Antihypertensive Drugs, Uses, Side Effects, Drug Interactions

Antihypertensive drugs

Antihypertensive drugs are a class of drugs that are used to treat hypertension (high blood pressure). Antihypertensives drugs therapy seeks to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Evidence suggests that reduction of the blood pressure by 5 mmHg can decrease the risk of stroke by 34%, of ischaemic heart disease by 21%, and reduce the likelihood of dementia, heart failure, and mortality from cardiovascular disease. There are many classes of antihypertensives, which lower blood pressure by different means. Among the most important and most widely used drugs are thiazide diuretics, calcium channel blockers, ACE inhibitors, angiotensin II receptor antagonists (ARBs), and beta blockers.

Includes therapeutic agents that can be used for lowering of blood pressure.

Alpha-Blockers (Antihypertensive)

Alpha blockers, also called alpha-adrenergic antagonists, dilate blood vessels by blocking postsynaptic alpha1-adrenergic receptors. Alpha blockers are generally not recommended as initial therapy.

Generic
Brand Name
Doxazosin
Cardura, Carduran
Prazosin
Minipress, Minipress XL
Terazosin
Hytrin

Alpha-2 Agonists, Central-Acting

Alpha-2 adrenergic receptor agonists work by stimulating alpha-2 receptors and decreasing sympathetic activity, which leads to decreased blood pressure and heart rate.

Generic
Brand Name
Clonidine
Catapres, Catapres TTS (patch), Dixarit, Duraclon, Jenloga, Kapvay, Nexiclon XR
Guanabenz
Wytensin
Guanfacine
Intuniv, Tenex
Methyldopa
Aldomet
Lofexidine
Britlofex

Aldosterone Antagonists, Selective

Generic
Brand Name
Eplerenone
Inspra

Angiotensin II Receptor Blockers

Angiotensin receptor blockers work by blocking the effects of hormone angiotensin II (type 1 receptor). As a result, blood vessels dilate and blood pressure is reduced.

Generic
Brand Name
Azilsartan
Edarbi
Candesartan
Atacand
Eprosartan
Teveten
Irbesartan
Avapro
Losartan
Cozaar
Olmesartan
Benicar
Telmisartan
Micardis
Valsartan
Diovan

ACE (Angiotensin Converting Enzyme) Inhibitors

ACE inhibitors remain the initial treatment of choice for hypertension. This class of drugs blocks the conversion of angiotensin I to angiotensin II by inhibiting angiotensin-converting enzyme (ACE), thus preventing constriction of blood vessels.

Generic
Brand Name
Benazepril
Lotensin
Captopril
Capoten
Enalapril
Vasotec
Fosinopril
Monopril
Lisinopril
Prinivil
Moexipril
Univasc
Perindopril
Aceon
Quinapril
Accupril
Ramipril
Altace
Trandolapril
Mavik

Beta-blockers

Beta-blockers produce antihypertensive action by reducing heart rate and cardiac output. Currently beta-blockers are not recommended as first-line treatment due to the risk of stroke and new-onset of type 2 diabetes when compared to other medications

Generic Brand Name
Beta-blockers with alpha activity
Carvedilol Coreg, Coreg CR
Labetalol Trandate
Beta-blockers with intrinsic sympathomimetic activity
Acebutolol Sectral
Pindolol Visken
Penbutolol Levatol
Beta-1 cardioselective beta-blockers
Atenolol Tenormin
Betaxolol Kerlone
Bisoprolol Zebeta
Celiprolol Selectol
Metoprolol Lopressor, Toprol XL
Nebivolol Bystolic
Sotalol Betapace, Betapace AF, Sorine
Nonselective beta-blockers
Nadolol Corgard
Propranolol Inderal LA, InnoPran XL
Timolol Blocadren

Calcium Channel Blockers

Calcium channel blockers decrease the entry of calcium into the cells of the heart and blood vessels. By blocking the entry of calcium, this class of drugs reduces heart rate and contractility and dilates arteries.

Generic
Brand Name
Amlodipine
Norvasc, Lotrel
Bepridil
Vascor
Clevidipine
Cleviprex
Diltiazem
Calan, Calan SR, Cardizem, Covera HS, Isoptin SR, Verelan, Verelan PM
Felodipine
Plendil
Lacidipine
Caldine, Lacimen, Lacipil, Midotens, Motens
Lercanidipine
Lercadip, Zanidip
Levamlodipine
EsCordi Cor, Esam, Eslo, S-Amlip
Isradipine
DynaCirc, DynaCirc CR
Nicardipine
Cardene SR
Nifedipine
Adalat, Nifediac, Nifedical, Procardia
Nimodipine
Nimotop
Nisoldipine
Sular
Verapamil
Calan, Calan SR, Covera-HS, Isoptin SR, Verelan, Verelan PM
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Diuretics, Loop

Loop diuretics lower blood pressure by reducing blood volume. These medications inhibit the sodium-potassium-chloride cotransporter in the thick ascending limb of the loop of Henle. Loop diuretics promote water loss and increase sodium excretion.

Generic
Brand Name
Bumetanide
Bumex
Ethacrynic acid
Edecrin
Furosemide
Lasix
Piretanide
Torsemide
Demadex

Diuretics, Potassium-Sparing

Potassium-sparing diuretics work by leaving more potassium in the blood, as a result more sodium and water are excreted in the urine. Potassium-sparing diuretics are weak antihypertensives when used alone.

Generic
Brand Name
Amiloride
Midamore
Spironolactone
Aldactone
Triamterene
Dyrenium

Diuretics, Thiazide

Thiazide diuretics reduce sodium absorption from the distal tubule segment of the kidney. Thiazide diuretics are known to worsen insulin sensitivity and elevate serum total cholesterol levels

Generic
Brand Name
Bendroflumethiazide
Aprinox
Chlorothiazide
Diuril
Chlorthalidone
Hygroton
Indapamide
Lozol
Hydrochlorothiazide
Hydrodiuril
Methyclothiazide
Enduron
Metolazone
Zaroxolyn, Diulo, Mykrox

Peripheral Adrenergic Inhibitors

These medications are rarely used unless other medications don’t help.

Generic
Brand Name
Guanadrel
Hylorel
Guanethidine
Ismelin
Reserpine
Serpasil

Renin Inhibitors

Renin inhibitors act by inhibiting the activity of renin, the enzyme responsible for angiotensin II levels.

Generic
Brand Name
Aliskiren
Tekturna

Vasodilators

Vasodilators work by dilating arterioles. However, vasodilatation by itself causes increased sympathetic outflow to the heart, leading to tachycardia and increased contraction.

Generic
Brand Name
Diazoxide
Proglycem
Hydralazine
Apresoline, Dralzine
Minoxidil
Loniten
Nitroprusside
Nipride, Nitropress, Sodium Nitroprusside

Antihypertensive Combinations

Generic Brand Name
Alpha blockers and diuretics
Prazosin/Polythiazide Minizide
ACE inhibitors and Diuretics
Benazepril Lotensin HCT
Captopril Capozide
Enalapril Vaseretic
Fosinopril Monopril HCT
Lisinopril Prinzide, Zestoretic
Moexipril Uniretic
Quinapril Accuretic
Angiotensin ll Antagonists and Diuretics
Candesartan Atacand HCT
Eprosartan Teveten HCT
Irbesartan Avalide
Losartan Hyzaar
Olmesartan Benicar HCT
Telmisartan Micardis HCT
Valsartan Diovan HCT
Beta-blockers and Diuretics
Atenolol/Chlorthalidone Tenoretic
Bisoprolol Ziac
Metoprolol Lopressor HCT
Nadolol/Bendroflumethiazide Corzide
Propranolol Inderide
Timolol Timolide
Calcium channel blockers and ACE inhibitors
Amlodipine/Benzapril Lotrel
Amlodipine/Perindopril Prestalia
Diltiazem/Enalapril Teczem
Felodipine/Enalapril Lexxel
Lercanidipine/Enalapril Carmen ACE, Coripren
Verapamil/Trandolapril Tarka
Calcium channel blockers and Angiotensin II receptor antagonist
Amlodipine/Olmesartan Azor
Amlodipine/Olmesartan Tribenzor
Amlodipine/Telmisartan Twynsta
Amlodipine/Valsartan Exforge
Amlodipine/Valsartan Exforge HCT
Centrally acting drugs and Diuretics
Methyldopa Aldoril
Reserpine/Chlorothiazide Diupres
Reserpine Hydropres
Diuretic combinations
Amiloride Moduretic
Spironolactone Aldactone
Triamterene Dyazide, Maxzide
Clonidine/Chlorthalidone Combipres
Hydralazine Apresazide
Methyldopa Aldoril
Prazosin/Polythiazide Minizide
Other combinations
Amlodipine/Atorvastatin Caduet
Amlodipine/Aliskiren Tekamlo
Amlodipine/Aliskiren Amturnide
Aliskiren/HCTZ Tekturna HCT
Aliskiren/Valsartan Valturna
Nebivolol/Valsartan Byvalson

Blood pressure medications

Telmisartan affects the renin-angiotensin-aldosterone. You shouldn’t take this drug with other medicines that affect this system. These drugs include:

  • aliskiren. Telmisartan and aliskiren shouldn’t be used together in adults with diabetes or moderate kidney disease.
  • angiotensin receptor blockers (ARBs), such as:
    • candesartan (Atacand, Atacand HCT)
    • eprosartan (Teveten)
    • irbesartan (Avapro, Avalide)
    • losartan (Cozaar, Hyzaar)
    • olmesartan (Benicar, Benicar HCT, Tribenzor, Azor)
    • valsartan (Diovan, Diovan HCT, Exforge, Exforge HCT)
    • azilsartan (Edarbi, Edarbyclor)
  • angiotensin-converting enzyme (ACE) inhibitors, such as:
    • benazepril (Lotensin, Lotrel, Lotensin HCT)
    • captopril
    • enalapril (Vasotec, Epaned)
    • fosinopril (Monopril)
    • lisinopril (Prinivil, Zestril, Prinzide, Zestoretic)
    • moexipril (Uniretic)
    • perindopril (Aceon)
    • quinapril (Accupril, Accuretic)
    • ramipril (Altace)
    • trandolapril (Mavik, Tarka)
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Mechanism of Action of Antihypertensives Drugs

Antihypertensive drug competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.

Antihypertensive drugs is classified as a non-cardioselective sympatholytic beta blocker that crosses the blood–brain barrier. It is lipid soluble and also has sodium channel blocking effects.  Antihypertensive drugs is a non-selective beta blocker; that is, it blocksthe action of epinephrine (adrenaline) and norepinephrine (noradrenaline) at both β1– and β2-adrenergic receptors. It has little intrinsic sympathomimetic activity, but has strong membrane stabilizing activity (only at high blood concentrations, e.g. overdose). Antihypertensive drugs is able to cross the blood–brain barrier and exert effects in the central nervous system in addition to its peripheral activity.

In addition to blockade of adrenergic receptors, Antihypertensive drugs has very weak inhibitory effects on the norepinephrine transporter and/or weakly stimulates norepinephrine release (i.e., the concentration of norepinephrine is increased in the synapse).Since propranolol blocks β-adrenoceptors, the increase in synaptic norepinephrine only results in α-adrenoceptor activation, with the α1-adrenoceptor being particularly important for effects observed in animal models. Therefore, it can be looked upon as a weak indirect α1-adrenoceptor agonist in addition to potent β-adrenoceptor antagonist.In addition to its effects on the adrenergic system, there is evidence that indicates that antihypertensive drugs may act as a weak antagonist of certain serotonin receptors, namely the 5-HT1A, 5-HT1B, and 5-HT2Breceptors.The latter may be involved in the effectiveness of propranolol in the treatment of migraine at high doses

or

Antihypertensive drugs competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.

Indications of Antihypertensive drugs

Cardiovascular

Psychiatric

Antihypertensive drugs is occasionally used to treat performance anxiety.Evidence to support its use in other anxiety disorders is poor.Some experimentation has been conducted in other psychiatric areas

Others

  • Essential tremor. Evidence for use for akathisia however is insufficient
  • Migraine and cluster headache prevention and in primary exertional headache
  • Hyperhidrosis (excessive sweating)
  • Proliferating infantile hemangioma
  • Glaucoma
  • Thyrotoxicosis by deiodinase inhibition
  • Akathisia caused by antipsychotic use
  • Angina Pectoris
  • Cardiovascular Mortality
  • Gastroesophageal variceal hemorrhage prophylaxis
  • Hemangiomas
  • High Blood Pressure (Hypertension)
  • Idiopathic hypertrophic subaortic stenosis
  • Migraines
  • Nonvalvular Atrial Fibrillation
  • Obstructive Hypertrophic Cardiomyopathy
  • Performance Anxiety
  • Pheochromocytomas
  • Supraventricular Arrhythmias
  • Tachyarrhythmia caused by Digitalis intoxication
  • Tachyarrhythmia caused by catecholamine excess
  • Thyroid Crisis
  • Thyrotoxicosis
  • Tremor caused by lithium
  • Tremor, Essential
  • Ventricular Tachycardia

Contra Indications of Antihypertensive drugs

Antihypertensive drugs may be contraindicated in people with

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Side Effects of Antihypertensive drugs

The most common

Common

Rare

Drug Interactions of Antihypertensive drugs

Antihypertensive drugs may interact with following drugs, supplyments, & may change the efficacy of drugs

This medication may interfere with certain laboratory tests (including glaucoma screening test, cardiovascular stress testing using arbutamine), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

References

  1. https://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0025447/
  2. https://en.wikipedia.org/wiki/Antihypertensive_drug

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