PHARMACOLOGY;

Pharmacology is the combination of greek words i.e pharmacon

(drug or medical agent) ,logos (study).

Pharmacology is the branch of medical Sciences which contains

the knowledge of history source physical properties chemical
properties , physiological effects, mechanism of actions,
absorption , distribution, biotransformation, excreation, therapeutic
uses and adverse or toxic effects of drugs. OR

pharmacology is the science that deals with the effects of drugs

on living system

DRUG:
It is a chemical Substance that effects the processes
(Physiological functions) of living organisms .Drugs are the
substances that can only modify physiological/pathological
functions of living organisms and it cannot create any new function
in living body. OR

Drug is the unfinished or unformulated form of medicines .

MEDICINE:
when the drugs are formulated in proper dosage form and used for
prevention and treatment of diseases then it is called medicines .

NOTE: Every medicine is a drug but not every drug is a medicine.

BRANCHES OF PHARMACOLOGY
1. PHARMACOKINETICS:
It means the movement of drug within the body . It includes
the process of absorption, Distribution, metabolism and
excreation i.e (ADME).

pharmacokinetics means that “what the body does to the drug” .

2. PHARMACODYNAMICS:
It is the study of drug related to their mechanism of action ,
pharmacological actions and their adverse effects or simply
“what the drug does to the body is called pharmacodynamics .
3. PHARMACOTHERAPEUTICS:
In this branch we study the uses of drugs for prevention and
treatment of diseases .
4. CLINICAL PHARMACOLOGY :
In this branch we study the effects of drugs on human
beings .
5. TOXICOLOGY :
In toxicology we study the possible toxic effects (side and
adverse effects) of the drug used for the treatment or
prevention of diseases.
6. EXPERMENTAL PHARMACOLOGY:
It deals with the study of effects of drugs on experimental OR
laboratory animals like rabbits, mice, rats, dogs, snakes etc.
7. PHARMACY:
It deals with the study of preparation, dispensing and
utilization of drugs.
 DRUG NOMENCLATORE;
“Naming drugs”
Drugs usually have three types of names which are as
follows.
1: BRAND NAME
2: GENERIC NAME
3: CHEMICAL NAME

1. BRAND NAME :
This name is given to a drug by its manufacturers . Brand
names are short and easy to recall. A drug usually has many
brand names Brand name are also called proprietary name
E.g. Panadol, Disprin etc
2. GENERIC NAME:
Generic names are given to a drug with respect to the active
constituent present in drug i.e (API) Generic names are same
for a drug worldwide. It cannot be changed .E.g Paracetamol,
Aspirin etc .
3. CHEMICAL NAME:
It denotes the chemical structure of a drug.

e.g Acetyl salicylic acid is chemical name of aspirin and

N-aceyl-p-aminophenol (Acetaminophen) is the chemical Name
of paracetamol.

Note: Brand names and generic names are suitable for

prescription of drugs but chemical names are not suitable in
order of prescription.
 SOURCES OF DRUGS:
Drugs can be obtained from various sources e.g.

1.Natural Source

2. Synthetic Source

3. Biosynthetic

Natural source of drugs:

In natural source all those drugs are included which are derived
from plants, animals, micro organisms or mineral source.

Example of plant source is morphine from papaver somniferum or

poppy plant. Atropine from belladona plant Quinine from Cinchona
bark etc.

Example of Animal source is insulin from pig or ox pancrease , cod

liver oil from cod fish etc .

Example of microorganism source is pencillin obtained from

pencillium, Bacitracin from bacillius sabtillis plant etc.

MINERAL SOURLE OF DRUGS

Example of mineral source is calcium <Ca+2> ,sodium<Na+>,
potassium<K+> , iron<fe>,magnesium<mg>, zinc<Zn> etc.

2.SYTHETIC SOURCE OF DRUGS

1. These drugs are prepared in laboratories by different

synthesis procedures.
Example is Aspirin, sulfonamides, Barbiturates, Benzodiazapines
etc.

3 . SEMI Synthetic source of drugs

These drugs are prepared in pharmaceutical Labs by Chemical

modification of natural products

4 . Biosynthetic source of drugs,

These drugs are obtained by genetic engineering (DNA

recombinant technology) e.g human insulin, human growth
hormones etc.

ROUTES OF DRUG ADMINISTRATION:

Routes of drug administration can be divided into different types

1. ENTERAL ROUTE
2. PARENTERAL ROUTE
3. INHALATIONAL ROUTE
4. TOPICAL ROUTE

1) ENTERAL ROUTE ; Enteral route is sub classified into

a) ORAL route
b) Sublingual route
c) Rectal route
ORAL route of drug administration:
In oral route drugs are administerd by mouth.
ADVANTAGES
 _ common and convenient route .
-safe route
- require no technical expert.
-A variety of drugs like tab, cap, syp, sus.etc are administered
through oral route
DISADVANTAGES
Oral route follow first pass metabolism
Require patient co-operation.
This route cannot be followed in case of unconscious and
vomiting conditions.

(B) SUBLINGUAL ROUTE:

Through this route drugs are administered into body by placing it

under the tounge from where it gets absorbed and reaches to
systemic circulation and finally to target tissues to show its effects.

ADVANTAGES;

Avoids first pass effect

Can be followed in emergency condition
Less quantity of drug can produce optimum pharmacological
effect.
Reduce toxicity because when patient get relief so the
remaining drug can be spit out easily.

DISADVANTAGES;

Too hard tab absorption will be delayed and also its

pharmacological effect will be delayed .
If the tab is too soft so it will be rapidly dissolved and patient will
spit it out then its effect will not be optimum.

(C) RECTAL ROUTE;

Through this route drugs are adminstred into the rectum from
where it get absorb into the local tissues and blood to show its
pharmacological effects.

ADVANTAGES;

IT Avoids first pass effect.

A safe route for unconscious and vomiting patients.

DISADVANTAGES;
It is an embaracing route of drug administration .

Patient hesitate from this route of drug administration .

Sometimes local irritation is also produced.

(2) PARENTERAL ROUTE:

By this route drugs are administred into body through injections.
Parenteral route is further classified into.

(a) I/V (intra venous)

b. I/M (intra muscular )

c. S/C (sub cutaneous)

d. I/D (intra dermal )

E. I/ventricular (intra ventricular)
F. Intra articular

ADVANTAGES;
Can be used in emergency conditions.
Can be used for unconcious patient.
Can be used for vomitting patients .
Rapid effect.
Avoids first pass effect.
Have high bio availability as compared to other routes of drug
administration.
I/v route has 100% bioavailability.
DISADVANTAGES;
Painful route
Needs a technical expert
Needs aseptic conditions.
Drugs should be sterile.
Expensive drugs administration route
Can cause severe type of adverse reactions in case of
contamination.
Mostly its effects are irreversible.

(3) INHALATIONAL ROUTRE.

By this route drugs are adminstred by inhalation .These drugs
directly reaches to lungs from where it get absorbed and goes to
blood and target site to show its pharmacological effect.

Advantages of INHALATIONAL ROUTE

 Rapid effect
Require less dose
Toxicity is minimized by less dose.

DISADVANTAGE

Can cause local irritation.

Only few drugs are administered through this route.

TOPICAL ROUTE
Through this route drugs are administered directly on skin surface or
mucous membrane of nose, eyes, mouth ,vagina, urethra etc.

ADVANTAGES:
Cheap method

Reduce toxicity and side effects.

Pharmacokinetics:
It means the movement of drug in the body or what the body does to the
drug is called pharmacokinetics. Pharmacokinetics can be best defined by
ADME.

A. Absorption of Drugs:
The movement of a drug from the site of administration into the blood
stream is known as drug absorption.

Absorption of drug in body takes place by;

1) Diffusion (simple diffusion process of drugs)
2) Filtration (depends on molecular size and weight of drug)
3) Active transport (movement of drug molecule from a region of lower to
higher concentration)
4) Facilitated diffusion ( carrier mediated transport of drug)
 5) Bidirectional diffusion (exchange of molecules across the cell
membrane)
Factors influencing/ affecting drug absorption

1) Nature of drug:
Absorption of lipid soluble (lyophilic) drug are more as compared to water
soluble (hydrophilic) drugs.

2) Physical State of drug:

Drugs in liquid form are rapidly absorbed than hard form of drugs.

3) Presence of food or other drugs in GIT:

In GIT, already another available drug or food substances can increase or
decrease absorption of a drug.
E.g. Presence of milk in GIT decreases absorption of doxycycline.

4) Surface area:
As intestines has greater surface area than stomach so that’s why
absorption of drugs is mostly occur in intestine.

5) Particle size of drug:

Smaller the particle size of drug so more will be the absorption rate.

6) Gastric pH changes:
When gastric pH change so drug absorption rate will also changes because
pH maintenance is important for drug dissolution and absorption

B. Distribution of drugs:
It is the transfer of drug from blood stream to cells or tissues. After
absorption distribution process occurs and drug is distributed in body fluids.

Factors influencing drug distribution:

Nature of drug:
If a drug is lipid in nature so it will be distributed easily and more as
compared to hydrophilic or water-soluble nature type of drug because our
body’s cell membrane is almost composed of lipid substances so that’s why
like attracts like phenomena will take place.

Blood brain barrier (BBB):

The capillary boundary that is present between blood and brain is called
blood brain barrier (BBB). So only lipid soluble drugs can pass though BBB to
show its pharmacological effects.

Free drug and bound drug:

Most of the drugs bind with blood proteins i.e. albumin that drug is called
bound or binded drug so its distribution become low was compared to the
free drug which is not binded with blood proteins so that drug flow easily and
distributed well.

Blood Supply:
Body organs like heart, brain, kidney has more blood supply as compared to
other organs of body so that’s why in these organs drugs are distributed
more.

C. METABOLISM of drug:
Change in Chemical structure of a drug in the body is called metabolism. The
metabolism of a drug usually converts lipids soluble and unionized drugs
into water soluble and ionized form for excretion. If a drug is highly polar
(ionized), hydrophilic so then it may not get metabolized and is excreted as
such. Metabolism mainly occur in liver but it may also occur in GI tract,,
Kidney, lungs, skin, blood in small amount.

Phases of metabolism:
Metabolism occur in 2 phases;

Phase I:
It includes oxidation reduction and hydrolysis of drug. Oxidation is carried by
crp 450 (cytochrome) enzymes.
Phase II:
Phase II consists of conjugation reactions. If the Phase I metabolites are
polar so they are excreted in urine or bile. However, many metabolites are
non-polar or less polar so they undergo conjugation reactions to become
polar i.e., water soluble for its effective removal from the body.

Factors affecting drug metabolism

Age:
Adults metabolize drugs more than neonates and elder people.

Diet:
poor nutrition can decrease enzyme function so rate of metabolism
becomes low.

Metabolic organ disease:

Failure of liver can also decrease drug metabolism.

Simultaneous administration of drug:

This can result in increased or decreased metabolism of drugs.

D. EXCREATION OF DRUG
Removal of drug and its metabolites from the body is known as drug exertion.
the main channel of excretion of drugs is kidney, however drugs can also be
excreted through lungs, bile, feaces, tears, sweat, saliva, breast milk.

CLINICAL PHARMACOKINETICS:
Bioavailability of drugs
Bioequivalence of drugs
Therapeutic equivalence of drugs.
Half-life of drugs (t ½)

A. BIOAVAILABILITY OF DRUGS:
The amount of active drug that is present in blood or target site is known as
bioavailability of that drug. Bioavailability is the quantitively analysis of
biological active drug that reaches to blood’ systemic circulation. Drugs
administered by I.V route has the highest bioavailability i.e., 100%. It is
because I.V route avoids Its pass effect and also the administered drug
directly reach to blood without requiring absorption from site of
administration.

FACTORS EFFECTING BIOAVALABILITY OF DRUG:

pH and ionization
presence of food and other drug
GI and other diseases
Route of administration
First pass metabolism
Hepatic diseases
Area of absorbing surface.
Importance of bioavailability:
By confirmation of bioavailability we determine the route of administration of
a particular drug. For example if a drug administered orally and it is
extensively metabolized, so as a result bioavailability of that drug become
low and thus it decreases the pharmacological effect of that drug. Then that
drug is formulated in I.V or I.M dosage form to achieve the desired
pharmacological effect.

B. BIO EQUIVALANCE OF DRUG

It is the equal bioavailability of two different brands of different
manufacturer (companies) containing the same (API). If both different
brands are used in same pathological conditions for a patient. If both these
drugs/brands produce the same bioavailability so these both drugs are
bioequivalent to each other.

C. THERAPEUTIC EQUIVALANCE OF DRUGS:

If two different drugs administered to patients for same therapeutic effect
and both drugs show same therapeutic effect at same time so it is known as
therapeutic equivalence of these drugs.
D. HALF LIFE OF DRUGS (t ½):
The time taken by a drug to reduce to half of its original concentration (t ½)
in the blood is called half-life of that drug. Round about a drug takes 4 to 6
half-life for its complete elimination.

Clinical importance of half-life:

It helps to determine;

The duration of action

The frequency of drug administration i.e. OD, B.D.T.D.S
Estimate the time required to reach the steady state of drug. (a steady
state is achieved when the amount of drug administered become
equal to drug eliminated).

Duration of Action (DOA)

The time to which the drug continuously show its pharmacological effect in
body is known as duration of action. So more the duration of action, more
will be the pharmacological effect.

ONSET OF ACTION
It is the time interval in which the drug just show/start its pharmacological
effect.

Agonist:
It is the drug/chemical agent or hormones that can activate/stimulate the
drug receptor to produce pharmacological effect or response.

Drug receptor:
These are the specialized protein present on cell surface or in cell and
receive the signal/stimulation from the agonist.

Antagonist:
It is the chemical substance that block/inhibit or cancel the effect of agonist
at the receptor site.

Receptor regulation:
It includes:
a) Down regulation:
when receptors becomes desensitized (less sensitive) or decrease in
number when repeatedly exposed to an agonist is known as down regulation.

b) Up regulation:
When receptor becomes more or super sensitized to an agonist is
known as up regulation.

Affinity of drug:
The combining capacity of a drug with its specific receptor is known as
affinity of drug.

Efficacy of drug:
It is the maximum effect of a drug. Increasing dose of a drug increase
effects of that drug but a stage reaches upon which further dose increasing
will not cause raise in effect of that drug i.e. maximum effect. So that
maximum effect is called efficacy of drug.

Potency of drug:
It is the amount of drug required to produce a desired response. Lower the
dose required for a given response so more potent is the drug

OR
If a drug produces same effect as compared to other drugs but
comparatively in low dose is known as potent drug and the whole
phenomena is known as potency of that drug.

For Example: Analgesic dose of morphine is 10 mg and that of pethidine is

100 mg. therefore morphine is ten times more potent than pethidine.

PRO DRUG:
It is the inactive form of drug and when prodrug gets metabolized in liver so
then it becomes active. E.g. methyl dopa.
USES OF PRO DRUGS:

1) To improve bioavailability:
For example dopamine is active form of drug and it cannot cross BBB so we
administered levodopa (pro drug) which cross BBB and then become active
and reach to target site in blood.

2) To prolong duration of action:

3) to improve taste

4) To provide site specific drug delivery.

PHARMACODYNAMIC INTERATCION OF DRUG:

These are the type of interactions due to which the effect of one drug
change due to presence of another drug at site of action.
Pharmacodynamics interaction are of the following four types.

1) Antagonism:
The reaction in which one drug cancel the effect/action of another drug at
receptor site.

Antagonism may be;

Competitive antagonism (agonist and antagonist compete for receptor
binding)
Noncompetitive antagonism (No completion)
Physical antagonism (Due to physical properties of agonist &
antagonist)
Chemical antagonism (due to chemical properties of agonist and
antagonist).

2) Potentiation:
When the combine effect of two drugs is greater than the effect of individual
drug so it is known as potentiation. In potentiation one drug will be inactive e.
g. two drugs with their effects (1+1>2).
3) Synergism
When the combine effect of two drugs is greater than the individual drug
effect is known as synergism. In synergism both drugs will be active.

4) Addition/Summation:
The combine effect of two drugs given together is the sum of the effect of
individual drugs its termed as addition. E.g., two drugs (20+20=40)
I

Tolerance:
it means need for larger doses of a drug to produce a given/desire effect
tolerance arises due to repeated use of a drug due to which body response
to that drug become decreases. Tolerance is commonly seen with drugs like
morphine, alcohol, amphetamine etc.

Habituation:
It is a condition due to repeated use of a drug with a desire to continue the
use of that specific drug with or without increasing the dose.

Drug dependence/Addiction:
It is a condition in which a person desire to use a drug with a tendency to
increase its dose with passage of time. Drug dependence maybe physical or
psychological such person feels discomfort it he/she stop these drugs
suddenly. E.g. A heroin addict person if suddenly stop heroin intake so that
person will face headache, pain sweating, nausea, vomiting etc. These
symptoms are called withdrawal symptoms.

HYPERSESITIVITY:
Hypersensitivity is an allergic response (immunological) of a body to a drug.
E.g. penicillin can cause hypersensitivity reactions which include
anaphylactic shock, skin rashes etc.

Therapeutic Index (TI):

Therapeutic index is an index of drug safety. It is the ratio of median lethal
dose to median effective dose. i.e.
(TI) =.Medianlethal doseLD50 of drugMedian effectivedose(ED50) of drug

LD50 = It is the dose of drug which is lethal for 50% of population. It can
cause death.

ED50 = It is the dose of drug which produces the desired effect in 50% of the
population. Higher the value of therapeutic index so safer is the drug. E.g.,
penicillin G has high TI than warfarin so penicillin is safer than warfarin.

LOADING DOSE:
Loading dose is that dose of a drug which is administered to achieve the
desired plasma level rapidly, followed by a maintenance dose which
maintain the required amount of drug in the body. Generally loading dose is
given in case of serious infections or arrhythmias.

Maintenance Dose:
A dose which maintains the required amount of drug in the body.

IDIOSYNCRASY:
The unusual response of a body to a certain drug is called idiosyncrasy
mainly occurs due to inherited abnormalities, or due to genetic differences
i.e.

Succinyl choline cause paralysis.

Primaquine can cause hemolysis.
Placebo:
Placebo is an inactive preparation (tab or cap or solution) given to satisfy
patient psychic need for a drug therapy. Placebo is mainly used in clinical
trials for discovery of new drugs.

Volume of distribution (VD):

The volume or fluid of the body in which the drug is assumed to be
distributed is called volume of distribution. VD is not actual volume; it is a
theoretical volume.

V.D = Dose(md)CPo
CPo = Plasma Concentration

Drug Clearance:
The volume of plasma cleared of a drug per unit time is called drug
clearance.

Drug elimination:
The irreversible removal of a drug from the body by either excretion process
or biotransformation/metabolism process is called drug elimination.

ANTHELMINTIC DRUGS:

Overview:
Nematodes, trematodes and cestodes are three major groups of helminthes
(worms) that infect humans. So anthelmintic are the drugs which are used to
destroy or expel the worms from human body.

Chemotherapy of helminthic infections for nematodes:

Diethylcarbamazine
Mebendazole
Pyrantel pamoate
Thiabendazole
Ivermectin

Chemotherapy of helminthic infection for trematodes:

Praziquantel

Chemotherapy of helminthic infections for cestodes:

Albendazole
Niclosamide

Albendazole:
It is an anthelmintic drug which is used for round worm, hook worm and pin
worms.

MOA:
It inhibit glucose uptake in nematodes/worms and thus causing their death.
USES:
Giardiasis, hook worm infection, pin worm infection, Ascariasis.

Adverse effect:
Vomiting, diarrhea, tachycardia, headache, respiratory distress.

Mebendazole:
It is a broad spectrum anthelmintic agent. It is effective in treating intestinal
worm infections

MOA:
Same to Albendazole.

Pyrantel Pamoate:
Pyrantel is effective in the treatment of infections caused by roundworms,
pinworms, hook worms.

MOA:
It cause release of acetylcholine and as a result cause paralysis of the
worms which is then removed from body in stools.

ADVERSE EFFECTS:
Nausea,

vomiting,

diarrhea,

insomnia,

headache,

dizziness.

Piperazine:

MOA:
It cause paralysis of worms and thus then expelled out from the body.
Uses:
Pin worm, round worm.

ADVERSE EFFECT:
Nausea,

vomiting,

headache,

diarrhea.

NICLOSAMIDE:
It is an alternative of praziquantel for treatment of cestode infections. It
mainly inhibits mitochondrial phosphorylation of cestodes and causing its
death.

USES:
Mostly used for tape worms.

Adverse Effects:
GI upset,

dizziness,

headache.

Anti-amebic/Anti protozoal drugs

Overview:
Amebiasis (amebic dysentery) is an infection of the intestinal tract caused
by Entamoeba histolytic. These protozoa/ amebae can cause different types
of diseases like malaria, leishmaniasis, toxoplasmosis, giardiasis, amebiasis,
trypanosomiasis etc. So, the drugs used for treatment of these diseases are
known as ant amebic/antiprotozoal drugs.

Anti-amebic Drugs:
Metronidazole\Nitazoxanide
Tinidazole
 Diloxanide furoate
Secnidazole
Bismuth subsalicylate etc.
METRONIDAZOLE:

MOA:
Metronidazole has a nitrogen group which bind with proteins of
microorganisms (ameba's) and also with its DNA resulting in death of
ameba's.

Uses:
Diarrhea, tetanus, sexually transmitted diseases, Dental infections, Bacterial
vaginosis, and Gingivitis.

ADVERSE EFFECTS:
Headache, depression, rashes, nausea, dry mouth, vomiting, Ataria.

TINDIDAZOLE:
It is a second generation nitroimidazole. Tinidazole is similar to
metronidazole in spectrum of activity.

ANTITUSSIVE:

Overview:
Antitussive are the drugs that suppress coughing by acting on cough center
located in the brain. They are typically used to treat dry cough caused by
allergies, respiratory illness or infections.

Cough is an important defense mechanism of the respiratory system in

response to irritants and is a common reason for patients to seek medical
care. But troublesome cough show different sign and symptoms like cold,
sinusitis etc. so then it needs treatment with identification its causes. So that
its treatment is done appropriately. Generally cough is of two types

a. Productive
b. Non productive
Antitussive Drugs:
The drugs used for nonproductive cough are called antitussive drugs. It
includes the following types of drugs.

Codeine, pholcodine, benzonatate, noscapine, dextromethorphan and some

antihistamines. E.g. diphenhydramine

Mode of action:
Antitussive suppress cough by decreasing the sensitivity of cough receptors
located in the brain.

Uses:
Almost used for dry cough

ADVERSE EFFECTS:
Headaches,

tinnitus,

sedation

nausea, vomiting.

Expectorants (Mucokinetics)
These are the drugs that increase bronchial secretion or reduce its viscosity
and facilitates its removal by coughing simply they enhance the clearance of
mucus. They are used against productive cough (cough with sputum).

Expectorants include codides, chlorides, bicarbonates, acetates,volatile oils

etc.

MUCOLYTICS:
These drugs reduce the viscosity of sputum so that sputum comes out easily
with less effort and thus causing clearance of respiratory airways from
sputum. It includes Bromhexine, Acetylcysteine and carbocisteino etc.

Uses:
For productive cough
 bronchodialation
Adverse Effects:
Bronchospasm,
Nausea, vomiting.
Anti-Asthmatic Drug:

Overview:
Bronchial Asthma is a disease in which impairment of airflow occur due to
contraction of bronchial smooth muscle there is inflammation and
hyperresponsiveness of airways in asthma. Asthma may be acute or chronic.

Classification of Anti asthmatic drug:

1) Bronchodilators (Salbutamol, Terbutaline, Theophylline etc.)
2) Leukotriene receptor antagonists (montelukast, zileuton, zafirlukast)
3) Mast cell stabilizer (ketotifen, sodium cromoglycate)
Bronchodilators:
These are the drugs that cause relaxation of the bronchial muscles of lungs.
So when these muscles are relaxed, they makes the airways larger as a result
air passes through lungs easily.

CLASSIFICATION;
1) Sympathomimetic which includes short acting and long acting.

a) short acting beta 2 agonists. E.g., salbutamol, terbutaline.

b) long acting beta 2 agonists. E.g., salmeterol, formoterol.

2) Anticholinergic: (Ipratropium bromide)

3) Methylxanthines: (Theophylline, aminophylline, doxofylline)

SALBUTAMIL.SYMPATHOMIMETICS:

MOA
Salbutamol relaxes the smooth muscles of all airways i.e. from trachea to
terminal bronchioles by binding to beta 2 receptors in lungs.
Uses:
Acute asthma, chronic asthma, COPD, hyperkalemia etc.

Adverse Effects:
Hypokalemia, tachycardia, fear, tremors etc.

Methylxanthines:

MOA:
Drugs like theophylline, aminophylli9ne inhibit phosphodiesterase's which in
result prevent degradation of CAMP, thus causing bronchodilation.

Uses:
COPD, Asthma

Adverse Effects:
Headache, hypotension, tachycardia, anxiety.

Anticholinergics/Ipratropium bromide:

MOA:
Ipratropium selectively block the effects of acetylcholine in bronchial
smooth muscles and cause bronchodilation.

Drug Receptors:
These are the specialized proteins that are located on the surface of cell
mostly. The drug substance interact with these receptors and produce
pharmacological effects.
Types of drug receptors with agonist and antagonist:

1) Adrenergic receptors:
These receptors are activated by adrenaline (agonist) they are sub
classified into alpha receptors and which includes (alpha1 and alpha 2)
beta receptors (b) which include B1 and B2 Antagonists of adrenergic
receptors are phenoxybenzamine, atenolol, propranolol.
2) Cholinergic Receptors:
These receptors are activated by acetylcholine. Cholinergic receptors
consists of muscarinic receptors and nicotinic receptors. Its antagonists
include atropine, scopolamine.

3) Histaminergic Receptors:
They are activated by histamine (agonist). They consist of H1, H2 H3, H4
and H5 receptors. Antagonists of these receptors include pheniramine,
chlorpheniramine, Cetirizine etc.

4) Dopaminergic receptors:
These receptors are activated by dopamine (agonists). They include D1,
D2, D3 and D4 receptors.

Antagonists of dopamine receptors include domperidone,

metoclopramide.

5) Serotonergic receptors:
These receptors are activated by serotonin. It consists of 5HT1, 5HT2,
5HT3, 5HT4, 5HT5, 5HT6, 5HT7 receptors.

Antagonist of serotonergic receptors are ondansetron, granisetron.

6) Prostaglandin receptors:
They are called PG receptors. They are synthesized in the body. Its
antagonist is paracetamol, diclofenac, aspirin etc.

7) Angiotensin receptors:
They are stimulated by the agonist angiotensin II. Its antagonist includes
losartan, valsartan, telmisartan etc.

8) OPIOD receptors:
Its agonist is morphine, codeine, noscapine etc. its antagonist is Naloxone,
Naltrexone.
GABA receptors:
Its agonist is gamma aminobutyric acid. Its antagonist is Anxiolytic and
barbiturates.

Antihypertensives:

Overview:
Hypertension:

Hypertension occurs when systolic blood pressure exceeds 130 mmHg or

diastolic blood pressure exceeds 80mm Hg. Hypertension is a common
disorder found in adults. Chronic hypertension can lead to heart disease and
stroke due to which death can occur.

So the drugs used to treat hypertension are called antihypertensive drugs.

Diuretics:
Diuretics may be of the following types:

a) Thiazide diuretics e.g., hydrochlorothiazide, chlorthalidone.

b) Loop diuretics e.g. Furosemide, torsemide, bumetanide
c) Potassium Sparing diuretics e.g. Amiloride, triamterene,
spironolactone.

MOA of Diuretics:
All types of diuretics decrease blood volume due to removal of water and
salts from body in urination process results blood pressure become
normalize.

ACE inhibitors (Angiotensin Converting Enzyme inhibitors)

It includes

Benazepril,

Enalapril,

Captopril,
Lisinopril,

Ramipril etc.

MOA:
ACE inhibitors lower B.P by reducing peripheral vascular resiztance without
increasing Heart rate.

These drugs block ACE which convert Angiotensin I to angiotensin II

because Angiotensin II is a vasoconstrictor and cause raise in B.P.

USES/ INDICATIONS
Hypertension, Heart failure, Migraine, coronary artery disease.

CONTRAINDICATIONS:

Hyper kalemia ,pregnancy, Angioedema, renal artery stenosis

;
ADVERSE EFFECTS Hypotension Altered taste, skin rash, dry cough etc.

Beta Blockers:
It includes Atenolol, propranolol, nebivolol, labetalol, nadolol, Esmolol.

B.blockers are used by hypertensive patient with heart failure.

MOA:
Beta blockers decreases the sympathetic stimulation of heart, resulting in
decrease heart rate & arterial pressure.

OR
The beta blockers reduce blood pressure primarily by decreasing cardiac
output they block the effect of hormone epinephrine also known as
adrenaline .

SELECTIVE & NON SELECTIVE BETA

BLOKERS;
Non selective beta blockers act on both beta1, & Beta 2 receptors e.g
propanolol, Nadolol, carvedilol

While selective beta blokers act selectively on Beta1, receptors e.g Atenolol,
Metoprolol, Nebivolol etc.

Selective Beta blockers are safe for asthamatic patients.

INDICATIONS :
Hypertension, Heart diseases, glaucoma, migraine prophylaxis;

CONTRAINDICATIONS:

Diabetes mellitus, COPD, peripheral vascular diseases

ADVERSE EFFECTS:

Sexual dysfunction, insomnia, Fatigue, Bradycardia, Hypotension.

Alpha blockers:
It includes

Prazosin,

Doxazosin,

Terazosin.
MOA:

They decrease peripheral vascular resistance and lower arterial blood

pressure by causing relaxation of both arterial and venous smooth muscle.

Calcium Channel Blockers:

It includes

Amlodipine, Nifedipine, Verapamil, clevidipine, Nicardipine.

MOA:
CALCIUM channel blockers block the inward movment of calcium by
binding to calcium channels in the heart and in smooth muscle of coronary
and peripheral artery.

This cause vascular smooth muscle to relax and dialate arteroils thus
normalize B.P

INDICATIONS:

Angina , hypertension, atrial fibrillation.

CONTRAINDICATIONS:

Aortic stenosis,hypersensitivity,platlet dysfunction

ADVERSE EFFECTS:

Constipation, dizziness headache, Fatigue , Hypotension etc

Angiotensin II Receptors blockers:

It includes Losartan, Telmisartan, Valsartan, Candesartan, Eprosartan.

MOA:
These agents produce the same effect as that of ACE inhibitors. They cause
arteriolar and venous dialation thus decrease salt and water retention in
body and normalize the B.P.

ANTI MYCO BACTERIAL DRUGS

OVER VIEW:
Mycobacteria are rod shaped aerobic bacilli that multiply slowly their cell
wall contain mycolic acids

These bacteria can cause tuberculosis (TB)

TB is leading infections cause of death worldwide

TB treatment include 1st line & second line drugs.

Second line drugs are typically less effective, more toxic and less
extensively studied. They are used for the patient who cannot tolerate the
first line drugs or infected due to resistant TB.

1st line drugs

Ethambutol

Isoniazid

Pyrazinamide

Rifampin

2nd line include

Aminoglycoside

Macrolides

Fluoroquinolone etc

ISONIAZID:
Isoniazid are administered with rifampin .

MOA;
Isoniazid are cell well synthesis inhibitors.
They inhibit cell wall synthesis of mycobacterium by inhibiting mycolic acid
formation.

ADVERSE EFFECTS

Hepatitis is most serious adverse effect of isoniazid, rashes, fever &

neuropathy are also its adverse effects.

RIFAMPIN (Rifampicin)

It has broader anti microbial activity than isoniazid.

MOA

Rifampin blocks RNA transcription by interacting with B subunit of

mycobacterial DNA dependent RNA polymerase.

ADVERSE EFFECTS:

Nausea , vomiting, rashers, fever, chills ,renal failure

ETHAMBUTOL :
It is a bacteriostatic & specific for mycobacteria.

MOA;
It inhibits the enzyme arabinosyl transferase which is important for synthesis
of the mycobacterial cell wall.

ADVERSE EFFECTS:
Optic neuritis with blurred vision red green color blindness,abdominal
pain,allergic rashes

PYRAZINAMIDE:
MOA:
Its MOA is unclear but it inhibits the synthesis of fatty acids by changes in
enzymes which disrupts cell membrane and disable energy production for
mycobacteria. and is effective in treating TB

USES:
TB, Acute leukemia,

ADVERSE EFFECTS:

Liver demage

GIT upset i.e nausea vomiting

Gout
 ANTI FUNGAL DRUGS

OVERVIEW.
Infectious diseases caused by fungi are called mycoses, & they are often
chronic in nature-.mycotic infection may involve only the skin cutaneous,
subcutaneous or systemic infections .

Cell wall of fungi is make up of chitin-

DRUGS FOR SUBCUTANEOUS AND SYSTEMIC MYCOSES

Amphotericin B

Flucytosine

Fluconazole

Ketoconazole

itraconazole etc

DRUGS FOR CUTANEOUS MYCOSES;

Clotrimazole

Butoconazole

Nystatin

Econazole

Miconazole etc
AMPHOTERICIN B:
It is a naturally occurring polyene antifungal drug. It is the drug of choice for
the treatment of several life threatening mycoses.

MOA:
Amphotericin B binds with ergosterol in the plasma membrane of fungal
cells therefore it forms pores in the cells of fungi as a result loss of
electrolytes occur through these pores from fungi thus cell death occur.

ANTIFUNGAL SPECTRUM OF AMPHOTERICIN B:

It is effective against a wide range of fungi including candida albicans,
histoplasma capsulatum ,Cryptococcus neoformans, blastomyces
dermatitidis

ADVERSE EFFECTS:

Fever and chills ,Renal impairment, hypotension,

thrombophlebitis .

FLUCYTOSINE:

MOA.

Flucytosine enters the fungal the fungal cell via a cytosine specific permease
enzyme and disrupt nucleic acid and protein synthesis

ADVERSE EFFECTS :
Reversible neutropenia, thrombocytopenia, Bone marrow depression ,
Hepatic dysfunction, Nausea, vomiting diarrhea.

AZOLE ANTIFUNGALS:
Azole antifungals are made up of 2 classes of drugs i.e imidazale and
triazoles.

Both have similar mechanism of actions. In general imidazoles are applied

topically and triazoles are administered systemically

Generally It include fluconazole, itraconazole, posconazole voriconazole,

clotrimazole, ketoconazole, miconazole etc.

MOA.

Azole are fungistatic.They inhibit 14-alpha demethylase enzyme which in

turn inhibit ergosterol biosynthesis as a result fungal membrane disrupts
thus inhibition of fungal cell growth occur .

ADVERSE EFFECTS;
Nausea , vomitting , diarrhea, hypokalemia, edema, hypertension, etc

NYSTATIN

MOA:
Nystatin binds to ergosterol, a major component of fungal cell membrane
and there it forms pores .

These pores allow electrolytes and small molecules to leak out of fungal cell ,
Thus causing cell death of fungi.

USES:
Candidiasis, oral fungal infections, vaginal infections.

ADVERSE EFFECTS:
Acute over dosage of nystatin Cause nephrotoxicity, vomiting, diarrhea, skin
irritation, Rashes, etc.
 ANTI INFLAMATORY DRUGS
Those drugs which are used for relieving inflammation are called
anti-inflammatory drugs e.g NSAIDS, STEROIDS
PARACETEMOL:

MOA.

It attacks on CNS and there inhibit the synthesis of inflammatory mediators

called prostaglandin (PG)

USES;
headache , muscle pain, joint pain Antipyretic

ADVERSE EFFECTS:
Skin rashes, nausea , vomiting, kidney damage etc

NSAIDS. (non steroidal anti inflammatory drugs)

NSAIDS are a group of chemically dissimilar agents that differ from one
another in their antipyretic,analgesic and anti inflanatory action .They relieve
pain without inducing sleep. NSAIDS may be selective or non selective.

NON SELECTIVE (COX 1 AND COX 2 INHIBITORS)

Aspirin

Diclofenac sodium

Flurbiprofen

Ibuprofen

naproxen

Piroxicam

Mefanamic Acid

Aceclofenac

Indomethacin
SELECTIVE NSAIDS (COX 2 INHIBITORS)

Meloxicam

Celocoxib

Etoricoxib

Nimesolide

MOA OF NSAID
Aspirin irreversibly inactivates cox while the other NSAID are reversible
inhibitors of cox enzymes.

So when Cox (cyclooxygenase) is blocked then as a result synthesis of

prostaglandin (PG) is inhibited thus relieving inflammation,pain or fever.

USES:
Fever , headache, joint pain, toothace muscle pain, heart disease etc.

ADVERSE EFFECTS;
Allergy ,nausea ,vomiting ,liver demage, peptic ulcer, abdominal pain etc

STEROIDS
Kidney has a type of gland called adrenal gland .Adrenal gland has two
portion (1) ADRENAL CORTEX (2) ADRENAL MEDULLA

The adrenal cortex release steroids called glucocorticods and mineralo

corticoids.

Glucocorticoids acts on glucose while mineralo corticoids act on minerals .

Gluco corticoids may be natural or synthetic .

Natural glucocorticoids are synthesized inside the body while synthetic are
prepared in lab and are called steroids

CLASSIFICATION OF GLUCOCORTICARTICOIDS STEROIDS;

(1)Short acting: cortisone, hydrocartisone
(2)Intermediate acting: predinisolone
(3)Long acting : dexa methasone ,betamethasone, beclomethasone

MOA:
They enter the cell and bind with glucocorticoid receptors making
complex and regulates transcription of DNA thus acting as an immuno
suppresive .

USES:
Allergy to drugs, Asthma, rheumatoid arthritis, Addison disease,insect
bites,itching,collagen diseases,sunburn etc

ADVERSE EFFECTS:
Cataracts, osteoporosis, hypertension, abdominal pain, nausea,
vommiting, Diarrhea etc.

AUTOCOIDS:
They are biologically active substances produced by wide variety of cell in
body

They generally act at the local site of synthesis and release. They are
called local hormones .They involved in a number of physiological &
pathological processes.

e.g Histamine, serotonin etc.

HISTAMINE AND ANTI HISTAMINE:

Over view:

Histamine
Histamine is derived from greek word “Histos” which means “tissue”
Histamine is present in almost all mamallian tissues, some wasps and
bee venoms and also in some of plants. Tissue which are rich in
histamines are lungs,liver GIT, Placenta and skin.

FUNCTION:
It function as a neurotransmitter as well as neuro modulator.

It also regulate gastric acid secreations in stomach.

HISTAMINERGIC RECEPTORS:

There are different types of histamine receptors which are present in

different tissues of the living body they are H1, H2, H3, H4 receptors .

Release of histamines:

When histamine are released so it bind to its specific histaminergic

receptor and when activated so it produce the following effects.

Itching, rashes ,redness of skin, hypotension due to vasodialation,

bronchospasm .

ANTI HISTAMINES
These are the drugs which block the effects of histamine competitively by
occupying the histamine receptors.

CLASSIFICTION OF ANTI HISTAMINES

Histamine may be
1st generation
It cause drowsiness in most people .

It include diphenhydramine, promethazine, chlorphenaramine phenaramine,

meclazine, cyproheptadine etc.

2nd generation
It causes less drowsiness as comparatively to 1st generation anti histamines.
It include cetrizine ,levocetrizine, loratidine, deslortadine etc.

3rd generation

These anti histamines are basically non sedative. It includes fexofinadine.

MOA
The primary mechanism of anti-histamine actions is that they block the
action of H1 receptor at target tissue however they may also cause inhibition
of H2 , H3, H4, RECEPTORS.

Therapeutic uses of Anti histamines

Allergic conditions, inflammatory conditions, nausea, motion sickness,
insomnia.

ADVERSE EFFECTS;
Increased appetite, Dry mouth, vertigo, hypotension, Drowsiness, urinary
retention, GI upset.

SEROTONIN
Serotonin is a neuro transmitter .
It plays a role in vasoconstriction ,inhibition of gastric secretion and
stimulation of smooth muscle contraction.

In brain it affect mood, appetite, body temperature regulation and sleep.

LOCATION
serotonin is largely present in GIT .

It is also present in raphe nuclei of brain stem.

STORAGE AND RELEASE

It is stored in vesicles and is released by exocytosis of the vesicles in
response to an action potential.

MOA
serotonin has seven families . Most of these are G protein coupled
receptors . In CNS it may cause a reduction in appetite and in GIT it Cause
emesis when activated .

USES
Selective serotonin agonists has many clinical uses. E.g in treatment of
anxiety and depression .Also it may be used in management of migraine and
obesity.

ADVERSE EFFECTS
Muscle rigidity, fever seizures, diarrhea, shivering etc.

OTHER AUTO COIDS

Amines: e.g Histamine, serotonin

Peptides: e.g Angiotensin, Bradykinin
Lipids: e.g prostaglandins, leukotrienes
 ANXIOLYTICS& HYPNOTICS
OVERVIEW

Anxiety
Anxiety is a mental disorders .It is an unpleasant state of tension, depression
or a fear that arises from a known or unknown source. Mild anxiety donot
require anti anxiety drugs. However severe chronic anxiety may be treated
with antianxiety drugs (anxiolytics) and some form of psychotherapy.

Anxiolytics contains huge classes of drugs most commonly used to treat or

manage various mental disorders. Anxiolytics are mainly used for

*sedation/sedative

*Hypnosis

SEDATIVE

They are the drugs most commonly used to produce cool and calm
condition. Such drugs are known as sedatives while the
phenomena related to cool and calm condition is known as
sedation. It does not induce the normal sleep.

Example. Alprazolam 0.25 mg is used as a sedative because 0.25

mg Alprazolam has the ability to cause membrane polarization.

Hypnotics
Hypnotics are the drugs, which have the ability to induce sleep, and that
sleep should be considered like a normal sleep.

Example. 1mg Alprazolam is to be used as hypnotics.

While using the drugs for sedation or hypnosis we have mainly two classes
of drugs. i.e

*Benzodiazapines

*Barbiturates

BARABITURATES;

Barbiturates contain different types of drugs that were initially used

commonly as sedative or hypnotics. But in present situations barbiturates
are replaced by benzodiazepines. Still they can be used as a drug of choice
i.e in case of Anesthesia .

Barbiturates are largely replaced by benzodiazepines because barbiturates

induce drug tolerance,drug addiction, physical dependence and may also
cause death in over doses. All barbiturates are controlled Substances
Barbiturates include Amobarbital, pentobarbital , Phenobarbital etc.

Mechanism of Action
Barbiturates act on GABA receptor which in turn prolong the duration of
chloride channel opening. They decrease neuronal activity.Barbiturates binds
to GABA receptors site other than benzodiazepines binding site.

Therapeutic uses:

Anesthesia, anticonvulsant, sedative, hypnotics ,Anxiety etc

ADVERSE EFFECTS:

Nausea, vomiting, Seizures, Cardiac arrest, weakness and death in over

doses.

BENZODIAZAPINES:
They contain huge drugs substance commonly used for
Anxiety hypnosis, sedation muscles relaxant, epileptic
conditions etc.
Benzodiazepines are most commonly used instead of barbiturates due to
their safety without inducing addiction, tolerance , habituation and
dependence of drugs

Benzodiazapines drugs:

Alprazolam, clonazepam, Diazepam, midazolam, temazepam, clorazepate,

Flurazepam, oxazepam

Machanism of action:
Benzodiazepines binds to GABA receptors at their specific sites and
modulate GABA effect thus decreases neuro transmission and causes hyper
polarization due to increase influx of chloride ions across the membrane.

:
NOTE when chloride channels are open then chloride ions enter across the
membrane which cause hyper polarization and decrease nervous
transmission.

Therapeutic uses :
Anxiety ,Sedative, hypnotics muscle relaxant , Anticonvulsant, sleep
disorders, Amnesia , Seizures.

ADVERSE EFFECTS :
Confusion, Drowsiness, Ataxia, memory problems, dizziness.

ANTAGONIST: Benzodiazepine antagonist is Flumazenil.

 ANALGESICS:
There are the drugs which relieve pain .They are further divided into Narcotic
analgesics and Non narcotic analgesic,

Narcotic analgesic relieve pain and also induce sleep e.g opioids

Non narcotic analgesic relieve pain but donot induce sleep e.g paracetemol,
NSAID.

OPIOIDS.
Opioids are natural semi synthetic or synthetic Compounds that produce
morphine like effects. They are basically stong analgesic

OPIOID CLASSIFICATION

It includes
(a) Analgesics: I.e morphine, Nalbuphene, Methadone, meperidine,
pentazocine, Tramadol, Tapentadol etc.Fentanyl,
(b) Anti-diarrheal: i.e coperamide, codeine
(c) Anti tussive: Pholcodine Dextromethorphan.

MECHANISM OF ACTION OF OPIODS:

Opioids drugs binds with opioids receptors (that are MU Kappa, sigma
and delta receptors) so as a result opioids inhibit release of many
excitatory transmitters which carry painful stimuli- Thus relieving the pain.

USES:

For relieving different types of pain, diarrhea, cough, sedation, Anxiety .

ADVERSE EFFECTS :
Sedation, Nausea, vomiting, constipation, Hypotension, Respiratory
depression. Dependence, Tolerance etc.

OPIOIDS ANTAGONIST:

Nalaxone: It is an opioids antagonist. It is used in Case of over dose of

opioids to reverse the toxicity of opioids.
 ANTI PSYCHOTIC DRUGS:

Over view of psychosis:

Psychosis is a condition that affects the way your brain processes

information. During this condition a person might see, hear, or believe
things that are not real.

So anti Psychotic are those drugs which are used to treat the symptons
of psychosis.

Anti psychotic drugs are primarily used to treat schizophrenia.

Schizophrenia is a type of chronic psychosis characterized by delusions,

hallucinations (in form of voices) and disturbances in thought

CLASSIFICATION OF ANTI PSYCHOTIC DRUGS :

They are divided into first and second generation agents.

First generation anti psychotics:

Chlorpromazine , thioridazine, Haloperidol, loxapine , thiothixene,
Pimozide.

Second generation anti psychotics:

Resperidone, Clozapine, Asenapine, olanzapine, paliperidone.

Mechanism of Action:

All the first and second generation anti-psychotic drugs block <D2>
dopamine receptors in the brain and periphery .

While most of second generation drugs also inhibit serotonin receptor .

USES:

Schizophrenia, prevention of nausea and vomiting, bipolar

disorders etc

ADVERSE EFFECTS:

Dry month, sexual dysfunction, sedation, seizure, weight gain, urinary

retention.

HALLUCINOGENS:(psychomimetics)
A psychoactive agent which cause hallucination or psychosis induction
are called Hallucinogens.

Hallucinogens are also called as psychomimetics because of enhancing

the psychosis like behavior.

It contain all the drugs of abuse these drugs cause psychological

dependence and tolerance of drugs by continuous use.

Many of these alter the state of visions of bright, colorful changes in

environment and changing shapes Constantly.

CLASSIFICATION
LSD (lysergic acid diethylamide)

Tetra hydro cannabinol (from marijuana)

(a)LSD (LYSERGIC acid diethyl amide)

First created from ergot by Hoffman .It is the most potent Hallucinogenic
agent. Aside from very colorful hallucinations, the drug is also responsible
for mood alterations, sleep disturbances and anxiety.

Mode of Action:
LSD is a 5HT2 receptor against

USES:

Anxiety, Depression, addiction, Psychosomatic diseases.

ADVERSE EFFECTS :
Mydraisis, Tachycardia, Hypertension, Dizziness, sweating, loss of
appetite .

(b) MARIJUANA:
marijuana is obtained from cannabis sativa plant. It is the most
frequently used illicit (illegal) drug.For marijuana special receptors
are present in brian i.e cannabinoid receptors. When these
receptors are activated by marijuana so it produce relaxation,
increase appetite, increase heart rate, decrease muscle
coordination, conjunctivitis.
 ANTIDEPRESSANTS:

Overview:
Depression is the symptoms of feelings of sadness and hopelessness, as
well as the inability to experience pleasure in usual activities, changes in
sleep patterns and appetite loss of energy , and suicidal thoughts.

ANTI DEPRESSANTS drugs classification:

The drugs used to treat depression are called anti-depressants.

Anti depressants include

(1) Selective serotonin Reuptake inhibitors(SSRIs)

It contains
citalopram,escitalopram,fluoxetine, paroxetine, sertraline,
Fluvoxamine.

(2) Serotonin NOR EPINEPHRINE Reuptake inhibitors

(SNRIs)
It contain (Duloxetine, Venalfaxine, Desvenlafaxine,)
 (3) ATYPICAL Anti depressants
(BUPROPION Mirtazapine, Trazodone, nefazodone, vortioxetine)

(4) TRICYCLIC Anti depressants

(Imipramine, Amoxapine, Doxepin, Nortriptyline,)

(5) MONOAMINE OXIDASE inhibitors (MAOIs)

(Selegiline, phenelzine, isocarboxazid, Tranylcypromine)
Mechanism of Action of Antidepressants:
The antidepressants inhibit revptake of neurotransmitters through selective
receptors therefore increasing the concentration of specific neuro
transmitter around the nerves in the brain.

MOA of SSRIs:
SSRIs block the reabsorption (reuptake) of serotonin into neurons and
increase serotonin activity .

MOA of SNRIs:

SNRIs affect the neuro transmitters used to communicate between brain

cells.

MOA of MAOIs:

They inhibit the activity of monoamine oxidase, thus preventing the break
down of monoamine neurotransmitters and also increase their availability.

USES of antidepressants:
Panic disorder, depression, migraine, insomnia, bulimia, obsessive
Compulsive disorder.

ADVERSE EFFECTS:
Sexual dysfunction, Anxiety, Nausea, Drowsiness, Dry mouth, Blurred vision
etc.

EPILEPSY AND ANTIEPILEPTIC DRUGS

Overview:
Epilepsy is a neurological condition that causes unprovoked, recurrent
Seizures. Seizure is a sudden rush of abnormal electrical activity in brain .

During epileptic conditions a patient may have tremors (shaking

movements), or jerking movements that can’t be controlled by patient
himself/herself.

Anti Epeliptic drugs:

The drugs used for the treatment of epilepsy are called anti-epileptic drugs.

Some of antiepileptic drugs are listed below

Corbamazepine, clobazam, Clonazepam, Diazepam, pregablin, Gabapentin,

Ethosuxamide, phenytoin, Primidone, Brivaracetam, Valproic acid and
divalproex.
CARBAMAZEPINE:

Mechanism of action:

It blocks sodium channel thus inhibiting the generation of repetitive action

potential (electrical activity) in the epileptic focus and preventing their
spread.

Uses:
Focal Seizure, trigeminal neuralgia, Bipolar disorder, partial Seizures etc.

ADVERSE EFFECTS:

Osteoporosis, Rashes, Ataxia, Sedation, Nausea, Vomiting etc.

PREGABLIN:
Pregablin is being used as anticonvulsant, analgesic, anxiolytic and
antiepileptic drug.

MECHANISM OF ACTION:
Pregablin reduce excitatory neurotransmitter release by binding to (alpha2)
of voltage gated calcium channels in the CNS.

USES:
Seizures, Diabetic peripheral neuropathy, postherpetic neuralgia and
fibromyalgia

VALPROIC ACID AND DIVALPROEX:

MOA :

It acts on GABA levels in the CNS also block voltage gated ion channel. Thus
show activity against epilepsies.

PHENYTOIN

MOA

Phenytoin acts by stabilizing neuronal membrane and prevent spread of

seizures discharges.it delay recovery of sodium channels and inhibit high
frequency firing.

ADVERSE EFFECTS

Hypocalcaemia,osteomalacia,anemia,hyperglycemia etc.

ANESTHETICS
Overview:
Anesthesia is a state of Controlled , temporary loss of Sensation or
awareness that is induced for medical purposes.Anesthesia is a way to
control pain during a surgery or procedure by using medicines called
anesthetics. Anesthetics create

Sedation and reduced anxiety

Lack of awareness and amnesia
 Skeletal muscle relaxation
Suppression of undesirable reflexes
Analgesia

STAGES OF GENERAL ANESTHESIA :

General anesthesia is a reversible state of CNS depression , causing loss of
response to and perception of stimuli .General anesthesia has three stages

*INDUCTION
*MANITENANCE

*RECOVERY

INDUCTION is time from administration of a potent anesthetic to

development of unconsciousness

Maintenance is the Sustained period of general anesthesia

Recovery starts with the discontinuation of anesthetic until conscious state

is returned .

CLASSIFICTION OF ANESTHETICS.

(1)Preoperative medications:

*Analgesics *Antacids *Antiemetic’s *Benzodiazepines

(2) Analgesics:

*Acetaminophen *Celecoxib * Gabapentin *Ketamine *Opioids.

(3) General anesthetics(INHALED )

*Desflurane *Isofluane *Sevoflurane *Nitrous oxide

(4) General anesthetics(I.V)

*Dexamedetomidine *Etomidate *Propofol *Methohexital.

(5)Local Anesthitics (Amides)

*Lidocane *Ropivacaine *Mepivacaine

(6) Neuro muscular Blockers:

*Succinylcholine, *Vecuronium.

Mechanism of action of General anesthetics:

General anesthetics increase the Sensitinty of the (GABAa) receptors to

the inhibitory to the inhibitory neurotransmitter GABA.

This increase chloride ion influx and cause hyperpolarization of neurons

and diminish CNS activity.

ANTIMICROBIAL Therapy
An Antimicrobial therapy kills or inhibits the growth of microorganisms
Such as bacteria, fungi, or protozoans. Therapies and those therapies that
only inhibit the growth of microbes are called micro biostatic therapies.

CLASSIFICATION of Anti bacterial drugs:

(1) INHIBITION OF cell wall synthesis

penicillin’s, cephalosporin’s.
 (2) INHIBITION OF Nucleic acid (DNA/RNA) synthesis:
Sulphonamides, quinolones, Azoles

(3) INHIBITION OF protein synthesis:

(Aminoglycosicles, Tetracycline’s, macrolides, chloramphenicol)

CELL WALL synthesis INHIBITIORS:

Those drugs which inhibit cell wall synthesis of some microbes are called
cell wall Inhibitors.

CELL wall inhibitors classification:

(a) Penicillin’s:
Amoxicillin, Ampicillin, Nafcillin,, oxacillin, Pencillin G etc.

MOA:
Penicillin compete for the binding to enzymes called penicillin binding
proteins (PBPs) due to which last step of bacterial cell wall synthesis is
catalyzed and thus cell death of bacteria occurs.

USES:

RTI e.g pneumonia, pharyngitis, Tonsillitis, otitis media, UTI, Typhoid fever,
sexually transmitted diseases, Diphtheria

Dose:

Amoxicillin 500 my (TDS).

(B) CEPHACOSPORINS:

cephalosporin’s contains the following types of drugs.

(1) Ist generation:

Cephalexin, cephradine, cefadroxil

(2) 2nd generation:

Cefprozil, cefuroxime, cefaclor
(3) 3rd generation:
ceftriaxone, cefotaxime, Cefpodoxime, Cefixime, cefdinir,
ceftizidime.
(4) 4th generation :
Cefipime, Cefpirome
(5) Advanced generation:
ceftaroline

MOA OF CEPHALOSPORIN:
Cephalosporin’s inhibit/block the synthesis of cell wall of bacteria and
cause bacterial death by binding with cephalosporin binding protein
(CBP)

USES:
RTI, (Pneumonia, tonsillitis, pharyngitis)

Otitis media, otitis externa, UTI, Typhoid sexually transmitted diseases , skin
infection,

ADVERSE EFFECTS:
 Anaphylactic shock, rashes, Diarrhea, nausea, vomiting oral
candidiasis.

Dose:
Cephradine = 500mg Cop TDS

Cefixime=400mg Cap OD

Inj cefotaxime= BD

Inj ceftraixone 1gm= OD/BD

FLORO QUINOLONES:
This class of antibiotic include the following types of drugs .

Ciprofloxacin
Levofloxacin
Moxifloxacin
Ofloxacin
Norfloxacin
Gatifloxacin

MOA:

Floroquinolones when reach to the target site so there it blocks DNA

synthesis By blocking DNA gyrase enzymes and cause permanent
chromosomal breaks thus Causing cell death of bacteria.
USES:
UTI (pylonephritis, cystitis, urethritis,)

Prostatitis, Typhoid, RTI, Ear infection,

Adverse EFFECTS:

Headache, Insomnia, Seizures, nausea, vomiting etc.

Dose

Ciprofloxacin= 500mg tab OD/BD

Levofloxacin = 250mgBD or 500 mg OD

Moxifloxacin= 400 mg OD

AMINOGLYCOSIDES:

It includes

*Amikacin,

*Gentamicin,

*Neomycin,

*Streptomycin,

*Tobramycin.

MOA:
Aminoglycosides kills bacteria by inhibiting protein synthesis by binding with
ribosomes 30s sub unit.
USES :
Skin infection, burns or wounds, UTI, Pneumonia, Sepsis, ear infections etc.

ADVERSE EFFECTS:

Nausea, Vomitting, muscle paralysis, ototoxicity, vertigo, etc.

MACROLIDES/KETOLIDES:

Macrolides includes

*Azithromycin

*clarithromycin

*Erythromycin

*Telithromycin

MOA :
Macrolides are also protein synthesis inhibitors. They bind with ribosome
50s sub unit and inhibit protein synthesis-Thus causing bacterial cell death.

USES:
RTI, Ear infections,Pertusis, Diptheria, Tonsillitis, sexually transmitted
diseases. Skin infections especially Acne.

Adverse effects:

Nausea, vomiting Diarrhea, Hepatitis.

DOSE:

Erythromycin 500mg BD/TDS

Azithromycin 500mg

SULFONAMIDE:

Sulfonamides include

*sulfadoxin

*Sulfamethoxazole

*sulfaacetamide

*Sulfasalazin

MOA:

sulfonamides compete with PABA (precursor molecule of dihydricfolic acid

for bacteria) to inhibit dihydric folic acid as a result DNA synthesis is
inhibited for bacteria.

USES:
RTI, UTI, Typhoid, malaria, Rheumatoid arthritis,etc

ADVERSE EFFECTS :
Hemolytic anemia, Nausea, vomiting,Diarrhea, kidney damages, Allergy
TETRA CYCLINES:
It include, Doxycyclines, tetracycline, Minocycline, Demeclocycline.

MOA:
Tetracyclines binds with 30s subunit of the bacterial ribosome. As a result it
inhibit bacterial protein synthesis.

USES:

RTI, ACNE, Cholera, Eye infections, sexually transmitted disease.

ADVERSE EFFECTS:
Kidney damage, Nausea, vomiting, Diarrhea, Liver damage, Allergy.

Dose:

Doxycycline 100mg Cap 2Cap stat and after that 1 Cap OD.

CHLORAMPHENICOL:

IT is a broad spectrum antibiotic .

It is effective against gram positive as well as gram negative bacteria.

MOA:

Choloramphenicol binds with 50s ribosomal subunit and inhibits protein

synthesis of bacterial cell .

USES:
Meningitis, Acromegaly, Typhoid, bacterial infections, corneal ulcers,
ADVERSE EFFECTS:

Vision problems, oto toxicity, Hepatitis, Aplastic anemia, Hair growth

depression, Nausea, vomiting Diarrhea, Headache,

CLINDAMYCIN:
IT IS used primarily in the treatment of infections caused by gram positive
bacteria.

MOA:

It binds with 50s ribosomal subunit of bacteria and thus inhibit protein
synthesis in bacteria .

USES:

Acne vulgaris, Bacterial infections Dental infections, Malaria, Bacterial

vaginoses

Adverse effects:

Anaphylactic shock Nausea, Vomitting Rashes, abdominal pain

ANTIVIRAL DRUG:

Overview:
viruses are obligate intracellular parasites .They donot have cell wall or cell
membrane and by self do not carry out metabolic processes. They use much
of the metabolic machinery of the host.

ANTIVIRAL DRUGS:
Amantadine, Ribavirin, Zanamivir, Acyclovir, oseltamivir, Interferons, Adefovir,
stavudine, Abacavir etc.

(1) RIBAVIRIN:
Rbavirin is effective against a broad spectrum of RNA and DNA Viruses.
It is commonly used in hepatitis B.

MOA:
Ribavirin inhibits replication of RNA and DNA viruses by increasing the
mutation frequency in the genomes of several RNA viruses.

NOTE – Ribavirin is contraindicated in pregnancy.

(2) Zanamivir and oseltamivir:

MOA:

Zanamivir and oseltamivir both selectively inhibit neuraminidase , thus

preventing the release of new virons and their spread from cell to cell .

ADVERSE EFFECT:

Nausea, Rashes, Bronchospasm, irritation of respiratory tract.

(3)Acyclovir:
MOA :

It inhibits the action of viral DNA polymerase and DNA replication of

different herpes virus.
USES:
It is used for Herpes viral infection i.e,

Herpes viral encephalitis

Herpes labialis (infection of lips)

Herpes infection of mouth, genital tract, skin

Adverse effects:
Nausea, Vomitting, Bronchospasm Headache, Kidney damage.

(4) INTERFERONS:
They are Synthesized by recombinant DNA technology.

MOA:
Interferons enhance activity of host cell enzymes which are involve in
inhibition of viral RNA.

USES:
Chronic HBV infection, bladder carcinoma, multiple myeloma etc.

Adverse effects:
Nausea, Vomitting, Depression, Fever, headache, muscle pain etc.

(5) AMANTIDINE:

MOA:
It blocks uncoating of the virus within the cell thus preventing
the release of viral RNA into the host cell.

USES:
influenza virus, Parkinson disease.

ADVERSE EFFECTS
Depression, headache, Dry moth Constipation, Urinary retention.

ANTI EMETICS
Overview:
Emesis or vomiting is the reflex action of ejecting the food contents of the
stomach through mouth chemoreceptor trigger Zone is
stimulated/activated directly by a stimuli e.g morphine.

Anti emetic drugs:

Those drugs which are used for treatment/controlling of vomiting or
emesis are called anti emetic drugs.

*Metoclopramide

*Dimenhydrinate

*Domperidone

*ondansetron

*Granisgron

*Cycizine

*Dolasetron

ONDANSETRON, Granisetron, Dolasetron

MOA:
All these drugs are 5-HT3 receptor antagonists.These agents selectively
block 5-HT3 receptors in the periphery and in the chemoreceptor trigger
zone.

USES:
Nausea, Vomitting, Motion sickness,

*MeToclopramide:
MOA:
Metoclopramide inhibit dopamine D2 receptor in the chemoreceptor
trigger Zone of brain thus controlling vomiting .

USES:
Same as that of 5-HT3 receptor antagonists.

Adverse effects:

Diarrhea, hypertension,skin rash,drowsiness etc

Dimenhydrinate/Diphenhydramine/Gravinate

MOA:
It is H1 receptor antagonist. It treat nausea and vomiting by blocking
histamine 1 (H1) receptor in brain.

USES:
vertigo, Nausea, Vomitting , migraine, post surgical conditions, allergy.

Adverse effects:

Dry mouth ,dizziness, Constipation, hypotension.