Subject: Pharmaceutical Chemistry

Unit 6.2: ADRENERGIC ANTAGONISTS

Points To Be Cover In This Presentation

 Introduction
 Classification, Properties of Various Drugs Use to Block α and β Receptors.

PRESENTATION BY: RAVI SHARMA

QUALIFICATION: M.PHARMACY
 INTRODUCTION
• Adrenergic antagonist An adrenergic antagonist is a drug that inhibits
the function of adrenergic receptors.
• They are competitive antagonists at α or β or both α and β adrenergic
receptors, and differ in important ways from the “adrenergic neurone
blocking drugs”, which act by interfering with storage or release of
adrenergic transmitter.
• They can be selective or non-selective so they can be classified
according to their affinity to the receptors.
 CLASSIFICATION
Phentolamine
Reversible
Tolazoline (priscoline)
Non-selective block α-1 and α-2
receptor Irreversible Phenoxybenzamine

Miscellaneous Ergot alkaloids

Prazosin

α-Adrenoceptor antagonists
Terazosin

α-1 blockers Doxazosin

Alfuzosin & Bunazosin

Selective
Tamsulosin & Silodosin

Yohimbine
α-2 blockers
β-Adrenoceptor antagonists Next Page….. Idazoxam
MECHANISMS OF ACTION
 Tolazoline
• Structure:-

• IUPAC name: 2-benzyl-4,5-dihydro-1H-imidazole

• Physical Properties: It is a white or creamy white, bitter, crystalline
powder with slightly aromatic odour. Soluble in water and alcohol,
and practically insoluble in ether.
• Storage: Well-closed container.
• Use: Vasodilator, used to reduce pulmonary artery pressure.
• Preparation: Tablet and injection
• Brand name: Priscoline Hydrochloride.
 Phentolamine
• Structure:-

• IUPAC name: 3-[[(4,5-dihydro-1H-imidazol-2-yl)methyl]-4-

methylanilino]phenol
• Physical Properties: It is a white or almost white, crystalline powder.
Which is slightly hygroscopic. Soluble in water.
• Storage: Well-closed container, protect from light and moisture.
• Use: Hypertention.
• Preparation: Injection
• Brand name: Regitine and Rogitine.
 Phenoxybenzamine
• Structure:-

• IUPAC name: Benzyl(2-chloroethyl)-1-phenoxypropan-2-amine

• Physical Properties: It is a white or almost white, crystalline powder.
Springly Soluble in water.
• Storage: Well-closed container.
• Use: Antihypertensive Agents, Vasodilator.
• Preparation: Capsule
• Brand name: Fenoxene
 Prazosin
• Structure:-

• IUPAC name: [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-

yl]-(furan-2-yl)methanone
• Physical Properties: It is a white or almost white, crystalline powder,
slightly Soluble in water.
• Storage: Well-closed container, protect from light.
• Use: Antihypertensive Agents, heart failure, benign prostatic hyerplasia.
• Preparation: Tablet
• Brand name: Hypovase and minipress
 Propranolol
• Structure:-

• IUPAC name: 1-[(1-methylethylamino]-3-(naphthalen-1-yloxy)propan-

2-ol
• Physical Properties: It is a white or almost white, crystalline powder,
Soluble in water.
• Storage: Well-closed container, protect from moisture.
• Use: Antihypertensive Agents,
• Preparation: Tablet, capsule, injection
• Brand name: Angylol, Inderal, Syprol
 Atenolol
• Structure:-

• IUPAC name: 4-(2-Hydroxy-3-

isopropylaminopropoxy)phenylacetamide
• Physical Properties: It is a white or almost white, crystalline powder,
sparingly soluble in water.
• Storage: Well-closed container, protect from moisture.
• Use: Antihypertensive Agents,
• Preparation: Tablet, oral solution, injection
• Brand name: Aten, Cadres, Hipers, Tenolol
CARVEDILOL

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