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Ranexa (Ranolazine) - Complete Drug information

Ranexa (Ranolazine) exerts antianginal and anti-ischemic effects without altering hemodynamic parameters like heart rate or blood pressure.

It is used to treat patients with the following conditions:

Chronic angina
- According to the 2012 ACCF/AHA/ACP/AATS/PCNA/SCAI/STS guidelines for patients with stable ischemic heart disease, ranolazine might be useful when used as a substitute for beta blockers for relief of symptoms if initial treatment with beta-blockers leads to unacceptable side effects, is not effective, or if initial treatment with beta-blockers is contraindicated.
- It can also be used in combination with beta-blockers, for relief of symptoms when initial treatment with beta-blockers is not successful.
Off Label Usage of Ranexa (Ranolazine) in Adults:
- It is used for the treatment of ventricular tachycardia

Ranexa (Ranolazine) dose in Adults:

It can be used with beta-blockers, nitrates, antiplatelet therapy, lipid-lowering therapy, calcium channel blockers, angiotensin-converting enzyme (ACE) inhibitors, and angiotensin-receptor blockers.

Ranexa (Ranolazine) dosage in the treatment of Chronic angina:

500 mg twice daily is given initially
It may be increased to 1,000 mg twice daily as needed (based on symptoms)
The maximum recommended dose is 1,000 mg twice daily
Missed doses:
- If a dose is missed, then it should be taken at the next scheduled time
- the next dose should not be doubled.

Off label dosage in the treatment of Ventricular tachycardia :

500 to 1,000 mg given every 12 hours
Dosage adjustment for ranolazine with concomitant medications:
Diltiazem, fluconazole, erythromycin, verapamil, and other moderate CYP3A inhibitors:
- Ranolazine dose should not exceed 500 mg twice daily
CYP3A inducers or strong CYP3A inhibitors:
- Concomitant use is strictly contraindicated
P-glycoprotein inhibitors (eg, cyclosporine):
- Titration of ranolazine based on clinical response

Ranexa (Ranolazine) dose in Childrens

Not recommended for use in children.

Pregnancy Risk Factor: C

Animal reproduction studies have shown that adverse events can be observed.

Ranolazine use during breastfeeding:

It is unknown if ranolazine gets into breast milk.
According to the manufacturer of the product, breastfeeding during therapy should be considered in light of the risks to the infant as well as the benefits to the mother.

Ranexa (Ranolazine) dose in kidney disease:

There are no dosage adjustments given in the manufacturer’s labeling.
However, plasma ranolazine levels are increased by about 40% to 50% in patients with varying degrees of renal dysfunction.
Stop if acute renal failure develops during treatment.
Ranolazine has not been used in patients requiring dialysis, although it is unlikely to be removed by hemodialysis due to plasma protein binding.

Ranexa (Ranolazine) dose in liver disease:

There are no dosage adjustments given in the manufacturer’s labeling.
Use is strictly contraindicated with hepatic cirrhosis.

Side Effects of (Ranexa) Ranolazine Include:

Cardiovascular:
- Bradycardia
- Hypotension
- Orthostatic Hypotension
- Palpitation
- Peripheral Edema
- Prolonged QT Interval On ECG
Central Nervous System:
- Dizziness
- Headache
- Confusion
- Syncope
- Vertigo
Dermatologic:
- Hyperhidrosis
Gastrointestinal:
- Constipation
- Abdominal Pain
- Anorexia
- Dyspepsia
- Nausea
- Vomiting
- Xerostomia
Genitourinary:
- Hematuria
Neuromuscular:
- Weakness
Ophthalmic:
- Blurred Vision
Otic:
- Tinnitus
Respiratory:
- Dyspnea

Contraindication to Ranexa (Ranolazine) Include:

Cirrhosis
concurrent strong CYP3A inhibitors
concurrent CYP3A inducers

Warnings and Precautions

Modified cardiac conduction
- Has been seen to prolong QTc interval in a dose/plasma concentration-related manner.
- Cirrhotic patients with mild to moderate hepatic impairment show a 3-fold increase QT prolongation
- Patients with liver cirrhosis are strictly prohibited from using this drug.
- Patients who are given a higher dose (>2,000mg/day) should consider the risks and benefits.
Acute coronary syndrome
- Ranolazine is not effective in relieving acute angina episodes. It has also not been shown to be beneficial in acute coronary syndrome.
Hepatic impairment
- The plasma levels of Ranolazine increase by 30% in mild (Child–Pugh class A), and by 80% for moderate (Child–Pugh class B), hepatic impairment.
- Patients with cirrhosis should not use this medication.
Renal impairment
- Some patients with severe renal impairment (CrCl 30mL/minute) have experienced acute renal failure.
- If acute renal failure occurs (markedly increased serum creatinine and/or an increase in BUN), discontinue ranolazine treatment.
- Patients with severe or moderate renal impairment should be monitored for changes in renal function, mainly for increased serum creatinine and/or higher BUN.
- Patients who require dialysis have not been prescribed Ranolazine.

Ranolazine: Drug Interaction

Risk Factor C (Monitor therapy)
Angiotensin II Receptor Blockers	Ranolazine may enhance the adverse/toxic effect of Angiotensin II Receptor Blockers.
Angiotensin-Converting Enzyme Inhibitors	Ranolazine may enhance the adverse/toxic effect of Angiotensin-Converting Enzyme Inhibitors.
ARIPiprazole	CYP3A4 Inhibitors (Weak) may increase the serum concentration of ARIPiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy and/or indication. Consult full interaction monograph for specific recommendations.
ARIPiprazole	CYP2D6 Inhibitors (Weak) may increase the serum concentration of ARIPiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy and/or indication. Consult full interaction monograph for specific recommendations.
AtorvaSTATin	Ranolazine may increase the serum concentration of AtorvaSTATin.
Brentuximab Vedotin	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Brentuximab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be increased.
Celiprolol	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Celiprolol.
Clofazimine	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Deferasirox	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Digoxin	Ranolazine may increase the serum concentration of Digoxin.
Dofetilide	CYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
Erdafitinib	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Erdafitinib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Erdafitinib	May increase the serum concentration of P-glycoprotein/ABCB1 Substrates.
Everolimus	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Everolimus.
Flibanserin	CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin.
Fosaprepitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Haloperidol	QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTcprolonging effect of Haloperidol.
Ivosidenib	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Larotrectinib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Larotrectinib	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Larotrectinib.
Lovastatin	Ranolazine may enhance the myopathic (rhabdomyolysis) effect of Lovastatin. Ranolazine may increase the serum concentration of Lovastatin. Ranolazine may also enhance the distribution of lovastatin to specific cells/tissues/organs where P-glycoprotein is present in large amounts (eg, brain, T-lymphocytes, testes, etc.).
Naldemedine	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Naldemedine.
Naloxegol	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Naloxegol.
NiMODipine	CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine.
Palbociclib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Perhexiline	CYP2D6 Inhibitors (Weak) may increase the serum concentration of Perhexiline.
P-glycoprotein/ABCB1 Inhibitors	May increase the serum concentration of Ranolazine.
P-glycoprotein/ABCB1 Substrates	Ranolazine may increase the serum concentration of Pglycoprotein/ABCB1 Substrates.
Prucalopride	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Prucalopride.
QT-prolonging Agents (Highest Risk)	QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk.
RifAXIMin	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of RifAXIMin.
Sarilumab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Silodosin	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Silodosin.
Siltuximab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Simeprevir	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Tacrolimus (Systemic)	Ranolazine may increase the serum concentration of Tacrolimus (Systemic).
Talazoparib	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Talazoparib. Management: These listed exceptions are discussed in detail in separate interaction monographs.
Tegaserod	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Tegaserod.
Tocilizumab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Risk Factor D (Consider therapy modification)
Afatinib	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Afatinib. Management: Reduce afatinib by 10 mg if not tolerated. Some non-US labeling recommends avoiding combination if possible. Iif used, administer the P-gp inhibitor simultaneously with or after the dose of afatinib.
Betrixaban	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Betrixaban. Management: Decrease the adult betrixaban dose to an initial single dose of 80 mg followed by 40 mg once daily if combined with a P-glycoprotein inhibitor.
Bilastine	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Bilastine. Management: Consider alternatives when possible; bilastine should be avoided in patients with moderate to severe renal insufficiency who are receiving p-glycoprotein inhibitors.
Calcium Channel Blockers (Nondihydropyridine)	May increase the serum concentration of Ranolazine. Management: Limit ranolazine dose to a maximum of 500 mg twice daily when used with diltiazem or verapamil. Exceptions: Bepridil.
Colchicine	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Colchicine. Colchicine distribution into certain tissues (e.g., brain) may also be increased. Management: Colchicine is contraindicated in patients with impaired renal or hepatic function who are also receiving a p-glycoprotein inhibitor. In those with normal renal and hepatic function, reduce colchicine dose as directed. See full monograph for details.
CYP3A4 Inhibitors (Moderate)	May increase the serum concentration of Ranolazine. Management: Limit the ranolazine adult dose to a maximum of 500 mg twice daily in patients concurrently receiving moderate CYP3A4 inhibitors (e.g., diltiazem, verapamil, erythromycin, etc.).
Dabigatran Etexilate	P-glycoprotein/ABCB1 Inhibitors may increase serum concentrations of the active metabolite(s) of Dabigatran Etexilate. Management: Dabigatran dose reductions may be needed. Specific recommendations vary considerably according to US vs Canadian labeling, specific P-gp inhibitor, renal function, and indication for dabigatran treatment. Refer to full monograph or dabigatran labeling.
DOXOrubicin (Conventional)	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of DOXOrubicin (Conventional). Management: Seek alternatives to P-glycoprotein inhibitors in patients treated with doxorubicin whenever possible. One U.S. manufacturer (Pfizer Inc.) recommends that these combinations be avoided.
Edoxaban	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Edoxaban. Management: See full monograph for details. Reduced doses are recommended for patients receiving edoxaban for venous thromboembolism in combination with certain P-gp inhibitors. Similar dose adjustment is not recommended for edoxaban use in atrial fibrillation.
Lefamulin	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Lefamulin. Management: Avoid concomitant use of lefamulin tablets with P-glycoprotein/ABCB1 inhibitors. If concomitant use is required, monitor for lefamulin adverse effects.
Lomitapide	CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lomitapide. Management: Patients on lomitapide 5 mg/day may continue that dose. Patients taking lomitapide 10 mg/day or more should decrease the lomitapide dose by half. The lomitapide dose may then be titrated up to a max adult dose of 30 mg/day.
MetFORMIN	Ranolazine may increase the serum concentration of MetFORMIN. Management: Limit the metformin dose to a maximum of 1,700 mg per day when used together with ranolazine 1,000 mg twice daily. Monitor patients for metformin toxicities, including lactic acidosis and carefully weigh the risks and benefits of this combination.
Simvastatin	Ranolazine may increase the serum concentration of Simvastatin. Management: Avoid the concurrent use of ranolazine with simvastatin when possible. If used together, avoid doses of simvastatin greater than 20 mg/day.
Stiripentol	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring.
Venetoclax	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Venetoclax. Management: Consider a venetoclax dose reduction by at least 50% in patients requiring concomitant treatment with P-glycoprotein (P-gp) inhibitors.
Risk Factor X (Avoid combination)
Antifungal Agents (Azole Derivatives, Systemic)	May decrease the metabolism of Ranolazine. Fluconazole and isavuconazonium considerations are addressed in separate monographs. Exceptions: Fluconazole; Isavuconazonium Sulfate.
Conivaptan	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
CYP3A4 Inducers (Moderate)	May decrease the serum concentration of Ranolazine.
CYP3A4 Inducers (Strong)	May decrease the serum concentration of Ranolazine.
CYP3A4 Inhibitors (Strong)	May increase the serum concentration of Ranolazine.
Fusidic Acid (Systemic)	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Idelalisib:	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
PAZOPanib	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of PAZOPanib.
Pimozide	CYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
RifAMPin	May decrease the serum concentration of Ranolazine.
St John's Wort	May decrease the serum concentration of Ranolazine.
Topotecan	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Topotecan.
VinCRIStine (Liposomal)	P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of VinCRIStine (Liposomal).

Monitor:

Baseline and follow up ECG to evaluate QT interval
monitor renal function periodically in patients with moderate to severe renal impairment, particularly for increases in serum creatinine accompanied by increased BUN
consider monitoring blood pressure in patients having renal dysfunction
correct and maintain serum potassium in normal limits

How to administer Ranolazine?

Give with or without meals.
Swallow the tablet whole.
Do not crush, break, or chew the tablet.

Mechanism of action of Ranolazine:

Ranolazine has anti-ischemic and anti-anginal effects, but does not alter hemodynamic parameters (heart rate, blood pressure).
Ranolazine, at therapeutic levels, also inhibits late phase of inward sodium channel (late II) in ischemic cardiac Myocytes during cardiac Repolarization.
This reduces intracellular sodium concentrations and reduces calcium influx via Na+/Ca2+ exchange.
A decrease in intracellular calcium can also lower ventricular tension, myocardial oxygen intake, and myocardial tension.
Although it is possible to see that ranolazine causes myocardial relaxation, and decreases anginal symptoms by this mechanism, this is not certain.
Ranolazine in higher concentrations also inhibits the Na rectifier potassium current (I) which is a rapid delayed Na rectifier voltage current.
This prolongs the ventricular action potential duration, and consequently prolongs the QT interval.

Absorption:

Highly variable

Protein binding:

almost 62%

Metabolism:

Extensively via Hepatic via CYP3A (major) and 2D6 (minor); intestines

Bioavailability:

Tablet: 76% (compared to solution)

Half-life elimination:

Ranolazine: Terminal: 7 hours
Metabolites (activity undefined): 6 - 22 hours

Time to peak, plasma:

2 - 5 hours

Excretion:

Mainly urine (75% mostly as metabolites; less than 5% as unchanged drug);
feces (25% mostly as metabolites; less than 5% as unchanged drug)

International Brands of Ranolazine:

Ranexa
Cartinex
Cartinex-OD
Ralozine
Ranasafe
Ranev
Ranexa
Ranola ER
Ranolin XR
Ranosin
Ranx
Razine

Ranolazine brands in Pakistan:

Ranolazine [Tabs 1 g]
Ranola	Highnoon Laboratories Ltd.
Razin Er	Getz Pharma Pakistan (Pvt) Ltd.

Ranolazine [Tabs 500 mg]
Rancard Xr	Searle Pakistan (Pvt.) Ltd.
Ranola	Highnoon Laboratories Ltd.

Ranolazine [Tabs 1000 mg]
Rancard Xr	Searle Pakistan (Pvt.) Ltd.

Ranolazine [Tabs SR 500 mg]
Ranzol	Maple Pharmaceuticals (Pvt) Ltd

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