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Antiasthma Drugs: Methylxanthines01:24

Antiasthma Drugs: Methylxanthines

Theophylline, a member of the methylxanthine class of bronchodilators, has long been used in asthma management. While its exact mechanism of action is not fully understood, it is believed to have multiple effects on various cellular processes.
Theophylline is thought to inhibit phosphodiesterase enzymes, increasing intracellular levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). This rise in cAMP and cGMP concentrations stimulates cardiac function,...
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Antiepileptic Drugs: Glutamate Antagonists

Glutamate is a fundamental neurotransmitter in the central nervous system, playing a vital role in neuronal communication and various cognitive processes. Glutamate stands as the principal excitatory neurotransmitter in the brain. Its presence is crucial for the communication between neurons, underpinning essential processes such as synaptic transmission, neuronal excitability, and plasticity. These functions are vital for higher-order cognitive processes, including learning and memory. The...
Drugs Acting on Autonomic Ganglia: Stimulants01:23

Drugs Acting on Autonomic Ganglia: Stimulants


Ganglionic stimulants activate NM nicotinic receptors in autonomic ganglia, falling into two categories: nicotine mimetics [e.g., lobeline, dimethylpiperazine, tetramethylammonium] and muscarinic receptor agonists [e.g., muscarine, methacholine]. The first category's action is rapid and blocked by nicotinic receptor antagonists, while the second category's action is delayed and blocked by atropine-like agents. Nicotine, an alkaloid, affects the heart rate by stimulating sympathetic or...
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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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Skeletal muscle relaxants are widely used for muscle paralysis and relieving pain following any muscle injury or stiffness. However, depending on the drug type, they can have adverse effects that range from mild to severe. Usually, nondepolarizing neuromuscular blockers have minimal side effects. For example, drugs like d-tubocurarine, cisatracurium, and rocuronium cause hypotension, whereas drugs like baclofen, when stopped abruptly, can lead to the recurrence of spastic conditions.
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Updated: Jun 8, 2026

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Methylxanthines, seizures, and excitotoxicity.

Detlev Boison1

  • 1R.S. Dow Neurobiology Laboratories, Legacy Research, Portland, OR 97232, USA.

Handbook of Experimental Pharmacology
|September 23, 2010
PubMed
Summary

Methylxanthines like theophylline can trigger seizures in individuals without epilepsy and worsen them in those with epilepsy. This occurs by blocking the brain

Area of Science:

  • Neuroscience
  • Pharmacology

Background:

  • Methylxanthines, including theophylline and caffeine, are clinically used but associated with seizures.
  • Theophylline is a known risk factor for seizure exacerbation in epilepsy patients.
  • Adenosine is the brain's endogenous anticonvulsant, and its dysfunction is linked to epilepsy.

Purpose of the Study:

  • To explore the proconvulsant effects of methylxanthines.
  • To elucidate the role of adenosine antagonism in methylxanthine-induced seizures.
  • To investigate potential adenosine-independent mechanisms and the involvement of free radicals.

Main Methods:

  • Review of clinical evidence on methylxanthine use and seizures.
  • Analysis of the interaction between methylxanthines and the adenosine system.

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  • Examination of recent findings on free radical involvement and alternative seizure mechanisms.

    • Main Results:

    • Methylxanthines act as adenosine receptor antagonists, explaining their proconvulsant activity.
    • Adenosine augmentation therapies show anticonvulsant effects, while antagonists exacerbate seizures.
    • The impact of methylxanthines on seizures is dose-, timing-, and usage-dependent (acute vs. chronic).
    • Emerging evidence points to a role for free radicals in theophylline-induced seizures.

    Conclusions:

    • Methylxanthines pose a risk for seizure induction and exacerbation due to adenosine antagonism.
    • Adenosine system modulation is crucial for seizure control.
    • Further research is needed to understand theophylline-induced seizures, including potential adenosine-independent pathways and free radical involvement.