Transdermal patches scopolamine

CNS damping effects. Scopolamine is effective in the prophylaxis ofkinetosis (motion sickness, sea sickness, see p.342) it is mostly applied by a transdermal patch. Scopolamine (pJCa = 7.2) penetrates the blood-brain barrier faster than does atropine (p/Ca = 9), because at physiological pH a larger proportion is present in the neutral, membrane-permeant form. 

These include atropine, scopolamine (hyoscine), trihexyphenidyl (benzhexol) and benzatropine. They block central muscarinic receptors involved in various afferent pathways of the vomiting reflex (Fig. 1). They have been used to control motion sickness, emesis in Meniere s disease and postoperative vomiting. Currently, hyoscine is largely restricted to the treatment of motion sickness where it has a fast onset of action but a short duration (4-6 h). Administration of hyoscine by transdermal patch produces a prolonged, low-level release of the drug with minimal side effects. To control postoperative vomiting, it should be applied >8 h before emesis is anticipated. 

Certain plants of the family Solanaceae, such as Atropa belladonna L., Hyoscyamus niger L., and Datura stramonium L., have been used medicinally for centuries in Europe because they contain tropane-type alkaloids.For example, atropine (1) [a racemic mixture of (+)- and (—)-hyoscyamine (2)] and (-)-hyoscyamine are competitive antagonists at the muscarinic acetylcholine receptor site, leading to antispasmodic and antiallergic effects. Scopolamine [(—)-hyoscine)] (3) is used in a transdermal patch for the prevention of motion sickness. Since these tropane alkaloids penetrate the blood-brain barrier, they also have psychoactive effects. ... 

Scopolamine inhibits excessive motility and hypertonus of the Gl tract in irritable colon syndrome, mild dysentery, diverticulitis, pylorospasm, and cardiospasm. Transdermal patch Prevention of nausea and vomiting associated with motion sickness and recovery from anesthesia and surgery in adults. 

Applied to the skin in a transdermal patch (transdermal therapeutic delivery system), this drug is used to prevent or reduce the occurrence of nausea and vomiting that are associated "with motion sickness. Diphenhydramine Chlorpromazine Ondansetron Dimenhydrinate Scopolamine... 

Certain vestibular disorders respond to antimuscarinic drugs (and to antihistaminic agents with antimuscarinic effects). Scopolamine is one of the oldest remedies for seasickness and is as effective as any more recently introduced agent. It can be given by injection or by mouth or as a transdermal patch. The patch formulation produces significant blood levels over 48-72 hours. Useful doses by any route usually cause significant sedation and dry mouth. 

Scopolamine Unknown mechanism in CNS Reduces vertigo, postoperative nausea Prevention of motion sickness and postoperative nausea and vomiting Transdermal patch used for motion sickness IM injection for postoperative use Toxicity Tachycardia, blurred vision, xerostomia, delirium Interactions With other antimuscarinics... 

Hyoscine (scopolamine), a prototypic muscarinic receptor antagonist, is one of the best agents for the prevention of motion sickness. However, it has a very high incidence of anticholinergic effects when given orally or parenterally. It is better tolerated as a transdermal patch. Superiority to dimenhydrinate has not been proved. 

In 1978 Tranderm Scop was the first transdermal patch to receive FDA approval. Scopolamine, the active ingredient, is a belladonna alkaloid that is frequently used to treat motion sickness and nausea resulting from anesthetics and analgesics. Transderm Scop is a membrane-moderated patch that has a three-day life span. It has a circular shape with an area (2.5 cm2) approximately the size of a quarter [26]. 

Transdermal patches are marketed worldwide with the drug substances glycerole trinitrate, estradiol, testosterone, clonidine, scopolamine, fentanyl and nicotine, respectively. The patch has to remain for up to one week at the appropiate body site. In this case the drug amount in the reservoir is rather high. As liquid crystalline vehicles with lamellar microstructure have... 

Anesthesiologists appreciate the fact that individuals who experience motion sickness are also at risk of having postoperative nausea and vomiting that may persist for days after surgery. Application of a scopolamine transdermal patch behind the ear for 3 days beyond surgery may serve as a useful adjunct to antiemetic therapy and eradicate this problem (11). 

Transderm-Scop Patch scopolamine Tridol tramadol... 

Transderm Scop (scopolamine) 2-day patch for prevention of nausea and vomiting associated with motion sickness. 

Scopolamine (Transderm Scop) 0.5 mg every 72 h prn Transdermal patch Rx... 

The most commonly used muscarinic receptor antagonist is scopolamine (hyoscine), which usually is administered as the free base in the form of a transdermal patch (transdee(M-scop). Its principal utility is in the prevention and treatment of motion sickness, although it also has some activity in postoperative nausea and vomiting. In general, anticholinergic agents have no role in chemotherapy-induced nausea. 

CNS Scopolamine is standard therapy for motion sickness this drug is one of the most effective agents available for this condition. A transdermal patch formulation is available. Benztropine, biperiden. and trihexyphenidyl are representative of several antimuscarinic agents used in parkinsonism. Although not as effective as levodopa (see Chapter 28), these agents may be useful as adjuncts or when patients become unresponsive to levodopa. Benztropine is sometimes used parenterally to treat acute dystonias caused by antipsychotic medications. 

Transdermal patches registered at present are patches containing active substances such as buprenorphine, estradiol, fentanyl, glyceryl trinitrate, nicotine, oxybutynine, rivastigmine, rotigotine and scopolamine. These transdermal patches are used in the treatment of a variety of diseases. They release the active substance during a period of 24 up to 72 h, depending on the type of patch used and the active substance. After application of the patch plasma concentration slowly rises until a steady concentration is reached. 

Holland MS. (1992). Central anticholinergic syndrome in a pediatric patient following transdermal scopolamine patch placement. Nurse Anesth. 3(3) 121-24. 

Parrott AC. (1987). Transdermal scopolamine effects of single and repeated patches upon psychological task performance. Neuropsychobiology. 17(1-2) 53-59. 

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