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Muscarinic antagonists antimuscarinic

Dicyclomine (Bentyl), oxybutynin (Ditropan), and tolterodine (Detrol) are nonselective smooth muscle re-laxants that produce relatively little antagonism of muscarinic receptors at therapeutic concentrations. The mechanism of relaxation is not known. Finally, some other classes of drugs can act in part as muscarinic antagonists. For example, the antipsychotics and antidepressants produce antimuscarinic side effects (e.g., dry mouth). [Pg.135]

Muscarinic antagonists have numerous effects on the digestive system (see Chapter 40). The inhibition of salivation by low doses of atropine results in a dry mouth and difficulty in swallowing. Antimuscarinic... [Pg.135]

Answer Antimuscarinics are not frequently used for peptic ulcer disease today because of their many side effects, but they stiU can play a useful role as adjunctive therapy. Unfortunately, high concentrations are required to block gastric acid secretion, which means that many side effects are difficult to avoid. This man works in a dangerous environment, and his concentration cannot be compromised. Although CNS depression and loss of concentration is a concern with tertiary amine muscarinic antagonists, quaternary ammonium muscarinic antagonists... [Pg.140]

Muscarinic antagonists are sometimes called parasympatholytic because they block the effects of parasympathetic autonomic discharge. However, they do not "lyse" parasympathetic nerves, and they have some effects that are not predictable from block of the parasympathetic nervous system. For these reasons, the term "antimuscarinic" is preferable. [Pg.152]

Oxybutynin Nonselective muscarinic antagonist Reduces detrusor smooth muscle tone, spasms Urge incontinence postoperative spasms Oral, IV, patch formulations Toxicity Tachycardia, constipation, increased intraocular pressure, xerostomia Patch Pruritus Interactions With other antimuscarinics... [Pg.167]

The antimuscarinic drug atropine, and its derivative ipratropiumbromide, can also be used for antiarrhyth-mic treatment. Muscarinic receptors (M2 subtype) are mainly present in supraventricular tissue and in the AV node. They inhibit adenylylcyclase via G proteins and thereby reduce intracellular cAMP. On the other hand, activation of the M2 receptor leads to opening of hyperpolarizing Ik.acii and inhibits the pacemaker current If probably via the (3y-subunit of the Gi protein associated with this receptor. The results are hyperpolarization and slower spontaneous depolarization. Muscarinic receptor antagonists like atropine lead to increased heart rate and accelerated atrioventricular conduction. There are no or only slight effects on the ventricular electrophysiology. [Pg.101]

Atropine Nonselective competitive antagonist at all muscarinic receptors in CNS and periphery Blocks muscarinic excess at exocrine glands, heart, smooth muscle Mandatory antidote for severe cholinesterase inhibitor poisoning Intravenous infusion until antimuscarinic signs appear continue as long as necessary Toxicity Insignificant as long as AChE inhibition continues... [Pg.167]


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Antimuscarinics

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Muscarines

Muscarinic

Muscarinic antagonists

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