Antimicrobial Agents contains anti fungal Drugs

1. Anti Fungal Drugs
Dr. Saroj K . Suwal

2. Anti Fungal Drugs
 Used for Fungal Infections
 Fungal infection can be Superficial or
Systemic
 Fungus
 have rigid cell walls made of polymer of N-
acetylglucosamine rather than peptidoglycan
 cell membrane contains ergosterol rather than
the cholesterol found in mammalian
membranes.

3. FUNGAL
INFECTIONS
Yeast
infections
Candida
species
Cryptococcus
neoformans
Moulds Infection
(filamentous fungi)
Aspergillus sp Dermatophytes Trichophyton Microsporum

4. Superficial fungal Infection in skin
( Dermatophyte Infection)
 Candidiasis
 Candida Diaper Rash

5. Fungal infections
 Tinea Infection
 Athelet's Foot( Tinea Pedis)
 Nail Infection( tinea unguium)
 Ringworm infection( Tenia Corporis
 Ringworm of scalp( Tinea Captis
 RIng worm of groin ( tinea cruis)

6. Systemic Fungal Infections
 Candidiasis
 Aspergillosis
 Cryptococcosis
 Mucormycosis
 Blastomycosis
 coccidiodomycosis
 zygomycosis
 pneumocystis infection

7. Classification of Antifungal Drugs
1. Disrupt Fungal Cell Membrane
 Polyenes→ Amphotericin,
Nystatin
 Azoles→ two type Imidazole(A)
and Triazole(B)
A→Ketoconazole, Miconazole,
Clotrimazole
B→ Fluconazole, Itraconazole
 Allylamines→ Terbinafine
 Echinocandin→ Capsofungin
2. Inhibits Mitosis→ Griseofulvin
3. Inhibits DNA synthesis→ Flucytosine

8. Amphotericin B
 Amphotericin A & B are antifungal Drug
 Amphotericin A is not used clinically.
 is a natural polyene macrolide
(polyene = many double bonds ) (macrolide = containing a large lactone
ring )
 used to treat include aspergillosis, blastomycosis, candidiasis
 Also used in untreatable protozoan infections such as visceral
leishmaniasis and primary amoebic meningoencephalitis.
 IV , given very slowly over 2-6 hrs

9. MOA
 Fungicidal
Amphotericin B
Bind to
ergostero
l ,
Disrupt
fungal cell
membrane
Change
permeabi
lity of
cell
membran
e
Leads to
leakage
of
intracellu
lar ions
macromo
lecules
Fungal
cell
death

10. Adverse Effect
 “Shake and bake” (fever, chills),
 headache,
 tachycardia,
 hypotension,
 muscle pain,
 anemia
 Renal toxicity
 neural toxicity (seizures, paresthesia)

11. Side effect can be minimize by
 A. Slowing the infusion
 B. Decreasing the daily dose
 C.Premedication with antipyretics, antihistamines or
corticosteroids.
 D. A test dose is need before giving

12. Clinical uses
 DOC for life-threatening mycotic infections.
 broad spectrum of activity & fungicidal action
 In cancer patients with neutropenia who remain febrile on
broad –spectrum antibiotics.

13. 1. IV For systemic fungal disease.
2. Intrathecal for fungal C.N.S. infections.
3- Topical drops & direct subconjunctival injection for Mycotic
corneal ulcers & keratitis.
4. Local injection into the joint in fungal arthritis.
5. Bladder irrigation in Candiduria.

14. Nystatin
 polyene macrolide ,similar in structure & mechanism to
amphotericin B.
 an antifungal that works by stopping the growth of fungus.
 For localized candidiasis, fungal vaginitis, oral candidiasis
 Too toxic for systemic use., mostly Used only topically.
 Adult→ Tablet 500000 units
 Child→ 2-500000 units

15. Clinical Uses
 Prevent or treat superficial
candidiasis of mouth, esophagus,
intestinal tract.
 Vaginal candidiasis
 Can be used in combination with
antibacterial agents &
corticosteroids.

16. Azoles
 synthetic fungistatic agents
 broad spectrum of activity .
 Interfere with ergosterol synthesis
 antibacterial , antiprotozoal anthelminthic & antifungal activity
 Two types
 A) Imidazole : Ketoconazole , Miconazole
 B) Triazoles : Fluconazole , Itraconazole

17. Ketoconazole
 azole antifungals→ Imidazole group
 Water soluble antifungal drugs
 they inhibit human gonadal and
steroid synthesis leading to decrease
testosterone & cortisol production.
 Also, inhibit human P-450 hepatic
enzyme

18. MOA
 Interfere with ergosterol
synthesis
 Work on fungal p450 system
( inhibit to form ergosterol
 So,, also Suppress
testosterone and cortisol
synthesis

19. Preparations
 20 mg tablet, ointment, shampoo (1%,2%)
 Tab . 200mg x OD ( max 400mg)
 Child 3mg/kg/day
 Half-life increases with the dose , it is (7-8
hrs).

20. Clinical use
 Used topically or systematic
(oral route only ) to treat :
 1- Oral & vaginal candidiasis.
 2- Dermatophytosis.
 3- Systemic mycoses.
Dermatophytosis
an infection of the
hair, skin, or nails
caused by a
dermatophyte,

21. Adverse Effects
 Alters synthesis of gonadal and
adrenal steroid hormones
 Nausea vomit dizziness
 – Allergy
 – Dyspepsia
 – Anorexia
 – Gynecomastia
 – Impotence
 – Menstrual irregularities
 Purities
 Thrombocytopenia

22. Clotrimazole
 Broad spectrum antifungal
 Topical and oral , intravaginal use
 Vaginal cream, pessaries, ointment, lotion, powder

23. MOA
Death
Alters permeability cell wall
Inhibits ergosterol synthesis
Clotrimazole

24. Indications
 Vulvovaginal candidiasis
 Trichomonas vaginitis
 Tinea infection
 Athlete's foot
 Otomycosis
 Oral and cutaneous candidiasis

25. Fluconazole
 Triazoles Groups Antifungal agen
 Penetrates well BBB so, it is the drug of choice of
cryptococcal meningitis
 Safely given in patients receiving bone marrow
transplants (reducing fungal infections)
 Excreted mainly through kidney
 Less drug interaction
 Half-life 25-30 hours

26. Griseofulvin
 Effective in ring worm
 Fungistatic
 has a narrow spectrum
 Given orally (Absorption increases with fatty meal )
 Half-life 26 hours
 Should be given for 2-6weeks for skin & hair infections

27. MOA
 Acts by concentration in keratin of nail,skin, and hair
 Inhibit fungal mitosis
 Inhibit nucleic acid synthesis by binding with RNA
 Inhibition of cell wall synthesis
 Inhibits fungal mitosis by interfering with microtubule function

28.  Tabs,
Adult → 500mgxOD
 Suspensions
Child → 10mg/kg/wt

29. Nursing management
 LFT check ( hepatotoxicity if >14 days
 Tell patient to take one glass of water after taking medicine
 Avoid dangerous jobs, like driving . (Dizziness and
drowsiness may occur)
 Take medicine with food → minimize GI irritation

30. Antiviral Drugs
Dr. Saroj K. Suwal