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Pharm > Lecture 6 > Flashcards

Lecture 6 Flashcards

1
Q

What are the two types of indirect-acting cholinomimetic drugs?

A

Carbamates

Phosphates

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2
Q

What are 4 carbamates (cholinesterase inhibitors)?

A

Physostigmine
Neostigmine
Pyridostigmine
Edrophonium

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3
Q

How do carbamates (cholinesterase inhibitors) work?

A

Bind AchE and block its active site

they are hydrolyzed within 2-8 hours

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4
Q

Are carbamates (cholinesterase inhibitors) reversible?

A

Yes, they are water soluble and hydrolyzed

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5
Q

WHat indirect-acting cholinomimetic drugs are irreversible?

A

Organophosphates (covalent binding, lipi-souble can cross BBB)

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6
Q

What are 2 examples of organophosphates that are indirect-acting cholinomimetric drug that is used for the treatment of glaucoma? They amplify the effects of Ach.

A

Echothiophate

Isoflurophate

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7
Q

What are some organophosphates that are volatile oils used in biologic warfare?

A 
Tabun
Sarin
Soman
Parathion
Malathion
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8
Q

This is a reversible water soluble cholinomimetic drug (indirect acting) that is used to treat glaucoma. It also increases intestinal and bladder motility; reverses CNS and cardiac effects of TCA and reverses CNS effects of atropine. It amplifies the effects of Ach.

A

Physostigmine

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9
Q

This 3 drugs are used for myasthenia gravis and reversal of neuromuscular block. They amplify effects of Ach and increase muscle strength. They are carbamates (cholinesterase inhibitors).

A

Neostigmine, Pyridostigmine, Edrophonium

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10
Q

What is a way to remember excessive acetylcholine effects?

A 
DUMBELS
Diarrhea
Urination
miosis
Bronchoconstriction
Excitation (CNS or skeletal muscle)
Lacrimation
Sweating and salivation
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11
Q

What is a way to remember nicotinic manifestations of acetycholine effects?

A 
M T W tH F
Mydriasis, muscle twitching 
Tachycardia
Weakness
tH Hypertension, Hyperglycemia
Fasiculations
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12
Q

How do you treat posioning with organophosphate insecticides (ex- Sarin, soman) ?

A

Atropine (anti-muscarinic, reduces the effects of Ach at muscarinic sites)
Pralidoxime (cholinesterase reactivator, reaks down bond b/w drug and enzymes if drug hasnt’ aged)

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13
Q

How long does it take for organophosphates (ex- sarin, soman) to age?

A

6-8 hours

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14
Q

What areas are most sensitive to atropines effects?

A

Salivary
Bronchial
Sweat glands
Smooth muscles and heart are intermediate

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15
Q

What are the effects of muscarinic blocking drugs

A

Basically opposite of Ach

ex- drowsiness, amnesia, mydriasis, slowed peristalsis, urinary retention, decrease of secretion

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16
Q

What is a clinical application of the antimuscarinic drug Ipatropium?

A

Bronchdilate in asthma / COPD

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17
Q

What is a clinical application of the antimuscarinic drug Benztropine?

A

Treat Parkinson’s disease and adverse effects of antipsychotics

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18
Q

What is a clinical application of the antimuscarinic drug Scopolamine?

A

Prevent or reduce motion sickness

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19
Q

What is the mnemoic that refers to the toxicity of antimuscarinic drugs?

A 
Red as a beat
Dry as a bone
Blind as a bat
mad as a hatter
Hot as a hare
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20
Q

What are other classes that cause anticholinergic toxicity?

A

H1 antagonists (antihistamines)-diphenhydramine
Tricyclic Antidepressants-amitryptyline
Atypical Antipsychotics-olanzapine
Neuroleptic Antipsychotics-chlorpromazine

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21
Q

What type of receptor is a nicotinic receptor?

A

Ion-channel-linked receptor

Allows Na into the cell

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22
Q

At the autonomic ganglia what response is ellicited by nicotinic receptors?

A

Depolarization

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23
Q

At the adrenal medulla what response is mediated by nicotinic receptors?

A

Secretion of epinephrine

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24
Q

At the NMJ what response is elicited by nicotinic receptors?

A

Depolarization of motor end-plate

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25
Q

What is the only drug available that activate nictonic receptors?

A

Nicotine (cigarettes, patches, gum)

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26
Q

What are the 2 types of nicotinic antagonists?

A

Neuromuscular blocking agents

Ganglionic blocking agents

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27
Q

What do nicotinic antagonists that are ganglionic blockers do?

A

Interfere w/ postsynpatic trnamission of Ach

Block actino of Ach on nicotinic receptors

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28
Q

Are ganglion-blocking drugs currently used?

A

No, once were for HTN but they have too many severe adverse effects

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29
Q

What are neuromuscular blocking drugs used for?

A

Induce skeletal muscle relaxation in surgery

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30
Q

Are non-depolarizing or depolarizing neuromuscular blocking agents competitive?

A

Non-depolarizing

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31
Q

How do depolarizing (non-competitive) neuromuscular blocking agents work?

A

Resistant to AChE so they persist in teh synpatic cleft and continually depolarizing the NMJ end-plate

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32
Q

What is an example of a depolarizing (non-competitive) neuromuscular blocking agent?

A

Succinylcholine

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33
Q

What are 2 long acting neuromuscular blocking agents?

A

Curare

Pancuronium

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34
Q

What are 2 intermediate acting neuromuscular blocking agents?

A

Cisatracurium
Atacurium
** Elimination not dependent on hepatic or renal function

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35
Q

What are 2 short acting neuromuscular blocking agents?

A

Mivacurium

Succinylcholine

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36
Q

Drugs that undergo ________ have a longer DOA.

A

Hepatic metabolism

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37
Q

Drugs that undergo __________ have a shorter DOA>

A

plasma cholinesterase or carboxylesterase metabolism

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38
Q

If Curare selective for NMJ?

A

No, it also effect ganglionic junction so it can lead to respiratory failure and death

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39
Q

What do nicotinic antagonists cause?

A

Tachycardia and hypotension

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40
Q

What do muscarinic antagonists induce?

A

Tachycardia

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41
Q

What does botulinum do?

A

Inhibits ach release thus interferes with nerve impulses

Causes flaccid paralysis of muscles

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42
Q

What is the only depolarizing (non-competitive) neuromuscular blocking agent?

A

Succinylcholine

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43
Q

Which neuromuscular blocking agents are eliminated by the liver metabolism?

A

Rocuronium

Vecuronium

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44
Q

What drug can cause malignant hyperthermia?

A

Succinylcholine

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45
Q

What are some clinical features of malignant hyperthermia?

A

Hyperthermia
metabolic acidosis
tachycardia
accelerated muscle metabolism and contractures

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46
Q

What drug can be used to stop the effects of malignant hyperthermia?

A

Dantrolene- blocks release from SR reducing heat production and muscular tone

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47
Q

is the sympathetic system considered essential for life?

A

No

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48
Q

Sympathetic innervation of the sweat glands is _______

A

cholinergic

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49
Q

Sympathetic innervation of renal vasculature is _______

A

dopaminergic

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50
Q

What must happen to DOPA to form dopamine?

A

be decarboxylated (occurs in cytoplams)

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51
Q

What blocks the transport of dopamine into synaptic vesicles by the amine transporter system?

A

Reserpine

52
Q

What metabolizes both DOPA and dopamine to inactive metabolites?

A

monoamine oxidase (MAO)

53
Q

What hydroxylates DA to norepinephrine (NE)?

A

dopamine B-hydroxylase within vesicles

54
Q

Where is NE methylated into Epi?

A

adrenal medulla

55
Q

Where is Epi stored?

A

choromaffin cells

56
Q

What blocks the release of NE? (2 drugs)

A

Guanethidine and bretylium

57
Q

What are the 3 mechanisms for for the reuptake and metabolism of catecholamines?

A
  1. Reuptake by NET (norepinephrine transporter) or Uptake 1
  2. Metabolism into an inactive metabolite by MAO or COMT
  3. Diffusion of catecholamine away from the clef and enter systemic circulation
58
Q

What inhibits tyrosine hydroxylase (first step in synthesis of catecholamines)?

A

alpha-methyltyrosine

59
Q

What blocks VMAT, trransport of bioamines (NE, DA, 5-HT) from cytoplasm into storage vesicles?

A

Reserpine

60
Q

What is a dietary amine that is usually metabolized by MAO in GI and liver. In patients with MAO inhibitors on board and large amount of this is absorbed and cause displacement of vesicular NE and non vesicular release –> hypertensive crisis.

A

Tyramine

61
Q

What displaces NE in storage vesicles and leads to a gradual depletion of NE?

A

Guanethidine

62
Q

This displaces endogenous NE, is a weak inhibitor of MAO, blocks reuptake by NET and DAT, and has little agonist action at alpha and beta receptors. Marked behavioral effects.

A

Amphetamine

63
Q

This is a potent inhibitor of NET, and essentially eliminates catecholamine transport.

A

Cocaine

64
Q

Name 2 drugs that are inhibitors of NET?

A

Imipramine, fluoxetine

65
Q

What class of drugs blocks Na/K ATPase and blocks NET thereby increasing the DOA .

A

Tricyclic antidepressants

66
Q

This drug inhibits MAO-A thereby increasing NE and 5-HT content.

A

Phenelzine

67
Q

This drug inhibits MAO, increasing DA.

Used in low doses for treatment of Parkinson’s

A

Selegiline

68
Q

What are the two families of adrenergic receptors?

A

Alpha

Beta

69
Q

What is the order from most to least of alpha affinity?

A

Epinephrine
Norepinephrine
Isoproteranol

70
Q

What is the order from most to least for beta affinity?

A

Isoproteranol
Epinephrine
Norepinephrine

71
Q

What are the 5 actions that occur when alpha 1 is activated?

A 
Vasoconstriction
increase PVR
increase BP
mydriasis
increase the closure of internal bladder sphincter
72
Q

What are the 2 actions that occur when alpha 2 is activated?

A

Inhibit norepinephrine release resulting in lower BP

Inhibit insulin release

73
Q

What are the 5 things that happen when Beta 1 is activated?

A 
tachycardia
increased myocardial contractility
Results in increased cardiac output
Increased release of renin
Increased lipolysis (Beta 3)
74
Q

What are the 7 things that happen when beta 2 is activated?

A 
Vasodilation
decreased PVR
decreased DBP
bronchodilation
increased muscle and liver glycogenolysis
increased glucagon release
relax uterine smooth muscle
75
Q

What is an adrenergic drug which acts directly on adrenergic receptor, activating it?

A

Symapthomimetic (aka adrenergic agonists)

76
Q

What are 3 endogenous catecholamines?

A

Epinephrine
Norepinephrine
Dopamine (at supraphysiologic concentrations)

77
Q

How do indirect acting adrenergic agonists work?

A

Work at the presynpatic terminals to cause release of NE.

Do not bind the adrenergic receptors.

78
Q

What are 2 drugs that are indirect andrenergic agoinsts?

A

Amphetamine

Tyramine

79
Q

What is a mixed (direct and in direct) adrenergic agonist?

A

Ephedrine

80
Q

What receptors does epinephrine (endogenous) interact with?

A

alpha and beta

81
Q

At low doses what receptor does epi interact with?

A

Beta (vasodilation)

82
Q

At high doses what receptor does epi mostly interact with?

A

alpha (vasoconstriction)

83
Q

Epi’s affects at Beta 1 lead to what effects?

A

Increased cardiac output due to increased inotropic and chronotropic effects

84
Q

What effects results from epi’s activaiton of alpha?

A

Vasoconstricts arterioles

85
Q

What effects result from epi’s activation of beta 2?

A

Vasodilates vessels to liver and skeletal muscles

86
Q

What is the net results of epi?

A

Increased SBP with slight decrease in diasotlic BP

87
Q

What affects does epi have on the respiratory system (beta 2)?

A

Bronchodilation of smooth muscle

88
Q

What effects does epi have on glucose?

A

Hyperglycemia
Decreased insulin release (alpha 2)
glycogenolysis, increase release of glucagon (beta 2)

89
Q

Epi’s activation of what receptor leads to lipolysis?

A

Beta 1

90
Q

What are some therapeutic uses of epinephrine?

A

Emergent treatment of asthma
Glaucoma
anaphylaxis
prolongs duration of local anesthetics thur vasoconstriction (local)

91
Q

How is epi administered?

A

Sub-Q
Inhalation
Endotracheal
Topically

92
Q

What are some ADRs w/ epi?

A

Anxiety, fear, tension, HA tremor
hemorrhage from increased BP
arrhythmias
pulmonary edema

93
Q

What happens if an individual with hyperthyroidism is given epi?

A

Exaggerated CV effects due to increased production of receptors

94
Q

Epi plus what drug will lead to exaggerated CV effects due to prevention of reuptake?

A

cocaine

95
Q

What receptors does norepinehprine affect?

A

Alpha 1 and Beta 1

96
Q

What CV effects does norepinephrine have?

A

Increased vasoconstriction –> increased BP

Increased baroreceptor reflex –> increased vagal activity causing bradycardia

97
Q

Why can norepinehprine be used to treat shock?

A

through vascular resistance, increases BP

98
Q

What receptors do low doses (<2 mcg/kg per minute) of dopamine act on?

A

D1 receptors in renal, mesenteric, and coronary vascular beds (vasocilation)

99
Q

What receptor does higher doses (2-10 mcg/kg/min) of dopamine affect?

A

Beta 1, positive inotrope

100
Q

What receptor do highes doses of dopamine (>10 mcg/kg/min) work on?

A

Alpha 1 leading to vasoconstriction

101
Q

What conditions is dopamine useful in treating?

A

Low CO associated with compromised renal function such as severe CHF

102
Q

What are three alpha-1 selective agonists?

A

Methoxamine
Phenylephrine
Oxymetazoline

103
Q

What alpha-1 selective agonists is used in relief of nasal congestions and is used topically?

A

Phenylephrine

104
Q

What alpha-1 selective agonist is used to constrict vascular smooth muscle in relief of opthalmic hyperemia?

A

Oxymetazoline

105
Q

What are three alpha-2 agonists?

A

Clonidine
Alpha-methlydopa
Guanfacine

106
Q

What alpha 2 agonist is used to decrease sympathetic outflow. Adverse effects include dry mouth, sedation.

A

Guanfacine

107
Q

What alpha-2 agonists lowers BP by suppressing sympathetic outflow. Adverse effects include dry mouth, sedation.

A

Clonidine

108
Q

What drug is a beta-nonselective agonist?

A

Isoproterenol

109
Q

What drug is used clinically to stimulate the heart in emergencies? It have ionotropic and chronotropic effects (beta 1) and vasodilation of arterioles of skeletal muscle (beta 2) and bronchodilation (beta 2)?

A

Isoproterenol

110
Q

What is a Beta 1 agonist?

A

Dobutamine

111
Q

What is dobutamine used for?

A

Increase cardiac rate and output (more inotrope effects versus chronotrope effects)

112
Q

What are 5 beta 2 selective agents?

A 
Albuterol
pirbuterol
terbutaline
salmeterol
formoterol
113
Q

Albuterol, pibuterol and terbutaline are all beta 2 _____ acting bronchodilator.

A

Short

114
Q

Salmeterol and formoterol and beta 2 _____ acting bronchodilators.

A

long

115
Q

What is a mixed-action drug that is used in nasals sparys for vasocontrictor activity and is used in urinary incontinence. Has a long DOA due to being a poor substrate for COMT and MAO.

A

Ephedrine

116
Q

What are some conditions where adrenergic agonists are used?

A

Narcolepsy
Weight Reduction
ADHD

117
Q

What is an adrenergic antagonist that is used to treat a pheochromocytoma to preclude HTN crisis. It is irreversible, nonselective and noncompetitive.

A

Phenoxybenzamine

118
Q

What are 3 drugs that are selective alpha 1 blockers. Used to treat HTN, BPH, CHF by relaxing arterial and venous smooth muscles

A

Prazosin
Doxazosin
terazosin

119
Q

What is a drug that is used to treat BPH by inhibiting alpha (1a) receptor on smooth tissue of the prostate.

A

Tamsulosin

120
Q

What is a non-selective beta blocker that lowers BP, used to terat angina, cardiac arrhythmias, MI, glaucoma and prophylaxis for migraines.

A

Propranolol

121
Q

What are 2 nonspecific beta-blockers used to treat glaucoma and HTN?

A

Timolol

Nadolol

122
Q

What are 4 drugs that preferentially block beta 1 receptors thereby eliminating unwanted bronchoconstriction and having little effect on CHO-meatbolism or PVR.

A

Acebutolol
Atenolol
Metoprolol
Esmolol

123
Q

What class of drugs can cause or exacerbate HF in compensated HR, acute MI, cause life threatening increase in airway resistance and blunt recognition of hypoglycemia in patients with T1DM?

A

Beta blockers

124
Q

What are 2 adrenergic antagonists with partial agonist acitivty?

A

PIndolol

acebutolol

125
Q

What is a drug that decreases lipid peroxdiation and vascular vall thickening and is an antagonists of alpha 1, beta 1 and 2?

A

Carvediol

126
Q

What adrenergic antagonist works at alpha 1 and beta 1 and 2 and is used to rapidly lower BP as well as for HTN, CHF, PIH, HTN?

A

Labetolol

Pharm (29 decks)

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