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PYRAZINAMIDE

Quick Overview

Our aim is to reach out to the globe within shortest possible time frame. 


 


To promote this objective, not only we distribute and market our Anti-Tuberculosis range of products globally through our distribution channels but we also undertake ‘contract manufacturing’& ‘formulation development ’of our wide range of generic products such as Pyrazinamide tablet which contains Pyrazinamide BP 500 mg tablet

PYRAZINAMIDE

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Details

COMPOSITION:

Each uncoated tablet contains:

Pyrazinamide BP                        500 mg

Excipients                                    q.s.

CHEMISTRY: Pyrazine-2-carboxamide

CATEGORY: Antituberculous agent

PHARMACOLOGY

PHARMACODYNAMICS:

Pyrazinamide may be bacteriostatic or bactericidal against Mycobacterium tuberculosis depending on the concentration of the drug attained at the site of infection. The mechanism of action is unknown. In vitro and in vivo studies have reported that the drug is active only at a slightly acidic pH.

PHARMACOKINETICS:

Absorption: Pyrazinamide is well absorbed from the GI tract and attains peak plasma concentrations within 2 hours.

 

Distribution: It is widely distributed in body tissues and fluids including the liver, lungs and cerebrospinal fluid (CSF). Pyrazinamide is approximately 10% bound to plasma proteins.

The half-life (t1/2) of Pyrazinamide is 9 to 10 hours in patients with normal renal and hepatic function.

Metabolism: Pyrazinamide is hydrolyzed in the liver to its major active metabolite, pyrazinoic acid. Pyrazinoic acid is hydroxylated to the main excretory product, 5-hydroxypyrazinoic acid.

Elimination: Approximately 70% of an oral dose is excreted in the urine, mainly by glomerular filtration within 24 hours.

INDICATIONS:

Pyrazinamide tablets are indicated for the initial treatment of active tuberculosis in adults and children when combined with other antituberculous agents.

It is also indicated after treatment failure with other primary drugs in any form of active tuberculosis.

Pyrazinamide tablets should only be used in conjunction with other effective antituberculous agents.

DOSAGE AND ADMINISTRATION:

Pyrazinamide tablets should always be administered with other effective antituberculous drugs.

It is administered for the initial 2 months of a 6-month or longer treatment regimen for drug-susceptible patients. Patients who are known or suspected to have drug-resistant disease should be treated with regimens individualized to their situation.

Pyrazinamide tablets frequently will be an important component of such therapy.

Patients with concomitant HIV infection may require longer courses of therapy.

 

Usual dose: Pyrazinamide tablets is administered orally, 15 to 30 mg/kg once daily. Older regimens employed 3 or 4 divided doses daily, but most current recommendations are for once a day. Three grams per day should not be exceeded.

Alternatively, a twice weekly dosing regimen (50 to 75 mg/kg twice weekly based on lean body weight) has been developed to promote patient compliance with a regimen on an outpatient basis.

Recommended Drugs for the Initial Treatment of Tuberculosis in Children and Adults

Daily Dose

Drug                                                       Children                                                           Adults

Pyrazinamide                                         15 to 30 mg/kg                                                 15 to 30 mg/kg

                                                                PO                                                                    PO

 

Maximal Daily Dose in Children and Adults

Drug

Pyrazinamide 2 g

 

Twice Weekly Dose

Drug                                                     Children                                             Adults

Pyrazinamide                                       50 to 70 mg/kg                                 50 to 70 mg/kg                                          

Definition of abbreviations: PO=per orally

 

CONTRAINDICATIONS:

Pyrazinamide tablets are contraindicated in persons:

  • With severe hepatic damage.
  • Who have shown hypersensitivity to it.
  • With acute gout.

WARNINGS AND PRECAUTIONS:

Patients started on Pyrazinamide tablets should have baseline serum uric acid and liver function determinations. Those patients with preexisting liver disease or those at increased risk for drug related hepatitis (e.g., alcohol abusers) should be followed closely.

Pyrazinamide tablets should be discontinued and not be resumed if signs of hepatocellular damage or hyperuricemia accompanied by an acute gouty arthritis appear.

PRECAUTIONS:

General:

Pyrazinamide tablets inhibit renal excretion of urates, frequently resulting in hyperuricemia which is usually asymptomatic. If hyperuricemia is accompanied by acute gouty arthritis, pyrazinamide should be discontinued.

Pyrazinamide tablets should be used with caution in patients with a history of diabetes mellitus, as management may be more difficult.

Primary resistance of M. tuberculosis to pyrazinamide is uncommon. In cases with known or suspected drug resistance, in vitro susceptibility tests with recent cultures of M. tuberculosis against pyrazinamide and the usual primary drugs should be performed. There are few reliable in vitro tests for pyrazinamide resistance. A reference laboratory capable of performing these studies must be employed.

INTERACTIONS:

Probenecid is known to block the excretion of pyrazinamide.

PREGNANCY AND LACTATION:

Pregnancy Category C

Animal reproduction studies have not been conducted with pyrazinamide. It is also not known whether pyrazinamide can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Pyrazinamide tablets should be given to a pregnant woman only if clearly needed.

Nursing Mothers:

Pyrazinamide has been found in small amounts in breast milk. Therefore, it is advised that Pyrazinamide tablets be used with caution in nursing mothers taking into account the risk-benefit of this therapy.

Pediatric Use:

Pyrazinamide tablets regimens employed in adults are probably equally effective in children. Pyrazinamide appears to be well tolerated in children.

Effect to Drive & Use the Machine:

No studies on the effects on the ability to drive and use machines have been performed. Nevertheless Pyrazinamide tablets can cause headache and dizziness and may impair the ability to drive and to use machines.

 

ADVERSE DRUG REACTIONS:

General:

Fever, porphyria and dysuria have rarely been reported.

 

Gastrointestinal:

The principal adverse effect is a hepatic reaction. Hepatotoxicity appears to be dose related, and may appear at any time during therapy. GI disturbances including nausea, vomiting and anorexia have also been reported.

Hematologic and Lymphatic:

Thrombocytopenia and sideroblastic anemia with erythroid hyperplasia, vacuolation of erythrocytes and increased serum iron concentration have occurred rarely with this drug. Adverse effects on blood clotting mechanisms have also been rarely reported.

 

Other:

Mild arthralgia and myalgia have been reported frequently. Hypersensitivity reactions including rashes, urticaria, and pruritis have been reported. Fever, acne, photosensitivity, porphyria, dysuria and interstitial nephritis have been reported rarely.

 

OVERDOSAGE:

Over dosage experience is limited. In one case report of overdose, abnormal liver function tests developed. These spontaneously reverted to normal when the drug was stopped. Clinical monitoring and supportive therapy should be employed. Pyrazinamide is dialyzable.

PRESENTATION: Blister of 10 tablets

STORAGE: Store in a cool and dry place. Protect from light. 

 
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