Pharmocology NSG 304

any substance that is taken to prevent, cure, or reduce symptoms of a medical condition

Study of drugs

Application of drugs for prevention of disease and treatment or suffering.

categorized as those drugs that offer treatment of disease

Categorized by mechanism of action

Drugs that overlap into different therapeutic and or pharmacological categories.

Selecting a single drug in a class and comparing it to all the other drugs in that class.

Learning the prototype drug in depth allows for predicting the adverse effects of other drugs in that same class

relates to the chemical and molecular structure

Often derived from the chemical name. Generic name is the common name of the drug.

the propriety name given by the manufacturer

Bioavailabilty issues

switching from brand to generic?

Why are generic brands becoming so popular?

the rate and extent to which active ingredients are absorbed from a drug product and beciomes available at the site of drug action to produce its effect.

dosages may be identical

drug formulations not always the same

may have different inert ingredients

-tablet form: active ingredients may be more tightly compressed in one of the preparations

-liquid drugs: may use different solvents such as water or alcohol

Cost half as much as brand name drugs

-Generic, Brand, and or chemical name

-indications for drug

-contraindictations of the drug

-adverse reactions/side effects

-administration: Dose, Route (PO,SQ,IV,PR, etc.)

-Nursing considerations

legal right to manufacture or sell drugs

patent medications contain a brand name that clearly identify the product

-purpose- to protect the public so that they could receive "safe" medications

-requires prescriptions for high doses of narcotic drugs and mandate that pharmacists and physicians keep narcotic records.

-corrected certain loop holes in previous laws

-first law preventing the sale of newly developed drugs that had not been thoroughly tested for safety before marketing

-drug labels were required to contain instructions for safe use

-this law was also the first attempt at regulating cosmetics and medical devices

-law did not clearly define "prescription" or specify which drugs required a prescription allowing many harmful and addictive drugs to be sold by corner druggists

-Ammendment to the FDCA delineated the difference between safer drugs, which may be sold over the counter, and more dangerous drugs that required prescriptions

-Drug companies offered developmental grants, tax credits for clinical investigation expenses, and 7 years exclusivity to market an orphan drug.

- Over 700 medications have been approved as orphan drugs since the passage of this act.

-Law needed because drug companies were reluctant to develop drugs for these disorders because there would not be enough sales to recoup their research and development costs

-Introduced to control misleading industry claims

-regulation of these products remains less stringent then other OTC drugs

-Law provides for a standard benefit that pays 75% of prescription drug spending up to the first $2,250.

-Those qualifying for the low income criteria may have their premiums and cost subsidized by the government

-Participants are protected against catastrophic costs at $3,600 per year with most beneficiaries paying a 5% co-pay amount.

-First comprehensive publication of drug standards

-A medical reference summarizing standards of drug purity, strength, and directions for synthesis

-All drug products were covered in USP

-First began in 1862 when president Lincoln appointed chemist to head agency for food and drugs in United States

-FDA established by PFDA of 1906 and later expanded to carry out the provisions of FDCA of 1938

-One of the oldest drug regulatory agencies in the world

-Protecting the bublic health by assuring the safety, efficacy, and security of human and veterinary drugs, biological products, medical devices, the nation's food supply, cosmetics, and products that emit radiation

-Advancing the publ;ic health by helping to speed innovations that make medicines and foods more effective, safer, and more affordable

-Helping the public get the accurate, science based information they need to use medicines and foods to improve their health

1)Center for Biologics Evaluation and research

2)Center for devices and radiological health

3)Center for drug evaluation and research

4)center for food safety and applied nutrition

5)center for veterinary medicine

6)National center for toxicological research

1) Preclinical Research

2)Phase 1

3) Phase 2

4)Phase 3

5) NDA Accepted

6) NDA Approved

7) Post marketing Surveillance

-if a drug appears promising, pharmaceutical company submits IND application to FDA that contains all the animal and cell testing data

-Scientists at the FDA study the data and must be convinced that the drug is safe enough to allow human testing,

-Approval from FDA is necessary before the next stage can begin

-second stage of drug testing

-takes place in 3 stages termed clinical phase trials

-longest part of drug approval process and occur in sequential stages

-Testing conducted on 20-80 healthy volunteers for several months to determine proper dosage and to assess for adverse effects

-Focus of phase 1 is on safety

-If unacceptable levels of toxicity are noted, clinicals are stopped

-Several hundred patients with the disease arte given the drug

-Primary focus is on effectiveness, although safety and data continue to be recorded

-usually compared to an inert substance or placebo which serves as a control "nontreatment" group

-May be compared to a standard drug used for the same condition

-Large number of patients with the disease are given the drug to determine patient variability

-potential drug-drug interactions are examined

- Patients with chronic conditions such as cardiac, renal, or hepatic impairment are given the drug to determine safety in these important populations

-Assessment of effectiveness and safety continues for several years and thousands of patients may be given the new drug during phase 3

-If drug continues to show promise through the clinical phase trials, a new drug application (NDA) is submitted to the FDA

-The NDA signals that the pharmaceutical company is ready to sell the new drug

-During NDA review, the FDA examines all the preclinical and clinical data to assess whether the proposed new drug is safe and effective.

-By law, the CDER is obligated to act on at least 90% of the NDAs for standard drugs within 10 months of submission. For priotiry drugs, the benchmark is 6 months

-If the NDA is approved, the manufacturer may begin selling the new drug. If the NDA is rejected, the FDA indicates whether the drug is approvable or not approvable

-"Approvable" means that the drug will likely be approved if the pharmaceutical company conducts additional testing or addresses specific issues identified by the FDA.

-"Not Approvable" means that a drug has significant barriers to approval

-Stage 4 of drug Approval process

-Begins after the NDA review has been completed.

-Purpose of stage 4 is to survey for harmful drug effects in a larger population

-Some adverse effects are very subtle, take longer to appear, and are not identified until a drug is prescribed for large numbers of people

-Adverse reactions are reported by manufacturers, health care providers and patients to the adverse event reporting system (AERS), a computerized database designed to support the FDAs postmarketing surveillance program.

-Caucasion males were predominantly used in drug research studies

-Women were excluded due to hormonal changes and pregnancy

Drug study results performed on causcasian males were generalized to females and other races

-Written by MD's, Nurse Practitioners, Physician Assistants

-Prescription rights vary by state

-Must be written for all drugs considered as RX

-OTC drugs do not require RX

Zyrtec

Claritin

Pepcid

Prilosec

-Highest Addictive

-The drug or other substance has a currently accepted medical use in treatment in the United states

-I.E. Heroin, Lsd, Peyote

-Highest Addictive

-The drug or other substances has a currently accepted medical use in treatment in the United States or a currently accepted medical use with severe restrictions

-I.E. Opioids (morphine), demerol, Dilaudid

-Less potential for Addiction

-The drug or other substances has a currently accepted medical use in treatment in the United States

-I.E. -Codeine, hydrocodone, Immediate-acting Barbituates

-Lower potential for addiction

-The drug or other substance has a currently accepted medical use in treatment in the United States

-I.E.- Benzodiazipines, long acting barbituates

-Lowest potential for addiction

-The drug or other substance has a currently accepted medical use in treatment in the united states

-I.E.- Cough medicines with codeine, Lomotil

-The pt is able to understand the reason for being on a particular medication and is able to take their medications as directed.

-The pt does not understand what the drug does

-The pt misunderstands the correct amount of drug to take

-Poly-Pharmacy

-Financial Issues

-Side effects of the drug

-Pts education

-Use of Critical Thinking Skills

-ADPIE

-Creative Ideas

-Expiration date: approximation date of when drugs lose their effectiveness

-Light: Some medications are degraded by exposure to light, should be stored out of direct light, often housed in amber colored containers, some meds are covered in foil because they are so sensitive to light

-Moisture and Air: some drugs interact with atmospheric gases or with water vapor, should be stored with tightly capped lids, storage in areas with high humidity will enhance deterioration

-Narcotic considerations: must be stored in lockers or boxes, access must be restricted from theft or misuse

By mouth

Subcutaneous route

Intravenous route

drop

Everyday

Twice per day (0800-2000)

Three times per day (0800-1600-2400)

Four times per day (0600-1200-1800-2400)

ml

L

mg

g

kg

minims

fluid dram

fluid ounce

pint

grains

tsp

tbsp

cup

quart

drops

=15-16 minims

or

=15-16 drops

=1 fluid drams

or

=1 tsp

or

60 drops

tablets and capsules

liquids

sublingual

dermatalogic prepartations are drugs applied to skin

-Include: creams, lotions, ointments, gels, powders, and sprays

-Transdermal patches contain a certain amount of medication

-rate of dosage may vary

-drugs given through this route avoid the first-pass effect of the liver and bypass digestive enzymes

-examples: nitroglycerine; scopolamine (motion sickness); testosterone;

eye drops

ointment

ear drops

sprays

inhalations

nasogastric and gastrostomy tubes

suppositories: rectal; vaginal

-intramuscular: ventrogluteal; dorsogluteal; deltoid; vastus lateralis; z track

-subcutaneus (subq)

-Intradermal

Intravenous injection:

radial vein

median cubital (just below bicept, antcubical)

cephalic vein (lateral anterior bicept)

Basilic vein (medial bicept)

-study of drug movement throughout the body

-what body does with med after administration

-crossing plasma membranes to reach targtet cells

-movement of chemical from an area of higher to lower concentration (IV- blood to tissue)

-may need a carrier (transport) proteins to cross membrane

-Movement across membranes vs their gradient from low to high concentration

-requires expenditure of cell energy and carrier protein (pumps)

1)Absorption

2)Distribution

3)Metabolism

4)Elimination & Secretion

-Drug molecules move from site of administartion to bloodstream

topicals

enterals

parenteral

IV

-absorbed across skin

-absorbed across mucous membrane of: vangina ;respiratory tract ; Nasal passages

Absorbed across membranes lining GI tract

Blood vessels in skin

-Directly into bloodstream (not absorbed)

-most rapid onset of action

IV - most rapid onset of action

Inhalation- rapid response

SQ/IM- absorbed rapidly (less than IV/Inhalation)

Tablets/capsules- slow absorption, must disolve

liquid formulations faster than tablets

Topicals- absorb slowly, keratin layer thick

-drug concentration and dose

-Higher dose = faster/greater response

-Creates greater diffusion rate

-most absorption in small intestine

-motility influences

-blood flow to absorption site

-Affects ability to cross plasma membranes & be excreted

-Acids absorbed in acids because they are non-ionized

-Bases absorbed in bases because they are non-ionized

-May delay/slow absorption

-food may delay/ slow absorption

-high fat meals

-larger increases absorption

-any preventable event that may cause or lead to inappropriate medicatio use or lead to inappropriate medication use or patient harm while medication is in control of the health care professional, patient, or consumer

-National Coordinatig council for medication error reporting and prevention (NCC MERP) classiifes in index

-Index categorizes errors by evaluating exten of harm error causes

dose

medication

patient

Infuencing Factors:

blood flow to tissues

-heart, liver, kidneys= highest exposure to drug

-skin, adipose tissue= least exposure

-lipid- soluble =more completely distributed

-water -soluble= less completely distributed

-high affinity= bone marrow, teeth, eyes, adipose tissue

Na Pentothan, valium

bind to plasma proteins e.g. albumin

form drug-protein complexes

-too large to cross capillary membranes (trapped coumadin)

-compete with other drugs for plasma protein binding sites (tagment displaces warfin)

-endothelial cells sealed and thick basement membrane

-astrocytes secrete chemicals adjusting capillary permeabiltiy

protect fetus

-ineffective for: alcohol, cocaine, caffeine, some prescription drugs

-process used by body to chemically change a drug molecule for excretion (usually)

-liver primary site

-kidneys and cells of intestinal tract-high rates

-changes from lipid-soluble to water soluble (absorption-distribution-excretion)

-chemical changes create metabolites-usually less active

-metabolites may be more active (90% inactive-codeine: 10% morphine)

-CYP= an enzyme metabolizes drugs, nutrients, endpgenous substances

-over 50 isozymes of cytochrome P450

-Drugs as:

substrate for enzyme- when drug metabolized by CYP

enzyme inhibitor-inhibit action of cyp isozyme

-enzyme inducers- drug increases metabolic activity in the liver/inactivation

-completely metabolized to inactive form on first trip through liver before enter general circulation

-bypass by giving sublingual, rectal, parenteral (still pass through liver)

kidneys

lungs

urine

glandular

renal:

primary site of excretion

dependent on PH of filtrate in the renal tubule

impaired kidney function affects

dependent on factors afecting gas exchange

diffusion

gas solubility

blood flow to lungs

excrete most drugs in unmetabolized form

water-soluble drugs secreted into:

saliva

sweat

breast milk

feces- certain oral excreted in feces

no absorption (worms, meds, barium sulfate)

-Bile: excreted in bile- "biliary excretion"

-drug enters duodenum via common bile duct and leaves body in feces

-enterohepatic recirculation: may be recirculated numerous times with bile back to liver

-prolongs activity

-directly related to concentration in plasma

-measure serum concentration:

minimum effective concentration

therapeutic range

toxic concentration

-length of time drug concentration remains in therapeutic range

drugs duration of action

-length of time required for plasma concentration of drug to decrease by 1/2 after administration

-long term- higher risk for adverse effects

-discontinued drug takes 4 half lives un til "functionally" eliminated (94%)

goal to keep drug plasma levels continually

next dose before plasma level falls

larger intitial dose

primes the bloodstream

quicker therapeutic range

keeps plasma levels @ therapeutic level

-study of drug concentration and its effect on the body in relation to the amount of drug in the plasma

median effective dose

-measures the index/ or range of the drug in relation to being safe or toxic

-median effective dose

-median toxicity dose- 50% of group patients

50% of lab rats death

• median lethal dose
• ___________________

median effective dose

occurs @ lowest doses

few target cells affected

-relationship between amoint of drug given and degree of response

-twice the drug =twice the response

-increasing drug= no more therapeutic effect

may produce adverse effects

onset

-peak= highest plasma drug concentration at a given time (estimated maximum efficacy)

IV drug=10 mintues

oral drugs= 3 hours: shows rate of absorption

-Duration of action

-trough- lowest plasma concentration od drug (drawn/measued before next dose) shows elimination

-ability of drug to reach therapeutic effect at lower dose comparted to other drug in same class

-more potent produces therapeutic effect @ lower dose

-maximal response that can be produced from drug

which is most important

-a cellular molecule to wich a med binds to produce its effect

-the drugs specific target

-response proportional to concentration of receptors bound

-enhance or inhibit normal cell function

-drugs with ability to bind to a receptor and produce action

high or low

-once receptor is occupied, second messenger events triggered in cell

-stimulates or inhibits normal activity of cell

--change permeabiltiy of cellular membranes

-depress membrane excitability

-alter activity of cellular pumps

-nonspecific mechanisms

-drug produces same response as receptor it is bound to

-enhances the desired effect

-partial agonist= weaker effect

-drug intentionally responds by blocking action of receptor it attaches to

-used when body producing too much of a response to endogenous chemical or drug overdose

unpredictable reaction

unexplained reaction

predictable

may occur @ therapeutic doses

less serious than adverse reactions

can be dose related

common side effects

nausea, heartburn, diatthea, etc

FDA defines

result in patient death, hospitilization or disability

cause congenital abnormally

case life threathening event

require intervention to prevent permanent damage

-take a thorough medical history

-thoroughly assess patient/diagnostic data

-prevent medication errors

-monitor pharmacotherapy S/S carefully

-know the drugs adverse effects

-be prepared for the unusual

-question unusual orders

-teach patients about adverse effects

-due to hypersensitive reaction to drug causing release of mast cells, eosinophil, basophils, or lymphocytes triggering allergic responses

-may be exposed to class of drugs over period of time and then develop allergic reaction

-characteristics= occurs with small or normal dosed drug (not proportional to dose)

-unrelated to the action of drug

-cross allergy

-common reactions

PCN -rash

radiologic contrast media

preservatives

-Category A= adequate studies in pregnant women show no risk to fetus

-Animal studies show no harm to fetus but no adequate studies done on pregnant women

Animal studies show adverse effects on fetus but no adequate studies on humans

Positive evidence of human fetal risk but benefits may outweigh the risks (risk-benefit ratio)

Animal or human studies shown fetal abnormalities or toxicity and the risks outweigh the benefits

Assess dehydration , renal function tests, adjust for renal impairment

-Blood Brain Barrier (BBB) controls access of drugs to brain

-Assess for change in behavior, seizure, sedation

-Assess for unexplained muscle pain and CK-MB level, EKG

-monitor liver enzymes

-observe for RUQ pain, anorexia, V/V

rash

urticaria

pruritus

phototoxicity

Decrease in RBC, WBC, platelets

-drug-drug

-food, nutrients and dietary supplememnts

-effects:

drug inhibited

drug enhanced

drug actions changed or new response

presence of food - <

alterations of PH -variable

drug-drug binding - <

Increased peristalsis- variable

slowed gastric emptying -variable

displacement of drug from plasma protein binding site ->

stimulation of cyp: enzyme induction - <

inhibition of cyp: enzyme inhibition

renal excretion - grf- >

interferences of other drugs - <

biliary excretion interferences by other drugs - <

2 drugs similiar therapeutic class produce combined summation response

-effects of 2 drugs greater than would be expected from each individual effect

adding a second drug results in diminished response

"any preventable event that may cause or lead to inappropriate medication use or patient harm while medication is in the control of the health care profesional, patient, or consumer"

-national coordinating council for medication eror reporting and prevention (NCC MERP) classifies in index

-index categorizes errors by evaluating extent of harm error causes

dose

medication

patient

route (of Admin)

time (of delivery)

reason documentation

education

evaluation

right to refuse

-check drugs with a colleague ex. heparin/insulin

-assessment of patient ex:wt/ht, labs

-do not accept a telephone/verbal order

-monitor patient medications for drug-to-drug interactions

-correct incomplete/illegible orders

patient issues

(non compliance, right to refuse, inappropriate use of medication)

identifies look alike drugs

identifies sound alike drugs

-maintaining error reporting program (MERP)

-shares info with FDA

-Provides newsletter: Medication Safety Alert/Safe medicine

-Education programs for healthcare workers

-standardize medication error reporting

-examines causes

-safety information and adverse event reporting program

-medwatch reports safety issues

-medmarx database

0track adverse events and med errors

hospital and healthcare systems

facility dictated policies and procedures

include interventions implemented

allergies

health concerns

OTC/herbals

5-10 rights

renal/hepatic functions

no unacceptable abbreviations

nu verbal drug orders

no unclear orders

patient education

focus on the task

identify patient

correct procedure/technique

double check high-risk drugs

calculate the correct dosage

document on the MAR

open in front of patient

confirm pt swallowed

dont crush SR,EX,XR,LA

Assess pt after giving med

assess for expected outcomes

assess for adverse effects

polypharmacy

reconciliation

list of all medications

-"a systemic, rational method of planning and providing nursing care"

systematic

data:

collection

organization

validation

documentation

data used to:

identify current health problems

develop nursing diagnosis and plan of care

patient history

analysis of assessmnet data

identification of health problems

formulation of nursing diagnosis:

used to set goals

set interventions- plan of care

constant flux

problem/risk for problem "related to" etiology

north american diagnosis association (NANDA)

Hierarchy

-acute confusion, related to drug effects

-Deficient fluid volume, related to drug effects

-Excess Fluid volume, related to drug effects

-risk for injury, related to drug effects

-deficient knowledge, related to new drug therapy

-ineffective health maintenance, related to knowledge deficit

prioritizes diagnosis

formulates desired outcomes

selects nursing intervention (evidenced based)

evaluation criteria

determine if goal is met

puts plan into action

achieve goals

patient achieves optimal wellness

-compare current health status with desired outcome

-determine if goal/outcome achieved

-does plan/intertvention require revision

poly pharmacy

drug interactions

multiple medications - comorbidities

multiple pharmacies

otc drugs

GI absorption:

slows, usually complete

decreased GI motility

decreased blood flow to/from GI tract

increased gastric PH

decrease in total body water for dilution

-increased fat storage in elderly lowers plasma/increases tissue levels

-reduced plasma protein levels + higher plasma levels

reduced hepatic function

decreased liver mass

diminished liver blood flow

altered activity of some hepatic enzymes

extended duration of action of drugs

mainly by kidney

decreased receptors in kidney

check creatinine/creatinine clearance

-no more symptoms 36%

-Financial 35%

-Belief of non-effective 33%

-Dont believe needed 33%

-Side/Adverse effects 23%

-Prevented from doing other things wanted 25%

-if needed, make sure patients eyeglasses clean and hearing aids in working order

-Speak in tone of voice thay can hear

-use large print and bright colors for teaching aides

-label with instructions

-use schedule dosing calendar

-document new signs of confusion-engage family

-review all medications on every new encounter with pt

-follow-up calls

-report adverse signs

-"socially transmitted knowledge of values, beliefs, norms, and lifeways of a particular group that guides their thoughts and behaviours"

-comparative study of cultures to understand similarities and differences across human groups

cultural awareness

cultural knowledge

cultural skills

cultural encounters

cultural desire

-racial and genetic -genetic polymorphism

pharmacokinetics

efficacy

adherence

high risk behaviors

-ethnocultural and racial background

-time away from country of origin

-travel history and language ability

-travel history and language ability

-nonverbal communication practices

-preferred foods and preparation

-health, illness/disease practices

-traditional and folk health practices

-Planning

-develop culturally congruent dietary plan so client understands dietary practices related to drug interactions

-interventions

-involve family in teaching about pharmacotherapeutics

-provide explanations for all Rx and OTC products at level appropriate to client/family

-provide written instruction in client's preferred language

evaluation

-cultural care preservation maintenance

-cultural care accomodation or negotiation

-Cultural care repatterning or restructuring

• -CNS- central nervous system
• Brian
• Spinal cord

-Periphreal Nervous System

nerves that carry messages to and from CNS

-carries nerve impulses to the central nervous system to rest of body

-neuron in PNS are motor and sensory

-Sensory: recognize changes to environment

_motor: respond to changes by moving muscles, respond to changes by secreting chemicals

-somatic nervous system

-autonomic nervous system

nerves that provide voluntary control of skeletal muscle

-provide involuntary control of vital functions of systems

cardiovascular

digestive

respiratory

GU

-controls vital life activities without our awareness

-Contraction of smooth muscle of bronchi, blood vessels, GI tract, eye, GU tract

-contraction of cardiac muscle

-Secretion of salivary, sweat, and gastric glands

-divided into two mostly opposing component branches

sympathetic

parasympathetic

-activated under emergency condition/stress

-fight or flight response to threat

-brain increases alertness/readiness

-heart rate and bp increase

-renin release from kidneys

-blood shunted to skeletal muscle for activity

-liver produces more glucose for energy

-bronchi dilate, breathing faster/deeper

-pupils dilate

-body warms/perspiration increases

-constriction of arterioles

-control adrenal medulla and sweat glands

-release of renin by kidneys (increase bp)

-mobilizes lipids for energy

-peristalsis and urine formation temporarily suspended

-always some degree present- autonomic tone

-effects last longer than those of parasympathetic

-activated in non-stressful situation

-produces "rest and digest response

-promote relaxation/body maintenance activities

digestion increases

peristalsis increases promoting defication

heart rate/bp decline

bronchi constrict/respirations slow

pupil constricts

salivation stimulated constricts breathing

erection of penis

-neurons communicate with each other, muscles, glands

-autonomic nervous system

-preganglion neuron originates in CNS

-connects with nerve outside CNS-ganglia

-Ganglia- neuron cell body waiting to receive action potential

-impulse crosses synapse

-crosses synapse with chemicals- neurotransmitters

-postganglionic neuron terminates on smooth muscle, gland @ specialized synapse called neuroeffector junction

-conveys message to muscle/gland

-preganglionic neuron originates in CNS

-connects with second nerve outside CNS in ganglia (mass of nerve cell bodies)

-information communicatd from nerves to muscles or glands

-message crosses synapse (space between two neurons)

-message uses neurotransmitters (chemicals) to travel from one cell to the other

-neurotransmitters enters synaptic cleft so impulse can cross over

-second neuron (postganglionic) terminates on smooth or cardiac muscle or gland @ neuroeffector junction

-the more neurotransmitters released into synapse=greater/longer lasting response

-directly activate a muscle or gland

-stimulate actions/release of natural neurotransmitters

-meds act at:

preganglionic neuron

ganglia @ synapse

postganglionic neuron at target tissue

-block actions/release/binding/storage/re-uptake of natural neurotransmitters

-Acetylcholine (Ach)

-Norepinephrine (NE)

-neurotransmitters released at cholinergic receptors

-neurons released ACH called cholinergic nerves

-located on postganglionic or neuroeffector cell membranes

-cholinergic receptors bind ACH to continue impulses @ ganglia or cause autonomic action @ neuroeffector tissue

-2 types of cholinergic receptors that bind ACH

Nicotinic

Muscarinic

-located @ preganglionic neurons ending in ganglia in sympathetic (fight or flight) and parasympathetic nervous systems (rest and digest)

-actions resmble those of nicotine

-found in skeletal muscle

-controlled by somatic nervous system and adrenal medulla

-produce profound effects on ANS and somatic nervous system

-Activation of ACH nicotinic receptors causes stimulation

tachycardia

HTN

>tone/motility in digestive tract

-enhances nerve conduction at ganlia

-used to promote skeletal muscle relaxation during surgical procedures

-located postganglionic neurons ending in neuroeffector target tissues in parasympathetic nervous system

-actions resembles those of poisonous mushroom

-found in most sweat glands and blood vessels serving skeletal muscles

-when ach binds to muscarinic receptors=stimulating or inhibiting depending on target tissue

decreased HR

Increased peristalsis

-used to block muscarinic receptors during opthalmic procedures, preanesthetic agents, asthma, bradycardia

-removed from synaptic cleft after effect produced

-Acetylcholinesterase (Ach)

AchE

found at synaptic cleft

-pseudocholinesterase (plasma cholinesterase)

destroys Ach

found in liver

may have genetic deficiency-unable to inactivate plasma Ach or succinylcholine

-primary neurotransmitter released at adrenergic receptors (postganglionic sympathetic nerves/synaptic =adrenergic *think adrenaline)

in sympathetic nervous system (fight or flight)

-its a catecholamine that helps neurotransmission

-inactivated by reuptake which is slower than

-endogenous hormone

-adrenergic receptors are either alpha 1,2 or beta 1,2

-stimulation causes:

-enzymes on inside of plasma membrane to activate

-changes occur within cell

-changes due to messenger, G-protein production initiating cascade

-Alpha 1 receptors stimulation

-receptors release intrcellular calcium stores, cause excitatory effects

-smooth muscle contraction

-sphincter closure

-used for effects on vascular smooth muscle e.g. tx of HTN

-cause mostly inhibitory actions

-stimulation causes:

inhibit norepinephrine (NE) release from sympathetic nerve endings

-suppress outflow of sympathetic activity from brain

-used to decrease blood pressure due to effects on CNS vs ANS

-act by increasing second messenger, cyclic adenosine monophosphate (cAMP) in target cells

-beta 1 receptors

primary tissues served = heart, coronary vessels

stimulation causes "fight or flight reaction"

increase heart rate

increases heart strength of contraction

dilation coronary arteries

kidney release renin to maintain BP

-located in smooth muscle in blood vessels, GI tract, lung

-Stimulation causes:

inhibit vasoconstriction= vasodilation

dilate bronchioles

slow peristalsis

decreased urine production

-50-80% of NE taken back into pregaglionic nerve-reuptake

-repackaged for future use

-destroyed portion by monoamine oxidase (MAO) enzyme

-NE in circulation destroyed by Catechol-O-methyltransferase (COMT) enzyme in kidney/liver cells

-slower inactivation via reuptake vs enzyme destruction of Ach

-specialed type of sympathetic nervous system tissue

-preganglionic neurons from spinal cord terminate in adrenal medulla

-neurons secrete epinephrine and norephhrine directly into blood

effects last longer as directly secreted into blood

-distributed to most body cells, not just those inervated by ANS

-Deactivated by liver

-25-50% of all sympathetic nervous system responses due to adrenal medulla circulation of hormones

-located throughout periphreal nervous system

-in autonomic system

-at neuroeffector junctions in parasympathetic divisions

-at ganglia in parasympathetic and sympathetic divisions

-in somatic nervous system

-at neuromuscular synapses responsible for skeletal muscle contraction

-cholinergic synpases present throughout central nervous system

-dependent an amount of acetylcholine (Ach) interacting with cholinergic receptors

cholinergic agonists/parasympathomimetics

-promote rest and digest responseincrease the action of Ach @ cholinergic receptors

-mimic the parasympathetic neurotransmitter Ach

-direct acting

-drug releases more Ach into synapse or binds directly to Ach receptor

- indirect acting

-drug blocks destruction of Ach allowing more to remain in synapse

-muscarine and nicotinic

-Ach stimulates both types but drugs may be selective for one or the other

-directly stimulate cholinergic receptors @ neuroeffector junctions in parasympathetic nervous system

-Actions:

-increase smooth muscle tone and contractions

-iris contraction producing pupil constriction (miosis)

-contraction of ciliary muscle- allows fluid to drain from anterior chamber

-reducing intaocular pressure pre-op for acute angle closure glaucoma

-pilocarpine to treat open angle glaucoma

-increased GI motility (tone/contractions)

-stimulate smooth muscle of urinary tract-promote emptying

-increased gladular secretion (salivary,lacrimal,sweat,digestive) (treat xerostomia0dry mouth) in sjogrens syndrome

-constriction bronchial smooth muscle (airways narrow) contraindicated with asthma

-decrease heart rate /BP

-may cause reflex tachycardia from receptors in cartotid arteries and aortic arch


-may cause atrial fibrillation in pts with hyperthyroidism

-contraindicated in serious heart disease

-poorly absorbed by GI tract, generally dont cross blood brain barrier

-stimulats smooth muscle contraction post general anesthesia- restore peristalsis

-relaxes sphincter, bladder muscle to contract for urinary retention

-Parasympathomimetic; Muscarinic agonist (direct acting)

-parasympathetic actions

-increased salivation

abd cramping

sweating

flushing of skin

miosis (pupil constriction)

blurred vision

N/V

low p/bp

reflex tachycardia

complete hearty block

acute bronchospasm

-suspected bowel obstruction (increased contraction)

-recent GI surgery (excessive GI Contraction)

-Active ulcer or inflammatory disease

-severe bradycardia, hypotension, (slows HR)

-COPD, asthma (bronchoconstriction)

-Hyperthyroid (dysrhythmias)

-Cystitus- force up kidneys if bladder sphincter doesnt open

-do not take with AchE inhibitors-overstimulation of muscarinic receptors

-ganglionic blockers = rapid fall in BP

-Montior BP and pulse, respirsatory status

-Assess urine output (renal excretion)

-obtain thorough PMH

-works to inhibit action AchE

-Allows Ach to remain on cholinergic receptors longer, prolonging its action

-nonselective- affect all Ach synapses

-Alzheimer's disease (mild/mod)- Improves memory and cognition

-Glaucoma - contract iris sphincter/ciliary muscle to decrease intraocular pressure

-Prophylaxis of nerve gas poisoning-cover active site of AchE so toxic agent counldnt bind to enzyme

-Myasthenina gravis- increase strength of muscular contraction

-intense parasympathetic stimulation

miosis

Nausea and vomitting

urinary incontinence

abdominal cramping

-Progression= sympathetic and nicotinic stimulation: muscle twittching, progressive muscle weakness, hyperglycemia

-Antidote: Atropine reverses muscarinic effects

-An autoimmune disorder caused by antibodies attack on nicotinic synapses on skeletal muscle

-muscular weakness and fatigue

-respiratory muscle paralysis/double vision

-ptosis (eyelid drooping) /inability to open eyes

-difficulty chewing or swallowing

-intensive AchE inhibitor therapy (pyridostigmine)

-Corticosteroids- reduce AchE receptor antibody levels

-Generalized muscle weakness that can involve muscles of respirtation including diaphragm

-tx with AchE inhibitor therapy (Neostigmine)

-stimulates the parasympathetic nervous system

-also called parasympathomemetics

-Agonist that help increase Acetylcholine neurotransmitter

-mimic effects of acetylcholine usually at muscarinic receptors

-stimulates the cell to produce a response-tone, strength, and secretions

-increases tone and motility of GI

-Contracts urinary bladder

-Increases pupillary constriction- myosis

-Maintain muscle strength and tone

-receptors located in autonomic ganglia

-synapse with neurons leading to skeletal muscles (nicotinic receptors ) and those leading to effector organs (muscarininc receptors)

-can produce widespread, nonselective effects on body

-stimulates parasympathetic and sympathetic responses

-Actions:

CNS alertness

stimulation of emetic center in CNS (nausea)

increased heart rate

increased BP

-only drug widespread use is nocotine-replacement therapy (nicorette, NicoDerm)

-Example: Smoking cessation Products