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First line drugs

Isoniazid

Rifampicin

Etambutol

Pyrazinamide

Second line drugs

Clarithromycin

Ciprofloxacin

Cycloserine

Kanamycin

Amikacin

Streptomycin

Isonaizid

Isoniazid is the hydrazide of isonicotinic acid.

Available pharmaceutical dosage form:

oral solid dosage form: uncoated tablets(50mg,100mg,300mg)

oral liquid dosage form: syrup(50mg/5mL)

parenteral: Intravenous, Intramuscular(100mg/mL)

Spectrum and Indications

Isoniazid is bactericidal in action

Active against:

Mycobacterium tuberculosis

Mycobacterium kansaii

Mycobacterium avium-intracellulare
Indications:

active tuberculosis

latent tuberculosis

Contraindication:

Diabetes mellitus

Hypersensitive patient

Epileptic patient

Severe liver problems

Precautions:

Minimize alcohol consumption while taking isoniazid, because alcohol can reduce the effectiveness of
this medication and increase side effect.

Isoniazid should be used in caution if patient is suffering with kidney or liver problems, diabetes mellitus.

Pregnancy And Lactation:

Pregnancy Category: C

Lactation: distributed into milk but safe for nursing infants

Side Effects:

Hepatitis (more risk in >35 years old)

peripheral neuropathy

pyridoxine deficiency

Epigastric distress

convulsions

hematologic abnormalities (granulocytosis, thrombocytopenia)

hypersensitivity reactions

Overdose Effects:

The ingestion of toxic amounts of isoniazid causes:

recurrent seizures
profound metabolic acidosis

coma and even death.

Pharmacological Properties

Mechanism of Action:

Isoniazid is a prodrug activated by a mycobacterial enzyme catalase-peroxidase(KatG). Isoniazid targets


the enzyme acyl carrier protein reductase(InhA) and beta ketoacyl-ACP synthase(KasA), which are
essential for the synthesis of mycolic acid. Inhibiting mycolic acid synthesis leads to disruption in
bacterial cell wall.

Pharmacokinetic Properties:

Absorption:

Oral absorption of Isoniazid is found to be 95.5% ±4.5.

Distribution:

The drug is distributed to all body fluids, cells and tissues and reaches intracellular concentration
sufficiently high to be effective against organisms inside cells and caseous leisions.

Side Effects:

Hepatitis (more risk in >35 years old)

peripheral neuropathy

pyridoxine deficiency

Epigastric distress

convulsions

hematologic abnormalities (granulocytosis, thrombocytopenia)

hypersensitivity reactions

Overdose Effects:

The ingestion of toxic amounts of isoniazid causes:

recurrent seizures

profound metabolic acidosis

coma and even death.


Pharmacological Properties

Mechanism of Action:

Isoniazid is a prodrug activated by a mycobacterial enzyme catalase-peroxidase(KatG). Isoniazid targets


the enzyme acyl carrier protein reductase(InhA) and beta ketoacyl-ACP synthase(KasA), which are
essential for the synthesis of mycolic acid. Inhibiting mycolic acid synthesis leads to disruption in
bacterial cell wall.

Pharmacokinetic Properties:

Absorption:

Oral absorption of Isoniazid is found to be 95.5% ±4.5.

Distribution:

The drug is distributed to all body fluids, cells and tissues and reaches intracellular concentration
sufficiently high to be effective against organisms inside cells and caseous leisions.

Elimination:

Pharmaceutical Particulants

List Of Excipients:

The active substance in Isoniazid Tablets BP is isoniazid.

The other ingredients in Isoniazid are

lactose 170 mesh

microcrystalline cellulose

alginic acid (E400)

magnesium stearate

purified water.

Incompatibilities

Not Applicable

Shelf Life:

2 years

Special Precaution For Storage:


For blister pack:

Do not store above 30℃.

protect it from light.

For bottle pack:

Do not store above 30℃. Protect from light, in tightly closed container.

Keep this medicine out of the sight and reach of children.

Do not use this medicine after the expiry date stated on the label.

Nature And Contents Of Container:

White to off-white, circular, biconvex, uncoated tablets, plain on both sides.

Blister pack Tablets are packed in PVC/PVDC-Alu blister of 10 or 28 tablets.

Bottle pack Tablets are packed in triple laminated pouch containing 500 or 1000 tablets, packed in HDPE
bottle with cap along with leaflet.

Special Precaution For Disposal And Other Handling:

Do not throw away any medicines in household waste

References

www.druginfocys.com

reference.medscape.com

www.drugs.com

www.medicines.org.uk0

Pharmacology Brenner and Stevens(5th edition)

British National Formulary

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