Cefadroxil Properties and Uses

Cephalosporins

• Cefadroxil monohydrate: white or almost white powder, slightly soluble in water and sparingly soluble in ethanol.
• Antibacterial spectrum of action and therapeutic indications similar to those of cephalexin and cephradine.
• D-p-hydroxyphenylglycyl isomer is more active than the L-isomer.
• Assayed by adopting liquid chromatography technique.
• Dosage forms: cefadroxil capsules, oral suspension, and tablets.

Cefaclor

• White or slightly yellow powder, slightly soluble in water, and practically insoluble in methanol and methylene chloride.
• Has a chloro group at C-3 position, making it stable in acid and achieving sufficient oral absorption.
• Used in treating upper respiratory tract infections caused by Streptococcus pneumoniae and Haemophilus influenzae.
• Dose: 250-500 mg every 8 hours orally for adults.
• Assayed by adopting liquid chromatography technique.
• Dosage forms: cefaclor capsules, oral suspension, and prolonged-release tablets.

Cefamandole

• White powder, soluble in water, and sparingly soluble in methanol.
• First compound of second-generation cephalosporin marketed in the United States.
• Unstable in solution and hydrolyzes rapidly to release cefamandole and formate.
• Dose: 0.5-2 g every 4-6 hours IV.
• Also available as injection in strengths of 0.5 and 1 mg/10ml.

Cefotaxime Sodium

• White solid, soluble in water, and exhibits broad-spectrum activity against both gram-positive and gram-negative bacteria.
• Used in treating genitourinary infections and lower respiratory infections.

Degradation of Cephalosporins

• In strong acid solutions
• In the presence of β-lactamase
• In the presence of acylase

Anti-TB Drugs

• Tuberculosis is a leading infectious disease worldwide, caused by Mycobacterium tuberculosis.
• Common infection sites: lungs, brain, bone, liver, and kidney.
• Main symptoms: cough, tachycardia, cyanosis, and respiratory failure.
• Classified into: pulmonary tuberculosis, genitourinary tuberculosis, tuberculous meningitis, and miliary tuberculosis.

First-Line Anti-TB Drugs

• Isoniazid
• Streptomycin
• Rifampicin
• Ethambutol
• Pyrazinamide

Isoniazid

• Prodrug activated by katG enzyme on the surface of M. tuberculosis to isonicotinic acid.
• Inhibits bacterial cell wall mycolic acid, making M. tuberculosis susceptible to reactive oxygen radicals.
• May be bacteriostatic or bactericidal in action, depending on the concentration and susceptibility of the infecting organism.
• Active against susceptible bacteria only during bacterial cell division.

Pyrazinamide

• Prodrug activated by M. tuberculosis amidase enzyme into pyrazine carboxylic acid.
• Has bactericidal activity, especially in the low pH environment that exists in macrophages.
• Used to treat tuberculosis and meningitis.
• Should be used with caution in patients with hyperuricemia or gout.

Diuretics

• Classified into: thiazide diuretics, loop diuretics, potassium-sparing diuretics, osmotic diuretics, and carbonic anhydrase inhibitors.
• Thiazide diuretics: hydrochlorothiazide, chlorthalidone; used in hypertension, edema, and nephrolithiasis.
• Loop diuretics: furosemide, bumetanide, torsemide; used in heart failure, edema, and hypertension.
• Potassium-sparing diuretics: spironolactone, eplerenone, amiloride, triamterene; used in hypertension, heart failure, and edema.
• Osmotic diuretics: mannitol, glycerol; used in intracranial hypertension, cerebral edema, and acute kidney injury.
• Carbonic anhydrase inhibitors: acetazolamide, dorzolamide; used in glaucoma, altitude sickness, and metabolic alkalosis.

Monitoring Tests

• Electrolyte levels: diuretics can affect electrolyte balance, leading to abnormalities such as hypokalemia, hyponatremia, and hypomagnesemia.
• Regular monitoring of electrolyte levels, including potassium, sodium, and magnesium, is crucial.
• Renal function tests: diuretics can impact renal function, particularly in patients with preexisting kidney disease.
• Monitoring tests such as serum creatinine and blood urea nitrogen (BUN) can help assess renal function and detect any deterioration.