[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Other antianginals](https://durgical.com/en/pharmacology/classes/other-antianginals/) › Ranolazine

# Ranolazine

## Other antianginals?

Other antianginals

A chronic angina drug that blocks the late sodium current. It reduces angina without changing heart rate or blood pressure, but it lengthens the QT.

Updated Nov 1, 2026

## Quick facts

**Group**
[Other antianginals](https://durgical.com/en/pharmacology/classes/other-antianginals/)

**Target**
Cardiac sodium channel Nav1.5 (late sodium current)

**Used for**
Chronic angina

**Key effects**
Dizziness · Headache · Constipation

**Monitor**
ECG · Kidney function at baseline · Angina frequency

**ATC**
C01EB18

No doses: the clinician sets them by the current guideline.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

⇅**Cardiac sodium channel Nav1.5 (late sodium current)**Ranolazine

ⓘ The figure shows ranolazine bound to the rat cardiac sodium channel Nav1.5, very similar to the human channel.

**Target in 3D:** Cardiac sodium channel Nav1.5 (late sodium current). PDB structure 8F6P (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/8F6P) · Drag to rotate · pinch to zoom

Ranolazine has anti-ischaemic effects that do not depend on heart rate or blood pressure. At therapeutic levels it inhibits the late inward sodium current of cardiac cells; in ischaemia this current loads cells with sodium and then calcium through the sodium-calcium exchanger. The exact link to angina relief is uncertain. It also blocks IKr, which prolongs the QT.

- Ranolazine inhibits the late sodium current in heart cells
- Less sodium loading means less calcium overload in ischaemia
- Diastolic tension falls; heart rate and pressure are unchanged
- IKr block lengthens the QT

## Indications

- Chronic angina, usually added to other antianginals [Stable angina →](https://durgical.com/en/conditions/stable-angina/)

## Adverse effects

### Common

- Dizziness
- Headache
- Constipation
- Nausea

### Serious (rare, important)

- QT prolongation
- Acute kidney failure in patients with severe kidney impairment
- Syncope

## Contraindications

- Strong CYP3A inhibitors (ketoconazole, clarithromycin, nelfinavir)
- CYP3A inducers (rifampicin, phenobarbital, St John's wort)
- Liver cirrhosis

## Key interactions

**Strong CYP3A inhibitors**
Large rise in ranolazine levels; contraindicated

**Diltiazem, verapamil, erythromycin, fluconazole, grapefruit**
Higher ranolazine levels; the ranolazine dose is limited

**Simvastatin and other CYP3A substrates (cyclosporine, tacrolimus)**
Ranolazine raises their levels

**Digoxin (P-glycoprotein)**
Higher digoxin levels

**Metformin (OCT2)**
Higher metformin levels at higher ranolazine doses

## What is monitored

- ECG: QT interval
- Kidney function at baseline and periodically when it is reduced
- Angina frequency

## Administration and safety

- Extended-release tablets are swallowed whole; not crushed, broken or chewed.
- It does not treat an acute attack: sublingual glyceryl trinitrate is kept for that.
- All medicines are reviewed for CYP3A interactions before starting.

## Pregnancy and breastfeeding

Human data are limited; it is used in pregnancy only if the benefit justifies the risk.

## Nursing care

- Check the ECG (QT) and report fainting or palpitations.
- Follow creatinine in patients with reduced kidney function.
- Teach the patient to avoid grapefruit and to report new medicines, including antibiotics and antifungals.

## Pharmacokinetics

**Absorption**
Extended-release tablet, with or without food

**Metabolism**
Liver, mainly CYP3A and to a lesser extent CYP2D6; substrate of P-glycoprotein

**Elimination**
Mostly as metabolites in urine; exposure rises in kidney impairment

## Memory aid

RANOLAZINE runs LATE: it blocks the late sodium current, leaves pulse and pressure alone, but stretches the QT.

## Test yourself

Think of the answer, then tap the question to see it.

## Which current does ranolazine inhibit, and why does it help ischaemic cells?

The late inward sodium current; less sodium loading means less calcium overload through the sodium-calcium exchanger.

## What are the three contraindications of ranolazine?

Strong CYP3A inhibitors, CYP3A inducers and liver cirrhosis.

## Which ECG change does ranolazine cause, and through which current?

QT prolongation, through block of IKr.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/ranolazine/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## Connections

## Related drugs 5

- [Ivabradine](https://durgical.com/en/pharmacology/ivabradine/)
- [Isosorbide mononitrate](https://durgical.com/en/pharmacology/isosorbide-mononitrate/)
- [Simvastatin](https://durgical.com/en/pharmacology/simvastatin/)
- [Metformin](https://durgical.com/en/pharmacology/metformin/)
- [Digoxin](https://durgical.com/en/pharmacology/digoxin/)

## Related conditions 1

- [Stable angina](https://durgical.com/en/conditions/stable-angina/)

[← Back to the class: Other antianginals](https://durgical.com/en/pharmacology/classes/other-antianginals/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [DailyMed - RANOLAZINE tablet, extended release](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d74f3dea-7357-4e9a-be9a-2f498a44108a) (DailyMed (U.S. National Library of Medicine), 2026); [Ranolazine: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a606015.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=C01EB18) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [8F6P: Rat Cardiac Sodium Channel with Ranolazine Bound](https://www.rcsb.org/structure/8F6P) (RCSB Protein Data Bank, 2023).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/ranolazine/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/ranolazine/