β lactam antibiotic
Binds to penicillin binding protein (transpeptidase) and
prevents crosslinking of bacterial peptidoglycan
impairs cell wall synthesis

fluorinated bis-triazole
reduction of ergosterol synthesis by inhibition of fungal cytochrome P450 enzymes (greater affinity for fungal than for human)

Orally not absorbed (need penicillin V)

Well absorbed orally

CSF and bone penetration if inflammation present

good CSF penetration

60% PB

Vd <1L/kg

Inactive metabolite penicollic acid

not metabolized well

90% excreted in urine by tubular secretion
25% unchanged

Urine unchanged

GIT– abdominal pain, N/V/D, pseudomembranous colitis, hepatitis
HAEM- agranulocytosis
CNS- confusion, seizure, encephalopathy
HYPERSENSITIVITY- rash, anaphylaxis

N/V/D, Abdominal pain
Headache
Skin rash
Reversible alopecia
Rare: Hepatic failure, SJS
Should be avoided in Pregnancy
Drug interactions: (inhibitor of CYP3A4, CYP2C9)

Narrow-Spectrum
Natural Penicillin

Highly bactericidal, only
gram positives/anaerobes,
susceptible to betalactamases

Targets
GPC: Streptococci, Meningococcus
Listeria (GPB)
GNC: Neisseria, Clostridia
Treponemma (Spiral)

Synergistic effects with
aminoglycosides

Candida
Cryptococcus
Coccidia
(No activity against histoplasma, blasto, sporotrichosis, Aspergillus, mucormycosis)

ANTIBIOTIC:
PENICILLIN

ANTIFUNGAL:
AZOLE

Narrow spectrum naturally occurring penicillin

Triazole

Level 1

Level 3

Resistance
MRSA
Many Staph
-Betalactamase prod
Gram Negatives

Some candida species,

Decreased drug concentration
Target site alteration
Up-regulation of target enzyme
Development of bypass pathways

potent CYP inhibitors with a wide range of drug interactions (including warfarin)