Monograph
C07AG02 - Carvedilol |
Propably not porphyrinogenic |
PNP |
Side effects
Common adverse reactions of carvedilol that can be confused with an acute porphyric attack are nausea, diarrhoea, vomiting and abdominal pains. These side effects may potentially be porphyrinogenic if leading to a decrease in carbohydrate intake.
Other common adverse reactions are bronchitis, pneumonia, upper respiratory tract infections and urinary infections. Since infections might trigger an acute porphyric attack, vigilance regarding signs and symptoms of an infection and/ or a porphyric attack is recommended.
Rationale
Carvedilol is not suspected to be an inducer or a mechanism-based inhibitor of CYP enzymes, and is not observed to alter the metabolism of other CYP metabolized drugs.
Chemical description
Carbazole
Therapeutic characteristics
Carvedilol is a combined α- and β-adrenergic receptor blocker indicated for the treatment of essential hypertension, chronic stable angina pectoris and chronic stable heart failure.
It is administered orally.
Metabolism and pharmacokinetics
Carvedilol is extensively metabolized in the liver by several CYP450 enzymes and glucuronidation. The CYP enzymes involved are mainly CYP2C9 and 2D6, with minor contribution from CYP3A4, 2C19, 1A2 and 2E1 (Oldham 1997, uptodate).
Carvedilol was found to be a moderate activator of hCAR, but was not found to be an inducer of CYP2B6 (Lynch 2012). No drug-drug interactions involving CYP450 enzymes are reported (interaktionsdatabasen.dk).
Carvedilol is not suspected to be an inducer or a mechanism-based inhibitor of CYP450 enzymes (Hisaka 2010, Isoherranen 2009, Pelkonen 2008).
IPNet drug reports
Uneventful use reported in 5 patients with acute porphyria.
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Prediction of pharmacokinetic drug-drug interaction caused by changes in cytochrome P450 activity using in vivo information.
Hisaka A, Ohno Y, et al. Pharmacol Ther. 2010 Feb;125(2):230-48. |
|
| 2. | Qualitative analysis of the role of metabolites in inhibitory drug-drug interactions: literature evaluation based on the metabolism and transport drug interaction database.
Isoherranen N, Hachad H, et al. Chem Res Toxicol. 2009 Feb;22(2):294-8. |
|
| 3. | Identification of novel activators of constitutive androstane receptor from FDA-approved drugs by integrated computational and biological approaches.
Lynch C, Pan Y, et al. Pharm Res. 2013 Feb;30(2):489-501. |
23090669 |
| 4. | In vitro identification of the human cytochrome P450 enzymes involved in the metabolism of R(+)- and S(-)-carvedilol.
Oldham HG, Clarke SE. Drug Metab Dispos. 1997 Aug;25(8):970-7. |
|
| 5. | Inhibition and induction of human cytochrome P450 enzymes: current status.
Pelkonen O, Turpeinen M, et al. Arch Toxicol. 2008 Oct;82(10):667-715. |
18618097 |
| * | Drug interaction databases | |
| 6. | Interaktionsdatabasen.
|
|
| 7. | Lexi-Comp in UpToDate. Carvedilol: Drug information.
|
|
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