GENERAL PHARMACOLOGY

ABOUT ME

✓ HIMT College of Pharmacy, Greater Noida

✓ NIPER Mohali (Pharmaceutical Management)

✓ GPAT and NIPER Qualified

✓ I teach Pharmacology, Biotechnology, and MBA

✓ Have taught over 1000+ and guided over 10,000

students

✓ Founder of Pharmaminds
 PHARMAMINDS CLASSES STARTING
FROM 15th JULY, 2024

REASONS TO JOIN PHARMAMINDS

✓ ALL COACHING TO HAVE GPAT AND NIPER QUALIFIED FACULTIES

✓ MOST AFFORDABLE COACHING IN INDIA

INTRODUCTION
Pharmacology is all about study of drugs. Pharmakon means drugs and logy means Study and hence
study of drugs.
BASIC TERMS
1, Pharmacodynamics
It is study of effect of drug on body

2. Pharmacokinetics
It is study of effect of body on drug

3. Drug
It is single chemical entity present in a medicine that is used for diagnosis, treatment and cure of disease.
BASIC TERMS
4. Pharmacotherapeutics
✓ Pharmacology + Therapeutics

✓ Therapeutics - Knowledge of Drug, Dosage and Duration

✓ Overall effect is improvement of the patient

BASIC TERMS
5. Chemotherapy
✓ Treatment of systemic infection with specific drugs that have selective toxicity for infecting organism and
malignant cell

✓ It has no or minimum effects on body or host

✓ Such specific drugs are Chemotherapeutic agents

BASIC TERMS
6. Orphan Drugs
They are Biological Products for diagnosis/treatment/ prevention of rare disease or common disease
(endemic only in resource-poor countries)

✓ Cost is High (Since customers are less)

Examples:-
1. Intermittent Porphyria
2. Systemic Sclerosis
LIST OF IMPORTANT ORPHAN DRUGS

FIRST BCP
Fomivirisen Thiotepa

Icatibant Bevacizumab

Rifamixin Busulfan

Rituximab Colchicine , Carboprost and Clofazimine

Sodium stibogluconate Paromomycin

Sodium thiosulfate
BASIC TERMS
7. Me- Too Drugs

✓Aka – Follow on Drugs

✓Drugs which are structurally similar to prototype drugs with only minor differences.

✓These carry a negative image and can lower down the prices.

ORPHAN – HIGH PRICE

ME- TOO – LOW PRICE

ROUTE OF ADMINISTRATION

Route of
Administration

Local Systemic

Enteral
Topical Intrathecal Intraarticular Parenteral
(Through GIT)

Inejcatables
Oral Rectal and Non-
injectables
ROUTE OF ADMINISTRATION (LOCAL)
1. Topical
a. Skin and Mucous Membranes
b. Eye; Nasal; Ear Drops

✓ Absorption depends upon on skin and the relation is inversely proportional.

Thicker the skin, lesser the absorption.
ROUTE OF ADMINISTRATION (LOCAL)
Posterior auricular > Scrotal > Scalp > Dorsum of hand >Plantar area.
(In terms of higher absorption)
ROUTE OF ADMINISTRATION (LOCAL)
2. Deeper Tissues

A. Intrathecal
Injection is applied in fluid filled space between thin layers of tissue that cover brain and spinal cord –
Example Amphotericin B

B. Intraarticular
Injection into joint

C. Intraarterial
Injection directly into an artery
ROUTE OF ADMINISTRATION (LOCAL)

INTRAARTICULAR INTRATHECAL INTRAARTERIAL

ROUTE OF ADMINISTRATION (LOCAL)

Artery is blood vessel so

why this route is local.

1. Giving injection in artery is very

difficult as it is deeply seated
2. We use artery for only localized
action such as cancer drugs and
angiography.
ROUTE OF ADMINISTRATION (SYSTEMIC)
ENTERAL PARENTERAL

✓ Oral
TIN
SYSTEMIC ✓ Rectal
✓ T – Transdermal

✓ I – Inhalational
✓ Sublingual
✓ N – Nasal
✓ Transbuccal

ENTERAL PARENTERAL
ROUTE OF ADMINISTRATION (SYSTEMIC)
1. Oral
✓ Safe and Economical but it has the most variable absorption (GPAT 2015) among all routes.

✓ Some drugs are not effective in oral due to:-

1. First pass metabolism
2. Incomplete absorption due to acid destruction.
SUPPOSITORY

2. Rectal
✓ In the rectal route, drug is given through the rectum (dosage form is suppository)

✓ First Pass Metabolism observed in the rectal dosage form is less as compared to oral.
ROUTE OF ADMINISTRATION (SYSTEMIC)
1. Oral
✓ Safe and Economical but it has the most variable absorption among all routes.

✓ Some drugs are not effective in oral due to:-

1. First pass metabolism
2. Incomplete absorption due to acid destruction.

2. Rectal
✓ In the rectal route, drug is given through the rectum (dosage form is suppository)

✓ First Pass Metabolism observed in the rectal dosage form is less as compared to oral.
MORE CLARITY ON FPM and BA
FIRST PASS METABOLISM

✓ Drug goes to the liver and the liver metabolizes some of the drug which is called Hepatic Extraction or
First Pass Metabolism (FPM) or Pre-systemic metabolism.

✓ Portal Circulation is the flow of Blood from GIT to Liver which occurs via Portal Vein.

✓ Therefore, in emergency cases, IV and sublingual are the best routes

✓ IV and SL Route - Drug directly enters the blood and it does not have to go through FPM therefore
bioavailability is 100%
BIOAVAILABILITY (B/A)
✓ Fraction of drug that reaches the systemic circulation in unchanged form is bioavailability.

✓ Bioavailability ranges from 0 to 100 and a fraction(0 to 1)

✓ Drugs given by IV(100% -Maximum) and Sublingual have the highest bioavailability as they reach blood
directly.

✓ Oral and Rectal are only two routes that have first-pass metabolism.

✓ B/A depends on site of administration(absorption) and First Pass Metabolism(FPM)

BIOAVAILABILITY (B/A)
DRUGS WITH HIGH FPM

Nitrates Have Large Pre- Systemic Metabolism

✓Nitrates – Nitrates
✓Have – Hydrocortisone
✓Large – Lidocaine
✓Pre – Propranolol
✓Systemic – Salbutamol
✓Metabolism – Morphine
BIOEQUIVALENCE
✓ Suppose there are two preparations say X and Z having the same drug, same dose, same dosage form and
the difference of bioavailability of these preparations is ±20% Then they are termed to be as
bioequivalent that is they will produce similar plasma concentration.

✓ Example – Adalat and Procardia containing Nifedipine are bioequivalent.

✓ Exception is Phenytoin

±20%
ROUTE OF ADMINISTRATION (SYSTEMIC)
3. Sublingual Route
✓ Sublingual has nearly 100% Bioavailability

✓ It can be Self – Administered and used for emergency purposes

These drugs are given via Sublingual - NICE

N – Nitroglycerine
N- Nifedipine
I- Isosorbide dinitrate
C- Clonidine
ROUTE OF ADMINISTRATION (LOCAL)

Why Sublingual is given

in emergency

IT’S SIMPLE BECAUSE

DRUG DIRECTLY REACHES
TO BLOOD
ROUTE OF ADMINISTRATION (SYSTEMIC)
4. Transbuccal

✓ Medication is delivered through the buccal mucosa (lining of the mouth)

✓ This route is often used for drugs that are not absorbed well through the stomach or intestines, such
as nicotine replacement therapy products.

✓ Medicine is kept between the cheek and gum (Buccal cavity)

ROUTE OF ADMINISTRATION (PARENTERAL)
INJECTION ANGLE KEY POINTS
Intramuscular (IM) 90 Degree Deep into Muscles
Subcutaneous (SC) 45 Degree Insulin + Self Administer
Intravenous(IV) 25 Degree Directly to Blood hence B/A is 100%

Intradermal Route 10-15 Degree ✓ Bleb Formation

✓ Drug Testing for Allergy
✓ BCG
ROUTE OF ADMINISTRATION (PARENTERAL)
HOW TO LEARN ANGLES IM SC

IM ------------------ 90 degree

SC ------------------- 45 degree

IV-------------------- 25 Degree
ROUTE OF ADMINISTRATION (PARENTERAL)

Intraperitoneal Nearly 45 degrees Directly into peritoneal cavity

(space that contains the organs in
abdomen)

Intravitreal Nearly 45 degrees Directly into vitreous humor

(into human eye).

Intraosseous Nearly 90 Degrees Bone Marrow

ROUTE OF ADMINISTRATION (PARENTERAL)

INTRAPERITONEAL INTRAVITREAL

INTRAOSSEUS
ROUTE OF ADMINISTRATION (PARENTERAL)
Non-Injectables --------- TIN

1. Transdermal Route
✓ Only For highly lipid-soluble drugs and those which can be absorbed through intact skin

✓ Constant release of drug and hence constant level is maintained in blood.

✓ Examples – Steroids, Nitroglycerine, Nicotine, Fentanyl, Hyoscine

ROUTE OF ADMINISTRATION (PARENTERAL)
Nasal Route
✓ Drugs insufflated through the nose

✓ Such route has advantages such as Low FPM/High Blood Flow/High Surface Area which means
good absorption and good bioavailability

✓ Examples – Nafarelin (GnRH Agonist), calcitonin and desmopressin

ROUTE OF ADMINISTRATION (PARENTERAL)
3. Inhalational Route
✓ Drugs must be atomized into smaller droplets so that it passes through trachea(windpipe).

✓ Examples – Asthma drugs and Inhalational Anaesthetic agents.

✓ Rate of drug delivery can be controlled.

✓ Drug Delivery System is Aerosol.

QUESTIONS
QUESTION 1
For intravenous injection, angle of administration is____________ degrees.
A. 30
B. 25
C. 60
D. 90
ROUTE OF ADMINISTRATION (PARENTERAL)
INJECTION ANGLE KEY POINTS
Intramuscular (IM) 90 Degree Deep into Muscles
Subcutaneous (SC) 45 Degree Insulin + Self Administer
Intravenous(IV) 25 Degree Directly to Blood hence B/A is 100%

Intradermal Route 10-15 Degree ✓ Bleb Formation

✓ Drug Testing for Allergy
✓ BCG
QUESTION 2
Which of the following injection is given into eyes:
a. Intraarticular
b. Intraarterial
c. Intravitreal
d. Intramuscular
ROUTE OF ADMINISTRATION (PARENTERAL)

Intraperitoneal Nearly 45 degrees Directly into peritoneal cavity

(space that contains the organs in
abdomen)

Intravitreal Nearly 45 degrees Directly into vitreous humor

(into human eye).

Intraosseous Nearly 90 Degrees Bone Marrow

QUESTION 3
What kind of drugs are costly due to less customers?
A. Rare Drugs
B. Follow on Drugs
C. Generic Drugs
D. Branded Generic Drugs
Orphan Drugs
They are Biological Products for diagnosis/treatment/ prevention of rare disease or common disease
(endemic only in resource-poor countries)

✓ Cost is High (Since customers are less)

Examples:-
1. Intermittent Porphyria
2. Systemic Sclerosis
QUESTION 4
Which of the following route is talked about here:-
A. Drug reaches blood
B. Drug is released in constant amount
C. Patches are applied

a. Inhalational
b. Transdermal Patch
c. Intrathecal
d. Intraosseous
1. Transdermal Route
✓ Only For highly lipid-soluble drugs and those which can be absorbed through intact skin

✓ Constant release of drug and hence constant level is maintained in blood.

✓ Examples – Steroids, Nitroglycerine, Nicotine, Fentanyl, Hyoscine

QUESTION 5
Aerosol is associated with which dosage forms:-

a. Inhalational
b. Transdermal Patch
c. Intrathecal
d. Intraosseous
3. Inhalational Route
✓ Drugs must be atomized into smaller droplets so that it passes through trachea(windpipe).

✓ Examples – Asthma drugs and Inhalational Anaesthetic agents.

✓ Rate of drug delivery can be controlled.

✓ Drug Delivery System is Aerosol.

QUESTION 6
Bioavailability of drug refers to:
A. Ratio of drug excreted unchanged in urine to that excreted as metabolites
B. Fraction of drug reaching the target to produce the action
C. Length of time an administered drug is available for action
D. Percentage of administered dose that reaches the systemic circulation in the unchanged form.

P. Only A
Q. B and C
R. C and D
S. D only
QUESTION 7
For a drug to be bioequivalent, there should not be a difference of more than:-

A. 10%

B. 20%

C. 30%

D. 5%
BIOEQUIVALENCE
✓ Suppose there are two preparations say X and Z having the same drug, same dose, same dosage form and
the difference of bioavailability of these preparations is ±20% Then they are termed to be as
bioequivalent that is they will produce similar plasma concentration.

✓ Example – Adalat and Procardia containing Nifedipine are bioequivalent.

✓ Exception is Phenytoin