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Pharmacology unit 3
Nervous system
94
Pharmacology
Undergraduate 2
09/17/2012

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Cards

Term
What are seven functions of the Parasympathetic Nervous System?
Definition

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

Term
What are the functions of the cholinergic receptor subtypes?
Definition

activation of nicotinicN (neuronal)

activation of nicotinicM (muscle receptors)

activation of muscarinic receptors

Term
What are the functions of Alpha1 Adrenergic receptors?
Definition
cause vasoconstriction, ejaculation, and contraction of bladder neck and prostate
Term
What are the functions of Alpha2 adrenergic receptors?
Definition

has minimal clinical significance

located in presynaptic junction

Term
What are the functions of Beta1 adrenergic receptors?
Definition

Targeted at heart

increase heart rate

increase force of contraction

increases velocity of conduction in AV node

targeted at the kidney for renin release

 

Term
What are the functions of Beta2 adrenergic receptors?
Definition

causes bronchial dilation

relaxation of uterine muscles in labor

vasodilation

glycogenolysis (break down of glycogen)

 

Term
What are the functions of dopamine (adrenergic receptor)?
Definition
responsible for dilation of renal blood vessels
Term
What receptors does epinephrine activate?
Definition
activates the alpha and beta adrenergic receptors
Term
What receptors does norepinephrine activate?
Definition

alpha 1

alpha 2

beta 1

 

Term
What adrenergic receptors does dopamine activate?
Definition

alpha 1

beta 1

dopamine

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

Term
What do muscarinic agonists do?
Definition

they mimic actions produced by the peripheral nervous system

they also bind to muscarinic receptors causing activation

 

Term
What is Bethanechol?
Definition

a muscarinic agonist

actually called urecholine and duvoid

main use is for urinary retention

Term
What are the two names for Bethanechol?
Definition
urecholine and duvoid
Term
What is Bethanechol used for?
Definition

main use is urinary retention

activates muscarinic cholinergic receptors

muscarinic agonist used to treat urinary retention

Term
What are the pharmacologic effects of Bethanechol?
Definition

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

Term
What is the availability of dosing/how can Bethanechol be administered?
Definition

oral dosing

poorly absorbed (positive charge)

Term
What are the therapeutic uses of Bethanechol?
Definition

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

investigational use for gastric reflux

Term
What are the adverse effects of Bethanechol?
Definition

hypertension

bradycardia

alimentary systems

urinary tract

exacerbation of asthma

dysrhythmias in hyperthyroid patients

reflex tachycardia

Term
What are the muscarinic antagonist?
Definition

atropine

anticholinergic drugs for overactive bladder (urge incontinence)

Term
What is the muscarinic agonists pilocarpine used for?
Definition

eye drops are used for glaucoma

orally used for dry mouth/Sjogren's syndrome

Term
What are the sources of muscarinic poisoning/toxicity?
Definition

direct acting muscarinic agonists

cholinesterase inhibitors

poisonous mushrooms

 

Term
What are the symtoms of toxicity of muscarinic agonists?
Definition

salivation

lacrination

visual disturbances

bronchospasm

diarrhea

bradycardia

hypotension

 

Term
What is the treatment of toxicity of muscarinic agonists?
Definition
ATROPINE
Term
What do muscarinic antagonists do?
Definition

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

Term
What is the mechanism of action of muscarinic antagonist atropine?
Definition

competitive blockade at muscarinic receptors

too high of doses/get some nicotinic blockade

Term
What is the muscarinic antagonist-- atropine pharmacological effects?
Definition

heart

exocrine glands

smooth muscle

eye

Term
How is atropine administered?
Definition

oral

topical (eye drops)

Injection

half life is three hours

metabolized in the liver and excreted in the urine

 

Term
What are the therapeutic uses of atropine?
Definition

preanesthetic medication

disorders of the eye

bradycardia

intestinal hypertonicity

hypermotility

muscarinic agonist poisoning (mushrooms)

peptic ulcer disease & asthma (rarely used)

biliary colic

Term
What are the adverse effects of atropine?
Definition

dry mouth (xerostomia)

blurred vision

photophobia

elevation of intraocular pressure

urinary retention

constipation

anhidrosis (absence of sweating)

tachycardia

asthma

 

Term
What are the drug interactions of Atropine?
Definition
avoid combining atropine with other drugs capable of causing muscarinic blockade such as antihistamines, tricyclic antidepressants, phenothiazine antipsychotics
Term
How do you administer Atropine?
Definition

oral

IV

IM

sub Q

eye drops (glaucoma)

sub Q pen (cholinesterase inhibitor poisoning)

Term
What are the anticholinergic drugs used for overactive bladder?
Definition

oxybutynin (Ditropan and oxytrol)

this drug is primarily an M3 blocker

Term
What are the available forms of Ditropan?
Definition

syrup

extended release tablets

transdermal patch

Term
What are the side effects of Ditropan?
Definition

dry mouth

 

 

 

 

 

 

Term
What does the anticholinergic drug (scopolamine)for overactive bladder do?
Definition

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

Term
What are sources of antimuscarinic poisoning?
Definition

mushrooms

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

antihistamines have antimuscarinic properties

Term
what are the symtoms of muscarinic antagonist toxicity?
Definition

dry mouth

blurred vision

photophobia

hyperthermia

CNS effects

hot, dry, and flush skin

hallucinations

delirium

Term
What are the treatments of muscarinic antagonist toxicity?
Definition

antidote is physostigmine (anticholinesterase inhibitor)

works by minimizing absorption

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

Term
what is the name of the reversible cholinesterase inhibitor that is used to prevent the breakdown of acetylcholine which keeps it at the junction for a longer period of time?
Definition
Neostigmine (Prostigmin)
Term
What is Neostigmine (Prostigmin) and what does it do?
Definition

it is positively charged

prevents breakdown of acetylcholine which keeps it at the junction longer

 

Term
What are the pharmacokinetics of the reversibe cholinesterase inhibitor Neostigmine?
Definition

it is oral

IM

IV

sub Q

the duration of action is 2-4 hours

after this period turns to inactive product

Term
What are the therapeutic uses of reversible cholinesterase inhibitor Neostigmine?
Definition

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

Term
What are the adverse effects of the reversible cholinesterase inhibitor Neostigmine?
Definition

excessive muscarinic stimulation and neuromuscular blockade

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

Term
what are the drug interactions of reversible cholinesterase inhibitor Neostigmine?
Definition

muscarinic antagonist (atropine)

non depolarizing neuromuscular blockers

depolarizing neuromuscular blockers (intensifies the blockade)

Term
What are the symptoms and treatment of acute toxicity of reversible cholinesterase inhibitor Neostigmine?
Definition

symptoms are respiratory depression, or respiratory arrest

treatment is atropine, intubation, and respiratory support

Term
What does reversible cholinesterase inhibitor Physostigmine do?
Definition
treats muscarinic antagonist poisoning
Term
What is the irreversible cholinesterase inhibitor used to treat glaucoma?
Definition
Echothiophate (phospholine)
Term
What is the antidote for irreversible cholinesterase inhibitor (such as Echothiaphate)?
Definition
Pralidoxine (protopam)
Term
What is the treatment for myasthenia gravis with cholinesterase inhibitors?
Definition

Neostigmine (prostigmin)

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

Term
What are the receptors of the peripheral nervous system?
Definition

subtypes of cholinergic receptors

-nicotinicN

-nicotinicM

-muscarinic

subtypes of adrenergic receptors

-alpha 1

-alpha 2

-beta 1

-beta 2

-dopamine

Term
What are the functions of adrenergic receptor alpha 1?
Definition

vasoconstriction

mydriasis (dilation of pupil)

ejaculation

contraction of bladder neck and prostate

Term
What are the functions of adrenergic receptor alpha 2?
Definition

located in presynaptic junction

has minimal clinical significance

Term
What are the Functions of Adrenergic
Receptor Subtype Beta 1? 
Definition

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

Term
What are the functions of adrenergic receptor Beta 2?
Definition
it affects the lungs, uterus, skeletal muscle, liver, and heart by causing bronchodilation, relaxation of the uterine muscle, vasodilation, and glycogenolysis
Term
What are the functions of adrenergic receptor dopamine?
Definition
it dilates renal blood vessels
Term
What is the receptor specificity of the adrenergic neurotransmitters?
Definition

Epinephrine--alpha1, alpha2, beta1, beta2

Norepinephrine--alpha1, alpha2, beta1

Dopamine--alpha1, beta1, dopamine

Term
The adrenergic receptors are activated by
Definition

DIRECT RECEPTOR BINDING

promotion of norepinephrine release

inhibition of norepinephrine reuptake

inhibition of norepinephrine inactivation

Term
What is the treatment of anaphylactic shock?
Definition

epinephrine injected sub Q

(which activates alpha1, alpha2, beta1, beta2)

Term
acetylcholine
Definition
neurotransmitter of the parasympathetic nervous system
Term
What are the pharmokinetics and adverse effects of epinephrine?
Definition

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

Term
What are the drug interactions with epinephrine?
Definition

MAO Inhibitors intensify or prolong effects of epinephrine

tricyclic antidepressants

general anesthetics

alpha adrenergic blocking

Term
what is norepinephrine (levophed) used for?
Definition

used for hypotension and cardiac arrest

it is parenteral only

no hyperglycemia effect because there is no Beta2 receptor effects

Term
What does the adrenergic agonist Isoproternol (Isuprel) do?
Definition

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

Term
What does the adrenergic agonist dopamine do?
Definition

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)

Term
adrenergic agonist dobutamine (dobutrex)
Definition

catecholamine

only receptor specific to beta 1

used for heart failure

Term
adrenergic agonist albuterol
Definition

non catecholamine

specific to beta 2 receptor

used for asthma

adverse effects minimal at therapeutic doses

tremors and tachycardia at higher doses

Term
What is immediate survival treatment for anaphylaxis?
Definition

epi pen and then call 911

epi pen is single use epinephrine sensitive to heat and light

Term
what do adrenergic antagonist do?
Definition

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

Term
what is the alpha adrenergic antagonist 2 prazosin (minipress) do?
Definition

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

Term
What does the alpha blocker terazosin (hytrin) do?
Definition
very similiar to prazosin used for hypertension and benign prostatic hypertrophy
Term
What does the alpha blocker tamsulosin (flomax) do?
Definition

a selective alpha 1 adrenergic antagonist

specific to benign prostatis hypertrophy

Term

What is the beta adrenergic antagonist 2 propranolol (inderal)

 

Definition

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

Term
What does beta adrenergic antagonist 2 metoprolol (lopressor and toprol XL)
Definition

pharmacological effects: blocks beta 1 only

high doses will also block beta 2

used for hypertension, angina, heart failure, and MI

also suppresses renin

 

Term
beta adrenergic antagonist 2 third generation carvedilol (coreg)
Definition

used for hypertension, MI, heart failure

blocks beta1, beta2 and alpha1 receptors

Term
What are the 2 categories of indirect acting antiadrenergic agents?
Definition
central acting alpha2 agonist (clonidine--catapress) and adrenergic neuron blocking agents (reserpine)
Term
what does centrally acting alpha2 agonists do?
Definition
reduces firing of sympathetic neurons that decrease release of norepinephrine from sympathetic nerves to decrease blood pressure and treat severe cancer
Term
What does clonidine do?
Definition

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

 

Term
What do adrenergic neuron blocking agents do?
Definition

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

they have little effect on release of epinephrine from adrenal medulla

Term
What does adrenergic neuron blocking agent reserprine do?
Definition

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

Term
Alpha 1
Definition
receptors found in the eyes, blood vessels, prostate gland, and bladder
Term
Atropine
Definition
increases heart rate and decreases secretions
Term
Beta 1
Definition
receptor found in the heart and kidneys
Term
Bethanecol (urecholine)
Definition
muscarinic agonist used to treat urinary retention
Term
clonidine (catapress)
Definition
oral or transdermal patch used for the treatment of hypertension
Term
dobutamine
Definition
Beta 1 specific drug that is most effective for treatment of heart failure
Term
Dopamine
Definition
used in treatment of shock to increase renal perfusion
Term
epinephrine
Definition
neurotransmitter released by the adrenal gland
Term
flomax
Definition
alpha 1 antagonist that is used to treat benign prostatic hypertrophy
Term
metoprolol (lopressor)
Definition
beta blocker that works primarily in the heart
Term
neostigmine
Definition
drug of choice for the treatment of myasthenia gravis
Term
physotigmine
Definition
antidote for muscarinic antagonist toxicity--mushrooms!
Term
Prazolin (Minipress)
Definition
alpha 1 antagonist that dilates arterioles and veins--may cause postural hypotension
Term
Propanolol (Inderal)
Definition
this beta blocker may mask the signs of hypoglycemia
Term
Reserpine
Definition
depletes epinephrine in the sympathetic nervous system, decreasing blood pressure
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