Besicor T

Uses

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

Telmisartan is an angiotensin II receptor blocker (ARB) used for treatment of hypertension and Cardiovascular (CV) risk reduction in patients who are used for ACE inhibitors.

Besicor T 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 arrhythmiaCardiovascular Events, Diabetic Nephropathy, Heart Failure, High Blood Pressure (Hypertension)

How Besicor T 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. 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. Bisoprolol reduces cardiac workload by decreasing contractility and the need for oxygen through competitive inhibition of β1-adrenergic receptors.

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.

Telmisartan interferes with the binding of angiotensin II to the angiotensin II AT₁-receptor by binding reversibly and selectively to the receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. Telmisartan does not inhibit the angiotensin converting enzyme, other hormone receptors, or ion channels. Studies also suggest that telmisartan is a partial agonist of PPARγ, which is an established target for antidiabetic drugs. This suggests that telmisartan can improve carbohydrate and lipid metabolism, as well as control insulin resistance without causing the side effects that are associated with full PPARγ activators.

Dosage

Besicor T 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.

Hypertension: Dosage must be individualized. The usual starting dose of Telmisartan tablets is 40 mg once a day. Blood pressure response is dose-related over the range of 20 to 80 mg

Most of the antihypertensive effect is apparent within 2 weeks and maximal reduction is generally attained after 4 weeks. When additional blood pressure reduction beyond that achieved with 80 mg Telmisartan is required, adiuretic may be added.

No initial dosage adjustment is necessary for elderly patients or patients with renal impairment, including those on hemodialysis. Patients ondialysismay develop orthostatic hypotension; their blood pressure should be closely monitored.

Cardiovascular Risk Reduction: The recommended dose of Telmisartan tablets is 80 mg once a day and can be administered with or without food. It is not known whether doses lower than 80 mg of telmisartan are effective in reducing the risk of cardiovascular morbidity and mortality.

When initiating Telmisartan therapy for cardiovascular risk reduction, monitoring of blood pressure is recommended, and if appropriate, adjustment of medications that lower blood pressure may be necessary.

Telmisartan tablets may be administered with other antihypertensive agents with or without food.

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.

Most people tolerate telmisartan well. Side effects are usually minor and either require no treatment or can easily be treated by physician. The most common telmisartan side effects include-Upper respiratory infection such as the common cold or flu up to 7 percent of people, Back pain up to 3 percent of people, Diarrhea up to 3 percent of people, Inflammation of the sinuses up to 3 percent of people.

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.

Intravenous LD₅₀ in rats is 150-200 mg/kg in males and 200 to 250 mg/kg in females. Acute oral toxicity is low: no deaths and no changes occurred in rats or dogs at 2000 mg/kg, the highest dose tested. Limited data are available with regard to overdosage in humans. The most likely manifestations of overdosage with telmisartan would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation.

Precaution

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

Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. Telmisartan may potentially cause extreme low blood pressure or a decrease in kidney function. Hyperkalemia may occur in patients on ARBs, particularly in patients with advanced renal impairment, heart failure, on renal replacement therapy or on potassium supplements, potassium-sparing diuretics, potassium containing salt substitutes or other drugs that increase potassium levels.

Interaction

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 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 Bisoprolol be discontinued for several days before the withdrawal of clonidine. 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 Bisoprolol, resulting in a shortened elimination half-life of Bisoprolol. However, initial dose modification is generally not necessary.

When certain medicines are taken together, there is a possibility of developing drug interactions. With Telmisartan, drugs such as potassium supplements or potassium-sparing diuretics may cause an interaction. When Telmisartan was co-administered with digoxin, median increases in digoxin peak plasma concentration (49%) and in through concentration (20%) where observed. Therefore, monitor digoxin levels when initiating, adjusting and discontinuing Telmisartan for the purpose of keeping the digoxin level within the therapeutic range. NSAID use may lead to increase risk of renal impairment and loss of antihypertensive effect. Monitor renal function periodically in patients receiving Telmisartan and NSAID therapy.

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. Bisoprolol is known to cross the placenta.

• 500 L

Elimination Route

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.

Absolute bioavailability depends on dosage. Food slightly decreases the bioavailability (a decrease of about 6% is seen when the 40-mg dose is administered with food).

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.

Bi-exponential decay kinetics with a terminal elimination half-life of approximately 24 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.

• >800 mL/min

Elimination Route

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.

Following either intravenous or oral administration of 14C-labeled telmisartan, most of the administered dose (>97%) was eliminated unchanged in feces via biliary excretion; only minute amounts were found in the urine (0.91% and 0.49% of total radioactivity, respectively).

Pregnancy & Breastfeeding use

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. 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.

Telmisartan has been assigned to pregnancy categories C (use during first trimester) by the FDA. When pregnancy is detected or expected, Telmisartan should be discontinued as soon as possible. The use of drugs that act directly on the RAA system during the second and third trimesters has been associated with fetal and neonatal injury, including hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure and death. There are no data on the excretion of Telmisartan into human milk, due to the potential for serious adverse effects in the nursing infant, a decision should be made to discontinue nursing or discontinue the drug.

Contraindication

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

Telmisartan is contraindicated in conditions like Pregnancy, Adjunct in treatment of opioid dependence, Dry or painful cough. Telmisartan is also contraindicated in patients with known hypersensitivity to telmisartan.

Special Warning

Pediatric Patients: There is no pediatric experience with 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).

Renal Impairment: Severe impairment or on haemodialysis: Initially, 20 mg once daily.

Hepatic Impairment: Mild to moderate: Max: 40 mg once daily. Severe: Contraindicated.

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.

Symptoms: Hypotension, bradycardia, tachycardia, dizziness, acute renal failure and elevated serum creatinine.

Management: Supportive and symptomatic treatment. Induction of emesis and/or gastric lavage. Activated charcoal may be useful. Salt and volume replacement should be given immediately if hypotension occurs and place patient in supine position.

Storage Condition

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

Store in a cool and dry place, protected from light. Keep out of children’s reach

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