Condition Characteristic Pathogens Mitigating Circumstances Recommended Empirical

Treatmenta

Acute uncomplicated Escherichia coli, None 3-Day regimens: oral TMP-

cystitis in women Staphylococcus SMX, TMP, quinolone; 7-day
saprophyticus, Proteus regimen: macrocrystalline
mirabilis, Klebsiella nitrofurantoinb
pneumoniae

Diabetes, symptoms for >7 Consider 7-day regimen:

d, recent UTI, use of oral TMP-SMX, TMP,
diaphragm, age >65 years quinoloneb

Pregnancy Consider 7-day regimen:

oral amoxicillin,
macrocrystalline
nitrofurantoin,
cefpodoxime proxetil, or
TMP-SMXb
company name
Condition Characteristic Pathogens Mitigating Circumstances Recommended Empirical
Treatmenta
Acute uncomplicated E. coli, P. mirabilis, S. Mild to moderate illness, no Oralc quinolone for 714 d
pyelonephritis in women saprophyticus nausea or vomiting; (initial dose given IV if
outpatient therapy desired); or single-dose
ceftriaxone (1 g) or
gentamicin (35 mg/kg) IV
followed by oral TMP-SMXb
for 14 d

Severe illness or possible Parenterald quinolone,

urosepsis: hospitalization gentamicin ( ampicillin),
required ceftriaxone, or aztreonam
until defervescence; then
oralc quinolone,
cephalosporin, or TMP-SMX
for 14 d

company name
Condition Characteristic Pathogens Mitigating Circumstances Recommended Empirical
Treatmenta
Complicated UTI in men E. coli, Proteus, Klebsiella, Mild to moderate illness, no Oralc quinolone for 1014 d
and women Pseudomonas, Serratia, nausea or vomiting:
enterococci, staphylococci outpatient therapy
Severe illness or possible Parenterald ampicillin and
urosepsis: hospitalization gentamicin, quinolone,
required ceftriaxone, aztreonam,
ticarcillin/clavulanate, or
imipenem-cilastatin until
defervescence; then oralc
quinolone or TMP-SMX for
1021 d

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 Trimethoprim and TMP-SMX
Fluoroquinolones
Macrocrystalline nitrofurantoin
Penicillins
Cefpodoxime proxetil (and other
Cephalosporins)

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Selectively inhibits
bacterial dihydrofolic
acid reductase, which
converts dihydrofolic
acid to tetrahydrofolic
acid, a step leading to
the synthesis of
purines and ultimately
to DNA.
company name
Trimethoprim and TMP-SMX

Trimethoprim is about 50,000 times less

efficient in inhibition of mammalian
dihydrofolic acid reductase.
Trimethoprim + Sulfonamide
Blocks sequential steps in folate
synthesis.
Bactericidal
(Sulfonamide alone is bacteriostatic)

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Pharmacokinetics
Mode of administration
PO (Trimethoprim, and TMP-SMX)
Intravenously (TMP-SMX) .
Trimethoprim is well absorbed from the gut
and distributed widely in body fluids and
tissues, including cerebrospinal fluid.

company name
Pharmacokinetics
Trimethoprim is more lipid-soluble than
sulfamethoxazole
Trimethoprim has a larger volume of
distribution than sulfamethoxazole.
TMP : SMX = 1 : 5 1:20 peak plasma
concentration
Optimal for the combined effects of these
drugs in vitro.
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Pharmacokinetics
Excretion
About 3050% of the sulfonamide and 5060%
of the trimethoprim (or their respective
metabolites) are excreted in the urine within 24
hours.
The dose should be reduced by half for patients
with creatinine clearances of 1530 mL/min.

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Pharmacokinetics
Concentrates in prostatic fluid and in
vaginal fluid, which are more acidic than
plasma.
Has more antibacterial activity in prostatic and
vaginal fluids than many other antimicrobial
drugs.

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Pharmacokinetics
Drug Half-Life Oral Absorption

Sulfonamides

Sulfacytine Short Prompt (peak levels in 14 hours)

Sulfisoxazole Short (6 hours) Prompt

Sulfamethizole Short (9 hours) Prompt

Sulfadiazine Intermediate (1017 hours) Slow (peak levels in 48 hours)

Sulfamethoxazole Intermediate (1012 hours) Slow

Sulfapyridine Intermediate (17 hours) Slow

Sulfadoxine Long (79 days) Intermediate

Pyrimidines

Trimethoprim Intermediate (11 hours) Prompt

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Adverse Effects
Megaloblastic anemia
Leukopenia
Granulocytopenia
Nausea and vomiting
Drug fever
Vasculitis
Renal damage
CNS disturbances company name
Adverse Effects
Patients with AIDS and pneumocystis pneumonia
have a particularly high frequency of untoward
reactions to trimethoprim-sulfamethoxazole,
Fever
Rashes
Leukopenia
Diarrhea
Elevations of hepatic aminotransferases,
Hyperkalemia
Hyponatremia
company name
 Active against a variety of gram-positive
and gram-negative bacteria.

company name
Mode of Action

Fluoroquinolones

Inhibiting bacterial
Inhibit bacterial
topoisomerase II (DNA
topoisomerase IV
gyrase)

Prevents the relaxation Interferes with

of positively supercoiled
DNA that is required for
normal transcription and
replication
separation of replicated
chromosomal DNA into
the respective daughter
cells during cell division
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Pharmacokinetics
Drug Half-Life (h) Oral Peak Serum Oral Dose (mg) Primary Route of
Bioavailability Concentration ( Excretion
(%) g/mL)
Ciprofloxacin 35 70 2.4 500 Renal

Gatifloxacin 8 98 3.4 400 Renal

Gemifloxacin 8 70 1.6 320 Renal &

nonrenal
Levofloxacin 57 95 5.7 500 Renal

Lomefloxacin 8 95 2.8 400 Renal

Moxifloxacin 910 > 85 3.1 400 Nonrenal

Norfloxacin 3.55 80 1.5 400 Renal

Ofloxacin 57 95 2.9 400 Renal

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Pharmacokinetics
Mode of administration
PO
IV
Well absorbed (bioavailability of 8095%) and
distributed widely in body fluids and tissues.
Serum half-lives range from 3 to 10 hours.
The relatively long half-lives of levofloxacin,
gemifloxacin gatifloxacin, and moxifloxacin permit
once-daily dosing.
company name
Pharmacokinetics
Oral absorption is impaired by divalent
cations, including those in antacids.
Excretion
Most are eliminated by renal mechanisms,
either tubular secretion or glomerular filtration.
Nonrenally cleared fluoroquinolones are
relatively contraindicated in patients with
hepatic failure.

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Pharmacokinetics
Norfloxacin
The least active of the fluoroquinolones against both
gram-negative and gram-positive organisms.
Minimum inhibitory concentrations (MICs) fourfold to
eightfold higher than those of ciprofloxacin.

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Pharmacokinetics
Ciprofloxacin, enoxacin, lomefloxacin, levofloxacin,
ofloxacin, and pefloxacin (second group of quinolones)
Excellent gram-negative activity.
Moderate to good activity against gram-positive bacteria.
MICs for gram-negative cocci and bacilli, including
Enterobacteriaceae, pseudomonas, neisseria, haemophilus,
and campylobacter, are 12 mcg/mL and often less.
Ciprofloxacin is the most active agent of this group against
gram-negatives, P aeruginosa in particular.
Levofloxacin, the L-isomer of ofloxacin, has superior activity
against gram-positive organisms, including S pneumoniae.

company name
Pharmacokinetics
Gatifloxacin, gemifloxacin, and moxifloxacin (third
group of fluoroquinolones)
Improved activity against gram-positive organisms,
particularly S pneumoniae and some staphylococci.
MICs of these agents for staphylococci are lower than
those of the second group.
None of these agents is as active as ciprofloxacin against
gram-negative organisms.
Moxifloxacin also has good activity against anaerobic
bacteria.
Because of toxicity, gatifloxacin is no longer available in
the USA.

company name
Adverse Effects
Extremely well tolerated.
The most common effects are
Nausea, vomiting, and diarrhea. Occasionally,
headache, dizziness, insomnia, skin rash, or
abnormal liver function tests develop.
Photosensitivity has been reported with
lomefloxacin and pefloxacin.

company name
Adverse Effects
QTc prolongation may occur with gatifloxacin,
levofloxacin, gemifloxacin, and moxifloxacin.
Ideally, these agents should be avoided or used with caution
in patients with
Known QTc interval prolongation or uncorrected hypokalemia;
In those receiving class IA (eg, quinidine or procainamide) or class
III antiarrhythmic agents (sotalol, ibutilide, amiodarone);
In patients receiving other agents known to increase the QTc
interval (eg, erythromycin, tricyclic antidepressants).
Gatifloxacin
Hyperglycemia in diabetic patients
Hypoglycemia in patients also receiving oral hypoglycemic agents.
Withdrawn from sales in the USA in 2006; it may be available
elsewhere.

company name
Adverse Effects
May damage growing cartilage and cause an
arthropathy.
Not routinely recommended for patients under
18 years of age.
Tendinitis
Rare
Contraindicated during pregnancy.

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 Bacteriostatic and bactericidal for many gram-
positive and gram-negative bacteria
but P aeruginosa and many strains of proteus are
resistant.
There is no cross-resistance between
nitrofurantoin and other antimicrobial agents and
resistance emerges slowly.
Thus, it becomes an important alternative oral agent
for treatment of uncomplicated urinary tract infection.

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Pharmacokinetics
Nitrofurantoin is well absorbed after ingestion.
It is metabolized and excreted so rapidly that no
systemic antibacterial action is achieved.
Excreted into the urine by both glomerular
filtration and tubular secretion.
With average daily doses, concentrations of 200
mcg/mL are reached in urine.

company name
Pharmacokinetics
Dose for urinary tract infection
Adults: 100 mg orally , 4x/day.
It is desirable to keep urinary pH below 5.5,
greatly enhances drug activity.
A single daily dose of nitrofurantoin, 100
mg, can prevent recurrent urinary tract
infections in some women.

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Adverse Effects
Nitrofurantoin is contraindicated in patients
with significant renal insufficiency.
It should not be used to treat upper urinary
tract infection.

company name
Adverse Effects
Anorexia
Nausea
Vomiting
Neuropathies and hemolytic anemia occur in
G6PD patients.
Rashes
Pulmonary infiltration
Fibrosis
Other hypersensitivity reactions
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 Inhibit bacterial growth by interfering with
the transpeptidation reaction of bacterial
cell wall synthesis.
Kill bacterial cells only when they are
actively growing and synthesizing cell wall.

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Penicillins (Amoxicillin, Ampicillin,
Ticarcillin/Clavulanate)

company name
Penicillins (Amoxicillin, Ampicillin,
Ticarcillin/Clavulanate)

Covalently bind
to the active site Inhibits the Halting
Lactam
of PBPs transpeptidation peptidoglycan Cell dies
antibiotics
(Penicillin- reaction synthesis
binding protein)

company name
Pharmacokinetics
Oral administration
Acid-stable and relatively well absorbed.
Serum concentrations :
48 mcg/mL (after a 500 mg oral dose)
Absorption is impaired by food (except
amoxicillin)
Should be administered at least 12 hours before or
after a meal.

company name
Pharmacokinetics
Parenteral administration
Absorption of most penicillins is complete and rapid.
Serum concentrations 30 minutes after an intravenous
injection of 1 g of a penicillin (equivalent to
approximately 1.6 million units of penicillin G) are 20
50 mcg/mL.
Only a small amount of the total drug in serum is
present as free drug, the concentration of which is
determined by protein binding.
Widely distributed in body fluids and tissues with a few
exceptions.
company name
Pharmacokinetics
Excretion
Rapidly excreted by the kidneys
10% of renal excretion is by glomerular filtration
90% by tubular secretion.
Ampicillin and the extended-spectrum
penicillins are secreted more slowly than
penicillin G and have half-lives of 1 hour.

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Pharmacokinetics
Administration Adult Dose Pediatric Dose1 Neonatal Dose2 Clcr Approx 50 Clcr Approx 10
mL/min mL/min

Extended-spectrum penicillins
Amoxicillin 0.250.5 g tid 2040 66% 33%
(PO) mg/kg/d in 3
doses
Ticarcillin 3 g q46h 200300 150200 5075% 2533%
(IV) mg/kg/d in 4 mg/kg/d in 2
6 doses or 3 doses

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Adverse Effects
The penicillins are remarkably nontoxic.
Most of the serious adverse effects are due
to hypersensitivity.

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Adverse Effects
Allergic reactions
Anaphylactic shock (very rare0.05% of recipients);
Serum sickness-type reactions
Now rare
Urticaria, fever, joint swelling, angioneurotic edema,
intense pruritus, and respiratory embarrassment
Occurring 712 days after exposure
A variety of skin rashes.

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Adverse Effects
Oral lesions
Fever
Interstitial nephritis (an autoimmune
reaction to a penicillin-protein complex)
Eosinophilia
Hemolytic anemia and other hematologic
disturbances
Vasculitis
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 First Generation
Second Generation
Third Generation
Fourth Generation

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 This includes cefadroxil, cefazolin,
cephalexin, cephalothin, cephapirin, and
cephradine.
Very active against gram-positive cocci,
such as
Pneumococci
Streptococci
Staphylococci
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Other Bacterias
o E coli o Indole-positive proteus (X)
o K pneumoniae o Enterobacter (X)
o Proteus mirabilis o Serratia marcescens (X)
o Anaerobic cocci (eg, o Citrobacter (X)
peptococcus, o Acinetobacter (X)
peptostreptococcus) are o Methicillin-resistant strains
usually sensitive of staphylococci (X)
o Bacteroides fragilis (X)
o P aeruginosa (X)

company name
Pharmacokinetics
Cephalexin, cephradine, and cefadroxil
are absorbed from the gut to a variable extent.
Serum levels are 1520 mcg/mL (After oral
doses of 500 mg)
Urine concentration is usually very high
In most tissues levels are variable and
generally lower than in serum.

company name
Pharmacokinetics
Cephalexin and cephradine
Orally, 0.250.5 g four times daily (1530 mg/kg/d)
Cefadroxil
IV, 0.51 g twice daily.
Excretion
Mainly by glomerular filtration and tubular secretion
into the urine.
Drugs that block tubular secretion, eg, probenecid,
may increase serum levels substantially.
company name
Pharmacokinetics
Adjusted Dose as a Percentage of
Normal Dose for Renal Failure
Based on Creatinine Clearance
(Clcr)

Antibiotic (Route Adult Dose Pediatric Dose1 Neonatal Dose2 Clcr Approx 50 Clcr Approx 10
of mL/min mL/min
Administration)
First-generation cephalosporins

Cefadroxil (PO) 0.51 g qdbid 30 mg/kg/d in 2 50% 25%

doses
Cephalexin, 0.250.5 g qid 2550 mg/kg/d 50% 25%
cephradine (PO) in 4 doses
Cefazolin (IV) 0.52 g q8h 25100 mg/kg/d 50% 25%
in 3 or 4 doses

The oral drugs are those used for UTI.

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 This innclude cefaclor, cefamandole,
cefonicid, cefuroxime, cefprozil,
loracarbef, and ceforanide and the
structurally related cephamycins cefoxitin,
cefmetazole, and cefotetan
Have activity against anaerobes.

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Second Generation Cephalosporins
Active against organisms inhibited by first-
generation drugs, but in addition they have
extended gram-negative coverage.
Klebsiellae
Cefamandole, cefuroxime, cefonicid,
ceforanide, and cefaclor
H influenzae
Serratia (X)
B fragilis (X) company name
Second Generation Cephalosporins
Cefoxitin, cefmetazole, and cefotetan
B fragilis
Some serratia strains
H influenzae (X)
Enterococci (X)
P aeruginosa (X)
Enterobacter (X) due to resistance

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Pharmacokinetics
Adjusted Dose as a Percentage of
Normal Dose for Renal Failure
Based on Creatinine Clearance
(Clcr)

Antibiotic Adult Dose Pediatric Dose1 Neonatal Dose2 Clcr Approx 50 Clcr Approx 10
(Route of mL/min mL/min
Administration)
Second-generation cephalosporins

Cefoxitin 12 g q68h 75150 5075% 25%

(IV) mg/kg/d in 3
or 4 doses
Cefotetan 12 g q12h 50% 25%
(IV)
Cefuroxime 0.751.5 g 50100 66% 2533%
(IV) q8h mg/kg/d in 3
or 4 doses
Cefuroxime 0.250.5 g bid 0.1250.25 g 100% 25%
axetil (PO) bid

company name
 Include cefoperazone, cefotaxime,
ceftazidime, ceftizoxime, ceftriaxone,
cefixime, cefpodoxime proxetil, cefdinir,
cefditoren pivoxil, ceftibuten, and
moxalactam.
Have expanded gram-negative coverage
Able to cross the blood-brain barrier.

company name
Third Generation Cephalosporins
o Citrobacter o Providencia (X) due to
o S marcescens resistance
o Providencia o Citrobacter (X) due to
o Lactamase-producing resistance
strains of haemophilus and o Ceftizoxime and
neisseria moxalactam
o B fragilis
o Ceftazidime and
cefoperazone o Cefixime and ceftibuten
o P aeruginosa o Pneumococci (X)
o Enterobacter (X) o S aureus (Poor)
o Serratia (X) due to company name
resistance
Pharmacokinetics
Penetrate body fluids and tissues well and, (Except
cefoperazone and all oral cephalosorins)
Cross BBB
Excretion
Cefoperazone and ceftriaxone mainly through the
biliary tract
The others are excreted by the kidney (require dosage
adjustment in renal insufficiency)

company name
Pharmacokinetics
Adjusted Dose as a Percentage of Normal
Dose for Renal Failure Based on
Creatinine Clearance (Clcr)

Antibiotic (Route of Adult Dose Pediatric Dose1 Neonatal Dose2 Clcr Approx 50 Clcr Approx 10
Administration) mL/min mL/min

Third- and fourth-generation cephalosporins

Cefotaxime (IV) 12 g q612h 50200 mg/kg/d 100 mg/kg/d in 50% 25%

in 46 doses 2 doses
Ceftazidime 12 g q812h 75150 mg/kg/d 100150 50% 25%
(IV) in 3 doses mg/kg/d in 2 or
3 doses
Ceftriaxone (IV) 14 g q24h 50100 mg/kg/d 50 mg/kg/d None None
in 1 or 2 doses once a day
Cefepime (IV) 0.52 g q12h 75120 mg/kg/d 50% 25%
in 2 or 3 divided
doses

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 Example: Cefepime.
More resistant to hydrolysis by chromosomal -
lactamases (eg, those produced by enterobacter).
P aeruginosa
Enterobacteriaceae
S aureus
S pneumoniae

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Fourth Generation Cephalosporin
Haemophilus
Neisseria
Penicillin-resistant strains of streptococci
Enterobacter infections
It penetrates well into cerebrospinal fluid
Excretion
It is cleared by the kidneys
Half-life : 2 hours

company name
Fourth Generation Cephalosporin
Clinical role is similar to that of third-
generation cephalosporins.

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 Writing a prescription should be based on a
series of rational steps

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 Prescriptions based merely on a desire to satisfy the
patient's psychological need for some type of therapy
are often unsatisfactory and may result in adverse
effects. A specific diagnosis, even if it is tentative, is
required to move to the next step. The diagnosis and
Make a specific the reasoning underlying it should be shared with the
diagnosis patient.

If the disorder is well understood, the prescriber is in

a much better position to offer effective therapy. The
Consider the patient should be provided with the appropriate level
pathophysiologic and amount of information about the pathophysiology.
implications of the
diagnosis

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 A therapeutic objective should be chosen for each of
the pathophysiologic processes defined in the
Select a specific preceding step.
therapeutic
objective

One or more drug groups will be suggested by each of

the therapeutic goals specified in the preceding step.
For certain drugs, characteristics such as age, other
diseases, and other drugs being taken are extremely
Select a drug of important in determining the most suitable drug for
choice management of the present complaint.

company name
 The dosing regimen is determined primarily by the pharmacokinetics of the drug
in that patient. If the patient is known to have disease of the organs required for
elimination of the drug selected, adjustment of the average regimen is needed.
Determine the
appropriate dosing
regimen

The prescriber should be able to describe to the patient the kinds of drug
effects that will be monitored and in what way, including laboratory tests (if
necessary) and signs and symptoms that the patient should report. For
conditions that call for a limited course of therapy (eg, most infections), the
duration of therapy should be made clear so that the patient does not stop
Devise a plan for taking the drug prematurely and understands why the prescription probably
need not be renewed. The prescriber should also specify any changes in the
monitoring the drug's patient's condition that would call for changes in therapy. Major toxicities that
action and determine an require immediate attention should be explained clearly to the patient.
end point for therapy

company name
 The prescriber and other members of the health
team should be prepared to repeat, extend, and
reinforce the information transmitted to the
patient as often as necessary. The more toxic the
Plan a program of drug prescribed, the greater the importance of
patient education this educational program.

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 Prescription can be written on any piece of
paper (as long as all of the legal elements
are present)
It usually takes a specific form

company name
company name
 Identity of the prescriber.
Name, license classification (ie, professional degree),
address, and office telephone number.

Identity of the patient.

Elements that specify the medication, the strength and

quantity to be dispensed, the dosage, and complete
directions for use. (8-11)

Refill information, waiver of the requirement for

childproof containers, and additional labeling
instructions (eg, warnings such as "may cause
drowsiness," "do not drink alcohol").

Prescriber's signature and other identification data.

company name
 Prescription Writing
Drug name [8]
Either the brand name (proprietary name) or the generic name
(nonproprietary name) may be used.
The strength of the medication [9]
Should be written in metric units.
The strength of a solution is usually expressed as the quantity of
solute in sufficient solvent to make 100 mL; for instance, 20%
potassium chloride solution is 20 grams of KCl per deciliter (g/dL)
of final solution. Both the concentration and the volume should be
explicitly written out.

company name
 Prescription Writing
1 grain (gr) = 0.065 grams (g), often rounded to 60 milligrams (mg)
15 gr = 1 g
1 ounce (oz) by volume = 30 milliliters (mL)
1 teaspoonful (tsp) = 5 mL
1 tablespoonful (tbsp) = 15 mL
1 quart (qt) = 1000 mL
1 minim = 1 drop (gtt)
20 drops = 1 mL
2.2 pounds (lb) = 1 kilogram (kg)

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 Prescription Writing
The quantity of medication
Should reflect the anticipated duration of
therapy, the cost, the need for continued
contact with the clinic or physician, the
potential for abuse, and the potential for
toxicity or overdose.

company name
 Prescription Writing
The directions for use [11]
Must be both drug-specific and patient-specific.
The simpler the directions, the better.
The fewer the number of doses (and drugs) per
day, the better.

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Example
Ms. GA, was diagnosed with acute uncomplicated cystitis,
infected by E. coli. Non-diabetic, not pregnant.

Treatment:
7-day regimen: macrocrystalline nitrofurantoin.
Available preparation:
Nitrofurantoin (generic, Macrodantin) Oral: 25, 50, 100 mg
capsules, 25 mg/5 mL suspension.
Dose: 100 mg orally , 4x/day for 7 days.

company name
Example

Ms. G. Abuan 13 Oct 09

Rayvells Dormitory. Tamag.

Macrodantin, 100 mg

#28 capsules

Take 1 capsule 4x a day. for 7 days.

0

John B. Doe
N/A

company name
 Women who experience frequent
symptomatic UTIs (3 per year on average)
Candidates for long-term administration of low-
dose antibiotics directed at preventing
recurrences.
Advised to avoid spermicide use and to void
soon after intercourse.

company name
 Prophylaxis
Daily or thrice-weekly administration of a single dose of
TMP-SMX (80/400 mg),
TMP alone (100 mg), or
Nitrofurantoin (50 mg)
Fluoroquinolones

Prophylaxis should be initiated only after

bacteriuria has been eradicated with a full-dose
treatment regimen.
company name
 The same prophylactic regimens can be used after
sexual intercourse to prevent episodes of
symptomatic infection in women in whom UTIs
are temporally related to intercourse.
Postmenopausal women who are not taking oral
estrogen replacement therapy can effectively
manage recurrent UTIs with topical intravaginal
estrogen cream.

company name
 Other patients for whom prophylaxis appears to
have some merit include
Men with chronic prostatitis;
Patients undergoing prostatectomy (during operation
and postoperatively)
Pregnant women with asymptomatic bacteriuria.
All pregnant women should be screened for
bacteriuria in the first trimester and should be
treated if bacteriuria is detected.

company name