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MEGHA SHAH
PENICILLINS
1ST antibiotic to be used clinically in 1941
MOA interferes with cell wall synthesis bactericidal Antibacterial spectrum Oral aerobes and anaerobes
Natural penicillins, aminopenicillins and penicillin resistance penicillins are mostly useful
NATURAL PENICILLINS
Penicillin G Acid labile Parenteral route 2-5 million units IM (Adult Dose)
Procaine penicillin G Longer acting Adequate serum levels for 8-12 hours, effective for 1-2 days when administered IM
Penicillin G Benzathine Even longer duration of serum levels Drug detectable for 1-3 weeks Penicillin V Acid stable 500mg QID orally
Spectrum of natural penicillins most gram + aerobes and most anaerobes. Staph. Aureus, bacteroides fragilis and H. influenza are commonly resistant to natural penicillins.
infections.
Dosage / administration:
0.25 to 1 gm TDS. Mostly given orally. Trade namesMox, novamox, Alphamox, Ambac, 250 / 500 mg caps; 125 mg/ 5ml syrup
Antibacterial spectrum-
ADVANTAGES Concentrations that are higher & last longer than an equivalent dose of Penicillin V.
Effective against infections involving streptococci or other
DISADVANTAGES Greater potential to produce superinfections of the GIT & vagina, because of broader spectrum of activity against gram ve aerobes. Can produce skin rashes as a result of allergy.
Ps. Aeruginosa
Carbenicillin Ticarcillin Piperacillin Mecillinam Limited benefits in head and neck infections
CEPHALOSPORINS
Less susceptible to b-lactamases as compared to
penicillin
As the generation increases, gram positive coverage
reduces, while effectiveness for gram ve organisms increase and for anaerobes the killing power decreases
Bactericidal
prophylaxis
Cefadroxil Cephalexin
phexin Tab 500mg BD Active against streptococci sp, staph. Aureus and not active against enterococci, listeria or MRSA
Cefoxitin Cefprozil Cefuroxime Brand name and dosage Ceftab, Ceftum - Tab 500 mg BD
Useful for treating upper & lower respiratory tract
against gram ve organisms. Cefixime Ceftriaxone Cefotaxime (0.25, 0.5 & 1 g per vial inj) Ceftibuten Cefdinir Cefpodoxime
Adverse effects:
MildStomach upset / cramps Nausea, vomitting Diarrhoea Sore tongue Sores in the mouth Vaginal yeast infections SevereBlack, tarry stools Chest pain Fever Difficult / painful urination Allergic reactions Serious colitis
MONOBACTAMS
Bactericidal effect similar to other drugs in this class
Only Aztreonam is approved for use No activity against g+ organisms, limiting its use in
CARBAPENEMS
Broad antibacterial spectrum
Commonly used to treat P.aeruginosa infections
TETRACYCLINES
Bacteriostatic in nature
Limited use because of rapid development of
treatment of orodental infections Tetracycline HCl (Alcyclin, Tetracyn) - Cap/ tab for paediatric dose. Adult dose between 1 and 2 g/per day in 34 divided doses. Doxycycline - Sparadoz, Sydox Cap 100mg, Tab 200mg )D
Adverse effects: Teratogenic Stains developing teeth Allergic manifestations like rash Photosensitivity Hepatic dysfunction GI disturbance like nausea, vomiting, epigastric distress Antianabolic effect Avoided in patients with renal impairment can lead to aggravation of aztemia and exaggerated anabolic effect Reversible Fanconi-like syndrome IV administration can lad tolocal thrombosis
VANCOMYCIN
Highly effective against MRSA, gram + cocci MOA cell wall inhibition Poor oral absorption and painful IM injection IV dose 2g daily in divided doses 500mg over 60 mins every 6 hours or 1g every 12 hours Vancocin CP Cap 250mg QID Adverse reactions local thrombophlebitis, generalised cutaneous reactions (Red Man Syndrome) and auditory damage
Used with caution in patients with renal damage
CHLORAMPHENICOL
Broad spectrum, bactriostatic agent
Rarely used these days Useful in ampicillin resistant H.influenza and
anaerobic bacteria Useful for brain abscess and meningitis S/E aplastic anaemia (rare)
- gray baby syndrome (neonates)
adults
MACROLIDES
Useful for maxillofacial infections
MOA bacteriostatic and interferes with protein
synthesis by attaching to 50S ribosome subunit Antibacterial spectrum g+organisms, G ve can resist it easily because of outer cell membrane and Methicillin resistant staph. Aureus is also resistant Common macrolides Erythromycin, Azithromycin, Clindamycin, Clarithromycin
ERYTHROMYCIN
Best known macrolide with g + spectrum similar to
penicillin, but less effective against anaerobes. But not used much because of its side effects and other agents are preferred
CLINDAMYCIN
Bacteriostatic at low concentrations and bactericidal at
slightly higher concentration Effective against gram + organisms, especially Staphylococci, Pneumococci, certain Streptococci Also useful for anaerobic infections Cap clincin, Dalacin 150 450 mg orally QID / 300 mg BD Adverse effect superinfection with Cl. Difficile Commonly used ddrug for serious odontogenic infections including osteomylitis
AZITHROMYCIN
Broad spectrum coverage including g+ and g-ve
aerobes and strict anaerobes Oral absorption and tissue peneration is better Brand name and dosage Azith , Azec tab 500mg OD/BD
NITROIMIDAZOLES METRONIDAZOLE
Stimulates production of toxic products to kill
Metrogyl, Flagyl 400mg tab TDS orally Can be given i.v. also (100 ml)
ORNIDAZOLE
Trade name and dosage Orni, Ornida Tab 500mg
BD
Uses: Pericoronitis Certain periapical infections Some cases of osteomyelitis Infected extraction socket
Adverse effects : Disulfiram reaction Can increase the action of anticoagulants Contraindicated in pregnant patients
FLUOROQUINOLONES:
Quinolones are a family of synthetic broad spectrum
antibiotics.
The parent of the quinolones class is nalidixic acid. Majority of quinolones in clinical use belong to the
subset of fluoroquinolones.
Generations: Quinolones are divided into generations based on their anti-bacterial spectrum.
1st generation Cinoxacine Nalidixic acid Oxolinic acid Rosoxacin Pipemidic acid Piromidic acid
3rd generation: 4th generation: (active against streptococci) Plurifloxacin Levofloxacin Gemifloxacin Sparfloxacin Clinafloxacin Balofloxacin Gatifloxacin Grepafloxacin Moxifloxacin Trade names: Ciplox, Cifran 250, 500 or 750mg tabs.; 200mg/100ml i.v. Norflox 200, 400, 800mg tabs
REFERENCES
Pharmacology and pharmacotherapeutics by R.S.Satoskar revised 20th edition 2. Essentials of medical pharmacology by K.D. Tripathi 5th edition
1.