1.

Drug, action, dosage, therapeutic uses, adverse

effect
2. Pharmacological terminologies
3. Routes of drug administration
4. Absorption, distribution, metabolism & excretion of
drugs
5. Receptor ; its types involved in drug interaction
6. Major receptor families
7. Renin Angiotensin System
8. Types of Pharmacologic antagonism
9. Therapeutic Index
10.Types of drugs formulations

The word pharmacology is

derived from Greek words
PHARMAKON which means drug
remedy (to do good) and logos
means study.
OR
The branch of medicine
concerned with the uses,
effects, and modes of action
of drugs.
DEFINITION:
According to WHO 1992-
A drug is any substance or product
that is used on intended to be used
to modify or explore physiological
system or pathological states for the
benefit of the recipient.
OR
A pharmaceutical drug, also called a
medication or medicine, is a
chemical substance used to treat,
cure, prevent, or diagnose a disease
or to promote well-being.

AIMS OF DRUG:
To improve quality of life

In pharmacology, the term mechanism of action (MOA) refers to

the specific biochemical interaction through which a drug substance
produces its pharmacological effect. Following are some examples
discussed:
i-Metformin (GLUCOPHAGE) (Anti-diabetic agent):The main MOA of
metformin is reduction of hepatic glucogenesis (formation of glucose)
thereby decreasing blood sugar levels.
ii- Antacids: Antacids are weak bases that reacts with gastric acid to
form water and a salt thereby diminish gastric acidity.
iii-Anti-Motility agents: They activate presynaptic opiod receptors in
Enteric nervous system to inhibit Acetylcholine release and decreases
peristalsis thereby treating loose motions. For example Lopermaide
(IMODIUM).
 iv-ACE Inhibitors(Antihypertensive agents): ACE inhibitors inhibits
the aldosterone release and eliminates sodium and water from the
kidney which in turn decreases Blood pressure of the patient.
Example Lisinopril (ZESTRIL), Captopril (CAPOTEN).
 v-Anti-hyperlipidemic drugs (Cholesterol lowering agents): These
drugs inhibit cholesterol synthesis by competing effectively to inhibit
the HMG CoA reductase the rate limiting step in the cholesterol
synthesis thus depleting the intracellular supply of cholesterol. This
depletion leads to lower the bad cholesterol i.e. LDL and increase the
good cholesterol i.e. HDL. Example: STATINS( Atorvastatin (STAT-A),
Rosuvastatin (XPLENDID)and Simvastatin (ZOCOR).

 vi-NSAIDS (Anti-inflammatory drugs) work by inhibiting the activity

of COX enzymes (CYCLOOXYGENASE ).In cells, these enzymes are
involved in the synthesis of key biological mediators,
namely prostaglandins which are involved in inflammation. For
example: Naproxen sodium (SYNFLEX), ketorolac (TORADOL),
ibuprofen (BRUFEN) and aspirin (DISPRIN)

DEFINITION:
Uses of medicinal agent which affect the
course of condition ,diseasis,syndromes or
pathology to benefits the health of an
individual .

EXAMPLE:

• Metformin (GLUCOPHAGE/NEODIPAR) use in

diabetes .
• Domperidone (MOTILIUM) use in emesis
(vomiting).
• Loperamide (IMODIUM) use in loose motions.
• Losartan (COOZAR/QSARTAN)use in
hypertension (increase BP)
• Atorvastatin (STAT-A/LIPIGET)use in lowering
serum cholesterol.
• Paracetamol (PANADOL) use as antipyretic.
• Allopurinol (ZYLORIC)use in lowering uric acid.
• Vit B12 (METHYCOBAL) use in B12 deficiency
• Morphine used as an analgesic.
• Omeprazole (RISEK) use in gastric reflux.
• Drotaverine (NOSPA) use as antispasmodic.
• Amoxycillin/clavulinic acid (AUGMENTIN): use to
treat several infections.
• Cefixime (CEFSPAN) use in treating enteric fever
and severe infections.
• Clopidpgrel (LOWPLAT) use as an antiplatelet
agent i.e. thinning blood.

 A symptoms produced by a drug or

therapy that is injurious to the patient .
Its basically an untoward reaction of the
drug. Following are some examples
discussed:
1- Domepridone(MOTILIUM) a drug used
in nausea and vomiting, may cause Skin
rash, dry mouth and soreness.

2-Metformin (GLUCOPHAGE), use for

controlling diabetes, may cause
megaloblastic anemia, diarrhea and
malabsorption of folic acid.

3- Lopermaide(IMODIUM), use for

diarrhea, may cause dizziness, drowsiness
and fatigue.
 4-Omeprazole (RISEK), use for controlling acid reflux,
may cause bone fracture, anemia and
hypomagnesemia.

5-Verapamil (CALAN), use in controlling BP, may

cause constipation.

6-Atorvastatin
(LIPIGET) use in cholesterol control,
may cause myopathy.

 7- Beclomethasone (CLENIL/RHINOCLENIL) inhaler

use in asthma, may cause palpitations, anxiety and
muscle cramps.

 8- Cetrizine (RIGIX) use in allergic conditions, may

cause dizziness, drowsiness and dry mouth.

 9-Bromazepam (LEXOTANIL) use in depression , may

cause irregular heart beat and unusual excitement.

 DOSE :
A specified quantity of a therapeutic agent, such as medicine,
prescribed to be taken at one time or at stated intervals.

Example : T.Paracetamol (PANADOL) 1 gm 6hrly or TDS

T. Clarithromycin (KLARICID) 500mg 12hrly
T. Domperidone(MOTILIUM)10mg TDS(30mins before
meal)
C. Omeprazole (RISEK) 40mg 0D (30 mins before meal)

 DOSAGE FORM :
Dosage forms are pharmaceutical drug products in the form in
which they are marketed for use, with a specific mixture of active
ingredients and inactive components (excipients), in a particular
configuration.

Example :
Syrup, ointment, tablet, capsule, injection, creams,etc
DEFINITION:
Uses of medicinal agent which affect the
course of condition ,diseasis,syndromes or
pathology to benefits the health of an
individual .

EXAMPLE:

• Metformin (GLUCOPHAGE/NEODIPAR) use in

diabetes .
• Domperidone (MOTILIUM) use in emesis
(vomiting).
• Loperamide (IMODIUM) use in loose motions.
• Losartan (COOZAR/QSARTAN)use in
hypertension (increase BP)
• Atorvastatin (STAT-A/LIPIGET)use in lowering
serum cholesterol.
• Paracetamol (PANADOL) use as antipyretic.
• Allopurinol (ZYLORIC)use in lowering uric acid.
• Vit B12 (METHYCOBAL) use in B12 deficiency
• Morphine used as an analgesic.
• Omeprazole (RISEK) use in gastric reflux.
• Drotaverine (NOSPA) use as antispasmodic.
• Amoxycillin/clavulinic acid (AUGMENTIN): use to
treat several infections.
• Cefixime (CEFSPAN) use in treating enteric fever
and severe infections.
• Clopidpgrel (LOWPLAT) use as an antiplatelet
agent i.e. thinning blood.

 A symptoms produced by a drug or

therapy that is injurious to the patient .
Its basically an untoward reaction of the
drug. Following are some examples
discussed:
1- Domepridone(MOTILIUM) a drug used
in nausea and vomiting, may cause Skin
rash, dry mouth and soreness.

2-Metformin (GLUCOPHAGE), use for

controlling diabetes, may cause
megaloblastic anemia, diarrhea and
malabsorption of folic acid.

3- Lopermaide(IMODIUM), use for

diarrhea, may cause dizziness, drowsiness
and fatigue.
 4-Omeprazole (RISEK), use for controlling acid reflux,
may cause bone fracture, anemia and
hypomagnesemia.

5-Verapamil (CALAN), use in controlling BP, may

cause constipation.

6-Atorvastatin
(LIPIGET) use in cholesterol control,
may cause myopathy.

 7- Beclomethasone (CLENIL/RHINOCLENIL) inhaler

use in asthma, may cause palpitations, anxiety and
muscle cramps.

 8- Cetrizine (RIGIX) use in allergic conditions, may

cause dizziness, drowsiness and dry mouth.

 9-Bromazepam (LEXOTANIL) use in depression , may

cause irregular heart beat and unusual excitement.

TERMINOLOGIES DESCRIPTION
TACHYCARDIA ↑ 𝐻𝐸𝐴𝑅𝑇 𝑅𝐴𝑇𝐸
BRADYCARDIA ↓ 𝐻𝐸𝐴𝑅𝑇 𝑅𝐴𝑇𝐸
MIC Minimium Inhibitory Concentration

TDM Therapeutic Drug Monitoring

SYNERGIST Additive effect of two drugs in combination for e.g:
NSAIDs produces additive analgesic effects with
paracetamol.
ANTAGONIST An antagonist blocks an action of another substance
for e.g: Omeprazole decreases the antiplatelet
effect of clopidogrel.
AGONIST an agonist causes an action of another substance.
For e.g: morphine mimics the actions of endorphins
at μ-opioid receptors in our CNS.
*( Endorphins inhibit the communication of pain
signal)
CYP450 CYTOCHROME P450 (Liver Metabolising Enzyme)
TERMINOLOGIES DESCRIPTION

ADR Adverse Drug Reaction

SIDE EFFECT Undesirable effect of a drug or medical treatment.
LD Lethal Dose a dose (usually recorded as dose per
kilogram of subject body weight) at which a
given percentage of subjects will die. For e.g: The
minimum LD of Digoxin is 10mg/70kg
PT Prothrombin Time is a blood test that measures how
long it takes blood to clot. For e.g: Measurement of
clotting time while using drug: Warfarin (an
anticoagulant drug).
HS At Bed Time For e.g: Sleeping pills: Alprazolam
(XANAX).
QID Four times a day
QD Once a day
SOS As Per Need for e.g: Pain killer
BD Twice a day
TDS Thrice a day

TERMINOLOGIES DESCRIPTION

PO PER ORAL
NPO NON PER ORAL
HALF LIFE the time required for any specified property (e.g.
the concentration of a substance in the body) to
decrease by half. For e.g: Half life of Omeprazole
is 1 HR
BRAND NAME Trade Name for e.g: PANADOL
GENERIC NAME Chemical name for e.g: Paracetamol
PPI Proton Pump Inhibitor For e.g: Omeprazole (RISEK)
H2 ANATAGONIST H2 receptor blocker For e.g: Ranitidine (ZANTAC)
ACE INHIBITOR Angiotensin converting enzyme inhibitor For e.g:
Lisinopril (ZESTRIL)
ARB Angiotensin Receptor Blocker For e.g: Losartan
(COOZAR)
DIURETICS A substance that increase production of urine
(DIRUESIS).For e.g: Furosemide (LASIX)
 Passive diffusion .Movement of drug
molecule from higher concentration to lower
concentration without the use of energy,lipid
soluble drug transported by passive diffusion
 Active transport . Movement of drug
molecule from lower concentration to higher
concentration with the use of energy e.g
transport of symphatomimetic drug into
neural tissues ,transport of choline into
cholinergic neuron and absorption of
levadopa from the intestine.
 Facilitated diffusion is the transport of
substances across a biological membrane
from an area of higher concentration to an
area of lower concentration with the help of
a transport molecule.
 Endocytosis involves engulfment of drug
molecule by the cell membrane eg vitamin
B12
 Exocytosis is the reverse of endocytosis and
is used by cells to secrete many substances
by a vesicle formation for example
acetylcholine and nor epinephrine

The rate and extent of absorption depend on

• Environment – where the drug is getting absorbed i.e.
favourable for the absorption of the drug or not. For
example an acidic drug can easily get absorbed from
stomach since stomach has got HCl(an acid), whereas an
acid sensitive drug requires another path or formulation
otherwise acid would degrade the drug.

• Chemical characteristic of drug- actually pertains to the

nature of the drug whether its basic or acidic, its lipophilic
or hydrophilic and so forth.

• Route of administration – is determined by mainly

therapeutic objective and properties of the drug. For
example Insulin is degradable in stomach and requires a
full day need therefore it is injected subcutaneously form
where it releases and absorbs time to time.
• Etc
 Drug distribution is the process by which a drug
reversibly leaves the bloodstream and enters the
interstitium(extracellular fluid)and the tissue. The
distribution of a drug from the plasma to the interstitium
depend upon :

• Cardiac output and local blood flow

• Capillary permeability
• The tissue volume
• Degree of binding drug to plasma and tissue protein
• Lipophilicity of drug

 Chemical alteration of the drug in a living

organsim is called biotransformation
 It converts the lipid soluble inionized drug
into water soluble and ionized compounds
which the body excrete in short period of
time.
 Sites liver is the main site for drug
metabolism other GI tract ,bile ,lungs, blood
,skin
 Phases I reaction includes oxidation ,reduction
hydrlysis
 Phase II reaction consist of conjugation
reaction.these conjugates are polar ,usually
water soluble such as
glucoronidation,acetylation etc

Kidney is the primary organ

for the removal of drug for
those are water soluble and
non volatile.
Other sites are lungs feaces
,bile, skin etc
 DEFINITION:
A Receptor is
a protein molecule that
receives chemical signals
from outside a cell. When
such chemical signals bind
to a receptor, they cause
some form of cellular/tissue
response, e.g. a change in
the electrical activity of a
cell.

 Receptor mechanism is
very important in
understanding the effect
of the drug.

 There are two major types of receptors:

1. Intracellular
2. Cell-surface receptors

1- Intracellular receptors: are located in the cytoplasm of the cell

and are activated by hydrophobic ligand molecules that can pass through the
plasma membrane.
2- Cell-surface receptors: bind to an external ligand molecule and
convert an extracellular signal into an intracellular signal.
 Three general categories of cell-surface receptors include: ion -channel,
G- protein, and enzyme -linked protein receptors.
 Ion channel -linked receptors bind a ligand and open a channel through
the membrane that allows specific ions to pass through.
 G-protein-linked receptors bind a ligand and activate a membrane
protein called a G-protein, which then interacts with either an ion
channel or an enzyme in the membrane.
 Enzyme-linked receptors are cell-surface receptors with intracellular
domains that are associated with an enzyme.
 The renin angiotensin system stabilizes blood pressure and volume via
liver, kidneys and adrenal cortex.
 When renal blood flow is reduced, juxtaglomerular cells in the kidneys
convert the precursor prorenin (already present in the blood)
into renin and secrete it directly into the circulation .
 Plasma renin then carries out the conversion of angiotensinogen,
released by the liver, to angiotensin I.
 Angiotensin I is subsequently converted to angiotensin II by
the angiotensin-converting enzyme (ACE) found on the surface of vascular
endothelial cells, predominantly those of the lungs.
 Angiotensin II is a potent vasoconstrictive peptide that causes blood
vessels to narrow, resulting in increased blood pressure.
 Angiotensin II also stimulates the secretion of the hormone aldosterone
from the adrenal cortex.
 Aldosterone causes the renal tubules to increase the reabsorption
of sodium and water into the blood, while at the same time causing the
excretion of potassium (to maintain electrolyte balance). This increases
the volume of extracellular fluid in the body, which also increases blood
pressure.
 If the RAS is abnormally active, blood pressure will be too high. There are
many drugs that interrupt different steps in this system to lower blood
pressure. These drugs are one of the primary ways to control high blood
pressure, heart failure, kidney failure, and harmful effects of diabetes.
 DEFINITION:

 The TI; It is the

therapeutic index (

ratio of dose that

produce toxic effect to
the dose that produces
therapeutic effects. .
  FORMULA FOR CALCULATING TI IN HUMANS:

Therapeutic index= TD50/ED50

o FORMULA FOR CALCULATING TI IN ANIMALS:

Therapeutic index= LD50/ED50

Where, TD= Toxic dose or median toxic dose,

ED=Effective dose,
LD=Lethal dose,
TI=Therapeutic Index.

 TOXIC DOSE OR MEDIAN TOXIC DOSE(TD50):

In toxicology, the median toxic dose (TD50) of a drug or toxin is
the dose at which toxicity occurs in 50% of cases. The median
toxic dose encompasses the category of toxicity that is greater
than half maximum effective concentration (ED50) but less than
the median lethal dose (LD50).

 EFFECTIVE DOSE (ED50):

An effective dose (ED) in pharmacology is the dose or
amount of drug that produces a therapeutic response or
desired effect in some fraction of the subjects taking it.
The ED50 is commonly used as a measure of the
reasonable expectancy of a drug effect, but does not
necessarily represent the dose that a clinician might use.
This depends on the need for the effect, and also the
toxicity.
 LETHAL DOSE (LD50):
The lethal dose or median lethal dose LD50 is a value of for a
substance is the dose required to kill half the members of a
tested population after a specified test duration. LD50 figures
are frequently used as a general indicator of a
substance's acute toxicity. A lower LD50 is indicative of
increased toxicity.

 Larger the therapeutic index safer the drug

 For e.g: penicillins have larger therapietic index
whereas digoxin has less therapeutic index.
 By knowing therapeutic index we can measure
the toxicity levels of the drug and thereby using
caution in the narrow therapeutic index drugs.
 Drugs having narrow therapeutic range:
1. Quinine
2. Digoxin
3. Lithium
4. gentamicin
• Intrathecal route (drug is injected into the
subarachnoid space so that it reaches the CSF
Eg lignocaine,antibiotic
• Intra articular (drug is injcted into joint
space.e.g hydrocortisone injection for
rheumatoid arthritis.
• Transdermal patch eg scopolamine patch
for motion sickness,nitroglycerin patch .
 Route of administration is the path by which a drug, fluid,
poison, or other substance is taken into the body. Routes of
administration are generally classified by the location at which
the substance is applied. Common examples include:

• Oral
• Intravenous
• Intramuscular
• Intraocular (in the eyes)
• Intra aural (in the ear)
• Intra nasal (in the nose)
• Intra arterial (into the artery)
• Intra rectal (into the rectum)
• Intra spinal (into the spinal)
• Intra osseous (into the bone)
• Subcutaneous (in the skin)
• Topical (on the skin)
• Transdermal (beneath the skin)
 SOLID
(tablets,capsules,powder,lozenges,suppositories
 Liquid
 (aqeous
solution,syrups,suspension,emulsions,lotions,injec
tions)
 Semi solid ( ointment,creams,paste,jel)
 Gas (inhalation,aerosal)

SOLID FORMULATIONS
 Tablets – a tablet is disc-shaped and prepared by compressing a granulated
powder in a die of suitable machinery. They are mostly coated with inert
substances like starch to help them disintegrate in the digestive tract of the
patient. A binding agent, lubricating material, and flavors are added to the
tablets to make them palatable.

 Enteric Coated Tablets – are coated with a material that does not disintegrate
in the acidic medium of the stomach but in the alkaline medium of the
intestine. They can’t be chewed but consumed only by swallowing.

 Controlled Release Tablet – is designed to release the active ingredient of the

drug in a specific amount over a specified period of time. Here, the amount of
drug released is gradual over the day and doesn’t depend upon the pH of the
digestive tract of the patient. Thus, a uniform amount of drug is released at a
uniform rate.

 Sustained release preparations – release a fixed amount of drug over an

extended period of time. Thus, they improve the treatment compliance by the
patient.

 Capsules – can be hard or soft. Hard capsules contain the drug in solid form,
which gets dissolved easily in water. Soft capsules have the drug in liquid or
semi-solid form,
 Lozenges –solid forms that dissolve slowly in
mouth e.g strepsils.
 Suppositories -are used for drugs which are
administered through the rectum. The drug is absorbed
by the rectal mucosa and directly enters the
bloodstream. The method is useful when a patient is
unconscious, has nausea or difficulty in swallowing.

 Aqeous solution (drug +water+preservatives)

 Syrup (soluble drug +water+flavouring
 Suspension ( insoluble drug+water)
 Emulsion (mixture of two or more unmixable
liquid
 Injections
 Elixirs ( solution that contain an alcohol and
water base and falvour)
 Contain both liquid and
solid
 Creams are semi –solid
emulsions that is
mixture of oil and water
 Paste are semisolid
dosage forms that
contain one or more
drug substances
intended for topical
application.
 Ointment a smooth oily
substance that is
rubbed on the skin for
medicinal purposes