Cartia (diltiazem) 240mgxt Caps

Manufacturer ACTAVIS 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, Antiarrhythmic
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Pharmacologic Class
Non-dihydropyridine Calcium Channel Blocker
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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 is a medication that helps lower your blood pressure and can also treat chest pain (angina) by relaxing blood vessels and slowing your heart rate. It's a type of medicine called a calcium channel blocker.
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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 feeling better.

Some medications may need to be taken with food, while others should be taken on an empty stomach. It's crucial to check with your pharmacist to determine the best way to take your specific medication. Additionally, some products can be opened and mixed with a spoonful of applesauce, while others must be swallowed whole. Your pharmacist can advise you on whether your medication can be opened or if it needs to be taken as is.

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 moisture and humidity can affect its potency. Keep all medications in a secure location, out of the reach of children and pets.

When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. 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.

What to Do If You Miss a Dose

If you miss a dose, 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.
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Lifestyle & Tips

  • Follow a heart-healthy diet (low in sodium, saturated fat, cholesterol).
  • Engage in regular physical activity as advised by your doctor.
  • Maintain a healthy weight.
  • Limit alcohol consumption.
  • Quit smoking.
  • Manage stress.

Dosing & Administration

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Adult Dosing

Standard Dose: 120-240 mg orally once daily (extended-release capsule)
Dose Range: 120 - 540 mg

Condition-Specific Dosing:

hypertension: Initial: 180-240 mg once daily; Titrate up to 540 mg once daily based on response.
chronic stable angina: 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 for hypertension or angina. Limited data for supraventricular tachycardia.
Adolescent: Not established for hypertension or angina.
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Dose Adjustments

Renal Impairment:

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

Hepatic Impairment:

Mild: Use with caution, monitor for exaggerated effects.
Moderate: Consider lower initial doses and titrate slowly due to prolonged half-life and increased bioavailability.
Severe: Contraindicated or use with extreme caution; significant dose reduction likely required.

Pharmacology

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Mechanism of Action

Diltiazem is a non-dihydropyridine calcium channel blocker that inhibits the influx of extracellular calcium ions across the myocardial and vascular smooth muscle cell membranes. This leads to relaxation of vascular smooth muscle, resulting in vasodilation and a decrease in peripheral vascular resistance. In the heart, it decreases myocardial contractility, slows sinoatrial (SA) node firing, and prolongs atrioventricular (AV) node conduction, leading to a reduction in heart rate and myocardial oxygen demand.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 40-65% (due to first-pass metabolism), highly variable.
Tmax: Extended-release formulations: 6-11 hours.
FoodEffect: Food may increase bioavailability for some ER formulations, but generally can be taken with or without food. Consult specific product labeling.

Distribution:

Vd: Approximately 3-13 L/kg (large volume of distribution).
ProteinBinding: Approximately 70-80%.
CnssPenetration: Limited, but can cross the blood-brain barrier.

Elimination:

HalfLife: Extended-release formulations: 5-10 hours (terminal half-life).
Clearance: Primarily hepatic clearance.
ExcretionRoute: Approximately 60-65% in urine (as metabolites), 35% in feces (as metabolites).
Unchanged: Less than 4% excreted unchanged in urine.
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Pharmacodynamics

OnsetOfAction: Extended-release: Hours (for full antihypertensive/antianginal effect).
PeakEffect: Extended-release: 6-11 hours (corresponds to Tmax).
DurationOfAction: 24 hours (for extended-release formulations).

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Attention Immediately

While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:

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). Be aware of:
+ Shortness of breath
+ Significant weight gain
+ Swelling in the arms or legs
Severe skin reactions, such as:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other severe skin reactions, which can be life-threatening. Seek medical help if you experience:
+ Red, swollen, blistered, or peeling skin
+ 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 can cause side effects. Many people may not experience any side effects or only minor ones. If you notice any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:

Headache
* Feeling dizzy, tired, or weak

Reporting Side Effects

This is not an exhaustive list of possible 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 lightheadedness
  • Fainting spells
  • Unusual swelling in your ankles, feet, or hands
  • Shortness of breath, especially with exertion or lying down
  • Very slow or irregular heartbeat
  • New or 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:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction you experienced, including the 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.
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 health problems you are experiencing. Your doctor and pharmacist need this information to ensure safe use of this medication 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 down position, and exercise caution when navigating stairs.

Follow your doctor's instructions for monitoring your blood pressure and heart rate. You may need to undergo an electrocardiogram (ECG) before initiating treatment and periodically while taking this medication. Discuss any concerns or questions with your doctor.

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 regularly consume grapefruit juice or eat grapefruit, 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 (very slow heart rate)
  • Second- or third-degree AV block
  • Cardiac arrest
  • Dizziness, confusion
  • Nausea, vomiting

What to Do:

Seek immediate medical attention. Call 911 or your local poison control center (e.g., 1-800-222-1222 in the US).

Drug Interactions

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Contraindicated Interactions

  • Dantrolene (IV)
  • Ivabradine
  • Patients with sick sinus syndrome (unless a pacemaker is present)
  • Second- or third-degree AV block (unless a pacemaker is present)
  • Hypotension (systolic <90 mmHg)
  • Acute myocardial infarction and pulmonary congestion
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Major Interactions

  • Beta-blockers (e.g., metoprolol, propranolol): Increased risk of bradycardia, AV block, and heart failure.
  • Digoxin: Increased digoxin levels, leading to toxicity.
  • Statins (e.g., simvastatin, lovastatin, atorvastatin): Increased statin levels due to CYP3A4 inhibition, leading to increased risk of myopathy/rhabdomyolysis.
  • Amiodarone: Increased risk of bradycardia, AV block, and hypotension.
  • Fentanyl: Increased fentanyl levels, leading to respiratory depression.
  • Midazolam, Triazolam: Increased benzodiazepine levels, leading to increased sedation.
  • Cyclosporine, Tacrolimus, Sirolimus: Increased immunosuppressant levels, requiring dose adjustment and monitoring.
  • Carbamazepine, Phenytoin: Increased anticonvulsant levels.
  • Alpha-blockers (e.g., prazosin, doxazosin): Increased risk of hypotension.
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Moderate Interactions

  • Other antihypertensives: Additive hypotensive effects.
  • Grapefruit juice: May increase diltiazem levels.
  • Clonidine: Increased risk of bradycardia and AV block.
  • Rifampin: Decreased diltiazem levels.
  • Cimetidine: Increased diltiazem levels.
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Minor Interactions

  • Not typically listed as clinically significant minor interactions for diltiazem.

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 in patients with pre-existing bradycardia or on other rate-lowering drugs.

Timing: Prior to initiation.

Electrocardiogram (ECG)

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

Timing: Prior to initiation.

Liver Function Tests (LFTs)

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

Timing: Prior to initiation.

Renal Function (SCr, eGFR)

Rationale: To assess kidney function, though dose adjustment is not typically required for mild-moderate impairment, caution is advised in severe.

Timing: Prior to initiation.

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Routine Monitoring

Blood Pressure (BP)

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

Target: Individualized, typically <130/80 mmHg for hypertension.

Action Threshold: Persistent hypotension (e.g., SBP <90 mmHg) or inadequate BP control.

Heart Rate (HR)

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

Target: Typically >50-60 bpm.

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

Electrocardiogram (ECG) - PR interval

Frequency: Periodically, especially during dose titration or if symptoms of AV block develop.

Target: Normal PR interval (0.12-0.20 seconds).

Action Threshold: Significant prolongation of PR interval or development of higher-degree AV block.

Signs/Symptoms of Peripheral Edema

Frequency: At each visit.

Target: Absence of significant edema.

Action Threshold: Development of new or worsening peripheral edema.

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Symptom Monitoring

  • Dizziness
  • Lightheadedness
  • Fainting (syncope)
  • Shortness of breath
  • Swelling of ankles/feet (peripheral edema)
  • Unusual fatigue or weakness
  • Chest pain (worsening or new onset)
  • Palpitations (especially slow or irregular heartbeats)

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 teratogenicity observed in animal studies (e.g., skeletal abnormalities, embryolethality).
Second Trimester: Risk of fetal bradycardia or other cardiac effects.
Third Trimester: Risk of fetal bradycardia or other cardiac effects; potential for uterine relaxation.
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Lactation

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

Infant Risk: L3 (Moderately safe - monitor infant).
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Pediatric Use

Safety and efficacy have not been established for the treatment of hypertension or angina in pediatric patients. Use in children for other indications (e.g., supraventricular tachycardia) is off-label and requires careful consideration and specialized dosing.

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Geriatric Use

Elderly patients may be more sensitive to the hypotensive and bradycardic effects of diltiazem due to age-related changes in pharmacokinetics and pharmacodynamics. Start with lower doses and titrate slowly, monitoring closely for adverse effects.

Clinical Information

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Clinical Pearls

  • Extended-release capsules (e.g., Cartia XT) should be swallowed whole and not crushed, chewed, or divided, as this can lead to rapid release of the drug and potential overdose.
  • Diltiazem is a non-dihydropyridine CCB, which means it has significant effects on heart rate and AV conduction, unlike dihydropyridine CCBs (e.g., amlodipine).
  • Caution is advised when combining diltiazem with other medications that slow heart rate or AV conduction (e.g., beta-blockers, digoxin, amiodarone) due to increased risk of bradycardia and AV block.
  • Patients should be advised to avoid grapefruit juice as it can increase diltiazem levels.
  • Peripheral edema is a common side effect, often dose-dependent, and may be managed by dose reduction or addition of a diuretic.
  • Monitor for signs of liver injury, especially with long-term use or in patients with pre-existing hepatic impairment.
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Alternative Therapies

  • Other calcium channel blockers (e.g., amlodipine, felodipine, verapamil)
  • ACE inhibitors (e.g., lisinopril, enalapril)
  • Angiotensin Receptor Blockers (ARBs) (e.g., valsartan, losartan)
  • Beta-blockers (e.g., metoprolol, carvedilol)
  • Diuretics (e.g., hydrochlorothiazide, furosemide)
  • Nitrates (for angina) (e.g., isosorbide mononitrate, nitroglycerin)
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Cost & Coverage

Average Cost: $30 - $150 per 30 capsules (generic 240mg ER)
Generic Available: Yes
Insurance Coverage: Tier 1 (generic) or Tier 2/3 (brand) for most commercial and Medicare Part D plans.
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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.