Penicillamine

Penicillamine is prescribed to help discharge excess copper related to Wilson's disease. It may also be prescribed to help minimize cystine in the urine or to help treat severe, active rheumatoid arthritis.

Cuprimine

Penicillamine

Atrmin, Penicitin, D-Penamine, Penicitin

10, 100

Panacea Biotec, Chandra Bhagat Pharma, Samarth Life Sciences

Capsules

125 mg, 250 mg

India

Penicillamine

I. Introduction

Brief History of Penicillamine

Penicillamine, commonly considered a chelation therapy component, can be traced back to the mid-20th century. It was initially derived as a byproduct of penicillin. It has since developed its therapeutic characteristics that set it apart from its original molecule.

Importance in Medical Therapeutics

Chelation ability: It effectively binds to metals and certain harmful substances, aiding their removal from the body. Properties that modify diseases are fundamental in conditions like rheumatoid arthritis as it helps regulate the progression of the disease. Going beyond symptom management, It tackles the root causes of various shapes.

Objective and Scope of the Article

This article aims to shed light on the nature of Penicillamine, delving into its composition, how it works, its uses, and possible side effects. The goal is to create a resource for medical professionals and anyone interested in understanding the pharmacological properties of this molecule.

II. Composition of Penicillamine

Chemical Structure

Penicillamine, also called β,β dimethylcysteine, has a thiol side chain that gives it its ability to chelate.

Formulations Available

Penicillamine is available in forms, including oral tablets and compounded creams, showcasing its versatility in different formulations. However, the standard way it is used is through capsules or tablets for systemic administration.

Stability and Solubility

Penicillamine, a compound that dissolves in water, needs to be stored to avoid moisture. Its stability depends on keeping it from light and following the recommended storage temperatures.

III. How Penicillamine Works

Mechanism of Action

Penicillamine is known for its ability to bind to metals and make them inactive. This binding process allows the complex to be eliminated from the body, thereby reducing the effects of the metal. Additionally, in conditions such as arthritis, it hinders specific cellular processes, which helps alleviate the severity of the disease.

Cellular Impact

The molecule disrupts the collagen cross-linking process, which impacts tissues' structure and makeup. This is particularly important in conditions such as scleroderma.

Therapeutic Effects

Chelation: Efficiently eliminates metals from the body. Anti-inflammatory; Adjusts immune responses to reduce inflammation. Tissue modification; Influences the characteristics of tissue.

IV. Approved Uses of Penicillamine

Treatment of Wilson's Disease

Wilson’s Disease is a genetic disorder that causes excessive copper accumulation in the liver, brain, and other organs. 1Penicillamine is a chelating agent that removes excess copper deposition from the body 123It binds with copper and helps remove it from the system, thereby preventing organ damage 1.

Here are some references that provide more information on Wilson’s Disease and Penicillamine:

  1. msn.com’s-disease/hp-Wilson’s-disease?source=conditioncdx): This website provides an overview of Wilson’s Disease, including its symptoms, diagnosis, and treatment options.
  2. Cleveland Clinic: This website provides detailed information on Wilson’s Disease, including its symptoms, causes, diagnosis, and treatment options.
  3. National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK): This website provides information on the treatment of Wilson’s Disease, including chelating agents such as Penicillamine.
  4. MSD Manual Professional Edition: This website overviews Wilson’s Disease, including its symptoms, diagnosis, and treatment options.
  5. Focus Medica’s-disease/hp-Wilson’s-disease?source=conditioncdx): This website provides an overview of Wilson’s Disease, including its symptoms, diagnosis, and treatment options.

Rheumatoid Arthritis Management

Penicillamine is a disease-modifying antirheumatic drug (DMARD) used to treat severe active rheumatoid arthritis in patients who have failed to respond to an adequate trial of conventional therapy 12It helps to decrease pain, tenderness, and swelling in the joints 3Penicillamine is known to suppress the immune system, which helps to stop it from attacking the tissues of the body and reduces the damaging effect of the disease on the joints 4.

Here are some references that provide more information on Penicillamine:

  1. WebMD: This website provides detailed information on Penicillamine, including its uses, side effects, interactions, and precautions.
  2. Cochrane Library: This website comprehensively reviews Penicillamine’s efficacy in treating rheumatoid arthritis.
  3. Medscape: This website provides detailed information on Penicillamine’s dosing, indications, interactions, adverse effects, and more.
  4. Patient.info: This website overviews Penicillamine’s uses and side effects.
  5. Drugs.com: This website provides detailed information on Penicillamine’s uses, dosage, side effects, and more.

Cystinuria Treatment

Penicillamine is a disease-modifying antirheumatic drug (DMARD) that is used to treat severe active rheumatoid arthritis in patients who have failed to respond to an adequate trial of conventional therapy 12. It helps to decrease pain, tenderness, and swelling in the joints . Penicillamine is also used to treat cystinuria, a rare genetic disorder characterized by the presence of cystine in urine 345It works by binding with cystine molecules and forming a soluble complex that can be excreted from the body, thereby preventing the formation of kidney stones 345.

Here are some references that provide more information on Penicillamine and its use in treating cystinuria:

  1. WebMD: This website provides detailed information on Penicillamine, including its uses, side effects, interactions, and precautions.
  2. National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK): This website overviews cystinuria, including its symptoms, diagnosis, and treatment options.
  3. Cleveland Clinic: This website provides detailed information on cystinuria, including its symptoms, causes, diagnosis, and treatment options.
  4. Mayo Clinic: This website overviews cystinuria, including its symptoms, diagnosis, and treatment options.
  5. Drugs.com: This website provides detailed information on Penicillamine’s uses, dosage, side effects, and more.

Heavy Metal Poisoning: Lead, Mercury, Copper

Penicillamine is a chelator used to treat Wilson’s disease, cystinuria, and rheumatoid arthritis 12It works by binding to metals such as copper and lead and removing them from the body 12Penicillamine decreases pain, tenderness, and swelling in the joints of patients with rheumatoid arthritis 1It also helps to reduce cystine excretion in cystinuria 1. To treat Wilson’s disease, penicillamine binds to copper and allows it to be eliminated in the urine. Decreasing copper levels helps to improve liver function and the mental/mood/nerve problems caused by the disease 1.

Here are some references that provide more information on penicillamine:

  1. WebMD
  2. GoodRx
  3. Medscape
  4. DrugBank Online

V. Off-Label Uses of Penicillamine

Scleroderma Management

Penicillamine is a chelator that is used to treat Wilson’s disease, cystinuria, and rheumatoid arthritis 12It works by binding to metals such as copper and lead and removing them from the body 12Penicillamine decreases pain, tenderness, and swelling in the joints of patients with rheumatoid arthritis 1It also helps to reduce cystine excretion in cystinuria 1. To treat Wilson’s disease, penicillamine binds to copper and helps it to be eliminated in the urine. Decreasing copper levels helps to improve liver function and the mental/mood/nerve problems caused by the disease 1.

Penicillamine has been used in the treatment of scleroderma due to its effects on tissue, which can help improve the texture and flexibility of the skin. Early open-label trials suggested that D-penicillamine was effective in scleroderma, resulting in improvements in skin thickening and in the progression of internal organ involvement 1. However, a large randomized controlled trial of low dose (62.5 mg daily) vs. high amount (750 mg daily) D-penicillamine failed to demonstrate significant differences in skin score, mortality, or incidence of renal crisis 1.

Here are some references that provide more information on penicillamine:

  1. Medscape
  2. WebMD
  3. GoodRx
  4. DrugBank Online

Systemic Lupus Erythematosus (SLE)

Penicillamine is a chelator that is used to treat Wilson’s disease, cystinuria, and rheumatoid arthritis 1 . It works by binding to metals such as copper and lead, and removing them from the body 1 . Penicillamine is known to decrease pain, tenderness, and swelling in the joints of patients with rheumatoid arthritis 1It also helps to reduce cystine excretion in cystinuria 1. For the treatment of Wilson’s disease, penicillamine binds to copper and helps it to be eliminated in the urine. Decreasing copper levels helps to improve liver function and the mental/mood/nerve problems caused by the disease 1.

Penicillamine has been studied as a potential treatment option for systemic lupus erythematosus (SLE) due to its ability to modulate the immune system. However, its use in this context is not officially approved and requires careful clinical assessment 2.

Here are some references that provide more information on penicillamine:

  1. Medscape
  2. Patient.info
  3. Europe PMC
  4. WebMD

Alzheimer’s Disease

Penicillamine has been investigated for its potential influence on the processes related to Alzheimer’s Disease. However, there is still a lack of evidence to draw any conclusive conclusions 1.

1: “Nasal Delivery of D-Penicillamine Hydrogel Upregulates a Disintegrin and Metalloprotease 10 Expression via Melatonin Receptor 1 in Alzheimer’s Disease Models.” Frontiers in Aging Neuroscience, vol. 13, 2021, doi: 10.3389/fnagi.2021.660249.

Other Investigative Applications

Penicillamine shows promise in therapeutic areas, including antiviral applications and potential roles in oncology. Its wide range of uses calls for further investigation and exploration.

VI. Dosage and Administration Guidelines

Standard Dosage Across Approved Indications

The required dosage can vary depending on the condition. For example, Wilson's disease may require a dosage compared to rheumatoid arthritis. It is crucial to follow the prescribed dosages.

Titration and Dose Adjustments

A commonly followed approach is starting with doses and gradually increasing them based on how the patient responds and tolerates the medication. In addition, if there are any kidney or liver issues, it may be necessary to adjust the dosage.

Frequency and Timing

Usually taken once a day, the effectiveness of its absorption can be affected by food. It's often recommended to take it on an empty stomach. However, the specifics may vary depending on the clinical situation.

Special Considerations: Hepatic and Renal Impairment

Both of these systems within the body have an impact on how Penicillamine is processed and distributed. As a result, if there are any issues or limitations with these systems, it can affect the dosage of the medication. This means careful monitoring and potential adjustments to the dosage may be needed.

VII. Drug Interactions with Penicillamine

Pharmacodynamic Interactions

Using this medication in combination with disease-modifying antirheumatic drugs (DMARDs) or immune suppressants could enhance specific effects, so it's important for doctors to be vigilant and closely monitor patients.

Pharmacokinetic Interactions

The absorption of penicillamine may be hindered by antacids and other medications, potentially reducing its effectiveness as a treatment.

Antacids and Mineral Supplements

It is recommended to administer them at times since they can attach themselves to Penicillamine, hindering its absorption.

Avoidance Strategies and Monitoring

Taking a stance means avoiding known interactive agents and regularly monitoring to ensure the therapy is effective and safe.

VIII. Common and Severe Side Effects

Gastrointestinal Upsets

The use of Penicillamine can lead to gastrointestinal issues such as nausea and diarrhea. To manage these effects, it may be necessary to make adjustments to the dosage or consider using medications alongside it.

Hematological Alterations

It has the potential to affect the blood cells, which can result in conditions such, as thrombocytopenia. It is essential to undergo blood tests to identify any issues at an early stage.

Dermatological Reactions

Rashes and dermatitis are some skin reactions that can occur when using Penicillamine.

Neurological Symptoms

The usage of this product may be associated with symptoms such as tremors or cognitive symptoms, like confusion. If you experience any of these, it is essential to seek medical attention.

IX. Warnings and Contraindications

Allergy and Hypersensitivity

People with a history of reactions, to Penicillamine, should avoid using it. There have been documented cases of skin problems and severe allergic reactions.

Liver Disease and Dysfunction

Extreme care should be taken when considering the use of Penicillamine for individuals with liver impairments. The presence of liver enzymes may indicate potential liver dysfunction shortly.

Renal Impairments

Renal clearance plays a role in how the drug is processed in the body. It is essential to take into account changes in dosage for patients with renal dysfunction. Regular monitoring of kidney function is necessary. Cannot be overlooked.

Blood Disorders

Thrombocytopenia, leucopenia, and other abnormalities in blood cell counts are side effects of Penicillamine treatment. In some cases, it may be necessary to discontinue the therapy.

X. Careful Administration and Important Precautions

Monitoring Liver and Kidney Function

It is not advisable but crucial to conduct regular tests to evaluate liver and kidney function, which is essential, for ensuring effective and safe treatment.

Routine Blood Tests

Regular blood tests are crucial to prevent complications. It is essential to monitor the levels of neutrophils and platelets.

Contraindicated Medications and Foods

It is advisable to avoid taking Penicillamine along with antacids and mineral supplements as they may reduce the effectiveness of the medication by binding with it.

XI. Special Populations

a. Administration to the Elderly

Dosing Adjustments: It is advisable to start with doses considering the reduced organ function often observed in elderly individuals. Monitoring, for Side Effects; It is essential to remain vigilant in order to promptly detect age-related susceptibility to reactions caused by medications.

b. Administration to Pregnant Women and Nursing Mothers

The FDA categorizes Penicillamine as Category D, which means there is a risk to the fetus. It is crucial to analyze the benefits and risks before using this drug and it should only be used if absolutely necessary.

c. Administration to Children

The dosage for children should be adjusted according to the severity of the illness and the child's weight. It is important to note that there is information available regarding the safety of this medication in pediatric populations, so it's best to proceed with caution.

XII. Overdose Management

Symptoms of Overdose

Symptoms can manifest as a decline in kidney function issues with muscle control and coordination, and intense discomfort, in the gastrointestinal tract.

Immediate Interventions

In case of an overdose, it is recommended to perform lavage promptly and administer activated charcoal. These measures can help reduce the effects of the overdose.

Antidotes and Supportive Care

There is currently no known antidote for this. Providing supportive care is essential. This includes administering fluids through a line and offering relief measures for symptoms.

XIII. Storage and Handling Precautions

Optimal Storage Conditions

Please keep the product stored at room temperature, ensuring it is protected from moisture and light to maintain its chemical stability.

Shelf-Life

Usually, the shelf life lasts for around 1 to 2 years. This can vary depending on how well it is stored.

Disposal Guidelines

Adhere to local pharmaceutical disposal guidelines to prevent any environmental detriments.

XIV. Conclusion

Summary of Key Points

The versatile abilities of Penicillamine highlight its role in modern medicine. However, there are considerations to keep in mind when using it, which require a personalized approach to treatment.

Clinical Relevance and Utility

The drug has a range of clinical applications, from treating Wilson's disease to rheumatoid arthritis. However, it is essential to administer it with discretion.

Future Research Avenues

Ongoing research has the potential to uncover possibilities for the drug leading to advancements in therapeutic treatments for various conditions such as neurodegenerative disorders and malignancies.

Rated: 5.0 / 5 based on 5.0 customer reviews.

Posted by Chalida on May 3, 2017 Verified Purchase

Penicillamine

Very good for chelate copper

Note: buy-pharma.md does not imply any medical claims from this review.

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