ANTIBIOTICS

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ANTIBIOTICS
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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).
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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
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Classificaion of macrolides

• ?. Natural substances erythromycin,
  oleandomycin,spiramycin, jozamycin, midecamycin.
• ??. Half-synthetic substances rozythromycin,
  clarithromycin, flurythromycin, dyrythromycin,
  miokamycin, rokitamycin.
• III. Azalides (neutrogen atom is introduced in
  lacton ring) azithromycin.

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Erythromycin
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Macropen (midecamycin)
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Sumamed (azithromycin)
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Action spectrum of maclrolides and azalides

• staphylo-, strepto-, hono-, anaerobe cocci,
  enterobacteria
• H.influenzae (clarythromycin, azithromycin)
• intracellular situated microorganisms (stamps of
  Helicobacter, Chlamydia, Legionell?, M.
  pneumoniae, U. urealyticum etc.)

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Pharmacokinetics of macrolides

• Quiclkly and fully distributed through the
  tissues (do not pass through HEB)
• Correlation tissues/blood
• Erythromycin (5-10) 1
• Azithromycin (100-500) 1
• Their concentration in phagocyting cells prevails
  concentration in blood pasma in 12-20 times, they
  get accumulated in source of inflammation -
  macrolides paradoxis

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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

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Side affects of microlides

• Dispeptic disorders, disbacteriosis,
  superinfection
• Cholestasis, cholestatic jaundice (erythromycin)
• Depression of liver microsome enzyme activity
  (erythromycin, oleandomycin can not be combined
  with theophylline, ergot alkaloids,
  carbamazepine)
• Development of resistance in process of
  treatment

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Linkosamides

• Linkomycin Clindamycin
• Action spectrum Gram positive aerobe cocci,
  grampositive and gramnegatvie anaerobes
• Penetrate all the tissues (dont pass through
  HEB) including intracellurally
• Usage usually in heavy infections, caused by
  anaerobe microorganisms
• Complicated side affects

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Linkomycini hydrochloridum
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Dalacyn C (clindamycini hydrochloridum)
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Tetracyclines

• 1. Natural - biosynthetic chlortetracycline,
  oxytetracycline, tetracycline, dimethylchlortetrac
  ycline.
• 2. Semisynthetic - doxycycline (vibramycin),
  metacycline (rondomycin), minocycline.

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Tetracycline
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Doxycycline
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Vibramycin (doxycycline)
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Shemes of tetracyclines administration

• Tetracycline - 0,25-0,5 g 4 times per 24 hours
• Methacycline 0,3-0,6 g 2 times per 24 hours
• Doxycycline 0,2 g (first day), 0,1g (next
  days) 1 time per 24 hours

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

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

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Photosensitization - tetracyclines
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tetracyclines
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AMINOGLYCOSIDES

• ? generation streptomycin, neomycin, monomycin,
  kanamycin.
• ?? generation gentamycin (garamycin),
  tobramycin, syzomycin.
• ??? generation netilmicin (netromycin),
  amikacin.

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Gentamycin
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Action spectrum of aminoglycosides

• wide
• gram-negative bacteria (escherichia colli,
  salmonella, klebsiella, especially K. ?neumoniae,
  proteus iersinia, brucella, campilobacteria,
  helicobacters,serratsia, shigella etc.).
  
• some gram-positive microorganisms, including
  staphylococci which are resistant to other
  antibiotics.

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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
• Amikacin, kanamycin 35-40 mkg/ml
• Gentamicin, tobramycin 10-12 mkg/ml

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Complications in administration of aminoglycosides

• Ototoxicity
• Nephrotoxicity
• Neurotoxicity
• According to extent of toxicity
• netilmicin lt gentamicin lttobramycin lt amikacin lt
  neomycin lt streptomycin lt monomycin lt kanamycin
• Leuko-, thrombocytopenia, hemmorhages, hemolisis
• Allergic reactions

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Chloramphenicol levomycetin

• Indications meningitis, typhoid fever,
  paratyphoid fever, brucellosis, tularemia
• Side affects
• Hypochrome and aplastic anemia
• Granulocytopenia, thrombocytopenia
• Grey syndrome of a featus
• Disbacteriosis and superinfection

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Glycopeptide antibiotics

• Vankomycin Teikoplanin
• Active towards ?RS ? MRCNS