ciprofloxacin (Rx) - Cipro, Cipro XR, more..

ProQuin XR

Class: Fluoroquinolones

Pharmacology
Mechanism of Action
Inhibits relaxation of DNA; inhibits DNA gyrase in susceptible organisms; promotes
breakage of double-stranded DNA

Absorption
Bioavailability (PO): ~50-85%
Peak plasma time (PO): Immediate-release, 0.5-2 hr; extended-release, 1-2.5 hr

Distribution
Distributed widely throughout body; tissue concentrations often exceed serum concentrations,
especially in kidneys, gallbladder, liver, lungs, gynecologic tissue, and prostatic tissue;
cerebrospinal fluid (CSF) concentration is 10% in noninflamed meninges and 14-37% in
inflamed meninges; crosses placenta; enters breast milk
Protein bound: 20-40%
Vd: 2.1-2.7 L/kg

Metabolism
Metabolized in liver
Enzyme inhibitor: CYP1A2

Elimination
Half-life: 2-5 hr (children); 3-5 hr (adults)
Excretion: Urine (30-50%), feces (15-43%)

Pharmacology doksisiklin
Mechanism of Action

Inhibits protein synthesis and, thus, bacterial growth by binding to 30S and possibly 50S
ribosomal subunits of susceptible bacteria; may block dissociation of peptidyl t-RNA from
ribosomes, causing RNA-dependent protein synthesis to arrest.
Absorption

Oral: Almost complete; reduced 20% by food or milk

Peak serum time: 1.5-4 hr
Bioavailability: Reduced at high pH
Distribution

Protein bound: 90%

Metabolism

Liver
Elimination

Half-life: 15-25 hr
Excretion: Urine (23%); feces (30%)

azithromycin (Rx) - Zithromax, Zmax

Pharmacology
Mechanism of Action

Binds to 50S ribosomal subunit of susceptible microorganisms and blocks dissociation of

peptidyl tRNA from ribosomes, causing RNA-dependent protein synthesis to arrest; does not
affect nucleic acid synthesis
Concentrates in phagocytes and fibroblasts, as demonstrated by in vitro incubation
techniques; in vivo studies suggest that concentration in phagocytes may contribute to drug
distribution to inflamed tissues

Absorption

Rapidly absorbed
Bioavailability: 37%; variable effect with food (increased with oral suspension, unchanged
with tablet)

Peak serum time: 2-3 hr (immediate release); 5 hr (extended release)

Distribution

Extensively distributed into skin, lungs, sputum, tonsils, and cervix; penetrates cerebrospinal
fluid (CSF) poorly
Protein bound: 7-50% (concentration dependent)
Vd: 33.3 L/kg (PO); 31.1 L/kg (IV)
Metabolism

Metabolized in liver
Elimination

Pharmacology Ceftriakson
Mechanism of Action
Third-generation cephalosporin with broad-spectrum gram-negative activity; has lower
efficacy against gram-positive organisms but higher efficacy against resistant organisms;
highly stable in presence of beta-lactamases (penicillinase and cephalosporinase) of gramnegative and gram-positive bacteria; bactericidal activity results from inhibiting cell-wall
synthesis by binding to 1 or more penicillin-binding proteins; exerts antimicrobial effect by
interfering with synthesis of peptidoglycan (major structural component of bacterial cell
wall); bacteria eventually lyse because activity of cell-wall autolytic enzymes continues while
cell-wall assembly is arrested

Absorption
IM preparation well absorbed
Peak plasma time: 2-3 hr (IM)

Distribution
Distributed throughout body, including gallbladder, lungs, bone, bile, and CSF (higher
concentrations achieved when meninges are inflamed); crosses placenta; enters amniotic fluid
and breast milk
Protein bound: 85-95%
Vd: 6-14 L

Metabolism
Metabolized in liver

Elimination

Half-life: 5-9 hr (normal hepatic and renal function); 12-16 hr (mild-to-severe renal
impairment)
Excretion: Urine (33-67% as unchanged drug), feces