Peringatan Keamanan

Overdosage may increase pharmacologic and adverse effects or cause death.

IV LD₅₀=53 mg/kg (mice), 42 mg/kg (rats). Oral LD₅₀ (as a solution in soybean oil)=1230 mg/kg (mice), 600 mg/kg (rats)

Propofol

DB00818

small molecule approved investigational vet_approved

Deskripsi

Propofol is an intravenous anaesthetic agent used for induction and maintenance of general anaesthesia. IV administration of propfol is used to induce unconsciousness after which anaesthesia may be maintained using a combination of medications. Recovery from propofol-induced anaesthesia is generally rapid and associated with less frequent side effects (e.g. drowsiness, nausea, vomiting) than with thiopental, methohexital, and etomidate. Propofol may be used prior to diagnostic procedures requiring anaesthesia, in the management of refractory status epilepticus, and for induction and/or maintenance of anaesthesia prior to and during surgeries.

Struktur Molekul 2D

Berat 178.2707

Wujud liquid

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) Initial distribution phase t1/2α=1.8-9.5 minutes. Second redistirubtion phase t1/2β=21-70 minutes. Terminal elimination phase t1/2γ=1.5-31 hours.

Volume Distribusi * 60 L/kg [healthy adults]

Klirens (Clearance) * 23 - 50 mL/kg/min * 1.6 - 3.4 L/min [70 Kg adults]

Absorpsi

Rapid - time to onset of unconsciousness is 15-30 seconds, due to rapid distribution from plasma to the CNS. Distribution is so rapid that peak plasma concentrations cannot be readily measured. Duration of action is 5-10 minutes.

Metabolisme

Hepatically metabolized mainly by glucuronidation at the C1-hydroxyl. Hydroxylation of the benzene ring to 4-hydroxypropofol may also occur via CYP2B6 and 2C9 with subsequent conjugation to sulfuric and/or glucuronic acid. Hydroxypropofol has approximately 1/3 of hypnotic activity of propofol.

Rute Eliminasi

It is chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney.

Interaksi Obat

1725 Data

Duloxetine	The risk or severity of orthostatic hypotension and syncope can be increased when Propofol is combined with Duloxetine.
Levodopa	The risk or severity of hypotension and orthostatic hypotension can be increased when Propofol is combined with Levodopa.
Risperidone	Propofol may increase the hypotensive activities of Risperidone.
Lomitapide	The metabolism of Lomitapide can be decreased when combined with Propofol.
Ramipril	Propofol may decrease the antihypertensive activities of Ramipril.
Remikiren	Propofol may decrease the antihypertensive activities of Remikiren.
Bethanidine	Propofol may decrease the antihypertensive activities of Bethanidine.
Guanadrel	Propofol may decrease the antihypertensive activities of Guanadrel.
Olmesartan	Propofol may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone	Propofol may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside	Propofol may decrease the antihypertensive activities of Nitroprusside.
Atenolol	Propofol may decrease the antihypertensive activities of Atenolol.
Bendroflumethiazide	Propofol may decrease the antihypertensive activities of Bendroflumethiazide.
Fosinopril	Propofol may decrease the antihypertensive activities of Fosinopril.
Trandolapril	Propofol may decrease the antihypertensive activities of Trandolapril.
Metolazone	Propofol may decrease the antihypertensive activities of Metolazone.
Benazepril	Propofol may decrease the antihypertensive activities of Benazepril.
Cyclothiazide	Propofol may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril	Propofol may decrease the antihypertensive activities of Candoxatril.
Mecamylamine	Propofol may decrease the antihypertensive activities of Mecamylamine.
Phentolamine	Propofol may decrease the antihypertensive activities of Phentolamine.
Lisinopril	Propofol may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin	Propofol may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide	Propofol may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine	Propofol may decrease the antihypertensive activities of Cryptenamine.
Perindopril	Propofol may decrease the antihypertensive activities of Perindopril.
Tolazoline	Propofol may decrease the antihypertensive activities of Tolazoline.
Fenoldopam	Propofol may decrease the antihypertensive activities of Fenoldopam.
Chlorothiazide	Propofol may decrease the antihypertensive activities of Chlorothiazide.
Quinapril	Propofol may decrease the antihypertensive activities of Quinapril.
Omapatrilat	Propofol may decrease the antihypertensive activities of Omapatrilat.
Phenoxybenzamine	Propofol may decrease the antihypertensive activities of Phenoxybenzamine.
Telmisartan	Propofol may decrease the antihypertensive activities of Telmisartan.
Trichlormethiazide	Propofol may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine	Propofol may decrease the antihypertensive activities of Deserpidine.
Pentolinium	Propofol may decrease the antihypertensive activities of Pentolinium.
Trimethaphan	Propofol may decrease the antihypertensive activities of Trimethaphan.
Diazoxide	Propofol may decrease the antihypertensive activities of Diazoxide.
Terazosin	Propofol may decrease the antihypertensive activities of Terazosin.
Guanethidine	Propofol may decrease the antihypertensive activities of Guanethidine.
Rescinnamine	Propofol may decrease the antihypertensive activities of Rescinnamine.
Epoprostenol	Propofol may decrease the antihypertensive activities of Epoprostenol.
Hydralazine	Propofol may decrease the antihypertensive activities of Hydralazine.
Bevantolol	Propofol may decrease the antihypertensive activities of Bevantolol.
Practolol	Propofol may decrease the antihypertensive activities of Practolol.
Polythiazide	Propofol may decrease the antihypertensive activities of Polythiazide.
Cilazapril	Propofol may decrease the antihypertensive activities of Cilazapril.
Saprisartan	Propofol may decrease the antihypertensive activities of Saprisartan.
Spirapril	Propofol may decrease the antihypertensive activities of Spirapril.
Dexpropranolol	Propofol may decrease the antihypertensive activities of Dexpropranolol.
Nebivolol	Propofol may decrease the antihypertensive activities of Nebivolol.
Diethylnorspermine	Propofol may decrease the antihypertensive activities of Diethylnorspermine.
Pinacidil	Propofol may decrease the antihypertensive activities of Pinacidil.
Temocapril	Propofol may decrease the antihypertensive activities of Temocapril.
Macitentan	Propofol may decrease the antihypertensive activities of Macitentan.
Indoramin	Propofol may decrease the antihypertensive activities of Indoramin.
Aliskiren	Propofol may decrease the antihypertensive activities of Aliskiren.
Trimazosin	Propofol may decrease the antihypertensive activities of Trimazosin.
Moxonidine	Propofol may decrease the antihypertensive activities of Moxonidine.
Rauwolfia serpentina root	Propofol may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat	Propofol may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7	Propofol may decrease the antihypertensive activities of Angiotensin 1-7.
Rilmenidine	Propofol may decrease the antihypertensive activities of Rilmenidine.
Imidapril	Propofol may decrease the antihypertensive activities of Imidapril.
BQ-123	Propofol may decrease the antihypertensive activities of BQ-123.
Naftopidil	Propofol may decrease the antihypertensive activities of Naftopidil.
Landiolol	Propofol may decrease the antihypertensive activities of Landiolol.
Zofenopril	Propofol may decrease the antihypertensive activities of Zofenopril.
Guanoxan	Propofol may decrease the antihypertensive activities of Guanoxan.
Delapril	Propofol may decrease the antihypertensive activities of Delapril.
Vincamine	Propofol may decrease the antihypertensive activities of Vincamine.
Linsidomine	Propofol may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz	Propofol may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine	Propofol may decrease the antihypertensive activities of Tolonidine.
Endralazine	Propofol may decrease the antihypertensive activities of Endralazine.
Esatenolol	Propofol may decrease the antihypertensive activities of Esatenolol.
Cadralazine	Propofol may decrease the antihypertensive activities of Cadralazine.
Cloranolol	Propofol may decrease the antihypertensive activities of Cloranolol.
Cyclopenthiazide	Propofol may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine	Propofol may decrease the antihypertensive activities of Bietaserpine.
Guanazodine	Propofol may decrease the antihypertensive activities of Guanazodine.
Methoserpidine	Propofol may decrease the antihypertensive activities of Methoserpidine.
Epanolol	Propofol may decrease the antihypertensive activities of Epanolol.
Guanoclor	Propofol may decrease the antihypertensive activities of Guanoclor.
Muzolimine	Propofol may decrease the antihypertensive activities of Muzolimine.
Xipamide	Propofol may decrease the antihypertensive activities of Xipamide.
Dexniguldipine	Propofol may decrease the antihypertensive activities of Dexniguldipine.
Tocopherylquinone	Propofol may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat	Propofol may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat	Propofol may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat	Propofol may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat	Propofol may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat	Propofol may decrease the antihypertensive activities of Quinaprilat.
Prazosin	Propofol may decrease the antihypertensive activities of Prazosin.
Bisoprolol	Propofol may decrease the antihypertensive activities of Bisoprolol.
Tadalafil	Propofol may decrease the antihypertensive activities of Tadalafil.
Nadolol	Propofol may decrease the antihypertensive activities of Nadolol.
Debrisoquine	Propofol may decrease the antihypertensive activities of Debrisoquine.
Ambrisentan	Propofol may decrease the antihypertensive activities of Ambrisentan.
Amlodipine	The metabolism of Propofol can be decreased when combined with Amlodipine.

Target Protein

Gamma-aminobutyric acid receptor subunit beta-2 GABRB2

Gamma-aminobutyric acid receptor subunit beta-3 GABRB3

GABA(A) Receptor GABRA1

Sodium channel protein type 4 subunit alpha SCN4A

Sodium channel protein type 2 subunit alpha SCN2A

Referensi & Sumber

Synthesis reference: John R. Carpenter, "Propofol-based anesthetic and method of making same." U.S. Patent US6150423, issued May, 1977.

Artikel (PubMed)

PMID: 12904852
Vasile B, Rasulo F, Candiani A, Latronico N: The pathophysiology of propofol infusion syndrome: a simple name for a complex syndrome. Intensive Care Med. 2003 Sep;29(9):1417-25. Epub 2003 Aug 6.
PMID: 18326136
Ke JJ, Zhan J, Feng XB, Wu Y, Rao Y, Wang YL: A comparison of the effect of total intravenous anaesthesia with propofol and remifentanil and inhalational anaesthesia with isoflurane on the release of pro- and anti-inflammatory cytokines in patients undergoing open cholecystectomy. Anaesth Intensive Care. 2008 Jan;36(1):74-8.
PMID: 18298873
Hong JY, Kang YS, Kil HK: Anaesthesia for day case excisional breast biopsy: propofol-remifentanil compared with sevoflurane-nitrous oxide. Eur J Anaesthesiol. 2008 Jun;25(6):460-7. doi: 10.1017/S026502150800375X. Epub 2008 Feb 26.

Link

FDA Approved Drug Products: DIPRIVAN (propofol) injectable emulsion for intravenous use

Contoh Produk & Brand

Produk: 62 • International brands: 30

Produk

Anesthesia S/I-40

Injection, emulsion; Kit • - • Intravenous; Topical • US • Approved
Anesthesia S/I-50

Injection, emulsion; Kit • - • Intravenous; Topical • US • Approved
Anesthesia S/I-60

Injection, emulsion; Kit • - • Intravenous; Topical • US • Approved
Diprivan

Injection, emulsion • 10 mg/1mL • Intravenous • US • Approved
Diprivan

Injection, emulsion • 10 mg/1mL • Intravenous • US • Approved
Diprivan

Injection, emulsion • 10 mg/1mL • Intravenous • US • Approved
Diprivan

Injection, emulsion • 10 mg/1mL • Intravenous • US • Approved
Diprivan 1%

Emulsion • 10 mg / mL • Intravenous • Canada • Approved

Menampilkan 8 dari 62 produk.

International Brands

Anepol — Ha Na Pharm
Anespro — Behrens
Anesvan — Chi Sheng
Critifol — Abbott
Disoprivan — AstraZeneca
Disoprofol
Dormofol — Actavis
Fresofol — Boryung
Gobbifol — Gobbi
Hipnolam — AC Farma

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.