Anticholinergics
Product name: Sal-Tropine
Manufacturer: Hope Pharmaceuticals, 8260 East Gelding Drive, Suite 104, Scottsdale, Ariz. 85260; 1-800-755-9595; "www.hopepharm.com"
ADA Acceptance: Received ADA Seal of Acceptance in 1995
Other ADA-Accepted products in this category:
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Description:
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Excessive salivation can complicate dental procedures such as taking impressions, lower arch surgery and placing restorations. Anticholinergic drugs are effective antisialogogues that can be used for reducing normal salivation during intraoral procedures. Sal-Tropine, atropine sulfate, is one such anticholinergic that is indicated for reduction of salivation and bronchial secretions and is the first anti-cholinergic marketed specifically for dentistry. Atropine is contraindicated in patients with glaucoma, synechiae (adhesions between the iris and lens of the eye) and asthma.
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Dosage:
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Atropine is usually the anticholinergic of choice for most uses in dentistry. The usual oral dose to control salivation in adults is 0.4 milligrams. In children, the dose is weight-dependent: 7–16 pounds, 0.1 mg; 17–24 lbs, 0.15 mg; 24–40 lbs, 0.2 mg; 40–65 lbs, 0.3 mg; 65–90 lbs, 0.4 mg. A low dose may be sufficient to achieve moderation of salivation; however, a larger dose may be necessary if secretions are preventing the successful accomplishment of a procedure. Reduced doses are indicated for geriatric patients and those with medical conditions that may alter their response to anticholinergics. Doses of 0.5 to 1.0 mg of atropine can be mildly stimulating to the central nervous system. Sal-Tropine comes in 0.4-mg tablets. The recommended dose is one tablet per 75 lbs body weight. Patients should take a dose of medication an hour prior to their appointment on an empty stomach. To facilitate dosing in children, the tablet is tasteless and water soluble.
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Consideration for Acceptance:
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Sal-Tropine is approved by the U.S. Food and Drug Administration. Control of salivation for dental procedures is a generally recognized indication for anticholinergics. The Council on Scientific Affairs evaluated the safety and effectiveness of Sal-Tropine for dentistry.
Pharmacokinetics
| Drug |
Time of onset (min) |
Duration of effect (h) |
Amine structure |
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| Atropine |
30-60 |
4-6 |
Tertiary |
| Scopolamine |
30-60 |
4-6 |
Tertiary |
| Glycopyrrolate |
30-45 |
8-12 |
Quaternary |
| Methantheline |
30-45 |
6 |
Quaternary |
| Propantheline |
30-45 |
6 |
Quaternary |
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Drug Interactions:
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Avoid administration within two to three hours of ingestion of antacids or absorbent antidiarrheal drugs, which may impair absorption of atropine. Atropine sulfate slows gastric emptying and, therefore, may interfere with the absorption of other medications. Patients taking ketoconazole should wait at least two hours before taking atropine. Use cautiously when the patient is taking antimyasthenics, central nervous system, or CNS, depressants, metoclopramide, opioid analgesics and drugs with anticholinergic side effects (such as antiparkinsonism drugs, antipsychotic agents, carbamazepine, digoxin, dronabinol, orphenadrine, procainamide, quinidine, sedative antihistamines, tricyclic antidepressants). Avoid concurrent use with potassium chloride. Cross-sensitivity may exist with belladonna alkaloids and methantheline. Atropine should not be given during pregnancy. Tertiary amines cross the blood-brain barrier and, therefore, will cause CNS effects, unlike quaternary amines. Scopolamine produces CNS depression, unlike atropine and the quaternary amines. Atropine and scopolamine are well-absorbed from the gastrointestinal tract, whereas the quaternary amines are less well-absorbed.
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Dose Response:
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0.5 mg–Slight dryness of the nose and mouth; bradycardia.
1.0 mg–Increased dryness of the nose and mouth, bradycardia, then tachycardia, and slight mydriasis.
2.0 mg–Very dry mouth, tachycardia with palpitations, mydriasis, slight blurring of vision, flushed and dry skin.
5.0 mg–Increase in above symptoms plus disturbance of speech, difficulty swallowing, headache, hot and dry skin, restlessness with asthenia.
10.0 mg or more–Increase in above symptoms plus ataxia, excitement, disorientation, hallucinations, delirium, coma.
Hyperthermia can develop in children due to inhibition of heat loss through evaporation, particularly when they are overdressed, physically active or in a warm environment.
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Benefits of Use:
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Improves success of some dental procedures such as bonding, bridge and crown cementation, impression-taking, operative dental procedures, orthodontic bracketing, periodontal procedures, prosthetics, restoration procedures, sealants and radiographic procedures when a dry field is important.
Facts about salivation
Salivary glands are under parasympathetic and sympathetic control. Parasympathetic innervation controls most of the flow of saliva, while sympathetic innervation modulates the composition of the saliva.1 Hypersalivation can result from increased parasympathetic input, as may be the case with the enhanced salivation that results from clozapine antipsychotic therapy.2,3 Enhanced salivation also can result from gastroesophageal reflux and oral infections.4 Hypersalivation normally is compensated for by increased swallowing; however, pharmacological intervention may be appropriate. In the case of gastroesophageal reflux and infection, treatment of the underlying disorder normally resolves the hypersalivation. Hypersalivation, also known as sialorrhea or ptyalism, is a term often used interchangeably with "drooling," even though these conditions have different etiologies.
Drooling is the result of a centrally or peripherally mediated disturbance in the muscular control required for swallowing and lip closure. The medical conditions that cause drooling include cerebral palsy, motor neuron damage, cerebrovascular accidents, Parkinsonism, congenital suprabulbar palsy, major resection of the oropharynx, Down syndrome and amyotrophic lateral sclerosis.5 Drooling can cause significant problems for the affected people and for their caretakers; consider that approximately 640 milliliters of saliva are produced in 24 hours. The most obvious is the psychosocial effect, but physical effects are also significant and include chronic irritation of the skin in contact with the saliva, increased perioral infections and dehydration.
Drooling can be treated with oral appliances, biofeedback, physiotherapy, drugs and, as a last resort, surgery. Oral appliances are used to correct the positioning of the tongue, lips and chin.6 Biofeedback and physiotherapy have been used with these appliances, or alone, to make affected people aware of their drooling and tongue position, and to encourage them to close their mouths and swallow.5
The drugs used to treat drooling and hypersalivation are of the anticholinergic class: glycopyrrolate, scopolamine and atropine. Glycopyrrolate does not cross the blood-brain barrier and, therefore, does not produce central effects. Glycopyrrolate has been used to treat chronic drooling, though not without side effects that often lead to discontinuation of therapy.7–9 Scopolamine is available as a transdermal patch that commonly is used for motion sickness. These patches can be useful to treat chronic drooling and hypersalivation; however, scopolamine, unlike the other anticholinergics, produces central nervous system depression. For controlling saliva for shorter periods, such as dental procedures, atropine is the drug of choice because of its effectiveness and shorter duration of action (as described on p. 1021). Surgical procedures aim to reduce the amount of saliva produced or redirect the flow of saliva.5 Reducing the amount of saliva is accomplished by selectively cutting part of the parasympathetic supply to the salivary glands. Redirection of salivary flow is accomplished by repositioning of the salivary duct to circumvent the swallowing defect. Excision of the salivary gland or ligation of the salivary duct will completely stop salivary flow at the surgical site. Recently, reports of the use of botulinum toxin A to control drooling have been published, showing that intraparotid injections of botulinum toxin A successfully treated drooling by interfering with neurotransmission at the salivary gland.10–14
Clinicians should take a multidisciplinary approach to the treatment of drooling and hypersalivation, with the dentist as an integral member of the team. The oral manifestations of these conditions should be considered, particularly because some of the treatments described can lead to xerostomia or hyposalivation. Xerostomia introduces many challenges to maintaining oral health, such as an increase in caries and a decline in dietary nutrition. The dentist can devise a plan for maintaining oral health in such people by providing treatment options such as fluoride, regular cleanings, fissure sealants and saliva substitutes.
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REFERENCES
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- Sturdevant CM, ed. The art and science of operative dentistry. 2nd ed. St. Louis: C.V. Mosby; 1985.
- Miller DD. Review and management of clozapine side effects. J Clin Psychiatry 2000;61(suppl 8):14–7.
- Davydov L, Botts SR. Clozapine-induced hypersalivation. Ann Pharmacother 2000;34(5):662–5.[Abstract]
- Mandel L, Tamari K. Sialorrhea and gastroesophageal reflux. JADA 1995;126:1537–41.
- Hussein I, Kershaw AE, Tahmassebi JF, Fayle SA. The management of drooling in children and patients with mental and physical disabilities: a literature review. Int J Paediatr Dent 1998;8:3–11.[Medline]
- Nunn JH. Drooling: review of the literature and proposals for management. J Oral Rehabil 2000;27:735–43.[Medline]
- Blasco PA, Stansbury JC. Glycopyrrolate treatment of chronic drooling. Arch Pediatr Adolesc Med 1996;150(9):932–5.[Abstract]
- Mier RJ, Bachrach SJ, Lakin RC, Barker T, Childs J, Moran M. Treatment of sialorrhea with glycopyrrolate: a double-blind, dose-ranging study. Arch Pediatr Adolesc Med 2000;154(12):1214–8.[Abstract/Free Full Text]
- Neverlien PO, Sorumshagen L, Eriksen T, Grinna T, Kvalshaugen H, Lind AB. Glycopyrrolate treatment of drooling in an adult male patient with cerebral palsy. Clin Exp Pharmacol Physiol 2000;27(4):320–2.[Medline]
- Jost WH. Treatment of drooling in Parkinson’s disease with botulinum toxin. Mov Disord 1999;14(6):1057.[Medline]
- Bhatia KP, Munchau A, Brown P. Botulinum toxin is a useful treatment in excessive drooling in saliva. J Neurol Neuro-surg Psychiatry 1999;67(5):697.[Free Full Text]
- Pal PK, Calne DB, Calne S, Tsui JK. Botulinum toxin A as treatment for drooling saliva in PD. Neurol 2000;54(1):244–7.[Abstract/Free Full Text]
- O’Sullivan JD, Bhatia KP, Lees AJ. Botulinum toxin A as treatment for drooling saliva in PD. Neurol 2000;55(4):606–7.[Free Full Text]
- Giess R, Naumann M, Werner E, et al. Injections of botulinum toxin A into the salivary glands improve sialorrhoea in amyotrophic lateral sclerosis. J Neurol Neurosurg Psychiatry 2000;69(1):121–3.[Abstract/Free Full Text]
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