Actions of Zebeta in details
Bioequivalence Study: When a single dose of 2 tablets of NIKP-Zebeta tablet 2.5 mg or two tablets of the reference product (both tablets contain 5 mg of Zebeta) were given to healthy male adults during fasting with a cross-over method, the plasma concentrations of Zebeta were measured. In a statistical analysis for the obtained pharmacokinetic parameters (AUC and Cmax), calculation results of 90% confidence intervals for the parameters were within a range between log (0.8) and log (1.25), demonstrating the bioequivalence of the 2 formulations.
Additionally, when 1 tablet of NIKP-Zebeta tablet 2.5 mg or 1 tablet of the reference product (both tablets contain 5 mg of Zebeta) was administered, similar bioequivalence results of both formations were observed.
Plasma concentration and pharmacokinetic parameters such as AUC and Cmax may vary depending on study conditions including selection of subjects, body fluid sampling frequency/sampling time, etc. Dissolution Profile:
How should I take Zebeta?
Take Zebeta exactly as it was prescribed for you. Do not take the medication in larger amounts or for longer than recommended by your doctor. Follow the directions on your prescription label.
Take this medication with a full glass of water.
Take Zebeta at the same time every day.
Your doctor may occasionally change your dose to make sure you get the best results from this medication.
Do not skip doses or stop taking Zebeta without first talking to your doctor. Stopping suddenly may make your condition worse or cause other serious heart problems.
To be sure this medication is helping your condition, your blood pressure will need to be checked on a regular basis. Do not miss any scheduled appointments.
If you need to have any type of surgery, tell the surgeon ahead of time that you are using Zebeta.
Zebeta 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.
Store Zebeta at room temperature away from moisture and heat.
Zebeta administration
Take Zebeta exactly as it was prescribed for you. Do not take the medication in larger amounts or for longer than recommended by your doctor. Follow the directions on your prescription label.
Take this medication with a full glass of water.
Take Zebeta at the same time every day.
Your doctor may occasionally change your dose to make sure you get the best results from this medication.
Do not skip doses or stop taking Zebeta without first talking to your doctor. Stopping suddenly may make your condition worse or cause other serious heart problems.
To be sure this medication is helping your condition, your blood pressure will need to be checked on a regular basis. Do not miss any scheduled appointments.
If you need to have any type of surgery, tell the surgeon ahead of time that you are using Zebeta.
Zebeta 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.
Store Zebeta at room temperature away from moisture and heat.
Zebeta pharmacology
Zebeta is a beta1-selective (cardioselective) adrenoceptor blocking agent without significant membrane stabilizing activity or intrinsic sympathomimetic activity in its therapeutic dosage range. Cardioselectivity is not absolute, however, and at higher doses (≥ 20 mg) Zebeta also inhibits beta2-adrenoceptors, chiefly located in the bronchial and vascular musculature; to retain selectivity it is therefore important to use the lowest effective dose.
Pharmacokinetics and Metabolism
The absolute bioavailability after a 10 mg oral dose of Zebeta is about 80%. Absorption is not affected by the presence of food. The first pass metabolism of Zebeta is about 20%.
Binding to serum proteins is approximately 30%. Peak plasma concentrations occur within 2-4 hours of dosing with 5 to 20 mg, and mean peak values range from 16 ng/mL at 5 mg to 70 ng/mL at 20 mg. Once daily dosing with Zebeta results in less than twofold intersubject variation in peak plasma levels. The plasma elimination half-life is 9-12 hours and is slightly longer in elderly patients, in part because of decreased renal function in that population. Steady state is attained within 5 days of once daily dosing. In both young and elderly populations, plasma accumulation is low; the accumulation factor ranges from 1.1 to 1.3, and is what would be expected from the first order kinetics and once daily dosing. Plasma concentrations are proportional to the administered dose in the range of 5 to 20 mg. Pharmacokinetic characteristics of the two enantiomers are similar.
Zebeta is eliminated equally by renal and non-renal pathways with about 50% of the dose appearing unchanged in the urine and the remainder appearing in the form of inactive metabolites. In humans, the known metabolites are labile or have no known pharmacologic activity. Less than 2% of the dose is excreted in the feces. Zebeta is not metabolized by cytochrome P450 II D6 (debrisoquin hydroxylase).
In subjects with creatinine clearance less than 40 mL/min, the plasma half-life is increased approximately threefold compared to healthy subjects.
In patients with cirrhosis of the liver, the elimination of Zebeta (Zebeta) is more variable in rate and significantly slower than that in healthy subjects, with plasma half-life ranging from 8.3 to 21.7 hours.
Pharmacodynamics
The most prominent effect of Zebeta is the negative chronotropic effect, resulting in a reduction in resting and exercise heart rate. There is a fall in resting and exercise cardiac output with little observed change in stroke volume, and only a small increase in right atrial pressure, or pulmonary capillary wedge pressure at rest or during exercise.
Findings in short-term clinical hemodynamics studies with Zebeta are similar to those observed with other beta-blocking agents.
The mechanism of action of its antihypertensive effects has not been completely established. Factors which may be involved include:
- 1.
- Decreased cardiac output,
- 2.
- Inhibition of renin release by the kidneys,
- 3.
- Diminution of tonic sympathetic outflow from the vasomotor centers in the brain.
In normal volunteers, Zebeta therapy resulted in a reduction of exercise- and isoproterenol-induced tachycardia. The maximal effect occurred within 1-4 hours post-dosing. Effects persisted for 24 hours at doses equal to or greater than 5 mg.
Electrophysiology studies in man have demonstrated that Zebeta significantly decreases heart rate, increases sinus node recovery time, prolongs AV node refractory periods, and, with rapid atrial stimulation, prolongs AV nodal conduction.
Beta1-selectivity of Zebeta has been demonstrated in both animal and human studies. No effects at therapeutic doses on beta2-adrenoceptor density have been observed. Pulmonary function studies have been conducted in healthy volunteers, asthmatics, and patients with chronic obstructive pulmonary disease (COPD). Doses of Zebeta ranged from 5 to 60 mg, atenolol from 50 to 200 mg, metoprolol from 100 to 200 mg, and propranolol from 40 to 80 mg. In some studies, slight, asymptomatic increases in airways resistance (AWR) and decreases in forced expiratory volume (FEV1) were observed with doses of Zebeta 20 mg and higher, similar to the small increases in AWR also noted with the other cardioselective beta-blockers. The changes induced by beta-blockade with all agents were reversed by bronchodilator therapy.
Zebeta had minimal effect on serum lipids during antihypertensive studies. In U.S. placebo-controlled trials, changes in total cholesterol averaged +0.8% for Zebeta-treated patients, and +0.7% for placebo. Changes in triglycerides averaged +19% for Zebeta-treated patients, and +17% for placebo.
Zebeta (Zebeta) has also been given concomitantly with thiazide diuretics. Even very low doses of hydrochlorothiazide (6.25 mg) were found to be additive with Zebeta in lowering blood pressure in patients with mild-to-moderate hypertension.
References
- DailyMed. "BISOPROLOL FUMARATE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Bisoprolol Fumarate: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Bisoprolol: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
The results of a survey conducted on ndrugs.com for Zebeta are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Zebeta. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.User reports
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Information checked by Dr. Sachin Kumar, MD Pharmacology
