Transcript Document 7364430
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
staphylo-, strepto-, hono-, anaerobe cocci, enterobacteria
H.influenzae (clarythromycin, azithromycin)
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:
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
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
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
Linkosamides
Linkomycin Clindamycin Action spectrum: Gram positive aerobe cocci, grampositive and gramnegatvie anaerobes
Penetrate all the tissues (don’t pass through HEB) including intracellurally
Usage: usually in heavy infections, caused by anaerobe microorganisms
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
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
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
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).
Photosensitization - tetracyclines
tetracyclines
AMINOGLYCOSIDES
І generation: streptomycin, neomycin, monomycin, kanamycin.
ІІ generation: gentamycin (garamycin), tobramycin, syzomycin.
ІІІ generation: netilmicin (netromycin), amikacin.
Gentamycin
Action spectrum of aminoglycosides
wide
gram-negative bacteria (escherichia colli, salmonella, klebsiella, especially K. рneumoniae, proteus iersinia, brucella, campilobacteria, helicobacters,serratsia, shigella etc.).
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.
Concentration of aminoglycosides in blood should not overcome:
Amikacin, kanamycin – 35-40 mkg/ml
Gentamicin, tobramycin – 10-12 mkg/ml
Complications in administration of aminoglycosides
Ototoxicity Nephrotoxicity Neurotoxicity According to extent of toxicity netilmicin < gentamicin
Leuko-, thrombocytopenia, hemmorhages, hemolisis Allergic reactions
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
Glycopeptide antibiotics
Vankomycin Teikoplanin
Active towards МRS і MRCNS