CINOPLUS SUPPOSITORY

Indications

• Bacterial infection in otitis externa

Dosage

Children: Apply 2–3 drops 4–5 times a day, including a dose at bedtime.

Adults: Apply 2–3 drops 4–5 times a day, including a dose at bedtime.

Mechanism of action

Framycetinsulfate exerts its antibacterial effect by inhibiting protein synthesis in bacteria. It binds to the 30S ribosomal subunit, causing misreading of mRNA and ultimately leading to the production of nonfunctional or toxic peptides. This action disrupts bacterial cell function and contributes to cell death.

Pharmacodynamics

Framycetinsulfate is effective against a range of gram-negative and some gram-positive bacteria. Its ability to penetrate bacterial cell walls and interfere with protein synthesis makes it a potent antibacterial agent. However, resistance can develop, particularly with prolonged use.

Pharmacokinetics

When applied topically, framycetinsulfate has limited systemic absorption. Its pharmacokinetic profile is characterized by minimal systemic exposure, which reduces the risk of systemic side effects. The drug is primarily excreted unchanged in urine. Local application leads to high concentrations at the site of infection, which is beneficial for treating localized infections like otitis externa.

Contra-indications

• Perforated tympanic membrane

Adverse effects

• Ototoxicity
• Local irritation
• Allergic reactions

Interactions

• Potential risk of ototoxicity may increase when used with other aminoglycosides

Precautions

• Avoid prolonged use
• Use with caution in patients with mitochondrial mutations

Pregnancy

Framycetin sulfate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult product literature for detailed guidance.

Breast-feeding

Caution is advised when administering framycetin sulfate during breastfeeding. Consult product literature for detailed guidance.

Storage

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

Formulations

• Ear drops containing framycetin sulfate

Indications

• Capillary fragility
• Vascular disorders
• Skin inflammation
• Post-sun exposure treatments

Dosage

Children: Refer to the BNF for Children for specific dosing information as this may vary based on the child's age, weight, and the condition being treated.

Adults: Refer to the BNF for specific dosing information as this may vary based on the formulation and condition being treated.

Mechanism of action

Aesculin primarily acts by improving capillary permeability and reducing fragility, which is crucial for maintaining vascular integrity. It inhibits catabolic enzymes such as hyaluronidase and collagenase, thereby preserving perivascular connective tissue. Additionally, its antioxidant properties protect triglycerides from auto-oxidation, contributing to its anti-inflammatory effects, making it useful for after sun treatments.

Pharmacodynamics

Topical application of Aesculin has been shown to increase capillary density, which refers to the number of capillaries open to blood flow per unit of surface area. This enhancement in capillary morphology supports improved blood circulation and nutrient delivery to tissues, promoting skin health and resilience.

Pharmacokinetics

The pharmacokinetics of Aesculin, particularly in systemic absorption, metabolism, and excretion, are not well-documented in the available literature. However, its topical application suggests localized effects with minimal systemic absorption, which is common for many topical agents. Further research is needed to elucidate its pharmacokinetic profile.

Pregnancy

There is limited data on the safety of Aesculin during pregnancy. Consult a healthcare professional before use.

Breast-feeding

Caution is advised when using Aesculin while breastfeeding due to insufficient data on its excretion in breast milk.

Storage

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

Formulations

• Topical cream
• Gel

Indications

• Adrenal insufficiency
• Allergic reactions
• Asthma
• Rheumatoid arthritis
• Inflammatory bowel disease
• Skin disorders such as eczema and dermatitis

Dosage

Children: Paediatric dosing is highly variable and should be determined based on the specific condition, age, and weight of the child. Refer to the BNF for Children for detailed dosing information.

Adults: Dosage varies based on the condition being treated and the patient's response. Typically, doses may start low and be gradually increased as necessary. For specific dosing recommendations, consult relevant clinical guidelines or resources.

Mechanism of action

Bhydrocortisone exerts its effects by binding to the glucocorticoid receptor, leading to the modulation of gene expression. This interaction results in the inhibition of pro-inflammatory cytokines and the induction of anti-inflammatory proteins. It also affects the metabolism of carbohydrates, proteins, and fats, promoting gluconeogenesis and influencing the distribution of body fat.

Pharmacodynamics

Bhydrocortisone has a broad range of effects on various tissues, including anti-inflammatory, immunosuppressive, and metabolic actions. It decreases the migration of leukocytes to sites of inflammation and stabilizes lysosomal membranes, reducing tissue damage. Additionally, it modulates the immune response, which can be beneficial in treating autoimmune diseases.

Pharmacokinetics

Bhydrocortisone is absorbed well from the gastrointestinal tract, with peak plasma concentrations typically occurring within 1 to 2 hours after oral administration. It is extensively metabolized in the liver, primarily through conjugation, and has a half-life of approximately 8 to 12 hours. The drug is excreted in urine, mainly as metabolites. Factors such as age, liver function, and concomitant medications can influence its pharmacokinetics.

Contra-indications

• Systemic fungal infections
• Hypersensitivity to hydrocortisone or any component of the formulation
• Live vaccines in immunosuppressed patients

Adverse effects

• Increased susceptibility to infections
• Cushing's syndrome
• Gastrointestinal disturbances
• Mood changes
• Insomnia
• Fluid retention
• Hypertension
• Hyperglycemia

Interactions

• Nonsteroidal anti-inflammatory drugs (NSAIDs) may increase the risk of gastrointestinal side effects
• Anticoagulants may have altered effects
• Antidiabetic medications may have reduced efficacy
• Live vaccines may be less effective

Precautions

• Use with caution in patients with diabetes mellitus
• Monitor for signs of infection
• Taper dosage gradually to avoid adrenal insufficiency after long-term use
• Use cautiously in patients with cardiovascular disease

Pregnancy

Hydrocortisone is classified as category C. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Hydrocortisone is excreted in breast milk, thus caution should be exercised when administered to a nursing mother.

Storage

Store at room temperature, away from moisture and heat. Protect from light.

Formulations

• Oral tablets
• Injection
• Topical cream
• Topical ointment

Indications

• Local anesthesia for dental procedures
• Pain relief for minor surgical interventions
• Management of anal fissures and hemorrhoids

Dosage

Children: Refer to the BNF for Children for specific dosing recommendations based on age and weight.

Adults: Refer to established guidelines for local anesthetic administration. Dosage varies based on the procedure and formulation used.

Mechanism of action

Cinchocain exerts its anesthetic effect by blocking voltage-gated sodium channels in the neuronal cell membrane. This inhibition prevents the influx of sodium ions during the depolarization phase of action potentials, thereby reducing neuronal excitability and conduction of nerve impulses. As a result, the transmission of pain signals to the central nervous system is interrupted.

Pharmacodynamics

The pharmacodynamic properties of cinchocain involve its potency as a local anesthetic, which is determined by its chemical structure and affinity for sodium channels. The onset of action is relatively rapid, and the duration of anesthetic effect can vary based on the formulation and site of administration. The drug is effective in providing short-term analgesia and is often used in combination with other agents to enhance anesthetic efficacy.

Pharmacokinetics

Cinchocain is absorbed at the site of administration, with the rate of absorption influenced by factors such as the formulation and local blood flow. It undergoes hydrolysis primarily in the liver, where it is metabolized to inactive metabolites. The elimination half-life can vary, but the drug is generally excreted in urine. Due to its potential for systemic absorption, careful consideration of dosing and administration technique is necessary to minimize the risk of systemic toxicity.

Contra-indications

• Hypersensitivity to cinchocain or any of its components
• Severe liver disease
• Severe heart block
• Myasthenia gravis

Adverse effects

• Local skin reactions
• Systemic allergic reactions
• Cardiovascular effects such as arrhythmias
• CNS effects including dizziness, tremors, and seizures
• Hypotension

Interactions

• Other local anesthetics may increase the risk of toxicity
• Beta-blockers may enhance the cardiovascular effects
• Drugs that affect liver enzymes may alter cinchocain metabolism

Precautions

• Use with caution in patients with cardiac conditions
• Monitor for signs of systemic toxicity
• Avoid use in areas with compromised blood supply
• Caution in patients with renal impairment

Pregnancy

Use only if the potential benefit justifies the potential risk to the fetus. Limited data available.

Breast-feeding

Cinchocain should be used with caution during breastfeeding due to limited data on excretion in breast milk.

Storage

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

Formulations

• Topical cream
• Injection solution

Indications

• Bacterial conjunctivitis
• Other bacterial eye infections

Dosage

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

Adults: Refer to the BNF for specific dosing information.

Mechanism of action

Framycetin binds to specific proteins within the 30S ribosomal subunit and to 16S rRNA, specifically targeting four nucleotides of the rRNA and a single amino acid of protein S12. This binding interferes with the decoding site near nucleotide 1400 in 16S rRNA, leading to misreading of mRNA. Consequently, incorrect amino acids are incorporated into the polypeptide chains, resulting in nonfunctional or toxic peptides and the disintegration of polysomes into nonfunctional monosomes. This mechanism ultimately leads to the bactericidal effect characteristic of aminoglycoside antibiotics.

Pharmacodynamics

Framycetin effectively treats bacterial infections by inhibiting protein synthesis in susceptible bacteria. It primarily targets aerobic bacteria and is not effective against anaerobic bacteria or non-bacterial pathogens. The drug has a bactericidal effect, suppressing the growth and survival of bacteria, which is critical in treating infections such as conjunctivitis and other bacterial eye conditions.

Pharmacokinetics

Framycetin's pharmacokinetic profile, including absorption, distribution, metabolism, and excretion specifics, is not extensively detailed in the provided data. However, as with other aminoglycosides, it is generally understood that these drugs can have significant renal excretion and may require monitoring in patients with renal impairment. The duration of activity can extend from 48 to 72 hours following administration.

Adverse effects

• Ocular irritation
• Allergic reactions
• Contact dermatitis
• Local discomfort

Precautions

• Use with caution in patients with known hypersensitivity to aminoglycosides
• Avoid prolonged use to minimize the risk of developing antibiotic resistance
• Monitor for signs of local irritation or sensitivity

Pregnancy

Framycetin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult a healthcare provider for guidance.

Breast-feeding

Framycetin may be excreted in breast milk. Caution is advised when administering to nursing mothers.

Storage

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

Formulations

• Eye drops
• Ointment
• Cream

Mechanism of action

The main activities of Esculine focus on capillary protection, as it improves capillary permeability and fragility. It is reported to inhibit catabolic enzymes such as hyaluronidase and collagenase, thus preserving the integrity of the perivascular connective tissue. Esculine also showed good antioxidant properties, protecting triglycerides against auto-oxidation at high temperatures . The antioxidant property might as well explain some of the anti-inflammatory activity of the product, making it a suitable product for after sun treatments, for example.

Pharmacodynamics

Topically applied Esculine increases the “capillary density” (the number of capillaries open to flow per surface unit) and improves the morphological aspect of the smallest blood vessels.

Mechanism of action

Framycetin binds to specific 30S-subunit proteins and 16S rRNA, four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes. Like other aminoglycoside antibiotic drugs, neomycin inhibits bacterial ribosomes by binding to the 30S ribosomal subunit of susceptible bacteria and disrupting the translational machinery of bacterial protein synthesis. Bacterial translation is normally initiated by the mRNA binding to the 30S ribosomal subunit and subsequent binding with 50S subunit for elongation. Aminoglycosides are usually bactericidal in action. Although the exact mechanism of action has not been fully elucidated, the drugs appear to inhibit protein synthesis in susceptible bacteria by irreversibly binding to 30S ribosomal subunits. /Aminoglycosides/ A class of angiogenesis inhibitor has emerged from our mechanistic study of the action of angiogenin, a potent angiogenic factor. Neomycin, an aminoglycoside antibiotic, inhibits nuclear translocation of human angiogenin in human endothelial cells, an essential step for angiogenin-induced angiogenesis. The phospholipase C-inhibiting activity of neomycin appears to be involved, because U-73122, another phospholipase C inhibitor, has a similar effect. In contrast, genistein, oxophenylarsine, and staurosporine, inhibitors of tyrosine kinase, phosphotyrosine phosphatase, and protein kinase C, respectively, do not inhibit nuclear translocation of angiogenin. Neomycin inhibits angiogenin-induced proliferation of human endothelial cells in a dose-dependent manner. At 50 microM, neomycin abolishes angiogenin-induced proliferation but does not affect the basal level of proliferation and cell viability. Other aminoglycoside antibiotics, including gentamicin, streptomycin, kanamycin, amikacin, and paromomycin, have no effect on angiogenin-induced cell proliferation. Most importantly, neomycin completely inhibits angiogenin-induced angiogenesis in the chicken chorioallantoic membrane at a dose as low as 20 ng per egg. These results suggest that neomycin and its analogs are a class of agents that may be developed for anti-angiogenin therapy. ... Aminoglycosides are aminocyclitols that kill bacteria by inhibiting protein synthesis as they bind to the 16S rRNA and by disrupting the integrity of bacterial cell membrane. Aminoglycoside resistance mechanisms include: (a) the deactivation of aminoglycosides by N-acetylation, adenylylation or O-phosphorylation, (b) the reduction of the intracellular concentration of aminoglycosides by changes in outer membrane permeability, decreased inner membrane transport, active efflux, and drug trapping, (c) the alteration of the 30S ribosomal subunit target by mutation, and (d) methylation of the aminoglycoside binding site. ... /Aminoglycosides/

Pharmacodynamics

Framycetin is used for the treatment of bacterial eye infections such as conjunctivitis. Framycetin is an antibiotic. It is not active against fungi, viruses and most kinds of anaerobic bacteria. Framycetin works by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Framycetin is useful primarily in infections involving aerobic bacteria bacteria. Neomycin mediates its bactericidal action by inhibiting bacterial protein synthesis, thereby suppressing the growth and survival of susceptible bacteria. Following oral administration, the duration of bactericidal activity of neomycin ranged from 48 to 72 hours. By decreasing colonic bacteria that produce ammonia, neomycin was shown to be effective as an adjunctive therapy in hepatic coma to improve neurologic symptoms. Neomycin is active against both gram positive and gram negative organisms, including the major _E. coli_ species resident in the colon as well as the enteropathogenic forms of _E. coli_. It is also active against _Klebsiella_-_Enterobacter_ group. Resistant strains of _E. coli_, _Klebsiella_ and _Proteus spp_. may emerge from neomycin therapy. Neomycin has no antifungal activity and has some activity against some protozoa.