Levamlodipine (Conjupri) is the active isomer of amlodipine. It is used orally for the treatment of patients with hypertension.

Levamlodipine Uses:

• Hypertension:
  • Adults and kids aged six and older who have hypertension are administered it to treat it.

Levamlodipine Dose in Adults:

Hypertension:

• Note: When treating individuals whose blood pressure is at least 20/10 mm Hg above target, it may first be combined with another suitable medication, such as an angiotensin-converting enzyme inhibitor, angiotensin II receptor blocker, or a thiazide diuretic.
• Some doctors advise an initial trial of monotherapy for individuals whose blood pressure is less than 20/10 mm Hg over the target, yet eventually, patients will need combo medication.
  • Orally: initially 1.25 to 2.5 mg once daily.
  • As per patients' response and need, titrate every one to two weeks.
  • The maximum daily dosage is 5 mg.
  • With larger dosages, the antihypertensive impact is lessened and there is a greater possibility of side effects.

Levamlodipine dose in children:

• Hypertension:

  • For young children and teenagers aged 6 to 17:
  • 1.25 to 2.5 mg orally, once a day.

Levamlodipine Pregnancy Risk Category: N

• Levamlodipine and Dextro amlodipine can be thought of as the racemic components of amlodipine.
• There is no placental barrier to amlodipine.
• For additional information, Refer to the amlodipine monograph.

Use during breastfeeding:

• Breast milk contains amlodipine.
• Amlodipine can be described as a racemic combination of levamlodipine, the pharmacologically active Iomer, and dextro amlodipine.
• For more information, refer to the amlodipine monograph

Dose in kidney disease:

• No dosage adjustments are necessary in kidney impairment in children and adolescents from 6 to 17 years.

Levamlodipine Dose in liver disease:

• Hypertension:
  • 1.25 mg once each day at first.
  • In individuals with severe hepatic impairment, titrate gradually.

Common Side Effects of Levamlodipine:

• Cardiovascular:
  • Edema

Less Common Side Effects of Levamlodipine:

• Cardiovascular:
  • Palpitations
  • Flushing
• Central nervous system:
  • Fatigue
  • Dizziness
  • Drowsiness
• Gastrointestinal:
  • Nausea
  • Abdominal pain

Contraindications to Levamlodipine:

• responses due to allergies to levamlodipine, amlodipine, or any other formulation ingredient.

Warnings and precautions

• Angina and myocardial Infarction
  • In case of reports, angina or myocardial enlargement were more common after treatment initiation or dosage adjustment of dihydropyridine calciumchannel blockers.
  • Patients with obstructive cardiomyopathy may experience tachycardia, especially if there is no concurrent beta-blockade.
• Hypotension
  • Some individuals' symptoms of hypotension may be present.
  • Hypotension is unlikely because of the slow development.
  • The rate of BP reduction should be proportionate to the clinical circumstances of the patient.
• Peripheral edema
  • The most frequent adverse effect is peripheral edoema. Peripheral edoema may appear 2 to 3 weeks after commencing medication.
• Aortic stenosis
  • Patients suffering from severe aortic stenosis must be cautious.
  • It can cause hypotension and reduce coronary perfusion. This could lead to ischemia.
• Heart failure:
  • Calcium channel blockers are to be kept away from by patients with lower ejection fractions whenever possible. 
• Hepatic impairment
  • Patients with hepatic impairment should be cautious.
  • Patients may need lower starting doses.
  • Patients with significant hepatic impairment ought to be able to gradually increase their dosage.
• Hypertrophic cardiomyopathy and outflow tract obstruction
  • The signs of this illness might get worse if the afterload is reduced.
  • When using amlodipine, patients with hypertrophic cardiomyopathy or outflow tract blockage should exercise caution.

Levamlodipine: Drug Interaction

Monitoring parameters:

Monitor the heart rate and Blood pressure.

High blood pressure in adults: The 2017 Guideline for the Prevention, Detection, Evaluation, and Management.

• A 10-year atherosclerotic cardiovascular disease risk of 10% or confirmed hypertension plus a history of cardiovascular disease:
  • Recommended target blood pressure is 130/80 mm Hg.
• A confirmed case of hypertension without signs of an elevated risk of atherosclerotic cardiovascular disease:
  • Recommended target blood pressure is 130/80 mm Hg.

Diabetes and hypertension: The American Diabetes Association guidelines.

• Patients between the ages of 18 and 65 who have a 10-year atherosclerotic cardiovascular disease risk of less than 15% and do not have the atherosclerotic cardiovascular disease:
  • It is advised to maintain a target blood pressure of 140/90 mm Hg.
• Patients between the ages of 18 and 65 with known atherosclerotic cardiovascular disease or a 10% risk in the next ten years:
  • If it is possible to do so safely, a target blood pressure of 130/80 mm Hg may be recommended.
• Patients >65 years old (in good, complicated, or mediocre health):
  • It is advised to maintain a target blood pressure of 140/90 mm Hg.
• Patients >65 years of age (very complex/poor health):
  • It is advised to maintain a target blood pressure of 150/90 mm Hg.

How to administer Levamlodipine?

• It may be taken once daily without regard to meals.

Mechanism of action of Levamlodipine:

• It immediately affects the blood vessel and smooth muscles, decreasing blood pressure and reducing peripheral vascular resistance. 
• Amlodipine, a dihydropyridine calcium-channel blocker, acts by blocking transmembrane calcium influx into calcium ions.
• It is most effective in the smooth muscle cells of the vessels but less so in the cardiac muscle cells.
• The pharmacologically potent antihypertensive isomer of levamlodipine, amlodipine, is a 1:1 racemic combination of levamlodipine and dextro-amlodipine.

• Protein binding:
  • ~93%.
• Onset:
  • Gradual.
• Duration:
  • less than or more than 24 hours.
• Excretion:
  • Urine (10% of total dose as unchanged drug, 60% of total dose as metabolites).
• Metabolism:
  • Hepatic (~90%) to inactive metabolites.
• Half-life elimination:
  • Terminal (biphasic): ~30 to 50 hours;
  • increased with hepatic dysfunction.
• Bioavailability:
  • 64% to 90%.
• Time to peak:
  • 6 to 12 hours.
• Clearance:
  • Clearance of the drug may be decreased in patients with hepatic insufficiency or moderate to severe heart failure;
  • Wweight-adjusted clearance in children >6 years of age is similar to adults

Levamlodipine Brand Names (International):

• S-Ambes
• Conjupri

Levamlodipine Brand Names in Pakistan:

No Brands Available in Pakistan.