Med Chem

Introduction:
What is Synthetic Drug ?

A synthetic drug is a substance created in a laboratory through chemical synthesis
rather than being derived from natural sources. These drugs are designed to mimic or
enhance the effects of natural substances or to create entirely new effects. Synthetic
drugs can include a wide range of substances, including pharmaceuticals, recreational
drugs, and performance-enhancing drugs.
What is Cholinergic ?
Cholinergic refers to the physiological effects associated with the neurotransmitter
acetylcholine. Acetylcholine plays a crucial role in the functioning of the nervous
system, particularly in transmitting signals between nerve cells (neurons) and
between neurons and muscles. Cholinergic effects are mediated by receptors called
cholinergic receptors, which are found in various tissues throughout the body.
Synthetic cholinergic blocking agents :

Synthetic cholinergic blocking agents, also known as anticholinergic drugs, are
pharmaceutical compounds that inhibit the action of acetylcholine at its receptor sites in
the nervous system. These drugs are widely used in the management of various medical
conditions, including gastrointestinal disorders, respiratory ailments, neurological
disorders, and as premedication in anaesthesia. This report aims to provide an overview
of synthetic cholinergic blocking agents, their mechanism of action, therapeutic uses,
side effects, and future prospects.
 Mechanism of Action:
Cholinergic blocking agents exert their pharmacological effects by competitively
antagonizing the binding of acetylcholine to its receptors, primarily muscarinic
1
receptors located in various tissues and organs. By blocking the action of acetylcholine,
these agents inhibit parasympathetic nervous system activity, leading to a range of
physiological effects depending on the specific receptors targeted.
Solanaceous alkaloids are ester of the tropine, these alkaloids are obtained from plants
these such as atropa belladonna, Hyoscyamus niger, Datura stramonium etc. It is an
optically active compound and levoform is potent. (-) scopolamine is slightly water
miscible viscous liquid.
Scopolamine occurs as Scopolamine hydrobromide salt, which is colorless, odorless,
water soluble powder.
1. Atropine sulphate :
Mechanism of action – It has both central and peripheral action. It first stimulates and
then depresses the CNS.
Uses - used in the treatment of gastric and duodenal ulcers and used in the treatment of
smooth muscle spasm .
2. Hyoscyamine sulphate :
Mechanism of action - Similar to atropine but more potent than atropine .
Uses – a) Treatment of gastric and duodenal ulcer.

b) Also used In treatment of parkinsonism .
c) Prevent motion sickness .
2
3. Scopolamine hydrobromide :
Mechanism of action - It has more rapid onset but shorter duration of action than
atropine also more potent than atropine . As well as it is more toxic .
Uses – a) Used in the treatment of motion sickness.

b) Sometimes used before surgery to decrease saliva .
4. Homatropine hydrobromide :
Mechanism of action - It is a competitive inhibitor of acetylcholine at the muscarinic
receptor, blocks parasympathetic stimulation .
Uses – It is used to dilate or enlarge pupils in eyes .
5. Ipratropium bromide :
Mechanism of action - It is quaternary ammonium compound which blocks muscarinic
acetylcholine receptors . It is non-selective Muscarinic antagonist .
Uses – a) Used in the treatment of Asthma.

b) Treatment of chronic obstructive pulmonary disease (COPD).
3
 Synthesis of Ipratropium bromide:-
 Therapeutic Uses :
Synthetic cholinergic blocking agents have diverse therapeutic uses across various
medical specialties.
i. Treatment of Overactive Bladder: Agents like tolterodine and oxybutynin are
used to reduce bladder spasms and urge incontinence by inhibiting detrusor muscle
contractions.
ii. Parkinson's Disease: Anticholinergic drugs such as benztropine and
trihexyphenidyl are used as adjunctive therapy to reduce tremors and muscle rigidity
in Parkinson's disease.
iii. Prevention of Motion Sickness: Scopolamine patches are applied transdermally to
prevent motion sickness by blocking cholinergic transmission in the vestibular
system.
iv. Anesthesia: Anticholinergic drugs like glycopyrrolate and atropine are administered
preoperatively to reduce secretions and prevent bradycardia during surgery.
4
 Side Effects and Precautions:
Despite their therapeutic benefits, synthetic cholinergic blocking agents can cause
various side effects due to their non-selective blockade of cholinergic receptors.
Common side effects include dry mouth, blurred vision, constipation, urinary retention,
and cognitive impairment, particularly in elderly patients. Additionally, long-term use
of anticholinergic drugs has been associated with an increased risk of cognitive decline
and dementia.
 Conclusion:
Synthetic cholinergic blocking agents play a vital role in the management of numerous
medical conditions by inhibiting cholinergic transmission at muscarinic or nicotinic
receptors. While these drugs offer significant therapeutic benefits, clinicians must
carefully consider their use, balancing the potential benefits against the risk of side
effects, particularly in vulnerable patient populations. Further research is needed to
better understand the long-term effects of anticholinergic therapy and to develop more
selective agents with improved efficacy and safety profiles.
 Reference:
i. Boura AL, Green AF. Adrenergic neurone blocking agents. Annual review of
Pharmacology. 1965 Apr;5(1):183-212.
ii. Reza KH, Das PP, Hossain CM, Shaharyar MA, Pal S, Ali SZ, Kazmi I.
Mechanism of action of cholinergic drugs. InHow Synthetic Drugs Work 2023
Jan 1 (pp. 27-46). Academic Press.
iii. McGeer PL, Eccles JC, McGeer EG, McGeer PL, Eccles JC, McGeer EG.
Cholinergic neurons. Molecular neurobiology of the mammalian brain.
1978:147-81.

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Introduction:

What is Synthetic Drug ?

Synthetic cholinergic blocking agents :

Uses – a) Treatment of gastric and duodenal ulcer.

Uses – a) Used in the treatment of motion sickness.

Uses – It is used to dilate or enlarge pupils in eyes .

Uses – a) Used in the treatment of Asthma.

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