Drug Information


     


    










Pharmacokinetics

   


Lacidipine is
rapidly but poorly absorbed from the gastrointestinal tract following
oral administration and undergoes extensive first-pass metabolism; the
bioavailability has been reported to be 2 to 9%, or 18.5% (range 4 to
52%) using a more sensitive assay method. Lacidipine is eliminated by
metabolism in the liver and metabolites are excreted mainly by the
biliary route. About 70% of an oral dose is eliminated in the faeces,
the remainder in the urine. The average steady-state terminal
elimination half-life of lacidipine is 13 to 19 hours. It is more than
95% bound to plasma proteins.

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Indication
& Dosage





Oral

ESSENTIAL HYPERTENSION:
Intially 4 mg once daily, preferably at the same
time every morning; increased upto 6mg after 3-4 weeks. Elderly &
liver disease: Intially 2mg o.d.; may be increased to 4mg depending on
response.

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Action

It is one of the most vascular selective of the dihydropyridines. It
has a long duration of action because of its high degree of lipophilicity,
its storage in the deep lipid compartment of  the membrane and its
continuous release to receptor. Antihypertensive effect apart, lacidipine
has also been show to have anti-atherosclerotic, antioxidant, platelet
antiaggregant & blockade of endothelin-1 induced vasoconstriction
effects. The drug has a favourable hemodynamic profile, with vasodilation
favoring vital-organ pefusion.

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Interactions

Avoid
grapfruit juice as it may affect metabolism. Other interactions as
with calcium channel blockers.






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Adverse
Effect & Precautions




Headache, flushing, GI disturbances, oedema, muscle cramps,
gumhyperplasia, dizziness, palpitation, asthenia, rash (including
pruritus erythema), mood disturbances.

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Brands available in market :















LACIVAS


Aztec(Sun Divn)


F-C TABS


2mg


10


27.00


F-C TABS


4mg


10


49.00


SINOPIL


Glaxo Pharma


TABS


2mg


10


33.55


TABS


2mg


3×10


100.65


TABS


4mg


10


67.63


TABS


4mg


3×10


202.89






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Drug Information
     

    

Pharmacokinetics
   

Lacidipine is rapidly but poorly absorbed from the gastrointestinal tract following oral administration and undergoes extensive first-pass metabolism; the bioavailability has been reported to be 2 to 9%, or 18.5% (range 4 to 52%) using a more sensitive assay method. Lacidipine is eliminated by metabolism in the liver and metabolites are excreted mainly by the biliary route. About 70% of an oral dose is eliminated in the faeces, the remainder in the urine. The average steady-state terminal elimination half-life of lacidipine is 13 to 19 hours. It is more than 95% bound to plasma proteins.

TOP
   

Indication & Dosage

Oral
ESSENTIAL HYPERTENSION:
Intially 4 mg once daily, preferably at the same time every morning; increased upto 6mg after 3-4 weeks. Elderly & liver disease: Intially 2mg o.d.; may be increased to 4mg depending on response.

TOP
   

Action

It is one of the most vascular selective of the dihydropyridines. It has a long duration of action because of its high degree of lipophilicity, its storage in the deep lipid compartment of  the membrane and its continuous release to receptor. Antihypertensive effect apart, lacidipine has also been show to have anti-atherosclerotic, antioxidant, platelet antiaggregant & blockade of endothelin-1 induced vasoconstriction effects. The drug has a favourable hemodynamic profile, with vasodilation favoring vital-organ pefusion.

TOP
   

Interactions

Avoid grapfruit juice as it may affect metabolism. Other interactions as with calcium channel blockers.


TOP
   

Adverse Effect & Precautions

Headache, flushing, GI disturbances, oedema, muscle cramps, gumhyperplasia, dizziness, palpitation, asthenia, rash (including pruritus erythema), mood disturbances.

TOP
   

Brands available in market :

LACIVAS

Aztec(Sun Divn)

F-C TABS

2mg

10

27.00

F-C TABS

4mg

10

49.00

SINOPIL

Glaxo Pharma

TABS

2mg

10

33.55

TABS

2mg

3×10

100.65

TABS

4mg

10

67.63

TABS

4mg

3×10

202.89


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By |2022-07-20T16:43:08+00:00July 20, 2022|Uncategorized|Comments Off on Lacidipine

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