Telmisartan/amlodipine

Mechanism of Action

Telmisartan is a vasoconstrictor angiotensin II receptor blocker (ARB); prevents angiotensin II from binding to its receptor, which in turn blocks the vasoconstriction and aldosterone secreting effects of angiotensin II.

Amlodipine is a dihydropyridine calcium channel blocker (CCB); acts in vascular smooth muscle to produce peripheral aterial vasodilation, which in turn reduces peripheral vascular resistance and blood pressure

Pharmacokinetics

Telmisartan

• Half-Life: 24 hr
• Onset: 1-2 hr
• Bioavailability: 42-58%; dose-dependent
• Vd: 500 L
• Peak Plasma Time: 0.5-1 hr
• Protein Bound: >99.5%
• Metabolism: Liver to inactive metabolite (not metabolized via CYP)
• Clearance: 800 mL/min
• Excretion: Feces (97%)

Amlodipine

• Half-Life: 30-50 hr
• Bioavailability: 64-90%
• Vd: 21 L/kg
• Peak Plasma Time: 6-12 hr
• Protein Bound: 93-98%
• Metabolism: Liver (>90%); P450 CYP3A4
• Clearance: 25 L/hr
• Excretion: Urine (70%)

Telmisartan/amlodipine can cause harm or death to an unborn baby. Talk to your doctor about other ways to lower your blood pressure if you plan to become pregnant. If you get pregnant while taking telmisartan/amlodipine, tell your doctor right away.

You should not take telmisartan/amlodipine if you are allergic (hypersensitive) to the active ingredients (telmisartan or amlodipine) or any of the other ingredients.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

This medication falls into category D. Telmisartan/amlodipine can cause harm or death to an unborn baby. Talk to your doctor about other ways to lower your blood pressure if you plan to become pregnant. If you get pregnant while taking telmisartan/amlodipine, tell your doctor right away.

The telmisartan/amlodipine dose must be individualized. Your doctor will determine the best dose for you. Follow the directions on your prescription label carefully. Your doctor may start you on a low dose and increase it after two weeks. 

The maximum recommended dose of telmisartan/amlodipine is 80/10 mg once daily.

WARNING: FETAL TOXICITY

• When pregnancy is detected, discontinue telmisartan/amlodipine as soon as possible.
• Drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus