FLORDOX SOLUTION

Indications

• Bacterial infections
• Acne
• Destructive (refractory) periodontal disease
• Exacerbations of chronic bronchitis
• Leptospirosis
• Chlamydia infections
• Rickettsial infections
• Mycoplasma infections
• Acute necrotising ulcerative gingivitis

Dosage

Children: For children aged 12–17 years, initially 200 mg daily in 1–2 divided doses for the

Adults: Initially 200 mg daily in 1–2 divided doses for the first day, then maintenance 100 mg daily.

Mechanism of action

Doxycycline exerts its antibacterial effects by binding to the 30S ribosomal subunit of bacterial ribosomes, inhibiting the binding of aminoacyl-tRNA to the mRNA-ribosome complex. This inhibition of protein synthesis is crucial for bacterial growth and is the primary mechanism by which doxycycline exhibits its antimicrobial activity. It also impacts cellular metabolism and has been associated with non-genotoxic carcinogenic effects.

Pharmacodynamics

Doxycycline has a broad spectrum of activity against Gram-positive, Gram-negative bacteria, and some protozoa. Its bacteriostatic action is particularly effective against certain resistant strains, including MRSA. The drug's efficacy may vary based on the sensitivity of the bacteria, and resistance can develop through various mechanisms, such as efflux pumps and ribosomal protection.

Pharmacokinetics

Doxycycline is well absorbed from the gastrointestinal tract, with peak plasma concentrations typically reached within 2 hours after oral administration. It has a high volume of distribution and is approximately 90% protein-bound. The drug is metabolized in the liver and excreted primarily in feces, with a smaller fraction eliminated in urine. The half-life of doxycycline is approximately 18 to 22 hours, allowing for once or twice daily dosing in most cases.

Contra-indications

• Pregnancy
• Breastfeeding
• Hypersensitivity to doxycycline or other tetracyclines
• Myasthenia gravis
• Severe hepatic impairment

Adverse effects

• Photosensitivity
• Dizziness
• Headache
• Nausea
• Vomiting
• Diarrhoea
• Angioedema
• Skin reactions
• Pseudomembranous enterocolitis
• Tooth discolouration
• Intracranial hypertension
• Thrombocytopenia
• Stevens-Johnson syndrome
• Pancreatitis

Interactions

• Fosphenytoin (decreases concentration)
• Rifampicin (decreases exposure)
• Ciclosporin (unknown effect on concentration)
• Antacids containing aluminium or magnesium (reduce absorption)
• Iron supplements (reduce absorption)
• Warfarin (may enhance anticoagulant effect)

Precautions

• Use with caution in renal impairment
• May cause increased intracranial pressure
• Risk of superinfection (e.g., fungal infections)
• Avoid exposure to sunlight or sun lamps
• Monitor liver function in patients receiving prolonged therapy

Pregnancy

Should not be given to pregnant women; effects on skeletal development have been documented in the first trimester in animal studies. Administration during the second or third trimester may cause discoloration of the child's teeth, and maternal hepatotoxicity has been reported with large parenteral doses.

Breast-feeding

Should not be given to women who are breastfeeding; absorption may lead to discoloration of teeth in the infant.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Formulations

• Tablets
• Capsules
• Oral suspension
• Oral solution

Indications

• Motion sickness
• Nausea and vomiting
• Gastrointestinal spasms
• Preoperative sedation

Dosage

Children: Refer to the BNF for Children for specific dosing recommendations based on the child's age, weight, and condition being treated.

Adults: Refer to the appropriate clinical guidelines or BNF for specific dosing recommendations based on the condition being treated and patient factors.

Mechanism of action

Hyclate exerts its effects by antagonizing muscarinic acetylcholine receptors, which are found throughout the central and peripheral nervous systems. This inhibition leads to a decrease in acetylcholine-induced effects, particularly in the gastrointestinal system and vestibular apparatus, thus alleviating symptoms of nausea and motion sickness.

Pharmacodynamics

The pharmacodynamic effects of hyoscine include reduced gastrointestinal motility, decreased secretions, and a sedative effect on the central nervous system. Its antimuscarinic activity can result in side effects such as dry mouth, blurred vision, constipation, and drowsiness, depending on the dose and individual patient response.

Pharmacokinetics

Hyclate is well-absorbed from the gastrointestinal tract, and its peak plasma concentrations are typically reached within 2 hours after oral administration. The drug is widely distributed throughout the body, including the central nervous system where it crosses the blood-brain barrier. Hyoscine is metabolized in the liver and excreted primarily through the urine. The half-life of hyoscine is approximately 3 to 5 hours, but this can vary based on the formulation and route of administration.

Contra-indications

• Hypersensitivity to hyoscyamine or any of the excipients
• Glaucoma
• Myasthenia gravis
• Severe ulcerative colitis
• Tachycardia

Adverse effects

• Dry mouth
• Blurred vision
• Constipation
• Urinary retention
• Dizziness
• Confusion
• Nausea
• Vomiting

Interactions

• Anticholinergic agents may enhance effects
• Opioids may increase risk of constipation
• Antidepressants may increase anticholinergic effects
• Antihistamines may have additive sedative effects

Precautions

• Use with caution in patients with prostate enlargement
• May exacerbate conditions like heart disease or hypertension
• Caution in elderly patients due to increased sensitivity

Pregnancy

Consult the prescribing information; safety during pregnancy is not established.

Breast-feeding

Consult a healthcare provider; may inhibit lactation.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Oral tablets
• Injection solution
• Extended-release capsules

Indications

• Urinary tract infections
• Cystitis
• Prostatitis
• Gastrointestinal infections
• Traveler's diarrhea

Dosage

Children: Refer to the BNF for Children for specific dosing information.

Adults: Refer to the relevant prescribing guidelines for specific dosing recommendations based on the condition being treated.

Mechanism of action

Norfloxacin exerts its antibacterial effects by inhibiting DNA gyrase and topoisomerase IV, which are critical for bacterial DNA replication and repair. This leads to disruption of the bacterial cell cycle and ultimately results in bacterial cell death.

Pharmacodynamics

Norfloxacin shows concentration-dependent bactericidal activity against susceptible organisms. Its mechanism involves interference with DNA synthesis, leading to the formation of double-stranded breaks in bacterial DNA, which prevents replication and transcription. The drug has a broad spectrum of activity against various gram-negative pathogens and some gram-positive bacteria.

Pharmacokinetics

Norfloxacin is well absorbed orally, with peak plasma concentrations achieved within 1 to 2 hours post-administration. It has a bioavailability of approximately 30-40%. The drug is widely distributed in body tissues and fluids, including the prostate and urine. It is metabolized in the liver and mainly excreted unchanged in the urine. The half-life of norfloxacin is about 3 to 4 hours, and dose adjustments may be necessary in patients with renal impairment.

Contra-indications

• Hypersensitivity to norfloxacin or other fluoroquinolones
• History of tendon disorders related to fluoroquinolone use
• Pregnancy and lactation

Adverse effects

• Nausea
• Diarrhea
• Headache
• Dizziness
• Rash
• Tendon rupture
• QT prolongation
• Photosensitivity

Interactions

• Antacids containing magnesium, aluminum, or calcium may decrease absorption
• Nonsteroidal anti-inflammatory drugs (NSAIDs) may increase the risk of CNS stimulation
• Warfarin may have increased anticoagulant effects

Precautions

• Use with caution in patients with renal impairment
• Monitor for signs of peripheral neuropathy
• Avoid in patients with a history of seizure disorders
• Caution in patients with myasthenia gravis as it may exacerbate muscle weakness

Pregnancy

Norfloxacin is contraindicated in pregnancy due to potential risks to the fetus.

Breast-feeding

Norfloxacin is excreted in breast milk; breastfeeding is not recommended during treatment.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Tablets
• Intravenous injection