Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

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,...
Adrenergic Agonists: Mixed-Action Agents01:28

Adrenergic Agonists: Mixed-Action Agents

Mixed-action adrenergic agonists, like ephedrine and pseudoephedrine, directly and indirectly affect adrenergic receptors. These agents stimulate adrenoceptors and indirectly release stored neurotransmitters, amplifying the adrenergic response.
Ephedrine and pseudoephedrine lack a catecholamine group, making them less susceptible to degradation by metabolic enzymes. They have increased oral bioavailability and lipophilicity, resulting in a longer duration of action. Their response is reduced by...
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...
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.
Pharmacokinetics in Geriatric Patients: Effect of Age on Drug Excretion01:18

Pharmacokinetics in Geriatric Patients: Effect of Age on Drug Excretion

In geriatric patients, renal physiology undergoes significant changes, including diminished renal blood flow and a lower glomerular filtration rate (GFR), leading to alterations in medication clearance. Drugs such as aminoglycoside antibiotics, lithium, and digoxin, which rely on glomerular filtration for removal from the body, particularly impact pharmacokinetics. These drugs tend to have slower clearance rates in older adults, necessitating careful dosage considerations.Evaluation of renal...
Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

Direct-Acting Cholinergic Agonists: Pharmacokinetics

Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

FGF21 underlies a hormetic response to metabolic stress in methylmalonic acidemia.

JCI insight·2018
Same author

Defective renal autoregulation in the chronic bile duct ligation model of liver failure.

Clinical and experimental nephrology·2018
Same author

Equilibrative nucleoside transporter 1 (ENT1) regulates postischemic blood flow during acute kidney injury in mice.

The Journal of clinical investigation·2017
Same author

Angiotensin II blockade causes acute renal failure in eNOS-deficient mice.

Journal of the renin-angiotensin-aldosterone system : JRAAS·2017
Same author

Profound hypothermia after adenosine kinase inhibition in A1AR-deficient mice suggests a receptor-independent effect of intracellular adenosine.

Pflugers Archiv : European journal of physiology·2016
Same author

Bombesin-like receptor 3 regulates blood pressure and heart rate via a central sympathetic mechanism.

American journal of physiology. Heart and circulatory physiology·2016
Same journal

Endothelial Cell Phenotypic Plasticity in Atherosclerosis.

Handbook of experimental pharmacology·2026
Same journal

Endothelial Dysfunction and Neurovascular Alterations in Autism Spectrum Disorder.

Handbook of experimental pharmacology·2026
Same journal

Molecular Mechanisms of Endothelial Shear Stress Mechanotransduction in Health and Disease.

Handbook of experimental pharmacology·2026
Same journal

Microvasculature of the Pancreatic Islets of Langerhans in Health and Diabetes.

Handbook of experimental pharmacology·2026
Same journal

Mechanisms of Actions of Physiological, Pharmacological, and Toxicological Dietary Bioactive Inorganic Boron.

Handbook of experimental pharmacology·2026
Same journal

BNCT Plus Luminescence: New Paradigm for Boron-Containing Drug Design.

Handbook of experimental pharmacology·2026
See all related articles

Related Experiment Video

Updated: Jun 8, 2026

Estimation of Urinary Nanocrystals in Humans using Calcium Fluorophore Labeling and Nanoparticle Tracking Analysis
07:45

Estimation of Urinary Nanocrystals in Humans using Calcium Fluorophore Labeling and Nanoparticle Tracking Analysis

Published on: February 9, 2021

Methylxanthines and the kidney.

Hartmut Osswald1, Jürgen Schnermann

  • 1Department of Pharmacology and Toxicology, University of Tübingen, Wilhelmstrasse 56, 72074, Tübingen, Germany.

Handbook of Experimental Pharmacology
|September 23, 2010
PubMed
Summary
This summary is machine-generated.

Caffeine and theophylline, natural methylxanthines, mildly increase urine output by inhibiting kidney tubule reabsorption via adenosine A1 receptor antagonism. While effective in animal models for preventing kidney injury, human data is insufficient to confirm therapeutic efficacy.

More Related Videos

Comparative Proteomic Analysis of Whole Kidney, Medulla, and Cortical Tubules in Diabetic Pathogenesis of Kidney Injury in Mice
10:31

Comparative Proteomic Analysis of Whole Kidney, Medulla, and Cortical Tubules in Diabetic Pathogenesis of Kidney Injury in Mice

Published on: May 2, 2025

Related Experiment Videos

Last Updated: Jun 8, 2026

Estimation of Urinary Nanocrystals in Humans using Calcium Fluorophore Labeling and Nanoparticle Tracking Analysis
07:45

Estimation of Urinary Nanocrystals in Humans using Calcium Fluorophore Labeling and Nanoparticle Tracking Analysis

Published on: February 9, 2021

Comparative Proteomic Analysis of Whole Kidney, Medulla, and Cortical Tubules in Diabetic Pathogenesis of Kidney Injury in Mice
10:31

Comparative Proteomic Analysis of Whole Kidney, Medulla, and Cortical Tubules in Diabetic Pathogenesis of Kidney Injury in Mice

Published on: May 2, 2025

Area of Science:

  • Nephrology
  • Pharmacology
  • Renal Physiology

Background:

  • Theophylline was historically used as a diuretic before modern diuretics emerged.
  • Methylxanthines like caffeine and theophylline influence kidney function through various mechanisms.

Purpose of the Study:

  • To elucidate the effects of natural methylxanthines (caffeine and theophylline) on kidney function.
  • To investigate the role of adenosine A1 receptors in methylxanthine-induced diuresis and renal protection.

Main Methods:

  • Utilized adenosine receptor antagonists and gene-deleted mice (A1AR knockout) to study methylxanthine action.
  • Examined the vasodilatory effects and renin secretion stimulation by methylxanthines.
  • Reviewed experimental animal data on theophylline's efficacy in various renal impairment models.

Main Results:

  • Methylxanthines inhibit proximal tubule fluid reabsorption, primarily through adenosine A1 receptor antagonism.
  • Caffeine and theophylline act as weak renal vasodilators and stimulate renin secretion.
  • Experimental animals showed functional improvements in nephrotoxic and ischemic renal injury models with theophylline treatment.

Conclusions:

  • Methylxanthines' diuretic effect is mainly mediated by adenosine A1 receptor antagonism in the proximal tubule.
  • Theophylline demonstrates potential therapeutic benefits in experimental models of renal injury.
  • Clinical evidence is lacking to confirm the efficacy of methylxanthines in preventing human nephrotoxic or post-ischemic renal injury.