Diltiazem ER 420mg Capsules (24 Hr)

Manufacturer OCEANSIDE 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
Calcium Channel Blocker
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Pharmacologic Class
Benzothiazepine Calcium Channel Blocker
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Pregnancy Category
Category C
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FDA Approved
Jan 1970
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Diltiazem is a medication that helps relax blood vessels and slow down your heart rate. This makes it easier for your heart to pump blood, which can help lower high blood pressure and reduce chest pain (angina). It's a long-acting capsule, meaning you usually 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, it's essential to take it as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. 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.

Some medications may need to be taken with food, while others should be taken on an empty stomach. Check with your pharmacist to determine the best way to take your specific medication. In some cases, you may be able to open the medication and mix it with a spoonful of applesauce, but be sure to check with your pharmacist first to see if this is acceptable. Other medications must be swallowed whole, so it's crucial to follow the correct administration instructions.

Storing and Disposing of Your Medication

To maintain the effectiveness and safety of your medication, store it at room temperature, protected from light, and in a dry place. Avoid storing your medication in a bathroom, as the humidity and temperature fluctuations can affect its potency. Keep all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion or overdose.

When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless specifically instructed to do so by your pharmacist or healthcare provider. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs in your area, which can provide a safe and environmentally responsible way to dispose of unwanted medications.

What to Do If You Miss a Dose

If you miss a dose of your medication, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one, as this can increase the risk of adverse effects.
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Lifestyle & Tips

  • Take the medication exactly as prescribed, usually once daily, at the same time each day.
  • Swallow the capsule whole; do not crush, chew, or divide it.
  • Do not stop taking this medication suddenly without consulting your doctor, as it can worsen your condition.
  • Monitor your blood pressure and heart rate regularly as advised by your doctor.
  • Maintain a healthy lifestyle, including a balanced diet (low in sodium and saturated fats), regular exercise, and limiting alcohol intake.
  • Avoid grapefruit and grapefruit juice while taking this medication, as it can increase drug levels and side effects.
  • Report any new or worsening symptoms to your doctor.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: 420 mg once daily
Dose Range: 120 - 540 mg

Condition-Specific Dosing:

hypertension: Initial dose typically 180-240 mg once daily, titrate up to 420 mg once daily based on response.
chronicStableAngina: Initial dose typically 120-180 mg once daily, titrate up to 420 mg once daily based on response.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established (safety and efficacy not established for ER formulations)
Adolescent: Not established (safety and efficacy not established for ER formulations)
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment generally needed, monitor for exaggerated effects.
Moderate: No specific adjustment generally needed, monitor for exaggerated effects.
Severe: Use with caution, monitor for exaggerated effects. Lower starting doses may be considered.
Dialysis: Diltiazem is not significantly removed by dialysis. 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. Lower starting doses may be considered.
Severe: Use with caution, monitor for exaggerated effects. Lower starting doses may be considered due to prolonged half-life.

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 through voltage-dependent L-type calcium channels. This leads to relaxation of vascular smooth muscle, resulting in peripheral and coronary vasodilation, and a reduction in myocardial contractility and heart rate. These actions decrease myocardial oxygen demand and increase myocardial oxygen supply.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 40-65% (variable due to first-pass metabolism, for ER formulations)
Tmax: Approximately 10-14 hours (for ER formulations)
FoodEffect: Food may increase bioavailability and delay Tmax, but generally does not significantly alter overall exposure for ER formulations; can be taken with or without food.

Distribution:

Vd: Approximately 3-13 L/kg
ProteinBinding: Approximately 70-85%
CnssPenetration: Limited

Elimination:

HalfLife: Approximately 5-10 hours (for ER formulations, can be longer with chronic dosing)
Clearance: Approximately 0.6-1.3 L/min
ExcretionRoute: Primarily urine (approximately 60-65%) and feces (approximately 35%)
Unchanged: Less than 4% (in urine)
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Pharmacodynamics

OnsetOfAction: Within 30-60 minutes (for ER formulations, clinical effect may take longer to stabilize)
PeakEffect: Approximately 10-14 hours (for ER formulations)
DurationOfAction: 24 hours (for ER 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), characterized by:
+ 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, which may be life-threatening
+ Symptoms may include:
- Red, swollen, blistered, or peeling skin
- Skin irritation (with or without fever)
- Red or irritated eyes
- Sores in the mouth, throat, nose, or eyes

Other Possible Side Effects

Most people experience either no side effects or only mild side effects while taking this medication. However, if you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention:

Headache
* Feeling dizzy, tired, or weak

Reporting Side Effects

This list is not exhaustive, and you may experience other side effects not mentioned here. 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 (e.g., less than 50 beats per minute)
  • Shortness of breath, especially with exertion or lying down
  • Swelling in your ankles, feet, or legs
  • Unusual fatigue or weakness
  • Worsening chest pain
  • Signs of liver problems (e.g., yellowing of skin/eyes, dark urine, persistent nausea/vomiting, severe stomach pain)
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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 conditions to ensure safe treatment:

Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
Certain types of abnormal heart rhythms, as this medication is not suitable for all types. If you are unsure, consult your doctor or pharmacist for guidance.
Specific health conditions, including:
+ Fluid accumulation in the lungs
+ Low blood pressure
+ Recent heart attack
Concurrent use of certain medications, such as:
+ Ivabradine
+ Rifampin

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. Your doctor and pharmacist need this information to assess potential interactions and ensure safe treatment. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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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 treatment and periodically while taking this medication. Consult with your doctor regarding the frequency of these checks.

If you have high blood pressure, 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, planning to become pregnant, or 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)
  • Heart block (abnormal heart rhythm)
  • Cardiogenic shock
  • Asystole (cardiac arrest)
  • Dizziness
  • Fainting
  • 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 gastric lavage, activated charcoal, IV fluids, atropine, calcium gluconate, vasopressors, or cardiac pacing.

Drug Interactions

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Contraindicated Interactions

  • Ivabradine (risk of severe bradycardia)
  • Dantrolene (IV) (risk of hyperkalemia and myocardial depression)
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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 (diltiazem is a CYP3A4 inhibitor)
  • Fentanyl (CYP3A4 substrate) - increased fentanyl levels, risk of respiratory depression
  • Immunosuppressants (e.g., cyclosporine, tacrolimus, sirolimus) - increased immunosuppressant levels, risk of toxicity
  • 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
  • CYP3A4 inhibitors (e.g., ketoconazole, erythromycin, grapefruit juice) - increased diltiazem levels
  • CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort) - decreased diltiazem levels
  • Benzodiazepines (e.g., midazolam, triazolam) - increased benzodiazepine levels
  • Carbamazepine - increased carbamazepine levels
  • Theophylline - increased theophylline levels
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Minor Interactions

  • NSAIDs - may reduce antihypertensive effect
  • Cimetidine - may increase diltiazem levels

Monitoring

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Baseline Monitoring

Blood Pressure (BP)

Rationale: To establish baseline and guide initial dosing.

Timing: Prior to initiation

Heart Rate (HR)

Rationale: To establish baseline and assess for bradycardia.

Timing: Prior to initiation

Electrocardiogram (ECG)

Rationale: To assess for pre-existing conduction abnormalities (e.g., AV block).

Timing: Prior to initiation, especially in patients with cardiac history

Liver Function Tests (LFTs)

Rationale: Diltiazem is metabolized by the liver; to assess baseline hepatic function.

Timing: Prior to initiation, especially in patients with hepatic impairment

Renal Function (SCr, BUN)

Rationale: To assess baseline renal function, though renal excretion is minor.

Timing: Prior to initiation, especially in patients with renal impairment

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Routine Monitoring

Blood Pressure (BP)

Frequency: Regularly, e.g., weekly during titration, then monthly/quarterly once stable

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

Action Threshold: Persistent hypotension (<90/60 mmHg) or uncontrolled hypertension

Heart Rate (HR)

Frequency: Regularly, e.g., weekly during titration, then monthly/quarterly once stable

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: New or worsening peripheral edema

Symptoms of dizziness/lightheadedness

Frequency: At each visit

Target: Absence of symptoms

Action Threshold: New or worsening dizziness/lightheadedness

ECG (PR interval)

Frequency: Periodically, or if symptoms of conduction disturbance occur

Target: Normal PR interval (<0.20 sec)

Action Threshold: Significant prolongation of PR interval or development of AV block

Liver Function Tests (LFTs)

Frequency: Periodically, or if symptoms of hepatic dysfunction occur

Target: Within normal limits

Action Threshold: Significant elevation of liver enzymes

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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)
  • Constipation
  • Rash

Special Patient Groups

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Pregnancy

Diltiazem is Pregnancy Category C. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects on the fetus.

Trimester-Specific Risks:

First Trimester: Potential for teratogenicity observed in animal studies at high doses; human data are limited.
Second Trimester: Limited human data; use with caution.
Third Trimester: Limited human data; use with caution. May cause fetal bradycardia or hypotension.
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Lactation

Diltiazem is excreted in breast milk. The American Academy of Pediatrics considers it compatible with breastfeeding, but caution is advised. Monitor the infant for bradycardia, hypotension, and sedation.

Infant Risk: L3 (Moderately Safe). Potential for infant bradycardia, hypotension, or sedation. Monitor infant closely.
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Pediatric Use

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

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Geriatric Use

Geriatric patients may be more sensitive to the effects of diltiazem, particularly regarding hypotension and bradycardia. Lower starting doses and careful titration are recommended. Monitor renal and hepatic function more closely.

Clinical Information

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Clinical Pearls

  • Diltiazem ER is designed for once-daily dosing; emphasize adherence and not crushing/chewing capsules.
  • It is a non-dihydropyridine CCB, affecting both vascular smooth muscle and cardiac conduction/contractility, unlike dihydropyridines (e.g., amlodipine) which are primarily vasodilators.
  • Caution is paramount when co-administering with beta-blockers or digoxin due to additive effects on heart rate and AV conduction.
  • Patients should be advised to avoid grapefruit products due to potential for increased diltiazem levels.
  • Peripheral edema is a common side effect, but it is typically less pronounced than with dihydropyridine CCBs.
  • Monitor for signs of heart failure exacerbation, especially in patients with pre-existing left ventricular dysfunction.
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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, typically $50-$300+ 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's essential to contact your doctor for further guidance. 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 be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.