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Related Concept Videos

Cholinergic Antagonists: Pharmacokinetics01:24

Cholinergic Antagonists: Pharmacokinetics

Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations,  while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and the conjunctiva.
Cholinergic Antagonists: Pharmacological Actions01:28

Cholinergic Antagonists: Pharmacological Actions

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...
Antipsychotic Drugs: Typical and Atypical Agents01:21

Antipsychotic Drugs: Typical and Atypical Agents

Antipsychotic drugs are classified into first-generation (typical) drugs including phenothiazines; and second-generation (atypical) drugs. Chlorpromazine hydrochloride (Thorazine), a phenothiazine derivative, broadly impacts the central, autonomic, and endocrine systems. This drug, along with typical agents like haloperidol (Haldol), primarily works by antagonizing D2 receptors, thus reducing dopaminergic neurotransmission. However, typical antipsychotics can cause side effects such as sedation...
Sedatives and Hypnotics Drugs: Miscellaneous Agents01:17

Sedatives and Hypnotics Drugs: Miscellaneous Agents

Sedatives and hypnotics encompass a wide range of substances, each with its unique mechanism of action, uses, and potential adverse effects.
Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...
Upper Respiratory Drugs: First and Second-Generation Antihistamines01:15

Upper Respiratory Drugs: First and Second-Generation Antihistamines

Antihistamines are a class of drugs widely used to alleviate the symptoms of allergies, such as sneezing, itching, and nasal congestion. They work by inhibiting the actions of histamine, which is released by immune cells in response to allergenic substances or tissue injuries.
Histamine binds to specific receptor sites, known as H1 receptors, on tissue cells, triggering inflammation and swelling. Antihistamines combat these effects by competing with histamine for these receptor sites. By...
Acid Suppressive Drugs for Peptic Ulcer Disease: Histamine H2-Receptor Antagonists01:28

Acid Suppressive Drugs for Peptic Ulcer Disease: Histamine H2-Receptor Antagonists

Histamine H2 receptors, which are intricately located on the basolateral membrane of parietal cells, play a crucial role in modulating gastric acid secretion. When released from enterochromaffin-like cells, histamine engages H2 receptors, initiating the cyclic AMP (cAMP) pathway. In this pathway, adenylyl cyclase converts ATP into cAMP, elevating intracellular cAMP levels. The activation of protein kinase A follows, stimulating the proton pump. This stimulation prompts the secretion of hydrogen...

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Drug-induced Sensitization of Adenylyl Cyclase: Assay Streamlining and Miniaturization for Small Molecule and siRNA Screening Applications
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Published on: January 27, 2014

New insights into the second generation antihistamines.

G M Walsh1, L Annunziato, N Frossard

  • 1Department of Medicine and Therapeutics, University of Aberdeen Medical School, Scotland. g.m.walsh@abdn.ac.uk

Drugs
|March 29, 2001
PubMed
Summary

Second generation antihistamines vary significantly in safety and efficacy, despite appearing similar. Careful consideration of individual drug profiles is crucial for optimal allergy treatment and to avoid potential adverse effects like cardiotoxicity and somnolence.

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Area of Science:

  • Pharmacology
  • Allergy and Immunology
  • Drug Safety

Background:

  • Second-generation antihistamines are widely used for allergy treatment.
  • They are generally considered safe and effective, with a favorable therapeutic index.
  • However, their classification as a homogeneous group may be misleading.

Purpose of the Study:

  • To highlight the heterogeneity among second-generation antihistamines.
  • To discuss the varying safety profiles, including cardiotoxicity and drug interactions.
  • To explore potential anti-inflammatory effects and adjunct use in asthma therapy.

Main Methods:

  • Review of existing literature on second-generation antihistamines.
  • Comparative analysis of chemical structures, pharmacokinetics, and pharmacodynamics.
  • Evaluation of reported adverse effects and clinical trial data.

Main Results:

  • Significant differences exist in chemical structure, metabolism, and tissue distribution.
  • Some agents possess cardiotoxic potential or risk of drug interactions.
  • Variability in anti-inflammatory properties and potential for somnolence is observed.

Conclusions:

  • The current broad classification of second-generation antihistamines obscures important differences.
  • A more refined classification, potentially leading to a 'third generation,' is needed.
  • Future antihistamine development should prioritize low toxicity, minimal drug interactions, and lack of sedation.