Peringatan Keamanan

Technetium-99m tetrofosmin has a very high safety margin in both single and repeated dose intravenous administration. It does not exhibit mutagenic potential in vitro and in vivo.^A31592 Reports have shown that technetium-99m tetrofosmin can cross the placenta thus, the possibility of pregnancy should be assessed.^L1147

Technetium Tc-99m tetrofosmin

DB09160

small molecule approved

Deskripsi

Technetium Tc-99m tetrofosmin is a drug used in nuclear myocardial perfusion imaging. The radioisotope, technetium-99m, is chelated by two 1,2-bisdi-(2-ethoxyethyl)phosphinoethane ligands which belong to the group of diphosphines and which are referred to as tetrofosmin. It is a lipophilic technetium phosphine dioxo cation that was formulated into a freeze-dried kit which yields an injection.^A31592 Technetium Tc-99m tetrofosmin was developed by GE Healthcare and FDA approved on February 9, 1996.

Struktur Molekul 2D

Berat 898.86

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) Technetium-99m tetrofosmin presents a very short half-life of 6.03 hours which is an advantage over other labeled radiopharmaceuticals.[A31592]

Volume Distribusi Reports have shown that it is possible to perform heart diagnosis and analysis as early as 5 minutes post-injection.[A31592] After absorption, technetium-99m tetrofosmin is accumulated in the myocardium, skeletal muscle, liver, spleen and kidneys. If administered during exercise, there is a sequestration of technetium-99m tetrofosmin by skeletal muscle due to increased flow in skeletal tissue.[L1147]

Klirens (Clearance) Technetium-99m tetrofosmin has a rapid clearance from the liver, lung and blood. The whole body clearance after 48 hours represents approximately 70% of the administered dose. Blood and plasma clearance follows an equal clearance profile in which at 10 min post injection there was less than 5% of the initial administered dose. The initial rate of urinary clearance accounts for 40% of the administered dose after 48 hours of the initial dose administration.[A31592]

Absorpsi

After intravenous admministration, technetium 99m tetrofosmin is taken up in the heart where the uptake is done by potential-driven diffusion of the lipophilic cationic complex accross the sarcolemmal and mitochondrial membranes.^L1146 The uptake in myocardium represents approximately 1.2% of the administered activity after 5 minutes of injection and this activity reduces to 1% at 2 hours. Once taken by the myocardium, there is a minimal redistribution in the following 3-4 hours.^L1147

Metabolisme

The liver activity post injection of technetium-99m tetrofosmin is very low and it decays over time.^L1147

Rute Eliminasi

The elimination of technetium-99m tetrofosmin is roughly the same for both fecal and urinary excretion and both account for apporximately 50% of the total excreted dose.^A31592 The washout from the heart is slow and it depends on the patient state being of 4% per hour at exercise and 0.6% at rest.^L1146 Complete elimination occurs after 48 hours. In this process, renal clearance accounts for approximately 40% of the administered dose in both rest and excercise; while fecal clearance accounts for 26-41% of the administered dose at rest and 17-34% of the administered dose after exercise.^L1147

Interaksi Obat

0 Data

Tidak ada data.

Referensi & Sumber

Artikel (PubMed)

PMID: 8418268
Higley B, Smith FW, Smith T, Gemmell HG, Das Gupta P, Gvozdanovic DV, Graham D, Hinge D, Davidson J, Lahiri A: Technetium-99m-1,2-bisbis(2-ethoxyethyl) phosphinoethane: human biodistribution, dosimetry and safety of a new myocardial perfusion imaging agent. J Nucl Med. 1993 Jan;34(1):30-8.

Textbook

Jadvar H. (2014). Cancer theranostics. Academic press.

Link

Contoh Produk & Brand

Produk: 0 • International brands: 0

Belum ada data produk/brand untuk obat ini pada database. Jalankan import DrugBank untuk mengisi field produk/brand.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.