Antimicrobial Agent

Meiriza Djohari

Kontrak Perkuliahan

4 SKS (2 T + 2P)
Anti Mikrobial agent (2)
Cancer drugs (2)
Vitamin and Supplement
NSAID
Hematology drugs

Kontrak Perkuliahan

Minggu I
Minggu II
Minggu III
Minggu IV

: Kontrak perkuliahan +
anti Mirobial agent
: Review + Anti microbial
: Kuis + Presentasi
Cancer Drugs
: Presentasi Cancer Drugs

Kontrak Perkuliahan

Minggu V
Minggu VI
Minggu VII

: Kuis + Vitamin
: Review + NSAID
: Presentasi Hematology Drugs +
Kuis

Kontrak Perkuliahan

Agen anti cancer terbagi beberapa golongan :

1. Bahan pengalkilasi
2. Anti metabolit
3. Bahan Alam
4. Senyawa Lain
5. Hormon antagonis

Kontrak Perkuliahan

No Hp/Gadget (kecuali pada saat diskusi

kelompok)
Terlambat tidak lebih dari 5 menit, kecuali
ada masalah (harus menghubungi dosen)
Tidak diperbolehkan tidak masuk kelas
(alpa) terkait kuis per paket
Tidak menggunakan celana ketat/ Jeans

DEFINITIONS

Antibiotic : antimicrobials of microbial origin,

most of which are produced by fungi or by
bacteria of the genus Streptomyces.
Antimicrobial : any substance with sufficient
antimicrobial activity that it can be used in
the treatment of infectious diseases.
Bactericidal : an antimicrobial that not only
inhibits growth but is lethal to bacteria.
Ryan & Drew, 2004
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DEFINITIONS
Bacteriostatic : an antimicrobial that inhibits
growth but does not kill the organisms.
Chemotherapeutic : a broad term that
encompasses antibiotics, antimicrobials and
drugs used in the treatment of cancer. In the
context of infectious diseases, it implies the
agent is not an antibiotic.
Minimal Inhibitory Concentration : a
laboratory term that defines the lowest
concentration (g/mL) able to inhibit growth
of the microorganism.
Ryan & Drew, 2004
8

DEFINITIONS
Resistant : organisms that are not inhibited by
clinically achievable concentrations of an antimicrobial
agent.
Sensitive : term applied to microorganisms indicating
that they will be inhibited by concentrations of the
antimicrobic that can be achieved clinically.
Spectrum : an expression of the categories of
microorganisms against which an antimicrobial is
typically active.

Ryan & Drew, 2004

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Classes and Actions of

Antimicrobial Agent
Microorganisms of medical importance fall into
four categories: bacteria, viruses, fungi, and
parasites.
The first broad classification of antibiotics follows
this classification closely, so that we have
(1) antibacterial, (2) antiviral, (3) antifungal, and
(4) antiparasitic agents
Drugs are further categorized by their biochemical
properties.
Goodman and Gillman
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Classes and Actions of

Antimicrobial Agent
The biochemical processes commonly :
Inhibited include cell wall synthesis in bacteria
and fungi, cell membrane synthesis, synthesis of
30s and 50s ribosomal subunits, nucleic acid
metabolism, function of topoisomerases, viral
proteases, viral integrases, viral envelope fusion
proteins, folate synthesis in parasites, and
parasitic chemical detoxification processes.
Goodman and Gillman
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Classes and Actions of

Antimicrobial Agent
Classification of an antibiotic is based on:
The class and spectrum of microorganisms it
kills
The biochemical pathway it interferes with
The chemical structure of its pharmacophore
(active chemical moiety of the drug that binds to the microbial receptor)

Goodman and Gillman

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Anti Bacterial Drugs

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1. Antibacterial
There are two term:
bactericidal and
bacteriostatic
Bactericidal drugs that kill
bacteria
Bacteriostatic drugs that
prevent their
reproduction, elimination
depending on host
defence

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1. Antibacterial

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1. Antibacterial

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BACTERIAL RESISTANCE
Mechanisms of drug resistance can be broadly divided into
three groups:
1. Inactivation of the antimicrobial agent either by
disruption of its chemical structure (e.g. penicillin) or by
addition of a modifying group that inactivates the drug
(e.g. chloramphenicol, inactivated by acetylation);
2. Restriction of entry of the drug into the bacterium by
altered permeability or efflux pump (e.g. sulphonamides,
tetracycline);
3. Modification of the bacterial target this may take the
form of an enzyme with reduced affinity for an inhibitor,
or an altered organelle with reduced drug-binding
properties (e.g. erythromycin and bacterial ribosomes)
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BACTERIAL RESISTANCE

The evolution of drug resistance involves:

Mutation-Selection
Streptomycin(ribosomal mutation)
Quinolones (gyrase or topoisomerase IV
mutations)
Rifampin (RNA polymerase mutation),
and Linezolid (ribosomal RNA mutation).

Horizontal Gene
Transfer
Conjugation,
the direct transfer of genes
by cell-to-cell contact
though a sex pilus or bridge

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DRUG COMBINATIONS
There are situations in which more than one antibacterial drug
is prescribed concurrently:
To achieve broad antimicrobial activity in critically ill patients
with an undefined infection (e.g. aminoglycoside plus a
penicillin to treat septicaemia)
To treat mixed bacterial infections (e.g. following perforation
of the bowel) in cases where no single agent would affect all
of the bacteria present
To prevent the emergence of resistance (e.g. in treating
tuberculosis )
To achieve an additive or synergistic effect (e.g. use of co
trimoxazolein the treatment of Pneumocystis carinii
pneumonia).
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COMMONLY PRESCRIBED ANTIBACTERIAL

DRUGS
-LACTAM ANTIBIOTICS
These drugs each contain a -lactam ring.
This can be brokendown by -lactamase enzymes
produced by bacteria, notably by many strains of
Staphylococcus and Haemophilus influenzae,which are
thereby resistant.
-Lactam antibiotics kill bacteria by inhibiting bacterial
cell wall synthesis.
Antibiotics in this group include the penicillins,
monobactams, carbapenems and cephalosporins

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COMMONLY PRESCRIBED ANTIBACTERIAL

DRUGS

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COMMONLY PRESCRIBED ANTIBACTERIAL

DRUGS

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COMMONLY PRESCRIBED ANTIBACTERIAL

DRUGS

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COMMONLY PRESCRIBED ANTIBACTERIAL

DRUGS

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----Lactams- Mechanisms of Action and Resistance.mp4

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COMMONLY PRESCRIBED ANTIBACTERIAL

DRUGS

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COMMONLY PRESCRIBED ANTIBACTERIAL

DRUGS

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COMMONLY PRESCRIBED ANTIBACTERIAL

DRUGS

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COMMONLY PRESCRIBED ANTIBACTERIAL

DRUGS

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Macrolides- Mechanisms of Action and Resistance.mp4

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COMMONLY PRESCRIBED ANTIBACTERIAL

DRUGS

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Fluoroquinolones- Mechanisms of Action and Resistance.mp4

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Anti Mycobacterial Drugs

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Antimycobacterial Drugs

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Antimycobacterial Drugs

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Antimycobacterial Drugs

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Antimycobacterial Drugs

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Antimycobacterial Drugs

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Anti Fungal Drugs

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Overview
Fungal infections classification:
Superficial infections: Ringworm (tinea) skin
and mucous membrane. Incidence rate is high.
Systemic infections: Candida albicans
opportunist infections. Fatality rate is high.

Antifungal agents classification:

Antibiotics: Amphotericin B;
Azole: Ketoconazole;
Allylamine: Terbinafine;
Pyrimidine: Flucytosine.
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Sites of action of antifungal drugs

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Anti Fungal Drugs

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Anti Fungal Drugs

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Anti Fungal Drugs

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Anti Viral Drugs

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Sites of action of antiviral

drugs

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Sites of action of antiviral drugs

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Mechanism of action of antiherpes agents.

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AGENTS TO TREAT HERPES SIMPLEX VIRUS (HSV)&

VARICELLA-ZOSTER VIRUS (VZV) INFECTIONS

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AGENTS TO TREAT HERPES SIMPLEX VIRUS (HSV)&

VARICELLA-ZOSTER VIRUS (VZV) INFECTIONS

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AGENTS TO TREAT CYTOMEGALOVIRUS

(CMV) INFECTIONS

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Drugs used to treat viral hepatitis

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ANTIRETROVIRAL AGENTS

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ANTIRETROVIRAL AGENTS

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ANTIRETROVIRAL AGENTS

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ANTIRETROVIRAL AGENTS

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ANTIRETROVIRAL AGENTS

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ANTIRETROVIRAL AGENTS

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ANTIRETROVIRAL AGENTS

NNRTI : Nonnucleoside reverse transcriptase inhibitor

NRTI
: Nucleoside/nucleotide reverse transcriptase inhibitor
PI
: Protease inhibitor

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The use of antiretroviral agents in

pregnancy.

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Life cycle of HIV

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RESISTANCE TO ANTIVIRAL

HSV to aciclovir
HIV to zidovudine
CMV to ganciclovir
Influenza A to rimantadine

Spicer, 2000
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64

ANTIVIRAL RESISTANCE
The likelihood of resistant mutant
results from :
Rate of viral replication. Higher rates of
replication are associated with higher rates of
spontaneous mutations.
Rate of viral mutations. The rate of mutations
differs among different viruses. ssRNA virus
have more rapid rates of mutation than dsDNA
viruses.
Rates of mutation in differing viral genes.
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ANTIVIRAL THERAPY

For most viral infections there is no specific

treatment.
The shortage of antiviral is partly due to the
difficulty of interfering with viral activity in the
cell without adversely affecting the host.

Spicer, 2000

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PROBLEMS WITH THE THERAPY

The incubation period is often 1 week or more
and by the time the patient becomes ill most
of the viral spread and replication has already
taken place.
Infections cannot be diagnosed during the
incubation period and even after the patient
becomes ill laboratory diagnosis often takes
several days.
Viruses that are latent in cells and not actively
replicating are generally insusceptible to
antivirals.
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Anti Parasit (anti malarial) and anti

amoeba Drugs

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Malaria
Malaria Life
Life Cycle
Cycle Life
Life Cycle
Cycle
Sporogony
Oocyst
Sporozoite
s
Mosquito
Zygote

Salivary Gland

Sporozoites

Hypnozoites
(for P. vivax
and P. ovale)

Gametocytes
Exoerythrocytic
(hepatic) cycle

Merozoites
Erythrocytic
Cycle

Schizogony

Merozoites

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Eradication of
dormant

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ANTIMALARIAL
AGENTS
No antimalarial drug kills sporozoites, it is not
truly possible to prevent infection; drugs can only
prevent the development of symptomatic malaria
caused by the asexual erythrocytic forms
No single antimalarial is effective against all
liver and intra-erythrocytic stages of the life cycle
that may co-exist in the same patient. Complete
elimination of the parasite infection, therefore,
may require more than one drug
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ANTIMALARIAL
AGENTS
The various stages of the malarial parasite life
cycle that occur in humans differ from one
another in their morphology, metabolism, and
drug sensitivity.
Thus, antimalarial drugs can be classified
based on their activities during this life cycle as
well as by their intended use for either
chemoprophylaxis or treatment

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Tissue
schizontocides:-.
1.Proguanil
(chlorguanide)
2.Pyrimethamine

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Blood
schizontocides:-.
2 types
1. Chloroquine,
Mefloquine,
Halofantrine, &
Quinine.
2. Proguanil,
Pyrimethamine, &
sulfadoxine.
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Gametocides:-destroy the
sexual forms of the parasite.
Primaquine, Chloroquine, & Quinie.
Primaquine the only drug that kills P.
falciparum gametocytes

Hypnozoitocides:
primaqunie
kills dormant hypnozoites
of P.vivax & P.ovale in
the liver.
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Sprontocides:interrupt
development of
sporogonic
phase in
mosquitos .
Proguanil,
pyremethamine
primaquine
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Major antimalarial drugs

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Treatment of malaria

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Drugs for the prevention of malaria in travelers

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Antiprotozoal Drugs

atovaquone (Mepron)
metronidazole (Flagyl)
pentamidine (Pentam 300)
paromomycin (Humatin)
Several drugs used to treat malaria are also
used to treat nonmalarial protozoal infections

Copyright 2014 by Mosby, an imprint of Elsevier Inc.

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Protozoal Infections

Amebiasis
Giardiasis
Pneumocystosis
Toxoplasmosis
Trichomoniasis

Copyright 2014 by Mosby, an imprint of Elsevier Inc.

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Treatment of amebiasis

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Tugas per orangan

Buat rangkuman untuk obat anti viral dan anti
parasit, dalm bentuk tabel, isi : nama generik,
nama dagang, mekanisme aksi, efek
klinik/indikasi, efek samping, kontraindikasi

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Terima Kasih

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