Ranexa (ranolazine) Cost, Indication, Mechanism of Action, and Dosage | Steven Ma, PharmD | RxEconsult
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Ranexa (ranolazine) Cost, Indication, Mechanism of Action Category: Heart Disease by - June 17, 2014 | Views: 20192 | Likes: 0 | Comment: 0  

Brand Name: Ranexa Ranexa Indication
Generic Name: ranolazine

Medication Class: anti-anginal, non-nitrate
Similar Drugs: no known drugs
Manufacturer: Gilead
FDA Approval Date: January 27, 2006

What is Ranexa and its mechanism of action?

Ranexa is an oral medication used for preventing angina (chest pain). Chronic angina usually causes pain or discomfort in the chest area and is triggered when there is too little oxygen reaching the heart muscles. The exact mechanism of action for Ranexa in the treatment of chronic angina is not known. Reduced delivery of oxygen to heart muscle causes ischemia (cell death) which involves an imbalance in sodium and calcium concentrations in muscle cells. Ranexa blocks the entry of sodium into heart cells but how this effect reduces chest pain is uncertain. 

What is the indication for Ranexa?

Ranexa is used for the treatment of chronic angina (chest discomfort or pain due to reduced blood flow in the heart).

How effective is Ranexa?

In a 12 week clinical trial called CARISA, 823 patients with chronic angina were treated with either Ranexa 750 mg, 1000 mg, or placebo all given twice daily. With Ranexa treatment, patient exercise time on a treadmill stress test went up on average of about 24 seconds compared to placebo. There were no difference between Ranexa 750 mg and 1000 mg.

In another clinical trial called ERICA, 565 patients with chronic angina and not controlled on maximum doses of angina medications were treated with either Ranexa 500 mg twice daily or placebo for one week then switched to 1000 mg twice daily or placebo for 6 weeks. The results of this study showed that patients treated with Ranexa had an average of 3.3 angina attacks per week compared to 4.3 attacks per week for placebo. In addition, nitroglyercin use was 2.7 doses per week for Ranexa treated patients compared to 3.6 doses per week for placebo.

Interesting Facts about Ranexa

  • Unlike other anti-anginal medications, Ranexa does not significantly affect heart rate or blood pressure.
  • Ranexa should not be used in the treatment of acute angina episode because it will not relieve acute symptoms.
  • Ranexa may be used with beta-blockers, nitrates, calcium channel blockers, anti-platelet, ACE inhibitors, and angiotensin receptor blockers.

What are side effects of Ranexa?

Some side effects include:

  • constipation
  • nausea
  • dizziness
  • headache
  • prolonged QT interval
  • syncope (fainting)
  • abnormal heart rhythm
  • palpitations
  • rash
  • allergic reactions

What is the dosage of Ranexa?

Ranexa is formulated as 500 mg and 1000 mg extended-release tablets.

The usual starting dose is Ranexa 500 mg orally twice daily. Ranexa may be increased to 1000 mg twice daily if needed based on symptoms. Ranexa should be swallowed whole; do not break, crush, or chew the tablets.

What are possible drug interactions with Ranexa?

Strong inhibitors of liver enzymes called CYP450 3A4 such as ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, ritonavir, indinavir, and saquinavir should not be combined with Ranexa due to the potential to increase the concentration of Ranexa in the body by about 220% when co-administered.

Moderate CYP450 3A4 inhibitors such as diltiazem, verapamil, erythromycin, fluconazole, and grapefruit juice may increase the concentration of Ranexa in the body by about 50-130%. Dose should be limited to Ranexa 500 mg twice daily when patients are on any moderate CYP450 3A4 inhibitors.

Cyclosporine may increase the concentration of Ranexa in the body.

Medications that increase the action of CYP450 3A4 such as rifampin, rifabutin, rifapentine, phenobarbital, phenytoin, carbamazepine, and St. John’s wort should not be combined with Ranexa because they may decrease the concentration of Ranexa in the body by about 95%.

Ranexa may increase the concentration of simvastatin, lovastatin, cyclosporine, tacrolimus, and sirolimus. Doses for these drugs should be reduced when administered with Ranexa.

Ranexa can increase the concentration of metformin in the body. If patient is on Ranexa, the metformin dose should not exceed 1700 mg/day.

What are warnings and precautions with Ranexa?

  • Ranexa may cause acute kidney failure in patients with poor kidney function. Monitor kidney function when starting treatment with Ranexa.
  • Ranexa can prolong heart beats which can lead to Torsades de pointes. Torsades de pointes is an abnormal heart rhythm that can cause sudden blood pressure drop, dizziness, fainting and can eventually lead to death.

Pregnancy: Ranexa is pregnancy category C which means it has not been adequately evaluated in pregnant women.

Nursing Mothers: It is not known if Ranexa is excreted into human milk. Because many drugs are excreted into human milk mothers should discontinue nursing or discontinue Ranexa.

What is the cost of Ranexa?

The average wholesale price for 60 tablets of Ranexa 500 mg is $258.56 and 60 tablets of Ranexa 1000 mg is $424.29.

How to obtain prescription assistance for Ranexa?

For more information on how to reduce the cost of Ranexa visit Ranexa Connect Co-pay Coupon Card.

References

Ranexa Prescribing Information


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