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Found. Pharm > Antibiotics: SULF, CYCLINE, and (FL)OXACIN > Flashcards

Antibiotics: SULF, CYCLINE, and (FL)OXACIN Flashcards

1
Q

SULF (Sulfonamides)

A
  • First effective chemotherapeutic agents used systemically for the prevention and cure of bacterial infections in humans (Prontosil (1932) => Nobel Prize in Medicine (1938))
  • Development of penicillin (1940s) => diminished usefulness of
    sulfonamides (except trimethoprim-sulfamethoxazole)
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2
Q

What is Sulfonamides drived from?

A

Para-aminobenzoic acid

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3
Q

MOA

Sulfonamides

A

Bacteriostatic
Competitive inhibitors of dihydropteroate synthase
- The bacterial enzyme responsible for incorporation of PABA into dihydropteroic acid, the immediate precursor of folic acid
- Competitive antagonism of PABA

Folic Acid Synthesis Inhibitor

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4
Q

SULF Types

A

Sulfamethoxazole
- Trimethoprim-Sulfamethoxazole (Bactrim, Septra, Cotrim): PO, and IV

Sulfadiazine: PO
Sulfacetamide: topical: cream, lotion, etc

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5
Q

Trimethoprim-Sulfamethoxazole (TMP-SMX)

A

Aka cotrimoxazole
- Wide variety of antimicrobial activity => range of clinical indications

Key spectrum of activity
- Staphylococcus aureus (including MRSA): Gram +
- E.coli, and other Enterobacteriaceae: Gram -
- Listeria monocytogenes (menagitis)
- Pneumocystitis jiroveci (most common)
- Taxoplasma gondii
- Nocaardia spp.
- Stenotrophomonas maltophilia

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6
Q

TMP-SMX: Indications

A
  • Skin and soft tissue infections
  • Urinary tract infections (UTIs)
  • Meningitis
  • Pneumocystis pneumonia
  • Toxoplasma encephalitis
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7
Q

TMP-SMX: ADRs

A
  • Gastrointestinal (nausea, vomiting, abdominal discomfort)
  • Dermatologic/hypersensitivity
    – (Rash, urticaria, Stevens-Johnson syndrome or toxic epidermal necrolysis)
  • Renal: Caution in renal impairment (dose adjustment needed),
    – Crystalluria (need to maintain adequate hydration for prevention)
  • Hematologic (bone marrow suppression, e.g neutropenia)
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8
Q

TMP/SMX: Other Warning

A
  • DDI: e.g warfaring; enhanced anticoagulant effect
  • Cross-allergenicity with other sulfonamide drugs: glipizide, furosemide, hydrochlorothiazide
  • Pregnancy catagory C: generally avoided in first trimester and near term
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9
Q

CYCLINE (Tetracyclines)

A

Introduced in late 1940s
- Basic four-ring chemcial structure with varying structural groups

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10
Q

MOA

A

Bacteriostatic
- Inhibit bacterial protein synthesis by binding to the 30S bacterial ribosome => preventing access of aminoacyl tRNA to acceptor A site on the mRNA-ribosome complex

Protein synthesis inhibitor

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11
Q

Tetracyclines

A

Tetracycline (PO)
Doxycycline (Vibramycin, PO and IV)
Minocycline (Minocin, PO, IV):older
Tigecycline (Tygacil, IV): Glycylglycine (minocycline derivative)
Omadacycline (Nuzyra, PO and IV): aminomethylcycline
Eravacycline (Xerava, IV): fluorocycline (similar to tigecycline)
Demeclocyline (PO): NOT USED TO TREAT INFECTIONS

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12
Q

Tetracyclines

Topical indications

A
  • Low-dose doxycycline (Oracea, PO): inflammatory pustules of rosacea
  • Extended relase minocycline (Solodyn, PO): acne vugaris
  • Sarecycline (Seysara, PO): acne vulgaris
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13
Q

Spectrum of Activity

A
  • Borrelia burgdorferi (lime disease)
  • Rickettsia (rocky mountain spotted fever)
  • Treponema paallidum
  • Chlamydia trachomatis
  • Staphylococcus aureus (including MRSA)
  • Atypicals: Mycoplasma pneumoniae, Chlamydia spp., Legionella spp.
  • OTHER: Yersina pestis (plague), Bacillus anthracis (anthrax), Vibrio
    cholerae (cholera), Bartonella henselae (cat scratch disease),
    Plasmodium spp. (malaria), Coxiella burnetii (Q fever)
  • Tetracycline – Helicobacter pylori
  • Tigecycline and eravacycline (add) – E. coli, other Enterobacteriaceae,
    Bacteroides, and other drug-resistant bacterial strains
  • Omadacycline (adds) – Streptococcus pneumoniae (drug-resistant
    strains), other streptococci, E. coli and other Gram-negative bacteria
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14
Q

Indication

Tetracyclines

A
  • Lyme disease
  • Rickettsial (RMSF) and other tickborne infections
  • Syphilis
  • Chlamydia
  • Skin and soft tissue infections
  • Community acquired pneumonia
  • Complicatied intra abdominal infections
  • Other zoonotic infections
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15
Q

Tigecycline BBW

A
  • Increased all cause mortality versus comparators in phase 3 and 4 clinical trials
  • Treaatment of hospital acquired pneumonia or ventilatory associated pneumonia
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16
Q

ADRs

cyclines

A

GI:
- Epigastric burning, abdominal discomfort, nausea, vomiting and diarrhea
- Esophagitis and esophageal ulcers

Photosensitivity:
- Avoid prolonged exposure to sunlight and use skin protection

Tooth enamel hypoplasia, permanent tooth discoloration
- Precaution in pediatrics

17
Q

Other warning

cyclines

A

DDI: mutivalent cations (Ca2+, Mg2+, Al3+)
Pregnancy category D: only when benift outweight risk (RMSF)

18
Q

(FL)OXACIN

Fluoroquinolones

A
  • First quinolone: halidixic acid (treated UTIs)
  • Broad antibacterial activity: treat wide vvariety of infectious disease
  • Potentially fatal ADRs: many withdrawn from US market
    – Lomefloxacin and sparfloxacin, Temafloxacin(immune hemolytic anemia), Trovafloxacin (hepatotoxicity), Grapafloxacin (cardiotoxicity), Clinafloxacin (phototoxicity)
19
Q

MOA

A
  • Bactericidal
  • Inhibit topoisomerase II (gram (+)) (DNA gyrase) and IV (gram (-)) => inhibit relaxation of supercoiled DNA and promotes DNA breakage
20
Q

Fluoroquinolones

A
  • Ciprofloxacin (Cipro®, PO and IV)
  • Ofloxacin
  • Levofloxacin (Levaquin®, PO and IV)
  • Moxifloxacin (Avelox®, PO and IV)
  • Delafloxacin (Baxdela®, PO and IV)
21
Q

Fluoroquinolones (ophthalmic/otic)

A
  • Gatifloxacin (Zymaxid®, ophthalmic)
  • Besifloxacin (Besivance®, ophthalmic)
  • Ciprofloxacin (Ciloxan®, ophthalmic and Cetraxal®; Otiprio®, otic)
  • Ofloxacin (Ocuflox®, ophthalmic and Floxin Otic®, otic)
  • Levofloxacin
  • Moxifloxacin (Moxeza®; Vigamox®, ophthalmic)
22
Q

Spectrum of Activity

Fluoroquinolones

A

Broad spectrum antibiotics
- Gram-negative bacteria – E. coli, other Enterobacteriaceae,
Pseudomonas aeruginosa, and more
- Gram-positive bacteria – Streptococcus pneumoniae, other
streptococci, Staphylococcus aureus (delafloxacin; including MRSA)
- Atypicals - Mycoplasma pneumoniae, Chlamydia spp., Legionella spp.
- OTHER: Yersina pestis (plague), Bacillus anthracis (anthrax),
Mycobacterium tuberculosis (MDR tuberculosis), Salmonella, Shigella

23
Q

Indications

Fluoroquinolones

A

Community acquired pneumonia
UTIs
Serious Systemic Gram Negative bacterial infections
- Hospital-acquired/ventilator-associated pneumonia
- Intra-abdominal infections
- Bloodstream infections

Bone/joint and skin/soft tissue infections
Sexually transmitted infections (chlamydia)
Acute sinusitis, COPD acute exacerbation

24
Q

BBW

Fluoroquinolones

A
  • CNS effects – seizures, tremors, dizziness
  • Peripheral neuropathy
  • Psychiatric reactions – nervousness, agitation, delirium,
    hallucinations, confusion, etc.
  • Tendinopathy/tendon rupture – most frequently Achilles tendon
    – Higher risk in older adults
  • Appropriate use - treatment of acute bacterial sinusitis, acute
    bacterial exacerbation of chronic bronchitis, or uncomplicated UTI
    should only happen if no alternatives
  • Myasthenia gravis - exacerbate muscle weakness
25
Q

ADRs

Fluoroquinolones

A
  • Gastrointestinal: Nausea, vomiting, and abdominal discomfort
  • Clostridioides (formerly Clostridium) difficile-associated diarrhea
    (CDAD) aka “C. diff infection”
  • QTc prolongation
  • Rash and photosensitivity
  • Dysglycemia (rare with quinolones currently on the market)
  • Aortic aneurysm and dissection (relatively new FDA warning)
  • Musculoskeletal disorders – concern in pediatrics
26
Q

Other Warnings

Fluoroquinolones

A

DDI:
- Multivalent cations (Ca2+, Mg2+, AI3+)
- QTc prolongation

Pregnancy Category C: Avoided unless benefit outweight risk

Found. Pharm (14 decks)

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