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1. Dr. Adanwali Hassan Ahmed
(Rn-Mw, Medical doctor (MD), Health Officer (HO)
Msc-Gyn/Obest.
Antibiotics

2. Introduction
 Contents
1. Sulfonamides ( broad spectrum, bacteriostatic)
2. Penicillin's (broad-spectrum, bacteriocidal)
3. Cephalosporin's: One of several broad spectrum antibiotic
substances obtained from fungi and related to penicillin
4. Tetracycline's (bacteriostatic)
5. Aminoglycosides ( bacteriocidal)
6. Quinolones/Fluoroquinolones (bacteriocidal)
7. Macrolides (bacteriostatic)
8. Miscellaneous Drugs (bacteriocidal)

3. Continue
 Antibiotics are drugs of pertaining ability to
destroy or interfere with the development of a
living organism.
Antibiotics can be classified into:
1. Bacteriostatic
2. Bactericidal

4. 1. Sulfonamides
 Sulfonamides are chemically related group of
antibiotics that are all synthetic derivatives of
sulfonamide.
 They were one of the first group of drugs used
as antibiotics and some of the more
commonly prescribed agents.
Sulfonamide: Antibacterial consisting of any of
several synthetic organic compounds capable of
inhibiting the growth of bacteria that require

5. Continue
 These antibiotics achieve very high concentration
in kidneys through which they are eliminated.
There fore they are primarily used for the
treatment of urinary tract infections (UTI).
Sulfonamides are also used in the treatment of
rheumatoid arthritis, in addition they may be
combined with other antibiotics to increase their
antibiotic potency.

6. Drugs
 Sulfadiazine
 Sulfamethiazole
 Sulfamethoxazole
 Sulfisoxazole
 Sulfadimidine
 Sulfametopyrazine
 Sulfapyridine

7. Chemistry

8. Sulfapyridine

9. Mechanism of action
 Sulfonamides donot actually destroy bacteria but inhibit
their growth.
 They inhibit the growth of susceptible bacteria by
preventing the synthesis of folic acid.
 The enzyme dihydrofolic acid DHF, synthase converts
para-amino benzoic acid PABA to DHF, which
subsequently converts into tetrahydrofolic acid THF.

10. Therapeutic Uses
 Sulfonamides are used for the treatment of:
1. Urinary tract infections caused by, enterobacter spp,
klebsiella spp, proteus vulgaris, & staphylococcus aureus.
2. Nocardiosis
3. Infected burns and leg ulcers (silver sulfadiazine)
4. Inflammatory bowel disease (sulfasalazine)

11. Side-effects
 Headache
 Convulsion
 Aplastic anemia
 Nausea
 Vomiting
 Diarrhea
 Toxic nephrosis

12. Sulfamethoxazole
 Sulfamethoxazole is an intermediate acting sulfonamide
antibiotic.
 Because it is eliminated by means of kidneys and reaches
very high concentrations there, it is commonly used to
treat urinary tract infections caused by susceptible
organisms.
 It is combined phenazopyridine (analgesic) that affects the
mucosa of UTI.
 Sulfamethoxazole by it self comes as a 500mg/5ml oral
suspension and 500mg tablet.
It is a pregnancy category C.

13. Co-trimaxazole
♥ Co-trimaxazole is a combination of
Sulfamethoxazole and Trimethoprim.
♥ The optimum synergistic in vitro effect against most
susceptible bacteria is achieved with 5: 1 ratio of
Sulfamethoxazole and trimethoprim.
 Has an half life of 10 hour.
♥ Used for UTI caused by susceptible bacteria, pneumocystis carinii
pneumonia.
♥ Used for ear infection (otitis media)
♥ Used for bronchitis
♥ Used for STD including gonorrhea and syphilis.

14. Continue
♥ Available 40mg/5ml oral suspension
♥ Available 80mg trimethoprim & 400mg
Sulfamethoxazole= 480mg co-trimaxazole.
♥ Available 180mg trimethoprim & 800mg
Sulfamethoxazole = 980mg co-trimaxazole.
♥ Available 16mg/ml trimethoprim & 80mg/ml
Sulfamethoxazole= 96mg/ml injection.

15. Sulfisoxazole
 Sulfisoxazole is a short acting sulfonamide antibiotic that
is primarily used urinary tract infections.
 Used for ear infection (otitis media) in small children.
It is a pregnancy category C agent.
 Available 500mg tablet & 500mg/5ml suspension.

16. 2. Penicillin's
 The penicillin's are very large group of
chemically related antibiotics that are derived
from a fungus or mold, often seen on bread or
fruit.
 The penicillin's may also be called beta-
lactam, a term which refers to their chemical
structure.

17. Continue
 The penicillin's was first introduced on the
market in the early 1940 and to this day they
have remained very effective and safe
antibiotics.
 They are bactericidal and can kill a wide variety
of gram positive bacteria
o Half life of penicillin's is 2hr approximately.

18. Classification of drugs
 The penicillin's can be divided into:
1. Natural penicillin's
2. The amino-penicillins
3. Penicillinase resistant penicillins
4. The extended spectrum penicillin's

19. Mechanism of action
 Penicillin's involves several steps that together
result in the inhibition of bacterial cell wall
synthesis.
 They block penicillin binding proteins (PBP), by
inhibiting peptidoglycan in the cell wall bacteria.

20. Side-effects
 Anemia
 Lethargy
 Bone-marrow depression
 Hallucination
 Nausea
 Vomiting
 Sore throat
 Abdominal pain

22. I. Natural Penicillin's
 Natural penicillin's are:
1. Pen G
2. Pen V
3. Pen M
4. Pen N
5. Pen X
6. Pen F

23. Penicillin G
 Penicillin G consists of:
1. Benzathine
2. Potassium
3. Sodium
4. Procaine

24.  Penicillin G Benzathine
 Given IM injection
 Long acting drug
 Expected to work over the course for several days.
 Penicillin G K+ & Na
 Commonly administered IV for the treatment of life
threatening illnesses such as:
1. Septicemia
2. Meningitis
3. Pericarditis (Inflammation of the pericardium)
4. Severe pneumonia

25. II. Aminopenicillins
 There are three aminopenicillins:
1. Amoxicillin
2. Ampicillin
3. Bacampicillin
 Because of the presence of a free amino group on
the penicillin's nucleus, the aminopenicillins have
enhanced activity against gram negative bacteria.
 Amoxicillin is an analogue of ampicillin and
bacampicillin is a prodrug of ampicillin.
 The aminopenicillins are contraindicated:
1. Hypersensitivity
 They are rated in a pregnancy category B drugs.

26. Ampicillin
 Ampicillin is the prototypical amino penicillin, that has
amino group.
o It is available in three different forms:
1. Anhydrous (without water)
2. Trihydrate (A hydrate whose solid contains three molecules of
water of crystallization per molecule)
3. Sodium
 Anhydrous and trihydrate Ampicillin are administered
orally.
Ampicillin sodium is given parenterally.
 Available 250mg, 500mg capsules, 250mg/5ml
suspension, 125, 250, 500, 1000, 2000, 10,000mg vial
for injection.
 Adult dosage is PO: 250mg- 500mg Qid, IM/IV:
250mg-500mg Qid.

27. III. Penicillinase Resistant Penicillin's
 These congeners have side chains that protect the beta-
lactam ring from attack by staphylococcal penicillinase.
 However this also partially protects the bacteria from the
beta lactam ring.
 Their only indication is infectious caused by penicillinase
producing staphylococci, for which they are the drugs of
choice except in areas where methicillin resistant staph
aureus (MRSA) has become prevalent.
Methicillin resistant staphylococcus aureus; a bacterial
infection that is resistant to common antibiotics

28. Methicillin
 It is highly penicillinase resistant but not acid
resistant, must injected. it is also an inducer of
penicillinase production.
 The MRSA have altered PBPs which donot bind
penicillins.
 The drug of choice for these organisms is
vancomycin/linezolid, but ciprofloxacin can also
be used.
 Hematuria, albuminuria, and nephritis are the side
effects of methicillin.
Methicillin: Antibiotic drug of the penicillin family used in the
treatment of certain staphylococcal infections

29. Cloxacillin
 It has an isoxazolyl side chain and is highly
penicillinase as well as acid resistant.
 It is more active than methicillin against
penicillinase producing staph.
Cloxacillin is incompatibly but dependably
absorbed from oral route, especially if taken in
empty stomach.
 Plasma half life is about 1 hour.
 Elimination occurs primarily by kidney, also partly
by liver.
 It is available 0.25g, 0.5g cap and injections.

30. PROCAINE PENICILLIN ALLERGIC
REACTION
 ID/CC: A 21 year old male comes to the health clinic
because of the development of fever, marked itching all
over his body, generalized rash with joint swelling and
difficulty breathing.
 HPI: he just returned from a trip abroad, where he had
developed a purulent urethral discharge and went to a
local doctor who gave him two pills of procaine penicillin.
 PE: mild hypotension, mild cyanosis and difficulty
breathing.
 Imaging: CXR is normal

31. Continue
Treatment: Subcutaneous epinephrine, oxygen,
hydrocortisone, antihistamines.
Maintain airway and provide assisted ventilation if
necessary.
Severe reactions may result in laryngeal obstruction,
hypotension and death.

32.  Penicillinase-resistant penicillins
include meticillin, nafcillin and oxacillin.
 These are primarily used in the treatment of
infection caused by penicillinase-producing
staphylococci.
 Ampicillin was the first broad-spectrum
penicillin and has a broader antibacterial
range of action than that of penicillin G

33. Continue
 Discussion: Penicillin’s are antimicrobial drugs that block
cell wall synthesis by inhibiting peptidoglycan cross linking;
they are bactericidal for gram positive cocci and rods,
gram negative cocci.
 Most adverse reactions to penicillin are allergic reactions
that result when one of it is metabolites acts as hapten.
 Anaphlytic reaction involves antigen reacting with IgE on
presensitized mast cells and basophils, it is usually severe
and immediate.

34. METHICILLIN RESISTANCE
STAPHYLOCOCCUS AUREUS (MRSA)
 ID/CC: A 25 year old male presents with spiking
fevers, malaise, left sided chest pain and cough.
 HPI: His symptoms started two weeks ago and have
progressively worsened despite a full course of oral
antibiotics. He also reports a history of prior IV drug
abuse.
 PE:VS: Fever (39 centigrade), Tachycardia (HR 105),
tachypnea. PE: amphoric, breath sounds heard over
left lower lobe; S1 & S2 normally heard without
murmurs, gallops or rubs.
 Labs: induced sputum cultures grew methicillin
resistant staphylococcus aureu.

35. Continue
 Imaging: XR, chest: 2 by 3cm cavity in left lower lobe
of lung with air fluid level. CT, chest: confirmed a left
lower lobe lung abscess.
 Treatment: Intravenous Vancomycin therapy, add
aminoglycoside for synergistic bactericidal effect.
 Discussion: Antibiotic resistant is continuing to
increase in both the hospital and the community. Major
resistant nosocomial organisms include s.aureus,
klebsiella, and pseudomonas.
 MRSA is becoming widespread in a number of
communities and is more commonly seen in IV drug
abusers, patients with recent hospitalizations.

36. 3. Cephalosporin's
 The cephalosporin's are semi-synthetic antibiotic
derivatives of cephaloporin C.
 These chemically altered derivatives of this fungus are
broadly referred to as cephalosporin's and they are
structurally and pharmacologically related to the
penicillin's.
 Cephalosporin's have a broad spectrum of bacteria.
 The safety profiles, contraindications and pregnancy
ratings of cephalosporin's are very similar to those of
penicillin's.

37. What is cephalosporin C used
for?
 Cephalosporins are used to treat bacterial
infections such as respiratory tract
infections, skin infections and urinary tract
infections.
 When a cephalosporin or any other antibiotic
is given as a treatment, the medication should
be taken for the fully prescribed time even if
symptoms disappear.

38. Continue
 Because of cephalosporin's are chemically very similar to
penicillin's, a person who has had an allergic reaction to
penicillin's have also allergic reaction in cephalosporin's,
this is referred to as cross sensitivity.
 Cephalosporin's of all generations are very safe agents
that are categorized as pregnancy category B agents.
 They are contraindicated:
1. Hypersensitivity
2. Younger than 1 month old

39. Classification of Drugs
 Cephalosporin's can be classified into:
1. First generation
2. Second generation
3. Third generation
4. Fourth generation

40. First Generation
 Drugs
1. Cefazolin sodium
2. Cephalothin
3. Cephalexin
4. Cephradine
5. Cephapirin
 First generation are usually active against gram positive
bacteria and have limited activity against gram negative
bacteria.
 They are available both parenteral and oral.

41. Cefazolin sodium
 First generation of cephalosporin
 Excellent coverage against gram positive and poor
coverage of gram negative.
 Only available in parenteral formulation that comes
500-1000mg vials for IM or IV injection.
Adult dosage is IM/IV: 250mg-1g q8h-q12h.

42. Second Generation
Drugs
1. Cefoxitin
2. Cefamandole
3. Cefuroxime
4. Cefonicid
5. Ceforanide
6. Cefmetazole
7. Cefaclor
8. Cefprozil

43. Continue
 The second generation cephalosporin's have
similar coverage against gram positive organisms
but enhanced gram negative bacteria.
They include both parenteral and oral formulations.
 The second generation cephalosporin's are also excellent
prophylactic antibiotics.
 The qualities that make them excellent
prophylactic agents are:
1. Safety profile
2. Broad range of organisms they can kill
3. Relatively low cost.

44. Cefoxitin
 It is a parenteral second generation
cephalosporin.
 Cefoxitin has been used extensively as a prophylactic
antibiotic in patients undergoing such surgical
procedures especially in abdominal and colorectal
operations.
 It is rated pregnancy category B.
 Available only in parenteral formulations 1,2, 10g vials for
injection

45. Third Generation
 Drugs
1. Cefoperazone
2. Cefotaxime
3. Ceftizoxime
4. Ceftriaxone
5. Ceftazidime
6. Cefixime
 Third generation cephalosporin's are the most potent in
fighting gram negative bacteria.

46. Ceftriaxone
 Ceftriaxone is a parenterally administered third generation
cephalosporin that differs from the other agents in that it has
a very long half life that allows it to be given once a day.
 It can be given both intravenously and intramuscularly.
 It can easily pass meningitis and BBB (blood-brain barrier),
making it an excellent agent for the treatment of CNS
infection.
 Available 250, 500mg, 1, 2, 10 gram vials.
 Adult dosage is: IM/IV 1-4 g/day as a single dose or
divided doses.

47. 4. Tetracycline's
The tetracycline's are small chemically
related group of five antibiotics, three of
which are naturally occurring and two of
which are semi-synthetic.
They are derivatives of streptomyces
organisms.
Tetracycline's can only inhibit the growth of
bacteria, they can’t kill bacteria, therefore they
are considered bacteriostatic.
Aerobic bacteria (some of which produce
the antibiotic streptomycin)

48. Continue
 The three naturally occurring
tetracycline's are:
1. Tetracycline
2. Demeclocycline
3. Oxytetracycline
 The two semi-synthetic tetracycline's are:
I. Doxycycline
II. Minocycline
Semi-synthetic medicines are derived from natural products, which often
provide a useful starting point for the discovery of physiologically effective
molecules and therefore play an important role in the development of new
medicines

49. Mechanism of action
 Tetracycline's work by inhibiting protein
synthesis 30S in susceptible bacteria
Synthesis: The process of producing a
chemical compound (usually by the union
of simpler chemical compounds)
 The 30S ribosomal subunit has two primary functions
in protein synthesis. It discriminates against aminoacyl
transfer RNAs that do not match the codon of
messenger RNA, thereby ensuring accuracy in
translation of the genetic message in a process called
decoding

50. Therapeutic uses
 Chlamydia
 Syphilis
 Lyme
 Rickettsiae
 Protozoa
 Acne
 Cholera
 Shigellosis
 Mycoplasma pneumonia
Lyme disease is caused by the bacterium Borrelia burgdorferi
and rarely, Borrelia mayonii. It is transmitted to humans
through the bite of infected blacklegged
Shigellosis : An acute infection of the intestine by
shigella bacteria; characterized by diarrhea and fever
and abdominal pains

51. Side-effects
 Discoloration of teeth
 Tooth enamel hypoplasia (Underdevelopment of an organ
because of a decrease in the number of cells)
 Retard fetal skeletal development
 Photosensitivity (Sensitivity to the action of radiant energy)
 Alteration of the intestinal flora
 Diarrhea
 Gastric upset
 Reduced bacterial vitamin K synthesis

52. Doxycycline
 Doxycycline is a semi synthetic tetracycline antibiotic.
 Doxycycline comes in the following three different salt
forms:
1. Calcium
2. Hyclate
3. Monohydrate
 It is useful in the treatment of rickettsial infections,
gonorrhea and many gram negative infections.
 It comes orally as a 25 and 50mg/5ml oral suspension,
50, 100mg capsules and 100, 200mg per ml injections.
 It is rated in a pregnancy category D drug

53. 5. Aminogylcosides
 Aminoglycosides are group of natural and semi-synthetic
antibiotics that destroy bacteria, rather than inhibit their
growth, so they are Bactericidal.
 They are derived from streptomyces organisms.
 They are not given orally because of their poor oral
absorption.
 They can kill both gram positive and gram negative
bacteria but are customarily used to kill gram negative
such as, pseudomonas, E. coli and klebsiella.
Pseudomonas: Type genus of the family Pseudomonodacea

54. Continue
 The aminogylcosides work in a way that is similar to that
of tetracycline's in that they also bind to ribosomes and
thereby prevent protein synthesis in bacteria.
 The aminogylcosides have been shown to cross the
placenta and cause fetal harm when administered to
pregnant women.
 The pregnancies categories of the various
aminogylcosides are as follows:
1. Gentamycin, Neomycin: Pregnancy category C
2. Tobramycin, Amikicin, kanamycin: pregnancy D
3. Streptomycin: pregnancy category B

55. Drugs
 Gentamycin
 Tobramycin
 Amikacin
 Kanamycin
 Neomycin
 Streptomycin

56. Mechanism of action
 Aminoglycosides kill bacteria by binding
and disrupting protein synthesis in bacteria
specifically they do this by binding to both
30s and 50s ribosomal subunit.

57. Side-effects
 Renal failure
 Hearing loss (Ototoxicity)
 Nausea
 Vomiting
 Proteinuria
 Increase serum creatinine level

58. Gentamycin
 Gentamycin is a naturally occurring aminoglycoside
that is obtained from cultures of micromonospora
purpurae.
 It is one of the Aminoglycosides most commonly
used in clinical practice today.
 It is classified pregnancy category C.
 Available 10, 40mg/ml injection IM/IV, 10, 60, 80 mg per
ml intravenous infusion.
 Available 3% solution or ointment for ophthalmic.
 Comes also 0.1% ointment for topical application on:
1. Superficial skin infection
2. Burns
3. Skin ulcers

59. GENTAMICIN SIDE EFFECTS
 ID/CC: A 34 year old women presents with her
family practitioner complaining of hearing loss,
vertigo and inability to walk properly due to lack of
balance.
 HPI: She took IV Gentamicin for 10 days
 PE: Well hydrated, oriented and cooperative
 Imaging: normal

60. Continue
 Treatment: Discontinuation of the drug, supportive
therapy.
 Discussion: Gentamicin is an aminoglycoside
and thus shares the Ototoxicity and Nephrotoxicty
of streptomycin, kanamycin, Amikacin, and
tobramycin.
 Ototoxicity is mainly cochlear and marked by
ataxia and vertigo.
 Nephrotoxicity is minimized if care is taken to
hydrate the patient and keep serum levels
therapeutic.

61. 6. Quinolones
The quinoline antibiotics are very potent broad spectrum
antibiotics.
 They are bactericidal
o The first of these agents to come available were:
1. Cinoxacin
2. Nalidixic acid
 The newer quinoline antibiotics include:
1. Norfloxacin
2. Ciprofloxacin
3. Enoxacin
4. Ofloxacin
5. Lomefloxacin
6. Perfloxacin.

62. Continue
A fluorine atom was added on to the basic quinolone
structure to create these newer agents and increased
their anti-bacterial activity.
Because of chemical, these agents are sometimes called
fluoroquinolones.
They are active against a wide variety of G-VE and
selected G+VE bacteria.
They are primarily excreted by the kidneys, which contain
a high percentage of unchanged drug, this makes them
good for treating of UTI.
 Their use in children is not currently recommended
because they have been shown to suppress growth in
laboratory animals.

63. Mechanism of action
 Quinolone antibiotics destroy bacteria by altering
DNA and they accomplish this by interfering with
DNA gyrase, enzyme necessary for the synthesis
of bacterial DNA, if bacteria cannot produce
DNA they die.

64. Side-effects
 Dizziness
 Insomnia
 Fatigue
 Nausea
 Rash
 Fever
 Blurred vision

65. Ciprofloxacin
 Ciprofloxacin was one of the first potent
fluoroquinolones to come available.
 First marketed in an oral form and advantage of
convenience of oral preparation plus excellent
bioavailability.
 Effective against to kill gram negative bacteria.
 Orally comes 250, 500, 750mg tablet, parenterally
comes 200, 400mg.
 The common dosage is 250mg-750mg Tid, Bid.

66. FLUOROQUINOLONE SIDE
EFFECTS
 ID/CC: A 21 year old college baseball player restarted his
training 3 days ago, running 1600 meters a day in
preparation for the upcoming state tournament, yesterday
he hit a home run and started off to first base when he
suddenly fell to the ground and couldn’t work due to
acute pain.
 HPI: He had spent 4 weeks in the hospital recovering from
perforated appendicitis where he received IV ciprofloxacin
for 2 weeks due to surgical wound infection with
pseudomonas aeruoginosa that was resistant to all other
antibiotics.

67. Continue
 PE: Surgical wound completely healed with no
evidence of infection or post incisional hernia;
penrose drain orifice within normal limits; inability
to plantarflex left foot; Achilles tendon completely
severed.
 Labs: CBC: no leukocytosis; no anemia. SMA-7
normal.
 UA: normal.
 Imaging: CXR/KUB: within normal limits.
 Micro Pathology: Achilles tendon shows
inflammatory neutrophilic infiltrate with areas of
hemorrhage and necrosis.

68. Continue
 Treatment: Surgical repair.
 Discussion: Fluoroquinolones such as ciprofloxacin
and Norfloxacin are bactericidal antibiotics that are
active against gram negative rods, including
pseudomonas; they are also active against
Neisseria and some gram positive organisms.
 They act by binding DNA gyrase.
 Side-effects include damage to cartilage,
tendonitis, and tendon rupture; they also produce
gastric upset and nausea and may cause super
infection.

70. 7. Macrolides
 The Macrolides are a large group of antibiotics
that first came available in the early 1950s with
the introduction of erythromycin.
 Macrolides have a macrocyclic lactone.
Macrolides are considered bacteriostatic but in
high concentration may be bactericidal in some
susceptible bacteria.
 Macrolides are POM drugs.
Macrolides are rated pregnancy category C.

71. Drugs
 Erythromycin
 Clarithromycin
 Azithromycin
 Troleandomycin
 Roxithromycin

72. Mechanism of action
 They bind 50s ribosomal subunit inside the
cells of bacteria and by doing so prevent the
production of the bacterial protein needed for
bacteria to grow, with the result that bacteria
eventually will die.

73. Antibacterial spectrum
 It is narrow, includes mostly gram positive and
a few gram negative bacteria.
 It is highly active in the following bacteria's:
1. str. pyogenes
2. Str. Pneumoniae
3. N. gonorrhoeae
4. Clostridia
5. C. dipthteriae

74. Uses
1. As an alternative to penicillin: streptococcal
pharyngitis, tonsillitis, community acquired
respiratory infections caused by pneumococci and H.
influenza, however many bacteria resistant to
penicillin are also resistant to erythromycin.
2. Diphtheria: erythromycin 250mg Qid, acute stage
as well as for carriers 7 day treatment, antitoxin is
the primary treatment.
3. Tetanus: erythromycin 500mg is given Qid for 10
days to eradicate clostridium tetani.
4. Syphilis and gonorrhea
5. Atypical pneumonia caused by mycoplasma
pneumoniae.

75. Continue
6. Whooping cough: 1 to 2 week course of
erythromycin is the most effective treatment for
eradicating Pertussis from upper respiratory tract.
7. Chlamydia trachomatis infection of urogenital
tract: erythromycin 500mg QID for 7.
8. Penicillin resistant staphylococcal infections
9. Helicobacter pylori infection: Clarithromycin
500mg in combination in Omeprazole 20mg, and
amoxicillin 1g each administered twice a day for 10 to
14 days, is effective for the treatment of peptic ulcer
disease.
10. Mycobacterial infection: Azithromycin or
Clarithromycin are recommended for the 1st line of
prophylaxis and RX of pulmonary disease. E.g AIDS.

76. Continue
7. Chlamydia trachomatis infection of urogenital
tract: erythromycin 500mg QID for 7.
8. Penicillin resistant staphylococcal infections
9. Helicobacter pylori infection: Clarithromycin
500mg in combination in Omeprazole 20mg, and
amoxicillin 1g each administered twice a day for 10
to 14 days, is effective for the treatment of peptic
ulcer disease.
10. Mycobacterial infection: Azithromycin or
Clarithromycin are recommended for the first line of
prophylaxis and treatment of pulmonary disease. E.g
AIDS.

77. Side-effects
 Headache
 Dizziness
 Palpitation
 Heart burn
 Nausea
 Anorexia
 Vomiting
 Rash
 Hearing loss

78. Drug-Drug Interactions
 Clarithromycin and erythromycin inhibit
CYP3A4.
 Erythromycin potentiates the effects of
Carbamazepine, corticosteroids, digoxin,
Theophylline, Warfarin.
CYP3A4 is a major cytochrome P450. It catalyses a broad
range of substrates including xenobiotics such as clinically
used drugs and endogenous compounds bile acids. Its
function to detoxify bile acids could be used for treating
cholestasis, which is a condition characterised by
accumulation of bile acids.

79. Erythromycin
 Most frequently prescribed macrolide antibiotic.
 It comes in several different salt and dosage forms that
were developed to circumvent some of the drawbacks
it has chemically.
 The absorption of oral erythromycin is enhanced if it is
taken on an empty stomach, but because of the high
incidence of stomach irritation, many of the agents are
taken after meal or snack.
 Dosage range is:
1. Children: 30-100mg/kg/day divided dose
2. Adult: 500mg as single dose or Bid

80. 8. Miscellaneous Drugs
 Vancomycin
 Clindamycin
 Metronidazole
 Chloramphenicol

81. Vancomycin
 It is a natural bactericidal antibiotic structurally
unrelated to any other commercially available
antibiotics.
 It is a glycopeptide antibiotic discovered in
1956.
 It destroys bacteria by binding to the bacterial
cell wall producing immediate inhibition of cell
wall synthesis and death.
 It is the antibiotic of choice for the treatment of MRSA.

82. Continue
 The parenteral form is indicated for the
treatment of bone and joint infections and
bacterial blood stream infections caused by
staphylococcus spp.
 Classified pregnancy category B.
 Caution use:
1. Renal dysfunction
2. Hearing loss
3. Elderly patients

83. Continue
 Contraindicated for hypersensitivity
 Available 125, 250mg capsules and 500mg, 1g for
intravenous infusions.
 Adult dosage is 0.5-2g per day in Tid for 7-10
days.

84. Mechanism of action
Vancomycin inhibits the cell wall synthesis by
binding with high affinity, D-alanyl D-alanine.
 Vancomycin is a bactericidal.
D-alanyl: It is a component of
bacterial peptidoglycan and forms
an important target for
development of antibacterial
drugs. It has a role as an
Escherichia coli
D-Alanine Aminopropionic acid) | Suitable
for detection | Alanine is a non essential
amino acid | D-Alanine is the non-
proteinogenic form of alanine
affinity: chemical attraction

85. Toxicity
 Systemic toxicity of Vancomycin is high. It can cause
plasma concentration dependant nerve deafness which
may be permanent.
 Kidney damage is also dose related.
 Skin allergy and fall of blood pressure during IV injection.
 Rapid IV injection has caused chills, fever and intense
flushing- Red man syndrome (an adverse anaphlytical
reaction to Vancomycin therapy causing pruritis, flushing
of the head and the upper part of the body, the condition
is caused by the release of histamine).

86. Uses
 MRSA
 Bacterial meningitis combination therapy
with Ceftriaxone or Cefotaxime.
 Used for dialysis patients
 Those undergoing chemotherapy for
cancer patients.
 Penicillin allergic patients
Methicillin resistant staphylococcus aureus; a bacterial
infection that is resistant to common antibiotics

87. Chloramphenicol
 Chloramphenicol was initially obtained from
streptomyces venezuelae in 1947.
 It was soon synthesized chemically and
the commercial product now is all
synthetic.
 It has a nitrobenzene substitution, which is
probably responsible for the antibacterial
activity and it is intensely bitter taste.

88. Mechanism of action
 Chloramphenicol inhibits bacterial protein
synthesis by interfering with transfer of
the elongating peptide.
 It specifically attaches 50S ribosome.

89. Pharmacokinetics
 Chloramphenicol is rapidly and completely
absorbed after oral ingestion.
 Chloramphenicol is primarily conjugated with
glucuronic acid in the liver and little is
excreted unchanged in urine.
 Plasma half life of chloramphenicol is 3-5
hours in adults.
 It is increased only marginally in renal failure.
Glucuronic acid is a uronic acid that was
first isolated from urine It is found in many
gums such as gum arabic ( approx. 18%),
xanthan, and kombucha tea

90. Therapeutic Uses
 Enteric fever- Typhoid
 Pyogenic meningitis: Chloramphenicol
50-75mg/kg per day may be used after
the third generation of cephalosporin's.
 Anaerobic infections: Wound infections,
pelvic and brain infections.
 Intraocular infections: Chloramphenicol
is given systemically.

91. Adverse Effects
Bone marrow depression
Hypersensitivity reactions like, fever, rashes, glossitis
Nausea
Vomiting
Diarrhea
Pain on injection
Gray baby syndrome: the baby stop feeding, vomited,
hypothermic, abdomen distended, respiration become
irregular and gray cyanosis occur.

92. CHLORAMPHENICOL SIDE
EFFECTS
 ID/CC: A 31 year old truck driver visits a health
clinic in Buroa Togdheer region, complaining of
recurrent infections, excessive bleeding, weakness
and anemia.
 HPI: He travels the border of Ethiopia daily and
eats and sleeps there. He has had a typhoid fever
three times over the past five years, for which he
has been treated with high dose of
chloramphenicol.
 PE: Normal
 Labs: Anemia

93. Continue
 Treatment: Blood transfusions, cyclosporin for
bone marrow transplantation.
 Discussion: Chloramphenicol is a bacteriostatic
antibiotic that acts by inhibiting peptidyl
transferase in the 50s ribosomal unit. It is active
against anaerobes and rickettsiae as well as
against typhoid fever and meningococcal.
 In infants they produce gray baby syndrome.
Owing to its potentially fatal side-effect of Aplastic
anemia, chloramphenicol is used primarily for
serious infections or acute salmonella typhi
infection.

94. END
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