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155 Cards in this Set

  • Front
  • Back

regulation of biological process

1. hormones


2. nt


3. histamine prostaglandins

Brain and Spinal Cord

CNS, incased in bondy strucutre

Peripheral

that comes out from CNS nerves (what extends from the brain)

Cranial nerve, optic nerve, vagus nerve

controll all function of body while at rest

peripheray

afferent sensory ex: posture, , unconsicioulsy sending signals from outside to inside

afferent neurons

sensory

efferent neurons

motor

autonomic nerrvous system

homeostasis


1. parasympathetic


2. sympathetic


3. enteric

somatic nervous system

skeletal muscle

sympathetic

anatomically designed to produce widespread physiological activity


thoraco-lumbar division

parasympathetic

anatomically designed to produce response on an organ basis


cranio-sacral divisoin

nt 2

sympathetic neuron= norepinephrine


cholinergic neuron= acetylcholine


neurotransmission

1. preganglionic synapse


2. postganglionic synapse


3. somatic motor end plates

norepinephrine

sympathetic,


adrenaline, produced by adrenal gland


WIDE SPREAD EFFECT

acetylcholin

cholinergic neuron, stimulate skeletal muscle tissue, targets motors

receptors

1.coupled to ion channels


2. coupled to adenyly cyclase


3. coupled to diaclyglycerol

indirectt

hormones like ADH, bind as surface receptor and secondary messenger regulate vasopressins

innervation

most visceral organs receive dual innervation


both working in opposition (balanced) the one exerting the greater function will prevail


specific effects of blood vessels:

innervated by sympathetic, maintains smooth muscle tone

innervation specific effects: heart and cardiovascular reflex

2- Heart
Sympathetic system
Positive chronotropic (heart rate)
Positive inotropic (force of contraction)
Positive dromotropic (conductivity)
Parasympathetic system
Negative inotropic
Negative dronotropic
3- Cardiovascular reflex
Mainly due to stretch receptors (carotid body) effects on cardiovsacular center at Medulla oblongata


innervation specific effects: eye

4- Eye
Pupil
Lens)
Sympathetic system (mydriasis)
Dilator pupillae (radial fibers)

Parasympatheic system (miosis)
Constrictor pupillae (circular fibers
At rest the suspensory ligaments of cilliary body exerts tension flattening the lens
Under parasympathetic stimuli the cilliary body contracts decreasing tension on the lens thickening the lens due to elasticity accommodating for near vision


innervation specific effects: lung and GI tract

5- Lung
Bronchial tree is dually innervated
Sympathetic system
Bronchodilation
Parasympatehtic system
Bronchoconstriction
6- Gastrointestinal tract
Dual effects but act on local neural regulators
Enkephalins
Substance P
Vasoactive intestinal peptide


innervation specific effects: salivary glands and adrenal medulla

7- Salivary glands
Dual stimulation produce secretion with different characteristics
Sympathetic stimuli
Thick and mucinous
Parasympathetic stimuli
Watery
8- Adrenal medulla
Behaves as a sympathetic ganglion producing primarily epinephrine, then norerpinephrine


chemical synapses

1. one way transmission


2. promotes a response in post-synaptic target

cholingeric neuron

actylcholine


produced by modification of acetylco-A Krebs cycle

muscarinic receptors

wider effects than acetylcholine,


have mild nicotine rxns

nicotinic receptors

stronger response to nicotine than acetylcholine


have mild effect to muscarine

adrenergic neuron

tyrosine is the building block for pigment of skin, IS RATE LIMITING STEP


Dopamine- is nt in brain, regulates and counteracts balance of brain


parkinson's disease: lose dopa, lose control over skeletal muscle tissue


Dopamine make norepinephrine

presynaptic cleft

3 outcomes:


1. binding to post syn receptor


2. catabolism of excess inside cleft by COMT and MAO


3. may be recycled back to presynaptic neuron

adrenrergic drugs

adrenergic neuron


release norepinephrine in CNS


drugs act on receptors stimulated by:


epinephrine and norepinephrine

biotransformation

COMT


MAO


enzymes that degrade excess in synaptic cleft MAO (metanphrine and VMA) measured in urine

adrenergic receptors alpha

have higher affinity for epinephrine

adrenergic receptors beta

have stronger affinity for isoproternol (synthetic) will not be destroyed

alpha 1 adrenoreceptor

vasoconstriction


increase peripheral resistance


increased blood pressure


mydriasis


increased closure of internal urinary bladder sphincter

alpha 2 adrenoreceptor

inhibition of norepinphrine rlease


inhibition of insulin release

beta 1 adrenoreceptor

tachycardia


increased myocardial contractility


increased lipolysis

beta 2 adrenoreceptor

vasodilation


slight decrease in peripheral resistance


bronchodilation


increased glycogenolysis (liver and muscle)


increased glucagon release


relaxation of uterine smooth muscle

adrenergic receptor desensitization

prolonged exposure to catecholamines reduces responsiveness of receptor


receptor sequestration (less # of receptors on surface)


down regulation (respond with lesser strength, but same # of receptors on surface, receptors are LESS SENSITIVE)


inability to couple w protein G

adrenergic agonists

drugs used to replace normal endogenous compound, drugs that mimic resemble in outcome of normal nt

adrenergic agonist

either indirect


direct


mixed action


direct acting adrenergic agonists

as a group are widely used catecholamines


catecholamines

high potency


rapid inactivation


MAO & COMT


Poor penetration into CNS


Catecholamines Naturally Occuring

epinephrine


norepinephrine


dopamine

Catecholamines synthetic compounds

dobutamine


isoproterenol

indirect acting adrenergic agents

As a group causes release of norepinephrine from presynaptic terminals
Amphetamines (“ups’ ”)
central stimulation
(A) & (B)
 Blood pressure and heart rate
Tyramine
Not a clinically useful drug found in cheese and Chianti wine


Cocaine

cocaine

local anesthetic that blocks Na/K pump required for reuptake of norepinephrine enhancing its sympathetic activity--> so too much nt in synaptic cleft

mixed-action adrenergic agents

induce norepinephrine release from presynaptic terminals and activate receptors in postsynaptic membranes


mixed action adrenergic agents 2

ephedrine


enhance contractility and improve motor function in Myasthenia gravis



metaraminol


alternative drug for shock treatment, may be used to treat acute hypotenstion

adrenerrgic agonists side effects: 6

arrhtythmias


headache


hyperactivity


insomnia


nausea


tremors

epinephrine

interacts with alpha and beta receptors


epinephrine low and high dose

low dose- beta receptor activity predominates (vasodilation)


high dose- alpha receptor predominates (vasoconstrictor)

actions

ACTIONS


Cardiovascular system


(+) inotropic and chronotropic (B1)
peripheral vasoconstriction with decrease renal blood flow (A)
dilation of hepatic and muscle vasculature (B2)

actions

Respiratory system
Bronchodilation (B2).


Hyperglycemia
Glycogenolysis (B2)
decrease Insulin (A2)


Lypolysis (B)

therapeutic use

Thearpeutic use


Bronchospasm (SC)
Anaphylactic shock
Type I hypersensitivity reactions
(Anaphylaxis)


Glaucoma open angle (2% sol)
decrease intraocular pressure


Anesthetics
increase duration of local anesthetics due to vasoconstiction


pharmacokinetics

Pharmacokinetics
rapid onset but brief duration: IV, SC, endotracheal tube
orally ineffective
metabolites excreted in urine (metanephrine & VMA)
Adverse effects
CNS disturbances
Intracerebral hemorrhage
cardiac arrythmias (digitalis)
pulmonary edema
Interactions
hyprethyroidism
cocaine


norepinephrine

affects mostly alpha receptors


actions: cardiovascular


vasoconstriction


baroreceptor reflex


atropine preteratment


if given after atropin it will cause tachycardia

therapeutic use for norepinephrine

shock (levarterenol)


dopamine is better because it doesn't decrease renal blood flow

isoproterenol

stimulates b1 and b2


actions:


cardiovascular


(+) inotropic (+) chronotropic


decrease peripheral resistance


pulmonar


bronchodilation

isopreterenol therapeutic use

asthma


heart block or cardiac arrest



pharmacokinetics


absorbed systemically by sublingual or aerosols

dopamine

activates a and b receptors


in addition D1 and D2 (mesenteric and renal beds)
Actions
cardiovascular (B1)
(+) inotropic (+)chronotropic
vasoconstriction (A)
renal and visceral
dilation of renal and splachnic beds
Therapeutic use
Shock (DRUG OF CHOICE)
adverse effects
short lived arrhythmias and nausea


other direct acting agents

1- Fenlodopan (D1 and A2)
Rapid vasodilation for severe hypertension in hospitalized patients.



2- Dobutamine (B1)
Use in congestive heart failure to  C.O.

other direct acting agents

3- Phenylephrine (A1)


4- Oxymetazoline
Use as nasal decongestant
Mydriasis


5- Methoxamine (A1 > A2)
Overcome hypotension during anesthesia with halothane


6- Clonidine (A2)
Essential hypertension due to CNS action
(diminish central adrenergic outflow)


Fenlodopan


other direct acting agent

D1 and A2


dopamine agent, which may be implied in hypertension pts that are hospitalized, can increase profusion

Dobutamine

b1 agonist


synthetic agent used to improve cardiac activity in heart failure

phenylephrine

A1, vasoconstriction, reduces histamine release

oxymetazoline

nasomucousa,


reducing glucosecretions, watery dischage (reduce the discharge), mydriasis, topically



methoxamine

A1>A2


parernterally, works by modulating the vasculature, smooth muscle contraction

Clonidine

A2


HYPERTENSIVE AGENT, slows down function of heart pump, vasodilation

b2 agonist are employed for asthma aerosols for b2 rescue agent

have effects produce smooth muscle

metaproterenol


albuterol, pributerol,


salmetrol, formetrol



-----------


Terbutaline

used for bronchodilation


--------


bronchodilator, decreases uterine contractions in premature labor

rescue agents bc

immediate

alpha adrenergic blockers

decrease sympathetic tone of blood vessels


decrease peripheral vascular resistance with reflex tachycardia

as a group act as equilibrium competitors


3 families


compete in supply and demand


commonly employed for hypertension


begins with first making diagnosis from increased blood pressure 130/90

1. haloalkylamines


2. imidazolines


3. quinazolines

first step in hypertension

weightloss, second step is drug

equilibrium competitors


haloalkylamine

phenoxybenzamine


(Dibenzyline)


equilibrium competitors


Imidazolines

phentolamine (Regitine)

Equilibrium competitors


Quinazolines

prazosin (Minipress®)
yohimbine (Yocon ®)
terazosin (Hytrin ®)
doxazosin (Cardura ®)
tamsulosin (Flomax ®)
afluzosin (Uroxatal ®)



phenoxybenzamine

Phenoxybenzamine
Irreversible and noncompetitive block overcome by synthesis of new receptors.
Used in treatment of pheochromocytoma prior to surgery.
Associated with postural hypotension

phentolamine

Phentolamine
(Only used for diagnosis of pheochromocytoma)
Competitive blocker (duration of 4 hrs.)

Quinazolines


Prazosin, terazosin and doxazosin


(Post synaptic alpha 1 receptors blockers)
used as antihypertensive agents (first dose effect) ( VASO – VAGAL reflex)

w 3 families halo, imi, quin side effects

hypotension, tachycardia, vertigo, sexual dysfunction

drugs affecting nt release or uptake

Reserpine


Guanethidine

Reserpine

Reserpine (Serprasil ®)
Blocks transport and storage of biogenic amines causing depletion of norepinephrine.

Guanethidine


(Ismelin®)
Blocks release of storage norepinephrine

alpha and beta antagonist


Alpha and Beta antagonist

Reversible Beta blockers with concurrent Alpha blocking
Labetolol
Carvelidol

beta blockers

Propranolo


Nadolol


Timolol


Acebutolol


Atenolol


Esmolol


Metaprolol


Carvelidol


Labetalol

B1 and B2 blockers

Propranolol


Nadolol


Timolol

B1 Selective ***ISA***

Acebutolol


Atenolol


Esmolol


Metaprolol


ISA

Intrinsic sympathetic activity (binds to receptor, but effect has lower strength)

A1, B1, B2

Carvelidol


Labetalol

Selective

Acebutolol


Atenolol


Esmolol


Metaprolol


Non-selective

Propranolol


Nadolol


Timolol


Carvelidol


Labetalol

What happens w insulin secretion?

beta blockers, beta cells create insulin, may decrease production from pancreas, don't take into consideration

Clinical Use

CLINICAL USE
Arrythmia prophylaxis after a myocardial infaction
propranolol, metropolol and timolol reduce cardiac output and renin secretion.


Supraventricular tachycardias
propranolol, esmolol and acebutolol slow AV conduction velocity.


Clinical Use

Angina pectoris
propranolol nadolol and other B blockers reduce heart rate and force of contraction
Hypertension
propranolol, metropolol, timolol and other B blockers reduce cardiac output and renin secretion.
Glaucoma
timolol and other B blockers reduce secretion of aqueous humor.


Clinical Use

Migrane
propranolo provides prophylactic effect.


Thyrotoxicosis
propranolol reduces cardiac rate and potential for arrythmias

Side effects w beta blockers

arrhythmias,


bronchoconstriction


sexual dysfunction

Regulation of Biological Process

Hormones, Neurotransmitters, Histamine (prostaglandins)inn

innveration

blood vessels, heart, cardiovascular, eye, lung, GI tract, Salivary Glands, Adrenal Medulla

Cholinergic neuron uses what for a nt?

acetylcholin

name the 2 receptors of a cholinergic neuron

muscarinic and nicotinic

adrenergic neuron uses what for nt's?

epinephrine and dopamine

CNS

is composed of brain and spinal cored

PNS

neurons located outside spinal cord

efferent division

EXIT- carry info (signals) AWAY from brain and spinal cord

afferent

bring information from PNS to CNS

efferent division divided into

somatic and autonomic

autonomic divided into

para


symp


enteric (endocrine and exocrine), GI tract

sympathetic region

thoracic and lumbar

parasympathetic region

cranium and sacral areas

effects of stimulation from sympathetic

flight or fight


increase heart rate, dilation of pupils and bronchioles


increase blood pressure

effects of stimulation from sympathetic

adrenal medulla release epinephrine and less neorephinephrine

parasympathetic

opposes sympathetic, and dominates over "rest and digest"


TO SPECIFIC ORGANS

Hypothalmus, medulla oblongata, and spinal cord

respond to stimuli by sending out efferent reflex impulses via autonomic nervous system

emotion: rage, fear, pleasure

can modify autonomic nervous system

dual innervation

by both para and sum, but one will predominate

controlling heart rate dual innervation

VAGUS NERVE predominate factor

Organs receiving only sympathetic innveration

adrenalla medulla, kidney, pilomotor muscles, and sweat glands



and basically control of blood pressure

somatic nervous system

single myelinated motor neuron, originating in the CNS

Local mediators

not distributed throughout body, only act locally


Histamine and prostaglandins!!**

hormones

specialized endocrine cells secrete hormones into the bloodstream

2 main nts in autonomic nervous system

acetylcholine and norepinephrine

cholernergic neurons use

acetylcholine

adernergic neurons use

ADRENALINE, epinephrine or norepinephrine

acetylcholine does:

decrease heart rate and cardiac output


decrease blood pressure


acetylcholine has 2 receptors:

1. muscarinic


2. nicotinic

M2

HEART, brain, autonomic ganglia, and smooth muscle

acetylcholine is not therapeutically important

because has so many actions

bethanecol

synthetically related to acetylcholine but not destroyed by acetylcholineterase


strong muscarinic action


increases intestinal motility and tone


stimulate detrussor muscle of bladder promoting urination

carbachol

muscarinic and nicotinic actions may last up to an 1 hr.

carbachol

because of its potency and long duration is rarely used except for the eye where causes mitosis ( decrease intraocular pressure)


can avoid systemic effects is applied topically

pilocarpine

for acute angle glaucoma

pilocarpine

miosis, also stimulates sweat, tears, and saliva production

pilocarpine

drug of choice for decreasing IOP in emergency treatment of glaucoma

Cholinergic adverse effects

diarrhea, diaphoresis,miosis, nausea, urinary urgency

reversible: pyridostigmine

both muscarinic and nicotinic receptors,


duration 2-4 hours


pyridostigmine therapeutic use:

promotes motility in bladder, decrease IOP topically, antidote for overdose of atropine, phenotiazine, Tricyclic antidepressants



USE IN MYASTHENIA GRAVIS

pyridostigmine adverse effects

convulsions, bradychardia

Neostigmine

doesn't cross the blood brain barrier, but has greater effect in skeletal muscle. used in myasthenia gravis and antidote for tobocurarine and neuromuscular blockers

Demecarium

similar action as Neostigmine but used for open angle glaucoma

Edrophonium

similar to neostigmine but shorter duration


USE IV IN DIAGNOSIS OF MYASTEHNIA

Tarcrine, Donazepil, Rivastigmine, and Galantamine,

used in treatment of alzheimer's disease

irreversible

extremely toxic

ecchothiophate


irreversible

covalently binds to active site of acetylcholinesterase and permanently activates. With "age" (loosing of isopropyl group) make is unavailable for activation

ecchothiophate


irreversible

one application lasts up to one week


misosis

pralidoxime

reactivation of acetylcholinesterase but be used before aging

cholinergic agonists

contraction of visceral smooth muscle


miosis


hypotension


bradycardia

atropine


anti muscarinic

mydriasis


cyclopegia


used for examination of funds, if pt suffers from glaucoma, might not be used

atropine


antimuscarinic

GI system: antipasmodic


CV: low dose--> bradycardia (block M1 receptors)


high dose--> tachycardia



xerostomia (dry mouth and eye)



antidote for insecticides

atropine

if too much, hallucinations

scoplamine

"scuba" used for motion sickness


blocks short term memory


can cross blood brain barrier and can produce hallucinations

ipratropium/ tiotropium

inhalation in asthma and COPD, decrease mucouse production



Topically: Topicamine and Cycopentolate - cyclopegia

benztripine/ trihexyphenidyl

parkinson disesase

Darifenacin/ Fesoterodine, Oxybutyin/ Solifenacin, Tolterodine

sythenitch atropin


used for over active bladders


these drugs reduce hypersensitivity to sensation of having to pee

Cholinergic antagonist side effects

blurred vision


confusion


mydriasis


constipation


urinary retention