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First Order Elimination Kinetic



The Fundamental Concept

  • A drug molecule is eliminated when it comes in contact with its elimination mechanism.

  • The elimination mechanism may be an inactivating enzyme or excretion process.

  • First-order elimination kinetic is seen when the elimination process is not saturated.

At high concentration of drug, more drug molecules come in contact with elimination mechanism

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More drugs molecule are eliminated. i.e. inactivated or excreted

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Drug concentration decreases

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Fewer molecules come in contact with elimination mechanism

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Fewer molecules are eliminated

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If we give next dose of drug

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Concentration of drug increases

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Again more drug molecules come in contact with elimination mechanism

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Elimination increases

  • Thus, at higher concentration, more molecules are eliminated, and at lower concentration, fewer molecules are eliminated.

  • All the properties of the first-order elimination kinetic are different manifestations of this same fundamental process.


Properties of First-Order Elimination Kinetic.

  • Rate of drug elimination is directly proportional to plasma concentration of the drug.

  • Constant fraction of drug is eliminated at constant interval of time.

  • Clearance remains constant.

  • Plasma half-life remains constant.

  • Plot of plasma concentration against time is curvilinear.

  • Single dose of drug is eliminated almost completely eliminated after 5 half-lives.

 

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