Drugs affecting salivary flow Flashcards Preview

GI Liver Pharmacology > Drugs affecting salivary flow > Flashcards

Flashcards in Drugs affecting salivary flow Deck (25):
1

Acetylcholine (ACh) binds to the

G protein–linked M3 muscarinic ACh receptor

2

G protein–linked M3 muscarinic ACh receptor which
causes

phospholipase C to generate
inositol 1,4,5-trisphosphate (InP3)

3

InP3 binds to & opens the

InP3 receptor on the endoplasmic reticulum,

4

InP3 receptor on the endoplasmic reticulum, which releases

Ca2+

5

This release of Ca2+ stimulates

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

6

Increased Ca2+ activates the apical membrane

Cl channel

7

Increased Ca2+ activates the basolateral membrane

K+ channel.

8

Efflux of Cl- into the acinar lumen draws

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

9

Parasympathetic activity evokes a copious secretion

relatively poor in protein

10

sympathetic innervation evokes sparse

protein-rich saliva.

11

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

neuropeptides, such as vasoactive intestinal peptide (VIP)

12

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

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

13

Systemic Rx: Muscarinic Agonists

Cevimeline & Pilocarpine

14

Cevimeline
Dose
[Metab]

PO
CYP3A3/4, 2D6
Interactions possible

15

Cevimeline
Receptor

M3>>M1

16

Cevimeline
Contraindicated:

asthma, closed angle glaucoma or iritis

17

Cevimeline
Precautions:

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)

18

Pilocarpine
Dose

PO

19

Pilocarpine
Receptor

All muscarinic receptors

20

Pilocarpine
Contraindicated:

asthma, closed angle glaucoma or iritis

21

Pilocarpine
Precautions:

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

22

Cevimeline or pilocarpine should be administered with

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

23

Amifostine was shown to be a

Radioprotector in Head & Neck Cancer

24

Amifostine reduced

acute & chronic xerostomia. Antitumor treatment efficacy was preserved.

25

Amifostine mechanism.

Works as ROS.