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Puri_pharmacology > Pharm I-The ANS > Flashcards

Pharm I-The ANS Flashcards

1
Q

Na+ dependent transport of choline into the presynaptic nerves is the first step in the synthesis of acetylcholine.

This drugs blocks this step and will stop ACh synthesis.

A

Hemicholinium

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2
Q

Ca++ dependent release of neurotransmitters from autonomic neurons is inhibited by ________.

A

Botulinum toxin

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3
Q

ACh is a neurotransmitter at these sites _______.

A
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4
Q

Inhibitory post-synaptic potential (IPSP) is due to increased permeability of what ion(s)?

A
  1. K+
  2. Cl-
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5
Q

Receptor subtypes for ACh are muscarinic and nicotinic. Which class is G-protein coupled and which is ligand gated ion channel?

A
  1. Nicotinic are ligand gated ion channels
  2. Muscarinic are G-protein coupled
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6
Q

_______ is the site of NM receptors and these receptors are selectively blocked by _______.

A

Neuromuscular junctions (at the ends of somatic nerves), curare (and analogs).

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7
Q

______ is a modified ganglia and has NN receptors; when activated by ACh ______ is released.

A

Adrenal medulla, adrenaline

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8
Q

These muscarinic subtypes activate the IP3-DAG pathway and increase intracellaular Ca2+

A

M1, M3, and M5

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9
Q

Constriction of ______ muscles of the iris causes pupillary constriction termed ______

A

circular, miosis

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10
Q

Activation of _____ receptors causes miosis

A

M3

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11
Q

Activation of _____ receptors contricts the _____ muscles of the iris and causes mydriasis

A

⍺-1, radial

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12
Q

Activation of ____ receptors on the ciliary muscles of the lens helps with far vision by _____

A

β2 receptors, dilation of the ciliary muscles

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13
Q

Activation of _____ receptors on the ciliary muscles of the lens helps with near vision by _____

A

M3 receptors, constriction of the ciliary muscles

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14
Q

Parasympathetic nervous system, via the vagus, DOES NOT supply this part of the heart.

A

The ventricles

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15
Q

Vascular endothelial cells release nitric oxide (EDRF) when this receptor is activated on their cell-surface.

A

M3

* Remember, this will only occur if a muscarinic agonist is given IV as the PNS nerves DO NOT supply the vasculature.

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16
Q

_____ receptor antagonists relax the ______ muscles and are useful t/t options for patients with urinary incontinence.

A

M3, detrusor

* Remember, this effect can cause urinary retention in patients with prostatic hyperplasia/hypertrophy

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17
Q

Agonist for this receptor is used to inhibit uterine contractions and delay premature labor.

A

β2

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18
Q

Male erection is caused by vasodilation induced by_____, which in turn is released by activation ____ receptor

A

Nitric Oxide, M3

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19
Q

Used in the t/t of BPH, blockers of ____ receptors increase urinary flow and cause retrograde ejaculation

A

⍺1

* Remember, ⍺1 receptors mediate contraction of urinary bladder trigone and sphincter, thus inhibit bladder emptying (you don’t wanna pee during flight or fight)

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20
Q

What is tonic pupil?

A

A pupil with parasympathetic denervation that constricts poorly to light but reacts better to accommodation (near response), such that the initially larger pupil becomes smaller than its normal fellow and remains tonically constricted, redilating very slowly when exposed to dark.

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21
Q

ACh when applied to ____ cells causes vasoconstriction, but causes vasodilation when applied to _____ cells.

A

Vascular smooth muscle, endothelial cells

* Both actions are M3-mediated

* This means that when vasculature is denuded of endothelial cells it constricts in response to ACh, while before it dilates.

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22
Q

Name two cholinergic agonists with only muscarinic activity that do not activate nicotinic receptors

A

Pilocarpine

Bethanechol

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23
Q

Agonists of _____ receptors will induce depolarization block at the NMJ and include, ______, ________, _______.

A

NM

ACh, succinylcholine, nicotine

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24
Q

Name key cholinergic agonists that are NOT substrates for hydrolysis by acetylcholinestrases (AChE)

A
  1. Carbachol
  2. Bethanechol
  3. Muscarine
  4. Pilocarpine
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25
Q

Acetylcholinesterase inhibitors will prolong the duration of action of these compounds.

A
  1. Acetlycholine
  2. Methacholine
  3. Succinylcholine is a substrate for plasma cholinestrases
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26
Q

List reversible inhibitors of acetylcholinestrases (AChE).

A
  1. Physostigmine
  2. Neostigmine
  3. Pyridostigmine
  4. Edrophonium
  5. Donepezil
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27
Q

List irreversible inhibitors of acetylcholinestrases (AChE).

A
  1. Organophosphates
    1. ​Dyflos
    2. Echothiophate
    3. The “thions”-parathion, malathion
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28
Q

The only AChE inhibitors to be orally absorbed and cross the blood-brain barrier and cornea are?

A

Physostigmine and organophosphates

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29
Q

When physostigmine is preadminstered in a pateint, what is the expected change in HR with vagal stimulation?

A

Marked fall in HR. Greater than vagal stimulation alone.

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30
Q

List major clinical uses of AChE inhibitors.

A
  1. Myasthenia gravis-orally, large doses of neostigmine and pyridostigmine
  2. Open angle glaucoma-eye drops physostigmine-work by contracting circular ciliary muscles
  3. To reverse competitive NMJ block after a surgery-i.v neostigmine
  4. Donepezil for alzheimer’s d/s
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31
Q

List cardinal symptoms of organophosphate poisoning

A
  1. Muscarinic effects
    1. ​Excessive salivation and respiratory secretions-the patient is “drowning” in his/her secretions
    2. Pinpoint pupils
    3. Bronchoconstriction
    4. Involuntary defecation and urination
    5. Convulsions and coma
  2. Effects of NN receptors on ganglia
    1. Activation of SNS ganglia causes tachycardia, hypertension and arrhythmias
  3. Effects of NM receptors on NMJ
    1. Muscular fasciculations
    2. Depolarizing block causing paralysis of respiratory muscles (cause of death)
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32
Q

List two drugs used in the t/t of organophosphate poisoning

A
  1. Atropine
  2. Pralidoxime-AChE reactivator
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33
Q

List major effects of cholinergic antagonists.

A
  1. Glandular secretions dry up first
  2. Tachycardia is next
  3. Mydriasis, photophobia and paralysis of accommodation
  4. ↓ GI motility and secretions
  5. Bladder contractions ↓
  6. Bronchodilation
  7. Hallucinations and delirium
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34
Q

Quaternary anticholinergic compound with incomplete oral absorption used in the t/t of COPD

A

Ipratropium bromide

Tiotropium bromide

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35
Q

Orally acting, potent antimuscarinic used for pre- anesthesia to reduce glandular secretions

A

Glycopyrrolate

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36
Q

Direct acting smooth muscle relaxant with antimuscarinic properties used in the t/t of irritable bowel syndrome

A

Dicyclomine

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37
Q

Selective M1/M3 antagonist used in the t/t of urinary incontinence and overactive bladder

A

Oxybutynin

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38
Q

Short acting, topically active anticholinergic for mydriasis during test for refraction

A

Tropicamide

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39
Q

Describe the symptoms of anticholinergic overdose (e.g. belladonna poisoning, tricyclic antidepressants overdose, scopolamine overdose)

A
  1. “Red as a beet” – Cutaneous vasodilation occurs as a means to dissipate heat by shunting blood to the skin, in order to compensate for the loss of sweat production.
  2. “Dry as a bone” (anhidrosis) – Sweat glands are innervated by muscarinic receptors, so anticholinergic medications produce dry skin.
  3. “Hot as a hare” (anhydrotic hyperthermia) – Interference with normal heat dissipation mechanisms (ie, sweating) frequently leads to hyperthermia.
  4. “Blind as a bat” (nonreactive mydriasis) – Muscarinic input contributes to both pupillary constriction and effective accommodation
  5. “Mad as a hatter” (delirium; hallucinations) – Blockade of muscarinic receptors in the central nervous system (CNS) accounts for these findings.
  6. “Full as a flask” – The detrusor muscle of the bladder and the urethral sphincter are both under muscarinic control; anticholinergic substances reduce detrusor contraction (thereby reducing or eliminating the desire to urinate) and prevent normal opening of the urethral sphincter (contributing to urinary retention).
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40
Q

The rate limiting step in catecholamine synthesis is the enzyme ______, and it is inhibited by _______.

A

Tyrosine hydroxylase, ⍺-methyltyrosine (also called metyrosine)

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41
Q

The antimuscarinic with CNS effects used in the t/t of Parkinson’s d/s

A

Benztropine

42
Q

Reserpine blocks this step in catecholamine synthesis.

A

Blocks the transport of dopamine into the secretory vesicles by blocking VMAT (vesicular monoamine transporter)

43
Q

What are the effects of drugs like bretylium and guanethedine on catecholamine neurotransmission?

A

They block the fusion of secretory vesicles with presynaptic membrane and thus, block the release of norepinephrine and other catecholamines

44
Q

How do drugs like cocaine, angiotensin II, and tricyclic antidepressants increase adrenergic neurotransmission?

A

They block NET (norepinephrine transporter), whose key substrates are NE and dopamine, and increase local concentrations of these compounds

45
Q

Activation of presynaptic _____ receptors by NE reduces NE and DA release from adrenergic neurons

A

⍺2

46
Q

This stress hormone increases the synthesis of epinephrine in the adrenal medulla

A

Glucocorticoids (cortisol)

47
Q

The major mechanism by which the effects of NE are terminated is ______.

A

Neuronal reuptake of NE via the NET (norepinehrine transporter)

48
Q

The major mechanism by which the effects of epinephrine are terminated is ______.

A

Extraneuronal reuptake of epi, mainly in the liver and kidneys

49
Q

Neuron degrade NE via _____, a mitochondrial enzyme widely distributed in the body

A

MAO-A

* there is NO COMT in sympathetic neurons or synpases

50
Q

This cytoplasmic enzymes degrades, both NE and Epi, in the periphery

A

COMT

51
Q

The common final product of both NE and Epinephrine metabolism, elevated levels of this compound in urine indicate excess production of catecholamines, like in pheochromocytoma.

A

VMA (vanillylmandelic acid)

52
Q

This directly acting sympathomimetic non-selectively activates β-receptors, without activating ⍺-receptors

A

Isoproterenol

53
Q

IV epinephrine will have these effects on the human heart.

A
  1. SA nodal depolarizations increase—elevated HR
  2. Increased strength of cardiac contraction—elevated stroke volume
  3. Enhanced AV nodal conduction—possible arrhythmias
  4. Shorter ERP—arrhythmias
  5. Coronary vasodilation—β2 effect
  6. Increased cardiac work and oxygen demand
54
Q

Epinephrine, they principle fight or flight hormone, has this effect on the systemic metabolic profile.

A

Adrenaline decreases insulin/glucagon ratio and thus activates glycogenolysis and causes hyperglycemia. It also elevates plasma lactate and free fatty acid concentrations.

55
Q

The beneficial effect of epinephrine during anaphylaxis is mainly attributable to _______.

A

its mast cell stabilizing properties and its ability to reduce mucosal congestion.

56
Q

Tyramine is a component of many foods and is inactivated by _______ before it reaches the sympathetic neurons.

A

MAO-A

57
Q

Tyramine, and indirectly acting sympathomimetic, is transported into the post-ganglionic SNS neurons via the _____. Its main effect is to displace _____ from these neurons.

A

NET (the one inhibited by cocaine)

Norepinephrine

58
Q

Dopamine activates ____ receptors at low doses, _____ receptors at medium doses, and _____ erectors at high doses.

A

D1, β1, ⍺1

59
Q

By improving cardiac output and increasing renal blood flow, _______ is very effective in the management of severe CHF with anuria.

A

Dopamine

60
Q

This drug is a nonselective β-agonist and increases cardiac output without significant affect on HR. Thus, very useful in post cardiac surgery patients and in decompensated MI or cardiogenic shock.

A

Dobutamine

* minimal effect on HR means that cardiac work is not significantly increased

61
Q

Which receptors are activated by isoproterenol?

A

β1 and β2

62
Q

What effect will isoproterenol will have on cardiac output, HR, systolic blood pressure, diastolic blood pressure, mean arterial pressure and pulse pressure?

A
  • Cardiac output ↑
  • HR ↑
  • SBP ↑
  • DBP ↓
  • PP ↑
  • MAP ↓
63
Q

Name two short-acting, β2 selective agonists.

A

Terbutaline
Albuterol

64
Q

β2 selective agonist specifically developed for termination of premature labor.

A

Ritodrine

65
Q

Selective ⍺-1 agonist, which increases MAP and causes reflex bradycardia

A

Phenylephrine

66
Q

List two major uses of phenylephrine

A
  1. Nasal decongestant
  2. Mydriatic in ophthalmology
67
Q

Classified as a “mixed” sympathomimetic, this drug activates ⍺ and β receptors directly; but, major effect is the release of endogenous norepinephrine.

A

Ephedrine

*response is reduced by prior t/t with reserpine (↓ NE stores) or guanethidine (↓ NE release)

68
Q

Response to tyramine or amphetamine will be abolished by prior t/t with ______, _________, __________, and _________.

A

Reserpine, guanethidine, cocaine, tricyclic antidepressants (imipramine)

69
Q

Majority of the effects of amphetamines are due to ________.

A

Release of endogenous NE or dopamine

70
Q

⍺-2 agonist used in the management of hypertension

A

Clonidine

*Clonidine is useful in confirming the diagnosis of pheochromocytoma. Failure to suppress plasma concentrations of norepinephrine in a patient with hypertension suggests pheochromocytoma.

71
Q

Activation of _________ receptors in the _____ reduces sympathetic outflow from the spinal cord and can cause orthostatic hypotension

A

⍺-2, NTS

72
Q

Used in the management of narcolepsy and childhood ADHD, this drug is similar to amphetamines with greater CNS effects and lesser motor effects.

A

Methylphenidate (Ritalin)

73
Q

One of the first antihypertensives ever developed, this drug depletes stores of NE, Epi and dopamine by inhibiting VMAT.

A

Reserpine

74
Q

Cocaine inhibits _____ and increase NE in the synaptic cleft; whereas, amphetamine use this transporter to get into the neuron and then displace NE.

A

Norepinephrine transporter (NET)

75
Q

Phenelzine, a non-selective MAO inhibitor, has adverse reactions with certain foods containing ______. This leads to a hypertensive crisis as excess NE is released from SNS neurons.

A

Tyramine

*tyramine is contained in cheese, beer, wine and pickled meats

76
Q

What is Horner’s syndrome?

A

The pathophysiological basis of Horner’s syndrome (ptosis, miosis and anhydrosis), is loss of sympathetic innervation to the affected region.

77
Q

List common causes of post-ganglionic Horner’s syndrome.

A
  1. Internal carotid artery dissection or thrombosis
  2. Neck massess
  3. Aneurysm of the cavernous sinus
78
Q

List common causes of pre-ganglionic Horner’s syndrome.

A

Trauma, surgery or malignant lesion at the thoracic outlet or the apex of the lung

79
Q

Name two, non-selective ⍺-blockers

A
  1. Phenoxybenzamine (non-competitive)
  2. Phentolamine (competitive)
80
Q

_____ is a competitive ⍺-1 blocker

A
  1. Prazosin
  2. Terazosin
  3. Doxazosin
81
Q

Selective ⍺1a blocker, ______ is used for the treatment of benign prostatic hyperplasia.

A

Tamsulosin

82
Q

What is the expected effect of phenoxybenzamine on—
Blood pressure
Cardiac output
HR

A

Blood pressure falls due to progressive vasodilation (⍺-1 effect). Cardiac output increases due to baroreflex increase in SNS activity and increased central sympathetic outflow (⍺-2 blockade). Thus, diastolic pressure falls more than systolic pressure and pulse pressure increases. Similar mechanisms also underlie tachycardia.

83
Q

Main therapeutic use of phenoxybenzamine is in the management of _____.

A

Pheochromocytoma

84
Q

Blockade of _____ receptors explain the phenomenon of “epinephrine reversal”

A

⍺-1

*Epinephrine increases blood pressure in an untreated patient. Prior treatment with ⍺-1 blocker causes epinephrine to reduce blood pressure due to unopposed β2 activation.

85
Q

Clinically, most significant side effect of ⍺-blockers is ______.

A

Postural hypotension

86
Q

Name the non-selective β-blocker with intrinsic sympathomimetic activity

A

Pindolol

87
Q

Name the prototype non-selective β-blocker

A

Propranolol

88
Q

Name three selective β-1 blockers

A
  1. Atenolol
  2. Metoprolol
  3. Esmolol
89
Q

Name two, third generation β-1, β-2 blockers with ⍺-1 blocking properties.

A
  1. Labetalol
  2. Carvedilol
90
Q

List some relative contraindications for the use of β-blockers

A
  1. Advanced heart failure
  2. Cardiomegaly
  3. Peripheral vascular disease
  4. Asthma or COPD
  5. Careful use in insulin-dependent diabetics
91
Q

______ is an absolute contraindication for the use of β-blockers

A

Complete heart block

92
Q

______ hormone up regulates β-receptors and β-blockers are useful in the management of diseases caused by excess activity of this hormone.

A

Thyroid

93
Q

Timolol, β-1 selective blocker is useful in the management of open angle glaucoma. How?

A

These agents reduce the production of aqueous humor (as opposed to ⍺-1 agonist or M3 antagonist)

94
Q

_________ is the only ganglionic blocker in use today. It blocks NN receptors in autonomic ganglia and block both, SNS and PNS transmission.

A

Trimethaphan

95
Q

The most significant cardiovascular effect of ganglionic blockers is, __________.

A

Orthostatic hypotension

96
Q

Reserpine depletes the neurons of the following major biogenic amines ________, ________, ________, and _________.

A
  1. Norepinephrine
  2. Epinephrine
  3. Dopamine
  4. Serotonin

*Recall, reserpine blocks VMAT an inhibits transport of dopamine of not the neurosecretory vesicles

97
Q

List major side effects of reserpine.

A

Orthostatic hypotension

Sexual dysfunction

Depression

98
Q

What is methyldopa? What is its main indication?

A

Methyldopa is covered to methyl-norepinephrine and blocks central SNS outflow by activating central ⍺-2 receptors (like clonidine). It does NOT cross the placental barrier and is very useful for hypertension in pregnancy.

99
Q

Identify the drugs.

A

Drug A- prazosin, phentolamine

Drug B- phenoxybenzamine (non-competitive)

100
Q

Name three drugs that can block renin release from the kidneys.

A
  1. Propranolol
  2. Atenolol
  3. Metoprolol

* All β-1 blockers

Puri_pharmacology (3 decks)

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