Pyrazinamide

Pyrazinamide
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Pyrazinamide (PZA) is an antimicrobial agent that is most commonly used for treatment of active tuberculosis (TB) during the initial phase of therapy (generally the first two months of treatment), in combination with other agents. The spectrum of PZA is relatively narrow; it demonstrates clinically significant antibacterial activity only against Mycobacterium tuberculosis and Mycobacterium africanum.
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Zhejiang Haizhou Pharmaceutical Co., Ltd. : Your Professional Pyrazinamide Manufacturer !

Established in 1970, Zhejiang Haizhou Pharmaceutical Co., Ltd. is a leading pharmaceutical company focusing on specialized pharmaceuticals and fine chemicals.The company, located in Yanhai Industrial Park, one of the largest pharmaceutical industrial zones in China, covers an area of 35 acres. Through its three product segments including Guaiacol derivatives, Epichlorohydrin derivatives and Lodine contrast media, Haizhou Pharm offers a portfolio of products and services globally.

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Zhejiang Haizhou Pharmaceutical Co., Ltd. is a leading pharmaceutical company focusing on high-quality specialized pharmaceuticals and fine chemicals, including but not limited to: Active Pharmaceutical Ingredient (API), Intermediates, and API underdevelopment, which meet the highest quality requirements as stipulated in ISO9001/14001 and OHSAS18001.

 

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Haizhou Pharma is approved and registered by the relevant national departments. With advanced technology, excellent quality and perfect service we are in the front of pharmaceutical industry. Our products undergo NMPA (China FDA), US-FDA and EDQM certifications, ensuring product quality and safety.

 

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Haizhou Pharma is ISO9001/14001 and OHSAS18001 approved, and we follow ISO/OHSAS management philosophy throughout the whole poroduction process of our company. Moreover, our API production is in line with cGMP standard and approved by NMPA (China FDA), US-FDA and EDQM.

 

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We have many years of industry experience, a complete production management, quality supervision, and sales service operation system. Whether you want to purchase Active Pharmaceutical Ingredient (API) or Intermediates, just email your requirements and we can customize the product for you.

 

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What is Pyrazinamide?

 

 

Pyrazinamide (PZA) is an antimicrobial agent that is most commonly used for treatment of active tuberculosis (TB) during the initial phase of therapy (generally the first two months of treatment), in combination with other agents. The spectrum of PZA is relatively narrow; it demonstrates clinically significant antibacterial activity only against Mycobacterium tuberculosis and Mycobacterium africanum.

 

Factors to Consider Before Using Pyrazinamide

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

 

Pediatric
Pyrazinamide has been used in children and, in effective doses, has not been reported to cause different side effects or problems in children than it does in adults.

 

Geriatric
Many medicines have not been studied specifically in older people. Therefore, it may not be known whether they work exactly the same way they do in younger adults. Although there is no specific information comparing pyrazinamide in the elderly with use in other age groups, this medicine is not expected to cause different side effects or problems in older people than it does in younger adults.

 

Breast Feeding
There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

 

Drug Interactions
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. Using this medicine with Cyclosporine, Ethionamide, Rifampin, or Zidovudine is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

 

Other Interactions
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

 

Other Medical Problems
The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

  • Gout (history of)-Pyrazinamide may worsen or cause a gout attack in patients with a history of gout.
  • Liver disease (severe)-Patients with severe liver disease who take pyrazinamide may have an increase in side effects.

 

Proper Use of Pyrazinamide

To help clear up your TB completely, it is important that you keep taking this medicine for the full time of treatment, even if you begin to feel better after a few weeks. It is important that you do not miss any doses.

 

Dosing
The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

 

Timing of Your Dose
Take your pyrazinamide tablets once a day, at about the same time each day. You can take your dose with or without food. Swallow the tablets whole with a glass of water. If you have problems swallowing the tablets, they may be halved or crushed. Ask your pharmacist for advice.

 

Missed Dose
If you forget to take your dose, take it as soon as you remember. But if it's nearly time for your next dose, take the next dose at the right time. Don't take extra doses to make up for a forgotten dose. If you often forget to take pyrazinamide, your tuberculosis may not be fully treated.

 

Storage
You should store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. The medicine should be kept from freezing and be kept out of the reach of children. Do not keep outdated medicine or medicine no longer needed.

 

Finish the Course
Keep taking your tablets regularly unless your doctor tells you to stop. It's important you finish the course so the infection doesn't come back. If you stop taking the tablets before your course has finished, then you must let your doctor know about it straightaway so you can be given different treatment for your TB.

 

Pyrazinamide

Mechanism of Action

The mechanism of action for PZA is unknown. The parent compound enters the bacterium passively and is metabolized via pyrazinamidase (PZase) within the cytoplasm to pyrazinoic acid; pyrazinoic acid is the active form of the drug. PZA and its analog, 5-chloro-PZA, may inhibit the fatty acid synthetase I enzyme of M. tuberculosis. PZA is generally considered to be a bacteriostatic agent.

 

PZA is thought to be more active at an acidic pH (eg, within macrophages). It demonstrates activity against both replicating and slow-growing populations. The role of PZA against intracellular organisms remains uncertain. In one study, pyrazinoic acid remained outside of M. tuberculosis cells at a neutral or alkaline pH but accumulated within cells at an acidic pH. In the same study, Mycobacterium smegmatis (which is not susceptible to PZA) was found to convert PZA to pyrazinoic acid but, due to an active efflux mechanism, did not accumulate the metabolite, even at an acidic pH. Other mycobacterial strains appear to have natural resistance to PZA due to lack of PZase activity or absence of transport mechanisms to take up the drug.

 

Potential Side Effects of Pyrazinamide

 

Gastrointestinal
The principal adverse effect is a hepatic reaction. Hepatotoxicity appears to be dose related, and may appear at any time during therapy. Gl 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.

 

 
Frequently Asked Questions
 

Q: What is Pyrazinamide?

A: Pyrazinamide (PZA) is an antimicrobial agent that is most commonly used for treatment of active tuberculosis (TB) during the initial phase of therapy (generally the first two months of treatment), in combination with other agents. The spectrum of PZA is relatively narrow; it demonstrates clinically significant antibacterial activity only against Mycobacterium tuberculosis and Mycobacterium africanum.

Q: What are uses of pyrazinamide?

A: Pyrazinamide is used with other medications to treat tuberculosis (TB). It is an antibiotic and works by stopping the growth of bacteria.This antibiotic treats only bacterial infections. It will not work for viral infections (such as common cold, flu). Using any antibiotic when it is not needed can cause it to not work for future infections.

Q: How to use pyrazinamide?

A: Take this medication by mouth with or without food as directed by your doctor, usually once daily or twice weekly. The dosage is based on your age, weight, medical condition, and response to treatment. For the best effect, take this antibiotic at evenly spaced times. Continue to take this medication (and other TB medications) until the full prescribed amount is finished, even if symptoms disappear. Stopping the medication too early or skipping doses may result in a return of the infection and cause the infection to be more difficult to treat (resistant).

Q: What is dosage for pyrazinamide?

A: The usual dose of Pyrazinamide is 15 to 30 mg/kg once daily, taken orally. It should always be administered with other effective anti-tuberculosis drugs. It is administered for the initial 2 months of a 6-month or longer treatment regimen for drug-susceptible patients.

Q: What drugs, substances, or supplements interact with pyrazinamide?

A: Pyrazinamide may interact with allopurinol, or Acetest and Ketostix urine tests for ketones. Other drugs may interact with pyrazinamide. Tell your doctor all prescription or over-the-counter medicines and supplements you use.

Q: How long should I take pyrazinamide?

A: Treatment of active tuberculosis (TB) requires taking antibiotics for many months. Most people with active TB infection will need to take pyrazinamide along with three other anti-TB antibiotics for the first 2 months of treatment. This is called the "initial phase" of treatment. It's important to take pyrazinamide exactly as prescribed. Don't stop taking your TB medications unless instructed by your provider.

Q: Why are pyrazinamide and isoniazid taken together?

A: Pyrazinamide and isoniazid are taken together to prevent antibiotic resistance. Antibiotic resistance happens when the bacteria finds a way to survive and the antibiotics don't work well anymore to fight the infection as a result. This makes tuberculosis (TB) difficult to treat. Resistance to isoniazid is the most common type of TB antibiotic resistance. The best way to prevent antibiotic resistance is to use multiple antibiotics that work in different ways to fight against TB. This is why the first-choice treatment of an active TB infection consists of a combination of four medications - isoniazid with pyrazinamide, rifampin, and ethambutol (Myambutol).

Q: How does pyrazinamide cause high uric acid levels (hyperuricemia)?

A: Pyrazinamide blocks the kidneys' ability to get rid of uric acid from your body. This often causes uric acid to build up in the body, resulting in high uric acid levels. Having high uric acid levels doesn't usually cause problems, but it can sometimes lead to gout. Let your provider know if you experience any symptoms of gout, like pain or swelling at the joints, during treatment with pyrazinamide. They might want to check your uric acid levels.

Q: Can I take pyrazinamide during pregnancy?

A: If you're pregnant, speak with your provider about the risks and benefits of taking pyrazinamide. It's not known how safe the medication is if it's taken during pregnancy. But it's important to note that untreated TB can be harmful to you and your unborn baby. You should take pyrazinamide only if it's clearly needed.

Q: Can I take pyrazinamide if I'm breastfeeding?

A: If you're breastfeeding or planning on breastfeeding, speak with your provider about the risks and benefits of doing so while you're taking pyrazinamide. The CDC guidelines say that it's okay to breastfeed while you're taking first-choice treatment - Pyrazinamide together with rifampin, isoniazid, and ethambutol (Myambutol) - And if your provider considers you to be non-Infectious. Small amounts of pyrazinamide can be found in breast milk. But in general, there haven't been any reports of serious harm in nursing babies when their mother took TB medications while breastfeeding.

Q: What are the instructions for the storage and disposal of Pyrazinamide?

A: This medication should be kept in its original container, and should be stored at room temperature, as long as the room does not exceed 86°F. Make sure this medication remains unreachable to children and pets.

Q: How does Pyrazinamide work?

A: This medicine belongs to an antitubercular class of drugs. It works by inhibiting the growth of the organism by decreasing the pH inside the cell by converting it into an active metabolite called pyrazinoic acid in the presence of pyrazinamidase.

 

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