocaril.
Disulfiram	The risk or severity of adverse effects can be increased when Ceftobiprole medocaril is combined with Disulfiram.
Furosemide	Furosemide may decrease the excretion rate of Ceftobiprole medocaril which could result in a higher serum level.
Lidocaine	The risk or severity of methemoglobinemia can be increased when Ceftobiprole medocaril is combined with Lidocaine.
Ropivacaine	The risk or severity of methemoglobinemia can be increased when Ceftobiprole medocaril is combined with Ropivacaine.
Bupivacaine	The risk or severity of methemoglobinemia can be increased when Ceftobiprole medocaril is combined with Bupivacaine.
Cinchocaine	The risk or severity of methemoglobinemia can be increased when Ceftobiprole medocaril is combined with Cinchocaine.
Dyclonine	The risk or severity of methemoglobinemia can be increased when Ceftobiprole medocaril is combined with Dyclonine.
Procaine	The risk or severity of methemoglobinemia can be increased when Ceftobiprole medocaril is combined with Procaine.
Prilocaine	The risk or severity of methemoglobinemia can be increased when Ceftobiprole medocaril is combined with Prilocaine.
Proparacaine	The risk or severity of methemoglobinemia can be increased when Ceftobiprole medocaril is combined with Proparacaine.
Meloxicam	The risk or severity of methemoglobinemia can be increased when Ceftobiprole medocaril is combined with Meloxicam.
Oxybuprocaine	The risk or severity of methemoglobinemia can be increased when Ceftobiprole medocaril is combined with Oxybuprocaine.
Cocaine	The risk or severity of methemoglobinemia can be increased when Ceftobiprole medocaril is combined with Cocaine.

Target Protein

MecA mecA

Penicillin-binding protein 2B penA

Penicillin-binding protein 2X pbpX

Referensi & Sumber

Synthesis reference: Kremminger P, Ludescher J, Sturm H. Sandoz AG. " Method for the production of ceftobiprole medocaril." US Patent US20120116070A1. May 10, 2012.

Link

Contoh Produk & Brand

Produk: 2 • International brands: 0

Produk

Zeftera

Powder, for solution • 500 mg / vial • Intravenous • Canada • Approved
Zevtera

Powder, for solution • 500 mg / vial • Intravenous • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.