Drugs affecting salivary flow

Question 1

Acetylcholine (ACh) binds to the

Answer 1

G protein–linked M3 muscarinic ACh receptor

Question 2

G protein–linked M3 muscarinic ACh receptor which

causes

Answer 2

phospholipase C to generate

inositol 1,4,5-trisphosphate (InP3)

Question 3

InP3 binds to & opens the

Answer 3

InP3 receptor on the endoplasmic reticulum,

Question 4

InP3 receptor on the endoplasmic reticulum, which releases

Answer 4

Ca2+

Question 5

This release of Ca2+ stimulates

Answer 5

Ca2+ induced Ca2+ release via the InP3 receptor & the ryanodine receptor.

Question 6

Increased Ca2+ activates the apical membrane

Answer 6

Cl channel

Question 7

Increased Ca2+ activates the basolateral membrane

Answer 7

K+ channel.

Question 8

Efflux of Cl- into the acinar lumen draws

Answer 8

Na+ across the cells, & the osmotic gradient generates fluid secretion.

Question 9

Parasympathetic activity evokes a copious secretion

Answer 9

relatively poor in protein

Question 10

sympathetic innervation evokes sparse

Answer 10

protein-rich saliva.

Question 11

Secretion & blood flow are thus controlled by acetylcholine & noradrenaline but are also regulated by

Answer 11

neuropeptides, such as vasoactive intestinal peptide (VIP)

Question 12

The glands themselves produce vasodilatory substances, including kallikrein, which causes

Answer 12

an increase in local levels of bradykinin, blood flow increases over resting levels.

Question 13

Systemic Rx: Muscarinic Agonists

Answer 13

Cevimeline & Pilocarpine

Question 14

Cevimeline
Dose
[Metab]

Answer 14

PO
CYP3A3/4, 2D6
Interactions possible

Question 15

Cevimeline

Receptor

Answer 15

M3»M1

Question 16

Cevimeline

Contraindicated:

Answer 16

asthma, closed angle glaucoma or iritis

Question 17

Cevimeline

Precautions:

Answer 17

angina, breast-feeding, bronchitis, cardiac arrhythmias, cardiac disease, children, cholelithiasis, COPD, driving or operating machinery (“ visual acuity), geriatric, myocardial infarction, nephrolithiasis, pregnancy
(HEART, LUNG, EYES, & BABY/MOM)

Question 18

Pilocarpine

Dose

Answer 18

PO

Question 19

Pilocarpine

Receptor

Answer 19

All muscarinic receptors

Question 20

Pilocarpine

Contraindicated:

Answer 20

asthma, closed angle glaucoma or iritis

Question 21

Pilocarpine

Precautions:

Answer 21

angina, breast-feeding, bronchitis, cardiac arrhythmias, cardiac disease, children, cholelithiasis, COPD, driving or operating machinery (“ visual acuity), geriatric, myocardial infarction, nephrolithiasis, pregnancy
(HEART, LUNG, EYES, & BABY/MOM)
plus psychosis, owing to greater CNS activity

Question 22

Cevimeline or pilocarpine should be administered with

Answer 22

caution in patients taking β-blockers because of the possibility of cardiac conduction disturbances.

Question 23

Amifostine was shown to be a

Answer 23

Radioprotector in Head & Neck Cancer

Question 24

Amifostine reduced

Answer 24

acute & chronic xerostomia. Antitumor treatment efficacy was preserved.

Question 25

Amifostine mechanism.

Answer 25

Works as ROS.