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Scopolamine


Scopolamine

Article Author:
Marina Riad
Article Editor:
Candice Hithe
Updated:
5/30/2020 9:03:23 PM
For CME on this topic:
Scopolamine CME
PubMed Link:
Scopolamine

Indications

Scopolamine is a medication used in the management and treatment of postoperative nausea and vomiting (PONV) and motion sickness. It is in the anticholinergic class of drugs.

FDA Labeled Indications: [1][2]

There are two FDA approved indications for the use of scopolamine:

  • Postoperative nausea and vomiting (PONV) associated with recovery from anesthesia, opiate analgesia and surgery
  • Nausea and vomiting associated with motion sickness 

Non-FDA Labeled Indications: [3][4][5][6]

Scopolamine can be used as an off-label adjunct to treat certain conditions listed below due to its anticholinergic properties.

  • Gastrointestinal spasms 
  • Chemotherapy nausea
  • Asthma attacks 
  • Depression
  • Smoking cessation therapy 
  • Excessive sweating

Mechanism of Action

Scopolamine derives from the plants of Datura stramonium (Jimsonweed), Scopolia carniolica, and Hyoscyamus niger (henbane). These plants produce the toxic compound, belladonna alkaloids, as a protective mechanism.[7] Scopolamine competitively inhibits G-protein coupled post-ganglionic muscarinic receptors for acetylcholine and acts as a nonselective muscarinic antagonist, producing both peripheral antimuscarinic properties and central sedative, antiemetic, and amnestic effects.[8] It is structurally very similar to atropine and is useful in conditions requiring decreased parasympathetic activity. Peripherally this results in smooth muscle relaxation and reduced gland secretion. Centrally, unlike atropine, scopolamine causes mostly sedation, but over-excitement and restlessness can occur at higher doses.[7]

The vomiting center of the brain is located in the medulla oblongata and contains a high amount of M1 muscarinic acetylcholine, H1 histamine, NK1, and 5-HT3 serotonin receptors. Thus, any agent that antagonize these receptors will have antiemetic properties. Scopolamine exerts its action by primarily affecting the M1 receptor. However, some research has reported H1 receptor activity.[7]

Administration

The most commonly used dose form of scopolamine in the United States is a transdermal patch. Each patch is a circular shape of about 2.5 cm in diameter and 0.2 mm in thickness. Its design is in four layers for step-wise delivery of a priming dose of 140 micrograms of scopolamine initially, followed by a steady 1.5 mg release over 72 hours.[9] The onset of action of scopolamine is four hours, and the peak effect of the patch occurs at 24 hours. Per package labeling, the recommendation is to apply scopolamine the night before surgery if using it for the prevention of postoperative nausea and vomiting, or four hours before exposure if used for motion sickness. For cesarean sections, apply one hour before surgery to limit exposure to the baby. The manufacturer also recommends discontinuation of the patch 24 hours after surgery because there was no significant antiemetic effect of scopolamine for PONV between 24 and 48 hours. For motion sickness, reapplication can be every 72 hours.[7][10][11]

Patch placement should be on the postauricular area (the hairless area behind the ear). The stratum corneum, which acts as a significant barrier to percutaneous absorption, is the thinnest at this location. Patients should not cut the scopolamine patch, as it will alter the delivery system, and blood levels become less controlled. There are two other scopolamine products available outside the USA: scopolamine hydrobromide and scopolamine butylbromide. Both are useable in parenteral, intramuscular, intravenous, and subcutaneous forms. The short duration of action, less predictable blood levels, and common side effects resulted in the exclusion of these products from U.S. markets.[9]

Adverse Effects

The most commonly reported side effects with scopolamine patch use are blurred vision, dilated pupils, and dry mouth. The vision disturbances are most often due to inadequate handwashing techniques after the application of the patch.[1] Less frequently reported side effects are related to anticholinergic toxidrome: flushed skin, tachycardia, agitation, and confusion. These side effects are usually mild and quick to resolve after patch removal. If needed, the clinician can administer a reversal agent like physostigmine if a side effect persists.[8][12] 

Contraindications

The FDA currently lists two contraindications for scopolamine: allergy to belladonna alkaloids and angle-closure glaucoma. Patients with angle-closure glaucoma should not be prescribed scopolamine. Scopolamine causes mydriasis or pupillary dilation. A dilated iris prohibits proper drainage of fluid from the anterior chamber, thus creating a further increase in anterior chamber pressure and precipitates acute angle-closure glaucoma.[13]

Monitoring

There are several conditions in which scopolamine use requires caution, or its effects monitored more frequently.

There are reports of scopolamine worsening psychosis. Reports also exist of acute toxic psychosis, agitation, speech disorder, hallucinations, paranoia, and delusions.[14][15] Patients need monitoring for new or worsening psychiatric symptoms during treatment.

Use caution in using scopolamine for patients with myasthenia gravis. Myasthenia gravis is caused by a lack of proper nerve impulse transmission due to antibodies to acetylcholine receptors, resulting in muscle fatigue. Although myasthenia gravis primarily affects skeletal muscle, the use of anticholinergic agents, like scopolamine, causes unpredictable results.[16]

There has been some concern about the use of scopolamine in patients with a seizure history. The speculated reason is that scopolamine might lower seizure threshold potential. However, further examination of medical records showed this not to be true. This false claim was primarily attributable to the coding of reported cases as "dizziness, rule out seizures." Patients in these cases did not experience an actual seizure or had it before the application of scopolamine.[17] Nonetheless, there is a valid concern for seizure induction with the use of scopolamine in patients with severe preeclampsia. Currently, the understanding of preeclampsia has its basis in a vasospasm theory, and the use of anticholinergic agents may leave the sympathetic system unopposed, further deteriorating the condition of preeclampsia into eclampsia and HELLP syndrome.[18]

Patients should also discontinue using a scopolamine patch before MRI. One of the four layers contains metal and can burn the skin during the imaging.[7]

Due to scopolamine's anticholinergic properties, its use can decrease gastrointestinal motility and cause urinary retention.[19] In patients suspected of having intestinal obstruction, pyloric obstruction, urinary bladder neck obstruction, or patients receiving other anticholinergic drugs, consider more frequent monitoring during treatment. Discontinue scopolamine in patients who develop difficulty urinating.

Scopolamine use also merits caution in special populations. Children, pregnant or lactating mothers, patients with hepatic or renal impairment, and the elderly should be monitored earlier for more severe side effects

There is no formal laboratory testing of scopolamine levels currently available.

Toxicity

Toxicity does not happen as frequently with the transdermal form of scopolamine due to its extended-release nature. Data on the toxic dose of scopolamine in the tablet form is scattered. Reports exist that 10 mg a day can be lethal for children. In adults, consumption of more than 100 mg a day did not result in death. The other feared toxidrome of scopolamine overdose is an anticholinergic syndrome resulting in tachycardia, hallucinations, hyperthermia, and dry membranes. Physostigmine 1 to 4 mg IV can serve as an antidote in such severe cases. However, with the transdermal application, only minor side effects are most commonly observed.[12][9]

Enhancing Healthcare Team Outcomes

Scopolamine is used extensively for the prevention of PONV in the hospital setting and motion sickness outside of the hospital, and its use and administration should have the involvement of an interprofessional team. Nursing staff should be knowledgeable about proper placement and side effects of scopolamine. The most commonly occurring are mucosal dryness and visual disturbances. The latter is usually due to touching the patch and then rubbing the eyes, or not properly washing hands after patch administration. Patch formulation prevents systemic toxicity, but one should be aware of the side effects of a possible overdose and monitor closely in specific populations. Nursing can monitor the patient's progress with therapy and check for adverse events in both inpatient and outpatient settings. Pharmacists should check for drug-drug interactions and educate patients and team members regarding the proper use and potential side effects. With a team paradigm, scopolamine can achieve maximum therapeutic benefit with minimal adverse events. [Level 5]


References

[1] Kassel L,Nelson M,Shine J,Jones LR,Kassel C, Scopolamine Use in the Perioperative Patient: A Systematic Review. AORN journal. 2018 Sep;     [PubMed PMID: 30156728]
[2] Brainard A,Gresham C, Prevention and treatment of motion sickness. American family physician. 2014 Jul 1;     [PubMed PMID: 25077501]
[3] del Valle-Laisequilla CF,Flores-Murrieta FJ,Granados-Soto V,Rocha-González HI,Reyes-García G, Ketorolac tromethamine improves the analgesic effect of hyoscine butylbromide in patients with intense cramping pain from gastrointestinal or genitourinary origin. Arzneimittel-Forschung. 2012 Dec;     [PubMed PMID: 23093479]
[4] Gaire BP,Subedi L, A review on the pharmacological and toxicological aspects of Datura stramonium L. Journal of integrative medicine. 2013 Mar;     [PubMed PMID: 23506688]
[5] Sun X,Sun C,Zhai L,Dong W, A Selective M{sub}1{/sub} and M{sub}3{/sub} Receptor Antagonist, Penehyclidine Hydrochloride, Exerts Antidepressant-Like Effect in Mice. Neurochemical research. 2019 Dec;     [PubMed PMID: 31606838]
[6] Schlereth T,Dieterich M,Birklein F, Hyperhidrosis--causes and treatment of enhanced sweating. Deutsches Arzteblatt international. 2009 Jan     [PubMed PMID: 19564960]
[7] Pergolizzi JV Jr,Philip BK,Leslie JB,Taylor R Jr,Raffa RB, Perspectives on transdermal scopolamine for the treatment of postoperative nausea and vomiting. Journal of clinical anesthesia. 2012 Jun;     [PubMed PMID: 22608591]
[8] Zhang XC,Farrell N,Haronian T,Hack J, Postoperative Anticholinergic Poisoning: Concealed Complications of a Commonly Used Medication. The Journal of emergency medicine. 2017 Oct;     [PubMed PMID: 28756934]
[9] Renner UD,Oertel R,Kirch W, Pharmacokinetics and pharmacodynamics in clinical use of scopolamine. Therapeutic drug monitoring. 2005 Oct;     [PubMed PMID: 16175141]
[10] Sah N,Ramesh V,Kaul B,Dalby P,Shestak K,Vallejo MC, Transdermal scopolamine patch in addition to ondansetron for postoperative nausea and vomiting prophylaxis in patients undergoing ambulatory cosmetic surgery. Journal of clinical anesthesia. 2009 Jun;     [PubMed PMID: 19502023]
[11] Pergolizzi JV,Raffa R,Taylor R, Prophylaxis of postoperative nausea and vomiting in adolescent patients: a review with emphasis on combination of fixed-dose ondansetron and transdermal scopolamine. Journal of drug delivery. 2011;     [PubMed PMID: 21773046]
[12] Corallo CE,Whitfield A,Wu A, Anticholinergic syndrome following an unintentional overdose of scopolamine. Therapeutics and clinical risk management. 2009 Oct;     [PubMed PMID: 19774213]
[13] Hamill MB,Suelflow JA,Smith JA, Transdermal scopolamine delivery system (TRANSDERM-V) and acute angle-closure glaucoma. Annals of ophthalmology. 1983 Nov;     [PubMed PMID: 6651138]
[14] Ziskind AA, Transdermal scopolamine-induced psychosis. Postgraduate medicine. 1988 Sep 1     [PubMed PMID: 2901077]
[15] MacEwan GW,Remick RA,Noone JA, Psychosis due to transdermally administered scopolamine. CMAJ : Canadian Medical Association journal = journal de l'Association medicale canadienne. 1985 Sep 1     [PubMed PMID: 4027811]
[16] Spiess JL,Scott SD, Anticholinergic agents for the treatment of     [PubMed PMID: 12850651]
[17] Strom BL,Carson JL,Schinnar R,Snyder ES,Shaw M,Waiter SL, No causal relationship between transdermal scopolamine and seizures: methodologic lessons for pharmacoepidemiology. Clinical pharmacology and therapeutics. 1991 Jul;     [PubMed PMID: 1855348]
[18] Kobayashi T,Sugimura M,Tokunaga N,Naruse H,Nishiguchi T,Kanayama N,Terao T, Anticholinergics induce eclamptic seizures. Seminars in thrombosis and hemostasis. 2002 Dec;     [PubMed PMID: 12536341]
[19] Dessie SG,Hacker MR,Apostolis C,Boundy EO,Modest AM,Jones SM,Rosenblatt PL, Effect of Scopolamine Patch Use on Postoperative Voiding Function After Transobturator Slings. Female pelvic medicine & reconstructive surgery. 2016 May-Jun     [PubMed PMID: 26825403]