Amlodipine

What is Amlodipine?

• Amlodipine (Amvaz; Katerzia; Norvasc), is a calcium channel blocker.

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Amlodipine

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What are the uses of this medicine?

• Amlodipine (Amvaz; Katerzia; Norvasc) is used alone or in combination with other antihypertensive and antianginal agents for the treatment of:

Hypertension:

• Amlodipine besylate tablets are indicated for the treatment of hypertension, to lower blood pressure.
• Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.

Coronary Artery Disease:

• Chronic Stable Angina
• Vasospastic Angina (Prinzmetal's or Variant Angina)
• Angiographically Documented Coronary Artery Disease in patients without heart failure or an ejection fraction

How does this medicine work?

• Amlodipine (am loe' di peen) belongs to the dihydropyridine class of calcium channel blockers and is used in the treatment of both hypertension and angina pectoris.
• Like other calcium channel blockers, amlodipine acts by blocking the influx of calcium ions into vascular smooth muscle and cardiac muscle cells during membrane depolarization.
• This action causes relaxation of vascular and arterial smooth muscle cells, resulting in arterial vasodilation and a decrease in cardiac work and oxygen consumption.

The precise mechanisms by which amlodipine relieves angina have not been fully delineated, but are thought to include the following:

Exertional Angina:

• In patients with exertional angina, amlodipine besylate reduces the total peripheral resistance (afterload) against which the heart works and reduces the rate pressure product, and thus myocardial oxygen demand, at any given level of exercise.

Vasospastic Angina:

• Amlodipine besylate has been demonstrated to block constriction and restore blood flow in coronary arteries and arterioles in response to calcium, potassium epinephrine, serotonin and thromboxane A2 analog in experimental animal models and in human coronary vessels in vitro.
• This inhibition of coronary spasm is responsible for the effectiveness of amlodipine besylate in vasospastic (Prinzmetal's or variant) angina.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are allergic to amlodipine (the active ingredient in amlodipine besylate tablets), or to the inactive ingredients.

What drug interactions can this medicine cause?

Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• certain medications for seizures such as carbamazepine (Carbatrol, Equetro, Tegretol), phenytoin (Dilantin, Phenytek), and phenobarbital
• clarithromycin (Biaxin, in Prevpac)
• cyclosporine (Gengraf, Neoral, Sandimmune)
• efavirenz (Sustiva)
• indinavir (Crixivan)
• itraconazole (Onmel, Sporanox)
• ketoconazole (Nizoral)
• lovastatin (Altoprev, in Advicor)
• nefazodone
• nelfinavir (Viracept)
• nevirapine (Viramune)
• rifabutin (Mycobutin)
• rifampin (Rifadin, Rimactane, in Rifamate), ritonavir (Norvir, in Kaletra), simvastatin (Zocor, in Simcor, in Vytorin), and tacrolimus (Astragraf SL, Prograf)

Is this medicine FDA approved?

• Amlodipine was approved in the United States in 1992 and it remains in wide use, with several million prescriptions filled yearly.
• Current indications include hypertension and coronary artery disease (angina pectoris).

How should this medicine be used?

Recommended dosage:

In Adults:

• The usual initial antihypertensive oral dose of amlodipine besylate tablets is 5 mg once daily, and the maximum dose is 10 mg once daily.
• Small, fragile, or elderly patients, or patients with hepatic insufficiency may be started on 2.5 mg once daily and this dose may be used when adding amlodipine besylate tablets to other antihypertensive therapy.

For Angina:

• The recommended dose for chronic stable or vasospastic angina is 5 to 10 mg, with the lower dose suggested in the elderly and in patients with hepatic insufficiency.
• Most patients will require 10 mg for adequate effect.

For Coronary artery disease:

• The recommended dose range for patients with coronary artery disease is 5 to 10 mg once daily.

In Children:

• The effective antihypertensive oral dose in pediatric patients ages 6 to 17 years is 2.5 mg to 5 mg once daily.
• Doses in excess of 5 mg daily have not been studied in pediatric patients.

Administration:

• Take amlodipine besylate once a day, with or without food.
• It may be easier to take your dose if you do it at the same time every day, such as with breakfast or dinner, or at bedtime.
• Do not take more than one dose of amlodipine besylate at a time.
• If you miss a dose, take it as soon as you remember.
• Do not take amlodipine besylate if it has been more than 12 hours since you missed your last dose. Wait and take the next dose at your regular time.
• Other medicines: You can use nitroglycerin and amlodipine besylate together.
• If you take nitroglycerin for angina, don't stop taking it while you are taking amlodipine besylate.
• While you are taking amlodipine besylate, do not stop taking your other prescription medicines, including any other blood pressure medicines, without talking to your doctor.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 2.5 mg, 5 mg and 10 mg

This medicine is available in fallowing brand namesː

• Amvaz; Katerzia; Norvasc

Recently, multiple fixed dose combinations of amlodipine with other agents have become available including the following:

• amlodipine (5 or 10 mg) with aliskiren (150 or 300 mg: Tekamlo),
• aliskiren with hydrochlorothiazide (12.5 and 25 mg: Amturnide),
• atorvastatin (10, 20, 40 or 80 mg: Caduet and generic),
• benzapril (10, 20 or 40 mg: Lotrel, Amlobenz, and generic),
• benzapril and hydrochlorothiazide (12.5 and 25 mg: Tribenzor),
• olmesaran (20 and 40 mg: Azor), and telmisartan (40 or 80 mg: Twynsta),
• valsartan (160 and 320 mg: Exforge) and
• valsartan with hydrochlorothiazide (25 mg: Exforge HCT).

What side effects can this medication cause?

The most common side effects of this medicine may include:

• swelling of your legs or ankles
• tiredness, extreme sleepiness
• stomach pain, nausea
• dizziness
• flushing (hot or warm feeling in your face)
• arrhythmia (irregular heartbeat)
• heart palpitations (very fast heartbeat)
• muscle rigidity, tremor and/or abnormal muscle movement

Less common, but serious side effects may include:

• more frequent or more severe chest pain
• rapid, pounding, or irregular heartbeat
• fainting

What special precautions should I follow?

• Symptomatic hypotension is possible, particularly in patients with severe aortic stenosis. Because of the gradual onset of action, acute hypotension is unlikely.
• Worsening angina and acute myocardial infarction can develop after starting or increasing the dose of amlodipine besylate, particularly in patients with severe obstructive coronary artery disease.
• Titrate slowly when administering amlodipine besylate to patients with severe hepatic impairment.
• Amlodipine has been linked to a low rate of serum enzyme elevations during therapy and to rare instances of clinically apparent acute liver injury.
• Limited available data from a published clinical lactation study reports that amlodipine is present in human milk. There is no available information on the effects of amlodipine on milk production.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• peripheral vasodilation
• hypotension
• reflex tachycardia

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• If massive overdose should occur, initiate active cardiac and respiratory monitoring.
• Frequent blood pressure measurements are essential.
• Should hypotension occur, provide cardiovascular support including elevation of the extremities and the judicious administration of fluids.
• If hypotension remains unresponsive to these conservative measures, consider administration of vasopressors (such as phenylephrine) with attention to circulating volume and urine output.
• As amlodipine besylate is highly protein bound, hemodialysis is not likely to be of benefit.

Can this medicine be used in pregnancy?

• The limited available data based on post-marketing reports with amlodipine besylate use in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage.

Can this medicine be used in children?

• Effect of amlodipine besylate on blood pressure in patients less than 6 years of age is not known.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• Amlodipine besylate

Inactive ingredients:

• calcium phosphate, dibasic, anhydrous
• magnesium stearate
• cellulose, microcrystalline
• sodium starch glycolate type a potato

Who manufactures and distributes this medicine?

Distributed by:

• Amneal Pharmaceuticals LLC
• Bridgewater, NJ

What should I know about storage and disposal of this medication?

• Keep amlodipine besylate away from children.
• Store amlodipine besylate tablets at room temperature (between 59° and 86°F).
• Keep amlodipine besylate out of the light.
• Do not store in the bathroom.
• Keep amlodipine besylate in a dry place.

calcium channel blockers

• amlodipine, diltiazem, felodipine, isradipine, nicardipine, nifedipine, nimodipine, nisoldipine, verapamil

Antihypertensive agents

• Dailymed label info on Amlodipine
• FDA Amlodipine

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