Scopolamine is present in human milk. There are no available data on the effects of scopolamine on the breastfed infant or the effects on milk production. Because there have been no consistent reports of adverse events in breastfed infants over decades of use, the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for scopolamine and any potential adverse effects on the breastfed child from scopolamine or from the underlying maternal condition.
Safety and effectiveness in pediatric patients have not been established. Pediatric patients are particularly susceptible to the adverse reactions of scopolamine; including mydriasis, hallucinations, amblyopia and drug withdrawal syndrome. Neurologic and psychiatric adverse reactions, such as hallucinations, amblyopia and mydriasis have also been reported.
Clinical trials of scopolamine transdermal system did not include sufficient number of subjects aged 65 years and older to determine if they respond differently from younger subjects. In other clinical experience, elderly patients had an increased risk of neurologic and psychiatric adverse reactions, such as hallucinations, confusion, dizziness and drug withdrawal syndrome [see Warnings and Precautions (5.2, 5.5)]. Consider more frequent monitoring for CNS adverse reactions during treatment with scopolamine transdermal system in elderly patients [see Warnings and Precautions (5.2)].
Scopolamine transdermal system has not been studied in patients with renal or hepatic impairment. Consider more frequent monitoring during treatment with scopolamine transdermal system in patients with renal or hepatic impairment because of the increased risk of CNS adverse reactions [see Warnings and Precautions (5.2)].
Scopolamine transdermal system contains scopolamine, which is not a controlled substance.
Termination 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. These withdrawal symptoms indicate that scopolamine, like other anticholinergic drugs, may produce physical dependence. The onset of these symptoms, generally 24 hours or more after the transdermal system has been removed, can be severe and may require medical intervention [see Warnings and Precautions (5.5)].
The signs and symptoms of anticholinergic toxicity include: lethargy, somnolence, coma, confusion, agitation, hallucinations, convulsion, visual disturbance, dry flushed skin, dry mouth, decreased bowel sounds, urinary retention, tachycardia, hypertension, and supraventricular arrhythmias. These symptoms can be severe and may require medical intervention.
In cases of toxicity remove the scopolamine transdermal system. Serious symptomatic cases of overdosage involving multiple transdermal system applications and/or ingestion may be managed by initially ensuring the patient has an adequate airway and supporting respiration and circulation. This should be rapidly followed by removal of all transdermal systems from the skin and the mouth. If there is evidence of transdermal system ingestion, endoscopic removal of swallowed transdermal systems, or administration of activated charcoal should be considered, as indicated by the clinical situation. In any case where there is serious overdosage or signs of evolving acute toxicity, continuous monitoring of vital signs and ECG, establishment of intravenous access, and administration of oxygen are all recommended.
The signs and symptoms of overdose/toxicity due to scopolamine should be carefully distinguished from the occasionally observed syndrome of withdrawal [see Warnings and Precautions (5.5)]. Although mental confusion and dizziness may be observed with both acute toxicity and withdrawal, other characteristic findings differ: tachyarrhythmias, dry skin, and decreased bowel sounds suggest anticholinergic toxicity, while bradycardia, headache, nausea and abdominal cramps, and sweating suggest post-removal withdrawal.
If over-exposure occurs, call your Poison Control Center at 1-800-222-1222 for current information on the management of poisoning or overdosage.
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 1.28 mg of scopolamine base. Scopolamine is (9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4 ]nonan-7-yl) 3-hydroxy-2-phenylpropanoate. The molecular formula is C17 H21 NO4 and its structural formula is:
Scopolamine has a molecular weight of 303.35 and a pKa of 7.55 to 7.81. The scopolamine transdermal system is a circular, 0.1 mm thick, 2.13 cm2 film with two layers. Proceeding from the visible surface towards the surface attached to the skin, these layers are: (1) a backing layer composed of a tan colored, pigmented, flexible film consisting of a polyethylene outer layer and a metalized polyester inner layer; (2) an adhesive matrix of the drug substance scopolamine, acrylic adhesive solution, isopropyl myristate, and oleyl alcohol. A release liner which protects the adhesive matrix layer during storage should be removed immediately prior to application.
Cross section of the system:
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.
The system is formulated to deliver approximately 1 mg of scopolamine to the systemic circulation over 3 days.
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.
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.
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.
No long-term studies in animals have been conducted to evaluate the carcinogenic potential of scopolamine. The mutagenic potential of scopolamine has not been evaluated.
Fertility studies were performed in female rats and revealed no evidence of impaired fertility or harm to the fetus due to scopolamine hydrobromide administered by daily subcutaneous injection. Maternal body weights were reduced in the highest-dose group (plasma level approximately 500 times the level achieved in humans using a transdermal system). However, fertility studies in male animals were not performed.
In 195 adult subjects of different racial origins who participated in clinical efficacy studies at sea or in a controlled motion environment, there was a 75% reduction in the incidence of motion-induced nausea and vomiting. Scopolamine transdermal system was applied from 4 to 16 hours prior to the onset of motion in these studies.
A clinical efficacy study evaluated 168 adult female patients undergoing gynecological surgery with anesthesia and opiate analgesia. Patients received scopolamine transdermal system or placebo applied approximately 11 hours before anesthesia/opiate analgesia. No retching/vomiting during the 24-hour post-operative period was reported in 79% of those treated with scopolamine transdermal system compared to 72% of those receiving placebo. When the need for additional antiemetic medication was assessed during the same period, there was no need for medication in 89% of patients treated with scopolamine transdermal system as compared to 72% of placebo-treated patients.
Scopolamine transdermal system 1 mg/3 days is available as the following:
Carton of 4 transdermal systems, packaged into individual foil pouches. NDC 0591-2258-04
Carton of 10 transdermal systems, packaged into individual foil pouches. NDC 0591-2258-79
Carton of 24 transdermal systems, packaged into individual foil pouches. NDC 0591-2258-23
Store upright at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].
Store pouch(es) in an upright position.
Do not bend or roll pouch(es).
Wash hands thoroughly with soap and water immediately after handling the transdermal system. 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 [see Dosage and Administration (2.1), Warnings and Precautions (5.6)].
Advise the patient to read the FDA-approved patient labeling (Medication Guide and Instructions for Use).
Counsel patients on how to apply and remove the transdermal system [see Dosage and Administration (2.1)]:
- Only wear one transdermal system at any time.
- Do not cut the transdermal system.
- Apply the transdermal system to the skin in the postauricular (hairless area behind one ear) area.
- After the transdermal system is applied on the dry skin behind the ear, wash hands thoroughly with soap and water and dry hands.
- 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.
Patients with Open-Angle Glaucoma
Advise patients with open-angle glaucoma to remove the scopolamine transdermal system immediately and contact their healthcare provider if they experience symptoms of acute angle closure glaucoma, including pain and reddening of the eyes, accompanied by dilated pupils, blurred vision and/or seeing halos around lights [see Warnings and Precautions (5.1)].
Neuropsychiatric Adverse Reactions
- Advise patients that psychiatric adverse reactions may occur, especially in patients with a past psychiatric history or in those receiving other drugs also associated with psychiatric effects, and to report to their healthcare provider any new or worsening psychiatric symptoms.
- Advise patients to discontinue scopolamine transdermal system and contact a healthcare provider immediately if they experience a seizure.
- Advise patients, especially elderly patients, that cognitive impairment may occur during treatment with scopolamine transdermal system, especially in those receiving other drugs also associated with CNS effects, and to report to their healthcare provider if they develop signs or symptoms of cognitive impairment such as hallucinations, confusion or dizziness.
- 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 [see Warnings and Precautions (5.2)].
Decreased Gastrointestinal Motility and Urinary Retention
Instruct patients to remove the transdermal system if they develop symptoms of intestinal obstruction (abdominal pain, nausea or vomiting) or any difficulties in urinating [see Warnings and Precautions (5.4)].
Drug Withdrawal/Post-Removal Symptoms
Inform patients that if they remove the scopolamine transdermal system before treatment is complete, withdrawal symptoms may occur and to seek immediate medical care if they develop severe symptoms after removing scopolamine transdermal system [see Warnings and Precautions (5.5)].
Inform patients that temporary dilation of the pupils and blurred vision may occur if scopolamine transdermal system comes in contact with the eyes. Instruct patients to wash their hands thoroughly with soap and water immediately after handling the transdermal system [see Dosage and Administration (2.1), Warnings and Precautions (5.6)].
MRI Skin Burns
Instruct patients to remove the scopolamine transdermal system before undergoing an MRI [see Warnings and Precautions (5.7)].
Teva Pharmaceuticals USA, Inc.
North Wales, PA 19454
|Scopolamine (skoe pol’ a meen) Transdermal System|
Read this Medication Guide before you start using scopolamine transdermal system and each time you get a refill. There may be new information. This information does not take the place of talking to your doctor about your medical condition or your treatment.
What is scopolamine transdermal system ?
Scopolamine transdermal system is a prescription medicine used for adults to help prevent:
It is not known if scopolamine transdermal system is safe or effective in children.
Who should not use scopolamine transdermal system ?
Do not use scopolamine transdermal system if you:
What should I tell my doctor before using scopolamine transdermal system ?
Before you use scopolamine transdermal system, tell your doctor about all of your medical conditions, including if you:
Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins and herbal supplements. Scopolamine transdermal system may affect the way other medicines work, and other medicines may affect how scopolamine transdermal system works. Medicines that you take by mouth may not be absorbed well while you use scopolamine transdermal system. Especially tell your doctor if you take:
Ask your doctor if you are not sure if your medicine is one that is listed above.
Know the medicines you take. Keep a list of them and show it to your doctor or pharmacist when you get a new medicine.
How should I use scopolamine transdermal system ?
What should I avoid while using scopolamine transdermal system ?
What are the possible side effects of scopolamine transdermal system ?
Scopolamine transdermal system may cause serious side effects, including:
The most common side effects of using scopolamine transdermal system include:
| || || || |
| || || |
Tell your doctor if you have any side effect that bothers you or that does not go away. These are not all the possible side effects of scopolamine transdermal system.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
General information about the safe and effective use of scopolamine transdermal system .
Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use scopolamine transdermal system for a condition for which it was not prescribed. Do not give scopolamine transdermal system to other people, even if they have the same symptoms you have. It may harm them.
You can ask your pharmacist or doctor for information about scopolamine transdermal system that is written for health professionals.
What are the ingredients in scopolamine transdermal system ?
Active ingredient: scopolamine
Inactive ingredients: acrylic adhesive solution, isopropyl myristate, and oleyl alcohol
Teva Pharmaceuticals USA, Inc., North Wales, PA 19454
For more information, call Teva Pharmaceuticals USA, Inc. at 1-888-838-2872.
DrugInserts.com provides trustworthy package insert and label information about marketed drugs as submitted by manufacturers to the US Food and Drug Administration. Package information is not reviewed or updated separately by DrugInserts.com. Every individual package label entry contains a unique identifier which can be used to secure further details directly from the US National Institutes of Health and/or the FDA.