Avlosulfone - General Information
A sulfone active against a wide range of bacteria but mainly employed for its actions against mycobacterium leprae. Its mechanism of action is probably similar to that of the sulfonamides which involves inhibition of folic acid synthesis in susceptible organisms. It is also used with pyrimethamine in the treatment of malaria. (From Martindale, The Extra Pharmacopoeia, 30th ed, p157-8)
Pharmacology of Avlosulfone
Avlosulfone is a sulfone with anti-inflammatory immunosuppressive properties as well as antibacterial and antibiotic properties. Avlosulfone is the principal drug in a multidrug regimen recommended by the World Health Organization for the treatment of leprosy. As an anti-infective agent, it is also used for treating malaria and, recently, for Pneumocystic carinii pneumonia in AIDS patients. Avlosulfone is absorbed rapidly and nearly completely from the gastrointestinal tract. Avlosulfone is distributed throughout total body water and is present in all tissues. However, it tends to be retained in skin and muscle and especially in the liver and kidney: traces of the drug are present in these organs up to 3 weeks after therapy cessation.
Avlosulfone for patients
1. Patients should use ACZONE Gel, 5%, as directed by the physician. ACZONE Gel, 5%, is for external topical use only. ACZONE Gel, 5%, is not for oral, ophthalmic or intravaginal use.
2. Patients should not use this medication for any disorder other than that for which it was prescribed.
3. Patients should tell their physician if they have any history of anemia or an enzyme deficiency (such as G6PD deficiency).
4. Patients should be informed as to the need for laboratory evaluation prior to starting ACZONE Gel, 5%.
5. Patients should report any signs of adverse reactions to their physician.
6. Protect ACZONE Gel, 5%, from freezing and light. Return to the original carton after application to protect from light.
ACZONE (dapsone) Gel 5%
Read this important information before you start using ACZONE (AK-zon) Gel and each time you refill your prescription. There may be new information that you need to know. This summary is not meant to take the place of your doctorís advice. If you have any questions or want more information about ACZONE Gel, ask your doctor or pharmacist.
What is ACZONE Gel?
ACZONE Gel is a prescription skin use (topical) medicine used to help treat acne in people 12 years and older.
ACZONE Gel has not been studied in children under 12 years of age.
Who should not use ACZONE Gel?
Do not use ACZONE Gel if you are allergic any of the ingredients in ACZONE Gel. Ask your doctor or pharmacist for a list of these ingredients. The active ingredient is dapsone. See the end of this leaflet for a complete list of ingredients in ACZONE Gel.
What should I tell my doctor before using ACZONE Gel?
Tell your doctor about all of your medical conditions, including if you:
· are pregnant or planning to become pregnant. It is not known if ACZONE Gel may harm your unborn baby.
· are breastfeeding. ACZONEGel passes into your milk and may harm your baby. You should choose either to use ACZONE Gel, or breastfeed, but not both. Talk to you doctor about the best way to feed your baby while using ACZONE Gel.
· have a history of anemia or have been diagnosed with glucose-6-phosphate dehydrogenase deficiency
Tell your doctor about all the medicines you are taking including prescription and nonprescription medicines, vitamins and herbal supplements. Especially, tell your doctor if you are using any other medicines applied to the skin.
How do I use ACZONE Gel?
· Use ACZONE Gel exactly as prescribed by your doctor. ACZONE Gel is usually used on your affected skin twice a day, once in the morning and once in the evening.
· Wash the areas of your skin where you will apply ACZONE Gel. Gently pat your skin dry with a clean towel.
· Apply a thin layer of ACZONE Gel to the areas of your skin that have acne. A pea- sized amount of ACZONE Gel will usually be enough.
· Rub the medicine in gently and completely
· Make sure to put the cap back on the ACZONE Gel tube. Close it tightly and put the tube back in its original box.
· Wash your hands after applying ACZONE Gel.
· Keep ACZONE Gel away from your mouth and eyes. Do not swallow ACZONE Gel. If you swallow ACZONE Gel, call your doctor or poison control center right away.
· If your acne does not get better after using ACZONE for 12 weeks, talk to your doctor about other treatments for acne.
What are the possible side effects of ACZONE Gel?
Like all medicines, ACZONE Gel can cause some side effects. These side effects are usually mild. The most common side effects of ACZONE Gel are dryness, redness, oiliness and peeling of the skin being treated.
Call your doctor if you have excessive tiredness or any side effects that do not go away or bother you. This is not a complete list of all the side effects. If you have any questions, ask your doctor or pharmacist.
How should I store ACZONE Gel?
Store ACZONE Gel at room temperature 68 to 76 ºF. Do not freeze ACZONE Gel. Protect ACZONE Gel tube from light. Store in original box after using it.
Keep ACZONE Gel out of the reach of children less than 12 years of age.
Where can I find more information about ACZONE Gel?
If you have any questions or want more information about ACZONE Gel, ask your doctor or pharmacist. Your doctor or pharmacist can also give you a copy of the ACZONE Gel Package Insert written for health professionals. Ask them to explain anything you do not understand.
You may call 1-800-727-7003 to obtain more information about ACZONE Gel.
A drug-drug interaction study evaluated the effect of the use of ACZONE Gel, 5%, in combination with double strength (160 mg/800 mg) trimethoprim/sulfamethoxazole (TMP/SMX). During co-administration, systemic levels of TMP and SMX were essentially unchanged. However, levels of dapsone and its metabolites increased in the presence of TMP/SMX. Systemic exposure (AUC0-12) of dapsone and N-acetyl-dapsone (NAD) were increased by about 40% and 20% respectively in presence of TMP/SMX. Notably, systemic exposure (AUC0-12) of dapsone hydroxylamine (DHA) was more than doubled in the presence of TMP/SMX. Exposure from the proposed topical dose is about 1% of that from the 100 mg oral dose, even when co-administered with TMP/SMX.
Certain concomitant medications (such as rifampin, anticonvulsants, St. Johnís wort) may increase the formation of dapsone hydroxylamine, a metabolite of dapsone associated with hemolysis. With oral dapsone treatment, folic acid antagonists such as pyrimethamine have been noted to possibly increase the likelihood of hematologic reactions.
ACZONE™ Gel, 5%, is contraindicated in persons with a hypersensitivity to dapsone or any other component of the formulation.
Additional information about Avlosulfone
Avlosulfone Indication: For the treatment and management of leprosy and dermatitis herpetiformis.
Mechanism Of Action: Avlosulfone acts against bacteria and protozoa in the same way as sulphonamides, that is by inhibiting the synthesis of dihydrofolic acid through competition with para-amino-benzoate for the active site of dihydropteroate synthetase. The anti-inflammatory action of the drug is unrelated to its antibacterial action and is still not fully understood.
Drug Interactions: Rifabutin Decreased levels of dapsone
Rifampin Decreased levels of dapsone
Trimethoprim Increased toxicity of both products
Aluminium Formation of non-absorbable complexes
Calcium Formation of non-absorbable complexes
Magnesium oxide Formation of non-absorbable complexes
Magnesium Formation of non-absorbable complexes
Food Interactions: Take without regard to meals.
Generic Name: Dapsone
Synonyms: P, P'-Sulfonyldianiline; P-Aminophenyl Sulfone; P,P-Sulphonyldianiline; P,P-Sulphonylbisbenzenamine; P,P-Sulphonylbisbenzamine; P,P-Sulfonylbisbenzenamine; P,P-Sulfonylbisbenzamine; P,P-Diaminodiphenyl Sulphone; P,P'-Diaminodiphenyl Sulfone; N, N'-Diphenyl Sulfondiamide; Metabolite C; Sulfonyldianiline; Sulphadione; Sulphonyldianiline; Diphenasone; Diaphenylsulphone; Diaphenylsulphon; Diaphenylsulfone; Diaphenylsulfon; Diaminodiphenyl Sulfone; Diaminodifenilsulfona; Dds, Pharmaceutical; Dds, Diaphenylsulfone; DDS; Dapsonum; Dapson; DADPS; Acedapsone; Diamino-diphenyl sulphone; DSS
Drug Category: Leprostatic Agents; Antimalarials; Anti-inflammatory Agents; Anti-Infectives; Antimycobacterials
Drug Type: Small Molecule; Approved
Other Brand Names containing Dapsone: Araldite Ht; Avlosulfon; Avlosulfone; Avlosulphone; Croysulfone; Croysulphone; Dimitone; Diphone; Dubronax; Dumitone; Eporal; ICI; Normet; Novophone; Recolip; Sulfadione; Sulfanona-Mae; Sulfon-Mere; Sulfona; Sulfona-Mae; Sulfone Ucb; Sulphon-Mere; Sumicure S; Tarimyl; Udolac;
Absorption: Bioavailability is 70 to 80% following oral administration.
Toxicity (Overdose): Overdosage might be expected to produce nasal congestion, syncope, or hallucinations. Measures to support blood pressure should be taken if necessary.
Protein Binding: 70 to 90%
Biotransformation: Hepatic, mostly CYP2E1-mediated.
Half Life: 28 hours (range 10-50 hours)
Dosage Forms of Avlosulfone: Tablet Oral
Chemical IUPAC Name: 4-(4-aminophenyl)sulfonylaniline
Chemical Formula: C12H12N2O2S
Dapsone on Wikipedia: http://en.wikipedia.org/wiki/Dapsone
Organisms Affected: Mycobacteria