Antimicrobial Drugs

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chemicals that affect physiology in any manner

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Drugs

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Drugs that act against diseases

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Chemotherapeutic drugs

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He proposed the term chemotherapy which describes the use of chemicals that selectively kill pathogens

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Paul Erlich

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It binds to receptors on germs to bring about their death while ignoring host cells

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Magic bullets

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Ehrlich's search for antimicrobial agents resulted in discovery of an arsenic compound that killed ______ and worked against ______

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Trypanosome parasites; syphilis

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He reported the antibacterial action of penicillin

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Alexander Fleming

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It creates a zone where bacteria don't grow

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Penicillin mold

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The first practical antimicrobial agent efficacious in treating a wide array of bacterial infections

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Sulfanilamide

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discovered sulfanilamide

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Gerhard Domagk

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He discovered other microorganisms that are sources of useful antimicrobials and coined the term antibiotics

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Selman Waksman

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These are chemically altered antibiotics — more effective, long lasting and easier to administer

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Semisynthetic antimicrobials

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Antimicrobials that are completely synthesized in a laboratory

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Synthetic drugs

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The key to successful chemotherapy against microbes

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Selective toxicity

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Major structural component of bacterial cell

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Peptidoglycan layer

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It is a huge macromolecule composed of polysaccharide chain of alternating NAM and NAG molecules

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Peptidoglycan

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How does beta la tams inhibit peptidoglycan?

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it irreversibly binds to the enzymes of NAM sub-units

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These drugs are stable in acidic environment of the stomach and us readily absorbed in intestinal tract

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Methicillin, imipenem

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A drug obtained from Amycolatopsis oreintalis

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Vancomycin

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A semisynthetic, disrupt cell wall formation in a different manner

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Cycloserine

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It blocks the transport of NAG and NAM from cytoplasm out of the wall

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Bacitracin

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Vancomycin, cycloserine and bacitracin results in ______ due to effects of osmotic pressure

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Cell lysis

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It inhibits the enzyme that synthesized glucan

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Caspofungin

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Without ____, fungal cells cannot make cell walls leading to _______

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Glucan, osmotic rupture

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70s and composed of 30s and 60s subunits

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Prokaryotic ribosomes

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80s with 60s and 40s subunits

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Eukaryotic ribosomes

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A ribosomal subunit that contains enzymatic portion that forms peptide bonds

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50S

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Antimicrobial agents that targets 30s ribosomal unit

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Aminoglycosides and tetracyclines

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Types of aminoglycosides that changes the shape of 30s subunit, making it impossible for ribosome to read codons of mRNA correctly

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Streptomycin and gentamicin

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______ block the enzymatic site if 50s subunit to prevent translation

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Chloramphenicol

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Drugs that binds to a different portion of 50s subunit that prevents movement of ribosome from one codon to another which causes translation to be frozen and protein synthesis is halted

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Lincosamides, streptogramins, macrolides

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A unique drug that selectively binds to bacterial tRNA that carries amino acid isoleucine

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Mupirocin

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It blocks protein synthesis

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Antisense nucleic acids

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Drug that inactivates cytomegalovirus and used for eye infections

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Fomivirsen

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Drugs that work to stop protein synthesis by blocking initiation of translation and is a last resort in treating gram positive resistant infections

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Oxazolidinones

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A short polypeptide drug that disrupts cytoplasmic membrane of the targeted cell by forming a channel through the membrane which damages it's integrity

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Gramicidin

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A lipid constituent of fungal membranes that disrupts the membrane and causes lysis of cells

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Ergosterol

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Polyenes that are fungicidal because they attach to ergosterol

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Nystatin and amphotericin B

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They disrupt cytoplasmic membranes by inhibiting synthesis of ergosterol

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Azoles and allylamines

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Without ______, the cell's membrane does not remain intact and the ______ dies

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Ergosterol, fungal cell

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Most bacteria lacks _____ making them naturally resistant to polyenes, azoles and allylamines

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Sterols

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It is produced by bacillus polymyxa

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Polymyxin

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It is affective against gram negative bacteria particularly pseudomonas

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Polymyxin

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It disrupts transport across the cytoplasmic membrane of mycobacterium tuberculosis

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Pyrazinamide

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It is most effective against intracellular, no replicating bacterial cells

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Pyrazinamide

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It changes the permeability of cell membranes of several type of parasitic worms

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Praziquantel and ivermectin

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The sum of all chemical reactions that take place within a cell

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Metabolism

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It interferes with electron transport in protozoa and fungi

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Atovaquone

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It inactivates enzymes which disrupt tubulin polymerization and glucose uptake by many protozoa and parasitic worms

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Heavy metals

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It is crucial in synthesis of nucleotides required for DNA and RNA synthesis

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Para-aminobenzoic acid

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A form of folic acid that is used as a conenzyme in synthesis of purine and pyrimidine nucleotides

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Tetrahydrofolic acid

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End result of competition of sulfonamide and PABA

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Creation cell metabolism to cell death

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It also interferes with nucleic acid synthesis that binds with enzyme involved in conversion of dihydrofolic acid to THF

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Trimethoprim

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These can neutralise avid of phagolysosomes that prevents viral uncoating

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Amantadine, rimantadine and weak organic bases

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It is used to prevent infections by influenza type A virus

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Amantadine

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It interferes with the action of protease — an enzyme that HIV needs near the end of its replication cycle

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Protease inhibitor

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It binds with DNA and effectively blocks DNA synthesis and RNA transcription

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Actinomycin

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They are active against prokaryotic DNA. They inhibit DNA gyrase

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Quinolones

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An enzyme necessary for correct coiling and uncoiling of relocating bacterial DNA

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DNA gyrase

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Molecules with structural similarities to normal nucleotide building block of nucleic acid

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Nucleoside analogs