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Silver Sulfadiazine

D06B - Chemotherapeutics for dermatological use ATC D06BA01 Small molecule approved 1973 Topical

🧬 Cross-allergy: Sulfonamides

JFDA label: No-Burn Cream

Mechanism of Action

Inhibitor of Dihydropteroate synthase — Bacterial dihydropteroate synthase inhibitor

TargetActionGene / class
Dihydropteroate synthase efficacy INHIBITOR folP

Indications

Approved

  • Burn treatment

Contraindications

Source: Lexicomp

  • Hypersensitivity to silver sulfadiazine or any component of the formulation Absolute
  • pregnant women approaching or at term Absolute
  • premature infants or neonates ≤2 months of age. Documentation of allergenic cross-reactivity for drugs in this class is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Hepatobiliary disorders (1)

Not Known Hepatitis

Renal and urinary disorders (1)

Not Known Interstitial nephritis

Blood and lymphatic system disorders (4)

Not Known Agranulocytosis · aplastic anemia · hemolytic anemia · leukopenia

Immune system disorders (1)

Not Known Hypersensitivity reaction (may be related to sulfa component)

Skin and subcutaneous tissue disorders (5)

Not Known Erythema multiforme · pruritus · skin discoloration · skin photosensitivity · skin rash

Dosing

Source: Lexicomp

Burn treatment: Topical: Apply to a thickness of 1/16 inch once or twice daily; reapply as needed to areas where the cream is removed by patient activity as the burned area should be covered with cream at all times. Continue use until healing has occurred or the burn site is ready for grafting. Do not discontinue therapy if the possibility of infection exists unless a significant adverse reaction has occurred.
(For additional information see "Silver sulfadiazine: Pediatric drug information") Burn treatment: Infants ≥2 months, Children, and Adolescents: Refer to adult dosing.
Refer to adult dosing.
There are no dosage adjustments provided in the manufacturer's labeling; use with caution; drug accumulation may occur.
There are no dosage adjustments provided in the manufacturer's labeling; use with caution; drug accumulation may occur.

Warnings & Precautions

Source: Lexicomp

Sulfonamide allergy

Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). Use in patients with sulfonamide allergy is specifically contraindicated in product labeling, however, a risk of cross-reaction exists in patients with allergy to any of these compounds; avoid use when previous reaction has been severe.

Superinfection

Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment. Fungal proliferation may rarely occur in and below the eschar.

Systemic effects

Systemic absorption may be significant and adverse reactions may occur. Disease-related concerns:

G6PD deficiency

Use with caution in patients with G6PD deficiency; hemolysis may occur.

Hepatic impairment

Use with caution in patients with hepatic impairment; sulfadiazine may accumulate.

Renal impairment

Use with caution in patients with renal impairment; sulfadiazine may accumulate. Concurrent drug therapy issues:

Drug-drug interactions

Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information. Dosage form specific issues:

Propylene glycol

Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Zar 2007). Other warnings/precautions:

Appropriate use

For topical use only. Avoid contact with eyes.

Pregnancy & Lactation

Pregnancy

Adverse events were not observed in animal reproduction studies. Because of the theoretical increased risk for hyperbilirubinemia and kernicterus, silver sulfadiazine is contraindicated for use near term, on premature infants, or on newborn infants during the first 2 months of life (refer to Sulfadiazine monograph).

Lactation

Contraindicated

It is not known if silver sulfadiazine is found in breast milk following topical application; however, sulfonamide serum concentrations may reach therapeutic levels following application to extensive areas. Due to the potential for serious adverse reactions in the nursing infant, the manufacturer recommends a decision be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of treatment to the mother. Oral sulfadiazine is contraindicated in nursing mo

Monitoring

Clinical pearlSerum electrolytes, urinalysis, renal function tests, CBC in patients with extensive burns on long-term treatment. Serum sulfa concentrations, if clinically indicated.

Chemistry & Properties

2D structure
FormulaC10H9AgN4O2S
Molecular weight357.14 g/mol
IUPAC namesilver (4-aminophenyl)sulfonyl-pyrimidin-2-ylazanide
CAS22199-08-2
PubChem CID441244
InChIKeyUEJSSZHHYBHCEL-UHFFFAOYSA-N
logP0.86
Polar surface area97.97 Ų
H-bond acceptors / donors5 / 2
Drug-likeness (QED)0.79
Lipinski violations0
SMILESNc1ccc(S(=O)(=O)[N-]c2ncccn2)cc1.[Ag+]

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability10.0%
Half-life1.015 h
Volume of distribution0.437 L/kg
Protein binding59.6%
BBB penetrantNo

Enzyme interactions

EnzymeRoleDetail
CYP2C9Substrate
CYP3A4Substrate

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OAT3 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (60, DDInter)

Interacting drugSeverityManagement
Aminobenzoic acid major
Aminolevulinic acid major
Cyclosporine major
Dicoumarol major
Nitrous acid major
Warfarin major
Acetohexamide moderate
Aminolevulinic acid (topical) moderate
Asparaginase Escherichia coli moderate
Balsalazide moderate
Brentuximab vedotin moderate
Celecoxib moderate
Chlorpropamide moderate
Clofarabine moderate
Dapsone moderate
Dapsone (topical) moderate
Diclofenac moderate
Epirubicin moderate
Ethinylestradiol moderate
Folic acid moderate
Glimepiride moderate
Glipizide moderate
Glyburide moderate
Idelalisib moderate
Insulin aspart (aspart protamine) moderate
Insulin aspart (aspart) moderate
Insulin degludec moderate
Insulin detemir moderate
Insulin glargine moderate
Insulin glulisine moderate
Insulin human moderate
Insulin human (inhalation, rapid acting) moderate
Insulin human (isophane) moderate
Insulin human (regular) moderate
Insulin human (zinc extended) moderate
Insulin human (zinc) moderate
Insulin lispro moderate
Insulin lispro (protamine) moderate
Interferon beta-1a moderate
Interferon beta-1b moderate

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Registered Products (7)

BrandForm / strengthPackAgentCitizen (JOD)
No-Burn Cream Cream 1 % 30 g tube pack varies PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN 1.430
Silvezin Cream Cream 1 % 50 g tube pack varies Sukhtian Group 2.380
No-Burn Cream Cream 1 % 200 g tube pack varies PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN 4.200
Flamazine cream Cream 1 % 250 g tube pack varies Petra Drug Store 7.900
Silvezin Cream Cream 1 % 500 g tube pack varies Sukhtian Group 12.840
Flamazine cream Cream 1 % 500 g tube pack varies Petra Drug Store 14.740
Flammacerium 1%, Cream 1 %, 2.2 % 500 g tube Hikma Pharmaceuticals Co.Ltd/Jordan 29.770