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Ciclosporin: Uses, Side Effects, Mechanism of Action

What is Ciclosporin?

Ciclosporin (cyclosporine) is an immunosuppressant medication you take to prevent organ rejection after a transplant (e.g., kidney, liver) or treat autoimmune conditions like rheumatoid arthritis, psoriasis, or severe eczema. It works by blocking T-cell activation, reducing your immune system’s response.

How Does Ciclosporin Work?

Ciclosporin works by suppressing your immune system. It binds to a protein called cyclophilin, forming a complex that inhibits calcineurin, an enzyme necessary for activating T-cells. Without active T-cells, the production of interleukin-2 and other cytokines decreases, reducing your body’s immune response. This mechanism helps prevent organ rejection in transplant patients and controls symptoms in autoimmune diseases.

What are the Uses of the Ciclosporin?

Ciclosporin is an immunosuppressant medication primarily used to prevent organ rejection after a transplant. It works by reducing the activity of your immune system, preventing it from attacking the transplanted organ. Doctors prescribe it for kidney, liver, and heart transplants, among others. 

In autoimmune diseases, ciclosporin is used to manage conditions where your immune system mistakenly attacks your body. It is effective in treating severe psoriasis, rheumatoid arthritis, and atopic dermatitis. For psoriasis, ciclosporin helps control skin inflammation, while in rheumatoid arthritis, it reduces joint damage and pain. 

In ophthalmology, ciclosporin eye drops are used to treat dry eye syndrome, particularly in cases caused by inflammation, such as keratoconjunctivitis sicca. It improves tear production and reduces eye irritation.

What are the Side Effects of the Ciclosporin?

Ciclosporin can cause side effects, especially if you take it for a long time or at high doses. The most common side effects include kidney damage, high blood pressure, and increased risk of infections due to its immunosuppressive effects. Regular blood tests are necessary to monitor kidney function and drug levels.

Common Side Effects

  • Kidney Toxicity
  • High Blood Pressure 
  • Infections 
  • Gum Overgrowth 
  • Increased Hair Growth (Hirsutism) 

Less Common but Serious Side Effects

  • Liver Damage 
  • Neurological Effects 
  • Electrolyte Imbalances 
  • Gastrointestinal Issues

Who Shouldn’t Use Ciclosporin?

You should not use ciclosporin if you have certain medical conditions or risk factors that could lead to serious complications. This medication suppresses your immune system, so it requires careful monitoring.

People with Uncontrolled High Blood Pressure

Patients with Severe Kidney Disease

Individuals with Active Infections 

People with Liver Disease

Patients with a History of Cancer

Pregnant or Breastfeeding Women

People with Severe Uncontrolled Inflammatory Conditions 
 
Individuals Taking Certain Medications

Does Ciclosporin Interacts with Foods and Drinks?

Ciclosporin can interact with specific foods and drinks, affecting how well the medication works in your body. Here are the key interactions: 

Grapefruit and Grapefruit Juice: These contain compounds that inhibit CYP3A4 enzymes. This interaction can increase ciclosporin levels by up to 200%, heightening the risk of side effects like kidney damage and high blood pressure. 

High-Potassium Foods: Since ciclosporin may raise potassium levels, consuming too many potassium-rich foods (such as bananas, oranges, and leafy greens) can lead to hyperkalemia. Elevated potassium may cause irregular heart rhythms and muscle weakness. 

Alcohol: Drinking alcohol can stress your liver, potentially reducing ciclosporin metabolism. This may lead to increased side effects like high blood pressure and liver toxicity. 

Dairy Products: Some studies suggest that taking dairy products with ciclosporin can lower its absorption. It is advisable to take your medication at least one hour before or two hours after dairy consumption. 

Caffeine: Because ciclosporin can increase blood pressure, high intake of caffeine (from coffee, tea, energy drinks, or chocolate) may worsen this effect.

What are the Ciclosporin Tablets Available in Pakistan?

In Pakistan, several brands of Ciclosporin tablets (capsules) are available, primarily used as immunosuppressants. Here are some notable options:

Cipol-N (50 mg): This brand contains cyclosporin and is used for its immunosuppressive effects, particularly in organ transplant cases. It is available in packs of 50 capsules1.

Sandimmun Neoral (100 mg): Another widely recognized brand, Sandimmun Neoral 100mg is utilized to prevent organ rejection post-transplant. It is also available in packs of 50 capsules26.

Bioral (25 mg and 50 mg): Bioral capsules are available in both 25 mg and 50 mg dosages, catering to different patient needs53.

Imun Heoral (50 capsules): Manufactured by Crystolite, this brand provides cyclosporin in a soft gelatin capsule form, ensuring quality assurance

Eltrombopag 1
CategoriesBlog

Eltrombopag: Uses, Side Effects and Mechanism of Action

What is Eltrombopag?

Eltrombopag is a medication used to treat low platelet counts in certain blood disorders. It works by stimulating your bone marrow to produce more platelets, reducing the risk of bleeding. You might take it if you have conditions like immune thrombocytopenia, chronic hepatitis C-related thrombocytopenia, or severe aplastic anemia. Typically taken as an oral tablet once daily, its dosage depends on your specific condition and medical guidance. While it helps manage symptoms, it isn’t a cure and may have side effects like headaches or liver issues. Always follow your healthcare provider’s instructions, as Eltrombopag requires regular monitoring.

How Does Eltrobopag Work?

Eltrombopag works by mimicking your body’s natural thrombopoietin, a protein that signals your bone marrow to produce platelets. It binds to and activates thrombopoietin receptors, encouraging stem cells to develop into mature platelets. This helps increase platelet counts if you have disorders where your body doesn’t make enough platelets naturally. Unlike treatments that suppress your immune system, Eltrombopag directly targets platelet production. Its effects are dose-dependent, requiring regular blood tests to ensure optimal levels and avoid overproduction.

What are the Side Effects of the Eltrobopag Tablet?

Eltrombopag tablets may cause side effects, which can vary in severity. Common side effects include: 

  • Nausea 
  • Headache 
  • Dizziness 
  • Fatigue 
  • Diarrhea 
  • Loss of appetite 
  • Muscle or joint pain 

Serious side effects may include: 

  • Liver problems (yellowing of skin or eyes, dark urine, abdominal pain) 
  • Blood clot risk (swelling, chest pain, trouble breathing) 
  • Eye problems (blurry vision, cataracts) 
  • Unusual bruising or bleeding

What are the Warning & Precautions of the Eltrombopag Tablets?

Warnings & Precautions for Eltrombopag Tablets

Liver Problems:

Eltrombopag can increase liver enzyme levels, leading to liver damage. 

You should have regular liver function tests. 

Contact your doctor if you notice yellowing of the skin/eyes, dark urine, or abdominal pain.

Blood Clot Risk:

Eltrombopag may increase the risk of blood clots, especially in people with certain conditions. 

Watch for symptoms like swelling, chest pain, or difficulty breathing.

Eye Problems:

Some people may develop cataracts or vision changes. 

Regular eye check-ups are recommended.

Bleeding Risks After Stopping the Medication:

Stopping Eltrombopag suddenly can lower platelet levels, increasing the risk of severe bleeding. 

Follow your doctor’s instructions when discontinuing the medication.

Iron Absorption Issues:

Eltrombopag can lower iron levels in your body. 

Your doctor may monitor iron levels if needed.

Avoid Certain Foods and Supplements:

Calcium-rich foods (like dairy products) can interfere with absorption. 

Take Eltrombopag at least 2 hours before or 4 hours after consuming dairy, antacids, or supplements containing calcium, magnesium, or aluminum.

Use in Pregnancy and Breastfeeding:

The safety of Eltrombopag in pregnancy is not well-established. 

If you are pregnant or planning to conceive, consult your doctor. 

It is unknown if Eltrombopag passes into breast milk, so discuss breastfeeding with your doctor. 

What Foods Should You Avoid When Taking Eltrombopag? 

When taking eltrombopag, you should avoid foods or supplements high in calcium, iron, aluminum, magnesium, or zinc within 4 hours of your dose, as they can reduce its effectiveness. This includes dairy products (like milk or yogurt), iron-fortified cereals, red meat, spinach, and antacids containing these minerals. Take eltrombopag on an empty stomach, either 1 hour before or 2 hours after meals, unless your doctor advises otherwise. Always check labels of fortified foods or supplements and consult your healthcare provider for tailored guidance.

How Long Can you take Eltrombopag Tablet for?

The duration of eltrombopag treatment varies based on your condition, how you respond to the medication, and your doctor’s monitoring. For chronic immune thrombocytopenia (ITP), for example, eltrombopag is often used as long-term, maintenance therapy. Clinical studies have shown that patients may take it for several years with a median duration around 2 to 3 years and some cases extending up to 8 years. Your doctor will regularly check your blood counts and liver function and adjust your treatment plan as needed.

What are the Eltrombopag Tablets Available in Pakistan?

Eltrombopag is available in Pakistan under various brand names and formulations. Here are the primary options including revolade, Elbonix, and Elopag. Here are the details for each of them below.

Revolade: 

Dosages: Available in 25 mg and 50 mg tablets. 

Pack Size: Typically sold in packs of 28 tablets. 

Manufacturer: GlaxoSmithKline. 

Indications: Used for treating low platelet counts in conditions like chronic immune thrombocytopenia (ITP) and thrombocytopenia related to hepatitis C134. 

Elbonix: 

Dosage: 50 mg tablets. 

Pack Size: Available in packs of 28 tablets. 

Indications: Similar to Revolade, it is used for managing chronic ITP, hepatitis C-related thrombocytopenia, and severe aplastic anemia2. 

Elopag: 

Dosage: 50 mg tablets. 

Indications: This brand is also used for treating thrombocytopenia in similar patient populations as Revolade and Elbonix 

 

 

Alteplase 1
CategoriesBlog

Alteplase: Uses, Side Effects & Mechanism of Action

What are the Uses of Alteplase?

Alteplase injection is a clot-dissolving medication used in life-threatening emergencies where blood flow is blocked. You may receive it for: 

Ischemic stroke (within 3–4.5 hours of symptoms) to restore brain blood flow and prevent permanent damage. 

Heart attack (STEMI type) to quickly reopen blocked heart arteries and minimize heart muscle injury. 

Severe pulmonary embolism to dissolve lung clots and improve breathing.

How Does Alteplase Injection Work?

Alteplase injection works by activating a protein in your blood called plasminogen, turning it into plasmin. Plasmin breaks down fibrin, the main component of blood clots. This process dissolves clots quickly, restoring blood flow to vital organs like your heart, brain, or lungs. You’ll receive it intravenously in emergencies, under close medical monitoring to balance clot-dissolving benefits with bleeding risks.

What are the Side Effects of the Alteplase Injection ?

While it is effective in treating conditions like acute ischemic stroke, myocardial infarction, and pulmonary embolism, it can also lead to various side effects. Understanding these side effects is crucial for you to recognize potential complications and seek timely medical attention.

Common Side Effects:

Bleeding: The most prevalent side effect of alteplase is bleeding, which can occur from puncture sites, gums, or as nosebleeds. You may also notice easy bruising or prolonged bleeding from cuts. 

Neurological Symptoms: Sudden headaches, dizziness, weakness, or numbness especially on one side of the body can indicate serious complications. You should seek immediate help if you experience slurred speech or balance issues. 

Gastrointestinal Issues: Symptoms such as bloody or tarry stools and vomiting blood may arise. Additionally, red or pink urine can be a sign of internal bleeding. 

Allergic Reactions: Rarely, you may experience hives, difficulty breathing, or swelling of the face and throat. These symptoms require urgent medical attention.

Serious Side Effects: 

Severe Bleeding: This includes internal bleeding in organs like the brain or gastrointestinal tract. If you notice any signs of severe bleeding that won’t stop, contact your healthcare provider immediately. 

Cardiovascular Symptoms: Chest pain, rapid weight gain, and significant changes in urination can indicate serious complications related to heart function. 

Pancreatitis: Severe upper abdominal pain that spreads to your back may signal pancreatitis, a rare but serious side effect.

When should alteplase be used?

Alteplase should be used only in emergencies to dissolve life-threatening blood clots, such as:

Ischemic stroke: You’ll receive it within 3–4.5 hours of symptom onset to restore brain blood flow. 

Heart attack (STEMI): It’s given promptly to reopen blocked heart arteries and limit heart damage. 

Severe pulmonary embolism: Used when clots in your lungs cause dangerously low oxygen levels or strain on the heart.

What are the Warnings & Precautions of the Alteplase Injection?

Alteplase injection is a potent thrombolytic agent used to dissolve blood clots in critical medical situations. While it can be lifesaving, there are important warnings and precautions you should be aware of to ensure safe administration and minimize risks.

Warnings and Precautions: 

Risk of Bleeding: Alteplase significantly increases the risk of severe or fatal bleeding. You should be monitored closely for any signs of bleeding, such as unusual bruising, prolonged bleeding from cuts, or blood in urine or stools. If you experience any bleeding that does not stop, seek immediate medical attention. 

Contraindications: Alteplase should not be administered if you have active internal bleeding, a history of recent stroke (within 3 months), or severe uncontrolled hypertension. Additionally, conditions such as brain tumors, aneurysms, or arteriovenous malformations can increase the risk of bleeding and are considered contraindications. 

Recent Surgeries or Trauma: If you have had major surgery or serious head trauma within the past three months, alteplase may not be suitable for you. It is essential to inform your healthcare provider about any recent medical procedures. 

Monitoring Requirements: Alteplase should only be administered in a hospital setting where appropriate monitoring is available. Your healthcare team will check your vital signs and watch for any complications during and after treatment. 

Allergic Reactions: Be aware of potential allergic reactions to alteplase. Symptoms may include hives, difficulty breathing, or swelling of the face and throat. If you notice any of these symptoms, seek emergency help immediately. 

Pregnancy and Breastfeeding: If you are pregnant or breastfeeding, inform your doctor before receiving alteplase. The effects on the fetus or infant are not fully understood, and careful consideration is necessary. 

How is Alteplase Injection given?

Alteplase injection is given intravenously (through a vein) in a hospital or emergency setting. You’ll receive it as follows: 

For stroke: A calculated dose based on your weight, with 10% given as a quick “bolus” and the rest infused over 1 hour. 

For heart attack: A total dose infused over 1.5–3 hours, depending on hospital protocols. 

For pulmonary embolism: A 2-hour infusion, adjusted for your condition. 

Your healthcare team will insert an IV line, monitor you closely for bleeding, and avoid other injections or procedures during treatment to reduce risks.

What are the Injection Available for the Alteplase in Pakistan?

In Pakistan, the primary injection available for alteplase is Actilyse. but it may require a prescription. It’s important to consult healthcare providers for proper guidance on its use and administration.

 

Ganciclovir 1
CategoriesBlog

Ganciclovir: Types, Uses, Side effects and Mechanism of Action

What are the Uses of Ganciclovir?

Ganciclovir is primarily used to treat and prevent cytomegalovirus (CMV) infections in immunocompromised individuals, such as those with HIV/AIDS (CD4 count <50 cells/mm³), organ transplant recipients, or chemotherapy patients. Key uses include: 

CMV retinitis: Administered via intraocular implant (4.5 mg sustained release) or systemic therapy to prevent vision loss. 

CMV colitis/pneumonia: Intravenous (IV) dosing (5 mg/kg every 12 hours for 14–21 days) for active infections. 

Preemptive therapy: Oral valganciclovir (900 mg daily), a prodrug with 60% bioavailability, prevents CMV reactivation post-transplant. 

How Does Ganciclovir Work ?

Ganciclovir works by selectively inhibiting viral DNA replication in cytomegalovirus (CMV) and related herpesviruses. As a synthetic guanosine analog, it undergoes a three-step phosphorylation process: first by the viral UL97 kinase (specific to CMV-infected cells), then by host kinases, forming ganciclovir triphosphate. This active form competes with natural dGTP, incorporating into viral DNA during replication. 

Once integrated, ganciclovir’s lack of a 3′-hydroxyl group prevents DNA chain elongation, causing premature termination. Its triphosphate form has a prolonged intracellular half-life (~18–24 hours), sustaining antiviral activity with fewer doses. 

You’ll see higher selectivity for CMV because UL97 kinase activation occurs predominantly in infected cells, minimizing harm to healthy ones. However, this mechanism still risks toxicity in dividing human cells (e.g., bone marrow), explaining side effects like neutropenia (~40% incidence).

What are the Side Effects of Ganciclovir?

Ganciclovir commonly causes bone marrow suppression and gastrointestinal issues. Key side effects include: 

Neutropenia (low white blood cells) in ~40% of patients, raising infection risk. 

Thrombocytopenia (low platelets) in ~20%, increasing bleeding tendency. 

Anemia (low red blood cells) in ~19%. 

Nausea/vomiting (20%) or diarrhea (15%). 

Severe risks involve renal toxicity (10–15% incidence) requiring dose adjustments if creatinine clearance is <80 mL/min, and seizures (~5%), especially with IV use. You may also experience fever (10%) or elevated liver enzymes (8%). 

Rarely, allergic reactions (rash, anaphylaxis) or central nervous system effects (confusion, headache) occur. 

Who Shouldn’t Use Ganciclovir?

Ganciclovir is contraindicated in specific groups due to toxicity risks: 

Hypersensitivity: You should avoid it if you’ve had allergic reactions (e.g., anaphylaxis) to ganciclovir, valganciclovir, or acyclovir (cross-reactivity risk <1%). 

Pregnancy: Category C animal studies show fetal abnormalities. Use contraception during and for ≥90 days post-treatment. 

Severe neutropenia (ANC <500 cells/μL) or thrombocytopenia (platelets <25,000/μL): Ganciclovir worsens bone marrow suppression (neutropenia occurs in ~40% of users). 

Severe renal impairment (creatinine clearance <10 mL/min): Dose adjustments are insufficient; hemodialysis clears only ~50% of the drug.

What are the Available Tablets of Ganciclovir in Pakistan?

In Pakistan, Valcyte 450mg tablets are available, which contain the active ingredient ganciclovir in the form of valganciclovir. Valganciclovir is converted into ganciclovir in the body. These tablets are primarily used to treat or prevent cytomegalovirus (CMV) infections, particularly in patients with weakened immune systems, such as those with AIDS or organ transplant recipients.  
 

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