Pharm II Cholinergic Drug Chapter

Cholinergic drugs mimic what system?

Parasympathetic

Sympathetic system effects ?

Eyes: pupils dilate, IOP increase
Heart: HR increase, BP increase
Lungs: Bronchial tubes dilate
GI Tract: decreases secretions
Bladder: slows down
skeletal muscle: contracts

Parasympathetic system effects?

eyes constrict, IOP decrease

HR and BP decrease

Bronchoconstriction and increased lung secretion

increased GI motility and secretions

contracts the bladder and relaxes the urinary sphincter

What patients are adrenergic drugs not good for?

glaucoma patients

what patients are cholinergic drugs not good for?

asthma, COPD, Ulcer patients

what patients are cholinergic drugs good for?

constipation and urinary retention

what's the neurotransmitter for the parasympathetic system?

acetylcholine

what are the two receptors of the parasympathetic system?

Nicotinic and Muscarinic

Nicotinic effects skeletal muscles, muscarinic stimulates smooth muscle and slow heart rate

What are the two types of cholinergic drug agonists?

direct acting (stimulates the receptor) and indirect acting (breaks down acetylcholine

Bethanechol (Urecholine) direct-acting indications?

post-operative and postpartum non-obstructive urinary retention

management of urinary retention associated with neurogenic atony of the bladder

Prevent and treat adverse effects of other drugs (i.e. bladder dysfunction associated with TCA)

Bethanechol (Urecholine) direct acting MOA?

stimulates cholinergic receptors --> promotes contraction of the bladder, increases GI secretions and peristalsis, pupillary constriction and bronchoconstriction

Bethanechol (Urecholine) route?

PO/Injection (subcut).

Contraindicated IV and IM

Bethanechol (Urecholine) contraindications?

Intestinal or urinary obstruction

Severe Bradycardia

Hypotension

Peptic Ulcer

Active Bronchial asthma

COPD

Parkinsonism ------ don't want acetylcholine levels with these patients

Bethanechol (Urecholine) Side effects

N/V/D

abdominal cramps, salivation, sweating, frequent urination, blurred vision from pupil constriction, miosis

Bethanechol (Urecholine) adverse effects ?

orthostatic hypertension, bradycardia, muscle weakness, heart block/cardiac arrest, acute asthma attacks

Bethanechol (Urecholine) drug interactions?

decreased effect of bethanechol with antidysrhythmics,

ganglionic blocking agents cause significant hypotension,

atropine counter acts

what occurs with a heart block?

a long PQ time

Nursing considerations of Urecholine?

Early ambulation and increased fluid intake if not contraindicated (CHF patients)

Monitor vital signs, assess urine output should be > 1500ml

Atropine antidote

Change position slowly - likely dehhydrated after surgery. High risk orthostatic hypertension

Give 1 hr before or 2 hrs after meals, can give with food if stomach upset

Monitor for cholinergic crisis: muscular weakness and increased salivation

Pilocarpine function

constricts pupils, used for glaucoma and promotes miosis in eye surgery

oral form for dry mouth treatments

Cholinesterase function?

breaks down acetylcholine

What do cholinesterase inhibitors do? (indirect acting)

bind with cholinesterase allowing the action of acetylcholine

activates muscarininc and nicotinic receptors

smooth muscle stimulation (increased force of contraction)

bradycardia, miosis, increased GI motility, bronchial constriction, increased urination

Reversible cholinesterase inhibitors indications ?

produce pupillary constriction in glaucoma

increase muscle strength in patients with MS (prostigmin and mestinon)

What is physostigmine?

antidote for anticholinergic toxicity (atropine)

reversible cholinesterase inhibitors side effects?

bradycardia, asthma, peptic ulcers

Physostigmine (Antilirium) indications?

indirect acting anti cholinesterase for MS and reversal of TCA overdose

Physostigmine (Antilirium) contraindications?

allergy

prior severe cholinergic reactions

asthma gangrene

hypothyroidism **

CAD

mechanical obstruction of GI or GU tracts

Physostigmine (Antilirium) adverse effects?

GI upset, excessive salivation

Physostigmine (Antilirium) interactions ?

anticholinergics (counteracts effects), atropine used

anti-cholinergics sites of action?

heart, respiratory, GI, bladder, eyes and glands

Atropine indications?

treatment of bradycardia (bradycardia ends in an A)

pre-op control of secretions, treatment of organophosphate poisoning (insecticides)

atropine contraindications?

closed angle glaucoma, adhesions between iris and lens, certain types of asthma, severe hepatic and renal dysfunction, reflux esophagitis, intestinal atony, haitial hernias, obstructive GI or GU conditions, severe ulcerative colitis

How is atropine administered?

PO, IV, and ophthalmic forms

pharmacokinetics of atropine?

Immediate onset, PP: 2-4 mins, Half-life: 2.5 hr, duration: 4-6hr

Atropine side effects?

Dry mouth, nausea, headache, constipation, dry skin, blurred vision, palpitations, urinary retention

Atropine adverse effects?

tachycardia, hypotension, V-fib, Stevens-Johnson syndrome, coma

biggest thing is dry mouth

Dicyclomine (Bentyl) indications?

antispasmodic cholinergic blocker for the treatment of IBS, colic, entercolitis in infants

Dicyclomine (Bentyl) contraindications ?

Known drug allergy to antcholinergics, angle closure glaucoma, GI tract obstruction, myasthenia gravis, paralytic ileus, GI atony. Toxic mega colon

Cogentin (anticholinergic) indications?

to decrease the rigidity and tremors of Parkinson's. little effect of bradykinesia due to drug induced parkinsonism

Cogentin (anticholinergic) MOA

inhibit the release of acetylcholine

Cogentin (anticholinergic) examples?

artane, cogentin, akineton, parisdol, norflex, occasionally Benadryl

Cogentin (anticholinergic) side effects?

dry mouth, dry secretions, urinary retention, constipation, blurred vision, increased heart rate, restlessness, confusion

paralytic ileus

Cogentin (anticholinergic) contraindications ?

glaucoma

Oxybutynin (Ditropan) indications?

overactive bladder, antispasmodic for neurogenic a/w spinal cord injuries and spina bifida

Oxybutynin (Ditropan) contraindications?

drug allergy, GU/GI retention, uncontrolled angle closure glaucoma

Oxybutynin (Ditropan) nursing indications for patch use?

remove previous dose, apply to clean, dry, non hairy skin, rotate sites to decrease irritation

take one hour before meals or 2 hours after with fluids

Tolterodine (Detrol) indications

urinary frequency, urgency, urge incontinence caused by bladder over activity

high specificity to the bladder --> less dry mouth

Tolterodine (Detrol) contraindications?

angle-closure glaucoma, urinary retention, decreased hepatic function

take without food

Petrol side effects?

dry mouth, eyes and skin, HA, dizziness, vertigo, nervousness, N/V/D/C abdominal pain, urinary retention

grapefruit juice may increase drug levels

Anticholinergics for motion sickness examples?

Scopolamine, ginger/ginger gum, dramamine, antivert, marzine

anticholinergics for motion sickness side effects?

dry mouth, blurred vision, constipation, urinary retention

Nursing considerations for anticholinergics?

assess urine output
check history (contraindicated for glaucoma)
monitor vitals
monitor bowel sounds
mouth care

major side effects for anticholinergics?

increase in IOP, elevated HR and BP, constipation and paralytic ileus, dry mouth