1. slow heart rate

2. increased gastric secretion

3. emptying the bladder

4. emptying the bowel

5. focusing the eye for near vision

6. constricting the pupil

7. contracting bronchial smooth muscle

activation of nicotinicN (neuronal)

activation of nicotinicM (muscle receptors)

activation of muscarinic receptors

has minimal clinical significance

located in presynaptic junction

Targeted at heart

increase heart rate

increase force of contraction

increases velocity of conduction in AV node

targeted at the kidney for renin release

causes bronchial dilation

relaxation of uterine muscles in labor

vasodilation

glycogenolysis (break down of glycogen)

alpha 1

alpha 2

beta 1

alpha 1

beta 1

dopamine

* dopamine can only activate dopamine, nothing else can do it

they mimic actions produced by the peripheral nervous system

they also bind to muscarinic receptors causing activation

a muscarinic agonist

actually called urecholine and duvoid

main use is for urinary retention

main use is urinary retention

activates muscarinic cholinergic receptors

muscarinic agonist used to treat urinary retention

Heart--causes bradycardia

exocrine--increases sweating and salivation, bronchial secretions, and gastric acid

smooth muscles--causes contraction of smooth muscles

eyes--contraction of ciliary muscles

oral dosing

poorly absorbed (positive charge)

used for urinary retention (it increases voiding pressure and relaxes sphincters)

investigational use for gastric reflux

hypertension

bradycardia

alimentary systems

urinary tract

exacerbation of asthma

dysrhythmias in hyperthyroid patients

reflex tachycardia

atropine

anticholinergic drugs for overactive bladder (urge incontinence)

eye drops are used for glaucoma

orally used for dry mouth/Sjogren's syndrome

direct acting muscarinic agonists

cholinesterase inhibitors

poisonous mushrooms

salivation

lacrination

visual disturbances

bronchospasm

diarrhea

bradycardia

hypotension

they competitively block the actions of acetylcholine at the muscarinic receptors

anticholinergic drugs produce selective blockade of muscarinic receptors

**not all cholinergic receptors (selective)

muscarinic antagonists are anticholinergic drugs

competitive blockade at muscarinic receptors

too high of doses/get some nicotinic blockade

heart

exocrine glands

smooth muscle

eye

oral

topical (eye drops)

Injection

half life is three hours

metabolized in the liver and excreted in the urine

preanesthetic medication

disorders of the eye

bradycardia

intestinal hypertonicity

hypermotility

muscarinic agonist poisoning (mushrooms)

peptic ulcer disease & asthma (rarely used)

biliary colic

dry mouth (xerostomia)

blurred vision

photophobia

elevation of intraocular pressure

urinary retention

constipation

anhidrosis (absence of sweating)

tachycardia

asthma

oral

IV

IM

sub Q

eye drops (glaucoma)

sub Q pen (cholinesterase inhibitor poisoning)

oxybutynin (Ditropan and oxytrol)

this drug is primarily an M3 blocker

syrup

extended release tablets

transdermal patch

dry mouth

suppresses emesis and motion sickness

given on cruise ships

causes sedation (alot of time given pre anesthesia)

psychlopesia (paralysis of the muscle)

mydriasis (dilation of the pupil) used for opthalmic procedures

mushrooms

selective antimuscarinic drugs are the atropine and scopalamine (antidote for poisoning)

antihistamines have antimuscarinic properties

dry mouth

blurred vision

photophobia

hyperthermia

CNS effects

hot, dry, and flush skin

hallucinations

delirium

antidote is physostigmine (anticholinesterase inhibitor)

works by minimizing absorption

differentiate between poisoning (mushroom) and actual psychotic episode (toxic)

it is positively charged

prevents breakdown of acetylcholine which keeps it at the junction longer

it is oral

IM

IV

sub Q

the duration of action is 2-4 hours

after this period turns to inactive product

used for myasthenia gravis

reversal of non depolarizing neuromuscular blockade

used post operatively treatment of overdose likely to elicit substantial muscarinic responses, may need to administer atropine

excessive muscarinic stimulation and neuromuscular blockade

the precautions and contraindications are the same as the direct muscarinic acting agents

muscarinic antagonist (atropine)

non depolarizing neuromuscular blockers

depolarizing neuromuscular blockers (intensifies the blockade)

symptoms are respiratory depression, or respiratory arrest

treatment is atropine, intubation, and respiratory support

Neostigmine (prostigmin)

--this increases muscle strength but causes a side effect of excessive muscarinic response

subtypes of cholinergic receptors

-nicotinicN

-nicotinicM

-muscarinic

subtypes of adrenergic receptors

-alpha 1

-alpha 2

-beta 1

-beta 2

-dopamine

vasoconstriction

mydriasis (dilation of pupil)

ejaculation

contraction of bladder neck and prostate

located in presynaptic junction

has minimal clinical significance

In the heart it increases heart rate, increases force of contraction, and increases the velocity of conduction in AV node

in the kidneys it releases renin

Epinephrine--alpha1, alpha2, beta1, beta2

Norepinephrine--alpha1, alpha2, beta1

Dopamine--alpha1, beta1, dopamine

DIRECT RECEPTOR BINDING

promotion of norepinephrine release

inhibition of norepinephrine reuptake

inhibition of norepinephrine inactivation

epinephrine injected sub Q

(which activates alpha1, alpha2, beta1, beta2)

inactivation in 10-20 min due to short half life

absorption (has quick absorption)

Adverse effects are: hypertensive crisis, dysrhythmias, angina pectoris, necrosis following extravasation, hyperglycemia

MAO Inhibitors intensify or prolong effects of epinephrine

tricyclic antidepressants

general anesthetics

alpha adrenergic blocking

used for hypotension and cardiac arrest

it is parenteral only

no hyperglycemia effect because there is no Beta2 receptor effects

it is a catecholamine

the receptors it affects are beta1 and beta 2

therapeutic uses are cardiovascular; asthma not used anymore; helps to relax the bronchioles (bronchiospasm)

adverse affects: angina, hyperglycemia, dysrhythmia

given IM or IV

it is a catecholamine

it is specific to dopamine, beta1 and alpha 1 receptors

it increases renal perfusion and cardiac output

therapeutic uses: shock, heart failure and acute renal failure

adverse effects: dysrhythmias, angina, tachycardia

Administration: has to be diluted in an aqueous solution (only administered IV drip never push)

catecholamine

only receptor specific to beta 1

used for heart failure

non catecholamine

specific to beta 2 receptor

used for asthma

adverse effects minimal at therapeutic doses

tremors and tachycardia at higher doses

epi pen and then call 911

epi pen is single use epinephrine sensitive to heat and light

cause direct blockade of adrenergic receptors (except for one)

more selective than adrenergic agonist

they are broken into two major groups alpha and beta blocking agents

it dilates arteries and veins (limited use due to potential postural hypotension)

competitive antagonist for alpha 1

it is given orally

it is metabolized in the liver

excreted in bile

adverse effects: orthostatic hypotension, reflex tachycardia, inhibits ejaculation, nasal congestion

a selective alpha 1 adrenergic antagonist

specific to benign prostatis hypertrophy

What is the beta adrenergic antagonist 2 propranolol (inderal)

used for hypertension, angina, MI, migraines, stage fright

it can be administered oral or IV and has a high first pass effect

pharmacologic effects: beta1 and beta 2 (nonselective)

adverse effects: bradycardia, AV heart block, heart failure, rebound cardia excitation, bronchoconstriction, inhibition of glycogenolysis, CNS effects

Drug interactions: calcium channel blocker

can disguise s/s of insulin induced hypoglycemia

pharmacological effects: blocks beta 1 only

high doses will also block beta 2

used for hypertension, angina, heart failure, and MI

also suppresses renin

used for hypertension, MI, heart failure

blocks beta1, beta2 and alpha1 receptors

stimulates the brain stem to regulate the cardiovascular system

it also decreases sympathetic outflow to blood vessels and heart

pharmocological effects: causes bradycardia and vasodilation

used for hypertension and severe cancer pain

adverse effects: drowsiness, dry mouth, rebound hypertension, teratogenic,

given orally once a day or transdermal every 7 days

they act pre synaptically to reduce release of norepinephrine from sympathetic neurons

they have little effect on release of epinephrine from adrenal medulla

depletes norepinephrine from post ganglionic sympathetic neurons

pharmocologic effects: decreases blood pressure, causes sedation, is used for hypertension and psychotic states;

adverse effects: depression and cardiovascular effects