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Anti-Hypertensive & Antianginal Agents (P. Chemistry | Ch-7 | Unit-2): D Pharma 1st year Notes

Anti-Hypertensive Agents

Antihypertensive agents are drugs used to treat hypertension (high blood pressure), a major risk factor for heart disease, stroke, and kidney disease. Different classes work through different mechanisms to lower blood pressure.

Classification of Anti-Hypertensive Agents

  • Diuretics: Hydrochlorothiazide, Furosemide
  • Beta-Blockers: Atenolol, Metoprolol, Propranolol
  • Calcium Channel Blockers: Amlodipine, Diltiazem, Verapamil
  • ACE Inhibitors: Captopril, Lisinopril, Ramipril
  • ARBs (Angiotensin Receptor Blockers): Candesartan, Losartan, Valsartan

1. Propranolol

Classification: Beta-Adrenergic Receptor Antagonist (Beta-Blocker) — Class II Anti-Arrhythmic

Propranolol chemical structure

IUPAC/Chemical Name: 1-(Isopropylamino)-3-(1-naphthoxy)-2-propanol

Uses:

  • High blood pressure (hypertension)
  • Angina (chest pain)
  • Arrhythmias (irregular heartbeats)
  • Hyperthyroidism (overactive thyroid)
  • Proliferating infantile hemangioma (a type of birthmark)

Stability and Storage: Stable at room temperature. Store in a cool, dry place away from direct sunlight.

Formulations: Tablets, Capsules, Extended-release tablets, Oral solution, Injection

Brand Names: Inderal, Inderal LA, Avlocardyl


2. Captopril

Classification: ACE Inhibitor (Angiotensin-Converting Enzyme Inhibitor)

Captopril chemical structure

IUPAC/Chemical Name: (2S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid

Chemical Description: Captopril is an L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group.

Mechanism of Action: ACE inhibitors block the production of angiotensin II, a powerful vasoconstrictor that causes blood vessels to narrow. By blocking angiotensin II, captopril relaxes blood vessels and lowers blood pressure.

Uses:

  • Treatment of high blood pressure (hypertension)
  • Heart failure management

Stability and Storage: Store at room temperature in a cool, dry place. Protect from direct sunlight.

Formulations: Tablets, Capsules, Oral solution, Intravenous solution

Brand Names: Capoten, Capozide, Aceon, Accupril


3. Ramipril

Classification: ACE Inhibitor

Ramipril chemical structure

IUPAC/Chemical Name: (2S,3aS,6aS)-1[(S)-N-[(S)-1-Carboxy-3-phenylpropyl]alanyl]octahydrocyclopenta[b]pyrrole-2-carboxylic acid, 1-ethyl ester

Uses:

  • Treatment of high blood pressure (hypertension) and heart failure
  • Prescribed after a heart attack
  • Prevention of future strokes, heart attacks, and kidney problems
  • Improves survival in patients with heart failure or post-heart attack

Stability and Storage: Store at room temperature in a cool, dry place. Protect from direct sunlight.

Formulations: Tablets, Capsules, Injectables

Brand Names: Altace, Prinivil, Zestril


4. Methyldopate Hydrochloride

Classification: Centrally Acting Anti-Hypertensive

Methyldopate Hydrochloride chemical structure

IUPAC/Chemical Name: Levo-3-(3,4-dihydroxyphenyl)-2-methylalanine, ethyl ester hydrochloride

Uses:

  • Treatment of high blood pressure (hypertension)
  • Some cases of Parkinson’s disease

Stability and Storage: Stable at room temperature. Store in a cool, dry place.

Formulations: Tablets, Capsules

Brand Names: Aldomet, Dopar, Parcopa


5. Clonidine Hydrochloride

Classification: Centrally Acting Alpha-2 Agonist / Anti-Hypertensive

Clonidine Hydrochloride chemical structure

IUPAC/Chemical Name: N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

Uses:

  • High blood pressure (hypertension)
  • Attention Deficit Hyperactivity Disorder (ADHD)
  • Drug withdrawal (alcohol, opioids, smoking)
  • Menopausal flushing
  • Diarrhea, spasticity, and certain pain conditions

Onset of action is typically within one hour, with blood pressure effects lasting up to eight hours.

Stability and Storage: Store at room temperature in a cool, dry place. Protect from direct sunlight.

Formulations: Tablets, Capsules, Liquid, Patches, Injectable solution

Brand Names: Catapres, Kapvay, Duraclon


6. Hydralazine Hydrochloride

Classification: Direct-Acting Vasodilator / Anti-Hypertensive

Hydralazine Hydrochloride chemical structure

IUPAC/Chemical Name: Phthalazin-1-ylhydrazine hydrochloride

Uses:

  • Treatment of high blood pressure (hypertension)
  • Control of high blood pressure during pregnancy (pre-eclampsia or eclampsia)
  • Hypertensive crisis (emergency situations with extremely high blood pressure)

Stability and Storage: Store at room temperature in a cool, dry place. Protect from direct sunlight.

Formulations: Tablets, Capsules, Injectable

Brand Names: Apresoline, Hydrex, Unipril


7. Nifedipine

Classification: Calcium Channel Blocker / Anti-Hypertensive

Nifedipine chemical structure

IUPAC/Chemical Name: 3,5-dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

Uses:

  • High blood pressure (hypertension)
  • Angina (chest pain)
  • Preterm labor
  • Raynaud’s phenomenon (a condition causing blood vessels in fingers and toes to narrow, resulting in cold and numbness)

Stability and Storage: Store at room temperature in a cool, dry place. Protect from direct sunlight.

Formulations: Tablets, Capsules, Transdermal patch

Brand Names: Adalat


Antianginal Agents

Antianginal agents treat angina pectoris — chest pain caused by reduced oxygen supply to the heart.

Classification of Antianginal Agents

Nitrates: Relax blood vessels to increase blood flow to the heart. Examples: Nitroglycerin, Isosorbide Dinitrate, Isosorbide Mononitrate.

Beta Blockers: Slow the heart rate and reduce the force of contractions, decreasing the heart’s oxygen demand. Examples: Atenolol, Metoprolol, Propranolol.

Calcium Channel Blockers: Relax muscles in blood vessel walls to increase blood flow to the heart. Examples: Diltiazem, Nifedipine, Verapamil.


8. Isosorbide Dinitrate

Classification: Nitrate / Antianginal Agent

Isosorbide Dinitrate chemical structure

IUPAC/Chemical Name: 1,4-Dioxane-3,5-diyl dinitrate

Mechanism of Action: Works by relaxing blood vessels, which increases blood flow to the heart.

Uses:

  • Treatment of angina pectoris (chest pain)

Stability and Storage: Store in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Formulations: Tablets, Capsules, Sublingual

Brand Names: Dilatrate-SR, Isordil, Isordil Titradose, ISDN