Nifedipine with Cimetidine Interaction Details

Brand Names Associated with Nifedipine

Brand Names Associated with Cimetidine

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Nov 20, 2023

Interaction Effect

Increased NIFEdipine serum concentrations and toxicity (headache, peripheral edema, hypotension, tachycardia)

Interaction Summary

Cimetidine in particular among H2 receptor antagonists can cause serum level elevations for most available calcium channel blockers, although clinically significant changes in hemodynamic response (heart rate, blood pressure) are most apparent only with NIFEdipine or diltiazem. Both alterations in hepatic metabolism of calcium channel blockers, and increased bioavailability secondary to reduced gastric acidity secondary to H2 blocker use are possible mechanisms .

Severity

Moderate

Onset

Delayed

Evidence

Probable

How To Manage Interaction

Monitor the cardiovascular response (blood pressure, heart rate) to the calcium channel blocker if cimetidine is added to the regimen. Dose reductions of up to 35% to 40% may be needed for diltiazem or NIFEdipine.

Mechanism Of Interaction

Decreased hepatic metabolism and increased bioavailability of NIFEdipine

Literature Reports

A) Several studies comparing the effects of cimetidine and ranitidine on NIFEdipine have consistently demonstrated a decrease in NIFEdipine's elimination and an increase in NIFEdipine's area under the plasma concentration-time curve when administered concurrently with cimetidine, but no alterations with ranitidine. Patients previously stabilized on NIFEdipine have experienced elevated heart rates and blood pressures when cimetidine was introduced .

B) Concomitant cimetidine (1000 mg daily) and NIFEdipine (40 mg daily) therapy resulted in an 80% increase in the peak plasma levels and a 74% increase in the area under the plasma concentration-time curve (AUC) for NIFEdipine in six healthy volunteers over a seven-day period. Ranitidine produced smaller and nonsignificant increases .

C) Concomitant administration of oral cimetidine 300 mg four times a day and oral NIFEdipine in single doses of 20 mg or multiple doses of 10 to 20 mg three times a day resulted in increases in the area under the plasma concentration-time curve (AUC) for NIFEdipine in 23 healthy patients . With both single and multiple NIFEdipine doses, cimetidine decreased the apparent oral clearance (dose/AUC) and prolonged the elimination half-life of NIFEdipine. NIFEdipine pharmacokinetics did not differ when single versus multiple dose elimination were compared. In addition, the elevations in heart rate were greater during the combined therapy when compared to NIFEdipine alone, but blood pressure reductions were similar. There was a trend towards a greater incidence of headache during combined therapy.

D) A 60% increase in area under the plasma concentration versus time curve (p less than 0.05) occurred in six individuals following administration of cimetidine 1 gram daily during chronic NIFEdipine (10 mg every six hours) administration. The mean peak plasma level of NIFEdipine increased by 80% during coadministration of cimetidine. A reduction in mean arterial blood pressure was also observed in these individuals suggesting an enhanced blood pressure reduction from NIFEdipine in combination with cimetidine . Even though no toxicity resulted from the combination of cimetidine and NIFEdipine, it is likely to be of clinical importance.

Nifedipine Overview

• Nifedipine is used to treat high blood pressure and to control angina (chest pain). Nifedipine is in a class of medications called calcium-channel blockers. It lowers blood pressure by relaxing the blood vessels so the heart does not have to pump as hard. It controls chest pain by increasing the supply of blood and oxygen to the heart.

• High blood pressure is a common condition and when not treated, can cause damage to the brain, heart, blood vessels, kidneys and other parts of the body. Damage to these organs may cause heart disease, a heart attack, heart failure, stroke, kidney failure, loss of vision, and other problems. In addition to taking medication, making lifestyle changes will also help to control your blood pressure. These changes include eating a diet that is low in fat and salt, maintaining a healthy weight, exercising at least 30 minutes most days, not smoking, and using alcohol in moderation.

Cimetidine Overview

• Cimetidine is used to treat ulcers; gastroesophageal reflux disease (GERD), a condition in which backward flow of acid from the stomach causes heartburn and injury of the food pipe (esophagus); and conditions where the stomach produces too much acid, such as Zollinger-Ellison syndrome. Over-the-counter cimetidine is used to prevent and treat symptoms of heartburn associated with acid indigestion and sour stomach. Cimetidine is in a class of medications called H₂ blockers. It decreases the amount of acid made in the stomach.

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Definitions

Severity Categories

Contraindicated

These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.

Major

This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.

Moderate

This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.

Minor

While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.

Onset

Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.

Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.

Evidence

Level of documentation of the interaction.

Established: The interaction is documented and substantiated in peer-reviewed medical literature.

Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.

How To Manage The Interaction

Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.

It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.

Mechanism Of Interaction

The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.

Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.

Where Does Our Information Come From?

Information for our drug interactions is compiled from several drug compendia, including:

• Gold Standard Drug Database
• Micromedex
• Lexicomp
• DrugBank

The prescribing information for each drug, as published on DailyMED, is also used. 

Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.

The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.