Cefadroxil Properties and Uses
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Cefadroxil Properties and Uses

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Questions and Answers

What is the effect of replacing sulphur with a methylene group in cephalosporins?

It increases chemical stability and half-life.

What is the significance of the olefinic linkage at C-3 and C-4 positions in cephalosporins?

It is essential for antibacterial activity.

What is the effect of strong acid solutions on cephalosporins?

They degrade cephalosporins.

Which of the following is NOT a first-line drug used in the treatment of tuberculosis?

<p>Ethionamide</p> Signup and view all the answers

What is the estimated number of people infected with Mycobacterium tuberculosis worldwide?

<p>2 billion</p> Signup and view all the answers

What is the primary site of infection in tuberculosis?

<p>Lungs</p> Signup and view all the answers

What is the category of tuberculosis that affects the respiratory tract?

<p>Pulmonary tuberculosis</p> Signup and view all the answers

What is the effect of β-lactamase on cephalosporins?

<p>It degrades cephalosporins.</p> Signup and view all the answers

What is the solubility of cefadroxil monohydrate in water?

<p>Slightly soluble</p> Signup and view all the answers

What is the difference between the D-p-hydroxyphenylglycyl isomer and the L-isomer of cefadroxil?

<p>The D-isomer is much more active than the L-isomer</p> Signup and view all the answers

What is the technique used to assay cefadroxil?

<p>Liquid chromatography</p> Signup and view all the answers

What is the characteristic of cefaclor that makes it stable in acid?

<p>The presence of a chloro group at C-3 position</p> Signup and view all the answers

What is the dose of cefaclor for adults?

<p>250-500 mg every 8 h</p> Signup and view all the answers

What is the characteristic of cefamandole nafate solutions?

<p>They are unstable in solution and hydrolyze rapidly</p> Signup and view all the answers

What is the IV dose of cefamandole?

<p>0.5-2 g every 4 to 6 h</p> Signup and view all the answers

What is the enzyme responsible for activating isoniazid on the surface of M.tuberculosis?

<p>KatG enzyme</p> Signup and view all the answers

What is the effect of replacing 6-Cl by electron-donating groups on diuretic activity?

<p>Reduces diuretic activity</p> Signup and view all the answers

What is the characteristic of cefotaxime sodium?

<p>It is soluble in water and exhibits broad-spectrum activity</p> Signup and view all the answers

What is the mechanism of action of isoniazid against M.tuberculosis?

<p>Inhibits bacterial cell wall mycolic acid</p> Signup and view all the answers

What is the result of saturating the thiadiazine ring to give a 3, 4-dihydro derivative?

<p>Little or no diuretic activity</p> Signup and view all the answers

What is the effect of pyrazinamide on M.tuberculosis?

<p>Bactericidal</p> Signup and view all the answers

What is the starting material for the synthesis of bendroflumethiazide?

<p>Phenylacetaldehyde</p> Signup and view all the answers

What is the optimal environment for the activity of pyrazinamide?

<p>Low pH environment</p> Signup and view all the answers

What is the indication for pyrazinamide therapy?

<p>Tuberculosis and meningitis</p> Signup and view all the answers

What is the role of ammonia solution in the synthesis of bendroflumethiazide?

<p>Solvent</p> Signup and view all the answers

What is the metabolic pathway of pyrazinamide?

<p>Hydrolysis by hepatic microsomal pyrazinamidase</p> Signup and view all the answers

Which diuretic is used to treat hypertension and heart failure, and is associated with a risk of hypokalemia?

<p>Hydrochlorothiazide</p> Signup and view all the answers

Which of the following diuretics is used to treat edema associated with liver cirrhosis?

<p>Furosemide</p> Signup and view all the answers

What is the precaution for using pyrazinamide in patients with hyperuricaemia or gout?

<p>Use with caution</p> Signup and view all the answers

What is the status of pyrazinamide in the short-term treatment of tuberculosis regimens?

<p>First-line status</p> Signup and view all the answers

Which of the following diuretics is used to treat glaucoma?

<p>Acetazolamide</p> Signup and view all the answers

What is the group replaced or removed at position C-7 to yield compounds with little or no diuretic activity?

<p>Sulfonamide group</p> Signup and view all the answers

Which of the following laboratory tests is used to monitor renal function in patients taking diuretics?

<p>Serum creatinine</p> Signup and view all the answers

What is the name of the compound synthesized from 2, 4-Disulphamoyl-5-trifluoromethylaniline and phenylacetaldehyde?

<p>Bendroflumethiazide</p> Signup and view all the answers

Which combination diuretic is used to treat hypertension and heart failure?

<p>Hydrochlorothiazide/triamterene</p> Signup and view all the answers

What is a potential complication of diuretic therapy that can be monitored by electrolyte levels?

<p>Hypokalemia</p> Signup and view all the answers

Which of the following diuretics is used to treat primary aldosteronism?

<p>Spironolactone</p> Signup and view all the answers

Which diuretic is used to treat acute kidney injury?

<p>Mannitol</p> Signup and view all the answers

Study Notes

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.

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Description

This quiz covers the properties and uses of cefadroxil, a type of antibiotic. Learn about its solubility, antibacterial spectrum, and therapeutic indications. Also, explore its assay and dosage forms.

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