Drug Information

 


                  











 

Pharmacokinetics

  


Simvastatin is absorbed from the gastrointestinal tract and is
hydrolysed to its active beta-hydroxyacid form. Other active metabolites
have been detected and a number of inactive metabolites are also formed.
Simvastatin undergoes extensive first-pass metabolism in the liver, its
primary site of action. Less than 5% of the oral dose has been reported
to reach the circulation as active metabolites. Both simvastatin and its
beta-hydroxyacid metabolite are about 95% bound to plasma proteins. It
is mainly excreted in the faeces via the bile as metabolites. About 10
to 15% is recovered in the urine, mainly in inactive forms. The
half-life of the active metabolite is 1.9 hours.

TOP

  

 

Indication
& Dosage


 


Oral

HYPERCHOLESTEROLEMIA WITH I.H.D; HYPERCHOLESTEROLEMIA IN TYPE IIa AND
TYPE IIb HPERLIPOROTEINEMIAS; COMINED HYPERTRIGLYCERIDEMIA AND
HYPERCHOLESTEROLEMAIA: Initially 5-10mg OD in the evening. Max dose
40mg/day. Dosage individualized and dose adjustments made at intervals
of 4 weeks or more.





TOP

  

 

Action


 


It is a prodrug which gets bioactivated in the liver to form the
active beta-hydroxyacid derivative. This inhibits the conversion of HMG-Co
A to mevalonic acid  by blocking the enzyme HMG-Co A reductase, an
early and rate limiting step in the biosynthesis of cholesterol.
Simvastatin has been demonstrated to reduce total cholesterol, LDL-cholesterol,
and triglycerides by 25%, 35% and 10% respectively; increase in HDL is
upt 12%. Major trials have documented simvastatin’s beneficial role in
substatially reducing both cardiovascular morbidity and mortality.

TOP

  

Interaction

 


There is an increased risk of myopathy if certain drugs such as
immunosuppressants (notably cyclosporin), fibric acid derivatives, or
nicotinic acid are given concurrently with statins; for further details
see Effects on Skeletal Muscle, under Adverse Effects. Bleeding and
increases in prothrombin time have been reported in patients taking
simvastatin with coumarin anticoagulants. Raised concentrations of
simvastatin have occurred in patients also given mibefradil.

 TOP

  

Adverse
Effect & Precautions






Constipation, diarrhoea, nausea,
dyspepsia, flatulence, dizziness, skin rash, fatigue, myopathy.



Precaution: Past history of liver disease, in patients who consume
substantial quantities of alcohol, renal failure, severe acute
infection. major surgery, trauma, electrolyte disorders and uncontrolled
seizures. Liver function tests should be performed during therapy with
simvastatin. Patients should be advised to report any unexplained muscle
pain, tenderness, particularly if accompained by malaise or fever.

Pregnancy: Contraindicated.

Breast Feeding: COntraindicated.

Man: Use with caution.

TOP

    

Brands
available in market
























SIMVAS

Micro Labs

TABS

5mg

15

75.00

TABS

10mg

15

120.00

TABS

20mg

15

210.00

SIMVASTOL

Themis

TABS

5mg

10

27.15

TABS

10mg

10

49.78

TABS

20mg

10

94.52

SIMVOTIN

Stancare

F-C TABS

5mg

10

50.40

F-C TABS

10mg

10

80.60

F-C TABS

20mg

10

141.00

ZOSTA

USV

TABS

5mg

10

36.50

TABS

10mg

10

58.00

TABS

20mg

10

102.00


TOP



 

                                                     


                                               






 

                               

 
Drug Information
 

                  

 
Pharmacokinetics
  
Simvastatin is absorbed from the gastrointestinal tract and is hydrolysed to its active beta-hydroxyacid form. Other active metabolites have been detected and a number of inactive metabolites are also formed. Simvastatin undergoes extensive first-pass metabolism in the liver, its primary site of action. Less than 5% of the oral dose has been reported to reach the circulation as active metabolites. Both simvastatin and its beta-hydroxyacid metabolite are about 95% bound to plasma proteins. It is mainly excreted in the faeces via the bile as metabolites. About 10 to 15% is recovered in the urine, mainly in inactive forms. The half-life of the active metabolite is 1.9 hours.

TOP
  

 
Indication & Dosage

 
Oral
HYPERCHOLESTEROLEMIA WITH I.H.D; HYPERCHOLESTEROLEMIA IN TYPE IIa AND TYPE IIb HPERLIPOROTEINEMIAS; COMINED HYPERTRIGLYCERIDEMIA AND HYPERCHOLESTEROLEMAIA: Initially 5-10mg OD in the evening. Max dose 40mg/day. Dosage individualized and dose adjustments made at intervals of 4 weeks or more.


TOP
  

 
Action

 
It is a prodrug which gets bioactivated in the liver to form the active beta-hydroxyacid derivative. This inhibits the conversion of HMG-Co A to mevalonic acid  by blocking the enzyme HMG-Co A reductase, an early and rate limiting step in the biosynthesis of cholesterol. Simvastatin has been demonstrated to reduce total cholesterol, LDL-cholesterol, and triglycerides by 25%, 35% and 10% respectively; increase in HDL is upt 12%. Major trials have documented simvastatin’s beneficial role in substatially reducing both cardiovascular morbidity and mortality.

TOP
  

Interaction
 

There is an increased risk of myopathy if certain drugs such as immunosuppressants (notably cyclosporin), fibric acid derivatives, or nicotinic acid are given concurrently with statins; for further details see Effects on Skeletal Muscle, under Adverse Effects. Bleeding and increases in prothrombin time have been reported in patients taking simvastatin with coumarin anticoagulants. Raised concentrations of simvastatin have occurred in patients also given mibefradil.

 TOP
  

Adverse Effect & Precautions

Constipation, diarrhoea, nausea, dyspepsia, flatulence, dizziness, skin rash, fatigue, myopathy.

Precaution: Past history of liver disease, in patients who consume substantial quantities of alcohol, renal failure, severe acute infection. major surgery, trauma, electrolyte disorders and uncontrolled seizures. Liver function tests should be performed during therapy with simvastatin. Patients should be advised to report any unexplained muscle pain, tenderness, particularly if accompained by malaise or fever.
Pregnancy: Contraindicated.
Breast Feeding: COntraindicated.
Man: Use with caution.

TOP
    

SIMVAS

Micro Labs

TABS

5mg

15

75.00

TABS

10mg

15

120.00

TABS

20mg

15

210.00

SIMVASTOL

Themis

TABS

5mg

10

27.15

TABS

10mg

10

49.78

TABS

20mg

10

94.52

SIMVOTIN

Stancare

F-C TABS

5mg

10

50.40

F-C TABS

10mg

10

80.60

F-C TABS

20mg

10

141.00

ZOSTA

USV

TABS

5mg

10

36.50

TABS

10mg

10

58.00

TABS

20mg

10

102.00

TOP

 

                                                     
                                               

 

By |2022-07-20T16:42:53+00:00July 20, 2022|Uncategorized|Comments Off on Simvastatin

About the Author: