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1.

WHO definition of Health :-Health is a state of complete physical,


mental and social well-being and not merely the absence of disease or
infirmity

2. What is a drug?:-Drug is a biological active substance, when


introduced into body, interacting with specific molecular in the body,
resulting in a physiological change to elevate or lower bodys function
OR

A substance used in the diagnosis, treatment, or prevention of

a disease or as a component of a medication.


3. What is a placebo?:-A placebo is an inactive pill, e.g., sugar pill,
liquid, or powder (made with corn, rice, etc) that has no treatment
value.Placebo can sometimes improve a patients condition
simply because the person has the expectation that it will be helpful.

-Placebo effects: The drug effects results from its own chemical and

physical properties and the expectation of the patient.


4. Describe the meaning of Pharmacology:- Pharmacology is the study
of the rule and mechanism of mutual interaction between drugs and
living systems, which include human species, animal, and organism.
Pharmacology comprises mainly Pharmacokinetics and
Pharmacodynemics, which provides the base for drugs in preventing,
diagnosing, and treating diseases.

5. What is pharmacokinetics? :-Studying of the dynamic changes of


drugs in the body, that is, the process of absorption, distribution,
biotransformation (metabolism) and excretion of drugs in the body.
6. Describe the feature of Passive transport

Passive transport has following features:

(a) transport from high to low concentration;


(b) needs no energy;

(c) no drug transport saturation;


(d) No drug competition and selectivity;

(e) drug transport is influenced by lipid solubility of drug and by


differences in pH across the membrane. The primary drive force is the
concentration gradient of drug across the membrane, so the transport
process achieves homeostasis when the concentration of both sides are
equal. (e) The majority of drugs are transported by passive transport,
which include Simple diffusion, Filtration.
7. Give the definition of Drug absorption? Do all kinds of
administration possess absorption?

Movement of drug molecules from the site of administration to the


systemic circulation by passing the cell membrane barrier is called
Absorption.
8. First pass effect : When a drug is absorbed across the GI tract, it
enters the portal circulation before entering the systemic circulation. If
the drug is rapidly metabolized by the liver, the amount of unchanged
drug that gains access to the systemic circulation is decreased.

9. BBB-The barriers between brain cell and blood, brain cell and
cerebrospinal fluid, as well as blood and cerebrospinal fluid are called
blood brain barrier. Blood brain barrier protects brain from circulating
toxin, high MW or highly water soluble drugs, e.g., quaternary amines,
and harmful solutes.

10.Placenta barrier:-Placenta barrier refers to the physiological barrier


separating the fetal blood from the maternal blood by placenta.
However, the permeability of the placenta doesnt differ dramatically
from other biological membranes, so most drugs can easily cross the
placenta and enter the breast milk. The difference is the limited
maternal blood flowing into placenta, the fastest time for drug
equilibration between mother and fetus is in the order of 10-15 min.

11. The importance of drug Plasma Protein binding

Drug-plasma protein binding is reversible and is served as a drug


reservoir

Only free drug has pharmacological effects,


A competition site for many different drugs

DPPB act as a transport mechanism for the drug to the site of action
or elimination.
Reduction of drug distribution, biotrans- formation and excretion

12. The difference between biotransformation and metabolism

metabolism means "breakdown" and "inactivation". However,


biotransformation include not only "breakdown" and "inactivation but
also synthetic reactions.

13.Bioavailability:-It is used to describe the fraction of an administered


dose that reaches the systemic circulation, one of the principle
pharmacokinetic properties of drugs. OR Bioavailability is expressed
as the fraction of administered drug that gains access to the systemic
circulation in a chemically unchanged form.It also express the fraction
of the dose(F)that is absorbed and escapes and first-pass elimination.

- absolute bioavailability
- relative bioavailability

14.Clearance:-It describes irreversible removal of drug from the body by


all processes and is made up of renal clearance and metabolic
clearance.

CL=rate of elimination/C

15.Pharmacology:-It is the study of how drugs exert their effects on


living systems.

Pharmacologists work to identify drug targets in order to learn how


drugs work.
Pharmacologists also study the ways in which drugs are modified
within organisms.

In most of the pharmacologic specialties, drugs are also used today as


tools to gain insight into both normal and abnormal function.
Divisions of Pharmacology
Pharmacokinetics

Pharmacodynamics
Pharmacogenomics
16.What does Pharmacodynamics mean?:-It describe biochemical and
biophysical actions of drugs on the body,
the mechanisms of their actions,

the dose-effect relationship of drugs, and the basis for reasonable


application of the drugs in clinics.

17.Receptor:A receptor can be defined as any biologic target


macromolecule in cells that interacts specifically with extra-cellular
signals

e.g., a ligand or a drug and converts it into intracellular effects.


18. How are receptors classified?

MEMBRANE BOUND RECEPTORS


G-Protein-coupled receptors

Serotonin, Muscarinic, Dopaminergic, Noradrenergic


Transmembrane kinase receptors
Tyrosine kinase

Ligand-gated ion channel receptors


Nicotinic, GABA, glutamate

INTRACELLULAR AND NUCLEAR RECEPTORS


Hormone receptors
Autocoid receptors

Growth factors receptors


Insulin receptors

19. What is drug action and drug effects?


Drug action: The interaction between drug and targetreceptor,
enzyme of biological system.

Drug effects: observable consequences caused by a drug action.

20.Specificity:-It measns that a drug only binds to one single type of


receptor and causes one single effect.

21.Selectivity:-It means that a drug binds to one or a few types of


receptors with higher affinity than to other receptors.

22.Cyp450:- Cytochrome P450 in the hepatic microsome is the main


enzyme for the biotransformation of endogenous and exogenous agents.
OR The metabolic enzymes known as the microsomal mixed function
oxidase system(cytochrome p-450).

23.Hepatoenteric circulation:- Some drug conjugates are excreted into the


bile and subsequently released into the intestine where they are
hydrolysis back to the parent compound , which forms hepato-enteral
circulation.
24.Apperant volume of distribution:- The apparent volume of distribution
(Vd) is purely a hypothetical and dose not represent an actual physical
volume inside the body.

Vd means that when the drug in the body reaches balance, the ratio
between the drug in the body and the blood drug level.
Vd(L)=D(mg)/C(mg/l)

C=plasma concentration of drug


D=total amount of drug in the body

25.Plasma Half life:- The t1/2 is the time it takes for the plasma
concentration or the amount of drug in the body to be reduced by
50%.
t1/2=0.693/K

26.Affinity :-the strength of the reversible interaction between a drug and


its receptor.
The measures of the propensity of a drug to bind with a given
receptor

Affinity is often expressed as 1/Kd

Affinity is in inverse ratio to Kd

D+R=DR=E, Kd=[D][R]/DR

- KD expresses the affinity of the drug for receptor

- Affinity index(pd2)= -logkD,larger pd2 is, the higher the affinity is.
27.Median effective dose (ED50):-It refers to the dose of a drug that
gives rise to a response in 50%of the subjects. The more potent the
drug, the lower its ED50 is

28.Therapeutic index:- The therapeutic index of a drug is the ratio of the


LD50 to ED50.TI is the measure of the drug safety.
Therapeutic index (TI) =LD50/ED50

29.Drug tolerance:- the intensity of some drugs responses to a given


dose may change during the course of therapy, usually decreasing as a
consequence of continued drug administration.
Pharmacokinetic tolerance and

Pharmacodynamic tolerance

30.Dependance:- a biologic phenomenon often associated with drug

abuse, including 1)Physical dependence 2) Psychological dependence.


31.Therapeutics window:-themargin of therapeutic concentration,that is to
see the plasma concentration between minimum effective
concentration(MEC) and minimum toxic concentration(MTC).

32.Certain safety factor(CSF):-It also described as margin of safety.


CSF=LD5/ED95

33.Margin of safety:-The equation value between minimum effective dose


and minimum toxic dose.

34.Maximal efficiency (Efficacy):-Maximal response a drug can produce.


The maximal biological response produced by a drug.Efficacy of a
drug depends on density or the number of active receptors.

For the drugs of same family, the higher affinity of a drug binding to
the receptors, the less concentration of a drug required to achieve same
effects.
35.Potency:-Measure of dose required to produce a response. Determined
by the affinity of a drug to the receptor , and by the efficacy of the
drug, expressed in terms of the amount required to produce an effect to
given intensity. The more potent a drug the less the amount required to
produce the effect.
36.Median lethal dose(LD50):-It refers to a dose that give rise to the
death of 50% of subjects.The larger of LD50, the smaller the toxicity.

37.Median toxic dose:- A dose that causes a toxic effect in 50% of

subjects. MTD- maximum tolerated dose (or minimum toxic dose)


(more than this will produce signs of toxicity).
Also called highest nontoxic dose (HNTD)

38.Threshold dose:-The least amount of drug needed to exest therapeutic


effects.Threshold dose also called minimal effective dose.
39.Steady-state concentration:- A steady-state plasma concentration of
drug occurs when the rate of drug elimination is equal to the rate of
administration.

40.Side effects:- A peripheral or secondary effect, especially an


undesirable secondary effect of a drug or therapeutic regimen.

In the range of therapeutic dosage, the drug effects, which are


not related to the current therapeutic purpose, are described as side
effects.

The pharmacological base of the presence of side effects is the

low selectivity of the drug.


41.Toxic effects:- All drugs can produce toxic effects if the dose is high
enough or drugs are long term used. Classification according to
on-set-speed of drug toxicity

the distribution of drug toxicity


the extent of drug toxicity
the cause of drug toxicity

42.Drug therapeutic effect:-The desirable and beneficial result of a drug


treatment.
43. Drug adverse reaction (ADR):- The unwanted ,negative, and harmful
effects resulting from drug therapy. ADR may cause physiological or
pathological change. ADR may be caused or influenced by therapeutic
purpose, such as overdose of a drug, stopping drug administration, long
term use of drug, non-compliance with a drug therapy regimen, etc.

44.Intrinsic activity ():-Biological response induced by drug-receptor


interaction.
The efficacy of a drug is decided by its intrinsic activity, and

numbers of receptor. Affinity and intrinsic activity is important to a


drug which binds to a receptor and induce biological responses.

the ability of drug activate receptor. The efficacy of a drug is decided


by its intrinsic activity.

E/Emax= [DR]/RT

45.AGONIST:- A drug is said to be an agonist when it binds to a


receptor and causes a response or effect. It has intrinsic activity = 1
OR

Full agonist ( a drug or endogenous ligand),

- two properties : the affinity to bind to receptor

exert maximal biologic effects

(intrinsic activity). = 100%


46.PARTIAL AGONIST:-A drug is said to be a partial agonist when it
binds to a receptor and causes a partial response. It has intrinsic
activity < 1. 0% < < 100%

two properties :can bind to receptors


produce low intrinsic activity.

47.ANTAGONIST:- A drug is said to be an antagonist when it binds to


a receptor and prevents (blocks or inhibits) a natural compound or a
drug to have an effect on the receptor. An antagonist has NO activity.
Its intrinsic activity is = 0. = 0

OR

A pure

antagonist : can bind to receptors without intrinsic activity but can


antagonize the biologic effects of corresponding agonist.
48.Competitive antagonist :- :- Reversibly binds to receptors in common
with an agonist;

the maximal effects of an agonist are not depressed by the


corresponding competitive antagonist.

The effect of a reversible antagonist can be overcome by more drug


(agonist). A small dose of the antagonist (inhibitor) will compete with
a fraction of the receptors thus, the higher the concentration of
antagonist used, the more drug you need to get the same effect.

49.Non-competitive antagonist :-Irreversibly binds to receptors; the


antagonism can not be overcome by increasing the concentration of
agonist.The effect of irreversible antagonists cannot be overcome by
more drug (agonist). The antagonist inactivates the receptors. The
maximal effects of the agonist are reduced by the corresponding
noncompetitive antagonist ,because the agonist and non-competitive
antagonist do not compete for the same site on the receptor.
50.Physiologic ANTAGONIST:- A drug that binds to a non-related
receptor, producing an effect opposite to that produced by the drug of
interest. Its intrinsic activity is = 1, but on another receptor.

51.Chemical ANTAGONIST:- A chelator (sequester) of similar agent that


interacts directly with the drug being antagonized to remove it or
prevent it from binding its receptor.
-A chemical antagonist does not depend on interaction with the
agonists receptor (although such interaction may occur).
ANTAGONIST:- A drug is said to be an antagonist when it binds to a

receptor and prevents (blocks or inhibits) a natural compound or a drug


to have an effect on the receptor. An antagonist has NO activity. Its
intrinsic activity is = 0.

= 0

OR

A pure antagonist can bind

to receptors without intrinsic activity but can antagonize the biologic


effects of corresponding agonist.

Therapeutic index:- The therapeutic index of a drug is the ratio of the


LD50 to ED50.TI is the measure of the drug safety.
Therapeutic index (TI) =LD50/ED50

Plasma Half life:- The t1/2 is the time it takes for the plasma

concentration or the amount of drug in the body to be reduced by 50%.


t1/2=0.693/K

First pass effect(elimination) : When a drug is absorbed across the GI


tract, it enters the portal circulation before entering the systemic

circulation. If the drug is rapidly metabolized by the liver, the amount of

unchanged drug that gains access to the systemic circulation is decreased.

Bioavailability:-It is used to describe the fraction of an administered dose


that reaches the systemic circulation, one of the principle

pharmacokinetic properties of drugs. OR Bioavailability is expressed as


the fraction of administered drug that gains access to the systemic

circulation in a chemically unchanged form.It also express the fraction of


the dose(F)that is absorbed and escapes and first-pass elimination.
absolute bioavailability
relative bioavailability

Side effects(After effect) (residual reaction):- A peripheral or secondary

effect, especially an undesirable secondary effect of a drug or therapeutic


regimen.

In the range of therapeutic dosage, the drug effects, which are not
related to the current therapeutic purpose, are described as side
effects.

Median effective dose (ED50):-It refers to the dose of a drug that gives
rise to a response in 50%of the subjects. The more potent the drug, the
lower its ED50 is.

Drug tolerance:- The intensity of some drugs responses to a given dose


may change during the course of therapy, usually decreasing as a
consequence of continued drug administration.
Pharmacokinetic tolerance and

Pharmacodynamic

tolerance

Absorption:- Movement of drug molecules from the site of administration


to the systemic circulation by passing the cell membrane barrier is called
Absorption.

MIC (minimal inhibitory concentration):- MIC is the lowest

concentration of antimicrobial agents that prevents(inhibit) visible


bacterial growth in 18-24 hours incubation.
Resistance:-

Means bacterial populations previously-sensitive to

antibiotics become insensitive.

OR The ability of bacteria and other microorganisms to withstand a drug


to which they were once sensitive and were once slowed in growth or
killed outright.

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