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ANTIJAMUR,

ANTIMALARIA
DAN ANTIHELMINTIK

Yesi Astri
Departemen Farmakologi dan Farmasi
Fakultas Kedokteran
Universitas Muhammadiyah Palembang

... ANTIJAMUR ...


(ANTIFUNGAL)

Drugs that affect fungal membranes

1. Amphotericin B (Fungizone)
a. Structure and mechanism of action
- is an antibiotic that binds to ergosterol (a major
componenet of fungal cell membranes) and alters
membrane to allow leakage of cellular contents.

b. Pharmacologic properties
- poorly absorbed from the gastrointestinal tract
and; has poor penetration into the CNS.
- eliminated predominantly through the biliary
route.
- Can be detected in urine for weeks after
cessation of therapy.

c. Therapeutic uses
is used to treat most severe fungal
infection, including those caused by Candida
albicants,
Histoplasma
capsulatum,
Cryptococcus neoformans,
especially in
immunocompromised patients.
Is the most effective antifungal agent and is
usually the drug of choise for major systemic
infections.
In some cases, combination therapy with
flucytosine is advantageous.

2.Ketonazole,
clotrimazole,

miconazole,
and fluconazole

a. General properties
are imidazole derivates that block the synthesis
of ergosterol by inhibiting the cytochrome P450-mediated sterol 14-demethylase.
Are broad-spectrum antifungals; also inhibit
many gram-positive bacteria and some
protozoa.

b.

Ketonazole (Nizoral)
- can be administered orally; elevation of
gastric pH impairs absorption. It does not
penetrate CSF.
- Is extensively bond to plasma protein.
- Most commonly causes gastric upset (3%20% of patients). Itching, rashes, and
headaches are observed in 1% of patients.
- Is useful for treatment of mucocutaneous
candidiasis, histoplasmosis, and
paraccoccidioidomycosis as well as
dermatophyte infections.

c.

Miconazole (Monistat)
- is available for IV administration, but this is
associated with a high incidence of adverse
effects (phlebitis, pruritus, nausea, and
anemia). It is generally used only when
amphotericin B is contraindicated.
- Is available for topical application, which is
associated with high incidence of burning
and itching. Can be used for tinea pedis,
ringworm, and cutaneous and vulvovaginal
candidiasis.

d. Clotrimazole (Lotrimin, Mycelex)


and terconazole (Terazol)
- are available for topical application and are
useful for many dermatophyte infections.

e. Fluconazole (Diflucan)
- is available for I or oral administration.
- Is useful for oropharyngeal, isopharyngeal,
and systemic candidiasis. Also used for
acute and maintenance therapy of
cryptococcalmeningitis.

3. Nystatin
- is a polyene antibiotic similar in structure
and mechanism of action to amphotericin
B.
- is too toxic for systemic administration. Is
not absorbed from the gastrointestinal tract;
oral preparations can be used
prophylactically with tetracycline to prevent
superinfection of the intestine.

Other antifungal agents


1. Griseofulvin (Fulvicin, Grisactin)
- binds to microtubules and prevents spindle
formation and mitosis in fungi. Also binds
filament proteins such as keratin. The drug
accumulates in skin, hair, and nails.
- adequately absorbed after oral
administration
- administered as oral therapy for
dermatophyte infections.
- used for long-term therapy of hair and nail
infections.

2.

Flucytosine (Ancobon)
Is actively transported into fungal cells and
is
converted
to
5-fluorouracil
and
subsequently to 5-fluorodeoxyyuridylic
acid, which is an inhibitor of pyrimidine and
nucleic acid synthesis. Human cells lack the
ability
to convert large amounts of
flucytosine to the uracil form.
Is well-absorbed afer oral administration;
penetrates many tissues, including the CNS.
Is rarely used as a single drug, but often is
used
in
combination
with
other
antifungal agents.

... ANTIMALARIA ...

KLASIFIKASI ANTIMALARIA
Skizontosid

jaringan

pencegahan
kausatif, pencegahan relaps
Skizontosid darah pengobatan supresi
dan klinik
Gametosid membunuh gametosid di
eritrosit
Sporontosid

menghambat
perkembangan gametosid, tapi tidak
membunuhnya

Antimalaria yang Tersedia


Klorokuin
Pirimetamin
Primakuin
Kina
Meflokuin
Proguanil
Artemisin
Atovakuon

Prinsip Kemoprofilaksis dan


Terapi Malaria
Endemis

atau tidaknya suatu daerah


sehingga dapat diketahui strain yang
resisten
Adanya P. ovale dan P. Vivax, yang sering
menyebabkan relaps
Kehamilan
Reaksi intoleransi

... Cont
Malaria

akut akibat P.falcifarum, P.vivax,


P.ovale dan P.malariae skizontosid
darah (klorokuin dan kina)
Ditambahkan Primakuin untuk infeksi
akibat P.vivax dan P.ovale.

... Cont
Kemoprofilaksis

malaria : skizontosid darah


(klorokuin), dosis dewasa 500mg/minggu
(anak-anak : 5mg/kgBB), dimulai 1 minggu
sebelum memasuki daerah endemis, selama
di lokasi dan berakhir 4 minggu setelah
meninggalkan lokasi.
Untuk daerah endemis yang diketahui
resisten terhadap klorokuin kombinasi
pirimetamin dan sulfadoksin (dosis tunggal
3 tablet)

... Cont
Pengobatan

pada wanita hamil :


- trimester 1 : klorokuin atau proguanil
- trimester 2 dan 3 :
klorokuin/proguanil/meflokuin

... ANTIHELMINTIK ...

ANTIHELMINTIK
Mekanisme

kerja obat :
- Lokal
: mengeluarkan cacing dari
saluran cerna
- Sistemik: mengeradikasi cacing
Antihelmintik yang ideal :
1. efektif dan aman
2. praktis pemakaiannya (oral, dosis
tunggal)
3. stabil pada jangka waktu tertentu

BENZIMIDAZOL
Derivat

mebendazol, albendazol,
tiabendazol
Mekanisme kerja :
1. menghambat polimerase mikrotubulus
parasit
2. menghambat fumarat reduktase
mitokondria

... Cont
Indikasi

1. Tiabendazol kutaneus larva migran


2. Mebendazol askariasis, enterobiasis,
trikuriasis
3. Albendazol nematoda, kista hidatid,
neurosistiserkosis

... Cont
DEC

... Cont
Prazikuantel

meningkatkan permeabilitas membran


terhadap Ca kontraksi dan paralisis
spastis.
Menyebabkan kerusakan tegumen
Indikasi : skistosomiasis, klonorsiasis,
taniasis

... Cont
Pirantel

Pamoat
Menghambat depolarisasi neuromuskular
paralisis spastik
Indikasi : askariasis dan enterobiasis,
A.duodenale, N.americanus, T.trichiura

...thank
you...

Asiklovir

TUGAS

Amphotericin

Amoksisilin
Ceftriaxon
Cefixim
Tetrasiklin
Vancomicin
Skizontosid
Gametosid
Ketokonazol
Mebendazol
Pirantel

Pamoat

Ivermektin
Prazikuantel
Nistatin
Kloramfenikol
Rifampisin
Eritromisin
Metronidazol
Karbapenem

PETUNJUK
TULISKAN

PROFIL FARMAKOKINETIK,
MELIPUTI : ABSORPSI, DISTRIBUSI,
METABOLISME DAN EKSKRESI

TULISKAN

PROFIL FARMAKODINAMIK,
MELIPUTI : MEKANISME KERJA, EFEK
SAMPING, INTERAKSI OBAT, DOSIS