FARDOBEN ORAL SPRAY

Indications

• Oral hygiene
• Skin antisepsis
• Bladder irrigation
• Urological surgery
• Management of infections associated with indwelling urinary catheters

Mechanism of action

Chlorhexidine's antimicrobial effects arise from its ability to disrupt microbial cell membranes. The positively charged chlorhexidine molecule interacts with negatively charged phosphate groups on microbial surfaces, compromising cell integrity and causing leakage of intracellular materials. This interaction allows chlorhexidine to enter the cell, precipitate cytoplasmic components, and ultimately induce cell death. At lower concentrations, chlorhexidine acts as a bacteriostatic agent, causing leakage of substances like potassium and phosphorus, while at higher concentrations, it exerts bactericidal effects.

Pharmacodynamics

Chlorhexidine exhibits broad-spectrum antimicrobial activity, effective against a variety of bacteria, yeasts, and viruses. Its action is dose-dependent, with lower concentrations (0.02%-0.06%) providing bacteriostatic effects, while higher concentrations (>0.12%) are bactericidal. Pharmacokinetic studies indicate that about 30% of chlorhexidine remains in the mouth after rinsing, allowing for slow release into oral fluids. This property, known as 'substantivity', helps prevent microbial colonization on surfaces like dentine, although prolonged use can lead to staining of oral surfaces.

Pharmacokinetics

Chlorhexidine is retained in the oral cavity at approximately 30% following rinsing, with a slow release into saliva. The pharmacokinetics of chlorhexidine indicate a high affinity for binding to tissues, which prolongs its antimicrobial action. The systemic absorption of chlorhexidine is minimal when used topically or as a rinse, making it safe for localized use. The elimination half-life and metabolism details are not well documented due to its primarily topical application.

Adverse effects

• Mucosal irritation
• Burning sensation
• Staining of teeth and oral surfaces
• Allergic reactions

Precautions

• Use with caution in patients with a history of hypersensitivity to chlorhexidine
• May cause irritation; discontinue if severe irritation occurs
• Staining may occur with prolonged use, particularly with oral formulations

Pregnancy

Chlorhexidine is generally considered safe for use during pregnancy; however, caution is advised and pregnant individuals should consult healthcare providers.

Breast-feeding

Chlorhexidine is considered safe during breastfeeding, but it is advisable to consult a healthcare provider.

Storage

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

Formulations

• Irrigation solution (0.02% and 0.05%)
• Capsules (various strengths)
• Catheter maintenance solution (1:5000)
• Topical solutions for oral hygiene

Indications

• Hypomagnesemia
• Hypocalcemia
• Electrolyte imbalance
• Support in conditions causing electrolyte loss
• Management of certain metabolic disorders

Dosage

Children: Refer to the BNF for Children and local guidelines for

Adults: Refer to specific clinical guidelines and local protocols for dosing recommendations, as no standard adult dosage is provided.

Mechanism of action

Digluconate acts by dissociating in the body to release the respective metal ions, which are crucial for various physiological functions. The released ions participate in numerous biochemical pathways, including enzymatic reactions, muscle contraction, and nerve conduction. The specific mechanism can vary depending on the ion being provided, but generally, these ions contribute to homeostasis and cellular function.

Pharmacodynamics

The pharmacodynamics of digluconate depend on the specific ions released upon dissociation. For example, magnesium ions are involved in over 300 enzymatic reactions, including ATP production and muscle function, while calcium ions are vital for bone health, neurotransmission, and muscle contraction. The balance of these ions is essential for normal physiological function, and their replenishment can correct underlying deficiencies and restore homeostasis in affected patients.

Pharmacokinetics

Digluconate is typically well absorbed when administered orally or intravenously, with peak plasma concentrations occurring relatively quickly, depending on the route of administration. The bioavailability of the ions released can be influenced by various factors, including the presence of food in the gastrointestinal tract. Distribution occurs to various tissues, with the kidneys playing a crucial role in regulating and excreting excess ions. The half-life of the individual ions can vary, but they are generally eliminated through renal pathways, necessitating careful monitoring in patients with renal impairment.

Pregnancy

Digluconate is classified as Category C. Animal reproduction studies have not been conducted, and it is not known whether digluconate can cause fetal harm when administered to a pregnant woman. It should only be given if clearly needed.

Breast-feeding

It is not known whether digluconate is excreted in human milk. Caution should be exercised when administering to nursing women.

Storage

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

Indications

• Sore throat
• Oral ulcers
• Inflammation of the mucous membranes
• Topical pain relief in inflammatory conditions

Dosage

Children: Refer to specific product guidelines for dosage, as it can vary based on formulation and indication.

Adults: Refer to specific product guidelines for dosage, as it can vary based on formulation and indication.

Mechanism of action

Benzydamine exerts its effects by inhibiting the synthesis of prostaglandins, which are mediators of inflammation and pain. It also stabilizes cellular membranes and has local anesthetic properties, which contribute to its analgesic effects.

Pharmacodynamics

Benzydamine has both anti-inflammatory and analgesic properties, making it effective in reducing pain and swelling associated with inflammatory conditions. Its ability to inhibit pain pathways and reduce inflammatory mediators helps to alleviate symptoms of discomfort in affected areas.

Pharmacokinetics

Benzydamine is absorbed locally when applied topically, with minimal systemic absorption. This results in a rapid onset of action at the site of application, while systemic effects are minimal due to its poor oral bioavailability. The drug is metabolized in the liver and eliminated primarily through the urine. The half-life is relatively short, necessitating frequent dosing for sustained effect.

Contra-indications

• Hypersensitivity to benzydamine or any of the excipients
• History of asthma or allergic reactions to non-steroidal anti-inflammatory drugs (NSAIDs)
• Severe liver or renal impairment

Adverse effects

• Local irritation or burning sensation at the site of application
• Dry mouth
• Nausea
• Dizziness
• Allergic reactions such as rash or urticaria

Interactions

• Possible interaction with other topical medications leading to increased local irritation
• No significant systemic interactions reported

Precautions

• Use with caution in patients with a history of hypersensitivity to NSAIDs
• Should not be used in large areas of damaged skin or on deep wounds
• Not recommended for prolonged use without medical supervision

Pregnancy

Benzydamine should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. Consult a healthcare provider before use.

Breast-feeding

Limited data available, consult a healthcare provider before use while breastfeeding.

Storage

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

Formulations

• Topical cream
• Oral rinse
• Spray form

Mechanism of action

Chlorhexidine’s broad-spectrum antimicrobial effects are due to its ability to disrupt microbial cell membranes. The positively charged chlorhexidine molecule reacts with negatively charged phosphate groups on microbial cell surfaces - this reaction both destroys the integrity of the cell, allowing leakage of intracellular material, and allows chlorhexidine to enter the cell, causing precipitation of cytoplasmic components and ultimately cell death. The specific means of cell death is dependent on the concentration of chlorhexidine - lower concentrations are bacteriostatic and result in leakage of intracellular substances such as potassium and phosphorous, whereas higher concentrations are bactericidal and cause cytoplasmic precipitation.

Pharmacodynamics

Chlorhexidine is a broad-spectrum antimicrobial with demonstrated activity against both gram-positive and gram-negative bacteria, yeasts, and viruses. Antimicrobial activity is dose-dependent - chlorhexidine is bacteriostatic at lower concentrations (0.02%-0.06%) and bactericidal at higher concentrations (>0.12%). Pharmacokinetic studies of oral chlorhexidine rinses indicate that approximately 30% of the active ingredient is retained in the mouth following rinsing, which is subsequently slowly released into oral fluids. This ability to adsorb to dentine, shared with tetracycline antibiotics such as [doxycycline], is known as "substantivity" and is the result of chlorhexidine's positive charge - it is likely that this substantivity plays at least some role in chlorhexidine's antimicrobial activity, as its persistence on surfaces such as dentine prevent microbial colonization. Dental chlorhexidine rinses may result in staining of oral surfaces, such as teeth. This effect is not ubiquitous and appears to be more significant with extended therapy (i.e. up to 6 months) - nevertheless, patients for whom oral staining is unacceptable should use chlorhexidine rinse with caution and for the shortest effective interval. Allergic reactions to chlorhexidine have been associated with the development of anaphylaxis.