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Letairis

13.57
Letairis (ambrisentan) is an endothelin receptor antagonist used to treat pulmonary arterial hypertension. By blocking the action of endothelin, a substance that narrows blood vessels, it helps lower blood pressure in the lungs. This treatment improves exercise capacity and slows the progression of physical limitations in adults.


Ingredient
Availability
In Stock
Delivery Time
Airmail (14-21 days) | EMS trackable (5-9 days)
Product is shipped in a fully discreet envelope with no content disclosure, including all required documentation inside

Product Sheet

Active Ingredient(s)
Ambrisentan
Reference Brand
Volibris
Manufacturer
Gilead Sciences
Product Form
Tablet
Regulatory Classification
Rx
Primary Category
Blood Pressure, Pulmonary Hypertension
Product Category
Antihypertensives, Pulmonary arterial hypertension agents
Pharmacological Class
Endothelin receptor antagonist
Manufacturer Description
Used to improve exercise capacity and delay clinical worsening in patients with high blood pressure in the lung arteries.
Mechanism of Action
It works by blocking the action of endothelin, a natural substance that causes blood vessels to narrow. By keeping the vessels in the lungs relaxed, it lowers blood pressure in the pulmonary arteries.
Route of Administration
Oral
Onset Time
2 hours
Duration
24 hours
Contraindications
Pregnancy, Idiopathic pulmonary fibrosis, Severe liver impairment
Severe Adverse Events
Hepatotoxicity, Decreased haemoglobin, Fluid retention
Common Side Effects
Nasal congestion, Flushing, Sinusitis
Uncommon Side Effects
Peripheral oedema, Palpitations, Abdominal pain
Drug Interactions
Cyclosporine, Ketoconazole, Rifampicin
Pregnancy Safety Warnings
Contraindicated; highly teratogenic
Age Restrictions
Over 18 years
Storage Guidelines
Store in original package to protect from light
Related Products
Bosentan, Macitentan

Letairis FAQ

Can I travel internationally with Letairis?

Yes, Letairis tablets can be taken while travelling. Carry the medication in its original packaging with the prescription label, and keep it in your hand luggage to avoid temperature extremes and loss.

Will Letairis show up on drug tests for work or sport?

Ambrisentan is not a substance screened for in standard employment or anti-doping tests. However, if a test specifically includes prescription drugs, a copy of your prescription may be requested.

What does a Letairis tablet look like?

In the UK, Letairis tablets are white, round, film-coated, and marked with the imprint “LET 5” for the 5 mg strength and “LET 10” for the 10 mg strength.

Are there any foods I should avoid while taking Letairis?

There are no specific dietary restrictions. Taking the tablet with a moderate-fat meal does not affect absorption, but maintaining a balanced diet supports overall cardiovascular health.

Can I drink alcohol while on Letairis?

Moderate alcohol intake (up to one standard drink per day for women and two for men) is generally acceptable, but excessive drinking can increase the risk of liver-related side effects and should be avoided.

Do I need to use birth control while on Letairis?

Yes. Ambrisentan is teratogenic, so women of child-bearing potential must use a reliable form of contraception. A non-hormonal method (e.g., copper IUD) is recommended in addition to a combined oral contraceptive, because Letairis can reduce hormonal efficacy.

How often should I have blood tests while on Letairis?

Liver function tests and hemoglobin should be checked at baseline, then every three months for the first year, and subsequently as advised by your specialist, usually every six months.

What should I do if I miss a dose?

Take the missed tablet as soon as you remember, unless it is almost time for your next scheduled dose. In that case, skip the missed tablet and continue with your regular dosing time. Do not double the dose.

Is Letairis covered by NHS prescriptions?

Letairis is available on the NHS for patients meeting the clinical criteria for PAH. Prescription eligibility and cost depend on local NHS formularies and the patient’s specific circumstances.

Letairis: Overview of Ambrisentan for Adults

Letairis is a brand-name medication that contains ambrisentan as its sole active ingredient. It is supplied as an oral pill in strengths of 5 mg and 10 mg. In the United Kingdom Letairis is a prescription-only medicine (POM) regulated by the Medicines and Healthcare products Regulatory Agency (MHRA).

Ambrisentan belongs to the class of endothelin receptor antagonists (ERAs) and is used primarily to treat a specific type of high blood-pressure disorder affecting the lungs. The following sections provide a detailed, evidence-based summary of how Letairis works, when it is prescribed, safety considerations, dosing guidance, and practical information for patients.

How Letairis Works in the Body

Ambrisentan blocks the activity of endothelin-1, a natural substance that causes blood vessels to narrow (vasoconstriction) and promotes the growth of vascular muscle cells. By selectively antagonising the endothelin-A (ET-A) receptor, ambrisentan reduces the abnormal tightening of the pulmonary arteries, leading to:

  • Lower pulmonary artery pressure - easing the workload on the right side of the heart.
  • Improved exercise tolerance - patients often notice less shortness of breath during activity.
  • Reduced vascular remodeling - slowing the progression of disease-related changes in the lung vessels.

The onset of action typically occurs within a few days, with steady-state plasma concentrations reached after about one week of daily dosing. Ambrisentan is well absorbed from the gastrointestinal tract, undergoes hepatic metabolism (mainly by CYP3A4), and is eliminated primarily via the bile.

Conditions Treated with Letairis

Letairis is approved in the UK for the treatment of pulmonary arterial hypertension (PAH) - a rare, progressive disorder characterised by high blood pressure in the arteries that supply the lungs. PAH belongs to the broader “Heart & Blood Pressure” therapeutic area, but it specifically involves the pulmonary circulation rather than systemic arterial pressure.

Key points of the approved indication:

  • Adult patients (≥ 18 years) with WHO functional class II or III PAH.
  • Used as monotherapy or in combination with other approved PAH agents, such as phosphodiesterase-5 inhibitors.
  • Not indicated for pulmonary hypertension due to left-heart disease, lung disease, or chronic thromboembolic disease.

Off-Label and Investigational Applications

Evidence from clinical studies suggests that endothelin-A antagonism may have benefits in other vascular conditions, such as systemic hypertension or certain forms of heart failure. However, these uses are not approved by the MHRA, and robust guideline support is lacking.

Disclaimer: Off-label use of Letairis should only occur under direct supervision of a qualified cardiologist or pulmonary hypertension specialist, with a careful risk-benefit assessment for each patient.

Who Should (or Should Not) Use Letairis?

Ideal Candidates

  • Adults diagnosed with PAH confirmed by right-heart catheterisation.
  • Patients who are not pregnant and agree to use effective contraception.
  • Individuals with adequate liver function (baseline liver enzymes ≤ 2 × ULN).

Absolute Contraindications

  • Known hypersensitivity to ambrisentan or any excipients in the tablet.
  • Pregnancy - ambrisentan is teratogenic (category X).
  • Severe hepatic impairment (Child-Pugh C).

Relative Contraindications & Cautions

  • Moderate hepatic impairment (Child-Pugh B) - requires liver-function monitoring.
  • Baseline anaemia (hemoglobin < 10 g/dL).
  • Concomitant use of potent CYP3A4 inducers (e.g., rifampicin) - may reduce efficacy.
  • Concomitant use of CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) - may increase exposure and risk of adverse effects.

Special populations such as the elderly (> 75 years) or patients with mild renal impairment generally do not require dose adjustment, but clinical judgement is essential.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Headache - often mild and transient.
  • Flushing - warm sensation, usually resolves with continued use.
  • Peripheral edema - swelling of ankles or feet; may require dose adjustment.
  • Nasal congestion or sinus discomfort.
  • Fatigue - generally improves with continued therapy.

Serious Adverse Events

  • Liver injury - elevation of transaminases; requires regular monitoring.
  • Anaemia - drop in hemoglobin; may necessitate investigation.
  • Pulmonary edema - rare but potentially life-threatening; patients should seek immediate medical attention for sudden breathlessness.
  • Teratogenicity - fetal exposure can cause severe birth defects; pregnancy must be avoided.

Drug Interactions

  • CYP3A4 inhibitors (e.g., clarithromycin, itraconazole) → increase ambrisentan levels → higher risk of liver toxicity and edema.
  • CYP3A4 inducers (e.g., carbamazepine, rifampicin) → decrease ambrisentan levels → possible loss of therapeutic effect.
  • Hormonal contraceptives - ambrisentan can reduce the effectiveness of combined oral contraceptives; an additional non-hormonal method (e.g., copper IUD) is recommended.
  • Other endothelin-receptor antagonists - co-administration is contraindicated due to additive toxicity.

Food, Alcohol, and Lifestyle

  • Letairis can be taken with or without food; consistent timing each day improves adherence.
  • Moderate alcohol consumption is permissible, but excessive intake may exacerbate liver-related side effects.
  • No known impairment of driving or use of machinery, but patients experiencing dizziness should exercise caution.

Safety Tip: Always inform your healthcare provider of all medicines, herbal products, and supplements you are taking before starting Letairis.

How to Take Letairis

  • Starting dose: 5 mg (one tablet) taken once daily.
  • Dose escalation: After at least four weeks, if the patient tolerates the 5 mg dose and clinical response is suboptimal, the dose may be increased to 10 mg once daily.
  • Administration: Swallow the tablet whole with a glass of water. Do not crush, chew, or split the tablet.
  • Missed dose: Take the missed dose as soon as remembered once; if it is close to the time of the next scheduled dose, skip the missed dose and resume the regular schedule. Do not double the dose.
  • Overdose: Symptoms may include severe headache, dizziness, nausea, and hypotension. Seek emergency medical care; treatment is supportive, and there is no specific antidote.
  • Discontinuation: Abrupt cessation is not associated with withdrawal syndrome, but the underlying PAH condition may worsen. Any change in therapy should be supervised by a specialist.

Renal or hepatic impairment: No routine dose adjustment is required for mild-to-moderate renal dysfunction. For patients with significant hepatic impairment, avoid initiation and consider alternative therapies.

Monitoring and Follow-Up

  • Liver function tests (ALT, AST, bilirubin): Baseline, then every 3 months for the first year, thereafter as clinically indicated.
  • Hemoglobin: Baseline and periodic monitoring (every 3-6 months) to detect anaemia.
  • Pregnancy testing: Women of child-bearing potential must have a negative pregnancy test before starting therapy and monthly thereafter.
  • Clinical assessment: Functional class, six-minute walk distance, and biomarkers (e.g., NT-proBNP) should be evaluated regularly by the PAH team.

Storage and Handling

  • Store Letairis tablets at room temperature (15-25 °C), protected from moisture and direct sunlight.
  • Keep the container tightly closed and out of reach of children.
  • Do not use the medication after the expiry date printed on the packaging.
  • Dispose of unused tablets according to local pharmacy take-back schemes or NHS guidelines for medicines waste.

Medication-Specific Glossary

Endothelin-A Receptor Antagonist
A drug that blocks the ET-A subtype of endothelin receptors, preventing vasoconstriction and cell proliferation caused by endothelin-1.
Pulmonary Arterial Hypertension (PAH)
A progressive disease characterised by elevated pressure in the pulmonary arteries, leading to right-heart strain and reduced exercise capacity.
CYP3A4
An enzyme in the liver responsible for metabolising many medications, including ambrisentan; its activity can be altered by other drugs.
Hemoglobin
The protein in red blood cells that carries oxygen; reductions may signal anaemia, a recognised side effect of Letairis.

Medical Disclaimer

This article provides educational information about Letairis (ambrisentan) and is not a substitute for professional medical advice. Treatment decisions, including use for unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Information for Letairis is sourced from established medical standards and updated frequently. It is provided for general guidance and should be confirmed with a healthcare professional before use.
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