PHARM: Drugs Affecting Salivary Flow Flashcards
For what type of pills should you: put capsule on tongue, medium sip of water (no swallowing), bend head forward by tilting chin toward chest, swallow capsule and water with head bent forward.
Floating pills
For what type of pills should you: put pill on back of tongue then seal mouth around water bottle and swallow water/ pill together
sinking pills
Which antihistamines cause xerostomia?
diphenhydramine
chlorpheniramine
Which decongestants cause xerostomia?
pseudoephedrine
Which antidepressants cause xerostomia?
amitryptiline
Which antipsychotics cause xerostomia?
Haloperidol
Phenothiazine derivatives
Which antihypertensives cause xerostomia?
Reserpine Methyldopa Cholorthiazidine Furosemide Metoprolol CCGs
Which anticholinergics cause xerostomia?
atropine
scopolamine
What are two mays to treat xerostomia?
Parasympatheticomimetics
Saliva substitutes
Are salliva substitutes effective?
no strong evidence these are effective (gum may be preferred in patients with residual secretory capacity)
What is the auto-immune disease that causes destruction of salivary glands?
Sjogren syndrome
How do you treat Sjogren’s?
DMARDs (to suppress the immune system)
What receptors control salivary secretion?
M3 or M2
What neurotransmitter stimulates M3 or M2 to stimulate salivary secreiton?
acetylcholine
Binding of Ach to M3 or M3 receptor causes what?
upregulation of PLC to generate IP3 (binds to and opens IP3 receptor on ER and leads to release of calcium)
What does the initial increased calcium from M3 receptor binding lead to?
stimulation of calcium induced calcium release via IP3 receptor and ryanodine receptor (cyclic ADP ribose)
How does increasing intracellular calcium lead to salivation?
increased intracellular Ca2+ activates the apical membrane Cl- channel and the basolateral K+ channel (flow of Cl- into acinar lumen draws Na+ and water across)
How do non-innervated M3 receptors at salivary gland blood vessels get activated?
exogenously added muscarinic agonists
What is the result of activation of non-innervated M3 receptors at salivary gland blood vessels?
dilation of salivary gland blood vessels (via NO release)
Which type of innervation effects the M3 receptors at the salivary glands?
parasympathetic nervous system
What type of saliva is produced by parasympathetic innervation?
copious but protein poor
True or false: saliva can be modified by sympathetic signals.
TRUE
How does activation of alpha-1 receptors affect salivation?
increased salivary gland secretions and constriction of salivary gland blood vessels
How does activation of alpha-2 receptors affect salivation?
only causes constriction of salivary gland blood vessels.
What type of saliva is produced by sympathetic innervation?
sparse but protein rich
What drug is notable for having muscarinic receptor selectivity (high binding affinity for M3 receptors on lacrimal and salivary gland epithelium)?
cevimeline
What other type of receptor is affected by cevimeline?
partial direct M1-receptor agonist activity in the CNS
Which drug interacts with ALL muscarinic receptors? What is the consequence of this?
Pilocarpine (has greater CNS activity and may lead to psychosis)
What are the contraindications to using cevimeline and pilocarpine?
Asthma, closed angle glaucoma, iritis
List come conditions that should raise caution when using cevimeline and pilocarpine.
Angina Use of beta-blockers Cardiac arrhythmias MI Bronchitis COPD Age extremes: children, geriatric Breast-feeding Pregnancy Reduced visual acuity (not for people who need to drive)
What drug is a free-radical scavenger that can be used for radioprotection to the head and neck when the parotid gland receives intense radiation?
amifostine
What does amifostine prevent?
reduces acute and chronic xerostomia from radiation while preserving anti-tumor effects
List 3 drugs used to treat hypersalivation (sialorrhea)?
- Oral anti-cholinergics (ex. glycopyrrolate)
- Botox injections
- Scopolamine
Which type of drug are used to prevent bronchial secretions and salivation prior to surgery?
Scopolamine
Which drug is used in some neurologic conditions (ex. Cerebral palsy) that feature hypersalivation?
Oral Anticholinergics
