Pharm 2

Front 1

Selectivity of Drug Action

Back 1

Extremely desirable and beneficial quality for a drug to have
Can allow the drug to treat a specific disease while not effecting other bodily functions

Front 2

3 Main Functions of Autonomic Nervous System

Back 2

Cardiac regulation
Glandular secretions
Smooth muscle regulation

Front 3

acetyolcholine

Back 3

Employed at most junctions of the peripheral nervous system

Front 4

norepinephrine

Back 4

Released by most postganglionic neurons

Front 5

epinephrine

Back 5

Released by the adrenal medulla

Front 6

cholinergic receptors

Back 6

Mediated by acetylcholine

Front 7

adrenergic receptors

Back 7

Mediated by epinephrine and norepinephrine

Front 8

sympathetic action on cardiovascular regulation

Back 8

Maintains blood flow to brain
Redistributes blood flow
Compensates for blood loss
Stimulation of heart – increase HR & CO
Nerves in bld vessels – vasoconstriction
Epinephrine from adrenal medulla – vasoconstriction and certain vasodilation

Front 9

2. Regulates body temperature

Back 9

Regulates blood flow to the skin
Dilates surface vessels: accelerates heat loss
Constricts cutaneous vessels: conserves heat

Promotes secretion of sweat
Promotes secretion of sweat glands: helps the body cool

Induces piloerection: promotes heat conservation

Front 10

3. Fight or Flight (release of epinephrine)

Back 10

Increases heart rate and blood pressure
Shunts blood from the skin and viscera
Dilates the bronchi
Dilates the pupils
Mobilizes stored energy

Front 11

SNS maintains Homeostasis

Back 11

Maintenance of blood flow to the brain
Redistribution of blood flow during exercise
Compensation for loss of blood, primarily by causing vasoconstriction

Front 12

Alpha 1 receptors
sns

Back 12

Blood vessels –constrict
GI sphincter – contract
Bladder sphincter-contract
Penis –ejaculate
Prostate -contraction

Front 13

Beta 1 receptors
sns

Back 13

Cardiac muscle-increase contractility
Atrioventricular node (AV) - increase heart rate
Sinoatrial node (SA) – increase heart rate
Kidney – release of renin

Front 14

Beta 2 receptors
sns

Back 14

Blood vessels – dilation
GI muscles – decreased motility
Uterus – relaxation
Bronchial muscles – dilation
Glycogenolysis
Dopamine
Dilates renal blood vessels

Front 15

Stimulation of Alpha-1 Receptors

Back 15

Vasoconstriction
Increased peripheral resistance
Increased blood pressure (BP)
Pupil dilation (mydriasis)
Closure of the internal sphincter of the bladder

Front 16

Stimulation of Alpha-2 Receptors - centrally

Back 16

Decreased release of NE, reducing sympathetic outflow from brain
Vasodilation

Front 17

Stimulation of Beta-1 Receptors

Back 17

Tachycardia
Increased myocardial contractility
Renin release - vasoconstriction

Front 18

Stimulation of Beta-2 Receptors

Back 18

Bronchodilation
Vasodilation
Slightly decreased peripheral resistance
Increased muscle and liver glycogenolysis
Increased release of glucagon
Relaxation of uterine smooth muscle

Front 19

Cholinergic receptors mediated by

Back 19

Acetylcholine - pre and post ganglionic neurotransmitter

Front 20

Cholinesterase inhibitors

Back 20

Indirectly prevent the breakdown of acetylcholine

Front 21

Principle Actions of Muscarinic Agonists
Bethanechol

Back 21

Slow heart rate – bradycardia
Increase secretions: gastric, bronchial, salivary and sweat
Contract bronchial and intestinal smooth muscle
Contract bladder detrusor muscle and relax sphincter
Miosis and accommodation for near vision

Front 22

Protoype drug

Back 22

A drug typical of drugs in that class.

Front 23

bethanechol mus agonist

Back 23

Urinary retention – major use
Adverse Effects Rare when given orally
Contraindications: weakness of bladder wall or urinary obstruction
-ADR’s -Cardiovascular : hypotension and bradycardia. Contraindicated in patients w/ low BP or CO
- excessive salivation, increased gastric secretions, abdominal cramps and diarrhea.
-Lung muscarinic receptors: cause bronchoconstriction. Contraindicated in asthma
-Hyperthyroid patients are Contraindicated because they cause dysrhythmias

Front 24

Pilocarpine mus agonist

Back 24

Used as an eye drop to produce miosis
Treats: Glaucoma and Increased intraocular pressure
ADR is sweating. Excessive use is broad spectrum of muscarinic effects.

Front 25

Cevimeline

Back 25

Used to treat dry mouth in patients with xerostomia
-ADR (similar to Bethanechol): *** basically muscarinic stimulation adrs
-sweating, nausea,rhinitis,diarrhea.
-hence patients need high fluid intake
-may slow heartrate/increase airway resistance.

Front 26

Muscarinic Poisoning

Back 26

Can be caused by some mushrooms
Overdose of either the direct acting muscarinic agonists or cholinesterase inhibitors
Poisoning Treated with the muscarinic blocker: Atropine – often referred to as an anticholinergic. So it is the antidote for cholinergics but frequently used prototype antimuscarinic.

Front 27

atropine effects

Back 27

prototype, found in many plants, prevents receptor activation by Ach p127
Actions: increases heart rate in patients with bradycardia, relaxes bronchi, decreases secretions, bladder tone, GI
tone/motility, mydriasis (pupil dilater), no effect on vascular smooth muscle tone since there are no parasympathetic
innervation to muscarinic receptors in Blood Vessels
Preanesthetics: helpful during surgeries (like eye and cardiac)
-antidote to muscarinic poisoning (like overdose or mushroom ingestions)
-aids morphine to treat Biliary Colic, intense abdominal pain due to gallstones
-Rare treatments:

Front 28

atropine adrs

Back 28

(Cant See, Pee, Spit or ****!) p 133
-xerostomia, blurry vision, increased intraocular pressure, urinary retention, tachycardia, decreased sweating
(anhydrosis), and asthma from drying of secretions

Front 29

oxybutinin

Back 29

Ditropan) approved only for OAB
-blocks M3 receptor
-Short acting: syrup and IR (immediate release) tablets
-Long acting: transdermal patches, gel, ER (extended release) tablet
ADR less intense with Long acting

Front 30

Darifenacin

Back 30

anticholinergic drug with GREATESt degree of M3 blockade
-treats incontinence
-relaxes destrusor muscle but also blocks m3 receptors outside bladder
-xerostomia, constipation,dry eyes, mydriasis

Front 31

neostigmine effects

Back 31

Protoype and reversible cholinesterase inhibitor p135
-poorly absorbed orally, or by injection via IM, IV, subQ.
-positive charge due to quaternary nitrogen atom (so little CNS effect), cant cross membranes
-ChE splits neostigimine slower than Ach.
Therapeutic Uses: affect muscarinic receptors of NMJ. (Increases force of muscular contractions)
-treats Myasthenia Gravis
-skeletal muscl

Front 32

neostigmine adr and overdose treatment

Back 32

ADR’s: excess cholinergic stimulation, hypotension, bradycardia, miosis, bronchial constriction, urinary urgency. P137
-Cholinergic Crisis: respiratory depression due to NMJ depol blockade and CNS depression.
Overdose Treatment: IV Atropine.
-Respiratory depression treated with mechanical ventilation with oxygen, not drugs.
How it is eliminated: Enzymatic degradation (cholinesterase converts Neo to inactive)

Front 33

physostigimine

Back 33

irreversible cholinesterase inhibitor (due to phosphorus atom)
-highly toxic, mainly for insecticides, may be for terrorism
-NO charge, so can cross
Route: 2 mg by IM or slow IV injection.
Therapeutic uses: Atropine poisoning and drugs that cause muscarinic blockade.

Front 34

Myasthenia Gravis

Back 34

autoimmune, neuromuscular disorder due to fluctuating muscle weakness and rapid fatigue.
• -reduction of NicotinicM receptors on motor end plate
• Symptoms: ptosis (drooping eyelids), difficulty swallowing, skeletal muscle weakness, respiratory muscle
weakness.
• -Antibodies attack NictotinicM receptors on skeletal muscle
• Treatment: symptom relief by Neostigmine

Front 35

Cholinergic Crisis

Back 35

Caused by an overdose of a cholinesterase inhibitor
Medical treatment
Respiratory support
Atropine

Front 36

NEUROMUSCULAR BLOCKING AGENTS:

Back 36

Blocks Ach from NicotinicM receptors on skeletal M.
used in surgery (abdominal wall),helps decrease anesthetic dose therefore decrease anesthetic ADR’s. p149,
Endotrachael Intubation
• Contraindications: Myasthenia Gravis and electrolyte disturbances (low K+ levels reduce paralysis)
• ADR’s: respiratory arrest

Front 37

Competitive Nondepolarizing Neuro Blockers

Back 37

must be administered parenteral
Pharm Effects: muscle relaxation, hypotension, no CNS effect. CAN STILL FEEL PAIN
Therapeutic uses: muscle relaxation during surgery, mechanical ventilation, and endotracheal intubation.
ADR’s: respiratory arrest (muscle paralysis), hypotension
Overdose Treatment: causes prolong apnea, treat with respiratory support plus ChE Inhibitor (neostigmine) to reverse
neuromuscular block
-antihistamines can be given to counter hypotension (high release of histamine) effects of Atracurium (a competitive
agent)

Front 38

Depolarizing Nuero Blockers: SUCCINYLCHOLINE

Back 38

-binds to NicotinicM receptors to cause depol, but it remains bound to prevent repol.
-constant depolarization: Paralysis
-no CNS effect, but can still feel pain.
Pharm Effects: paralysis from drug is preceded by transient contractions and paralysis from drug ends (abates) more
rapidly
Therapeutic Use: muscle relaxation during short procedures (endoscopy, electroconvulsive therapy, endotracheal
intubation)
ADR’s: Apnea, Genetic predisposition (drug can remain for hours instead of days due to low Pseudo cholinesterase p
148) patient has prolong apnea.
-muscle rigidity with high temperature (malignant hyperthermia) genetic, muscle pain, hyperkalemia (drug promotes K+
release from tissues), hypertension, muscle breakdown.
Contraindicated: low pseudoChE, history of malignant hyperthermia, hyperkalemia history, burns, trauma, denervation
of skeletal muscle, and motor neuron injury.
Overdose Treatment: no specific antidote, just supportive. ChE inhibitors prolong the drug by delaying degradation.

Front 39

adrenergic agonists

Back 39

activate adrenergic receptors (similar to sympathetic)
Catecholamine (NE and Epinephrine, dopamine)
-unable to pass BBB, short halflife
-can’t be used orally
-inactivated by MAO
Non-catecholamine (ephedrine, albuterol, phenylephrine)
-can pass BBB, long halflife
-can be oral

Front 40

alpha 1 agonist

Back 40

USES: Mydriasis and Vasoconstriction (most often used for) P155
-stop bleeding due to hemostasis, combined with local anesthetics to delay anesthetic absorption, decrease nasal
congestion, increase BP, dilate pupils.
Drugs: Epinephrine, NE, Phenylephrine, Dopamine
ADR’s: High BP, Hypertension, tissue necrosis if alpha1 leaks into surrounding tissues, reflex bradycardia (compensatory
due to baroreceptor reflex, which decreases heart rate).
Treatment: Tissue necrosis given alpha1 blocking agent (phentolamine)

Front 41

alpha 2 agonist

Back 41

Peripheral receptors are presynaptic and inhibit release of NE. P156
-little periphery significance (not therapeutic), more effective in the CNS (therapeutic)
-acts centrally to reduce sympathetic flow to heart/blood vessels
-relief of severe pain

Front 42

beta 1 agonist

Back 42

Clinically beneficial for the heart. P156
Therapeutic uses:
-improve cardiac performance by increasing force of contraction in patients with heart failure (heart failure - +inotropic)
- treat shock (low tissue perfusion) by increasing heart rate, contraction force, and cardiac output.
-treat AV heart block by enhancing impulse conduction through AV node. Temporary. Pacemaker = long term treatment.
-in Cardiac arrest it’s not preferred, but can start contraction in a heart that stopped beating. Epinephrine administered
by IV or directly to heart.
Drugs: Epinephrine, NE, Isoproterenol, dopamine, dobutamine, and ephedrine.
ADR’s: due to irritation of being stimulated, cardiac tachycardia or dysythmias occur. Myocardial Ischemia (Angina
pectoris from increased oxygen demand [pain] ).

Front 43

Beta 2 agonist

Back 43

Limited to lungs and uterus. P156-157
Drugs: Epinephrine, Isoproterenol, and Albuterol.
Therapeutic Uses:
-selective drugs preferred over less-selective for Asthma (albuterol). Route by Inhalation.
-relaxes uterine smooth muscle to delay preterm labor
ADR’s: Tremor (skeletal muscle) and Hyperglycemia (glycogenolysis to get glucose to muscles to prepare for fight/flight).
Think Bear analogy.

Front 44

dopamine

Back 44

Vasodilation of Kidneys
-reduces risk of renal failure by dilating renal BV
-treats shock, enhances cardiac performance due to beta1 activation in heart.

Front 45

epinephrine

Back 45

Nonselective, broad spectrum (all alpha/beta receptors) P157-159
Therapeutic uses: Cardiopulmonary arrest, Anaphylactic shock (temporary, epipen), asthma, delay local anesthetic
absorption, control superficial bleeding, increase BP, dilates pupil (mydriasis), and treats AV block.
*Epipen (page 158).
ADR’s: P159 multiple due to all 4 receptors stimulated; Hypertensive crisis due to high BP, dysrhythmias due to
sensitivity especially in hyperthyroid patients, Angina pectoris due to high oxygen demand, extravasation (fluid leaking
to other tissues) followed by necrosis, and hyperglycemia by breakdown of glycogen.
Routes: Topical, inhalation, parenteral. Not oral due to MAO inactivation.

Front 46

epinephrine drug interactions and dose

Back 46

Drug Interactions:
- MAO inhibitors suppress MAO, which inactivates catecholamines. Inhibiting MAO prolongs epinephrine effects.
-tricyclic antidepressants block uptake of catecholamines into adrenergic neurons. Prolongs epinephrine effects.
-inhalation anesthetics make the heart hypersensitive, and epinephrine/beta1 agonists can cause tachydysrythmias.
Correct Preparations, Dosage, and Administration:
-Check and monitor IV for less concentrated epinephrine in solution since more would

Front 47

NOREPINEPHRINE

Back 47

Same as epinephrine but doesn’t activate beta2
-limited clinical applications to hypotensive states and cardiac arrest
ADR’s not seen: hyperglycemia (beta2 mediated).
Route: 1mg/mL in IV solution. Monitor and avoid for extravasations.

Front 48

isoproterenol

Back 48

Nonselective beta1 and beta2 stimulant P160
Therapeutic Uses: helps patients with AV heart block, cardiac arrest, and increase cardiac output during shock (beta1
activation)
ADR’s: related to cardiac stimulation. Angina pectoris and tachycardia.
Drug Interactions: like epinephrine. Enhanced by MAO inhibitors and reduced by beta adrenergic blocking agents.

Front 49

dopamine

Back 49

Class: catecholamine. P160. Dopamine receptor.
-Has dose dependent receptor specificity (low=dopamine only, high= alpha1/beta1/dopamine).
Therapeutic Uses: Shock by increasing cardiac output and renal perfusion, Heart failure by increasing myocardial
contractions.
-WAS used for Acute renal failure(ARF) to preserve renal function with low doses. Fail treatment.
ADR’s: tachycardias, dysrhythmias, angina pain, necrosis with extravasation.
Route: IV administration

Front 50

PHENYLEPHRINE

Back 50

Class: Noncatecholamine. P161. On Alpha1 receptor.
Therapeutic Uses: reduce nasal congestion via nasal spray, elevates BP parenterally, mydriasis via eye drops, delays
anesthetic absorption.

Front 51

albuterol

Back 51

Class: Noncatecholamine. On Beta2 receptor.
Therapeutic Uses: replaced isoproterenol for Asthma.
ADR’s: tremor (beta 2 in skeletal muscle) and tachycardia, anxiety
Route: inhalation
Implication: if using more than twice a week or more than one container a month, there is poor control. Need a
maintenance drug to get them in better control of asthma.

Front 52

alpha 1 blockade

Back 52

Treats: hypertension by causing vasodilation, lowers BP. Reverses Alpha1 agonist toxicities. Reduces contraction of
smooth muscle in prostatic capsule and bladder neck of patients with Benign prostatic hyperplasia.
-Raynaud’s Disease: relieves symptoms of pain and cold in toes and fingers by preventing vasoconstriction.
-Pheochromocytoma are tumors of the adrenal medulla. Alpha1 suppresses hypertension and acute hypertension in
surgical procedures.
ADR’s: Most Serious: Orthostatic Hypotension which reduces blood flow to brain when alpha 1 blocks receptors in veins.
Blood pools in veins while standing and venous wall muscle tone is reduced.
-reflex tachycardia, nasal congestion, inhibition of ejaculation, Na+ retention and high blood volume.

Front 53

prasozin

Back 53

Alpha 1 blockade. Selective. P167
Treats: Hypertension
ADR’s: First dose syncope (faint). Don’t drive 12-24 hours after taking. Take before bedtime.
-orthostatic hypotension, reflex tachycardia, inhibition of ejaculation, nasal congestion.
Route: oral

Front 54

BETA-ANDRENERGIC BLOCKADE

Back 54

Reduces heart rate, force of contractions, and velocity of impulse conduction
Therapeutic Uses: Angina Pectoris, hypertension, cardiac arrhythmias, myocardial infarction, heart failure, stage fright,
glaucoma, migraine, hyperthyroidism, pheochromocytoma.
ADR’s P169: Bradycardia, reduced

Front 55

PROPRANOLOL

Back 55

Nonselective. Blocks beta 1 and beta 2.
-lipid soluble,c an cross membranes including CNS.
Route: Undergoes first pass orally (30%)
Excretion: Urine and feces.
Therapeutic Uses: Cardiovascular disorders. Reduces cardiac output in cardiac beta1 receptors. Suppress renin secretion
by blocking renal beta1 receptors.
-Blocking beta2 receptors: bronchoconstriction in lung, vasoconstriction in certain BV, reduced glucogenolysis in skeletal
muscle and liver.
ADR’s: cardiac and respiratory effects like AV block and bronchoconstriction (increases airway resistance).
Contraindications p171: Diabetes, Severe allergies (anaphylactic shock), patients with heart and respiratory disorders
like heart block and asthma.

Front 56

METOPROLOL

Back 56

Cardioselective. Blocks Beta2.
-high lipid solubility, selective, preferred over nonselective drugs
-like Propranolol, but it doesn’t block bronchial beta2 receptors at usual doses and doesn’t increase airway resistance.
ADR’s: most same like propranolol. But unlike propranolol, metoprolol causes minimal bronchocontstriction and doesn’t
interfere with beta2 glycogenolysis.
Route: Oral 100mg once a day.

Front 57

Centrally Acting Alpha2 Agonists:

Back 57

acts with CNS to reduce firing of sympathetic neurons
-primary use is for hypertension
-similar to direct acting adrenergic receptor blockers
-Drugs: Clonidine, Guanabenz and guanfacine, and Methyldopa and methyldopate.

Front 58

CLONIDINE

Back 58

selective activation for alpha2 receptors in CNS. P177
-reduces sympathetic outflow to heart and blood vessels
Pharmacologic Effects: suppressing nerves to heart may cause bradycardia and decrease in cardiac output. Also
vasodilation (decreased BP).
Therapeutic Use: approved for use of severe pain and hypertension
Route: oral and transdermal (every 7 days on hairless upper arm or torso)
ADR’s: Xerostomia, drowsiness, rebound

Front 59

METHYLDOPA AND METHYLDOPATE:

Back 59

Not an alpha 2 agonist
!!!! Early drug, not 1rst in line.
-gets CONVERTED to alpha 2 agonist in brain stem
Pharm Effects: lowers BP by acting within CNS (supine and standing patients), activates alpha2, and causes vasodilation
(not cardiosuppression).
Therapeutic use: hypertension
ADR’s: Positive Coombs’test and hemolytic anemia. Hepatotoxicity, xerostomia, orthostatic hypertension.