Ciprofloxacin

BRAND NAMES:

Ciplox – It includes the active components of ciprofloxacin hydrochloride. It is offered as tablets. 

Cetraxa -  It contains the active components of ciprofloxacin. It comes in the form of a treatment for external otitis. 

Ciloxan- Contains the active compounds found in ciprofloxacin HCl. It takes the form of ocular and otic solutions. 

Cipro-  Comprises the active components of ciprofloxacin HCL. It is accessible as oral pills. 

Proquin - Comprises the active components from ciprofloxacin HCL. It is offered as tablets. Proquin XR - These pills are exclusively used to treat uncomplicated, mild urinary tract infections.

MECHANISM OF ACTION:

Ciprofloxacin acts on bacterial topoisomerase Ⅱ and topoisomerase IV. ciprofloxacin targeting of the alpha subunits of DNA gyrase prevents it from supercoiling the bacteria DNA which prevents DNA replication. 

PHARMACOKINETICS:

Absorption: Ciprofloxacin is readily absorbed but typically does not achieve complete absorption. The bioavailability of oral ciprofloxacin is 70% to 80%. The peak concentrations after oral administration Tmax are 1 to 1.5 hours. Avoid concurrent administration of ciprofloxacin with dairy products or calcium-fortified juices due to decreased absorption.

Distribution: The mean volume of distribution of ciprofloxacin is 2.0 to 3.04L/kg.

Metabolism: Ciprofloxacin inhibits human cytochrome P450 1A2. Ciprofloxacin co-administration with other medicines metabolized by CYP1A2 increases plasma concentrations of these drugs, which may lead to toxicity. 

Excretion: Approximately 40 to 50 percent of an oral given dose is eliminated in the urine as unmodified medication. Ciprofloxacin caused 45% recovery in urine and 62% recovery in feces.

PHARMACODYNAMICS:

Ciprofloxacin is a second-generation fluoroquinolone that works against both gram-negative and gram-positive bacteria. It exerts its function by inhibiting bacterial DNA gyrase and topoisomerase IV. Ciprofloxacin has a 100-fold higher affinity for bacterial DNA gyrase than mammalian DNA gyrase. 

DOSAGE AND ADMINISTRATION:

These are available in tablets, capsules, and oral suspensions.

Tablets contain a strength of 250mg and capsules are available with a strength of 500mg.

Oral suspensions –

• 5% of oral suspension- 250 mg of ciprofloxacin per 5ml after reconstitution
• 10% oral suspension- 500mg of ciprofloxacin per 5ml after reconstitution.

Ciprofloxacin is available orally, intravenously, and in topical formulations. Ciprofloxacin is administered orally twice daily for 7 to 14 days or at least two days after signs and symptoms of the infection are over. The recommended oral dose regimen is 250 mg twice daily to treat mild to moderate and 500 mg twice daily for severe or complicated urinary tract infections. Therapy for mild to moderate respiratory tract or skin and soft tissue infections requires 500mg twice–daily dosing. Comparatively, a dosage of 750mg twice daily is recommended for severe or complicated infections. Ciprofloxacin should be given with food to minimize gastrointestinal upset. 

CONTRAINDICATIONS:

Ciprofloxacin is contraindicated in people who have a documented allergy to the medication or its formulation components. Tizanidine was administered concurrently. Ciprofloxacin and its fluoroquinolone class should be avoided in people with myasthenia gravis because they can worsen muscular weakness.

DRUG INTERACTIONS:

Drug interactions with ciprofloxacin include

Inflammatory drugs- corticosteroids

• Nonsteroidal anti-inflammatory drugs- ibuprofen, naproxen
• Muscle relaxant- Tizanidine
• Gout drugs- Probenecid
• Anti-psychotic- medicines for certain mental health conditions
• Breathing problems- Theophylline
• Anti-arrhythmic- which is a medicine to control  your heartbeat
• Blood thinner-warfarin
• Seizures- Phenytoin
• Immuno suppressants- Cyclosporine
• Methotrexate
• Parkinson's disease- Ropinirole
• Diuretics- Edema

SIDE EFFECTS:

• Nausea

• Vomiting

• Diarrhea

• Stomach pain 

• Headache

• Low blood sugar

• Irritability

• Dizziness

• Fast heartbeat

• Numbness

• Tingling

• Pain in your hands, arms, legs or feet

• Behavior changes

• Nervousness

• Confusion 

• Agitation

• Paranoia

• Hallucinations

• Trouble concentrating on thoughts of suicide.

• Signs of tendon rupture

• Stiffness movement problems of joints.

• Severe skin reaction 

• Fever

• Sore throat

OVERDOSE:

Acute kidney injury following ciprofloxacin overdose has been reported. There is no specific antidote to ciprofloxacin in overdose. Consider using magnesium and calcium-containing antacids to reduce the oral absorption of ciprofloxacin. Consider intermittent hemodialysis for ciprofloxacin. 

TOXICITY:

Clinical data indicate no significant evidence of osteoarticular toxicity in newborns and children. In these studies, the drug exposure of neonates and children was at much higher doses compared to children whose exposure was via breastfeeding. Therefore  limited evidence suggesting ciprofloxacin excretion in breast milk.

STORAGE:

Store at room temperature (68-77°F/20-25°C). Keep away from sunlight.