ANTI-TB DRUGS

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BY:- ANURAG M SISODIA.

ROLL.NO:-21014
 SECOND LINE DRUGS:-
These are less effective or less tolerated anti TB drugs that are used only
in case the bacilli are resistant to one or more first line drugs.
Or may also be used when first line drugs are contraindicated.
CLASSIFICATION:-

SECOND
SECONDLINE DRUGS.
LINE DRUGS

Fluoroquinolones Injectable drugs Other oral drugs

Ethionamide
Ofloxacin Prothionamide
Levofloxacin Kanamycin Cycloserine
Moxifloxicin Amikacin Terizidone
Ciprofloxacin Capreomycin PAS
Rifabutane
Rifapentane
 Fluoroquinolones:-
Ofloxacin,Levofloxacin,Moxifloxicin
Ciprofloxacin

MECHANISM OF ACTION

Fluoroquinolones bind to topoisomerase IV.

Inhibitis gyrase activity.
DNA cleavage.
Inability to repair DNA.
Broken DNA strands.
Cessation of DNA replication.
CELL DEATH
PHARMACOKINETICS:-

• ADMINISTERED BY ORAL, IV OR TOPICAL ROUTE.

• IT IS WELL ABSORBED FROM GUT BUT FOOD DELAYS ITS ABSORBTION.
• IT IS WIDELY DISTRIBUTED IN THE BODY AND REACHES HIGH CONC IN KIDNEY,
LUNG, PROSTATIC TISSUE, BILE, MACROPHAGE, ETC.
• IT IS EXCREATED MAINLY IN URINE.
USES OF FLOROQUINOLONES:-

• MULTIPLE DRUG RESISTANT TB.

• ATYPICAL MYCOBACTERIAL INFECTION.

• M.AVIUM COMPLEX (MAC INFECTION IN AIDS AND LEPROSY PATIENT)

• OTHER USES:- UTI, PROSTATITIS, BACTERIAL DIARRHEA, TYPHOID FEVER,

ANTHRAX.
ADVERSE EFFECTS:-
• GIT:- Nausea, vomiting, abdominal discomfort.
• CNS:- Headache, dizziness, insomnia, confusion, convulsion.
• Hypersensitivity Reaction:- skin rashes, urticaria, itching, photosensitivity.periferal

• CONTRA INDICATED in preagnancy and children less then 18 years because they cause
damage to cartilage and tendon.
• FDA(Food and drug agency) has given a black box warning against FQ regarding their
neurological side effect which include seizures and peripheral neuropathy.
• The risk of seizures increase when taken with NSAIDS.
 INJECTABLE DRUGS
KANAMYCIN, AMIKACIN, CAPREOMYCIN.
 KANAMYCIN/AMIKACIN
• These aminoglycoside antibiotics are very similar to streptomycin in
antitubercular activity, pharmacokinetic properties and types of adverse effects.
• Many S resistant and MDR strains of M. tuberculosis remain sensitive to them.
• One of these is mostly included in the regimen for MDR-TB during the intensive
phase.
• The RNTCP standardized regimen for MDR-TB include KANAMYCIN but in many
countries AMIKACIN is preffered, because it is considered less toxic.
PHARMACOKINETICS:-

• Absorption:
• Kanamycin is not absorbed significantly from the gastrointestinal tract when
taken orally, so it is typically administered via intramuscular or intravenous
injection.
• Distribution:
• After intramuscular or intravenous administration, kanamycin is distributed
throughout the body. It can cross into various tissues and fluids, including the
cerebrospinal fluid, but its distribution may be somewhat limited in some tissues.
• Metabolism:
• Kanamycin is not metabolized in the body. It is excreted mostly unchanged in the
urine.
USES OF KANAMYCIN/AMIKAYCIN:-

• Drug-Resistant TB: Kanamycin is considered a second-line drug for the treatment

of drug-resistant tuberculosis, including multidrug-resistant tuberculosis (MDR-
TB) and extensively drug-resistant tuberculosis (XDR-TB).
• It is typically used when other first-line and second-line drugs have proven
ineffective or when there is documented susceptibility to kanamycin.
• Combination Therapy: Kanamycin is often used in combination with other
second-line anti-TB drugs as part of a comprehensive regimen. Combining
multiple drugs with different mechanisms of action is essential to increase the
effectiveness of treatment, reduce the risk of resistance, and improve the
chances of successful TB therapy.
ADVERSE EFFECTS:-

• Nephrotoxicity.
• Ototoxicity: Hearing defect
• Neurotoxicity.
• Gastrointestinal Disturbances.
• Allergic Reactions.
• Hypersensitivity Reactions.
 CAPREOMYCIN:-
• PHARMACOKINETICS:-
• Administration:
• Capreomycin is typically administered by intramuscular injection (IM). This route of
administration ensures that the drug is efficiently absorbed into the bloodstream.
• Absorption:
• After intramuscular injection, capreomycin is slowly and incompletely absorbed from
the injection site.
• Distribution:
• Capreomycin is distributed throughout the body, including into tissues and body fluids,
but its penetration into some tissues may be limited.
• Metabolism:
• Capreomycin is not metabolized in the body. It is administered in its active form.
• Elimination:
• Capreomycin is primarily eliminated through the kidneys. A significant portion of the
drug is excreted unchanged in the urine.
• USES:-
• Capreomycin is used to treat tuberculosis, particularly when the TB strain is
resistant to other first-line and second-line drugs.
• It is often employed as part of a combination therapy, meaning it is used in
conjunction with other anti-TB drugs to enhance the treatment's effectiveness
and reduce the risk of developing resistance.

• ADVERSE EFFECTS:-
• Capreomycin, like other anti-TB drugs, can have side effects. Common adverse
effects include kidney toxicity, hearing loss (ototoxicity), and balance problems
(vestibular toxicity).
• Renal function should be monitored regularly during capreomycin treatment, and
it is important to perform hearing assessments to detect any signs of ototoxicity.
• Gastrointestinal disturbances, such as nausea and vomiting, can also occur.