Peringatan Keamanan

Calcium carbimide presents antithyroid activity which can be of clinical relevance in patients with preexisting hypothyroid disease. It can also present some other minor side effects as fatigue, skin rash, ear ringing, mild depression, increased urination and impotence.^L1114

Calcium carbimide

DB09116

small molecule approved withdrawn

Deskripsi

Calcium carbimide, sold as the citrate salt, is an alcohol-sensitizing agent. Its effects are similar to the drug disulfiram (Antabuse) in that it interferes with the normal metabolism of alcohol by preventing the breakdown of the metabolic product acetaldehyde. Calcium carbimide was conceived as an alternative for the treatment of alcoholism with a reduced side effect profile either when it is consumed accompanied by alcohol or without it.^A31516 This drug was developed by Lederle Cyanamid Canada Inc and approved for marketing in Canada in 1959. The current status of calcium carbimide is cancelled post marketing.^L1113

Struktur Molekul 2D

Berat 80.103

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) Calcium carbimide is metabolized and eliminated very rapidly so the apparent half-life is of 92.4 minutes.[L1114]

Volume Distribusi The apparent volume of distribution of ethanol in the presence of calcium carbimide is 0.64 l/kg compared to 0.68 l/kg when administered in the absence of any drug.[A31520] All the reports studying the pharmacokinetic profile of ethanol after administered with calcium carbimide agree with a reduced volume of distribution driven by the effect of calcium carbimide.

Klirens (Clearance) After intravenous administration of calcium carbimide, there was a two compartment pharmacokinetic profile with a total plasma clearance rate ranging from 0.0123 to 0.0190 L/kg min.[A31522]

Absorpsi

It presents a very rapid absorption which has caused the presence of side effects as nausea, headache and vomiting.^L1114 The oral bioavailability of calcium carbimide depends on the administered dose which can vary from 50-81% on a dose of 0.3-1.5 mg/kg respectively.T74 In preclinical trials, peak plasma concentration occurred at 60 minutes after administration.^L1114 The values of Cmax, AUC and T max of calcium carbimide of a dose of 1.5 mg/kg were 1.65 mcg/ml, 77.86 mcg/mg min and 12 minutes respectively.^A31522

Metabolisme

The activity of calcium carbimide requires an initial metabolic transformation to the bioactive form. The transformation requires the activity of catalase and the presence of H2O2 for the formation of N-hydroxycyanamide. This bioactive compound will later spontaneosly decompose into cyanide and nitroxyl. The nitroxyl component will be the direct inhibitor of the aldehyde dehydrogenase.T75

Rute Eliminasi

The rate of elimination of ethanol when calcium carbimide is administered tends to be around 5% slower than the one presented in patients without any treatment. In the presence of calcium carbimide, the blood levels of acetaldehyde were increased from 1.7-6.5 microM to 40-242 microM.^A31521

Interaksi Obat

13 Data

Ethanol	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Ethanol.
Disulfiram	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Disulfiram.
Chlorhexadol	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Chlorhexadol.
Phenylacetaldehyde	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Phenylacetaldehyde.
Malonaldehyde	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Malonaldehyde.
Phosphonoacetaldehyde	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Phosphonoacetaldehyde.
Glutaral	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Glutaral.
P-Hydroxybenzaldehyde	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with P-Hydroxybenzaldehyde.
Pyruvaldehyde	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Pyruvaldehyde.
Tucaresol	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Tucaresol.
Cinnamaldehyde	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Cinnamaldehyde.
Formaldehyde	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Formaldehyde.
Protocatechualdehyde	The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Protocatechualdehyde.

Target Protein

Aldehyde dehydrogenase family 3 member B2 ALDH3B2

Aldehyde dehydrogenase, mitochondrial ALDH2

Aldehyde dehydrogenase X, mitochondrial ALDH1B1

Aldehyde dehydrogenase 1A1 ALDH1A1

Referensi & Sumber

Artikel (PubMed)

PMID: 13316670
ARMSTRONG JD, KERR HT: A new protective drug in the treatment of alcoholism; preliminary clinical trial of citrated calcium carbimide. Can Med Assoc J. 1956 May 15;74(10):795-7.
PMID: 4888318
Mukasa H, Arikawa K: A new double medication method for the treatment of alcoholism using the drug cyanamide. Kurume Med J. 1968;15(3):137-43.
PMID: 3358883
Jones AW, Neiman J, Hillbom M: Concentration-time profiles of ethanol and acetaldehyde in human volunteers treated with the alcohol-sensitizing drug, calcium carbimide. Br J Clin Pharmacol. 1988 Feb;25(2):213-21.
PMID: 3426682
Jones AW, Neiman J, Hillbom M: Elimination kinetics of ethanol and acetaldehyde in healthy men during the calcium carbimide-alcohol flush reaction. Alcohol Alcohol Suppl. 1987;1:213-7.
PMID: 10826131
Colom H, Prunonosa J, Peraire C, Domenech J, Azcona O, Torrent J, Obach R: Absolute bioavailability and absorption profile of cyanamide in man. J Pharmacokinet Biopharm. 1999 Aug;27(4):421-36.

Textbook

Barh D., Dhawan D. and Ganguly NK. (2013). Omics for personalized medicine. Springer.
Vasiliou V. and Petersen D. (2010). Comprehensive toxicology (2nd ed., pp. 131-147). Elsevier.

Link

Contoh Produk & Brand

Produk: 1 • International brands: 0

Produk

Temposil Tab 50mg

Tablet • 50 mg / tab • Oral • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.