INDIVIDUAL

ANTIBIOTICS
PENICILLINS was 1st antibiotic to be used in man with revolution 3rd the Ht of
injection.

Classification :
•Penicillase sensitive penicillin
Penicillin G
Penicillin V

•Penicillin resistant penicillin

•Methicillin
•Oxacillin
•Cloxacillin
•Nafcillin
•Broad spectrum penicillin
•Ampicillin
•Amoxicillin
•Bacampicillin
•Carbenicillin
•B lactamase inhibitors
•Clavulanic acid
•Salbactum

Source :
* The fungus penicillium notatum and related species produce naturally
occurring penicillin.
•Semisynthetic penicillins are produced by chemically altering naturally occuring
penicillins. It is done either by combining side chains or by incorporating
specific precursors in the mould cultures.
 Pharmacokinetics:
•It may be administered orally or parenterally but should not be applied topically
due to their allergic potential.
•Penetration of this antibiotic is poor in CNS. Bone, synovial, and pericardial fluid.
Drug Trade Dosage Dose Indications Contraindic Adverse
Names form ations effects
Tetracycline Achromy Capsule 1-2 gm Juvenile Pregnancy Gl
cin Injection daily periodontitis, Children disturbance,
Terramy divided Chronic below 8 tooth
Ointment
cin into 4 periodontal years discoloration,
dose disease, enamel
Refractory hypoplasia
periodontitis
Desquamative
gingivitis
Clindamycin Clincin Tablet 150-300 Anaerobic Hypersensiti Urticaria,
Dalcap Capsule mg 6 streptococci, vity , infancy diarrhea,
hourly Clostridium abdominal
Injection
infections, pain,
Refractory jaundice,
periodontitis liver
abnormalities
Erythromycin Althrocin Tablet 250-500 Refractory Hypersensit Mild
Erythroci mg 8 periodontitis ivity epigastric
n hourly pain,
diarrhea,
E. Mycin
allergic
reaction
Metronidazole Flagyl Tablet 200-400 Ulcerative Neurologica Anorexia,
Metroyg Suspensi mg tds gingivitis, l disease, nausea,
yl on periodontitis, blood metallic
ANUG dyscrasias, taste,
Aldezole Injection 200
pregnancy glossitis
mg/5 ml
Quinolone Ciplox Tablet 250-500 Osteomyelitis Hypersensit Diarrhea,
Ciprofloxacin Cipin Injection mg 12 ANUG, joint ivity, vomiting,
hourly infection, children and abdominal
recurrent elderly pain,
periodontitis arthritis,
restlessness
Penicillin Kaypen Capsule, 250 mg- Refractory Sensitivity Skin rash,
Amoxicillin Ampilin, Syrup 1 gm tds periodontitis Pregnancy Urticaria,
Amox 125 GIT upset,
Ampicillin
mg/ml diarrhea
Cephalosp Alcephin Capsule 2-6 gm Inhibits growth Hypersensit GIT upset
orin biotax Injection daily in of gram-ve ivity, Renal Allergic
Cefotaxime 2-3 anaerobes, Failure reaction
Syrup
divided Osteomyelitis Increased
Cefaclor
dose 4 SGPT
Ceixime gm candidiasis
initially
followed
by 2 gm
IV
Chlorhexidi Hexidine Suspensi 0.2% Oral hygiene Allergy to Burning
ne Rexidin on w/v becterial chlorhexidin sensation,
100 ml infection e candidiasis
sensation,
bad taste
sensation
staining of
teeth
Antimicrobial Drugs :
•In crosses the placental barrier and its metabolized in liver
• Excreted by tubular secretion and glomerular filtration.

Mechanism of Action :
•It acts interfering with synthesis of bacterial cell wall.
• It is inactive against dormant organisms.;
• It inhibits the enzyme transpeptidases so that crosslinking( which maintains the
close knit structure of the cell wall)
dose not take place.

Antibacterial Spectrum :
•Cocci-streptococci are highly sensitive. Pneumococci, Neisseria gonorrhoeae
are also sensitive to penicillin.
• Bacilli-Corynebacterium dihitheriae, Clostridium tetani, Treponema Pallidum
are sensitive to penicillin. Actinomyces israelii is only moderately sensitive.
• Gram negative bacilli-Mycobacterium tuberculosis. H. influenzae are sensitive
to penicillin.
Bacterial Resistance :
•The staphylococci that are present in a large number in hospital environment
become resistant by producing penicilliase which inactivates penicillin by
breaking the β-lactam ring.
• Some resistant bacteria become tolerant and not penicillin destroying.

Adverse Reaction :
Toxicity
* The margin of safety is very high when penicillin is administered.
With massive intravenous doses, direct central nervous system irritation can
result in convulsions.
Large doses of penicillin G have been associated with renal damage
manifested as fever, eosinophilia, rashes, albuminuria and rise in blood ura
nitrogen.
Hemolytic anemia and bone marrow depression have also been induced by
penicillin.
The Irritation caused by injection of penicillin can produce sterile abscesses, if
given intramuscularly or thrombophlebitis, if given intravenously.
Anaphylactic reaction
• An acute allergic reaction occurs within ½ hour after the administration
penicillin.
• It is characterized by smooth muscle contraction. Capillary dilation and
urticaria caused by release of histamine and bradykinin..
• If treatment does not begin, immediately death can result.
•Rash- this type of reaction accounts for 80 to 90 percent of allergic
reactions to penicillin.
• Delayed serum sickness-serum sickness is manifested as fever, skin rash
and eosinophilia or severely as arthitis, purpura,
lymphadenopathy.splenomegaly and edema. It usually takes 6 days to
develop and can occur during treatment or up to 2 weeks after treatment
has ceased.
• Oral lesion-delayed reaction includes severe stomatitis, furred tongue,
black tongue, acute glossitis and cheilosis.
Penicillin G (Benzyl Penicillin)
It is active in low concentrations against all forms of gram +ve cocci and bacilli
while in high concentrations it acts against gram –ve bacilli. It is available in
various forms.
•Aqueous penicillin G
* It is given intravenously for obtaining high serum concentration and
when large amount is needed.
* The Half-life is 30 minutes.
* Dose – 5 to 20 million units/per day intravenously often continuously
or at intervals of 2 to 4 hours.
•Procaine Penicillin G
•Low serum concentration gives good results
• Due to the presence of procaine the onset is slower, but prolonged.
•Used in meningits, syphilis and endocarditis.
•Dose-6 to 12 lac units intramuscularly every 12 to 24 hourly. In
endocarditis 1.2 million units every 6 hourly is given.
Benzathine Penicillin G
* It is used only when blood level is acceptable in patients with
rheumatic heart disease under-going long-term prophylaxis of bacterial
endocarditis.
* It is released over a period of a week after administration.
* Dose- 0.6 to 2.4 MU intramuscularly every 2 to 4 weeks as aqueous
suspension.

Penicillin V
•It differs from penicillin G only in that it is acid stable.
•It can be given orally and produces higher blood level than penicillin G.
• It is most commonly used in treatment and prevention of dental Infection. It can
be given in pharyngitis, sinusitis, otitis media and prophylaxis of rheumatic fever.
• Dose
• Adult – 250-500 mg 6 hourly
•Infants – 60 mg 6 hourly.
•Children – 125 to 250 mg 6 hourly.
Penicillinase Resistant Penicillin :
•They are resistant to degradation by staphylococcal penicillinase.
• They have a very narrow spectrum of action and primarily used for treatment
of Staphylococcus aureus infections such as soft tissue infection.
• Side effects are gastrointestinal disturbances, bone marrow depression. And
abnormal renal and hepatic function.
• Patients allergic to penicillin are also allergic to this group of drug.
• In serious infections methivillin and oxacillin are given IV 0.25 to 1 gm/4 hourly.
• In soft tissue infections cloxacillin is given orally 250 to 500 mg 6 hourly.
Broad Spectrum Penicillin
They are most resistant and they inhibit the cell wall synthesis. These are
used against large spectrum of bacteria.
Ampicillin and amoxicillin produce higher and prolonged blood levels.
Ampicillin
It is active against all organism sensitive to penicillin G in addition, many
gram-negative bacilli.
Oral absorption is incomplete but adequate. Food interferes with the
absorption.
Plasma half-life is 1 hour.
Adverse effects- diarrhea is frequent after oral administration. It
produces high incidence of rashes.
Dose – 0.5 to 2 g oral /i,m/iv depending on severity infection, every 6
hours.
Bacampicillin
• It is an ester of ampicillin which is nearly completely absorbed from the
gastrointestinal tract.Thus. Higher plasma levels are attained.
• It does not markedly disturb intestinal ecology and due to incidence of
diarrhea, it is claimed to be lower.
•Dose – 400 to 800 mg bd.

Amoxicillin
* Oral absorption is better and food does not interfere
* Higher and more sustained blood levels are produced
* Dose – 0.25 to 1 g tds orally.
CHEPHALOSPORINS
These come under broad spectrum antibiotics. They are bactericidal
against gram +ve and –ve organisms. They inhibit cell wall synthesis of
bacteria.
Classification
First generation
Parenteral – cefazolin.
Oral –cephalexin, cefadroxil, cephradine
Second Generation
Parenteral – cefuroxime.
Oral –cefaclor, cefuroxime
•Third Generation
•Parenteral – ceftzidime, cefotaxime, ceftizoxime
•Oral - cefixime
•Fourth Generation
•Parenteral- cefpirome

Cefazolin
•Parenteral administration result in higher blood level that persists longer.
• It has a half-life of 2 hour due to slower tubular secretion
• Dose – 0.25 g 8 hourly (mild cases). 1 g 6 hourly(severe cases) IM and IV.

Cephalexin
•It is effective against most gram +ve cocci, baccilli, E. coli and Klebsiella.
• It is an orally effective first generation cephalosporin.
• Dose – 0.5 to 1 6 6 to 8 hourly and in children 25 to 100 mg/kg/day
Cefadroxil
 It is close congener of cephalexin, has good tissue penetration and it exerts more
sustained action at the site of infection.
 Dose-0.5 to 1 g bd.

Cefaclor
 It retains significant activity by the oral route.
 It is more active against H. influenzae, E. coli.
 Dose-125 oto 250 mg daily.

Cefuroxime
 It is highly active against ampicillin resistant H. influenzae.
 It is well tolerated by the IM route and attains relatively higher CSF level.
 Dose-0.75 to 1.5 G IM 8 Hourly.
Cefixime
 It is an Orally active and is highly active against Enterobacteriaceae.
 Dose-200 to 400 mg bd.
Uses :
E. Dental Infection
1. It can be given as alternative to penicillin especially in patients allergic to
penicillin
2. 1st and 2nd generation cephalosporin are active orally for orodental infection.
3. It can be given for orodental infection mainly caused by klebsiella.
4. Cephalexin and cephadroxil are given for prophylaxis of local wound infection
following the dental surgery.
B. General Medical Use :
1. As alternative of PnG in allergic patients
2. Respiratory, urinary, soft tissue infection caused by gram –ve
3. Septicaemias
4. Surgical Prophylaxis
AMINOGLYCOSIDES
It is a bactericidal drug and acts by inhibiting bacterial protein synthesis. They
have good activity against aerobic bacilli but also are active against anaerobic
bacteria. It can cause ototoxicity, nephrotoxicity and neuromuscular blockade.

Streptomycin
It is active against aerobic gram-negative bacilli.
Initially, it is used with rifampicin and isoniazid in treatment of tuberculosis
and with penicillin in treatment and prophylaxis of endocarditis.
Absorption from the injection site in muscles is rapid. It is excreted
unchanged in urine.
The plasma half-life is 2 to4 hours.
Adverse effects-there are vestibular and auditory disturbances. Pain at the
injection site is common.
dose-0.5 to 1 gm 12 hourly for 7 days in acute infection.
Neomycin
 It is a wide spectrum aminoglycoside, active against most gram-negative
bacilli and some gram-positve cocci.
 It is not used systemically, as it is highly toxic to the kidney. Oral and
topical application does not cause systemic toxicity.
 it is used topically for infected wound, ulcers, burns and external ear
infection.
Dose-0.25 to 1 g qid oral and 0.3-0.5 percent topical.

Gentamicin
 It is useful in treatment of serious gram-ve bacterial infection.
 Adverse reaction-nephrotoxicity, ototoxicity.
 dose-for an average adult with normal real function 1 to 1.5 mg kg IM or IV
8 hourly should be given.

TETRACYSLINE
Broad-spectrum bacteriostatic antibiotic isolated from soil actinomycetes in
1948.
Action
 It inhibits protein synthesis by binding to 30S ribosomes in susceptible organism.
 It is effective against variety of gram-ve and gram +ve bacteria. Rickettsial,
spirochetes, protozoa, and Mycoplasma.
 It is mainly given orally and it is secreted in saliva, concentrated in liver and
excreted in bile.
 they cross placental barrier.
 Dose-250 to 500 mg qid.

Adverse Reactions
 GIT disturbances like anorexia, vomiting, diarrhea, gastroenteritis and
superinfection.
 Hepatic toxicity and renal toxicity can occur.
 hypoplasia and brown discoloration of teeth can occur; hence it is not used in 3rd
trimester.
 tetracycline reduces protein synthesis and has an overall catabolic effect. They
induce negative nitrogen balance and can increase blood urea level.
 Tetracyclines are the most common antibiotics responsible for superinfection.
Uses :
Orodental Condition :
Tetracyclines are of limited usefulness in treating acute dental infection.
However they are benefit certain forms of periodontal disease.
Tetracycline plays important role in management of chronic periodontitis.
Tetracyclines are highly active against the Actinobacillus sp. That is held
responsible for destruction of gums and bone loss in juvenile periodontitis.
General Medical Uses :
Tetracycline are still the drug of first choice in –
i. Venereal disease
j. A typical pneumonia
k. Cholera
l. Plague
SULFONAMIDES
 These are bacteriostatic drugs which inhibit bacterial folate synthesis hence folic
acid is not formed and number of essential metabolic reactions suffer.
 It is effective against gram +ve and gram –ve bacteria like streptococcus
pyogenes, Actinomyces and H. influenzae.
 They are distributed throughout the body including the cerebrospinal fluid and it is
metabolized in liver and excreted in urine.
Adverse reactions
 There may be allergic reaction in the form of urticaria, poruritus, fever,
polyarteritis nodosa, erythema multiforme and Stevens-Johnson syndrome.
 Sulfonamides can cause hemolysis.
 Topical use of sulfonamides in not recommended because of risk of contact
sensitization.
 There may be nausea, vomiting and epigastric pain.
Dose
 Sulfadiazine-0.5 g qid to 2 g tds.
 Sulfamoxole-1 g bd on first day then 0.5 gm bd.
ERYTHROMYCIN
 It is isolated from streptomyces erythreus in 1952.
 It is bacteriostatic and interferes with protein synthesis by inhibiting enzyme
transferase at the 50S subunit of ribosome.
 It is effective against gram +ve and gram –ve bacteria.
 It is used as prophylaxis against endocarditis before dental procedures and in
patients allergic to penicillin. It is also used in tertanus, diphtheria and syphilis.
 It is excreted through urine, faeces and bile.
 Adverse reactions- there may be stomatitis, abdominal pain, nausea, vomiting,
jaundice, diarrhea, urticaria, and anaphylaxis.
Dose-it is given orally in dose of 250 to 500 mg 8 hourly.
CLINDAMYCIN
 It is a lincosamide antibiotic. They are bacteriostatic and effective against gram
+ve bacteria. It is mainly used against anaerobic bacteria.
 Oral absorption of clindamycin is good. It poenetrates most skeletal and soft
tissues.
 It crosses placental barrier and excreted in urine and bile.

Adverse reactions- there may be pseudomembranous enterocolitis, severe

persistent diarrhea. Passage of blood and bloody stool, skin rashes, dizziness,
nausea and vomiting.
Dose-150 to 300 mg qid orally and 200 to 600 mg IV 8 hourly
VANCOMYCIN
 It is a glycopeptide antibiiotic. It is a bactericidal agent which is active against gram
+ve cocci and bacilli.
 It acts by inhibiting bacterial cell wall synthesis.
 It is not absorbed orally. After IV administration, it is widely distributed, penetrates
serous cavities, inflamed meninges and is excreted by glomerular filtration.
Adverse reaction- it can cause plasma concentration dependent nerve deafness
which may be permanent.
Dose-250 to 500 mg 6 hourly orally and 500 mg 6 hourly or 1 g 12 hourly injected
IV.
METRONIDAZOLE
 Metronidazole in a dose of 200-400 mg TDS (15-30 mg/kg/day) is extensively used
to treat orodental infections, because anaerobic bacteria are frequently involved.
 After entering the microorganisms by diffusion, its nitro group is reduced to
intermediate compounds which cause cytotoxicity, probably by damaging DNA.
It should be avoided during first trimester of pregnancy, blood dyscrasias.

Adverse reactions- there may be nausea, anorexia, epigastric pain, headache,

metallic taste, glossitis, stomatitis and hairy tongue. Patient may get peripheral
neuropathy and CNS effects.
Dose- 200-400 mg/8 hourly orally, 15 mg/kg body weight 6 hourly IV.