Calcium Carbimide
Calcium Carbimide Uses, Dosage, Side Effects, Food Interaction and all others data.
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. 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.
Administration of calcium carbimide causes a syndrome characterized by intense flushing, rapid pulse, panting respiration and perception of acetaldehyde in the exhaled breath. This syndrome remains for a few hours after alcohol consumption and it stops completeley after 24 hours. This syndrome is caused by the accumulation of acetaldehyde and altered vascular reaction. Therefore, the more the alcohol consumption the more the adverse effects caused by acetaldehyde accumulation.
| Trade Name | Calcium Carbimide |
| Generic | Calcium carbimide |
| Calcium carbimide Other Names | Calcium carbimide, calcium cyanamide, carbimida calcica, carbimide calcique, Cyanamide calcique, Lime nitrogen, Lime-nitrogen, Nitrogen lime |
| Type | |
| Formula | CCaN2 |
| Weight | Average: 80.103 Monoisotopic: 79.9687389 |
| Protein binding | The metabolism and elimination of calcium carbimide is very rapid, which makes it unlikely to bind to plasma proteins. |
| Groups | Approved, Withdrawn |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Calcium Carbimide has not been approved by the FDA but the intended indication is for the treatment of alcoholism. This medication was marketed in Canada, United Kingdom and Europe under the trade name of Temposil for the sole use of alcoholism treatment.
How Calcium Carbimide works
Calcium Carbimide is a potent inhibitor of the aldehyde dehydrogenase. Ethanol is normally metabolized to acetaldehyde that is quickly metabolized because this molecule is toxic, thus it has to stay in very low quantities in the body. Carbimide performs its effect by being a competitive inhibitor of the hepatic aldehyde-NAD oxidoreductase dehydrogenase which is the enzyme responsible for the oxidation of acetaldehyde to water and acetate.
Toxicity
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.
Volume of Distribution
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. 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.
Elimination Route
It presents a very rapid absorption which has caused the presence of side effects as nausea, headache and vomiting. 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. In preclinical trials, peak plasma concentration occurred at 60 minutes after administration. 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.
Half Life
Calcium Carbimide is metabolized and eliminated very rapidly so the apparent half-life is of 92.4 minutes.
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.
Elimination Route
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.
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