Antibiotics and Their Types, Uses Indication Contraindication Dose Side Effects &Adverse effect.Cephalosporins are grouped into "generations" by their antimicrobial properties. Cephalosporins are categorized chronically, and are therefore divided into first, second, and third generations.The later-generation cephalosporins have greater effect against resistant bacteria.Fluoroquinolones are known as broad-spectrum antibiotics, meaning they are effective against many bacteria. Fluoroquinolones are used to treat most common urinary tract infections, skin infections, and respiratory infections (such as sinusitis, pneumonia, bronchitis).Tetracyclines are a family of antibiotics used to treat a broad spectrum of bacterial infections.

1. 3 important Antibiotics
Cephalosporin
Tetracyclines&
Fluoroquinolones
Presented by:
Md.Mustahasin Karim

2. Cephalosporin
 Cephalosporins are grouped into "generations" by their
antimicrobial properties. Cephalosporins are categorized
 chronically, and are therefore divided into first, second,
and third generations. Currently, three generations of
 cephalosporins are recognized and a fourth has been
proposed. Each newer generation of cephalosporins has
 greater gram negative antimicrobial properties than the
preceding generation. The later-generation
 cephalosporins have greater effect against resistant
bacteria.

3. Cephalosporin
 Cephalosporins are beta-lactam compounds in which the
beta-lactam ring is fused to a 6-membered dihydrothiazine
ring, thus forming the cephem nucleus. Side chain
modifications to the cephem nucleus confers 1)an
improved spectrum of antibacterial activity,2)
pharmacokinetic advantages, and 3) additional side effects.
Based on their spectrum of activity, cephalosporin's can be
broadly categorized into four generations.

4. Structure:
Cephalosporin

5. Mechanism of action:
 Cephalosporins are bactericidal and have the same mode of
action as other beta-lactam antibiotics (such as penicillins)
but are less susceptible to penicillinases. Cephalosporins
disrupt the synthesis of the peptidoglycan layer of bacterial
cell walls. The peptidoglycan layer is important for cell wall
structural integrity. The final transpeptidation step in the
synthesis of the peptidoglycan is facilitated by
transpeptidases known as penicillin-binding proteins
(PBPs). PBPs bind to the D-Ala-D-Ala at the end of
muropeptides (peptidoglycan precursors) to crosslink the
peptidoglycan. Beta-lactam antibiotics mimic(অনুকরণপ্রিয়)
the D-Ala-D-Ala site, thereby irreversibly inhibiting PBP
crosslinking of peptidoglycan.

6. CLASSIFICATION
A. First Generation
 Cephaloridine-Loridine, Ceporan
 Cephalothin-Keflin
 Cephalexin-Keflex, Ceporex
 Cefazolin-Cefacidal
 Cephradine-Velosef
 Cepharpirin-Cefadyl
 Cephadroxil-Doricef, Cefamox

7. Second Generation
 Cefaclor-Ceclor
 Cefoxitin – Mefoxin
 Cefuroxime – Zinacef, Zinnat
 Cefonicid – Monocid
 Cefotetan - Cefotan
 Cefamdandole – Mandol
 Cefprozil – Cefzil
 Loracarbef – Lorabid
 Cefmetazole – Zefazone
 Ceforanide

8. Third Generation
 Cefotaxime – Claforan
 Cefoperazone – Cefobid
 Moxolactam – Moxam
 Ceftizoxime – Cefizox
 Ceftriaxone – Rocephin
 Ceftazidime – Fortum
 Cefotiam – Ceradolan
 Cefixime – Suprax
 Cefetamet – Globocef
 Cefpodoxime – Vantin
 Ceftibuten – Cedax
 Cefdinir –Omnicef
 Cefditoren

9. Fourth Generation
Cefepime – Maxipime
Cefpirome – Cefrom

10. CEFADROXIL
Indication:
 It has been successfully used for the treatment of upper
respiratory tract infection.
 It is also used in U.T.I.
 Community acquired pneumonia(প্রনয়য়োয় োপ্রনয়ো) is well
treated by cefadroxil.
 It is effective against Gram-positive and Gram-negative
organisms.

11.  Contraindication:
 It is not used in an individuals with porphyria(rare inherited
or acquired disorder).
 If the patient hypersensitive to cephalosporin.
 Adverse effect:
 Diarrhoea.
 Nausea , Vomiting.
 Allergic reaction may occur.
 Blood disorders; including
thrombocytopenia(abnormally low amount of platelets).
 Leucopenia(Decrease of white blood cell).
 Aplastic anemia(damage of bone marrow).

12. Dose:
 Adult:
500mg twice daily for skin, soft tissue and U.T.I.
 Child:
250mg twice daily , soft tissue and U.T.I.(Age: 1-6 years).
Brand Name:
 Adora – Incepta.
 Trubid –Opsonin.
 Arocef –SK₊F.

13. CEFALEXIN/CEPHALEXIN
Indication:
 It has highly activity against Gram-positive organisms and
moderate activity against Gram-negative organism such as E.coli
, Klebseilla and proteus.
 It is useful for U.T.I. and R.T.I.
 It is effective in Sinusitis and Skin and Soft tissue infection.
Contraindication:
 It should not be used in infection caused by H. influenza.
 It should not used in Syphilis(sexually transmitted infection).
 Cephalosporin hypersensitivity.

14. Adverse effect:
 Diarrhea, Vomiting.
 Abdominal discomfort are relatively common.
 Neurological disturbances may occur rarely.
Dose:
 Adult:
500mg twice daily for severe infection.
 Child:
250mg twice daily for U.T.I.
Prophylaxis of recurrent U.T.I , 125mg at night.
Brand Name:
 Ceporin – Square.
 Keflin – Opsonin.
 Alexin – Reneta.

15. CEFOXITIN
Indication:
 It is effective against betalactamase producing strains of
Haemophilus influenzae.
 It is effective against Gram-negative organisms , except
pseudomonas.
 It can also be used in the treatment of U.T.I and lower respiratory
tract infections.
 It is useful in otitis ( কোয়নর িদোহ) media.
Contraindication:
 Hypersensitive to cephalosporin.
 Porphyria.

16. Adverse effect:
 Diarrhea.
 Nausea , Vomiting.
 Allergic reaction may also occur.
 GI upset.
Dose:
 200 – 400 mg daily in 1-2 divided dose.
 Brand Name:
 Cef-3−Square.
 Cefid−Opsonin.
 Rokim−SK₊F

17. CEFDINIR
Indication:
 It is very active against Staphylococci , Streptococci and H.
influenza.
 It is used in the treatment of gonrrhoea ( sexuall
transmitted infections).
 It is also used in R.T.I.
Contraindications:
 Hypersensitive to cephalosporin.
 Porphyria.

18. Adverse effect:
 Diarrhea.
 Allergic reaction.
 Gastrointestinal upset.
 Uncomfortable abdomen.
Dose:
 200-400mg daily in 1-2 divided doses.
 Brand Name:
 Efdinir-Incepta.
 Cednir-SK₊F.
 Cefida-Beximco.

19. CEFOTAXIME
Indication:
 It is widely used in in respiratory infection.
 It is effective in meningitis( প্রিষ্ক প্রিল্লীর িদোহ).
 It is used in the treatment of Typhoid fever , U.T.I.
 It is useful in gonorrhoea and intra-abdominal sepsis.
Contraindication:
 Hypersensitive to cephalosporin.
 Porphyria.

20. Adverse effect:
 Dermatological problem.
 Hematological problem may occur.
 Diarrhea.
 Allergic reaction.
Dose:
 I.M,I.V 1-2g every 8hours depends on severity of infection.
Brand Name:
 Cefotax – Renata.
 Maxcef – Square.
 Taxim – Acme.

21. CEFPODOXIME
Indications:
 It is used in upper respiratory tract infection.
 It is used in the treatment of lower respiratory tract
infection including bronchitis , pneumonia , skin and soft
tissue infection.
 It is used in the treatment of gonorrhoea.
Contraindication:
 Cephalosporin sensitivity.
 Porphyria.

22. Adverse effect:
 GI upset.
 Diarrhea.
 Nausea , Vomiting.
 Allergic reaction also occur.
Dose:
 100-200mg every 12hours for R.T.I. and U.T.I.
Brand Name:
 Vanprox – Square.
 Vercef – Beximco.
 Ximeprox – Incepta.
 Cefdox – ACI.

23. CEFTRIAXONE(INJ.)
Indication:
 It is effective in uncomplicated gonorrhoea and genital
ulceration.
 It has been commanded for the treatment of enteric fever.
 It is also used in meningitis.
 It is used in osteomyelitis (অপ্রির িদোহ).
Contraindication:
 Cephalosporin sensitivity.
 Porphoria.

24. Adverse effect:
 Abdominal pain , Diarrhea.
 Rush , fever.
 Thrombocytopenia , thrombocytosis , leucopenia.
Dose:
 A single 250mg dose is effective for gonorrhoea and genital
ulceration.
 I.M , I.V 1 g/day as a single dose in moderate infaction.
Brand Name:
 Traxon – opsonon.
 Arixon – Baximco.
 Ceftron – Square.
 Axon – Aristopharma.

25. CEFEPIME(INJ.)
Indication:
 It is indicated for the treatment of serious infection due to
organism resistance to cefotaxime.
 It is used in the treatment of respiratory tract infection.
 It is useful in gonorrhoea.
 It is effective in enteric fever.
Contraindication:
 Hypersensitivity to cephalosporin.
 Porphyria.

26. Adverse effect:
 Allergic reaction occurs.
 Nausea , Vomiting.
 GI upset.
Dose:
 I.V 2g of cefepime is given over 30min.
Brand Name:
 Xenim – Opsonin.
 Ultrapime – Incepta.
 Ceftipime – Reneta.

27. MAFENIDE
Indication:
 It is used extensively in burns(second and third degree burn)
 It is bacteriostatic against many Gram-positive and Gram-
negative organisms.
 Its capacity to inhibit carbonic anhydrous which could
potentially result in metabolic acidosis(when body produce
much acid or when the kidney remove enough acid).
Contraindications:
 Renal impairment.
 Mefenide is contraindicated in those with sulfonamide
hypersensitivity.

28. Adverse effect:
 Super infection.
 Pain.
 Rash.
 Pruritus.
Dose:
 It should apply topically to a thickness of approx. 1.6mg to
cleaned and debrided wound once or twice per day.
Brand Name:
 Mafanil.
 Sulphamylar.
 Sulfamylon.

29. CEFTOBIPROLE
Indications:
 It is effective against MRSA.
 It is also used in the treatment of complicated skin and skin
structure infections.
 It gives better result in community –acquired pneumonia (it is
pneumonia acquired infectious from normal social
contact)compared to ceptriaxone.
Contraindications:
 Hypersensitivity to cephalosporin.
 Hepatic failure.
 Renal impairment.

30. Adverse effect:
 Nausea
 Diarrhea
 Allergic reaction.
Dose:
 400 mg daily for MRSA.
Brand Name:
 Zeftera-UK,EU

31. CEFTAROLINE FOSAMIL
Indications:
 It has activity against MRSA(Methicillin-resistant
Staphylococcus aureus)
 It is also used in treatment of complicated skin and skin
structure infections.
 It gives better result in community –acquired pneumonia
compared to ceftriaxone.
Contraindications:
 Known serious hypersensitivity to ceftarolin.
 Porphyria.

32. Adverse effect:
 Diarrhea.
 Nausea.
 Rush.
Dose:
 400mg daily for M.R.S.A.; in serve case it may be two time
daily.
Brand Name:
 Teflaro in US.
 Zinforo in Europe.

33. Tetracyclines
 - Tetracyclines are a group of broad-spectrum
antibiotics
 - They are natural product derived from
Streptomyces sp
 - Tetracyclines are so named for their four (tetra)
hydrocarbon rings

34. Tetracyclines
 - The general usefulness of tetracyclines has been
reduced with the onset of antibiotic resistance.
Despite this, they remain the treatment of choice for
some specific indications

35. General Consideration
- Source: Streptomyces grasius, a soil organism
- Spectrum: Broad spectrum of activity i.e., active
against both gm(+) and gm(-) bacteria
- Mode of action: Bacteriostatic in nature
- Mechanism of ACTION: Protein synthesis inhibition

36. History
 The development of the tetracycline antibiotics was
the result of a systemic screening of soil specimens
collected from many parts of the world for antibiotic-
producing microorganisms. The first of these
compounds chlortetracycline was introduced in 1948
followed by oxytetracycline and tetracycline in 1950
and 1952 respectively.

37. Types
 Tetracyclines are of two types:
 1. Natural Tetracycline: (Short acting)
- Chlortetracycline (S.aureofaciens )
- Oxytetracycline (S. rimosus )
- Demeclocycline (S. aureofaciens )

38. Types
 2. Semisynthetic Tetracycline: (long acting)
-Doxycyclicline
- Methecycline
- Minocycline
3. Both natural and semisynthetic:
-Tetracycline :
Natural from S. grasius
Semisynthetic from Chlortetracycline

39. Mechanism of ActionTetracycline
Enters into bacteria by
-passive diffusion
-Active transport
Binds reversibly to receptor on the 30s ribosomal subunit
Block the binding of charged aminoacyl tRNA to the ‘A’ site of the ribosome mRNA
complex
(-) addition of aminoacid in growing peptide chain
(-) Protein synthesis
(-) Bacterial growth & multiplication
Note: At high conc. they can inhibit protein synthesis of mammal cell

40. Mechanism of Tetracycline resistance
>>The drug is not actively transported into the cell
>>The drug leaves the cell so rapidly that the required
conc. Of the drug is not maintained
>>Enzymatic inactivation of tetracycline
>>Production of protein that interferes binding of
tetracycline to ribosome

41. Therapeutic uses
 Drug of first choice
●Rickettsial infection
-Rocky mountain spotted fever
-Typhus
-Rickettsialpox
●Mycoplasma infection
-Mycoplasma pneumonia
●Borrelia infection
-Lyme disease
-Relapsing fever
●Vibrio infection
-Cholera
●Plague, brucellois ( with aminoglycoside)

42. Therapeutic uses
 Drug of second choice
●Diarrhoea
●Dysentery
●Mixed bacterial infection e.g. repiratory tract infection
●Acne
●SIADH (Syndrome of inappropriate ADH secretion)
●Leptospiral infection
●Tularemia (An acute plague like infectious disease
Caused by Francisella tularensis transmitted to the human by
the bite of an infected tick or other blood sucking insect
●Weils disease

43. Adverse effect
 A) Organ/ system toxicity
●GIT
-Nausea
-Vomiting
-Diarrhoea
-Alteration of intestinal flora
● Hepatotoxicity
●Nephrotoxicity (due to inhibition of protein synthesis)
-Renal tubular acidosis
-Nephrogenic diabetes insipidus
-Fanconis syndrome
● Bony stucture and teeth:
-Discoloration and hypoplasia of teeth
●Vestibular toxicity:
-Dizziness
-Vertigo

44. Adverse effect
 B) Super infection:
-Candida or resistant staphylococci
 C) Hypersensitivity:
-Urticaria
-Anaphylaxix
-Angioedema

45. Contraindication
●Pregnancy and lactation
●Young children ( upto 8 years)
●Renal failure
●History of hypersensitivity

46. Oxytetracycline
● Indications:
-treatment of Spirochaetal infection.
-treatment of Non-Specific-Urethritis.
-treatment of Clostridial wound infection and Anthrax.
●Contraindication:
-Renal impairment
-Pregnancy & breast feeding
-SLE (Systemic lupus eryyhematosus)
●Side effects:
-Local irritation after intramuscular injection.
-Gastrointestinal:-anorexia, nausea, vomiting.
-Renal toxicity.
-Hypersensitivity reactions: Urticaria.
-Blood: Hemolytic anemia, thrombocytopenia, neutropenia

47. Oxytetracycline
●Dose:
250-500 mg every 6 hours
●Market preparations
-Renamycin® (Renata)
-Oxecylin® (ACME)
-Oxycap® (Globe Pharma)

48. Doxycycline
●Indications:
-Treatment of chronic adult periodontitis.
-Chronic prostatitis
-Brucellosis
●Contraindication:
-Renal impairment
-Pregnancy & breast feeding
-SLE (Systemic lupus eryyhematosus)
●Side effects:
-Watery diarrhea
-Bloody stools
-photosensitivity, rash

49. Doxycycline
●Dose:
-By mouth 200 mg on first day, then 100 mg daily
-In severe infections 200 mg daily for 4 days
●Market preparations:
-Doxin (Opsoni)
-Doxy-A (ACME)
-Servidoxyne (Novartis)

50. Tetracycline
●Indications:
-Tetracycline's primary use is for the treatment of acne
vulgaris and rosacea.
-It is also used to treat a very wide range of infections.
●Contraindication:
-Renal impairment
-Pregnancy & breast feeding
-SLE (Systemic lupus eryyhematosus)
●Side effects:
-Superinfection
-Enamel dysplasia
-Impairment in bone growth

51. Tetracycline
●Dose:
-By mouth 250 mg every 6 hours
-Increased in severe infections to 500 mg every 6-8 hours
●Market preparations:
-Jmycin (Jayson)
-Tetracycline (Opsonin)
-Tetracyn (Renata)
-Tetrax (Square)

52. Fluoroquinolones
 Fluoroquinolones are known as broad-spectrum antibiotics,
meaning they are effective against many bacteria.
 Fluoroquinolones are used to treat most common urinary tract
infections, skin infections, and respiratory
 infections (such as sinusitis, pneumonia, bronchitis). Common
side effects of fluoroquinolones include mainly
 the digestive system: mild stomach pain or upset, nausea,
vomiting, and diarrhea. These are usually mild and go
 away over time. Fluoroquinolones should not be given during
pregnancy.
 Fluoroquinolones inhibit bacteria by interfering with their
ability to make DNA. This activity makes it difficult
 for bacteria to multiply. This effect is bacteriocidal.

53. Quinolones
 The quinolones are family of synthetic broad spectrum
antibacterial drugs
 Quinolones exert their antibacterial effect by
preventing bacterial DNA fom unwinding and
duplicating
 The majority of quinolones in clinical use belong to
the subset fluroquinolones

54. History
 The first generation of quinolones began with the
introduction of nalidixic acid in 1962 for treatment of
urinary tract infections in humans. Nalidixic acid was
discovered by George Lesher and coworkers in a
distillate during an attempt at chloroquine synthesis.

55. Types
A) First generation:
●Non flurinated quinolone
●Narrow spectrum
-Nalidixic acid
B) Second generation:
● Flurinated quinolones, 6o times more active then nalidixic acid
●Broad spectrum
●Not effective against anaerobes and community acquired pneumonia caused by
Streptococcus pneumoniae
-Ciprofloxacin
-Enoxacin
-Lomefloxacin
-Acrosoxzacin
-Norfloxacin
-Ofloxacin

56. Types
C) Third generation:
●Broad spectrum
●Effective against anaerobes and community acquired pneumonia caused
by Streptococcus pneumoniae
-Sparfloxacin
-Levofloxacin
D) Fourth generation:
●More effective against anaerobes and community acquired pneumonia
caused by Streptococcus pneumoniae
-Moxifloxacin
-Trovafloxacin

57. Mechanism of Action
 Mechanism of action:
-Inhibit bacterial DNA synthesis by
inhibiting DNA gyrase and topo-isomerase
IV resulting to rapid cell death
-Post antibiotic effect: lasts 1 to 2
hours, increases with increasing
concentration

58. Mechanism of Action
Quinolone
Enter into cell via passive diffusion
(-) Rejoining of DNA
(-) Supercoiling of DNA
Cell death
Note: Quinolone (-) human DNA gyrase only at much higher
conc. i.e., 100-1000 µ gm/ml

59. Mechanism of Quinolone resistance
●Chromosomal:
-Alter target enzymes: DNA gyrase and topoisomerase IV
-Decreased drug penetration: Pseudomonas, E. coli
●Plasmid: seen in some K. pneumoniae and E. coli
●Mutations in both target enzymes are needed to produce significant
resistance

60. Therapeutic uses
●Urinary tract infections
●Gastrointestinal infections
-Enteric fever
-Bacillary dysentery
-Septicaemia
●Respiratory tract infections (but not in pneumococcal
pneumonia
●Gynecological infection
●Intraabdominal infection
●Severe systemic infection

61. Adverse effect
-Tendon inflammation
-Arthralgia
-Myalgia
-Hypersensitivity reactions (sometimes involving
blood cells
-Photosensitivity
-Nausea, Vomiting

62. Contraindication
-Epilepsy
-myasthenia gravis
-Pregnant and lactating women
-Children

63. Nalidixic acid
●Indications:
-In complicated UTI
●Contraindication:
-Hypersensitivity to drug
-Porphyria
-Liver disease
-Renal impairment
●Side effects:
-Psychosis
-Cranial nerve palsy
-Metabolic acidosis

64. Nalidixic acid
●Dose:
By mouth 1g every 6hours for 7 days
●Market preparations:
-Naligram® (ACME)
-Nebactil® (Beximco)
-Utirex® (Opsonin)

65. Ciprofloxacin
●Indications:
- Nosocomial pneumonia
- Intra-abdominal infections
-Uncomplicated/complicated UTI
-Anthrax exposure and prophylaxis
●Contraindications:
-Pregnant and lactating women
-myasthenia gravis
-Hypersensitivity
●Side effects:
-CNS toxicity
-GIT upset
-Hypersensitivity

66. Ciprofloxacin
●Dose
By mouth,
-In RTI 250-500 mg every 12 hours
-In pseudomonal lower RTI 750 mg twice daily
-In UTI 250-500 mg twice daily
●Market preparations:
-Beuflox (Incepta)
-Cipro-A (ACME)
-Flontin (Renata)
-Neofloxin XR (Beximco)

67. Lomefloxacin
●Indications:
-Treatment of bronchitis due to H. inflenzae
-UTI
●Contraindications:
-Pregnant and lactating women
-myasthenia gravis
-Hypersensitivity
●Side effects:
-Phototoxicity
-CNS toxicity
-GIT upset
-Hypersensitivity

68. Lomefloxacin
●Dose:
400 mg once daily
●Market preparations:
-Lomeflox (Aristopharma)
-Mexio (Square)
-Namicin (Nipa)

69. Ofloxacin
●Indications:
-UTI
-Lower RTI
-Gonrrhoea
-Cervicitis
●Contraindications:
-Hepatic and renal impairment
-History of psychiatric illness
●Side effects:
-Hypersensitivity reactions (sometimes involving
blood cells

70. Ofloxacin
●Dose:
By mouth,
-UTI: 200-400 mg daily in the morning. Increased
upto 400 mg twice daily for upper UTI
-Chronic prostatitis 200 mg twice daily for 28 days
-Lower RTI 400 mg daily in the morning
●Market preparations:
-Oflacin (Drug Intl.)
-Rutix (Square)

71. Levofloxacin
●Indications:
-Chronic bronchitis and CAP
- Nosocomial pneumonia
-SSTIs
-Intra-abdominal infections
●Contraindictions:
-Renal impairment
-Pregnant and lactating women
-Children
●Side effects:
-Asthenia
-Rarely tremor
-Anxiety
-Tachycardia

72. Levofloxacin
●Dose:
Oral,
-Acute sinusitis: 500mg daily for 10-14 days
- -Exacerbation of chronic bronchitis: 250-500 mg daily for 7-10 days
- -Community acquired pneumonia: 500 mg once or twice daily for
7-14 days
●Market preparations:
-Evo (Beximco)
-Exolev (Novartis)
-Levoking (Renata)
-Trevox (Square)

73. Moxifloxacin
●Indications:
-Chronic bronchitis
-Bacterial conjuctivitis
-Sinusitis
●Contraindications:
-Should be avoided in patients with existing QT prolongation
●side effects:
-CNS toxicity
-GIT upset
-Hypersensitivity

74. Moxifloxacin
●Dose:
Adult dose is 400 mg daily
●Market preparations:
-Maximox (Orion)
-Odycin (Beximco)
-Optimox (aristopharma)