ANTIBIOTICS

Monobactams

Aetreonam

Action spectrum - Gram (-) bacteria, including Escherichia colli, Clebsiellas, Proteum, Haemophilus influenzae (activity is equal to the activity of cephaloporins of third generation) Ways of introduction: oral (20% are being absorbed), intramuscular, intravenous Clinical uses: sepsis, infection of urinary tracts, soft tissues, meningitis and others (often combined with aminoglycosides , clindamycin, metronidazole, vankomycin).

Carbapenems (tienamytsin)

Tienam (imipenem + cylastatin) Meropenem The widest spectrum of antibacterial action - most of aerobe and anaerobe Gram(+) and Gran (-) bacteria, including those which produse beta lactamase

Classificaion of macrolides

І. Natural substances: erythromycin, oleandomycin,spiramycin, jozamycin, midecamycin.

ІІ. Half-synthetic substances: rozythromycin, clarithromycin, flurythromycin, dyrythromycin, miokamycin, rokitamycin.

III. Azalides (neutrogen atom is introduced in lacton ring): azithromycin.

Erythromycin

Macropen (midecamycin)

Sumamed (azithromycin)

Action spectrum of maclrolides and azalides

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staphylo-, strepto-, hono-, anaerobe cocci, enterobacteria

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H.influenzae (clarythromycin, azithromycin)

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intracellular situated microorganisms (stamps of Helicobacter, Chlamydia, Legionellа, M. pneumoniae, U. urealyticum etc.)

Pharmacokinetics of macrolides

Quiclkly and fully distributed through the tissues (do not pass through HEB) Correlation tissues/blood:

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Erythromycin – (5-10) : 1

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Azithromycin – (100-500) : 1

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Their concentration in phagocyting cells prevails concentration in blood pasma in 12 20 times, they get accumulated in source of inflammation - macrolides paradoxis

Indications for usage of macrolides and azalides LOR- infections, infections of upper respiratory tracts, hynecological infection, skin and soft tissues infections; ulcer disease; dyphteria; whooping-cough; honorrhea; syphilis; typhoid fever (azithromycin).

Drugs of choice for: mycoplasma, chlamidial, legionela pneumonia

Side affects of microlides

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Dispeptic disorders, disbacteriosis, superinfection

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Cholestasis, cholestatic jaundice (erythromycin)

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Depression of liver microsome enzyme activity (erythromycin, oleandomycin can not be combined with theophylline, ergot alkaloids, carbamazepine)

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Development of resistance in process of treatment

Linkosamides

Linkomycin Clindamycin Action spectrum: Gram positive aerobe cocci, grampositive and gramnegatvie anaerobes

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Penetrate all the tissues (don’t pass through HEB) including intracellurally

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Usage: usually in heavy infections, caused by anaerobe microorganisms

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Complicated side affects

Linkomycini hydrochloridum

Dalacyn C (clindamycini hydrochloridum)

Tetracyclines

1. Natural - biosynthetic: chlortetracycline, oxytetracycline, tetracycline, dimethylchlortetracycline.

2. Semisynthetic - doxycycline (vibramycin), metacycline (rondomycin), minocycline.

Tetracycline

Doxycycline

Vibramycin (doxycycline)

Shemes of tetracyclines administration

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Tetracycline - 0,25-0,5 g 4 times per 24 hours

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Methacycline – 0,3-0,6 g 2 times per 24 hours

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Doxycycline – 0,2 g (first day), 0,1g (next days) 1 time per 24 hours

Pharmacokinetics of tetracyclines when combined with other drugs Drugs Results of combined administration Antacides (Ca+, Mg+ etc.) Decrease of absorbtion Iron preparations Rifampicin Decrease of absorbtion Increase of elimination

Side affects of tetracyclines

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Dispeptic disorders, stomatitis, glositis, esophagitis, pruritus etc).

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Disbacteriosis and superinfection with Candida fungi, proteus, pseudomonadas or staphylococci. Photodermatosis. Liver toxicity. Absorbtion by bones and teeth of a featus or a child: hipoplasia of dental enamel, disorder of teeth formation, tendency for caries.

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Antianabolic action, damage of kidneys (when using tetracyclines with long termed storage, using big doses).

Tetracyclines are forbidden for children under the age of 8, during pregnancy, liver diseases, kidney insufficiency, miastenia).

Photosensitization - tetracyclines

tetracyclines

AMINOGLYCOSIDES

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І generation: streptomycin, neomycin, monomycin, kanamycin.

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ІІ generation: gentamycin (garamycin), tobramycin, syzomycin.

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ІІІ generation: netilmicin (netromycin), amikacin.

Gentamycin

Action spectrum of aminoglycosides

wide

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gram-negative bacteria (escherichia colli, salmonella, klebsiella, especially K. рneumoniae, proteus iersinia, brucella, campilobacteria, helicobacters,serratsia, shigella etc.).

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some gram-positive microorganisms, including staphylococci which are resistant to other antibiotics.

Indications for usage of aminoglycosides at the beginning stage of infectious processes of unknown ethiology and severe complexity (combined with beta lactamase); - considerable purulent-inflammatory component of heavy infections (peritonitis, sepsis, mediastinitis, abscesses and flegmones of soft tissues); - acute attack of chronical purulent-inflammatory diseases, including secondary immune defficiency; - early stage of development of secondary bacterial meningitis; - bacterial endocarditis; - infections of urinary tracts; - for prophilaxis of postoperative pustural complications (combined with beta-lactamase antibiotics, metronidazole or other antianaerobe drugs); - skin infections and subcutaneous fat tissue infections, burns.

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Concentration of aminoglycosides in blood should not overcome:

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Amikacin, kanamycin – 35-40 mkg/ml

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Gentamicin, tobramycin – 10-12 mkg/ml

Complications in administration of aminoglycosides

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Ototoxicity Nephrotoxicity Neurotoxicity According to extent of toxicity netilmicin < gentamicin

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Leuko-, thrombocytopenia, hemmorhages, hemolisis Allergic reactions

Chloramphenicol – levomycetin

Indications: meningitis, typhoid fever, paratyphoid fever, brucellosis, tularemia Side affects:

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Hypochrome and aplastic anemia

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Granulocytopenia, thrombocytopenia

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«Grey syndrome of a featus»

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Disbacteriosis and superinfection

Glycopeptide antibiotics

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Vankomycin Teikoplanin

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Active towards МRS і MRCNS