Diltiazem XR 120mg Capsules (24 Hr)

Manufacturer APOTEX USA Active Ingredient Diltiazem Long-Acting Capsules(dil TYE a zem) Pronunciation dil TYE a zem
It is used to treat high blood pressure.It is used to treat some types of chest pain (angina).It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Antihypertensive, Antianginal
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Pharmacologic Class
Calcium Channel Blocker, Benzothiazepine
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Pregnancy Category
Category C
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FDA Approved
Sep 1982
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Diltiazem XR is a medication used to treat high blood pressure (hypertension) and chest pain (angina). It belongs to a class of drugs called calcium channel blockers. It works by relaxing blood vessels, which helps lower blood pressure and allows more blood and oxygen to reach the heart, reducing chest pain. The 'XR' means extended-release, so you take it once a day.
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How to Use This Medicine

Taking Your Medication Correctly

To get the most benefit from your medication, follow these guidelines:

Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication at the same time every day to establish a routine.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.

Special Instructions for Taking Your Medication

Some medications may need to be taken with food or on an empty stomach. Check with your pharmacist to determine the best way to take your medication. Additionally, some products can be opened and sprinkled on a spoonful of applesauce, while others must be swallowed whole. Consult with your pharmacist to see if this is an option for your medication.

Storing and Disposing of Your Medication

To ensure the safety and effectiveness of your medication:

Store it at room temperature, protected from light and moisture.
Keep it in a dry place, away from the bathroom.
Store all medications in a secure location, out of reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. Check with your pharmacist for guidance on the best way to dispose of your medication, and consider participating in a drug take-back program in your area.

What to Do If You Miss a Dose

If you miss a dose of your medication:

Take it as soon as you remember.
If it's close to the time for your next dose, skip the missed dose and resume your regular schedule.
* Do not take two doses at the same time or take extra doses to make up for the missed one.
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Lifestyle & Tips

  • Continue to follow a heart-healthy diet (low in sodium, saturated fat, and cholesterol).
  • Engage in regular physical activity as advised by your doctor.
  • Maintain a healthy weight.
  • Limit alcohol intake.
  • Avoid smoking.
  • Manage stress effectively.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: 120 mg once daily
Dose Range: 120 - 540 mg

Condition-Specific Dosing:

hypertension: Initial: 120-240 mg once daily; Titrate up to 540 mg once daily based on response.
chronicStableAngina: Initial: 120-180 mg once daily; Titrate up to 480 mg once daily based on response.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment generally required, monitor closely.
Moderate: Use with caution, monitor for exaggerated effects. Consider lower initial doses.
Severe: Use with caution, monitor for exaggerated effects. Consider lower initial doses.
Dialysis: Diltiazem is not significantly removed by hemodialysis. Use with caution, monitor for exaggerated effects.

Hepatic Impairment:

Mild: Use with caution, monitor for exaggerated effects.
Moderate: Use with caution, monitor for exaggerated effects. Consider lower initial doses and slower titration.
Severe: Use with caution, monitor for exaggerated effects. Consider lower initial doses and slower titration.

Pharmacology

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Mechanism of Action

Diltiazem is a non-dihydropyridine calcium channel blocker. It inhibits the influx of extracellular calcium ions across the myocardial and vascular smooth muscle cell membranes. This leads to relaxation of vascular smooth muscle and coronary vasodilation, increasing myocardial oxygen delivery. In the heart, it decreases sinoatrial (SA) and atrioventricular (AV) nodal conduction, prolonging the effective refractory period and slowing heart rate. These actions result in decreased peripheral vascular resistance, reduced blood pressure, and decreased myocardial oxygen demand.
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Pharmacokinetics

Absorption:

Bioavailability: 40-65% (due to first-pass metabolism)
Tmax: 10-14 hours (for XR formulations)
FoodEffect: Food may increase bioavailability slightly but is not clinically significant; can be taken with or without food.

Distribution:

Vd: 5.3 L/kg
ProteinBinding: 70-80%
CnssPenetration: Limited

Elimination:

HalfLife: 5-10 hours (for XR formulations, apparent half-life is longer due to sustained release)
Clearance: Not available (highly variable)
ExcretionRoute: Renal (35% as metabolites, <5% unchanged), Fecal (60% as metabolites)
Unchanged: <5%
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Pharmacodynamics

OnsetOfAction: Within 30-60 minutes (for immediate release); longer for XR
PeakEffect: 6-11 hours (for XR formulations)
DurationOfAction: 24 hours (for XR formulations)

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Severe dizziness or fainting
Slow heartbeat
New or worsening abnormal heartbeat
Worsening heart failure (if you have a history of heart failure, consult your doctor). Seek immediate medical attention if you experience:
+ Shortness of breath
+ Significant weight gain
+ Swelling in the arms or legs
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other severe skin reactions (sometimes fatal). Seek medical help right away if you notice:
+ Red, swollen, blistered, or peeling skin
+ Other skin irritation (with or without fever)
+ Red or irritated eyes
+ Sores in your mouth, throat, nose, or eyes

Other Possible Side Effects

Like all medications, this drug may cause side effects in some people. Many individuals experience no side effects or only mild ones. If you are bothered by any of the following side effects or if they persist, contact your doctor or seek medical attention:

Headache
* Feeling dizzy, tired, or weak

This is not an exhaustive list of potential side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Severe dizziness or fainting
  • Very slow heart rate (less than 50 beats per minute)
  • New or worsening swelling in your hands, ankles, or feet
  • Shortness of breath, especially with exertion or lying down
  • Unusual fatigue or weakness
  • Yellowing of the skin or eyes (jaundice)
  • Dark urine or pale stools (signs of liver problems)
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain types of abnormal heart rhythms, as this medication is not suitable for use with many types of irregular heartbeats. If you are unsure, consult your doctor or pharmacist for guidance.
Any of the following health conditions: fluid accumulation in the lungs, low blood pressure, or a recent heart attack.
If you are currently taking ivabradine or rifampin, as these medications may interact with this drug.

This list is not exhaustive, and it is crucial to disclose all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any existing health problems, to your doctor and pharmacist. This will enable them to assess the safety of taking this medication in conjunction with your other treatments and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

When starting this medication, be cautious when performing tasks that require alertness, such as driving, until you understand how it affects you. To minimize the risk of dizziness or fainting, get up slowly from a sitting or lying position, and exercise caution when navigating stairs.

As directed by your doctor, regularly monitor your blood pressure and heart rate. You may need to undergo an electrocardiogram (ECG) before initiating this medication and during treatment. Consult with your doctor regarding the frequency of these checks.

If you have high blood pressure and are taking this medication, consult your doctor before using over-the-counter (OTC) products that may increase blood pressure, such as cough or cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, and certain natural products or aids.

If you consume grapefruit juice or eat grapefruit regularly, discuss this with your doctor, as it may interact with your medication. Additionally, you may need to avoid consuming alcohol while taking this medication; consult your doctor or pharmacist to determine if this is necessary.

If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.

If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor, as they will need to discuss the potential benefits and risks of this medication to both you and your baby.
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Overdose Information

Overdose Symptoms:

  • Severe hypotension (very low blood pressure)
  • Profound bradycardia (extremely slow heart rate)
  • AV block (heart block)
  • Cardiogenic shock
  • Asystole (cardiac arrest)
  • Dizziness
  • Confusion
  • Lethargy

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Treatment may involve supportive care, intravenous fluids, atropine, calcium gluconate, vasopressors, or glucagon.

Drug Interactions

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Contraindicated Interactions

  • Ivabradine (risk of severe bradycardia)
  • Dantrolene (IV) (risk of cardiovascular collapse)
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Major Interactions

  • Beta-blockers (e.g., metoprolol, carvedilol) - increased risk of bradycardia, AV block, heart failure
  • Digoxin - increased digoxin levels, risk of toxicity
  • Amiodarone - increased risk of bradycardia, AV block, hypotension
  • Statins (e.g., simvastatin, lovastatin) - increased statin levels, risk of myopathy/rhabdomyolysis
  • Cyclosporine, Tacrolimus, Sirolimus - increased immunosuppressant levels, risk of toxicity
  • Fentanyl (CYP3A4 substrate) - increased fentanyl levels, risk of respiratory depression
  • Alpha-blockers (e.g., prazosin, doxazosin) - increased risk of hypotension
  • Clonidine - increased risk of bradycardia, AV block
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Moderate Interactions

  • Other antihypertensives - additive hypotensive effects
  • Grapefruit juice - increased diltiazem levels
  • Carbamazepine - increased carbamazepine levels
  • Phenytoin - increased phenytoin levels
  • Theophylline - increased theophylline levels
  • Rifampin, Phenobarbital, Phenytoin (CYP3A4 inducers) - decreased diltiazem levels
  • Cimetidine, Ranitidine - increased diltiazem levels
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Minor Interactions

  • NSAIDs - may attenuate antihypertensive effect

Monitoring

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Baseline Monitoring

Blood Pressure (BP)

Rationale: To establish baseline and guide initial dosing for hypertension/angina.

Timing: Prior to initiation

Heart Rate (HR)

Rationale: To establish baseline and assess for bradycardia, especially given its negative chronotropic effect.

Timing: Prior to initiation

Electrocardiogram (ECG)

Rationale: To assess baseline cardiac rhythm and PR interval, especially in patients with pre-existing conduction abnormalities.

Timing: Prior to initiation (consider in high-risk patients)

Liver Function Tests (LFTs)

Rationale: Diltiazem is extensively metabolized by the liver; baseline assessment is prudent, especially in patients with hepatic impairment.

Timing: Prior to initiation (consider)

Renal Function (SCr, eGFR)

Rationale: To assess baseline renal function, as dose adjustments may be needed in severe impairment.

Timing: Prior to initiation (consider)

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Routine Monitoring

Blood Pressure (BP)

Frequency: Regularly (e.g., weekly initially, then monthly or as clinically indicated)

Target: <130/80 mmHg (or individualized target)

Action Threshold: Persistent BP above target or symptomatic hypotension

Heart Rate (HR)

Frequency: Regularly (e.g., weekly initially, then monthly or as clinically indicated)

Target: 50-90 bpm (or individualized target)

Action Threshold: Persistent bradycardia (<50 bpm) or symptomatic bradycardia

Symptoms of Edema

Frequency: At each visit

Target: Absence of significant peripheral edema

Action Threshold: Development of new or worsening peripheral edema

Symptoms of Dizziness/Lightheadedness

Frequency: At each visit

Target: Absence of symptoms

Action Threshold: Frequent or severe dizziness/lightheadedness

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Symptom Monitoring

  • Dizziness
  • Lightheadedness
  • Fatigue
  • Headache
  • Peripheral edema (swelling of ankles/feet)
  • Bradycardia (slow heart rate)
  • Palpitations
  • Shortness of breath
  • Chest pain (worsening angina)

Special Patient Groups

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Pregnancy

Diltiazem is classified as Pregnancy Category C. Animal studies have shown adverse effects on the fetus, but there are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Trimester-Specific Risks:

First Trimester: Potential for developmental abnormalities observed in animal studies; human data limited.
Second Trimester: Limited human data; use only if clearly needed.
Third Trimester: Limited human data; use only if clearly needed. Potential for fetal bradycardia or hypotension.
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Lactation

Diltiazem is excreted in human milk. The American Academy of Pediatrics considers diltiazem to be compatible with breastfeeding, but caution is advised. Monitor the infant for signs of bradycardia, hypotension, or sedation.

Infant Risk: L3 (Moderate concern - limited data, potential for adverse effects in infant; monitor infant)
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Pediatric Use

Safety and effectiveness of diltiazem extended-release capsules in pediatric patients have not been established. Use is generally not recommended.

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Geriatric Use

Elderly patients may have increased sensitivity to the effects of diltiazem, particularly regarding hypotension and bradycardia, due to age-related decreases in renal and hepatic function. Start with lower doses and titrate slowly, monitoring closely for adverse effects.

Clinical Information

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Clinical Pearls

  • Diltiazem XR should be swallowed whole; do not chew, crush, or divide the capsule, as this can lead to rapid release of the drug and potential overdose.
  • Take consistently at the same time each day.
  • Avoid abrupt discontinuation, especially in patients with angina, as it may exacerbate symptoms.
  • Monitor heart rate and blood pressure regularly, especially during dose titration.
  • Educate patients about symptoms of hypotension (dizziness, lightheadedness) and bradycardia (fatigue, fainting).
  • Be aware of significant drug interactions, particularly with beta-blockers, digoxin, and CYP3A4 substrates like statins.
  • Peripheral edema is a common side effect, often dose-dependent, and may be managed with diuretics or by lowering the dose.
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Alternative Therapies

  • Other calcium channel blockers (e.g., Amlodipine, Felodipine, Verapamil)
  • Beta-blockers (e.g., Metoprolol, Atenolol)
  • ACE inhibitors (e.g., Lisinopril, Ramipril)
  • Angiotensin Receptor Blockers (ARBs) (e.g., Valsartan, Losartan)
  • Diuretics (e.g., Hydrochlorothiazide, Furosemide)
  • Nitrates (for angina, e.g., Isosorbide mononitrate)
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Cost & Coverage

Average Cost: Varies widely, check current pharmacy pricing per 30 capsules
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (for generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide information about what was taken, the amount, and the time it occurred.