S-Ambes

S-Ambes

levamlodipine

Manufacturer:

GPO

Distributor:

GPO
Full Prescribing Info
Contents
Levamlodipine besylate (S-amlodipine).
Description
Each tablet contains: Levamlodipine besylate equivalent to Levamlodipine 2.5 mg.
Each tablet contains: Levamlodipine besylate equivalent to Levamlodipine 5 mg.
Action
Pharmacology: Pharmacodynamics: S(-)amlodipine, the chirally pure form of amlodipine is a calcium channel antagonist belonging to the dihydropyridine class. The S(-)isomer of amlodipine is found to possess greater pharmacological effects than R(+)amlodipine. S(-)amlodipine is 1000 times more potent than the R(+)isomer in binding to the dihydropyridine receptor. In humans, the dominant effects of amlodipine are consequent to vasodilation. S(-)amlodipine lowers peripheral vascular resistance without causing a reflex tachycardia. It is effective as a once daily dosage in the control of hypertension.
SESA (Safety and efficacy of S(-)amlodipine) study was designed to evaluate the efficacy and tolerability of effects of S(-)amlodipine. This study involved 1859 patients with hypertension from 359 different centers across India. This study states that S(-)amlodipine has an excellent antihypertensive activity and is highly beneficial in all grades of hypertension with concomitant cardiovascular diseases like angina pectoris. The SESA study also enrolled 552 patients who were earlier treated with conventional amlodipine. Out of these, 314 patients presented with peripheral edema at the time of enrollment. When these patients were switched over to S(-)amlodipine, in 310 (98.72%) patients, edema was found to be completely resolved. These patients remained without edema thereafter. The findings of this study therefore state that S(-)amlodipine 2.5/5 mg was found to be effective and well tolerated in the treatment of hypertension and is an ideal switch over therapy for patients having peripheral edema with conventional amlodipine.
A randomized, comparative, single blinded, single centered, prospective and parallel group study was conducted to compare the efficacy and tolerability of racemic amlodipine 5 mg O.D to S(-)amlodipine O.D at the half its racemic dose (2.5 mg) in 108 patients with mild to moderate hypertension. The study observed that the mean SBP and DBP were significantly reduced from baseline in both the study groups at 2, 6 and 12 weeks (p<0.0001) proving the efficacy of both the study drugs in reduction of blood pressure to target level. This study also proves that S(-)amlodipine 2.5 mg is equally efficacious in reducing B.P compared to racemic amlodipine 5 mg as evidenced by other studies. Regarding the appearance of ankle edema which is the common adverse effect with calcium channel antagonist, the higher incidence of ankle edema with racemic amlodipine compared to S(-)amlodipine was found significantly.
An open non-comparative Post Marketing Surveillance (PMS) study to assess the efficacy and tolerability of S(-)amlodipine 2.5 / 5 mg in the treatment of hypertension was carried out in 1042 patients with hypertension from 121 centers across India. All patients were given either 2.5/5 mg of S(-)amlodipine (Asomex) depending upon the baseline BP values. Patients with history of MI, cerebrovascular accident, asthma, anemia, edema with earlier treatment and obesity were also included in the study. Results were analyzed by student's t-test. Reduction in the average SBP and DBP in S(-)amlodipine 2.5 and 5 mg group after 4 weeks of treatment was found to be statistically significant. The average SBP and DBP reduced from 161/99 mm Hg to 132/84 mm Hg in the 2.5 mg group (n=848); and from 180/107mm Hg to 138/86 mm Hg in the 5 mg group (n=194) after 4 weeks. Of the 247 patients, 243 (98.38%) reported resolution of edema after switching over from conventional amlodipine to Asomex. Only 21 patients reported mild side effects, such as vertigo, tachycardia, cough, headache, fever, difficulty in breathing and edema (1.15%). S(-)amlodipine 2.5 and 5 mg are effective and well tolerated in the treatment of hypertension and is an ideal switch over therapy for patients having peripheral edema with conventional amlodipine.
Pharmacokinetics: Administration of S(-)amlodipine 2.5 mg as a single dose in the fasting state produced maximum plasma concentration (Cmax) of 8.30 ± 1.071 ng/ml in 2.73 ± 0.88 hrs. (Tmax). Amlodipine 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. Ex vivo studies have shown that approximately 93% of the circulating drug is bound to plasma proteins in hypertensive patients. The mean AUC0-t value (t= 48 hrs.) of tablet S(-)amlodipine (2.5 mg) is 95.33 ± 14.45 ng.hr/ml. The AUC0-∞ value is recorded to be 140.91 ± 28.06 ng.hr/ml. The plasma elimination half-life of S(-)amlodipine has been found to be in the range of 14.62- 68.88 hrs.
Indications/Uses
Treatment of hypertension.
Treatment of angina pectoris.
Dosage/Direction for Use
Recommended Dose: The normal recommended dose of S(-)amlodipine is 2.5 mg once daily in the treatment of hypertension and angina pectoris. If required, the dose may be increased up to 5 mg once daily.
Mode of Administration: Tablets for oral administration.
Overdosage
There are no reported cases of overdosage with the use of S(-)amlodipine. Overdosage with racemic amlodipine has been reported to cause excessive peripheral vasodilation with marked hypotension and possibly a reflex tachycardia. Hence, caution should be taken in case of an overdosage with S(-)amlodipine. If massive overdose occurs, active cardiac and respiratory monitoring should be instituted. Frequent blood pressure measurements should be performed. If hypotension occurs, cardiovascular support including elevation of the extremities and the judicious administration of fluids should be initiated. If hypotension remains unresponsive to these conservative measures, administration of vasopressors (such as phenylephrine) should be considered with attention to the circulating drug. If massive overdose occurs, gastric lavage should be employed. As this product is highly plasma protein bound, hemodialysis is not likely to be of benefit.
Contraindications
Hypersensitivity to any of the components of the formulation.
Special Precautions
General: Since the vasodilation induced by S(-)amlodipine besylate is gradual in onset, acute hypotension has not been reported after oral administration of S(-)amlodipine.
Patients with hepatic impairment: No controlled clinical study of S(-)amlodipine has been performed in patients with hepatic impairment. Clinical studies in patients with normal liver function have shown that there is no elevation in the hepatic enzymes with the use of S(-)amlodipine. However, caution should be taken while administering S(-)amlodipine to patients with hepatic impairment.
Patients with renal impairment: No controlled clinical study of S(-)amlodipine has been performed in patients with renal impairment. Hence caution should be taken while administering S(-)amlodipine to patients with renal impairment.
Use In Pregnancy & Lactation
Pregnancy: There is no data available on the use of S(-)amlodipine in pregnant women, hence the drug should be administered only when the potential benefits outweighs the risk to the patient and fetus.
Nursing mothers: There is no data available on the use of S(-)amlodipine in nursing mothers, hence the drug should be administered only when the potential benefits outweighs the risk to the patient and breastfed infant.
Adverse Reactions
Adverse events (AEs) were reported in 13 studies of S(-)amlodipine. The number of patients who experienced AEs with S(-)amlodipine were 40 in 907 (4.41%). S(-)amlodipine was associated with a significantly smaller change in heart rate than with racemic amlodipine (WMD,-0.99; 95% CI, -1.70 to -0.28).
Drug Interactions
S(-)amlodipine did not show any incidence of drug interaction when used along with telmisartan, aspirin, nitrates, beta-blockers, statins, ACE inhibitors, H2 blockers, and proton pump inhibitors.
Storage
Do not store above 30°C.
Store in original container.
ATC Classification
C08CA - Dihydropyridine derivatives ; Used in the treatment of cardiovascular diseases.
Presentation/Packing
Tab 2.5 mg (pale yellow, flat, round, one side debossed with "2.5" and the other side bisected) x 10 x 10's. 5 mg (dark yellow, flat, round, one side debossed with "5" and the other side bisected) x 10 x 10's.
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