Ralozine

Indications

Ranolazine is used together with other heart medicines to treat long term (chronic) stable angina, which is chest pain or tightness that comes on with exertion because the heart muscle is not getting enough oxygen. It is usually added when angina is not well controlled by medicines such as beta blockers or calcium channel blockers, or when these cannot be used.

How It Works

When the heart muscle is short of oxygen, too much sodium and then calcium build up inside its cells, making the muscle stiff and using more energy. Ranolazine blocks a late sodium current in heart cells, which reduces this build up. The heart muscle relaxes better and needs less oxygen, so angina attacks happen less often. It does not lower heart rate or blood pressure much.

Dosage and Administration

The usual adult starting dose is 375 mg to 500 mg twice a day, taken as prolonged release tablets. After 2 to 4 weeks the doctor may increase it to a maximum of 750 mg to 1000 mg twice a day depending on response and tolerance. Swallow the tablets whole with water; do not crush, break or chew them. It can be taken with or without food. Ranolazine is not for relieving an angina attack that is already happening; use your quick acting angina medicine for that.

Interactions

• Strong CYP3A4 blockers such as Ketoconazole, Itraconazole, Clarithromycin and some HIV medicines must not be used with it, as they greatly raise its blood level.
• Moderate CYP3A4 blockers such as Diltiazem, Verapamil, Erythromycin and Fluconazole may require a lower dose.
• Rifampicin, Carbamazepine, Phenytoin and St John's Wort can reduce its effect.
• It can raise blood levels of Digoxin, Simvastatin, Metformin, Tacrolimus and Ciclosporin; doses may need adjusting.
• Grapefruit juice should be avoided.
• Use caution with other medicines that affect heart rhythm (QT prolongation).

Contraindications

• Allergy to Ranolazine.
• Severe kidney impairment.
• Moderate or severe liver impairment.
• Use with strong CYP3A4 blockers or with certain anti arrhythmic medicines such as Quinidine, Dofetilide or Sotalol.

Side Effects

Common side effects include dizziness, headache, constipation, nausea and feeling weak. Less often there may be vomiting, tiredness, blurred vision, ringing in the ears, swelling of the legs or confusion, especially in older people.

Get urgent medical help if you faint, feel a fast, pounding or irregular heartbeat, have chest pain that does not settle, notice very little urine, or have signs of a serious allergic reaction such as swelling of the face or throat or difficulty breathing.

Pregnancy and Lactation

There is not enough information on use in pregnancy, so it should be avoided unless a doctor decides it is clearly needed. It is not known whether it passes into breast milk; breastfeeding is generally not recommended during treatment.

Precautions and Warnings

• Ranolazine can lengthen the QT interval on the ECG; your doctor may check an ECG, especially if you have heart rhythm problems.
• Kidney function should be checked before and during treatment.
• Older people, people with low body weight and those with heart failure may be more sensitive and need careful dosing.
• It may cause dizziness or blurred vision; do not drive if affected.

Overdose

Overdose may cause dizziness, nausea, vomiting, double vision, confusion, fainting and dangerous heart rhythm changes. Seek emergency medical help straight away. Treatment is supportive with heart monitoring in hospital.

Therapeutic Class

Anti anginal medicine; late sodium current inhibitor.

Storage

Store below 30°C in a dry place, away from light and out of the reach of children.