|Composition||Benidipine Hydrochloride 4 mg + Telmisartan 40 mg tablets|
|Mechanism of Action||
Benidipine: The vasorelaxant effect of benidipine is due to its affinity towards dihydropyridine binding sites in calcium channels. Binding of benidipine with calcium channels inhibits calcium current. The onset of action is slow, which results in minimal tachycardia or palpitation
Telmisartan: is a nonpeptide AT1 angiotensin II receptor antagonist. It exerts antihypertensive activity by preventing angiotensin II from binding to AT1 receptors thus inhibiting the vasoconstricting and aldosterone-secreting effects of angiotensin II.
Benidipine: Rapid absorption. Cmax within 2 h. Highest level in the liver and also distribution in the kidneys, plasma, and other tissues. No tissue showed a particularly high accumulation of the drug following repeated oral administrations. Protein binding 98% The percentage urinary excretion of benidipine following an oral dose is about 36%
Telmisartan: Onset: 1-2 hr.
Duration: Up to 24 hr.
Absorption: Rapidly absorbed from the GI tract. Food may slightly decrease the bioavailability. Absolute bioavailability: Dose-dependent (approx 42% after 40-mg dose; 58% after 160-mg dose). Time to peak plasma concentration: Approx. 0.5-1 hr.
Distribution: Volume of distribution: 500 L. Plasma protein binding: >99%.
Metabolism: Undergoes conjugation w/ glucuronic acid to form inactive metabolites.
Telmisartan: Onset: 1-2 hr.
Excretion: Via faeces (97%, as unchanged drug). Terminal elimination half-life: Approx. 24 hr.
Benidipine: Palpitation, facial flushing, hot flushes, chest pressure sensation, headache, dizziness, sleepiness, constipation, nausea, abdominal discomfort, oedema, malaise, tinnitus, redness and warm feeling in the fingers, shoulder stiffness, increased frequency of micturition. Hypersensitive reactions e.g. Rash and itching. Elevation of SGOT, SGPT, alkaline phosphatase, total bilirubin, creatinine and uric acid.
Telmisartan: Dizziness, fatigue, headache, sinusitis, upper resp tract infection, pharyngitis, UTI, back pain, myalgia, diarrhoea, abdominal pain, dyspepsia, nausea.
Potentially Fatal: Intermittent claudication and skin ulcer.
Benidipine Elderly. In case of dizziness or lightheadedness, advise patients against handling of heavy machines or working at elevated spots. Reduce dosage gradually while withdrawing drug. Liver function tests.
Telmisartan: Volume- or salt-depleted patients including patients on prolonged diuretic therapy. Patients w/ renal artery stenosis, aortic or mitral stenosis, obstructive biliary disease. Renal and mild to moderate hepatic impairment. Lactation. Monitoring Parameters Monitor BP, electrolytes and serum creatinine levels.
Benidipine: Adult: PO HTN 2-4 mg once daily, up to 8 mg once daily if needed. Angina pectoris 4 mg twice daily.
Telmisartan: Adult: PO HTN Initial: 40 mg once daily, may be adjusted to 20-80 mg once daily. CV risk reduction 80 mg once daily.