SULFADIAZINE

SULFADIAZINE

SULFADIAZINE

SULFADIAZINE

Overview and uses

Sulfadiazine is a short-acting (4-8 hr) antibiotic of the sulfonamide family of drugs.

Indication (uses)

  • Used for the treatment of infections like:
    • Nocardiosis
    • Trachoma
    • Chancroid
    • Inclusion conjunctivitis
    • As a secondary treatment in urinary tract infections
    • Toxoplasmosis encephalitis
    • Acute otitis media
    • Meningococcal meningitis
    • Rheumatic fever
    • Lymphogranuloma venerum

Pharmacological classification

Sulfonamide antibacterial

Brand names

Not available, available only as a generic medicine.

Dosage form

  • Available as oral tablets and compounding powder for oral use.

Mechanism of action

Sulfonamides inhibit the formation of bacterial folic acid by inhibiting folate synthase enzyme. Since sulfonamides are structurally similar to PABA, they inhibit the union of PABA with pteridine residue to form dihydropteroic acid which conjugates with glutamic acid to produce dihydrofolic acid. Also, being structurally similar to PABA, sulfonamides may get directly incorporated into the bacterial cell to form an altered folate which is metabolically injurious.

Dosage

Dosage (for adults)

  • For the prophylaxis of rheumatic fever:
    • 1 g orally once a day.
  • For the treatment of toxoplasmic encephalitis:
    • Treatment should be initiated with pyrimethamine 200 mg once a day.
    • The maintenance dose of sulfadiazine 1 g orally after every 6 hours along with pyrimethamine 50 mg once a day if the body weight of the patient is less than 60 kg.
    • The maintenance dose of sulfadiazine 1500 mg orally after every 6 hours along with pyrimethamine 75 mg once a day if the body weight of the patient is more than or equal to than 60 kg.
    • Leucovorin 10 to 20 mg once a day should also be given. Anti-convulsants and corticosteroids may be given if required.
  • For the prophylaxis of toxoplasmic encephalitis:
    • Sulfadiazine 500 mg orally after every 6 hours along with pyrimethamine 25 mg once a day if the body weight of the patient is less than 60 kg.
    • The maintenance dose of sulfadiazine 1000 mg orally after every 6 hours along with pyrimethamine 50 mg once a day if the body weight of the patient is more than or equal to than 60 kg.
    • Leucovorin 10 to 20 mg once a day should also be given. Anti-convulsants and corticosteroids may be given if required.
    • Duration of prophylaxis can be determined from the MRI of the brain. In HIV patients, it should be continued life-long. Treatment can be discontinued only if the level of CD4+ cells is maintained in HIV patients.

Dosage (for pediatric patients)

Sulfadiazine is not recommended in infants less than 2 months of age.

  • For the prophylaxis of rheumatic fever:
    • 500 mg orally once a day if the patient is more than 2 months of age and has less than or equal to 27 kg body weight.
    • 1 g orally once a day if the body weight of the patient is more than 27 kg.
  • For the treatment of toxoplasmosis:
    • For congenital toxoplasmosis:
      • Treatment should be initiated with pyrimethamine 2 mg/kg orally once a day for 2 days.
      • The maintenance dose of sulfadiazine 50 mg/kg orally twice a day along with pyrimethamine 1 mg/kg orally once a day with leucovorin 10 mg orally or IM once a day for 12 months. After 2 to 6 months, decrease pyrimethamine to 1 mg/kg orally 3 times a week.
    • For acute acquired toxoplasmosis:
      • Treatment should be initiated with pyrimethamine 2 mg/kg orally (maximum 50 mg) once a day for 3 days.
      • Maintenance dose of sulfadiazine 25 to 50 mg/kg orally (not more than 1 to 1.5 g depending on body weight) every 6 hours along with pyrimethamine 1 mg/kg (not more than 25 mg) orally once a day with leucovorin 10 to 25 mg orally once a day for a minimum of 6 weeks followed by chronic suppressive therapy.
    • For the prophylaxis of toxoplasmic encephalitis:
      • Sulfadiazine 85 mg/kg/day in 2 to 4 divided orally with pyrimethamine 1 mg/kg or 15 mg/m2 (based on body surface area) once a day with leucovorin 5 mg every 3 days. Prophylaxis should be continued for lifetime in HIV infected patients.

RENAL DOSE ADJUSTMENTS

  • Patients with creatinine clearance less than 10 ml/min:
    • Usually avoided due to high risk of crystalluria.
  • Patients with creatinine clearance equal to 10 ml/min but less than 25 ml/min:
    • Dosing interval should be increased to every 24 hours.
  • Patients with creatinine clearance equal to 25 ml/min but less than 50 ml/min:
    • Dosing interval should be increased to every 12 hours.

HEPATIC DOSE ADJUSTMENT

  • Strict monitoring is recommended.

ELDERLY PATIENTS

  • No adjustments needed if creatinine clearance is normal.

OVERDOSAGE

  • Gait (the way a person walks) and hypotension in addition to other symptoms that are associated with ranitidine side effects.
  • No specific antidote is known.
  • Removal of unabsorbed material from the Gastrointestinal tract should be considered.
  • Dialysis should be considered as ranitidine is removed by dialysis.
  • Supportive treatment should be given as and when required.
  • Contact the emergency department of your local hospital in cases of overdose or suspected overdose.

Side effects or unwanted effects

  • Hypersensitivity reaction including urticarial rash (most common), allergic myocarditis, arthralgia, epidermal necrolysis, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, urticaria, serum sickness, photosensitization and generalized skin eruptions.
    • Consult your doctor as soon as possible if you observe skin rash, red or purple colored skin rash, facial swelling, swelling of the tongue, hives on the skin, joint pain, a painful red area on the skin that spreads quickly, peeling of the skin without blistering, fever, shortness of breath during exercise at first and then at night time while lying down, abnormal heartbeat, lightheadedness, sharp or stabbing chest pain and fatigue are some of the symptoms. This may require immediate medical attention and discontinuation of the therapy.
  • Gastrointestinal side effects include nausea, vomiting, abdominal pain, diarrhea, anorexia, pancreatitis and stomatitis.
    • Ask your pharmacist to recommend a suitable medicine and consult your doctor.
  • The occurrence of hepatitis and jaundice, though rare cannot be ruled out.
    • Nausea, stomach pain, dark colored urine, yellowing of the skin and whites of the eye, light or clay-colored stools, fever and unusual tiredness are some of the symptoms. Consult your doctor as soon as possible. This may require discontinuation of the treatment with sulfadiazine.
  • Aplastic anemia, hemolytic anemia, hypoprothrombinemia, leucopenia, purpura and agranulocytosis.
    • Purple-colored spots under skin, sudden fever, chills, sore throat, weakness in limbs, mouth ulcers, bleeding gums, easy bruising and prolonged bleeding are some of the symptoms of the above-mentioned condition. Consult your doctor as soon as possible as some of the above-mentioned conditions are serious and life-threatening.
  • Tremulousness, delirium and disorientation have been frequently reported
    • Shaking of a body part or even full body, anxiety, fear, hallucinations, irritability, rapid and unpredictable mood swings, difficulty in reading, writing, recalling or speaking of words are some of the symptoms of the above-mentioned condition. Consult your doctor as soon as possible.
  • The occurrence of frank psychosis is rare.
  • Ataxia, convulsions, hallucinations, headache, insomnia, mental depression, peripheral neuritis, tinnitus and vertigo have also been reported.
  • Crystalluria, lupus periarteritis nodosa, toxic nephrosis with oliguria and anuria have also been reported.
  • The occurrence of hypoglycemia has also been reported with sulfadiazine use.
  • Kernicterus may be precipitated in newborn, commonly observed with premature born babies.

Pregnancy

Category C, which means animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Nursing

  • Use of Sulfadiazine is contraindicated in breastfeeding women.

Interactions

Drug-drug interactions

  • Concomitant use of sulfadiazine with indomethacin, probenecid or aspirin (including all salicylates) may worsen the side effects of sulfadiazine.
  • Anti-coagulants like warfarin increases the risk of bleeding when co-administered with sulfadiazine.
  • Side effects of methotrexate and thiazide diuretics like Hydrochlorothiazide, Benzthiazide, Hydroflumethiazide and Clopamide may be increased when co-administered with sulfadiazine.
  • Sulfonylurea’s like Glipizide, Glimepiride and Glyburide may increase the risk of low blood sugar when co-administered with sulfadiazine.
  • Consult your doctor before taking sulfadiazine with clozapine, cyclosporine, anisindione, sodium nitrite, methenamine, lomitapide, mipomersen and live cholera vaccine.

Drug-food interactions

  • Sulfadiazine can be taken with or without food.
  • Avoid consuming alcohol when taking sulfadiazine.

Note: The sole purpose of every information shared on this article is to bring awareness. Do not use this information as a piece of medical advice or prescription advice or as a tool for the treatment, diagnosis or prevention of the disease.