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Anti-Infective

Hello!!!!!!!!!!!!! I am Bacterium. Just because you can’t see me, you don’t even know me. Next
time you stay at home of nasty cold or have diarrhea, remember, I am at work.

I am a bacterium, just one of the many types of micro-organism present all around you. Not all of
us are as bad as you think. Some of us stay in your body in harmony without causing any harm to
you. These are called as Commensals. Few of us can cause problem to you. Those are mainly
parasites that need your body as a host to survive. And some of us even wait for the right
opportunity to cause you problem….we are then can be called as Opportunists’.

Like your name and surname we also have two parts to our name. In “Streptococcus aureus”
the first part is the genus while aureus stands for species name.

Let me introduce my 3 cousins, who are equally capable of making your life painful at times

Viruses
 Viruses are microscopic particle that can infect the cells of any biological organism.
 Viruses can only replicate themselves by infecting a host cell.
 Most common human viral infections are -
- Hepatitis B, C, D, E
- AIDS
- Poliomylitis
Fungi
 Fungi are generally multicellular organisms with complex cell structure.
 Fungi cause common skin infections like Tinea, Ringworms, etc. Can sometimes cause
serious infections in patients whose immune system is weak – like Candidiasis,
aspergillosis.
Protozoa

 Protozoa are single celled organisms and highly motile.

– Plasmodium falciparum – Malaria


– Entamoeba histolytica - Amoebiasis or amoebic dysentary
– Giardia lamblia – Giardiasis
– Trichomonas vaginalis-Trichomoniasis
– Toxoplasma Gondii – Toxoplasmosis

We Bacteria are responsible for the largest number of disease, compared to any other micro-
organism. We, like you a lot as you give us place to stay, give us food and give us a chance to
reproduce. Of course we don’t ask your permission to do all that….but then no formalities between
friends! Now I am going to tell more about the Great Bacteria family.

Bacteria are single celled organisms and the most common cause of infections. Bacteria are not
visible through naked eyes. Bacteria are available in various shapes like Round (Coccus), Rod
(Bacilli), Spiral (Spirillum).Bacterial cells are surrounded by a cell wall. They are found
everywhere & have incredible multiplication capability; every 30 mins (one day each bacterium
would produce over 16,500,000 bacteria)

Bacteria are natural habitat of human mouth, stomach, and intestine but become pathogens when
body’s defense system is weak or normal flora of the system is disturbed.

Bacterium cell Types of Bacteria

Classification of Bacteria:
Bacteria are difficult to see through microscope unless they are colored or stained. Danish scientist
Hans Christian Gram developed the method of staining. Hence the method is called Gram
Staining.

A bacterium that stains Blue or Purple color is called Gram +ve bacteria and those, which takes
Red or Pink Stain, is called Gram -ve.

Another major difference is in the cell wall composition

Depending on their O2 requirement for survival Bacteria can be aerobes or anaerobes

Hence gm + ve bacteria can be either aerobes or anaerobes. Similarly gm – ve bacteria can also be
aerobes or anaerobes.

Examples of Gram +ve aerobic and anaerobic and Gram-ve aerobic and anaerobic
bacteria.

The most common infection causing Gram + ve aerobic bacteria are –

 Staphylococcus aureus
 Staphylococcus epidermidis
 Streptococcus pneumoniae
 Streptococcus pyogenes (Group A β-hemolytic)
 Streptococcus viridans (Group B β-hemolytic)
 Streptococcus faecalis (enterococcus)
The most common infection causing Gram + ve anaerobes are

 Peptostreptococcus
 Clostridium species

The most common infection causing Gram - ve aerobes

 E.Coli
 Klebsiella pneumoniae
 Proteus mirabilis
 Enterobacter species
 Haemophilus influenzae
 Moraxella catarrhalis
 Salmonella typhi / paratyphi
 Shigella
 Neisseria gonorrhoea / meningitides
 Helicobacter pylori

The most common infection causing Gram - ve anaerobes


 Bacteroid Fragilis
 Fusobacterium

What are atypical bacteria?


Some bacteria don’t have well defined cell wall and are potential pathogens – they are called atypical
bacteria. Chlamydia trachomatis / pneumoniae, Mycoplasma pneumoniae / hominis.

Now let me explain to you how Microorganisms invade your body?

 Bacteria are able to surpass the first line defense

 Second line defense destroys the bacteria - “NO Infection”

 Body’s defense system is not entirely able to destroy the bacteria - “carrier state” e.g. s typhi.
Bacteria is able to overcome body’s defense system - “Infection”

Infections of the Upper Respiratory Tract. (URTI)

 Pharyngitis - Inflammation of the Pharynx.


 Tonsillitis – Inflammation of the Pharynx.
 Otitis Media – Inflammation of the middle ear.
 Pharyngotonsillitis.
 Sinusitis – Inflammation of the paranasal sinuses.
Infections of the Lower Respiratory Tract. (LRTI)

 Pneumoniae - Inflammation of the Lungs.


 CAP (Community-acquired pneumonia): CAP is a disease in which individuals who have not
recently been hospitalized develop an infection of the lungs (pneumonia).

 Bronchitis – Inflammation of the Bronchi.

 AECB – Acute Exacerbation of chronic bronchitis.

 COPD – Chronic obstructive pulmonary disease

Now let me tell you some of those Bacteria which are responsible for causing URTI,
LRTI & UTI.

 LRTI

 S pneumoniae

 M catarrhalis

 H influenzae

 URTI

 S pneumoniae

 M catarrhalis

 H influenzae

 S pyogenes

 UTI

 E coli

 Klebsiella

 Proteus

 Bone & Joint /Skin and Soft tissue infection

 Most common bacteria is S aureus

 S epidermidis

Well now that you have understood in details about the different microorganisms and the different
types of infections caused by them. Now I will brief you about those chemical substances which are
meant for killing or inhibiting the growth of the bacteria.

Yes I am talking about ANTIBIOTICS.


Antibiotics
Chemicals produced by microorganisms, which in small quantity inhibits the growth
or kills other microorganism.

Antibiotics are classified mainly on the basis of their chemical structures. The different types of
antibiotics are as follows.

1) Beta-lactams
2) Fluroquinolones
3) Amino glycosides
4) Macrolides
5) Tetracycline
6) Sulphonamides
7) Nitroimidazoles

Let us now discuss about one of the most widely used antibiotics which have a very
wide spectrum of coverage. Yes we will now discuss about Beta lactam antibiotics.

Beta lactam antibiotics


These are the most prescribed antibacterial because of their wide spectrum and safety profile. The
beta lactam antibacterial are characterized by the presence of a Beta-Lactam ring e.g. Penicillin,
Cephalosporins, Monobactams and Carbapenems.

Mode of action of Beta lactam antibiotics


Penicillin act by inhibiting the synthesis of the peptidoglycan layer of bacterial cell wall.

The peptidoglycan layer is important for cell wall structural integrity, especially in gm + ve
organisms. They are bactericidal. All β-lactam antibiotics have time dependent killing. As long
the plasma conc. remains above MIC, it exhibits bactericidal activity

How Cephalosporins are classified?


Cephalosporins are classified on the basis of their generations. The generations vary as per the
spectrum of pathogens they cover.

Generation Names Descriptions

First Cephalexin, Cefazolin Very good gm + ve, narrow - ve

Second Cefaclor, Cefuroxime, Good gm + ve, Good gm - ve

Second Cefotetan, Cefoxitin Moderate gm + ve & gm – ve with


Cephamycins
Anaerobic coverage

Third Oral Cefpodoxime, Adequate gm + ve,


Cefixime
Very good gm – ve

Third inject able Cefotaxime, Adequate gm + ve,


Ceftriaxone,
Very good gm – ve
Third inject able Ceftazidime, Adequate gm + ve,
Cefoperazone
Very good gm – ve with

Anti-pseudomonal activity

Fourth Cefpirome, Cefepime Adequate gm + ve, very good gm – ve with anti-


pseudomonal & anaerobic activity

OMNATAX-O

Composition:

Each Tablet of “Omnatax-O 200” contain Cefixime 200 mg


Each Tablet of “Omnatax-O 100 DT” contains Cefixime 100 mg in Dispersible form.
Each 5 ml of “Omnatax-O 30ml” contains Cefixime 50mg/5ml in dry syrup form.

Class: Omnatax-O contains Cefixime, which is a semi-synthetic oral 3rd generation Cephalosporin,
with broad spectrum of antibacterial activity. It is known as a Beta-Lactam antibiotic due to the
presence of B-Lactam ring in its molecular structure.

Antibacterial Spectrum

Gram +ve:

 S. pneumoniae

 S. pyogenes

Gram –ve:

 E. coli

 P. mirabilis

 H. influenzae (including B-Lactamase producing strains)

 M. catarrhalis (most are B-Lactamase producing)

 N. gonorrhoea (Penicillinase & Non-Penicillinase producing strains)

**Cefixime is highly stable in the presence of B-Lactamase enzyme.


** It is inactive or poorly active against staphylococci, enterococcus and bacteroides species.

Mechanism of Action
Cefixime binds to PBPs (Penicillin Binding Proteins) in cell wall of the bacteria and inhibits the cell-
wall synthesis. Thus, it is Bactericidal in action.

Pharmacokinetics

Absorption

Cefixime is absorbed to an extent of 50% when given orally with or without food. However, time to
maximum absorption increased approximately 0.8 hours when administered with food. The peak
plasma concentration achieved with oral suspension is approximately 25-50% higher than that
achieved with tablets.

Distribution

It is widely distributed in most tissues and fluids in the body. High concentration of the drug is
attained in bile. Peak plasma concentration is reached in 2-6 hours. Half-life is 3-4 hours. Plasma
protein binding is 65%. Average AUCs at steady state in elderly patients are approximately 40%
higher than average AUCs in healthy adults.

Metabolism

There is no evidence of metabolism of Cefixime in vivo.

Excretion

Approximately 50% of the absorbed dose is excreted unchanged in the urine in 24 hours. 5-10% of
the drug is also excreted in the bile.

Indications and Causative Pathogens

 Uncomplicated UTI – E. coli, P. mirabilis


 Otitis Media -H.influenzae, M.catarrhalis & S. pyogenes
 Pharyngitis and Tonsillitis -S. pyogenes
 AECB (Acute exacerbations of Chronic Bronchitis) – S pneumoniae & H. influenzae.
 Uncomplicated Gonorrhea (cervical/urethral)–Neisseria gonorrhoeae
 Typhoid fever–S. typhi / S.paratyphi
 Switch Therapy from other 3rd generation parenteral cephalosporins

Dosage
RTI
Adult – 400mg/day as single or two divided doses for 5 to 7 days.
Children-(Less than 50 kg / below 12 years age) 8mg/kg/day as single or two divided doses for 5 to 7
days
Uncomplicated UTI
400mg/day as single dose for 5 days.
Uncomplicated Gonorrhea
Single dose of 400mg in uncomplicated gonorrhea
Typhoid Fever
Adults-200mg to 400mg once or twice daily for 14 days.
Children (Less than 50 kg / below 12 years age) – 15 to 20mg/kg/day in 2 divided doses
In infants below 6 months age, the Efficacy / Safety of Cefixime is not established.
Renal Insufficiency –

Adverse effects

The drug is generally well tolerated. Mild and transient incidences of diarrhea, nausea, vomiting,
dyspepsia, abdominal pain, skin rash, drug fever, Pruritus, dizziness, and headache may be noted.
Rarely Pseudo-membraneous Colitis, Anaphylaxis may occur (seen with all antibiotics).

USPs of Cefixime

 Combines the power of 3rd generation Cephalosporin and the convenience of Oral Therapy.
 Contains just 6.3gm of powder compared to other Cefixime Dry syp, so easy to reconstitute.
 Thin suspension formed with viscosity of just 0.31 poise. (easy to swallow)
 Homogeneous suspension which does not have any sedimentation even after 3 days
compared to other brands.
 Ideal for switch therapy from any other 3rd generation parenteral Cephalosporin
 Highly resistant to B-Lactamase enzyme
 Lower bulk density and Pure Cefixime makes a good sturdy formulation ensuring good
quality.
 100 DT tablet and Dry syrup available as Strawberry flavor.

Competitor Brands

Brand Name Company


Zifi FDC
Taxim O Alkem Labs
Cefolac Macleods
Mahacef Mankind
Hifen Hetero

Thank You