Atropine: Difference between revisions

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Administer supportive and symptomatic therapy as indicated.
Administer supportive and symptomatic therapy as indicated.
Physostigmine 1 to 3 mg I.V. has been utilized to reverse anticholinergic effects. However, profound bradycardia, asystole and seizures may occur. The role of physostigmine is not clear; its use should be avoided if other therapeutic agents are successful in reversing cardiac dysrhythmias. Neostigmine methylsulfate 0.5 to 2 mg I.V., repeated as needed, may be given. Diazepam or short-acting barbiturates may control excitement. Hemodialysis is ineffective for atropine poisoning. Hyperpyrexia may be treated with physical cooling measures. If photophobia occurs, the patient may be kept in a dark room.
Physostigmine 1 to 3 mg I.V. has been utilized to reverse anticholinergic effects. However, profound bradycardia, asystole and seizures may occur. The role of physostigmine is not clear; its use should be avoided if other therapeutic agents are successful in reversing cardiac dysrhythmias. Neostigmine methylsulfate 0.5 to 2 mg I.V., repeated as needed, may be given. Diazepam or short-acting barbiturates may control excitement. Hemodialysis is ineffective for atropine poisoning. Hyperpyrexia may be treated with physical cooling measures. If photophobia occurs, the patient may be kept in a dark room.
|drugBox=<!--Mechanism of Action-->
|drugBox={{Drugbox2
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 458781584
| IUPAC_name = (''RS'')-(8-Methyl-8-azabicyclo[3.2.1]oct-3-yl) 3-hydroxy-2-phenylpropanoate
| image = Atropine.png
| image2 = Atropine-D-and-L-isomers-from-DL-xtal-2004-3D-balls.png
| width2 = 260
 
<!--Clinical data-->
| tradename = Atropen
| Alternate names = Daturin <ref>{{cite book|url=http://books.google.com/?id=amgVAAAAYAAJ&pg=PA148&lpg=PA148&dq=daturin#v=onepage&q=daturin&f=false |title=Medical Flora; Or, Manual of the Medical Botany of the United States of ... - Constantine Samuel Rafinesque - Google Books |publisher=Books.google.com |accessdate=2012-11-07|year=1828}}</ref>
| Drugs.com = {{drugs.com|monograph|atropine}}
| MedlinePlus = a682487
| pregnancy_AU = A
| pregnancy_US = C
| legal_status = Rx-only
| routes_of_administration = Oral, [[Intravenous therapy|IV]], [[Intramuscular injection|IM]], rectal
 
<!--Pharmacokinetic data-->
| bioavailability = 25%
| metabolism = 50% [[hydrolyse]]d to [[tropine]] and [[tropic acid]]
| elimination_half-life = 2 hours
| excretion = 50% excreted unchanged in urine
 
<!--Identifiers-->
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 51-55-8
| ATC_prefix = A03
| ATC_suffix = BA01
| ATC_supplemental = {{ATC|S01|FA01}}
| PubChem = 174174
| IUPHAR_ligand = 320
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00572
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 10194105
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 7C0697DR9I
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D00113
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 16684
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 9751
 
<!--Chemical data-->
| C=17 | H=23 | N=1 | O=3
| molecular_weight = 289.369
| smiles = CN3[C@H]1CC[C@@H]3C[C@@H](C1)OC(=O)C(CO)c2ccccc2
| InChI = 1/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?
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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?
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = RKUNBYITZUJHSG-SPUOUPEWSA-N
}}
 
|mechAction=tropine inhibits the muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites including smooth muscle, secretory glands and CNS sites. Large doses may block nicotinic receptors at the autonomic ganglia and at the neuromuscular junction.
|mechAction=tropine inhibits the muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites including smooth muscle, secretory glands and CNS sites. Large doses may block nicotinic receptors at the autonomic ganglia and at the neuromuscular junction.
  Specific anticholinergic responses are dose-related. Small doses of atropine inhibit salivary and bronchial secretions and sweating; moderate doses dilate the pupil, inhibit accommodation and increase the heart rate (vagolytic effect); larger doses will decrease motility of the GI and urinary tracts; very large doses will inhibit gastric acid secretion.
  Specific anticholinergic responses are dose-related. Small doses of atropine inhibit salivary and bronchial secretions and sweating; moderate doses dilate the pupil, inhibit accommodation and increase the heart rate (vagolytic effect); larger doses will decrease motility of the GI and urinary tracts; very large doses will inhibit gastric acid secretion.

Revision as of 04:26, 15 December 2014

Atropine
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Ammu Susheela, M.D. [2]

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Overview

Atropine is a anticholinergic that is FDA approved for the treatment of the treatment of poisoning by susceptible organophosphorous nerve agents,. Common adverse reactions include mild to moderate pain, dryness of the mouth, blurred vision, photophobia, confusion, headache, dizziness, tachycardia, palpitations, flushing, urinary hesitance or retention, constipation, abdominal distention, nausea, vomiting, loss of libido and impotency.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Atropine Sulfate Injection, USP, may be given parenterally as a pre-anesthetic medication in surgical patients to reduce salivation and bronchial secretions. It may also be used to suppress vagal activity associated with the use of halogenated hydrocarbons during inhalation anesthesia and reflex excitation arising from mechanical stimulation during surgery.

   The antispasmodic action of atropine is useful in pylorospasm and other spastic conditions of the gastrointestinal tract. For ureteral and biliary colic, atropine concomitantly with morphine may be indicated.
   Atropine relaxes the upper GI tract and colon during hypotonic radiography.
   In poisoning by the organic phosphate cholinesterase inhibitors found in certain insecticides and by chemical warfare nerve gases, large doses of atropine relieve the muscarine-like symptoms and some of the central nervous system manifestations. It is also used as an antidote for mushroom poisoning due to muscarine in certain species such as Amanita muscaria.

Usual adult dosage: Antimuscarinic: Intramuscular, intravenous, or subcutaneous, 400 to 600 μg (0.4 to 0.6 mg) every four to six hours. Arrhythmias: Intravenous, 400 μg (0.4 mg) to 1 mg every one to two hours as needed, up to a maximum of 2 mg. Gastrointestinal radiography: Intramuscular, 1 mg. Preanesthesia (antisialagogue): Intramuscular, 200 to 600 μg (0.2 to 0.6 mg) one-half to one hour before surgery. Cholinergic adjunct (curariform block): Intravenous, 600 μg (0.6 mg) to 1.2 mg administered a few minutes before or concurrently with 500 μg (0.5 mg) to 2 mg of neostigmine methylsulfate, using separate syringes. Antidote (to cholinesterase inhibitors): Intravenous, 2 to 4 mg initially, then 2 mg repeated every five to ten minutes until muscarinic symptoms disappear or signs of atropine toxicity appear. Antidote (to muscarine in mushroom poisoning): Intramuscular or intravenous, 1 to 2 mg every hour until respiratory effects subside. Antidote (to organophosphate pesticides): Intramuscular or intravenous 1 to 2 mg, repeated in twenty to thirty minutes as soon as cyanosis has cleared. Continue dosage until definite improvement occurs and is maintained, sometimes for two days or more.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Atropine in adult patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Atropine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Antimuscarinic: Subcutaneous, 10 μg (0.01 mg) per kg of body weight, not to exceed 400 μg (0.4 mg), or 300 μg (0.3 mg) per square meter of body surface, every four to six hours.

   Arrhythmias: Intravenous, 10 to 30 μg (0.01 to 0.03 mg) per kg of body weight.
   Preanesthesia (antisialagogue): or

Preanesthesia (antiarrhythmic): Subcutaneous–

   Children weighing up to 3 kg: 100 μg (0.1 mg).
   Children weighing 7 to 9 kg: 200 μg (0.2 mg).
   Children weighing 12 to 16 kg: 300 μg (0.3 mg).
   Children weighing 20 to 27 kg: 400 μg (0.4 mg).
   Children weighing 32 kg: 500 μg (0.5 mg).
   Children weighing 41 kg; 600 μg (0.6 mg).

Antidote (to cholinesterase inhibitors): Intravenous or intramuscular, 1 mg initially, then 0.5 to 1 mg every five to ten minutes until muscarinic symptoms disappear or signs of atropine toxicity appear.

NOTE: Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Atropine in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Atropine in pediatric patients.

Contraindications

Atropine Sulfate is contraindicated in patients with a history of hypersensitivity to this drug.

   Ocular: Narrow-angle glaucoma; adhesions (synechiae) between the iris and lens of the eye.
   Cardiovascular: Tachycardia; unstable cardiovascular status in acute hemorrhage.
   GI: Obstructive disease (e.g., achalasia, pyloroduodenal stenosis, or pyloric obstruction, cardiospasm, etc.); paralytic ileus; intestinal atony of the elderly or debilitated patient; severe ulcerative colitis; toxic megacolon complicating ulcerative colitis; hepatic disease.
   GU: Obstructive uropathy (e.g., bladder neck obstruction due to prostatic hypertrophy); renal disease.
   Musculoskeletal: Myasthenia gravis.

Warnings

Heat prostration can occur with anticholinergic drug use (fever and heat stroke due to decreased sweating) in the presence of a high environmental temperature.

   Diarrhea may be an early symptom of incomplete intestinal obstruction, especially in patients with ileostomy or colostomy. Treatment of diarrhea with these drugs is inappropriate and possibly harmful.
   Usage in the elderly: Elderly patients may react with excitement, agitation, drowsiness and other untoward manifestations to even small doses of anticholinergic drugs.
   Usage in gastric ulcer may produce a delay in gastric emptying time and may complicate such therapy (antral stasis).

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Atropine in the drug label.

Postmarketing Experience

GI: Xerostomia; altered taste perception; nausea; vomiting; dysphagia; heartburn, constipation; bloated feeling; para lytic ileus; gastroesophageal reflux. GU: Urinary hesitancy and retention; impotence. Ocular: Blurred vision; mydriasis; photophobia; cycloplegia; increased intraocular pressure. Cardiovascular: Palpitations; bradycardia (following low doses of atropine); tachycardia (after higher doses). CNS: Headache; flushing; nervousness; drowsiness; weakness; dizziness; insomnia; fever. Elderly patients may exhibit mental confusion or excitement to even small doses. Large doses may produce CNS stimulation (restlessness, tremor). Dermatologic - Hypersensitivity: Severe allergic reactions including anaphylaxis, urticaria and other dermal manifestations. Other: Suppression of lactation; nasal congestion; decreased sweating. Complete anhidrosis cannot occur because large doses would be required, producing severe side effects from parasympathetic paralysis.

Drug Interactions

  • Drug
  • Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): B Reproduction studies performed in mice at doses of 50 mg per kg of body weight have revealed no evidence of impaired fertility or harm to the fetus due to atropine. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Atropine in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Atropine during labor and delivery.

Nursing Mothers

Atropine may be excreted in milk, causing infant toxicity, and may reduce breast milk production. Documentation is lacking or conflicting. Safety for use in nursing mothers has not been established.

Pediatric Use

There is no FDA guidance on the use of Atropine with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Atropine with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Atropine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Atropine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Atropine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Atropine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Atropine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Atropine in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Intravenous

Monitoring

There is limited information regarding Monitoring of Atropine in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Atropine in the drug label.

Overdosage

Symptoms: GI: Dry mouth; dysphagia; vomiting; nausea; abdominal distention. CNS: Theoretically, a curare-like action may occur, i.e., neuromuscular blockade leading to muscular weakness and paralysis. CNS stimulation; delirium; drowsiness; stupor; fever; dizziness; headache; restlessness; seizures; depression; tremor; hallucina- tions; ataxia; coma; psychotic behavior; other signs of an acute organic psychosis. Cardiovascular: Circulatory failure; rapid pulse and respiration; tachycardia with weak pulse; hypertension; palpitations. GU: Urinary urgency with difficulty in micturition. Ocular: Blurred vision; photophobia; dilated pupils. Miscellaneous: Leukocytosis, flushed hot dry skin, rash; respiratory failure.

Treatment: Administer supportive and symptomatic therapy as indicated. Physostigmine 1 to 3 mg I.V. has been utilized to reverse anticholinergic effects. However, profound bradycardia, asystole and seizures may occur. The role of physostigmine is not clear; its use should be avoided if other therapeutic agents are successful in reversing cardiac dysrhythmias. Neostigmine methylsulfate 0.5 to 2 mg I.V., repeated as needed, may be given. Diazepam or short-acting barbiturates may control excitement. Hemodialysis is ineffective for atropine poisoning. Hyperpyrexia may be treated with physical cooling measures. If photophobia occurs, the patient may be kept in a dark room.

Pharmacology

Template:Px
Template:Px
Atropine
Systematic (IUPAC) name
(RS)-(8-Methyl-8-azabicyclo[3.2.1]oct-3-yl) 3-hydroxy-2-phenylpropanoate
Identifiers
CAS number 51-55-8
ATC code A03BA01 S01FA01 (WHO)
PubChem 174174
DrugBank DB00572
Chemical data
Formula Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox 
Mol. mass 289.369
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 25%
Metabolism 50% hydrolysed to tropine and tropic acid
Half life 2 hours
Excretion 50% excreted unchanged in urine
Therapeutic considerations
Pregnancy cat.

A(AU) C(US)

Legal status

Template:Unicode Prescription only

Routes Oral, IV, IM, rectal

Mechanism of Action

tropine inhibits the muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites including smooth muscle, secretory glands and CNS sites. Large doses may block nicotinic receptors at the autonomic ganglia and at the neuromuscular junction.

Specific anticholinergic responses are dose-related. Small doses of atropine inhibit salivary and bronchial secretions and sweating; moderate doses dilate the pupil, inhibit accommodation and increase the heart rate (vagolytic effect); larger doses will decrease motility of the GI and urinary tracts; very large doses will inhibit gastric acid secretion.

Structure

Atropine rarely occurs as such in any of the plants and has been prepared by synthesis. It is usually employed in the form of atropine sulfate (the sulfate [2:1] monohydrate salt of atropine), which has much greater solubility in water.

   Atropine Sulfate Injection, USP, is a sterile aqueous solution of atropine sulfate. Each mL contains atropine sulfate, 0.1 mg; sodium chloride, 8.8 mg, for isotonicity; citric acid, 0.63 mg, and sodium citrate, 0.29 mg, as buffers. May contain additional citric acid and/or sodium citrate for pH adjustment (3.0-6.5). The air above the liquid in the container has been displaced by nitrogen gas.
File:Atropine01.png
This image is provided by the National Library of Medicine.

Atropine rarely occurs as such in any of the plants and has been prepared by synthesis. It is usually employed in the form of atropine sulfate (the sulfate [2:1] monohydrate salt of atropine), which has much greater solubility in water.

   Atropine Sulfate Injection, USP, is a sterile aqueous solution of atropine sulfate. Each mL contains atropine sulfate, 0.1 mg; sodium chloride, 8.8 mg, for isotonicity; citric acid, 0.63 mg, and sodium citrate, 0.29 mg, as buffers. May contain additional citric acid and/or sodium citrate for pH adjustment (3.0-6.5). The air above the liquid in the container has been displaced by nitrogen gas.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Atropine in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Atropine in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Atropine in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Atropine in the drug label.

How Supplied

ATROPINE SULFATE INJECTION, USP.

In unit-use packages containing the Luer-Jet™ Luer-Lock Prefilled Syringe. Stock No. Size NDC NO. 3339 1 mg (0.1 mg/mL) 10 mL 0548-3339-00 FOR I.V. USE

Ten cartons per package.

Syringe Assembly Directions:

USE ASEPTIC TECHNIQUE Do not assemble until ready to use.

File:Atropine01.png
This image is provided by the National Library of Medicine.

Storage

File:Atropine01.png
This image is provided by the National Library of Medicine.

Images

Drug Images

{{#ask: Page Name::Atropine |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

{{#ask: Label Page::Atropine |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

There is limited information regarding Patient Counseling Information of Atropine in the drug label.

Precautions with Alcohol

  • Alcohol-Atropine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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