ANS 2 Flashcards by Anna Dunlop

what are the effects of anticholinesterases on the ANS?

Salivation
Lacrimation
Urination
Defecation
Gastrointestinal upset
Emesis

Bradycardia
Bronchoconstriction
Hypotension
Pupillary constriction (miosis)

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what are predominate locations of nicotinic Ach receptors?

NMJ
sympathetic ganglia
parasympathetic ganglia
CNS

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what are predominate locations of muscarinic Ach receptors?

parasympathetic target organs
sweat glands (sympathetic)
vascular smooth muscle
CNS

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which agonists have specificity with muscarinic receptors?

acetylcholine
muscarine
bethanechol
pilocarpine

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which agonists have specificity with nicotinic receptors?

achetylcholine

- nicotine

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which agonists do nicotinic and muscarinic Ach receptors share?

achetylcholine

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what are the 3 classes of muscarinic Ach receptors?

M1 (neural)
M2 (cardiac)
M3 (glandular/smooth muscle)

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what are the main locations of M1 (neural) Ach receptors?

autonomic ganglia glands:

gastric
salivary
lacrimal

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what are the main locations of M2 (cardiac) Ach receptors?

heart

- atria

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what are the main locations of M3 (glandular/smooth muscle) Ach receptors?

exocrine glands:

gastric
salivary

smooth muscle:

GI tract
eye
airways
bladder

blood vessels:
- endothelium

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what is the cellular response of M1 Ach receptors?

↑ IP3, DAG

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what is the cellular response of M2 Ach receptors?

↓ cAMP

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what is the cellular response of M3 Ach receptors?

↑ IP3, DAG

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what is the functional response of M1 Ach receptors?

gastric secretion

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what is the functional response of M2 Ach receptors?

cardiac inhibition

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what is the functional response of M3 Ach receptors?

gastric, salivary secretion
GI smooth muscle contraction
ocular accommodation
vasodilation

what are the pharmacological properties of pilocarpine?

non-selective muscarinic agonist

what are clinical uses of pilocarpine?

constriction of pupils (miosis)
glaucoma (to decrease IOP)
xerostomia (following head/neck radiotherapy)

what are the pharmacological properties of bethanechol?

non-selective muscarinic agonist

what are the pharmacological properties of atropine?

non-selective agonist
well absorbed orally
CNS effects

what type of receptor is a muscarinic receptor?

g-protein linked receptor (metabotropic)

what type of receptor is an nicotinic receptor?

ionotropic

what does acetylcholine have receptor specificity for?

muscarinic and nicotinic

what does nicotine have receptor specificity for?

nicotinic

what does muscarine have receptor specificity for?

muscarinic

what does bethanechol have receptor specificity for?

muscarinic

what does pilocarpine have receptor specificity for?

muscarinic

what are the clinical uses of bethanechol?

bladder and gastrointestinal hypotonia

what are the clinical uses for atropine?

- adjunct for anaesthesia - anticholinesterase poisoning - bradycardia/cardiac arrest

what are the pharmacological properties of glycopyrronium?

similar to atropine: - non-selective agonist - wel absorbed orally - CNS effects - does not cross blood brain barrier

what are the clinical uses of glycopyrronium?

- adjunct for anaesthesia - anticholinesterase poisoning - bradycardia/cardiac arrest

what are the pharmacological properties of hyoscine hydrobromide?

similar to atropine: - non-selective agonist - wel absorbed orally - CNS effects

what are the clinical uses of hyoscine hydrobromide?

- hypersalivation | - motion sickness

what are the pharmacological properties of ipratropium?

- delivered via inhaler or nebuliser | - does not cross blood brain barrier

what are the clinical uses of ipratropium?

maintenance treatment of COPD

what are pharmacological properties of tropicamide?

similar to atropine but shorter acting: - non-selective agonist - well absorbed orally - CNS effects

what are clinical uses of tropicamide?

opthalmic use (mydriasis)

why is there little therapeutic uses for agonists?

very few diseases of decreasing parasympathetic activity, more due to increasing activity

what are the general problems of selectivity with antagonists?

- few differentiate between subtypes effectively - muscarinic ACh receptors widespread; side effects - control by route of administration and distribution