Zero Order
Zero-order kinetics is described when a
constant amount of drug is eliminated per
unit time.
The rate is independent of the
concentration of the drug.
Bioequivalence
In Bioequivalence the two drugs release
the active ingredient into the bloodstream
at the same amount.
It has the same rate and quality.
pH
pH is simply the measure of acidity (or
alkalinity/basicity) of a solution.
when pH is equal to pKa, the drug is
ionized halfly.
Therapeutic Index
The therapeutic index is a quantitative
measurement of the relative safety of a
drug.
It is a comparison of the amount of
a therapeutic agent that causes
the therapeutic effect to the amount that
causes toxicity.
Pre Oral
A majority of the drugs are administered
orally as it is a convenient, safe and
affordable route of administration.
The effect of the drug in the body is
dependent on its absorption in the
digestive system.
Potency
It is an expression of a drug in terms of the
conc of the drug required to produce a
defined effect
First Order
First order kinetics occur when a constant
proportion of the drug is eliminated per unit
time.
It is a concentration-dependent process
Therapeutic Equivalence
Drug products are considered to be
therapeutic equivalents only if they are
pharmaceutical equivalents and have
same effects.
It has the same clinical effect and safety
profile when administered to patients .
pKa
The pKa of a drug is the hydrogen ion
concentration (pH) at which 50% of the
drug exists in its ionized hydrophilic form .
The pKa of a drug influences lipophilicity,
and permeability which in turn
directly affects pharmacokinetic
characteristics.
Margun of Safety
In margin of safety of a drug we can use a
drug for therapeutic purposes without
risking too many adverse effects at the
same time.
The margin of safety is estimated by
something known as the therapeutic index
.
Sublingual Route
Sublingual administration of drug refers to
the placement of drug under the tongue.
It involves placing a drug under your
tongue to dissolve and absorb into your
blood through the tissue there.
Efficacy
Efficacy judges the therapeutic
effectiveness of the drug in humans.
Potency denotes the amount of drug
needed to produce a given effect.
Competitive Antagonist
A competitive antagonist binds to the
same site as the agonist but does not
activate it, thus blocks the agonist's action
Atropine is a competitive antagonist of the
actions of acetylcholine and other
muscarinic agonists.
Bioequivalence
In Bioequivalence the two drugs release
the active ingredient into the bloodstream
at the same amount.
It has the same rate and quality.
Phase I
Phase I reactions of
drug metabolism involve oxidation,
reduction, or hydrolysis of the parent drug,
resulting in its conversion to a more polar
molecule.
This phase perform the functionalization
reactions.
H.E Inducer
Hepatic enzyme induction is generally an
adaptive response associated with increases
in liver weight
It help in induction of gene expression, and
morphological changes in hepatocytes
Pharmacokinetics
Pharmacokinetics is the study of what the
body does to the drug,
It refers to the movement of any drug
going into, through, and out of the body.
It refers to the relative ability of a drug-
receptor complex to produce a maximum
functional response.
Non-Competitive Antagonist
A non-competitive antagonist binds to an
allosteric (non-agonist) site on the receptor
to prevent activation of the receptor.
ketamine is a non-competitive antagonist .
Bioavailability
Bioavailability refers to the extent and rate
at which the active moiety enters systemic
circulation, thereby accessing the site of
action.
It is largely determined by the properties of
the dosage form, which depend partly on
its design.
Phase II
Phase II reactions involve conjugation by
coupling the drug or its metabolites to
another molecule, such as glucuronidation,
acylation, sulfate, or glicine.
This phase perform the biosynthetic
reactions.
H.E Inhibitor
Drugs that cause CYP450 drug interactions
are referred to as
either inhibitors or inducers.
An inducing agent can increase the rate of
another drug's metabolism by as much as two-
to threefold that develops over a period of a
week.
Pharmacodynamics
Pharmacodynamics is the study of what
the drug does to the body. ...
The drug interactions occur
on pharmacodynamic
Oral Route Patental Route
Oral administration of drugs is the most Parenteral products are liquid preparations
used method of drug therapy. Absorption administered directly into body tissues
of these drugs is given by the membrane
permeability.
For drugs administered orally, absorption Administration of parenteral includes the
may begin in the mouth and stomach. following routes:
• Subcutaneous (under the skin)
• Intramuscular (in a muscle)
• Intravenous (in a vein)
• Intrathecal (around the spinal cord)

SHORT ANSWERS
ANS NO - 01

IMPORTANCE OF FIRST PASS EFFECT:

The first pass effect is a phenomenon in which a drug gets metabolized at a specific
location in the body. The liver metabolizes many drugs, sometimes to such an extent
that only a small amount of active drug emerges from the liver to the rest of the
circulatory system. This first pass through the liver thus may greatly reduce the
bioavailability of the drug.

ANS NO – 02

PHYSICO-CHEMICAL PROPERTIES OF DRUGS

Solubility and permeability are considered as the major physicochemical factor

that affect the rate and extent of oral drug absorption, moreover other physicochemical
properties always show their effects to drug absorption via affecting solubility and
permeability.

ANS NO – 03

URINARY EXCRETION OF BASIC DRUG

Excretion of a drug is dependent on intrinsic properties of the drug, such as pH and

size. For example, weakly acidic drugs display increased excretion in basic urine, while
weakly basic drugs are excreted more readily in acidic urine. Alkalinization of urine has
the opposite effect. In some cases of overdose, these principles are used to enhance
the excretion of weak bases or acids.
 ANS NO – 04

MECHANISM OF UP AND DOWN REGULATION

UP REGULATION:

An increase in the number of receptors on the surface of target cells, making the cells
more sensitive to a hormone or another agent. For example, there is an increase in
uterine oxytocin receptors in the third trimester of pregnancy, promoting the contraction
of the smooth muscle of the uterus.

DOWN REGULATION:

An decrease in the number of receptors on the surface of target cells, making the cells
less sensitive to a hormone or another agent. For example, insulin receptors may be
downregulated in type 2 diabetes.

ANS NO – 05

INTRACELLULAR RECEPTORS WORKING

Intracellular receptors. Once stimulated by lipid-socluble ligands, intracellular

receptors translocate to the nucleus and bind to response elements of the spacer DNA,
altering the rate of gene expression. The hormone-receptor complex binds to promoter
regions of responsive genes and stimulate or sometimes inhibit transcription from those
genes.

ANS NO – 06

IMPORTANCE OF SECOND MESSENGER

Second messengers are intracellular signaling molecules released by the cell in

response to exposure to extracellular signaling molecules the first messengers. Second
messengers trigger physiological changes at cellular level such as proliferation,
differentiation, migration, survival, apoptosis and depolarization.

ANS NO – 07

IMPORTANCE OF ION TRAPPING

Ion trapping alters the urine pH to inhibit reabsorption of toxins across the renal tubular
membranes. The principle behind this approach is to “trap” the toxin in its ionized form
in the urine where it can be excreted.