Amlodipine is a calcium channel blocker used to treat hypertension and angina, with an onset of action not clinically established and effects lasting approximately 24 hours. It works by relaxing blood vessels to lower blood pressure and can be administered in various forms, including tablets and solutions. Common side effects include peripheral edema, dizziness, and flushing, while contraindications include known sensitivity to the drug and severe hypotension risk.

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October 2, 2022
Amlodipine
medicaldialogues.in/generics/amlodipine-2721953
Indications, Uses, Dosage, Drugs Interactions, Side effects
Amlodipine
Medicine Type :
Allopathy
Prescription Type:
Prescription Required
Approval :
DCGI (Drugs Controller General of India)
Schedule
Schedule H
Pharmacological Class:
Calcium channel blocker
Therapy Class:
Antihypertensive
Innovator name:
Pfizer Medicals
Amlodipine is an antihypertensive agent belonging to the Calcium Channel Blocker class.
Amlodipine is a Calcium Channel Blocker used to treat Hypertension and Angina.
Amlodipine absorbed slowly and almost completely from the gastrointestinal tract. Peak
plasma concentrations are achieved 6-12 hours after oral administration. The estimated
bioavailability of amlodipine is 64-90%. Steady-state plasma amlodipine levels are

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achieved after 7-8 days of consecutive daily dosing. Absorption is not affected by food.
The plasma protein binding of Amlodipine is approximately 98%. Amlodipine is heavily
(approximately 90%) converted to inactive metabolites via hepatic breakdown with 10%
of the parent compound and 60% of the metabolites found excreted in the urine.
Amlodipine shows common side effects swelling of the hands, feet, ankles, or lower legs,
headache, upset stomach, nausea, stomach pain, dizziness or light-headedness,
drowsiness, excessive tiredness, flushing, etc.
Amlodipine is available in the form of Oral Tablet, Oral Solution and Oral Suspension.
Amlodipine is available in India, US, UK, Canada, Russia, China, Japan, Korea,
Singapore, and South Africa.
Amlodipine belonging to the Calcium Channel Blockers acts as an antihypertensive agent.
Mechanism of action on Hypertension
Amlodipine is considered a peripheral arterial vasodilator that exerts its action directly on
vascular smooth muscle to lead to a reduction in peripheral vascular resistance, causing a
decrease in blood pressure. Amlodipine is a dihydropyridine calcium antagonist (calcium
ion antagonist or slow-channel blocker) that inhibits the influx of calcium ions into both
vascular smooth muscle and cardiac muscle. Experimental studies imply that amlodipine
binds to both dihydropyridine and non-dihydropyridine binding sites, located on cell
membranes. The contraction of cardiac muscle and vascular smooth muscle are
dependent on the movement of extracellular calcium ions into these cells by specific ion
channels. Amlodipine blocks calcium ion influx across cell membranes with selectivity. A
stronger effect of amlodipine is exerted on vascular smooth muscle cells than on cardiac
muscle cells. Direct actions of amlodipine on vascular smooth muscle result in reduced
blood pressure.
Mechanism of action in angina
The exact mechanism by which amlodipine relieves the symptoms of angina have not
been fully elucidated to this date, however, the mechanism of action is likely twofold:
Amlodipine has a dilating effect on peripheral arterioles, reducing the total peripheral
resistance (afterload) against which the cardiac muscle functions. Since the heart rate
remains stable during amlodipine administration, the reduced work of the heart reduces
both myocardial energy use and oxygen requirements.
Dilatation of the main coronary arteries and coronary arterioles, both in healthy and
ischemic areas, is another possible mechanism of amlodipine reduction of blood pressure.
The dilatation causes an increase in myocardial oxygen delivery in patients experiencing
coronary artery spasm (Prinz metals or variant angina) and reduces coronary
vasoconstriction caused by smoking.
The Onset of action of Amlodipine is not clinically established.

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The Duration of Action for Amlodipine in the body is approximately 24 hours.
The Tmax was found within 6-12 hours following the administration of Amlodipine.
Amlodipine is available in the form of Oral Tablet, Oral Solution and Oral Suspension.
Amlodipine tablet, solution and suspension taken orally. Usually once a day.
Amlodipine is a medicine used for the treatment of high blood pressure. This medicine
works by relaxing the blood vessels which make the blood flow easily, thus lowering the
blood pressure. This will reduce your risk of heart attack or a stroke by making it easier
for your heart to pump blood around your body.
Amlodipine is an antihypertensive agent belonging to Calcium Channel Blockers. It
inhibits calcium ion from entering the “slow channels” or select voltage-sensitive areas of
vascular smooth muscle and myocardium during depolarization, producing a relaxation of
coronary vascular smooth muscle and coronary vasodilation; increases myocardial oxygen
delivery in patients with vasospastic angina. Amlodipine directly acts on vascular smooth
muscle to produce peripheral arterial vasodilation reducing peripheral vascular resistance
and blood pressure.
Amlodipine is approved for use in the following clinical indications
HYPERTENSION
Amlodipine is 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. These benefits have been seen in controlled
trials of antihypertensive drugs from a wide variety of pharmacologic classes including
Amlodipine.
CORONARY ARTERY DISEASE (CAD)
Chronic Stable Angina
Amlodipine is indicated for the symptomatic treatment of chronic stable angina.
Amlodipine may be used alone or in combination with other antianginal agents.
Vasospastic Angina (Prinz metals Or Variant Angina)
Amlodipine is indicated for the treatment of confirmed or suspected vasospastic angina.
Amlodipine may be used as monotherapy or in combination with other antianginal
agents.
Angiographically Documented CAD
In patients with recently documented CAD by angiography and without heart failure or an
ejection fraction <40%, Amlodipine is indicated to reduce the risk of hospitalization for
angina and to reduce the risk of a coronary revascularization procedure.

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Hypertension
Adult Dose
Initial dose: 5 mg orally once a day
Maintenance dose: 5 to 10 mg orally once a day
Maximum dose: 10 mg/day
Pediatric Dose (6 to 17 years)
Maintenance dose: 2.5 to 5 mg orally once a day
Maximum dose: 5 mg/day
Pediatric dose (<6 years)
Limited data available:
Oral: Initial: 0.1 mg/kg/dose once daily; titrate based on clinical response.
Maximum daily dose: 0.6 mg/kg/day or 5 mg/day
Geriatric Dose
Initial dose: 2.5 mg orally once a day
Maintenance dose: 2.5 to 10 mg orally once a day
Maximum dose: 10 mg/day
Angina Pectoris
Adult Dose
Maintenance dose: 5 to 10 mg orally once a day
Maximum dose: 10 mg/day
Geriatric Dose
Initial dose: 5 mg orally once a day
Maintenance dose: 5 to 10 mg orally once a day
Maximum dose: 10 mg/day
Coronary Artery Disease
Maintenance dose: 5 to 10 mg orally once a day

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Maximum dose: 10 mg/day
Amlodipine is available in various strengths as 2.5mg, 5mg, 10mg and 1mg/mL(150mL).
Amlodipine is available in the form of Oral Tablet, Oral Solution and Oral Suspension.
Avoid grapefruit juice while taking Amlodipine.
Amlodipine is contraindicated in patients with known sensitivity towards Amlodipine.
Hypotension
Symptomatic hypotension is possible, particularly in patients with severe aortic stenosis.
Because of the gradual onset of action, acute hypotension is unlikely.
Increased Angina or Myocardial Infarction
Worsening angina and acute myocardial infarction can develop after starting or
increasing the dose of Amlodipine, particularly in patients with severe obstructive
coronary artery disease.
Beta-Blocker
Withdrawal is not a beta-blocker and therefore gives no protection against the dangers of
abrupt beta-blocker withdrawal; any such withdrawal should be by gradual reduction of
the dose of beta-blocker.
Patients with Hepatic Failure
Because Amlodipine is extensively metabolized by the liver and the plasma elimination
half-life (t 1/2) is 56 hours in patients
Alcohol Warning
No information is available.
Breast Feeding Warning
It is not known whether amlodipine is excreted in human milk. In the absence of this
information, it is recommended that nursing be discontinued while Amlodipine is
administered.
Pregnancy Warning
Pregnancy category C: Animal reproduction studies have shown an adverse effect on
the fetus and there are no adequate and well-controlled studies in humans, but potential
benefits may warrant use of the drug in pregnant women despite potential risks.
Food Warning

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Avoid grapefruit juice while taking Amlodipine.
Common Adverse effects
Peripheral edema, Flushing, palpitations, Pruritus, skin rash, Abdominal pain, nausea,
Male sexual disorder, Asthenia, dizziness, drowsiness, Muscle cramps, Dyspnea.
Rare Adverse effects
Peripheral ischemia, sinus tachycardia, syncope, vasculitis, Diaphoresis, erythema
multiforme, Hot flash, hyperglycemia, weight gain, weight loss, Anorexia, constipation,
dysphagia, flatulence, gingival hyperplasia, pancreatitis, vomiting, xerostomia, Difficulty
in micturition, female sexual disorder, nocturia, urinary frequency, Leukopenia, purpuric
disease, thrombocytopenia, Angioedema, hypersensitivity reaction, Abnormal dreams,
anxiety, depersonalization, depression, hypoesthesia, insomnia, malaise, pain,
paresthesia, peripheral neuropathy, rigors, tremor, vertigo, Arthralgia, back pain,
myalgia, osteoarthritis, Conjunctivitis, diplopia, eye pain, Tinnitus, Epistaxis.
CYP3A Inhibitors
Co-administration with CYP3A inhibitors (moderate and strong) results in increased
systemic exposure to amlodipine and may require dose reduction. Monitor for symptoms
of hypotension and edema when amlodipine is co-administered with CYP3A inhibitors to
determine the need for dose adjustment.
CYP3A Inducers
No information is available on the quantitative effects of CYP3A inducers on amlodipine.
Blood pressure should be closely monitored when amlodipine is co-administered with
CYP3A inducers.
Sildenafil
Monitor for hypotension when sildenafil is co-administered with amlodipine.
Simvastatin
Co-administration of simvastatin with amlodipine increases the systemic exposure of
simvastatin. Limit the dose of simvastatin in patients on amlodipine to 20 mg daily.
Immunosuppressants
Amlodipine may increase the systemic exposure of cyclosporine or tacrolimus when co-
administered. Frequent monitoring of trough blood levels of cyclosporine and tacrolimus
is recommended and adjust the dose when appropriate.
The common side effects of Amlodipine include the following
Common

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Swelling of the hands, feet, ankles, or lower legs, headache, upset stomach, nausea,
stomach pain, dizziness or light-headedness, drowsiness, excessive tiredness, flushing.
Rare
More frequent or more severe chest pain, rapid, pounding, or irregular heartbeat,
fainting.
Pregnancy
Pregnancy Category C
There are no adequate and well-controlled studies in pregnant women. Amlodipine
should be used during pregnancy only if the potential benefit justifies the potential risk to
the fetus. No evidence of teratogenicity or other embryo/fetal toxicity was found when
pregnant rats and rabbits were treated orally with amlodipine maleate at doses up to 10
mg amlodipine/kg/day (respectively, 8 times2 and 23 times2 the maximum
recommended human dose of 10 mg on a mg/m2 basis) during their respective periods of
major organogenesis. However, litter size was significantly decreased (by about 50%) and
the number of intrauterine deaths was significantly increased (about 5-fold) in rats
receiving amlodipine maleate at a dose equivalent to 10 mg amlodipine/kg/day for 14
days before mating and throughout mating and gestation. Amlodipine maleate has been
shown to prolong both the gestation period and the duration of labor in rats at this dose.
Nursing Mothers
It is not known whether amlodipine is excreted in human milk. In the absence of this
information, it is recommended that nursing be discontinued while Amlodipine is
administered.
Pediatric Use
Effect of Amlodipine on blood pressure in patients less than 6 years of age is not known.
Geriatric Use
Clinical studies of Amlodipine did not include sufficient numbers of subjects aged 65 and
over to determine whether they respond differently from younger subjects. Other reported
clinical experience has not identified differences in responses between the elderly and
younger patients. In general, dose selection for an elderly patient should be cautious,
usually starting at the low end of the dosing range, reflecting the greater frequency of
decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug
therapy. Elderly patients have decreased clearance of amlodipine with a resulting increase
of AUC of approximately 40–60%, and a lower initial dose may be required.
Overdosage might be expected to cause excessive peripheral vasodilation with
marked hypotension and possibly a reflex tachycardia. In humans, experience with
intentional overdosage of Amlodipine is limited.

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Single oral doses of amlodipine maleate equivalent to 40 mg amlodipine/kg and 100
mg amlodipine/kg in mice and rats, respectively, caused deaths. Single oral
amlodipine maleate doses equivalent to 4 or more mg amlodipine/kg or higher in
dogs (11 or more times the maximum recommended human dose on a mg/m2 basis)
caused a marked peripheral vasodilation and hypotension.
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 is highly protein bound, hemodialysis is not likely to be of benefit.
Pharmacodynamic
Amlodipine has a strong affinity for cell membranes, modulating calcium influx by
inhibiting selected membrane calcium channels. This drug's unique binding properties
allow for its long-acting action and less frequent dosing regimen.
Pharmacokinetics
Absorption
Amlodipine absorbed slowly and almost completely from the gastrointestinal tract. Peak
plasma concentrations are achieved 6-12 hours after oral administration. The estimated
bioavailability of amlodipine is 64-90%. Steady-state plasma amlodipine levels are
achieved after 7-8 days of consecutive daily dosing. Absorption is not affected by food.
Distribution
The plasma protein binding of Amlodipine is approximately 98%.
Metabolism and Excretion
Amlodipine is heavily (approximately 90%) converted to inactive metabolites via hepatic
breakdown with 10% of the parent compound and 60% of the metabolites found excreted
in the urine. Ex vivo studies have shown that about 93% of the circulating drug is bound
to plasma proteins in hypertensive patients. Characteristics that add to amlodipine's
unique pharmacologic profile include nearly complete absorption, late-peak plasma
concentrations, high bioavailability, and slow hepatic breakdown. Approximately 10% of a
given dose is excreted in the urine.
There are some clinical studies of the drug Amlodipine mentioned below:
1. Levine CB, Fahrbach KR, Frame D, Connelly JE, Estok RP, Stone LR, Ludensky V.
Effect of amlodipine on systolic blood pressure. Clinical therapeutics. 2003 Jan
1;25(1):35-57.

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2. Pitt B, Byington RP, Furberg CD, Hunninghake DB, Mancini GJ, Miller ME, Riley
W, Prevent Investigators. Effect of amlodipine on the progression of atherosclerosis
and the occurrence of clinical events. Circulation. 2000 Sep 26;102(13):1503-10.
3. Burges RA, Dodd MG, Gardiner DG. Pharmacologic profile of amlodipine. The
American Journal of Cardiology. 1989 Nov 7;64(17):I10-20.
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019787s047lbl.pdf
https://www.uptodate.com/contents/amlodipine-drug-information
https://go.drugbank.com/drugs/DB00381
https://www.drugs.com/amlodipine.html
https://medlineplus.gov/druginfo/meds/a692044.html
https://reference.medscape.com/drug/katerzia-norvasc-amlodipine-342372
https://www.rxlist.com/consumer_amlodipine_norvasc/drugs-condition.htm
Jyoti Suthar
Jyoti is a Post graduate in Pharmaceutics ( M Pharm) She did her
graduation ( B Pharm) From SSR COLLEGE OF PHARMACY And
thereafter did her M Pharm specialized in Pharmaceutics from SSR
COLLEGE OF PHARMACY
Dr JUHI SINGLA
Dr JUHI SINGLA has completed her MBBS from Era’s Lucknow
Medical college and done MD pharmacology from SGT UNIVERSITY
Gurgaon. She can be contacted at editorial@medicaldialogues.in.
Contact no. 011-43720751