Bacampicillin

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Absorption Absorbed following oral administration.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Enteric bacteria and other eubacteria

Aztreonam

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Absorption Less than 1% absorbed from the gastrointestinal tract following oral administration. Completely absorbed following intramuscular administration.
Volume of distribution
  • 12.6 L
Protein binding Serum protein binding averaged 56% and is independent of dose. Impaired renal function, 36 to 43%.
Metabolism
Approximately 6 to 16% metabolized to inactive metabolites by hydrolysis of the beta-lactam bond, resulting in an open-ring compound.
Route of elimination In healthy subjects, aztreonam is excreted in the urine about equally by active tubular secretion and glomerular filtration. Urinary excretion of a single parenteral dose was essentially complete by 12 hours after injection.
Half life The serum half-life of aztreonam averaged 1.7 hours (1.5 to 2.0) in subjects with normal renal function, independent of the dose. In elderly patients and in patients with impaired renal function, the mean serum half-life of aztreonam increased (4.7 to 6 hours and 2.1 hours, respectively).
Clearance
  • 91 mL/min [healthy]
Toxicity Not Available
Affected organisms
  • Enteric bacteria and other eubacteria

Azlocillin

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Absorption Not significantly absorbed from the gastrointestinal tract.
Volume of distribution Not Available
Protein binding 20 to 46% bound to plasma proteins
Metabolism
Eliminated predominantly by renal mechanisms, but also undergoes biotransformation within body tissues and intraintestinal degradation by bowel bacteria, with high concentrations found in bile.
Route of elimination Not Available
Half life Mean elimination half-life is 1.3 to 1.5 hours. Longer in neonates, and 2 to 6 hours in patients with renal impairment.
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Enteric bacteria and other eubacteria

Azithromycin

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Absorption Bioavailability is 37% following oral administration. Absorption is not affected by food. Azithromycin is extensively distributed in tissues with tissue concentrations reaching up to 50 times greater than plasma concentrations. Drug becomes concentrated within macrophages and polymorphonucleocytes giving it good activity against Chlamydia trachomatis.
Volume of distribution
  • 31.1 L/kg
Protein binding Serum protein binding is variable in the concentration range approximating human exposure, decreasing from 51% at 0.02 µg/mL to 7% at 2 µg/mL.
Metabolism
Hepatic. In vitro and in vivo studies to assess the metabolism of azithromycin have not been performed.
Route of elimination Biliary excretion of azithromycin, predominantly as unchanged drug, is a major route of elimination.
Half life 68 hours
Clearance
  • apparent plasma cl=630 mL/min [following single 500 mg oral and i.v. doses]
Toxicity Potentially serious side effects of angioedema and cholestatic jaundice were reported
Affected organisms
  • Enteric bacteria and other eubacteria

Azidocillin

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Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Not Available
Affected organisms Not Available
Pathways Not Available

Azelastine

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Absorption Absorption of azelastine following ocular administration was relatively low. Systemic bioavailability is approximately 40% after nasal administration.
Volume of distribution
  • 14.5 L/kg
Protein binding In-vitro studies in human plasma indicate that the plasma protein binding of azelastine and N-desmethylazelastine are approximately 88% and 97%, respectively.
Metabolism
Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system, however the exact cytochrome P450 isoenzyme involved has not been determined. The major metabolite, desmethylazelastine, also has H1-receptor antagonist activity.
Enzyme Metabolite Reaction Km Vmax
Cytochrome P450 2D6 Desmethylazelastine


Cytochrome P450 1A2 Desmethylazelastine


Cytochrome P450 3A4 Desmethylazelastine


Cytochrome P450 2C19 Desmethylazelastine


Route of elimination Approximately 75% of an oral dose of radiolabeled azelastine hydrochloride was excreted in the feces with less than 10% as unchanged azelastine. Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system.
Half life Elimination half-life (based on intravenous and oral administration) is 22 hours. Elimination half-life of the active metabolite, desmethylazelastine, is 54 hours (after oral administration of azelastine).
Clearance
  • 0.5 L/h/kg [symptomatic patients]
Toxicity Not Available

Azelaic Acid

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Absorption Approximately 4% of the topically applied azelaic acid is systemically absorbed.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Mainly excreted unchanged in the urine but undergoes some b-oxidation to shorter chain dicarboxylic acids.
Route of elimination Azelaic acid is mainly excreted unchanged in the urine, but undergoes some ß-oxidation to shorter chain dicarboxylic acids.
Half life The observed half-lives in healthy subjects are approximately 45 minutes after oral dosing and 12 hours after topical dosing, indicating percutaneous absorption rate-limited kinetics.
Clearance Not Available
Toxicity Oral LD50 in rat: >5 g/kg
Affected organisms
  • Various aerobic and anaerobic microorganisms
Copyright 2011 Pharmacokinetics of Drugs.
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