Amlodipine Besylate 2.5mg Tablets
It is used to treat high blood pressure.It is used to treat some types of chest pain (angina).It is used in some people to lower the chance of having to go to the hospital for chest pain (angina) and needing certain heart procedures.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antihypertensive, Antianginal
Pharmacologic Class
Calcium Channel Blocker (Dihydropyridine)
Pregnancy Category
Category C
FDA Approved
Aug 1992
DEA Schedule
Not Controlled
Overview
What is this medicine?
Amlodipine is a medicine that helps relax your blood vessels, making it easier for your heart to pump blood. This helps lower high blood pressure and can also reduce chest pain (angina).
How to Use This Medicine
Taking Your Medication
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Take your medication at the same time every day, with or without food, as directed by your doctor. Continue taking your medication as prescribed, even if you start to feel well.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature, away from direct light and moisture. Keep it in a dry place, avoiding storage in a bathroom. Protect your medication from heat and light. Always keep your medication in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it has been 12 hours or more since the missed dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Take your medication at the same time every day, with or without food, as directed by your doctor. Continue taking your medication as prescribed, even if you start to feel well.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature, away from direct light and moisture. Keep it in a dry place, avoiding storage in a bathroom. Protect your medication from heat and light. Always keep your medication in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it has been 12 hours or more since the missed dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Take medication exactly as prescribed, usually once daily.
- Do not stop taking the medication suddenly without consulting your doctor.
- Continue to monitor your blood pressure regularly at home if advised by your doctor.
- Adopt a heart-healthy lifestyle: low-sodium diet, regular exercise, maintain a healthy weight, limit alcohol, and quit smoking.
- Report any new or worsening swelling in your ankles or feet to your doctor.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
5 mg orally once daily
Dose Range:
2.5 - 10 mg
Condition-Specific Dosing:
hypertension:
Initial: 5 mg orally once daily; Max: 10 mg orally once daily. Titrate over 7-14 days.
chronic stable angina:
Initial: 5 mg orally once daily; Max: 10 mg orally once daily.
vasospastic angina (Prinzmetal's):
Initial: 5 mg orally once daily; Max: 10 mg orally once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
6-17 years (Hypertension): Initial: 2.5 mg orally once daily; Max: 5 mg orally once daily. Doses above 5 mg have not been studied in pediatric patients.
Adolescent:
6-17 years (Hypertension): Initial: 2.5 mg orally once daily; Max: 5 mg orally once daily. Doses above 5 mg have not been studied in pediatric patients.
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment necessary.
Moderate:
No dosage adjustment necessary.
Severe:
No dosage adjustment necessary.
Dialysis:
Amlodipine is not dialyzable. No dosage adjustment necessary.
Hepatic Impairment:
Mild:
Consider lower starting dose (2.5 mg once daily).
Moderate:
Consider lower starting dose (2.5 mg once daily).
Severe:
Initial dose of 2.5 mg once daily is recommended. Titrate slowly.
Pharmacology
Mechanism of Action
Amlodipine is a dihydropyridine calcium channel blocker (CCB) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. This inhibition is selective for vascular smooth muscle, resulting in peripheral arterial vasodilation and reduction in peripheral vascular resistance, which lowers blood pressure. In angina, it reduces myocardial oxygen demand by decreasing afterload and may increase myocardial oxygen supply by dilating coronary arteries and arterioles.
Pharmacokinetics
Absorption:
Bioavailability:
64-90%
Tmax:
6-12 hours
FoodEffect:
Food does not affect the absorption of amlodipine.
Distribution:
Vd:
21 L/kg
ProteinBinding:
Approximately 97.5%
CnssPenetration:
Limited
Elimination:
HalfLife:
30-50 hours
Clearance:
Not available
ExcretionRoute:
Renal (inactive metabolites)
Unchanged:
Approximately 10% (renal)
Pharmacodynamics
OnsetOfAction:
Within 24 hours (antihypertensive effect)
PeakEffect:
6-12 hours (plasma concentration), 7-14 days (full antihypertensive effect)
DurationOfAction:
At least 24 hours
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Severe dizziness or fainting
New or worsening chest pain
Fast or abnormal heartbeat
Swelling
Stiff muscles, shakiness, or abnormal muscle movements
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor or seek medical help:
Dizziness
Drowsiness
Fatigue
Weakness
Flushing
Upset stomach
Stomach pain
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Severe dizziness or fainting
New or worsening chest pain
Fast or abnormal heartbeat
Swelling
Stiff muscles, shakiness, or abnormal muscle movements
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor or seek medical help:
Dizziness
Drowsiness
Fatigue
Weakness
Flushing
Upset stomach
Stomach pain
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe dizziness or fainting
- New or worsening chest pain
- Unusual swelling of the hands, ankles, or feet that is bothersome or severe
- Shortness of breath
- Irregular heartbeat
- Signs of liver problems (e.g., yellowing of skin/eyes, dark urine, persistent nausea/vomiting)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor and pharmacist identify potential interactions between this medication and other substances you are taking.
* Any health problems you have, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that it is safe to take this medication with all your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor and pharmacist identify potential interactions between this medication and other substances you are taking.
* Any health problems you have, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that it is safe to take this medication with all your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
Important Warnings and Cautions
When taking this medication, it is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, about your treatment.
To ensure your safety, avoid driving and other activities that require alertness until you understand how this medication affects you. To minimize the risk of dizziness or fainting, rise slowly from a sitting or lying position, and exercise caution when climbing stairs.
Regularly monitor your blood pressure as directed by your healthcare provider. Although rare, new or worsening chest pain can occur after starting this medication or increasing the dose, which may lead to a heart attack. This risk is higher in individuals with severe heart blood vessel disease. Discuss any concerns with your doctor.
If you have high blood pressure, consult your doctor before using over-the-counter (OTC) products that may increase blood pressure, such as cough or cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, and certain natural products or aids.
Before consuming alcohol, discuss the potential risks with your doctor. Liver problems have been associated with this medication, and in some cases, hospitalization has been necessary. Inform your doctor about any liver concerns.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects. Pregnant or breastfeeding women, or those planning to become pregnant, should discuss the benefits and risks of this medication with their doctor.
Specific Instructions for Chest Pain
Do not use this medication to treat sudden chest pain, as it will not provide relief. Instead, consult your doctor for appropriate treatment.
When taking this medication, it is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, about your treatment.
To ensure your safety, avoid driving and other activities that require alertness until you understand how this medication affects you. To minimize the risk of dizziness or fainting, rise slowly from a sitting or lying position, and exercise caution when climbing stairs.
Regularly monitor your blood pressure as directed by your healthcare provider. Although rare, new or worsening chest pain can occur after starting this medication or increasing the dose, which may lead to a heart attack. This risk is higher in individuals with severe heart blood vessel disease. Discuss any concerns with your doctor.
If you have high blood pressure, consult your doctor before using over-the-counter (OTC) products that may increase blood pressure, such as cough or cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, and certain natural products or aids.
Before consuming alcohol, discuss the potential risks with your doctor. Liver problems have been associated with this medication, and in some cases, hospitalization has been necessary. Inform your doctor about any liver concerns.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects. Pregnant or breastfeeding women, or those planning to become pregnant, should discuss the benefits and risks of this medication with their doctor.
Specific Instructions for Chest Pain
Do not use this medication to treat sudden chest pain, as it will not provide relief. Instead, consult your doctor for appropriate treatment.
Overdose Information
Overdose Symptoms:
- Profound and prolonged systemic hypotension (low blood pressure)
- Bradycardia (slow heart rate)
- Tachycardia (fast heart rate)
- Peripheral vasodilation with possible reflex tachycardia
- Shock with fatal outcome has been reported
What to Do:
Call 1-800-222-1222 (Poison Control Center) immediately. Management involves supportive care, including monitoring cardiac and respiratory function, elevating extremities, and administering intravenous fluids. Vasopressors (e.g., norepinephrine) may be used for persistent hypotension. Intravenous calcium gluconate may temporarily reverse the effects of calcium channel blockade. Gastric lavage may be considered if ingestion is recent. Activated charcoal may be beneficial.
Drug Interactions
Major Interactions
- Simvastatin (increased simvastatin exposure, risk of myopathy/rhabdomyolysis; limit simvastatin dose to 20 mg/day)
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin) - may significantly increase amlodipine exposure, leading to hypotension and edema. Monitor for symptoms and consider dose reduction of amlodipine.
- Strong CYP3A4 inducers (e.g., rifampin, St. John's Wort) - may decrease amlodipine exposure, reducing efficacy. Monitor blood pressure and consider dose adjustment of amlodipine.
Moderate Interactions
- Moderate CYP3A4 inhibitors (e.g., erythromycin, diltiazem) - may increase amlodipine exposure. Monitor for symptoms and consider dose reduction.
- Sildenafil (additive hypotensive effects) - use with caution, consider lower initial sildenafil dose.
- Tacrolimus (increased tacrolimus blood levels) - monitor tacrolimus levels and adjust dose as needed.
- Cyclosporine (increased cyclosporine trough concentrations) - monitor cyclosporine levels and adjust dose as needed.
Minor Interactions
- Grapefruit juice (may increase amlodipine exposure, but generally not clinically significant with usual consumption)
- Other antihypertensives (additive hypotensive effects)
Monitoring
Baseline Monitoring
Blood Pressure (BP)
Rationale: To establish baseline and guide initial dosing.
Timing: Prior to initiation of therapy.
Heart Rate (HR)
Rationale: To establish baseline and monitor for reflex tachycardia.
Timing: Prior to initiation of therapy.
Liver Function Tests (LFTs)
Rationale: Amlodipine is extensively metabolized by the liver; baseline assessment is prudent, especially in patients with suspected hepatic impairment.
Timing: Prior to initiation, especially if hepatic impairment is suspected.
Routine Monitoring
Blood Pressure (BP)
Frequency: Regularly, typically weekly or bi-weekly during dose titration, then monthly or every 3-6 months once stable.
Target: <130/80 mmHg (or individualized target based on patient comorbidities)
Action Threshold: If BP remains above target, consider dose increase or addition of another agent. If BP is too low (<90/60 mmHg or symptomatic hypotension), consider dose reduction.
Heart Rate (HR)
Frequency: Regularly, especially during dose titration.
Target: 60-100 bpm (or individualized)
Action Threshold: Persistent bradycardia (<50 bpm) or significant tachycardia (>100 bpm) should be evaluated.
Peripheral Edema
Frequency: Regularly, especially during dose titration and with higher doses.
Target: Absence of significant edema
Action Threshold: Development of significant or bothersome peripheral edema may warrant dose reduction or addition of a diuretic.
Symptom Monitoring
- Dizziness
- Headache
- Flushing
- Palpitations
- Fatigue
- Nausea
- Abdominal pain
- Gingival hyperplasia (rare, long-term)
Special Patient Groups
Pregnancy
Amlodipine is Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown reproductive toxicity.
Trimester-Specific Risks:
First Trimester:
Limited human data, animal studies show some reproductive toxicity at high doses.
Second Trimester:
Limited human data.
Third Trimester:
Limited human data. Potential for adverse effects on the fetus (e.g., hypotension, bradycardia) due to pharmacologic action, though not well-established in humans.
Lactation
Amlodipine is excreted in human milk. The effect of amlodipine on the breastfed infant is unknown. Amlodipine has a long half-life. Monitor breastfed infants for hypotension, bradycardia, and somnolence. Use with caution.
Infant Risk:
Low to Moderate (L3 - Moderately Safe). Limited data suggest low levels in milk, but long half-life warrants caution.
Pediatric Use
Approved for hypertension in children 6-17 years. Dosing is lower than adults (initial 2.5 mg, max 5 mg). Safety and efficacy in children younger than 6 years have not been established.
Geriatric Use
Clearance of amlodipine is decreased in elderly patients, resulting in increased AUC and half-life. A lower starting dose (2.5 mg once daily) is recommended for elderly patients, and dose titration should be done slowly. Monitor closely for adverse effects, especially peripheral edema.
Clinical Information
Clinical Pearls
- Amlodipine is a long-acting CCB, allowing for once-daily dosing and smooth blood pressure control.
- Peripheral edema is a common dose-dependent side effect, often managed by dose reduction or adding a diuretic.
- Unlike some other CCBs, amlodipine has minimal negative inotropic effects at therapeutic doses, making it generally safe in patients with compensated heart failure.
- Gingival hyperplasia is a rare but recognized side effect with long-term use; good oral hygiene is important.
- The full antihypertensive effect may not be seen for 7-14 days after starting or increasing the dose due to its long half-life.
Alternative Therapies
- Other Dihydropyridine Calcium Channel Blockers (e.g., Felodipine, Nifedipine, Nicardipine)
- Non-Dihydropyridine Calcium Channel Blockers (e.g., Diltiazem, Verapamil)
- ACE Inhibitors (e.g., Lisinopril, Enalapril)
- Angiotensin Receptor Blockers (ARBs) (e.g., Losartan, Valsartan)
- Thiazide Diuretics (e.g., Hydrochlorothiazide, Chlorthalidone)
- Beta-blockers (e.g., Metoprolol, Atenolol)
Cost & Coverage
Average Cost:
Varies, typically $10-$30 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.