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PHARM 1 Self > prelimpharm1 > Flashcards

prelimpharm1 Flashcards

1
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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2
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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3
Q

methacholine

A 
-muscarinic cholinergic agonist
-
-CH3 decreases nicotinic affinity
-oral or subQ
-
-
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4
Q

muscarine

A 
-muscarinic cholinergic agonist
-
-alkaloid
-oral or subQ
-
-
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5
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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6
Q

varenicline

A 
-Nicotinic cholinergic agonist
-
-alkaloid
-
-
-
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7
Q

ambenonium

A

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

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8
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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9
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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10
Q

physostigmine

A

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

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11
Q

diisopropylfluorophosphate

A

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

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12
Q

echothiophate

A

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

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13
Q

carbaryl

A

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

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14
Q

malathion

A

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

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15
Q

parathion

A

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

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16
Q

tetraethylpyrophosphate

A

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

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17
Q

sarin

A 
-noncompetitive cholinesterase inhibitor
-
-
-
-nerve gas
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18
Q

soman

A 
-noncompetitive cholinesterase inhibitor
-
-
-
-nerve gas
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19
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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20
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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21
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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22
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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23
Q

methscopolamine

A 
-Muscarinic Cholinergic antagonist
-
-quaternary ammonium
-longer DOA
-
-GI diseases, can inhibit respiratory tract secretions
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24
Q

trihexyphenidyl

A 
-muscarinic cholinergic antagonist
-
-tertiary amine
-3-6hrs DOA
-
-anti-parkinson, excess salivation
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25
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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26
Q

cyclopentolate

A

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

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27
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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28
Q

tiotropium

A 
-Muscarinic Cholinergic antagonist
-
-
-longer DOA, topical
-
-bronchodilation and min. mucociliary clearance problems
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29
Q

darifenacin

A 
- M3 selective cholinergic antagonist
-
-
-longer DOA
-
-
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30
Q

solifenacin

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

tolterodine

A 
-M3 selective cholinergic antagonist
-
-
- longer DOA
-
-
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32
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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33
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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34
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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35
Q

curare

A 
-N2 competitive inhibitor
-
-quaternary nitrogens
-
-
-
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36
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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37
Q

cisatracurium

A

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

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38
Q

mivacurium

A

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

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39
Q

pancuronium

A
  • Ammonio Steroids
  • ## Competitive Nicotinic N2 blocker-
    -long DOA
    -muscarinic block-vagal blockade, tachycardia
    -
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40
Q

vecuronium

A

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

41
Q

albuterol

A

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

42
Q

salmeterol

A

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

43
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

44
Q

beclomethasone

A

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

45
Q

budesonide

A

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

46
Q

fluticasone

A

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

47
Q

prednisone

A

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

48
Q

triamcinolone

A

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

49
Q

montelukast

A

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

50
Q

zafirlukast

A

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

51
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

52
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
53
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
54
Q

ipratropium

A 
-muscarinic cholinergic antagonist
-
-quaternary ammonium
-shorter DOA, topical inhalant 
-tachycardia, decreased salivation
-bronchodilation and min. mucociliary clearance problems
55
Q

theophylline

A
  • Misc. Bronchodilator
  • inhibit phosphodiesterase degradation of cAMP
  • methylxanthine
  • oral, LongDOA
  • tachycardia and CNS stimulation
  • long-term maintenance of asthma
56
Q

metaraminol

A 
Alpha-1 Selective Agonist 
-
-
- Long acting beta 1 and alpha 1 stimulant, Displaces NE
-
-
-
57
Q

methoxamine

A 
Alpha-1 Selective Agonist (less alpha 2)
-
-
-
-
-
- treat hypotensive crisis
58
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
59
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

60
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

61
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

62
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

63
Q

amphetamine

A 
Alpha and beta adrenergic agonist
-
- Releasing agent (increases NE release), also releases intraneuronal NE – reverse transport
-
-
-
-
64
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

65
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
66
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

67
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

68
Q

dobutamine

A 
Beta 1 Selective agonist 
-
-
-(Less binding to beta-2)
-
-
- Cardiogenic shock, heart failure
69
Q

isoproterenol

A 
Beta 1 and 2 agonist
-
-
-
-
-
- Used for relaxation of bronchial smooth muscle, also cardiac stimulation (potent vasodilator)
70
Q

albuterol

A 
Beta 2 Selective agonist 
-
-
-(Less binding to beta-1)
-
-
- Bronchial asthma
71
Q

metaproterenol

A 
Beta 2 Selective agonist 
-
-
-(Less binding to beta-1)
-
-
- Bronchial asthma
72
Q

terbutaline

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

bromocriptine

A

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

74
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

75
Q

fenoldopam

A 
Dopamine Agonist, DA-1 selective 
-
-
-
-
-
- Vasodilation of renal and mesenteric vessels
76
Q

doxazosin

A 
Alpha-1 Selective antagonist
-
-
-
-
-
- Urinary obstruction from BPH
77
Q

prazosin

A

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

78
Q

tamsulosin

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

terazosin

A 
Alpha-1 Selective antagonist
-
-
-
-
-
- Urinary obstruction from BPH
80
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
81
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

82
Q

labetalol

A 
Alpha and beta antagonist
-
- Binds beta receptors better than alpha
-
-
-
-
83
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

84
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

85
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

86
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

87
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

88
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

89
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

90
Q

carteolol

A

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

91
Q

levobunol

A

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

92
Q

metipranolol

A

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

93
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

94
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

95
Q

cocaine

A

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

96
Q

DMI (desmethylimipramine)

A

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

97
Q

tyramine

A 
Releasing Agent 
-
-
- Enhance NE release via Amine 1 transporter
-
-
-
98
Q

pseudoephedrine

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

PHARM 1 Self (6 decks)

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