Levamlodipine also was known as S-amlodipine, is a pharmacologically active enantiomer of amlodipine, an antihypertensive and anti-anginal medication. Levamlodipine belongs to the dihydropyridine group of calcium channel blockers. This medication is currently marketed in Russia and India. The names S-amlodipine and levamlodipine may be used interchangeably as both substances are the same, however, with differing nomenclature. As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity
Levamlodipine (INN), also known as levoamlodipine or S-amlodipine is a pharmacologically active enantiomer of amlodipine. It is a pharmacologically active enantiomer of amlodipine, an antihypertensive and anti-anginal medication. Levamlodipine belongs to the dihydropyridine group of calcium channel blockers. Amlodipine belongs to the dihydropyridine group of calcium channel blocker used as an antihypertensive and antianginal agent.
Mechanism of Action Levamlodipine
Levamlodipine blocks the transmembrane influx of calcium into the vascular and cardiac smooth muscles resulting in vasodilation and a subsequent decrease in blood pressure. This drug is an allosteric modulator and acts on the L-type calcium channels. It exerts the same mechanism of action, differing only in its form as an enantiomer.
Levamlodipine blocks the transmembrane influx of calcium into the vascular and cardiac smooth muscles resulting in vasodilation and a subsequent decrease in blood pressure. This drug is an allosteric modulator and acts on the _L-type calcium channels_. It exerts the same mechanism of action, differing only in its form as an enantiomer [L1485]. The exact mechanisms by which levamlodipine relieves angina have not been fully understood, but the mechanism is thought to be twofold. Firstly, the modulation of calcium influx caused by levamlodipine leads to decreased peripheral resistance by arteriolar vasodilatation and subsequent reduction in oxygen requirement for cardiac muscle. Secondly, a decrease in coronary vascular resistance which can lead to an increase in coronary blood flow. Negative inotropic effects can be demonstrated in vitro but such effects have not been observed in live animals at therapeutic doses [L1485]. Receptor binding studies of amlodipine have shown that out of the two enantiomer forms, only the (S) enantiomer of amlodipine (levamlodipine) binds to and blocks L-type calcium channels. The (R) enantiomer has no activity on these channels
Receptor binding studies of amlodipine have shown that out of the two enantiomer forms, only the (S) enantiomer of amlodipine (levamlodipine) binds to and blocks L-type calcium channels. The (R) enantiomer has no activity on these channels .
Indications of Levamlodipine
- High blood pressure (Hypertension)
- Angina pectoris prophylaxis
- Raynaud’s Syndrome
- Heart failure
- Angina pectoris prophylaxis
Contra-Indications of Levamlodipine
- Acute syndrome of the heart
- Severe narrowing of the aortic heart valve
- Severe heart failure
- Abnormally low blood pressure
- Kidney disease with a reduction in kidney function
- Fluid Retention in the Legs, arms or hands
- Blood Circulation Failure due to Serious Heart Condition
- Chronic idiopathic constipation
- Stomach or intestine blockage
- Narrowing of the intestines
- Decreased motility function of stomach or itestines
Dodage of Levamlodipine
Strengths: 1.25mg,2.5mg ,5mg
Hypertension
- The recommended starting dose is 5 mg once daily, alone or in combination with other agents.
- It may be increased up to 40 mg once daily, if needed. Heart failure: The recommended starting dose is 1.25 mg once daily. May double dose 1-2 weekly up to a max of 10 mg once daily.
Side Effects of Levamlodipine
The most common
- a severe headache, rapid heartbeat, stiffness in your neck,
- chest pain, fast or slow heart rate;
- swelling, rapid weight gain;
- Xerostomia (dry mouth)
- Headache
- Fatigue
- Skin reactions
- Hypotension
- Anxiety
- Constipation
- Nausea/vomiting
- Weight gain/loss
- Erectile dysfunction
More common
- Abdominal or stomach pain, discomfort, or tenderness
- chills or fever
- difficulty with moving
- a headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in the chest
- discomfort in arms, shoulders, neck or upper back
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- decreased amount of urine
Rare
- Anxiety
- change in vision
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- a headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- nervousness
Drug Interactions of Levamlodipine
Levamlodipine may interact with the following drugs, suppliments, & may change the efficacy of the drug
- alpha blockers (e.g., alfuzosin, doxazosin, tamsulosin)
- alpha agonists (e.g., clonidine, methyldopa)
- angiotensin II receptor blockers (ARBs; e.g., candesartan, losartan)
- antidiabetes medications (e.g., insulin, metformin, glyburide)
- atypical anti-psychotics (e.g., clozapine, olanzapine, quetiapine, risperidone)
- azathioprine
- barbiturates (e.g., butalbital, pentobarbital phenobarbital)
- beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- canagliflozin
- ciprofloxacin
- calcium supplements (e.g., calcium carbonate, calcium citrate)
- carbamazepine
- clopidogrel
- cyclosporine
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
- duloxetine
- “gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
- guanfacine
- heparin
- levodopa
- medications that increase potassium levels (e.g., potassium supplements, spironolactone, amiloride, and salt substitutes containing potassium)
- metformin
- nonsteroidal anti-inflammatory drugs (NSAIDs; e.g., ibuprofen, indomethacin, naproxen)
- other angiotensin-converting-enzyme inhibitors (ACEIs; e.g., captopril, ramipril)
- pentoxifylline
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- methylphenidate
- monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline,selegiline, tranylcypromine)
- phosphodiesterase-5 inhibitors (e.g., sildenafil, tadalafil, vardenafil)
- pregabalin
- sodium phosphates
- tizanidine
- trimethoprim
- valproic acid
- warfarin
Pregnancy Category
FDA Pregnancy Category D
Pregnancy
This medication should not be taken by women who are or may become pregnant, as levamlodipine may cause harm to the developing baby if it is taken by the mother during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.
Lactation
This medication should not be taken by women who are breast-feeding.T he safety and effectiveness of using this medication have not been established for children.
