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Sialogogues and Antisialogogues
Sanjaya Mani Dixit
Assistant Prof of Pharmacology
Salivary stimulants
A sialogogue is a drug or substance that
increases the flow rate of saliva.
Saliva
• Saliva has a bactericidal effect, so when low
levels of it are secreted
– the risk of caries increases.
– Not only this, but fungal infections such as
oral candidiasis also can be a consequence of low
salivary flow rates.
– The buffer effect of saliva is also important,
neutralizing acids that cause tooth enamel
demineralization.
Causes of dry mouth
• Iatrogenic
– Drugs
– Irradiation
• Dehydration
• Psychogenic
• Disease
– Salivary gland disease
– Salivary aplasia (agenesis)
– Sjogren’s syndrome
– Sarcoidosis
– Cystic fibrosis
– Primary biliary cirrhosis
– Infections
• HIV
• Hepatitis C
• Human T lymphotropic virus 1 (HTLV-1)
Cevimeline
Cevimeline has a long-lasting sialogogic action and may have fewer
side effects than pilocarpine.
Cevimeline also enhances lacrimal secretions in Sjögren’s syndrome.
Mechanism of Action
• Muscarinic receptor agonist , exhibits high binding affinity for
muscarinic M3 receptors on lacrimal & salivary gland
epithelium: increases salivation
Elimination
• Half-Life: ~5 hr
• Excretion: Urine 97%; feces 0.5%
Cevimeline
Uses
• Xerostomia: Indicated for xerostomia in patients with Sjogren's syndrome
• 30 mg PO TID
A/Es
• Sweating
• Nausea
• Rhinitis
Contraindications
• Uncontrolled asthma, conditions in which miosis is undesirable (eg, narrow-
angle glaucoma, acute iritis)
• Hypersensitivity
Pilocarpine
Pilocarpine 5-10 mg dose is given three times daily
in the treatment of xerostomia.
Mechanism of Action
Cholinergic parasympathomimetic, binds with
muscarinic M3 receptors on lacrimal & salivary
gland epithelium hence increases salivation
Half-Life: 0.76-1.35 hr
Pilocarpine
Uses:
• Radiation-induced Xerostomia
• Xerostomia Associated with Sjogren's
Syndrome (An autoimmune disorder that
occurs primarily in women decreasing salivary
and lacrimal secretions)
Pilocarpine
A/Es
• Sweating (most common)
• Headache
• Flushing
• Chills
Bethanecol is oral alternative drug with less diaphoresis.
Contraindications
• Uncontrolled asthma, anterior eye inflammation, any time miosis in
undesirable (eg, narrow-angle glaucoma, acute iritis)
• Hypersensitivity
Sialogogues Uses
• In the treatment of xerostomia (the subjective
feeling of having a dry mouth)
• Radiotherapy induced xerostomia
– Pilocarpine reduces difficulty in speaking and
swallowing
• to stimulate any functioning salivary
gland tissue to produce more saliva.
• Sjogren’s syndrome- Cevimeline
Drugs causing Xerostomia
• Anticholinergic drugs
• Phenothiazines
• Clonidine
Drugs for treatment of xerostomia
• Parasympathomimetic drugs
• Pilocarpine
• Bethanecol
• Cevimeline
• Chewing gum
Antisialogogues
• A substance that reduces the salivary
secretion
• Atropine and anti-cholinergic drugs are known
to decrease salivary secretion
• Propantheline bromide, atropine substitute is
commonly used for the purpose.
Antisialogogues Uses
Sialocele
• A sialocele is a localized, subcutaneous cavity
containing saliva.
• They are a relatively common complication
following surgery to the salivary glands
commonly parotidectomy
In this case the sialocele is the result of saliva
draining out of remaining parotid tissue.
That’s All
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  • 1. Sialogogues and Antisialogogues Sanjaya Mani Dixit Assistant Prof of Pharmacology
  • 2. Salivary stimulants A sialogogue is a drug or substance that increases the flow rate of saliva.
  • 3. Saliva • Saliva has a bactericidal effect, so when low levels of it are secreted – the risk of caries increases. – Not only this, but fungal infections such as oral candidiasis also can be a consequence of low salivary flow rates. – The buffer effect of saliva is also important, neutralizing acids that cause tooth enamel demineralization.
  • 4. Causes of dry mouth • Iatrogenic – Drugs – Irradiation • Dehydration • Psychogenic • Disease – Salivary gland disease – Salivary aplasia (agenesis) – Sjogren’s syndrome – Sarcoidosis – Cystic fibrosis – Primary biliary cirrhosis – Infections • HIV • Hepatitis C • Human T lymphotropic virus 1 (HTLV-1)
  • 5. Cevimeline Cevimeline has a long-lasting sialogogic action and may have fewer side effects than pilocarpine. Cevimeline also enhances lacrimal secretions in Sjögren’s syndrome. Mechanism of Action • Muscarinic receptor agonist , exhibits high binding affinity for muscarinic M3 receptors on lacrimal & salivary gland epithelium: increases salivation Elimination • Half-Life: ~5 hr • Excretion: Urine 97%; feces 0.5%
  • 6. Cevimeline Uses • Xerostomia: Indicated for xerostomia in patients with Sjogren's syndrome • 30 mg PO TID A/Es • Sweating • Nausea • Rhinitis Contraindications • Uncontrolled asthma, conditions in which miosis is undesirable (eg, narrow- angle glaucoma, acute iritis) • Hypersensitivity
  • 7. Pilocarpine Pilocarpine 5-10 mg dose is given three times daily in the treatment of xerostomia. Mechanism of Action Cholinergic parasympathomimetic, binds with muscarinic M3 receptors on lacrimal & salivary gland epithelium hence increases salivation Half-Life: 0.76-1.35 hr
  • 8. Pilocarpine Uses: • Radiation-induced Xerostomia • Xerostomia Associated with Sjogren's Syndrome (An autoimmune disorder that occurs primarily in women decreasing salivary and lacrimal secretions)
  • 9. Pilocarpine A/Es • Sweating (most common) • Headache • Flushing • Chills Bethanecol is oral alternative drug with less diaphoresis. Contraindications • Uncontrolled asthma, anterior eye inflammation, any time miosis in undesirable (eg, narrow-angle glaucoma, acute iritis) • Hypersensitivity
  • 10. Sialogogues Uses • In the treatment of xerostomia (the subjective feeling of having a dry mouth) • Radiotherapy induced xerostomia – Pilocarpine reduces difficulty in speaking and swallowing • to stimulate any functioning salivary gland tissue to produce more saliva. • Sjogren’s syndrome- Cevimeline
  • 11. Drugs causing Xerostomia • Anticholinergic drugs • Phenothiazines • Clonidine
  • 12. Drugs for treatment of xerostomia • Parasympathomimetic drugs • Pilocarpine • Bethanecol • Cevimeline • Chewing gum
  • 13. Antisialogogues • A substance that reduces the salivary secretion • Atropine and anti-cholinergic drugs are known to decrease salivary secretion • Propantheline bromide, atropine substitute is commonly used for the purpose.
  • 14. Antisialogogues Uses Sialocele • A sialocele is a localized, subcutaneous cavity containing saliva. • They are a relatively common complication following surgery to the salivary glands commonly parotidectomy In this case the sialocele is the result of saliva draining out of remaining parotid tissue.