API Levofloxacin hydrochloride

Levofloxacin hydrochloride More Info

Levofloxacin Hydrochloride is a synthetic, broad-spectrum fluoroquinolone antibiotic that belongs to the third generation of quinolone drugs. It is the pure (-)-S-enantiomer of the racemic compound ofloxacin, which gives it approximately double the antibacterial activity of its racemic counterpart.

Key Chemical and Physical Properties:

Chemical Name: (3S)-9-Fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid hemihydrate (Levofloxacin Hydrochloride).

Molecular Formula: C₁₈H₂₀FN₃O₄·0.5H₂O (monohydrate).

Molecular Weight: Approximately 370.38 g/mol.

Physical Appearance: Light yellow to yellowish-white crystalline powder.

Solubility: Highly soluble in water (≈100 mg/mL) across a wide pH range (0.6 to 5.8).

Pharmacology and Mechanism of Action:

Levofloxacin Hydrochloride exerts its antibacterial effect by inhibiting bacterial DNA gyrase (DNA topoisomerase II) and topoisomerase IV. This inhibition blocks DNA replication and transcription, leading to bacterial cell death.

Spectrum of Activity:

The drug has a broad antibacterial spectrum, effective against a wide range of aerobic Gram-positive and Gram-negative bacteria. It also demonstrates activity against certain anaerobic bacteria.

Dosage Forms and Administration:

Levofloxacin Hydrochloride is available in multiple dosage forms:

Oral Tablets: Typically 250 mg, 500 mg, and 750 mg, often film-coated.

Oral Solution: Typically 25 mg/mL, clear yellow to greenish-yellow.

Injectable Formulations: Includes single-use vials and premixed infusion bags (often combined with sodium chloride) for intravenous administration.

Indications:

The drug is indicated for the treatment of infections caused by susceptible microorganisms in various systems, including:

Respiratory Tract: Acute and chronic bronchitis, diffuse bronchiolitis, bronchiectasis with infection, pneumonia, tonsillitis, and peritonsillar abscess.

Urinary Tract: Acute pyelonephritis, complicated urinary tract infections.

Reproductive System: Acute prostatitis, acute epididymitis, endometritis, salpingo-oophoritis, and pelvic inflammatory disease (often combined with metronidazole if anaerobic infection is suspected).

Skin and Soft Tissue: Infectious impetigo, cellulitis, lymphangitis, subcutaneous abscess, perianal abscess.

Gastrointestinal Tract: Bacterial dysentery, infectious enteritis, salmonella enteritis, typhoid, and paratyphoid fever.

Other: Septicemia, infections in neutropenic patients, and infections in immunocompromised individuals.

Pharmacokinetics:

Absorption: Levofloxacin Hydrochloride is rapidly and completely absorbed after oral administration, with a bioavailability of approximately 99%.

Distribution: It has a high volume of distribution (74–112 L) and penetrates well into various tissues, including the skin and lungs.

Metabolism and Excretion: Minimal metabolism occurs; the drug is primarily excreted unchanged in the urine. The terminal half-life is approximately 6–8 hours, and dose adjustment may be required in patients with renal impairment.

Safety Profile:

While the drug is generally well-tolerated, it has a range of potential severe side effects, including:

Serious Adverse Reactions: Anaphylaxis, Stevens-Johnson syndrome, toxic epidermal necrolysis, QT interval prolongation, seizures, and acute renal failure.

Musculoskeletal: Tendon rupture (especially Achilles tendon) and exacerbation of myasthenia gravis.

Metabolic: Hypoglycemia and hyperglycemia.

Neurological: Peripheral neuropathy and delirium.

Regulatory and Usage Notes:

Levofloxacin Hydrochloride is a prescription-only medication (Rx) and should be used under the guidance of a qualified healthcare professional. The drug is not recommended for use in patients with known hypersensitivity to fluoroquinolones or in those with a history of tendon disorders related to quinolone therapy.