B1 blockade is essential component for reducing the cardiac Load, the oxygen requirement and excitability of the heart1 Bisoprolol [Valvozid®] is a "B blocker" with highest B1 selectivity
Subtype selectivity of B1 blockers2,3
 
 
Propranolol Two Fold B2 selective
Atenolol 35 flod B1 selective
   
Betaxolol 35 fold B1 selective
   
Bisoprolol (Valvozid®) 75-fold B1 selectivity
   

Related to the affinity for B2 receptors4
 
 
Propranolol No B1 selectivity
  
Carvedilol No B1 selectivity
  
Atenolol 6-fold B1 selectivity
  
Metoprolol 6-fold B1 selectivity
  
Betaxolol 7-fold B1 selectivity
  

Bisoprolol (Valvozid®)

 19-fold B1selectivity
  

B1 Selectivity of Bisoprolol [Valvozid®] is best among the rest
Which ensures that with Bisoprolol [Valvozid®] treatment, the B2 receptors in different organs will remain unaffected in therapeutic doses and beyond.
Offers excellent pharmacokinetic Profile

Bisoprolol: Comparison to B1- selective B-blockers
 
Criteria
Bisoprolol
Atenolol Metoprolol Acebutolol Celiprolol
Plasma elimination half-life(h)
10-12
 6 -9 3-4 7-13 5
Absorption (%)
>99
 50 >95 70 50
First-pass effect
-
 - + + -
Bioavailability (%)
88
 50 50 40-60 50*
Protein binding (%)
30
 3 12 11-25 25
Active metabolites
-
 - - + -
Balanced clearance
+
 - - - -
*dose-dependent Borchard U.B Rezeptorenblocker, Klinik Und Praxis, Aesopus Veriage 1998.
  • Appropriate half life
  • 90% absorption
  • Small first pass effect
  • 88% bioavailability
  • No active metabolites
  • Balanced clearance

Giving excellent clinical profile

Efficacy with Convenient Dosage
In two double-blind randomized studies, the dose dependent efficacy of bisoprolo (Valvozid®) , using doses 5-20 mg once daily, has been confirmed.

Bisoprolol: Dose-dependent blood pressure reduction in hypertensives

In patients with essential hypertension having an initial diastolic blood pressure of 90- 120 mm Hg, bisoprolol (Valvozid®) reduced blood pressure approximately in proportion to the dose.

Equally effective in all age Groups

Bisoprolol: Responder rate in Hypertension in dependence on age after 8 weeks of treatment

Bisoprolol (Valvozid®) normalized the diastolic blood pressure (to 90mm Hg or below) in 80% of hypertensive patients over 60 years of age.
Safe in Diabetic Patients
Bisoprolol [Valvozid] has been found to have no negative effects on glucose metabolism in either healthy volunteers9 or diabetic patients 10

Bisoprolol:B1-selectivity and glucose metabolism in hypertensives With type II diabetes mellitus ( 2h after administration)
 
Glucose metabolism in diabetic patients

The potential effects of bisoprolo on insulin sensitivity have also been investigated. Glucose uptake is used as an index of insulin sensitivity. Bisoprolo [Valvozid®] shows no negative effects on glucose uptake, indicating that it is unlikely to provoke or exacerbate insulin resistance.11
Unlike other B1 blocker no dosage adjustment of Bisoprolol[Valvozid®] is required for diabetic patients.

Safe in Hyperlipidimic Patients
In a long term randomized comparative study bisoprolol [Valvozid®] affected triglycerides less than Propranolol and Atenolol and produced no significant changes in HDL , LDL , or total cholestrol 1.

Bisoprolol:b1- selectivity and lipid metabolism in long - term therapy.

Due to lipid neutrality of bisoprolol [Valvozid®], no increase in atherogenic risk factory.

In Hypertension, CHF & Angina

  • Balanced hepatic and renal clearance
  • Highest B1 selectivity
  • Favorable plasma half life
  • consistent Bioavailability (unaffected by food intake)
  • high absorption rate, small first pass effect, high bioavailability
  • No active metabolites
  • No age dependant pharmacokinetics
  • Unchanged airway resistance
  • No change in lipid parameters Reduction in renin activity
  • No impairment of psychophysiological functions
  • High B1 blocking potency
  • Improves exercise tolerance
  • Does not alter carbohydrate metabolism

 

Valvozid®
  • For Best B1 Selectivity
  • For the achievement of treatment objectives.
  • For Better efficacy and convenience
  • For All Age Groups
  • No Pressure of Diabetes While Prescribing in Diabetic patients.
   
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