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PHARMACOLOGY REVIEWER

PHARMACOLOGY
- Greek: pharmakon + logos
- Study of drugs and their actions
- Study of biologic effect of chemicals

DRUGS
- Dutch: droog meaning dry
- Chemical substances that have an effect on living organisms
- Therapeutic drugs

PHARMACOTHERAPEUTICS
- Clinical pharmacology
- Branch of pharmacology involving drugs used to treat, prevent or diagnose disease

MEDICINES
- Therapeutic drugs
- Sources
o Plants
o Animal products
o Inorganic compounds
o Synthetic sources

ROLE IN NURSING CARE

1. PREVENTION
- First level
- Health impact of environment
- Health aspects of social, medicinal and illegal drug abuse

2. EARLY DETECTION OF DISRUPTION IN A HEALTHY CLIENT

- Second level
- Case finding and referral
- Seeks evidence of habituation, toxicity addiction and untoward side effects

3. CARE NEEDED FOR CLIENTS WITH ACUTE HEALTH NEEDS

- Third level
- Institutional setting
- Administering drugs to acutely ill patients

4. REHABILITATION AND RESUMPTION OF NORMAL LIVING

- Fourth level
- Focus  education and assistance
- Long term use of drugs necessary

PHARMACOLOGY IN NURSING EDUCATION

- Integrated in curriculum

PHARMACOLOGY IN RESEARCH
- Drug research
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-Considerations in drug research

o Nurse
 Fully informed
o Information available to physician
o Research and pharmacist
o Recommended dosage
o Route of administration
o Desired therapeutic effects
o Adhere to the study protocol
ETHICAL PRINCIPLES
- Respect for person
o Individuals are independent meaning they are capable of making decisions
- BENEFICENCE – duty to do no harm
- JUSTICE – social benefits can be allocated objectively and that those with equivalent circumstances should be
treated equally

PRINCIPLES OF DRUG ADMINISTRATION

NURSE- should understand professional responsibilities
- Medical administrations
- Medication delivery systems
- Durg orders

DRUG DISTRIBUTIONS SYTEM

1. FLOOR STOCK
- All medications are stocked at nursing station
- Except dangerous drugs
- Utilized in small hospitals, government hospitals

2. INDIVIDUAL PRESCRIPTION PRDER SYSTEM

- Medications dispensed form pharmacy
- Receipt prescription or drug order

3. COMPUTER-CONTROLLED DISPENSING SYSTEM

- Drug order sent to pharmacy
- Encode order to a computer system
- Nurse with the use of security code and password access the system

4. UNIT DOSE SYSTEM

- Single unit packages of drugs
- Dispensed to fell each dose required
- Individual packages placed in individual labelled drawers kept in
- Refilled every 24 hours and large unit dose cabinet; 3 to 7 days in long term facilities

NARCOTIC CONTROL SYSTEM

- Within hospitals
- It is a standard policy that controlled substances are issued in single unit packages and are kept in separate locked
cabinet in each nursing unit
- Head nurse designated individuals is responsible for the key
- When controlled substances are issued to a nursing unit
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DRUG ORDERS

 STAT
- emergency doses
- Meds given ASAP but ONCE only
 SINGLE ORDER
- Administration at a certain time only but once
 STANDING ORDER
- Meds given for a specific number of doses
 PRN (pro re nata)
- For the thing born
- As needed
- Allows nurse to practice judgement to when a medication should be administered
 VERBAL ORDERS
- Should be avoided
- Physician should co-sign and date the order in 24 hours

RESPONSIBILITIES IN DRUG THERAPY

RIGHT
1. Patient
2. Drug
3. Time
4. Dose
5. Route
6. Administration

LEGAL AND ETHICAL

- Practice under professional license

PATIENT’S CHART
- Primary source of information

THE NURSING PROCESS

ASSESSMENT
- Subjective and objective
- Prescriptions
- OTCs
- Herbals
- Responses to medications

NURSING DIAGNOSIS
- Decision about the needs/problems of patient
- Critical thinking, creativity and accurate data

PLANNING
- Goals and outcome criteria
- Specific and measurable
- Patient-centered
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- Time-frame
- Prioritization

IMPLEMENTATION
- Initiation and completion of nursing plans

LEGAL REGULATIONS OF PHARMACOLOGY

1. US PHARMACOPEIA (USP)
- Drug standard revised every 5 years
- Drugs have high standards for therapeutic use
- International Pharmacopeia first published in 1951

2. FEDERAL LEGISLATION
- Public protected from drugs that are impure, toxic, ineffective or not tested prior to public use

3. FOOD, DRUG AND COSMETIC ACT 1938

- To monitor and regulate the manufacture and marketing of drug
- It is FDA’s responsibility to ensure that all drugs are tested for harmful effects have label with accurate
information, an enclose with drugs packaging detailed literature that explains adverse effects

4. DURHAM-HUMPHREY AMENDMENT 1938 (1952)

- Distinguishes between drugs that are solid with or without prescription and those that should not be refilled
without new prescription

5. KEFAUVER-HARRIS AMENDMENT OF 1938 (1962)

- Resulted from the Thalidomide tragedy of the 1950’s
 Taken during first trimester Babies were born with extreme limb deformities

6. COMPREHENSIVE DRUG ABUSE PREVENTION AND CONTROL ACT

- Categorize substances into schedules

7. CONTROLLED SUBSTANCES ACT

- Designed to remedy the escalating problem of drug abuse, included several provisions
o Promotion of drug education and research into the prevention and treatment of drug dependence
o Strengthening of enforcement authority
o Establishment of treatment and rehabilitation facilities
o Designation of schedules or categories for controlled substances according to abuse liability
o CONTROLLED SUBSTANCES
 SCHEDULE I- not approved for medical use, abuse potential and extent of physical and
psychologic dependence are greater with schedule I
 SCHEDULE II to V- have accepted medical use
 SCHEDULE V- limited potential and extent of physical and psychologic dependence
 CODEINE- schedule II but when added to acetaminophen it becomes a schedule II drugs and
when it is used in combination as a cough preparation becomes schedule V drug
NURSING INTERVENTIONS: CONTROLLED SUBSTANCES
 Account for all controlled drugs
 Keep a special controlled-substance record for required information
 Countersign all discarded or wasted medication
 Ensure that records and drugs on hand match
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 Keep all controlled drugs locked up; narcotics must be kept under double lock
 Be certain that only authorized persons have access to the keys
o DRUG ENFORCEMENT ADMINISTRATION of the DOJ- charged with the role of being the nation’s
sole legal drug enforcement agency
8. DRUG REGULATION REFORM ACT1978
- Shortened the time in which new drugs could be developed and marketed
9. DRUG RELATIONS ACCT 1992
- The regulations were change to increase the approval rate of drugs used to treat AIDS and cancer
- Pharmaceutical companies pay a user fee at the time they file the application for the new drug
10. THE FOOD AND DRUG ADMINISTRATION MODERNIZATION ACT 1997
- FIVE PROVISIONS
o Review and use of new drugs is accelerated
o Drugs can be tested in children before marketing
o Clinical trial data are necessary for experimental drug use for serious or life-threatening health conditions
o Drug companies are required to give information on “off-label” drugs and their uses and costs
o Drug companies that plan to discontinue drugs must inform health professionals and clients at least 6
months before stopping drug production
11. HEALTH INSURANCE PORTABILITY AND ACCOUNTABILITY ACT (HIPPA) 2003
- Sets te standards for the privacy of individually indentifiable health information as of 2003
- Gives clients more control over their health information, including boundaries on the use and release of health
records
- Limitations on access to information from the pharmacy
- Pharmacist must provide a private are for consultation with the client and have all clients sign a statement that
they have received a copy of the privacy statement
12. PDIATRIC RESEARCH EQUITY ACT 2003
- FDA is authorized to require testing of drugs and biologic products for safety and effectiveness in children by
drug manufacturers
- One must not assume that children are small adults
13. MEDICARE PRESCRIPTION DRUG IMPROVEMENT AND MODERNIZATION ACT 2003
- Serves to provide financial assistance to seniors to purchase needed prescription medications
-

LEGAL REGULATIONS

1. CANADIAN FOOD AND DRUG ACT OF 1953

- Schedule G and H
- Advertising, labelling and quality
o SCHEDULE F- prescription drugs; no potential for abuse
o SCHEDULE G- written prescription and refills require written or verbal prescription; potential for abuse
and must have a G on the label
o SCHEDULE H- no recognized medical use and are potentially dangerous

2. WHEELER-LEA ACT OF 1938

- Non-fraudulent advertising of drugs food and cosmetics

3. NURSE PRACTICE ACT

- Cannot prescribe or administer drugs without MD order

LEGAL TERM
1. MISFEASANCE
a. Negligence
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b. Nonfeasance
c. Omission
2. MALFEASANCE
a. Giving right drug by wrong route

PHILIPPINE LAWS

1. NATIONAL DRUG POLICY 1987

- Ensures drugs are safe, effective and essential
- Reasonable and affordable

Components
o Quality assurance of drugs
o Rational use of drugs by health professionals and consumers
o Self reliance and self sufficiency
o Targeted drug procurement by government in support for the 1stof 3 pillars

2. GENERIC ACT OF 1988 (RA 6675)

- Identifies by their scientific and internationally recognized active ingredients

ADVANTAGES
- Decreases prices
- Ensures adequate drug supply
- Promote safety
- For scientific basis use of drugs

DISADVANTAGES
- Some have inert fillers and binders that may result in differences in effectiveness
- May have some variation in action or response
- Too long and difficult to pronounce

3. SENIOR CITIZEN ACT

- Provision in which senior citizen will be given 20% discount
4. RA 9502- UNIVERSALLY ACCESIBLE CHEAPER AND QUALITY MEDS ACT OF 2008
- Effective September 2008
- Lowering of drug prices thru free competition and better access to affordable brand
- Generic forms to test, produce and register generic versions of patented drugs
- Prohibits ne patent of newly discovered uses of unknown drugs
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CHAPTER 1
DRUG ACTION: PHARMACEUTIC, PHARMACOKINETIC AND PHARMACODYNAMIC PHASES

PHARMACEUTIC PHASE
- Dissolution- drugs in solid form must disintegrate into small particles to dissolve into a liquid
- Excipients – fillers and inert substances; used in drug preparation to take on a particular size and shape and to
enhance drug dissolution
- Disintegration- breakdown of a tables into smaller particles
- Dissolution – dissolving of the smaller particles in the GI fluid before absorption
- Rate limiting- the time it takes the drug to disintegrate and dissolve to become available for the body to absorb it

** drugs are both disintegrated and absorbed faster in acidic fluids with a pH of 1 or 2 rather than alkaline fluids

- Enteric-coated drugs- resist disintegration in the gastric acid of the stomach, so the disintegration does not occur
until the drug reaches the alkaline environment of the small intestine; should not be crashed

PHARMACOKINETIC PHASE
- The process of drug movement to achieve drug action
1. ABSORPTION
- Movement of drug particles from the GI tract to body fluids by passive absorption, active absorption or
pinocytosis
- Most oral drugs are absorbed into the surface area of the small intestine through the action of the extensive
mucosal villi
- Dec. number of villi = dec. absorption
- Protein-based drugs- ( insulin and growth hormones) destroyed in the s.intestine by digestive enzymes
- PASSIVE ABSORPTION- occurs mostly by diffusion
- ACTIVE ABSORPTION- requires a carrier such as an enzyme or protein to move the drug against a
concentration gradient
- PINOCYTOSIS- process by which cells carry drug across their membrane by engulfing the drug particles
** drugs that are fat soluble pass rapidly through the GI membrane
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** weak acid drugs such as aspirin are less ionized in the stomach and they pass through the stomach lining
easily and rapidly
***calcium carbonate and many of the antifungals need an acidic environment to achieve greater absorption
- FIRST-PASS EFFECT or HEPATIC FIRT PASS- process in which the drug passess to the liver first;
example: Coumadin, morphine
- BIOAVAILABILITY- subcategory of absorption; percentage of the administered drug that reaches the
systemic circulation
- FACTORS THAT ALTER BIOAVAILABILITY
o Drug form
o Route of administration
o GI mucosa and motility
o Food and other drugs
o Changes in liver metabolism

2. DISTRIBUTION
- Process by which the drug becomes available to body fluids and body tissues
- Influenced by blood flow, its affinity to the tissue and protein-binding effect
- VOLUME OF DRUG DISTRIBUTION- dependent on drug dose and its concentration in the body
- Larger Vd = longer half-life
- FREE DUGS- portion of drug that is bound is inactive because it is not available to receptors, and the
portion that remains unbound; are active and can cause pharmacologic effect
- Two highly protein bound drugs = drug accumulation and possible drug toxicity

3. METABOLISM OR BIOTRANSFORMATION
-LIVER – primary site of metabolism
*** Most drugs are inactivated by liver enzymes and are then converted or transformed by hepatic
enzymes to inactive metabolites or water-soluble substances for excretion
- HALF LIFE- the time it takes for one half of the drug concentration to be eliminated
- SHORT HALF-LIFE= 4 to 8 hours
- LONG HALF-LIFE= 24 hours or longer
- Administration of the drug for three to five half-lives saturates the biologic system to the extent that the
intake of drugs equals the amount metabolized and excreted
- STEADY-STATE SERUM CONCENTRATION is the predictive of therapeutic effect

4. EXCRETION or ELIMINATION
- Main route of elimination is through the kidneys
- KIDNEYS filter free, unbound drugs; water soluble drugs and drugs hat are unchanged
- LUNGS eliminate volatile drugs substances and products metabolized to CO2 and H2O
- ACID URINE promotes elimination of weak base drugs
- ALKALINE URINE promotes elimination of weak acid drugs
- ASPIRIN  a weak acid; excreted rapidly in alkaline urine
- SODIUM BICARBONATE – antidote for aspirin
- CRANBERRY JUICE- can decrease urine pH
- CREATININE CLEARANCE- most accurate test to determine renal function; varies with age and gender;
lower in elderly and female clients
- CREATININE- metabolic byproduct of muscles that is excreted by the kidneys
- CREATININE CLEARANCE TEST – 12 or 24 hour urine collection
- NORMAL CREATININE CLEARANCE- 85 to 135ml/min
- AGING- decreases muscle mass and results in a decrease in functioning nephrons

PHARMACODYNAMIC PHASE
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- PHARMACODYNAMICS- the study of drug concentration and its effects on the body
- Primary effect may be desirable; secondary effect may be desirable or undesirable
- DOSE RESPONSE- relationship between the minimal versus the maximal amount of drug dose needed to
produce the desired drug response
- ONSET OF ACTION- time it takes to reach the minimum effective concentration after a drug is administered
- PEAK ACTION- occurs when the drug reaches its highest blood or plasma concentration
- DURATION OF ACTION- the length of time the drug has a pharmacologic effect
- RECEPTORS- protein in structure; found on cell membranes
- LIGAND-BINDING- the site on the receptor in which drugs bind
- FOUR RECEPTOR FAMILIES
o CELL MEMBRANE-EMBEDDED ENZYMES – LIGAND BINDING DOMAIN- on the cell surface;
the drug activates the enzyme and a response is initiated
o LIGAND-GATED ION CHANNELS – the drug spans the cell membrane and with this receptor, the
channel opens, allowing for the flow of ions into and out of the cells. The ions are primarily sodium and
calcium.
o G PROTEIN-COUPLE RECEPTOR SYSTEMS
 Receptor
 G protein than binds with guanosine triphosphate
 Effector that is either an enzyme or an ion channel
o TRANSCRIPTION FACTORS – on the DNA in the cell nucleus and not on the surface of the
cellmembrane
 Drugs act through receptors by binding to the receptor to produce a response or to block a
response
 Activity of many drugs is determined by the ability of the drug to bin to a specific receptor
- AGONISTS- drug that produce a response
- ANTAGONISTS- drugs that block a response
- CHOLINERGIC RECEPTORS- located in the bladder, heart, blood vessels, lungs and eyes
- NON SELECTIVE DRUGS- drugs that affect various sites
- FOUR CATEGORIES OF DURG ACTION
o STIMULATION OR DEPRESSION
 STIMULATION- the rate of cell activity or secretion from a gland increases
 DEPRESSION-cell activity and function of a specific organ are reduced
o REPLACEMENT- replace essential body compounds
o INHIBIT OR KILL- interfere with bacterial cell growth
o IRRITATION
- THERAPEUTIC INDEX- estimates the margin of safety of a drug through the use of a ratio that measure the
effective dose and the lethal dose
o LOW THERAPEUTIC INDEX- have a narrow margin of safety
o HIGH THERAPEUTIC INDEX- wide margin of safety and less danger of a producing toxic effects
- THERAPEUTIC RANGE- between the minimum effective concentration in the plasma for obtaining desired drug
action and the minimum toxic concentration in the plasma for obtaining desired drug action and the minimum
toxic concentration
- PEAK DRUG LEVEL- highest plasma concentration of drug at a specific time
o Orally- 1 to 3 hours
o IV- 10 minutes
- TROUGH LEVEL- lowest plasma concentration of a drug and it measures the rate at which the drug is eliminated
- LOADING DOSE- initial dose
- DIGITALIZATION- the process by which the minimum effective concentration level for digoxin is achieved in
the plasma within a short time
- SIDE EFFECTS- physiologic effects not related to desired drug effects
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- ADVERSE REACTIONS- more severe than side effects; a range of untoward effects that cause mild to severe
side effects including anaphylaxis
- TOXIC EFFECTS or TOXICITY- can be identified by monitoring plasma therapeutic range of the drug
- PHARMACOGENICS- effect of a drug action that varies from a predicted drug response because of genetic
factors or hereditary influence
- TACHYPHYLAXIS- drug tolerance to a frequently repeated administration of a certain drug
- PLACEBO EFFECT- psychologic benefit from a compound that may not have the chemical structure of a drug
effect
PHARMACEUTIC PHARMACOKINETICS PHARMACODYNAMICS
S ABSORPTION DRUG ACTION
DISTRIBUTION RECEPTORS
SOLID FORM METABOLISM OR
LIQUID FORM BIOTRANSFORATION ENZYMES
EXCRETION HORMONES

UNIT FIVE
ADRENERGICS AND ADRENERGIC BLOCKERS
AUTONOMIC NERVOUS SYSTEM AGENTS

- CENTRAL NERVOUS SYSTEM- body’s primary nervous system that consists of the brain and spinal cord
- PERIPHERAL NERVOUS SYSTEM- located outside the brain and spinal cord
- AUTONOMIC NERVOUS SYTEM- acts on smooth muscles and glands; control and regulation of heart, respiratory
system, gastrointestinal tract, bladder, eyes and glands; an involuntary nervous
- AUTONOMIC COMPONENTS OF THE PNS
o AFFERENT NEURONS- sends impulses to the CNS where they are interpreted
o EFFERENT NEURONS- receive the impulses from the brain and transmit those impulses through the
spinal cord to the effector organ cells
- EFFERENT PATHWAYS
o SYMPATHETIC NERVOUS SYSTEM- also known as the ADRENERGIC NERVOUS SYSTEM
 At one time it was believed that adrenaline was the neurotransmitter that innervated the smooth
muscle  NOREPINEPHRINE – the actual neurotransmitter
o PARASYMPATHETIC NERVOUS SYSTEM- called the CHOLINERGIC SYSTEM
 Neurotransmitter at the end of the neuron that innervates the muscle is ACETYLCHOLINE
 Cholinergic receptors are either NICOTINIC or MUSCARINIC
- Drugs that mimic the neurotransmitters norepinephrine and acetylcholine produces response opposite to each
other in the same organ

CNS PNS

BRAIN SPINAL CORD ANS SNS

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PARASYMPATHETIC

BODY TISSUE/ORGAN SYMPATHETIC RESPONSE PARASYMPATHETIC

RESPONSE
EYES Dilates pupils Constricts pupils
LUNGS Dilates bronchioles Constricts bronchioles and increases secretions
HEART Increases heart rate Decreases heart rate
BLOOD VESSELS Constricts blood vessels Dilates blood vessels
GASTROINTESTINAL Relaxes smooth muscles of GI tract Increases peristalsis
BLADDER Relaxes bladder muscle Constricts bladder
UTERUS Relaxes uterine muscle ---------------
SALIVARY GLAND -------------- Increases salivation

SYMPATHETIC STIMULANTS PARASYMPATHETIC STIMULANTS

DIRECT ACTING
SYMPATHOMIMETICS PARASYMPATHOMIMETICS
- adrenergics, adenomimetics - Cholinergics or cholinergic agonists
or adrenergic agonists Decrease blood pressure
Decrease pulse rate
Increase BP Constrict brongchioles
Constrict pupil of eyes
Increase PR
Increase urinary contraction
Relax bronchioles
Increase peristalsis
Dilate pupils of eyes INDIRECT ACTING
Relax uterine muscles CHOLINESTERASE INHIBITORS
Increase blood sugar Increase muscle ton

SYMPATHETIC DEPRESSANTS PARASYMPATHETIC DEPRESSANTS

SYMPATHOLYTICS PARASYMPATHOLYTICS
- Adrenergic blockers, adrenolytics - Anticholinergics, cholinergic
or adrenergic antagonists antagonists or anti spasmodic

Decrease pulse rate Increase pulse rate

Decrease blood pressure Decrease mucous secretions
Constrict bronchioles Decrease gastrointestinal motility
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 ACETYLCHOLINE- between nerves and muscles

 NOREPINEPHRINE AND EPINEPHRINE- catecholamine. Released in the nerves of the sympathetic branch of
ANS
 DOPAMINE- increase in concentration in the brain for coordination of impulses (motor and intellectual)
 GABA- in brain; inhibits nerve activity
 SEROTONIN- limbic system; arousal and sleep; prevents depression and promotes motivation

ANS

 NOREPINEPHRINE  adrenergic NS
 ACETYLCHOLINE  cholinergic NS
 ADRENERGIC- stimulate the sympathetic nervous system; located throughout the body, alpha and beta receptors

CHAPTER 17

ADRENERGICS AND ADRENERGIC BLOCKERS

 ADRENERGICS- drugs that stimulate the sympathetic nervous system

 they mimic the sympathetic neurotransmitters
 they act on one or more adrenergic receptor sites located on the cells of smooth muscles, such as
the heart, bronchiole walls, GI tract, urinary bladder and ciliary muscle of the eye
o ALPHA-ADRENERGIC RECEPTORS- located in the vascular tissues (vessels) of smooth muscles
o STIMULATION OF ALPHA1 RECEPTORS- arterioles and venules constrict. Thereby decreasing
peripheral resistance and blood return to the heart improved circulation and increased blood pressure
o ALPHA2 RECEPTORS- located in the postganglionic sympathetic nerve endings
 When stimulated it inhibits the release of norepinephrine thus leading to a decrease in
vasoconstriction and this results to decrease in blood pressure
o BETA1 RECEPTORS- located primarily in the heart; stimulation increases myocardial contractility and
heart rate
o BETA2 RECEPTORS- found mostly in the smooth muscles of the lung, the arterioles of skeletal muscles
and the uterine muscle
 Stimulation causes
 Relaxation of the smooth muscles of the lungs, resulting in bronchodilation
 An increase in blood flow to the skeletal muscles
 Relaxation of the uterine muscle, resulting in a decrease in uterine contractions
 DOPAMINERGIC- located in renal, mesenteric, coronary and cerebral arteries
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o When stimulated, the vessels dilate and blood flow increases

ALPHA1 RECEPTOR

BLOOD VESSELS EYE BLADDER PROSTATE

VASOCONSTRICTION MYRDIASIS CONTRACTION CONTRACTION

(PUPIL DILATION)

INCREASED BP
ALPHA2 RECEPTOR
INC. CONTRACTIBILITY OF
THE HEART
BLOOD VESSELS SMOOTH MUSCLES
GI TRACT

DEC. BP DEC. GI TONE AND

(REDUCED NOREPINEPHRINE) MOTILITY
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BETA1 RECEPTOR

HEART KIDNEY

INC. HEART CONTRACTION INC. RENIN SECRETION

INC. HEART RATE INC. ANGIOTENSIN

INC BP

BETA2 RECEPTOR

SMOOTH MUSCLE LUNGS UTERUS LIVER

GI TRACT

DEC. GI TONE AND BRONCHODILATION RELAXATION OF UTERINE ACTIVATION OF

MOTILITY
SMOOTH MUSCLE GLYCOGENOLYSIS

INC. BLOOD SUGAR

INACTIVATION OR NEUROTRANSMITTERS

- Caused by
o Reuptake of the transmitter back into the neuron (nerve terminal)
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o Enzymatic transformation or degradation

o Diffusion away from the receptor
- MECHANISM OF NOREPINEPHRINE UPTAKE plays more important role in inactivation of the enzymatic
action