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Related Concept Videos

Indirect-Acting Cholinergic Agonists: Pharmacological Actions01:30

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Indirect-acting cholinergic agonists, also known as anticholinesterases, exert their pharmacological effects by enhancing cholinergic transmission in various body parts, including the neuromuscular junction, autonomic cholinergic synapses, and the brain.
At the neuromuscular junction, these agents work by inhibiting the breakdown of acetylcholine, allowing it to remain bound to the receptor and bind to nearby receptors. This process leads to repetitive firing of the endplate, causing muscle...
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Cholinergic Antagonists: Pharmacological Actions01:28

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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...
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Cholinergic Antagonists: Therapeutic Uses01:26

Cholinergic Antagonists: Therapeutic Uses

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Antimuscarinic drugs have various therapeutic applications by inhibiting parasympathetic stimulation in different systems. Here are the key therapeutic uses of antimuscarinics:    
Respiratory Tract: Ipratropium, aclidinium, and tiotropium treat asthma, chronic bronchitis, and chronic obstructive pulmonary disease (COPD). They protect against bronchoconstriction caused by irritants like cigarette smoke, sulfur dioxide, and ozone. They also help reduce nasopharyngeal...
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Antipsychotic Drugs: Therapeutic Uses and Side Effects01:21

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Antipsychotic drugs primarily block dopamine and serotonin receptors and cholinergic, adrenergic, and histaminergic receptors, thereby reducing hallucinations and delusions in conditions like schizophrenia. However, they can trigger unwanted extrapyramidal effects such as dystonias, Parkinson-like symptoms, and tardive dyskinesia.
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Sedatives and Hypnotics Drugs: Miscellaneous Agents01:17

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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...
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Upper Respiratory Drugs: First and Second-Generation Antihistamines01:15

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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.
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Polygraphic Recording Procedure for Measuring Sleep in Mice
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Performance effects of antihistamines.

E O Meltzer1

  • 1Division of Allergy and Immunology, University of California, San Diego.

The Journal of Allergy and Clinical Immunology
|October 1, 1990
PubMed
Summary

First-generation antihistamines cause sedation and impair performance due to central nervous system effects. Newer second-generation antihistamines are less likely to cause drowsiness or affect driving ability.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Clinical Medicine

Background:

  • Antihistamines are widely used, with significant market spending.
  • First-generation antihistamines cross the blood-brain barrier, causing central nervous system effects like sedation.
  • Sedation affects 10-25% of users and is linked to receptor blockade.

Purpose of the Study:

  • To compare the central nervous system effects of first-generation and second-generation antihistamines.
  • To evaluate the impact of antihistamines on psychomotor performance and driving.
  • To examine antihistamine interactions with alcohol and tranquilizers.

Main Methods:

  • Review of studies on antihistamine effects on psychomotor reflexes and driving.
  • Analysis of methodologies used to assess antihistamine-induced drowsiness.

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  • Examination of drug interaction studies involving antihistamines, alcohol, and tranquilizers.

    • Main Results:

    • First-generation antihistamines cause significant performance decrements.
    • Second-generation antihistamines, due to their molecular properties, have limited brain penetration and reduced sedative effects.
    • Sedation is a common side effect of older antihistamines, unlike newer agents.

    Conclusions:

    • First-generation antihistamines pose a greater risk for sedation and impaired performance compared to second-generation agents.
    • Second-generation antihistamines offer a safer alternative for individuals requiring antihistamines without cognitive impairment.
    • Understanding antihistamine pharmacology is crucial for patient safety and effective treatment.