Cardiloc 2.5

Cardiloc 2.5 is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension. Cardiloc 2.5 is structurally similar to metoprolol, acebutolol and atenolol in that it has two substituents in the para position of the benzene ring. The β1-selectivity of these agents is thought to be due in part to the large substituents in the para position. At lower doses (less than 20 mg daily), Cardiloc 2.5 selectively blocks cardiac β1-adrenergic receptors with little activity against β2-adrenergic receptors of the lungs and vascular smooth muscle. Receptor selectivity decreases with daily doses of 20 mg or greater. Unlike propranolol and pindolol, Cardiloc 2.5 does not exhibit membrane-stabilizing or sympathomimetic activity. Cardiloc 2.5 possesses a single chiral centre and is administered as a racemic mixture. Only l-Cardiloc 2.5 exhibits significant β-blocking activity.

Cardiloc 2.5 fumarate, a type of medication known as a beta-blocker, is used to treat high blood pressure. Beta-blockers lower blood pressure by decreasing the force and rate of heart contractions, which reduces the heart’s demand for oxygen. Cardiloc 2.5 fumarate can be used alone or in combination with other high blood pressure medications.

Cardiloc 2.5 is used alone or together with other medicines to treat high blood pressure (hypertension). High blood pressure adds to the workload of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. These problems may be less likely to occur if blood pressure is controlled.

Cardiloc 2.5 is a beta-blocker. It works by affecting the response to nerve impulses in certain parts of the body, like the heart. As a result, the heart beats slower and decreases the blood pressure. When the blood pressure is lowered, the amount of blood and oxygen is increased to the heart.

Cardiloc 2.5 is available only with your doctor's prescription.

Treatment should always be started gradually with low doses and then increased slowly. The dosage should be determined on an individual basis in each case, particularly depending on the pulse rate and success of treatment.

Essential Hypertension: Recommended Dose: 5 mg once daily (equivalent to 1 film-coated tablet of Cardiloc 2.5 5 mg or ½ film-coated tablet of Cardiloc 2.5 10 mg).

In milder forms of hypertension (diastolic blood pressure up to 105 mmHg), treatment with Cardiloc 2.5 fumarate 2.5 mg once daily (equivalent to ½ film-coated tablet of Cardiloc 2.5 5 mg) may be sufficient.

If required, the dose may be increased to Cardiloc 2.5 fumarate 10 mg once daily (equivalent to 2 film-coated tablets of Cardiloc 2.5 5 mg or 1 film-coated tablet of Cardiloc 2.5 10 mg).

Further dose increase is justified only in exceptional cases.

Maximum Recommended Dose: 20 mg once daily.

Coronary Heart Disease (Angina Pectoris): Recommended Dose: 5 mg once daily (equivalent to 1 film-coated tablet of Cardiloc 2.5 5 mg or ½ film-coated tablet of Cardiloc 2.5 10 mg).

If required, the dose may be increased to Cardiloc 2.5 fumarate 10 mg once daily (equivalent to 2 film-coated tablets of Cardiloc 2.5 5 mg or 1 film-coated tablet of Cardiloc 2.5 10 mg).

Further dose increase is justified only in exceptional cases.

Maximum Recommended Dose: 20 mg once daily.

Treatment with Cardiloc 2.5 5 mg or 10 mg should not be stopped abruptly, particularly in patients with coronary heart disease, since this may lead to acute worsening of patient's condition. If discontinuation of treatment is necessary, the dose should be reduced gradually (eg, divided into halves weekly).

Hepatic and/or Renal Dysfunctions: In patients with mild or moderate hepatic and/or renal dysfunction, dose adjustment is not necessary in general. In patients with advanced renal insufficiency (CrCl <20 mL/min) and in patients with severe hepatic dysfunction, daily dose of Cardiloc 2.5 fumarate 10 mg should not be exceeded.

Stable Chronic Heart Failure: Standard treatment of chronic heart failure is performed with an ACE inhibitor (or another vasodilator if ACE inhibitors are not tolerated), a β-blocker, diuretics, and if necessary, cardiac glycosides. The patients should have stable chronic heart failure (without acute heart failure) at the beginning of Cardiloc 2.5 treatment.

Recommendation: It is recommended that the treating physician should be experienced in management of chronic heart failure.

Transient exacerbation of heart failure, hypotension or bradycardia may occur during and after titration phase.

Titration Phase: Treatment of chronic heart failure with Cardiloc 2.5 requires gradual dose titration.

Treatment with Cardiloc 2.5 must be initiated with gradual dose increase according to the following scheme: 1.25 mg once daily for 1 week (other dose strengths are available for this dosage). If this dose is well tolerated, increase to 2.5 mg once daily for 1 week; then, increase to 3.75 mg once daily for 1 week (other dose strengths are available for this dosage). If this dose is well tolerated, increase to 5 mg once daily for 4 week; then, increase to 7.5 mg once daily for 4 weeks (other dose strength are available for this dosage). If this dose is well tolerated, increase to 10 mg daily as maintenance dose.

Maximum Recommended Dose: Cardiloc 2.5 10 mg once daily.

Close monitoring of vital functions (heart rate, blood pressure) as well as for signs of worsening heart failure is recommended during the titration phase. Symptoms may already occur on the first day when starting treatment.

Dose Adjustment: If the highest recommended dosage is not tolerated, gradual reduction may be considered.

In case of transient exacerbation of heart failure, hypotension or bradycardia, the dosage of the adjuvant medication should be re-assessed. Transient reduction or discontinuation of Cardiloc 2.5 may also be necessary.

When the patient's condition has stabilized again, resumption of treatment and/or increase in the Cardiloc 2.5 dose should always be considered.

If discontinuation of treatment is considered, the dose should be reduced gradually, since abrupt withdrawal may lead to acute exacerbation of the disease.

Treatment of stable chronic heart failure with Cardiloc 2.5 is generally long-term treatment.

Treatment with Cardiloc 2.5 should not be discontinued abruptly, since this might lead to a transitory worsening of heart failure. If discontinuation of treatment is necessary, the dose should be gradually decreased (eg, divided into halves weekly).

Renal or Hepatic Insufficiency: There are no pharmacokinetic studies in patients with chronic heart failure, and with impaired liver or renal function. Increase of the dose in these patients should therefore be made with additional caution.

Elderly: No dose adjustment is necessary.

Children: There is no pediatric experience with Cardiloc 2.5; therefore, its use cannot be recommended for children.

Administration: The film-coated tablets are to be taken unchewed together with sufficient liquid, preferably on an empty stomach in the morning or together with breakfast.

Duration of Use: The duration of use is not limited. It depends on the type and severity of the disease.

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What is the most important information I should know about Cardiloc 2.5?

Do not skip doses or stop taking Cardiloc 2.5 without first talking to your doctor. Stopping suddenly may make your condition worse or cause other serious heart problems.

If you need to have any type of surgery, tell the surgeon ahead of time that you are using Cardiloc 2.5.

Cardiloc 2.5 can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert.

Avoid drinking alcohol. It can increase some of the side effects of Cardiloc 2.5.

Cardiloc 2.5 is only part of a complete program of treatment for hypertension that may also include diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely if you are being treated for hypertension.

Keep using this medicine as directed, even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.

Use Cardiloc 2.5 as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Cardiloc 2.5 by mouth with or without food.
• Taking Cardiloc 2.5 at the same time each day will help you remember to take it.
• Continue to take Cardiloc 2.5 even if you feel well. Do not miss any doses.
• If you miss a dose of Cardiloc 2.5, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Cardiloc 2.5.

Use: Labeled Indications

Hypertension: Management of hypertension. Note: Beta-blockers are not recommended as first-line therapy (ACC/AHA [Whelton 2017]).

Off Label Uses

Acute MI

According to the American College of Cardiology/American Heart Association (ACC/AHA) guidelines for the management of ST-elevation myocardial infarction (STEMI) and the ACC/AHA guidelines for the management of non-ST-elevation ACS (NSTE-ACS), oral beta-blockers should be initiated within the first 24 hours unless the patient has signs of heart failure, evidence of a low-output state, an increased risk for cardiogenic shock, or other contraindications. However, recommendations do not specify any particular beta-blocking agent for optimal treatment of NSTE-ACS. Thus, clinicians must use practical experience to determine proper therapy in managing patients.

Based on the American College of Cardiology Foundation/American Heart Association (ACCF/AHA) 2013 heart failure guidelines, the use of 1 of the 3 beta-blockers (ie, Cardiloc 2.5, carvedilol, or extended-release metoprolol succinate) is effective and recommended for all patients with recent or remote history of MI or ACS and reduced ejection fraction (rEF) to reduce mortality, for all patients with rEF to prevent symptomatic heart failure (HF) even if no history of MI, and for all patients with current or prior symptoms of HF with reduced ejection fraction (HFrEF), unless contraindicated to reduce morbidity and mortality.

Ventricular arrhythmias

Based on the American Heart Association/American College of Cardiology/Heart Rhythm Society (AHA/ACC/HRS) guideline for management of patients with ventricular arrhythmias and prevention of sudden cardiac death, beta-blockers are effective for control of ventricular arrhythmias and ventricular premature beats.

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What other drugs will affect Cardiloc 2.5?

Cardiloc 2.5 may potentiate the effect of other antihypertensive drugs concurrently administered. Concomitant therapy of Cardiloc 2.5 and reserpine, α-methyldopa, clonidine and guanfacine, may cause a considerable decrease in heart rate.

In concomitant treatment with clonidine, clonidine should not be discontinued unless administration of Cardiloc 2.5 has been terminated for a few days.

The concurrent use of nifedipine may potentiate the antihypertensive effect of Cardiloc 2.5. In concurrent use of Cardiloc 2.5 and calcium antagonists of the verapamil and diltiazem type or other antiarrhythmic agents, careful monitoring of the patient is indicated, as this can cause hypotension, bradycardia and other conditions of arrhythmia. The IV administration of calcium antagonists and antiarrhythmic agents is therefore not recommended during treatment with Cardiloc 2.5.

The concurrent use of Cardiloc 2.5 and rifampicin can slightly reduce the half-life of Cardiloc 2.5. An increase in dose is generally not necessary.

The concurrent use of Cardiloc 2.5 and insulin or oral blood sugar-reducing drugs may potentiate the effect of the latter. The symptoms of hypoglycemia (in particular tachycardia) are masked or mitigated. Blood sugar levels should be monitored regularly.

As cardiac output may be impaired under anesthesia, prior to an operation, the anesthetist should be informed if the patient is being treated with Cardiloc 2.5.

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What are the possible side effects of Cardiloc 2.5?

Applies to Cardiloc 2.5: oral tablet

As well as its needed effects, Cardiloc 2.5 (the active ingredient contained in Cardiloc 2.5) may cause unwanted side effects that require medical attention.

Major Side Effects

If any of the following side effects occur while taking Cardiloc 2.5, check with your doctor immediately:

Less common:

• Body aches or pain
• chest pain
• chills
• cough
• difficult or labored breathing
• ear congestion
• fever
• headache
• loss of voice
• nasal congestion
• pain or tenderness around eyes and cheekbones
• shortness of breath or troubled breathing
• sneezing
• sore throat
• stuffy or runny nose
• tightness in chest
• unusual tiredness or weakness
• wheezing

• Chest discomfort
• lightheadedness, dizziness, or fainting
• slow or irregular heartbeat

If any of the following symptoms of overdose occur while taking Cardiloc 2.5, get emergency help immediately:

Symptoms of overdose:

• Anxiety
• blurred vision
• cold sweats
• coma
• confusion
• cool, pale skin
• decreased urine output
• depression
• dilated neck veins
• dizziness, faintness, or lightheadedness when getting up from a lying or sitting position suddenly
• extreme fatigue
• fast heartbeat
• increased hunger
• irregular breathing
• nausea
• nervousness
• nightmares
• noisy breathing
• seizures
• shakiness
• slurred speech
• sweating
• swelling of face, fingers, feet, or lower legs
• weight gain

Minor Side Effects

Some Cardiloc 2.5 side effects may not need any medical attention. As your body gets used to the medicine these side effects may disappear. Your health care professional may be able to help you prevent or reduce these side effects, but do check with them if any of the following side effects continue, or if you are concerned about them:

Less common:

• Abnormal or decreased touch sensation
• diarrhea
• difficulty in moving
• lack or loss of strength
• muscle pain or stiffness
• pain in joints
• sleeplessness
• trouble sleeping
• unable to sleep
• vomiting