Description

Simple

Clinical

Overview

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.[1] 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.[8]

Pharmacology

Indication

Calcium carbimide has not been approved by the FDA but the intended indication is for the treatment of alcoholism.[6] This medication was marketed in Canad... Read more

Pharmacodynamic

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 ca... Read more

Mechanism of action

Calcium carbimide is a potent inhibitor of the aldehyde dehydrogenase.[6] Ethanol is normally metabolized to acetaldehyde that is quickly metabolized becau... Read more

Absorption

It presents a very rapid absorption which has caused the presence of side effects as nausea, headache and vomiting.[9] The oral bioavailability of calcium carbimide depends on the administered dose which can vary from 50-81% o... Read more

Protein binding

The metabolism and elimination of calcium carbimide is very rapid, which makes it unlikely to bind to plasma proteins.

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.[ Read more

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.[ Read more

Half life

Calcium carbimide is metabolized and eliminated very rapidly so the apparent half-life is of 92.4 minutes.[9]

Route of elimination

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.[ Read more

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.[ Read more

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Calcium carbimide
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Chlorhexadol
The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Chlorhexadol.
Cinnamaldehyde
The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Cinnamaldehyde.
Disulfiram
The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Disulfiram.
Ethanol
The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Ethanol.
Formaldehyde
The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Formaldehyde.
Glutaral
The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Glutaral.
Malonaldehyde
The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Malonaldehyde.
P-Hydroxybenzaldehyde
The risk or severity of adverse effects can be increased when Calcium carbimide is combined with P-Hydroxybenzaldehyde.
Phenylacetaldehyde
The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Phenylacetaldehyde.
Phosphonoacetaldehyde
The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Phosphonoacetaldehyde.
Protocatechualdehyde
The risk or severity of adverse effects can be increased when Calcium carbimide is combined with Protocatechualdehyde.
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.
9 References
  1. 1 . 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.PubMed: 13316670
  2. 2 . 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.PubMed: 4888318
  3. 3 . 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.PubMed: 3358883
  4. 4 . 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.PubMed: 3426682
  5. 5 . 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.PubMed: 10826131
  6. 6 . Barh D., Dhawan D. and Ganguly NK. (2013). Omics for personalized medicine. Springer.
  7. 7 . Vasiliou V. and Petersen D. (2010). Comprehensive toxicology (2nd ed., pp. 131-147). Elsevier.
  8. 8 . Health Canada Link
  9. 9 . Encyclopedia Link