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1
types of drug kinitics
first order kinetics and zero order kinetics
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describe reactions where the rate is not affected by the concentration of the drug used.
Zero-order kinetics
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The rate of metabolism/elimination remains constant and is independent of the concentration of a drug.
Zero-order kinetics
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The rate of metabolism/elimination is directly proportional to the plasma concentration of a drug.
First-order kinetics: (curve line)
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, a plot of the natural logarithm of the concentration of a reactant versus time is a straight line with a slope of -k.
First-order kinetics: (curve line)
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is the relationship between the concentrations of species and the rate of a reaction.
reaction order
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is the exponent to which the concentration of the species is raised and it indicates to what extent the concentration of a species affects the rate of a reaction, as well as which species has the greatest effect.
reaction order
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means that the rate is independent of the concentration of a particular reactant. Enough concentration must be present to allow the equilibrium mixture to form.
Zero-order
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Describing drug behavior in the body
Rate Order Kinetics
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In general, drugs will be inactivated or
biotransformedaccording to one of the two general
chemistry principles:
first order kinetics and zero order kinetics
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the velocity with which it occurs
rate
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is the velocity with which the reaction occurs.
rate of reaction
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Rate Order Kinetics depends on?
reactant concentration, Ph, temperature, presence of solvent and additives
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o the way in which the concentration of drug or reactants influences the rate of a chemical reaction or process.
Order of reaction
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o The amount of drug eliminated for each time interval is constant regardless of the amountin the body
Zero Order Reaction
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O The amount of drug in the body does change with the amount or concentration of the drug in the body but the fraction removed varies.
1. Zero Order Reaction
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o The amount of drug eliminated over a certain time period increases as the amount of drug in the body increases.
1st order reaction
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-The period of time required for the amount or concentration of a drug to decrease by 1/2 or 50%
half life (t1/2)
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half life depends on?
volume of distribution and clearance
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- Half-life is not constant
Zero-order half- life
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-Half-life is a constant
First-order half life
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are chemicals, specific molecules,molecule complexes or parts of these, which binds the drugchemically and the complex exerts pharmacological action.
Receptors
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macromolecular component of a cell in which a drug interacts to produce a response. (usually a protein)
Drug Receptor
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specific areas of cell membrane.
proteins and glycoprotein
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Receptor is analogous to a switch in that it has two configurations:
on and off
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drug receptor is known to be located on the ?
membrane
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4 Types of Protein Receptors
regulatory, enzyme, transport, structural
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4 Regulatory proteins that interact with drug or
hormones &initiate a cellular response.
G protein coupled receptor, receptor enzymes, ion channel, cytosolic nuclear enzyme
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2 Acts as transducer proteins.
receptor and post receptor signal transduction
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4 theories
hypothesis of clark, hypothesis of ariens and stephenson , hypothesis of paton, lock and key hypothesis
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in hypothesis of clark Chemical Binding follow the
Law of Mass Action
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the pharmacological effect depends on the
percentage ofreceptors occupied.
Hypothesis of Clark
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- in the bio-phase may initiate responses by altering the permeability of membranes, by interfering with transport mechanisms, by modifying templates, or by acting on enzymes.
Drug Receptors Interactions
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2 Chemical Messengers
neurotransmitter, hormones
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Chemicals released from nerve endings which travel across a nerve synapse to bind with receptors on target cells, such as muscle cells or another nerve. Usually short lived and responsible for messages between individual cells
Neurotransmitters:
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Chemicals released from cells or glands and which travel some distance to bind with receptors on target cells throughout the body
Hormones:
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allows the agonist to bind to receptors.
affinity
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- allows the bound agonist to activateor turn on its receptor function.
INTRINSIC ACTIVITY
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4 Binding of a drug to a receptor is determined by the ff.
covalant bond, hydrogren bond, ionic bond, van del waal forces
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agonist have both
affinity and intrinsic activity
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a measure to efficacy
response
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ability of a bound drug to change the receptor in a way that produces ar effect:some drugs possess affinity but NOT efficacy.
efficacy
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- measure of propensity of a drug to bind
receptor;the attractiveness of drug and receptor.
Affinity
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2 properties of drug
affinity and efficacy
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2 Factors Governing Drug Action
intrinsic acitivity and affinity
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2 Properties of Biological System
potency and magnitude of effect
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magniude of effect aka
efficacy
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2 Determinants of Response
intrinsic efficacy ,number of receptors in the tissue
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3 Graded Dose Response Curves
threshold, ceiling, ED50
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2 types of agonist drug
partial and full
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2 types of antagonist
competitive and noncompetitive
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4 types of antagonist
competitive antagonism, chemical antagonism, irreversible antagonism, partial antagonism
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3 types of antagonist
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