Kaplan-Pharmacology Drugs

Front 1

Central NS includes?

Back 1

Brain, spinal cord and pre-ganglionic neurons.

Front 2

Centrally acting drugs affect?

Back 2

the brain - makes you drowsy

Front 3

PNS includes

Back 3

ganglion and post-ganglionic neurons

Front 4

Clonidine

Back 4

Alpha 1 Agonist

Hypertension (pre-ganglionic)>> centrally acting drug. Makes you drowsy.
ADR=Rebound HTN

Front 5

Periphery acting drugs

Back 5

don’t make you drowsy.

Front 6

Drugs can work at

Back 6

1) Axon (only local anesthetics)
2) Or synapse (gap)
3) One nerve to another
4) Direct to muscle (terminal) Somatic).

Front 7

Neurotransmitters are made of

Back 7

protein and glucose, metabolized in Krebs cycle

Front 8

ACh

Back 8

Acetalcholine (comes from AcetylCoA)

Front 9

Drugs that compete w/binding site

Back 9

Competitive antagonist

Front 10

Steps in Nerve transmission

Back 10

1.Synthesis of NT
2.Storage of NT (in nerve endings) most of the time
3.Binding receptor (to match)
4.Action happens
5.Termination (all are degraded)

Front 11

PNS subdivisions

Back 11

1) Autonomic NS
2) Somatic NS

Front 12

Autonomic subdivisions

Back 12

1.Parasympathetic
2.Sympathetic

Front 13

Axonal conduction

Back 13

ONly local anesthetics

Front 14

Synaptic conduction

Back 14

can be selective, influences a specific type of NT

Front 15

Receptors

Back 15

has abilitity to influence behavior of another cell, ultimately depends on ability of that neuron to alter receptor activity on target cell

Front 16

Neoropharmacology

Back 16

Study of drugs that alter processes controlled by Nervous System

Front 17

Brain Stem

Back 17

Midbrain
Pons
Medulla

Front 18

Forebrain

Back 18

cerebrum. Includes Thalamus

Front 19

Somatic NS

Back 19

Voluntary activity: Skeletal muscle contraction

Front 20

Sympathetic NS

Back 20

Adrenergic

Front 21

Parasympathetic NS

Back 21

Cholinergic

Front 22

Automonic NS functions:

Back 22

1. regulation of heart
2. Regulation of secretory glands
3. regulation of smooth muscles
ex: urogenitcal muscles, git, blood vessels.

Front 23

Innervation of SNS and PNS.

Back 23

(generally) opposing action

Front 24

Exception to opposing action of dual innervation SNS/PNS

Back 24

Heart rate and dec. HR. Except in blood vessels. Only sympathetic effect.

Front 25

Complementary innervation SNS/PNS

Back 25

SNS-causes ejaculation
PNS-erection in repro. organs

Front 26

Neurotransmitters in PNS

Back 26

1. Epinephrine - (Epi) most from adrenal medulla
2. Norepinephrine (NE) released in POSTganglionic neurons of the SNS.
3. ACh
4. Dopamine - most junctions in PNS.

Front 27

Forebrain

Back 27

memory learning

Front 28

Temporal

Back 28

speech, hearing

Front 29

Optic nerve

Back 29

decussation ends in occipital lobe vision

Front 30

Sympathetic NT =

Back 30

epinephrine and norepinephrine (Adrenergic)
-adrenergic stimulant = sympathetic stimulant

Front 31

Effects of sympathetic (adrenergic agonist)
similar to "fight or flight"

Back 31

Eye=Pupil dilates=Far vision
Heart=Increased contractility=Pumps faster, HR goes up
Lungs=Bronchials dilate( Need more air to breath
Coronary Arteries=dilate=Increase blood flow to heart. Increased nutrients.
GI=Slows motility=No food digestion
Glucose=Glycogenolysis=More fuel/sugar
Urinary= Detrussor(relax) + Sphincter constricts=No pee pee.
Skeletal Muscles=Contract=RUN
Peripheral blood vessels=Constrict=BP up
Alimentary (poop)=colon GI relax=Sphincter (Constrict)No poop

Front 32

Adrenergic agonists/sympathetic agonists

Back 32

Non-selective: direct action: Epinephrine and Norepineprhine, Isoproterenol

Front 33

1-Epiniphrine Tx for

Back 33

1-anaphylactic shock Subq 0.1 ml of 1:1000 PRN acts in 20 min.

Front 34

2-Epiniphrine Tx for

Back 34

2-Cardiac resuscitation: 1:1000 IV (1mg/ml) acts 5-10 min) can be diluted in 10 ml saline

Front 35

3-Epiniphrine Tx for

Back 35

3-Allergic rxn (bee sting etc).

Front 36

4-Epiniphrine Tx for

Back 36

4-Bronchospasm

Front 37

Indirect acting sympathetic NT (adrenergic agonist). Stimulates the RELEASE of NE

Back 37

Amphetamines (Tx ADHD - improves motor tasks and Narcolepsy)

Front 38

Mixed acting sympathetic NT (adrenergic agonist).Stimulates the receptors AND release

Back 38

Ephedrine. Stimulates adrenergic receptors AND stimulates release of NE.

Front 39

CAUTIONS for using sympathetic agonists

Back 39

HTN: HR goes too high. Prostatic hypertrophy: because constricts sphincter (can't pee pee).
Cardiac arrythmias.

Front 40

More CAUTIONS for using sympathetic agonists

Back 40

Check vital signs q3-5 minutes incl. BP and HR. Check IV site can cause tissue necrosis. check blood sugar (since glycogenolysis is increased)

Front 41

More CAUTIONS for using sympathetic agonists

Back 41

Peudoephedrine (Sudafed, Pedia care, Co-tylenol) are alpha 1 and beta 1 agonists. Tx for nasal congestion. Do not give with cardiac, HTN.

Front 42

Alpha2 agonist

Back 42

Clonidine (catapres) and Methyldopa (aldomet) Tx HTN

Front 43

Caution for Alpha2 agonist

Back 43

Rebound HTN (if withdrawn abruptly)

Front 44

Beta 2 selective agonist

Back 44

Inhalders (relax bronchials) dilaation.

Front 45

Examples of Beta 2 SELECTIVE agonist

Back 45

Terbutaline (bricanyl)
Levalbuterol (Xopenex)
Albuterol (ventolin)
Salmetrerol (Serevent)

Front 46

Beta 1 and Beta 2 NON-SELECTIVE agonist

Back 46

Metaproterenol (alupent)
Isoproterenol (Isuprel)
Ritodrine (Yutopar)

Front 47

Alpha 1 antagonist Tx for HTN

Back 47

Prazocin (minipres)
Doxazocin (cardura)
Phentolamine (regitine)
used for dopamine infiltration, hypertensive emergcency. T 1/2 = 20 min.

Front 48

Tamsulosin-What kind of receptor?

Back 48

Selective Alpha 1 (peripheral) Antagonist.
Tx BPH
Do not drive or operate machinery after 1st dose (b/c Alpha 1 dilates eyes) blurry vision

Front 49

Tamsulosin- TX for

Back 49

Indications

Management of outflow obstruction in male patients with prostatic hyperplasia

Front 50

Tamsulosin-method of action

Back 50

Decreases contractions in smooth muscle of the prostatic capsule by preferentially binding to alpha1-adrenergic receptors

Front 51

Indirect acting sympathetic NT (adrenergic agonist). Stimulates the RELEASE of NE

Back 51

Amphetamines (Tx ADHD - improves motor tasks and Narcolepsy)

Front 52

Alpha 1 (action of stimulation)

Back 52

Blood vessels=Vaso-constrict
Eyes=Dilates
Bladder=contraction (sphincter)
Prostrate=contraction

Front 53

Mixed acting sympathetic NT (adrenergic agonist).Stimulates the receptors AND release

Back 53

Ephedrine. Stimulates adrenergic receptors AND stimulates release of NE.

Front 54

CAUTIONS for using sympathetic agonists

Back 54

HTN: HR goes too high. Prostatic hypertrophy: because constricts sphincter (can't pee pee).
Cardiac arrythmias.

Front 55

Alpha 2 (action of stimulation)

Back 55

Located on nerve terminals. Presynaptic or prejunctional. Regulate NT release. NE can bind to A-2 (on same neuron that (NE was released)>> suppression of further NE release. REDUCE NE.

Front 56

More CAUTIONS for using sympathetic agonists

Back 56

Check vital signs q3-5 minutes incl. BP and HR. Check IV site can cause tissue necrosis. check blood sugar (since glycogenolysis is increased)

Front 57

More CAUTIONS for using sympathetic agonists

Back 57

Peudoephedrine (Sudafed, Pedia care, Co-tylenol) are alpha 1 and beta 1 agonists. Tx for nasal congestion. Do not give with cardiac, HTN.

Front 58

Beta 1 (action of stimulation)

Back 58

Heart=increase HR; Increase force of contraction; Increase AV velocity
Kidney=increase Renin>
vasoconstriction>BP up

Front 59

Alpha2 agonist

Back 59

Clonidine (catapres) and Methyldopa (aldomet) Tx HTN

Front 60

Caution for Alpha2 agonist

Back 60

Rebound HTN (if withdrawn abruptly)

Front 61

Beta 2 (action of stimulation)
Affects the...

Back 61

Arterioles, Heart, Lung, Skeletal muscles=Dilation

Front 62

Beta 2 selective agonist

Back 62

Inhalders (relax bronchials) dilaation.

Front 63

Examples of Beta 2 SELECTIVE agonist

Back 63

Terbutaline (bricanyl)
Levalbuterol (Xopenex)
Albuterol (ventolin)
Salmetrerol (Serevent)
1st choice for COPD b/c less ADRs assoc. w/Beta 1's & HTN.

Front 64

Beta 2 (action of stimulation)
Affects the...

Back 64

Lungs=Bronchodilation (Albuterol)

Front 65

Beta 1 and Beta 2 NON-SELECTIVE agonist

Back 65

Metaproterenol* (alupent) COPD
Isoproterenol* (Isuprel) COPD
Ritodrine (Yutopar) Relax uterus. For premature labor
(Bronchospasm treatment)
DO NOT GIVE TO PATIENT W/HTN B/C NOT SELECTIVE AND *AFFECTS B1- WHICH BP GOES UP. But is more selective for Beta-2.

Front 66

Beta 2 (action of stimulation)
Affects the...

Back 66

GI Tract=increases GI motility
Uterus=Relaxation
Liver=Glycogenolysis
Skeletal muscle=Enhanced contraction, glycogenolysis

Front 67

Beta 2 is like... (my words)

Back 67

Giving birth. uterus relaxes, other muscles contract, more blood sugar, lungs breath better. All blood vessels dilate to lower BP

Front 68

Beta 1 is like (my words)

Back 68

"you betta renin" faster b/c your HR is up and BP is up from renin in kidneys.

Front 69

Alpha 2- is like (my words)

Back 69

The great inhibitor. Opposite to the Alpha male type.

Front 70

Alpha 1- is like (my words)Like the Alpha male, dominant and aggressive

Back 70

dilated pupils, High BP (from constriction), can't pee but can ejaculate

Front 71

Peripheral Adrenergic Receptor Subtypes

Back 71

Alpha 1
Alpha 2
Beta 1
Beta 2

Front 72

Non-selective Alpha 1, B1 and B2 blockers ANTAGONISTS

Back 72

Carvedilol (Coreg) Tx HTN mild to mod. heart failure
Labetalol (trandate) doing surgery.

Front 73

Non-Selective Beta Blockers CANNOT BE USE FOR...

Back 73

asthmatic patients b/c can cause brochoconstriction.

Front 74

Nursing checks for Non-selective Alpha 1, B1 and B2 blockers.

Back 74

low BP and HR and wheezing.

Front 75

Nonselective B1 and B2 ANTAGONIST
Hint >N (in alphabet)

Back 75

Propanolol (interal) tx HTN, supraventricular tachycardia
Pindolol (visken)
Timolol (opthalmic ointment, tx for IOP.
Sotalol (betapace)
(Do not use w/Asthma, Rebound HTN).
Nadolol (corgard)

Front 76

Contraindication of NON-SELECTIVE B1 and B2 ANTAGONIST

Back 76

1) asthmatic patients b/c can cause brochoconstriction.
2) rebound HTN
3) Sedation

Front 77

SELECTIVE B1 ANTAGONIST
Tx HTN

Back 77

Metoprolol (lopressor)
Atenolol (Tenormine)
Esmolol
Betaxolol
(decreases BP, and MI/agina, also used for CHF)
Acebutolol

Front 78

Glucagon counteracts the effect of sympatholytic effect of...

Back 78

beta blockers

Front 79

Cholinergic agonists or parasympathomimetics

Back 79

Direct acting Cholinergic agonists: Acethylcholine

Front 80

Direct acting Cholinergic agonists

Back 80

Bethanicol (urecholine)

Front 81

Muscarinic agonists
“HESE” mimics ACh

Back 81

bethanechol:
1.Heart-down
2.Exocrine glands-gland secretion up
3.Smooth muscles-smooth muscle contract
4.Eye-pupils constrict/lens curves-near vision
HESE - PNS

Front 82

Muscarinic ANTagonists

Back 82

Atropine=
1.Heart-up
2.Exocrine glands-gland secretion dwn
3.Smooth muscles-relax
4.Eye-pupils dilate far vision

Front 83

Ganglionic stimulating agents

Back 83

nicotine-Promotes ganglionic transmission

Front 84

Ganglionic blocking agents

Back 84

mecamylamin-Blocks ganglionic transmission

Front 85

Neuromuscular blocking agents

Back 85

d-Tubocurarine, succinylcholine. Blocks Skeletal muscle contraction

Front 86

Cholinesterase inhibitors

Back 86

increases activation @ ALL cholinergic receptors by inhibiting cholinsterase (which would degrade ACh) so it keeps ACh in the synapse and working.

Front 87

Bethanacol is a selective agonist @ muscarinic cholinergic Rxns. Predict it's actions: (Caution w/Asthma b/c bronchoconstriction)

Back 87

1.Muscarinic receptors: ocular effects (miosis and ciliary muscle contraction)
2.Slow heart rate
3.Bronchial constriction
4.Urination
5.Glandular secretion
6.Stimulation of GI tract
7.Penile erection
8.vasodilation

Front 88

Muscarinic Agonists

Back 88

Cause receptor activation:
1. Heart
2. Exocrine glands
3. Smooth muscles
(lung and GI tract)
4. Eye

Front 89

Muscarinic Agonists (also called Cholinergic)

Back 89

Heart-Bradycardia
Exocrine glands-increase sweating,
glands -secrete>saliva, bronchial secretion and gastric acid
Smooth muscles>(lung and GI tract)>contraction
Eye>Miosis, ciliary muscle contracts
Bladder>Pee pee

Hint 89

All parasympathetic target organs.
1. Eye-constrict
2.Heart-slows
3.Lung-constriction
4.Bladder-relax sphincter, contstrict trigone=pee pee
5. GI tract-constriction
6. Sweat Glands-more secretion
7. Sex organs-more secretion
8.Blood vessels-dilates BP down

Front 90

Muscarinic (cholinergic) Agonists affects on eye

Back 90

Eye-Miosis, ciliary muscle contract>>Pupils constrict, accommodation for near vision.

Front 91

Muscarinic (cholinergic) Agonists affects on smooth muscles

Back 91

Smooth muscles
(lung and GI tract)>contraction>>tone and motility of GI tract (up), bladder emptying>>Vasodilation - BP down

Front 92

Muscarinic (cholinergic) Agonists

Back 92

Resemble stimulation of PS nerve. Also known as PS mimetic agents

Front 93

Bethanacol

Back 93

-Direct acting muscarinic agonist.
-Bind irreversibly to muscarinic cholinergic receptors causes activation
Has little or no effect on nicotinic receptors or ganglia or skeletal muscle.

Front 94

Pharmacological effect-Bethanacol

Back 94

Purpose: alleviates urinary retention (stimulates bladder to empty). By relaxing trigone and sphincter muscles.
Also used to treat GI reflux. Increased GI motility and GI paralysis (but NOT w/obstruction)

Front 95

Bethanacol- CONTRAINDICATED

Back 95

If blockage b/c muscles contract but pee pee can’t come out. Also for asthma, hypotension, coronary insufficiency and hyperthyroidism.

Front 96

Bethanacol- Assessments

Back 96

Assess – I&O
Patient teaching: take 1 hour BEFORE or 2 hours AFTER meals to reduce GI upset.

Front 97

Bethanocol-OVERDOSE:

Back 97

S&S- bradycardia. Atropine (muscarinic antagonist)

Front 98

Toxicology of Muscarinic Agonists- Inocybe and Cilocybe (lots of muscarine)
(Cholinesterase inhibitors)

Back 98

Symptoms:
Excessive activation of muscarinic receptors.
Profuse salivation, lacrimation (tears), visual disturbances, bronchospams, diarrhea

Front 99

Muscarinic Antagonists

Back 99

Anticholinergic Drugs= less ACH. Muscles relax.

Front 100

Muscarinic Antagonists-Anticholinergic Drugs

Back 100

Produce receptor blockade of ACH at muscarinic receptors. Also known as:
-parasympatholytic drugs
-Antimuscarinic, muscarinic blockers
-anticholinergic drugs – ONLY @ muscarinic receptors NOT ALL cholinergic receptors.

Front 101

Muscarinic Antagonists-Anticholinergic Drugs Example

Back 101

Atropine. Used for pre-op to dec. salv. secretions, dilate pupils, relax smooth muscle. Also to treat bradycardia b/c BP goes up when ACH is blocked.

Front 102

Muscarinic Antagonists-Anticholinergic Drugs Effects

Back 102

Heart-HR up
Exocrine-salivation (Xerostomia) - down
Hyperthermia
smooth muscles bronchi (down) tone in bladder (down)
eye-mydriasis (dialates pupil) (far vision)
mild CNS excitation
TOO MUCH hallucinations/delirium, coma, rep. arrest, death

Front 103

Muscarinic Antagonists-Anticholinergic Drugs Effects @low dose

Back 103

Can be blocked at some sites w/low dose

Front 104

Muscarinic Antagonists-Anticholinergic Drugs Effects
@ high dose

Back 104

-more for stomach blockade.
-If give enough for effect, will also cause affects in heart, exocrine glands, smooth muscle and eye.

Front 105

Drug interactions: Some other drugs (not muscarinic antagonists)

Back 105

can also produce blockade (have anti-cholinergic actions). They can enhance effects of atropine and related agents. Avoid use w/atropine, makes effect too strong.
1.Antihistamines
2.Phenothiazine antipsychotics
3.Tricyclic antidepressants

Front 106

Anticholinergic drugs for Overactive bladder (Urge incontinence) (OAB).

Back 106

Four symptoms:
1. Urinary urgency (have to go).
2. frequency (> 8x/24 hours)
3. Nocturia (waking 2+ times/night to go).
4. Urge incontinence (leakage)
Comes from involuntary contraction of bladder detrusor muscle. Detrustor instabilility or overactivity.

Front 107

Drug treatment for Overactive Bladder (OAB)

Back 107

block muscarinic receptors in bladder detrusor, inhibit voiding urge.

Front 108

Drugs treatment for Overactive Bladder (OAB)

Back 108

1. Oxybutynin- (Ditropan, Oxytrol)
a. 2 short acting, 2 long actin, less intense side effects but only 30% effective.
b. IR tabs – works but only modest effectiveness.
c.Undergoes 1st pass effect.
d. Highly lipid soluble, can pass BBB
e. Short half life, need multiple dosing
2. Tolterodine
3.Darifenacin – most selective for M3. Low side effects (ER tabs)

Front 109

Side effects of (OAB) drugs that block muscarinic receptors

Back 109

CNS: drowsiness, confusion, hyperpyrexia.
EENT: blurred vision, cycloplegia, photophobia, dry eyes, mydriasis.
CV: tachycardia, palpitations, arrhythmias.
GI: dry mouth, constipation, impaired GI motility.
GU: urinary hesitancy, retention, impotency.
Resp: tachypnea, pulmonary edema.
Misc: flushing, decreased sweating.

Front 110

How to minimize side effects of OAB drugs

Back 110

1. Use long acting formulation – steady but low dose.
2. Drugs that don’t cross BBB – can’t cause CNS effects
3. Selective for drugs to bladder muscarinic receptors- M3 receptor specific to bladder detrusor. Will NOT cause tachycardia b/c that is an M2 receptor. But will have other less serious side effects.

Front 111

Cholinesterase inhibitors are:

Back 111

drugs that prevent degradation of (ACh) by acetylcholinesterase (ChE). Have broad range of effects. Make ACh work better/longer.

Front 112

Cholinesterase (ChE)

Back 112

Normally ChE breaks down ACh → choline + acetic acid (hydrolysis reaction)

Front 113

Other characterstics of ChE on the break down of ACh

Back 113

2. Involves water = hydrolysis
3. Very fast
4.1 molecule of ChE can break down large amounts of ACh.
5. Prevent inactivation of ACh → enhance actions of ACh from cholinergic Neurons) at:
a.Muscarinic
b.Ganglionic
c.Neuromuscular
6.Therefore C. inhibitors are – indirect acting cholinergic agonist.

Front 114

Cholinesterase inhibitors are:

Back 114

also called...indirect acting cholinergic agonist. (make ACh work better)

Front 115

Purposes Cholinesterase inhibitors:

Back 115

1.Treat Myasthenia Gravis
2.Glaucoma – reduce IOP
3.Treat Alzheimers
4.Antidote to Atropine poisoning.

Front 116

Direct acting Cholinergic agonists (acethycholine)

Back 116

Bethanocol (urecholine) tx to increase urination and abnormal abdominal distention

Front 117

Nursing assessment: Bethanocol
(cholinergic agonist)

Back 117

assess urine output > 600 ml/day check for Orthstatic hypotension

Front 118

Metoclopramide (regland) Tx
(cholinergic agonist)

Back 118

for GERD and gastroperesis (incl. gastric emptying time)

Front 119

Carbachol (miostate

Back 119

cholinergic agonist

Front 120

Pilocarpine(Pilocar) TX

Back 120

IOP due to glaucoma

Front 121

Indirect acting cholinesterase inhibitors (prevent degradation of Ach Tx

Back 121

for alzheimers

Front 122

Other Indirect acting cholinesterase inhibitors

Back 122

1. Tacrine (cognex)
2. Donezepil (aricept)
(enhances cholinergic function).

Front 123

Atropine used for
(Anti-Cholinergic)

Back 123

pre-operative. Decrease salivation and dilate pupils. Antispasmotic to relax smooth muscles and decrease peristalysis. Bradycardia

Front 124

Atropine (secondary) Tx for
(Anti-Cholinergic)

Back 124

anti-muscarinic poinsing like Bethanicol.

Front 125

Cautions for Atropine
(Anti-Cholinergic)

Back 125

COPD, CHF, Renal and hepatic OD

Front 126

Nursing assessment Atropine
(Anti-Cholinergic)

Back 126

Urinary retention, GI obstruction, check vital signs.

Front 127

Other anti-cholinergic drugs

Back 127

Scopalamine, Dimehhydrinate (dramamine) = tx motion sickness.

Front 128

Cholinergic agonists or parasympathomimetics

Back 128

1. Bethanicol (urecholine) OAB
2. Metoclopramide (reglan) GERD
3. Pilocarpine (IOP)
4. Carbachol (miostat)
ADRs - lungs constrict and BP (down)

Front 129

Indirect acting cholinesterase inhibitors

Back 129

prevent degradation of ACh (for Tx Alzheimers

Front 130

Examples of indirect acting cholinesterase inhibitors (CHE-I)
(prevents degradation of ACH)
Tx Alzheimers

Back 130

1. Tacrine (cognex)
2. Donezepil (aricept)

Front 131

Drugs to treat Myasthenia gravis and Multiple sclerosis

Back 131

1)Pryridostigmine (mestinon)
2) Neostigmine (prostigmine) dur. 2-4 hrs. freq. dosing
3) Edrophonium Cl (Tensilon)
(CHE-I) = more ACH. Antagonist. Curare.

Front 132

Myasthenia gravis etiology

Back 132

autoimmune disease involves an antibody response agains the receptors of ACH in skeletal muscles. Leads to degradation of Ach receptors resulting in lack of ACH reaching cholindergic receptors

Front 133

Myasthenia gravis S&S

Back 133

weakness starting in facial muscles, resuling in dysphagia, res. muscle weakness.

Front 134

CAUTIONS W/Pryridostigmine (mestinon)
to treat Myasthenia gravis and Multiple sclerosis

Back 134

Asthma, bradycardia, dysrimias, pregnancy.

Front 135

CAUTIONS W/Edrophonium Cl (Tensilon) to treat Myasthenia gravis and Multiple sclerosis

Back 135

ineffective breathing, myasthenic crisis, resp. depression, bronchospasm.

Front 136

Antagonist for Drugs to treat Myasthenia gravis and Multiple sclerosis

Back 136

Curare (decreases muscle contraction) Too much = total flacid parlysis

Front 137

Non-depolarizing Neuromuscular Blockers I:

Back 137

Tubocurarine

Front 138

MOA Tubocurarine

Back 138

1) Muscle relaxation-during surgery (CNS)
2) Facilitation of mechanical ventiation
3) adjunct to electroconvulsive therapy.
4) Endotracheal intubation
5) Diagnonsis of myasthenia gravis.

Front 139

Parkinson's Disease

Back 139

neurodegenerative disease of extrapryamidal system (NOT Corticospinal) assoc w/disruption of NT w/i striatum. Too little Dopamina. Too much ACH.

Front 140

Parkinson's Disease

Back 140

Characterized by dyskinesias and akinesia

Front 141

Parkinson's Disease

Back 141

proper function of striatum req. balance between NT dopamine and ACh.

Front 142

Parkinson's Disease and dopamine

Back 142

Dopamine usually maintains control of ACh and INHIBIT it's excitatory response.

Front 143

Parkinson's Disease and dopamine

Back 143

Degeneration of dopaminergic neurons result in unopposed Ach thereby causing excititation of GABA

Front 144

Parkinson's Disease S&S

Back 144

Bradykinesia (slow movements) (initiation of movement), and tremors, stooping.

Front 145

Parkinson's Disease DRUGS

Back 145

1) Levodopa (will convert to dopamine and cross BBB).
2) Carvidopa - permits more levopopa to reach striatum nerve terminals (increase lifetime of dopa)
3) Amantadine (dopamine agonist) MAIO (monamine oxidase inhibitor) Increases synthesis of dopamine-agonist)
4) COMT inhibitors.) NOT USED
(used to treat anti-virals, influenza. Now works for anti-parkinson)

Front 146

Dopamine Agents

Back 146

1) Levodopa-promotes dopamine synthesis
2) dopamine agonist - stimulate dopamine receptors directly.
3) Selegiline: Inhibits dopamine breakdown.
4) amantadine: promotes dopamine release.
5) COMT inhibitors: Enhance effects of levodopa by blocking it's degradation.

Front 147

Succinnylcholine (CNS drug)

Back 147

NEUROMUSCULAR BLOCKER. For intubation of clients. Causes paradoxical muscle relaxation.
Cation channels remain open. Short acting (2 min). Causes persistent depolarization.

Front 148

Succinnylcholine (addtl. uses)

Back 148

NEUROMUSCULAR BLOCKER.Muscle relaxation - surgery
Mechanical ventilation
Electroconvulsive therapy
To diagnose Myasthenia Gravis

Front 149

How Succinnylcholine is used to diagnose Myasthenia Gravis

Back 149

NEUROMUSCULAR BLOCKER. Can differentiate between MG and cholinergic crisis. Aggravates MG but no effect on cholinergic crisis.

Front 150

Parkinsons is a problem of...

Back 150

Too little Dopamine (from the Substania Negra) and too much ACH.

Front 151

What are MAOI's

Back 151

Monanamine Oxidase Inhibitors

Front 152

What do MAOI's do?

Back 152

They degrade Epi and NE in the synapse (recycle). Net effect is increase in Dopamine in the synpase.

Front 153

What are MAOI's used for

Back 153

Depression b/c they lack Seratonin and NE, Epi. This increases the amount in synpase. Also to Parkinson's patients.

Front 154

What food(s) are contraindicated for people on MAOI's?

Back 154

Anything that is fermened i.e. Alcohol, aged cheeses, pickles. Can cause HTN Rxn.

Front 155

What kind of disease is Parkinsons?

Back 155

Progressive, degenerative. WE can slow down progression but not cure it.

Front 156

What is pre-cursor to Dopamine and where does it come from?

Back 156

Phenalanine (an essential amino acid) we must eat it, then it's converted to Tyrosine, then Dopamine.

Front 157

What causes lack of Dopamine in Parkinsons Patients?

Back 157

Dopaminic neurons degenerate, resulting in unopposed ACH, causing GABA excitation.

Front 158

Best drugs for Parkinsons

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Levodopa
Carvidopa
(give them what they need)
*Dopamine doesn't easily cross BBB.

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Other drugs for Parkinsons

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Amantadine (promotes Dopamine release)
Selegilne (inhibits dopamine breakdown).

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Altzheimers-what are contributing factors?

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Degeneration of Cholinergic receptors. Development of neuritic plaques.
SSX: memory loss due to dementia.

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Drugs for Alzheimers

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Cholinergic agonists - increase ACH to improve memory.
1. Tacrine (cognex) (CHE-I)
2. Donexepil (aricept)
3. Galantamine (razadyne)
Rivastigmine (excelon) CHE-I

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Alzheimers S&S

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Memory loss
Confusion
Disoriented
Impaired judgement
Personality Changes
Diff. w/self care
Behav. probl. (pacing, watering , agitation, screaming).
Inability to remember family.
Inability to communicate.

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Drugs for Alzheimers

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Cholinesterase Inhibitors. (helps slow progress - not a cure).
ADRs Cholinergic side effects.
GI, Dizzy, Headache, Bronchoconstriction, Liver injury (tacrine). OPPOSITE OF PS.

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NEW Drugs for Alzheimers
(better tolerated)

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Memantine (Namenda)
N-methyl D-aspartate. Receptor antagonists. Lowers amt. of Calcium

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Multiple Sclerosis Disease Process

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Autoimmune disease that attacks myelin sheath of nerve fibers in brain and spinal cord, causing plaques, common 20-40 yr. old white women.

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Multiple Sclerosis Diagnois

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Increase in IgG in the CSF /albumin ratio and multiple lesions in MRI

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Drugs for Multiple Sclerosis

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1. Diazepam (valium) - enhances GABA. Relieve muscle spasm.
2. Muscle relaxants - baclofen
(look for depression, dizzy, cloudy consciousness, hypotension)

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Drugs for Multiple Sclerosis

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1. Since Myelin sheath is made of proteins...give protein
2. Steroid to decrease inflammation.
3. Anti-convulsives

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NEW DRUGS to treat Multiple Sclerosis

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1. Immuno regulators = Interferon Beta. Glycoprotein. Supresses destruction of sheat. AVONEX, REBIF (flu-like ADRs)

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Other NEW DRUGS to treat Multiple Sclerosis

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Glatiramer Acetate (Copaxone or copylomer) similar to glycoprotein structure of myelin sheath.
Mitoxantrone - inhibits DNA and RNA synthesis.

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Other S&S Multiple Sclerosis

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1. Photophobia
1. Spastic Gait
3. Tingling.
4. Inability to reg. Temp.

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CHOLINERGIC (PS) EFFECTS.

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All parasympathetic target organs.
1. Eye-constrict
2. Heart-slows
3. Lung-constriction
4. Bladder-relax sphincter, contstrict trigone=pee pee
5. GI tract-constriction
6.Sweat Glands-more secretion
7. Sex organs-more secretion
8. Blood vessels-dilates BP down

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BETA 2 RECEPTOR ACTIVATION CAUSES

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1. Arterioles, Heart, Skeletal Muscle (Dilation)
2. Bronchi-Dilation
3. Uterus-Relaxation
4. Liver-Glycogenolysis
5. Skeletal muscle-Enhanced contraction, Glycogenolysis

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BETA 1 RECEPTOR ACTIVATION CAUSES

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1. Heart-Increases rate & force of contraction & Increases AV conduction velocity
2. Kidney-Renin release

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ALPHA 2 - RECEPTOR ACTIVATION CAUSES

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Presynaptic nerve terminal-Inhibits transmitter release

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ALPHA 1 - RECEPTOR ACTIVATION CAUSES

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1. Eye-Contracts radial muscle of eye (causes mydriasis)
2. Constricts: Arterioles, Skin
Viscera, Mucous membranes
3. Constricts: Prostate capsule, Veins, Sex Organ, male Ejaculation.
4. Relaxes Bladder-Constricts trigone and sphincter =no pee

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NICOTINIC (N) RECEPTOR ACTIVATION CAUSES

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all automomic ganglia and adrenal medulla- promotes transmission at PS and S POST ganglionic nerve and promotes release of epinephrine

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NICOTINIC (M) RECEPTOR ACTIVATION CAUSES

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Neuromuscular junction-Causes contraction of skeletal muscle.

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Epinephrine is the only NT that works on

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Beta 2 receptors

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Dopamine only works on

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Alpha1 and Beta 1 receptors

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Dopamine only works on

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Dopamine receptors