Combipack of Ambrisentant Tablets 5mg & Tadalafil Tablets 20mg
The Endobloc T Kit tablets combines two key components, Ambrisentan and Tadalafil, to treat pulmonary arterial hypertension (PAH).
Endobloc T Kit combination of two drugs:
- Ambrisentan 5 mg
- Tadalafil 20 mg
Tadalafil is classified as a phosphodiesterase-5 (PDE5) inhibitor, while Ambrisentan is an endothelin receptor antagonist. Their combined effect is to ease the blood vessels in the lungs. Refrain from taking this medication if you have an allergy to Ambrisentan, Tadalafil, or any of its components. It’s also advisable to avoid it if you suffer from liver issues or low blood pressure. Additionally, do not use this medicine if you are expecting a child or breastfeeding, use organic nitrates or GC stimulators, have experienced vision loss in one eye, or have idiopathic pulmonary fibrosis (IPF).
| Manufacturer: | CIPLA LTD |
| Country of Origin: | India |
| Treatment: | Pulmonary Arterial Hypertension (PAH) in adults |
| Pharma Form: | Tablet/s |
| Power: | 5mg + 20mg |
How does Endobloc T Kit work?
The Endobloc T Kit consists of a pair of medications: Ambrisentan and Tadalafil.
Ambrisentan 5 mg
Ambrisentan acts as an endothelin receptor antagonist. It functions by blocking the effects of endothelin, a naturally occurring substance that causes the narrowing of blood vessels. This narrowing elevates the pressure in the pulmonary blood vessels. Consequently, ambrisentan helps to relax these blood vessels, enhancing the flow of blood to the lungs.
Tadalafil 20 mg
Tadalafil belongs to the category of phosphodiesterase-5 (PDE5) inhibitors. PDE5 is a compound present in the lungs and other body regions. By reducing the activity of PDE5, tadalafil promotes the relaxation and expansion of blood vessels within the lungs. This process diminishes the pulmonary blood pressure by easing and enlarging blood vessels, thereby decreasing the blood pressure within the lungs.
The combination of these medications, ambrisentan and tadalafil, is employed in the treatment of pulmonary arterial hypertension, which involves elevated blood pressure in the lungs.
Before starting to consume Endobloc T Kit:
Prior to taking Endobloc T Kit tablets, it is essential to inform your physician if you suffer from low blood pressure, have a history of heart failure, or have significant liver issues. Make sure to let your doctor know if you’ve recently experienced a stroke or heart attack. Additionally, disclose if you currently have or have had any lung problems, anemia, or fluid retention (edema). Before starting treatment, communicate any concerns such as penile deformity, limb swelling, prolonged or painful erections (priapism), cancer (such as leukemia or multiple myeloma), severe kidney disease, red blood cell disorders, or any hearing loss to your doctor. This medication is not recommended for individuals under 18 years old. Your doctor will perform blood tests to detect anemia and evaluate liver function.
Is it possible to consume the Endobloc T Kit alongside meals?
The Endobloc T Kit comes exclusively in tablet form for oral consumption. You may take it with or without food, but it is important to discuss the correct dosage with your physician. The details provided here are based on the medication’s salt composition. The uses and effects can differ from one individual to another.
Endobloc T Kit Uses
Ensure you take Endobloc T Kit Combipack pills at consistent times each day to maintain the appropriate level of medication in your system. It’s important not to skip a dose. Your physician will conduct regular blood tests to monitor your liver’s performance. Steer clear of activities or tasks that are stressful or demand intense concentration.
Endothelin-1 (ET-1) is a highly effective peptide functioning both as autocrine and paracrine. Its effects in the endothelium and vascular smooth muscle are mediated by two receptor types, ETA and ETB. The ETA receptor primarily induces vasoconstriction and promotes cell proliferation, whereas the ETB receptor chiefly facilitates vasodilation, antiproliferation, and aids in ET-1 elimination.
In individuals with pulmonary arterial hypertension (PAH), plasma levels of ET-1 can rise up to 10 times higher, correlating with heightened mean right atrial pressure and disease severity. In the lung tissue of PAH patients, ET-1 and its mRNA levels see a significant increase, up to 9 times, most notably in the endothelium of pulmonary arteries. These observations indicate that ET-1 might play a pivotal part in PAH development and progression.
Ambrisentan is a substantially selective ETA receptor antagonist with a binding affinity of Ki=0.011 nM, exhibiting more than 4000-fold preference for the ETA receptor over ETB. The exact clinical significance of this high ETA selectivity remains unknown.
A daily dose of Ambrisentan 10 mg did not substantially alter the QTc interval, while a dose of 40 mg per day slightly raised mean QTc at peak concentration by 5 ms, with the upper 95% confidence limit reaching 9 ms. Significant QTc extension is unlikely in patients using ambrisentan in the absence of simultaneous metabolic inhibitors. A study showed that B-type natriuretic peptide (BNP) plasma levels significantly decreased after 12 weeks of ambrisentan administration. In two Phase III placebo-controlled trials, the BNP plasma levels were reduced by 29% in the 2.5 mg dosage group, 30% in the 5 mg group, and 45% in the 10 mg group (p < 0.001 for each dosage group), while the placebo group saw an 11% increase.
When sexual arousal leads to the release of nitric oxide in the corpus cavernosum, this in turn activates guanylyl cyclase enzyme, resulting in elevated cGMP levels. The increased cGMP levels in the corpus cavernosum cause smooth muscle relaxation, promoting blood inflow into penile tissues, and subsequently, an erection. The enzyme PDE5 breaks down cGMP in the corpus cavernosum, and Tadalafil’s inhibition of PDE5 sustains higher cGMP levels, supporting erections. Tadalafil does not affect blood flow to the penis without sexual arousal.
Tadalafil treats male erectile dysfunction and PAH. A pivotal part of the erection process is nitric oxide (NO) release in the corpus cavernosum, activating guanylate cyclase, which increases cyclic guanosine monophosphate (cGMP) levels, relaxing smooth muscles in the corpus cavernosum and flooding it with blood for an erection. Tadalafil effectively and selectively blocks cGMP-specific phosphodiesterase type 5 (PDE5), which would normally degrade cGMP in the corpus cavernosum. With Tadalafil, normal sexual arousal results in enhanced cGMP in the corpus cavernosum, improving erections. Without sexual arousal and corresponding NO/cGMP activation, Tadalafil should not induce an erection.
Side effects of Endobloc T Kit:
- Upset stomach
- Migraine
- Persistent cough
- Stuffy nose
- Swelling in the limbs
- Low red blood cell count (anemia)
- Airway inflammation (bronchitis)
Cautionary Measures:
- Refrain from self-prescribing this medication; follow your doctor’s recommended dosage and duration.
- Read the instructions on the package before use.
- Store in a cool, dry location, out of children’s reach.
- Ensure the product is within its expiration date before use.
- Keep at room temperature, protected from sunlight.
Terms and Conditions:
It is assumed you have sought medical advice prior to purchasing this medication and are not self-administering.
Endobloc T Kit:
- Read the Medication Guide provided by your pharmacist before you start using Ambricentan and every time you receive a refill. If you have any questions, contact your doctor or pharmacist.
- Take this medicine orally with or without food, usually once a day or as directed by a doctor. Do not crush, chew or break the pills.
- The dosage depends on your health condition, reaction to treatment and other medications that you are taking.Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, over-the-counter medicines and herbal products).
- Use this drug regularly to get the maximum benefit from it. To help you remember, take it at the same time every day.
- Do not stop taking this medicine without consulting a doctor. Some conditions can get worse when the drug is suddenly stopped. Your dose may need to decrease gradually.
- Women who are pregnant or may become pregnant should not handle pills or inhale dust from this medicine.
- Tell your doctor if your condition persists or worsens.
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