Universidad De Dagupan

Arellano St., Dagupan City

School of Health Sciences-College of Nursing

Academic Year 22-23, First Semester

NCM 106 (Nursing Pharmacology)

Anti-infective Agents

• This chapter discuss the specific agents that are used to treat particular infections: anti-
bacterial used to treat bacterial infections; antiviral; antifungals; antiprotozoals which are
used to treat infections caused by a specific protozoa including malaria, antihelmintics
that are used to treat infections caused by worms; and antineoplastics which are used to
treat cancers caused by abnormal cells
• Before the ancient Chinese found that applying moldy soybean curds to boils and
infected wounds helped prevent infection or hastened cure in which their finding was,
perhaps, a precursor to the penicillins used today.
• Paul Ehrlich was the first scientist to work on developing a synthetic chemical that would
be effective only against infection-causing cells, not human cells.

Mechanism of actions

• Some anti-infectives interfere with biosynthesis of the bacterial cell wall.

• Many anti-infectives interfere with the steps involved in protein synthesis, a necessary
function to maintain the cell and allow for cell division.
• Some anti-infectives interfere with DNA synthesis in the cell, leading to inability to
divide and cell death.
• Other anti-infectives alter the permeability of the cell membrane to allow essential
cellular components to leak out, causing cell death.

Resistance

• Because ant-infectives act on specific enzyme systems or biological processes, many

microorganisms that do not use that system or process are not affected by a particular
anti-infective drug.
• This can result in a serious clinical problem. The emergence of resistant strains of
bacteria and other organisms poses a threat.
• Producing an enzyme that deactivates the antimicrobial drug like for example, some
strains of bacteria that were once controlled by penicillin now produce an enzyme called
penicillinase, which inactivates penicillin before it affects the bacteria.
• Changing cellular permeability to prevent the drug from entering the cell or altering
transport systems to exclude the drug from active transport into the cell.
• Altering binding sites on the membranes or ribosomes, which then no longer accept the
drug
• Producing a chemical that acts as an antagonist to the drug.
 • Drug dosage is important in preventing the development of resistance. Doses should be
high enough and the duration of drug therapy should belong enough to eradicate even
slightly resistant microorganisms
• The recommended dosage for a specific anti-infective agent takes this issue into account
• Around the clock dosing eliminates the peaks and valleys in drug concentration and helps
maintain a constant therapeutic level to prevent the emergence of resistant microbes
during the times of low concentration.
• The duration of the time is critical to ensure that the microbes are completely, not
partially, eliminates and are not given the chance to grow and develop resistant strains.
• Many people stop taking the drug once they start to feel better and then keep the
remaining pills to treat themselves at some time in the future when they do not fell well.
• Health care providers who prescribe anti-infectives without knowing the causative
organism and which the drugs might be appropriate are promoting the emergence of
resistant strains of microbes.

Combination Therapy

• This allow the health care provider to use smaller dosage of each drug, leading to fewer
adverse effects but still having a therapeutic impact on the pathogen.
• Some drugs are synergistic, which means that they are more powerful when given in
combination.
• Many microbial infections are caused by more than one organism, and each pathogen
may react to a different anti-infective agent.
• Diseases that needs combination therapy treatment like tuberculosis and malaria.

Adverse Reactions of ANTI-INFECTIVE THERAPY

• Kidney Damage

- When patients are taking drugs like aminoglycosides, they should be monitored closely
for any signs of renal dysfunction.
- To prevent any accumulation of the drug in the kidney, patients should be well hydrated
throughout the course of the drug therapy.

• Gastrointestinal Toxicity

- This is very common with anti-infectives and have a direct toxic effects on the cells
lining on the GI tract causing nausea, vomiting, stomach upset or diarrhea.
- In addition, some anti-infectives are toxic to the liver like cephalosporins, and they
should be monitored closely and the drug should be stopped at any sign of liver
dysfunction.

• Neurotoxicity

- This can damage or interfere with the function of nerve tissue.

- Aminoglycosides can be collect at eight cranial nerve and can cause dizziness, vertigo,
and loss of hearing
- Chloroquine, the drugs that is used to treat malaria can accumulate to retina and optic
nerve and may cause blindness

• Hypersensitivity Reactions
 - Some drugs have demonstrated cross-sensitivity (e.g. penicillins, cephalosporins) and
care must be taken to obtain a complete patient history before administering one of these
drugs.

SUPERINFECTIONS

- When the normal flora is destroyed, opportunistic pathogens that were kept in check by
the normal bacteria have the opportunity to invade tissues and cause infections.
- Example of these are vaginal or yeast infections, Pseudomonas and Proteus.

PROPHYLAXIS

- It is clinically useful to prevent infections before they occur.

- Example of these are Crede’s prophylaxis, Pen G administration to congenital heart
disease.

Antibiotics

- These are the chemicals that inhibit specific bacteria.

- These substances that prevent the growth of bacteria is called bacteriostatic.
- These substances that kills bacteria directly is called bactericidal.
- These are used to treat a wide variety of systemic and topical infections.

Classifications of Anti-bacterials:

1. Aminoglycosides
2. Cephalosporin
3. Flouroquinolones
4. Lincosamides

5. Macrolides

6. Monobactams

7. Penicillins

8. Sulfonamides

9. Tetracyclines

10. Anti-TB and Anti-Leprosy

Aminoglycosides

- Are group of powerful antibacterial used to treat serious infections caused by gram-
negative, aerobic bacilli.

• Amikacin
 • Gentamicin
• Kanamycin
• Neomycin
• Tobramycin

Therapeutic Actions and Indications:

• Bactericidal. They inhibit CHON synthesis in susceptible strains of gram-negative

bacteria, which in turn leads to loss of functional integrity of the cell membrane, causing
cell death.

Pharmacokinetics

• Peak levels: within 1 hour

• Average half-life: 2-3 hours

Contraindications and Cautions

• Renal and hepatic disease

• Pre-existing hearing loss
• Active infection like herpes and mycobacterium
• Myasthenia gravis and Parkinsonism
• Lactating mothers

Adverse Effects

CNS: ototoxicity

Renal: nephrotoxicity

Hema: Bone marrow depression

GI: nausea, vomiting, diarrhea, weight loss, stomatitis and hepatotoxicity

CV: palpitations, hypotension, hypertension,

Immune: Hypersensitivity like purpura, rash, urticaria

Drug-Drug Interactions:

• Potent diuretics, Anesthetics, Neuromuscular blockers

Cephalosporins
- First introduced in the 1960s.
- Overtime, four generations of cephalosporins have been introduced, each group with it’s
own spectrum of activity.

FIRST GENERATON CEPHALOSPORINS

- Largely effective against the gram-positive bacteria that are affected by Penicillin G., as
well as the gram-negative bacteria

• Cefadroxil
• Cefazolin
• Cephalexin

• Cephradine

SECOND GENERATION CEPHALOSPORINS

- Are effective for those strains, as well as Haemophilus influenzae, Enterobacter
aerogenes, and Neisseria species (HENPecK)

• Cefaclor
• Cefmetazole
• Cefoxitin
• Cefprozil
• Cefuroxime
• Loracerbef

THIRD GENERATION CEPHALOSPORINS

- Is relatively weak against gram-positive bacteria but more potent against the gram-
negative bacilli, as well as, Serratia macescens.

• Cefdinir
• Cefoperazone
• Cefotaxime
• Cefpodoxime
• Ceftazidime
• Ceftibuten
• Ceftizoxime
• Ceftriaxone

FOURTH GENERATION CEPHALOSPORINS

- it’s first drug of this group, Cefipime, is an active against grame-negative and gram-
positive organisms, including cephalosporin-resistant staphylococci and P. aeruginosa.

• Cefditoren
• Cefipime
• Cefpirole

Therapeutic Actions and Indications

• Both bactericidal and bacteriostatic, depending on the dose used and the specific drug
involved. Basically, interfering with cell-wall building ability of bacteria when they
divide; they prevent the bacteria from biosynthesizing the framework of their cell walls.

Pharmacokinetics
 • Peak: 30-60 min (oral)
• Duration: 810 hours

Contraindications and Cautions

• Allergic reaction – cross-sensitivity
• Renal failure
• Lactating clients

Adverse Effects
GI: nausea, vomiting, diarrhea, anorexia, abdominal pain, and flatulence,
pseudomembranous colitis
CNS: headache, dizziness, lethargy, and paresthesia
Renal: increased BUN and serum crea
Immune: superinfections

Drug-Drug Interactions
• Oral anticoagulants – increased risk of bleeding (bruising, bleeding gums)
• Alcohol – disulfiram like-reactions (flushing, throbbing headache, nausea and vomiting,
chest pain, palpitations, blurred vision

Fluoroquinolones

- New class of antibacterial with a broad spectrum of activity. Made synthetically that are
associated mild adverse reactions.
- The most widely used is CIPROFLOXACIN (CiproBay), that is effective against a wide
spectrum of gram-negative bacteria. It is available in oral, injectable and topical forms.

• Ciprofloxacin
• Gemifloxacin
• Levofloxacin
• Lomefloxacin
• Moxifloxacin
• Norfloxacin
• Ofloxacin
• Sparfloxacin

Therapeutic Actions and Indications

• Both bactericidal and bacteriostatic.
• Enter the bacterial cell by passive diffusion through channels in the cell membrane. Once
inside, they interfere with the action of DNA enzymes necessary for growth and
reproduction of the bacteria. This leads to cell death because the bacterial DNA is
damaged and the cell cannot be maintained.

Pharmacokinetics
• Onset: Varies (oral), 10 mins (IV)
• Peak: 60-90 mins, 30 mins
• Duration: 4-5 hours

Contraindications and Cautions

• Pregnant women
• Renal dysfunction
 Drug-Drug Interactions
• Iron salts, sucralfate, mineral supplements or antacids – therapeutic effects will
decreased; separated administration by at least 4 hours.
• Quinidine, amiodarone, erythromycin, pentamidine, tricyclics - torsades de pointes
• Theophylline –increased theophylline levels

Adverse Effects
CNS: headache, dizziness, insomnia, depression
GI: nausea, vomiting, diarrhea, dry mouth
Hema: bone marrow depression
Immune: fever, rash, skin reactions
Others: photosensitivity

Macrolides

- These are antibiotics that interfere with protein synthesis in susceptible bacteria.

• Erythromycin - drug of choice for Legionnaire’s disease

• Azithromycin - used to treat mild to moderate upper respiratory infections; urethritis and
otitis media, pharyngitis, and tonsillitis
• Clarithromycin - expensive oral agents used to treat several skin, sinus and maxillary
infections
• Dirithromycin – effective in treating upper and lower respiratory tract infections, skin
infections and pharyngitis/tonsillitis.

Therapeutic Actions and Indications

• Both bactericidal and bacteriostatic. It exerts their effect by binding to the bacterial cell
membranes and changing protein function.

Pharmacokinetics
• Erythromycin - half-life: 1.6 hours
• Azithromycin - half-life: 68 hours
• Clarithromycin - half-life: 3-7 hours
• Dirithromycin – half-life: 2-36 hours

Contraindications and Cautions

• Known allergy, renal disease
• Lactating women

Adverse Effects
CNS: confusion, abnormal thinking, uncontrollable emotions
GI: abdominal cramping, anorexia, nausea, vomiting, pseudomembranous colitis
Immune: hypersensitivity reactions like rash, anaphylaxis, superinfections
Drug-Drug Interactions
• Digoxin, oral anticoagulants, theophyllines, carbamazepine, corticosteroids, cycloserine –
increased levels

Drug-Food Interactions
• Given on an empty stomach berore or at least 2-3 hours after meals and be taken with a
full, 8 ozz glass of water.
Lincosamides

- Similar to macrolides, but more toxic. It reacts at almost the same site in bacterial protein
synthesis and are effective against the same strains of bacteria.

• Clindamycin
- Has as half-life of 2-3 hours
- Needs to be given cautiously in patients with hepatic or renal impairment
• Lincomycin
- Has a half-life of 5 hours

Adverse Effect
- Bone marrow depression, bloody diarrhea, pseudomembranous colitis

Monobactam Antibiotics

- With its structure as a unique, it has a little cross-resistance occurrence.

• Aztreonam

- Effective against gram-negative enterobacteria and has no effect on gram-positive or

anaerobic bacteria
- Absorbed well after IM injection, reaching its peak levels in 1-1.5 hours with its half-life
of 1.5-2 hours.

Therapeutic Actions and Indications

• It disrupts bacterial cell wall synthesis, which promotes leakage of cellular contents and
cell death in susceptible bacteria

Adverse Effects

GI: GI upset, vomiting, increased hepatic liver enzymes

Others: inflammation, phlebitis, discomfort, anaphylaxis

PENICILLINS & PENICILLINASE-Resistant Antibiotics

- First antibiotic introduced in 1920s. Penicillium molds was used by Dr. Alexander Fleming.

- With the prolonged use of penicillins, more and more bacterial species have synthesized
the enzyme penicillinase to counteract the effects of penicillin.
- Culture and sensitivity testing is mandatory to be implemented when using this antibiotic
to ensure that the causative organism is sensitive to penicillin selected for use.

PENICILLINS

• Penicllin B benzathine
• Penicllin G potassium
• Penicillin G procaine
• Penicillin V
EXTENDED PENICILLIN-SPECTRUM

• Amoxicillin
• Ampicillin
• Carbenicillin
• Ticarcillin

PENICILLIN-RESISTANT ANTIBIOTICS

• Nafcillin
• Oxacillin

Therapeutic Action and Indications

• Penicillin and penicillinase-resistant antibiotics produce a bactericidal effects by

interfering with the ability of susceptible bacteria to build their cell walls when they are
dividing
• The penicillin’s are indicated for the treatment of streptococcal infections, including
pharyngitis, tonsillitis, scarlet fever, and endocarditis.
Pharmacokinetics
• In the GI tract, it reaches it’s peak level in 1 hour. And must be taken in an empty
stomach to ensure adequate absorption.
Contraindications and Cautions
• These drugs are contraindicated in patients who have allergy in penicillin or
cephalosporins.
• Cautiously used in patients who have renal disease, pregnant and lactating mothers.

Adverse Effects
GI: nausea, vomiting, diarrhea, abdominal pain, glossitis, stomatitis, gastritis, sore mouth
and furry tongue
Others: hypersensitivity reactions like rash, fever, wheezing, anaphylaxis

Drug-Drug Interactions
• Tetracyclines – decrease effectiveness of the penicillin
• Aminoglycoside – inactivation itself by the penicillin

Sulfonamides

- SULFA DRUGS.
- Are drugs that inhibit folic acid synthesis.

• Sulfadiazine
• Sulfisoxazole
• Sulfasalazine
• Cotrimoxazole

Therapeutic Actions and Indications

• It competitively blocks para-aminobenzoic acid (PABA) to prevent folic acid synthesis in

susceptible bacteria that synthesize their own folates for the production of RNA and
DNA.
 Contraindications and Cautions
• Known allergy to sulfa, sulfonylureas or thiazide diuretics – cross-sensitivities
occurences
• Pregnancy – teratogenic effects (Pregnancy Category X)
• Lactation, renal disease or history of kidney stones

Adverse Effects
GI: nausea, vomiting, diarrhea, abdominal pain, anorexia, stomatitis, and hepatic injury
Renal: crystalluria, hematuria, proteinuria
CNS: headache, dizziness, vertigo, ataxia, convulsions, depression
Hema: Bone marrow depression
Others: Photosensitivity, rash

Drug-Drug Interactions
• Tolbutamide, Tolazamide, Glyburide, Glipizide, Acetazolamide, or Chlorpropramide –
hypoglycemia
• Cyclosporine – nephrotoxicity

Tetracyclines

- Were developed as semi-synthetic antibiotics based on the structure of a common soild

mold.
- They work by inhibiting protein synthesis in susceptible bacteria, they are composed of
four rings.

• Tetracycline
• Demeclocyline
• Doxycycline
• Minocycline
• Oxytetracycline

Therapeutic Actions and Indications

• It can be also an adjunct in the treatment of certain protozoal infections.

Pharmacokinetics
• Half-life is ranging from 12-25 hours
Contraindication and Cautions
• Contraindicated in pregnant women, lactating mothers and children younger than 8 years
old

Adverse Effects
GI: nausea, vomiting, diarrhea, abdominal pain, glossitis, dysphagia, hepatotoxicity
Hema: hemolytic anemia, bone marrow depression
Others: bone fractures, photosensitivity and rash, superinfections, hypersensitivity
reactions

Drug-Drug Interactions
• Penicillin and tetracycline when taken concurrently – decrease the effectiveness of Pen
G.
• Oral contraceptives – decrease effectiveness of contraceptives
• Methoxyflurane – increased risk of nephrotoxicity
• Digoxin – rising levels when taken concurrently with tetracyclines
• Calcium alts, magnesium salts, zinc salts, aluminum salts, bismuth salts, iron, urinary
alkalinizers, charcoal - decreased absorption of tetracyclines
 Drug-Food Interactions
• Do not take with food or dairy products. Given in an empty stomach 1 hour before or 2-3
hour after meals or other medication

Antimycobacterial Antibiotics

• Antituberculosis
 Rifampicin
 Isoniazid
 Ethambutol
 Streptomycin

• Antileprosy
 Dapsone – mainstay treatment for leprosy
 Thalidomide (Thalomid)

Prepared by:

Edberg S. De Guzman, MSN, RN, CNN

NCM 106 Instructor

Approved by:

May Jacklyn Radoc-Samson, RN, LPT,

MANc

Dean, School of Health Sciences