The Topic PHARMACOKINETICS & METABOLISM gives you detail information about (1st pass metabolism of drug, organs & enzymes involed in drug metabolism, All Phases of Drug) & All you need to know about BIO-TRANSFORMATION.
Pharmacokinetics is the study of the movement of drug molecules in the body. It includes absorption, distribution, metabolism, and excretion of drugs. Pharmacokinetics is the study of what happens to drugs once they enter the body (the movement of the drugs into, within, and out of the body). For a drug to produce its specific response, it should be present in adequate concentrations at the site of action. This depends on various factors apart from the dose.
Four pharmacokinetic properties determine the onset, intensity, and the duration of drug action (Figure 1.6.1):
• Absorption: First, absorption from the site of administration permits entry of the drug (either directly or indirectly) into plasma.
• Distribution: Second, the drug may then reversibly leave the bloodstream and distribute it into the interstitial and intracellular fluids.
• Metabolism: Third, the drug may be biotransformed by metabolism by the liver or other tissues.
• Elimination: Finally, the drug and its metabolites are eliminated from the body in urine, bile, or feces.
In short, pharmacokinetics means what the body does to the drug.
biotransformation of drug
Biotransformation/Xenobiotic metabolism/ drug metabolism/detoxification.
-Xenobiotics: a wide variety of foreign compounds to which humans get exposed in day to day life.
-It includes unknown compounds, drugs, environmental pollutants, toxins.
-Many xenobiotics can evoke biological responses.
DEFINITION
The biochemical alteration of drug or xenobiotic in the presence of various enzymes that acts as a catalyst which themselves not consumed in the reaction and there by may activate or deactivate the drug is called biotransformation.
Why Biotransformation is necessary?:
To easily eliminate the drug
To terminate drug action by inactivating it
Consequences of Biotransformation
Active to Inactive:
Phenobarbitone---- Hydroxyphenobarbitone
Inactive (prodrug) to Active :
L-Dopa ---- Dopamine
Parathion -- Paraoxon
Talampicillin -- Ampicillin
Active to equally active:
Diazepam -- Oxazepam
Amitriptyline -- Nortriptyline
Imipramine -- Des-imipramine
Codeine -- Morphine
Sites of biotransformation
In the body: Liver, small and large intestines, lungs, skin, kidney, nasal mucosa & brain.
Liver is considered “metabolite clearing house” for both endogenous substances and xenobiotics.
Intestines are considered “initial site of drug metabolism”.
FIRST PASS METABOLISM:
First pass metabolism or presystemic
metabolism or ‘first pass effect’
After oral administeration many drugs are absorbed from the small intestine - transported first via portal system to the liver, where they undergo extensive metabolism before reaching systemic circulation.
fundamental concepts in drug biotransformation
Lipid soluble drugs are poorly excreted in the urine. They tend to store in fat and/or circulate until they are converted (phase I biotransformation) to more water soluble metabolites or metabolites that conjugate (phase II biotransformation) with water soluble substances.
Water soluble drugs are more readily excreted in the urine. They may be metabolized, but generally not by the CYP enzyme systems.
Enzymes catalyzing phase I biotransformation reactions
Enzymes catalyzing phase I biotransformation reactions include:
cytochrome P-450
aldehyde and alcohol dehydrogenase
deaminases
esterases
amidases
epoxide hydratases
Addition of water
Cleavage of R-O or R-N bond accompanied by addition of H2O
CYTOCHROME P450
The cytochrome P-450 families are referred to using an arabic numeral, e.g., CYP1, CYP2, etc.
Each family has a number of subfamilies denoted by an upper case letter, e.g., CYP2A, CYP2B, etc.
The individual enzymes within each subfamily are denoted by another arabic numeral, e.g., CYP3A1, CYP3A2, etc.
Pharmacokinetics is the study of the movement of drug molecules in the body. It includes absorption, distribution, metabolism, and excretion of drugs. Pharmacokinetics is the study of what happens to drugs once they enter the body (the movement of the drugs into, within, and out of the body). For a drug to produce its specific response, it should be present in adequate concentrations at the site of action. This depends on various factors apart from the dose.
Four pharmacokinetic properties determine the onset, intensity, and the duration of drug action (Figure 1.6.1):
• Absorption: First, absorption from the site of administration permits entry of the drug (either directly or indirectly) into plasma.
• Distribution: Second, the drug may then reversibly leave the bloodstream and distribute it into the interstitial and intracellular fluids.
• Metabolism: Third, the drug may be biotransformed by metabolism by the liver or other tissues.
• Elimination: Finally, the drug and its metabolites are eliminated from the body in urine, bile, or feces.
In short, pharmacokinetics means what the body does to the drug.
biotransformation of drug
Biotransformation/Xenobiotic metabolism/ drug metabolism/detoxification.
-Xenobiotics: a wide variety of foreign compounds to which humans get exposed in day to day life.
-It includes unknown compounds, drugs, environmental pollutants, toxins.
-Many xenobiotics can evoke biological responses.
DEFINITION
The biochemical alteration of drug or xenobiotic in the presence of various enzymes that acts as a catalyst which themselves not consumed in the reaction and there by may activate or deactivate the drug is called biotransformation.
Why Biotransformation is necessary?:
To easily eliminate the drug
To terminate drug action by inactivating it
Consequences of Biotransformation
Active to Inactive:
Phenobarbitone---- Hydroxyphenobarbitone
Inactive (prodrug) to Active :
L-Dopa ---- Dopamine
Parathion -- Paraoxon
Talampicillin -- Ampicillin
Active to equally active:
Diazepam -- Oxazepam
Amitriptyline -- Nortriptyline
Imipramine -- Des-imipramine
Codeine -- Morphine
Sites of biotransformation
In the body: Liver, small and large intestines, lungs, skin, kidney, nasal mucosa & brain.
Liver is considered “metabolite clearing house” for both endogenous substances and xenobiotics.
Intestines are considered “initial site of drug metabolism”.
FIRST PASS METABOLISM:
First pass metabolism or presystemic
metabolism or ‘first pass effect’
After oral administeration many drugs are absorbed from the small intestine - transported first via portal system to the liver, where they undergo extensive metabolism before reaching systemic circulation.
fundamental concepts in drug biotransformation
Lipid soluble drugs are poorly excreted in the urine. They tend to store in fat and/or circulate until they are converted (phase I biotransformation) to more water soluble metabolites or metabolites that conjugate (phase II biotransformation) with water soluble substances.
Water soluble drugs are more readily excreted in the urine. They may be metabolized, but generally not by the CYP enzyme systems.
Enzymes catalyzing phase I biotransformation reactions
Enzymes catalyzing phase I biotransformation reactions include:
cytochrome P-450
aldehyde and alcohol dehydrogenase
deaminases
esterases
amidases
epoxide hydratases
Addition of water
Cleavage of R-O or R-N bond accompanied by addition of H2O
CYTOCHROME P450
The cytochrome P-450 families are referred to using an arabic numeral, e.g., CYP1, CYP2, etc.
Each family has a number of subfamilies denoted by an upper case letter, e.g., CYP2A, CYP2B, etc.
The individual enzymes within each subfamily are denoted by another arabic numeral, e.g., CYP3A1, CYP3A2, etc.
By the end of this lecture, students should:
Explain why drug metabolism is essential
Describe the phases of drug metabolism
Explain the role of cytochrome p 450 enzyme system in drug metabolism
Definition
Chemical reactions which occur in the body to change drugs from nonpolar lipid soluble forms to polar water soluble forms that are easily excreted by the kidney.
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3. Biotransformation of Drug is defined as the conversion from one chemical from to another. The ter
ms is used synonymously with Metabolism
The Drug which are enter the through ingestion inhalation or absorption are called as xenobiotics (G
reek: xenos =foreign) or exogenous compound
DEFINITION
4. ORGANS :
1] Liver. 2] Lungs. 3] Kidney 4] Intestine 4] Plasenta 5] Adrenals 6] Skin
1) Liver is primary site for Metabolism of almost all drug because a large variety of Enzymes in large amount in Liv
er are present
2) Metabolism by organs other than liver called as extrahepatic Metabolism
3) The decreasing order of Drug Metabolism Ability of various Organs I.e
Liver > Lungs > Kidney > Intestine > Plasenta > Adrenals > Skin
4) Brain , testes , Muscle , Spleen etc also metabolites drug to a Small extent
Organs Involved in Drug Metabolisum
6. NON MICROSOMAL ENZYMES :
1) Present in soluble from of the cytoplasm & those attached to the mitochondria but not the endoplasmic reticulu
m
2) Non specific that Catalyze few oxidation reaction hydrolytic reaction Nd Conjugation reaction other than Glucaru
nidation
Example: Oxidases, perioxidases, dehydrogenase Esterase
7. FIRST PASS METABOLISM
1) This refers.to Metabolism of a drug during its passage from the site of adsorption into the systemic circulation.
2) All orally admistered drug are exposed to the drug Metabolism Enzymes in the esenssial wall liver
3) presystem Metabolism of limited magnitude can also occur in the skin and in Lungs .
Attribute of Drug With High First pass Metabolism :
* Oral dose is comsiderally higher than sublingual or parental dose
* There is marked individual variation in the oral dose due to difference in the extent of First pass Metabolism
* Oral bioavailability is apparently increase in patient with sever liver disease
* Oral bioavailability of a drug is increase if another drug competing with it in First pass Metabolism is given concurr
ently
Example : Chlorpromazine & Propranolol
8.
9.
10. PHASES OF DRUG METABOLISM
R.T Williams divided the pathways of Metabolism reaction two genernal category phase 1 and phas
e 2 reaction .
PHASE I :
1) Oxidation Reaction
2) Reduction Reaction
3) Hydrolytic Reaction
A】 OXIDATION REACTION :
Oxidation reaction increase hydrophilicity of xenobiotics by introduction polar function
al group such as -oH such a polar metabolites can thus rapidly undergoes phase II reaction or is excreta
ble by the kidney . Oxidation of xenobiotics is nonspecifically catalysed by a number of Enzymes locate
d in the micromes .
RH +O + NADPH + H ------------> ROH + H2O + NADPH
Since NADPH reduced NADP ++
2
12. Others Oxidation Reaction :
1) Oxidation of aromatic carbon atom
2) Oxidation of olefinc (C=C) bonds.
3) Oxidation of benzylic allylic carbon atom
4) Oxidation of aliphatic carbon atom
5) Oxidation of alicyclic carbon atom
B】 REDUCTIVE REACTION :
A number of reductive reaction are extract opposite to Oxidation
Sum Reductive reaction are as follows :
1) Reduction of carbonyl function
2) Reduction of alcohol and C=C bonds
3) Reduction of N- compound
13. C】 HYDROLYTIC REACTION :
* These reaction differ from oxidation and Reductive reaction
* The reaction does not involve change in the state of oxidation of the substance
Sum Hydrolytic Reaction are as follows :
1) Hydrolysis of amides
2) Hydrolytic of ester and ethers
3) Hydrolytic cleavage of non aromatic heterocycles
4) Hydrolytic deologenation
5) Miscellaneous Hydrolytic Reaction
14.
15.
16. FACTORS AFFECTING DRUG METABOLISM :
1.Physiochemical properties of the drug
2.Chemical Factors
a] Induction of Drug Metabolism Enzymes
b] Induction of Drug Metabolism Enzymes
C] Environmental chemical
3. Biological Factors
a] Species Differences
b] Strain Difference
C] Sex difference
d] Age
e] Altered physiologic Factors
F] Temporal Factors