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Levamlodipine

levamlodipine besylate, levamlodipine vs amlodipine
Levamlodipine INN, 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 agent1 Levamlodipine is currently marketed in Russia under the brand name EsCordi Cor Actavis Pharma and in India under the trade names Eslo Zuventus Healthcare Ltd, Asomex Emcure Pharmaceutical Ltd, and Espin Intas Pharmaceuticals Ltd23

Contents

  • 1 Mechanism of action
  • 2 Pharmacokinetics and metabolism
  • 3 Clinical experience
  • 4 Safety and tolerability
  • 5 References

Mechanism of actionedit

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 channels45 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 channels6

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 flow1

Pharmacokinetics and metabolismedit

Administration of levamlodipine 25 mg as a single dose gives maximum plasma concentration Cmax of 83 to 93 ng/mL in 2 to 3 hrs Tmax It is extensively about 90% converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine Levamlodipine shows approximately 93% plasma protein binding in hypertensive patients The mean AUC0–t value t = 48 hrs of levamlodipine tablets 25 mg is 7001950000000000000♠95±14 ng·hr/mL The plasma elimination half-life of levamlodipine has been found to be 7001310000000000000♠31±13 hrs7

Clinical experienceedit

Various clinical studies have shown that levamlodipine has more selectivity and better efficacy than R-amlodipine In pooled data, from three comparative studies conducted in 200 patients with mild to moderate hypertension, 25 mg of levamlodipine was found to be equivalent in its blood pressure lowing efficacy to 5 mg of amlodipine The average reduction in systolic BP was 19±3 vs 19±4, 20±2 vs 19±3 and 20±2 vs 19±3 mm of Hg recorded in standing, supine and sitting position respectively for levamlodipine compared to racemic amlodipine The studies also reported a significant reduction in total cholesterol and triglyceride levels with levamlodipine, which was not seen with amlodipine8910

Efficacy and safety of levamlodipine 25 mg, once daily has been evaluated in the patients with isolated systolic hypertension ISH Levamlodipine effectively reduced the systolic BP mean reduction 22±14 mm of Hg in all grades of ISH After 28 days of the treatment, overall responder rate was 73% It significantly reduced the systolic and diastolic BP within 4 weeks with a responder rate of 965%11

Elderly hypertensives with diabetes mellitus exhibits higher response to levamlodipine therapy than non-diabetic patients Levamlodipine is an effective switch-over option for the elderly patients who experience oedema and other adverse events with racemic amlodipine12

Safety and tolerabilityedit

The use of racemic amlodipine is commonly associated with adverse events like peripheral edema and other side effects like headache, dizziness, flushing and abdominal pain13 Controlled clinical trials showed that levamlodipine is rarely associated with these side effects14 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 levamlodipine1 However, caution should be taken while administering levamlodipine to such patients

In a postmarketing surveillance study, levamlodipine 25/5 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 patients 9872% at the end of 4 weeks Only in 4 patients was edema 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 mild in nature and no serious adverse events were reported14

Referencesedit

  1. ^ a b c Thacker HP 2007 "S-amlodipine – the 2007 clinical review" J Indian Med Assoc 105 4: 180–86 PMID 17822186 
  2. ^ "Asomex by Emcure" PDF Medical Update Newsletter 20 1: 1–2 January 2010 
  3. ^ "Zuventus Brands for S- Amlodipine" DrugsUpdatecom 
  4. ^ Burges RA, Gardiner DG, Gwilt M, Higgins AJ, Blackburn KJ, Campbell SF, Cross PE, Stubbs JK January 1987 "Calcium channel blocking properties of amlodipine in vascular smooth muscle and cardiac muscle in vitro: evidence for voltage modulation of vascular dihydropyridine receptors" J Cardiovasc Pharmacol 9 1: 110–9 PMID 2434785 doi:101097/00005344-198701000-00018 
  5. ^ Goldmann S, Stoltefuss J December 1991 "1,4-Dihydropyridines: Effects of Chirality and Conformation on the Calcium Antagonist and Calcium Agonist Activities" Angewandte Chemie International Edition in English 30 12: 1559–1578 doi:101002/anie199115591 
  6. ^ Goldmann S, Stoltefuss J, Born L September 1992 "Determination of the absolute configuration of the active amlodipine enantiomer as −-S: a correction" Journal of Medicinal Chemistry 35 18: 3341–4 PMID 1388206 doi:101021/jm00096a005 
  7. ^ Park JY, Kim KA, Park PW, Lee OJ, Ryu JH, Lee GH, Ha MC, Kim JS, Kang SW, Lee KR November 2006 "Pharmacokinetic and pharmacodynamic characteristics of a new S-amlodipine formulation in healthy Korean male subjects: a randomized, open-label, two-period, comparative, crossover study" Clin Ther 28 11: 1837–47 PMID 17213004 doi:101016/jclinthera200611008 
  8. ^ Hiremath MS, Dighe GD August 2002 "A Randomized, Double-blind, Double dummy, Multicentric, Parallel Group, Comparative Clinical Trial of S-Amlodipine 25 mg vs Amlodipine 5 mg in the Treatment of mild to moderate Hypertension" JAMA-India 1 8: 86–92 
  9. ^ "Clinical Trial of S-Amlodipine 25 mg versus Amlodipine 5 mg in the Treatment of Hypertension" Indian Journal of Clinical Practice 13 11: 49–54 April 2003 
  10. ^ Pathak L, Hiremath, Kerkar PG, Manade VG March 2004 "Multicentric, clinical trial of S-Amlodipine 25 mg versus Amlodipine 5 mg in the treatment of mild to moderate hypertension--a randomized, double-blind clinical trial" J Assoc Physicians India 52: 197–202 PMID 15636308 
  11. ^ SESA Study group June 2005 "MICRO-SESA-I – Safety and Efficacy of S−-Amlodipine in the treatment of isolated systolic hypertension" Indian Medical Gazette 139 6: 243–250 
  12. ^ SESA Study group August 2005 "MICRO-SESA-II – Safety and Efficacy of S- Amlodipine in the Treatment of Hypertension in Elderly Patients" Indian Medical Gazette 139 8: 353–358 
  13. ^ Stöppler MC "Side Effects of Norvasc Amlodipine Besylate Drug Center" RxList Inc 
  14. ^ a b SESA Study group August 2003 "Safety and Efficacy of S-Amlodipine – SESA study" JAMA-India 2 8: 87–92 

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