Cahpter 19- cholinergic agonists and anticholinergics

Cholinergics

Drugs that stimulate parasympathetic nervous system (PNS).
Mimic parasympathetic neurotransmitter acetylcholine

Muscarinic recpetors (cholinergic)

stimulate smooth muscle and slow the heart rate

Nicotinic receptors (cholinergic)

(neuromuscular) affect the skeletal muscles

Why are many cholinergic agonists nonselective?

They can affect both the muscarinic and nicotinic receptors

Effects of cholinergics on eye

constrict pupil

Effects of cholinergics on lungs

constrict bronchioles and increase secretions

Effects of cholinergics on heart

decreased heart rate, blood vessels dilate

Effects of cholinergis on GI

increase peristalis and secretions, relax sphincters, cause urination

Effects of cholinergics on bladder

muscles contract

Effects of cholinergics on salivary glands

increased salivation

direct acting cholinergics

Selective to muscarinic receptors, nonspecific because muscarinic receptors are located in smooth muscles
Heart, GI, GU, glands

Bethanechol Chloride (Urecholine)

direct acting cholinergic agonist, acts on the muscarinic receptor, primarily used to increase urination

Metoclopramide HCL (Reglan)

direct acting cholinergic agonist, used to treat GERD

Metoclopramide

direct acting cholinergic agonist, increases gastric emptying time

Indirect acting cholinergic agonists

dont act on receptors, inhibit or activate the enzyme cholinesterase, permitting acetylcholine to accumulate at the receptor sites

Pilocarpine (Pilocar)

direct acting cholinergic, constricts pupils

Functions of indirect acting cholinergics

Break down cholinesterase enzyme into choline and acetic acid, Allow Ach to activate muscarinic and nicotinic cholinergic receptors

Effects of indirect acting cholinergics

Stimulate skeletal muscles, increase tone GI motility, bradycardia, miosis. Bronchial constriction, promote urination

Side effects of indirect acting cholinergics

bradycardia, asthma, peptic ulcers

Contradictions of indirect acting cholinergics

intestinal and urinary obstruction

Primary use of indirect acting cholinergics

treat myasthenia gravis, glaucoma, alzheimers, muscarinic antagonist poisoning

Use of Reversible cholinesterase inhibitors

Pupil constriction in glaucoma
Increase muscle strength in myasthenia gravis

Side effects of Reversible cholinesterase inhibitors

Muscle cramps, twitching, bradycardia, increase bronchial secretions

Anticholinergics

inhibit actions of acetylcholine by occupying the acetylcholine receptors

Effects of Anticholinergic drugs on heart

large doses increase P; small doses decrease P

Effects of Anticholinergic drugs on lungs

bronchodilation, decrease secretions

Effects of Anticholinergic drugs on GI

Relax smooth muscle tone, decrease motility and peristalsis, decrease secretions

Effects of Anticholinergic drugs on urinary tract

Relax detrusor muscle, increase sphincter constriction

Effects of Anticholinergic drugs on eyes

dilate pupils, decrease accommodation

Effects of Anticholinergic drugs on glands

decrease salivation, perspiration

Effects of Anticholinergic drugs on CNS

decrease tremors and rigidity of muscles. Drowsiness, disorientation, and hallucinations can result from large doses

Atropine (anticholinergic) action

Increase P, decrease motility and peristalsis, decrease salivary secretions
-Contraindicated in glaucoma

Atropine side effects

Tachycardia, palpitations, nasal congestion, flushing, photophobia, blurred vision, dry mouth and skin, abdominal distention, urinary retention, impotence

Atropine nursing interventions

Monitor vital signs, urine output, bowel sounds
Safety: use bedside rails, caution against driving motor vehicles
Provide mouth care and eye drops
Avoid hot environments
Avoid alcohol, cigarettes, caffeine, and aspirin at bedtime
Warn to wear sunglasses i

Antihistamines

Treats motion sickness
Scopolamine (Transderm Sc?p)
Dimenhydrinate (Dramamine)
Donepezil (Aricept)
AChE inhibitor - Alzheimer's disese

Antihistamine side effects

Dry mouth, visual disturbances, constipation, urinary retention, flushing, muscle weakness, tachycardia, hypotension

What is used for motion sickness?

anticholinergics ex)scopolamine

What is used for antiparkinsons?

trihexphenidyl HCl (cogentin)
biperiden lactate (akineton)
benzotropine

Atropine?

anticholinergic for IBS

nicotinic

parasympathetic targets, fast postsynaptic response

M1 - muscarinic

smooth muscles, glands of the gut-contraction and glandular secretion, slow

M2

smooth and cardiac muscles of cardiovascular system, contraction, intropic on cardiac muscle

M3

smooth muscles and glands, contraction and glandular secretion