PHARMACOLOGY NOTES BY MUNEEB

CHOLINERGIC DRUGS :
Cholinergic medications are a category of pharmaceutical agents that act
upon the neurotransmitter acetylcholine, the primary neurotransmitter
within the parasympathetic nervous system (PNS). There are two broad
categories of cholinergic drugs:
1) Direct-acting
2) Indirect-acting

Cholinergic Agonists (Parasympathomimetic ):

Direct-Acting Cholinergic Agonists :
The direct-acting cholinergic agonists work by directly binding to and
activating the muscarinic receptors. Examples of direct-acting cholinergic
agents include :
 Choline esters (acetylcholine, methacholine, carbachol,
bethanechol,)
 Alkaloids (muscarine, pilocarpine, cevimeline).

Indirect-Acting Cholinergic Agonists ( Anticholinesterases ):

Anticholinesterases are drugs that stimulate cholinergic transmission
indirectly by inhibiting the enzyme AChE, which hydrolysis and inactivates
ACh in the synaptic clefts of the autonomic nervous system, the CNS, and
the neuromuscular junction of the somatic nervous system. Indirect-acting
cholinergic agents increase the availability of acetylcholine at the
cholinergic receptors. These include :
 Reversible agents (physostigmine, neostigmine, pyridostigmine,
edrophonium, rivastigmine, donepezil, galantamine)
 Irreversible agents (echothiophate, parathion, malathion, diazinon,
sarin, soman).
Cholinergic Antagonists (Parasympatholytic) :
Parasympatholytic drugs, also known as anticholinergic or cholinergic
antagonists, are substances that block or inhibit the effects of
acetylcholine in the parasympathetic nervous system. The
parasympathetic nervous system is responsible for the "rest and digest"
functions of the body. By inhibiting the action of acetylcholine,
parasympatholytic drugs can produce various physiological effects. These
drugs are used for a variety of therapeutic purposes. Here are some
examples of parasympatholytic drugs and their applications:

1. Atropine:
 Mechanism of Action: Blocks muscarinic receptors.
 Therapeutic Uses:

 Dilates the pupils (mydriasis) during eye examinations

or surgery.
 Treats bradycardia (slow heart rate) and
organophosphate poisoning.
 Inhibits salivary and respiratory secretions during
anesthesia.
2. Scopolamine:
 Mechanism of Action: Blocks muscarinic receptors.

 Therapeutic Uses:
 Prevention of motion sickness.
 Treatment of nausea and vomiting, especially in
postoperative and chemotherapy settings.
3. Tolterodine, Oxybutynin, Solifenacin:
  Mechanism of Action: Muscarinic receptor antagonists.
 Therapeutic Uses:
 Treatment of overactive bladder by reducing
involuntary contractions of the bladder muscles.
4. Ipratropium, Tiotropium:
 Mechanism of Action: Blocks muscarinic receptors in the
respiratory tract.

 Therapeutic Uses:
 Bronchodilation in conditions like asthma and chronic
obstructive pulmonary disease (COPD).
5. Darifenacin, Fesoterodine:
 Mechanism of Action: Muscarinic receptor antagonists.

 Therapeutic Uses:
 Treatment of overactive bladder, similar to tolterodine
and oxybutynin.
6. Benztropine, Trihexyphenidyl:
 Mechanism of Action: Muscarinic receptor antagonists.
 Therapeutic Uses:

 Used in the treatment of Parkinson's disease to help

control tremors and muscle stiffness.
7. Glycopyrrolate:
 Mechanism of Action: Muscarinic receptor antagonist.
 Therapeutic Uses:

 Reduces salivary and respiratory secretions during

surgery.
 Used to treat excessive sweating (hyperhidrosis).
8. Dicyclomine, Hyoscyamine:
 Mechanism of Action: Muscarinic receptor antagonists.
 Therapeutic Uses:
 Treatment of irritable bowel syndrome (IBS) by
reducing gastrointestinal spasms.