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1 Pharm Unit > MASTERTEST1 > Flashcards

MASTERTEST1 Flashcards

1
Q

Drug Name

A 
Drug Class
Mechanism
Distinguishing Chem Characteristics (Unique or "weird" features)
Pharmacological characteristics
Side Effects
Special side effects
Use
[mnemonic] (put in brackets)
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2
Q

Bethanechol

A 
-Muscarinic Cholinergic agonist
-
-CH3(down nicotinic) and NH2 (down AChE)
-oral or subQ
-
-treat depressed smooth muscle activity (ileus, megacolon)
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3
Q

carbachol

A

-muscarinic cholinergic agonist
-Stim M3 receptor on ciliary body & iris improving uveoscleral outflow
-NH2 grp. Poor substrate for AChE
-oral or subQ
-
-miotic. open or closed angle glaucoma.

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4
Q

methacholine

A 
-muscarinic cholinergic agonist
-
-CH3 decreases nicotinic affinity
-oral or subQ
-
-often used to suppress tachycardia
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5
Q

muscarine

A 
-muscarinic cholinergic agonist
-
-alkaloid
-oral or subQ
-
-
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6
Q

pilocarpine

A

-Muscarinic Cholinergic agonist
-Stim M3 receptor on ciliary body & iris improving uveoscleral outflow
-alkaloid
-topical use for eye
-sweat glands particularly sensitive
-acute closed or open angle glaucoma, increase salivary secretion
[tears, saliva on your “pillow”]

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7
Q

varenicline

A 
-Nicotinic cholinergic agonist
-
-alkaloid
-
-
-
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8
Q

ambenonium

A

-cometitive inhibitor of cholinesterase
-carbamoylates AChE at esteratic site
-carbamate
-4-8 DOA
-
-myasthenia gravis, neuromuscular bloackade

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9
Q

edrophonium

A

-competitive cholinesterase inhibitor
-antagonize competitive inhibitor of NMJ
-alcohol w/ quaternary ammonium group
-short DOA
-
-myasthenia gravis, ileus, arrhythmias

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10
Q

neostigmine

A

-competitive cholinesterase inhibitor
-carbamoylates AChE at esteratic site, antagonize NMJ comp. inhibitors
-carbamate
-med DOA
-
-myasthenia gravis, neuromuscular blockade, ileus

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11
Q

physostigmine

A

-competitive cholinesterast inhibitor
-carbamoylates AChE at esteratic site
-carbamate
-med DOA
-
-glaucoma

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12
Q

diisopropylfluorophosphate

A

-noncompetitive cholinesterase inhibitor
-irreversible phosphoryl AChE at esteratic site
-
-
-
-insecticide

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13
Q

echothiophate

A

-Organophosphate Derivative
-Non - Competitive AChE inhibitor
-
-
-
-
- Used to treat glucoma

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14
Q

carbaryl

A

-noncompetitive cholinesterase inhibitor
-phoshphoryl group in AChE esteratic site
-
-
-
-insecticide

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15
Q

malathion

A

-noncompetitive cholinesterase inhibitor
-phoshphoryl group in AChE esteratic site
-
-
-
-insecticide

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16
Q

parathion

A

-noncompetitive cholinesterase inhibitor
-phoshphoryl group in AChE esteratic site
-
-
-
-insecticide

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17
Q

tetraethylpyrophosphate

A

-noncompetitive cholinesterase inhibitor
-phoshphoryl group in AChE esteratic site
-
-
-
-insecticide

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18
Q

sarin

A 
-noncompetitive cholinesterase inhibitor
-
-
-
-nerve gas
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19
Q

soman

A 
-noncompetitive cholinesterase inhibitor
-
-
-
-nerve gas
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20
Q

pralidoxime

A

-AChE reactivator
-release phosphoryl moeity in AChE esteratic site
-2-PAM
-Must B4 AChE aging occurs
-
-supplement atropine in O-P intoxication

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21
Q

atropine

A
  • muscarinic cholinergic antagonist
  • antagonize O-P by competitively bind muscarinics, block M3 on iris & ciliary muscle
  • tertiary amine
  • doses limited due to crosss BBB, long DOA, (salivary,bronch,sweat+++), bound by melanin in iris
  • no alleviation of neuromusc hyperactivity, CNS effects!
  • May elicit acute glaucoma
  • O-P intoxication,block paraSNA, mydriasis/cycloplegia (7-10 days)
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22
Q

homatropine

A

-muscarinic cholinergic antagonist
-block M3 on iris & ciliary muscle
-tertiary amine
-med DOA
-
-mydriasis/cycloplegia (1-3 days) EYE EXAM!

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23
Q

scopolamine

A
  • Muscarinic Cholinergic antagonist
  • block M3 on iris & ciliary muscle
  • tertiary amine
  • long DOA, quick CNS, (injection, oral, transdermal only)
  • sedation/amnesisa, dry mouth
  • anti-motion sickness, adjunct for pre-amnesia, mydriasis/cycloplegia (3-7 days)
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24
Q

methscopolamine

A 
-Muscarinic Cholinergic antagonist
-
-quaternary ammonium
-longer DOA
-
-GI diseases, can inhibit respiratory tract secretions
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25
Q

trihexyphenidyl

A 
-muscarinic cholinergic antagonist
-
-tertiary amine
-3-6hrs DOA
-
-anti-parkinson, excess salivation
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26
Q

tropicamide

A

-Muscarinic Cholinergic antagonist
-Block M3 on iris & ciliary muscle
-
-short DOA, only topically
-
-mydriasis and cycloplegia (1/4 day)

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27
Q

cyclopentolate

A

-muscarinic cholinergic antagonist
-block M3’s on iris & ciliary muscle
-
-med DOA
-
-
-Elicit mydriasis & cycloplegia (1 day)

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28
Q

ipratropium

A 
-Muscarinic Cholinergic antagonist
-
-quaternary ammonium
-shorter DOA, topical inhalant
-tachycardia, decreased salivation
-bronchodilation and min. mucociliary clearance problems
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29
Q

tiotropium

A 
-Muscarinic Cholinergic antagonist
-
-
-longer DOA, topical
-
-bronchodilation and min. mucociliary clearance problems
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30
Q

darifenacin

A 
- M3 selective cholinergic antagonist
-
-
-longer DOA
-
-
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31
Q

solifenacin

A 
-M3 selective cholinergic antagonist
-
-
-longer DOA
-
-
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32
Q

tolterodine

A 
-M3 selective cholinergic antagonist
-
-
- longer DOA
-
-
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33
Q

mecamylamine

A
  • N1 non-depolarizing cholinergic competitive antagonist
  • ganglionic blocker
  • secondary amine (improve GI absorb)
  • Med DOA 12 hours
  • CNS-tremor, confusion, seizure, mania, depression
  • hypertensive emergency,periph vasc disease
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34
Q

trimethaphan

A
  • N1 non-depolarizing Cholinergic competitive antagonist
  • ganglionic blocker
  • sulfonium+
  • shrot DOA, intravenous
  • hypotension, brain anoxia
  • surgically to reduce bleeding=controlled hypotension
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35
Q

succinylcholine

A

-N2 non-competitive depolarizing inhibitor
-agonist for Na channel and keeps it open
-
-hydrolysis from plasma ChE nor AChE!, short DOA
-K–>cardiac arrest, contraction of eye muscles
-relax muscles during surgery/vent

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36
Q

curare

A 
-N2 competitive inhibitor
-
-quaternary nitrogens
-
-
-
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37
Q

atracurium

A

-benzylisoquinolines
-Competitive Nicotinic N2 blocker (N2 Specific)
-Non-depolarizing – Prevent Depolarization
-Intermediate in duration
-Histamine Release (hypotension) is side effect
-
-Muscle relaxation (e.g. before surgery)

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38
Q

cisatracurium

A

-benzylisoquinolines
-N2 competitive inhibitor
-Competitive Nicotinic N2 blocker (N2 Specific)
-quaternary nitrogens
-medium DOA
-histamine release
-

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39
Q

mivacurium

A

-benzylisoquinolines
-N2 competitive inhibitor
-Competitive Nicotinic N2 blocker (N2 Specific)
-
-short DOA
-histamine release
-

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40
Q

pancuronium

A
  • Ammonio Steroids
  • ## Competitive Nicotinic N2 blocker-
    -long DOA
    -muscarinic block-vagal blockade, tachycardia
    -
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41
Q

vecuronium

A

-N2 competitive inhibitor
-Competitive Nicotinic N2 blocker
-quaternary nitrogens
-med DOA
-muscarinic block-vagal blockade, tachycardia
-

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42
Q

albuterol

A

-Beta-2 agonist
-stim adenyl cyclase and cAMP–>relax bronch smooth m.
-
-short DOA
-tachycardia, muscle tremor, headache
-bronchodilate acute asthma

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43
Q

salmeterol

A

-Beta-2 agonist
-stim adenyl cyclase and cAMP–>relax bronch smooth m
-
-long DOA
-tachycardia, muscle tremor, headache
-bronchodilate

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44
Q

salmeterol with fluticasone

A

-Beta-2 agonist with corticosteroid
-stim adenyl cyclase and cAMP–>relax bronch smooth m
-
-combination necessary in maintenance therapy
-
-maintenance bronchodilation

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45
Q

beclomethasone

A

-corticosteroid
-inhibit inflam. response system thru gene expression
-
-topical inhalation
-generally none
-long term asthma reduction

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46
Q

budesonide

A

-corticosteroid
-inhibit inflam. response system thru gene expression
-
-topical inhalation
-generally none
-long term asthma reduction

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47
Q

fluticasone

A

-corticosteroid
-inhibit inflam. response system thru gene expression
-
-topical inhalation
-generally none
-long term asthma reduction

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48
Q

prednisone

A

-corticosteroid
-inhibit inflam. response system thru gene expression
-
-oral or intravenous
- glucose metab.,Cushing’s, hypert, increased infection
-asthma

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49
Q

triamcinolone

A

-corticosteroid
-inhibit inflam. response system thru gene expression
-
-topical inhalation
-generally none
-long term asthma reduction

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50
Q

montelukast

A

-leukotriene modulator
-receptor antagonist of LTD4
-
-oral
-
-long-term controller of asthma

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51
Q

zafirlukast

A

-leukotriene modulator
-receptor antagonist of LTD4
-
-oral
-
- long term controller of asthma

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52
Q

zileuton

A

-leukotriene modulator
-inhibitor of 5-lipoxygenase inhibiting synthesis of LTB/D4
-
-oral
-liver toxicity, and inhibits some CYPs
-long term controller of asthma

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53
Q

cromolyn

A
  • degranulation inhibitor
  • possible inhibit of Ca channels in Mast cell degranulation
  • poorly soluble salt
  • Topical
  • well tolerated
  • long term prophylactic maintenance of asthma
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54
Q

nedocromil

A
  • degranulation inhibitor
  • possible inhibit of Ca channels in Mast cell degranulation
  • poorly soluble salt
  • Topical
  • well tolerated
  • long term prophylactic maintenance of asthma
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55
Q

ipratropium

A 
-muscarinic cholinergic antagonist
-
-quaternary ammonium
-shorter DOA, topical inhalant 
-tachycardia, decreased salivation
-bronchodilation and min. mucociliary clearance problems
56
Q

theophylline

A
  • Misc. Bronchodilator
  • inhibit phosphodiesterase degradation of cAMP
  • methylxanthine
  • oral, LongDOA
  • tachycardia and CNS stimulation
  • long-term maintenance of asthma
57
Q

Drug Name

A 
Drug Class
Mechanism
Distinguishing Chem Characteristics (Unique or "weird" features)
Pharmacological characteristics
Side Effects
Special side effects
Use
[mnemonic] (put in brackets)
58
Q

metaraminol

A 
Alpha-1 Selective Agonist 
-
-
- Long acting beta 1 and alpha 1 stimulant, Displaces NE
-
-
-
59
Q

methoxamine

A 
Alpha-1 Selective Agonist (less alpha 2)
-
-
-
-
-
- treat hypotensive crisis
60
Q

phenylephrine

A 
Alpha-1 Selective Agonist (less alpha 2)
-
- Long acting
-
-
-
- Vasoconstriction, prevent shock, nasal decongestant, treat hypotensive crisis, reduce drug diffusion, reduce mucus membrane congestion, mydriasis
61
Q

alpha-methyldopa

A

*α2 selective agonist/false transmitter
*MNE (α-methyl NE) causes potent stimulation in vasomotor area of brainstem
*converted to MNE by NE synthetic pathway (partially replaces DOPA); MNE replaces NE in vesicles but greatly reduced efficacy than NE
*
*sedation, xerostomia, anorexia, fluid retention, vivid dreams, & CNS stimulation (all diminish over time)
*dizziness, sleep disturbances, impotence, dry mouth, nasal congestion (diminish after 2 weeks), postural hypotension; chronic therapy may result in hemolytic anemia, leukopenia, hepatitis, lupus-like problems
*hypertension

62
Q

clonidine

A

*α2 selective agonist
*stimulate both PNS & CNS α2 receptors - inhibit NE release by nerve terminal (elicit hypotension by decr. TPR, HR, CO)
*
*
*sedation, xerostomia, anorexia, fluid retention, vivid dreams, & CNS stimulation (all diminish over time)
*
*hypertension

63
Q

apraclonidine

A

*α2 selective agonist
*stimulate both PNS & CNS α2 receptors - inhibit NE release by nerve terminal (elicit hypotension by decr. TPR, HR, CO).
*
*
*sedation, xerostomia, anorexia, fluid retention, vivid dreams, & CNS stimulation (all diminish over time)
*
*hypertension, EXTREME open angle glaucoma

64
Q

guanabenz

A

*α2 selective agonist
*stimulate both PNS & CNS α2 receptors - inhibit NE release by nerve terminal (elicit hypotension by decr. TPR, HR, CO)
*
*
*sedation, xerostomia, anorexia, fluid retention, vivid dreams, & CNS stimulation (all diminish over time)
*
*hypertension

65
Q

amphetamine

A 
Alpha and beta adrenergic agonist
-
- Releasing agent (increases NE release), also releases intraneuronal NE – reverse transport
-
-
-
-
66
Q

ephedrine

A

-
- Releasing agent, Stimulant of most adrenergic receptors, Long acting – Displaces NE
-
-
- Increase CO and arterial pressure, treat orthostatic hypotension, reduce mucus membrane congestion, stress incontinence

67
Q

epinephrine

A 
Alpha and beta adrenergic agonist
-
-
- Binds all adrenergic receptors equally
-
-
- Potent vasoconstrictor and cardiac stimulant, hemostasis during surgery, reduce drug diffusion, anaphylaxis
68
Q

norepinephrine

A

-
- Binds Beta-2 a lot less than all other adrenergics
-
-
- IV infusion for shock, increase CO and cause vasoconstriction (increase BP, treat hypotensive crisis), reduce drug diffusion

69
Q

dipivefrin

A

*Mixed alpha, beta agonist
*stim alpha 2 on ciliary body, alpha 1 on ciliary vessels
*Prodrug metabolized to Epi.
*
*
*
*Open angle glaucoma

70
Q

dobutamine

A 
Beta 1 Selective agonist 
-
-
-(Less binding to beta-2)
-
-
- Cardiogenic shock, heart failure
71
Q

isoproterenol

A 
Beta 1 and 2 agonist
-
-
-
-
-
- Used for relaxation of bronchial smooth muscle, also cardiac stimulation (potent vasodilator)
72
Q

albuterol

A 
Beta 2 Selective agonist 
-
-
-(Less binding to beta-1)
-
-
- Bronchial asthma
73
Q

metaproterenol

A 
Beta 2 Selective agonist 
-
-
-(Less binding to beta-1)
-
-
- Bronchial asthma
74
Q

terbutaline

A 
Beta 2 Selective agonist 
-
-
-(Less binding to beta-1)
-
-
- Bronchial asthma, relax pregnant uterus
75
Q

bromocriptine

A

-
-
- postural hypotension and cardiac arrhythmia
-
- Anti-parkinson agent (for its CNS effects)

76
Q

dopamine

A

-
- Binds Alpha and Beta 1 at high concentrations, Enhance NE release (displaces it)
-
-
- IV for shock, vasoconstriction, increase CO and dilate renal arteries

77
Q

fenoldopam

A 
Dopamine Agonist, DA-1 selective 
-
-
-
-
-
- Vasodilation of renal and mesenteric vessels
78
Q

doxazosin

A 
Alpha-1 Selective antagonist
-
-
-
-
-
- Urinary obstruction from BPH
79
Q

prazosin

A

-
- Oral admin
-
- Little to no tachycardia because doesn’t bind beta receptors
- Antihypertensive (mild / moderate), urinary obstruction from BPH

80
Q

tamsulosin

A 
Alpha-1 Selective antagonist
-
-
-
-
-
- Urinary obstruction from BPH
81
Q

terazosin

A 
Alpha-1 Selective antagonist
-
-
-
-
-
- Urinary obstruction from BPH
82
Q

phenozybenzamine

A

Alpha-1 and Alpha-2 Selective antagonist
- Non-competitive – alkylates alpha receptors (~24 hrs)

  • ## Can cause postural hypotension and tachycardia – due to decreased MAP
  • Used to treat hypertension associated with pheochromocytoma
83
Q

phentolamine

A

Alpha-1 and Alpha-2 Selective antagonist
- Competitive antagonist
-
- Dirty drug, binds histamine and muscarinic receptors
- Increases NE release, will cause tachycardia and increased CO
-
- Diagnostic for pheochromocytoma, also for its assoc. hypertension

84
Q

labetalol

A 
Alpha and beta antagonist
-
- Binds beta receptors better than alpha
-
-
-
-
85
Q

atenolol

A

*β1 selective antagonist
*inhibit CO; class generally pure antagonist (binds but does not activate receptor)
*β1&raquo_space;> β2; t1/2=6-9 hours; diminished ability to cross BBB
*combination with diuretics and other antihypertensive agents
*
*less prone to induce bronchial smooth muscle constriction in asthma patients; fewer CNS effects
*hypertension

86
Q

betaxolol

A

*β1 selective antagonist
*block B1 receptors on ciliary body to reduce aq. humor production; inhibit CO; class generally pure antagonist
*β1&raquo_space;> β2; ; t1/2=14-22 hours
*combination with diuretics and other antihypertensive agents
*
*less prone to induce bronchial smooth muscle constriction in asthma patients
*Open angle glaucoma; hypertension

87
Q

metoprolol

A

*β1 selective antagonist
*inhibit CO; class generally pure antagonist
*β1&raquo_space;> β2; t1/2=3-4 hours
*combination with diuretics and other antihypertensive agents
*
*ataxia, dizziness; less prone to induce bronchial smooth muscle constriction in asthma patients
*hypertension, angina pectoris; prophylaxis for MI recurrence

88
Q

nadolol

A

*β non-selective antagonist
*inhibit CO & dilation/relaxation
*β1 = β2; t1/2=14-24 hours; diminished ability to cross BBB
*combination with diuretics and other antihypertensive agents
*may inhibit dilation of bronchioles (significant in asthma patients); may induce cardiac failure (significant in cardiac insufficiency patients); fewer CNS side effects
*
*hypertension

89
Q

pindolol

A

*β non-selective antagonist
*inhibit CO & dilation/relaxation
*β1 = β2; t1/2=3-4 hours
*combination with diuretics and other antihypertensive agents
*may inhibit dilation of bronchioles (significant in asthma patients); may induce cardiac failure (significant in cardiac insufficiency patients)
*
*hypertension

90
Q

propranolol

A

*β non-selective antagonist
*inhibit CO & dilation/relaxation
*β1 = β2; t1/2=3-6 hours
*
*may inhibit dilation of bronchioles (significant in asthma patients); may induce cardiac failure (significant in cardiac insufficiency patients)
*ataxia, dizziness
*hypertension, arrhythmia, angina pectoris, migraine headache; prophylaxis for MI recurrence

91
Q

timolol

A

*B non-selective antagonist
*block B1R’s on ciliary body to reduce aq. humor production ->lower intraocular pressure;
*t1/2=4-5 hours
*topical for glaucoma
*may inhibit dilation of bronchioles (significant in asthma patients); may induce cardiac failure (significant in cardiac insufficiency patients)
*
*Open angle glaucoma, antihypertensive, angina pectoris; prophylaxis for MI recurrence

92
Q

carteolol

A

*B non-selective antagonist
*block B1R’s on ciliary body to reduce aq. humor production
*
*topical
*
*
*Open angle glaucoma

93
Q

levobunolol

A

*B non-selective antagonist
*block B1R’s on ciliary body to reduce aq. humor production
*
*topical
*
*
*Open angle glaucoma

94
Q

metipranolol

A

*B non-selective antagonist
*block B1R’s on ciliary body to reduce aq. humor production
*
*topical
*
*
*Open angle glaucoma

95
Q

guanethidine

A

*pre-junctional inhibition of NE release
*stabilizes neuronal membranes, interfering with exocytosis of NE vesicles
*transported into adrenergic neurons via Amine I transport; does not cross BBB
*orally effective
*
* chronic administration->depleting NE within synaptic vesicles; minimal adverse CNS effects; minimal effects with other biogenic amines
*hypertension – reserved for therapy of most severely elevated arterial pressures

96
Q

reserpine

A

*pre-junctional inhibition of NE release
*depletes stores of biogenic amines (Epi, NE, DA, serotonin) in both CNS & PNS by blocking transport into storage vesicles
*long DOA; very potent
*orally effective
*
*increased GI motility (>ulcers); CNS: sedation, depression, parkinsonian symptoms
*hypertension

97
Q

cocaine

A

*Amine I transport (NET) inhibitor
*NE levels rise in synapse -> mimic sympathetic nerve stimulation
*
*
*vasoconstriction, tachycardia, mydriasis
*
*hemostasis during surgery

98
Q

DMI (desmethylimipramine)

A

*Amine I transport (NET) inhibitor
*NE levels rise in synapse -> mimic sympathetic nerve stimulation
*
*
*vasoconstriction, tachycardia, mydriasis
*
*

99
Q

tyramine

A 
Releasing Agent 
-
-
- Enhance NE release via Amine 1 transporter
-
-
-
100
Q

pseudoephedrine

A 
Releasing Agent 
-
-
-
-
-
- Reduces congestion of mucus membranes
101
Q

Drug Name

A 
Drug Class
Mechanism
Distinguishing Chem Characteristics (Unique or "weird" features)
Pharmacological characteristics
Side Effects
Special side effects
Use
[mnemonic] (put in brackets)
102
Q

Azathioprine

A
  • General Growth Inhibitors
  • ## Metabolized to 6-mercaptopurine then 6 thioguanine (blocks purine synthesis). Also incorporates into DNA
  • Inactivated by xanthine oxidase
  • ## Myelosuppression, nausea, vomiting
  • Used for renal and other tissue transplantation, autoimmune disease, and gout
103
Q

Cyclophosphamide

A

-General Growth Inhibitors
-Cross links DNA, kills all proliferating cells
-
-
- Myelosuppression, nausea, vomiting,
- Infertility
- Used for autoimmune diseases, bone marrow transplant

104
Q

Leflunomide

A

*General Growth Inhibitors
- Decreases pyrimidine synthesis
-
-
- Diarrhea, modest hepatotoxicity, reduced myelosuppresion
-
- Used for Rheumatoid arthritis, some autoimmune disease

105
Q

Methotrexate

A

*-General Growth Inhibitors
- Inhibits dihydrofolate reductase, prevents thymidide and purine synthesis
-
-
- Causes nausea, mucosal ulcers, modest hepatotoxicity, reduced myelosuppression
-
- Rheumatoid arthritis, some autoimmune disease

106
Q

Mycophenolate Mofetil

A

*-General Growth Inhibitors
- prevents purine synthesis
-
-Prodrug of mycophenolic acid, active form
- myelosuppression, nausea, vomiting
-
- Used for solid organ transplant (cyclosporine alternative) autoimmune disease

107
Q

Prednisone

A

*-Glucocorticoid
-Upregulates / Downregulates expression of genes assoc. with inflammation and immunosuppression (e.g. IL2 and IFN-gamma). Inhibition of annexins genes (thus phospholipase A2). Esp. affects IL-2 & IFNgamma
- No serious bone marrow toxicity
-
-
- Cushings syndrome, osteoporosis, glucose intolerance, hypertension, susceptibility to infection
- Used for solid organ transplantation (first line), stem cell transplantation, autoimmune diseases, asthma, allergic reactions, systemic inflammation

108
Q

Sirolimus

A

*- mTOR inhibitor
- Binds FKBP12 to form complex that inhibits IL2 activation
-
- Antagonizes tacrolimus, synergistic with cyclosporine
- Myelosuppression, hyperlipidemia, hypertension, edema, hepatotoxicity
-
- Solid organ transplants, steroid resistant graft v. host disease

109
Q

Cyclosporin

A

*- Calcineurin inhibitor
- Binds Cyclophilin to form complex that inhibits NFAT activation
-
- Often combined with other immunosuppressant agents
- Nephrotoxicity, hypertension, hyperglycemia, liver dysfunction.
- Increased cancer incidence documented
- Kidney, liver and cardiac transplants, inflammatory diseases (asthma) & autoimmune

110
Q

Tacrolimus

A

*- Calcineurin inhibitor
- Binds FKBP12 to form complex that inhibits NFAT activation
-
- 10-100 X more potent than cyclosporine
- Nephrotoxicity, hypertension, hyperglycemia, liver dysfunction.
- Increased cancer incidence documented
- Kidney, liver and cardiac transplants, inflammatory diseases (asthma)

111
Q

Anti-T cell globulin

A
    • Antibody / Fusion Protein
  • Blocks T cell surface receptors and opsonizes T cells
  • Product of repeated injection of human T cells into animals
  • Cytokine release syndrome (reduce w/ pretreat. With acetaminophen and antihistamine, serum sickness
  • Anaphylaxis potential (with repeat use)
  • Prevent maternal (Rh-) from attacking fetus
112
Q

Alemtuzumab (anti CD52)

A

*- Antibody / Fusion Protein
- Depletes cells expressing CD52 (T and B cells, monocytes, macrophages, NK cells)
- Prolonged depletion (1 yr) of T cells and other immunecells
-
- Myelosuppresion, flu like symptoms
-
-

113
Q

Basiliximab (Anti CD25)

A

*- Antibody / Fusion Protein
- Blocks and opsonizes alpha chain of IL-2 (CD25), found only on activated T cells
- Depletes only antigen activated T cell , reduced incidence of infection and malignancy
- Moderate effect relative to anti-T cell globulin
- Well tolerated
-
-

114
Q

Rh(D) immune globulin

A

*- Antibody / Fusion Protein
- Binds and clears up D-antigen, prevents mother’s immune rxn
-
-
-
-
- Prevent maternal (Rh-) from attacking fetus

115
Q

Belatacept

A

*- Antibody / Fusion Protein
- Fusion of IgG and high-affinity B7 ligand, so without this signal acting on CD28 T cells go into anergy when presented with an antigen. (Binds and clears up D-antigen, prevents mother’s immune rxn?)
-
- Comparable to calcineurin inhibitors in preventing transplant rejection
- Anemia, neutropenia, peripheral edema
- Increased risk of infection and malignancy, especially post-transplant lymphoproliferative disorder
- Use for kidney transplant

116
Q

Interleukin-2

A

*- Cytokines
- Increases proliferation of activated T cells, increases IFN-gamma and cytotoxic killer cell activity
-
-
- Capillary leak syndrome, hypotension, reduced organ perfusion, can be fatal
-
- Used to treat metastatic melanoma, renal cell carcinoma

117
Q

IFN-gamma

A

*- Cytokines
- Stimulates activity of cytotoxic cells
-
-
-
-
- Severe recurrent infections

118
Q

BCG

A

*-Adjuvant
- Increases APC activity by binding pattern recognition receptors
- Live attenuated bacillus calmette-guerin
- Can’t use systemically, will cause septic shock
-
-
- Used topically for bladder cancer

119
Q

Drug Name

A 
Drug Class
Mechanism
Distinguishing Chem Characteristics (Unique or "weird" features)
Pharmacological characteristics
Side Effects
Special side effects
Use
[mnemonic] (put in brackets)
120
Q

acetazolamide

A

*Carbonic anhydrase inhibitor
*reduce HCO3 production to slow aq. humor production
*
*
*diuretic
*
*Open angle glaucoma

121
Q

dichlorphenamide

A

*Carbonic anhydrase inhibitor
*reduce HCO3 production to slow aq. humor production
*
*
*diuretic
*
*Open angle glaucoma

122
Q

dorzolamide

A

*Carbonic anhydrase inhibitor
*reduce HCO3 production to slow aq. humor production
*TOPICAL
*
*diuretic
*
*Open angle glaucoma

123
Q

botulinum toxin A

A

*Miscellaneous
*Paresis of skeletal muscle (relaxation 3-6 wk duration) because presynaptic vesicles can’t exocytose
*Injected
*Use EMG to confirm needle placement
*diuretic
*
*extraocular muscles (squint) & blepharospasm of eyelid.

124
Q

Drug Name

A 
Drug Class
Mechanism
Distinguishing Chem Characteristics (Unique or "weird" features)
Pharmacological characteristics
Side Effects
Special side effects
Use
[mnemonic] (put in brackets)
125
Q

cetirizine (Zyrtec®)

A
  • Second-Generation H1 Antihistamine
  • ## Block histamine at H1 receptors
  • ## High selectivity for H1 sites and has few anti-cholinergic side effects; Penetrates poorly into CNS, reducing sedative effects-
  • allergies
    [mnemonic] (put in brackets)
126
Q

cyclizine (Marezine®)

A
  • First-Generation H1 Antihistamine
  • ## Block histamine at H1 receptors-
  • Sedation
  • Anticholinergic effects (Atropine-like effects toward muscarinic receptors, dry mouth, urinary retention, tachycardia)
  • motion sickness
    [mnemonic] (put in brackets)
127
Q

dimenhydrinate (Dramamine®)

A
  • First-Generation H1 antihistamine
  • ## Block histamine at H1 receptors-
  • Sedation
  • Anticholinergic effects (Atropine-like effects toward muscarinic receptors, dry mouth, urinary retention, tachycardia)
  • motion sickness
    [mnemonic] (put in brackets)
128
Q

diphenhydramine (Benadryl®)

A
  • First-Generation H1 antihistamine
  • ## Block histamine at H1 receptors-
  • Sedation
  • Anticholinergic effects (Atropine-like effects toward muscarinic receptors, dry mouth, urinary retention, tachycardia); Local anesthesia: Block sodium channels
  • motion sickness
    [mnemonic] (put in brackets)
129
Q

fexofenadine (Allegra®)

A
  • Second-Generation H1 Antihistamine
  • ## Block histamine at H1 receptors
  • ## High selectivity for H1 sites and has few anti-cholinergic side effects; Penetrates poorly into CNS, reducing sedative effects-
  • Allergies
    [mnemonic] (put in brackets)
130
Q

loratadine (Claritin®)

A
  • Second-Generation H1 Antihistamine
  • ## Block histamine at H1 receptors
  • ## High selectivity for H1 sites and has few anti-cholinergic side effects; Penetrates poorly into CNS, reducing sedative effects-
  • Allergies
    [mnemonic] (put in brackets)
131
Q

promethazine (Phenergan®)

A
  • First-Generation H1 Antihistamine
  • ## Block histamine at H1 receptors-
  • Sedation
  • Anticholinergic effects (Atropine-like effects toward muscarinic receptors, dry mouth, urinary retention, tachycardia); Local anesthesia: Block sodium channels
  • antiemetic
    [mnemonic] (put in brackets)
132
Q

adalimumab (Humira®)

A
  • anti-TNFalpha agent
  • Binds to TNFalpha, prevents it from binding to its receptor and reduces circulating levels
  • Human antibody to TNFalpha
  • Parenteral administration required
  • increased frequency of infections (upper
    respiratory, urinary)
    -
    -Rheumatoid arthritis, Crohn’s
    [mnemonic] (put in brackets)
133
Q

etanercept (Enbrel®)

A
  • anti-TNFalpha agent
  • Binds to TNFalpha, prevents it from binding to its receptor and reduces circulating levels
  • Fusion protein containing the ligand binding domain of the
    TNFalpha receptor and the Fc domain of human IgG.
  • Parenteral administration required
  • increased frequency of infections (upper
    respiratory, urinary)
    -
    -Rheumatoid arthritis, Crohn’s
    [mnemonic] (put in brackets)
134
Q

infliximab (Remicade®)

A
  • anti-TNFalpha agent
  • Binds to TNFalpha, prevents it from binding to its receptor and reduces circulating levels
  • Humanized antibody to TNFalpha
  • Parenteral administration required
  • increased frequency of infections (upper
    respiratory, urinary)
    -
    -Rheumatoid arthritis, Crohn’s
    [mnemonic] (put in brackets)
135
Q

anakinra (Kineret®)

A
  • Anti-IL1 agent
  • ## Competitive IL-1 receptor antagonist (IL-1Ra analog)
  • Short half-life, daily injection required
    Increased susceptibility to infection
    -
  • Rheumatoid Arthritis, possibly other inflammatory diseases
    [mnemonic] (put in brackets)
136
Q

tofacitinib (Xeljanz®)

A
  • Jak kinase inhibitor
  • Inhibits all activity of cytokines required for adaptive immunity (eg., IL-2, IL-4, etc.) and inhibits all activities for many inflammatory cytokines (eg., IL-6)
    Distinguishing Chem Characteristics (Unique or “weird” features)
  • oral administration; therapeutic doses chosen to produce incomplete Jak inhibition, because higher doses expected to produce potent
    immunosuppression AND adverse effects.
  • ## Anemia, neutropenia, general myelosuppression, increased risk of infection (especially Herpes Zoster)
  • RA: Currently second line therapy for those failing methotrexate
    [mnemonic] (put in brackets)

1 Pharm Unit (14 decks)

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