Rifampicin reverses nicardipine effect inducing uncontrolled essential hypertension

Cordeanu, Elena-Mihaela; Gærtner, S.; Faller, Alix-Marie; Mirea, C.; Lessinger, Jean‐Marc; Kemmel, Véronique; Stephan, Dominique

doi:10.1111/fcp.12292

Cited by 10 publications

(11 citation statements)

References 11 publications

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“…Nifedipine may possibly meet the requirements of being a selective antagonist by exerting its best effect on the vessels compared to the myocardium, and also has no (or very little) effect on nodal tissue or atrioventricular conduction; The problem is that its selectivity for vessels is associated with rapid uptake and plasma distribution, as well as a rapid rate of fixation to its "receptor" in the complex of the calcium ion channel, for this reason produces rapid peripheral vasodilation. As a consequence, the autonomic nervous system is stimulated, determining a rapid and significant increase of the heart rate, which forces to concomitant treatment with β-blocker or a preparation of prolonged release [24][25][26][27][28][29].…”

Section: Mechanism Of Actionmentioning

confidence: 99%

Dihydropyridines as Calcium Channel Blockers: An Overview

Bandyopadhyay¹,

Salazar²,

González³

2017

JAPLR

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A heartfelt tribute to the memory of Professor AsimaChatterjee, the legendary scientist-teacher-humanitarian, on the occasion of her birth centenary . AbstractCardiovascular disease remains one of the leading causes of death in the United States. It is estimated that 1 in every 3 American adults suffer from high blood pressure. Hypertension, a precursor to most cardiovascular diseases, continues to grow at an alarming rate and is seldom managed carefully. Attempts have been made to manage hypertension and reduce the morbidity and mortality of the cardiovascular organ through methods including diets, increased amount of exercise, and medications. Many commercial drugs have been derived from dihydropyridine due to its antihypertensive property. Dihydropyridine derivatives work by acting as calcium channel blockers blocking the intake of calcium ions into the vascular smooth muscle and, to a lesser extent, cardiac muscles. Dihydropyridine moiety is well-known in pharmacology as L-type calcium channel blockers, which is extremely important since it treats hypertension in people who suffer from it. It is also highly important to understand the antagonists of calcium in the arterial hypertension. A brief overview is presented in this mini-review.

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Section: Mechanism Of Actionmentioning

confidence: 99%

Dihydropyridines as Calcium Channel Blockers: An Overview

Bandyopadhyay¹,

Salazar²,

González³

2017

JAPLR

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“…She had a 6year history of essential hypertension that had been well controlled with amlodipine 5 mg/day and valsartan 80 mg/day. Fourteen days later, her blood pressure became uncontrolled at 163/ 77 mm Hg and surged to 200/100 mm Hg on day 16. Amlodipine was increased to 5 mg twice/day, valsartan was changed to losartan 50 mg-hydrochlorothiazide 12.5 mg/day, and several doses of sublingual nifedipine 10 mg and captopril 12.5 mg were given for 286 PHARMACOTHERAPY Volume 40, Number 4, 2020 immediate blood pressure control.…”

Section: Case Reportmentioning

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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“…Rifampin has been shown to reduce the bioavailability of nifedipine , most likely by mediating its metabolism in the gut wall . Other studies have also shown that coadministration of rifampin ameliorates the antihypertensive effects of calcium‐channel blockers including benidipine, amlodipine, nifedipine, and nisoldipine, leading to adverse events . Enantioselectivity of a drug has been addressed in relation to pharmacokinetics, pharmacological activity and safety.…”

Section: Introductionmentioning

confidence: 99%

Effect of rifampin on enantioselective disposition and anti‐hypertensive effect of benidipine

Sunwoo

Nguyen

Chien

et al. 2019

Brit J Clinical Pharma

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AIMSIn vitro study showed that benidipine is exclusively metabolized by cytochrome P450 (CYP) 3A. This study evaluated the effect of rifampin on the enantioselective disposition and anti-hypertensive effect of benidipine. METHODSBenidipine (8 mg) was administered to healthy subjects with or without repeated rifampin dosing, in a crossover design. Plasma concentrations of (S)-(S)-(+)-α and (R)-(R)-(À)-α isomers of benidipine and blood pressure were measured for up to 24 h after dosing. In addition, CYP3A metabolic capacity was evaluated in each subject using oral clearance of midazolam. RESULTSThe exposure of (S)-(S)-(+)-α-benidipine was greater than that of (R)-(R)-(À)-α-benidipine by approximately three-fold following single dose of benidipine. Repeated doses of rifampin significantly decreased the exposure of both isomers. Geometric mean ratios (GMRs) (95% CI) of C max and AUC ∞ for (S)-(S)-(+)-α-benidipine were 0.14 (0.10-0.18) and 0.12 (0.08-0.18), respectively. GMRs (95% CI) of C max and AUC ∞ for (R)-(R)-(À)-α-benidipine were 0.10 (0.06-0.17) and 0.10 (0.06-0.17), respectively. Oral clearances of both isomers were increased equally by approximately 10-fold. There were no significant differences in cardiovascular effect following benidipine administration between control and rifampin treatment. CYP3A activity using midazolam did not appear to correlate with oral clearance of benidipine. CONCLUSIONSAfter single administration of racemic benidipine, enantioselective disposition of (S)-(S)-(+)-αand (R)-(R)-(À)-α-benidipine was observed. Treatments with rifampin significantly decreased the exposure of both isomers but appeared to marginally affect its blood pressure-lowering effect in healthy subjects. Impact of coadministration of rifampin on the treatment effects of benidipine should be assessed in hypertensive patients. British Journal of Clinical PharmacologyBr J Clin Pharmacol (2019) 85 737-745 737• Benidipine is a racemic mixture of two isomers ((R)-(R)-(À)-α and (S)-(S)-(+)-α).• Our previous study indicated that benidipine was metabolized by CYP3A4 and CYP3A5.• Rifampin is a potent inducer of CYP3A4 that can decrease the antihypertensive effects of calcium channel blockers. WHAT THIS STUDY ADDS• A clinical study in healthy subjects was conducted to evaluate the enantioselective disposition of benidipine.• This study describes for the first time the effect of rifampin on the pharmacokinetic and pharmacodynamic properties of benidipine and its enantiomers to establish the mechanism of the drug interaction. Study design flow chart Effect of rifampin on benidipine PK/PD Br J Clin Pharmacol (2019) 85 737-745 739 Effect of rifampin on benidipine PK/PD Br J Clin Pharmacol (2019) 85 737-745 745

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Rifampicin reverses nicardipine effect inducing uncontrolled essential hypertension

Cited by 10 publications

References 11 publications

Dihydropyridines as Calcium Channel Blockers: An Overview

Dihydropyridines as Calcium Channel Blockers: An Overview

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

Effect of rifampin on enantioselective disposition and anti‐hypertensive effect of benidipine

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