Norvasc 5 mg side effects. Norvasc (Amlodipine): Comprehensive Guide to Side Effects, Uses, and Dosage
What are the primary uses of Norvasc. How does Norvasc work to lower blood pressure. What are the common side effects of Norvasc. How should Norvasc be taken for maximum effectiveness. What precautions should be considered when using Norvasc.
Understanding Norvasc: A Powerful Calcium Channel Blocker
Norvasc, also known by its generic name Amlodipine, is a widely prescribed medication belonging to the calcium channel blocker class of drugs. This potent medication plays a crucial role in managing hypertension and certain types of chest pain, offering relief to millions of patients worldwide.
The Mechanism of Action
How does Norvasc work to lower blood pressure? Norvasc functions by relaxing blood vessels, allowing for improved blood flow throughout the body. This relaxation effect is achieved by blocking calcium channels in the smooth muscle cells of blood vessels, preventing calcium from entering these cells. As a result, the blood vessels dilate, reducing peripheral resistance and lowering blood pressure.
Primary Uses of Norvasc: Beyond Hypertension
While Norvasc is primarily known for its blood pressure-lowering effects, its applications extend beyond this primary use. Here are the main conditions Norvasc is prescribed for:
- Hypertension (high blood pressure)
- Angina (chest pain)
- Coronary artery disease
Can Norvasc prevent heart attacks and strokes? By effectively managing high blood pressure, Norvasc indirectly contributes to the prevention of serious cardiovascular events such as heart attacks, strokes, and kidney problems. However, it’s important to note that Norvasc is not a cure for these conditions but rather a management tool.
Dosage and Administration: Ensuring Optimal Results
Proper administration of Norvasc is crucial for achieving the desired therapeutic effects. The dosage is typically individualized based on the patient’s medical condition and response to treatment.
Standard Dosing Guidelines
What is the typical starting dose for Norvasc? Most adults begin with a 5 mg dose taken once daily. However, your doctor may adjust this dose based on your specific needs. Some patients may require a lower starting dose of 2.5 mg, while others might need up to 10 mg per day for optimal blood pressure control.
Administration Tips
- Take Norvasc at the same time each day to maintain consistent blood levels.
- The medication can be taken with or without food.
- If using the liquid form, shake well before use and use a special measuring device for accurate dosing.
- Do not discontinue Norvasc without consulting your healthcare provider, even if you feel well.
Is it safe to crush or split Norvasc tablets? While some tablets can be split, it’s essential to consult your pharmacist or doctor before doing so, as not all formulations are suitable for splitting.
Common Side Effects: What to Expect
Like all medications, Norvasc can cause side effects. While not everyone experiences these, it’s important to be aware of potential adverse reactions.
Frequently Reported Side Effects
- Dizziness
- Lightheadedness
- Swelling in ankles or feet (edema)
- Flushing
- Fatigue
- Nausea
- Abdominal pain
Are these side effects permanent? Most side effects are mild and tend to diminish as your body adjusts to the medication. However, if any side effects persist or worsen, it’s crucial to consult your healthcare provider.
Serious Side Effects: When to Seek Medical Attention
While rare, some patients may experience more severe side effects that require immediate medical attention.
Red Flags to Watch For
- Fast, irregular, or pounding heartbeat
- Fainting
- Severe dizziness
- Worsening chest pain
- Symptoms of a heart attack (chest/jaw/left arm pain, shortness of breath, unusual sweating)
How quickly should you seek medical help for serious side effects? If you experience any of these severe side effects, it’s crucial to seek medical attention immediately. Prompt intervention can prevent potential complications and ensure your safety.
Drug Interactions: Navigating Potential Risks
Norvasc can interact with various medications and substances, potentially altering its effectiveness or increasing the risk of side effects.
Common Interactions to Be Aware Of
- Other blood pressure medications
- Certain antifungal medications
- Some antibiotics
- HIV protease inhibitors
- Simvastatin (cholesterol-lowering medication)
Does grapefruit juice interact with Norvasc? Yes, grapefruit and grapefruit juice can interact with Norvasc, potentially increasing its concentration in the blood. It’s advisable to avoid consuming grapefruit products while taking this medication unless specifically approved by your doctor.
Precautions and Contraindications: Ensuring Safe Usage
Certain medical conditions and circumstances may require special consideration when using Norvasc.
Important Precautions
- Inform your doctor of all allergies, especially to other calcium channel blockers.
- Disclose your complete medical history, particularly regarding liver disease or aortic stenosis.
- Exercise caution when driving or operating machinery, as Norvasc can cause dizziness.
- Limit alcohol consumption while taking this medication.
- Inform your healthcare provider if you are pregnant, planning to become pregnant, or breastfeeding.
Is Norvasc safe for elderly patients? While Norvasc can be used in older adults, they may be more sensitive to its effects, particularly dizziness and falls. Careful monitoring and possibly lower initial doses may be necessary for this population.
Long-Term Use and Monitoring: Ensuring Continued Effectiveness
Long-term use of Norvasc requires ongoing monitoring to ensure its continued effectiveness and safety.
Regular Check-ups and Tests
- Blood pressure measurements
- Kidney function tests
- Liver function tests
- Electrolyte levels
How often should blood pressure be monitored while on Norvasc? Initially, your doctor may recommend more frequent blood pressure checks, possibly weekly. As your condition stabilizes, these checks may be reduced to monthly or quarterly, depending on your individual circumstances.
Lifestyle Modifications
To maximize the benefits of Norvasc, consider implementing the following lifestyle changes:
- Maintain a healthy diet low in sodium
- Engage in regular physical activity
- Manage stress through relaxation techniques
- Quit smoking if applicable
- Limit alcohol consumption
Can lifestyle changes reduce the need for Norvasc? In some cases, adopting a healthier lifestyle may allow for a reduction in medication dosage. However, never adjust your medication without consulting your healthcare provider.
Special Populations: Tailoring Treatment
Certain groups may require special considerations when using Norvasc.
Pediatric Use
Is Norvasc safe for children? Norvasc has been studied in children aged 6-17 years for hypertension. The safety and effectiveness in younger children have not been established. Dosing for children is typically based on weight and may differ from adult dosing.
Geriatric Use
Older adults may be more sensitive to the effects of Norvasc, particularly in terms of blood pressure lowering. Careful monitoring and potentially lower starting doses may be necessary.
Pregnancy and Breastfeeding
Can Norvasc be used during pregnancy? The use of Norvasc during pregnancy should be discussed thoroughly with your healthcare provider. While some studies suggest it may be safe, the potential risks and benefits must be carefully weighed.
Is it safe to breastfeed while taking Norvasc? Amlodipine does pass into breast milk. While no adverse effects have been reported in nursing infants, it’s important to discuss this with your doctor if you are breastfeeding or plan to breastfeed.
Alternative Treatments: Exploring Other Options
While Norvasc is effective for many patients, alternative treatments may be considered in certain situations.
Other Calcium Channel Blockers
- Nifedipine
- Diltiazem
- Verapamil
Different Classes of Blood Pressure Medications
- ACE inhibitors
- Angiotensin II receptor blockers (ARBs)
- Beta-blockers
- Diuretics
Are there natural alternatives to Norvasc? While some natural remedies like CoQ10, garlic, and fish oil have shown promise in managing blood pressure, it’s crucial to discuss any alternative treatments with your healthcare provider before making changes to your medication regimen.
Future Developments: Advancing Hypertension Treatment
Research in the field of hypertension management continues to evolve, with new treatments and approaches on the horizon.
Emerging Therapies
- Combination medications for improved compliance
- Novel drug delivery systems for more consistent blood levels
- Personalized medicine approaches based on genetic profiles
What advancements can we expect in hypertension treatment? Future developments may include more targeted therapies with fewer side effects, improved long-acting formulations, and potentially even gene therapies targeting the underlying causes of hypertension.
In conclusion, Norvasc (Amlodipine) remains a cornerstone in the management of hypertension and certain types of angina. Its effectiveness, coupled with a generally favorable side effect profile, makes it a valuable tool in cardiovascular health management. However, as with any medication, it’s crucial to use Norvasc under the guidance of a healthcare professional, adhering to prescribed dosages and monitoring protocols. By understanding the benefits, potential side effects, and proper usage of Norvasc, patients can play an active role in managing their health and reducing their risk of serious cardiovascular events.
Norvasc Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing
Uses
Amlodipine is used with or without other medications to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Amlodipine belongs to a class of drugs known as calcium channel blockers. It works by relaxing blood vessels so blood can flow more easily.Amlodipine is also used to prevent certain types of chest pain (angina). It may help to increase your ability to exercise and decrease the frequency of angina attacks. It should not be used to treat attacks of chest pain when they occur. Use other medications (such as sublingual nitroglycerin) to relieve attacks of chest pain as directed by your doctor.
How to use Norvasc
Read the Patient Information Leaflet if available from your pharmacist before you start taking amlodipine and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
Take this medication by mouth with or without food as directed by your doctor, usually once daily.
If you are using the liquid form of this medication, check the manufacturer’s information or ask your pharmacist for specific directions. Some brands of the liquid form should be shaken before use, while other brands do not need to be shaken before use. Carefully measure the dose using a special measuring device/spoon. Do not use a household spoon because you may not get the correct dose
The dosage is based on your medical condition and response to treatment. Your doctor may gradually increase your dose. Follow your doctor’s instructions carefully.
Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day. Keep taking this medication even if you feel well. Most people with high blood pressure do not feel sick.
If used for angina, this medication must be taken regularly to be effective. It should not be used to treat angina when it occurs. Use other medications (such as sublingual nitroglycerin) to relieve an angina attack as directed by your doctor. Consult your doctor or pharmacist for details.
Tell your doctor if your condition does not improve or if it worsens (for example, your blood pressure readings remain high or increase, chest pain continues or worsens).
Side Effects
Dizziness, lightheadedness, swelling ankles/feet, or flushing may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.
To lower your risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.
Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Tell your doctor right away if you have any serious side effects, including: fast/irregular/pounding heartbeat, fainting.
Although this medication is effective in preventing chest pain (angina), some people who already have severe heart disease may rarely develop worsening chest pain or a heart attack after starting this medication or increasing the dose. Get medical help right away if you experience: worsening chest pain, symptoms of a heart attack (such as chest/jaw/left arm pain, shortness of breath, unusual sweating).
A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.
In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
Precautions
Before taking amlodipine, tell your doctor or pharmacist if you are allergic to it; or to other dihydropyridine calcium channel blockers (such as nisoldipine, nifedipine) or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: a certain structural heart problem (aortic stenosis), very low blood pressure, liver disease.
This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).
Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).
Older adults may be more sensitive to the effects of this drug, especially dizziness.
During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.
This drug passes into breast milk. Consult your doctor before breast-feeding.
Interactions
Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.
Some products have ingredients that could raise your blood pressure. Tell your pharmacist what products you are using, and ask how to use them safely (especially cough-and-cold products, diet aids, or NSAIDs such as ibuprofen/naproxen).
Does Norvasc interact with other drugs you are taking?
Enter your medication into the WebMD interaction checker
Overdose
If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: fainting, severe dizziness.
Do not share this medication with others.
Lifestyle changes that may help this medication work better include exercising, stopping smoking, reducing stress, and eating a low-cholesterol/low-fat diet. Consult your doctor for more details.
Lab and/or medical tests (such as blood pressure) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
Check your blood pressure regularly while taking this medication. Learn how to monitor your own blood pressure at home, and share the results with your doctor.
If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
Store the tablets at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.
Different brands of the liquid form of this medication have different storage needs. Check the product package for instructions on how to store your brand, or ask your pharmacist.
Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Images
Norvasc 2.5 mg tablet
Color: whiteShape: diamondImprint: NORVASC 2.5
This medicine is a white, diamond, tablet imprinted with “NORVASC” and “2.5”.
Norvasc 5 mg tablet
Color: whiteShape: octagonalImprint: NORVASC 5
This medicine is a white, diamond, tablet imprinted with “NORVASC” and “2.5”.
Norvasc 10 mg tablet
Color: whiteShape: roundImprint: NORVASC 10
This medicine is a white, diamond, tablet imprinted with “NORVASC” and “2.5”.
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Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.
CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.
Amlodipine Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing
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Arpimed
What Amlodipine is and what it is used for
The active ingredient in Amlodipine is amlodipine, which belongs to a group of medicines called calcium channel blockers.
Amlodipine is used to treat high blood pressure (hypertension) or a certain type of chest pain known as angina, a rare form of which is Prinzmetal’s angina or variant angina.
In patients with high blood pressure, this drug causes blood vessels to relax, making it easier for blood to pass through. In patients with angina pectoris, amlodipine improves the blood supply to the heart muscle and, accordingly, increases the flow of oxygen to it, thereby preventing the occurrence of pain in the chest. This drug does not provide immediate relief from chest pain due to angina pectoris.
What you need to know before you use Amlodipine
Do not take Amlodipine to other calcium antagonists. Allergies can be manifested by itching, redness of the skin, or difficulty breathing. Warnings and precautions Talk to your doctor or pharmacist before taking Amlodipine. If you have or have had any of the following conditions, you should inform your doctor: Children and adolescents Amlodipine has not been studied in children under 6 years of age. Amlodipine can only be used in children and adolescents with arterial hypertension aged 6 to 17 years. For more information, consult your doctor. Other medicines and Amlodipine Tell your doctor or pharmacist if you are currently taking or have recently taken any other medicines drugs, including over-the-counter drugs. Amlodipine may or may be affected by other drugs such as: Amlodipine may lower blood pressure more when other medicines are used to treat high blood pressure.
Interaction with food and drink to a more pronounced decrease in blood pressure.
Pregnancy and breastfeeding
Pregnancy
The safety of amlodipine in pregnant women has not been established. If you suspect pregnancy or are planning to become pregnant, talk to your doctor before taking this medicine.
Breastfeeding
Amlodipine has been found to pass into breast milk. If you are breast-feeding or plan to breast-feed, consult your doctor before taking this medicine.
Driving and using machines
Amlodipine may affect the ability to drive or use machines. If you feel unwell, dizzy, tired or have a headache after taking the tablets, do not drive or operate machinery and contact your doctor immediately.
Amlodipine contains sodium
practically does not contain sodium.
How to take Amlodipine
Always take your medicine exactly as your doctor or pharmacist has told you. If you have any doubts about taking the drug, consult your doctor or pharmacist.
The recommended starting dose of amlodipine is 5 mg once daily. The dose of amlodipine can be increased up to 10 mg once a day.
This medicine can be taken before or after food and drinks. This medicine should be taken at the same time of day with water. Amlodipine should not be taken with grapefruit juice.
Use in children and adolescents
For children and adolescents (6 to 17 years of age), the recommended starting dose is 2.5 mg once daily. The maximum recommended dose is 5 mg once daily. Amlodipine 5 mg tablets may be divided into two equal doses.
It is important not to stop taking the drug. Don’t wait until you run out of pills before going to the doctor.
If you have taken more Amlodipine than recommended
Taking too many tablets can cause your blood pressure to drop to dangerous levels. This may cause dizziness, weakness, or fainting. With a very strong drop in blood pressure, shock can develop. The skin becomes cold and clammy, and unconsciousness may develop. If you have taken too many Amlodipine tablets, seek medical attention immediately.
If you forget to take Amlodipine
Don’t worry. If you forget to take a tablet, skip this dose. Take the next dose at the correct time. Do not take a double dose to make up for a missed dose.
If you stop taking Amlodipine
Your doctor will tell you how long to take this medicine. If you stop taking this drug before the recommended time, you may have a relapse.
If you have any further questions on the use of this medicine, ask your doctor or pharmacist.
Possible side effects
Like all medicines, amlodipine can cause side effects, although not everyone gets them.
If you experience any of the following side effects after taking this drug, call your doctor immediately:
- sudden wheezing, chest pain, shortness of breath, or trouble breathing;
- swelling of the eyelids, face or lips;
- swelling of the tongue and throat, making breathing very difficult;
- severe skin reactions, including severe skin rash, urticaria, redness of the skin of the entire body, severe itching, blistering, peeling and swelling of the skin, inflammation of the mucous membranes (Stevens-Johnson syndrome, toxic epidermal necrolysis) or other allergic reactions;
- myocardial infarction, cardiac arrhythmia;
- inflammation of the pancreas, which can manifest itself as severe pain in the abdomen and back, accompanied by a feeling of severe malaise.
The following side effect is very common . If this effect causes you problems, or if it lasts more than a week, you should contact your doctor.
Very common : may affect more than 1 in 10 people
- Edema (fluid retention).
Often the following side effects occur. If any of them cause you problems, or if they last more than a week, you should see your doctor.
Common: may affect up to 1 in 10 people
- Palpitations (feeling your own heartbeat), hot flashes
- Abdominal pain, nausea
- Defecation disorder, diarrhoea, constipation, indigestion
- Weakness, fatigue
- Impaired vision, double vision
- Muscle cramps
- Ankle edema.
The following is a list of other reported adverse reactions. If any of these side effects become serious or if you notice side effects not listed in this leaflet, please tell your doctor or pharmacist.
Uncommon: may affect up to 1 in 100 people,
- Mood changes, anxiety, depression, insomnia
- Trembling, taste disturbances, syncope
- Numbness or tingling in limbs, loss of pain sensation
- Ringing in the ears
- Low blood pressure
- Sneezing/runny nose caused by inflammation of the nasal mucosa (rhinitis)
- Cough
- Dry mouth, vomiting
- Hair loss, increased sweating, pruritus, red spots on the skin, discoloration of the skin
- Urinary disorder, frequent urge to urinate at night, frequent urination
- Inability to achieve an erection, malaise or breast enlargement in men
- Pain, deterioration of health
- Pain in joints or muscles, back pain
- Weight gain or loss.
Rare : may affect up to 1 in 1,000 people
- Confusion,
Very rare : may affect up to 1 in 10,000 people 20
Reporting of side effects leaflet. You can also report side effects to Arpimed LLC by going to the website www.arpimed.com and filling out the appropriate form “Report a side effect or ineffectiveness of a drug” and to the Scientific Center for Expertise of Drugs and Medical Technologies named after. Academician E.Gabrielyan, by going to the website www.pharm.am in the section “Report a side effect of a drug” and fill out the form “Map of reporting a side effect of a drug”. Scientific center hotline: +37410200505; +37496220505 By reporting side effects, you help gather more information about the safety of this drug.
How to store Amlodipine
- The drug should be stored out of the reach of children, protected from moisture and light at a temperature of 15 0 C -25 0 C.
- Shelf life – 3 years. Do not take Amlodipine after the expiry date which is stated on the package. When specifying the expiration date, the last day of the specified month is meant.
- If the tablets have changed color or show other signs of deterioration, do not take the drug.
- Medicines should not be disposed of into wastewater or sewers. Ask your pharmacist how to dispose of a medicine you no longer need. These measures are aimed at protecting the environment.
Contents of the pack and additional information
What Amlodipine contains
One Amlodipine 10 mg tablet contains:
active substance: amlodipine (in the form of besylate) – 10 mg stearate.
What Amlodipine looks like and contents of the pack: oh on one side; without smell.
Tablets 10 mg
Carton containing 30 tablets with leaflet: 3 blisters of 10 tablets each.
Dispensing conditions
Available by prescription.
official instructions for use, analogues, price, availability in pharmacies
See where the instructions come from MEDI RU
Registration number:
P N015567/01-260707
Brand name: NORVASC ®
International generic name:
amlodipine.
Dosage form:
tablets.
Composition
Active ingredient: amlodipine besilate at a dose of 6.935 mg and 13.870 mg, equivalent to 5 and 10 mg of amlodipine, respectively.
Excipients: fine crystalline cellulose, anhydrous calcium hydrogen phosphate, sodium starch glycolate type A, magnesium stearate.
Description
Tablets 5 mg – white or almost white tablets in the form of an emerald (octahedron with uneven sides) with the Pfizer logo on one side and AML-5 on the other.
Tablets 10 mg – white or almost white tablets in the form of an emerald (octahedron with uneven sides) with the Pfizer logo on one side and AML-10 on the other.
Pharmacotherapeutic group:
BMKK (blocker of “slow” calcium channels).
ATX code: C08CA01.
PHARMACOLOGICAL PROPERTIES
Pharmacodynamics
Amlodipine is a derivative of dihydropyridine. By binding to dihydropyridine receptors, it blocks “slow” calcium channels, inhibits the transmembrane transition of calcium into the smooth muscle cells of the heart and blood vessels (to a greater extent – into vascular smooth muscle cells than into cardiomyocytes). It has a hypotensive and antianginal effect.
The mechanism of the hypotensive action of amlodipine is due to a direct relaxing effect on vascular smooth muscle.
Amlodipine reduces myocardial ischemia in the following two ways:
- Expands the peripheral arterioles and thus reduces the total peripheral resistance (afterload), while the heart rate remains practically unchanged, which leads to a decrease in energy consumption and myocardial oxygen demand.
- Expands the coronary and peripheral arteries and arterioles in both normal and ischemic areas of the myocardium, which increases the supply of oxygen to the myocardium in patients with vasospastic angina (Prinzmetal’s angina) and prevents the development of coronary congestion caused by smoking.
In patients with arterial hypertension, a single daily dose of Norvasc provides a decrease in blood pressure (BP) for 24 hours (both in the “lying” and “standing” positions). Due to the slow onset of action, amlodipine does not cause a sharp decrease in blood pressure.
In patients with angina pectoris, a single daily dose of the drug increases the time of exercise, delays the development of another angina attack and ST segment depression (by 1 mm) during exercise, reduces the frequency of angina attacks and the consumption of nitroglycerin.
Use in patients with ischemic heart disease (CHD)
In patients with cardiovascular diseases (including coronary atherosclerosis with lesions of one vessel and up to stenosis of 3 or more arteries and atherosclerosis of the carotid arteries), who have had a myocardial infarction, percutaneous transluminal angioplasty of the coronary arteries (TLP) or suffering from angina pectoris, the use of Norvasc prevents the development of intima-media thickening of the carotid arteries, significantly reduces mortality from cardiovascular causes, myocardial infarction, stroke, TLP. coronary artery bypass surgery, leads to a decrease in the number of hospitalizations for unstable angina and progression of chronic heart failure (CHF), reduces the frequency of interventions aimed at restoring coronary blood flow.
Use in patients with heart failure
Norvasc does not increase the risk of death or the development of complications and deaths in patients with chronic heart failure (CHF) III-IV functional class (according to NYHA) during therapy with digoxin, diuretics and ACE inhibitors. In patients with CHF I1I-IV functional class according to NYHA of non-ischemic etiology, when using Norvasc, there is a possibility of pulmonary edema. Norvasc does not have any adverse effect on metabolism and plasma lipid concentrations.
Pharmacokinetics
Suction. After oral administration at therapeutic doses, amlodipine is well absorbed, reaching peak blood concentrations 6-12 hours after ingestion. Absolute bioavailability is 64-80%. The volume of distribution is approximately 21 l/kg. Communication with plasma proteins is approximately 97.5%. Eating does not affect the absorption of amlodipine, it penetrates the blood-brain barrier.
Biotransformation/elimination. The elimination half-life (T1 / 2) from plasma is about 35-50 hours, which corresponds to the administration of the drug once a day. In patients with liver failure and severe CHF, T1 / 2 increases to 56-60 hours. The total clearance is 0.43 l / h / kg.
Steady-state plasma concentration is reached after 7-8 days of constant intake of amlodipine, it is metabolized in the liver to form inactive metabolites; 10% of the parent drug and 60% of the metabolites are excreted in the urine. Excretion in breast milk is unknown. It is not removed during hemodialysis. Use in patients with renal insufficiency. Tug from plasma in patients with renal insufficiency increases up to 60 hours. The change in the concentration of amlodipine in plasma does not correlate with the degree of impaired renal function.
Use in the elderly. In the elderly, the time required to reach the maximum concentration of amlodipine in the blood plasma, and its value, practically do not differ from those in younger people. In elderly people suffering from CHF, there was a tendency to reduce the clearance of amlodipine, which leads to an increase in the area under the concentration-time curve and T1 / 2, up to 65 hours.
INDICATIONS FOR USE
- Arterial hypertension (both in monotherapy and in combination with other antihypertensive drugs).
- Stable angina and vasospastic angina (Prinzmetal’s angina) (either alone or in combination with other antianginal agents).
CONTRAINDICATIONS
- Hypersensitivity to amlodipine and other dihydropyridip derivatives, as well as to excipients that make up the drug.
- Severe arterial hypotension
WITH CAUTION is prescribed to patients with hepatic insufficiency, CHF of non-ischemic class III-IV etiology, aortic stenosis, acute myocardial infarction (and within 1 month after it), under the age of 18 years (efficacy and safety not clearly established).
As with the appointment of other BMCC, care must be taken while taking amlodipine in patients with sick sinus syndrome, mitral stenosis, hypertrophic obstructive cardiomyopathy, arterial hypotension.
PREGNANCY AND BREASTFEEDING
The safety of Norvasc during pregnancy and lactation has not been established, therefore, use during pregnancy is possible only if the benefit to the mother outweighs the risk to the fetus and newborn. For the period of breastfeeding, it is recommended to stop either taking the drug or breastfeeding (data on the excretion of amlodipine in breast milk are not available).
DOSAGE AND ADMINISTRATION
Inside, once a day, washing down with the required volume of water (100 ml).
In hypertension and angina, the usual initial dose is 5 mg, depending on the patient’s individual response, it can be increased to a maximum of 10 mg.
Use in the elderly. It is recommended to use at usual doses, no change in the dose of the drug is required.
Use in patients with impaired liver function. Despite the fact that T1 / 2, Norvasca, like all BMCC, increases in patients with this pathology, no changes in the dosage of the drug in patients with impaired liver function are usually required (see section “Special Instructions”).
Use in renal failure. It is recommended to use in usual doses, however, a possible slight increase in T1 / 2 must be taken into account. Changing the dosage regimen of Norvasc with the simultaneous use of thiazide diuretics, beta-blockers or ACE inhibitors is not required.
SIDE EFFECTS
Further, the frequency of adverse reactions is understood as: frequent (> 1%), infrequent myocardial infarction and atrial fibrillation), myocardial infarction, chest pain, migraine.
On the part of the musculoskeletal system: not often – arthralgia, muscle cramps, myalgia, back pain, arthrosis, rarely – myasthenia gravis.
Central and peripheral nervous system: sensation of heat and “flushing” of blood to the skin of the face, increased fatigue, dizziness, headache, drowsiness, infrequently – malaise, fainting, increased sweating, asthenia, hypesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, mood lability , unusual dreams, nervousness, depression, anxiety; rarely – convulsions, apathy, agitation; very rarely – ataxia, amnesia.
Digestive tract: abdominal pain, nausea, infrequently – vomiting, changes in bowel habits (including constipation, flatulence), dyspepsia, diarrhea, anorexia, dry mouth, thirst, rarely – gingival hyperplasia, increased appetite, very rarely – gastritis, pancreatitis, hyperbilirubinemia, jaundice (usually cholestatic), increased activity of “liver” transaminases, hepatitis.
Hematopoietic system: very rarely – thrombocytopenic purpura, leukopenia, thrombocytopenia.
Metabolic disorders: very rare – hyperglycemia.
Respiratory system: not often – shortness of breath, rhinitis, very rarely – cough.
Genitourinary system: not often – frequent urination, painful urination, nocturia, impotence, very rarely – dysuria, polyuria.
Allergic reactions: not often – pruritus, rash, very rarely – angioedema, erythema multiforme, urticaria.
Other: infrequently – alopecia, ringing in the ears, gynecomastia, weight gain / decrease, visual disturbances, diplopia, accommodation disturbance, xerophthalmia, conjunctivitis, eye pain, taste perversion, chills, epistaxis, rarely – dermatitis; very rarely – parosmia, xeroderma, “cold” sweat, impaired skin pigmentation.
OVERDOSE
Symptoms: pronounced decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (there is a possibility of severe and persistent arterial hypotension, including the development of shock and death).
Treatment: Administration of activated charcoal (especially in the first 2 hours after an overdose), gastric lavage (in some cases), elevation of the limbs, active maintenance of cardiovascular function, monitoring of heart and lung function, control of circulating blood volume and diuresis.
To restore vascular tone and blood pressure, if there are no contraindications, it may be useful to use vasoconstrictor drugs. Use intravenous administration of calcium gluconate. Since amlodipine is largely bound to serum proteins, hemodialysis is not effective.
OTHER DRUG INTERACTIONS
It can be expected that inhibitors of microsomal oxidation will increase the plasma concentration of amlodipine, increasing the risk of side effects, and inducers of microsomal liver enzymes – to reduce.
Cimetidine: with the simultaneous use of amlodipine with cimetidine, the pharmacokinetics of amlodipine does not change.
Grapefruit juice: Simultaneous single dose of 240 ml of grapefruit juice and 10 mg of amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine.
Unlike other BMCs, no clinically significant interaction of Norvasc (3rd generation BMC) was found when co-administered with non-steroidal anti-inflammatory drugs (NSAIDs), especially indomethacin.
It is possible to increase the antianginal and hypotensive effect of BMCC when used together with thiazide and “loop” diuretics, verapamil, ACE inhibitors, beta-blockers and nitrates , as well as increase their hypotensive effect when used together with alpha1-blockers, antipsychotics. Although no negative inotropic effect has generally been observed with Norvasc, some CBCAs may increase the negative inotropic effect of QT prolonging antiarrhythmic drugs (eg, amiodarone and quinidine).
When combined with the use of BMCC with lithium preparations (data are not available for Norvasc), it is possible to increase the manifestation of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Amlodipine does not affect in vitro plasma protein binding of digoxin, phenigoin, warfarin and indomethacin .
Aluminum/Magnesium containing antacids: their single dose does not significantly affect the pharmacokinetics of amlodipine.
Sildepafii (Viagra): a single dose of 100 mg of sildenafil in patients with essential hypertension does not affect the pharmacokinetic parameters of amlodipine.
Atorvastatin: Repeated use of amlodipine 10 mg and atorvastatin 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.
Digoxin: Co-administration of amlodipine with digoxin in healthy volunteers does not alter serum levels and renal clearance of digoxin.
Ethanol (alcoholic beverages): when administered once and repeatedly at a dose of 10 mg, amlodipine does not significantly affect the pharmacokinetics of ethanol.
Warfarin: amlodipine does not affect changes in prothrombin time caused by warfarin.
Cyclosporine: amlodipine does not cause significant changes in the pharmacokinetics of cyclosporine.
SPECIAL INSTRUCTIONS
In the treatment of arterial hypertension, Norvasc can be used in combination with thiazide diuretics, alpha- and beta-blockers, ACE inhibitors, long-acting nitrates, sublingual nitroglycerin, NSAIDs, antibiotics and oral hypoglycemic agents.
For the treatment of angina pectoris, Norvasc may be given alone or in combination with other antianginal agents, including in patients refractory to treatment with nitrates and/or beta-blockers at adequate doses. Norvasc does not have any adverse effect on metabolism and plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes mellitus and gout.
Norvasc can also be used in cases where the patient is predisposed to vasospasm/vasoconstriction.
Patients with low body weight, patients of short stature and patients with severe hepatic impairment may require a lower dosage. During treatment, body weight control and supervision by a dentist is necessary (to prevent soreness, bleeding and gum hyperplasia).
Effects on the ability to drive and use machinery
Although while taking Norvasc, no negative effect on the ability to drive a car or other technical means was observed, however, due to a possible excessive decrease in blood pressure, the development of dizziness, drowsiness, etc. side effects should be carefully considered for the individual effect of the drug in these situations, especially at the beginning of treatment and when changing the dosing regimen.