ATII Blockers and nitrates

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Flashcards about ATII Blockers and nitrates.

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20 Terms

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ATII Blockers and nitrates

Blockers and nitrates are the main focus.

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Effects of ATII Blockers and Nitrates

Reduced Blood Pressure, Renin Release, Lowered Sodium Excretion, Vasoconstriction, Aldosterone Secretion, Sodium and Fluid Retention, Increased Peripheral Resistance, Increased Cardiac Output, Elevated Blood Pressure

<p>Reduced Blood Pressure, Renin Release, Lowered Sodium Excretion, Vasoconstriction, Aldosterone Secretion, Sodium and Fluid Retention, Increased Peripheral Resistance, Increased Cardiac Output, Elevated Blood Pressure</p>
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Renin metabolism pathway

A biochemical pathway that regulates blood pressure, controlling the conversion of angiotensinogen to angiotensin I, and then to angiotensin II, influencing vascular tone and fluid balance.

<p>A biochemical pathway that regulates blood pressure, controlling the conversion of angiotensinogen to angiotensin I, and then to angiotensin II, influencing vascular tone and fluid balance. </p>
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Angiotensin I

ASP-ARG-VAL-TYR-ILE-HIS-PRO-PHE-HIS-LEU

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Angiotensin II

ASP-ARG-VAL-TYR-ILE-HIS-PRO-PHE-HIS-LEU

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Angiotensin III

ARG-VAL-TYR-ILE-HIS-PRO-PHE

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ARB Mechanism

ARB bind and inhibit angiotensin II (ATII) type 1 receptor (AT1).

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AT1 Activation

causes vascular smooth muscle contraction, sodium and water retention, and aldosterone secretion.

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ARBs Uses

ARBs are used to treat hypertension, heart failure, diabetic nephropathy and for patients who cannot tolerate ACE inhibitors.

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Examples of ARBs

EXP3174, Valsartan, Telmisartan, Candesartan, Olmesartan, Azilsartan, Irbesartan

<p>EXP3174, Valsartan, Telmisartan, Candesartan, Olmesartan, Azilsartan, Irbesartan</p>
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ARB SAR

Imidazole ring mimics His6 in angiotensin II. Butyl/propyl substituent mimics Ile. Biphenyl group has ortho acidic substituent (tetrazole is best).

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Losartan

a Prodrug that is converted to its active form, EXP3174, in the liver. It is primarily used for hypertension and to protect against kidney damage in diabetic patients.

<p>a Prodrug that is converted to its active form, EXP3174, in the liver. It is primarily used for hypertension and to protect against kidney damage in diabetic patients. </p>
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Metabolite of Losartan

Losartan 5-carboxylic acid derivative

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ARBs Requiring Hydrolysis (Prodrugs)

Olmesartan medoxomil, Candesartan cilexetil, Azilsartan medoxomil

<p>Olmesartan medoxomil, Candesartan cilexetil, Azilsartan medoxomil</p>
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Active Metabolite ARBs

Olmesartan, Candesartan, Azilsartan

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ARBs Characteristics

Highly variable bioavailability, high protein binding, primarily fecal elimination unchanged, Interactions with other antihypertensive drugs, contraindicated in pregnancy/nursing.

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Organic nitrates

Nitroglycerin, Isosorbide dinitrate, Pentaerythrityl tetranitrate, Isosorbide mononitrate, Amyl nitrite, Sodium nitroprusside, Nicorandil

<p>Nitroglycerin, Isosorbide dinitrate, Pentaerythrityl tetranitrate, Isosorbide mononitrate, Amyl nitrite, Sodium nitroprusside, Nicorandil</p>
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Organic nitrate mechanism & use

Prodrugs for nitric oxide (NO). Causes relaxation of vascular smooth muscle cells. Decreases cardiac preload and increases coronary blood flow. Used for treating angina (prophylactic and acute), hypertension, and heart failure. Nitrate tolerance can develop.

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Organic nitrates Characteristics

Lipophilic nitrate esters, are very well absorbed, has a wide variety of dosage forms, metabolically activated to deliver NO and has interactions.

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Big Picture

These drugs act on renin-angiotensin-aldosterone-system (RAAS) or generate nitric oxide directly. DDIs with each other or diuretics can be beneficial or harmful. They have similar mechanism-based DDIs