Antimicrobial Drugs Flashcards
What class of drug is Amoxycillin (Amoxil)?
Moderate-spectrum penicillin
What class of drug is Ampicillin (Principen)?
Moderate-spectrum penicillin
What class of drug is Benzylpenicillin (Benpen)?
Narrow-spectrum penicillin
What class of drug is Vancomycin (Vancocin)?
Glycopeptide antibiotic
What class of drug is Clarithromycin (Klacid)?
Macrolide antibiotic
What class of drug is Gentamicin?
Aminoglycoside antibiotic
What class of drug is Ethambutol?
Antimycobacterial
What class of drug is Isoniazid?
Antimycobacterial
What class of drug is Pyrazinamide?
Antimycobacterial
What class of drug is Rifampicin?
Rifamycin antibiotic
What class of drug is Metronidazole?
Nitroimidazole antibiotic
What class of drug is Streptomycin?
Aminoglycoside antibiotic
What class of drug is Tetracycline?
Tetracycline antibiotics
What class of drug is Doxycycline?
Tetracycline antibiotics
What class of drug is Acyclovir?
Anti-viral guanosine nucleoside analogue
What class of drug is Miconazole?
Azole anti-fungal
What class of drug is Fluconazole?
Systemic azole anti-fungals
What class of drug is Itraconazole?
Systemic azole anti-fungals
What class of drug is Nystatin?
Polyene anti-fungal
What class of drug is Amphotericin B?
Polyene anti-fungal
What class of drug is Caspofungin?
Echinocandin anti-fungal
What class of drug is Flucytosine?
Anti-fungal
What class of drug is Artemether (Riamet)?
Artemisinin antimalarial
What class of drug is Chloroquine (Aralen)?
Quinine antimalarial
What class of drug is Oseltamivir (Tamiflu)?
Neuraminidase inhibitor
What class of drug is Trimethoprim (Triprim)?
DNA synthesis inhibitor
What is the mechanism of action of Amoxycillin (Amoxil)?
Inhibits bacterial cell wall proteoglycan synthesis
What is the mechanism of action of Ampicillin (Principen)?
Inhibits bacterial cell wall proteoglycan synthesis
What is the mechanism of action of Benzylpenicillin (Benpen)?
Inhibits bacterial cell wall proteoglycan synthesis
What is the mechanism of action of Vancomycin (Vancocin)?
Bactericidal; inhibit bacterial cell wall synthesis by preventing formation of peptidoglycan polymers., Binds to peptidoglycan precursors and disrupts cross-linking of peptidoglycan by PBPs – disruption of cell wall synthesis leads to bacterial apoptosis.
What is the mechanism of action of Clarithromycin (Klacid)?
Inhibits bacterial protein synthesis
What is the mechanism of action of Gentamicin?
Inhibits bacterial protein synthesis
What is the mechanism of action of Ethambutol?
Inhibits incorporation of mycolic acid into mycobacterium cell wall, bacteriostatic against M. tuberculosis
What is the mechanism of action of Isoniazid?
May involve inhibiting synthesis of mycolic acids, constituents of the mycobacterial cell wall. It is bactericidal against actively dividing M. tuberculosis and bacteriostatic against resting bacteria; it is active against intra- and extracellular organisms.
What is the mechanism of action of Pyrazinamide?
Bactericidal against M. tuberculosis in acid pH (inactive against non-tuberculous mycobacteria); active against bacteria within macrophage; activity declines with time (pH increases as inflammation decreases).
What is the mechanism of action of Rifampicin?
Inhibits bacterial RNA polymerase. Bactericidal against rapidly dividing M. tuberculosis and active against intracellular organisms which are semi-dormant
What is the mechanism of action of Metronidazole?
Interferes with DNA synthesis by causing a loss of helical structure, strand breakage and inhibition of nucleic acid
What is the mechanism of action of Streptomycin?
Inhibits protein synthesis by binding to 30S subunit of bacterial ribosome. This leads to codon misreading, eventual inhibition of protein synthesis and ultimately death of microbial cells. It has been hypothesised that binding of the molecule to the 30S subunit interferes with 50S subunit association with the mRNA strand. This results in an unstable ribosomal-mRNA complex, leading to a frameshift mutation and defective protein synthesis; leading to cell death.
What is the mechanism of action of Tetracycline?
Bacteriostatic; inhibits bacterial protein synthesis by reversibly binding to 30S subunit of the ribosome.
What is the mechanism of action of Doxycycline?
Bacteriostatic; inhibits bacterial protein synthesis by reversibly binding to 30S subunit of the ribosome.
What is the mechanism of action of Acyclovir?
Active form of the pro-drug valacyclovir. Following phosphorylation by viral and cellular enzymes (thymidine kinase), acyclovir inhibits viral DNA polymerase and DNA synthesis by causing premature chain termination.
What is the mechanism of action of Miconazole?
Impairs the synthesis of ergosterol in fungal cell membranes leading to their breakdown → cell leakage and death occur by lytic activity of the host defence system
What is the mechanism of action of Fluconazole?
Impairs the synthesis of ergosterol in fungal cell membranes leading to their breakdown → cell leakage and death occur by lytic activity of the host defence system
What is the mechanism of action of Itraconazole?
Impairs the synthesis of ergosterol in fungal cell membranes leading to their breakdown → cell leakage and death occur by lytic activity of the host defence system
What is the mechanism of action of Nystatin?
Binds to ergosterol in fungal cell membranes → forms transmembrane channel → altered membrane permeability → leakage of ions (especially K+) → cell death
What is the mechanism of action of Amphotericin B?
Binds to ergosterol in fungal cell membranes → forms transmembrane channel → altered membrane permeability → leakage of ions (especially K+) → cell death
What is the mechanism of action of Caspofungin?
Inhibits synthesis of fungal cell wall glucan, altering cell membrane permeability → fungal cell death
What is the mechanism of action of Flucytosine?
Converted to fluorouracil in fungal cells → inhibits DNA synthesis and protein synthesis
What is the mechanism of action of Artemether (Riamet)?
Artemether (an artemisinin) is metabolised to the active metabolite artenimol. Combination acts in the food vacuole of the malaria parasite interfering with the conversion of haem to nontoxic haemozoin; also inhibits nucleic acid and protein synthesis.
What is the mechanism of action of Chloroquine (Aralen)?
Rapidly acting schizonticide with some gametocytocidal activity., Increases intravacuolar pH and affects parasite’s ability to metabolise haemoglobin; interferes with DNA or RNA synthesis., It has anti-inflammatory activity and may also have immunosuppressive effects.
What is the mechanism of action of Oseltamivir (Tamiflu)?
Reduce influenza virus replication by inhibiting the viral surface enzyme neuraminidase, preventing release of new virus from cells.
What is the mechanism of action of Trimethoprim (Triprim)?
Trimethoprim binds to dihydrofolate reductase and inhibits the reduction of dihydrofolic acid (DHF) to tetrahydrofolic acid (THF). THF is an essential precursor in the thymidine synthesis pathway and interference with this pathway inhibits bacterial DNA synthesis.
What are the side effects of Amoxycillin (Amoxil)?
- Diarrhoea
- Anaphylaxis
- Penicillin hypersensitivity
What are the side effects of Ampicillin (Principen)?
- Diarrhoea
- Rash
- Urticaria
- Anaphylaxis
- Penicillin hypersensitivity
What are the side effects of Benzylpenicillin (Benpen)?
- Diarrhoea
- Rash
- Urticaria
- Vomiting
- Fatigue
- Fever
- Anaphylaxis
- Penicillin hypersensitivity
What are the side effects of Vancomycin (Vancocin)?
- Indigestion
- Nausea
- Vomiting
- Diarrhoea
- Chills
- Local pain from IV injection
What are the side effects of Clarithromycin (Klacid)?
- Abdominal pain
- Diarrhoea
- Nausea
- Vomiting
- Headache
- Hepatitis
- Liver failure
- Hypersensitivity reaction
What are the side effects of Gentamicin?
- Ototoxicity
- Nephrotoxicity
- Hypersensitivity reaction
What are the side effects of Ethambutol?
- Hyperuricaemia
- Nausea
- Vomiting
- Mania
- Thrombocytopenia
- Neutropenia
- Anaphylactoid reaction
- Peripheral neuropathy
What are the side effects of Isoniazid?
- Rash
- Fever
- Peripheral neuritis (if pyridoxine is not given concurrently)
- Hepatitis
- Acne
- Tiredness
What are the side effects of Pyrazinamide?
- Hyperuricaemia
- Nausea
- Vomiting
- Arthralgia
- Anaemia
- Hepatotoxicity
What are the side effects of Rifampicin?
- Discolouration of skin, sweat and other bodily fluids (orange-red)
- Heartburn
- Loss of appetite
- Nausea
- Thrombocytopenia
- Hepatotoxicity
- Nephrotoxicity
What are the side effects of Metronidazole?
- Nausea
- Jarisch Herxheimer reaction
- Dizziness
- Headache
- Candida infection of genital region
- Vaginal irritation
- Thrombophlebitis (if IV administration)
What are the side effects of Streptomycin?
- Fever
- Rash
- Sterile abscess at injection site
- Urinary casts
- Albuminuria
What are the side effects of Tetracycline?
- Nausea
- Vomiting
- Diarrhoea
- Epigastric burning
- Tooth discolouration
- Phototoxicity
- Acidosis
- Azotaemia
- Elevated serum BUN (Blood urea nitrogen)
- Raised intercranial pressure
- Rash
- Bone deformity
What are the side effects of Doxycycline?
- Nausea
- Vomiting
- Diarrhoea
- Epigastric burning
- Tooth discolouration
- Phototoxicity
- Acidosis
- Azotaemia
- Elevated serum BUN (Blood urea nitrogen)
- Raised intercranial pressure
- Rash
- Bone deformity
What are the side effects of Acyclovir?
- Contact dermatitis (topical form only)
- Diarrhoea
- Nausea
- Vomiting
- Headache
- Malaise
What are the side effects of Miconazole?
- Mild GI disturbances
What are the side effects of Fluconazole?
- Rash
- Headache
- Dizziness
- Nausea
- Vomiting
- Diarrhoea
- Abdominal pain
What are the side effects of Itraconazole?
- Rash
- Headache
- Dizziness
- Nausea
- Vomiting
- Diarrhoea
- Abdominal pain
- Constipation
- Dyspepsia
- Anorexia
Fatigue
What are the side effects of Nystatin?
- Nausea
- Vomiting
- Diarrhoea
What are the side effects of Amphotericin B?
- Infusion reactions
- Thrombophlebitis
- Anaemia
- Nephrotoxicity
- Nausea, vomiting, diarrhoea (oral administration)
- Hypotension, hypertension, cardiac arrest, arrhythmias, GI bleeding, hepatotoxicity, rash, neurologic effects (IV infusion)
What are the side effects of Caspofungin?
- Fever
- Phlebitis at injection site
- Flushing
- Chills
- Nausea
- Vomiting
- Diarrhoea
- Rash
- Itch
- Anaemia
Headache
What are the side effects of Flucytosine?
- Anaemia
- Leukopenia
- Thrombopenia
- Diarrhoea
- Nausea
- Vomiting
- Rash
- Elevated liver enzymes
What are the side effects of Artemether (Riamet)?
- Headache
- Dizziness
- Sleep disorder
- Anorexia
- Nausea
- Vomiting
- Diarrhoea
- Myalgia
- Arthralgia
- Weakness
- Fatigue
- Palpitations
- Itch
- Rash
What are the side effects of Chloroquine (Aralen)?
- Headache
- Skin eruptions
- Itch
- GI disturbances
What are the side effects of Oseltamivir (Tamiflu)?
- Nausea
- Vomiting
- Headache
What are the side effects of Trimethoprim (Triprim)?
- Fever
- Itch
- Rash
- Nausea
- Vomiting
- Hyperkalaemia
- Sore mouth
What are the indications for use of Amoxycillin (Amoxil)?
Administration: oral tablet or IV, may be combined with a beta-lactamase such as clavulanate
- Active against Gram-positive and a greater range of Gram-negative bacteria than narrow-spectrum penicillins
What are the indications for use of Ampicillin (Principen)?
Administration: oral tablet or IV
- Active against Gram-positive and a greater range of Gram-negative bacteria than narrow-spectrum penicillins
What are the indications for use of Benzylpenicillin (Benpen)?
Administration: oral tablet or IV
- Active against Gram-positive bacteria
Destroyed by penicillinase-producing organisms
What are the indications for use of Vancomycin (Vancocin)?
Administration: oral capsule or IV
- Endocarditis prophylaxis in penicillin allergy
- Severe infections caused by susceptible organisms in cases of penicillin resistance or intolerance
- MRSA infections
- Clostridium difficile-associated disease
Contraindications: Inflammatory GI conditions
What are the indications for use of Clarithromycin (Klacid)?
Administration: oral tablet or IV
- Community acquired respiratory infections
- Gram-positive and Gram-negative cocci
- Gram-positive and Gram-negative anaerobes
Not effective against Gram-negative rods
What are the indications for use of Gentamicin?
Administration: IV, IM or topical (not systematically active when given orally)
- Empirical treatment of serious Gram-negative infections
- Systemic enterococcal infections (with β-lactams or vancomycin)
- Surgical and non-surgical prophylaxis
- Cystic fibrosis, bronchiectasis (inhalation)
What are the indications for use of Ethambutol?
Administration: oral tablet in the first two months of TB treatment
- Spectrum limited to mycobacteria
- Pulmonary tuberculosis
- Extrapulmonary tuberculosis
- Mycobacteria avium infection
What are the indications for use of Isoniazid?
Pyridoxine 25 mg with each dose of isoniazid is recommended to reduce the risk of peripheral neuropathy.
Administration: oral tablet in the first six months of TB treatment
- Active tuberculosis
- HIV infection with inactive tuberculosis
What are the indications for use of Pyrazinamide?
Administration: oral tablet in the first two months of TB treatment
- Tuberculosis with/without HIV infection
What are the indications for use of Rifampicin?
Administration: oral tablet in the first six months of TB treatment, IV
- Tuberculosis active infection or reactivation
- Leprosy
- Other mycobacterial infections
- MRSA infection, with other agents
- Selected serious or prosthesis-associated infection with other anti-staphylococcal agents
- Prophylaxis for close contacts of people with meningococcal disease, H. influenzae type b disease
What are the indications for use of Metronidazole?
Administration: oral tablet or IV
- Infection due to anaerobic bacteria
- Prophylaxis for surgeries with increased risk of infection with anaerobic bacteria
What are the indications for use of Streptomycin?
Administration: IM second-line treatment for TB
- Infections due to M. tuberculosis where the strain is resistant to other TB drugs or when other TB drugs are contraindicated (Streptomycin is bactericidal against M. tuberculosis)
- Infections due to non-tuberculosis mycobacteria
- Serious enterococcal infection with high level gentamicin (but not streptomycin) resistance, seek specialist advice
What are the indications for use of Tetracycline?
Administration: oral tablet
- Sinusitis
- Infective exacerbations of COPD
- Community-acquired pneumonia
- Q fever
- Brucellosis
- Syphilis
- Periodontal disease
- Rickettsiosis
- H. pylori eradication, withother agents
- Acne
What are the indications for use of Doxycycline?
Administration: oral tablet
- Acne
- M. pneumonia infections
- Community-acquired pneumonia
- Exacerbation of chronic bronchitis
- Acute bacterial sinusitis
- Chlamydial other non-gonococcal genital tract infections
- Rickettsial infections
- Chronic prostatitis
- Prophylaxis of malaria
What are the indications for use of Acyclovir?
Administration: oral, topical, IV
- Treatment and prevention of herpes simplex infections
- Shingles (varicella zoster virus reactivation)
- Acute chickenpox (varicella zoster) in immunocompromised patients
- Herpetic eye infections
What are the indications for use of Miconazole?
Administration: gel
- Oropharyngeal candidiasis
- Apply gel to dentures after cleaning for oral candidiasis associated with dentures
What are the indications for use of Fluconazole?
Administration: capsule, oral liquid, IV
- Use topical antifungal preparations first for mucocutaneous and vulvovaginal candidiasis; reserve fluconazole for resistant cases and itraconazole for even later
What are the indications for use of Itraconazole?
Administration: capsule or oral liquid
- Use topical antifungal preparations first for mucocutaneous and vulvovaginal candidiasis; reserve fluconazole for resistant cases and itraconazole for even later
What are the indications for use of Nystatin?
Administration: tablet, capsule or oral liquid
- Oropharyngeal candidiasis
- Treatment and suppression of intestinal candidiasis
What are the indications for use of Amphotericin B?
Administration: oral or IV
- Severe systemic fungal infections (last line treatment for candidiasis)
What are the indications for use of Caspofungin?
Administration: IV
- Mainly active against Aspergillus and Candida infections
What are the indications for use of Flucytosine?
Administration: IV/oral, with IV amphotericin
- Flucytosine has a narrow spectrum of activity and resistance may develop rapidly; it must be used with another antifungal
What are the indications for use of Artemether (Riamet)?
Administration: oral tablet
- Treatment of acute uncomplicated P. falciparum malaria
- Treatment of chloroquine-resistant P. vivax malaria
Contraindications:
Treatment with rifampicin
First trimester pregnancy
Administered in combination with lumefantrine as resistance is developing.
What are the indications for use of Chloroquine (Aralen)?
Administration: oral tablet
- Prophylaxis and treatment of malaria due to susceptible organisms
Contraindications:
Retinal damage
Allergy to chloroquine
Epilepsy
Mefloquine (Lariam) used in Australia
What are the indications for use of Oseltamivir (Tamiflu)?
Administration: oral capsule, liquid
- Treatment of infections due to influenza A and B virus in selected people
- Prevention of influenza
Contraindications:
Children < 1 year
What are the indications for use of Trimethoprim (Triprim)?
Administration: oral tablet
- Empirical treatment for uncomplicated lower UTIs
- Prostatitis
- Mild-to-moderate Pneumocystis jiroveci pneumonia
Contraindications:
Folate deficiency
Megaloblastic anaemia
1st trimester pregnancy
Often combined with sulfamethoxazole (co-trimoxazole – Septra) as they block sequential steps of the folic acid pathway.
