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Amlodipine Use, Side Effects, Mechanism Action, Dosage and Many Information


What is Amlodipine?

Amlodipine chemical name is 3-Ethyl-5-methyl (±)-2-[(2-aminoethoxy)methyl]-4-(2- chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate, monobenzenesulphonate. This avalible in the market as Amlodipine basilate, which is salt form of the drug.

What Amlodipine use for?

Amlodipine tablet use for the treatment of high blood pressure (hypertension). It is also used for the chest pain due to angina. And also use for other diseases like prinzmental’s, variant angina.
Amlodipine tablets use for the treatment of Blood pressure
Amlodipine tablets

Amlodipine is used in the management of hypertension and coronary arteries disease in people with either stable angina (when people are suddenly get shock or more physical work) vasospastic angina (Which is coronary artery vasospasm) and it is use in case of heart attack but not heart failue. It can be used as single dose or combination of other medicine to manage hypertension. 
It is also use for coronary disease. This medicine provide better protection against stroke than other classes of blood pressure-lowering drugs.
This medicine is use as first choice of medicine to treatment of Raynaud’s phenomenon (spasm of arteries so reduce of blood pressure).
This drug helps to relaxing blood vessel of high blood pressure patients so blood flow is normal.
This drug is also use for kidney problem. 

Amlodipine Side Effect

Like other medicine amlodipine have some side effects but not every patients are seen these side effects.
  • Sudden wheeziness
  • Chest pain
  • Shortness of breath or difficulty in breathing
  • Swelling of eyelids
  • Face and lips swelling
  • Swelling of the tongue and throat
  • Skin rash
  • Hives
  • Redness of skin over hole body
  • Severe itching
  • Blistering
  • Peeling
  • Inflammation of mucous membrane (Stevens Johnsons syndrome)
  • Heart attack or abnormal heart beat
  • Inflammation in pancreas
  • Back pain

Very common side effects are Seen give below but if the symptoms are not gone in a week consult with doctor or pharmacist.
Common Side effects are
  • Edema
  • Headache
  • Dizziness
  • Slpeepiness
  • Plapitations and flushing
  • Abdominal pain, feeling sick
  • Alter bowel habits
  • Diarrhea
  • Constipation
  • Indigestion
  • Tiredness and felling weakness
  • Visual disturbances
  • Muscle cramp
  • Ankle swelling

Some uncommon side effects are also reported if patients are seen these below side effect immediately inform the doctor or pharmacist.
Mood changes, Anxiety, depression
Trembling, Mouth test change, fainting
Numbness or tingling sensation in your limbs or loss of pain sensation
Ears false ringing
Sneezing/running nose caused by inflammation of lining of inner nose
Cough
Dry mouth
Vomiting
Hairloss and increase sweating
Urination procress
Joint pain or back pain
May be weight increase or descrease
Blood sugar level increase leads to diabetes
Decrease the number of Red blood cells and blood platelets
Swelling from gums
Gastric
Liver may not function properly or yellowing of skin and eye
Increase muscle tension
Sensitivity to light

Mechanism of action

Amlodipine is calcium channel blockers (CCB)  and it belogs to group of dihydropyridine which is lipophilic drug. This category is very effective to calcium channel blocker. This drug is more sensitive towards voltage sensitive L-type channel. It like to bind with alpha subunit and helps to restrict all the calcium ions into vascular smooth muscle.
There are two main actions of this medicine is
(i)               Smooth muscle relaxation
(ii)            Negative chronotropic, inotropic and dromotropic action on the heart.

How Amlodipine helps depolarize smooth muscle?
In smooth muscle primarily depolarize by ca2+ which is comes from voltage sensitive channel. These ca2+ ions are trigger release of more ca2+ from the intracellular stores. In that case amlodipine helps to reduce the available of intracellular ca2+. Which is very effective for artery and less active against veins.
How Amlodipine works in Heart?
Mainly in the heart arterial fiber and ventricular fiber are working. When more ca2+ aions are secrets from sarcoplasmic reticulum at that time contraction action are shows binds with cells like troponin. In that case amlodipine helps to normalized the contraction action in heart.

Pharmacokinetic of amlodipine

This drug is very popular according pharmacokinetic data. Oral absorption of this medicine is very slow but total amount of drug are absorbed completely. Oral dose bioavailability is 60-65 % and plasma concentration rise gradually upto 8 hours. This medicine is metabolized in the liver and very slowly eliminated from the body. Half life of this medicine is 40-50 hours. Volume of distribution is 21 L/kg and Protein binding capacity is 98%. This drug is suitable for the single dose in a time.

Amlodipine Dosage

This medicine is available in the market 2 strength 5 mg and 10 mg. Drug can be take before or after eating food. Take this medicine in constant time daily with water not the fruit juice or alchol. 
The recommended initial dose is 5 mg tablet once in a day, dose can be increase gradually to 10 mg per day.
For the children age 6-17 year age group recommended dose is 2.5 mg per day. The maximum dose is 5 mg per day for this age group patient. But this 2.5 mg tablets are not available in the market make sure break the tablets into two equal halves.
Do not take more amlodipine tablets in single time which is lower the pressure. Do not worry if you miss the dose take next dose timely. Do not take extra dose to make up previous missing dose.

Warning and precaution   

Doctor intention is cure the disease they try to know about your self but due to busy schedule some time miss to ask your health history. So your responsibility is tell the doctor if you suffer any disease like
Recent heart attack
Heart failure
Sever increase in blood pressure
Liver disease
If you take this medicine before and need to increase the dose of amlodipine.
Don’t take amlodipine if you allergy to this drug or any other ingredient use for preparing this formulation.
Don’t take this medicine if you have allergy to any calcium channel blocker.
If you suffer sever low blood pressure don’t take this medicine.
If your aortic heart valve is narrow or cardiogenic shock then told your doctor before prescribing this medicine.
This medicine is not tested below 6 year age group patient so don’t give the medicine to children.

Interaction of Amlodipine

Amlodipine may interact with other drugs to reduce the effect it shelf or affect other medicine like
Antifungal drug like ketoconazole, itraconazole.
Antiretroviral drug like ritonavir, indinavir, nelfinavir.
This drug may interact with antibiotics like rifampicin, erythromycin, clarithromycin etc.
  • Hypericum perforatum (st.John’s Wort) which is a flowering plant in the family Hypericaceae.
  • Heart medicine like verapamil, diltiazem.
  • Dantrolene
  • Tacrolimus
  • Simvastatin use cholesterol lowering medicine
  • Cyclosporine immunosuppressant

Amlodipine food interaction

This medicine is alter the action if patients are taking grape fruits or grape fruit juice, which is increase the volume of the blood so blood pressure may increase. Along with don’t take such a food which is increase the blood volume.
Those patients are taking this medicine they must reduce eating of meat and fish and egg. Reduce the quantity of consumption of dried fruits leafy vegetable like kale and spinach.

Amlodipine for pregnancy

This medicine is not tested any pregnant women so there are no any information. If you are pregnant or plan to pregnant then tell your doctor before taking amlodipine tablet.
Amlodipine is easily pass the breast milk so those mother giving milk to her baby tell the doctor before continue this medicine.

What are the alternative of amlodipine?

There are many other calcium channels are available in the market which is working same as amlodipine.
Nifedipine, felodipine, nitrendipine, Nimodipine, Lacidipine, Lercanidipine, Benidipine.
Reference: Kd tripathy pharmacology book, NCBI and Wikipedia.






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