ORALEX C

Indications

• Painful inflammatory conditions of the oropharynx
• Oral ulceration and inflammation
• Anaesthesia of mucous membranes

Dosage

Children: For children aged 1 month to 5 years: 1-3 sprays every 1.5-3 hours, dependent on body weight and condition; refer to the BNF for Children for precise dosing.

Adults: Refer to the BNF for specific dosing recommendations.

Mechanism of action

Benzydamine hydrochloride exerts its effects by inhibiting the synthesis of prostaglandins, which are mediators of inflammation and pain. It also possesses local anesthetic properties, providing relief from pain upon application to mucous membranes.

Pharmacodynamics

Benzydamine demonstrates anti-inflammatory, analgesic, and local anesthetic effects. It reduces pain and inflammation in the oropharynx, making it beneficial for various inflammatory conditions.

Pharmacokinetics

Benzydamine is rapidly absorbed when administered topically. It is distributed throughout the body, crosses the placenta, and is present in breast milk in small amounts. The drug undergoes hepatic metabolism and is excreted primarily in urine. Caution is advised in patients with hepatic and renal impairment due to potential accumulation.

Contra-indications

• Hypersensitivity to benzydamine or any component of the formulation

Adverse effects

• Oral disorders
• Photosensitivity reaction
• Skin reactions
• Angioedema

Interactions

• Caution with antiarrhythmics
• Caution with NSAIDs

Precautions

• Can damage plastic cuffs of endotracheal tubes
• Caution in hepatic impairment
• Caution in renal impairment

Pregnancy

Crosses the placenta but not known to be harmful in animal studies-use if benefit outweighs risk.

Breast-feeding

Present in milk but amount too small to be harmful.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Oromucosal Spray 0.15% (sugar-free)
• Mouthwash 0.15% (sugar-free)

Indications

• Sore throat
• Mouth ulcers
• Inflammatory conditions of the oral cavity
• Pain relief in conditions causing inflammation in the throat and mouth

Dosage

Children: Refer to the BNF for Children for appropriate dosing information based on the child's age

Adults: The dosage depends on the formulation and the condition being treated. Refer to the specific product information or the BNF for detailed dosing guidelines.

Mechanism of action

Benzydamine acts by inhibiting the synthesis of pro-inflammatory cytokines, such as tumor necrosis factor-alpha (TNF-α) and interleukin-1β (IL-1β), while exerting minimal effects on other pro-inflammatory and anti-inflammatory cytokines. It is a weak inhibitor of prostaglandin synthesis, primarily affecting cyclooxygenase (COX) and lipoxygenase enzyme activity at high concentrations. Additionally, benzydamine is believed to inhibit the oxidative burst of neutrophils and stabilize lysosomes, contributing to its anti-inflammatory and analgesic effects. Its local anesthetic action is attributed to its ability to stabilize neuronal membranes.

Pharmacodynamics

Benzydamine provides local anesthetic and analgesic effects, focusing on the local mechanisms of inflammation such as pain and edema. It is absorbed through the oral mucosa and intact skin, binding selectively to inflamed tissues to exert its effects. The drug typically reaches peak plasma concentration within 2 to 4 hours, enhancing its localized therapeutic efficacy while minimizing systemic adverse effects.

Pharmacokinetics

Benzydamine is primarily administered topically, resulting in limited systemic absorption. Once applied, it accumulates in inflamed tissues, allowing for effective local action. The pharmacokinetic profile indicates that peak concentrations are achieved within 2 to 4 hours post-application, although specific systemic absorption metrics are not extensively characterized due to its localized use.

Adverse effects

• local irritation
• burning sensation
• dryness of the mouth
• nausea
• dizziness

Precautions

• Caution in patients with hypersensitivity to benzydamine or other NSAIDs
• Use with caution in patients with asthma or history of allergic reactions

Pregnancy

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

Breast-feeding

It is unknown whether benzydamine is excreted in human milk. Caution is advised when administering to breastfeeding women.

Storage

Store at room temperature, away from light and moisture. Do not freeze.

Formulations

• oral rinse
• topical gel
• spray

Indications

• Preoperative skin disinfection
• Postoperative wound care
• Oral antiseptic for gingivitis and periodontitis
• Treatment of skin infections
• Irrigation of surgical wounds

Dosage

Children: Refer to BNF for Children for appropriate dosages based on age and condition.

Adults: Refer to specific product guidelines and BNF for appropriate dosages based on condition and formulation.

Mechanism of action

Chlorhexidine works by disrupting the cell membranes of microbes, leading to cell lysis. It binds to negatively charged bacterial cell walls, causing leakage of intracellular components and ultimately resulting in cell death. Its effectiveness is due to its ability to remain active on surfaces and tissues, providing prolonged antimicrobial action.

Pharmacodynamics

Chlorhexidine exhibits a rapid bactericidal effect, with activity increasing with concentration and exposure time. It is particularly effective against gram-positive cocci and some gram-negative rods, as well as fungi. Its residual activity allows it to remain effective even after initial application, making it beneficial for long-term use in certain applications, such as oral rinses.

Pharmacokinetics

Chlorhexidine is poorly absorbed through the gastrointestinal tract when ingested and primarily acts locally at the site of application. When used topically, the absorption through the skin is minimal. The elimination half-life varies depending on the formulation and application, but it is generally short, with the compound being excreted in urine. Its pharmacokinetic profile allows for frequent application without significant systemic effects.

Contra-indications

• Hypersensitivity to chlorhexidine or any of its components
• Ototoxicity when used in the ear canal

Adverse effects

• Skin irritation
• Allergic reactions
• Staining of teeth
• Altered taste sensation
• Dryness of the mouth
• Esophageal ulceration (when used as a mouthwash)

Interactions

• Chlorhexidine may inactivate certain anionic agents, including some soaps and detergents
• Concurrent use with antiseptic agents containing anionic surfactants may lead to reduced efficacy

Precautions

• Avoid contact with the eyes and ears
• Use cautiously in patients with a history of hypersensitivity to chlorhexidine or related compounds
• Prolonged use may lead to the development of resistant microorganisms

Pregnancy

Chlorhexidine is generally regarded as safe for use during pregnancy, but should be used only if clearly needed.

Breast-feeding

Chlorhexidine is considered safe during breastfeeding, but it is recommended to rinse the mouth after use to minimize exposure to the infant.

Storage

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

Formulations

• Topical solutions (0.5% to 4% concentration)
• Mouthwash (0.12% to 0.2% concentration)
• Gels
• Surgical scrubs

Indications

• Oral health maintenance
• Nutritional intake
• Speech production
• Prevention of oral diseases
• Administration of medications

Dosage

Children: Refer to specific medications for dosing guidelines as the mouth itself does not have a dosing regimen.

Adults: Refer to specific medications for dosing guidelines as the mouth itself does not have a dosing regimen.

Mechanism of action

The mouth itself does not have a pharmacological mechanism of action, but it is involved in the mechanical breakdown of food through mastication and the enzymatic breakdown of carbohydrates by saliva. Saliva contains enzymes like amylase, which begins the digestion of starches. Additionally, the mouth is a crucial site for the absorption of certain medications and nutrients.

Pharmacodynamics

Pharmacodynamics in the context of the mouth involves the interaction of substances, including drugs, with the tissues and secretions in the oral cavity. The pH, enzymatic activity, and presence of mucosal barriers affect drug absorption and efficacy. The oral mucosa has a rich blood supply, which can facilitate rapid systemic absorption of certain medications administered sublingually or buccally.

Pharmacokinetics

Pharmacokinetics related to the mouth involves the absorption, distribution, metabolism, and excretion of drugs administered via the oral route. Drugs can be absorbed through the mucosal membranes in the mouth, leading to rapid onset of action. Factors such as saliva production, the presence of food, and the formulation of the drug (e.g., tablet, liquid) can influence the pharmacokinetic profile.

Pregnancy

The safety of mouth-related medications or treatments during pregnancy varies widely depending on the specific substance or therapy being used. Consult specific guidelines for each drug.

Breast-feeding

The safety of mouth-related medications or treatments during breastfeeding varies depending on the specific substance or therapy. Consult specific guidelines for each drug.

Storage

Store medications related to oral health in a cool, dry place away from direct sunlight, and keep out of reach of children.

Indications

• Preoperative skin preparation
• Wound cleansing
• Hygiene maintenance
• Infection prevention
• Treatment of skin conditions (e.g., acne, dermatitis)

Dosage

Children: Use as directed for the child’s age and condition, ensuring gentle application and rinsing. Consult specific product instructions and guidelines for paediatric use.

Adults: Use as directed, typically involving application of the wash to the affected area, followed by thorough rinsing with water. Consult specific product instructions for detailed use.

Mechanism of action

Washes primarily work by physically removing dirt, debris, and microorganisms from the skin's surface. Antiseptic washes contain active ingredients that can disrupt microbial cell membranes, denature proteins, or interfere with metabolic processes, thus reducing bacterial load.

Pharmacodynamics

The effectiveness of a wash depends on the concentration of the active ingredients, the type of microorganisms present, and the duration of contact. For antiseptic washes, mechanisms may include bactericidal or bacteriostatic effects, depending on the nature of the surfactants or antiseptics used.

Pharmacokinetics

As a topical application, washes have minimal systemic absorption. Their effects are localized, and they work primarily at the site of application. The duration of effect can vary based on the formulation and the presence of residual active ingredients on the skin.

Pregnancy

Safety during pregnancy has not been established. Use with caution and consult a healthcare professional.

Breast-feeding

Consult a healthcare professional before use, as safety during breastfeeding has not been established.

Storage

Store in a cool, dry place away from direct sunlight. Ensure the cap is tightly closed when not in use.

Mechanism of action

Despite being categorized as a non-steroidal anti-inflammatory drug (NSAID), benzydamine demonstrates various mechanisms of action that differ from those of traditional aspirin-like NSAIDs. In particular, benzydamine predominantly acts by inhibiting the synthesis of pro inflammatory cytokines like tumour necrosis factor-alpha (TNF-α) and interleukin-1β (IL-1β) without largely affecting other pro inflammatory cytokines (ie. such as IL-6 and IL-8) or anti-inflammatory cytokines (ie. like IL-10 or IL-1 receptor antagonist). Moreover, benzydamine is largely a weak inhibitor of prostaglandin synthesis as it has been shown to effectively inhibit cyclooxygenase (COX) and lipoxygenase enzyme activity only at concentrations of 1mM or greater. Considering most contemporary usages of benzydamine are topical applications that are generally not well absorbed through the skin and/or non-specialized mucosae, benzydamine does not often achieve the kind of absorption or blood concentrations necessary to cause any extraneous distant systemic effects or COX inhibition, allowing it to localize its action. Additionally, it is also hypothesized that benzydamine is capable of inhibiting the oxidative burst of neutrophils and membrane stabilization. These actions are exhibited by the substance’s ability to inhibit the release of granules from neutrophils and to stabilize lysosomes. Furthermore, benzydamine is capable of a local anaesthetic effect that may be related to its capability for inhibiting the release of inflammatory mediators like substance P and calcitonin gene related peptide from sensory nerve endings. Since substance P is capable of causing the release of histamine from mast cells, benzydamine’s prevention of substance P release further contributes to an anti-inflammatory effect. Benzydamine also demonstrates a non-specific antibacterial activity against various bacterial strains that are resistant to broad-spectrum antibiotics such as ampicillin, chloramphenicol, and tetracycline at concentrations of about 3 mmol/L. Combinatorial use of benzydamine and other antibiotics like tetracycline and chloramphenicol are also synergistic against antibiotic resistant strains of *Staphylococcus aureus* and *Pseudomonas aeruginosa*.

Pharmacodynamics

Benzydamine is a non-steroidal anti-inflammatory drug (NSAID) designed to elicit local anesthetic and analgesic effects mainly for the mouth and throat. It specifically acts on the local mechanisms of inflammation such as pain, oedema, or granuloma. Typically applied topically, the drug demonstrates anti-inflammatory activity reducing oedema as well as exudate and granuloma formation. Moreover, benzydamine exhibits analgesic properties and local anaesthetic activity if pain is caused by an inflammatory condition. Benzydamine can be absorbed into the oral mucosa and intact skin. Once absorbed in the local area of pain or inflammation, benzydamine binds selectively to local inflamed tissues, usually allowing it to act with few adverse systemic effects. On average a period of 2 to 4 hours is necessary for the substance to reach peak plasma concentration. Benzydamine can be synthesized with the reaction of the N-benzyl derivative from methyl anthranilate with nitrous acid to give N-nitoso derivative. This is next reduced by sodium thiosulfate to give transient hydrazine. This hydrazine can then undergo spontaneous internal hydrazide formation. Treating this resultant enolate with 3-chloro-1-dimethylamkino propane ultimately yields benzydamine.