CEFARIX-250

Indications

• Bacterial infections due to sensitive Gram-positive and Gram-negative bacteria
• Skin infections
• Soft-tissue infections
• Uncomplicated urinary-tract infections
• Acute diverticulitis (in combination with metronidazole)
• Prophylaxis of recurrent urinary-tract infections

Dosage

Children: Child 1 month–11 years: 25 mg/kg 2–4 times a day (max. per dose 500 mg). Child

Adults: 250 mg every 6 hours, alternatively 500 mg every 8–12 hours; increased to 1–1.5 g every 6–8 hours for severe infections.

Mechanism of action

Cefalexin inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins located in the bacterial cytoplasmic membrane. This action prevents the cross-linkage of peptidoglycan chains, which is essential for bacterial cell wall strength and rigidity. Consequently, this leads to cell lysis and death, particularly in rapidly dividing bacteria.

Pharmacodynamics

Cefalexin is bactericidal and exhibits activity primarily against Gram-positive bacteria. It is effective in treating superficial infections resulting from minor wounds or lacerations. By interfering with the cross-linking reaction between N-acetyl muramic acid and N-acetylglucosamine in the bacterial cell wall, cefalexin promotes cell lysis, making it a widely used antibiotic in clinical practice.

Pharmacokinetics

Cefalexin is well absorbed when taken orally, with peak plasma concentrations typically occurring within 1 hour of administration. It is widely distributed throughout body tissues and fluids, including bile, urine, and synovial fluid. The drug is primarily excreted unchanged in the urine, and its half-life is approximately 1 hour. Renal impairment may necessitate dosage adjustments.

Contra-indications

• Hypersensitivity to cephalosporins
• History of immediate hypersensitivity to penicillin and other beta-lactams

Adverse effects

• Abdominal pain
• Diarrhoea
• Dizziness
• Eosinophilia
• Headache
• Leucopenia
• Nausea
• Neutropenia
• Pseudomembranous enterocolitis
• Skin reactions
• Thrombocytopenia
• Vomiting
• Vulvovaginal candidiasis
• Anaphylactic reaction
• Angioedema
• Agranulocytosis
• Hemolytic anemia
• Tubulointerstitial nephritis
• Severe cutaneous adverse reactions (SCARs)

Interactions

• Probenecid may increase the serum concentration of cephalexin
• Antacids may decrease the absorption of cephalexin
• Other nephrotoxic drugs may increase the risk of kidney damage

Precautions

• Use with caution in patients with renal impairment
• Monitor for signs of superinfection during prolonged therapy
• Caution in patients with a history of gastrointestinal disease, particularly colitis

Pregnancy

Not known to be harmful.

Breast-feeding

Present in milk in low concentration, but generally considered appropriate to use.

Storage

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

Formulations

• Capsules: 250 mg, 500 mg
• Oral suspension: 125 mg/5 mL, 250 mg/5 mL

Indications

• Constipation
• Dietary fiber supplementation
• Irritable bowel syndrome
• Diverticular disease
• Weight management

Dosage

Children: Refer to appropriate guidelines for specific dosage; generally taken with adequate fluid intake.

Adults: Refer to appropriate guidelines for specific dosage; generally taken with adequate fluid intake.

Mechanism of action

Cellulose acts primarily as a bulk-forming laxative. It absorbs water in the intestines, which increases stool bulk and stimulates peristalsis, thus facilitating bowel movements. Additionally, cellulose is not digestible by human enzymes, leading to fermentation by gut bacteria, which may enhance gut health and alter gut microbiota composition.

Pharmacodynamics

Cellulose increases stool weight and frequency of bowel movements. It works by retaining water in the intestines, leading to softer stools and improved passage through the gastrointestinal tract. The bulking effect of cellulose can help alleviate constipation and promote overall digestive health. It may also play a role in cholesterol reduction and glycemic control through its effects on digestion and absorption of nutrients.

Pharmacokinetics

Cellulose is not absorbed into the bloodstream due to its indigestible nature. Instead, it passes through the gastrointestinal tract, where it adds bulk to the stool. Its fermentation by colonic bacteria produces short-chain fatty acids, which may have beneficial effects on colon health. The onset of action for cellulose as a laxative can vary but is generally within 24 to 72 hours after ingestion.

Adverse effects

• Bloating
• Flatulence
• Diarrhea
• Abdominal discomfort

Precautions

• Use with caution in patients with a history of gastrointestinal disorders.
• Monitor for potential allergic reactions in sensitive individuals.

Pregnancy

Cellulose is generally considered safe during pregnancy as it is a non-toxic, indigestible fiber.

Breast-feeding

Cellulose is also considered safe during breastfeeding; it is excreted in breast milk in negligible amounts.

Storage

Store in a cool, dry place away from direct sunlight.

Formulations

• Powder
• Capsules
• Tablets
• Granules

Indications

• Used as an excipient in tablet formulations
• Used as a bulking agent in capsule formulations
• Used in food products as a thickener or stabilizer

Dosage

Children: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.

Adults: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.

Mechanism of action

Microcrystalline cellulose acts as a non-digestible filler that enhances the flow properties of powders during the manufacturing of tablets and capsules. It does not have a direct pharmacological action on the body but ensures that the active ingredients are effectively delivered to the patient.

Pharmacodynamics

As a non-active ingredient, microcrystalline cellulose does not exert pharmacodynamic effects typical of active pharmaceutical ingredients. Its primary role is to provide a stable and consistent matrix for the drug, facilitating the release of the active compound once ingested.

Pharmacokinetics

Microcrystalline cellulose is not absorbed in the gastrointestinal tract; it passes through the digestive system largely unchanged. It adds bulk to the stool, which may aid in promoting regular bowel movements. The substance is excreted in feces, where it contributes to dietary fiber intake.

Pregnancy

Data regarding the use of microcrystalline cellulose during pregnancy is limited. It is advisable to consult with healthcare professionals before use.

Breast-feeding

Microcrystalline cellulose is considered safe during breastfeeding, as it is not absorbed systemically.

Storage

Store in a cool, dry place away from direct sunlight and moisture.

Dosage

Children: Refer to the specific drug's prescribing information for paediatric dosing guidelines.

Adults: Refer to the specific drug's prescribing information for adult dosing guidelines.

Mechanism of action

The mechanism of action would depend on the specific drug referred to by 'size'. Generally, drugs exert their effects through interaction with biological targets such as receptors, enzymes, or ion channels, leading to a physiological response.

Pharmacodynamics

Pharmacodynamics refers to the effects of the drug on the body, including the relationship between drug concentration and effect. This can involve receptor binding, signal transduction, and the resulting biological effects. Specific dynamics would vary based on the drug in question.

Pharmacokinetics

Pharmacokinetics describes the absorption, distribution, metabolism, and excretion (ADME) of a drug. Factors such as bioavailability, volume of distribution, half-life, and clearance would vary significantly based on the specific drug being considered.

Pregnancy

Safety in pregnancy has not been established. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Use with caution, as it is not known whether it is excreted in human milk.

Storage

Store in a cool, dry place away from direct sunlight.

Mechanism of action

Cephalexin is a first generation cephalosporin antibiotic. Cephalosporins contain a beta lactam and dihydrothiazide. Unlike penicillins, cephalosprins are more resistant to the action of beta lactamase. Cephalexin inhibits bacterial cell wall synthesis, leading breakdown and eventualy cell death. CEPHALOTHIN & ITS CONGENERS INHIBIT BACTERIAL CELL-WALL SYNTHESIS IN MANNER SIMILAR TO THAT OF PENICILLIN. /CEPHALOSPORINS/ The penicillins and their metabolites are potent immunogens because of their ability to combine with proteins and act as haptens for acute antibody-mediated reactions. The most frequent (about 95 percent) or "major" determinant of penicillin allergy is the penicilloyl determinant produced by opening the beta-lactam ring of the penicillin. This allows linkage of the penicillin to protein at the amide group. "Minor" determinants (less frequent) are the other metabolites formed, including native penicillin and penicilloic acids. /Penicillins/ Bactericidal; action depends on ability to reach and bind penicillin-binding proteins located in bacterial cytoplasmic membranes; cephalosporins inhibit bacterial septum and cell wall synthesis, probably by acylation of membrane-bound transpeptidase enzymes. This prevents cross-linkage of peptidoglycan chains, which is necessary for bacterial cell wall strength and rigidity. Also, cell division and growth are inhibited, and lysis and elongation of susceptible bacteria frequently occur. Rapidly dividing bacteria are those most susceptible to the action of cephalosporins. /Cephalosporins/ CEPHALOSPORIN C IS VERY RESISTANT TO ACTION OF PENICILLINASE, FOR WHICH IT IS BOTH COMPETITIVE & NONCOMPETITIVE INHIBITOR, DEPENDING ON SUBSTRATE TESTED... /CEPHALOSPORINS/

Pharmacodynamics

Cephalexin (also called Cefalexin) is a first generation cephalosporin antibiotic. It is one of the most widely prescribed antibiotics, often used for the treatment of superficial infections that result as complications of minor wounds or lacerations. It is effective against most gram-positive bacteria through its inihibition of the cross linking reaction between N-acetyl muramicacid and N-acetylglucosamine in the cell wall, leading to cell lysis.