A possible drug interaction between rifampicin and enalapril

Kandiah, David Arumaisingam; Penny, W J; Fraser, A. G.; Lewis, M J

doi:10.1007/bf00561378

Cited by 14 publications

(8 citation statements)

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“…Most of the ACEIs are not metabolized by CYPs. Although in one case, rifampin coadministration with enalapril reduced the AUC of the active metabolite enalaprilat by 31% while showing no effect on the enalapril concentration 6 . The investigators assumed it was more likely due to the enhanced renal clearance of enalaprilat.…”

Section: Discussionmentioning

confidence: 99%

“…These interactions have been particularly problematic with the concurrent use of rifampin and antihypertensive drugs. Many case reports documented that blood pressure in these patients was more difficult to control, [4][5][6][7][8][9][10][11][12][13][14][15][16] and most of the drugs used were calcium channel blockers (CCBs). However, rifampin can also affect the function of drug transporters because it is an inhibitor of organic anion transporter polypeptides (OATPs) and P-glycoprotein (P-gp), as well as an inducer of P-gp.…”

mentioning

confidence: 99%

“…Previous case reports and human pharmacokinetic and pharmacodynamic studies reported the interactions between rifampin and antihypertensive drugs. [4][5][6][7][8][9][10][11][12][13][14][15][16][21][22][23][24][25][26][27][28][29][30][31][32][33][34][35][36][37][38][39][40] However, to our knowledge, no systematic summary or predictions of these interactions have been published. Thus we used the Biopharmaceutics Drug Disposition Classification System (BDDCS) to predict the direction and relative extent of both transporterbased DDIs and metabolic interactions.…”

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confidence: 99%

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Predicting Interactions between Rifampin and Antihypertensive Drugs Using the Biopharmaceutics Drug Disposition Classification System

et al. 2020

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Study Objective Lack of blood pressure control is often seen in hypertensive patients concomitantly taking antituberculosis medications due to the complex drug‐drug interactions between rifampin and antihypertensive drugs. Therefore, it is of clinical importance to understand the underlying mechanisms of these interactions to help formulate recommendations on the use of antihypertensive drugs in patients taking these medications concomitantly. Our objective was to assess the reliability of the Biopharmaceutics Drug Disposition Classification System (BDDCS) to predict potential interactions between rifampin and antihypertensive drugs and thus provide recommendations on the choice of antihypertensive drugs in patients receiving rifampin. Design Evidence‐based in vitro and in vivo predictions of drug‐drug interactions. Measurements and Main Results We systematically evaluated interactions between rifampin and antihypertensive drugs using the theory of the BDDCS, taking into consideration the role of drug transporters and metabolic enzymes involved in these interactions. We provide recommendations on the selection of antihypertensive drugs for patients with tuberculosis. Antihypertensive drugs approved by the U.S. Food and Drug Administration and the China National Medical Products Administration were included in this study. The drugs were classified into four categories under the BDDCS classification. Detailed information on cytochrome P450 (CYP) enzymes and drug transporters for each antihypertensive drug was searched in PubMed and other electronic databases. This information was combined with the effects of rifampin on CYP enzymes and drug transporters, and the direction and relative extent of the potential interactions between rifampin and antihypertensive drugs were predicted. Recommendations were then made using the theory of BDDCS. A thorough systematic literature review was performed, and data from all published human studies and case reports were summarized for the validation of our predictions. Interventional and observational studies published in PubMed and two Chinese databases (CNKI and WanFang) through December 16, 2019, were included, and data were extracted for validation of the predictions. Using the BDDCS theory, class 3 active drugs were predicted to exhibit minimal interactions with rifampin. On reviewing case reports and pre‐post studies, the predictions we made were found to be reliable. When antituberculosis medications that include rifampin are started in patients with hypertension, it is recommended that the use of calcium channel blockers and classes 1 and 2 β‐blockers be avoided. Angiotensin‐converting enzyme inhibitors, olmesartan, class 3 β‐blockers, spironolactone, and hydrochlorothiazide would be preferable because clinically relevant interactions would not be expected. Conclusion Application of the BDDCS to predict interactions between rifampin and antihypertensive drugs for patients with both tuberculosis and hypertension was found to be reliable. It should be noted, however, that bas...

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Section: Discussionmentioning

confidence: 99%

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Predicting Interactions between Rifampin and Antihypertensive Drugs Using the Biopharmaceutics Drug Disposition Classification System

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“…There is 1 case report of a pharmacokinetic interaction between enalapril and rifampicin (Kandiah et al 1988). When a patient with essential hypertension was treated with enalapril and antibiotics for brucellosis his blood pressure rose significantly.…”

Section: Rifampicin (Rifampin)mentioning

confidence: 99%

Pharmacokinetic Drug Interactions with ACE Inhibitors

Shionoiri

1993

Clinical Pharmacokinetics

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Angiotensin converting enzyme (ACE) inhibitors which have active moieties excreted mainly in urine require adjustment of either the dose or the interval between doses in patients with moderate to severe renal dysfunction or severe congestive heart failure. Those agents such as temocapril (CS 622) and fosinopril, excreted both in urine and bile, may not require such adjustment. Renal clearance of ACE inhibitors may be reduced and some accumulation may occur in elderly patients with mild renal dysfunction or congestive heart failure. The bioavailability of ACE inhibitors is reduced by concomitant food or antacids which may slow gastric emptying and raise gastric pH. Pharmacokinetic interactions with ACE inhibitors are unlikely in patients receiving thiazide or loop diuretics. When ACE inhibitors are given hyperkalaemia may occur in patients with renal insufficiency, those taking potassium supplements or potassium-sparing diuretics, and in diabetic patients with mild renal impairment. While no pharmacokinetic interaction precludes use of this combination, the pharmacokinetics of some ACE inhibitors are subject to greater variability when patients also receive beta-blockers. Calcium antagonists and ACE inhibitors have additive anti-hypertensive effects and pharmacokinetic interactions between these agents are unlikely. One report exists of a significant effect of coadministered hydralazine on the pharmacokinetics and urinary excretion of lisinopril. Data on interactions between ACE inhibitors and digitalis are contradictory. There is no evidence that the concomitant use of ACE inhibitors and digoxin is associated with an increased risk of digitalis toxicity. ACE inhibitors are mainly excreted by glomerular filtration and renal tubular secretion. Possible interactions between ACE inhibitors and probenecid have been noted, with renal and total body clearance of ACE inhibitors being potentially reduced in the presence of probenecid. Probenecid pretreatment may enhance the pharmacodynamic response of ACE inhibitors. Few but contradictory data exist on the effects of H2-blockers on ACE inhibitor pharmacokinetics and little information is available on interactions between ACE inhibitors and hypoglycaemic drugs. Some case reports link ACE inhibitors with the induction of lithium toxicity. Coadministration of lithium should be undertaken with caution, and frequent monitoring of lithium concentrations is recommended with all ACE inhibitors. Nonsteroidal anti-inflammatory drugs (NSAIDs) may attenuate the haemodynamic actions of ACE inhibitors. NSAIDs reduce renal excretion of ACE inhibitors, with a corresponding increase in circulating drug concentrations. There is little information available on the pharmacokinetic interaction with ACE inhibitors and cyclosporin, but caution should be employed when they are used together.(ABSTRACT TRUNCATED AT 400 WORDS)

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“…A pharmacokinetic interaction has been documented between enalapril and rifampicin (Kandiah et al 1988). A patient with essential hypertension was treated with enalapril 15mg twice daily; since this patient had fever of unknown origin, rifampicin 300mg twice daily was given for 5 days.…”

Section: Drug 1nteractionsmentioning

confidence: 99%

Metabolites of Antihypertensive Drugs

Ebihara

Fujimura

1991

Clinical Pharmacokinetics

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Many antihypertensive drugs are extensively metabolised in humans. Since some metabolites are active and may therefore contribute to the pharmacological activity of the parent drugs, knowledge of the pharmacokinetic properties of active metabolites is important for understanding the overall effects of drugs. Four categories of antihypertensive drugs with active metabolites are dealt with, with selected examples described in some detail. First, drugs with effects relying totally on active metabolites include agents such as methyldopa, cadralazine and many angiotensin converting enzyme (ACE) inhibitors. Secondly, those with effects primarily due to active metabolites include drugs such as triamterene and spironolactone. Thirdly, agents with effects primarily due to the parent drug, but with active metabolites providing significant contributions to the overall pharmacological effect, include drugs such as indoramin, alprenolol, acebutolol, diltiazem and verapamil. Lastly, agents with pharmacological effects with only minor (if any) contributions from active metabolites include drugs such as propranolol, metoprolol, carteolol and others.

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A possible drug interaction between rifampicin and enalapril

Cited by 14 publications

References 2 publications

Predicting Interactions between Rifampin and Antihypertensive Drugs Using the Biopharmaceutics Drug Disposition Classification System

Predicting Interactions between Rifampin and Antihypertensive Drugs Using the Biopharmaceutics Drug Disposition Classification System

Pharmacokinetic Drug Interactions with ACE Inhibitors

Metabolites of Antihypertensive Drugs

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