Anti tb drugs dr-z pharmacy practice

PATIENT PROFILE & PATIENT COUNSELING
C. DRUG PROFILE OF ATLEAST 25 IMPORTANT
MEDICATIONS
3. ANTI TUBERCULAR DRUGS
CLINICAL PHARMACY
BY
Zul Kamal
DEPARTMENT OF PHARMACY
SHAHEED BENAZIR BHUTTO UNIVERSITY,
SHERINGAL

C. DRUG PROFILE OF ATLEAST 25 IMPORTANT MEDICATIONS
TUBERCULOSIS (TB)
 TB is caused by several types of mycobacteria, usually Mycobacterium
tuberculosis (Aerobic Gram Positive).
 The disease usually attacks the lungs, but it can also affect other parts of the
body.
Slow-growing bacillus Dormant forms in macrophages

TUBERCULOSIS (TB) …
HOW IT SPREAD?
The bacteria can travel through the air and spread
from one person to the next. This happens when
infected people cough, sneeze, or spit.
Between five and ten people show symptoms, for
every hundred people infected. In these people, the
disease is called active.
Kill 2 million people each year
Increase incidence due to HIV associated Mycobateria
Prevalence of TB in Sri Lanka is 79 per 100 000
population

TUBERCULOSIS (TB) …
70 years ago drugs were developed
Now multi- drug resistance strains are emerging

ANTI-TUBERCULOUS DRUGS
First-line
– Isoniazid
– Rifampicin
– Ethambutol
– Pyrazinamide
NOTE: more effective and
less toxic then line 2nd)
Second-line
– Clarithromycin
– Ciprofloxacin
– Capreomycin
– Cycloserine
– Kanamycin
– Amikacin
– streptomycin
NOTE: These drugs are not
recommended in 1st stage but
if the body doesn’t response
to 1st line than these are
administered. More toxic and
comparatively less effective.

ANTI-TUBERCULAR DRUGS (TB) …
ISONIAZID (Iso- nicotinic acid hydrazide INH)
PHARMACOKINETICS
ADMINISTRATION
 Oral
 IM
METABOLISIM
 Metabolized in liver via acetylation.
NOTE: Will be determined genetically; People who acetylate it
fast are called Fast Acetylators will required high dose of
drugs, while those who acetylate it slowly are called Slow
acetylators and will required low amount).

PHARMACODYNAMICS
MECHANISIM OF ACTION
 INH inhibit the synthesis of Mycolic acid which are essential
components of bacterial cell walls.
 INH is a pro-drug and for its activation the Mycobacterial
enzyme catalase per oxidases is required.
 In activated form INH form a covalent complex with the acyl
carrier protein which blocks Mycolic acid synthesis and kills
the cell.

INDICATIONS
 Tuberculosis
CONTRAINDICATION
 Liver diseases (a it is metabolized in liver by acetylation).
ADVERSE DRUG REACTION
 Neurotoxicity so must be given in combination with Vitamin B
6 (Paradoxin).
 Induction of Hepatitis.
 Hypersensitivity reaction like skin rashes.

DRUG INTERACTION
 As INH inhibits Cyt-P450 enzyme of liver; so drugs that are
concerns with these enzymes will not be metabolized e.g.
Phenytoin (Narrow therapeutic index drug).
 Also enhances the toxicity of Paracetamol.

BRAND
 Niazid (Pharma Wise) Tab, 100 mg
 Isoniazid (Geofman) Tab, 100 mg
 I.N.H (Lisko Pharma), Tab, 100 and 300 mg
DOSAGE FORM
 Tablets and Injectables
DOSES
 300 mg/day (combination with other antibiotic because
microbes develop resistance against it))

2. RIFAMPICIN
TWO TYPES
Rifampicin A
Rifampicin B
NOTE: The Rifampicin which is used against TB is Rifampicin B;
which is mostly obtained from microorganism named
Streptomyces medditerranei

2. RIFAMPICIN…cont
PHARMACOKINETICS
 Administered Orally.
 Absorbed from GIT
 85% Protein bound.
 Metabolized by Liver
 Excreted via Bile
 NOTE: Entero-hepatic circulation (EHC)- drug passes through
GIT then to liver and then excreted in liver. Those drugs which
undergoes through EHC have high duration of action as
Rifampicin has the duration of action 24-hrs; very small
quantity of drug will excrete in urine)

PHARMACODYNAMICS
MECHANISM OF ACTION
 Rifampicin inhibits the enzyme RNA-Polymerses which blocks
the synthesis of RNA. This will result in inhibition of protein
synthesis of Mycobacterium tuberculosis results in death of
the bacteria.
INDICATIONS
 TB
 Leprosy
 Meningitis (Meningio cocci)

CONTRAINDIACTIONS
 Jaundice
 Porphyria (Abnormality in the heme synthesis of hemoglobin)
 Increase level of uric acid (gout)
ADVERSE DRUG REACTION
 Jaundice
 Hemolytic anemia
 Acute renal failure
 Thrombocytopenia (decrease level of platelets)
 Gives orange color to all body secretions e.g saliva, tears, urine and
sweat etc.
 Alopecia (Abnormal hair loss).

DRUG INTERACTIONS
 Rifampicin is an enzyme inducer so it will increase the
metabolism of drugs which are metabolized by Cyt-450 like
 Corticosteroids,
 Sulphonylurea,
 Oral anti coagulants,
so there Bioavailability will be decreased.

BRAND
 Lederrif (Wyeth) Tab, 300, 450, 600 mg
 Rimactal (Novartis) Cap: 300 mg, Tab: 400 mg, Syp: 600 mL
 Abrifam (Abbott), Tab 450, 600 mg
DOSE
450-600 mg OD, Befor breakfast.

Anti tb drugs dr-z pharmacy practice

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