Medicine nifedipine. Nifedipine: Uses, Side Effects, and Important Information for Patients
What are the common uses of nifedipine. How does nifedipine work to prevent angina. What are the most frequent side effects of taking nifedipine. When should you seek immediate medical attention while on nifedipine. How can patients manage common side effects of nifedipine at home.
Understanding Nifedipine: A Comprehensive Guide
Nifedipine is a calcium channel blocker medication commonly prescribed to treat various cardiovascular conditions. This article provides an in-depth look at its uses, mechanism of action, side effects, and important information for patients taking this drug.
Primary Uses and Benefits of Nifedipine
Nifedipine is primarily used for:
- Preventing certain types of chest pain (angina)
- Treating high blood pressure (hypertension)
- Managing certain types of heart rhythm disorders
For patients with angina, nifedipine can improve exercise tolerance and reduce the frequency of chest pain episodes. In hypertensive patients, it helps lower blood pressure by relaxing and widening blood vessels.
How Does Nifedipine Work?
Nifedipine belongs to a class of medications called calcium channel blockers. It works by:
- Blocking calcium channels in heart and blood vessel walls
- Reducing the amount of calcium entering cells
- Causing blood vessels to relax and widen
- Decreasing the workload on the heart
This action results in improved blood flow and reduced blood pressure, which helps alleviate symptoms associated with angina and hypertension.
Common Side Effects of Nifedipine
While nifedipine is generally well-tolerated, some patients may experience side effects. Common side effects occurring in more than 1 in 100 people include:
- Headaches
- Dizziness
- Flushing
- Palpitations (fast or irregular heartbeat)
- Swollen legs or ankles (edema)
- Constipation
These side effects are usually mild and often improve as the body adjusts to the medication. However, if they persist or become bothersome, patients should consult their healthcare provider.
Managing Common Side Effects
Patients can take steps to manage common side effects of nifedipine:
- For headaches: Rest, stay hydrated, and use over-the-counter pain relievers like paracetamol
- For dizziness: Sit or lie down until the feeling passes, and avoid driving or operating machinery
- For flushing: Reduce intake of caffeine, alcohol, and hot beverages
- For edema: Elevate legs when sitting and engage in light exercise
- For constipation: Increase fiber intake, stay hydrated, and exercise regularly
Serious Side Effects and When to Seek Medical Attention
While rare, nifedipine can cause serious side effects in less than 1 in 1,000 people. Patients should stop taking nifedipine and seek immediate medical attention if they experience:
- Yellowing of the eyes or skin (jaundice), which may indicate liver problems
- Severe chest pain that doesn’t subside after a few minutes
- Signs of a serious allergic reaction (anaphylaxis)
Recognizing Anaphylaxis
Anaphylaxis is a severe allergic reaction that requires immediate medical intervention. Symptoms include:
- Sudden swelling of lips, mouth, throat, or tongue
- Difficulty breathing or wheezing
- Tightness in the throat or trouble swallowing
- Blue or pale discoloration of skin, tongue, or lips
- Sudden confusion, drowsiness, or dizziness
- Fainting or unresponsiveness
If any of these symptoms occur, call emergency services immediately.
Important Considerations for Nifedipine Use
Patients taking nifedipine should be aware of the following:
- Take the medication as prescribed by your healthcare provider
- Do not stop taking nifedipine suddenly without consulting your doctor
- Inform your doctor of all other medications you’re taking to avoid potential interactions
- Avoid grapefruit and grapefruit juice, as they can interact with nifedipine
- Regular blood pressure monitoring may be necessary to ensure the medication is effective
Special Populations
Certain groups may require special consideration when taking nifedipine:
- Pregnant women: Nifedipine should only be used during pregnancy if the potential benefits outweigh the risks
- Breastfeeding mothers: Nifedipine can pass into breast milk, so consult your doctor before use
- Elderly patients: May be more sensitive to side effects and require dose adjustments
- Patients with liver disease: May require dose adjustments or alternative treatments
Drug Interactions and Precautions
Nifedipine can interact with various medications and substances, potentially affecting its efficacy or increasing the risk of side effects. Some important interactions include:
- Other blood pressure medications
- Certain antibiotics
- Antifungal medications
- HIV protease inhibitors
- Herbal supplements like St. John’s Wort
Always inform your healthcare provider about all medications, supplements, and herbal products you’re taking to avoid potential interactions.
Alcohol and Nifedipine
Alcohol can enhance the blood pressure-lowering effect of nifedipine, potentially leading to dizziness or fainting. Patients are advised to:
- Limit alcohol consumption while taking nifedipine
- Avoid drinking alcohol when first starting the medication or after dose changes
- Be aware of how alcohol affects them while on nifedipine
Long-term Use and Monitoring
Patients on long-term nifedipine therapy should be aware of the following:
- Regular check-ups with your healthcare provider are essential
- Blood pressure should be monitored periodically
- Liver function tests may be required occasionally
- Report any new or worsening symptoms to your doctor promptly
Long-term use of nifedipine is generally safe and effective when monitored properly. However, patients should never adjust their dosage or stop taking the medication without consulting their healthcare provider.
Lifestyle Modifications
In addition to taking nifedipine, patients can make lifestyle changes to improve their cardiovascular health:
- Maintain a healthy diet low in salt and saturated fats
- Engage in regular physical activity as approved by your doctor
- Quit smoking and limit alcohol consumption
- Manage stress through relaxation techniques or counseling
- Monitor and maintain a healthy weight
These lifestyle modifications can enhance the effectiveness of nifedipine and improve overall cardiovascular health.
Alternative Treatments and Combination Therapy
In some cases, healthcare providers may consider alternative treatments or combination therapy:
- Other calcium channel blockers (e.g., amlodipine, diltiazem)
- ACE inhibitors or ARBs for blood pressure control
- Beta-blockers for angina management
- Diuretics to reduce fluid retention
The choice of treatment depends on individual patient factors, including overall health, other medical conditions, and response to therapy. Always consult your healthcare provider before making any changes to your medication regimen.
Newer Formulations of Nifedipine
Advancements in pharmaceutical technology have led to the development of extended-release formulations of nifedipine. These newer versions offer several advantages:
- Once-daily dosing for improved convenience and adherence
- More consistent blood levels throughout the day
- Potentially fewer side effects due to smoother drug release
Discuss with your healthcare provider whether a newer formulation of nifedipine might be appropriate for your treatment plan.
Side effects of nifedipine – NHS
Common side effects
These common side effects of nifedipine happen in more than 1 in 100 people. There are things you can do to help cope with them:
Headaches
Make sure you rest and drink plenty of fluids. Try not to drink too much alcohol. Ask your pharmacist to recommend a painkiller. Paracetamol is safe to take with nifedipine.
Headaches should usually go away after the first week of taking nifedipine. Talk to your doctor if they last longer than a week or are severe.
Feeling dizzy
If nifedipine makes you feel dizzy, stop what you’re doing and sit or lie down until you feel better. Do not drive, ride a bike or operate tools or machinery until the dizziness passes. Speak to a doctor if the dizzy feelings last for more than a couple of days.
Flushing
This usually happens when you first start taking nifedipine. Try cutting down on coffee, tea and alcohol. If the flushing is also making you feel hot, it might help to keep the room cool and use a fan. You could also spray your face with cool water or sip cold or iced drinks.
The flushing should go away after a few days, so try to carry on taking nifedipine for this time. If it does not go away or is causing you problems, contact your doctor.
A fast, pounding or irregular heartbeat (palpitations)
If this happens regularly after you take your medicine, try to take it at a time when you can sit or lie down while the symptoms are at their worst. It might also help to cut down on alcohol, smoking, caffeine and big meals as these can make the problem worse.
If you have a history of heart disease, and you are having these symptoms for a long time, these symptoms do not improve, or you are concerned, speak to your doctor.
Swollen legs or ankles (oedema)
Try raising your legs when you’re sitting down.
Constipation
Eat plenty of high-fibre foods such as fresh fruit and vegetables and cereals, and drink lots of water. Try to exercise regularly, for example by going for a daily walk or run. It’s OK to occasionally use a laxative.
Speak to a doctor or pharmacist if the advice on how to cope does not help and a side effect is still bothering you or lasts more than a few days.
Serious side effects
Serious side effects after taking nifedipine are rare and happen in less than 1 in 1,000 people.
Stop taking nifedipine and call 111 straight away if the whites of your eyes turn yellow, or your skin turns yellow although this may be less obvious on brown or black skin. These can be signs of liver problems.
Immediate action required: Call 999 now if:
- you get chest pain that does not stop after a few minutes, or is new or worse if you already have angina
Chest pain is a possible sign of a heart attack and needs to be checked as soon as possible.
Serious allergic reaction
In rare cases, it’s possible to have a serious allergic reaction (anaphylaxis) to nifedipine.
Immediate action required: Call 999 now if:
- your lips, mouth, throat or tongue suddenly become swollen
- you’re breathing very fast or struggling to breathe (you may become very wheezy or feel like you’re choking or gasping for air)
- your throat feels tight or you’re struggling to swallow
- your skin, tongue or lips turn blue, grey or pale (if you have black or brown skin, this may be easier to see on the palms of your hands or soles of your feet)
- you suddenly become very confused, drowsy or dizzy
- someone faints and cannot be woken up
- a child is limp, floppy or not responding like they normally do (their head may fall to the side, backwards or forwards, or they may find it difficult to lift their head or focus on your face)
You or the person who’s unwell may also have a rash that’s swollen, raised, itchy, blistered or peeling.
These can be signs of a serious allergic reaction and may need immediate treatment in hospital.
Other side effects
These are not all the side effects of nifedipine. For a full list, see the leaflet inside your medicine packet.
Information:
You can report any suspected side effect using the Yellow Card safety scheme.
Visit Yellow Card for further information.
Page last reviewed: 18 February 2022
Next review due: 18 February 2025
Nifedipine Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing
Uses
This medication is used to prevent certain types of chest pain (angina). It may allow you to exercise more and decrease the frequency of angina attacks. Nifedipine belongs to a class of medications known as calcium channel blockers.
It works by relaxing blood vessels so blood can flow more easily. This medication must be taken regularly to be effective. 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. Consult your doctor or pharmacist for details.Older adults should discuss the risks and benefits of this medication with their doctor or pharmacist, as well as other possibly safer forms of nifedipine (such as the long-acting tablets).
How to use nifedipine oral
Take this medication by mouth with or without food as directed by your doctor, usually 3 times daily. Swallow this medication whole. Do not crush, chew, or break the capsule.
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.
Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely.
Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.
Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.
Tell your doctor if your condition worsens (for example, your chest pain worsens or is more frequent).
Side Effects
Dizziness, flushing, weakness, swelling ankles/feet, constipation, and headache may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.
To reduce 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, vision changes.
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 this medication, tell your doctor or pharmacist if you are allergic to it; 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: certain heart problems (such as heart failure, aortic stenosis), liver problems, kidney problems.
Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).
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).
Older adults may be more sensitive to the side effects of this drug, especially dizziness, constipation, or swelling ankles/feet.
During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.
This medication passes into breast milk. Consult your doctor before breast-feeding.
Interactions
See also the How to Use section.
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.
Other medications can affect the removal of nifedipine from your body, which may affect how nifedipine works. Examples include apalutamide, cimetidine, enzalutamide, mitotane, quinupristin/dalfopristin, St.
John’s wort, rifamycins (such as rifabutin, rifampin), drugs used to treat seizures (such as carbamazepine, phenytoin), among others.
Some products have ingredients that could raise your heart rate or worsen your chest pain. 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 nifedipine oral 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.
Do not share this medication with others.
Lab and/or medical tests (such as blood pressure, liver/kidney tests, electrocardiogram) may be done while you are taking this medication.
Keep all medical and lab appointments. Consult your doctor for more details.
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 at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.
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
nifedipine 10 mg capsule
Color: reddish-brownShape: oblongImprint: IMI 10
This medicine is a reddish-brown, oblong, capsule imprinted with “IMI 10”.
nifedipine 10 mg capsule
Color: whiteShape: oblongImprint: HP 194
This medicine is a reddish-brown, oblong, capsule imprinted with “IMI 10”.
nifedipine 20 mg capsule
Color: redShape: oblongImprint: N20
This medicine is a reddish-brown, oblong, capsule imprinted with “IMI 10”.
nifedipine 10 mg capsule
Color: orangeShape: oblongImprint: N10
This medicine is a reddish-brown, oblong, capsule imprinted with “IMI 10”.
nifedipine 20 mg capsule
Color: peachShape: oblongImprint: HP 195
This medicine is a reddish-brown, oblong, capsule imprinted with “IMI 10”.
nifedipine 10 mg capsule
Color: yellowShape: oblongImprint: logo and 497
This medicine is a reddish-brown, oblong, capsule imprinted with “IMI 10”.
nifedipine 20 mg capsule
Color: red brownShape: oblongImprint: logo and 530
This medicine is a reddish-brown, oblong, capsule imprinted with “IMI 10”.
nifedipine 10 mg capsule
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This medicine is a reddish-brown, oblong, capsule imprinted with “IMI 10”.
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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.
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💊 Composition of Nifedipine ✅ Use of Nifedipine Save Search for analogues Interaction Description of the active ingredients of the preparation Nifedipine The scientific information provided is general and cannot be used to make decisions. Update date: 2021.02.01 Marketing authorization holder: VALENTA PHARMACEUTICS, PJSC ATX code: C08CA05 (Nifedipine) Active substance: Rec.INN WHO registered Dosage form
Release form, packaging and composition |
– blisters (2) – packs of cardboard. 
It is metabolized during the “first pass” through the liver. Protein binding is 92-98%. Metabolized in the liver to form inactive metabolites. T 1/2 – about 2 hours Excreted mainly by the kidneys in the form of metabolites and in trace amounts unchanged; 20% is excreted through the intestines as metabolites.| I10 | Essential [primary] hypertension |
| I20 | Angina pectoris [angina pectoris] |
| I20.1 | Angina with documented spasm (Prinzmetal’s angina, variant angina) |
I73. 0 | Raynaud’s syndrome |
Dosage regimen
The method of administration and dosing regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. Compliance of the dosage form of a particular drug with indications for use and dosing regimen should be strictly observed.
Individual. For oral administration, the initial dose is 10 mg 3-4 times / day. If necessary, the dose is gradually increased to 20 mg 3-4 times / day. In special cases (variant angina pectoris, severe arterial hypertension) for a short time, the dose can be increased to 30 mg 3-4 times / day. For the relief of a hypertensive crisis, as well as an attack of angina pectoris, 10-20 mg (rarely 30 mg) can be used sublingually.
In / in for the relief of an attack of angina pectoris or hypertensive crisis – 5 mg for 4-8 hours.
Intracoronary administration for the relief of acute spasms of the coronary arteries is administered as a bolus of 100-200 mcg.
With stenosis of large coronary vessels, the initial dose is 50-100 mcg.
Maximum daily doses: when taken orally – 120 mg, when administered intravenously – 30 mg.
Side effects
From the side of the cardiovascular system: hyperemia of the skin, feeling of warmth, tachycardia, arterial hypotension, peripheral edema; rarely – bradycardia, ventricular tachycardia, asystole, increased angina attacks.
From the digestive system: nausea, heartburn, diarrhea; rarely – deterioration of liver function; in isolated cases – gingival hyperplasia. With prolonged use in high doses, dyspeptic symptoms, increased activity of hepatic transaminases, intrahepatic cholestasis are possible.
From the side of the central nervous system and peripheral nervous system: headache. With prolonged use in high doses, paresthesia, muscle pain, tremor, mild visual disturbances, and sleep disturbances are possible.
On the part of the hematopoietic system: in isolated cases – leukopenia, thrombocytopenia.
From the urinary system: increased daily diuresis. With prolonged use in high doses, impaired renal function is possible.
From the endocrine system: in isolated cases – gynecomastia.
Allergic reactions: skin rash.
Local reactions: when administered intravenously, burning at the injection site is possible.
Within 1 min after intracoronary administration, a negative inotropic effect of nifedipine, an increase in heart rate, and arterial hypotension are possible; these symptoms gradually disappear after 5-15 minutes.
Contraindications
Arterial hypotension (systolic blood pressure below 90 mmHg), collapse, cardiogenic shock, severe heart failure, severe aortic stenosis; hypersensitivity to nifedipine.
Use during pregnancy and lactation
Adequate and well-controlled studies of the safety of nifedipine in pregnancy have not been conducted. The use of nifedipine during pregnancy is not recommended.
Since nifedipine is excreted in breast milk, its use during lactation should be avoided or breast-feeding should be discontinued during treatment.
In experimental studies , embryotoxic, fetotoxic and teratogenic effects of nifedipine were detected.
Use in hepatic dysfunction
In case of liver dysfunction, nifedipine should only be used in a clinical setting under the strict supervision of a physician. In patients with impaired liver function, high doses of nifedipine should be avoided.
Use in patients with impaired renal function
In patients with impaired renal function, nifedipine should only be used in a clinical setting under strict medical supervision. In patients with impaired renal function, high doses of nifedipine should be avoided.
Elderly use
Elderly patients are more likely to have decreased cerebral blood flow due to severe peripheral vasodilation.
Special instructions
Nifedipine should only be used in the clinic under the strict supervision of a physician in acute myocardial infarction, severe cerebrovascular accident, diabetes mellitus, impaired liver and kidney function, in malignant arterial hypertension and hypovolemia, as well as in patients on hemodialysis.
In patients with impaired liver and / or kidney function, high doses of nifedipine should be avoided. Elderly patients are more likely to have reduced cerebral blood flow due to severe peripheral vasodilation.
When taken orally, nifedipine can be chewed to speed up the effect.
If chest pain occurs during treatment, nifedipine should be discontinued. Cancel nifedipine should be gradual, because with a sudden discontinuation of the reception (especially after long-term treatment), the development of a withdrawal syndrome is possible.
When intracoronary administration in the presence of stenosis of two vessels, nifedipine should not be injected into a third open vessel due to the danger of a pronounced negative inotropic effect.
During the course of treatment avoid drinking alcohol due to the risk of an excessive decrease in blood pressure.
Influence on the ability to drive vehicles and mechanisms
At the beginning of treatment, driving and other potentially hazardous activities that require quick psychomotor reactions should be avoided.
In the course of further treatment, the degree of restriction is determined depending on the individual tolerability of nifedipine.
Drug interactions
When used simultaneously with antihypertensive drugs, diuretics, phenothiazine derivatives, the antihypertensive effect of nifedipine is enhanced.
When used simultaneously with anticholinergics, memory and attention disorders may occur in elderly patients.
When used simultaneously with beta-blockers, severe arterial hypotension may develop; in some cases – the development of heart failure.
When used simultaneously with nitrates, the antianginal effect of nifedipine is enhanced.
When used simultaneously with calcium preparations, the effectiveness of nifedipine decreases due to antagonistic interaction caused by an increase in the concentration of calcium ions in the extracellular fluid.
Cases of development of muscular weakness at simultaneous use with salts of magnesium are described.
When used simultaneously with digoxin, it is possible to slow down the excretion of digoxin from the body and, consequently, increase its concentration in the blood plasma.
When used simultaneously with diltiazem, the antihypertensive effect is enhanced.
With simultaneous use with theophylline, changes in the concentration of theophylline in blood plasma are possible.
Rifampicin induces the activity of liver enzymes, accelerating the metabolism of nifedipine, which leads to a decrease in its effectiveness.
When used simultaneously with phenobarbital, phenytoin, carbamazepine, the concentration of nifedipine in the blood plasma decreases.
There are reports of an increase in plasma concentrations of nifedipine and an increase in its AUC when used simultaneously with fluconazole, itraconazole.
When used simultaneously with fluoxetine, the side effects of nifedipine may be increased.
In some cases, with simultaneous use with quinidine, a decrease in the concentration of quinidine in the blood plasma is possible, and when nifedipine is canceled, a significant increase in the concentration of quinidine is possible, which is accompanied by a prolongation of the QT interval on the ECG.
Cimetidine and, to a lesser extent, ranitidine, increase the plasma concentration of nifedipine and thus enhance its antihypertensive effect.
Ethanol may enhance the effects of nifedipine (excessive hypotension), causing dizziness and other adverse reactions.
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Nifedipine . Description of the drug in the reference book Vidal.
Nifedipine: instruction, price, analogues | film-coated tablets Technolog
Nifedipine is a calcium channel blocker in the dihydropyridine subgroup. The drug is prescribed as an antihypertensive drug (drugs that lower blood pressure) and antianginal drug.
FDA Approved Indications
1. Chronic stable angina pectoris is a clinical syndrome characterized by chest pain due to myocardial ischemia (absolute or relative impairment of myocardial blood supply) not associated with necrosis of cardiocytes.
Nifedipine reduces the frequency and strength of heart contractions; does not inhibit myocardial conduction.
2. Hypertension is a syndrome of increased systolic or diastolic blood pressure. This is a condition in which the blood vessels are constantly under increased pressure. Nifedipine can be used as monotherapy or in combination with several different drugs for the treatment of hypertension or coronary artery disease.
3. Severe hypertension during pregnancy (chronic, gestational) and postpartum hypertension (increase in blood pressure to more than 140/90 mm Hg).
Other indications
1. Primary (develops without signs of other diseases) and secondary Raynaud’s syndrome. The drug can prevent or reduce vasospasm of the extremities.
2. Alpine (altitude) pulmonary edema is the accumulation of blood plasma in the tissues of the lungs, and then in the lumen of the alveoli. Occurs against the background of acute mountain sickness.
3. Pulmonary hypertension — a group of diseases characterized by increased pressure in the pulmonary artery.
4. Achalasia (lack of relaxation) is a chronic neuromuscular disease.
5. Stones in the distal ureter.
Mechanism of action
During the depolarization phase of smooth muscle cell membranes, an influx of calcium ions occurs through voltage-gated L-type calcium channels. Nifedipine inhibits the entry of calcium ions by blocking L-type channels of vascular smooth muscle and myocardial cells. A decrease in the level of intracellular calcium leads to a decrease in peripheral resistance of arterial vessels and expansion of the coronary arteries, which leads to a decrease in systemic arterial pressure and an increase in oxygen delivery to the myocardium. Thus, nifedipine has antihypertensive and antianginal properties.
Today Nifedipine is available in fast (immediate) and extended release dosage forms. Initially, the pharmaceutical industry produced the drug only in a short-acting but fast-acting dosage form; therefore, the drug had to be taken several times a day.
It caused rapid vasodilation (relaxation of the smooth muscles in the walls of blood vessels) followed by reflex activation of the sympathetic nervous system, leading to side effects such as headache, heart palpitations, and flushing. These side effects contributed to the introduction of an extended-release preparation on the pharmaceutical market, which had a stable 24-hour antihypertensive effect and was characterized by fewer side effects. Adjustment of the dose of the drug should be carried out at intervals of 7-14 days. When switching from a fast-release preparation to a prolonged-release preparation, the same total daily dose should be used. Rapid release formulations can be taken with or without food.
Immediate-release preparations begin to act within 20 minutes, their T ½ – 4-7 hours. The prolonged-release preparation acts within 24 hours. It is metabolized in the liver with the help of cytochrome CYP 3A4. Extended release formulations have up to 89% bioavailability compared to immediate release formulations.
Bioavailability is significantly increased in patients with hepatic impairment requiring dose adjustment.
Recommended dosage regimen
Chronic stable angina:
Nifedipine immediate: 10 mg bid; the maximum dose is 180 mg / day.
Long-acting drug: 30 or 60 mg/day; the maximum daily dose is 120 mg.
Hypertension:
Nifedipine long-acting: 30 or 60 mg/day; the maximum daily dose is 120 mg.
Hypertension during pregnancy or the puerperium:
immediate action: 10 mg; may be repeated at a dose of 20 mg every 20 minutes.
Side effects
The manifestation of adverse reactions is typical for 20-30% of patients who are prescribed Nifedipine . This is primarily due to its vasodilating properties. The most common side effects include hot flashes, peripheral edema, dizziness, headache, heartburn, and nausea. Tolerance (drug addiction syndrome) is a decrease in response to repeated (repeated) administration of the drug.
This syndrome is more characteristic of immediate-release nifedipine than sustained-release preparations. Hypersensitivity reactions such as pruritus, urticaria and bronchospasm are rare. Abrupt discontinuation of the drug after prolonged use can lead to withdrawal symptoms (a group of symptoms of various combinations that occur when the drug is completely discontinued), such as hypertension or angina pectoris.
Contraindications
Hypersensitivity to nifedipine or other components of the drug. The use of the drug is contraindicated in patients with myocardial infarction with segment elevation ST . For patients with unstable angina, the use of immediate-release nifedipine is not recommended, except in cases with concomitant beta-blockade. The drug should be avoided in patients with cardiogenic shock, severe aortic stenosis, hypotension, heart failure and moderate or severe hepatic insufficiency. Nifedipine immediate-release formulations (sublingual or oral) for hypertensive emergencies are neither safe nor effective.
With cardiogenic shock, there is a sharp decrease in myocardial contractility and the situation is aggravated by the suppression of calcium ions entering the heart muscle cells. In severe aortic stenosis, nifedipine can cause ventricular collapse and dysfunction. In unstable angina pectoris, nifedipine causes a reflex increase in myocardial contractility, which increases its oxygen demand, thereby exacerbating ischemia. Nifedipine may also exacerbate vital organ hypoperfusion in patients with severe hypotension. In addition, patients with hepatic insufficiency may be unable to metabolize nifedipine, resulting in a prolongation of T ½ increases the risk of toxicity and side effects. Finally, abrupt discontinuation of treatment may reactivate angina and cause a “rebound phenomenon” in patients with CAD.
Monitoring
No need for laboratory monitoring in patients taking Nifedipine . Since nifedipine is an antihypertensive drug, clinicians (physicians working in the clinic) and patients should regularly measure blood pressure to achieve a therapeutic effect of the prescribed therapy in accordance with the recommendations of the American College of Cardiology / American Heart Association (ACC / AHA) 2017.
Patients need to constantly monitor for the development of adverse reactions, such as peripheral edema (swelling of soft tissues), dizziness, hyperemia (overflow of blood vessels of the circulatory system), etc.
Overdose. Therapy in case of overdose
The complex of first aid measures in case of overdose Nifedipine depends on the dose of the drug taken, time of meal, age and concomitant diseases of the patient. First of all, it is necessary to carry out the following measures: to ensure the patency of the respiratory tract, breathing, blood circulation. An overdose of nifedipine can lead to vasodilation, severe hypotension and reflex tachycardia. Prolonged systemic hypotension can progress to shock and even death. Activated charcoal at a dose of 1 g/kg of body weight is effective if no more than 1-2 hours have passed since the drug was taken. An intestinal irrigation procedure is possible if a prolonged-release drug was used or when taking a large amount of food.
The establishment of a nasogastric tube and lavage (lavage) of the stomach and the evacuation of gastric contents are usually ineffective. Intravenous resuscitation fluids, calcium salts, vasopressor therapy with dopamine or norepinephrine usually alleviate the patient with hypotension. The introduction of high doses of insulin – it was found that such manipulation helps to reduce the number of deaths and improve hemodynamics. In case of an overdose during therapy, it is necessary to constantly monitor the results of the ECG, the patient’s vital signs, kidney function, and the amount of urine output. Patients with an overdose of immediate-release drugs should be observed for 4-7 hours. Patients with an overdose of extended-release drugs – 24 hours. There is no specific antidote.
Application features
The drug may cause the development of hypotension, therefore, careful selection of the dose (starting from the minimum) is recommended to achieve a therapeutic effect (long-term monitoring of the patient).
Sublingual preparations are not recommended in emergencies or emergencies associated with hypertension due to lack of efficacy data and numerous severe side effects such as uncontrolled lowering of blood pressure, reflex tachycardia and cerebral ischemia/myocardial infarction (Khan K.M. et al., 2019).
Interesting research
Preterm birth is an important obstetric problem and the most common cause of neonatal death and morbidity. Therefore, the search for a way to prevent them is always of particular interest to scientists.
A double-blind, randomized clinical trial was conducted in pregnant women 26-34 weeks gestation who presented to the hospital for preterm labor. They were randomly assigned to 3 groups, which were administered: indomethacin and placebo; nifedipine and placebo; and a combination of indomethacin and nifedipine, respectively. Evaluated the inhibition of uterine contractions within 2 hours and the prevention of preterm labor within 48 hours and 7 days.