marka

1. Antimicrobial Agents
Dr.Mutaz AL-shawabekah

2. Mode of Action
 Antimicrobials affect the viability of microorganisms
by five known processes:
 (1) inhibition of cell wall synthesis,
 (2)alteration of cell membrane integrity,
 (3) inhibition of ribosomal protein synthesis,
 (4) suppression of deoxyribonucleic acid (DNA)
synthesis
 (5) inhibition of folic acid synthesis

3.  Microbial cell wall synthesis inhibition and
membrane effects are extracytoplasmic, and
inhibition of nucleic acid, protein, and folic acid
synthesis is intracytoplasmic.

4.  Drugs that affect bacterial cell wall or membrane
integrity and DNA synthesis are usually, but not
always, bactericidal (inducing cell death), and
protein and folic acid synthesis inhibitors are
usually bacteriostatic (preventing cell growth or
replication).
 Whether an antimicrobial agent is bactericidal (cidal)
or bacteriostatic (static) can also depend on its
concentration at the infected site and the particular
offending organism because some static drugs
become cidal at high concentrations.

5.  Cell membrane
 Amphotericin B
 Azoles
 Nystatin
 Polymyxins

6.  Protein synthesis
 Aminoglycosides
 Chloramphenicol
 Clindamycin
 Macrolides
 Tetracyclines
 lincomycin

7.  Cell wall synthesis
 Bacitracin
 Carbacephams
 Cephalosporins
 Imipenem
 Penicillins
 Vancomycin
 Cycloserine
 aztreonam

8.  Nucleic acid synthesis
 Flucytosine
 Fluoroquinolones
 Metronidazole
 Nalidixic acid
 Rifampin
 Intermediary metabolism
 Aminosalicylic acid
 Sulfonamides
 Sulfones
 Trimethoprim

9. PATTERNS OF ANTIBIOTIC USE AND
MISUSE
 Inappropriate antibiotic use in dentistry includes the
following
 situations:
 (1) antibiotic therapy initiated after surgery to
prevent an infection unlikely to occur and not
documented effective for this purpose by clinical
trials;
 (2) failure to use prophylactic antibiotics according
to the principles established for such use;
 (3) use of antibiotics as analgesics in endodontics;
 (4) overuse in situations in which patients are not at
risk for metastatic infections;

10.  (5) treatment of chronic periodontitis almost totally
amenable to mechanical therapy;
 (6) administration of antibiotics instead of
mechanical therapy for periodontitis;
 (7) long-term administration in the management
 of periodontal diseases;
 (8) antibiotic therapy instead of incision and
drainage;
 (9) administration of antibiotics to avoid claims of
negligence;
 (10) administration in improper situations, dosage,
and duration of therapy.

11.  MICROBIAL RESISTANCE TO ANTIBIOTICS:
 Microorganisms have developed seven known
mechanisms to evade the bactericidal or bacteriostatic
actions of antimicrobials, as follows:
 (1) enzymatic inactivation,
 (2)modification/protection of the target site,
 (3) limited access of antibiotic (altered cell membrane
permeability),
 (4) active drug efflux,
 (5) failure to activate the antibiotic,
 (6) use of alternative growth requirements,
 (7) overproduction of target sites

12. Penicillins
 All penicillins are derivatives of 6-aminopenicillanic acid and
contain a beta- lactam ring (( beta-lactam ring a four
membered imbedded ring structure consisting of 3 carbons
and one nitrogen atom which is responsible for the
antibacterial activity))structure to thiazolidine ring. The beta-
lactam ring is essential for its antibacterial activity. This basic
structure is synthesized by the penicillium mold from two
amino acid (L-cysteine and L-Valine).
 Penicillins are bactericidal and they inhibit cell wall
synthesis
 Antibiotics containing this beta-lactam ring are referred to
collectively as beta-lactam antibiotics and include the
penicillins and cephalosporins and the two newer groups of
agents , the carbapenems and monobactams.
 Penicillinase is an enzyme secreted by bacteria which splits
open the beta-lactam ring. This renders the penicillin molecule
ineffective against those penicillinase secretors.

13.  Penicillin G( benzylpenicllin) is the prototype for
comparison. By side chain substitutions ( substituting
other groups at the R position of the penicillin
molecule) of the basic 6- aminopenicillanic acid
molecule, the semi-synthetic penicillins are produced
which are more acid stable have broader
spectrum or are penicillinase resistant.

14.  Other naturally occurring penicillin :
 Penicillin VK : preferred for treating oral infections
because it is more acid stable
 Penicillin G parental : always given by IM route
 Penicillin G benzathine: always given by IM route.
Used to treat Syphilis and prevention of rheumatic
fever

15.  Acid stable penicillins :
 Penicillin VK : has a relative limited spectrum of action
against aerobic gram-positive cocci and anaerobes
 Amoxicillin: is an aminopenicillin which has an extended
spectrum of action which includes not only aerobic gram
positive cocci and anaerobes but some gram negative
bacilli (Hemophilus Proteus Salmonella)
 Ampicillin is an aminopenicillin
 Nafcillin
 Oxacillin
 Cloxacillin
 Dicloxacillin has a similar spectrum as penicllin VK but
is active against penicillinase producing staphylococcus

16.  Extended Spectrum penicillin
 The aminopenicillins(-ampicillin and amoxicillin).
 Aminopenicllins (Ampicillin and Amoxicillin )are characterized by the
amino substitution of penicillin G .They work against many Gram
positive organisms and some Gram Negative bacteria such as
Haemophilus influenze, some E-coli and Proteus mirabilis. They are
not penicillinase resistant. They are used for upper respiratory
infections.
 The major difference in the Drugs is the higher oral absorption,
higher serum levels and longer Half life for amoxicillin compared
with ampicillin. Amoxicillin is given Orally while Ampicillin can be
given Orally and IV.
 Oral Amoxicillin is recommended as the drug of choice for standard
general prophylaxis for Bacterial Endocarditis in patients undergoing
invasive dental procedures.
 Parenteral Ampicillin is recommended as the drug choice in patients
unable to take Oral medications and who are not allergic to penicillin
.

17.  Broad spectrum penicillin:
 Piperacillin
 Ticarcillin
(they have the widest spectrum of all the penicillin )
They are active against gram positive cocci
(streptococci and staphylococci and pneumococci)
and gram positive rods ( bacillus and others) and
Pseudomonas Proteus Klebsiella, Bacteroides.
They are recommended for the Urinary tract Infections
.

18.  Penicillinase-resistant penicillins include:
 -
Nafcillin
Oxacillin
Cloxacillin
dicloxacillin
--Cloxacillin and Dicloxacillin resist the
actions of penicillinase because they
have a protected beta-lactam ring which
prevents the actions of the enzyme.

19.  Augmentin and Unasyn: contain the agents
clavulanate potassium and sulbactam
respectively which blocks the actions of
penicillianase from reaching the beta lactam ring.

20.  The majority of penicillins are directly excreted into
the urine through renal tubular cell secretion.
 Note: Probenecid (an inhibitor of renal tubular cell
secretion) raises the blood level of the penicillins by
diminishing their tubular secretion.

21.  Three Groups of allergic Reactions to the penicillins:
 1)Acute (anaphylactic shock): occurs within 30 minutes. Characterized
by urticaria.angioedema,bronchoconstriction, GI disturbances and shock.
Death can result in a short time if treatment is not instituted immediately(
Parenteral administration of Epinephrine). This reaction most commonly
occurs with parenteral administration of penicillin.
 2) Accelerated: occurs 30to 48 hours after .manifestations include
urticaria .pruritis, wheezing .mild laryngeal edema and local inflammatory
reactions. Not life threatening .
 3)Delayed :occurs after 2-3 days . Approximately 80-90% of all allergic
reactions occurring with penicillin are of this type. Manifested by skin Rash.
 Hypersensitivity reactions occur in up to 10% of patients receiving penicillin
.manifestations range from a mild rash to anaphlylaxisl. The rash may be
urticarial,vesicular,bullous,or maculopapular.Rarely thromboepnic purpura
develops.
 The major Disadvantages of penicillin is their high incidence of allergic
reaction

22. Tetracyclines:
 Are group of a broad-spectrum, bacteriostatic
antibiotics that inhibit protein synthesis in the
susceptible organism by binding to the 30s ribosome
subunit, thereby impeding the binding of aminoacyl
tRNA to the receptor site on the messenger RNA
ribosome complex. The inhibition of this ribosomal
functions interferes with the attachment of the growing
amino acid chain thus preventing complete formations of
peptides from the ribosomes. Since no peptides are
formed , no protein are formed. since proteins are
necessary for the bacterial cell to metabolically function,
the lack thereof will cause a static state in which the
bacterium becomes vulnerable to phagocytosis by the
body`s immune system.

23.  Absorption of the tetracyclines from the GI tract in
inhibited by divalent and trivalent cations such as
Ca, Mg, Fe, Al. this is why tetracycline should not be
given with milk and dairy products (contain Ca), iron-
containing Vitamins ( contain Fe),mineral
supplements containing these irons, or antacids
(contain Mg)

24.  Tetracyclines are useful in treating the following
infections:
 Medical infections caused by Gram Positive and Gram
Negative bacteria
 Infections caused by Mycoplasma, Chlamydia,Protozoa
or Rickettsia.
 Exacerbations of Chronic Bronchitis
 Lyme Disease
 Treatment of Acne
 Treatment of Gonorrhea and syphilis in patients allergic
to penicllin
 Dentally: treatment of periodontits associated with the
presence of Actinobacillus Actionmycetemcomiyans (AA)
 Note: tetacyclines are not the drug of choice for
streptococcus or Staphylococus.

25.  Side effect:
 Nausea
 Diarrhea
 Discoloration of teeth and enamel hypoplasia in
young children
 A photosensitivity reaction can be caused by the
tetracycline, resulting in red rashes or blotches over
the skin in the presence of sunlight.

26.  Tetracyclines are contraindicated in children up to 8
years old and in pregnant women. Tetracyclines
have the ability to chelate calcium ions and become
incorporated in the bony tissues. The teeth of
children who have been given the drug may develop
a Greenish-brown discoloration this is seen in the
newly erupted teeth of infants whose mothers have
received tetracycline during pregnancy.

27.  Members of the tetracycline family of antibiotics:
 Short acting: Tetracycline
 Intermediate acting: Demeclocycline(declomycin)
 Long acting: Minocycline( minocin)
Doxycycline( Vibramycin)

28. Chloramphenicol
 Broad-spectrum antibiotic effective against Gram
positive and Gram Negatives bacteria and against
anaerobes.
 It is used as asecond or third line drug in medicine to
treat serious infections due to organisms resistant to
other less toxic antibiotics
 Used to treat: Typhoid Fever, Bacterial Meningitis,
Anaerobic Infections, Rickettesial Diseases, and
Brucellosis
 It inhibits protein synthesis in bacteria and to a lesser
extent in eukaryotics cells,the drug readily penetrates
bacterial cells probably by facilitated diffusion. It acts
primarily by binding reversibly to the 50s ribosomal
subunits.

29.  The most important adverse effect of chloramphenicol is on
the bone marrow. it affects the hematopoietic system in 2
ways:
 By an non-dose related idiosyncratic response manifested by
aplastic anemia , leading in many case to fatal
pancytopenia
 By a dose-related toxic effect that presents as anemia ,
lukopenia, thrombocytopenia.
 The risk of aplastic anemia does not contraindicate the use of
chloramphenicol in situations in which it is necessary;
however, it emphasizes that the drug should never be
employed in undefined situations or in disease readily ,safely,
and effectively treatable with other antimicrobial agents.
 Fatal chloramphenicol toxicity may develop in neonates
when they are exposed to excessive doses of the drug. The
illness( Gray Baby syndrome) usually begins 2-9 days after
treatment is started.

30. Clindamycin
 Binds to the 50s ribosomal subunit, blocking bacterial protein synthesis .
 Its use is restricted by its side effects such as severe diarrhae and
pseudomembranous colitis.
 These side effects are caused by the overgrowth of the bacterium known as
Clostridium difficile
 Its bacteriostatic and is active against gram positive( streptococcus,
pneumoniae, viridans, pyogenes as well as staphylococcus aureus) and
anaerobic organism including anaerobic gram negative bateria Bacteroides
fragilis.
 In dentistry, clindamycin ia as alternate antibiotic in the following
situations:
 When amoxicillin cannot be used for the standered regimen for prevention of
bacterial endocarditis in patients undergoing dental procedures.
 For treatment of common oral facial infections caused by aerobic gram
positive cocci and anaerobes
 For prophylaxis for dental patients with total joints replacement.
 There is no cross allergenicity between penicillin and clindamyin

31. Vancomycin
 Vancomycin is given IV and issued most often in
serious or life threatening Staphylococcal or
streptoccocal infections
 It remains the drug of choice for severe cases of
Clostridium difficile
 Vancomycin inhibits bacterial cell wall synthesis
 Adverse effects: ototoxicity and Red man
syndrome (sudden and profound fall in blood
pressure with or without a maculopapular rash over
the face neck upper cheat and extermities.

32. Sulfonamides
 Is often referred as a sulfa drugs because their molecules contain
sulfur atoms.
 The sulfonamides are structurally similar to PABA and this
similarity is the basis for their antibacterial actions
 PABA is needed by bacteria for the synthesis of folic acid, in turn folic
acid is needed for the synthesis of cellular components within the
bacteria to allow for cell growth. Because of structural similarities
between sulfonamides and PABA . The sulfonamides compete with
PABA and are able to inhibit the actions of PABA, with PABA
inhibited . Folic acid is not synthesized within the bacteria and
bacterial cellular growth is inhibited.
 It is bacteriostatic
 It is not used for treatment of dental infections because of a low
degree of effectiveness against oral pathogens.
 It is used in medicine primarily for the treatment of urinary tract
infection
 Hypersensitivity reactions are common although blood dyscrasias
are relatively rare, they can be fatal

33. Aminoglycosides
 Potent bactericidal antibiotics that act by creating fissures in the outer
membrane of the bacterial cell
 They are particularly active against aerobic ,gram-negative bacteria and act
synergistically against certain gram positive organism
 Aminogylcosides bind irreversibly to the 30s ribosomal subunit of
bacteria ( inhibit protein synthesis)
 Gentamicin is the most commonly used aminoglycoside , but amikacin may
be particularly effective against resistant organism
 Are used in the treatment of severe infections of the abdomen and urinary
tract as well as bacteremia and endocarditis, and for prophylaxis especially
against endocarditis
 Resistance is rare but increasing in frequency
 Avoiding prolonged use ,and volume depletion and concomitant
administration of other potentially nephrotoxic agents decreases the risk of
toxicity
 Single daily dosing of aminoglycosides is possible because of their rapid
concentration- dependent killing and post antibiotic effect and has the
potential for decreased toxicity


34.  Aminoglycisides:
 Gentamicin, Amikacin and Tobramycin: these are
effective against serious infections caused by
aerobic gram –negative bacteria including Ecoli
,Enterobacter ,Klebsuella, Proteus, Pseuodomonas
aeruginosa and Serratia
 Stretomycin :used to treat Tuberculosis. Seldom is
used today
 Neomycin and Kanamycin: due to its toxic potential
neomaycin is used only topical or locally while
kanamycin is rarely used because of its marked
tendency to cause ototoxicity

35.  Aminoglycoiside may cause severe neuromuscular
weakness lasting hours to days because of their
potential curare-like effect. And may aggravate
muscle weakness in patients with muscular disorder
( myasthenia gravis, infant botulism or parkinsonism)
 Two well know adverse effects are ototoxicity and
nephrotoxictiy

36. cephalosporin
 Penicillin-like in action against bacteria
 They are bactericidal and interefere with cell wall
synthesis through inhibition of the synthesis of the
peptidoglycan in the cell wall. the antibiotic binds to the
enzymes (transpeptidase) that build/maintain the cell
wall, this makes the cell wall osmotically unstable/
bacteria eventually lyses resulting in the death of the cell.
 Cephalosporins act against a wide range of gram
positive and gram negative bacteria
 There are 4 generations of cephalosproin. each newer
generation has significantly greater gram negative
antimicrobial properties than the preceding one and a
decreased maximum activity against gram-positive
organisms.

37.  Cephalosporins
 First Generation
 Cefadroxil (Duricef)*
 Cefazolin (Ancef, Kefzol, Zolicef)†
 Cephalexin (Biocef, Keflex, Keftab)*
 Cephalothin (Keflin)†
 Cephapirin (Cefadyl)†
 Cephradine (Velosef)‡
 …most activity against S.aureua Group A beta hemolytic streptococci and Pneumococcus.
 Second Generation
 Cefaclor (Ceclor)*
 Cefamandole (Mandol)†
 Cefonicid (Monocid)†
 Cefotetan (Cefotan)†
 Cefoxitin (Mefoxin)†
 Cefprozil (Cefzil)*
 Cefuroxime (Ceftin, Kefurox, Zinacef)‡
 Loracarbef (Lorabid)*
 have efficacy against gram-postive oragnisms but also posses good activity against Ecoli
and H.influenzae

38.  Third Generation
 Cefdinir (Omnicef)*
 Cefixime (Suprax)*
 Cefoperazone (Cefobid)†
 Cefotaxime (Claforan)†
 Cefpodoxime (Vantin)*
 Ceftazidime (Ceptaz, Fortaz, Tazicef, Tazidime)†
 Ceftibuten (Cedax)*
 Cefditoren (Spectracef)*
 Ceftizoxime (Cefizox)†
 Ceftriaxone (Rocephin)†
 have the broadest spectrum of activity of all cephalosporins and are
extremely effective against gram negative oragnism .they are more
active against Ecoli , Klebsiella pneumoniae, Enterobacter, Salmonella
and SHigella
 Fourth Generation
 Cefepime (Maxipime)† effective against Pseudomas aerginosa

39.  Approximately 10% of individuals expressing allergy
to the penicillin family of antibiotics will have cross
allergenicity to the cephalosporins.

40. macrolide
 Azithromycin
 Clarithromycin
 Erythromycin (prototype agent.)
 Macrolide antibiotics are generally used to treat infections
caused by streptococcal bacteria and respiratory
infections generally. They are also active against syphilis
lyme disease and leprosy and tuberculosis
 It has a toxic effect on the liver causing liver toxicity and
jaundice and so should not be given to people who have
an underlying liver problem such as an infection with
hepatitis C
 They are bacteriostatic
 The mechanism of action involves inhibition of protein
synthesis that results from binding specifically to the 50s
ribosomal subunit., this causes the RNA to dissociate
from the ribosome and prevents protein synthesis

41.  The bacterial spectrums of activity of azithromycin
and clarithromyicin are similar to that of
erythromycin but possess greater intrinsic activity
against H.influenzae and H pylori, these two
macrolides concentrate within macrophages ,
making them useful against organisms that are taken
up by macrophages such as Mycobacterium avium
intracullulare.
 The significant tissue penetration of both agents and
the prolonged elimination half life of azithromycin(11-
14 hours) allows for once daily dosing for
azithromycin and twice daily dosing for
clarithromycin.

42.  In genral , oral bioavailability of erythromycin is poor. It
is readily inactivated by stomach acid, and several salts
have been developed to overcome this drawback;
 Erythromuycin stearate
 Erythromycin ethylsuccinate
Adverse GI effects are reported for approximately 21% of
patients receiving eryhtromycin about 10% of patients
receiving calrithromycin and less that 5% for azithromycin
Note: the GI upset is the most common side effect of the
erythromycin (take with food)
All of the erythromycin are very effective against Gram-
postivie bacteria but not so effective against gram
negative bacteria

43. fluoroquinolones
 Inhibit DNA gyrase ;an enzyme that is essential in
the transcription , replication, repair of bacterial DNA
 Drugs in this class include:
 Ciprofloxacin,norfloxiacin,levofloxacin,moifloxacin,
gemifloxcain
 It is active against many gram positive organisms
and gram negative aerobes including: Moraxella
catarrhalis ,H influenzae, Ecoli, chlamydia,
Myocoplasma pneumoniae , not active against
clostridium difficle
 The most common adverse effects are GI (Nausea
Vomiting, Diarrhea, abdominal pain) CNS( headache
Dizziness confusion ) dermatologic ( rash pruritis).

44. Recommended Doses of Some Antibiotics
 β-Lactams
 Penicillin V Adult: 250-500 mg every 6 hr; child (<12 yr old): 250-500 mg
every 6 hr
 Amoxicillin Adult: 250-500 mg every 8 hr; child (<20 kg): 20-40 mg/kg in
8-hr divided doses or 6.7-13.3 mg/kg every 8 hr
 Amoxicillin-clavulanate Adult: 250-500 mg every 8 hr; child: 25-40
mg/kg/day in 8-hr divided doses or 6.6-13.3 mg/kg every 8 hr
 Dicloxacillin Adult: 125-500 mg every 6 hr; child (<20 kg): 50-100
mg/kg/day in 6-hr divided doses or 3.125-6.25 every 6 hr
 Cephalexin Adult: 125-1000 mg every 6 hr; child: 25-100 mg/kg/day in 4
divided doses
 Cephradine Adult: 250-1000 mg every 6 hr; child: 25-100 mg/kg/day in 2
or 4 divided daily doses
 Cefaclor Adult: 250-500 mg every 8 hr; child: 20-40 mg/kg/day in
divided doses every 8 hr

45.  Macrolides
 Erythromycin Adult: 250-500 mg (stearate, base, or estolate salts) or 400 mg
ethylsuccinate salt every 6 hr; child:
 30-50 mg/kg per day in divided doses every 6 hr
 Azithromycin Adult: 500 mg every 12 hr; child: 5-12 mg/kg/day
 Clarithromycin Adult: 250-500 mg every 12 hr; child: 7.5 mg/kg twice daily up
to 500 mg twice daily
 Miscellaneous Antibiotics
 Clindamycin Adult: 150-450 mg every 6 hr; child: 8-20 mg/kg/day in 3 or 4
equal doses
 Metronidazole Adult: 250-750 mg every 8 hr, not to exceed 4 g in 24 hr
 Ciprofloxacin Adult: 250-500 mg every 12 hr; child: 25 mg/kg/day divided
every 12 hr
 Doxycycline Adult: 200 mg on day 1 (100 mg every 12 hr) then 100 mg daily;
child (≥8 yr old): 4.4 mg/kg in 2 divided doses
 on day 1 then 2.2 mg/kg daily
 Linezolid Adult: 375-625 mg every 12 hr

46. Summary
Penicillins:
Penicillin VK
Amoxicillin
Amoxicillin/clav.
Acid(augmentin)
Ampicllin
Inhibit cell wall
synthesis
bactericidal hypersensitivity
Cephalosporins:
Cephalexin
Cefaclor
Other:
Clindamycin
Inhibits cell wall
synthesis
Inhibits 50s
Ribosomes
Bactericidal
bacteriostatic
Hypersensitivity
Pseudomembrano
us colitis
Macrolides:
Azithromycin
Clarithromycin
Erthomycin
Inhibits 50s
ribosomes
bacteriostatic
None significant
GI hyperactiviy
GI hyperactivity

47. Tetracyclines:
Tetracyclines
Doxycyclines
Minocyclines
Inhibits 30s
ribosomes
bacterostatic
Superinfectin
None significant
same
Aminolglycosides:
Streptomycin
Gentamycin
Inhibits 30s
ribosomes
Bactericidal Ototoxicity,
nephrotoxicty
Miscellaneous:
Ciprofloxacin
Bacitracin
chloramphenicol
Inhibits DNA
Inhibit cell wall
Synthesis
Inhibit 50s
ribosomes
Bactericidal
Bactericidal
bacteriostatic
Nausea headache
Nephrotoxicity
Blood disorders

48.  Premedication requirements for
patients with valvular heart disease
or congenital cardiac defects:
 Amoxicllin:
 -adults: 2 g orally 30-60 minutes prior to appointment
 -children: 50 mg/kg orally 30-60 minutes prior to
appointment

49.  Allergy to Amoxicillin:
 Clindamycin
 Adults :600mg orally 30-60 minutes prior to appointment
 Children: 20mg/kg orally 30-60 minutes prior to appointment
 Cephalexin:
 Adults :2g orally 30-60 minutes prior to appointment
 Children: 20mg/kg orally 30-60 minutes prior to appointment
 Azithromycin
 Adults :500mg orally 30-60 minutes prior to appointment
 Children: 15mg/kg orally 30-60 minutes prior to appointment
 Clarithromycin
 Adults :500mg orally 30-60 minutes prior to appointment
 Children: 15mg/kg orally 30-60 minutes prior to appointment

50. Prophylaxis medications in patients with
Total joints replacement
 Cephalexin: 2 gram orally 1 hour prior to the dental
procedure
 Cephradine: 2 gram orally 1 hour prior to the dental
procedure
 Amoxiclline: 2 gram orally 1 hour prior to the dental
procedure
 Cefazolin 1g or ampicllin 2 g (IM /IV) 1 hour prior to
the dental procedure

51. Antifungal
 Candidiasis is an infection usually of the oral cavity
or vagina with a candida species usually C albicans
which causes an inflammatory pruritic infection
characterized by a thick white discharge
 It is common in patients who have a deficiency in T-
lymphocytes or who are receiving chemotherapy
and un immunpsuppressed individuals (AIDS)
 This yeast like fungi is a normal inhabitant of the oral
cavity and vaginal tract

52. Topical agents
Topical agents
(dissolve and
swallow)
Clotrimazole
(Mycelex Torche)
Oropharyngeal
Candidiasis
Alter cell
membrane
(Inhibition of
ergosterol
synthesis)
Torche
Nystatin(Mycostatin) Oral Cavity
Candidiasis
Alter cell
membrane(Bindin
g to ergosterol of
fungal membrane)
Oral suspension

53. Topical agents
Amphotericin-B
(fungizone)
Cutaneous and
mucocutaneous
candidiasis
Alter cell
membrane
cream
Ketoconazole
(NizoraL)
Alter cell
membrane
cream
Nystaatin
(Mycostatin)
Alter cell
membrane
cream,

54. Systemic agents
Amphotericin-B Systemic
candida
Alter cell
membrane
IV injection
Ketoconazole
(Nizoral)
Oral
esophageal
candidiasis
Alter cell
membrane
tablets
Fluconazole(diflucan) Oral
pharyngeal
candidiasis
Alter cell
membrane
(Inhibition of
ergosterol
synthesis)
tablets

55.  Systemic amphotericin-B is associated with high
incidence of kidney toxicity

56. AntiViral
 Oseltamivir and zanamivir inhibit influenza virus
neuraminidase enzymes altering virus particle
aggergation and release …used to treat influenza (A or
B) infection
 Acyclovir( zovirax) inhibit DNA synthesis rather than
neuraminidase enzymes
 Amantadine is a synthetic anti viral drug that can
inhibit the replication of viruses in cells. It interfere with a
viral protein M2 which is required for the viral particle to
become uncoated once taken in side a cell by
endocytosis
 Rimantadine is a synthetic antiviral drug that can
prevent viruses in cells from multiplying. It is chemically
related to amantadine but rimantadine has fewer side
effects on the nervous system than amantadine

57. Anti-HIV Agents
 Protease inhibitors suppress viral replication by
inhibiting protease (the enzyme responsible for
cleaving viral precursor peptides into infective
virions) : indinavir and nefinavir and ritonavir
saquinivir
 Nonnucleoside reverse transcriptase inhibitors:
inhibit reaction of reverse transcriptase that is
independent of nucleotide binding,: delavirdine,
adefovir ,nevirapine
 Nucleoside inhibitor: inhibiting reverse
transcriptase enzymes ( inhibition of the HIV viral
RNA from being made into DNA segment thus the
genome of the HIV virus is not copied from RNA) :
didanosine, zalcitabine zidovudine