Sulphadiazine ( *** ) @-(FDC- List )
Drug Name:Sulphadiazine ( *** ) @-(FDC- List )
List Of Brands:
Indication Type Description:
Drug Interaction
Indication
Adverse Reaction
Contra-Indications
Dosages/ Overdosage Etc
Other Information
Patient Information
Pharmacology/ Pharmacokinetics
Pregnancy and lactation
Drug Interaction:
Sulphonamides include- Sulfisoxazole, Sulfasalazine.
Refer Sulpdadiazine
Interacting drugs - summary
Sulfonamides +
Anticoagulants
warfarins anticoagulation action enhanced. Haemorrhage
could occur
Barbiturate Anesthetics
the anesthetic effects of thiopental enhanced
Cyclosporine
cyclosporine concetrations are decreased, and the risk of
nephrotoxicity increased
Digoxin
digoxins bioavailability decreased , possibly resulting
in a reduced therapeutic effect
Folic acid
signs of folate deficiency have occurred (eg low folate.
megaloblastic anemia,macrocytosis, teticulocytosis) but
specific symptoms related to the defiency not reported
Hydantoins
serum hydantoin levels increased
Methotrexate
the risk of methotrexate-induced bone marrow suppression enhanced
Sulfonylureas
increased sulfonylurea half-lives and hypoglycemia
Methenamine
an insoluble precipiate between the sulfonamide and fomaldehyde
form in the urine
Typhoid vaccine
the vaccine should not be administered to individuals receiving
sulfonamides and antibiotics since these agents may be active
against the vaccine strain and prevent a sufficient degree of
multiplication to occur to induce a protective immune response.
Indication:
Sulphonamides include- Sulfisoxazole, Sulfasalazine. Refer Sulphadiazine
FIXED DOSE COMBINATIONS APPROVED BY DCG(I)
FROM JANUARY 1961 TILL NOVEMBER 2014
Name of Drug Indication Date of Approval
1.Sulphadiazine 200mg + Jan-1987
Trimethoprim 40mg suspn
2.Sulphadizine 400mg + Jan-1987
Trimethoprim 80mg tablet
Adverse Reaction:
Hematologic- Agranulocytosis, aplastic anemia, thrombocytopenia, leukopenia, hemolytic anemia,hypothrombombinemia, cyanosis, methomoglobinemia, megaloblastic (macrocytic ) anemia, Heinz body anemia
Hypersensitivity- Stervens-Johnsons type multiforme, parapsoriasis variolioformis acuta , generalized skin eruptions, allergic myocarditis, epidermal necrolysis with or without corneal damage, urticaria, serum sickness, pruritus,exfoliative dermatitis, anaphylactoid reactions, periorbital edema, conjuntival, scleral injection, photosentization,
.
GI-- nausea, emesis, abdominal pains, diarrhea, boody diarrhea, anorexia, pancreatitis, stomatitis, impaired folic acid, absorption, hepatitis, hepatocellular necrosis, pseudomembraneous enterocolitis
CNS- headache, peripheral neuropathy, mental depression, convulsions, ataxia, hallucinations, tinnitis, vertigo,insomnia, hearing loss, drowsiness, transcient lesions of posterior spinal column, transverse myelitis,
Renal- crystalluria, hematuria, proteinuria, elevated creatinine, nephrotic syndrome, toxic nephrosis with lliguria and auria.
Miscellaneous- drug fever, chills, pyrexia, alopecia, arthalgia, myalgia,pulmonary infiltrates,
periateritis nodosum, L.E. phenomenon
Sulfasalazine produces an orange-yellow color urine when the urine is alkaline. Similar discolration of the skin has also occured
Drug/Lab test interactions-
Sulfonamides may produce false-positive urinary glucose tests when performed by benedicts method.
Sulfisoxazole may interfere with the Urobilix test and may produce false results with sulfosalicylic acid
tests for urinary protein.
Contra-Indications:
Hypersenstivity to sulphanamides
Special precautions-
Allergy or asthma- give with caution to patients with severe allergy or bronchial astma.If toxicity or hypersensitivity reactions occur, discontinue immediately.
Hemolytic anemia- frequently dose-related,may occur in G6-PD deficient individuals.
Warnings-
Group A beta hemolytic streptococcal infections- do not use for treatment of these infections. In establisahed infection, they do not eradicate the streptococcus and will not prevent sequalae, such as rheumatic fever and glomerulonephritis
Severe reactions- including deaths due to sulfonamides have been associated with hypersensitivity reactions,agranulocytosis, aplastic anemia, and other blood dyscrasias and renal and hepatic damage. Irreversible neuromuscular and CNS changes and fibrosing alevolitis may occur.
Sore throat, fever, pallor, purpura orjaundice may be early indications of serious blood disorders. Perform complete blood counts.
Porphyria- in patients with porhyria, these drugs have precipitated an acute attack.
Photosentivity- photosentization (photoallergy or phototoxicity ) may occur, therfore, caution patients to take protective measures (ie sunscreens, protective clothing, ) against exposure to sunlight or ultraviolet light, until tolerance is detremined.
Renal/hepatic function impairment- use with caution. Obtain urine analysis with microsocpic examinations and perfrom liver and kidney function tests during long-term treatment. Maintain adequate fluid intake to prevent crystalluria and stone formation.
Fertility impairment- oligospermia and infertility have been described in men treated with sufasalazine. Withdrawal of the drug appears to reverse the effects.
Pregnancy- safety for use during pregnancy has not been established.
Lactation- according to the American Academy of Pediatrics, breast feeding and sufonamide use are comptaible since sulphonamide excretion into breast milk dose not pose significant risk to the healthy full-term neonate.
Children- Do not use in infants < 2 months old. Sulfacytine is not recommended for children , 14 years. There are insuffcient clinical data on prolonged and recurrent therapy with Sulfamethozole in chronic renal disease of children < 6 years.
Dosages/ Overdosage Etc:
Dosage-
Adults- Loading dose- 2 to 4 g . Maintenance- 4 to 8g in 4 to 6 divided doses
Children- > 2 months- loading dose- 75mg/kg or 2g/m2. Maintenance- 120 to 150mg/kg/day (4g/m2/day in 4 to 6
divided dose. Maximum- 6g/day
Infants- < 2 months-contraindicated
Overdosage-
Symptoms
GI- anorexia, colic, nausea, vomiting
CNS- dizziness, headache, drowsiness, unconsciousness,
Toxic fever- precedes serious manifestations and may develop > 1 day after the fever due to infection has subsided
Serious manifestations-
Acidosis,acute hemolytic anemia, agranulocytosis,
sensitivity reactions, dermatitis(maculopapular)
toxic neutitis, hepatic jaundice, death (occuring after several days after first dose)
Treatment
1. Discontinue the drug immediately.
2. Within 1 or 2 days after discontinuation, less serious symptoms disappear, grave symptoms require 1 to 3 weeks
3. Empty stomach if large doses have been ingested
4. Alkaine the urine to enhance solubility and excretion
5. Force fluids if kidney function is normal up to 4L/day to increase excretion
6.If anuria is present treat for renal failure.
7. Catheritazation of the ureterss may be indicated for complete renal blockage by crystals.
8. For agranulocytosis, give antibiotic therapy to combat infection, and blood or platelet transfusions for severe anemia or thrombocytopenia.
Missed dose-
1. If you miss a dose of this medicine, take it as soon as possible.
2. However, if it is almost time for next dose, skip the missed dose and go back to your regular dosing schedule.
3. Do not double doses.
Other Information:
For Availability/supplies
Contact -
1.Indian Drug Manufacturers Association (IDMA)
Phone- 022- 24944624/ 24974308
Fax- 022- 24950723
Email- idma@vsnl.com
Website: www.idma-assn.org
2.Bulk Drug Manufacturers Association (India)(BDMA)
Phone - 040-23703910/ 23706718
Fax- 040-23704804
Email- info@bdmai.org
Website: www.info@bdmai.org
Erythewma nodum- ( 244 )
The erythem nodum syndrome refewrs too te ocurance of multiple bilateral tender nodules appearing principaaly on the
anterior aspect of lower extremirites and occassionally on the extremities of the face. Theerythema nodum is associated
with primary tuberculosis and primary coccidiomycosis , histoplamosis.
Drugs causing advese reaction - ( 386 )
1. Penicilins
2. Sulfonamides
3. Oral contraceptives
EVIDENCE BASED MEDICINE (April 2003)
Treatment of Scabies
Comparative effectiveness of various interventions
Beneficial
1. Permethrin - cure rate of about 90%
Likely to be beneficial
1. Crotamiton
Unknown effectiveness
1. Malathion
2. Benzyl benzoate - cure rate of about 50 percent
3. Oral ivermectin
4. Sulphur compounds
Trade-off between benefits and harms
1. Gamma benzene hexachloride (lindane)
KEY POINTS
1. One systemic review of mainly small randomised clinical trials has found that topical permethrine and gamma benzene hexachloride has been linked to rare reports of serious side effects
2. There is limited evidence that crotamiton is safe but less effective than permethrine
3. There is insuffcient evidence on the effects of other topical agents (malathion, benzyl benzoate, and sulphur compounds). On the basis of case series, malathion acheived 80% cure rates but its safety has not been established
4. There is insufficient evidence on the effects of oral invercetin. It s known to be safe in adults based on the experience of its use in onchocerciaciasis, but its safety in elderly and children is uncetain.
Patient Information:
SULFONAMIDES-
1. Complete full course of therapy
2. Take on an empty stomach with a full glass of water.
3. Avoid prolonged exposure to sunlight, photosentivity may occur. If outside , wear protective clothing
and apply sunscreen to exposed areas.
4. Notify physician if any of the following occurs. May cause an orange-yellow discoloration of the urine or skin.
May permenently stain soft contact lenses yellow.
5. Oral suspension- shake well, refrigerate afteropening. discard unused potion after 14 days.
6. Allergies- tell your doctor if you have ever had any unusual or allergic reaction to sulfa medicines.
Also tell your doctor if you are allergic to any other substances, such as foods, presevatives or dyes.
7.Pregnancy- studies in rabbits, rats and mice have shown that sulfonamides cause birth defects including cleft palate and bone problems.
8.Breast feeding- Sulfonamides pass into breast milk. This medicine is not recommended for use during breast feeding
9. Children- sulfonamides should not begiven to infants under 2 months of age unless directed by the childs doctor.
10. Elderly- elderly people are more sensitive to sulfonamides
11. Other medicines -
Acetoaminophen or
Amiodarone or
Anabolic steroids or
Androgens or
Antithyroid agents or
Carbamazepine or
Carmustine or
Chloroquine or
Dantrolene or
Daunorubicin or
Disulfram or
Divalproex or
Estrogens or
Etretinate or
Gold salts or
Hydroxychloroquine or
Mercaptopurine or
Naltrexone or
Oral contraceptives or
Other anti-infectives by mouth or
Phenothiazines or
Plicamycin or
Valproic acid - use of sulfonamides with these medicines may increase the chance of side effects affecting
the liver
Acetohydroxamic acid or
Dapsone or
Furazolidone or
Nitrofurantoin or
Primaquine or
Procainamide or
Quinidine or
Quinine or
Sulfoxone or
Vitamin K - use of sulfonamides with these medicines may increase the chance of side effects affecting the
blood.
Anticoagulants or
Ethotion or
Mephenytoin - use of sulfonamides with these medicines may increase the chance of side effects
Antidiabetic , oral - use of sulfonamides may increase the chance of side effects affecting the blood and/or
the side effects of oral antidiabetics
Metheamine - use of this medicine with sulfonamides may increase the chance of side effects of sulfonamides
Methotrexate or
Phenytoin - use of these medicines with sulfonamides may increase the chance of side effects affecting
the liver and/or the side effects of these medicines
Methyldopa - use of methyldopa may increase the chance of side effects afecting the liver/ and or the blood.
9. Other medical problems -
Tell your doctor if you have any other medical problems especially -
Anemia or
G6PD- deficiency - pateients with these problems may have an increase in side efects affecting the blood.
Kidney disease or
Liver disease - patients with liver disease may have an increased chance of side effects.
Porphyria- this medicine may bring on an attack of porphyria
10. Missed dose -
If you miss a dose of this medicine, take it as soon as possible. however, if it is almost time for the next dose, skip the missed dose. Do not double doses.
11. Storage -
Keep out of reach of children. Store away from heat or direct sunlight. Do not store
the capsule in bathroom, near the kitchen sink, or in other damp places.
12. Outdated medicines -
Do not keep outdated medicine or medicine no longer needed. Be sure that any
discarded medicine is out of reach of children.
Pharmacology/ Pharmacokinetics:
Ref- Drug Facts And Comparisons(2010)
Pharmacology:
Sulfonamides exert their bacteriostatic action by competitive antagonsim of para-aminobenzoic acid an esstentialcomponent in folic acid synthesis. Microorganisms that require exogenous folic acid and do not synthesize folic acid are not susceptible to the action of sufonamides.
Pharmacokinetics-
The oral sulfonamides are readily absorbed from the GI tract. These agents are distributed throughout all body tissues and readily enter the cerebrospinal fluid. The excretion is mainly by glomurular filtration, tubular reabsorption occurs in varying degrees. Small amounts are eliminated in the feces, and in bile, breast milk and other secretions.
Sulfonamides Pharmacokinetic Parameters
Cmax Tmax Protein binding Elimination
(mcg/mL) (h) (%) t 1/2 (h)
Sulfadiazine
60.04 4 38 to 48 -
(46.5) free
drug
Sulfisoxazole
122 to 282 1 to 4 85 4.6 to 7.8
(mean 2.5) (primarily
albumin;
68 to 72
of unbound
portion is in
nonacetylated
form)
Pregnancy and lactation:
Pregnancy-
Safety for use during pregnancy has not been established. Lactation- According to the American Academy of Pediatrics, breast feeding and sufonamide use are comptaible since sulphonamide excretion into breast milk dose not pose significant risk to the healthy full-term neonate.
Children-
Do not use in infants < 2 months old. Sulfacytine is not recommended for children , 14 years. There are insuffcient clinical data on prolonged and recurrent therapy with Sulfamethozole in chronic renal disease of children < 6 years.
