Medical Editor: John P. Cunha, DO, FACOEP
What Is Aspruzyo Sprinkle?
What Are Side Effects of Aspruzyo Sprinkle?
Side effects of Aspruzyo Sprinkle include:
- weakness, and
Dosage for Aspruzyo Sprinkle
The dose of Aspruzyo is 500 mg orally twice daily and increased to 1000 mg orally twice daily, based on clinical symptoms.
Aspruzyo Sprinkle In Children
Safety and effectiveness of Aspruzyo is have not been established in pediatric patients.
What Drugs, Substances, or Supplements Interact with Aspruzyo Sprinkle?
Aspruzyo Sprinkle may interact with other medicines such as:
- strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, ritonavir, indinavir, and saquinavir),
- moderate CYP3A inhibitors (e.g., diltiazem, verapamil, erythromycin, fluconazole, and grapefruit juice or grapefruit-containing products),
- CYP3A inducers (e.g., rifampin, rifabutin, rifapentine,
- phenobarbital, phenytoin, carbamazepine, and St. John's wort),
- P-gp inhibitors (e.g., cyclosporine),
- CYP3A substrates (e.g., lovastatin, cyclosporine, tacrolimus, sirolimus),
- OCT2 substrates (e.g., metformin),
- drugs transported by P-gp (e.g., digoxin),
- drugs metabolized by CYP2D6 (e.g., tricyclic antidepressants), and
Tell your doctor all medications and supplements you use.
Aspruzyo Sprinkle During Pregnancy and Breastfeeding
Tell your doctor if you are pregnant or plan to become pregnant before using Aspruzyo Sprinkle; it is unknown how it might affect a fetus. It is unknown if Aspruzyo Sprinkle passes into breast milk. Consult your doctor before breastfeeding.
Our Aspruzyo Sprinkle (ranolazine) Extended-Release Granules, for Oral Use Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Clinical Trial Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
A total of 2018 patients with chronic angina were treated with ranolazine in controlled clinical trials. Of the patients treated with ranolazine, 1026 were enrolled in three doubleblind, placebo-controlled, randomized studies (CARISA, ERICA, MARISA) of up to 12 weeks' duration. In addition, upon study completion, 1251 patients received treatment with ranolazine in open-label, long-term studies; 1227 patients were exposed to ranolazine for more than 1 year, 613 patients for more than 2 years, 531 patients for more than 3 years, and 326 patients for more than 4 years.
At recommended doses, about 6% of patients discontinued treatment with ranolazine because of an adverse event in controlled studies in angina patients compared to about 3% on placebo. The most common adverse events that led to discontinuation more frequently on ranolazine than placebo were dizziness (1.3% versus 0.1%), nausea (1% versus 0%), asthenia, constipation, and headache (each about 0.5% versus 0%). Doses above 1000 mg twice daily are poorly tolerated.
In controlled clinical trials of angina patients, the most frequently reported treatmentemergent adverse reactions (> 4% and more common on ranolazine than on placebo) were dizziness (6.2%), headache (5.5%), constipation (4.5%), and nausea (4.4%). Dizziness may be dose-related. In open-label, long-term treatment studies, a similar adverse reaction profile was observed.
The following additional adverse reactions occurred at an incidence of 0.5 to 4.0% in patients treated with ranolazine and were more frequent than the incidence observed in placebo-treated patients:
Cardiac Disorders - bradycardia, palpitations
Ear and Labyrinth Disorders - tinnitus, vertigo
Eye Disorders - blurred vision
Gastrointestinal Disorders - abdominal pain, dry mouth, vomiting, dyspepsia
General Disorders and Administrative Site Adverse Events - asthenia, peripheral edema
Metabolism and Nutrition Disorders - anorexia
Nervous System Disorders - syncope (vasovagal)
Psychiatric Disorders - confusional state
Renal and Urinary Disorders - hematuria
Respiratory, Thoracic, and Mediastinal Disorders - dyspnea
Skin and Subcutaneous Tissue Disorders - hyperhidrosis
Vascular Disorders - hypotension, orthostatic hypotension
Other (< 0.5%) but potentially medically important adverse reactions observed more frequently with ranolazine than placebo treatment in all controlled studies included: angioedema, renal failure, eosinophilia, chromaturia, blood urea increased, hypoesthesia, paresthesia, tremor, pulmonary fibrosis, thrombocytopenia, leukopenia, and pancytopenia.
A large clinical trial in acute coronary syndrome patients was unsuccessful in demonstrating a benefit for ranolazine, but there was no apparent proarrhythmic effect in these high-risk patients [see Clinical Studies].
Ranolazine produces elevations of serum creatinine by 0.1 mg/dL, regardless of previous renal function, likely because of inhibition of creatinine's tubular secretion. In general, the elevation has a rapid onset, shows no signs of progression during long-term therapy, is reversible after discontinuation of ranolazine, and is not accompanied by changes in BUN. In healthy volunteers, ranolazine 1000 mg twice daily had no effect upon the glomerular filtration rate. More marked and progressive increases in serum creatinine, associated with increases in BUN or potassium, indicating acute renal failure, have been reported after initiation of ranolazine in patients with severe renal impairment [see WARNINGS AND PERCAUTIONS, Use In Specific Populations].
The following adverse reactions have been identified during post-approval use of ranolazine. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure:
Nervous System Disorders - Abnormal coordination, myoclonus, paresthesia, tremor, and other serious neurologic adverse events have been reported to occur, sometimes concurrently, in patients taking ranolazine. The onset of events was often associated with an increase in ranolazine dose or exposure. Many patients reported symptom resolution following drug discontinuation or dose decrease.
Metabolism and Nutrition Disorders - Cases of hypoglycemia have been reported in diabetic patients on antidiabetic medication.
Psychiatric Disorders - hallucination
Renal and Urinary Disorders - dysuria, urinary retention
Skin and Subcutaneous Tissue Disorders - angioedema, pruritus, rash
Effects Of Other Drugs On Ranolazine
Strong CYP3A Inhibitors
Concomitant use of ASPRUZYO Sprinkle with strong CYP3A inhibitors, including ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, ritonavir, indinavir, and saquinavir is contraindicated [see CONTRAINDICATIONS, CLINICAL PHARMACOLOGY ].
Moderate CYP3A Inhibitors
Limit the dose of ASPRUZYO Sprinkle to 500 mg twice daily in patients on moderate CYP3A inhibitors, including diltiazem, verapamil, erythromycin, fluconazole, and grapefruit juice or grapefruitcontaining products [see DOASAGE AND ADMINISTRATION, CLINICAL PHARMACOLOGY].
Concomitant use of ASPRUZYO Sprinkle and P-gp inhibitors, such as cyclosporine, may result in increases in ranolazine concentrations. Titrate ASPRUZYO Sprinkle based on clinical response in patients concomitantly treated with predominant P-gp inhibitors such as cyclosporine [see DOASAGE AND ADMINISTRATION].
Concomitant use of ASPRUZYO Sprinkle with CYP3A inducers such as rifampin, rifabutin, rifapentine, phenobarbital, phenytoin, carbamazepine, and St. John's wort is contraindicated [see CONTRAINDICATIONS, CLINICAL PHARMACOLOGY].
An in-vitro dissolution study was conducted to evaluate the impact of alcohol on extended-release characteristics of ASPRUZYO Sprinkle. The in-vitro study showed that alcohol causes a rapid release of ranolazine from ASPRUZYO Sprinkle that may increase the risk of adverse events associated with ASPRUZYO Sprinkle. Patients should not consume alcohol when taking ASPRUZYO Sprinkle [see CLINICAL PHARMACOLOGY].
Effects Of Ranolazine On Other Drugs
Drugs Metabolized By CYP3A
Limit the dose of simvastatin in patients on any dose of ASPRUZYO Sprinkle to 20 mg once daily, when ASPRUZYO Sprinkle is co-administered. Dose adjustment of other sensitive CYP3A substrates (e.g., lovastatin) and CYP3A substrates with a narrow therapeutic range (e.g., cyclosporine, tacrolimus, sirolimus) may be required as ASPRUZYO Sprinkle may increase plasma concentrations of these drugs [see CLINICAL PHARMACOLOGY].
Drugs Transported By P-gp
Concomitant use of ASPRUZYO Sprinkle and digoxin results in increased exposure to digoxin. The dose of digoxin may have to be adjusted [see CLINICAL PHARMACOLOGY].
Drugs Metabolized By CYP2D6
The exposure to CYP2D6 substrates, such as tricyclic antidepressants and antipsychotics, may be increased during co-administration with ASPRUZYO Sprinkle, and lower doses of these drugs may be required.
Drugs Transported By OCT2
In subjects with type 2 diabetes mellitus, concomitant use of ASPRUZYO Sprinkle 1000 mg twice daily and metformin results in increased plasma levels of metformin. When ASPRUZYO Sprinkle 1000 mg twice daily is co-administered with metformin, metformin dose should not exceed 1700 mg/day. Monitor blood glucose levels and risks associated with high exposures of metformin.
Metformin exposure was not significantly increased when given with ranolazine 500 mg twice daily [see CLINICAL PHARMACOLOGY].
Read the entire FDA prescribing information for Aspruzyo Sprinkle (Ranolazine Granules)
© Aspruzyo Sprinkle Patient Information is supplied by Cerner Multum, Inc. and Aspruzyo Sprinkle Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.
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