Слайд 2Tetracyclines
Usually bacteriostatic
Act on ribosomes
Слайд 3Doxycycline
Good absorbed
Cmax — 2,60 hrs
T1/2 — 16,33 hrs
Penetrates to most of tissues including
the gums
Accumulates in bones, tooth,liver, spleen
Low penetration to cerebral fluid
50%
excreted by kidneys
No decreased excretion in non-severe renal failure
Forms insoluble complexes with calcium in bones and tooth
Слайд 4Streptococcus pneumoniae), Staphylococcus spp. (inclStaphylococcus aureus, Staphylococcus epidermidis), Propionibacterium acnes, Listeria spp., Bacillus
anthracis, Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Brucella spp., Mycoplasma spp., Clostridium spp., Escherichia
coli, Shigella spp., Salmonella spp., Listeria, Spirocheta, E.hystolica, Yersinia pestis, Vibrio spp., Francisella tularensis, Enterobacter, Klebsiella spp., Bacteroides spp., Chlamydia spp., Rickettsia, Ureaplasma.
Highest efficacy - Haemophilus influenzae (91–96%) and intracellular pathogens
Less active - Proteus, Pseudomonas spp., Serratia, Providencia, Enterococci.
Active in Protozoa (malaria, entameba)
Cross reactivity to other tetracyclines and penicillines
Highly effected in pneumonias caused by micoplasma
Good in asthma and COPD exacerbations with infection in patients <65 yrs old (usually due to Haemophilus influenzae or Staph), in cystic fibrosis
Reiter disease
Skin leushmaniosis
In aged – prostatitis and Escherichia-related urinary infections
Malaria - - with quinine.
Blocks metalloproteinases of matrix in cartilage, because of this decreases injury in osteoarthritis (in experiment)
Слайд 5Indications
Sensitive microorganisms infections (incl.intracellular, incl.Q fever, typhoid fever, brucellosis, yersiniosis,
disentery, tylaremia, cholera, Lyme disease, malaria)
In combinations – leptospirosis, trachoma,
ornitosis
ENT organs and upper and lower respiratory tract
Cholecystitis cholangitis gastroenterocolitis
Urinary – cystitis, pyelonephritis, urogenital mycoplasmosis
Endometritis
Skin end eye infections (inc.ulcerative keratitis)
Prevention of postsurgical infections (incl.uterus and rectum)
Prevention of Plasmodium falciparum infecton in presence in territories where resistanc eof plasmodium to chloroquine is detected
Слайд 6Contraindications
Porphyria
WBC decrease
Pregnancy
Age
myasthenia
Pregnancy – contraindicated (calcium complexes)
Слайд 7Side effects
Benign intracranialhypertension, anorexia, headache, disk edema, vision changes, dizziness,
instability of walking
Hemolytic anemia, thrombocytopenia, neutropenia, Eos increase
Protrombin decrease
Слайд 8Interactions
Barbiturates, carbamazepin, riphampicin decrease plasma concentration and T1/2 (monooxygenases induction)
Don’t
use together with bactericidal
Decrease contraception ability
Potentiate indirect anticoagulant action
Слайд 9Unidox Solutab®
100 mg
200 mg daily (100 mg 2 times) first
day, then 50 mg 2 times daily
In severe infections
- 100 mg 2 times – all treatment course
Usually 7-10 days
Слайд 10Tetracycline
Bartonella bacilliformis, Brucella spp., Calymmatobacterium granulomatis, Campylobacter fetus, Francisella tularensis, Haemophilus ducreyi, Haemophilus influenzae , Listeria monocytogenes, Neisseria gonorrhoeae, Vibrio
cholerae, Yersinia pestis, грамположительных бактерий: Streptococcus spp., icl. Streptococcus viridans, Streptococcus pneumoniae (except A groups,
pyogenes and 74% of Streptococcus faecalis are resistent), Actinomyces spp., Bacillus anthracis, Balantidium coli, Borrelia recurrentis ,Chlamydophila (Chlamydia) psittaci, Chlamydophila (Chlamydia) trachomatis, Clostridium spp.,Entamoeba spp., Fusobacterium fusiforme, Mycoplasma pneumoniae, Rickettsiae,Propionibacterium acnes, Treponema pallidum, Treponema pertenue, Ureaplasma urealyticum.
Resistent Pseudomonas aeruginosa, Proteus spp., Serratia spp., most of Bacteroides spp., fungi, viruses
Слайд 11Cmax— 2–3 ч
Good penetrates to fluids incl.cerebrospinal, to tooth, to
liver, bones
T1/2 — 6–11 hrs, in anuria 57–108 hrs
Urine – high
concentration from 2 hrs to 6-12 hrs
Слайд 12Indications
Respiratory - Mycoplasma pneumoniae;Haemophilus influenzae, Klebsiella spp.
Urinary infections
Skin, soft
tissues infection
Ulcerative necrotic stomatitis
Actinomycosis
Interstinal amebiasis
Antrax, brucellosis, bartonellosis, cholera, chlamidiosis,
gonorea, ricketsiosis, typhoid fever, syphilis, tularemia
Skin oinment – acne, bacterial infections
Opthalmic oinment –blepharitis, ceratitis, trahhoma
Слайд 13Side effects
CNS – increase of intracranial pressure, dizzines
Hemolytic anemia, decrease
of platelets and neutrophils
GI – decrease of appetitis, vomiting, diarrhea,
gastritis, peptic ulcer, dysphagia, enzymes increase, pancreatitis
Nephrotoxic, increased creatinin
Allergy up to shock
SLE
Photosensibilization (avoid insolation!!!) Bone and tooth development impairment
Superinfection, candidosis, B vitamines deficiency
Слайд 14Interactions
Antacides, iron,magnesium, calcium decrease absorbtion
Decrease efficacy of contraceptives
If used with
A vitamine increase risk of intracerebral hypertension
Слайд 15Glycopeptides
Vancomycin
staphylococcus spp. (icl Staphylococcus aureus , Staphylococcus epidermidis, meticillin resistent), Streptococcus spp., в т.ч. Streptococcus bovis, Streptococcus
viridans, Streptococcus pyogenes, Streptococcus pneumoniae (incl.penicillin resistent),Streptococcus agalactiae, Listeria monocytogenes;
Anaerobes Gr+ Actinomyces
spp., Enterococcus spp. (incl Enterococcus faecalis),Corynebacterium diphtheriae, Clostridium spp.
In decrease pH up to 6 effect decreases
Active for actively proliferating microorganisms
Слайд 16Low absorbtion
After i.v. present in different fluids, including liqour in
meningitis
T1/2 4–6 hrs, in renal failure with anuria 7,5 days
Prolonged
excretion in single kidney
Слайд 17Indications
Pseudomembranous colitis!!! (oral)
Sepsis, endocarditis, osteomyelitis
Lower respiratory tract infections
CNS infections
Слайд 18Contraindications
Otoneuritis
Pregnancy (vital indications only), breast feeding
Newborns
Aged
Слайд 19Complications
Vertigo, hearing decrease, sounds in ears
Decreased Neutr, WBC, platelets, rare
agranulocytosls; Eos may increase
Diarrhea, vomiting
Nephrotoxicity (up to renal failure), more
common with aminoglycosides and in high concentration s more than 3 weeks
Rare interstitial nephritios
Allergyt – rashm Steven Jones, vasculitis, Drug induced rash and eosinophylia syndrome (DRESS) , anaphylaxy, “red person syndrome” – upper part skin hyperemia, muscular spasm
Necrosis and thrombophlebitis at the injection site
Слайд 20Edicin®
1000 mg (i.v. 1 gram every 12 hrs)
Orally
– 250-500 mg 4 times daily (pseudomembranous colitis) - solution
Duration of treatment 7-10 days
Слайд 21Monobactams
Aztreonam)
Citrobacter spp., Enterobacter spp., incl.E. сloacae, Escherichia coli, Haemophilus influenzae (incl.resistent
to other antibiotics), Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa,
Serratia species, incl.S. marcescens.
Слайд 22After i.,. Cmах — 1 hr
T1/2 1,7 hrs
Слайд 23Indications
Anaerobic Gr- infections
Urinary
Pneumonia
Sepsis, peritonitis, endometritis
Abscesses
Surgical infections
Слайд 24Limitations
Renal failure
Allergy to beta lactams
Слайд 25Side effects
Vertigo, headache, paresthesia, conscious disorders, oral ulceration, seizures, diplopia,
numbness of tongue
BP decrease, PVC (bigimenia), flushes, decrease of WBC,
RBC, platelets (or increase of these cells), eosinophils
Wheesing, chest pain
Spastic pain in abdomen, hepatitis, jaundice, rare pseudomembranous colitis or bleeding
Toxic epidermal necrolisis, purpira, rash, angioedema, bronchospasm, anaphylaxy
Candidosis
Phlebits
Слайд 26Azactam®
I.m. (deep), i.v
I.m - 0,5 g/1.5 ml, 1g /3 ml fluid
I.v.
1 g/6-10 ml, used in 2-5 min injection
Infusion – 0.5-1 g
/ 50–100 fluid
0.5 g with interval 12 hrs
Слайд 27Oxazolidons
Linezolid
Enterococcus faecium resistent to vancomycin,Staphylococcus aureus (incl.methycillinresistent), Streptococcus agalactiae, Streptococcus pneumoniae (incl. MDRS), Streptococcus pyogenes
Слайд 28Resistent
Haemophilus influenzae, Moraxella catarrhalis, Neisseria spp., Enterobacteriaceae spp., Pseudomonas spp.
Слайд 29Cmax 1,5 hrs, in fatty food- 2,2 hrs
T1/2 –
4-6 hrs
No changes in A and B class of cirrhosis
Слайд 30Indications
Nosocomial pneumonia or CAP caused by resistant species
Complicated skin infections
Слайд 31Side effects
Dizziness, insomnia, tongue tremor
Liver enzymes elevation
Anemia, decrease of platelets
Prolactin
elevation
Creatinin elevation
Serotonin syndrome (especially in antidepressants)
Слайд 32Zivox®)
Pneumonia 600mg i.v. or oral 10-14 days
Enterococci – 600 mg
14-28 days
Tablets 600 mg
Слайд 33Lincozamides
Lincomycin
Antibacterial
Staphylococcus spp., Streptococcus spp.,. Streptococcus pneumoniae, Corynebacterium diphtheriae), Clostridium spp.) Bacteroides spp., Mycoplasma
spp.).
Resistant spp
Not sensitive - Enterococcus spp., Gr-, protozoa
Слайд 34 Cmax 2–4 hrs
In most tissues excluding spinal
High concentration in bones, tooth
and bile
T1/2 4–6 hrs, in advanced kidney failure 10–20 hrs
Слайд 35Indications
Severe infections
Mostly
Lower respiratory (abscess, empyema, aspiration pneumonia)
Otitis
Bones, joints, tooth
infections
Skin purulent infections
Слайд 36Limitations
Skin fungi
Myasthenia (for parenteral)
Слайд 37Side effects
Nausea, diarreha, enzymes elevation
Candidosis, diarrhea, pseudomembranous colitis
Reversible WBC, neutrophils,
platelets decrease
Allergy
Phlebitis – in i.v., also may be asthenia, BP
decrease, relaxation of skeletal muscles
Слайд 38Lincomycin hydrochloride in capsules 0,25 g
1–2 hrs befor meals or
2–3 hrs after meals
Intervals 8–12 hrs
Single dose 500 mg, daily
dose 1–1,5 g