CEFO-L DRY SYRUP

Indications

• Bacterial infections due to sensitive Gram-positive and Gram-negative bacteria
• Surgical prophylaxis
• Haemophilus influenzae epiglottitis
• Acute infections
• Meningitis (emergency treatment)
• Uncomplicated gonorrhoea
• Disseminated gonococcal infection

Dosage

Children: In children aged 1 month to 11 years

Adults: For adults, the typical dosage is 1 g every 12 hours for severe infections, or 400 mg for a single dose in cases of uncomplicated gonorrhoea.

Mechanism of action

Cefixime binds to penicillin-binding proteins (PBPs) located in the bacterial cell wall. This binding inhibits the transpeptidase activity essential for peptidoglycan cross-linking, thereby disrupting cell wall synthesis and integrity, which ultimately leads to bacterial cell lysis, especially in rapidly growing bacteria.

Pharmacodynamics

Cefixime exhibits bactericidal activity by preventing the final stages of bacterial cell wall synthesis. It is stable against certain beta-lactamases, making it effective against some resistant bacterial strains. The drug can cause hypersensitivity reactions and is associated with a risk of Clostridium difficile-associated diarrhea. It may also lead to a decrease in prothrombin activity, necessitating caution in susceptible populations.

Pharmacokinetics

Cefixime is well-absorbed after oral administration, with a bioavailability of approximately 40-50%. Peak plasma concentrations occur within 2-6 hours post-dose. It is widely distributed in body tissues and fluids, including urine. The drug is primarily eliminated via the kidneys, with dose adjustments required in patients with renal impairment. Cefixime has a half-life of about 3-4 hours, necessitating multiple doses for sustained therapeutic effect.

Contra-indications

• Hypersensitivity to cefixime or other cephalosporins
• Severe renal impairment

Adverse effects

• Acute kidney injury
• Arthralgia
• Drug fever
• Dyspepsia
• Dyspnoea
• Edema
• Flatulence
• Genital pruritus
• Hypereosinophilia
• Jaundice
• Serum sickness-like reaction
• Thrombocytosis

Interactions

• Probenecid may increase cefixime levels
• Cephalosporins may interact with anticoagulants and increase bleeding risk
• Certain antibiotics may have additive effects

Precautions

• Caution in patients with a history of gastrointestinal disease, particularly colitis
• Monitor renal function in patients with renal impairment
• Use with caution in patients on dialysis

Pregnancy

Not known to be harmful.

Breast-feeding

Present in milk in low concentrations; use with caution.

Storage

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

Formulations

• Oral tablets
• Injection (intravenous and intramuscular)

Indications

• Bladder cancer
• Tuberculosis vaccination

Dosage

Children: Refer to the BNF for Children for appropriate dosing based on indication.

Adults: Refer to specific guidelines based on indication. For bladder cancer, a common regimen is instillation once a week for six weeks.

Mechanism of action

BCG works by stimulating the immune system, particularly through the activation of T-cells and macrophages. It enhances the immune response against tumor cells and Mycobacterium tuberculosis, promoting the release of cytokines and other immune mediators that contribute to the destruction of cancerous cells and pathogens.

Pharmacodynamics

The pharmacodynamics of BCG involve the induction of a robust immune response characterized by the activation of both innate and adaptive immunity. This includes the proliferation of T-lymphocytes and the production of cytokines such as tumor necrosis factor-alpha (TNF-alpha) and interleukins, leading to increased immune surveillance and anti-tumor activity. The effectiveness of BCG is influenced by factors such as the host's immune status and the presence of any concurrent infections.

Pharmacokinetics

BCG is administered locally, and its pharmacokinetics are determined by the route of administration. After intravesical administration, BCG remains in the bladder and exerts its effects locally, with minimal systemic absorption. The half-life and clearance of BCG can vary based on the patient's immune response and presence of any concurrent conditions.

Interactions

• normal immunoglobulin + bacillus calmette-gurin vaccine: Unknown (decreases efficacy)

Pregnancy

Bacillus Calmette-Guérin (BCG) vaccine can be administered during pregnancy if the potential benefit outweighs the potential risk.

Breast-feeding

BCG vaccine may be administered during breastfeeding; however, caution is advised.

Storage

Store at 2-8 degrees Celsius. Do not freeze.

Formulations

• Bacillus Calmette-Guérin vaccine

Indications

• Metabolic acidosis
• Lactic acidosis
• Support in shock or severe dehydration
• Exercise physiology research

Dosage

Children: Refer to clinical guidelines for specific dosing recommendations based on the clinical condition being treated.

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

Mechanism of action

Lactic acid primarily functions by contributing to the acid-base balance in the body. It can serve as a substrate for gluconeogenesis in the liver and is utilized in the Cori cycle, where it is converted back to glucose. Furthermore, lactic acid can act as a signaling molecule in various physiological processes, influencing metabolism and cellular responses during hypoxic conditions.

Pharmacodynamics

Lactic acid dissociates into lactate and hydrogen ions in solution, which can lead to a decrease in pH (acidosis) when produced in excess. Its accumulation in the body is indicative of anaerobic metabolism, often observed during intense exercise or in conditions of oxygen deprivation. The body can buffer the effects of lactic acid through bicarbonate and other mechanisms, maintaining homeostasis.

Pharmacokinetics

Lactic acid is rapidly absorbed and distributed throughout the body. It is metabolized primarily in the liver, where it can be converted to glucose or further metabolized to carbon dioxide and water. The elimination half-life of lactate varies depending on the metabolic state of the individual and the presence of underlying conditions. Renal function also plays a role in the clearance of lactate from the body.

Adverse effects

• Nausea
• Vomiting
• Abdominal pain
• Diarrhea
• Hypersensitivity reactions

Precautions

• Use with caution in patients with renal impairment
• Monitor for signs of metabolic acidosis
• Caution in patients with liver disease

Pregnancy

Lactic acid is generally regarded as safe, but clinical use should be evaluated on a case-by-case basis during pregnancy.

Breast-feeding

Considered safe for use during breastfeeding, but consult healthcare provider for individual cases.

Storage

Store at room temperature, away from direct sunlight and moisture.

Formulations

• Lactic acid injection
• Lactic acid oral solution

Indications

• Heart failure
• Hypertension
• Mitochondrial disorders
• Neurodegenerative diseases
• Statin-associated myopathy

Dosage

Children: Refer to specific dosing guidelines in clinical literature or pharmacological references.

Adults: Refer to specific dosing guidelines in clinical literature or pharmacological references.

Mechanism of action

Coenzyme Q10 acts as an electron carrier in the mitochondrial electron transport chain, facilitating ATP synthesis. It also exhibits antioxidant properties by scavenging free radicals and regenerating other antioxidants, thus protecting cellular components from oxidative damage. Its involvement in maintaining mitochondrial membrane potential is critical for energy production.

Pharmacodynamics

Coenzyme Q10 enhances energy production in cells, particularly in tissues with high energy demands, such as the heart and skeletal muscles. Its antioxidant action helps reduce oxidative stress, which is implicated in various pathological conditions, including cardiovascular diseases and aging. Clinical studies suggest that it may improve cardiac function and exercise tolerance in patients with heart failure and may have a positive effect on blood pressure.

Pharmacokinetics

Coenzyme Q10 is absorbed in the gastrointestinal tract, with bioavailability influenced by its formulation (solubility and presence of fats). Peak plasma concentrations are typically reached within 6 to 8 hours post-ingestion. It is metabolized in the liver and has a half-life of around 33 hours. Coenzyme Q10 is excreted primarily in the bile and urine. Its absorption can be enhanced when taken with meals that contain fat.

Pregnancy

Consult healthcare provider for risks versus benefits.

Breast-feeding

Consult healthcare provider for risks versus benefits.

Storage

Store in a cool, dry place away from light.

Indications

• Bacterial infections
• Probiotics
• Biodefense
• Food preservation
• Fermentation processes

Dosage

Children: Paediatric dosing varies widely based on the condition being treated and the specific spore type. Refer to paediatric guidelines for

Adults: Dosage depends on the specific clinical context and the organism involved. Refer to appropriate clinical guidelines for specific dosing information.

Mechanism of action

Bacterial spores, such as those from Bacillus anthracis, can form endospores that are highly resistant to heat, desiccation, and chemical agents. Upon exposure to favorable conditions, these spores can germinate into vegetative cells, leading to infection. In contrast, fungal spores can germinate and develop into mycelium, contributing to the organism's growth and reproduction. The germination process involves the breakdown of the spore coat, hydration, and metabolic activation of the dormant spore.

Pharmacodynamics

The pharmacodynamics of spores largely depend on the type of spores and the context of their use. For instance, Bacillus spores can produce toxins that contribute to pathogenicity upon germination. In probiotics, certain spores are utilized for their beneficial effects on gut health, such as enhancing the immune response and outcompeting harmful bacteria. The effects can be dose-dependent and vary with the strain and formulation used.

Pharmacokinetics

Spores do not follow traditional pharmacokinetic profiles, as they are not absorbed or distributed in the body in the same way as conventional drugs. In the case of bacterial spores, their resistance to environmental stresses allows them to survive passage through the gastrointestinal tract. Upon reaching a suitable environment, they can germinate and produce active bacteria. For probiotic spores, the efficacy can be influenced by the formulation, including the presence of prebiotics and the delivery mechanism.

Pregnancy

The safety of spores during pregnancy is not well established. Caution is advised.

Breast-feeding

Data on the excretion of spores in breast milk is limited. Use with caution while breastfeeding.

Storage

Store in a cool, dry place away from direct sunlight. Ensure that the container is sealed tightly.

Mechanism of action

The bacterial cell wall, which is located at the periphery of Gram-positive bacteria and within the periplasm of Gram-negative bacteria, comprises a glycopeptide polymer synthesized through cross-linking of glycans to peptide stems on alternating saccharides, which is known commonly as peptidoglycan. Cell wall formation, recycling, and remodelling require numerous enzymes, including a family of enzymes with similar active site character despite distinct and sometimes overlapping roles as carboxypeptidases, endopeptidases, transpeptidases, and transglycosylases, known as "penicillin-binding proteins" (PBPs). The number of PBPs differs between bacteria, in which some are considered essential and others redundant. In general, inhibition of one or more essential PBPs results in impaired cell wall homeostasis, loss of cell integrity, and is ultimately bactericidal. Cefixime is a cephalosporin and cephalosporins work by using their beta-lactam rings to inhibit bacterial cell wall synthesis by binding to the penicillin-binding proteins transpeptidases on bacteria. The inhibition of synthesis of the bacteria cell wall will cause lysis, particularly in fast growing organisms such as bacteria. Specifically, cephalosporins inhibit penicillin-sensitive enzymes responsible for the final 3D structure of the bacterial cell wall which in turn inhibit bacterial cell wall peptidoglycan synthesis.

Pharmacodynamics

Cefixime, a broad-spectrum antibiotic, is an orally-active third-generation semisynthetic cephalosporin. Like other cephalosporins, the antibacterial action of cefixime results from inhibition of cell wall synthesis. Also like other cephalosporins, cefixime is stable when in the presence of certain beta-lactamase enzymes, which means certain organisms resistant to penicillins and some cephalosporins due to the presence of beta-lactamases could be susceptible to cefixime. Use of cefixime can result in hypersensitivity reactions including anaphylactic/anaphylactoid reactions and _Clostridium difficile_-associated diarrhea (CDAD); it may also be associated with a fall in prothrombin activity. Cefixime doses should be adjusted for patients that have renal impairment and patients undergoing continuous ambulatory peritoneal dialysis (CAPD) and hemodialysis (HD), while patients on dialysis should be monitored while taking cefixime.