Pharm Exam 1 Flashcards

1
Q

Autonomic Nervous System (ANS)

A

Functions in homeostasis, stress response, and body tissue repair

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2
Q

Primary Neurotransmitters in ANS

A

norepinephrine + acetylcholine

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3
Q

Ligands

A

molecule that binds to another

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4
Q

Affinity

A

how well a drug can bind to the receptors in the ANS

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5
Q

Agonist

A

a ligand that alters receptor function and triggers a physiological response

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6
Q

Antagonist

A

a ligand that binds to a receptor but fails to activate physiological response (or blocks the response)

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7
Q

Signal transduction

A

cascade of intracellular events that occur when receptors located on target tissues are stimulated by a ligand

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8
Q

SNS Receptors

A

Adrenergic

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9
Q

Three Adrenergic Neurotransmitters

A

Norepinephrine, Epinephrine, Dopamine

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10
Q

Monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT)

A

Metabolize norepinephrine and allows reuptake to occur. Also more slowly metabolizes epinephrine

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11
Q

Tyrosine

A

Needed in diet to produce Norepinephrine

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12
Q

Anaphylaxis

A

Narrowing of the airway

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13
Q

Low dose Dopamine

A

increases renal blood flow to try and wake up the kidneys

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14
Q

High Dose Dopamine

A

increases blood pressure or the pumping of the heart

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15
Q

Endrogenous

A

Produced inside the body

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16
Q

Exogenous

A

Produced by an outside force

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17
Q

Catecholamines

A

Can be neurotransmitters or neurohormones depending on where they are synthesized

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18
Q

Alpha 1 Receptors

A

Located in the smooth muscle and in the blood vessels, GI and GU tracts
Stimulation: production of muscle, bladder, and eye contraction

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19
Q

Alpha 2 Receptors

A

Located in the brain/pancreatic beta cells
stimulation: has an antiandrenergic effect which causes the bladder to relax and inhibits insulin release

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20
Q

Beta 1 Receptors

A

located in the cardiac cells
Stimulation: increase in HR and force a contraction

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21
Q

Beta 2 Receptor

A

Located primarily in the smooth muscle of the lungs/skeletal/detrusor and uterine muscles
Stimulation: relaxation of smooth muscles in the lungs to cause bronchodilation

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22
Q

Atenolol

A

Selective Beta One Blocker: this will be good for an asthmatic who needs a lower BP or HR

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23
Q

Selective

A

Act on a receptor site which induces the normally occurring action on that receptor site. Has less effects than non-selective

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24
Q

Non-selective

A

Act on more than one receptor site and has a broader range of effects with more side effects because it is innervating multiple receptors

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25
Q

Phenylephrine

A

Stimulation of the alpha 1s to constrict secretions. Shrinks the nasal vessels to decrease congestion

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26
Q

Which receptors do Norepi stimulate

A

A1, A2, B1

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27
Q

Which receptors does Epi stimulate

A

A1, A2, B1, B2

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28
Q

Midodrine

A

Alpha Adrenergic Agonist: treats orthostatic hypotension. Increases BP

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29
Q

Albuterol

A

selective Beta2 adrenergic agonist. Used to open the airway for someone with a high HR or BP

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30
Q

Isoproterenol

A

non-selective Beta 1 + Beta 2 adrenergic agonist. Not safe for someone with tachycardia or hypertension

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31
Q

Pheochromocytoma

A

a rare neoplasm that secretes catecholamines and is usually found in the adrenal medulla. This is a contraindication for an adrenergic sympathomimetics

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32
Q

Thyroid disease

A

This is a contraindication for an adrenergic sympathomimetics because thyroid hormone increase target cell responsiveness to catecholamines

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33
Q

Hypovolemia

A

Low blood volume. This is a contraindication for an adrenergic sympathomimetics because we don’t want the heart beating faster with little amounts of blood

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34
Q

TCAs

A

Inhibit the reuptake of norepinephrine. This is a contraindication for an adrenergic sympathomimetics

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35
Q

MAOIs

A

inhibits liver metabolism of norepinephrine and epinephrine. This is a contraindication for an adrenergic sympathomimetics.

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36
Q

Parasympathetic Nervous System

A

Cholinergic Receptors

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37
Q

Primary Neurotransmitter of the PNS

A

Acetylcholine (ACH)

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38
Q

Acetylcholine (ACH)

A

Formed in cholinergic nerve endings/located in brain, ANS, and neuromuscular junctions

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39
Q

acetylcholinesterase

A

The enzyme that breaks down ACH

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40
Q

Choline

A

Taken up by presynaptic neurons to make more ACH

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41
Q

Cholinesterase

A

The enzyme that breaks down Choline

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42
Q

PNS Receptors

A

Nicotinic + Muscarinic

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43
Q

Nicotinic

A

located in the CNS motor nerves and skeletal muscle and adrenal medulla
Activation by ACH causes muscle contraction and releases epinephrine from adrenal medulla

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44
Q

Muscarinic

A

located in the internal organs and activation by ACH has effects on cardiac, respiratory, GI, and GU

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45
Q

Direct Acting Ligands

A

bind to and activate receptors themselves to create a cholinergic response in the cholinergic receptors. This has widespread systemic cholinergic effects

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46
Q

Indirect Acting Ligands

A

inhibit the action of AchE which, in turn, has a cholinergic effect because more ACH is able to activate their synapses. This is used to improve muscle tone and strength

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47
Q

Bethanechol

A

Direct Acting Cholinergic agonist. Increases detrusor tone which causes contraction and then micturition which will empty the bladder

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48
Q

Carbachol

A

Direct acting Cholinergic agonist used to treat glaucoma by causing miosis (pupil constriction) which causes constriction which excretes fluid which decreases intraoccular pressure

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49
Q

Donepezil/Aricept

A

Indirect acting cholinergic medication that is a selective acetylcholinesterase inhibitor used for treatment of confusion for Alzheimer pts. More ACH in the brain may compensate for the loss of functioning cholinergic brain cells

50
Q

Pyridostigmine

A

Acetylcholinesterase inhibitor used to treat Myasthenia gravis

51
Q

Atropine

A

Parasympatholytic that stimulates HR, reduces salivation and GI spasms

52
Q

Dicyclomine

A

Parasympatholytic that is used as a GI antispasmodic to treat IBS

53
Q

Propantheline

A

Parasympatholytic used as an antimuscarinic to treat excessive sweating and for cramps/IBS/involuntary urination

54
Q

Meclizine

A

Parasympatholytic: Used to treat motion sickness and vertigo

55
Q

Scopolamine

A

Parasympatholytic that blocks acetylcholine. Can be given as a patch. Treatment for motion sickness. Has an anticholinergic side effect.

56
Q

Glycopyrrolate

A

Parasympatholytic used to decrease oral secretions on oral patients. They are not really breathing so we want to stop salivary secretions to prevent buildup. Also used for cerebral palsy

57
Q

Ipratropium/Atrovent

A

Parasympatholitic that blocks muscarinic receptors and opens airways and causes bronchodilation

58
Q

Tiotropium

A

Anticholinergic for pts with COPD and works as a bronchodilator

59
Q

Anticholinergic Contraindications

A

Glaucoma, GI Conditions, BPH or bladder obstruction, Cardiac Arrhythmias, tachycardia, MI, Renal or hepatic impairment, Pts taking antihistamines, antiparkinsonian drugs, MAOIs and TCAs

60
Q

Physostigmine

A

Used to reverse the effects of certain drugs or subranges that interfere with nerve-muscle communication. Tx of severe anticholinergic toxicity.

61
Q

Ipratropium

A

Anticholinergic used for Asthma because it dilates the lungs out

62
Q

Blood brain barrier drugs requirements

A

must be highly lipid soluble to make it to the brain

63
Q

Where do direct acting cholinergic medications effect

A

PNS because they do not readily enter the CNS

64
Q

Myasthenia Gravis Definition

A

Chronic autoimmune neuromuscular disease. Weakness and rapid fatigue of muscle under voluntary control. Drug therapy for this disease includes CHOLINERGIC drugs and ACETYLCHOLINESTERASE inhibitors

65
Q

Myasthenia Gravis Etiology

A

defect in the transmission of nerve impulses to muscles

66
Q

Myasthenia Gravis Pathophysiology

A

Occurs when normal communication between the nerve and muscle is interrupted at the neuromuscular junction. Or the NMJ.

67
Q

Clinical Manifestations for Myasthenia Gravis

A

facial expression (diplopia: double vision). Dysphagia (trouble swallowing). Dysarthria (slurred speech) choking or aspiration risk. weakness of the eye muscles. SOB.

68
Q

s/sx for Myasthenia Gravis

A

increase with action and improve with rest

69
Q

Neostigmine

A

Acetylcholinesterase Inhibitor used to treat Myasthenia Gravis. Used for long term treatment of myasthenia gravis and as an antidote for nondepolarizing skeletal muscle relaxants used in surgery. Interrupt the enzyme to keep acetylcholine.
Contraindications: cholinergic responses
Does not cross the blood brain barrier

70
Q

Pharmacokinetics of Neostigmine

A

Administered slowly intravenously because it is not absorbed well through GI, metabolized in the liver, excreted in the kidneys. Watch out for folks with hepatic issues, kidneys or liver problems.

71
Q

Action of Neostigmine

A

Decreases the inactivation of acetylcholine in the synapses by the enzyme acetylcholinesterase because it reduces the enzyme.

72
Q

Neostigmine

A

Medication given IV to put electricity through a muscle and see if it contracts

73
Q

Pyridostigmine

A

indirectly increasing the concentration of acetylcholine at the neuromuscular junction and promoting increased cholinergic nicotinic receptor activation

74
Q

SLUDGE

A

Indicators of a cholinergic overdose: Salivation, lacrimation, urinary incontinence, diarrhea, GI upset, emesis

75
Q

Atropine

A

Works on the muscarinic receptors (not the nicotinic) so that you will see changes in the heart, smooth muscles, and glands when this drug is administered to reverse or stop the cholinergic crisis.

76
Q

BAGPUDDLES

A

Bronchoconstriction, apnea, grey vision, pupil constriction, increased urination, diaphoresis, defecation, lachrymation, emesis, seizures. Overstimulation of the PNS

77
Q

Alzheimer’s Disease

A

memory Loss, loss of other intellectual abilities serious enough to interfere with daily life. Etiology: most common form of dementia
Pathophysiology: Deficiency in cholinergic function in the cortex and basal forebrain

78
Q

Drug therapy for Alzheimer’s Disease

A
  1. cholinesterase inhibitors
  2. n-mythyl-d-aspertate receptor antagonists
  3. cholinesterase inhibitor n-methyl-d aspartate receptor antagonist
79
Q

Donepezil

A

Cholinesterase Inhibitor that is used to inhibit acetylcholinesterase and increases stimulation of cholinergic receptors in the CNS/PNS.
Crosses the blood brain barrier.
Side effects: increased Parasympathetic response

80
Q

Pharmacokinetics of Donepezil

A

absorption with oral administration is good and is unaffected with food (PO). Peak of action is 3-4 hours. Metabolizm is in the liver, excretion is mainly in the urine.

81
Q

Sick Sinus Syndrome

A

Sinus node dysfunction. This is not good for pts. taking a cholinesterase inhibitor

82
Q

memantine/namenda

A

N-Methyl-D-Aspartate Receptor Antagonist which blocks flow through NMDA receptors which are a breakout of glutamine which is linked to Alzheimers.

83
Q

memantine/namenda action

A

likes to glutamate receptor for an antagonist effect; binds to the magnesium site to block the excitatory function by slowing intracellular calcium accumulation

84
Q

memantine/namenda pharmacokinetics

A

well absorbed orally, 100% absorption in the GI tract, partially metabolized in the liver

85
Q

Managing Cholinergic Toxicity

A
  1. Hydration
  2. Activated charcoal
  3. atropine: antidote
86
Q

Cholinesterase Inhibitor- N-Methyl-d-aspartate receptor antagonist

A

Combination therapy of donepezil and memantine used for pt. with severe dementia

87
Q

Neurogenic Bladder

A

any condition that impairs afferent and efferent bladder from occurring.

88
Q

Spastic Neurogenic Bladder

A

normal or small volume of urine but involuntary contraction happens. Brian or spinal cord damage (above T12) or detrusor sphincter dysregulation.

89
Q

Flaccid Neurogenic Bladder

A

Large volume of fluid in the bladder, but there is a decrease in pressure so there is an absence of contraction. Can happen from peripheral nerve damage or damage of s2-s4 in the spinal cord.

90
Q

Drug Therapy for Urinary Retention

A

Cholinergic Agonist

91
Q

Bethanechol chloride

A

Cholinergic Agonist used to treat urinary retention. This is well absorbed in the GI tract, site of metabolism is unknown, does not cross the BBB, but crosses the placenta

92
Q

Action of Bethanechol chloride

A

Parasympathomimetic agent, acts at the cholinergic receptors in the urinary and GI tracts to increase muscle tone and cause micturition

93
Q

Parkinson’s Disease

A

chronic, progressive, degenerative disorder of the central nervous system characterized by resting tremor, bradykinesia, rigidity and postural instability. Cause of the nerve cell damage is unknown

94
Q

Pathophysiology of Parkinson’s Disease

A

Progressive destruction of or degenerative changes in dopamine producing nerve cells in the substantia nigra in the basal ganglia, decrease in dopamine and increase in acetylcholine

95
Q

Drug Therapy for Parkinson’s Disease

A

Dopamine receptor agonists, and COMT inhibitors

96
Q

Levodopa-Carbidopa (Sinemet)

A

Dopamine Receptor Agonists used to treat Parkinson’s disease

97
Q

Levodopa-Carbidopa (Sinemet) Action

A

Levodopa produces dopamine in the brain and carbidopa prevents the breakdown of levodopa in the blood so that it can get to the brain and we do not have to give as much as an initial dose. It is well absorbed in the small intestine after oral administration, primarily excreted in the urine.

98
Q

Levodopa-Carbidopa (Sinemet) Cautions

A

Adverse effects: CNS (headache, anxiety, drowsiness, hallucinations) Cardiovascular (orthostatic HTN), increase in HR and decrease in BP. GI: Anorexia (loss of appetite) and N+V and teeth grinding.
MUST STOP TAKING MAOI
Cannot crush it.

99
Q

MOA

A

Mechanisms of Action

100
Q

Other drugs in the class of Levodopa-Carbidopa (Sinemet)

A

amantadine, pramipexole, ropinirole, selegiline.

101
Q

Black Box for Levodopa-Carbidopa

A

risk for fulminant fatal acute renal failure. Check I+O, BUN, Creatinine, and GFR

102
Q

GFR

A

glomerular filtration rate: greater than 60 is normal

103
Q

Ropinirole

A

Can be used with restless leg syndrome. Can also be paired with Levo/Carb if LC is decreased. Well absorbed orally (p=1-2h) steady concentration state of 2 days, 40% protein bound, metabolized in the liver, 1/2 life=6 hours

104
Q

Tolcapone

A

Catechol-o-Methyltransferase Inhibitors (COMT) Add on therapy with LevoCarb. 2-3 hour half life. Tapered off over 2 weeks. Dont quit suddenly

105
Q

Tolcapone Pharmakokinetics

A

absorbed rapidly and is highly protein bound, metabolized in the liver, crosses the placenta, excreted in the feces and urine

106
Q

COMT

A

this enzyme breaks down dopamine and levodopa. If we stop the enzyme, we stop the process from happening. Inhibits the metabolism of levodopa in the bloodstream, may also inhibit COMT in the brain and prolong the activity of dopamine at the synapse

107
Q

Adjudivent

A

Add on therapy

108
Q

Other drug in Tolcapone’s class

A

entacapone

109
Q

entacapone

A

Adjudivent for Levo//Carb. COMT and Decarboxylase Inhibitor. Entacapone alters levodopa to increase serum concentration. Contraindication with MAOI

110
Q

entacapone Adverse Effects

A

GI (diarrhea, N+V, and drug induced colitis) somnolence (not interactive), dyskinesia (bad or dysrhythmic or unusual movement) bruxism (teeth grinding)

111
Q

Anticholinergics Overdose s/sx

A

hyperthermia, mydriasis, delirium, tachycardia, myoclonic movements, seizures, coma, and respiratory arrest. Affects the PNS. Cycloplegia: paralysis of ciliary muscles of the eyes

112
Q

Atropine Sulfate

A

is extracted from the belladonna plant or prepared synthetically. It is a salt that is very soluble in water. This medication is also classified as a muscarinic antagonist.
IV peak: 2-4 minutes and lasts 4 hours
Well absorbed in all forms of administration. Metabolized by liver and excreted in the urine

113
Q

Atropine Sulfate Action

A

blocks the effects of acetylcholine at muscarinic cholinergic receptors that mediate the effects of parasympathetic postganglionic impulses. Pupils dilate

114
Q

Atropine Sulfate Use

A

bradycardia, preoperatively, eye drops, and as an antidote

115
Q

Centrally Acting Anticholinergics Adverse Effects/Contraindications

A

CNS (disorientation, confusion), Cardiovascular (HTN, Tachycardia, heaviness of limbs)
glaucoma, GI, myasthenia gravis, cardiovascular

116
Q

Dicyclomine Hydrochloride Use and Administration

A

Gastrointestinal Anticholinergic used for peptic ulcer disease. Oral and parenteral administration. Metabolized in the liver, excreted in the kidneys

117
Q

Dicyclomine Hydrochloride Action

A

GI smooth muscle relaxant, blocks the effects of acetylcholine at muscarinic cholinergic receptors to help with Irritable bowel syndrome

118
Q

oxybutynin medication and Pharmacokinetic

A

Urinary antispasmodic that is metabolized in the liver and excreted in the urine. Used for bladder instability in patients with uninhibited and reflex neurogenic bladder overactive bladder, incontinence, urgency and frequency

119
Q

oxybutynin action

A

acts directly on the smooth muscle and inhibits the effects of acetylcholine at muscarinic receptors cause antispasmodic effects to reduce urinary bladder muscle

120
Q

oxybutynin caution

A

We cannot give someone who has urinary retention an antispasmodic. Max dose in elders: 2.5mg/PO/bid-tid. Typically given once daily at morning or night.