Pharmacokinetics

and
Pharmacodynamic

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 Pharmacology is a study of the effects of chemical
substances on the function of living systems

 A drug may is a substance that brings about a change in

biologic functions through its chemical actions

 A pro-drug is a chemical that is converted to active

drug/form by biologic processes inside the body

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 A medicine is a chemical preparation, which usually but not
necessarily contains one or more drugs, administered with
the intention of producing a therapeutic effect

 Medicines usually contain other substances (i.e. excipients,

stabilisers, solvents, etc.) besides the active drug, to make
them more convenient to use

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• Pharmacodynamics, Receptor, Agonist, Antagonist and
Synergy
 Pharmacodynamics refers to the relationship between drug
concentration at the site of action and the resulting effect,
including the time course and intensity of therapeutic and
adverse effects
 A drug receptor is a specialized target macromolecule,
present on the cell surface intracellularly, that binds a drug
and mediates its pharmacological actions

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Cont,,,,,

 Study of action-effect of drugs and dose-effect

relationship
 It is the study of biochemical and physiological effects of drugs
and their mechanism of action at organ level as well as
cellular level
 Also Modification of action of one drug by another drug

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Types of Drug Action
EFFECT (Type of responses):-
1.Stimulation
2.Inhibition/Depression
3.Replacement
4.Irritation
5.Cytotoxic
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 Receptors are the sensing elements in the system of
chemical communications that coordinates the function of all
the different cells in the body

 Most drugs must bind to their specific receptors which is

followed by a sequence of events before producing their
effects

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 The effect of a drug present at the site of action is
determined by that drug’s binding with a receptor
 An agonist is a drug which binds to and activate the receptor
to bring a pharmacological effect directly or indirectly
 Antagonist are drugs which act by binding to receptors and
therefore prevent the binding of other molecules or drugs to
the receptor resulting into diminished/reduced/blocked
effects of the molecules or drugs

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 The effect of one drug is diminished or completely abolished
in the presence of another

 Many therapeutically useful drugs act, either as agonists or

antagonists, on receptors for known endogenous mediators

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Combined effects of drug
• Synergism
The combined effect of two drugs is higher than either individual effect
 Drug synergy occurs when drugs can interact in ways that enhance or magnify one
or more effects, or side-effects, of those drugs
 The combined effect of two drugs is higher than either individual effect
Ex:-
1.Sulfamethaxazole+ Trimethoprim
2. Levodopa + Carbidopa
 Synergism means – 1+1=3
 Additive means – 1+1=2

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DOSE
It is the required amount of drug in weight, volumes, moles or IU to
provide a desired effect.

In clinical it is called as Therapeutic dose

In experimental purpose it is called as effective dose.

The therapeutic dose varies from person to person

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 Single dose:
1.Piperazine (4-5g) is sufficient to eradicate round worm.
2.Single IM dose of 250mg of ceftriaxone to treat gonorrhoea.

Daily dose:
It is the quantity of a drug to be administered in 24hr, all at once or equally
divided dose.
1.10mg of cetrizine (all at once) is sufficient to relive allergic reactions.
2.Erythromycin is 1g per day to be given in 4 equally divided dose (i.e.,
250mg every 6 hr)

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• Total dose: It is the maximum quantity of the drug that is needed the
complete course of the therapy.
Ex:- procaine penicillin early syphilis is 6 million unit  given as 0.6 million
units per day for 10days.

Loading dose:- It is the large dose of drug to be given initially to provide the
effective plasma concentration rapidly. The drugs having high Vd of
distribution.
Chloroquine in Malaria – 600 mg Stat
300mg after 8 hours
300 mg after 2 days.

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Maintenance dose:- Loading dose normally followed by
maintenance dose.
• Needed to maintain the steady state plasma
concentration attained after giving the loading dose.

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Pharmacokinetics Absorption (A), Distribution (D),
Metabolism (M) and Elimination (E).
 When a drug is administered it must be absorbed into blood
from its site of administration, distributed to its site of action,
metabolized (mainly by the liver and other processes) and
finally eliminated from the body by excretion and other
processes
 In short pharmacokinetics (PK) = Absorption (A), Distribution
(D), Metabolism (M) and Elimination (E). Therefore,
PK=ADME
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 When a drug is administered it must be absorbed into blood
from its site of administration, distributed to its site of
action, metabolized (mainly by the liver and other processes)
and finally eliminated from the body by excretion and other
processes
 In short pharmacokinetics (PK) = Absorption (A),
Distribution (D), Metabolism (M) and Elimination (E).
Therefore, PK=ADME

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 The common terms used in description of pharmacokinetics
are: Bioavailability (F) for absorption, Volume of
distribution (Vd) for distribution, extraction ratio (ER) for
metabolism and Clearance (CL) for elimination

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• Bioavailability and Half-life of Drugs
 Bioavailability is the fraction of administered drug that
reaches systemic circulation. For example, if 100mg of a
drug is administered orally and 80mg of the drug is
absorbed, the bioavailability is 80% or 0.8
 The capital letter F is used to represent bioavailability
 When a drug is administered through intravenously, all of
the amount reaches systemic circulation, and thus
bioavailability is 100% or 1

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 Half-life (t1/2) is the time required for the concentration of
drugs in the body (blood) to remain to half of the original
concentration
 Half-life is useful in designing drug dosage regimens,
predicting elimination (clearance) and distribution of a drug
(volume of distribution)

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• Drug interactions can lead to synergetic (when the drug's
effect is increased) or antagonistic (when the drug's effect is
decreased) effects

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• Toxic Dose, Therapeutic Dose and Therapeutic Index
 Therapeutic dose is the dose that produces a clinically desired or
effective response.
 Toxic dose is the dose that produces toxicity
 Therapeutic index (TI) of a drug is the ratio of the dose that produces
toxicity to the dose that produces a clinically desired or effective
response
 Therapeutic Index=Toxic dose/Effective dose=TD/ED
 Therapeutic index is a measure of drug’s safety. The higher the TI
indicates that there is a wider margin between doses that are effective
and doses that are toxic
 The higher TI the higher the safety of the drug and vice versa
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 Some drugs with a low therapeutic index include;
• Lithium
• Digoxin
• Carbamazepine
• Cyclosporin
• Phenytoin
• Phenobarbitone
• Theophylline (Aminophylline)
• Warfarin

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• Tolerance, Habituation, Dependence and Addiction
 The term tolerance is used to describe a more gradual
decrease in responsiveness to a drug, taking days or weeks
to develop
 Generally, tolerance is the decrease in pharmacological
effect on repeated administration of the drug

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 Drug dependence describes the state when drug-taking
becomes compulsive, taking precedence over other needs,
often with serious adverse consequences. This involves
physical and psychological dependence

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 Drug dependence is viewed as a reversible pharmacological
phenomenon whereas addiction is a chronic, relapsing
human condition, a distinct from acute illness that can be
cured by abstinence

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• Habituation or adaptation is a process which occur when a
drug is given repeatedly or continuous, such that cessation of
the drug has an aversive effect, negative reinforcement, from
which the subject will attempt to escape by self-
administration of the drug

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• Adverse Drug Reactions (ADRs)
A response to a medicinal product that is noxious or potentially
harmful and unintended and which occurs at doses normally used in
human for prophylaxis, diagnosis or therapy of a disease or for the
modification of physiological function in which individual factors may
play an important role

• Side effect
Any unintended effect of a pharmaceutical product occurring at doses
used in man which is related to the pharmacological properties of the
product and in which there is no deliberate overdose

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• Drug indications are those diseases, signs and symptoms that may be
treated by using a specific drug.

• Indication specifies which condition the medication can treat and

sometimes also dictates which age group is meant to receive the
medication

• A drug indication does not suggest complete resolution, total relief or

a cure from using the drug but is based on success achieved in clinical
trials

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• A contraindication is when a drug should not be used because it
could cause harm to the person taking the drug
• Contraindications refers to those conditions, physical, mental or
emotional state as well as other signs and symptoms which may be
present where a specific drug should not be used

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• Off- label uses of medications means a medication is being used to
treat something other than the original approved uses. Well
sometimes the side effects of a medication are actually more helpful
than the medication itself

• Drug warning is a notice to inform the patient that there may be risk
in using the drug in certain diseases or medical states
• Placebo is a medicine or procedure prescribed for the psychological
benefit to the patient rather than for any physiological effect.

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• Drug interaction is a situation in which a substance (usually another
drug) affects the activity of a drug when both are administered
together
OUTCOMES OF DRUG INTERACTIONS
• Loss of therapeutic effect
• Toxicity
• Unexpected increase in pharmacological activity
• Beneficial effects e.g. additive & potentiation (intended) or
antagonism (unintended).
• Chemical or physical interaction e.g. I.V incompatibility in fluid or
syringes mixtures

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• Precautions are methods or procedures intended to prevent or avoid
adverse outcomes

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RECAP
 What is Pharmacology?
 What is a drug?
 What is a pro-drug?
 What are the main sources of drugs?
 What is Pharmacokinetics?
 What is drug bioavailability?
 What is half-life of drugs?
 What is pharmacodynamics?
 What is therapeutic index?
 What do you understand by the terms tolerance, habituation, dependence and addiction?

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