Pro-Bisoprolol

Uses

Pro-Bisoprolol is used for the treatment of hypertension, angina and heart failure. It may be used alone or in combination with other antihypertensive agents.

Pro-Bisoprolol is also used to associated treatment for these conditions: Atrial Fibrillation, Cardiovascular Events, Chronic Stable Angina Pectoris, Heart Failure, High Blood Pressure (Hypertension), Mild Hypertension, Premature Ventricular Contraction (PVC), Supraventricular Arrhythmias, Moderate Hypertension, Perioperative arrhythmia

How Pro-Bisoprolol works

Though the mechanism of action of bisoprolol has not been fully elucidated in hypertension, it is thought that therapeutic effects are achieved through the antagonism of β-1adrenoceptors to result in lower cardiac output. Pro-Bisoprolol is a competitive, cardioselective β1-adrenergic antagonist. When β1-receptors (located mainly in the heart) are activated by adrenergic neurotransmitters such as epinephrine, both the blood pressure and heart rate increase, leading to greater cardiovascular work, increasing the demand for oxygen. Pro-Bisoprolol reduces cardiac workload by decreasing contractility and the need for oxygen through competitive inhibition of β1-adrenergic receptors.

Pro-Bisoprolol is also thought to reduce the output of renin in the kidneys, which normally increases blood pressure. Additionally, some central nervous system effects of bisoprolol may include diminishing sympathetic nervous system output from the brain, decreasing blood pressure and heart rate.

Dosage

Pro-Bisoprolol dosage

The usual starting dose is 5 mg once daily. In some patients, 2.5 mg may be an appropriate starting dose. If the antihypertensive effect of 5 mg is inadequate, the dose may be increased to 10 mg and then, if necessary, to 20 mg once daily.

For heart failure: Initially 1.25 mg once daily (in the morning) for 1 week then, if well tolerated, increased to 2.5 mg once daily for 1 week, then 3.75 mg once daily for 1 week, then 5 mg once daily for 4 weeks, then 7.5 mg once daily for 4 weeks, then 10 mg once daily; max. 10 mg daily.

Side Effects

Diarrhoea, dizziness, drowsiness, fatigue, headache, lightheadedness, nausea, sleeplessness, unusual tiredness, weakness, Severe allergic reactions (rash, hives, itching, difficulty breathing, tightness in the chest, swelling of the mouth, face, lips, or tongue), chest pain, difficulty breathing, lightheadedness or dizziness when rising from a lying or sitting position, very slow heartbeat.

Toxicity

LD50 information Oral LD50 of bisoprolol in the mouse was 730 mg/kg.

Overdose information

Signs of a β-blocker overdose include cardiovascular symptoms such as hypotension, congestive heart failure, and bradycardia. Other symptoms such as bronchospasm, and hypoglycemia may occur. If an overdose occurs with bisoprolol, supportive treatment should be initiated. Glucagon has been shown to be beneficial in bradycardia and hypotension associated with beta-blocker overdosage. Hypoglycemia may be managed by administering IV glucose. Monitor the patient and administer atropine in cases of bradycardia, pressors and fluids in the case of hypotension, and conventional heart failure therapy if heart failure occurs. If heart block occurs, the patient must be closely monitored and isoproterenol infusion or transvenous cardiac pacemaker insertion should take place. For the management of overdose-related bronchospasm, administer bronchodilators with or without IV aminophylline. Limited research suggests that bisoprolol fumarate is not removed adequately by hemodialysis sessions.

Precaution

Pro-Bisoprolol Fumarate must be used with caution in:

• Bronchospasm (bronchial asthma, obstructive airways diseases)
• Diabetes Mellitus with large fluctuations in blood glucose values; symptoms of hypoglycemia can be masked
• Strict fasting
• Ongoing desensitization therapy
• First degree AV block
• Prinzmetal's angina
• Peripheral arterial occlusive disease (intensification of complaints might happen especially during the start of therapy)
• General anesthesia

Interaction

Pro-Bisoprolol should not be combined with other beta-blocking agents. Patients receiving catecholamine-depleting drugs, should be closely monitored, because the added beta-adrenergic blocking action of Pro-Bisoprolol may produce excessive reduction of sympathetic activity.In patients receiving concurrent therapy with clonidine, if therapy is to be discontinued, it is suggested that Pro-Bisoprolol be discontinued for several days before the withdrawal of clonidine. Pro-Bisoprolol should be used with care when myocardial depressants or inhibitors of AV conduction, such as certain calcium antagonists or antiarrhythmic agents are used concurrently.Other Alfred Angelo wedding dress collection comes in mermaid dress cut. There are two samples of beach wedding dresses shown in the pictures. Both dresses are different indeed with stylish and creative details on certain areas such as skirt, waist and chest. To match the latest dress model, these mermaid cut wedding dresses a la princess of fairytale apply sweetheart strapless neckline cut. Thick ruffle details are applied on the first mermaid dress. The ruffle application is combined with pleated details on the dress. Thus, in conclusion, the dress is extremely very marvelous for your modern fairytale bridal.Concomitant use with digitalis glycosides can increase the risk of bradycardia.Concurrent use of rifampin increases the metabolic clearance of Pro-Bisoprolol, resulting in a shortened elimination half-life of Pro-Bisoprolol. However, initial dose modification is generally not necessary.

Food Interaction

• Take with or without food. The absorption is unaffected by food.

Pro-Bisoprolol Alcohol interaction

[Moderate]

Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.

Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.

Caution and close monitoring for development of hypotension is advised during coadministration of these agents.

Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.

Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.

Pro-Bisoprolol Cholesterol interaction

[Moderate] Beta-adrenergic receptor blocking agents (aka beta-blockers) may alter serum lipid profiles.

Increases in serum VLDL and LDL cholesterol and triglycerides, as well as decreases in HDL cholesterol, have been reported with some beta-blockers.

Patients with preexisting hyperlipidemia may require closer monitoring during beta-blocker therapy, and adjustments made accordingly in their lipid-lowering regimen.

Pro-Bisoprolol multivitamins interaction

[Moderate] ADJUST DOSING INTERVAL: Concurrent administration with calcium salts may decrease the oral bioavailability of atenolol and possibly other beta-blockers.

The exact mechanism of interaction is unknown.

In six healthy subjects, calcium 500 mg (as lactate, carbonate, and gluconate) reduced the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of atenolol (100 mg) by 51% and 32%, respectively.

The elimination half-life increased by 44%.

Twelve hours after the combination, beta-blocking activity (as indicated by inhibition of exercise tachycardia) was reduced compared to that with atenolol alone.

However, during a 4-week treatment in six hypertensive patients, there was no difference in blood pressure values between treatments.

The investigators suggest that prolongation of the elimination half-life induced by calcium coadministration may have led to atenolol cumulation during long-term dosing, which compensated for the reduced bioavailability.

It may help to separate the administration times of beta-blockers and calcium products by at least 2 hours.

Patients should be monitored for potentially diminished beta-blocking effects following the addition of calcium therapy.

Pro-Bisoprolol Drug Interaction

Minor: aspirin, aspirin, aspirin, aspirinUnknown: rosuvastatin, rosuvastatin, apixaban, apixaban, atorvastatin, atorvastatin, acetaminophen, acetaminophen, clopidogrel, clopidogrel, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

Pro-Bisoprolol Disease Interaction

Major: bradyarrhythmia/AV block, cardiogenic shock/hypotension, CHF, diabetes, hemodialysis, hypersensitivity, ischemic heart disease, PVD, renal/liver diseaseModerate: cerebrovascular insufficiency, glaucoma, hyperlipidemia, hyperthyroidism, myasthenia gravis, pheochromocytoma, psoriasis, tachycardia, asthma/COPD

Volume of Distribution

The volume of distribution of bisoprolol is 3.5 L/kg. The mean volume of distribution was found to be 230 L/kg in heart failure patients, which was similar to the volume of distribution in healthy patients. Pro-Bisoprolol is known to cross the placenta.

Elimination Route

Pro-Bisoprolol is well absorbed in the gastrointestinal tract. The AUC is 642.87 g.hr/mL and bioavailability of bisoprolol is about 90% due to the minimal first pass effects. Absorption is unaffected by food intake. Peak plasma concentrations of bisoprolol are attained within 2-4 hours and steady-state concentrations are achieved within 5 days of administration. In a pharmacokinetic study, the mean peak concentration of bisoprolol was 52 micrograms/L. Cmax at steady state concentrations of bisoprolol is 64±21 ng/ml administered at 10 mg daily.

Half Life

A pharmacokinetic study in 12 healthy individuals determined the mean plasma half-life of bisoprolol to be 10-12 hours. Another study comprised of healthy patients determined the elimination half-life to be approximately 10 hours. Renal impairment increased the half-life to 18.5 hours.

Clearance

Total body clearance in healthy patients was determined to be 14.2 L/h. In patients with renal impairment, clearance was reduced to 7.8 L/h. Hepatic dysfunction also reduced the clearance of bisoprolol.

Elimination Route

Pro-Bisoprolol is eliminated equally by both renal and hepatic pathways. About 50% of an oral dose is excreted unchanged in the urine with the remainder of the dose excreted as inactive bisoprolol metabolites. Under 2% of the ingested dose is found to be excreted in the feces.

Pregnancy & Breastfeeding use

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Pro-Bisoprolol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.Nursing Mothers:Small amounts of bisoprolol fumarate (< 2% of the dose) have been detected in the milk of lactating rats. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk caution should be exercised when bisoprolol fumarate is administered to nursing women.

Contraindication

Pro-Bisoprolol is contraindicated in patients with cardiogenic shock, overt cardiac failure, second or third degree AV block, and marked sinus bradycardia.

Special Warning

Pediatric Patients: There is no pediatric experience with Pro-Bisoprolol.

Geriatric Patients: It is not necessary to adjust the dose in the elderly, unless there is also significant renal or hepatic dysfunction.

Renal impairment: Reduce dose if eGFR less than 20 ml/ minute/ 1.73 m2 (max. 10 mg daily).

Hepatic impairment: Maximum 10 mg daily in severe impairment (hepatitis or cirrhosis).

Acute Overdose

The most common signs expected with overdosage of a beta-blocker are bradycardia, hypotension, congestive heart failure, bronchospasm, and hypoglycemia. To date, a few cases of overdose (maximum: 2000 mg) with bisoprolol have been reported. Bradycardia and/or hypotension were noted. Sympathomimetic agents were given in some cases, and all patients recovered. In general, if overdose occurs, bisoprolol therapy should be stopped and supportive and symptomatic treatment should be provided. Limited data suggest that bisoprolol fumarate is not dialyzable. Based on the expected pharmacologic actions and recommendations for other beta-blockers, the following general measures should be considered when clinically warranted.

Storage Condition

Keep out of the reach of children. Protect from light and moisture, keep in a cool and dry place.

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