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Cholinergic Antagonists: Pharmacological Actions

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Cholinergic antagonists, such as antimuscarinics, block muscarinic receptors to inhibit muscarinic functions in the body.

Tertiary antimuscarinics can cross the BBB and have greater excitatory central effects than quaternary agents.

They also inhibit perspiration and regulate the hypothalamus, increasing the body temperature.

In the eye, antimuscarinics relax the ocular ciliary muscles, inducing mydriasis and cycloplegia. Furthermore, they decrease aqueous humor drainage, leading to increased intraocular pressure.

In the respiratory system, antimuscarinics relax the smooth muscles and reduce secretions, to prevent bronchoconstriction.

Following administration, antimuscarinics often cause tachycardia, leading to an increase in blood pressure.

Within the gut, inhibition of the parasympathetic stimulation by antimuscarinics reduces gut motility and secretions.

In the urinary system, by limiting parasympathetic inputs, antimuscarinics decrease bladder contraction to effectively inhibit micturition.

Antimuscarinics have dose-dependent side effects, and severe cases of poisoning are associated with convulsions and coma.

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Antimuscarinic drugs block muscarinic receptors in multiple systems, including the gut, eye, smooth muscles, respiratory tract, cardiovascular, and central nervous systems. They produce similar effects with varying selectivity depending on the specific agent and tissue. Here are the key pharmacological actions of antimuscarinics:

Gastrointestinal Effects: Antimuscarinics reduce gut contractions, increase gastric emptying, and slow intestinal transit. They partly inhibit gastric acid secretion and significantly reduce salivary secretions. Mucin and proteolytic enzyme secretions are partially inhibited, while bile production remains unaffected.

Smooth Muscle Relaxation: Antimuscarinics relax smooth muscles in the bronchi, biliary, and urinary tract. They inhibit secretions in the mouth, nose, bronchi, and pharynx, leading to dryness of airway mucous membranes and preventing reflex bronchoconstriction. They also decrease bladder and ureter tone, reducing the urge to urinate.

Ocular Effects: Antimuscarinics cause pupil dilation (mydriasis) and paralysis of accommodation (cycloplegia) in the eye, impairing near vision. They increase intraocular pressure and inhibit lacrimal secretions, which can be problematic for individuals with narrow-angle glaucoma.

Cardiovascular Effects: Antimuscarinics increase heart rate, resulting in tachycardia. Low doses may paradoxically cause bradycardia. However, they have minimal impact on blood pressure, as cholinergic impulses do not regulate vascular tone. Nevertheless, tachycardia can indirectly elevate blood pressure.

Central Nervous System Effects: Antimuscarinics have excitatory effects on the central nervous system. Higher doses can cause hallucinations and agitation. They help prevent motion sickness, suppress rigidity and tremors in Parkinson's disease, and inhibit sweating, leading to dry and warm skin. They also possess mild anesthetic properties. Tertiary agents have more pronounced central effects as they can cross the blood-brain barrier.

Antimuscarinic drugs can have side effects that vary with the dose. These may include dry mouth, difficulty swallowing, flushing, fever, impaired gastric emptying, and heart palpitations. Higher doses can result in excitement, rapid pulse, hallucinations, psychotic behavior, cardiovascular collapse, convulsions, and coma.

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Cholinergic Antagonists

Antimuscarinic Drugs

Muscarinic Receptors

Gastrointestinal Effects

Smooth Muscle Relaxation

Cardiovascular Effects

Central Nervous System

Pharmacological Actions

Drug Side Effects