Antibiotic classes Flashcards

1
Q

B-Lactams (types, MoA, indications)

A

Drugs:
- Penicillin G
- Penicillinase resistant penicillins: fluclox
- Aminopenicillins: Ampicillin, amoxicillin
- Antipseudomonal: piperacillin, ticarcillin

  • (Often combined with B-lactamase inhibitors including clavulanic acid (co-amoxyclav), tazobactam (pip-taz)

MoA:
- Bactericidal. B-lactam acts as a cell wall inhibitor by binding to PBPs

Indications:
Penicllin G:
- GPC: staph/strep/entero-cocci. Staph aureus is mostly resistant to penicillin. Strep and enterococci are sensitive.
- GPB: Clostridium mostly sensitive, except c. difficile which is not
- GNC: N meningitidis and N. gonorrhoea sensitive
- GNCB: H. influenzae sensitive
- GNB: Resistant to penicillins (eg E. Coli, Klebsiella, Enterobacter, salmonella) except syphilis is sensitive

Flucloxacillin: used in S. aureus infections
Amocillin/ampicillin: added gram negative coverage
Co-amoxyclav: improved gram positive cover eg S.aureus
Piperacillin/ticarcillin: used to treat P. aeruginosa as well as febrile neutropenia

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2
Q

Flucloxacillin notable side effects

A

Increased risk of hepatitis (monitor LFTs)

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3
Q

Cephalosporins: drugs, MoA, indications

A

Carry increasing gram negative coverage through generations
MoA: Bactericidal. Interfere with cell wall synthesis by binding to PBPs

Indications:
All don’t cover enterococcus

1st generation (cephalexin, cephazolin)
- Covers gram positives and some common gram negatives such as E. Coli
- No MRSA, enterococci or anaerobe coverage

2nd generation (rarely used)
- Covers gram positives well and also enhanced gram negative coverage - H. influenzae
- Cefoxitin has some coverage against anaerobes

3rd generation (ceftriaxone)
- Less gram positive coverage
- Enhanced gram negative activity
- If penicillin allergic, can use ceftriaxone eg in moderate community acquired pneumonia

4th generation (ceftazidime, cefepime)
- Ceftazidime: covers gram negatives such as Pseudomonas, but poor against S. aureus
- Cefepime: covers gram negatives such as Pseudomonas and has gram positive activity against S. aureus

5th generation: (rare use)
- Ceftaroline: gram positive including S. aureus, gram negative except Pseudomonas
- Ceftolazane: gram negatives including Pseudomonas

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4
Q

Cephalosporin side effects

A

Thrombophlebitis (in IV form)
Allergy (cross-reactivity 10% with penicillins)
Increased bleeding (decreased vitamin K, which is synthesized by gut microbes)
Diarrhoea
Sludge in GB and CBD
Nephrotoxicity

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5
Q

Glycopeptides (vancomycin): MoA, Indications

A

MoA: Bactericidal. Binds to the terminal D-ala-D-ala structure of peptidoglycan, hence is a cell wall inhibitor

Indications:
- GPC only
- Vancomycin is the drug of choice if treating MRSA
- Also used if anaphylactic to B-lactams
- Oral vanc can be used in in c. diff colitis, although metronidazole is first line

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6
Q

Vancomycin side effects

A

Red man syndrome - treat with anti-histamines
Thrombophlebitis - slow the infusion rate to avoid this
DRESS syndrome - Drug reaction with eosinophilia and systemic symptoms
Ototoxicity
Nephrotoxicity

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7
Q

Carbapenems: drugs, MoA, indications

A

Meropenem, imipenem

MoA: Bactericidal. Cell wall synthesis inhibitor - able to resist hydrolysis by many B-lactamases.

Indications:
Good broad spectrum cover: gram positives (except MRSA), gram negative, anaerobes

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8
Q

Aminoglycosides (gentamicin): Drugs, MoA, Indications

A

Drugs: gentamicin, tobramycin, streptomycin
MoA:
Bactericidal. Inhibit the 30S subunit of ribosomes to inhibit protein synthesis.

Indications:
Gram negative infections
Useful against S. Aureus
Used synergistically with cell wall active agent (eg penicillins) against Gram positives in:
- Enterococcal endocarditis
Streptococcal endocarditis
- Used synergistically with cell wall active agent (eg penicillins) against gram positives in enterococcal endocarditis, streptococcal endocarditis

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9
Q

Gentamicin side effects

A

Renal toxicity
- Due to ATN
- More important to save the patient and give them a renal hit as can dialyse and renal function returns (reversible)

Ototoxicity
- Irreversible damage, badly impacts balance through vestibular damage
- Can also cause cochlear damage leading to tinnitus

Need tight monitoring of levels - at 30 minutes and 2 hours post dose

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10
Q

Tetracyclines (doxycycline): drugs, MoA, indications

A

Doxycycline, minocycline

MoA:
Inhibitor of protein synthesis through inhbition of 30S subunit of ribosomes
BACTERIOSTATIC

Indications:
Used in coverage of atypical pneumonias
- Mycoplasma pneumonia
- Legionella
- Chlamydia psitacci
Chlamydia trichomonas
- First line treatment
Tick borne bacteria - Rickettsial infections
Severe acne
Faecal clearance means safe for use in kidney dysfunction

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11
Q

Doxycycline side effects, contraindications

A

S/E:
Skin photosensitivity
Suppresses normal gut flora, may cause diarrhoea and bacterial overgrowth

Absorption decreased by multivalent cations - calcium, iron, magnesium

Contraindications: pregnancy (due to teeth and bone deformities, and in children <8 due to tooth discolouration)

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12
Q

Lincosamides (clindamycin, lincomycin): MoA, Indications

A

MoA:
Inhibits the 50S subunit of ribosomes to inhibit protein synthesis. Bacteriostatic.

Indications:
Anaerobic gram-negative infections (bacteriodes, fusobacterium, prevotella)

Aerobic gram-positive cocci:
Some members of staphylococci and streptococci, but not enterococci or MRSA

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13
Q

Clindamycin side effects

A

Serious risk of C. diff colitis which limits use
(C. diff colitis mainly associated with “C” antibiotics - clindamycin, cipro, ceftriaxone)
Rash
High dose associated with metallic taste

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14
Q

Macrolides (-omycin): drugs, MoA, indications

A

Azithromycin, erythromycin, clarithromycin

MoA: Act as inhibitors of protein synthesis
- Inhibit the 50S subunit of ribosomes
- Bacteriostatic

Indications:
Often used in penicillin allergy or as alternative to tetracyclines eg in pregnancy
Community acquired pneumonia:
- Strep. Pneumoniae
- H.Influenzae
- M.Catarrhalis
Atypical pneumonia:
- M.pneumoniae
- Legionella
- Chlamydia pneumoniae
Used as a single dose for Chlamydia trichomonas (STI) (alternative to doxycyline)
Neonatal infections - C. trachomatis (pneumonia), N. gonorrheae
Diphtheria
H.Pylori triple therapy: clarithromycin, ampicillin, PPI

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15
Q

Macrolide side effects

A

Increased QT -> torsades

Increased gastric motility
Associated with cytochrome p450 inhibition

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16
Q

Bactrim (trimethoprim-sulfamethoxazole) MoA, indications

A

MoA: Folic acid synthesis inhibitors
Combined as they inhibit sequential steps in the synthesis of folate.
Selective against bacteria as humans do not synthesize folate, they acquire from diet
Bacteriostatic

Indications:
PJP pneumonia/prophylaxis
UTI
URTIs, pneumonia

17
Q

Fluoroquinolones (ciprofloxacin) drugs, MoA, indications

A

Ciprofloxacin, norfloxacin, moxifloxacin

MoA:
Bacterial topoisomerase inhibitors (inhibit DNA replication)
Bactericidal
Work well in rapidly dividing bacteria

Indications:
- Gram negative infections and most gram positives
- Very effective against PSEUDOMONAS

  • Complicated UTIs, prostatitis (if resistant to trimethoprim or cefalexin)
  • Gram negative OM
  • Bacillus anthracis
18
Q

Ciprofloxacin side effects

A

Risk of prolonged QT -> can lead to torsades
Tendon/cartilage damage, particularly in the elderly and those on steroids. Risk of Achilles tendinopathy/rupture

Teratogenic: c/i in pregnancy and those <10

19
Q

Metronidazole: MoA, indications

A

Nitroimidazoles - metro/tind-azole

MoA:
Disrupt DNA strands through interfering with electron transport, leading to formation of ROS
Bactericidal

Indications:
ANAEROBES
Good against protozoal infections: giardia, entamoeba, trichomonas vaginalis

First line in C. Diff colitis

20
Q

Metronidazole side effects

A

Alcohol has an antabuse effect (instruct patient to cease alcohol 24 hours before and until 24 hours after last metro dose)

21
Q

Chloramphenicol

A

Inhibits protein synthesis

Gram +, gram -, anaerobes, rickettsiae
Used to treat bacterial meningitis
Used also to treat bacterial conjunctivitis and ear infections

22
Q

Rifampicin

A

RNA polymerase inhibitor - bactericidal
Used in TB

Turns urine, sweat, saliva orange
Contraindicated in pregnancy

23
Q

Fusidic acid

A

Inhibits protein synthesis - bacteriostatic

Used in gram positives esp staph
Good for staph osteomyelitis
Give with another anti-staph agent

24
Q

Anti-fungals: Types, MoA

A

Most anti-fungals currently used are membrane-active compounds
They inhibit the production of the sterol ergosterol in the cell membrane
This method works because ergosterol is a major component of the fungal, but not the human, cell membrane

Fluconazole
- The azole group of antifungals (eg fluconazole) inhibits the cyt p450 activity in the ergosterol pathway
○ May interact with other drugs (Eg cyclosporine) where the cyt p450 is also targeted
- It has excellent penetration into the CSF and peritoneum

Indicated for:
○ Candida species in surgical patients (oral fluconazole is the agent of choice in most cases)
○ Cryptococcosis in non-immunocompromised patients
○ Long-term suppressive treatment of cryptococcal meningitis
○ Oesophageal candidasis in AIDs patients

Side effects
○ Nausea, abdo pain, dry mouth, diarrhoea, skin rash
○ Dose dependent hepatotoxicity can occur (eg in AIDS patients)

Polyenes (eg amphotericin B) inhibit in some way the amount of ergosterol in the membrane
- Cells lacking in sufficient ergosterol in the membrane ‘leak’ and die
Amphotericin B has some effects on the membranes of human cells
- Well documented toxicity profile is noted
- Hence, usually reserved for situations where WCC numbers are impaired (eg neutropenia)

Nystatin (polyene) is presently only available as a cream/ointment for topical use (usually for lesions involving mouth/vagina)
- It is not absorbed from the gut following oral administration

Griseofulvin is only active against dermatophytes (ringworm fungi)