Atropine
Identification
- Summary
Atropine is a muscarinic antagonist used to treat poisoning by muscarinic agents, including organophosphates and other drugs.
- Brand Names
- Atnaa, Atropen, Busulfex, Donnatal, Duodote, Enlon-plus, Isopto Atropine, Lomotil, Minims Atropine Sulphate, Motofen, Phenohytro
- Generic Name
- Atropine
- DrugBank Accession Number
- DB00572
- Background
Atropine is an alkaloid originally synthesized from Atropa belladonna. It is a racemic mixture of d-and l-hyoscyamine, of which only l-hyoscyamine is pharmacologically active.3,8 Atropine is generally available as a sulfate salt and can be administered by intravenous, subcutaneous, intramuscular, intraosseous, endotracheal and ophthalmic methods. Oral atropine is only available in combination products.1,9 Atropine is a competitive, reversible antagonist of muscarinic receptors that blocks the effects of acetylcholine and other choline esters.1,5,6,8 It has a variety of therapeutic applications, including pupil dilation and the treatment of anticholinergic poisoning and symptomatic bradycardia in the absence of reversible causes.1 Atropine is a relatively inexpensive drug and is included in the World Health Organization List of Essential Medicines.4
- Type
- Small Molecule
- Groups
- Approved, Vet approved
- Structure
- Weight
- Average: 289.3694
Monoisotopic: 289.167793607 - Chemical Formula
- C17H23NO3
- Synonyms
- (±)-atropine
- (±)-hyoscyamine
- Atropin
- Atropina
- Atropine
- Atropinum
- dl-Hyoscyamine
- dl-tropyltropate
- Tropine tropate
- External IDs
- NSC 61810
Pharmacology
- Indication
The intravenous, intramuscular, subcutaneous, intraosseous and endotracheal use of atropine is indicated for the temporary blockade of severe or life-threatening muscarinic effects.5,8 The intramuscular use of atropine in the form of a pen injector is indicated for the treatment of poisoning by susceptible organophosphorus nerve agents having cholinesterase activity as well as organophosphorus or carbamate insecticides in adult and pediatric patients.6 The ophthalmic use of atropine is indicated for mydriasis, cycloplegia, and penalization of the healthy eye in the treatment of amblyopia.7
In combination with difenoxin or diphenoxylate (tablets for oral use), atropine is indicated as adjunctive therapy in the management of acute nonspecific diarrhea.9,11
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Amblyopia •••••••••••• •••••••••• Treatment of Atrioventricular block •••••••••••• Prophylaxis of Bradycardia ••• ••••• Treatment of Bronchial spasm •••••••••••• •••••••••• •••••••••• •••••••• Management of Crying •••••••••••• •••••••••• •••••••••• •••••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Atropine is an antimuscarinic agent that antagonizes the effects of acetylcholine.5,6,8 In small doses, atropine slows heart rate, and tachycardia develops due to paralysis of vagal control. Compared to scopolamine, atropine has a more potent and prolonged effect on the heart, intestine and bronchial muscle, but a weaker effect on the iris, ciliary body and certain secretory glands. Atropine leads to increased respiratory rate and depth of respiration, possibly due to the drug-induced bronchiolar dilatation rather than its mild effect on vagal excitation.8
At an adequate dose, atropine abolishes different types of reflex vagal cardiac slowing or asystole. Atropine can be used to prevent or abolish bradycardia or asystole induced by the injection of choline esters, anticholinesterase agents or other parasympathomimetic drugs, and cardiac arrest produced by stimulation of the vagus.8 When vagal activity is an etiologic factor, atropine may also lessen the degree of partial heart block. In clinical doses, atropine counteracts the peripheral dilatation and abrupt decrease in blood pressure produced by choline esters. However, when given by itself, atropine does not exert a striking or uniform effect on blood vessels or blood pressure.8 The use of topical atropine in the eye induces mydriasis by inhibiting the contraction of the circular pupillary sphincter muscle normally stimulated by acetylcholine. This results in the contraction of the countering radial pupillary dilator muscle and pupil dilation.7
The use of atropine may precipitate acute glaucoma and convert partial organic pyloric stenosis into complete obstruction. Atropine may also lead to complete urinary retention in patients with prostatic hypertrophy and cause the thickening of bronchial secretions and formation of viscid plugs in patients with chronic lung disease.8
- Mechanism of action
Atropine binds to and inhibits muscarinic acetylcholine receptors, competitively blocking the effects of acetylcholine and other choline esters.5,6,8 It acts as a reversible non-specific antagonist of muscarinic receptors, showing affinity for the M1, M2, M3, M4 and M5 receptor subtypes.2 Atropine antagonizes the effects of acetylcholine on tissues innervated by postganglionic cholinergic nerves, such as smooth muscle, cardiac tissue, exocrine glands and the central nervous system. Also, it acts in less innervated smooth muscle that responds to endogenous acetylcholine.3,5 The actions of atropine can be overcome by increasing the concentration of acetylcholine at receptor sites (for instance, the use of anticholinesterase agents that inhibit the hydrolysis of acetylcholine).8
Target Actions Organism AMuscarinic acetylcholine receptor M1 antagonistHumans AMuscarinic acetylcholine receptor M2 antagonistHumans AMuscarinic acetylcholine receptor M3 antagonistHumans AMuscarinic acetylcholine receptor M4 antagonistHumans AMuscarinic acetylcholine receptor M5 antagonistHumans UGlycine receptor subunit alpha-1 antagonistHumans UNeuronal acetylcholine receptor subunit alpha-4 Not Available Humans UNeuronal acetylcholine receptor subunit beta-2 Not Available Humans - Absorption
Intravenous atropine follows a non-linear pharmacokinetic model at doses between 0.5 and 4 mg.8 After intramuscular administration, atropine is rapidly absorbed. In adults given 1.67 mg of atropine intramuscularly, the Cmax was 9.6 ng/mL and the Tmax went from 3 to 60 minutes.6 In healthy subjects given 30 µL of atropine ophthalmic solution, the Cmax and Tmax were 288 pg/mL and 28 minutes, respectively.7 Atropine is well absorbed in the gastrointestinal tract and rapidly delivered to systemic circulation. When administered intramuscularly, atropine has a bioavailability of 50%.2 The AUC0-INF and Cmax of atropine are higher in females than males (15%).6
- Volume of distribution
Atropine is distributed throughout the body. Following intravenous administration, the total apparent volume of distribution of atropine ranged between 1.0 and 1.7 L/kg.3
- Protein binding
The protein binding of atropine ranges from 14% to 44%,3,5,6 and is saturable between 2 and 20 μg/mL.5
- Metabolism
Atropine is mainly metabolized by enzymatic hydrolysis in the liver.5,6,8 The major metabolites of atropine are noratropine, atropin-n-oxide, tropine, and tropic acid. The metabolism of atropine is inhibited by organophosphate pesticides.5,8
- Route of elimination
Approximately 13 to 50% of atropine is excreted unchanged in the urine.5,6,8 In healthy volunteers given intravenous atropine, 29% of tropine was excreted in urine, along with 15% of an unidentified metabolite.3
- Half-life
Following intravenous and intramuscular doses of atropine, half-life values range from approximately 2 to 4 hours.3,8 In geriatric patients (65-75 years old), intravenous atropine has a longer half-life (10 hours). Also, the half-life of atropine is slightly shorter (approximately 20 minutes) in females than in males.6
In healthy volunteers given 30 µL of atropine sulfate by topical ocular administration, the half-life of atropine was approximately 2.5 hours.7
- Clearance
Following intravenous administration, the total clearance of atropine ranged between 5.9 and 6.8 mL/min/kg.3 Exercise, before and after intramuscular administration, decreases the clearance of atropine.5
- Adverse Effects
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- Toxicity
High doses of atropine may cause palpitation, dilated pupils, difficulty swallowing, hot dry skin, thirst, dizziness, restlessness, tremor, fatigue and ataxia. Toxic doses of atropine lead to restlessness and excitement, hallucinations, delirium and coma.8 In cases of severe intoxication, atropine can cause a circulatory collapse, leading to a decline in blood pressure and respiratory failure that may ensue in death following paralysis and coma.6,8
In case of atropine overdose, supportive treatment should be administered. Provide artificial respiration with oxygen if respiration is depressed, and follow cooling methods to reduce atropine-induced fever, especially in pediatric patients. In case of urinary retention, catheterization may be required. Atropine is mainly eliminated through the kidney; therefore, urinary output must be maintained and increased if possible. In case of atropine-induced photophobia, the room should be darkened.6 A short-acting barbiturate or diazepam may be given as needed to control marked excitement and convulsions; however, large doses should be avoided since central depressant action may coincide with the depression that occurs late in atropine poisoning. Central stimulants are not recommended.8 The acute oral toxicity (LD50) of atropine in mice is 75 mg/kg.10
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcebutolol Atropine may increase the arrhythmogenic activities of Acebutolol. Aceclofenac The risk or severity of hypertension can be increased when Atropine is combined with Aceclofenac. Acemetacin The risk or severity of hypertension can be increased when Atropine is combined with Acemetacin. Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Atropine. Acetylsalicylic acid The risk or severity of hypertension can be increased when Atropine is combined with Acetylsalicylic acid. - Food Interactions
- Avoid alcohol.
- Take with food. Food reduces irritation.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Atropine hydrochloride EUF58V826B 33952-38-4 OJIPQOWZZMSBGY-RIMUKSHESA-N Atropine sulfate 03J5ZE7KA5 5908-99-6 JPKKQJKQTPNWTR-CHYDPLAESA-N Atropine sulfate anhydrous KAE4PSB0Z3 55-48-1 HOBWAPHTEJGALG-AADVZIIPSA-N - Product Images
- International/Other Brands
- Anespin (Oriental Chemical Works) / Antol (Ying Yuan) / AtroPen (Meridian) / Atropt (Sigma) / Atrospan (Fischer) / Bellapan (Farmapol) / Dysurgal (MaxMedic) / Kintropine (Synpac-Kingdom) / Tromine (The Central)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Alcon Atropine Solution 1 % w/v Ophthalmic Alcon, Inc. 1964-12-31 Not applicable Canada ATROPEN Auto-Injector Injection 2 mg/0.7mL Intramuscular Meridian Medical Technologies LLC 2003-06-19 Not applicable US ATROPEN Auto-Injector Injection 0.25 mg/0.3mL Intramuscular Meridian Medical Technologies LLC 2004-09-17 Not applicable US ATROPEN Auto-Injector Injection 1 mg/0.7mL Intramuscular Meridian Medical Technologies LLC 2003-06-19 Not applicable US ATROPEN Auto-Injector Injection 2 mg/0.7mL Intramuscular Meridian Medical Technologies LLC 1973-05-15 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Atropine Solution / drops 10 mg/1mL Ophthalmic Amneal Pharmaceuticals NY LLC 2022-07-19 Not applicable US Atropine Solution / drops 10 mg/1mL Ophthalmic A-S Medication Solutions 2021-11-26 Not applicable US Atropine Solution / drops 10 mg/1mL Ophthalmic Akorn 2022-05-02 Not applicable US Atropine Solution / drops 10 mg/1mL Ophthalmic Amneal Pharmaceuticals NY LLC 2022-07-19 Not applicable US Atropine Solution / drops 10 mg/1mL Ophthalmic Apotex Corp. 2021-11-26 Not applicable US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image ALCON ATROPINE SULFATE EYE DROPS 1% Solution 1 % Ophthalmic ALCON PTE LTD 1990-04-17 Not applicable Singapore ยูเมด้า อะโทรปิน Solution 0.5 mg/1ml บริษัท ยูเมด้า จำกัด 1999-09-21 2020-08-23 Thailand - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ATNAA atropine and pralidoxime chloride Auto-Injector Atropine (2.1 mg/0.7mL) + Pralidoxime chloride (600 mg/2mL) Kit Intramuscular Meridian Medical Technologies, LLC 2002-01-17 Not applicable US BEAMOTIL TABLETS Atropine sulfate anhydrous (0.025 mg) + Diphenoxylate hydrochloride (2.5 mg) Tablet, film coated Oral BEACONS PHARMACEUTICALS PTE. LTD. 1991-06-01 Not applicable Singapore DHAMOTIL TABLET Atropine sulfate anhydrous (0.025 mg) + Diphenoxylate hydrochloride (2.5 mg) Tablet, film coated Oral TEVA PHARMACEUTICAL INVESTMENTS SINGAPORE PTE. LTD. 1991-01-29 Not applicable Singapore Diban Cap Atropine sulfate (9.7 mcg) + Attapulgite (300 mg) + Hyoscyamine sulfate (0.0519 mg) + Opium (12 mg) + Pectin (71.4 mg) + Scopolamine (3.3 mcg) Capsule Oral Wyeth Ayerst Canada Inc. 1998-02-18 2001-01-30 Canada Diban Cap Atropine sulfate (9.7 mcg) + Attapulgite (300 mg) + Hyoscyamine sulfate (0.0519 mg) + Opium (12 mg) + Pectin (71.4 mg) + Scopolamine (3.3 mcg) Capsule Oral Ayerst Laboratories 1992-12-31 1999-04-12 Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Atropine Care Atropine sulfate anhydrous (10 mg/1mL) Solution / drops Ophthalmic Akorn, Inc 1995-06-01 2008-06-01 US Atropine Sulfate Atropine sulfate (10 mg/1g) Ointment Ophthalmic Physicians Total Care, Inc. 2012-01-27 2013-01-15 US Atropine Sulfate Atropine sulfate (0.4 mg/1mL) Injection, solution Intramuscular; Intravenous; Subcutaneous HF Acquisition Co LLC, DBA HealthFirst 2018-12-21 Not applicable US Atropine Sulfate Atropine sulfate (1 mg/1mL) Solution Ophthalmic Sandoz Inc. 2000-06-30 2015-08-25 US Atropine Sulfate Atropine sulfate (1 mg/1mL) Injection, solution Intramuscular; Intravenous; Subcutaneous Physicians Total Care, Inc. 2002-04-15 2011-06-30 US
Categories
- ATC Codes
- S01FA01 — AtropineA03CB03 — Atropine and psycholeptics
- A03CB — Belladonna and derivatives in combination with psycholeptics
- A03C — ANTISPASMODICS IN COMBINATION WITH PSYCHOLEPTICS
- A03 — DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
- A — ALIMENTARY TRACT AND METABOLISM
- Drug Categories
- Adjuvants, Anesthesia
- Agents producing tachycardia
- Agents that produce hypertension
- Alimentary Tract and Metabolism
- Alkaloids
- Anti-Asthmatic Agents
- Antiarrhythmic agents
- Anticholinergic Agents
- Antimuscarinics Antispasmodics
- Autonomic Agents
- Aza Compounds
- Azabicyclo Compounds
- Belladonna Alkaloids
- Belladonna Alkaloids, Tertiary Amines
- Belladonna and Derivatives, Plain
- Bronchodilator Agents
- BSEP/ABCB11 Substrates
- Cardiovascular Agents
- Central Nervous System Agents
- Cholinergic Agents
- Drugs for Functional Gastrointestinal Disorders
- Moderate Risk QTc-Prolonging Agents
- Muscarinic Antagonists
- Mydriatics
- Mydriatics and Cycloplegics
- Neurotransmitter Agents
- Ophthalmologicals
- Parasympatholytics
- Peripheral Nervous System Agents
- QTc Prolonging Agents
- Respiratory System Agents
- Sensory Organs
- Solanaceous Alkaloids
- Tropanes
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as tropane alkaloids. These are organic compounds containing the nitrogenous bicyclic alkaloid parent N-Methyl-8-azabicyclo[3.2.1]octane.
- Kingdom
- Organic compounds
- Super Class
- Alkaloids and derivatives
- Class
- Tropane alkaloids
- Sub Class
- Not Available
- Direct Parent
- Tropane alkaloids
- Alternative Parents
- Beta hydroxy acids and derivatives / Piperidines / N-alkylpyrrolidines / Benzene and substituted derivatives / Trialkylamines / Carboxylic acid esters / Amino acids and derivatives / Monocarboxylic acids and derivatives / Azacyclic compounds / Primary alcohols show 4 more
- Substituents
- Alcohol / Amine / Amino acid or derivatives / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Beta-hydroxy acid / Carbonyl group / Carboxylic acid derivative / Carboxylic acid ester show 18 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- racemate (CHEBI:16684) / Tropane alkaloids, Alkaloids, Tropan alkaloids (C01479)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 7C0697DR9I
- CAS number
- 51-55-8
- InChI Key
- RKUNBYITZUJHSG-SPUOUPEWSA-N
- InChI
- InChI=1S/C17H23NO3/c1-18-13-7-8-14(18)10-15(9-13)21-17(20)16(11-19)12-5-3-2-4-6-12/h2-6,13-16,19H,7-11H2,1H3/t13-,14+,15+,16?
- IUPAC Name
- (1R,3S,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl 3-hydroxy-2-phenylpropanoate
- SMILES
- CN1[C@H]2CC[C@@H]1C[C@@H](C2)OC(=O)C(CO)C1=CC=CC=C1
References
- Synthesis Reference
Pei-Chang Wu, Hsi-Kung Kuo, Po-Chiung Fang, Jong-Jer Lee, Chih-Hsin Chen, "Low-concentration atropine solution for preventing myopia progression and preparing method thereof." U.S. Patent US20070254914, issued November 01, 2007.
US20070254914- General References
- McLendon K, Preuss CV: Atropine . [Article]
- Buels KS, Fryer AD: Muscarinic receptor antagonists: effects on pulmonary function. Handb Exp Pharmacol. 2012;(208):317-41. doi: 10.1007/978-3-642-23274-9_14. [Article]
- Kanto J, Klotz U: Pharmacokinetic implications for the clinical use of atropine, scopolamine and glycopyrrolate. Acta Anaesthesiol Scand. 1988 Feb;32(2):69-78. doi: 10.1111/j.1399-6576.1988.tb02691.x. [Article]
- Smulyan H: The Beat Goes On: The Story of Five Ageless Cardiac Drugs. Am J Med Sci. 2018 Nov;356(5):441-450. doi: 10.1016/j.amjms.2018.04.011. Epub 2018 Apr 25. [Article]
- FDA Approved Drug Products: Atropine sulfate injection for intravenous use [Link]
- FDA Approved Drug Products: ATROPEN (atropine) injection for intramuscular use [Link]
- FDA Approved Drug Products: ISOPTO ATROPINE (atropine sulfate) ophthalmic solution for topical ophthalmic use [Link]
- FDA Approved Drug Products: Atropine sulfate injection, for intravenous, intramuscular, subcutaneous, intraosseous or endotracheal use. [Link]
- FDA Approved Drug Products: MOTOFEN (difenoxin and atropine sulphate) tablets for oral use [Link]
- Cayman chemical: Atropine SDS [Link]
- FDA Approved Drug Products: LOMOTIL (diphenoxylate hydrochloride and atropine sulfate) tablets for oral use [Link]
- External Links
- Human Metabolome Database
- HMDB0014712
- KEGG Drug
- D00113
- KEGG Compound
- C01479
- PubChem Compound
- 174174
- PubChem Substance
- 46507540
- ChemSpider
- 10194105
- BindingDB
- 50403547
- 1223
- ChEBI
- 78734
- ChEMBL
- CHEMBL517712
- Therapeutic Targets Database
- DAP000377
- PharmGKB
- PA448505
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- OIN
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Atropine
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Basic Science Myopia (Disorder) 1 4 Completed Diagnostic Intraocular Pressure Changes During Tracheal Extubation 1 4 Completed Other Arrhythmia / Bradycardia 1 4 Completed Prevention Alzheimer's Disease (AD) / Delirium, Dementia, Amnestic, Cognitive Disorders / Mild Cognitive Impairment (MCI) 1 4 Completed Prevention Arrhythmia / Respiratory Arrest (Disorder) 1
Pharmacoeconomics
- Manufacturers
- Meridian medical technologies inc
- Solvay pharmaceuticals
- United states army office surgeon general
- Hospira inc
- Mission pharmacal co
- Packagers
- Advanced Pharmaceutical Services Inc.
- Akorn Inc.
- Alcon Laboratories
- American Regent
- Amphastar Pharmaceuticals
- APP Pharmaceuticals
- A-S Medication Solutions LLC
- Baroli
- Bausch & Lomb Inc.
- Baxter International Inc.
- Bioniche Pharma
- Cardinal Health
- Carlisle Laboratories Inc.
- Clipper Distributing Co. LLC
- Contract Pharm
- Dispensing Solutions
- E. Fougera and Co.
- Falcon Pharmaceuticals Ltd.
- General Injectables and Vaccines Inc.
- Hawthorn Pharmaceuticals
- Hope Pharmaceuticals
- Hospira Inc.
- Luitpold Pharmaceuticals Inc.
- Mallinckrodt Inc.
- Mckesson Corp.
- Meridian Medical Technologies Inc.
- MWI Veterinary Supply Co.
- Nycomed Inc.
- Ocumed Inc.
- OMJ Pharmaceuticals
- PD-Rx Pharmaceuticals Inc.
- Pharmedium
- Physicians Total Care Inc.
- Prometic Pharma Inc.
- Rx Veterinary Products
- Spectrum Pharmaceuticals
- Teva Pharmaceutical Industries Ltd.
- Vedco Inc.
- Wa Butler Co.
- Dosage Forms
Form Route Strength Injection Intramuscular; Intravenous; Subcutaneous Solution Ophthalmic 0.100 mg Solution Intravenous 1.00 mg Kit Intramuscular Injection Intramuscular 0.25 mg/0.3mL Injection, solution Parenteral 0.1 mg/ml Solution Intramuscular; Intravenous; Subcutaneous 0.5 mg Solution Intramuscular; Intravenous; Subcutaneous 0.5 mg/ml Solution Intramuscular; Intravenous; Subcutaneous 0.25 mg Solution Intramuscular; Intravenous; Subcutaneous 0.25 mg/1ml Solution Intramuscular; Intravenous; Subcutaneous 0.5 mg/1ml Solution Intramuscular; Intravenous; Subcutaneous 1 mg Solution Intramuscular; Intravenous; Subcutaneous 1 mg/1ml Injection, solution 0.25 mg/1ml Injection, solution 0.5 mg/1ml Solution Intramuscular; Intravenous; Subcutaneous 0.25 mg/ml Solution Parenteral 1 mg Solution Conjunctival; Ophthalmic 10 mg Injection, solution Intravenous 0.5 % Injection, solution Intravenous 1 % Ointment Ophthalmic 0.5 g/100ml Ointment Ophthalmic 0.5 % Ointment Ophthalmic 1 g/100ml Solution / drops Ophthalmic 10 MG/ML Solution / drops Ophthalmic 5 MG/ML Injection, solution 0.5 MG/ML Injection, solution 1 MG/ML Solution Ophthalmic Tablet 0250 MG Injection, solution 0.1 MG/ML Injection, solution Injection, solution Parenteral 0.21 MG/ML Injection, solution Parenteral 0.5 MG/ML Injection, solution Parenteral 1 MG/ML Solution Intravenous; Subcutaneous 1 mg Solution Intravenous 1 mg Solution Intramuscular; Subcutaneous 1 mg Solution Intramuscular; Intravenous; Subcutaneous 100000 mg Solution Ophthalmic 1 % Tablet Solution / drops Ophthalmic 1 % Solution / drops Ophthalmic 10 mg/1mL Solution Intramuscular; Intravenous; Subcutaneous 0.4 mg / mL Injection Intramuscular; Intravenous; Subcutaneous 600 mcg/ml Ointment Ophthalmic 1 % Solution Intramuscular; Intravenous; Subcutaneous 1 mg/ml Injection Injection Endotracheal; Intramedullary; Intramuscular; Intravenous; Subcutaneous 0.4 mg/1mL Injection Intramuscular; Intravenous; Subcutaneous 0.4 mg/1mL Injection Intravenous 0.05 mg/1mL Injection Intravenous 0.1 mg/1mL Injection Intravenous; Parenteral 0.1 mg/1mL Injection Parenteral 0.1 mg/1mL Injection, solution Endotracheal; Intramedullary; Intramuscular; Intravenous; Subcutaneous 0.4 mg/1mL Injection, solution Endotracheal; Intramuscular; Intravenous; Subcutaneous 0.05 mg/1mL Injection, solution Endotracheal; Intramuscular; Intravenous; Subcutaneous 0.1 mg/1mL Injection, solution Intramuscular 0.1 mg/1mL Injection, solution Intramuscular; Intravenous; Subcutaneous 0.1 mg/1mL Injection, solution Intramuscular; Intravenous; Subcutaneous 0.4 mg/1mL Injection, solution Intramuscular; Intravenous; Subcutaneous 0.4 mg/0.5mL Injection, solution Intramuscular; Intravenous; Subcutaneous 1 mg/1mL Injection, solution Intravenous 0.05 mg/1mL Injection, solution Intravenous 0.1 mg/1mL Injection, solution Intravenous 0.4 mg/1mL Injection, solution Intravenous 1 mg/1mL Ointment Ophthalmic 10 mg/1g Solution Ophthalmic 1 mg/1mL Liquid Intravenous .1 mg / mL Solution Intramuscular; Intravenous; Subcutaneous 0.3 mg / mL Solution Intramuscular; Intravenous; Subcutaneous 0.8 mg / mL Solution Intramuscular; Intravenous; Subcutaneous 0.6 mg / mL Solution Intramuscular; Intravenous; Subcutaneous 1 mg / mL Solution Intramuscular; Intravenous; Subcutaneous 0.5 mg / 5 mL Solution Intramuscular; Intravenous; Subcutaneous 1 mg / 5 mL Solution Intramuscular; Intravenous; Subcutaneous 3 mg / 10 mL Solution Intramuscular; Intravenous; Subcutaneous .6 mg / mL Solution Intramuscular; Intravenous; Subcutaneous 1 mg / 10 mL Solution 0.6 mg/1ml Injection Intramuscular; Intravenous; Subcutaneous 0.6 mg/ml Injection Parenteral Injection Parenteral 1 mg/ml Injection, solution 0.2 mg/ml Solution Parenteral 0.50 mg Solution / drops Ophthalmic 10 mg / mL Solution Ophthalmic 0.5 % Solution Ophthalmic 10.0 mg/ml Tablet, film coated Oral 0.025 mg Solution Intravenous 1.000 mg Solution / drops Ophthalmic Tablet, film coated Oral Capsule Oral Solution Oral Tablet Oral Tablet, extended release Oral Tablet, film coated, extended release Oral Injection, solution 1 mg/1ml Injection 0.5 mg/ml Injection 0.25 mg/ml Injection, solution Intravenous Injection Intravenous Solution Ophthalmic 10 mg/1mL Ointment Ophthalmic Liquid Oral Tablet Oral 0.025 mg Injection, solution Intramuscular; Intravenous; Subcutaneous 600 mcg/ml Solution / drops Ophthalmic 0.5 % Solution Ophthalmic 1 % w/v Solution / drops Ophthalmic 1 % w/v Solution / drops Ophthalmic 0.025 % W/V Injection Intramuscular 0.5 mg/0.7mL Injection Intramuscular 1 mg/0.7mL Injection Intramuscular 2 mg/0.7mL Solution / drops Ophthalmic Injection Intramuscular; Intravenous; Subcutaneous 1 mg/ml Elixir Oral Liquid Ophthalmic 1 % Syrup Oral 0.025 mg/5ml Solution Parenteral 1.0 mg Injection, solution Intramuscular; Intravenous; Subcutaneous 0.25 mg/ml Injection, solution Intramuscular; Intravenous; Subcutaneous Injection, solution Intramuscular; Intravenous; Subcutaneous 0.5 mg/ml Injection, solution Intramuscular; Intravenous; Subcutaneous 1 mg/ml Tablet Solution 0.5 mg/1ml Solution 1 mg/1ml Tablet 0.6 mg Solution Suspension - Prices
Unit description Cost Unit Atropine Sulfate 1% Solution 15ml Bottle 101.27USD bottle Isopto Atropine 1% Solution 15ml Bottle 34.65USD bottle Atropine powder 34.48USD g Isopto Atropine 1% Solution 5ml Bottle 26.59USD bottle Atropine Sulfate 1% Solution 5ml Bottle 16.82USD bottle Atropine Sulfate 1% Ointment 3.5 gm Tube 15.92USD tube Atropine-Care 1% Solution 2ml Bottle 7.99USD bottle Isopto atropine 1% eye drops 5.06USD ml Atropine-ns 1 mg/2.5 ml syr 4.8USD ml Atropine-ns 0.8 mg/2 ml syr 3.9USD ml Atropine 1% eye drops 2.88USD ml Atropine sulfate powder 2.06USD g Atropine care 1% eye drops 2.03USD ml Atropine-ns 2 mg/5 ml syringe 1.92USD ml Atropine Sulfate 0.4 mg/ml 1.6USD ml Atropine Sulfate 0.6 mg/ml 1.6USD ml Atropine 1 mg/ml vial 1.44USD ml Atropine Sulfate 0.4 mg/ml Solution 1.22USD ml Atropine 0.4 mg/0.5 ml ampul 1.2USD ampul Atropine 1 mg/ml ampul 1.2USD ml Atropine 0.4 mg/ml vial 0.96USD ml Isopto Atropine 1 % Solution 0.68USD ml Sal-tropine 0.4 mg tablet 0.36USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 118.5 °C Pharmacology in Clinical Neurosciences: A Quick Guide. (2020). Germany: Springer Singapore. water solubility 2200 mg/L (at 25 °C) DEHN,WM (1917) logP 1.83 HANSCH,C ET AL. (1995) logS -2.12 ADME Research, USCD pKa 9.43 SANGSTER (1994) - Predicted Properties
Property Value Source Water Solubility 2.52 mg/mL ALOGPS logP 2.19 ALOGPS logP 1.57 Chemaxon logS -2.1 ALOGPS pKa (Strongest Acidic) 15.15 Chemaxon pKa (Strongest Basic) 9.39 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 49.77 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 80.82 m3·mol-1 Chemaxon Polarizability 31.28 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9286 Blood Brain Barrier + 0.9569 Caco-2 permeable + 0.8866 P-glycoprotein substrate Substrate 0.5 P-glycoprotein inhibitor I Non-inhibitor 0.6542 P-glycoprotein inhibitor II Non-inhibitor 0.8595 Renal organic cation transporter Inhibitor 0.7956 CYP450 2C9 substrate Non-substrate 0.7041 CYP450 2D6 substrate Non-substrate 0.6838 CYP450 3A4 substrate Substrate 0.5496 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9275 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9285 CYP450 3A4 inhibitor Non-inhibitor 0.95 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9113 Ames test Non AMES toxic 0.7742 Carcinogenicity Non-carcinogens 0.9631 Biodegradation Ready biodegradable 0.5527 Rat acute toxicity 2.7305 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8354 hERG inhibition (predictor II) Inhibitor 0.5378
Spectra
- Mass Spec (NIST)
- Download (7.92 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 176.055658 predictedDarkChem Lite v0.1.0 [M-H]- 181.234558 predictedDarkChem Lite v0.1.0 [M-H]- 169.36101 predictedDeepCCS 1.0 (2019) [M+H]+ 176.451658 predictedDarkChem Lite v0.1.0 [M+H]+ 181.485258 predictedDarkChem Lite v0.1.0 [M+H]+ 171.71901 predictedDeepCCS 1.0 (2019) [M+Na]+ 175.948158 predictedDarkChem Lite v0.1.0 [M+Na]+ 181.051258 predictedDarkChem Lite v0.1.0 [M+Na]+ 178.38545 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM1
- Uniprot ID
- P11229
- Uniprot Name
- Muscarinic acetylcholine receptor M1
- Molecular Weight
- 51420.375 Da
References
- Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [Article]
- Buels KS, Fryer AD: Muscarinic receptor antagonists: effects on pulmonary function. Handb Exp Pharmacol. 2012;(208):317-41. doi: 10.1007/978-3-642-23274-9_14. [Article]
- Wall SJ, Yasuda RP, Li M, Ciesla W, Wolfe BB: Differential regulation of subtypes m1-m5 of muscarinic receptors in forebrain by chronic atropine administration. J Pharmacol Exp Ther. 1992 Aug;262(2):584-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- G-protein coupled acetylcholine receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM2
- Uniprot ID
- P08172
- Uniprot Name
- Muscarinic acetylcholine receptor M2
- Molecular Weight
- 51714.605 Da
References
- Roman S, Badia A, Camps P, Munoz-Torrero D, Clos MV: Nicotinic-receptor potentiator drugs, huprine X and galantamine, increase ACh release by blocking AChE activity but not acting on nicotinic receptors. Brain Res. 2005 Nov 9;1061(2):73-9. Epub 2005 Oct 24. [Article]
- Minaba M, Ichiyama S, Kojima K, Ozaki M, Kato Y: Activation of nematode G protein GOA-1 by the human muscarinic acetylcholine receptor M2 subtype. Functional coupling of G-protein-coupled receptor and G protein originated from evolutionarily distant animals. FEBS J. 2006 Dec;273(24):5508-16. Epub 2006 Nov 3. [Article]
- May LT, Lin Y, Sexton PM, Christopoulos A: Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators. J Pharmacol Exp Ther. 2005 Jan;312(1):382-90. Epub 2004 Aug 27. [Article]
- Cembala TM, Forde SC, Appadu BL, Lambert DG: Allosteric interaction of the neuromuscular blockers vecuronium and pancuronium with recombinant human muscarinic M2 receptors. Eur J Pharmacol. 2007 Aug 13;569(1-2):37-40. Epub 2007 May 22. [Article]
- Nelson CP, Nahorski SR, Challiss RA: Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor. J Pharmacol Exp Ther. 2006 Jan;316(1):279-88. Epub 2005 Sep 27. [Article]
- Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [Article]
- Buels KS, Fryer AD: Muscarinic receptor antagonists: effects on pulmonary function. Handb Exp Pharmacol. 2012;(208):317-41. doi: 10.1007/978-3-642-23274-9_14. [Article]
- Wall SJ, Yasuda RP, Li M, Ciesla W, Wolfe BB: Differential regulation of subtypes m1-m5 of muscarinic receptors in forebrain by chronic atropine administration. J Pharmacol Exp Ther. 1992 Aug;262(2):584-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM3
- Uniprot ID
- P20309
- Uniprot Name
- Muscarinic acetylcholine receptor M3
- Molecular Weight
- 66127.445 Da
References
- Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [Article]
- Buels KS, Fryer AD: Muscarinic receptor antagonists: effects on pulmonary function. Handb Exp Pharmacol. 2012;(208):317-41. doi: 10.1007/978-3-642-23274-9_14. [Article]
- Wall SJ, Yasuda RP, Li M, Ciesla W, Wolfe BB: Differential regulation of subtypes m1-m5 of muscarinic receptors in forebrain by chronic atropine administration. J Pharmacol Exp Ther. 1992 Aug;262(2):584-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Guanyl-nucleotide exchange factor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM4
- Uniprot ID
- P08173
- Uniprot Name
- Muscarinic acetylcholine receptor M4
- Molecular Weight
- 53048.65 Da
References
- Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [Article]
- Buels KS, Fryer AD: Muscarinic receptor antagonists: effects on pulmonary function. Handb Exp Pharmacol. 2012;(208):317-41. doi: 10.1007/978-3-642-23274-9_14. [Article]
- Wall SJ, Yasuda RP, Li M, Ciesla W, Wolfe BB: Differential regulation of subtypes m1-m5 of muscarinic receptors in forebrain by chronic atropine administration. J Pharmacol Exp Ther. 1992 Aug;262(2):584-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM5
- Uniprot ID
- P08912
- Uniprot Name
- Muscarinic acetylcholine receptor M5
- Molecular Weight
- 60073.205 Da
References
- Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [Article]
- Buels KS, Fryer AD: Muscarinic receptor antagonists: effects on pulmonary function. Handb Exp Pharmacol. 2012;(208):317-41. doi: 10.1007/978-3-642-23274-9_14. [Article]
- Wall SJ, Yasuda RP, Li M, Ciesla W, Wolfe BB: Differential regulation of subtypes m1-m5 of muscarinic receptors in forebrain by chronic atropine administration. J Pharmacol Exp Ther. 1992 Aug;262(2):584-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- Curator comments
- Atropine is a weak antagonist of glycine receptor subunit alpha-1
- General Function
- Transmitter-gated ion channel activity
- Specific Function
- The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
- Gene Name
- GLRA1
- Uniprot ID
- P23415
- Uniprot Name
- Glycine receptor subunit alpha-1
- Molecular Weight
- 52623.35 Da
References
- Jensen AA, Kristiansen U: Functional characterisation of the human alpha1 glycine receptor in a fluorescence-based membrane potential assay. Biochem Pharmacol. 2004 May 1;67(9):1789-99. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Ligand-gated ion channel activity
- Specific Function
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeabl...
- Gene Name
- CHRNA4
- Uniprot ID
- P43681
- Uniprot Name
- Neuronal acetylcholine receptor subunit alpha-4
- Molecular Weight
- 69956.47 Da
References
- Smulders CJ, Zwart R, Bermudez I, van Kleef RG, Groot-Kormelink PJ, Vijverberg HP: Cholinergic drugs potentiate human nicotinic alpha4beta2 acetylcholine receptors by a competitive mechanism. Eur J Pharmacol. 2005 Feb 21;509(2-3):97-108. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Ligand-gated ion channel activity
- Specific Function
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeabl...
- Gene Name
- CHRNB2
- Uniprot ID
- P17787
- Uniprot Name
- Neuronal acetylcholine receptor subunit beta-2
- Molecular Weight
- 57018.575 Da
References
- Smulders CJ, Zwart R, Bermudez I, van Kleef RG, Groot-Kormelink PJ, Vijverberg HP: Cholinergic drugs potentiate human nicotinic alpha4beta2 acetylcholine receptors by a competitive mechanism. Eur J Pharmacol. 2005 Feb 21;509(2-3):97-108. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
- Gene Name
- ORM1
- Uniprot ID
- P02763
- Uniprot Name
- Alpha-1-acid glycoprotein 1
- Molecular Weight
- 23511.38 Da
References
- FDA Approved Drug Products: Atropine sulfate injection for subcutaneous, intramuscular or intravenous use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54