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Pharmacology Test 1 > Lecture 3 > Flashcards

Lecture 3 Flashcards

1
Q

Somatic Nervous System

A

Activates skeletal muscle contraction Consists of motor neurons/sensory neurons Sensory (afferent) – go TO CNS Motor (efferent) - go FROM CNS to skeletal muscle Adjusts to external environment VOLUNTARY

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2
Q

Autonomic Nervous System

A

Further subdivided into Parasympathetic NS and Sympathetic NS Regulates activity of smooth muscle, exocrine glands, cardiac tissue and certain metabolic activities Sensory neurons go from smooth muscle & cardiac muscle TO CNS Motor neurons go to glands, smooth & cardiac muscle FROM CNS Adjust to internal environment INVOLUNTARY

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3
Q

Enteric Nervous System

A

Aka 3rd division of ANS Network of autonomic nerves in gut wall Receives innervation from SNS & PNS and regulates GI motility and secretion Responds to Neurotransmitters – peptides and nitric oxide

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4
Q

Preganglionic neuron

A

cell body in CNS, axon extends out of CNS

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5
Q

Postganglionic neuron

A

innervate an effector outside the CNS

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6
Q

ganglion

A

small mass of nerve tissue containing the cell bodies of neurons

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7
Q

Primary neurotransmitter in Sympathetic Nervous System

A

Norepinephrine (nor adrenaline)

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8
Q

Primary neurotransmitter in Parasympathetic Nervous System

A

Acetylcholine

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9
Q

Acetylcholine

A

Primary NT of PNS. Released at ALL autonomic ganglia (PNS & SNS), at PNS neuroeffector junction (nej), somatic neuromuscular junction (nmj), and some SNS nej- neuroeffector junction

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10
Q

Dopamine (DA)

A

important NT in CNS, and released at several peripheral Sympathetic NS fibers

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11
Q

Parasympathetic Responses

A

Responses are specific Rest & digest Miosis ↑ gi motility/salivation ↑ urination/defaction ↓ heart rate Bronchoconstriction Erection

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12
Q

Sympathetic Responses

A

Responses are diffuse Fight or flight Mydriasis ↓ gi motility/salivation ↓ urination/defaction ↑ heart rate Bronchodilation Ejaculation

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13
Q

Muscarinic Receptors

A

Located at PNS nej, some SNS nej (sweat glands), CNS, and autonomic ganglia Activated by ACH and muscarine Found in body in greater numbers than nicotinic receptors Effects of Stimulation: Mediate smooth muscle contraction (except sphincter contraction) Stimulates gland secretion Decrease heart rate and conduction Bronchoconstriction Peripheral vasodilation Miosis Salivation Lacrimation Urination Defaction GI motility Erection

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14
Q

Nicotinic Receptors

A

Activated by ACH and nicotine Located on autonomic ganglia and when activated will excite neurotransmission Located at somatic neuromuscular junction and when activated will mediate muscle contraction Nicotinic have some opposing effects of muscarinic (tachycardia, HTN)

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15
Q

α1 adrenergic receptors

A

constricts vascular smooth muscle constricts blood vessels Increase basal metabolic rate Located at SNS nej effector (primarily smooth muscle)

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16
Q

α2 adrenergic receptors

A

Inhibition of NE release from nerve endings at pre synaptic post ganglionic neuron (negative feedback) Also located on some postsynaptic tissue & blood platelets

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17
Q

β1 receptor

A

Mediates cardiac stimulation (↑ HR & contractility) Located on SNS effector (cardiac muscle, vascular smooth muscle, renal cells - ↑ renin release) Increased lipolysis

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18
Q

β2 receptor

A

Mediates smooth muscle relaxation Located on SNS effector (bronchioles in lung, uterine smooth muscle and vascular smooth muscle) In liver and muscle – mediate glycogenolysis

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19
Q

Direct agonists

A

Activate postsynaptic receptors

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20
Q

Indirect agonists

A

Stimulate release of NT Inhibit reuptake of NT Inhibit metabolism of NT

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21
Q

Direct antagonists

A

Block postsynaptic receptors

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22
Q

Indirect antagonists

A

Inhibit synthesis of NT Prevent vesicular storage of NT Inhibit release of NT

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23
Q

Bethanechol (Urecholine)

A

direct cholinergic agonist acts at muscarinic only Stimulates bladder w/o significant effects on HR or BP TX of urinary retention post-op & post partum

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24
Q

Carbachol (Isoptocarbachol, Miostat)

A

direct cholinergic agonist For chronic open-angle glaucoma Produce miosis during ophthalmic surgery

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25
Pilocarpine (Isoptocarpine, Ocusert, Salagen)
direct cholinergic agonist (plant alkaloid) Higher affinity for muscarinic receptor Treats glaucoma: stimulate contraction of ciliary muscle fibers ® ↑ aqueous humor outflow ® ↓ Intraocular pressure
26
Cevimeline (Exovac)
direct cholinergic agonist (plant alkaloid) To treat dry mouth associated with Sjogren’s syndrome
27
MOA cholinesterase inhibitor
Inhibit breakdown of ACH at all cholinergic synapses ® increase ACH concentration
28
Donepezil (Aricept)
reversible cholinesterase inhibitor Tx of Alzheimer's Disease
29
Edrophonium (Enlon)
reversible cholinesterase inhibitor very short DOA. Used in Dx of Myasthenia gravis
30
Neostigmine (Prostigmin)
reversible cholinesterase inhibitor Tx of Myasthenia gravis, antidote for skeletal muscle relaxants
31
Physostigmine (Eserine)
reversible cholinesterase inhibitor Tx Overdoses of drugs with anticholinergic effects (i.e. atropine, TCAs)
32
Pyridostigmine (Mestinon)
reversible cholinesterase inhibitor Tx of Myasthenia gravis
33
Ecothiophate (Phospholine)
– Irreversible Cholinesterase Inhibitors (organophosphates) Tx of chronic refractory glaucoma. DOA of up to one week Pesticides (palathion and malathion) Soman (chemical warfare agent)
34
Organophosphate poisoning
Augmented cholinergic neurotransmission at central and peripheral synapses Produces all effects of muscarinic activation SLUDGE, spasm, bronchoconstriction, ↓HR & CO, etc Cholinergic activation in CNS – seizures, respiratory depression, coma Excessive activation of nicotinic receptors Neuromuscular blockade & muscle paralysis Treatment Symptomatic - maintain only Decontamination Antidotes – Use Atropine to counteract ACH and pralidoxime (2-PAM) to regenerate cholinesterase
35
Cholinergic Antagonists Muscarinic receptor antagonists
Plant alkaloids - Atropine, Scopalamine Semi synthetic/synthetic – several
36
Cholinergic Antagonists (Nicotinic receptor antagonists)
Ganglionic blockers Neuromuscular blockers – “curium” Depolarizing neuromuscular blocker - succinylcholine
37
Muscarinic receptor antagonists
BellaDonna Alkaloids -Atropine, scopolamine, hyoscyamine Synthetic/ Semi synthetic – ipratropium, tolterodine, oxybutynin, propantheline, dicyclomine, benztropine, etc Both types inhibit effects of PNS stimulation Smooth muscle relaxation, increase HR & cardiac conduction and inhibit exocrine gland secretion
38
Muscarinic receptor antagonists Ocular effects
Relax iris sphincter ® mydriasis Inhibits lacrimal gland – dry eyes Therapeutic uses – mydriatic to facilitate eye exam (atropine, tropicamide, scopolamine)
39
Muscarinic receptor antagonists Cardiac
Increase HR and AV conduction nTherapeutic Uses: Sinus bradycardia & AV block (atropine)
40
Muscarinic receptor antagonists Respiratory effects
INCREAE Bronchodilation Therapeutic Uses: COPD, emphysema, bronchitis ipratropium (Atrovent) tiotropium (Spiriva)
41
Muscarinic receptor antagonists GI and Urinary Tract Effects
Relax gi muscle, reduce intestinal motility, inhibit gastric acid secretion and urinary retention Therapeutic Uses: TX of intestinal spasms/pain – Hysosamine, Donnatal, Dicyclomine TX of dysuria & urinary incontinence – oxybutynin, tolterodine, darifenacin, solifenacin
42
Muscarinic receptor antagonists CNS effects
TX of motion sickness by blocking cholinergic transmission from vestibular apparatus to vomiting center (Scopolamine patch) TX of Parkinson’s Disease – reduce tremor (benztropine & trihexyphenidyl) CNS side effects include: sedation, confusion, altered mental status
43
Nicotinic Receptor Antagonists
Ganglionic blockers Limited use due to adverse effects Trimethaphan – used rarely for hypertensive emergency Neuromuscular blocking agents Nondepolarizing Depolarizing
44
Neuromuscular blocking agents Nondepolarizing
aka curariforms Atracurium, pancuronium, vecuronium Competitive antagonist of ACH at nicotinic muscle receptors Causes muscle relaxation and paralysis Effects reversed by cholinesterase inhibitors Used for surgery
45
Neuromuscular blocking agents Depolarizing
Succinylcholine Causes “persistent” depolarization Used for surgery Effects not reversed by cholinesterase inhibitors therefore not antidote if an overdose
46
Adrenergic Agonists (3 types)
Direct Acting Agonists Catecholamines (epi, NE, isoproterenol, dopamine and dobutamine) Non-catecholamines (albuterol, clonidine, phenylephrine) Indirect Agonists Amphetamine, cocaine, tyramine Mixed direct/indirect agonists pseudoephedrine
47
Catecholamines
Direct Adrenergic Agonists Rapidly metabolized by monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT) enzymes in gut, liver and other tissues – must give parenterally Effects depend on affinity and specificity for type of Adrenergic receptor
48
Epinephrine
Direct Adrenergic Agonists -Catecholamines Epinephrine – can bind to ALL the adrenergic receptors Vasoconstriction & increase BP (a1) Cardiac stimulation (B1) Bronchodilation & skeletal muscle vasodilation (B2) Used in anaphylactic shock and cardiac arrest
49
Norepinephrine
Direct Adrenergic Agonists -Catecholamines Vasoconstriction & increase BP (a1) Cardiac stimulation (B1) Used in hypotension and shock
50
Isoproterenol (Isoprel)
Direct Adrenergic Agonists -Catecholamines Cardiac stimulation (B1) & Bronchodilation (B2) Used to TX asthma, AV block and bradycardia
51
Dopamine
Direct Adrenergic Agonists -Catecholamines precursor to epi, NE Renal vasodilation (D1) Cardiac stimulation (B1) increase BP (a1) Used to TX cardiogenc shock, septic shock, heart failure and adjunct to fluid administration in hypovolemic shock
52
Dobutamine
Direct Adrenergic Agonists -Catecholamines Highest affinity for B1 receptor Less activity at a1 receptor Used to Tx cardiogenic shock, cardiac arrest and heart failure
53
Phenylephrine (Neosynephrine )
Direct Adrenergic Agonists – Non-catecholamines Vasoconstriction, increase BP and mydriasis (a1) Used as nasal decongestant, ocular decongestant and maintenance of BP during surgery
54
Albuterol (Proventil )
Direct Adrenergic Agonists – Non-catecholamines Bronchodilation (B2) Used in asthma
55
Clonidine (Catapres)
Direct Adrenergic Agonists – Non-catecholamines Inhibits NE release from nerve terminal of postganglionic neuron (feedback inhibition: a2) Used to treat chronic hypertension Can have effects in CNS (sedation)
56
Terbutaline (Brethine )
Direct Adrenergic Agonists – Non-catecholamines Bronchodilation and uterine relaxation (B2) Used to TX asthma and premature labor (tocolytic)
57
Amphetamine
Indirect Adrenergic agonists Increase the release of NE & DA from SNS neurons Vasoconstriction, cardiac stimulation and increase BP Penetrates CNS - CNS stimulation (increases mood and alertness (but decreases appetite)
58
Cocaine
Local anesthetic Simulates SNS by blocking reuptake of NE & DA in the PNS & SNS – similar effects as amphetamine
59
Tyramine
Indirect Adrenergic Agonists Normal by-product of tyrosine metabolism in body Found in high concentrations in fermented foods such as certain cheeses, beers, red wine, certain cured meats (salami & pepperoni) Indirect sympathomimetic b/c it causes the release of stored catecholamines . Normally metabolized by MAO. So if taking an MAO inhibitor must avoid tyramine-containing foods.
60
Mixed acting Adrenergic Agents
Cause vasoconstriction by binding to 1 Increase release of NE from SNS neurons Nasal decongestants – Pseudoephedrine
61
(a) adrenergic receptor antagonists
Nonselective (a)-blockers Selective a1-blockers (“azosin”)
62
B adrenergic receptor antagonists (“olol”)
Nonselective B-blockers Selective B1 blockers
63
Adrenergic Antagonists
Mixed  and  adrenergic receptor antagonists
64
Phenoxybenzamine (Dibenzyline)
Nonselective a-blockers block both areceptors Noncompetitive, irreversible TX hypertensive episodes associated w/ pheochromocytoma (tumor in adrenal medulla that secretes Catecholamines)
65
Phentolamine (Regitine)
Nonselective a-blockers Competitive, reversible DX and TX hypertensive episodes from pheochromocytoma Tx necrosis and ischemia from extravasations of epinephrine
66
azosin
Selective a1-blockers Relax vascular smooth muscle and smooth muscle in bladder and prostate. Produce vasodilation and decrease BP Used to treat hypertension and urinary retention due to benign prostatic hyperplasia (BPH) Agents include: Doxazosin (Cardura), Prazosin (Minipress), Terazosin (Hytrin) nTamsulosin (Floma) Alfuzosin (Uroxatra)– only for BPH not for HTN
67
Selective 1-blockers (“azosin”) Agents
Doxazosin (Cardura ), Prazosin (Minipress ), Terazosin (Hytrin ) Tamsulosin (Flomax) Alfuzosin (Uroxatral)– only for BPH not for HTN
68
Nonselective b-blockers effects
Block b1 receptors in heart and b2 in smooth muscle, liver and other tissues B1 blockade - decrease BP , decrease cardiac output, decrease renin release and decrease aqueous humor secretion B2 blockade – bronchoconstriction, decrease glycogenolysis, mask signs of hypoglycemia TX HTN, angina, arrhythmias, MI, migraine, glaucoma
69
Nonselective B-blockers Agents
Agents include: Propranolol (Inderal), Nadolol (Corgard), Timolol (Timoptic )
70
Selective B1-blockers Effects
Selective for B1 receptors (primarily in cardiac tissue) Produce less bronchoconstriction and other B2 receptor mediated effects Aka cardioselective B-blockers TX HTN, angina, MI
71
Selective 1-blockers Agents
Atenolol (Tenormin), Metoprolol (Lopressor)
72
Mixed a and b receptor antagonists
Block both a and B receptors Carvedilol (Coreg ) – Tx HTN and CHF Labetalol (Trandate ) – Tx HTN
73
Atropine
Muscarinic receptor antagonists BellaDonna Alkaloids
74
Scopolomine
Muscarinic receptor antagonists BellaDonna Alkaloids
75
hyoscyamine
BellaDonna Alkaloids Muscarinic receptor antagonists
76
ipratropium
Synthetic/ Semi synthetic Muscarinic receptor antagonists
77
tolterodine
Synthetic/ Semi synthetic Muscarinic receptor antagonists
78
oxybutynin
Synthetic/ Semi synthetic Muscarinic receptor antagonists
79
propantheline
Synthetic/ Semi synthetic Muscarinic receptor antagonists
80
dicyclomine
Synthetic/ Semi synthetic Muscarinic receptor antagonists
81
benztropine
Synthetic/ Semi synthetic Muscarinic receptor antagonists
82
Atracurium, pancuronium, vecuronium
Nondepolarizing Neuromuscular blocking agents
83
Trimethaphan
Nicotinic Receptor Antagonists Ganglionic blocker used rarely for hypertensive emergency
84

Pharmacology Test 1 (5 decks)

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