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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
Q

Pilocarpine (Isoptocarpine, Ocusert, Salagen)

A

direct cholinergic agonist (plant alkaloid) Higher affinity for muscarinic receptor Treats glaucoma: stimulate contraction of ciliary muscle fibers ® ↑ aqueous humor outflow ® ↓ Intraocular pressure

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26
Q

Cevimeline (Exovac)

A

direct cholinergic agonist (plant alkaloid) To treat dry mouth associated with Sjogren’s syndrome

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27
Q

MOA cholinesterase inhibitor

A

Inhibit breakdown of ACH at all cholinergic synapses ® increase ACH concentration

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28
Q

Donepezil (Aricept)

A

reversible cholinesterase inhibitor Tx of Alzheimer’s Disease

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29
Q

Edrophonium (Enlon)

A

reversible cholinesterase inhibitor very short DOA. Used in Dx of Myasthenia gravis

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30
Q

Neostigmine (Prostigmin)

A

reversible cholinesterase inhibitor Tx of Myasthenia gravis, antidote for skeletal muscle relaxants

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31
Q

Physostigmine (Eserine)

A

reversible cholinesterase inhibitor Tx Overdoses of drugs with anticholinergic effects (i.e. atropine, TCAs)

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32
Q

Pyridostigmine (Mestinon)

A

reversible cholinesterase inhibitor Tx of Myasthenia gravis

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33
Q

Ecothiophate (Phospholine)

A

– Irreversible Cholinesterase Inhibitors (organophosphates)

Tx of chronic refractory glaucoma. DOA of up to one week Pesticides (palathion and malathion) Soman (chemical warfare agent)

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34
Q

Organophosphate poisoning

A

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
Q

Cholinergic Antagonists Muscarinic receptor antagonists

A

Plant alkaloids - Atropine, Scopalamine Semi synthetic/synthetic – several

36
Q

Cholinergic Antagonists (Nicotinic receptor antagonists)

A

Ganglionic blockers Neuromuscular blockers – “curium” Depolarizing neuromuscular blocker - succinylcholine

37
Q

Muscarinic receptor antagonists

A

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
Q

Muscarinic receptor antagonists Ocular effects

A

Relax iris sphincter ® mydriasis
Inhibits lacrimal gland – dry eyes

Therapeutic uses – mydriatic to facilitate eye exam (atropine, tropicamide, scopolamine)

39
Q

Muscarinic receptor antagonists Cardiac

A

Increase HR and AV conduction

nTherapeutic Uses: Sinus bradycardia & AV block (atropine)

40
Q

Muscarinic receptor antagonists Respiratory effects

A

INCREAE Bronchodilation

Therapeutic Uses: COPD, emphysema, bronchitis ipratropium (Atrovent) tiotropium (Spiriva)

41
Q

Muscarinic receptor antagonists GI and Urinary Tract Effects

A

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
Q

Muscarinic receptor antagonists CNS effects

A

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
Q

Nicotinic Receptor Antagonists

A

Ganglionic blockers

Limited use due to adverse effects Trimethaphan – used rarely for hypertensive emergency

Neuromuscular blocking agents Nondepolarizing Depolarizing

44
Q

Neuromuscular blocking agents Nondepolarizing

A

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
Q

Neuromuscular blocking agents Depolarizing

A

Succinylcholine

Causes “persistent” depolarization

Used for surgery

Effects not reversed by cholinesterase inhibitors therefore not antidote if an overdose

46
Q

Adrenergic Agonists (3 types)

A

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
Q

Catecholamines

A

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
Q

Epinephrine

A

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
Q

Norepinephrine

A

Direct Adrenergic Agonists -Catecholamines

Vasoconstriction & increase BP (a1) Cardiac stimulation (B1) Used in hypotension and shock

50
Q

Isoproterenol (Isoprel)

A

Direct Adrenergic Agonists -Catecholamines

Cardiac stimulation (B1) & Bronchodilation (B2) Used to TX asthma, AV block and bradycardia

51
Q

Dopamine

A

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
Q

Dobutamine

A

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
Q

Phenylephrine (Neosynephrine )

A

Direct Adrenergic Agonists – Non-catecholamines

Vasoconstriction, increase BP and mydriasis (a1)

Used as nasal decongestant, ocular decongestant and maintenance of BP during surgery

54
Q

Albuterol (Proventil )

A

Direct Adrenergic Agonists – Non-catecholamines

Bronchodilation (B2) Used in asthma

55
Q

Clonidine (Catapres)

A

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
Q

Terbutaline (Brethine )

A

Direct Adrenergic Agonists – Non-catecholamines

Bronchodilation and uterine relaxation (B2)

Used to TX asthma and premature labor (tocolytic)

57
Q

Amphetamine

A

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
Q

Cocaine

A

Local anesthetic Simulates SNS by blocking reuptake of NE & DA in the PNS & SNS – similar effects as amphetamine

59
Q

Tyramine

A

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
Q

Mixed acting Adrenergic Agents

A

Cause vasoconstriction by binding to 1 Increase release of NE from SNS neurons Nasal decongestants – Pseudoephedrine

61
Q

(a) adrenergic receptor antagonists

A

Nonselective (a)-blockers

Selective a1-blockers (“azosin”)

62
Q

B adrenergic receptor antagonists (“olol”)

A

Nonselective B-blockers

Selective B1 blockers

63
Q

Adrenergic Antagonists

A

Mixed  and  adrenergic receptor antagonists

64
Q

Phenoxybenzamine (Dibenzyline)

A

Nonselective a-blockers

block both areceptors

Noncompetitive, irreversible

TX hypertensive episodes associated w/ pheochromocytoma (tumor in adrenal medulla that secretes Catecholamines)

65
Q

Phentolamine (Regitine)

A

Nonselective a-blockers

Competitive, reversible

DX and TX hypertensive episodes from pheochromocytoma

Tx necrosis and ischemia from extravasations of epinephrine

66
Q

azosin

A

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
Q

Selective 1-blockers (“azosin”) Agents

A

Doxazosin (Cardura ), Prazosin (Minipress ), Terazosin (Hytrin ) Tamsulosin (Flomax) Alfuzosin (Uroxatral)– only for BPH not for HTN

68
Q

Nonselective b-blockers effects

A

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
Q

Nonselective B-blockers Agents

A

Agents include: Propranolol (Inderal), Nadolol (Corgard), Timolol (Timoptic )

70
Q

Selective B1-blockers Effects

A

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
Q

Selective 1-blockers Agents

A

Atenolol (Tenormin), Metoprolol (Lopressor)

72
Q

Mixed a and b receptor antagonists

A

Block both a and B receptors

Carvedilol (Coreg ) – Tx HTN and CHF

Labetalol (Trandate ) – Tx HTN

73
Q

Atropine

A

Muscarinic receptor antagonists

BellaDonna Alkaloids

74
Q

Scopolomine

A

Muscarinic receptor antagonists

BellaDonna Alkaloids

75
Q

hyoscyamine

A

BellaDonna Alkaloids

Muscarinic receptor antagonists

76
Q

ipratropium

A

Synthetic/ Semi synthetic Muscarinic receptor antagonists

77
Q

tolterodine

A

Synthetic/ Semi synthetic Muscarinic receptor antagonists

78
Q

oxybutynin

A

Synthetic/ Semi synthetic Muscarinic receptor antagonists

79
Q

propantheline

A

Synthetic/ Semi synthetic Muscarinic receptor antagonists

80
Q

dicyclomine

A

Synthetic/ Semi synthetic Muscarinic receptor antagonists

81
Q

benztropine

A

Synthetic/ Semi synthetic Muscarinic receptor antagonists

82
Q

Atracurium, pancuronium, vecuronium

A

Nondepolarizing
Neuromuscular blocking agents

83
Q

Trimethaphan

A

Nicotinic Receptor Antagonists

Ganglionic blocker
used rarely for hypertensive emergency

84
Q
A

Pharmacology Test 1 (5 decks)

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