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Amlodipine

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Amlodipine (Besilate) is a calcium channel blocker used to treat high blood pressure and chest pain (angina). By relaxing the smooth muscles of the arterial walls, Amlodipine dilates blood vessels, which lowers blood pressure and increases oxygen supply to the heart. It is a fundamental medication for cardiovascular health management.


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In Stock
Delivery Time
Airmail (14-21 days) | EMS trackable (5-9 days)
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Product Sheet

Active Ingredient(s)
Amlodipine Besilate
Reference Brand
Istin
Manufacturer
Pfizer Ltd
Product Form
Tablet, Oral solution
Regulatory Classification
Rx
Primary Category
Blood Pressure, Chest Pain
Product Category
Calcium channel blockers, Dihydropyridines
Pharmacological Class
Calcium channel blockers
Manufacturer Description
A commonly prescribed medication to lower high blood pressure and prevent chest pain (angina).
Mechanism of Action
Amlodipine relaxes and widens the blood vessels. This makes it easier for blood to flow, which lowers blood pressure and makes it easier for the heart to pump blood around the body.
Route of Administration
Oral
Onset Time
24-48 hours for blood pressure effect
Duration
24 hours
Contraindications
Severe hypotension, Aortic stenosis, Unstable heart failure after heart attack
Severe Adverse Events
Severe allergic reaction, Heart attack symptoms, Inflammation of the pancreas, Liver problems
Common Side Effects
Swollen ankles, Flushing, Headache, Palpitations
Uncommon Side Effects
Dizziness, Abdominal pain, Fatigue, Visual disturbances
Drug Interactions
Grapefruit juice, Clarithromycin, Simvastatin, St John's wort
Pregnancy Safety Warnings
Consult a doctor; only used if benefits outweigh risks.
Age Restrictions
Children 6-17 years for hypertension
Storage Guidelines
Store below 25°C in a dry place.
Related Products
Felodipine, Nifedipine, Lercanidipine

Amlodipine FAQ

Can amlodipine be taken with other blood pressure medicines?

Yes, amlodipine is frequently combined with other antihypertensives such as ACE inhibitors, ARBs, or diuretics to achieve better blood-pressure control. The combination is usually safe, but your prescriber may adjust doses to avoid excessive lowering of blood pressure.

What should I do if I develop ankle swelling while on amlodipine?

Mild peripheral edema is a common side effect. Elevating the legs, reducing salt intake, and wearing supportive stockings can help. If swelling becomes pronounced or painful, contact your healthcare provider, as a dose adjustment or alternative therapy may be needed.

Is it safe to use amlodipine during pregnancy?

Amlodipine is classified as Pregnancy Category C in the UK, meaning risk cannot be ruled out. It should only be used if the potential benefit justifies the possible risk to the fetus, and this decision requires careful medical evaluation.

How does amlodipine differ from other calcium-channel blockers like diltiazem?

Amlodipine primarily affects vascular smooth muscle, causing peripheral vasodilation, whereas diltiazem has more pronounced effects on heart rate and conduction. Consequently, amlodipine is preferred for isolated hypertension, while diltiazem is often chosen when rate control is also needed.

Can grapefruit juice increase amlodipine levels?

Yes, grapefruit juice can inhibit CYP3A4 enzymes in the intestine, potentially raising amlodipine concentrations and increasing the risk of hypotension. Limiting grapefruit consumption while on amlodipine is advisable.

Do I need to get blood tests while taking amlodipine?

Routine blood tests are not required solely for amlodipine, but baseline liver function tests may be performed in patients with known hepatic disease. Your clinician will order labs based on your overall health profile and any co-prescribed medications.

What is the appearance of a typical amlodipine tablet?

In the UK, a 5 mg amlodipine tablet is generally white, round, and bears the imprint “5 mg A” on one side and “Amlodipine” on the other. Appearance can vary between manufacturers, so always verify the imprint code on the packaging.

Can amlodipine cause dizziness when standing up quickly?

Yes, the vasodilatory effect can lead to orthostatic hypotension, especially after the first few doses. To minimize dizziness, rise slowly from sitting or lying positions and stay hydrated.

Is amlodipine detectable in workplace drug tests?

Amlodipine is not a controlled substance and is not screened for in standard workplace drug-testing panels. It should not affect employment drug-test results.

How long does it take for amlodipine to show full blood-pressure reduction?

While blood-pressure lowering can start within a few hours, the full therapeutic effect may take up to two weeks as steady-state plasma levels are reached. Regular monitoring is important during this period.

Amlodipine Besilate: Generic Medication Overview

Amlodipine Besilate is the active ingredient in the widely used blood-pressure pill known simply as amlodipine. It is available as a generic medication and marketed under brand names such as Norvasc, Istin, and Loressa in the United Kingdom. Belonging to the calcium-channel blocker class, amlodipine is prescribed for the management of hypertension and chronic stable angina. The medication is supplied in tablet form (pill) at strengths of 2.5 mg, 5 mg, and 10 mg, and is classified as a prescription-only medicine (POM) by the Medicines and Healthcare products Regulatory Agency (MHRA).

How Amlodipine Works in the Body

Amlodipine belongs to the dihydropyridine subclass of calcium-channel blockers. It blocks L-type calcium channels in the smooth muscle of arterial walls, which prevents calcium ⁺⁺ from entering cells. By reducing intracellular calcium, the drug causes vasodilation of peripheral arteries, leading to lowered peripheral resistance and a drop in blood pressure. In the coronary arteries, similar vasodilation improves oxygen delivery to the heart muscle, relieving angina symptoms. The onset of action occurs within 2-3 hours after oral intake, with a long half-life of approximately 30-50 hours, allowing once-daily dosing.

Conditions Treated by Amlodipine

  • Primary hypertension - the first-line treatment for many adults when lifestyle measures are insufficient.
  • Chronic stable angina - helps prevent chest pain episodes by improving coronary blood flow.
  • Secondary hypertension - may be added when high blood pressure results from other conditions (e.g., renal disease) and requires additional control.

In the UK, the National Institute for Health and Care Excellence (NICE) recommends amlodipine as part of the initial pharmacologic regimen for patients whose blood pressure remains above target after lifestyle modification.

Patient Suitability and Contraindications

Who Should Use Amlodipine?

  • Adults (≥ 18 years) with diagnosed hypertension or stable angina.
  • Patients who can tolerate calcium-channel blockers and have no known hypersensitivity to amlodipine or related compounds.

Absolute Contraindications

  • Known hypersensitivity to amlodipine besilate or any excipients in the tablet.
  • Severe aortic stenosis (the vasodilatory effect can precipitate hypotension).

Relative Contraindications

  • Pregnancy and lactation - amlodipine crosses the placenta and is excreted in breast milk; use only if the benefit outweighs risk.
  • Severe hepatic impairment - reduced metabolism may increase drug exposure; dose adjustment is often required.
  • Elderly patients - may be more sensitive to blood-pressure-lowering effects; start at the lowest dose (2.5 mg).

Special Populations

  • Renal impairment - no dose adjustment needed for mild to moderate renal dysfunction, but monitor blood pressure closely.
  • Geriatric patients - begin with 2.5 mg and titrate slowly, watching for dizziness or falls.

If you have any of the above conditions, discuss them with your prescribing clinician before starting amlodipine.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Peripheral edema - swelling of ankles or feet, reported in up to 20 % of patients.
  • Headache - often mild and transient during treatment initiation.
  • Flushing - a warm sensation, typically resolves with continued use.
  • Dizziness - may occur, especially when standing quickly; advise rising slowly.

Serious Adverse Events

  • Hypotension - symptomatic low blood pressure (dizziness, fainting) warrants immediate medical review.
  • Bradycardia - rarely, heart rate may fall below 50 bpm; seek urgent care if accompanied by fatigue or weakness.
  • Severe allergic reactions - rash, itching, swelling of face/lips, or difficulty breathing require emergency attention.

Drug Interactions

  • CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole) - can increase amlodipine plasma concentrations, potentially heightening hypotension risk.
  • Simultaneous use with other antihypertensives - additive blood-pressure-lowering effect; dose titration may be necessary.
  • Statins metabolized by CYP3A4 - modest increase in statin levels; monitor for muscle symptoms.

Food and Lifestyle Interactions

  • Alcohol - excessive intake can amplify vasodilatory effects; moderate consumption is advisable.
  • Grapefruit juice - may inhibit CYP3A4 and raise amlodipine levels; limit intake.
  • Driving or operating machinery - generally safe, but avoid if you feel dizzy or light-headed.

Patients should provide a complete medication list-including over-the-counter drugs, herbal supplements, and vitamins-to their pharmacist or prescriber before starting amlodipine.

How to Take Amlodipine

  • Standard dosing - most adults begin with a 5 mg tablet once daily. The dose may be increased to 10 mg if blood pressure remains uncontrolled, or reduced to 2.5 mg for those who experience side effects.
  • Special populations - start at 2.5 mg for elderly patients, those with severe hepatic impairment, or individuals who are particularly sensitive to blood-pressure changes.
  • Administration - swallow the tablet whole with water; it can be taken with or without food. Do not crush or chew the tablet.
  • Missed dose - take the missed dose as soon as you remember, unless it is near the time of the next scheduled dose. Do not double the dose.
  • Overdose - symptoms may include severe hypotension, fainting, and rapid heart rate. Seek emergency medical care; treatment is supportive, and there is no specific antidote.
  • Discontinuation - abrupt stopping is not usually problematic, but if you have been on high doses for a prolonged period, a gradual taper may reduce the risk of rebound hypertension. Follow your prescriber’s guidance.

Monitoring and Follow-Up

  • Blood pressure - check weekly until target is reached, then at least every 3-6 months.
  • Heart rate - monitor for bradycardia if combined with other rate-slowing agents.
  • Liver function - baseline tests are recommended for patients with known hepatic disease; repeat as clinically indicated.
  • Renal function - not routinely required for amlodipine alone, but monitor if other nephrotoxic drugs are co-prescribed.

Report any new or worsening symptoms-especially swelling, dizziness, or fainting-to a healthcare professional promptly.

Storage and Handling

  • Store tablets at room temperature (15-30 °C) in the original container, tightly closed, and out of direct sunlight.
  • Keep out of reach of children and pets; the packaging includes child-resistant caps.
  • Do not use tablets beyond their expiry date; discard according to local pharmacy guidelines or NHS “medicine waste” instructions.

Medication-Specific Glossary

Calcium-Channel Blocker
A class of drugs that inhibit the influx of calcium ions into vascular smooth muscle, leading to vasodilation and reduced blood pressure.
Peripheral Edema
Swelling of the lower extremities caused by fluid accumulation, a common side effect of vasodilating agents.
CYP3A4
An enzyme in the liver that metabolizes many medications; inhibitors can raise levels of drugs like amlodipine.
Bioavailability
The proportion of the administered dose that reaches systemic circulation unchanged; amlodipine’s oral bioavailability is approximately 60-70 %.
Half-Life
The time required for the plasma concentration of a drug to decrease by half; amlodipine’s long half-life supports once-daily dosing.

Medical Disclaimer

This article provides educational information about amlodipine 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 Amlodipine 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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