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MEDICINAL PLANTS

HISTROY

In the early years, there is little written evidence of the use of herbs in medicine as it
was usual to pass on knowledge verbally; as knowledge grew written records began to
emerge. Herbs were of significant importance as they were used not only for medicine
but also in magic and ceremonies. As far back as 3000 B.C., medical treatments are
shown on Babylonian clay tablets, prior to the importation of herbs.

China and The Chinese

One of the oldest records of such medicinal recommendations is found in the


writings of the Chinese scholar-emperor Shen Nung, who lived in 2735 B.C., or 4730
B.P. (before the present). He compiled a book about herbs, a forerunner of the
medieval pharmacopoeias that listed all the then-known medications.

One of the most famous written records of the Chinese use of herbs is the
Canon of Herbs, the result of the knowledge of the emperor Shen Nung who died in
2698 B.C. It is compiled of 252 plant descriptions, including medicinal effects,
growing locations, use and preservation, in fact a blueprint for future pharmacopoeias.

Ayurvedic medicine was practiced in India as far back as 5000 years ago and
one of the oldest known Indian books on plants, Vedas, records the medicinal and
religious use of herbs and plants. The most famous of the ancient Romans writings on
the medicinal use of herbs is recorded by Dioscorides in De Materia Medica,a book
filled with descriptions of hundreds of healing plants. This book was widely
referenced until the seventeenth century.

John Gerard (1545- 1612) was a highly respected English herbalist of the 16th
century; in 1596, he was first credited with publishing records of the plant species
found in his garden, at Holburn, but it is for his later publication in 1597, the Herball,
for which he is most remembered.
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Nicholas Culpeper (1616 – 1654), although educated at Cambridge University


and a practicing physician, choosing to make medicine accessible to the poorer classes
and not just the rich. Nicholas Culpeper's most famous publication was published in
1653 and is referred to as The English Physician or Culpeper's Herbal.

Definition of a Herb

Today, the term 'herb' is more commonly used to describe 'any seed-bearing plant
which does not have a woody stem and dies down to the ground after flowering' or
'any plant with leaves, seeds or flowers used for flavoring, food, medicine or perfume'.

ATROPINE

 Alkaloid Tropane. Extracted from deadly night shade Atropa Belladonna.

Medicinal value

 Anticholinergic drug- Drug that blocks the neurotransmission in central


nervous and peripheral nervous system.
 Competitive antagonist – Administered to reduce the effects mediated by acetyl
choline receptors in neurons through competitive inhibition.

RAUWOLFIA SERPENTINA

Wonder drug in India in 1944 treating high Blood Pressure.

 Alkaloid Reserpine.

Medicinal value

 Antihypertension.

CINCHONA TREE

 Alkaloid Cinchonine
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Medicinal value

 Treatment of Malaria.

HIBISSCUS ROSA (Sembarathi)

 Active constituent aliphatic esters. High vitamin C and anthocyanins.

Medicinal value

 Flowers- Used as emollient (soften or soothen skin), demulcents


( agents wihish soothe irritation) in cough, decoctions of flowers used in
bronchial infections.
 Leaves- Used as emollient, oil made from it increases the growth and
color of hair.

OCIMUM SANCTUM (Tulsi)

 Active constituent MONO TERPENOIDS.

Medicinal value

 Leaves- Used as expectorant, treatment of bronchitis and gastric


disorder. Infusion of leaves used in malaria and hepatic infection, juice of leaves
excellent remedy of skin infections like leprosy, itches.
 All parts of the plant have medicinal value.

PHYLLANTHUS AMARANTHUS (Keezhanelli)

 Active constituent PHYLLANTHIN.

Medicinal value

 Anti-hypertensive
 Anti-hepatotoxic- Act against liver damage
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 Anti-lithic- Act against formation of kidney stones.


 The roots of leaves in powder form can also be used in Jaundice.

SOLANUM TRILOBATUM (Thuduvalai)

Medicinal value

 All parts is used as medicine


 Very useful in Asthama.
 In siddha medicine it is used in all kind of lung diseases.
 Decoction of the plant used in chronic bronchitis.
 Berries and flowers are given in cough.

VINCA ROSIA (Nithyakalyani)

 Active constituent Vinblastin and Vincristine.

Medicinal value

 Antidiabetic
 Treatment of Hodgkin’s disease (Lymphoma-type of cancer originates
from WBC).
 Treatment of Leukemia ( cancer)
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ANTIBIOTICS

In common usage, an antibiotic (from the Ancien Greek: ἀντί – anti, "against", and
βίος – bios, "life") is a substance or compound that kills, or inhibits the growth of,
bacteria. Antibiotics belong to the broader group of antimicrobial compounds, used to
treat infections caused by microorganisms, including fungi and protozoa.

The term "antibiotic" was coined by Selman Waksman in 1942 to describe


“Any substance produced by a microorganism that is antagonistic to the growth
of other microorganisms in high dilution”.

Testing the susceptibility of Staphylococcus aureus

to antibiotics by the Kirby-Bauer disk diffusion method. Antibiotics diffuse out from
antibiotic-containing disks and inhibit growth of S. aureus resulting in a zone of
inhibition

With advances in medicinal chemistry, most antibiotics are now semisynthetic


—modified chemically from original compounds found in nature, as is the case with
beta-lactams (which include the penicillins, produced by fungi in the genus
Penicillium, the cephalosporins, and the carbapenems). Some antibiotics are still
produced and isolated from living organisms, such as the aminoglycosides, and others
have been created through purely synthetic means: the sulfonamides, the quinolones,
and the oxazolidinones.
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CLASSIFICATION OF ANTIBIOTICS

I. Classification based on the source

 Natural - Bacitracin
 Semisynthetic – Benzyl penicillin
 Synthetic – Chloramphenicol.

II. Classification based on clinical effectiveness and degree of selectivity

 Narrow spectrum antibiotics – Those inhibiting only one group of


microorganisms. These drugs have high degree of selectivity. Eg. Bacitracin
and nystatin.
 Broad spectrum antibiotics – Those inhibiting large group of
microorganisms. Eg. Chloramphenicol.

III. Classification based on effectiveness against class of bacteria

 Gram positive antibiotics – Those inhibiting only gram positive bacteria.


 Gram negative antibiotics – Those inhibiting only gram negative bacteria.

[ Naming of Bacteria based on shape of Bacterial cell- Sperical ( coccus) ,


Rod-like ( bacillus), Spiral ( spirillium), Comma-shaped ( vibrio)].

Antibiotics may be divided into two broad groups according to their effect on
microorganisms:

 Those that kill bacteria are bactericidal agents.


 Those that only impair bacterial growth are known as bacteriostatic agents.

Synthetic antibiotic chemotherapy as a science and the story of antibiotic


development began in Germany with Paul Ehrlich, a German medical scientist in the
late 1880s.
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Dr. Ehrlich noted that certain dyes would bind to and color human, animal or
bacterial cells, while others did not. He then extended the idea that it might be
possible to make certain dyes or chemicals that would act as a magic bullet or
selective drug that would bind to and kill bacteria while not harming the human host.
After much experimentation, screening hundreds of dyes against various
organisms, he discovered a medicinally useful drug, the man-made antibiotic,
Salvarsan. However, the adverse side-effect profile of salvarsan, coupled with the
later discovery of the antibiotic penicillin, superseded its use as an antibiotic.
Arsphenamine was marketed under the trade name Salvarsan in 1910. It was
also called 606, because it was the 606th compound synthesized for testing. Salvarsan
was the first organic anti-syphillitic, and a great improvement over the inorganic
mercury compounds that had been used previously. A more soluble (but slightly
less effective) arsenical compound, Neosalvarsan, (neoarsphenamine), became
available in 1912.

Prontosil, the first commercially available antibacterial antibiotic was


developed by a research team led by Gerhard Domagk (who received the 1939
Nobel Prize for Medicine for his efforts) at the Bayer Laboratories of the IG Farben
conglomerate in Germany. Prontosil had a relatively broad effect against Gram-
positive cocci. The discovery and development of this first sulfonamide drug opened
the era of antibiotics.

Alexander Fleming’s discovery of Penicillin in 1928. Even then the


therapeutic potential of penicillin was not pursued. More than ten years later, Florey
and Chain succeeded in purifying penicillin. The purified antibiotic displayed
antibacterial activity against a wide range of bacteria. It also had low toxicity and
could be taken without causing adverse effects. Because of their discovery of
penicillin Ernst Chain, Howard Florey and Alexander Fleming shared the 1945 Nobel
Prize in Medicine. Fleming identified the mould that had contaminated his culture
plates as being from the Penicillium genus, and—after some months' of calling it
"mould juice"— named the substance it released penicillin on 7 March 1929.
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PENICILLIN

PENICILLINE

In the basic skeleton it contains a five membered thiazolidine ring and a four
membered beta-lactam ring.

R group can be varied to get higher generations of the penicillin drugs.

CH2
Eg: If R = , the drug is benzyl penicillin.

If R =

HO CH

NH2 , the drug is amoxicillin.

If R=

CH

NH2 , the drug is ampicillin.


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PENICILLIN

ACTION OF ACIDIC AND BASIC CONDITIONS

Natural penicillin are said to be acid and base unstable. Instability in acid media
logically terminates its oral administration due to the highly acidiC pH of the gastric
juice in stomach.

Penicillin under acidic pH condition is converted to penillic acid which has no drug
activity. Similarly under basic condition it is converted to penicilloic acid which
again does not have any drug activity.

Action of beta- Lactamase enzyme

Beta- Lactamase enzyme cleaves the beta-lactam ring and thereby making the
drug inactive.

MEDICAL APPLICATION

Ophthalmia neonatorum – a gonococcal infection in infants –first recorded


cure with penicillin, on November 25, 1930.

MASS PRODUCTION

The chemical structure of penicillin was determined by Dorothy Crowfoot Hodgkin


in the early 1940s.

DEVELOPMENTS FROM PENICILLIN

The narrow range of treatable diseases or spectrum of activity of the penicillins, along
with the poor activity of the orally active phenoxymethylpenicillin, led to the search
for derivatives of penicillin that could treat a wider range of infections. The isolation
of 6-APA, the nucleus of penicillin, allowed for the preparation of semisynthetic
penicillins, with various improvements over benzylpenicillin (bioavailability,
spectrum, stability, tolerance).
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The first major development was ampicillin, which offered a broader spectrum
of activity than either of the original penicillins. Further development yielded beta-
lactamase-resistant penicillins including flucloxacillin, dicloxacillin and
meticillin.

MECHANISM OF ACTION

β-Lactam antibiotics work by inhibiting the formation of peptidoglycan


cross-links in the bacterial cell wall. The β-lactam moiety (functional group) of
penicillin binds to the enzyme (DD-transpeptidase) that links the peptidoglycan
molecules in bacteria, which weakens the cell wall of the bacterium (in other words,
the antibiotic causes cytolysis or death due to osmotic pressure).

Gram-positive bacteria are called protoplasts when they lose their cell wall.
Gram-negative bacteria do not lose their cell wall completely and are called
spheroplasts after treatment with penicillin.

ADVERSE EFFECTS

Common adverse drug reactions (≥1% of patients) associated with use of the
penicillins include diarrhea, hypersensitivity, nause, rash, neurotoxicity. Infrequent
adverse effects (0.1–1% of patients) include fever, vomiting, dermatitis, seizures

ANTIBIOTIC MISUSE

The first rule of antibiotics is try not to use them, and the second rule is try not to
use too many of them.

—Paul L. Marino , The ICU Book

Inappropriate antibiotic treatment and overuse of antibiotics have been a


contributing factor to the emergence of resistant bacteria. The problem is further
exacerbated by self-prescribing of antibiotics by individuals without the guidelines of
a qualified clinician.
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STREPTOMYCIN

Streptomycin is an antibiotic drug, the first of a class of drugs called


aminoglycosides to be discovered, and was the first antibiotic remedy for
tuberculosis. It is derived from the Streptomyces griseus. Streptomycin is a
bactericidal antibiotic. Streptomycin cannot be given orally, but must be
administered by regular intramuscular injections. An adverse effect of this
medicine is ototoxicity, which can lead to hearing loss.

They are mixture of water soluble basic carbohydrates.

MECHANISM OF ACTION

Streptomycin is a protein synthesis inhibitor. This prevents initiation of protein


synthesis and leads to death of microbial cells. Humans have structurally different
ribosomes from bacteria, thereby allowing the selectivity of this antibiotic for bacteria.
However at low concentrations Streptomycin only inhibits growth of the bacteria

TREATMENT OF DISEASES

Tuberculosis in combination with other anti-TB drugs.

CHLORAMPHENICOL

Chloramphenicol is a bacteriostatic antimicrobial. It is considered a prototypical


broad-spectrum antibiotic. Chloramphenicol is effective against a wide variety of
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Gram-positive and Gram-negative bacteria, including most anaerobic organisms. Used


topically for eye infections. In low-income countries, chloramphenicol is still widely
used because it is exceedingly inexpensive and readily available.

HISTORY

Chloramphenicol was originally derived from the bacterium Streptomyces


venezuelae, isolated by David Gottlieb, and introduced into clinical practice in 1949,
under the trade name Chloromycetin. It was the first antibiotic to be manufactured
synthetically on a large scale.

ADVERSE EFFECTS

The most serious adverse effect associated with chloramphenicol treatment is bone
marrow toxicity, which may occur in two distinct forms: bone marrow suppression,
which is a direct toxic effect of the drug and is usually reversible, and anemia, which
is (rare, unpredictable, and unrelated to dose) and generally fatal.

SPECTRUM OF ACTIVITY

Because it functions by inhibiting bacterial protein synthesis, chloramphenicol has a


very broad spectrum of activity: it is active against Gram-positive bacteria, Gram-
negative bacteria.

MECHANISM OF ACTION

Chloramphenicol is bacteriostatic (that is, it stops bacterial growth). It is a protein


synthesis inhibitor.

THERAPEUTIC USES

The original indication of chloramphenicol was in the treatment of typhoid, but the
now almost universal presence of multi-drug resistant Salmonella typhi.
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TETRACYCLINES

Tetracyclines are a group of broad-spectrum antibiotics whose general usefulness has


been reduced with the onset of bacterial resistance. Despite this, they remain the
treatment of choice for some specific indications. They are so named for their four
(“tetra-”) hydrocarbon rings (“-cycl-”) derivation (“-ine”).

HISTORY

The first member of the group to be discovered was Chlortetracycline


(Aureomycin) in the late 1940s by Dr. Benjamin Duggar, a scientist employed by
Lederle Laboratories who derived the substance from a golden-colored, fungus-like,
soil-dwelling bacterium named Streptomyces aureofaciens. Oxytetracycline
(Terramycin) was discovered shortly afterwards by AC Finlay et al., it came from a
similar soil bacterium named Streptomyces rimosus. In June 2005, tigecycline, the
first member of a new subgroup of tetracyclines named glycylcyclines was introduced
to treat infections which are resistant to other antimicrobics including conventional
tetracyclines.
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MECHANISM OF ACTION

Tetracycline antibiotics are protein synthesis inhibitors.

ADMINISTRATION

When ingested, it is usually recommended that tetracyclines should be taken with a


full glass of water, either two hours after eating or one hour before eating. This is
partly because tetracycline binds easily with magnesium, aluminium, iron, and
calcium, which reduces its ability to be completely absorbed by the body. Dairy
products or preparations containing iron are not recommended directly after taking the
drug.

ANTIVIRAL AGENTS

Viruses represent a separate and unique class of infectious agents.

Virus

1. Possesses simple chemical composition.


2. Lacks the metabolic enzyme machinery.
3. Lacks the protein-synthesising system.
4. Contains only one of nucleic acid (i.e., either DNA and RNA)
5. Possesses a host cell dependent machinery of multiplication.

COMPOSITION

 Viruses do not possess cell wall. Viruses consist of either DNA or RNA
enclosed in a shell of protein known as CAPSID. The capsid is composed of
several sub-units known as capsomeres that decide the shape of the capsid.
Though often spherical, capsid may possess different shapes. In certain cases,
capsid may be surrounded by an outer protein of lipoprotein envelope. This
encircling membrane may be called as envelope.
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 The biology of ciral replication is dependent on the host cell metabolic


machinery (e.g., protein synthesis).
 Virus replicates only in the host cell. Hence they are considered as obligatory
intracellular parasites that utilizes many of biochemical machinery and products
of host cell to sustain their living.

VIRAL DISEASES

 Influenza , small pox, rabbies, poliomyelitis.

CLASSIFICATION OF VIRUSES

Classified based on the nucleic acid present.

1. DNA viruses: Contains Deoxy ribonucleic acid. Includes POXVIRUSES,


PAPOVIRUSES, HERPESVIRUSES.
2. RNA viruses: Contains Ribonucleic acid. Includes ARBOVIRUSES,
RHINOVIRUSES.

Poxviruses: Contains large DNA, Papoviruses: Contains small DNA causes


tunour, Herpes virus: Causes chicken pox, Arboviruses: Causes yellow fever
which affects kidney and liver and Rhinoviruses: Leads to respiratory infection.

CLASSIFICATION OF ANTIVIRAL DRUGS BASED ON CHEMICAL


STRUTURE:

1. Purine nucleosides and nucleotides


2. Pyrimidine nucleosides and nucleotides
3. Thiuosemicarbazones
4. Benzimidazoles
5. Adamantane amines
6. Interferons
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Antiviral agents have certain drawbacks:

1. Lack of satisfactory experimental models.


2. Use of wrong virus in the laboratory of study.
3. Narrow spectrum of activity.
4. Limitations on uses due to their toxicity.
5. Difficulties in their clinical assessment.

Various antiviral agents are found to possess very narrow spectrum of activity. The
development of antiviral agents having selective toxicity to viral cell leaving host cells
unaffected still remains a dream.

ACYCLOVIR TRIPHOSPHATE (Acycloguanosine)

It is synthetic purine nucleoside analog.

N
HN

H2N N
N

CH2OCH2CH2OH

MODE OF ACTION

ACYCLOVIR

Thymidine Kinase Enzyme

ACYCLOVIR TRIPHOSPHATE

This selectively inhibits HERPESVIRUS DNA


polymerase

Inhibition of viral replication process.

The affinity of viral thymidine kinase enzymes for acyclovir is 200 times greater than
that of Mammalian enzymes.
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VIRAL REPLICATION

MEDICAL APPLICATION

It can be used orally, topically and intravenously.

It is effective against herpes virus infections. A 3% ointment may be used for


the treatment of ocular (eye) herpetic infection. It may also be used intravenously in
the treatment of herpes simplex encephalitis ( inflammation of brain)
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ANTIPYRETIC ANALGESICS

Antipyretic analgesics are also known as febrifuges. They are defined as drugs
that lower the temperature of the body in PYREXIA (situations when body
temperature has been raised above normal).

They exert their action on the heat regulating centre in the hypothalamus.

CLASSIFICATION

They are classified on the basis of their chemical structure:


1. Aniline and p-aminophenol Analogues
2. Salicylic acid Analogues.
3. Quinoline derivatives
4. Pyrazolones and pyrazolodiones
5. N-Arylanthranilic acids

1. Aniline and p-aminophenol analogues:

Cohn and Hepp first identified the powerful antipyretic activities in both
aniline and acetanilide. The ortho, meta and para amino phenols are reported to be
relatively less toxic than aniline. The para- isomer is found to be the least toxic.

Eg.,
Paracetamol

HO NHCOCH3

It may be prepared by reduction of p-nitro phenol. It is employed as an


antipyretic and analgesic. It is particularly useful in aspirin-sensitive patients.

2. Salicylic acid Analogues:

Salicin was the first compound belonging to this category that exhibited
medical value. It was used as a substitute for quinine as a febrifuge. Acetyl salicylic
acid of aspirin was first synthesized by Gerhardt in 1852. The name aspirin originated
form the old name of salicylic or spiric acid, obtained from spirea plants.

Eg.,
Aspirin
COOH

OCOCH3
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It is used as an antipyretic, anti-inflammatory and an analgesic in a variety


of conditions ranging form headache, discomfort and fever associated with the
common cold, and muscular pains and aches.
As aspirin inhibits platelet function, it has been employed prophylactically to
minimize the incidence of myocardial infraction.

3. Quinoline derivatives:

The historical importance and utility of quinine was known in the medical
practice for a long time as a potent antipyretic in addition to its remarkable effect
against the malarial fever. Two quinoline derivatives first synthesized though
possessed significant antipyretic action, yet could not gain importance as drug because
of their high toxic effects on the red blood corpuscles and damaging after-effect on
kidneys. Eg., Thalline.

4. Pyrazolones and pyrazolodiones:

One of the first and foremost synthetic organic compounds which were
successfully used as drugs was found to be a heterocylce.

Eg.,
Phenylbutazone

N
O
N

H3CH2CH2CH2C O

It is a pyrazole derivative which has antipyretic, analgesic and anti-


inflammatory actions. Because of its toxicity it is not used as a general antipyretic
analgesic. It is used in the treatment of rheumatic disorders.

5. N-Arylanthranilic acids:

New horizon of antipyretic analgesic and anti-inflammatory which has


recently gained importance.

Eg., Mefenamic Acid


COOH

NH

H3C CH3
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It is analgesic drug usually used for the treatment of mild pain and pain due to
dental extractions.

MODE OF ACTION

The antipyretic and anti-inflammatory action are probably due to their


inhibitory effect on prostaglandin synthesis (prostaglandins sensitize nerves to the
action of pain stimulants).

NARCOTIC ANALGESICS
(Opiate analgesics)

Opium is obtained by making superficial incisions on the immature and unripe


capsules of Papaver somniferum (or poppy plant). The exudates is air-dried and then
powdered to give the official powdered opium. The alkaloid isolated from opium
includes morphine, codeine, papaverine and thebaine.

The opium class of narcotic drugs are considered not only as the most potent
and clinically useful agents causing depression of central nervous system, but also as
very stong analgesics. Morphine and morphine like drugs are referred to as opiods or
opiates. They are also known as narcotic analgesics (narcotic derived from the Greek
word ‘narcotuc’ meaning drowsiness).

Morphine and morphine like drugs may not alter the sensation of pain but they
modify the emotional reaction to pain. The pain may be present but may not be felt as
painful.

The narcotic analgesics tend to produce euphoria which is an important factor


in their addictive property which limits their use. Other limitations include respiratory
depression, decreased gastrointestinal motility leading to constipation.

Morphine

It possesses potent narcotic analgesic property. It is employed extensively as an


analgesic, antitussive agent. Morphine is responsible for altering the psychological
response to pain and thereby suppresses anxiety. It is specifically used for the
management of postoperative pain.

Codeine

It is methoxy derivative of Morphine. It is also a narcotic analgesic with


utilities similar to those of morphine, but its analgesic activity is relatively much less.
It exhibits only mild sedative effects.
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NON-STEROIDAL ANTI-INFLAMMATORY DRUG


(NSAID)

Inflammation may be defined as the series of changes that occur in living


tissues following injury. The injury which is responsible for inflammation may be
brought about by a variety of conditions such as: physical agents like UV radiations,
chemical agents like organic and inorganic compounds, toxins to various bacteria.

The seriousness and enormous after effects of steroid therapy necessitated the
development of non-steroidal anti-inflammatory drugs.

Eg.,

Ibuprofen:
It is an anti-inflammatory drug that possesses anti-pyretic and analgesic
actions. It is used for the treatment of rheumatoid arthritis and osteoarthritis.

Diclofenac Sodium:
It has analgesic, antipyretic and anti-inflammatory actions. It is mostly
employed in the treatment of rheumatoid arthritis and other rheumatic disorders.

ANTIHISTAMINES

Histamine occurs in many storage sites in the body in varying amounts. It is


present in the mast cells of many body organs, in blood basophiles, in the
hypothalamus.

In the living organism, histamine is synthesized from the naturally occurring α-


amino acid histidine by the loss of a carboxyl group through bacterial or enzymatic
decarboxylation.

A variety of antigens (sensitizing substance) derived from food products,


pollens, dust human hair, sheep wool etc., may cause serious allergic reactions in
human beings due to release of histamine. The release of histamine gives rise to a
number of physiological actions which are attributable to the activation of histamine
(H1 and H2) receptors by histamine.

A relatively mild release of histamine in the body leads to allergic reactions


displayed by vivid skin rashes with itching.

The action of histamines can be antagonized chemically using histaminase. The


actions are best modified by the use of substances that block competitively the
histamine sensitive receptors. Such substances are known as antihistamines.
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The most common side effect of antihistamine is sedation which may be


followed by drowsiness.

CLASSIFICATION

1. Histamine H1-Receptor Antagonist: Eg: Diphenhydramine hydrochloride.


2. Histamine H2-Receptor Antagonist: Eg: Cimetidine, Ranitidine.

GENERAL ANAESTHETICS

General anaesthetics are a group of drugs that produce loss of consciousness


and therefore loss of all sensation. The absolute loss of sensation is termed as
anaesthesia (derived from Greek word meaning insensitivity or lack of feeling).

These drugs are used in surgical operations to induce unconsciousness and


hence undo the sensation of pain.

CLASSIFICATION:

1. Inhalation anaesthetics
2. Intravenous anaesthetics
3. Basal anaesthetics.

1. INHALATION ANAESTHETICS

Inhalation anaesthetics could be either volatile liquids or gases and they are
administered through inhalation process. Eg:

a) Ether:
CH3CH2OCH2CH3
It still continues to be employed as an anaesthetic for producing insensitivity to pain
in surgical trauma.

b) Nitrous oxide:
N2 O
It is the weakest but the safest inhalation general anaesthetic. It is usually
administered in conjunction with other potent inhalation anaesthetics such as
halothane. Some patients often get an attack of hysteria and for this reason it is
invariably termed as laughing gas. In is an inhalation anaesthesia of choice in dental
surgery.

2. INTRAVENOUS ANAESTHETICS

Intravenous anaesthetics usually cause unconsciousness when administered


parenterally. Eg:
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Ketamine hydrochloride
It is rapid acting general anaesthetic drug which cause anaesthesia
accompanied by deep analgesia. It is an intravenous anaesthetic of choice for surgical
operations of short duration.

3. BASAL ANAESTHETICS

Basal anaesthetics are agents which induce a state of unconsciousness but the
depth of unconsciouness is not enough for surgical procedures. They are often used to
induce basal anaesthesia before the administration of inhalation anaesthetics. They are
often administered through rectum.

Basal anaesthetics have three merits namely:


a) Lack of mental distress
b) Pleasant induction
c) Lesser respiratory irritation.

Fenatyl Citrate
It is employed basically as an analgesic for the control of pain associated with
all kinds of surgery. It may be used along with all drugs commonly employed for
general anaesthesia.

LOCAL ANAESTHETICS

Local anaesthetics are used to abolish the sensation of pain in a restricted area
of the body and for minor surgical operations when loss of consciousness is not
desirable. The area is determined by the site and the technique of administration.
Usually smaller diameter nerve fibres are more susceptible to the action of local
anaesthetics than the larger diameter ones.

CLASSIFICATION

Based on the different modes of administration:

1. Surface of Topical Anaesthesia


They are applied to the mucous membrane, e.g., throat, damaged skin surface.

2. Infilteration Anaesthesia
The drug is injected subcutaneously to paralyze the sensory nerve endings
around the area to be rendered insensitive. Eg., for tooth extraction.

3. Nerve Block anaesthesia


The local anaesthesia is injected as close as possible to the nerve trunk
supplying the specific area to be anaesthetized. Eg., Minor operation of the limb.
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4. Spinal Anaesthesia
The drug is injected into the cerebral spinal fluid to paralyse the roots fo the
spinal nerves. Eg., Induce anaesthesia for abdominal and pelvic surgical operations.

5. Epidural Anaesthesia
This is special type of nerve block anaesthesia in which the drug injected into
the epidural space. Eg., the roots of spinal nerves are anaesthetized.

PROCAINE HYDROCHLORIDE

It is a local anaesthetic. It is an ester.

It is one of the least toxic and most commonly used local anaesthetics. The
salient features for its wide popularity is attributed to its lack of local irritation,
minimal systemic toxicity, longer duration of action and low cost. It is effectively
used for causing anaesthesia by infilteration, nerve block or spinal anaesthesia.