Levamlodipine , also known as levoamlodipine or S-amlodipine is a pharmacologically active enantiomer of amlodipine. Amlodipine belongs to the dihydropyridine group of calcium channel blocker used as an antihypertensive and antianginal agent. Levamlodipine is currently marketed in India under the trade names Eslo (Zuventus Healthcare Ltd.), Asomex (Emcure Pharmaceutical Ltd), and Espin (Intas Pharmaceuticals Ltd.
(S)-3-ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
Hypertension - Adult: 2.5 mg once daily.
Hepatic impairment: Dosage reduction may be required.
Should be taken on an empty stomach. Take on an empty stomach.
MECHANISM OF ACTION
Amlodipine blocks the transmembrane influx of calcium into the vascular and cardiac smooth muscles resulting in vasodilation and hence a fall in blood pressure. Levamlodipine is an allosteric modulator and acts on the L-type of calcium channels.Receptor binding studies have shown that out of the two forms only the (S)-enantiomer of amlodipine binds to and blocks L-type calcium channels whereas the (R)-enantiomer has no activity on these channels.
The precise mechanisms by which levamlodipine relieves angina have not been fully explored, but are thought to include the following:
Decreases peripheral resistance by arteriolar vasodilatation leading to the reduction in oxygen requirement and energy consumption of cardiac smooth muscles.
Decreases coronary vascular resistance and can lead to an increase in coronary blood flow.
Safety and tolerability
The use of racemic amlodipine is commonly associated with adverse events like peripheral edema and other side effects like headache, dizziness, flushing and abdominal pain. Controlled clinical trials showed that levamlodipine is rarely associated with these side effects. No controlled clinical study of levamlodipine has been performed in patients with hepatic impairment and renal impairment. Clinical studies in patients with normal liver function have shown that there is no elevation in the hepatic enzymes with the use of levamlodipine.However, caution should be taken while administering levamlodipine to such patients.
In a post-marketing surveillance study, levamlodipine (2.5/5 mg) was found to be well tolerated (n = 1859) in patients with hypertension. Out of 314 patients, who reported peripheral edema with conventional amlodipine were switched over to levamlodipine and edema was resolved in 310 patinets at the end of 4 weeks. Only in 4 patients, edema was sustained. Only 30 patients (out of 1859) reported side effects. These side effects included vertigo, tachycardia, cough, headache, fever, mild difficulty in breathing and edema. Adverse events were of mild in nature and no serious adverse events were reported.
Amlovas-SN (Levamlodipine and Nebivolol) - Macleods, India
Atenova-SA (Levamlodipine and Atenolol) - Lupin, India
Esam - Torrent, India
Esam-AT (Levamlodipine and Atenolol) - Torrent, India
Esam-LT (Levamlodipine and Losartan) - Torrent, India
Esam-R (Levamlodipine and Ramipril) - Torrent, India
Esamlovin - East West, India
Eslo - Zuventus, India
Eslo TAN (Levamlodipine and Losartan) - Zuventus, India
Eslo-AT (Levamlodipine and Atenolol) - Zuventus, India
Listril-SM (Levamlodipine and Lisinopril) - Torrent, India
Modlip-AM (Levamlodipine and Atorvastatin) - Torrent, India
Nebicard-SM (Levamlodipine and Nebivolol) - Torrent, India
Nebipril-SA (Levamlodipine and Nebivolol) - Alkem, India
Nebistar-SA (Levamlodipine and Nebivolol) - Lupin, India
Nubeta-SM (Levamlodipine and Nebivolol) - Abbott, India
Nusar-AM - Emcure, India
Q-Spin - Q-Check, India
Ramipro-A - Emcure, India
S-Amcard - Systopic, India -
S-Amlip - Cipla, India
S-Amlong - Micro Carsyon, India
S-Amlovas - Macleods, India
Shi Hui Da - Shihuida Group, China
S-Numlo - Emcure, India
Xinta - Simcere, China