New generation Antibiotics /certified fixed orthodontic courses by Indian dental academy

NEW
GENERATION

INDIAN DENTAL ACADEMY
Leader in continuing dental education
www.indiandentalacademy.com

INTRODUCTION
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“against life”.
Produced by
microorganisms.
BUT


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Beta Lactams
Penicillins
(PCN)
Cephalosporins
Carbapenems
Monobactams
Vancomycin
Bacitracin
Polymyxin

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Macrolides
Aminoglycosides
Sulfonamides
Flouroquinolones
Other” antibiotics


GLYCYLCYCLINE


TIGECYCLINE
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Glycylcline
FDA – 2005,june17.
Similar – Tc & minocycline.(D-9).
Action
: inhibits 30 s ribosome
Indication : GPV & GNV & anaerobes.
MRSA,VRE,ESBL-Klebsiella & E-coli
SST infection, Intra-abdominal
NOT – pseudomonas or proteus
Dose
: 100 mg than 50 mg BD
liver –lower
kidney-not

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NOT – children , HS
Pregnancy, lactating mother, geriatrics ?
No oral forms
Ad – effects: GIT,
TEETH & BONE

Tgc;first of a new class of antimicrobial agent:eugene Applebaun, USA:
pharmacotherapy -2006 aug 26 (18) .
Tgc; a new glycylcycline antibiotics :kasbekan,pennsylvania,usa:Amj
health syst pharm 2006 1;63

KETOLIDE


TELITHROMYCIN
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Ketolide (macro)
Semi-synthetic erythromycin.
FDA -2004 April
Action
: 50 s ribosome & 30 s – propagation.
carried - phagocytes .
Indication : RTI( pneumonia.strep), H.Inf .
Dose
: 800 mg OD. 7 days.
Ad – eff : GIT, Blurring of vision, Jaundice.

FDA – WARNING – NOT – acute bacterial sinusitis
and bronchitis.
- myasthenia

OXAZOLIDINONES


LINEZOLID
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Oxazolidinones
FDA - 2001
Action: 30 s & 50 s – initiation .
Indication: MR strep, MRSA
SSSI, Nasocomial pneu.
No action on GN .
Cont-ind; HS, Platelet Disorders .
Pregnancy , child , lactating mother & geriatrics ?


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Ad – eff : GIT, platelets.
Interaction : MAO,SSRI - seratonin syn.
Dose : 600 mg BD.(100 Rs)
Light sensitive.
Ranbezolid.

Tsiodras s.gold HS – Linezolid resistance in a clinical isolate of
stap..aureus. Lancet.2006 jul (21).
Vonder lipper: efficacy & safety of Linezolid in MDR – TB 2006: J
infection.

LIPOPEPITIDE


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DAPTOMYCIN

Sep-2003
Sapaotroph streptomyces reseosporus.
Action – rapid depolarization.
- inhibition of protein, DNA, RNA
Indication – SSSI, Stap.aureus bacterimia ,
Not in pneumonia – surfactants
Dose – 4 mg/kg iv OD
Ad – eff – myopathy & rhabdomyolysis

Lin, dap, tig – supplement for vancomycin resistant MRSA & VRE
update on antibiotic resistance in hospital – June 2006 - Medline


LINCOSAMIDE


STREPTOGRAMINS
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Lincosamide
FDA – 1999
Pristinamycin – quinupristin/dalfopristin (30:70).
Action : early step protein & bond formation.
Dual mechanism
Indicated : MRSA, VRE- faecum, SSSI.
AD – Eff : myalgia , arthralgia – 30%

Quinupristin/Dalfopristin : med lett drugs ther 1999: 41
Nadler et al . quinupristin/dalfopristin: a novel selective spectrum antibiotic
for MRSA & GP. Clin. Microbial news 1999;130

GLYCOPEPTIDE
(MACROLIDE)


vancomycin
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1956
Workhorse .
VRE, VISSA, VRSA


FOSFOMYCIN
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Phosphonic acid - glycopeptides
Action – enolpyruvyltransferase – cell wall
- attachment
Indicated – UTI
E-coli, entero- faecalis.
Dose – 1 sachet – 4 ou.
No cross reaction with beta lactam.
Child, geriatrics, nursing mother - ?
pregnancy – Not
Fosfomycin- 70% Vs Cipro %

TEICOPLANIN
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Glycopeptide
Actinoplanes teicomyceticus .
More lipophilic ( vancomycin)
Lesser toxicity.
Action : inhibits peptidoglycan syn.
Indication : MRSA, PRS, Entero.
AD-Eff : Granulocytopenia
Dose : 400 mg – 1 st then 200 mg iv or im
Other s under investigation

RAMOPLANIN
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Glycolipodepeptide – macrocyclic
10 time > vanco.
Broad spectrum.
Clinical trial.


SPECTINOMYCIN

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Structurally different from aminoglycosides.
Indication : penicillin HS, gonorrhoea.
Ad – Eff : GIT.
Dose : 2 g deep im


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ROKITAMYCIN – borrelia
RU 28965 – sterp. Pneu.
TE – 0381 – legionnaires.
EVEROLIMUS -rapamycin –psoriasis.
ORITAVANCIN.
TELAVANCIN.
ALBAVANCIN.

Severe psoriasis Tx with new macrolid –everolimus: BJD ; 2007 vol 156

AMINOGLYCOSIDES


DIBEKACIN
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Analog – kanamycin
Broad spectrum.
E-Coli, pseudomonas .
Dose : 100 mg im or iv.
Indication : RTI, UTI, Burns
Ad – Eff : Nepro, Oto toxicity .

ISEPAMICIN – diaminocyclitol
derivatives

NEW use of OLDER ones


CARBAPENEMS


ERTAPENEM
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Similar to meropenem
Indication : GN & anaerobic
CA infection – 1st line (FDA)
HA infection – NOT – ESBL
Dose : 1gm iv – 30 min.
Highly protein bound
Ad – Eff : no clinical study( child, pregnant,
lactating mother)


Faropenem
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Effective – GP & GN.
PBPS 2&1A.
Indication : L & U RTI, ENT, UTI.
AD-Eff : GIT.
Dose : 150 – 300 mg – TID.
Caution : pregnant.
No study – child, geriatrics .


CEPHALOSPORINS


CEFTOBIPROLE

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FDA – 2003 – clinical trial.
Indicated : MRSA, SSSI, Nasocomial
Injectable.


CEFEPINE HCL
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Semisynthetic 4th gen.
Indication : pneumonia, UTI, SSSI.
Caution : Child, pregnancy, geriatrics.
Dose : 0.5 to 1gm. BD.
AD – Eff : GIT, Injectable site,
C-Ind : pseudomembranous colitis.


QUINOLONES


TROVAFLOXACIN
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1997
4 – gen.
Broadest spectrum.
Action : DNA gyrus, ty 4 topoisomerase (dormant)
Indication :CAP, nosocomial, pneumonia, bronchitis
NOT – UTI, pyelonephrites
Meningitis
Dose : 100mg to 200 mg/day ; oral or iv
Ad – Eff : hepatic

FDA – WARNING 1999,JUNE-LIVER
TOXICITY.RESERVED FOR LIFE THREATING .

GEMIFLOXACIN-MESYLATE
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4 gen.
Action : similar.
GP & GN .
Indication : MRSA, MDR, H.inf, klebsella
pneu.
Ad –Eff : GIT.
Dose : 320 mg OD – po or iv.
Only FQ – therapeutic level.


MOXIFLOXCIN
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3rd gen.
2000 – FDA.
Indication : penicillin resistant pneu,
sinusitis, bronchitis & CAP.
Cont-ind : QT interval, HS.
Ad – Eff : GIT,QT prolonged.
Dose : 400mg /day.


 PRULIFLOXACIN
 RUFLOXACIN
 TEMOFLOXACIN
 SITAFLOXACIN
 GREPAFLOXACIN

(1999torsedes de pointes)


SULFONAMIDES
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No new (drotrecogin – alfa)
Upjohn – presence of sulfo with
antiviral drug .


TEMOCILLIN
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MR – GN (klebsella , H.Inf, e-coli)
Action : same pen
Narrow spectrum BLRP.
Indication : renal impaired pt .
Dose : 1gm iv or im 12 hrs.
Ad – Eff : angioedema, HS.
Pregnancy, child, geriatrics ?

Liver more et al : 2005 activity of temocilline Vs prevalent ESBL
enterobacterecia : SE England FIS medline nov 2005.

 PIPERACILLIN

& TAZOBACTAM

 SULBACTAM


ANTIFUNGAL


VORICONAZOLE
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Triazole
Indication : Serious fungal infection.
1st & only drug – FDA (ampo – B).
Ad – Eff : vision,
Dose : 3mg/kg iv or 200mg.

Walsh T – National institute A & I :Mycosis study group
jan2002 /;compared voriconazole Vs ampo-B.


POSACONAZOLE
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Triazole .(NOXAFI)
FDA – july- 13- 2004
Action : cytochrome p450 14a –
demethylase (sterol)
Invasive infection.
Dose : oral 600 to 800mg / day.
More potent than varico.
Zygomycetes.
Ad – Eff : GIT, taste.

TERCONAZOLE :
-Vaginal
 ISAVUCONAZOLE :
-Clinical phase.
-resistant – fluconazole
 RAVUCONAZOLE :
-Clinical trial.
-related to vari & flu.
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CASPOFUNGINS
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FDA & EU
Action : cell wall .
Indicated : invasive aspergillosis, refractory
to ampo – B, oesophagities .
Dose : 70 mg iv
Ad – Eff ; GIT , skin
Caution : hepatic, preg, lactating,


MICAFUNGIN
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Glucan synthesis.
Action : cell wall 1-3 beta- D- glucan.
Broad spectrum.( no –zygo)
Dose : 150mg/day
Indication : stem cell transplant pt.
oesophageal candida.

ANIDULA – similar
aspergilluse nidulans.

SERATOCONAZOLE
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Imidazole
Action : cell wall.
Indicated : Athletes foot .
Ad – Eff : burning, dermatitis


ANTIVIRAL


ATAZANAVIR
Protease inhibitor.
 Anti-retro viral.
 FDA-2003
 1st - OD.(2006) -300mg
 Ad – Eff : bilirubin, torsades de points,
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TENOFOVIR:
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Blocks reverse transcriptase.
FDA – 2001

FOSAMPRENAVIR:
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FDA – 2003
Active – amprenavir.
Protease inhibitor.

FOMIVIRSEN:
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Blocks viral mRNA - coding
CMV – retinitis ; HIV

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ADEFOVIR DIPIVOXIL :
- Inhibits HBV DNA polymerase.
- indication : HBV
- Ad – Eff : GIT, Nepro.
- dose : 10mg OD.

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ENTECAVIR :
- Inhibits DNA reverse
transcriptase.
- Dose : 0.5mg OD.


NOVEL MODES
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Focus – virulence
Molecular biology & genomics – NOT

Nancy khardori -2006 med clin. N Am 90

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ANTI-QUORUM SENSING MECHANISM:
- Protective biofilm.

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ENZYMES:
- Damage to DNA .

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PATHOGENICITY ISLAND:
- Virulence encoded genes.
- VREF.
- Virstatin - Cholera toxin gene.

Hung DT . Small-molecule inhibitor of vibrio cholerae. science 2005;310
Goldsmith. Plasmid-encoded MucB protein is a DNA polymerase:Natl AcadSci USA
2000;97

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CHEMICAL MODIFICATION
– Beta – lactamas inhibitors – saturated by
ext.spectrum Beta-lactamas .
– LY333328 – vancosamine sugar.
– L786392 – carbapenem – PBP2a
- PBP 5
Waldor MK.a new approch for antibiotics development .N Engl j
Med 2006 :354

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ANTIBIOTICS HYBRIDE

– Two in One

Hamilton-miller JM .Dual – action antibiotic hybrid. J antimicro
chemotherapy 1994;33


AMP
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NATURAL ANTIBIOTICS:
– Innate immunity.
– Lipid – peptide interaction.
– Defensins.

MERD 2007 AMP – SMART BOMBS (frog skin &
human lung)


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Designed AMP:
– Laboratory synthesized
– Anti pneumococcal – peptide
analogue


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BACTERIAL ATTACHMENT INHIBITORS:
– Bacterial receptors Vs oligosaccharide –
mucosa
– Non cellular oligosaccharides.


BACTERIOPHAGES (1917)
– Intravenous phage –
stap.aureus.
– Alernative antibiotics.


METAGENOMICS:
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Removal of Plasmid DNA

CISRO GENE TECHNOLOGY:
- cytokine & interferon
- adenovirus - vector


PROTIEN INHIBITORS:
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Hemocidins

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Staphostatins


NANOTECNOLOGY
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Nanopills
- carbon
- amino acid
- semiconductors
- plastic
Quantum dot
Target antibiotics – bucky ball

Thank you
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New generation Antibiotics /certified fixed orthodontic courses by Indian dental academy

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