ANTI TUBERCULAR DRUGS

GROUP B TWO
ANEEQUA
ANEEBA
FAIZ
FAREED
 TUBERCULOSIS

 INFECTIOUS DISEASE CAUSED BY VARIOUS STRAINS

OF MYCOBACTERIUM TUBERCULOSIS
 MYCOBACTERIUM IS AEROBIC NON MOTILE
BACILLUS
 TYPICALLY ATTACKS LUNGS
 MODE OF TRANSMISSION

 IT IS TRANSMITTED THROUGH THE AIR WHEN

PEOPLE WHO HAVE AN ACTIVE TB INFECTION COUGH
OR SNEEZE
 A SINGLE SNEEZE RELEASE UPTO 40,000 DROPLETS.
 SYMPTOMS AND DIAGNOSIS

SYMPTOMS
 CHEST PAIN
 CHRONIC COUGH WITH BLOOD TINGED SPUTUM
 FEVER
 NIGHT SWEATS
 WEIGHT LOSS
 NAIL CLUBBING
 DIAGNOSIS

 RADIOLOGY
 MICROSCOPIC EXAMINATION
 TYPES OF TB

PULMONARY
TUBERCULOSI EXTRA
S PULMONARY
TUBERCULOSIS
TB DEVELOPS
EFFECTS OUTSIDE THE
LUNGS LUNGS

5-20% MOSTLY IN
IMMUNOSUPPRE
SSDED PATIENTS
 RISK FACTORS

 HIV
 PEOPLE WHO INJECT ILLICIT DRUGS
 CHRONIC LUNG DISEASE
 SMOKING
 DIABETES MELLITUS
 ALCOHOLISM
TUBERCULOSIS MANAGEMENT AND
CURE

ANTI TB DRUGS
CLASSIFICATION OF ANTI TB AGENTS

FIRST LINE SECONG

DRUGS LINE
DRUGS
Isoniazid Clarithromycin

Rifampicin Ciprofloxacin

Ethambutol Capreomycin

Pyrazinamid Cycloserine

Kanamycin

Amikasin

streptomycin
 FIRST LINE DRUGS
o good efficacy
o less toxicity
o Being well tolerated for patients
o Kill active bacteria
 SECOND LINE DRUGS
o Hinder bacterial growth
o Less efficient and more toxic
FIRST LINE DRUGS
 ISONIAZID

MOST ACTIVE DRUG FOR THE CLASS OF

TUBERCULOSIS
CLASS : Anti tubercular
IUPAC Name : isonicotinohydrazide
Trade Names : hydra , Isovit , Laniazid , Nydrazid
Routes of administration : oral, IM , IV
 PHARMACOKINETICS

 PROTEIN BINDING : Very low

 METABOLISM : Liver
 Half life : 0.5-1.6 h
 Excretion : 75-95% of a dose is excreted in the urine in 24 hrs.,
mostly as metabolites.
 Dosage form : tablet , syrup , IM IV injections
 Fatty food & aluminum-containing antacids may reduce
absorption
 MECHANISM OF ACTION

 Probably related to the inhibition of synthesis

of mycolic acids, which are important and
characteristic components of mycobacterial
cell wall. As a result of the activity, tubercle
bacilli lose their features of acid-resistance,
water-resistance and proliferating ability,
leading to death.
 Bacteriostatic – to resting organism

 Bactericidal – to multiplying organism

PHARMACOLOGICAL ACTIVITY

 It is bactericidal for actively growing

tubercle bacilli. But, for resting tubercle
bacilli, it is bacteriostatic.
 Isoniazid is able to penetrate into
phagocytic cells and thus is active against
both extracellular and intracellular
organisms.
 This drug is not effective against atypical
mycobacteria.
 CLINICAL USE

 Isoniazid is the most widely used agent in

the treatment and prophylaxis of tuberculosis.
 Isoniazid is usually given by mouth but can
be given parenterally in the same dosage.
 DOSE

 300 mg Isoniazid once daily for 6-12 months

 Adverse effect

 Hepatotoxicity
 Polyneuropathy
( Prevented by concurrent pyridoxine )
 Rashes, acne
 Heamatological – haemolytic anaemia in G6PD
deficiency
 ADVERSE EFFECTS

 Allergic Reaction: fever,skin rash

 ­Hepatotoxicity : Up to 20% of patients taking INH
 develop elevated serum amino transferase levels.
 ¨Severe hepatic injury occurs more frequently
in patients over the age of 35, especially in
those who drink alcohol daily.
 CONTRAINDICATIONS

 PREGNANCY
 CHILDREN UNDER THE AGE OF 2
 DOCTORS PRESCRIBE VIT B6 TO MASK SOME OF THE
SIDE EFFECTS
 STORAGE

 Tightly close container

 Out of reach of chldren
 Keep at room temp
 WARNINGS

 IF U HAVE DIABETES DONOT USE CLINITEST TO TEST

YOUR URINE FOR SUGAR BECAUSE IT CAN CAUSE
FALSE RESULTS .
 Rifampicin

Generic Name : Rifampin

Brand Name : Rifadin IV
Class : anti tubercular
Rifampin is als used to treat patients who donot have
meningitis but carry the meningitis bacteria in their
nose and throat and may spread the bateria .
 PHARMACOKINETICS

 oral administration, well absorbed, widely

distributed in body, including sputum adequate CSF
 concentrations are achieved only in the
presence of meningeal inflammation.
 most of the drug is excreted as a deacylated
metabolite in feces and in the urine.
 Half life is about 4 hours.
 Rifampin: Pharmacologic activity

 broad-spectrum
 It is active against G+ cocci (including drug resistant
S.aureus)
 It is bactericidal for mycobacteria.
 It can kill organisms that are poorly accessible
to many other drugs, such as intracellular
organisms and those sequestered in abscesses
and lung cavities.
 Mechanism of rifampin

 RFP binds strongly to theβ-subunit of

DNA-dependent RNA polymerase and
thereby inhibits RNA synthesis.
Drug-resistance to RFP, due to target
mutations in RNA polymerase, occurs
readily.
 No cross-resistance to other classes of
antimicrobial drugs.
 Rifampin: Clinical uses

 Mycobacterial infections
 It often uses in combination with other agents
(Tuberculosis, rifampin) in order to prevent
emergence of drug-resistant mycobacteria.
 Leprosy
 Rifampin can be used in a variety of gram-positive
coccal infections
 It is also used as prophylaxis for meningitis caused by
highly penicillin-resistant strains of pneumococci.
 Rifampin: Adverse effects

 Urine, sweat, tears, and contact lenses may

take on an orange color
 Light-chain proteinuria
 Rifampin induces hepatic microsomal enzymes
 When taken erratically in large doses, a febrile
“flu-like” syndrome can occur.
• Rashes, hepatotoxicity, thrombocytopenia
 Clinical Usage

DOSAGE
10mg/kg/day
OTHER INDICATIONS
oral dosage of 600mg twice daily
for two days to eliminate meningococal carriage
ADVERSE EFFECTS
 DONOT USE RIFAMPIN IF
 You are allergic to any ingredient in rifampin
 Pregnancy
 Diabetes
 Liver problems ( jaundice , cirrhosis )
 Inflammation of bile duct
 You are taking
 Atazanavir
 Cabazitaxel
 Darunavir
 Delaviridine
 Tyrosine kinase receptor inhibitor
 Ethambutol

 Inhibits arabinosyl transferases involved in cell wall

biosynthesis

 Bacteriostatic to M.tuberculosis

 Resistance develops rapidly if used alone

 CLINICAL USAGE

 DOSAGE
15-25mg/kg as a single dose
50mg/kg when twice weekly schedule is followed
 Adverse effects

 Optic retro-bulbar neuritis

 Red-green colour blindness → reduced visual acuity
 Dose-related
 Reversible
 May be unilateral
 Pyrazinamide

 Interferes with mycobacterial fatty acid synthesis

 Inactivate mycobateria at acidic PH

 Effective against intracellular organism in

machrophages – PH is low
 Clinical usage

 50-70mg/kg/day twice/thrice for weekly treatment

regimensGI disturbances
ADVERSE EFFECTS
 Hepatotoxicity

 Hyperuricaemia – gout

 Arthralgia