gemifloxacin


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gemifloxacin

(gem-i-flox-a-sin) ,

Factive

(trade name)

Classification

Therapeutic: anti infectives
Pharmacologic: fluoroquinolones
Pregnancy Category: C

Indications

Treatment of the following bacterial respiratory infections: :
  • Acute bacterial exacerbations of chronic bronchitis,
  • Community-acquired pneumonia.

Action

Inhibits bacterial DNS synthesis by inhibiting DNA gyrase enzyme.

Therapeutic effects

Death of susceptible bacteria resulting in resolution of infection.
Active against gram-positive pathogens including:
  • Streptococcus pneumoniae.
Gram-negative spectrum notable for:
  • Klebsiella pneumoniae,
  • Haemophilus influenzae,
  • Haemophilus parainfluenzae,
  • Moraxella catarrhalis.
Additional spectrum includes:
  • Chlamydophylia pnaumoniae,
  • Mycoplasma pneumoniae.

Pharmacokinetics

Absorption: 71% absorbed following oral administration.
Distribution: Widely distributed; penetrates lung tissue and fluids well.
Metabolism and Excretion: Minimal metabolism; 61% excreted unchanged in feces, 36% excreted unchanged in urine.
Half-life: 7 hr.

Time/action profile (blood levels)

ROUTEONSETPEAKDURATION
POrapid0.5–2 hr24 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity (cross-sensitivity within class may exist); History of myasthenia gravis (may worsen symptoms including muscle weakness and breathing problems); QTc interval prolongation; Uncorrected hypokalemia or hypomagnesemia; Concurrent use of Class IA antiarrhythmics (disopyramide, quinidine, procainamide) or Class III antiarrhythmics (amiodarone, sotalol) (↑risk of QTc interval prolongation and torsade de pointes); Obstetric / Lactation / Pediatric: Safety not established.
Use Cautiously in: Known or suspected CNS disorder; Renal impairment (↓ dose if CCr ≤40 mL/min); Concurrent use of erythromycin, antipsychotics, and tricyclic antidepressants (↑risk of QTc interval prolongation and torsade de pointes); Concurrent use of corticosteroids (↑ risk of tendinitis/tendon rupture); Kidney, heart, or lung transplant patients (↑ risk of tendinitis/tendon rupture); Geriatric: ↑ risk of adverse reactions.

Adverse Reactions/Side Effects

Central nervous system

  • elevated intracranial pressure (including pseudotumor cerebri) (life-threatening)
  • seizures (life-threatening)
  • agitation
  • anxiety
  • confusion
  • depression
  • dizziness
  • drowsiness
  • hallucinations
  • headache
  • insomnia
  • nightmares
  • paranoia
  • tremor

Cardiovascular

  • torsade de pointes (life-threatening)
  • QT interval prolongation

Gastrointestinal

  • pseudomembranous colitis (life-threatening)
  • diarrhea
  • abdominal pain
  • nausea
  • vomiting

Dermatologic

  • stevens-johnson syndrome (life-threatening)
  • photosensitivity
  • rash

Musculoskeletal

  • tendinitis
  • tendon rupture

Neurologic

  • peripheral neuropathy

Interactions

Drug-Drug interaction

Concurrent use ofamiodarone, disopyramide, erythromycin, procainamide, dofetilide, quinidine, some antipsychotics, sotalol, or tricyclic antidepressants ↑ risk of torsade de pointes in susceptible individuals (avoid concurrent use).Administration with magnesium and aluminum-containing antacids, iron salts, bismuth subsalicylate, sucralfate, didanosine (chewable/buffered tablets or pediatric powder for oral solution), zinc salts, and other metals ↓ absorption.Concurrent use of corticosteroids may ↑ the risk of tendon rupture.May ↑ the risk of nephrotoxicity from cyclosporine.Levels are ↑ by probenecid.

Route/Dosage

Acute bacterial exacerbation of chronic bronchitis (ABECB)

Oral (Adults) 320 mg once daily for 5 days.

Community-acquired-pneumonia (CAP)

Oral (Adults) 320 mg once daily for 7 days.

Renal Impairment

Oral (Adults) CCr ≤40 mL/min AECB: 160 mg once daily for 5 days; CAP: 160 mg once daily for 7 days.

Availability

Tablets: 320 mg

Nursing implications

Nursing assessment

  • Assess patient for infection (vital signs; appearance of wound, sputum, urine, and stool; WBC; urinalysis; frequency and urgency of urination; cloudy or foul-smelling urine) prior to and during therapy.
  • Obtain specimens for culture and sensitivity before initiating therapy. First dose may be given before receiving results. To prevent development of resistant bacteria, therapy should only be used to treat infections that are proven or strongly suspected to be caused by susceptible bacteria.
  • Observe patient for signs and symptoms of anaphylaxis (rash, pruritus, laryngeal edema, wheezing). Discontinue drug and notify physician or other health care professional immediately if these problems occur. Keep epinephrine, an antihistamine, and resuscitation equipment close by in case of an anaphylactic reaction. Patients at greater risk for rash are those receiving gemifloxacin for >7 days, <40 yrs of age, females, and postmenopausal females receiving hormone replacement therapy.
  • Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of pseudomembranous colitis. May begin up to several weeks following cessation of therapy.
  • Assess for rash periodically during therapy. May cause Stevens-Johnson syndrome. Discontinue therapy if severe or if accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis and/or eosinophilia.
  • Lab Test Considerations: May cause ↑ serum AST and ALT levels.
    • Monitor prothrombin time closely in patients receiving gemifloxacin and warfarin. Other fluoroquinolones have been reported to enhance the anticoagulant effects of warfarin.

Potential Nursing Diagnoses

Risk for infection (Indications)

Implementation

  • Oral: May be taken with a full glass of liquid, without regard to meals. Tablet should be swallowed whole; do not crush, break, or chew. Products or foods containing calcium, magnesium, aluminum, iron, or zinc should not be ingested for 4 hr before and 2 hr after administration. Gemifloxacin should be taken at least 2 hr before sucralfate.

Patient/Family Teaching

  • Instruct patient to take medication as directed and to finish drug completely, even if feeling better. Take missed doses as soon as remembered, unless almost time for next dose. Do not double doses or take more than 1 dose/day. Advise patient that sharing of this medication may be dangerous. Caution patients that gemifloxacin should only be used to treat bacterial infections; it is not effective against viral infections, such as the common cold.
  • Encourage patient to maintain a fluid intake of at least 1500–2000 mL/day to prevent crystalluria.
  • Advise patient that antacids or medications containing calcium, magnesium, aluminum, iron, or zinc will decrease absorption and should not be taken within 4 hr before or 2 hr after gemifloxacin.
  • May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
  • Advise patient to notify health care professional of any personal or family history of QTc prolongation or proarrhythmic conditions such as recent hypokalemia, significant bradycardia, or recent myocardial ischemia or if fainting spells or palpitations occur. Patients with this history should not receive gemifloxacin.
  • Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions during and for 5 days after therapy. Notify health care professional if a sunburn-like reaction or skin eruption occurs.
  • Advise patient to notify health care professional if signs and symptoms of peripheral neuropathy (pain, burning, tingling, numbness, weakness, other alterations in sensations of light touch, pain, temperature, position sense, and vibratory sensation). May require discontinuation of therapy; may be irreversible.
  • Advise patient to report signs of superinfection (furry overgrowth on the tongue, vaginal itching or discharge, loose or foul-smelling stools).
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
  • Instruct patient to notify health care professional if fever and diarrhea develop, especially if stool contains blood, pus, or mucus. Advise patient not to treat diarrhea without consulting health care professional.
  • Instruct patient to notify health care professional immediately if rash, jaundice, signs of hypersensitivity, or tendon (shoulder, hand, Achilles, and other) pain, swelling, or inflammation occur. If tendon symptoms occur, avoid exercise and use of the affected area. Increased risk in >65 yrs old, kidney, heart and lung transplant recipients, and patients taking corticosteroids concurrently. Therapy should be discontinued.

Evaluation/Desired Outcomes

  • Resolution of the signs and symptoms of bacterial infection. Time for complete resolution depends on organism and site of infection.
References in periodicals archive ?
* A single dose of gemifloxacin 320 mg PO plus azithromycin 2 g PO or
In vitro activity of gemifloxacin against a broad range of recent clinical isolates from the USA.
(Fournier B et al., 2000, Solanki K et al., 1993).In research by Syed Qaiser Shah * Muhammad Rafiullah Khan was released in December 2010 , the composition of, Gemifloxacin - technetium- 99 , introduced as a special agent for imaging of infections caused by Streptococcus pneumonia.
Other fluoroquinolones such as gemifloxacin, sparfloxacin, grepafloxacin, trovafloxacin, and garenoxacin have been shown to be effective against M.
The recruited subjects were divided into eight groups of fluoroquinolones: - Ofloxacin, Ciprofloxacin, Norfloxacin, Levofloxacin, Lomefloxacin, Moxifloxacin, Gemifloxacin and Sparfloxacin.
Some practitioners have found drugs such as ciprofloxacin (Cipro), levofloxacin (Levaquin), gemifloxacin (Factive), and moxifloxacin (Avelox) to be helpful in those with Bartonella, though these drugs may lead to long-term tendon damage and ruptures, retinal detachment, and a host of other symptoms that may persist long after these medications have been stopped.
Table 1 shows single drug percentage price variation for various fluoroquinolones, which was as follows: ofloxacin (200 mg) 869%; sparfloxacin (200 mg) 648%; gemifloxacin (320 mg) 477%; norfloxacin (400 mg) 291%; ciprofloxacin (500 mg) 290%; levofloxacin (250 mg) 264%; lomefloxacin (400 mg) 104%; and moxifloxacin (400 mg) 60%.
Gemifloxacin mesylate (GMF) is (R,S)-7-[(4Z)-3-(aminomethyl)-4-(methoxyimino)-1-pyrrolidinyl]-1-cydopropyl-6- fluoro-1, 4-dihydro-4-oxo-1, 8-naphthyridine-3-carboxylic acid methanesulfonate, and moxifloxacin (MOX) is {1-cyclopropyl-7-[2,8-diazobicyclo (4.3.0) nonane]-6-fluoro-8-methoxy-1,4 dihydro-4-oxo-3-quinoline carboxylic acid} (Scheme 1) [1].
Liu et al., "Synthesis and in vitro antibacterial activity of gemifloxacin derivatives containing a substituted benzyloxime moiety," European Journal of Medicinal Chemistry, vol.
Tetracyclines and macrolides are often used, with quinolones for alternative treatment, particularly gemifloxacin. For Bartonella henselae, Chlamydia trachomatis, and Chlamydophila pneumoniae the combination with rifampicin is recommended [105].