Difference between revisions of "Atropine"
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| uses = Treatment of bradycardia, | | uses = Treatment of bradycardia, | ||
Antidote for acetylcholinesterase inhibitor toxicity | Antidote for acetylcholinesterase inhibitor toxicity | ||
| contraindications = | | contraindications = Known hypersensitivity | ||
| routes = IV, IM | | routes = IV, IM, PO, oral or endotracheal inhalation, ophthalmic solution | ||
| dosage = | | dosage = Treatment of bradycardia: | ||
1 mg every 3 to 5 minutes (3mg max), repeat until obtaining desired heart rate | |||
Treatment of acetylcholinesterase inhibitor toxicity: | |||
2 to 3 mg every 20 to 30 min | |||
Antisialagogue/anti-vagal: | |||
0.5 to 1mg every 1 to 2 hours | |||
Pediatric: | |||
0.01 mg/kg to 0.03 mg/kg every 3 to 5 minutes. Minimum dose is 0.1 mg. Maximum dose is 0.5mg (child) or 1 mg (adolescent). | |||
| dosage_calculation = atropine | |||
| mechanism = Muscarinic acetylcholine antagonism | | mechanism = Muscarinic acetylcholine antagonism | ||
| adverse_effects = | | adverse_effects = | ||
| time_onset = | | time_onset = | ||
| duration = | | duration = | ||
| metabolism = | | metabolism = Enzymatic hydrolysis in the liver | ||
| halflife_redistribution = | | halflife_redistribution = | ||
| halflife_elimination = | | halflife_elimination = | ||
| clearance = | | clearance = | ||
| protein_binding = | | protein_binding = 14-22% | ||
| formula = C<sub>17</sub>H<sub>23</sub>NO<sub>3</sub> | |||
| molar_mass = 289.369 g/mol | |||
}} | }} | ||
'''Atropine''' is a tertiary amine extracted from belladonna alkaloid as a racemic mixture of d and l-hyoscyamine, which vary in their potency as anticholinergic agents. It reversibly binds to peripheral muscarinic acetylcholine receptors where it acts a competitive inhibitor. Its primary uses include treatment of bradycardia or bradycardia-induced cardiac arrest, treatment of cholinergic effects of organophosphate, nerve agent, or insecticide toxicity, or in ophthalmic surgery to produce mydriasis and cycloplegia. It can also be utilized in conjunction with cholinesterase inhibitors for reversal of neuromuscular blockade in order to reduce their muscarinic effects. | |||
==Uses<!-- Describe uses of the drug. If appropriate, add subsections for each indication. -->== | |||
* Treatment of bradycardia (vasovagal response, AV block, bradyarrhythmias) | |||
*Treatment of acetylcholinesterase inhibitor toxicity (chemical nerve agents, carbamate, organophosphates) | |||
*Perioperatively for reduction of secretions and vagal responses | |||
*Perioperatively for prophylaxis against muscarinic effects when anticholinesterase agents (neostigmine, physostigmine, pyridostigmine) are used to reverse neuromuscular blockade | |||
*For ophthalmic surgery, to induce mydriasis or cycloplegia | |||
*Treatment of amblyopia | |||
==Contraindications<!-- List contraindications and precautions for use of the drug. -->== | |||
== | ===Absolute contraindications<!-- List absolute contraindications for use of the drug. If none, this section may be removed. -->=== | ||
*Atropine or belladonna alkaloids hypersensitivity. Note: IM/IV administration of atropine can cause flushing of face and trunk, which is not associated with a hypersensitivity response.<ref>{{Cite web|date=07/2018|title=Atropine Injection, 2mg|url=https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/212319s000lbl.pdf|url-status=live|access-date=01/05/2024|website=FDA Drug Safety Data}}</ref> | |||
== | ===Precautions<!-- List precautions for use of the drug. If none, this section may be removed. -->=== | ||
*Coronary artery disease, acute myocardial infarct, congestive heart failure, tachycardia, or hypertension | |||
*Chronic lung disease | |||
*Obstructive gastrointestinal disease, including toxic megacolon, paralytic ileus, pyloric stenosis | |||
*Obstructive urinary disease, including uropathy and prostatic hypertrophy | |||
* Acute-angle glaucoma | |||
*[[Myasthenia gravis]] | |||
*Insufficient data regarding atropine use during pregnancy to determine risk of adverse developmental outcomes | |||
== | ==Pharmacology== | ||
=== | ===Pharmacodynamics<!-- Describe the effects of the drug on the body. If appropriate, add subsections by organ system -->=== | ||
== | ====Mechanism of action<!-- Describe the mechanism of action for the primary uses of the drug. -->==== | ||
Atropine is a competitive inhibitor at autonomic postganglionic cholinergic receptors.<ref name=":0">{{Citation|last=McLendon|first=Kevin|title=Atropine|date=2023|url=http://www.ncbi.nlm.nih.gov/books/NBK470551/|work=StatPearls|place=Treasure Island (FL)|publisher=StatPearls Publishing|pmid=29262018|access-date=2024-01-11|last2=Preuss|first2=Charles V.}}</ref> Atropine’s activity is primarily due to the l-hyoscyamine enantiomer. Atropine binds receptors found in GI and pulmonary smooth muscle, exocrine glands, heart and eye; it does not block acetylcholine’s action at the NMJ. It does not inhibit nicotinic cholinergic receptors at typical doses. Atropine’s primary clinical effects include changes in heart rate, reduction in salivary, bronchial, and sweat gland secretions, bronchodilation, mydriasis and cycloplegia, decreased GI motility and gastric secretions, and contraction of the bladder detrusor muscle. | |||
=== | ====Adverse effects<!-- Describe any potential adverse effects of the drug. -->==== | ||
*Dry mouth (xerostomia) | |||
*Blurred vision, including photophobia and loss of visual acuity | |||
*GI symptoms: dysphagia, constipation, nausea, vomiting | |||
*Bradycardia (at doses of 0.4-0.6mg) | |||
*Tachycardia (at doses of 1-2mg) | |||
*Palpitations, arrhythmias, asystole | |||
*Flushing | |||
*Urinary retention | |||
*Delirium and coma at high doses | |||
=== | ===Pharmacokinetics<!-- Describe the pharmacokinetics of the drug. -->=== | ||
=== Pharmacokinetics | * IV administration has a distribution half life of about 1 minute, with rapid decline in concentration within the first 8-10 minutes.<ref name=":0" /> | ||
* Crosses the blood-brain barrier and the placenta<ref name=":1">{{Cite journal|last=Ali–Melkkilä|first=T.|last2=Kanto|first2=J.|last3=Iisalo|first3=E.|date=1993-10|title=Pharmacokinetics and related pharmacodynamics of anticholinergic drugs|url=https://onlinelibrary.wiley.com/doi/10.1111/j.1399-6576.1993.tb03780.x|journal=Acta Anaesthesiologica Scandinavica|language=en|volume=37|issue=7|pages=633–642|doi=10.1111/j.1399-6576.1993.tb03780.x|issn=0001-5172}}</ref> | |||
* Undergoes enzymatic hydrolysis in the liver into active metabolites<ref name=":1" /> | |||
* Atropine and its metabolites are primarily exreted renally, with small contributions from pulmonary and fecal routes of excretion. 13-57% of atropine is excreted unchanged in the urine.<ref name=":1" /> | |||
== Chemistry and formulation<!-- Describe the chemistry and formulation of the drug. --> == | ==Chemistry and formulation<!-- Describe the chemistry and formulation of the drug. -->== | ||
== History<!-- Describe the historical development of the drug. --> == | == History<!-- Describe the historical development of the drug. -->== | ||
== References == | == References== | ||
[[Category:Drug reference]] | [[Category:Drug reference]] | ||
[[Category: | [[Category:Anticholinergics]] | ||
[[Category:Positive chronotropes]] | [[Category:Positive chronotropes]] | ||
[[Category:Antidotes]] | |||
<references /> | |||
Latest revision as of 17:18, 10 January 2024
Atropine
| Clinical data | |
| Drug class |
Anticholinergic |
|---|---|
| Uses |
Treatment of bradycardia, Antidote for acetylcholinesterase inhibitor toxicity |
| Contraindications |
Known hypersensitivity |
| Routes of administration |
IV, IM, PO, oral or endotracheal inhalation, ophthalmic solution |
| Dosage |
Treatment of bradycardia: 1 mg every 3 to 5 minutes (3mg max), repeat until obtaining desired heart rate Treatment of acetylcholinesterase inhibitor toxicity: 2 to 3 mg every 20 to 30 min Antisialagogue/anti-vagal: 0.5 to 1mg every 1 to 2 hours Pediatric: 0.01 mg/kg to 0.03 mg/kg every 3 to 5 minutes. Minimum dose is 0.1 mg. Maximum dose is 0.5mg (child) or 1 mg (adolescent). |
| Dosage | |
| Pharmacodynamics | |
| Mechanism of action |
Muscarinic acetylcholine antagonism |
| Pharmacokinetics | |
| Metabolism |
Enzymatic hydrolysis in the liver |
| Protein binding |
14-22% |
| Physical and chemical data | |
| Formula |
C17H23NO3 |
| Molar mass |
289.369 g/mol |
| Article quality | |
| Editor rating | |
| User likes | 0 |
Atropine is a tertiary amine extracted from belladonna alkaloid as a racemic mixture of d and l-hyoscyamine, which vary in their potency as anticholinergic agents. It reversibly binds to peripheral muscarinic acetylcholine receptors where it acts a competitive inhibitor. Its primary uses include treatment of bradycardia or bradycardia-induced cardiac arrest, treatment of cholinergic effects of organophosphate, nerve agent, or insecticide toxicity, or in ophthalmic surgery to produce mydriasis and cycloplegia. It can also be utilized in conjunction with cholinesterase inhibitors for reversal of neuromuscular blockade in order to reduce their muscarinic effects.
Uses
- Treatment of bradycardia (vasovagal response, AV block, bradyarrhythmias)
- Treatment of acetylcholinesterase inhibitor toxicity (chemical nerve agents, carbamate, organophosphates)
- Perioperatively for reduction of secretions and vagal responses
- Perioperatively for prophylaxis against muscarinic effects when anticholinesterase agents (neostigmine, physostigmine, pyridostigmine) are used to reverse neuromuscular blockade
- For ophthalmic surgery, to induce mydriasis or cycloplegia
- Treatment of amblyopia
Contraindications
Absolute contraindications
- Atropine or belladonna alkaloids hypersensitivity. Note: IM/IV administration of atropine can cause flushing of face and trunk, which is not associated with a hypersensitivity response.[1]
Precautions
- Coronary artery disease, acute myocardial infarct, congestive heart failure, tachycardia, or hypertension
- Chronic lung disease
- Obstructive gastrointestinal disease, including toxic megacolon, paralytic ileus, pyloric stenosis
- Obstructive urinary disease, including uropathy and prostatic hypertrophy
- Acute-angle glaucoma
- Myasthenia gravis
- Insufficient data regarding atropine use during pregnancy to determine risk of adverse developmental outcomes
Pharmacology
Pharmacodynamics
Mechanism of action
Atropine is a competitive inhibitor at autonomic postganglionic cholinergic receptors.[2] Atropine’s activity is primarily due to the l-hyoscyamine enantiomer. Atropine binds receptors found in GI and pulmonary smooth muscle, exocrine glands, heart and eye; it does not block acetylcholine’s action at the NMJ. It does not inhibit nicotinic cholinergic receptors at typical doses. Atropine’s primary clinical effects include changes in heart rate, reduction in salivary, bronchial, and sweat gland secretions, bronchodilation, mydriasis and cycloplegia, decreased GI motility and gastric secretions, and contraction of the bladder detrusor muscle.
Adverse effects
- Dry mouth (xerostomia)
- Blurred vision, including photophobia and loss of visual acuity
- GI symptoms: dysphagia, constipation, nausea, vomiting
- Bradycardia (at doses of 0.4-0.6mg)
- Tachycardia (at doses of 1-2mg)
- Palpitations, arrhythmias, asystole
- Flushing
- Urinary retention
- Delirium and coma at high doses
Pharmacokinetics
- IV administration has a distribution half life of about 1 minute, with rapid decline in concentration within the first 8-10 minutes.[2]
- Crosses the blood-brain barrier and the placenta[3]
- Undergoes enzymatic hydrolysis in the liver into active metabolites[3]
- Atropine and its metabolites are primarily exreted renally, with small contributions from pulmonary and fecal routes of excretion. 13-57% of atropine is excreted unchanged in the urine.[3]
Chemistry and formulation
History
References
- ↑ "Atropine Injection, 2mg" (PDF). FDA Drug Safety Data. 07/2018. Retrieved 01/05/2024. Check date values in:
|access-date=and|date=(help) - ↑ 2.0 2.1 McLendon, Kevin; Preuss, Charles V. (2023), "Atropine", StatPearls, Treasure Island (FL): StatPearls Publishing, PMID 29262018, retrieved 2024-01-11
- ↑ 3.0 3.1 3.2 Ali–Melkkilä, T.; Kanto, J.; Iisalo, E. (1993-10). "Pharmacokinetics and related pharmacodynamics of anticholinergic drugs". Acta Anaesthesiologica Scandinavica. 37 (7): 633–642. doi:10.1111/j.1399-6576.1993.tb03780.x. ISSN 0001-5172. Check date values in:
|date=(help)
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