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Chemotherapeutic Agents / Antibiotics, chapter 34-39. Antibacterial compounds (procaryotes) Antiparasitic agents (eucarytotes) - Chapt 35 Antifungal compounds (eucarytotes) Antiviral compounds Anticancer compounds. Protozoa Helmints Insects (Scabies lice etc.)

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slide1

Chemotherapeutic Agents / Antibiotics, chapter 34-39

  • Antibacterial compounds (procaryotes)
  • Antiparasitic agents (eucarytotes) - Chapt 35
  • Antifungal compounds (eucarytotes)
  • Antiviral compounds
  • Anticancer compounds

Protozoa

Helmints

Insects (Scabies lice etc.)

(Fungi chapt. 36)

slide2

Protozoa

Eucaryotes, unicellular (may exist in colonies)

Protozoa and algae (protocista)

Complex replication (sexual and asexual)

Patogenic P. most common tropical area

3. world diseases

Many diseases can be prevented by clean drinking water

Certain protozal diseases spread by insects

slide3

Treatment of diseases caused by amebia, giardia, trichomonas

Related comp.

treatment of

African sleeping sickness

Metronidazol

Flagyl®, Metronidazol®

Also effective against anaerobic bacteria

Probably pro-drug -reductive activation

(mech. not fully understood)

Formation of toxic

reactive oxygen species

slide4

Anti - Malaria drugs

Mal aria = bad air

Plasmodium sp.

Vektor: Anopheles moskito.

Complex life cyclus.

40% of world population at risk

300 mil acute illnessess pr year

ca 1 mill deaths pr year

Malaria kills a child every 30 sec.

90% in incidents sub-sahara Africa

De fleste l.m.

aktive her

slide5

Historic drugs

-Azodyes and salvarsan (1. synthetic effective drug)

-Quinine fra Cinchona (Kinabark)

Cinchona pubescens (Kinatre) from South America

slide6

Quinolines

Mechanism

(DNA Intercalation)

Ferriprotoporphyrin IX: Binds to FPIX (metabolite from hemoglobine);

tox. form of FPIX, proteinbound FPIX less tox.)

Weak base Hypothesis: Increase pH in parasite

Hydroksyklorokin

Plaquenil®

Quinine

Kinin®

Klorokin

Klorokinfosfat®

Meflokin

Lariam®

More active, less tox (comp Quinine)

Resistance!

Also klorokin

resistant

P. palsifarum

slide7

Biguanides

Pro-drug

Inhib. protozoan folate reduktase

(c.f. Trimetoprim)

Proguanil (= Chloroguanide)

Paludrine®

Malarone® + atovakvon

Other biguanides

Klorhexidine

slide8

Others

Atovakvon

Malarone® + proguanil.

Also other parasites (P. carinii)

Ubiquinone antimetabolite?

Mech. involves radicals

No cross resist.

Synth. analogs, active field

Artemeter og Lumefandrin

Riamet®

slide9

Drugs for Helmint infections

Eukaryotes – Invertebrates.

Tropical diseases!

Animal parasites; ex Trichinella spiralis (trikiner).

Benzimidazoles

Many active analogs known

Binds to tubulin - prevents formation of microtubules

inhib. mitosis (c.f. certain anticancer drugs)

May also inhib. fumarate reductase

Mebendazol

Vermox®

slide10

Drugs against Ectoparasites (insects)

Lice, scabies etc

Permetrin

Nix®

slide11

Irreversible Inhibitors

Acetylcholine esterase

Not drugs, nerve gasses, insecticides etc.

Malation

Prioderm® lice

slide12

Chemotherapeutic Agents / Antibiotics, chapter 34-39

  • Antibacterial compounds (procaryotes)
  • Antiparasitic agents (eucarytotes) -
  • Antifungal compounds (eucarytotes) - Chapt 36
  • Antiviral compounds
  • Anticancer compounds

Fungicides / Fungistatika / Antimykotika

Chemotherapeutics / Antibiotics

slide13

Synthetic Antifungals

Azoles

Component of

fungus cell walls

slide15

Klotrimazol:

Canesten®, Klotrimazol® utvortes

Canesten®, vaginal behandlig

Ekonazol:

Pevaryl®, utvortes

Pevaryl®, vaginal behandlig

Miconazol:

Daktar®, utvortes

Daktar®, vaginal behandlig

Ketokonazol:

SAR:

-Weakly basic azole ring, imidazol / 1,2,4-triazol

(less tox. humans), pKa 6.5-6.8

-2 or 3 other aromatic rings

-Cl (or F) on at least one aromatic ring

(F i flukonazol)

-Lipophilic structures (as lanosterol)

Vorikonazol

Flukonazol

(Racemate)

Itrakonazol:

slide16

Allylic amines

Terbinafin

Lamicil®

Prevents formation of cell wall comp.

Accumulation of toxic squalene

slide17

Antimycotic Antibiotics

Polyenes

  • Proad spectrum. Some effect on certain protozoa.
  • Isolated, Streptomyces sp.
  • Binds to sterols in fungal cell membrane; cell leaks K+, small org. molecules
  • SAR:
    • Macrolaktone [26 eor 38-ring, Larger than macrolides ( erytromycin etc)]
    • Polyene (Macrolides not polyenes)
    • Several OH-groups
    • amino sugar, mykosamin
    • Bad water sol.
slide18

Nystatin A

toxic, bad oral avail;

Local treatment, mouth, GI tract

Amfotericin B

Systhemic infect (infusion)

Somewhat less tox.

slide19

Peptides

Caspofungin

Serious systhemic infect.

Semisynth. from prod. of fermentation ( Glarea lozoyensis)

Inhib. synth of b-1,3-D-glucan; cell wall comp. certain fungi

Few good inhib. of fungi cell wall comp.

compared to antibacterials

slide20

Chemotherapeutic Agents / Antibiotics, chapter 34-39

  • Antibacterial compounds (procaryotes)-Antimycobacterials chapt. 37
  • Antiparasitic agents (eucarytotes)
  • Antifungal compounds (eucarytotes)
  • Antiviral compounds
  • Anticancer compounds

G-

Mycobacteria

G+

slide22

First effective drug: Streptomycin 1946

  • Treatment
  • Long time ≥6 mnds
  • Combination of drugs

Different stages of bacterial growth

DOT: Directly observed therapy

slide23

First-line drugs

Isoniazid

Isoniazid®

Long Chain ACP-Enoyl

Fatty Acid Reductase (inhA)

Mycolic acid

slide24

First-line drugs

Ethambutol

Pyrazinamide

Mechanism not fully known

Synth of cell wall comp.:

Inhib. arabinocyl transferase?

Arabinose,

Arabinomannan

and Lipoarabinomannan

Mechanism not known

Rifampicin

Rimactan®

Broad spectrum antibiotic

From Streptomyces sp

Inhib bacterial RNA polymerase

(p-p intract. naphtalene rings aromatic AA?)

Induce CYP2C; increased metabol. of certain anti AIDS drugs

slide25

Second-line drugs

Cycloserine

Isolated Spreptomyces sp

p-Aminosalicylic acid

Ethionamide

Inhib. alanine racemase

and alanine ligase;

Inhib. peptidoglycan synth

Mech. ≈ Isoniazide

PABA antimetabolite

Folic acid synth (≈antibact. sulfa)

Kanamycin

(aminoglycoside antibiotics)

slide26

Others

Oxazolidinones

Quinolones

Treatment of MAC infections

Clarithromycin

(Macrolide)

Other macrolides

Ethambutol

Quinolones

Rifabutin (Rifamycin)