1types of drug kinitics
first order kinetics and zero order kinetics
2describe reactions where the rate is not affected by the concentration of the drug used.
Zero-order kinetics
3The rate of metabolism/elimination remains constant and is independent of the concentration of a drug.
Zero-order kinetics
4The rate of metabolism/elimination is directly proportional to the plasma concentration of a drug.
First-order kinetics: (curve line)
5, 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)
6 is the relationship between the concentrations of species and the rate of a reaction.
reaction order
7 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
8means 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
9 Describing drug behavior in the body
Rate Order Kinetics
10 In general, drugs will be inactivated or
biotransformedaccording to one of the two general
chemistry principles:
first order kinetics and zero order kinetics
11the velocity with which it occurs
rate
12is the velocity with which the reaction occurs.
rate of reaction
13Rate Order Kinetics depends on?
reactant concentration, Ph, temperature, presence of solvent and additives
14o the way in which the concentration of drug or reactants influences the rate of a chemical reaction or process.
Order of reaction
15o The amount of drug eliminated for each time interval is constant regardless of the amountin the body
Zero Order Reaction
16O 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
17o The amount of drug eliminated over a certain time period increases as the amount of drug in the body increases.
1st order reaction
18-The period of time required for the amount or concentration of a drug to decrease by 1/2 or 50%
half life (t1/2)
19half life depends on?
volume of distribution and clearance
20- Half-life is not constant
Zero-order half- life
21-Half-life is a constant
First-order half life
22are chemicals, specific molecules,molecule complexes or parts of these, which binds the drugchemically and the complex exerts pharmacological action.
Receptors
23macromolecular component of a cell in which a drug interacts to produce a response. (usually a protein)
Drug Receptor
24specific areas of cell membrane.
proteins and glycoprotein
25 Receptor is analogous to a switch in that it has two configurations:
on and off
26drug receptor is known to be located on the ?
membrane
274 Types of Protein Receptors
regulatory, enzyme, transport, structural
284 Regulatory proteins that interact with drug or
hormones &initiate a cellular response.
G protein coupled receptor, receptor enzymes, ion channel, cytosolic nuclear enzyme
292 Acts as transducer proteins.
receptor and post receptor signal transduction
304 theories
hypothesis of clark, hypothesis of ariens and stephenson , hypothesis of paton, lock and key hypothesis
31in hypothesis of clark Chemical Binding follow the
Law of Mass Action
32the pharmacological effect depends on the
percentage ofreceptors occupied.
Hypothesis of Clark
33 - 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
342 Chemical Messengers
neurotransmitter, hormones
35Chemicals 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:
36Chemicals released from cells or glands and which travel some distance to bind with receptors on target cells throughout the body
Hormones:
37allows the agonist to bind to receptors.
affinity
38 - allows the bound agonist to activateor turn on its receptor function.
INTRINSIC ACTIVITY
394 Binding of a drug to a receptor is determined by the ff.
covalant bond, hydrogren bond, ionic bond, van del waal forces
40agonist have both
affinity and intrinsic activity
41a measure to efficacy
response
42ability of a bound drug to change the receptor in a way that produces ar effect:some drugs possess affinity but NOT efficacy.
efficacy
43 - measure of propensity of a drug to bind
receptor;the attractiveness of drug and receptor.
Affinity
442 properties of drug
affinity and efficacy
452 Factors Governing Drug Action
intrinsic acitivity and affinity
462 Properties of Biological System
potency and magnitude of effect
47magniude of effect aka
efficacy
482 Determinants of Response
intrinsic efficacy ,number of receptors in the tissue
493 Graded Dose Response Curves
threshold, ceiling, ED50
502 types of agonist drug
partial and full
512 types of antagonist
competitive and noncompetitive
524 types of antagonist
competitive antagonism, chemical antagonism, irreversible antagonism, partial antagonism