Antimicrobial Agent

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 : Kontrak perkuliahan + anti Mirobial agent

• Minggu II : Review + Anti microbial • Minggu III : Kuis + Presentasi

Cancer Drugs• Minggu IV : Presentasi Cancer Drugs•

Kontrak Perkuliahan

• Minggu V : Kuis + Vitamin• Minggu VI : Review + NSAID• Minggu VII : Presentasi Hematology Drugs +

Kuis

Kontrak Perkuliahan

Agen anti cancer terbagi beberapa golongan :1. Bahan pengalkilasi2. Anti metabolit3. Bahan Alam4. 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

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.

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DEFINITIONSDEFINITIONS

Ryan & Drew, 2004

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.

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Ryan & Drew, 2004

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.

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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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• 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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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 intothree 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-SelectionStreptomycin(ribosomal mutation)

Quinolones (gyrase or topoisomerase IVmutations)

Rifampin (RNA polymerase mutation), and Linezolid (ribosomal RNA mutation).

Horizontal Gene TransferConjugation,

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 drugis 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

• β-LACTAM ANTIBIOTICSThese drugs each contain a β-lactam ring. This can be brokendown by β-lactamase enzymes produced by bacteria, notably by many strains of Staphylococcus and Haemophilus influenzae,which are thereby resistant. β-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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---ß-Lactams- Mechanisms of Action and Resistance.mp4

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Macrolides- Mechanisms of Action and Resistance.mp4

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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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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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NNRTI : Nonnucleoside reverse transcriptase inhibitorNRTI : Nucleoside/nucleotide reverse transcriptase inhibitorPI : 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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• HSV to aciclovir• HIV to zidovudine• CMV to ganciclovir• Influenza A to rimantadine

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RESISTANCE TO ANTIVIRAL RESISTANCE TO ANTIVIRAL

Spicer, 2000

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• 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 RESISTANCEANTIVIRAL RESISTANCE

The likelihood of resistant mutant results from :

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• 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.

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ANTIVIRAL THERAPYANTIVIRAL THERAPY

Spicer, 2000

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• 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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PROBLEMS WITH THE THERAPYPROBLEMS WITH THE THERAPY

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Anti Parasit (anti malarial) and anti amoeba Drugs

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Exo-erythrocytic

(hepatic) cycle

Sporozoites Mosquito

Salivary Gland

Gametocytes

Oocyst

Erythrocytic Cycle

Zygote

Schizogony

Sporogony

Hypnozoites(for P. vivax and P. ovale)

Malaria Life Cycle Life CycleMalaria Life Cycle Life Cycle

Sporozoites

Merozoites

Merozoites

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Eradication of dormant

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• 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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ANTIMALARIALANTIMALARIALAGENTSAGENTS

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• 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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ANTIMALARIALANTIMALARIALAGENTSAGENTS

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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:primaquniekills 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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• atovaquone (Mepron)• metronidazole (Flagyl)• pentamidine (Pentam 300)• paromomycin (Humatin)• Several drugs used to treat malaria are also

used to treat nonmalarial protozoal infections

Antiprotozoal Drugs

Copyright © 2014 by Mosby, an imprint of Elsevier Inc. 82

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• Amebiasis• Giardiasis• Pneumocystosis• Toxoplasmosis• Trichomoniasis

Protozoal Infections

Copyright © 2014 by Mosby, an imprint of Elsevier Inc. 83

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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

Documents

Antimicrobial Agent