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 has a variable effect on chemical stability and half-life.

It has no effect on chemical stability and half-life.

It increases chemical stability and half-life. (correct)

It decreases chemical stability and half-life.

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

It has no effect on antibacterial activity.

It is essential for antibacterial activity. (correct)

It reduces antibacterial activity.

It is variable in its effect on antibacterial activity.

What is the effect of strong acid solutions on cephalosporins?

They increase the stability of cephalosporins.

They degrade cephalosporins. (correct)

They have a variable effect on the stability of cephalosporins.

They have no effect on the stability of cephalosporins.

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

Ethionamide Signup and view all the answers

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

2 billion Signup and view all the answers

What is the primary site of infection in tuberculosis?

Lungs Signup and view all the answers

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

Pulmonary tuberculosis Signup and view all the answers

What is the effect of β-lactamase on cephalosporins?

It degrades cephalosporins. Signup and view all the answers

What is the solubility of cefadroxil monohydrate in water?

Slightly soluble Signup and view all the answers

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

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

What is the technique used to assay cefadroxil?

Liquid chromatography Signup and view all the answers

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

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

What is the dose of cefaclor for adults?

250-500 mg every 8 h Signup and view all the answers

What is the characteristic of cefamandole nafate solutions?

They are unstable in solution and hydrolyze rapidly Signup and view all the answers

What is the IV dose of cefamandole?

0.5-2 g every 4 to 6 h Signup and view all the answers

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

KatG enzyme Signup and view all the answers

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

Reduces diuretic activity Signup and view all the answers

What is the characteristic of cefotaxime sodium?

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

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

Inhibits bacterial cell wall mycolic acid Signup and view all the answers

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

Little or no diuretic activity Signup and view all the answers

What is the effect of pyrazinamide on M.tuberculosis?

Bactericidal Signup and view all the answers

What is the starting material for the synthesis of bendroflumethiazide?

Phenylacetaldehyde Signup and view all the answers

What is the optimal environment for the activity of pyrazinamide?

Low pH environment Signup and view all the answers

What is the indication for pyrazinamide therapy?

Tuberculosis and meningitis Signup and view all the answers

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

Solvent Signup and view all the answers

What is the metabolic pathway of pyrazinamide?

Hydrolysis by hepatic microsomal pyrazinamidase Signup and view all the answers

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

Hydrochlorothiazide Signup and view all the answers

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

Furosemide Signup and view all the answers

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

Use with caution Signup and view all the answers

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

First-line status Signup and view all the answers

Which of the following diuretics is used to treat glaucoma?

Acetazolamide 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?

Sulfonamide group Signup and view all the answers

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

Serum creatinine Signup and view all the answers

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

Bendroflumethiazide Signup and view all the answers

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

Hydrochlorothiazide/triamterene Signup and view all the answers

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

Hypokalemia Signup and view all the answers

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

Spironolactone Signup and view all the answers

Which diuretic is used to treat acute kidney injury?

Mannitol 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.