Immune Modulator Drugs

For Systematic Therapy

Dermatology Department

September 18th, 2019

Agenda

Introduction : Immunomodulatory Drugs

Dapsone

Pharmokinetics

Pharmodynamics

Contradictions

Doses and Monitoring

Introduction
Immunomodulatory Drugs

A chemical agent that modifies the immune

response or the functioning of the immune system
(as by stimulation of antibody formation or the
inhibition of white body cells activity).
Dapsone

It is a potent anti-inflammatory agent used in wide variety of primary

dermatological inflammatory disorders.

Dermatological Uses Other with Unpredictable Efficacy

 Leprosy
 Dermatitis Herpetiformis  Auto immune hectoring disorders
 Chronic Bullous Disease of childhood
 Bullous lupus Erythematosus  Vasculitis
 IGM - Pemphigus
 Sub Corneal Pustular Dermatosis  Neutrophilic Dermatoses
 Linear IGA Disease
Dapsone
Pharmacological Properties

Administration
 Oral ingestion – 50 and 100mg tablet
 Topical Gel – Dapsone 5% gel
Pharmacokinetics

 Efficiently absorbed from GIT and have significant enterohepatic

circulation. Peak plasma cone occurs 2-6 hours after ingestion, widely
distributed, crossing placenta and passing into breast milk. Metabolization
occur into the liver along with 2 – pathways
• Acetylation
• Hydroxylation
Dapsone
Pharmacological Properties

Pharmacokinetics

 Acetylation results in non- toxic metabolites i.e. GIT monoacetyl dapsone

and diacetyl dapsone.

 Hydroxylation yields potentially toxic dapsone hydroxylamine

 Excretion of metabolites in urine
 It has a long half life elimination of 1-2 days
Dapsone
Pharmacological Properties

Pharmacodynamics

 It inhibits folic acid metabolic pathway

 It has inhibitory actions on neutrophil and eosinophil functions
Adverse Effects

 Hemolysis and methemoglobinemia

 Agranulocytosis
 Peripheral Neuropathy
 Ocular side effects
 Dapsone Hypersensitivity Syndrome
Dapsone
Pharmacological Properties

Contradictions
 Severe G6PD Deficiency
 Advanced CVS or Pulmonary Diseases
Adverse Effects

 Pregnancy : If unavoidable than moderately safe Folic acid is advised

during pregnancy
 G6PD deficiency
 Significant Cardiopul Disease
 Severe Hepatic and Renal Impairment
 Pre-existing peripheral Neuropathy with pre-treatment screening for all
above mentioned conditions
Dapsone
Pharmacological Properties
Dose and Regimens

 Single daily dose of 50-100 mg increasing to 100-200mg/day

 Once disease control has been attained, dose should be gradually tapered
to lowest effect level to minimize toxicity

Monitoring

 CBD, differentiated WDC every week for first 4 weeks and fortnightly for
next 8 weeks
 Patient education to discontinue medication in event of fever, chills and
sore throat within 3 months of starting dapsone
 FBC reticulocytosis – 3 months : Sign of Hemolysis as reticulocytes and
bilirubin should prompt request for blood film, LDH and Haptoglobin
Dapsone
Pharmacological Properties

Monitoring

 Methemoglobin level
 Lfts – fortnightly for 3 months so Lfts and Rfts & CBC every 3 months
 Motor and Sensory neurons sys assessment
Thanks