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Amlodipine (Besylate) - Indications, dose, side effects ...

Amlodipine besylate is a medication primarily used to treat high blood pressure and chest pain (angina). It belongs to a class of drugs called calcium channel blockers. Amlodipine works by relaxing blood vessels, allowing blood to flow more easily and reducing the workload on the heart.

Strong calcium channel blocker amlodipine is used to treat the following conditions:

Symptomatic chronic stable angina
Treatment of confirmed or suspected vasospastic angina
Treatment of hypertension.
Raynaud's phenomenon

Amlodipine Dose in Adults

Amlodipine dose in treatment of angina:

For chronic stable angina:

A common starting dose of amlodipine is 5 to 10 milligrams once a day.

Note:

If you have chronic stable angina and are already taking a beta-blocker but still have symptoms, your doctor may add amlodipine.
If you have contraindications or bad side effects with beta-blockers, amlodipine can be used as an alternative therapy.

For vasospastic angina, which involves spasms in the blood vessels, amlodipine can be used alone or with nitrates.

The typical dose is 5 to 10 milligrams once daily.

Amlodipine dose in Hypertension:

The typical starting dose of amlodipine is 2.5 to 5 milligrams once a day.
Your doctor will adjust the dose based on how your body responds, usually every 1 to 2 weeks, up to a maximum of 10 milligrams per day.
It's important to note that higher doses may not provide additional benefit and could lead to more side effects.

Note:

If your blood pressure is significantly higher than the goal by 20/10 mm Hg or more, your doctor may combine amlodipine with another medication like an ACE inhibitor, ARB, or thiazide diuretic.
If your blood pressure is just slightly above the goal, your doctor might start you on a single medication first (monotherapy), but many patients eventually need more than one medication (combination therapy).

Amlodipine dose in Raynaud phenomenon:

The typical starting dose is 5 milligrams once a day.
Your doctor may adjust the dose gradually based on how you respond to the medication and how well you tolerate it.
The maximum recommended dose is 20 milligrams per day.

Amlodipine Dose in Children

Amlodipine dose in children with Hypertension:

Children aged 1 to 5 years:

Limited data are available, but there's some indication that younger children may need higher doses per kilogram of body weight compared to older children.
Initial doses in this age group have ranged from 0.05 to 0.1 milligrams per kilogram of body weight per day.
However, these doses are subject to adjustment based on individual response.

Children and adolescents aged 6 to 17 years:

The typical starting dose is 2.5 to 5 milligrams once daily.
Doses higher than 5 milligrams per day have not been fully studied.
In a study involving children aged 6 to 16 years, both 2.5 milligrams and 5 milligrams once daily doses were effective in reducing systolic blood pressure.
The recommended initial dose is 0.06 milligrams per kilogram of body weight per day, up to a maximum of 0.34 milligrams per kilogram per day (not exceeding 10 milligrams total per day).

In both age groups, the dose may be adjusted based on the individual's response and tolerability.

Pregnancy Risk factor C

Amlodipine can pass from a pregnant person to their baby.
Studies have shown that the amount of amlodipine in the baby's bloodstream at birth is about one-third of what's in the mother's blood.
In some cases, the levels in newborns were too low to even measure within 48 hours of birth.
There isn't a lot of information about using amlodipine during pregnancy, but some studies suggest that it might not be the best option for treating high blood pressure in pregnant people because of changes in how the body processes drugs during pregnancy.
It's important to treat high blood pressure during pregnancy because it can cause problems for both the baby and the mother, but doctors usually prefer other medications over amlodipine in pregnant patients.

Amlodipine uses during breastfeeding

Amlodipine can pass into breast milk, but the amount is relatively low compared to the mother's dose.
Studies have shown that the relative amount of amlodipine in breast milk, compared to the mother's weight-adjusted dose, is about 4.18%, with some variability.
This falls within the acceptable range for breastfeeding, which is typically considered safe when the relative infant dose is below 10%.
Even though the maximum relative infant dose calculated was 15.2%, adverse events were not observed in breastfed infants in the study.
This suggests that breastfeeding while taking amlodipine is generally considered safe for both the mother and the baby.

Amlodipine Dose in Renal Disease:

For individuals with end-stage renal disease (ESRD) undergoing dialysis, such as hemodialysis or peritoneal dialysis, dosage adjustment of amlodipine is not necessary.
Both hemodialysis and peritoneal dialysis do not significantly increase the elimination of amlodipine from the body.
Therefore, there is no need for a supplemental dose of amlodipine in these patients.

Amlodipine Dose in Liver Disease:

For chronic stable angina and vasospastic angina, the typical starting dose of amlodipine is 5 milligrams once a day when taken orally. However, in patients with severe liver problems, the dose should be adjusted carefully, starting at the same 5-milligram dose but titrating slowly as needed.
For hypertension, the usual starting dose is 2.5 milligrams once daily when taken orally. Again, in patients with severe liver impairment, the dose should be titrated slowly and cautiously.

Common side effects of amlodipine:

Cardiovascular:
- Peripheral edema
Respiratory:
- Pulmonary edema
Cardiovascular:
- Palpitations and flushing
Central nervous system:
- Fatigue, dizziness, male sexual disorder, and drowsiness.
Dermatologic:
- Pruritus and skin rash
Gastrointestinal:
- Nausea, constipation and abdominal pain
Neuromuscular & skeletal:
- Muscle cramps and weakness.
Respiratory:
- Dyspnea

Contraindications to Amlodipine include:

In both Canadian and US labeling, amlodipine is contraindicated if there's a known hypersensitivity to amlodipine itself or any component of the medication.
In Canadian labeling, additional contraindications include hypersensitivity to other dihydropyridines, severe hypotension (when systolic blood pressure is less than 90 mm Hg), and breastfeeding.
It's important to adhere to these contraindications to prevent adverse reactions and ensure safe use of the medication.
If any hypersensitivity reactions or severe hypotension occur, medical attention should be sought promptly.

Warnings and Precautions

Angina and Myocardial infarction:

When starting or adjusting the dosage of dihydropyridine calcium channel blockers, including amlodipine, there's a risk of increased angina or myocardial infarction (MI).
This can happen due to reflex tachycardia, which means the heart rate increases in response to the medication, potentially leading to more angina or MI episodes, especially in patients with obstructive coronary disease.
This risk is higher when dihydropyridine calcium channel blockers are used without concurrent beta-blockade.

Hypotension:

Symptomatic hypotension, where a person experiences low blood pressure with symptoms like dizziness or fainting, can happen with amlodipine.
However, it's unlikely to occur immediately after starting the medication because amlodipine takes time to have its full effect.
When using amlodipine to lower blood pressure, the rate at which blood pressure is reduced should be tailored to the individual's clinical needs.
This means adjusting the dose gradually and monitoring the patient's response closely to avoid excessive drops in blood pressure that could lead to symptoms.

Peripheral edema

Peripheral edema, swelling in the arms, legs, or ankles, is the most common side effect of amlodipine.
It typically appears within 2 to 3 weeks after starting the medication.
This swelling occurs because amlodipine relaxes blood vessels, allowing fluid to leak into surrounding tissues.
While peripheral edema can be uncomfortable, it's usually not serious.

Aortic stenosis and hypertrophic cardiomyopathy:

In patients with severe aortic stenosis, extreme caution should be exercised when using amlodipine.
Aortic stenosis is a condition where the heart's aortic valve is narrowed, restricting blood flow from the heart to the body.
Amlodipine may reduce coronary perfusion, which means it could decrease blood flow to the coronary arteries that supply the heart muscle.
This reduction in blood flow could lead to myocardial ischemia, a condition where the heart muscle doesn't receive enough oxygen-rich blood.
Therefore, patients with severe aortic stenosis should be closely monitored if prescribed amlodipine, and alternative treatment options may be considered.

Heart failure:

In patients with heart failure with reduced ejection fraction (HFrEF), calcium channel blockers are generally avoided due to concerns about worsening heart function.
However, amlodipine may be considered for managing hypertension or ischemic heart disease in these patients.

Hepatic impairment:

In patients with hepatic impairment (liver problems), amlodipine should be used cautiously.
Depending on the severity of the impairment, a lower starting dose may be necessary.
Additionally, in patients with severe hepatic impairment, the dose should be titrated slowly and carefully.
This cautious approach helps to ensure that the medication is well tolerated and effective while minimizing the risk of adverse effects.

Hypertrophic cardiomyopathy (HCM) with outflow tract obstruction:

In patients with hypertrophic cardiomyopathy (HCM) and outflow tract obstruction, amlodipine should be used cautiously.
This caution is due to the fact that amlodipine can reduce afterload, potentially exacerbating symptoms associated with this condition.
HCM involves thickening of the heart muscle, particularly the septum between the heart chambers, which can lead to obstruction of blood flow out of the heart.
By reducing afterload, amlodipine may inadvertently increase the obstruction and worsen symptoms in these patients.
Therefore, careful monitoring and consideration of alternative treatment options may be necessary in individuals with HCM and outflow tract obstruction who require treatment for conditions like hypertension or angina.

Amlodipine: Drug Interaction

Note: Drug Interaction Categories:

Risk Factor C: Monitor When Using Combination
Risk Factor D: Consider Treatment Modification
Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy).
Alfuzosin	May intensify blood pressure lowering medications' hypotensive effects.
Alpha1-Blockers	May intensify calcium channel blockers' hypotensive effects.
Amphetamines	May lessen the effects of antihypertensive medications in treating hypertension.
Antipsychotic Agents, Second Generation (Atypical)	Antipsychotic drugs can have a greater hypotensive effect when blood pressure-lowering medications are used (Second Gen [Atypical]).
Aprepitant	High risk of inhibitors increasing serum CYP3A4 substrate concentrations. It's crucial to keep an eye out for any heightened pharmacologic effects of aripiprazole. Depending on the indication and/or concurrent medication, aripiprazole dosage modifications may be required. Consult the interaction monograph in its entirety for more details.
ARIPiprazole	Weak CYP3A4 Inhibitors may raise serum levels of ARIPiprazole.
Atosiban	Calcium channel blockers may make atosiban's toxic/unwanted effects worse. The likelihood of developing pulmonary edoema or dyspnea may rise.
Barbiturates	Metabolism may be boosted by calcium channel blockers. Monitoring: When calcium channel blockers are administered in conjunction with barbiturate medication, look for any diminished therapeutic effects. It could be necessary to change the dosage of calcium channel blockers. The concurrent use of phenobarbital and nimodipine is not recommended.
Barbiturates	May intensify blood pressure lowering medications' hypotensive effects.
Benperidol	May intensify blood pressure lowering medications' hypotensive effects.
Bosentan	Could decrease serum levels of CYP3A4 substrates (High Risk with Inducers).
Brigatinib	May lessen the effects of antihypertensive medications in treating hypertension. The bradycardic effects of antihypertensive medications may be exacerbated by brutinib.
Brimonidine (Topical)	Might increase the hypotensive effects of Blood Pressure Lowering Agents.
Calcium Channel Blockers (Nondihydropyridine)	Dihydropyridine, a calcium channel blocker, may increase the hypotensive effects of calcium channel blockers (Nondihydropyridine). Nondihydropyridine may raise the serum level of calcium channel blockers (Dihydropyridine).
Calcium Salts	The therapeutic benefits of calcium channel blockers can be lessened as a result.
Clofazimine	High likelihood that inhibitors will raise serum concentrations of CYP3A4 substrates
Clopidogrel	Calcium channel blockers may reduce the therapeutic effects of clopidogrel.
CycloSPORINE Systemic	Dihydropyridine, a calcium channel blocker, may raise the serum level of CycloSPORINE Systemic. The serum levels of calcium channel blockers (Dihydropyridine) may increase after using CycloSPORINE Systemic.
Moderate CYP3A4 Inducers	Could decrease serum levels of CYP3A4 substrates (High Risk with Inducers).
Moderate CYP3A4 inhibitors	May raise serum levels of amelodipine
Strong CYP3A4 inhibitors	May increase serum AmLODIPine concentrations
Dapoxetine	May intensify calcium channel blockers' orthostatic hypotensive effects.
Deferasirox	Could decrease serum levels of CYP3A4 substrates (High Risk with Inducers).
Dexmethylphenidate	Antihypertensive agents may have a less therapeutic effect.
Diazoxide	May intensify blood pressure lowering medications' hypotensive effects.
Dofetilide	CYP3A4 inhibitors could increase the amount of dofetilide (Weak).
DULoxetine	By reducing blood pressure, DULoxetine may exacerbate hypotension.
Duvelisib	High likelihood that inhibitors will raise serum concentrations of CYP3A4 substrates
Efavirenz	Decrease serum calcium channel blockers
Flibanserin	CYP3A4 inhibitors may result in an increase in flibanserin (Weak).
Fluconazole	Serum calcium channel blockers may rise.
Fosaprepitant	High likelihood that inhibitors will raise serum concentrations of CYP3A4 substrates
Fosnetupitant	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Herbs (Hypertensive Properties)	May lessen the effects of antihypertensive medications in treating hypertension.
Herbs (Hypotensive properties)	May intensify blood pressure lowering medications' hypotensive effects.
Hypotension-Associated Agents	The hypotensive action of hypotension-associated agents may be strengthened by blood pressure lowering medications.
Ivosidenib	Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Larotrectinib	High likelihood that inhibitors will raise serum concentrations of CYP3A4 substrates
Levodopa-Containing Products	Levodopa-Containing Products' hypotensive effects may be amplified by blood pressure-lowering medications.
Lormetazepam	May intensify blood pressure lowering medications' hypotensive effects.
Lovastatin	AmLODIPine may raise the serum levels of lovastatin.
Magnesium Salts	Magnesium salts can have more hazardous or harmful effects when taken with calcium channel blockers. The hypotensive effects of calcium channel blockers can be enhanced by magnesium salts.
Melatonin	Dihydropyridine, a calcium channel blocker, may have less antihypertensive effects.
Methylphenidate	May lessen the effects of antihypertensive medications in treating hypertension.
Molsidomine	May intensify blood pressure lowering medications' hypotensive effects.
Naftopidil	May intensify blood pressure lowering medications' hypotensive effects.
Netupitant	High likelihood that inhibitors will raise serum concentrations of CYP3A4 substrates
Neuromuscular-Blocking Agents (Nondepolarizing)	The neuromuscular-blocking impact of neuromuscular-blocking agents may be enhanced by calcium channel blockers (Nondepolarizing).
Nicergoline	May intensify blood pressure lowering medications' hypotensive effects.
Nicorandil	May intensify blood pressure lowering medications' hypotensive effects.
NiMODipine	NiMODipine serum levels may rise in response to weak CYP3A4 inhibitors.
Nitrogen	Blood pressure lowering medications may intensify Nitroprusside's hypotensive effects.
Palbociclib	High likelihood that inhibitors will raise serum concentrations of CYP3A4 substrates
Pentoxifylline	May intensify blood pressure lowering medications' hypotensive effects.
Pholcodine	Pholcodine's ability to reduce blood pressure may help to increase hypotensive effects.
Phosphodiesterase 5 Inhibitors	May intensify blood pressure lowering medications' hypotensive effects.
Prostacyclin Analogues	May intensify blood pressure lowering medications' hypotensive effects.
Quinagolide	May intensify blood pressure lowering medications' hypotensive effects.
QuiNIDine	Dihydropyridine, a calcium channel blocker, may raise the serum levels of quinine. The serum concentration of calcium channel blockers (Dihydropyridine) may rise in response to quinine. Dihydropyridine, a calcium channel blocker, may reduce the serum levels of quinine.
Sarilumab	Could decrease serum levels of CYP3A4 substrates (High Risk with Inducers).
Siltuximab	Could decrease serum levels of CYP3A4 substrates (High Risk with Inducers).
Simeprevir	High likelihood that inhibitors will raise serum concentrations of CYP3A4 substrates
Tacrolimus (Systemic)	Dihydropyridine, a calcium channel blocker, may raise the serum concentrations of tacrolimus.
Tocilizumab	Could decrease serum levels of CYP3A4 substrates (High Risk with Inducers).
Yohimbine	Antihypertensive medications may not have as much of an effect.
Risk Factor D (Regard therapy modification)
Amifostine	The hypotensive effects of amifostine may be strengthened by blood pressure reducing medications. Treatment: Stop taking blood pressure medications at least 24 hours before taking amifostine. If taking blood pressure medicine cannot be stopped, amifostine should be avoided.
Antifungal Agents (Azole Derivatives, Systemic)	Itraconazole may make calcium channel blockers more toxic or harmful. Particularly itraconazole has the potential to worsen the inotropic side effects of verapamil and diltiazem. Calcium channel blocker metabolism can be decreased by antifungal agents (azole derivatives systemic). Fluconazole and isavuconazonium probably have less powerful effects than other azoles. In different monographs, these are covered. Management: Concurrent use of itraconazole and felodipine is not permitted under any circumstances. Any medicine combination involving these ones should undergo routine monitoring. Reduced dosages of calcium channel blockers might also be required. Fluconazole and isavuconazonium sulphate are exceptions.
Antihepaciviral Combination Products	Amlodipine serum levels might rise. When using an antihepaciviral combination treatment, reduce the dosage of amlodipine by at least half and keep an eye out for any heightened amlodipine side effects (such as hypotension).
CarBAMazepine	Dihydropyridine, a calcium channel blocker, may speed up metabolism. Treatment: Patients taking calcium channel blockers concurrently with carbamazepine should think about adjusting their doses (CCB). The Canadian labelling for nimodipine expressly forbids taking it alongside carbamazepine.
Strong CYP3A4 Inducers	May speed up CYP3A4 substrate metabolism (High Risk with Inducers). Management: You might think about switching out one of the interfering medications with another medication. Contraindications may apply to specific combinations. the relevant manufacturer's label.
Dabrafenib	High chance that inducers will lower serum CYP3A4 substrate levels. Management: If at all possible, look for CYP3A4 substrate substitutes. It is best to avoid concurrent therapy wherever possible. Keep a close eye on the substrate's clinical effects (especially therapeutic effects).
Enzalutamide	High chance that inducers will lower serum levels of CYP3A4 substrates. Management: Steer clear of using enzalutamide and CYP3A4 substrates simultaneously. When utilising enzalutamide or any other CYP3A4 sub-substance, you should use caution.
Fosphenytoin	Fosphenytoin serum levels can rise in response to calcium channel blockers. Management: After stopping the use of a calcium channel blocker (CCB), monitor for a decrease in the effects of phenytoin. Keep an eye out for diminished CCB therapeutic effects. The Canadian labelling for nimodipine specifically forbids the use of phenytoin.
Lomitapide	CYP3A4 inhibitors may result in a rise in lomitapide (Weak). Treatment: Patients who are currently taking lomitapide 5 mg/day can keep doing so. Patients must cut their lomitapide dosage in half if they are taking 10 mg or more per day. then you can change the dosage of lomitapide.
Lorlatinib	High chance that inducers will lower serum levels of CYP3A4 substrates. Management: Avoid taking lorlatinib at the same time as any CYP3A4 substrates. A therapeutic failure or negative clinical outcomes could result from even a modest drop in serum concentrations.
Antibiotics with Macrolide	The metabolic activity of calcium channel blockers may be reduced. Use a non-interacting macrolide for management. The Canadian labelling for felodipine expressly advises against using it in conjunction with clarithromycin. Fidaxomicin, Roxithromycin, and Spiramycin are exceptions to the rule; azithromycin (systemic).
MiFEPRIStone	High chance that inhibitors will raise serum levels of CYP3A4 substrates. Management: During and two weeks after mifepristone treatment, reduce doses of CYP3A4 substrates and keep an eye out for elevated amounts or toxicity. Avoid ergotamine and dihydroergotamine.
Mitotane	High chance that inducers will lower serum levels of CYP3A4 substrates. Treatment: Patients on mitotane may need to significantly change their CYP3A4 Substrates dosage.
Obinutuzumab	The effects of blood pressure lowering medications may become more hypotensive as a result. Treatment: Starting 12 hours before the obinutuzumab injection and continuing for 1 hour after the infusion, you may temporarily stop taking blood pressure-lowering medications.
Phenytoin	The serum level of phenytoin can rise after taking calcium channel blockers. Phenytoin may reduce the levels of calcium channel blockers in the serum. Management: Nimodipine and nifedipine shouldn't be used with phenytoin. With any concurrent use, it's crucial to monitor for phenytoin toxicities and/or diminished calcium channel blocking effects.
Pitolisant	High chance that inducers will lower serum levels of CYP3A4 substrates Avoid combining a CYP3A4 substrate with a low therapeutic index with pitolisant. Pitolisant and other CYP3A4 sub-substances shouldn't be mixed.
Rifamycin Derivatives	A reduction in serum calcium channel blockers may result from this. The main culprit here is an oral calcium channel blocker. Management: Using rifampin with certain calcium channel blockers is not advised according to the labelling in the US and Canada. Look up the relevant labelling.
Simvastatin	AmLODIPine may increase the effects of simvastatin. Amlodipine and simvastatin shouldn't be taken concurrently. Adults should not take more than 20 mg of simvastatin daily in combination.
Sincalide	Sincalide may be less effective if drugs that affect gallbladder function are taken. Management: Before Sincalide is used to stimulate the gallbladder, discontinue any drugs that affect gallbladder motility.
St John's Wort	High chance that inducers will lower serum CYP3A4 substrate levels. Management: You might think about switching out one of the interfering medications with another medication. Contraindications may apply to specific combinations. the relevant manufacturer's label.
Stiripentol	High chance that inhibitors will raise serum levels of CYP3A4 substrates. Treatment: Steer clear of using stiripentol with CYP3A4 substrates that have a limited therapeutic index. This is done to prevent negative consequences and toxicity. Any CYP3A4 substrate that is administered in conjunction with stiripentol should be strictly monitored.
Risk Factor X (Avoid Combination)
Bromperidol	The hypotensive effects of bromperidol may be strengthened by blood pressure-lowering medications. The hypotensive effects of blood pressure-lowering medications may be lessened by bromperidol.
Conivaptan	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Fusidic Acid (Systemic).	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Idelalisib	High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Pimozide	Pimozide may be increased by CYP3A4 inhibitors (Weak).

Monitoring parameters:

Heart Rate and Blood Pressure

Hypertension

Confirmed Hypertension with Known Cardiovascular Disease (CVD) or High Cardiovascular Risk:
- Target blood pressure: <130/80 mm Hg as recommended by the 2017 ACC/AHA Guideline.
Confirmed Hypertension without Increased Cardiovascular Risk:
- Target blood pressure: <130/80 mm Hg may be reasonable according to the 2017 ACC/AHA Guideline.
Diabetes and Hypertension:
- Goal blood pressure: <140/90 mm Hg according to the American Diabetes Association (ADA) guidelines (2019).
Known Atherosclerotic Cardiovascular Disease (ASCVD) or High ASCVD Risk:
- Goal blood pressure: <130/80 mm Hg if safely attainable.
ASCVD Risk <15% (Lower Risk of CVD):
- Goal blood pressure: <140/90 mm Hg.

In summary, for individuals with hypertension, the target blood pressure goals may vary based on the presence of cardiovascular disease, diabetes, and ASCVD risk factors. The overall aim is to reduce blood pressure to levels that decrease the risk of cardiovascular events and complications while considering individual patient characteristics and safety.

How to Administer Amlodipine?

Oral: Amlodipine is typically administered orally in adults. It can be taken with or without food, as its effectiveness is not affected by meals.

Oral: Amlodipine can also be given orally to children. Like in adults, it can be administered with or without food. This flexibility in administration allows for easier dosing in pediatric patients.

Mechanism of action of Amlodipine:

Amlodipine works by blocking calcium ions from entering specific areas in the vascular smooth muscle and myocardium, known as "slow channels" or voltage-sensitive areas, during depolarization.
This action leads to relaxation of the coronary vascular smooth muscle, causing dilation of the coronary arteries.
As a result, more oxygen-rich blood can flow to the heart muscle, particularly beneficial in patients with vasospastic angina.
Additionally, amlodipine directly acts on the vascular smooth muscle, causing peripheral arterial vasodilation, which reduces peripheral vascular resistance and subsequently lowers blood pressure.
Overall, amlodipine helps improve blood flow to the heart and throughout the body by relaxing blood vessels, thereby reducing strain on the heart and lowering blood pressure.

Onset of Action:

Antihypertensive Effect: Amlodipine typically starts reducing blood pressure significantly within 24 to 48 hours after the first dose. There might be a slight increase in heart rate within 10 hours of administration, reflecting some vasodilating activity.

Duration:

Antihypertensive Effect: The antihypertensive effect of amlodipine lasts for at least 24 hours after a dose. Studies have shown that this effect can extend to at least 72 hours when the medication is discontinued after 6 to 7 weeks of therapy.

Absorption:

Amlodipine is well absorbed into the bloodstream.

Distribution:

In adults, the mean volume of distribution (V) is about 21 liters per kilogram. In children over 6 years old, the weight-adjusted V is similar to adults. However, in younger children under 6 years old, the weight-adjusted V may be greater than in older children.

Protein Binding:

Approximately 93% of amlodipine binds to proteins in the blood.

Metabolism:

Amlodipine is primarily metabolized in the liver, with about 90% of it being converted into inactive metabolites.

Bioavailability:

The bioavailability of amlodipine ranges from 64% to 90%, indicating the percentage of the administered dose that reaches the bloodstream.

Half-life Elimination:

The terminal elimination half-life of amlodipine is biphasic, ranging from 30 to 50 hours. This half-life can be prolonged in individuals with hepatic dysfunction.

Time to Peak, Plasma:

It takes about 6 to 12 hours for amlodipine to reach its peak concentration in the blood plasma after administration.

Excretion:

Amlodipine is primarily excreted in the urine, with approximately 10% of the total dose being eliminated unchanged and about 60% as metabolites.

Clearance:

Clearance of amlodipine may be decreased in patients with hepatic insufficiency or moderate to severe heart failure. In children over 6 years old, weight-adjusted clearance is similar to adults. However, in younger children under 6 years old, weight-adjusted clearance may be greater than in older children.

International brands of Amlodipine:

A-B Vask
Actapin
Adipin
Aforbes
Agen
Aladin
Alopine
Alozur
Amaday
Ambesyl
Amcal
Amcard
Amdepin
Amdhapine
Amdipin
Amdixal
Amedin
Amilo
Amlate
Amlibon
Amlibon BES
Amlo-H10
Amlo-H5
Amlo-M
Amlober
Amloc
Amlocar
Amlocard
Amlocor
Amlodac
Amlodar
Amlode
Amlodigamma
Amlodin
Amlodine
Amlodno
Amloget
Amlogrix
Amlong
Amlopine
Amlopres
Amlopress
Amlor
Amlorine
Amlostar
Amlosyn
Amlotan
Amlotens
Amlotrene
Amlovasc
Amlovasc 5
Amlow
Amlozen
Amodin
Amodipin
Amopress
Ampliron
Amtas
Amvasc
Amze
An Nei
Zhen
Anoldin
Anydipine
Ao Wan Lu
Arainno
Asomex-5.0
Astudal
Avevasc
Avistar
Awar
Bezam
Cab
Calbloc
Calchek
Calvase
Cardilopin
Cardol
Cobisk
Cordarene
Covasc
CP-Lovac
Cydipin
DAILYvasc
Deten
Dipsope
Du.Q
Duactin 5
Ertensi
Evasc
Fulopin
Gensia
Gravask
Hovasc
Istin
Istolde
Konipid
Lama
Licodipin
Lodibes
Lodip
Lodipam
Lofral
Lomanor
Lotense
Lowdipine
Lowrac
Lowvasc
Lupin
Narvin
Nexus
Noloten
Nopidin
Nor-Lodipina
Nordip
Normodipine
Norvapine
Norvas
Norvasc
Norvasc ODT
Norvask
Novaspin
Odasyl
Opivask
Prelod
Presilam
Provasc
Remedopin S
Sinnorvapin
Sinop
Sistopress
Stadovas
Stamlo
Stamlo-10
Tenox
Tensiblat
Terloc
Varodipine
Vascodipine
Vascor
Vasocal
Vasotop
Vasten
Zynor
ACCEL-Amlodipine
ACT Amlodipine
AG-Amlodipine
APO-Amlodipine
Auro-Amlodipine
BIO-Amlodipine
DOM-Amlodipine
GD-Amlodipine
JAMP-Amlodipine
M-Amlodipine
Mar-Amlodipine
MINT-Amlodipine
MYLAN-Amlodipine
Norvasc
NRA-Amlodipine
PHARMA-Amlodipine
PHL-Amlodipine
PMS-Amlodipine
Priva-Amlodipine
Q-Amlodipine
RAN-Amlodipine
SANDOZ Amlodipine
Septa-Amlodipine
TEVA-Amlodipine
VAN-Amlodipine

Amlodipine Brands in Pakistan:

Amlodipine (Besylate) [Tabs 5 Mg]
Adoptin	Fynk Pharmaceuticals
Adoptine	Tread Pharmaceuticals Pvt Ltd
Amdipine	Nabiqasim Industries (Pvt) Ltd.
Amdipine	Nabiqasim Industries (Pvt) Ltd.
Amdocal	Bex Pharma (Pvt) Ltd.
Aml	Batala Pharmaceuticals.
Amlobest	Pearl Pharmaceuticals
Amlocard	Pharmatec Pakistan (Pvt) Ltd.
Amlod	Atco Laboratories Limited
Amlodip	Searle Pakistan (Pvt.) Ltd.
Amlofine	Medline Health Care
Amlomak	Makson Pharmaceuticals
Amlomed	Medifine Laboratories
Amlopal	Alson Pharmaceuticals
Amlopin	Shaigan Pharmaceuticals (Pvt) Ltd
Amlopro	Wns Field Pharmaceuticals
Amlosaf	Saaaf Pharmaceuticals
Amlotac	Hygeia Pharmaceuticals
Amlowan	Nawan Laboratories (Pvt) Ltd.
Amodip	Mass Pharma (Private) Limited
Amolin	F.M. Pharmaceuticals International
Amotel	Ideal Pharmaceutical Industries
Ampress	Barrett Hodgson Pakistan (Pvt) Ltd.
Amrx	Siza International (Pvt) Ltd.
Amvasc	Aries Pharmaceuticals (Pvt) Ltd
Amvazam	Cirin Pharmaceuticals (Pvt) Ltd.
Anam	Tagma Pharma (Pvt) Ltd.
Angipin	Standpharm Pakistan (Pvt) Ltd.
Ardepin	Ardin Pharmaceuticals
Aviant	Gray`S Pharmaceuticals
Bescard	Flow Pharmaceuticals (Pvt) Ltd.
Besipine	Csh Pharmaceuticals-North (Pvt) Ltd
Ca-B	Saydon Pharmaceutical Industries (Pvt) Ltd.
Cabok	Platinum Pharmaceuticals (Pvt.) Ltd.
Caloc	Bosch Pharmaceuticals (Pvt) Ltd.
Canta	Shaheen Pharmaceuticals
Cardiocare	Jawa Pharmaceuticals(Pvt) Ltd.
Cardiosil	Himont Pharmaceuticals (Pvt) Ltd.
Cardiovasc	Werrick Pharmaceuticals
Co-Cardiovasc	Werrick Pharmaceuticals
Coram	Brookes Pharmaceutical Laboratories (Pak.) Ltd.
Corcont	Swiss Pharmaceuticals (Pvt) Ltd.
Cordfed	Fedro Pharmaceutical
Cordium	Pharmix Laboratories (Private) Limited.
Corinor	P.D.H. Pharmaceuticals (Pvt) Ltd.
Dipivas	Fassgen Pharmaceuticals
Enalatac	Hygeia Pharmaceuticals
Endip	English Pharmaceuticals Industries
Envas	Lowitt Pharmaceuticals (Pvt) Ltd
Farlod	Un Pharma International
G-Sac	Global Pharmaceuticals
Hartvasc-Plus	Scotmann Pharmaceuticals
Hibiohit	Unipharma (Pvt) Ltd.
Hiblohit	Unipharma (Pvt) Ltd.
Hodip	Heal Pharmaceuticals Pvt Ltd
Hypercor	Novins International
Hypotin	Don Valley Pharmaceuticals (Pvt) Ltd.
Hypres	Don Valley Pharmaceuticals (Pvt) Ltd.
Leaf	Scotmann Pharmaceuticals
Lipinox	Friends Pharma (Pvt) Ltd
Lodipin	Schazoo Zaka
Lodivasc	Dosaco Laboratories
Lodopin	Merck Private Ltd.
Lopin	Ambrosia Pharmaceuticals
Megadip	Mega Pharmaceuticals (Pvt) Ltd
Mevodip	Alliance Pharmaceuticals (Pvt) Ltd.
Midopine	Welmark Pharmaceuticals
Miosil	Europak Pharma (Pvt) Ltd
Mlow	Scilife Pharma (Private) Ltd
Modopine	Askari Pharmaceuticals.
Nencure	Nenza Pharmaceuticals (Pvt) Limited
Neopres	Biogenics Pakistan (Pvt) Ltd.
Norvasc	Pfizer Laboratories Ltd.
Norvasc	Pfizer Laboratories Ltd.
Onato	Sami Pharmaceuticals (Pvt) Ltd.
Orelop	Flow Pharmaceuticals (Pvt) Ltd.
Quvasc	Novartis Pharma (Pak) Ltd
Rasdipin	Rasco Pharma
Ravapine	Rakaposhi Pharmaceutical (Pvt) Ltd.
Ravapine	Rakaposhi Pharmaceutical (Pvt) Ltd.
Rydem	Werrick Pharmaceuticals
S-Dip	Shrooq Pharmaceuticals
Salome	Lahore Chemical & Pharmaceutical Works (Pvt) Ltd
Sicknor	Everest Pharmaceuticals
Sofvasc	Wilsons Pharmaceuticals
Sofvasc	Wilsons Pharmaceuticals
Sofvasc Plus	Wilsons Pharmaceuticals
Swint	Libra Pharmaceuticals (Pvt) Ltd
Tarovasc	Everest Pharmaceuticals
Vasic	Miracle Pharmaceuticals(Pvt) Ltd
Vasodil	Pharmedic (Pvt) Ltd.
Vasodipine	Alfalah Pharma (Pvt) Ltd.
Vespin	Amson Vaccines & Pharma (Pvt) Ltd.
Wincoram	Polyfine Chempharma (Pvt) Ltd.
Zamlo	Zafa Pharmaceutical Laboratories (Pvt) Ltd.
Zodip	Zafa Pharmaceutical Laboratories (Pvt) Ltd.

Amlodipine (Besylate) [Tabs 10 Mg]
Amdipine	Nabiqasim Industries (Pvt) Ltd.
Amdipine	Nabiqasim Industries (Pvt) Ltd.
Amlobest	Pearl Pharmaceuticals
Amlocard	Pharmatec Pakistan (Pvt) Ltd.
Amlodip	Searle Pakistan (Pvt.) Ltd.
Amlofine	Medline Health Care
Amlomak	Makson Pharmaceuticals
Amlomed	Medifine Laboratories
Amlopal	Alson Pharmaceuticals
Amlopro	Wns Field Pharmaceuticals
Amlosaf	Saaaf Pharmaceuticals
Amlosyl	Lexicon Pharmaceuticals(Pvt) Ltd.
Amlotac	Hygeia Pharmaceuticals
Amodip	Mass Pharmaceuticals(Private) Limited
Amotel	Ideal Pharmaceuticals Industries
Ampress	Barrett Hodgson Pakistan (Pvt) Ltd.
Amrx	Siza International (Pvt) Ltd.
Amvasc	Aries Pharmaceuticals (Pvt) Ltd
Anam	Tagma Pharma (Pvt) Ltd.
Angipin	Standpharm Pakistan (Pvt) Ltd.
Ardepin	Ardin Pharmaceuticals
Aviant	Gray`S Pharmaceuticals
Bescard	Flow Pharmaceuticals(Pvt) Ltd.
Ca-B	Saydon Pharmaceuticals Industries (Pvt) Ltd.
Cabok	Platinum Pharmaceuticals(Pvt.) Ltd.
Caloc	Bosch Pharmaceuticals(Pvt) Ltd.
Canta	Shaheen Pharmaceuticals
Cardiocare	Jawa Pharmaceuticals (Pvt) Ltd.
Cardiosil	Himont Pharmaceuticals(Pvt) Ltd.
Cardiovasc	Werrick Pharmaceuticals
Coram	Brookes Pharmaceuticals Laboratories (Pak.) Ltd.
Corcont	Swiss Pharmaceuticals (Pvt) Ltd.
Corinor	P.D.H. Pharmaceuticals(Pvt) Ltd.
Dipcare	Silver Oak Corporation.
Dipivas	Fassgen Pharmaceuticals
Enalatac	Hygeia Pharmaceuticals
Endip	English Pharmaceuticals Industries
Envas	Lowitt Pharmaceuticals (Pvt) Ltd
Farlod	Un Pharma International
Hartvasc-Plus	Scotmann Pharmaceuticals
Hodip	Heal Pharmaceuticalspvt Ltd
Hypercor	Novins International
Hypocard	Caylex Pharmaceuticals (Pvt) Ltd.
Hypotin	Don Valley Pharmaceuticals(Pvt) Ltd.
Hypres	Don Valley Pharmaceuticals(Pvt) Ltd.
Lodipin	Schazoo Zaka
Lodopin	Merck Private Ltd.
Lopin	Ambrosia Pharmaceuticals
Megadip	Mega Pharmaceuticals(Pvt) Ltd
Midopine	Welmark Pharmaceuticals
Miosil	Europak Pharma (Pvt) Ltd
Mlow	Scilife Pharma (Private) Ltd
Modopine	Askari Pharmaceuticals.
Nencure	Nenza Pharmaceuticals (Pvt) Limited
Neopres	Biogenics Pakistan (Pvt) Ltd.
Norvasc	Pfizer Laboratories Ltd.
Norvasc	Pfizer Laboratories Ltd.
Onato	Sami Pharmaceuticals (Pvt) Ltd.
Orelop	Flow Pharmaceuticals(Pvt) Ltd.
Provasc	Genome Pharmaceuticals (Pvt) Ltd
Quvasc	Novartis Pharma (Pak) Ltd
Ravapine	Rakaposhi Pharmaceuticals(Pvt) Ltd.
Ravapine	Rakaposhi Pharmaceuticals(Pvt) Ltd.
Rydem	Werrick Pharmaceuticals
S-Dip	Shrooq Pharmaceuticals
Sicknor	Everest Pharmaceuticals
Sofvasc	Wilsons Pharmaceuticals
Swint	Libra Pharmaceuticals(Pvt) Ltd
Tarovasc	Everest Pharmaceuticals
Vasic	Miracle Pharmaceuticals (Pvt) Ltd
Vatlo	Alkemy Pharmaceuticals Laboratories (Private) Ltd.
Wincoram	Polyfine Chempharma (Pvt) Ltd.

Amlodipine (Besylate) [Tabs 2.5 Mg]
Amlocard	Pharmatec Pakistan (Pvt) Ltd.
Amodip	Mass Pharma (Private) Limited
Cardiovasc	Werrick Pharmaceuticals
Hartvasc-Plus	Scotmann Pharmaceuticals
Lodopin	Merck Private Ltd.
Quvasc	Novartis Pharma (Pak) Ltd
Rydem	Werrick Pharmaceuticals
Sofvasc	Wilsons Pharmaceuticals

Amlodipine (Besylate) - Indications, dose, side effects ...

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