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Gatifloxacin, Uses, Dosage, Side Effects, Interactions, Pregnancy

Gatifloxacin is a synthetic 8-methoxyfluoroquinolone with antibacterial activity against a wide range of gram-negative and gram-positive microorganisms. Gatifloxacin exerts its effect through inhibition of DNA gyrase, an enzyme involved in DNA replication, transcription and repair, and inhibition of topoisomerase IV, an enzyme involved in the partitioning of chromosomal DNA during bacterial cell division.

Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Bristol-Myers Squibb introduced Gatifloxacin in 1999 under the proprietary name Tequin for the treatment of respiratory tract infections, having licensed the medication from Kyorin Pharmaceutical Company of Japan. Allergan produces an eye-drop formulation called Zymar. Gatifloxacin is available as tablets and in various aqueous solutions for intravenous therapy.

Mechanism of Action of Gatifloxacin

Gatifloxacin is a synthetic broad-spectrum 8-methoxyfluoroquinolone antibacterial agent for oral or intravenous administration. is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Gatifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

The bactericidal action of Gatifloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination.

Indications of Gatifloxacin

Ophthalmic Surgery
Conjunctivitis
Conjunctivitis, Bacterial
For the treatment of bronchitis,
Sinusitis,
Community-acquired pneumonia,
Skin infections (abscesses, wounds) caused by S. pneumoniae, H. influenzae, S. aureus, M. pneumoniae, C. pneumoniae, L. pneumophila, S. pyogenes
For the treatment of bronchitis, sinusitis, community-acquired pneumonia, and skin infections (abscesses, wounds) caused by S. pneumoniae, H. influenzae, S. aureus, M. pneumoniae, C. pneumoniae, L. pneumophila, S. pyogenes
Infections when due to gatifloxacin-susceptible pathogens: community-acquired pneumonia (mild to moderate) and complicated urinary tract infections (excluding prostatitis and epididymitis.

Contra-Indications of Gatifloxacin

History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of beta-lactam antibacterial agent (penicillins, monobactams, and carbapenems).
Hemolytic anemia
Liver problems
Interstitial nephritis
Subacute cutaneous lupus erythematosus
Systemic lupus erythematosus
use should be avoided in pregnant or lactating women, and in children with developing teeth because they may result in permanent staining (dark yellow-gray teeth with a darker horizontal band that goes across the top and bottom rows of teeth), and possibly affect the growth of teeth and bones.

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Dosage of Gatifloxacin

Strengths: 0.5%; 0.3%

Bacterial Conjunctivitis

0.3% solution

Days 1 and 2: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
Days 3 through 7: Instill 1 drop in the affected eye(s) up to 4 times a day while awake.

0.5% solution

Day 1: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
Days 2 through 7: Instill 1 drop in the affected eye(s) 2 to 4 times a day while awake.

Bacterial Conjunctivitis

1 year or older, 0.3% solution

Days 1 and 2: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
Days 3 through 7: Instill 1 drop in the affected eye(s) up to 4 times a day while awake.

0.5% solution

Day 1: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
Days 2 through 7: Instill 1 drop in the affected eye(s) 2 to 4 times a day while awake.

Pediatric Bacterial Conjunctivitis

1 year or older; 0.3% solution

Days 1 and 2: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
Days 3 through 7: Instill 1 drop in the affected eye(s) up to 4 times a day while awake.

0.5% solution

Day 1: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
Days 2 through 7: Instill 1 drop in the affected eye(s) 2 to 4 times a day while awake.

Side Effects of Gatifloxacin

The most common side effects

allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
Eye irritation
eye pain
eye redness
pain, swelling, irritation where injected
Abdominal pain
sweating
skin color change, mild diarrhea
mild nausea
loss of appetite
vaginal discharge and itching
swelling of feet or legs
chest pain
constipation
a cough
diarrhea or loose stools
difficulty with breathing
dizziness
heartburn

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More common

Abdominal or stomach pain, discomfort, or tenderness
chills or fever
a headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
excessive sweating
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
decreased amount of urine

Rare

Drug Interactions of Gatifloxacin

Gatifloxacin may interact with following drugs, supplements, & may change the efficacy of drugs

antacids that contain aluminum, calcium, or magnesium
birth control medications
bismuth subsalicylate
calcium supplements
digoxin
Rosuvastatin
Duloxetine
Albuterol
Topiramate
Carbamazepine
Vitamin D3 (cholecalciferol)
Alprazolam
Cetirizine
insulin
iron supplements
penicillin
vitamin A derivatives (e.g. isotretinoin)
warfarin
zinc sulfate or gluconate

Pregnancy & Lactation of Gatifloxacin

FDA Pregnancy Category C

Pregnancy

There are no data available on gatifloxacin ophthalmic use in pregnancy to inform a drug-associated risk. However, animal data have shown that administration of oral gatifloxacin throughout organogenesis and during late gestation through lactation did not produce adverse maternal, fetal, or neonatal effects at clinically relevant doses.

Breastfeeding

There are no data available regarding the presence of gatifloxacin in human milk, the effect of gatifloxacin on breastfeeding infants, or the effect of gatifloxacin on milk production. Animal data have shown that gatifloxacin is excreted in breast milk following oral administration;

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