Nisoldipine is a calcium channel blocker used primarily in the treatment of hypertension (high blood pressure). It works by blocking calcium channels in the blood vessels, leading to vasodilation (relaxation of blood vessels) and hence, lowering blood pressure. This medication is often prescribed as an extended-release tablet to be taken once daily.

Nisoldipine is a dihydropyridine calcium channel blocker that relaxes the vascular smooth muscles. It is used in the management of hypertension.

Nisoldipine Uses:

• Hypertension:
  • Used for management of hypertension

Guideline recommendations:

• In the absence of comorbidities (such as cerebrovascular disease, chronic kidney disease, diabetes, heart failure, ischemic heart disease, etc.), the 2017 Guideline for the Prevention, Detection, Evaluation, and Management of High Blood Pressure in Adults suggests that thiazide-like diuretics or dihydropyridine calcium channel blockers may be preferable options due to improved cardiovascular endpoints (eg, prevention of heart failure and stroke).
• ARBs and ACE inhibitors are also suitable for monotherapy.
• Combination therapy is first favoured in individuals with high risk conditions (stage 2 hypertension or atherosclerotic cardiovascular disease), where it may be necessary to meet blood pressure targets.

Nisoldipine Dose in Adult

Nisoldipine Dose in the treatment of Hypertension: Oral:

• Sular (Geomatrix delivery system):
  • You start with 17 mg once a day. Then, your doctor may increase it gradually, like by 8.5 mg each week until your blood pressure is under control.
  • The usual range is between 17 to 34 mg once daily. But going beyond 34 mg isn't recommended.
• Nisoldipine extended-release tablet (original formulation):
  • At first, you'd take 20 mg once daily. Then, depending on how you respond, your doctor may adjust it weekly, by 10 mg each time.
  • Typically, you'll end up taking between 20 to 40 mg once daily. But taking more than 60 mg isn't recommended.

If you're switching from the original extended-release tablet to Sular, here's a guide:

• 10 mg of the original tablet equals 8.5 mg of Sular.
• 20 mg of the original tablet equals 17 mg of Sular.
• 30 mg of the original tablet equals 25.5 mg of Sular.
• 40 mg of the original tablet equals 34 mg of Sular.

So, if you're switching, your doctor will adjust the dose accordingly.

Use in Children:

Not indicated

Pregnancy Risk Factor C

• During pregnancy, Nisoldipine is classified as Pregnancy Risk Factor C, meaning adverse effects on the fetus haven't been confirmed but can't be ruled out either.
• Animal studies haven't shown problems unless very high doses were used that harmed the mother.
• However, untreated high blood pressure during pregnancy can lead to complications for both the mother and baby.
• If medication is necessary for managing hypertension during pregnancy, doctors usually opt for other medications deemed safer for pregnancy according to recommendations from the American College of Obstetricians and Gynecologists (ACOG) in 2013.

Nisoldipine use during breastfeeding:

• It's uncertain whether Nisoldipine passes into breast milk.
• The manufacturer advises making a decision about either stopping breastfeeding or discontinuing the medication, considering how crucial the treatment is for the mother.

Nisoldipine Dose in Kidney Disease:

• For individuals with mild to moderate kidney problems, no changes to the Nisoldipine dosage are typically needed.
• If someone has severe kidney impairment, the manufacturer's labeling doesn't specify any adjustments to the dosage.

Nisoldipine Dose in Liver disease:

Sular (Geomatrix delivery system):

• For individuals with liver impairment, specific dosing guidelines are provided for both the Sular (Geomatrix delivery system) and the original formulation of Nisoldipine. In the case of Sular, it's advised not to start with a dose higher than 8.5 mg once daily.

Nisoldipine extended-release (original formulation):

• For the original extended-release formulation, the initial dose shouldn't exceed 10 mg once daily for patients with hepatic impairment.
• These recommendations are made to ensure the safety and effectiveness of the medication in individuals with compromised liver function.

Common Side Effects of Nisoldipine:

• Cardiovascular:
  • Peripheral Edema
• Central Nervous System:
  • Headache

Less Common Side Effects Of Nisoldipine:

• Cardiovascular:
  • Vasodilation
  • Palpitations
  • Exacerbation Of Angina Pectoris
  • Chest Pain
• Central Nervous System:
  • Dizziness
• Dermatologic:
  • Skin Rash
• Gastrointestinal:
  • Nausea
• Respiratory:
  • Pharyngitis
  • Sinusitis

Contraindications to Nisoldipine:

• If someone has a hypersensitivity or allergic reaction to Nisoldipine, any ingredient in the medication, or to other dihydropyridine calcium channel blockers, they should avoid taking Nisoldipine.
• This caution is crucial because allergic reactions can range from mild to severe and may include symptoms like rash, itching, swelling, dizziness, difficulty breathing, or a rapid heartbeat.

Warnings and precautions

Angina/MI

• Sometimes, especially when starting or changing doses, Nisoldipine can cause low blood pressure (hypotension), which might lead to fainting (syncope).
• This doesn't happen often, but it's crucial to lower blood pressure at a pace that's safe for each person's health situation.
• Doctors will keep a close eye on blood pressure when starting Nisoldipine or adjusting the dose to make sure it doesn't drop too much.
• If you feel dizzy, lightheaded, or faint, it's important to let your doctor know so they can adjust your treatment if needed.

Hypotension/syncope

• Sometimes, especially when starting or adjusting the dose, Nisoldipine can cause low blood pressure (hypotension), which might lead to fainting (syncope).
• This doesn't happen often, but it's crucial to lower blood pressure at a pace that's safe for each person's health situation.
• Doctors will closely monitor blood pressure during the initial phase and when changing the dose to make sure it stays in a safe range.
• If someone experiences dizziness, lightheadedness, or fainting, they should inform their doctor promptly.

Peripheral edema

• Peripheral edema, swelling in the legs or ankles, is the most common side effect of Nisoldipine.
• It typically shows up about 2 to 3 weeks after starting the medication.
• This swelling occurs because Nisoldipine relaxes the blood vessels, allowing more fluid to leak into the tissues.
• While this side effect is common, it's usually mild and goes away on its own without causing any harm.

Aortic stenosis

• If someone has severe aortic stenosis (a narrowing of the aortic valve in the heart), it's important to be cautious when using Nisoldipine.

Heart failure (HF):

• In cases of heart failure, it's generally advised to avoid using Nisoldipine.
• Guidelines from the American College of Cardiology (ACC) and the American Heart Association (AHA) suggest this because calcium channel blockers, including Nisoldipine, may not provide benefits and could potentially lead to worse outcomes for people with heart failure.

Hepatic impairment

• For individuals with severe liver problems, it's important to be cautious when using Nisoldipine.
• In such cases, a lower starting dose may be necessary.
• Since the liver plays a crucial role in processing medications, severe liver impairment can affect how Nisoldipine is metabolized and eliminated from the body.

Hypertrophic cardiomyopathy with outflow tract obstruction (HCM)

• In individuals with hypertrophic cardiomyopathy (HCM) and outflow tract obstruction, it's important to exercise caution when using Nisoldipine.
• This caution is advised because Nisoldipine reduces afterload, which is the force the heart must overcome to pump blood out to the body.
• In some cases of HCM with outflow tract obstruction, lowering afterload can worsen symptoms associated with the condition.

Nisoldipine: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring parameters:

Blood Pressure Guidelines:

• Hypertension Management:
  • For confirmed hypertension and known cardiovascular disease (CVD) or a high 10-year risk of atherosclerotic cardiovascular disease (ASCVD):
    • Target blood pressure should be below 130/80 mm Hg, as per the 2017 ACC/AHA guidelines (Whelton 2017).
  • For confirmed hypertension without markers of increased ASCVD risk:
    • Keeping blood pressure below 130/80 mm Hg may be a reasonable goal.
• Diabetes and Hypertension:
  • For patients aged 18 to 65 without ASCVD and a 10-year ASCVD risk below 15%:
    • Target blood pressure should be below 140/90 mm Hg according to the American Diabetes Association (ADA) guidelines (ADA 2019).
  • For patients aged 18 to 65 with known ASCVD or a 10-year ASCVD risk above 15%:
    • Achieving a target blood pressure below 130/80 mm Hg may be appropriate if it can be done safely.
  • For patients over 65 years old:
    • Target blood pressure below 140/90 mm Hg is recommended for those in good health or with intermediate health complexity.
    • For those in very poor health or with complex medical issues, a target blood pressure below 150/90 mm Hg is recommended.

How to administer Nisoldipine?

• Consistent Timing:
  • Take the medication at the same time each day to maintain consistent serum levels.
• Dietary Considerations:
  • Avoid consuming high-fat meals while taking the medication.
• Empty Stomach:
  • Administer the medication on an empty stomach, either one hour before or two hours after a meal.
• Swallowing Instructions:
  • Swallow the tablet whole; do not crush, break, split, or chew it.

Mechanism of action of Nisoldipine:

• As a dihydropyridine calcium channel blocker, Nisoldipine works similarly to nifedipine.
• It blocks the movement of calcium ions into both vascular smooth muscle and cardiac muscle cells.
• These medications, known as dihydropyridines, are powerful vasodilators, meaning they relax blood vessels.
• Unlike other calcium channel blockers like verapamil and diltiazem, dihydropyridines such as Nisoldipine are less likely to slow down heart rate or affect heart contractility.
• In fact, Nisoldipine is even more potent as a vasodilator compared to nifedipine, with a strength that's 5 to 10 times greater.

Duration:

• Nisoldipine's effects last for more than 24 hours.

Absorption:

• The medication is well absorbed by the body.
• Peak concentrations are notably higher when taken with high-fat meals, although the total amount of the drug in the body (AUC) is reduced.

Protein Binding:

• Nisoldipine is highly bound to proteins in the bloodstream, with more than 99% of it being bound.

Metabolism:

• It undergoes extensive metabolism primarily in the liver, where it produces one active metabolite.
• This metabolite is only about 10% as potent as the parent drug.
• The liver's initial processing of the medication before it reaches the bloodstream is known as the first-pass effect.

Bioavailability:

• Approximately 5% of the medication reaches systemic circulation and is available for use by the body.

Half-life Elimination:

• Nisoldipine has a relatively long elimination half-life, lasting between 9 to 18 hours.

Time to Peak:

• It takes between 4 to 14 hours for the medication to reach its peak concentration in the bloodstream.

Excretion:

• The majority of the drug and its inactive metabolites are eliminated through urine (about 60% to 80%), with the remainder being excreted through feces.

International Brands of Nisoldipine:

• Sular
• Angiolat
• Baymycard
• Bo Ping
• Corasol
• Ke Di
• Mo Tai
• Nisodipen
• Nisoldin
• Sular
• Syscor
• Syscor CC
• Syscor MR

Nisoldipine Brand Names in Pakistan:

No Brands Available in Pakistan.