Agicardi 2.5 Agimexpharm medicine for hypertension, chronic stable angina (3 blisters x 10 tablets)

ATC code: C07AB07.

Bisoprolol is a selective blockbuster Beta1 (β1) but has no membrane stability and has no effect like intrinsic sympathetic nerve when used within the scope of treatment. With low doses, Bisoprolol inhibits selectively responding to adrenalin stimulation by competing receptors β1 adrenergic of the heart, but has little effect on receptor β2 adrenergic of bronchial muscles and vascular walls. With high doses (for example, 20 mg or more), the selective properties of bisoprolol on receptors β1 usually decrease and the drug will compete inhibiting both receptors β1 and β2.

Bisoprolol is used to treat hypertension. Bisoprolol's effectiveness is equivalent to other beta blockers. Bisoprolol's mechanism of hypotension may include the following factors:

Reducing heart flow, renal inhibition releases renin and reducing the impact of sympathetic nerve from vascular centers in the brain.

But Bisoprolol's most prominent effect is to reduce the heart frequency, both at leave and at exertion.

Bisoprolol reduces the flow of the heart at the time of rest and when exertion, accompanied by few changes in the volume of blood emul for each heart squeeze, and only increases less right atrial pressure or pulmonary capillary pressure at rest and exertion.

The good effect of beta blockers in the treatment of congestive heart failure is mainly due to inhibition of the effects of sympathetic nervous system. Using long -term beta blockers, as well as angiotensin enzyme inhibitors, can reduce the symptoms of heart failure and improve the clinical condition of people with chronic heart failure. These beneficial effects have been proven in people who are taking an enzyme inhibitor, showing the coordination of the reinforcement effect of the renin-ankiotensin system and inhibiting sympathetic nervous system is the effects of copper in the treatment of chronic heart failure.

Dynamic pharmacokinetics

absorption: Bisoprolol is almost completely absorbed through the gastrointestinal tract, food does not affect the absorption of drugs.

Distribution: About 30% of the drug is attached to plasma proteins. The distribution volume is 3.5 liters/kg. Total clearance of about 15 liters/hour

Metabolism: Because only the initial metabolism is very little in the liver, oral bioavails are about 90%. After drinking, the peak concentration in plasma is reached from 2 - 4 hours.

Elimination: Sell waste time in plasma from 10 to 12 hours. Bisoprolol is moderately dissolved in lipid.

Metabolic drugs in the liver and excretion in urine, about 50% in constant form and 50% in the form of metabolites.

In the elderly, the sale time in plasma is slightly longer than young people, although the average plasma concentration in a stable state increases, but there is no significant difference in the accumulation of bisoprolol between young people and the elderly.

In people with creatinine clearance coefficient below 40 ml/minute, plasma disposal time increases about 3 times higher than normal people.

In people with cirrhosis, the rate of excretion of Bisoprolol changes more and lower is significant than normal people (8.3 - 21.7 hours).

Change of treatment:

During the dose adjustment phase or then, if the bad cases occur such as severe heart failure, hypotension or slow heart rate, it is advisable to review the dose of the in combination and reduce the dose of Bisoprolol temporary or consider stopping bisoprolol treatment as needed.

Should consider reusing bisoprolol or adjusting the dose increasing when the patient is stable again.

Treatment of chronic heart failure with bisoprolol is usually long -term treatment, should not stop suddenly because it can worsen the heart failure. If the drug is needed, the dose should be reduced gradually, dividing the dose half a week.

Special subjects:

People with liver or kidney failure:

Treatment of hypertension or chronic stable angina: No need to adjust the dose of bisoprolol in patients with liver or kidney dysfunction mild or medium level. In patients with severe renal impairment (creatinine clearance

Treatment of stable chronic heart failure: There is no information on bisoprolol pharmacokinetics in patients with chronic heart failure with liver or kidney failure. Determining the dose for these cases should be very cautious.

Elderly:

usually do not need to adjust the dose. Should start with the lowest dose possible.

Children:

There is no experience using bisoprolol in children, so it is recommended not to use this drug in children.

Some special notes on drug treatment before and after using the drug:

There is no special requirement on drug treatment after use.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.

What to do when overdose?

Overdose:

There are some cases of overdose with Bisoprolol Fumarat that have been notified (maximum: 2,000 mg). Observed the slow heart rate and/or hypotension. In some cases, the drugs have been used as sympathetic nerve and all the patients have recovered.

Signs of overdose due to beta blockers include slow heartbeat, hypotension and sleeping, and if severe, delirium, coma, convulsions and respiratory arrest. Sound blood failure, bronchospasm and hypoglycemia may occur, especially in people who have diseases in these organs.

How to handle:

If an overdose occurs, bisoprolol must be stopped, supported treatment and symptoms. There are a few data that suggest bisoprolol fumarat cannot be separated.

Actively monitor for timely management measures.

In an emergency, call the 115 emergency center immediately or go to the nearest local health station.

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Must stop the drug when there is an unwanted effect.

Notify the physician the unwanted effects when using the drug.

Be cautious when used

heart failure: Beta blockers can lead to an additional decline in heart muscle contraction and promote more severe heart failure. Bisoprolol can be used in patients with congested heart failure, in this case, the medication must be used carefully and only added when it is available for heart failure with basic drugs (diuretics, digitalis, inhibitors) under the strict control of a specialist.

Patients with no history of heart failure: The continuous inhibition of myocardial muscle of beta blockers can lead to heart failure. When there are signs or first symptoms of heart failure, it is necessary to consider stopping bisoprolol. In some cases, it is possible to continue beta blocking treatment during heart failure treatment with other drugs.

Sudden stop treatment: severe angina and in some cases of myocardial infarction or ventricular arrhythmia appears in people with coronary artery disease after a sudden stop of beta blockers.

Peripheral vascular disease: Beta blockers can promote or aggravate the symptoms of artery failure in people with peripheral artery disease.

Bronchospasm: Use carefully Bisoprolol in patients with bronchospasms that do not respond or cannot be tolerated with other anti -hypertension treatment. Because of the beta selection, absolutely not, the lowest Bisoprolol dose is possible, and starts at a dose of 2.5 mg. There must be a Beta2 motorbike owner (bronchodilator).

Anesthesia and surgery: If it is necessary to continue treating with bisoprolol near surgery, it is necessary to be especially cautious when using anesthesia to impair myocardial function such as ether, cyclopropan and tricloroethylen.

Diabetes and hypoglycemia: Beta blockers can cover the manifestations of hypoglycemia, especially tachycardia. Unstolant beta blockers can increase the level of hypoglycemia by insulin and slow down the recovery of serum glucose concentration. Due to the selective nature of Beta1, this is less likely to occur with Bisoprolol. However, it is necessary to warn patients or hypoglycemia, or diabetes who are taking insulin or blood glucose medications for these possibilities and must be used carefully.

Thyroid poisoning: The beta-adrenergic blocker can cover clinical signs of thyroid hyperplasia such as tachycardia. The sudden stop of beta blockers can worsen the symptoms of the thyroid function or may promote the storm.

Risk of anaphylaxis: During the use of beta blockers, patients have a history of anaphylactic reaction with different allergens that may react stronger with the use of repeated drugs, by accident, guess or due to treatment. Such patients may not respond to epinephrin doses often used to treat allergic reactions.

impaired kidney and liver function: Needing the dose of bisoprolol should be renal for kidney failure or liver failure.

Use for children: It is not recommended to use bisoprolol for children because they have no experience in using bisoprolol for children.

This drug contains lactose. Patients with rare genetic problems in tolerance Galactose, Lapp Lapp Lactase or Glucose - Galactose should not use this drug.

The effect of the drug on driving and operating machinery

There has been no research on the effect of the drug on the ability to drive and operate machinery. However, depending on the reaction of each individual and due to the various effects of the drug, the ability to drive and operate machinery may be impaired. It should be paid special attention when starting treatment and when increasing the dose, when taking the drug with alcohol.

Use drugs for women during pregnancy and lactation

Pregnancy:

Only use bisoprolol for women during pregnancy if the expected benefits are higher than the risk of fetus.

Women who are likely to be pregnant or are using contraception should consult a doctor carefully before treatment with this drug.

There is no information on the toxicity on the fetus.

breastfeeding period:

Do not know if bisoprolol is excreted in human milk or not, need to be cautious when using bisoprolol for women who are breastfeeding.

Interactive drug

Interaction of drugs with other drugs and other types of interactions:

The effect and tolerance of the drug can be affected when used simultaneously. The interactions can occur when this drug is used immediately after another.

Combined not to use:

Treatment of stable chronic heart failure: Anti -arrhythmia group I (such as Quinidin, Disopyramid, Lidocaine, Phenytoin, Flecainid, Propafenon) can increase the inhibitory effect of bisoprolol on the transmission of the atrial pulse and the heart spasm.

For all indications:

Verapamil and diltiazem antagonists can reduce the cardiomyopathy and slow down the atrial impulses when used with bisoprolol. Especially when the Verapamil intravenous injection for patients being treated with beta blockers can cause strong hypotension and atrial block.

Hematopsotic drugs have a central effect (such as clonidin, methyldopa, moxonidin, rilmenidin) that can reduce heart rate and cardiac arc as well as vasodilation due to decrease in central sympathetic tone. Stop using the drug suddenly, especially when stopping the use of beta blockers may increase the risk of "corresponding hypertension".

Combine must be cautious:

Treatment of hypertension and angina: Anti -arrhyths group I (such as Quinidin, Disopyramid, Lidocaine, Phenytoin, Flecainid, Propafenon) can increase the inhibitory effect of bisoprolol on the atrial impulse transmission and the heart spasm.

For all indications:

Dihydropyridin -style calcium antagonists (such as nifedipin, felodipine, amlodipin) may increase the risk of lowering blood pressure when used with bisoprolol. Do not rule out the risk of impaired ventricular pump function in patients with heart failure.

Anti -arrhythmia group III (such as Amiodaron) may increase the inhibitory effect of bisoprolol on the atrial impulse transmission.

Topical blockers (such as glaucoma eye drops) may increase the systemic effect of bisoprolol.

Paralysis can increase the inhibitory effect on the Oblil Insulin Atrial Pulse transmission and oral diabetes treatments: The reduction of insulin blood glucose and oral diabetes can be increased when used with bisoprolol. Warning signs of hypoglycemia - especially an increase in heart rate - can be covered. These interactions often occur with unsatisfactory beta blockers.

Anesthesia may increase the risk of bisoprolol's heart inhibition, leading to hypotension (see the cautious part when taking the drug).

Digitalis (digitalis) can increase the time of impulse transmission and thus reduces the heart rate when used with bisoprolol.

Non -steroid anti -inflammatory drugs (NSAIDs) can reduce the hypotension effect of bisoprolol.

Beta sympathetic substances (such as isoprenalin, Dobutamin) used with bisoprolol may reduce the effect of both.

The combination of bisoprolol and sympathetic enhancement of both receptors β and α (such as noradrenalin, adrenalin) can increase the indirect vasoconstrictor effect through the receptor A of these drugs that increases blood pressure and is more severe than lame. These interactions often occur with unsatisfactory beta blockers.

Medicines on hypertension as well as other drugs that are likely to lower blood pressure (such as three -round antidepressants, barbiturat, phenothiazin) can increase the hypotension effect of bisoprolol.

Combining to consider:

Mefloquin: may increase the risk of slow heart rate if used in combination with bisoprolol.

Monoamine inhibitors of oxidase (except IMAO-B): may increase the hypotension effect of beta blockers. However, use at the same time may also have a sudden risk of hypertension.

Rifampicin: may reduce the half -life of bisoprolol due to stimulating the liver metabolic enzyme. Usually no dose adjustment.

Ergotamine conduction: Increased peripheral circulatory disorders.

The cavalry of the drug:

Due to the absence of studies on the correlation of the drug, not mixing this drug with other drugs.