Scolopamine Transdermal System

Prescription

Tên thương mại: Scopolamine Trandermal System

Dạng bào chế

Patch

Đường dùng

TRANSDERMAL

Nhà sản xuất

Bryant Ranch Prepack

About This Medication

11 DESCRIPTION Scopolamine transdermal system is designed for continuous release of scopolamine following application to an area of intact skin on the head, behind the ear. Each system contains 1.3 mg of scopolamine base. Scopolamine is (9-methyl-3-oxa-9-azatricyclo[3.3.1.0 2,4 ]nonan-7-yl) 3-hydroxy-2-phenylpropanoate. The empirical formula is C 17 H 21 NO 4 and its structural formula is: Scopolamine has a molecular weight of 303.35 and a pKa of 7.55-7.81. The scopolamine transdermal system is a circular, 0.2 mm thick, 2.5 cm 2 film with four layers. Proceeding from the visible surface towards the surface attached to the skin, these layers are: (1) a backing membrane of tan-colored, aluminized, polyester film; (2) a drug layer of scopolamine, crospovidone, isopropyl palmitate, light mineral oil, and polyisobutylene; (3) an ethylene vinyl acetate copolymer membrane that controls the rate of delivery of scopolamine from the system to the skin surface; and (4) an contact layer formulation of crospovidone, isopropyl palmitate, light mineral oil, polyisobutylene, and scopolamine. A release liner of siliconized polyester, which covers the adhesive layer, is removed before the system is used. Cross section of the system:

Hoạt chất

Thành phần	Hàm lượng
Scopolamine	-

Chỉ định & Cách dùng

1 INDICATIONS AND USAGE Scopolamine transdermal system is indicated in adults for prevention of: • nausea and vomiting associated with motion sickness • post-operative nausea and vomiting (PONV) associated with recovery from anesthesia and/or opiate analgesia and surgery . Scopolamine transdermal system is an anticholinergic indicated in adults for the prevention of: • nausea and vomiting associated with motion sickness. ( 1 ) • post-operative nausea and vomiting (PONV) associated with recovery from anesthesia and/or opiate analgesia and surgery. ( 1 )

Cơ chế hoạt động

12.1 Mechanism of Action Scopolamine, a belladonna alkaloid, is an anticholinergic. Scopolamine acts: i) as a competitive inhibitor at postganglionic muscarinic receptor sites of the parasympathetic nervous system, and ii) on smooth muscles that respond to acetylcholine but lack cholinergic innervation. It has been suggested that scopolamine acts in the central nervous system (CNS) by blocking cholinergic transmission from the vestibular nuclei to higher centers in the CNS and from the reticular formation to the vomiting center. Scopolamine can inhibit the secretion of saliva and sweat, decrease gastrointestinal secretions and motility, cause drowsiness, dilate the pupils, increase heart rate, and depress motor function.

Liều dùng & Cách dùng

2 DOSAGE AND ADMINISTRATION Application and Removal ( 2.1 ) • Each scopolamine transdermal system delivers 1 mg of scopolamine over 3 days. • Only wear one transdermal system at a time. • Do not cut the transdermal system. • Wash hands thoroughly after application. • Upon removal, fold used transdermal system in half with sticky side together, and discard to prevent accidental contact or ingestion. Recommended Dosage : • Motion Sickness : Apply one transdermal system to the hairless area behind one ear at least 4 hours before antiemetic effect is required for use up to 3 days. If therapy for more than 3 days is required, remove the first transdermal system and apply a new transdermal system behind the other ear. ( 2.2 ) • PONV : For surgeries other than cesarean section, apply one transdermal system behind the ear the evening before surgery and remove 24 hours following surgery. ( 2.2 ) 2.1 Important Application and Removal Instructions • Each scopolamine transdermal system is formulated to deliver in vivo approximately 1 mg of scopolamine over 3 days. • Only wear one transdermal system at any time. • Do not cut the transdermal system. • Apply the transdermal system to the skin in the postauricular area (hairless area behind one ear). • After the transdermal system is applied on the dry skin behind the ear, wash hands thoroughly with soap and water and dry hands [see Warnings and Precautions ( 5.6 )] . • If the transdermal system becomes displaced, discard the transdermal system, and apply a new transdermal system on the hairless area behind the other ear. • Upon removal, fold the used transdermal system in half with the sticky side together, and discard in household trash in a manner that prevents accidental contact or ingestion by children, pets or others. 2.2 Recommended Adult Dosage Motion Sickness Apply one scopolamine transdermal system to the hairless area behind one ear at least 4 hours before the antiemetic effect is required – for use up to 3 days. If therapy is required for longer than 3 days, remove the first transdermal system and apply a new scopolamine transdermal system behind the other ear. PONV For surgeries other than cesarean section : Apply one scopolamine transdermal system the evening before scheduled surgery. Remove the transdermal system 24 hours following surgery.

Side Effects Overview

6 ADVERSE REACTIONS The following serious adverse reactions are described elsewhere in labeling: • Acute Angle Closure Glaucoma [see Warnings and Precautions ( 5.1 )] • Neuropsychiatric Adverse Reactions [see Warnings and Precautions ( 5.2 )] • Eclamptic Seizures in Pregnant Women [see Warnings and Precautions ( 5.3 )] • Gastrointestinal and Urinary Disorders [see Warnings and Precautions ( 5.4 )] • Drug Withdrawal/Post-Removal Symptoms [see Warnings and Precautions ( 5.5 )] • Blurred Vision [see Warnings and Precautions ( 5.6 )] • MRI Skin Burns [see Warnings and Precautions ( 5.7 )] Most common adverse reactions are: • Motion Sickness (>15%): dry mouth, drowsiness, blurred vision and dilation of the pupils. ( 6.1 ) • PONV (≥ 3%): dry mouth, dizziness, somnolence, agitation, visual impairment, confusion, mydriasis and pharyngitis. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Perrigo at 1-866-634-9120 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Motion Sickness The most common adverse reaction (approximately two thirds) was dry mouth. Less common adverse reactions, included drowsiness (less than one sixth), blurred vision and dilation of the pupils. PONV Common adverse reactions, occurring in at least 3% of patients in PONV clinical trials are shown in Table 1. Scopolamine Transdermal System % (N = 461) Placebo % (N = 457) Dry mouth 29 16 Dizziness 12 7 Somnolence 8 4 Agitation 6 4 Visual Impairment 5 3 Confusion 4 3 Mydriasis 4 0 Pharyngitis 3 2 *occurring in at least 3% of patients and at a rate higher than placebo 6.2 Postmarketing Experience The following adverse reactions have been identified during post-approval use of scopolamine transdermal system. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Psychiatric disorders : acute psychosis including: hallucinations, disorientation, and paranoia Nervous system disorders : headache, amnesia, coordination abnormalities, speech disorder, disturbance in attention, restlessness General disorders and administration site conditions : application site burning Eye disorders : dry eyes, eye pruritus, angle closure glaucoma, amblyopia, eyelid irritation Skin and subcutaneous tissue disorders : rash generalized, skin irritation, erythema Renal and urinary disorders : dysuria Ear and labyrinth disorders : vertigo

Cảnh báo & Thận trọng

5 WARNINGS AND PRECAUTIONS • Acute Angle Closure Glaucoma : Monitor for increased intraocular pressure in patients with open-angle glaucoma and adjust glaucoma therapy as needed. Discontinue if signs or symptoms of acute angle closure glaucoma develop. ( 5.1 ) • Neuropsychiatric Adverse Reactions : May cause psychiatric and cognitive effects, seizures and impair mental and/or physical abilities. Monitor patients for new or worsening psychiatric symptoms during treatment and during concomitant treatment with other drugs that are associated with similar psychiatric effects. ( 5.2 , 7.1 ) • Eclamptic Seizures in Pregnant Women : Avoid use in patients with severe preeclampsia. ( 5.3 ) • Gastrointestinal and Urinary Disorders : Consider more frequent monitoring during treatment in patients suspected of having intestinal obstruction; patients with pyloric obstruction, urinary bladder neck obstruction or receiving other anticholinergic drugs. Discontinue if patient develops difficulty in urination. ( 5.4 , 7.2 ) • Drug Withdrawal/Post-Removal Symptoms : Anticholinergic symptoms may occur 24 hours or more after removal of the transdermal system. ( 5.5 ) • Blurred Vision : Avoid contact with the eyes. ( 2.1 , 5.6 ) • Magnetic Resonance Imaging (MRI) Skin Burns : Remove scopolamine transdermal system prior to MRI scan. ( 5.7 ) 5.1 Acute Angle Closure Glaucoma The mydriatic effect of scopolamine may cause an increase in intraocular pressure resulting in acute angle closure glaucoma. Monitor intraocular pressure in patients with open angle glaucoma and adjust glaucoma therapy during scopolamine transdermal system use, as needed. Advise patients to immediately remove the transdermal system and contact their healthcare provider if they experience symptoms of acute angle closure glaucoma (e.g., eye pain or discomfort, blurred vision, visual halos or colored images in association with red eyes from conjunctival congestion and corneal edema). 5.2 Neuropsychiatric Adverse Reactions Psychiatric Adverse Reactions Scopolamine has been reported to exacerbate psychosis. Other psychiatric reactions have also been reported, including acute toxic psychosis, agitation, speech disorder, hallucinations, paranoia, and delusions [see Adverse Reactions ( 6.2 )] . Monitor patients for new or worsening psychiatric symptoms during treatment with scopolamine transdermal system. Also, monitor patients for new or worsening psychiatric symptoms during concomitant treatment with other drugs that are associated with similar psychiatric effects [see Drug Interactions ( 7.1 )] . Seizures Seizures and seizure-like activity have been reported in patients receiving scopolamine. Weigh this potential risk against the benefits before prescribing scopolamine transdermal system to patients with a history of seizures, including those receiving anti-epileptic medication or who have risk factors that can lower the seizure threshold. Cognitive Adverse Reactions Scopolamine can cause drowsiness, disorientation, and confusion. Discontinue scopolamine transdermal system if signs or symptoms of cognitive impairment develop. Elderly and pediatric patients may be more sensitive to the neurological and psychiatric effects of scopolamine transdermal system. Consider more frequent monitoring during treatment with scopolamine transdermal system in elderly patients [see Use in Specific Populations ( 8.5 )] . Scopolamine transdermal system is not approved for use in pediatric patients [see Use in Specific Populations ( 8.4 )] . Hazardous Activities Scopolamine transdermal system may impair the mental and/or physical abilities required for the performance of hazardous tasks such as driving a motor vehicle, operating machinery or participating in underwater sports. Concomitant use of other drugs that cause central nervous system (CNS) adverse reactions (e.g., alcohol, sedatives, hypnotics, opiates, and anxiolytics) or have anticholinergic properties (e.g., other belladonna alkaloids, sedating antihistamines, meclizine, tricyclic antidepressants, and muscle relaxants) may increase this effect [see Drug Interactions ( 7.1 )] . Inform patients not to operate motor vehicles or other dangerous machinery or participate in underwater sports until they are reasonably certain that scopolamine transdermal system does not affect them adversely. 5.3 Eclamptic Seizures in Pregnant Women Eclamptic seizures have been reported in pregnant women with severe preeclampsia soon after injection of intravenous and intramuscular scopolamine [see Use in Specific Populations ( 8.1 )]. Avoid use of scopolamine transdermal system in patients with severe preeclampsia. 5.4 Gastrointestinal and Urinary Disorders Scopolamine, due to its anticholinergic properties, can decrease gastrointestinal motility and cause urinary retention. Consider more frequent monitoring during treatment with scopolamine transdermal system in patients suspected of having intestinal obstruction, patients with pyloric obstruction or urinary bladder neck obstruction and patients receiving other anticholinergic drugs [see Drug Interactions ( 7.2 )] . Discontinue scopolamine transdermal system in patients who develop difficulty in urination. 5.5 Drug Withdrawal/Post-Removal Symptoms Discontinuation of scopolamine transdermal system, usually after several days of use, may result in withdrawal symptoms, such as disturbances of equilibrium, dizziness, nausea, vomiting, abdominal cramps, sweating, headache, mental confusion, muscle weakness, bradycardia and hypotension. The onset of these symptoms is generally 24 hours or more after the transdermal system has been removed. Instruct patients to seek medical attention if they experience severe symptoms. 5.6 Blurred Vision Scopolamine can cause temporary dilation of the pupils resulting in blurred vision if it comes in contact with the eyes. Advise patients to wash their hands thoroughly with soap and water and dry their hands immediately after handling the transdermal system [see Dosage and Administration ( 2.1 )] . 5.7 Magnetic Resonance Imaging (MRI) Skin Burns Scopolamine transdermal system contains an aluminized membrane. Skin burns have been reported at the application site in patients wearing an aluminized transdermal system during an MRI scan. Remove scopolamine transdermal system before undergoing an MRI.

Chống chỉ định

4 CONTRAINDICATIONS Scopolamine transdermal system is contraindicated in patients with: • angle closure glaucoma. [see Warnings and Precautions ( 5.1 )] • hypersensitivity to scopolamine or other belladonna alkaloids or to any ingredient or component in the formulation or delivery system. Reactions have included rash generalized and erythema [see Adverse Reactions ( 6.2 ), Description ( 11 )] . • Angle closure glaucoma ( 4 , 6.2 ) • Hypersensitivity to scopolamine or to other belladonna alkaloids or to any ingredient or component of the formulation or delivery system. ( 4 , 7 )

Dược động học

12.3 Pharmacokinetics The system is formulated to deliver approximately 1 mg of scopolamine to the systemic circulation over 3 days. Absorption Following application to the skin behind the ear, circulating plasma concentrations are detected within 4 hours with peak concentrations being obtained, on average, within 24 hours. The average plasma concentration produced is 87 pg/mL (0.28 nM) for free scopolamine and 354 pg/mL for total scopolamine (free + conjugates). Following removal of the used transdermal system, there is some degree of continued systemic absorption of scopolamine bound in the skin layers. Distribution The distribution of scopolamine is not well characterized. It crosses the placenta and the blood brain barrier and may be reversibly bound to plasma proteins. Elimination Metabolism and Excretion Scopolamine is metabolized and conjugated with less than 5% of the total dose appearing unchanged in the urine. The enzymes responsible for metabolizing scopolamine are unknown. The exact elimination pattern of scopolamine has not been determined. Following transdermal system removal, plasma concentrations of scopolamine decline in a log linear fashion with an observed half-life of 9.5 hours. Less than 10% of the total dose is excreted in the urine as the parent drug and metabolites over 108 hours. Drug Interaction Studies An in vitro study using human hepatocytes examined the induction of CYP1A2 and CYP3A4 by scopolamine. Scopolamine did not induce CYP1A2 and CYP3A4 isoenzymes at the concentrations up to 10 nM. In an in vitro study using human liver microsomes which evaluated the inhibition of CYP1A2, 2C8, 2C9, 2C19, 2D6 and 3A4, scopolamine did not inhibit these cytochrome P450 isoenzymes at the concentrations up to 1 micromolar. No in vivo drug-drug interaction studies have been conducted.

Frequently Asked Questions

1 INDICATIONS AND USAGE Scopolamine transdermal system is indicated in adults for prevention of: • nausea and vomiting associated with motion sickness • post-operative nausea and vomiting (PONV) associated with recovery from anesthesia and/or opiate analgesia and surgery . Scopolamine transdermal system is an anticholinergic indicated in adults for the prevention of: • nausea and vomiting associated with motion sickness. ( 1 ) • post-operative nausea and vomiting (PONV) associated with recovery from anesthesia and/or opiate analgesia and surgery. ( …

2 DOSAGE AND ADMINISTRATION Application and Removal ( 2.1 ) • Each scopolamine transdermal system delivers 1 mg of scopolamine over 3 days. • Only wear one transdermal system at a time. • Do not cut the transdermal system. • Wash hands thoroughly after application. • Upon removal, fold used transdermal system in half with sticky side together, and discard to prevent accidental contact or ingestion. Recommended Dosage : • Motion Sickness : Apply one transdermal system to the hairless …

5 WARNINGS AND PRECAUTIONS • Acute Angle Closure Glaucoma : Monitor for increased intraocular pressure in patients with open-angle glaucoma and adjust glaucoma therapy as needed. Discontinue if signs or symptoms of acute angle closure glaucoma develop. ( 5.1 ) • Neuropsychiatric Adverse Reactions : May cause psychiatric and cognitive effects, seizures and impair mental and/or physical abilities. Monitor patients for new or worsening psychiatric symptoms during treatment and during concomitant treatment with other drugs that are associated with similar …

4 CONTRAINDICATIONS Scopolamine transdermal system is contraindicated in patients with: • angle closure glaucoma. [see Warnings and Precautions ( 5.1 )] • hypersensitivity to scopolamine or other belladonna alkaloids or to any ingredient or component in the formulation or delivery system. Reactions have included rash generalized and erythema [see Adverse Reactions ( 6.2 ), Description ( 11 )] . • Angle closure glaucoma ( 4 , 6.2 ) • Hypersensitivity to scopolamine or to other belladonna alkaloids or to any …

Scolopamine Transdermal System is a prescription medication. You will need a valid prescription from a licensed healthcare provider.

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References & Data Sources

• DailyMed — Scolopamine Transdermal System drug label (National Library of Medicine)
• openFDA — Scolopamine Transdermal System label data (U.S. Food & Drug Administration)
• RxNorm — RXCUI 226552 (NLM Normalized Drug Names)
• NDC Directory — Scolopamine Transdermal System (FDA National Drug Code)

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Nguồn dữ liệu: DailyMed (NLM), openFDA, MFDS