AMH Summary: Chapter 5 – Anti-infectives 1

AMH SUMMARY
CHAPTER 5: ANTI-INFECTIVES

A. ANTIBACTERIALS

OVERVIEW OF PRINCIPLES
• Indications listed for monographs are not comprehensive, based on clinical practice and
evidence of appropriate use
• Choice considers likely infecting organism. Ideally use a narrow spectrum agent with few
adverse effects
• Anti-infectives should be used if there is clear evidence that it will not recover without its
use as many common infections can resolve spontaneously
• Never treat viral infections with anti-bacterials
• For prophylaxis, restrict to certain clinical conditions
• Use for surgical prophylaxis in procedures with high risk of infection such as abdominal
surgery, surgery with breach of colon, cardiac surgery
• Combination therapy used in mixed infections to cover whole spectrum, when anti-infective
synergy is needed or to prevent infective resistance to treatment
• Avoid topical use (except in eye) as sensitivity and resistance may occur
• Oral or rectal doses of anti-infectives are adequate, unless they are not available
• Duration of therapy dependent of the severity of infection
• Broader spectrum anti-infectives affect bacterial flora, more likely to cause gastrointestinal
adverse effects and superinfection with resistant organisms
• Resistance: judicious use of anti-infectives may slow emergence of resistant strains
• Probiotics should be avoided in severely ill or immunocompromised patients as they can
cause infections

AMINOGLYCOSIDES
(amikacin, gentamycin, tobramycin)
• Works by inhibiting protein synthesis by binding 30 S ribosome, causing membrane
damage
• Used for Gram negative infections, surgical and non-surgical prophylaxis
• Adverse effects include nephrotoxicity (presents as gradual worsening renal failure),
ototoxicity (nausea and vertigo)
• Counselling: If using for more than 7-10 days, kidneys may not work as well. Stopping
medication will improve its function
• Creatinine clearance and drug monitoring required if using for more than 48 hours.

CARBAPENEMS
(ertapenem, imipenem, meropenem)
• Works by inhibiting bacterial cell wall synthesis, bactericidal
• Specific conditions: allergy to penicillins- possibility of cross reactivity
• Adverse effects include nausea, vomiting, diarrhoea

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AMH Summary: Chapter 5 – Anti-infectives 2

• Broad spectrum antibiotics with good activity against Gram positive, Gram negative
bacteria and anerobes
• Practice points
- Useful when single treatment required for complex mixed infections
- P. aeruginosa may develop resistance quickly
- Monitor renal, hepatic function, complete blood picture during prolonged treatment

CEPHALOSPORINS
(cefaclor, cefepime, cefotaxime, cefoxitin, ceftazidime, ceftriaxone, cefuroxime, cephelexin,
cephalothin, cephazolin)
• Works by interfering with bacterial cell wall peptidoglycan synthesis
• Specific conditions:
• Allergy to penicillins- possibility of cross reactivity
• Impaired vitamin K synthesis- increased risk of bleeding
• Adverse effects include nausea, rash, electrolyte disturbances
• Cephalothin, cephalexin, cephazolin, cefaclor and cefoxitin considered moderate spectrum
cephalosporins
• Cefotaxime, ceftriaxone, ceftazidime are broad spectrum, with less Gram positive activity
• Practice points
- Monitor renal function and complete blood pictures
- Superinfection may occur, especially with broad spectrum cephalosporins

GLYCOPEPTIDES
(teicoplanin, vancomycin)
• Works by inhibiting bacterial cell wall synthesis by preventing formation of peptidoglycan
polymers
• Used in serious infections such as MRSA, surgical prophylaxis for major procedures
• Adverse effects: oral vancomycin- usually GI adverse effects, others include phlebitis,
nephrotoxicity and ototoxicity
• Narrow spectrum of action, mainly working on Gram positive bacteria
• Practice points: monitor renal function, blood picture and hearing during long courses

LINCOSAMIDES
(clindamycin, lincomycin)
• Inhibiting protein synthesis binding to 50S ribosomal subunit
• Alternative for those with severe allergy to penicillins
• Adverse effects include diarrhoea (mild to severe), nausea, vomiting, abdominal pains and
cramps
• Active against staphylococci and streptococci and most anaerobes
• Monitor complete blood count, hepatic and renal function
• Cross resistance of lincosamides and macrolides for staphylococci and streptococci

MACROLIDES
(azithromycin, roxithromycin, erythromycin, clarithromycin
• Works by binding to 50S subunit

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AMH Summary: Chapter 5 – Anti-infectives 3

• Used as an alternative to individuals with penicillin or cephalosporin allergies

• Also has immunomodulatory and anti-inflammatory effects
• Adverse effects include nausea, vomiting, diarrhoea, abdominal pain and cramps
• Oral erythromycin poorly tolerated due to GI effects
• Broad spectrum antibiotics against Gram positive and some Gram negative bacteria
• High degree of cross resistance between erythromycin and newer macrolides

NITROIMIDAZOLES
(metronidazole, tinidazole)
• Works by interfering with DNA synthesis
• Used for anaerobic infections, protozoal, amoebic infections and surgical prophylaxis
• Adverse effects include nausea, anorexia, abdominal pain and metallic taste
• Tinidazole has a longer half life and can be used daily and better tolerated than
metronidazole
• Practice points
- Monitor blood count and neurotoxic reactions for long treatment
- Most active against anaerobes
- No alcohol while on this medication (can cause severe reactions)

PENICILLINS
(amoxycillin and clavulanic acid, ampicillin, amoxycillin, benzathine penicillin, benzylpenicillin,
dicloxacillin, flucloxacillin, phenoxymethylpenicillin, piperacillin, procaine penicillin, ticarcillin)
• Works by affecting peptidoglycan synthesis
• Contraindications: allergic reactions to penicillins
• Adverse effects include diarrhoea, nausea, rash, urticaria, superinfection, broncospasm
(severe)
• Narrow spectrum penicillins act on Gram positive organisms (dicloxacillin, flucloxacillin)
• Moderate spectrum penicillins include amoxycillin and ampicillin
• Clavulanic acid extends the activity of pencillins such as amoxycillin to make it broad
spectrum
• Practice points
- Use frequent doses for maximal antibacterial effect
- Monitor renal and hepatic function

QUINOLONES
(ciprofloxacin, moxifloxacin, norfloxacin, ofloxacin)
• Works by inhibitng DNA gyrase and topoisomerase IV
• Reserved for suspected infections where other antibiotics are ineffective
• Specific conditions
• Can induce seizures
• Combination with steroid use can increase risk of tendon damage
• Adverse effects include rash, itch, nausea, vomiting, severe tendon rupture (rare and
serious)
• Quinolones have excellent activity against haemophilis influenzae, enteric and other Gram
negative bacteria

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AMH Summary: Chapter 5 – Anti-infectives 4

• Counselling
- Medication can cause dizziness
- Stop taking medication if tendon soreness or inflammation occurs

RIFAMYCINS
(rifabutin, rifampicin)
• Works by inhibiting RNA polymerase
• Reserved for MRSA, mycobacterial infection and prophylaxis of meningitis and epiglottitis
• Adverse effects include nausea, vomiting, cramp, discolouration of urine (orange red) and
stained contact lenses
• Counselling: tell doctor if any loss of appetite, tiredness, and jaundice occurs.

TETRACYCLINES
(doxycycline, minocycline)
• Works by inhibiting 30S subunit (bacteriostatic)
• Used for respiratory infections and acne
• Not to be used for children under 8 years and pregnancy
• Adverse effects include nausea, vomiting, teeth discolouration, photosensitivity
• Counselling
- Take with food or milk to reduce stomach upset
- Remain upright for an hour after taking
- Do not take antacids, calcium, iron or zinc supplements within 2 hours of medication.
- Avoid sun exposure by sunscreen or covering up

ANTIMYCOBACTERIALS

• Used for mycolbacterium avium complex infection

Capreomycin
• Used for tubercolosis
• Adverse effects include nephrotoxicity, transient proteinuria, eosinophilia, haemolysis,
hearing loss
• Counselling: tell doctor if you have hearing loss or feel unsteady or dizzy.
• Practice points
- Monitor plasma creatine and potassium before starting
- Check audio and vestibular function

Cycloserine
• Interferes with cell wall synthesis
• Used in tuberculosis
• Contraindicated in epilepsy, severe renal function and frequent alcohol use
• Adverse effects include drowsiness, malaise, confusion, depression
• Counselling
- Medication can cause drowsiness, do not operate machinery while affected
- Can affect feelings, causing depression, excitement or confusion, let doctor know
• Practice points

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AMH Summary: Chapter 5 – Anti-infectives 5

- Monitor renal function, full blood count and liver function

- Monitor CNS toxicity each month and obtain cycloserine blood concentration

Dapsone
• Used for leprosy, pneumonia and for preventing toxoplasmosis
• Adverse effects include dose related asymptomatic haemolytic anaemia
• Dapsone syndrome can occur, starting in the first six weeks with symptoms of rash,
fever and jaundice. Resolves after ceasing
• Counselling
- Take with food
- Stop if troublesome rash occurs
• Practice points
- Full blood count, liver function required
- Stop if serious skin reaction or muscle weakness occurs

Ethambutol
• Used to treat tubercolosis
• Contraindicated in optic neuritis
• Adverse effects include optic neuritis decreasing visual acuity and causing colour
blindness. This is reversible.
• Counselling - may affect the vision, stop taking it and tell doctor if changes to eyesight
occur
• Practice points
- Measure creatinine clearance
- Monitor visual acuity and colour vision

OTHER ANTIBACTERIALS

Aztreonam
• Inhibit cell wall synthesis, binding to protein in Gram negative bacteria
• Used for gram negative aerobes
• Adverse effects include rash, diarrhoea, nausea, abnormal taste
• Practice points - combine with other agents to cover anaerobic and Gram positive
infections

Chloramphenicol
• Inhibit bacterial protein synthesis of 50S subunit
• Contraindicated in bone marrow depression and blood dyscrasias
• Adverse effects include nausea, vomiting and bone marrow suppression, grey
syndrome
• Grey syndrome involves grey skin, low body temperature, lethargy
• Counselling - tell doctor if pale skin, sore throat, fever or bruising occurs after stopping
the medication
• Practice points
- Broad spectrum activity (Gram positive and negative) and anaerobes
- Complete blood picture required before and during treatment
- Stop if haematological changes occur

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Colistin
• Works by binding to phospholipids in bacterial cell wall
• Used for infections due to multidrug resistant Gram negative bacteria and respiratory
infection
• Adverse effects include nephrotoxicity, neurotoxicity, cough, bronchospasm
• Practice points - monitor renal function during systemic treatment

Hexamine hippurate
• Works by being hydrolysed to ammonia and formaldehyde
• Used in prophylaxis of chronic or recurrent urinary tract infection
• Contraindicated in severe hepatic impairment and dehydration
• Adverse effects include nausea, vomiting, diarrhoea
• Counselling - avoid anything with sodium bicarbonate such as Ural as it reduces the
agent’s effectiveness.

Nitrofurantoin
• Works by inhibiting bacterial protein DNA, RNA, cell wall synthesis
• Used for lower UTI and its prophylaxis
• Contraindicated in severe allergy and moderate to severe renal impairment
• Adverse effects include nausea, vomiting, anorexia, abdominal pain
• Counselling
- Take with food to reduce nausea and improve absorption
- May cause drowsiness, do not operate machinery if affected
- Tell doctor if breathing difficulty, cough, numbness occurs
- Urine discolouration may occur (brown), contact lenses may be stained
- Monitor pulmonary function, liver function, renal function

Quinupristin with dalfopristin

• Binds to bacterial ribosome, inhibit protein synthesis
• Used in severe MRSA or vancomycin resistant enterococcus faecium infection
• Adverse effects include thrombophlebitis, arthralgia, myalgia

Sodium fusidate
• Inhibit protein synthesis
• Used in S aureus infections
• Adverse effects include nausea, epigastric discomfort, lethargy
• Counselling
- Take with food to reduce indigestion
- Practice points - resistance develops rapidly with single use. Medication used in
combination with other antibiotics

Sulfadiazine
• Inhibits bacterial folate production
• Used in toxoplasma gondii infection
• Contraindicated in sulphonamide allergy, late pregnancy, neonates less than 4 weeks,
severe renal and hepatic impairment
• Adverse effect includes fever, nausea, rash
• Counselling

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- Tell doctor if sore throat, fever, rash occur

- Avoid sun exposure by covering up or using sunscreen
- Drink plenty of fluids while on this medication
• Practice points - monitor renal function

Trimethoprim
• Inhibits bacterial folate production
• Used in UTI, prostatitis, epididymo-orchitis
• Contraindicated in allergy, severe renal impairment and megaloblastic anaemia (folate
deficient)
• Adverse effects include fever, itch, rash, hyperkalaemia
• Practice points
- Monitor blood and folate levels
- Monitor potassium
- Give at night for UTI

Trimethoprim with sulfamethoxazole

• Contraindicated in sulphonamide allergy, late pregnancy, renal and hepatic impairment,
megaloblastic anaemia
• Counselling
- Take with food
- Drink plenty of fluids
- Avoid sun exposure, cover up or use sunscreen
- Tell doctor if sore throat, rash, fever occurs

B. ANTIFUNGALS

AZOLES
(fluconazole, itraconazole, ketoconazole, miconazole, posaconazole, voriconazole)
• Work by impairing ergosterol in fungal cell membranes
• Adverse effects include rash, headache, dizziness, abdominal pain
• Miconazole and ketoconazole have wide spectrum of activity
• Itraconazole has broader spectrum than fluconazole
• Itraconazole capsules and liquid are not interchangeable

OTHERS

Amphotericin
• Binds to ergosterol in cell membranes
• Used in severe systemic fungal infections
• Adverse effects include infusion reactions (IV), thrombophlebitis, nephrotoxicity,
neurological effects such as seizure, tinnitus, hearing loss
• Monitor renal function

Griseofulvin
• Disrupts fungal cell microtubule function

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• Used in dermal fungal infection

• Contraindicated in lupus and severe hepatic disease
• Adverse effects include headache, nausea, diarrhoea, anorexia
• Counselling
- Take with food
- May cause dizziness, if affected, do not operate machinery
- Minimise sun exposure by sunscreen or covering up
- The contraceptive pill may not be as effective when taking this medication

Nystatin
• Bind to ergosterol in fungi
• Used in oral thrush
• Adverse effects include nausea, vomiting diarrhoea
• Best to take after meals, continue for 2 days after symptoms disappear

Terbinafine
• Works by inhibiting squalene epoxidase in fungi, causing membrane disruption
• Used in onchyomycosis
• Contraindicated in hepatic disease (severe, chronic or active)
• Adverse effects include nausea, vomiting, abdominal pain, rash
• Counselling - tell doctor if you feel tired, nauseous, or have ulcers
• Obtain liver function tests while on this medication

C. ANTIVIRALS

GUANINE ANALOGUES
(acyclovir, famiciclovir, ganciclovir, valiciclovir, valganciclovir)
• Work by inhibitng viral DNA polymerase and DNA synthesis
• Used in herpes simplex infections, shingles and CMV
• Contraindicated in those with severe reactions to the medication
• Adverse effects include nausea, heading and vomiting
• Medication can cause dizziness

NEURAMINIDASE INHIBITORS
(oseltamivir, zanamivir)
• Works by reducining influenza virus by inhibiting neuraminidase and viral load
• Adverse effects include nausea, vomiting, abdominal pain and bronchospasm (zanamivir)
• Take with food with oseltamivir

D. HIV ANTIRETROVIRALS

NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)

(abacavir, didanosine, emtricitabine, lamivudine, stavudine, zidovudine)

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• Converted by cellular enzymes to active phosphorylated metabolites that inhibit viral

reverse transcriptase and viral DNA synthesis
• Used in HIV in adults and children, prophylaxis during pregnancy to prevent vertical
transmission of HIV
• Adverse effects include headache, nausea, myalgia, peripheral lipotrophy
• Counselling - lactic acid in body can build up and cause symptoms, tell doctor if nausea,
vomiting fatigue stomach pain occurs
• Practice points
- Avoid the combinations of stavudine with didanosine or zidovudine, lamuvidine with
emtricitabine, didanosine with tenofovir
- Measure lactate concentration
- Stop if lactic acidosis develops

NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)

(delavirdine, efavirenz, nevirapine)
• Works by reversibly inhibiting HIV-1 reverse transcriptase
• Used for HIV infection
• Contraindicated in those with serious adverse reactions to individual NNRTIs
• Adverse effects include rash, malaise, nausea
• Rash occurs but treatment usually continues unless severe
• Practice points
- Stop NNRTI if elevated liver enzymes or severe rash
- When choosing NNRTI consider adverse effects of other drugs used to treat HIV
patients

PROTEASE INHIBITORS
(atazanavir, darunavir, fosamprenavir, indiavir, lopinavir with ritonavir, nelfinavir, ritonavir,
saquinavir, tipranvir)
• Works by inhibiting HIV-1 and HIV-2 protease, preventing maturation and replication
• Used for HIV infection
• Contraindicated in those with serious reactions to protease inhibitors
• Adverse effects include headache, diarrhoea, nausea, vomiting, fat accumulation, weight
gain, hyperglycaemia

E. ANTIPROTOZOALS

DRUGS FOR MALARIA

(e.g. atovaquone with proguanil)
• Inhibits parasite mitochondrial electron transport, reduce pyrimidine biosynthesis
• Proguanil - plasmodial dihydrofolate reductase inhibitor
• Best taken with food. Start 1-2 days before entering and 7 days after leaving area

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F. ANTHELMINTICS

• For worm infections

BENZIMIDAZOLES
(albendazole, mebendazole)
• Inhibits microtubule polymerisation by binding to beta tubulin in parasite
• Use for roundworm, threadworm, hookworm, tapeworm
• Adverse reactions include headache, nausea, vomiting, diarrhoea
• Counselling - tablets may be crushed, chewed or swallowed

PYRANTEL
• Works by depolarising neuromuscular blocking agent, causing worm detachment of worm
and expulsion
• Used for threadworm, roundworm and hookworm
• Adverse reactions include nausea, vomiting, diarrhoea, cramps, headache

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Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

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