Antibiotics

Antibiotics are agents made from living microorganisms, synthetic manufacturing,

and genetic engineering that are used to inhibit specific bacteria. They can be
bacteriostatic, bactericidal, or both.

The major classes of antibiotics include: aminoglycosides, penicillins and

penicillinase-resistant drugs, sulfonamides, tetracyclines, and antimycobacterials (e.g.
antitubercular and leprostatic)

Others include ketolides, lincosamides, lipoglycopeptides, macrolides, and

monobactams.

Antibiotics: Generic and Brand Names

Here is a table of commonly encountered antibiotics, their generic names, and brand
names:

Classification Generic Name Brand Name

amikacin Amikin

Aminoglycosides gentamicin Garamycin

streptomycin generic

Imipenem-cilastatin Primaxin

Carbapenems meropenem Merrem IV

Cephalosporins

cefazolin Zolicef
 First-Generation
cephalexin Keflex
 Second-Generation cefaclor Ceclor
 cefuroxime Zinacef

cefpodoxime Vantin
ceftazidime Ceptaz, Tazicef
 Third-Generation
ceftizoxime Cefizox
ceftriaxone Rocephin
cefepime Maxipime
 Fourth-Generation
ceftaroline Teflaro
ciprofloxacin Cipro
Fluoroquinolones levofloxacin Levaquin

ofloxacin Floxin, Ocuflox

Penicillins and Penicillinase- Resistant Antibiotics
penicillin G Bicillin,
 Penicillins benzathine Permapen

amoxicillin Amoxil, Trimox

 Extended-Spectrum Penicillins
ampicillin Principen
nafcillin
 Penicillinase-Resistant Antibiotics
oxacillin
sulfadiazine generic
Sulfonamides sulfasalazine Azulfidine
cotrimoxazole Septra, Bactrim
demeclocycline Declomycin
doxycycline Doryx, Periostat
Tetracyclines
minocycline Minocin
tetracycline Sumycin
Antimycobacterials
Antituberculosis
ethambutol Myambutol
pyrazinamide Nydrazid
rifampin generic
 First-line
Rifadin,
rifapentine
Rimactane
streptomycin generic
capreomycin Capastat
 Second-line cycloserine Seromycin
ethionamide Trecator-SC
 rifabutin Mycobutin
Leprostatic dapsone generic
Other Antibiotics
Ketolide telithromycin Ketek
clindamycin Cleocin
Lincosamides
lincomycin Lincocin
Lipoglycopeptides telavancin Vibativ
azithromycin Zithromax
Macrolides clarithromycin Biaxin
erythromycin Ery-Tab, Eryc
Monobactam aztreonam Azactam

Spotlight: Bacteria and Antibiotics

 Bacteria are microorganisms that invade the human body through many
routes like respiratory, gastrointestinal, and skin.
 Human immune response is activated once bacteria invade the body. As the
body tries to rid itself of bacteria, classic signs of inflammation (e.g.
swelling, heat, redness, and pain), fever, and lethargy begin to show up.
 The goal of antibiotic therapy is to decrease the population of invading
bacteria to a point at which the human immune system can effectively deal
with the invader.

Aminoglycosides
 Aminoglycosides are a group of antibiotics indicated for infections caused
by gram-negative aerobic bacilli.
 They were replaced by newer, less-toxic drugs in treating less serious
infections because these drugs have potentially serious adverse effects.

Therapeutic Action

The desired and beneficial action of aminoglycosides is:

 Exert bactericidal effect through inhibition of protein synthesis in

susceptible strains of gram-negative bacteria. Specifically, they bind to a
unit of the bacteria ribosomes and cause misreading of the genetic code
leading to cell death.
Indications

Aminoglycosides are indicated for the following medical conditions:

 Infections caused by susceptible strains: Pseudomonas aeruginosa,

Escherichia coli, Proteus spp., Klebsiella-Enterobacter-Serratia group,
Citrobacter spp., and Staphylococcus spp.
 Serious infections susceptible to penicillin when penicillin is
contraindicated.
Here are some important aspects to remember for indication of antibiotics in different
age groups:

Children

This age group is very sensitive to GI and CNS adverse effects of antibiotics.
Therefore, it is important to monitor their nutritional and hydration status while on
therapy. Oral candidiasis as a superinfection is common in this age group which
makes eating and drinking difficult. Fluoroquinolones are associated with damage
to developing cartilage and are not recommended for growing children. In addition to
this, pediatric dosages should be double-checked to decrease the risk for adverse
effects. Most of all, parent education is important in cutting down the unnecessary use
of antibiotics in children.

Pharmacokinetics

Here are the characteristic interactions of aminoglycosides and the body in terms of
absorption, distribution, metabolism, and excretion:

Route Onset Peak Duration

IM, IV Rapid 30-90 min N/A

T1/2: 2-3 h
Metabolism: liver
Excretion: kidney (urine)
Contraindications and Cautions

Contraindications and Cautions

The following are contraindications and cautions for the use of aminoglycosides:

 Known allergy to aminoglycosides.

 Renal or hepatic disease. Can be exacerbated by aminoglycosides and may
interfere wih metabolism and excretion of these drugs.
 Preexisting hearing loss. Can be intensified by toxic drug effects on the
auditory nerve.
 Active infection with herpes or mycobacterial infections. Can be
worsened by the effects of an aminoglycoside on normal defense
mechanisms.
 Myasthenia gravis or parkinsonism. Can be exacerbated by the effects of
a particular aminoglycosides on the nervous system.
 Lactation. Aminoglycosides are excreted in the breast milk and can
potentially cause serious effects in the infant.
 Amikacin should not be used for longer than 7-10 days because it is
particularly toxic to the bone marrow, kidneys, and GI.
 Streptomycin is only for special situations because it is very toxic to the 8th
cranial nerve and kidney.

Adverse Effects

Use of aminoglycosides may result to these adverse effects:

 CNS: ototoxicity, irreversible deafness, vestibular

paralysis, confusion, depression, disorientation, numbness, tingling,
weakness
 Renal: renal failure
 Hematology: bone marrow depression, leading to immunosuppression and
resultant superinfections
 GI: nausea, vomiting, diarrhea, weight loss, stomatitis, hepatotoxicity
 CV: palpitations, hypotension, hypertension
 Hypersensitivity reactions: purpura, rash, urticaria, exfoliative dermatitis
Interactions

The following are drug-drug interactions involved in the use of aminoglycosides:

 Penicillins, cephalosporins, ticarcillin: synergistic bactericidal effect

 Diuretics: increased incidence of ototoxicity, nephrotoxicity, and
neurotoxicity
 Anesthetics, nondepolarizing NM blockers, succinylcholine, citrate
anticoagulated blood: increased NM blockade with paralysis

Amikacin

Dosage Forms & Strengths

injectable solution

50mg/mL

250mg/mL

General Dosing

15 mg/kg/day divided IV/IM q8-12hr

Urinary Tract Infection

250 mg IV/IM q12hr

Extended Interval Dosing (q24 Hours)

First dose: 15 mg/kg IV based on lean body weight

Subsequent doses: consult pharmacist

Hospital Acquired Pneumonia

 20 mg/kg/day IV; may administer with antipseudomonal beta-lactam or
carbapenem

Dosage Modifications

Renal impairment

CrCl >90 mL/min and aged <60 yr: q8hr

CrCl 60-90 mL/min OR aged ≥60 yr: q12hr

CrCl 25-60 mL/min: q24hr

CrCl 10-25 mL/min: q48hr

CrCl <10 mL/min: q72hr

Administer after dialysis in ESRD

Dosing Considerations

Monitor: peak, trough, renal & auditory function

Peak 15-40 mg/L, trough 5-10 mg/L

Aminoglycosides