Drug Interaction:
Reports not available
Indication:
Hypertension
Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
FDC of Nebivolol 5mg + 14-09-2004
S-Amlodipine 2.5mg tablet
Anti-Hypertensive
Adverse Reaction:
S-amlodipine- Headache, fatigue, insomnia, nausea, abdominal pain, flushing, dizziness, pruritus, skin rash, dyspnea, weakness, muscular spasm and dyspepsia
Nebivolol- Long term tloerability of nebivolol monotherapy found that nebivolol wasa well tolerated with a low incidence of drug-related adverse events, such as tiredness, cold extremities, impotence, and shortness of breath
Contra-Indications:
Patients allergic to dihydropyridine calcium antagonist,lactation, hypersensitivity to the active substance or to any of the exceipients, liver insufficiency or low function impairment and pregnancy
Dosages/ Overdosage Etc:
Indication-
Hypertension
Dosage-
Adult- 1 cap s-amlopine 2.5mg + nebivolol 5mg - once daily
Pharmacology/ Pharmacokinetics:
Pharmacology
S-amlodipine-
S-amlodipine is is an enantiomer of amlodipine which is long-acting calcium channel blocker, which blocks calcium ions outside the cardiac muscle cells and vascular smooth cells via the calcium channel cytomembrane. It directly diastole vascular smooth muscle resisting hypertension.
The mechanism of remiting angina pectoris is not yet detremined completely. It can abate myocartdial ischemia through dialating the peripheral small artery, decreasing peripheral resistence causing the reduction of energy consumption and oxygen requirement of cardiac muscle and dilating the coronary artery and coronary small artery at normal and ischemic areas, increasing the oxygen supply of the cardiac muscle of the coronary spasm patients
Nebivolol-
Nevivolol is a lipophilic beta1 blocker administered clinically as a racemic mixture of equal propositions of its d- and l-enantiomers. The drug is devoid of intrinsic sympathomimetic or membrane stabilizing activity but appears to have a nitric oxide-medicated vasodilatory effect.
Pharmacokinetics
S- amlodipine-
Following oral administration of S-amlodipine besylate tablet, the blood concentration reaches its peak value within 6-12 hrs with 64-84% of absolute biological utilisation coefficient. S-amlodipine is metabolized via the liver and excreted through urine, with 10% as unchanged 60% of metabolite
Nebivolol-
Nevibilol is rapidly absorbed after oral administration of standard 5mg dose and reaches peak plasma levels between 30 mins to 2hrs after intake.Time for Cmax after oral administration of nebivolol is reported to be about 0.5 to 2 hrs and is not significantly affected by the presence of food Generally steady-state plasma concentrations are acheived within 1 day for nebivolol and within a few days for theactive metabolites
Interaction with Food:
Not significantly affected by the presence of food
Pregnancy and lactation:
Contraindicated during pregnancy and lactation