Antileprotic drug information https://informationtech044mobile.blogspot.com/2023/07/isro-launch-chandrayan-3-mission.html?m=1

1. ANTILEPROTIC DRUG
CREATED BY SONSALE PRASAD

2. INTRODUCTION
 LEPROSY Definition⚫ It is a contagious skin disease, causing serious and
permanent damage of the body, including loss of fingers, nose etc..
 Leprosy is caused by a slow-growing type of bacteria called Mycobacterium
leprae (M. Leprae) Also known as Hansen’s disease, after the scientist ho
discovered M. Leprae in 1873.
 ▷ It primarily affects the skin and the peripheral nerves.
 Long Incubation period (3-5 years).

3. SIGNS AND SYMPTOMS
 SIGNS & SYMPTOMS
 ⚫ Skin lesions are the primary external sign.. Left
untreated, leprosy can be progressive, causing
permanent damage to the skin, nerves, limbs,
and eyes.
 ⚫ Contrary to folklore, leprosy does not cause
body parts to fall off, but tissues can become
numb and other microbes can invade them as
secondary infections when the disease weakens
the body's defences.

4. SIGNS AND SYMPTOMS OF LEPROSY

5. CLASSIFICATION OF ANTILYPROTIC DRUG

6. DAPSONE
 Mechanism of action:
 Dapsone is a sulfone for the primary
treatment of Dermatitis herpetiformis and an
antibacterial drug for susceptible cases of
leprosy. Dapsone is bactericidal as well as
bacteriostatic against Mycobacterium leprae.
As an antibacterial, dapsone inhibits bacterial
synthesis of dihydrofolic acid, via
competition with para- aminobenzoate for
the active site of dihydropteroate synthetase.

7. DAPSONE STRUCTURE

8. ADVERSE EFFECTS
 Adverse EffectsGIT Side effects-Anorexia, Nausea, Vomiting
 Hemolytic Anaemia>
 Methaemoglobinaemia
 Sulfone Syndrome - Fever, Malaise, Exfoliative
dermatitis,Jaundice, Anaemia, Methaemoglobinaemia,
Lymphadenopathy
 Lepra Reaction
 CNS-headache, Nervousness, Insomnia, Paresthesia, Blurring of
Vision, Peripheral Neuropathy

9. THERAPEUTIC USES OF DAPSONE
 Therapeutic Uses
 >Leprosy
 P. Falciparum Malaria
 Pneumocystis Jiroveci Pneumonia
 Toxoplasmosis
 Dermatological Disorders-Acne, Dermatitis herpatiformis, Bullous SLE,
Pemphigus

10. PHARMACOKINETICS
 Pharmacokinetics
 ⚫ Dapsone is completely absorbed after oral
 administration and is widely distributed in the body.
 ⚫ Metabolites are excreted in bile and reabsorbed from intestine, so that
ultimate excretion occurs mainly in urine.

11. DOSE
 Dosing:
 ▸ Oral
 > Leprosy:
 Oral 1-2 mg/kg/day as single dose in combination with rifampicin.
 Maximum Dose: 100 mg/day.
 Pneumocystis Pneumonia Prophylaxis:>1 month: 2 mg/kg/day (up to 100 mg)
orally once a day OR 4mg/kg orally once weekly Maximum dose = 200
mgAdolescents: 100 mg once orally or in two divided doses in single drug
treatment OR 50 mg once every day in combination therapy.

12.  2) Phenazine derivatives
 Clofazimine:
 It is a dye with leprostatic and anti
inflammatory properties; acts probably
by interfering with template function of
DNA in M.Leprae. When used along,
resistance to Clofazimine develops in 1
to 3 years.

14. PHARMACOKINETICS OF CLOFAZIMINE
Pharmacokinetics
Is orally active 40 to 70% absorbed.
DOSE:
CLOFOZINE, HANSEPRAN 50, 100 mg Capsule . Is used as a component of
multidrug therapy of leprosy. Because of its anti inflammatory property, it is
valuable in lepra reaction.

15. ADVERSE EFFECTS
 Adverse effects
 Skin- Major disadvantage is reddish-black discolouration of skin, especially on
exposed parts.
 > Discoloration of hair and body secrections.
 itching. Dryness of skin and Acne form eruptions.
 GI SYMPTOMS-> Loose stools,Nausea,Abdominal pain,Anorexia and> Weight
loss.

16.  3) Antitubercular drugs
 Rifampin :
 It is an important antitubercular drug also
bactericidal to M.Leprae. Upto 99.99%
M.Leprae are killed in 3 to 7 days. Included
in the multidrug therapy of leprosy: shortens
duration of treatment.
 The 600mg monthly dose used in leprosy is
relatively nontoxic and does not include
Metabolism of other drugs. It should not be
given to patients with hepatic or renal
dysfunction.

18. 2.Ethionamide
⚫A 2nd line anti TB agent, analogue of
isonicotinamide but it is di-substituted
and contains S in place of O
It contains ethyl group at position 2
• In vitro it is less active but in vivo
more active because of increased
lipocity due to C₂H,
• Mechanism of action is similar to INH
• Its active metabolite is ethionamide
sulfoxide

20.  4) Other Antibiotics
 Ofloxacine:
 As a component of multidrug therapy
and found it to hasten the
bacteriological and clinical response.
Over 99.9% bacilli were found to be
killed by 22 daily doses of Ofloxacin
monotherapy. DOSE:
 400mg/day.

22. MINOCYCLINE
 Minocycline
 High lipophilicity helps to penetrate M.leprae
 -Efficacy in-between clarithromycin and rifampicin
 Rapid relief from lepromatous symptoms
 Vertigo on long term use
 Used in alternate regimes

24. CLARITHROMYCIN
 Clarithromycin
 Only macrolide effective in Leprosy
 Rapid clinical improvement
 Synergistic action with minocycline
 Used in alternate regimes

26. REACTIONS IN LEPROSY
 Reactions in Leprosy
 Reversal reaction
 >Seen in TT and BL due to delayed hypersensitivity to antigen of M.leprae
 -Cutaneous ulceration, Multiple nerve involvement with Swollen, painful
 and tender nerves.
 Prednisolone-4-60mg daily till reaction subside and tapered gradually
 Clofazimine is effective

27. LEPRA REACTION
 Lepra reaction
 Temporary discontinuation of Dapsone in
severe cases
 -Clofazimine 200 mg
 Prednisolone 40-60 mg/day
 >Thalidomide-100-300 mg OD alternate to
prednisolone
 >Chloroquine
 Analgesics, antipyretics and antibiotics

28. SUMMARY
 Summary
 >Leprosy
 -Dapsone
 Rifampicin
 Clofazimine
 Alternative drugs
 Treatment strategies
 Lepra reaction