Cardizem

$ 124.52$ 464.11

Category: Blood Pressure
Commercial name: Cardizem
Active ingredient: Diltiazem
Production form: Pills
Available dosage: 60 mg, 90 mg, 120 mg, 180 mg

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Description

Cardizem (Diltiazem). Dosage, Side Effects, Interactions

Cardizem (Diltiazem) is used as a calcium channel antagonist (calcium channel blocker) to treat heart disease. The heart drug has a vasodilating effect and delays conduction, which means that it is also used in arrhythmias (cardiac arrhythmias) as a class IV antiarrhythmic. Diltiazem also lowers blood pressure and can be used locally to treat anal fissures.

The calcium channel blocker diltiazem has the following indications:

  • chronic stable angina pectoris (stress angina)
  • unstable angina pectoris (crescendo angina, resting angina)
  • vasospastic angina pectoris (Prinzmetal’s angina, variant angina)
  • hypertension
  • cardiac arrhythmias

The active ingredient is available on the market in the form of tablets, film-coated tablets, sustained-release tablets and sustained-release hard capsules.

How Cardizem (Diltiazem) works

Diltiazem is a cationic amphiphilic drug whose positively charged nitrogen is important for binding to the channel protein. As a calcium channel blocker , diltiazem inhibits the influx of calcium ions through the voltage-gated L-type calcium channel. As a result, the drug has a vasodilating and blood pressure-lowering effect by reducing peripheral vascular resistance. Diltiazem reduces heart rate, AV conduction, contractile force and has antiarrhythmic effects. In addition, diltiazem has a negative dromotropic effect on the AV node and a negative chronotropic effect on the sinus node.

Pharmacokinetics

  • Diltiazem is subject to a pronounced first pass metabolism, so that the systemic availability is only about 40%.
  • Maximum plasma concentrations are reached after 3 to 4 hours after oral administration.
  • Plasma protein binding is 70-85%, with 35-40% bound to albumin.
  • Diltiazem is almost completely metabolised in the liver.
  • Compared to the unchanged substance, the primary metabolites N-desmethyldiltiazem and desacetyldiltiazem show a reduced pharmacological effect (about 20% and about 25 to 50% of the potency, respectively).
  • The other metabolites are pharmacologically inactive.
  • Delayed metabolism is to be expected in the presence of liver dysfunction.
  • The elimination half-life averages 6 hours and may be longer, particularly in elderly patients and patients with hepatic impairment.

Dosage of Cardizem (Diltiazem)

Treatment hypertension

  • Extended release capsules: Initial dose: 120 to 240 mg po once daily. Increase dose as needed to a maintenance dose of 120 to 540 mg po once daily. The maximum dose is 540 mg/day.
  • Extended-Release Coated Capsules : Starting dose: 180 to 240 mg po once daily, increasing dose as needed. Maintenance dose: 240 to 360 mg po once daily. Maximum dose: 480 mg/day.
  • Extended release tablets: Starting dose: 180 to 240 mg po once daily. Increase dose as needed to a maximum dose of 540 mg/day.

treatment of atrial fibrillation

  • Bolus injection : Initial bolus dose: 0.25 mg/kg IV as a bolus administered over 2 minutes. After 15 minutes, a second bolus of 0.35 mg/kg IV (over 2 minutes) can be administered if needed.
  • Continuous infusion: The continuous infusion should begin immediately after a 0.25 mg/kg iv bolus or 0.35 mg/kg iv over 2 minutes. Initial infusion rate: 10 mg/h. Maintenance infusion rate: The infusion rate can be increased in increments of 5 mg/h up to 15 mg/h. Maximum duration: 24 hours.

treatment of atrial flutter

  • Bolus injection : Initial bolus dose: 0.25 mg/kg IV as a bolus administered over 2 minutes. After 15 minutes, a second bolus of 0.35 mg/kg IV (given over 2 minutes) may be administered if needed.
  • Continuous infusion: The continuous infusion should begin immediately after a bolus injection of 0.25 mg/kg IV or 0.35 mg/kg IV over 2 minutes. Initial infusion rate: 10 mg/h. Maintenance infusion rate: The infusion rate can be increased in increments of 5 mg/h up to 15 mg/h. Maximum duration: 24 hours.

Supraventricular tachycardia

  • Bolus injection : Initial bolus dose: 0.25 mg/kg IV as a bolus administered over 2 minutes. After 15 minutes, a second bolus of 0.35 mg/kg IV (over 2 minutes) can be administered if needed.
  • ontinuous infusion: The continuous infusion should begin immediately after a bolus injection of 0.25 mg/kg iv or 0.35 mg/kg iv over 2 minutes. Initial infusion rate: 10 mg/h. Maintenance infusion rate: The infusion rate can be increased in increments of 5 mg/h up to 15 mg/h. Maximum duration: 24 hours.

Angina pectoris prophylaxis

  • Extended-Release Capsules : Starting dose: 120 to 180 mg po once daily, increasing dose every 7 to 14 days as needed. Maximum dose: 540 mg/day.
  • Extended-Release Coated Capsules: Starting dose: 120 to 180 mg po once daily, increasing dose every 7 to 14 days as needed. Maximum dose: 480 mg/day
  • Extended release tablets: Starting dose: 180 mg po once daily, increasing dose every 7 to 14 days as needed. Maximum dose: 360 mg/day.
  • Immediate release tablets: Starting dose: 30 mg po 4 times a day (before meals and at bedtime), increasing gradually every 1 to 2 days until optimal response is achieved. Maintenance dose: 180 to 360 mg orally per day in divided doses (3 to 4 times daily).

Congestive heart failure

  • Extended release capsules: Starting dose: 120 to 180 mg po once daily, increasing dose every 7 to 14 days as needed. Maximum dose: 540 mg/day.
  • Extended-Release Coated Capsules: Starting dose: 120 to 180 mg po once daily, increasing dose every 7 to 14 days as needed. Maximum dose: 480 mg/day
  • Extended release tablets: Starting dose: 180 mg po once daily, increasing dose every 7 to 14 days as needed. Maximum dose: 360 mg/day.
  • Immediate release tablets: Starting dose: 30 mg po 4 times a day (before meals and at bedtime), increasing gradually every 1 to 2 days until optimal response is achieved. Maintenance dose: 180 to 360 mg orally per day in divided doses (3 to 4 times daily).

Side effects of Cardizem (Diltiazem)

Very common side effects (≥1/10) include:

  • peripheral edema

Very common (≥ 1/100 to < 1/10) include:

  • Headache, dizziness, tiredness, feeling weak
  • AV block, ankle or leg edema
  • flush
  • Constipation, dyspepsia, stomach pain, nausea
  • allergic skin reactions, itching, reddening of the skin
  • general mood disorders

Interactions

  • Diltiazem is metabolised by CYP3A4 . In cases of concomitant use with a stronger CYP3A4 inhibitor, there may be an increase in diltiazem plasma levels
  • CYP3A4 substrates: increase in plasma levels of each of the two drugs co-administered
  • CYP3A4 inducer: reduction in diltiazem plasma levels
  • Glucocorticoids ( methylprednisolone ): inhibition of methylprednisolone metabolism (CYP3A4) and inhibition of P-glycoprotein
  • Lithium : Risk of increased lithium toxicity
  • Nitrate derivatives: Increased antihypertensive effect and feeling of weakness
  • Alpha antagonists: hypotension
  • Amiodarone and digoxin : increased risk of bradycardia
  • Beta-receptor blockers , antiarrhythmics or cardiac glycosides : increased effect possible
  • Drugs that are broken down via CYP3A4 e.g. simvastatin , lovastatin or atorvastatin : Increased and/or prolonged effect including side effects (e.g. rhabdomyolysis, myositis or hepatitis )
  • Carbamazepine , midazolam , triazolam , alfentanil , theophylline , ciclosporin A , digoxin and digitoxin : Plasma levels may increase during concomitant treatment with diltiazem
  • Rifampicin : risk of decreasing diltiazem plasma levels
  • Cimetidine or ranitidine : increase in diltiazem plasma levels
  • Nifedipine : decreased clearance of nifedipine

Contraindication

Diltiazem must not be used in:

  • Hypersensitivity to the active substance
  • AV block II. or III. degrees
  • SA block II. and III. degrees
  • Sinus node syndrome, except in patients with a pacemaker
  • shock
  • Acute myocardial infarction with complications (bradycardia, pronounced hypotension, left ventricular failure)
  • manifest heart failure
  • severe bradycardia (resting heart rate below 40 beats per minute)
  • simultaneous intravenous administration of dantrolene
  • simultaneous intravenous administration of beta-blockers
  • Combination with ivabradine
  • Left ventricular failure with pulmonary congestion
  • pregnancy and breast feeding period

Pregnancy

Diltiazem should not be taken during pregnancy.

Lactation

Diltiazem should not be taken while breast-feeding.

Driving ability

Verapamil can have individually different effects on the ability to react and change it to such an extent that the ability to drive, use machines or work without a secure footing can be impaired.

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Additional information

Dosage

60 mg, 90 mg, 120 mg, 180 mg

Quantity

30, 60, 90, 120, 180

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