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PHARM 1 Self > prelimpharm1 > Flashcards

prelimpharm1 Flashcards

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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
tropicamide
-Muscarinic Cholinergic antagonist -Block M3 on iris & ciliary muscle - -short DOA, only topically - -mydriasis and cycloplegia (1/4 day)
26
cyclopentolate
-muscarinic cholinergic antagonist -block M3's on iris & ciliary muscle - -med DOA - - -Elicit mydriasis & cycloplegia (1 day)
27
ipratropium
``` -Muscarinic Cholinergic antagonist - -quaternary ammonium -shorter DOA, topical inhalant -tachycardia, decreased salivation -bronchodilation and min. mucociliary clearance problems ```
28
tiotropium
``` -Muscarinic Cholinergic antagonist - - -longer DOA, topical - -bronchodilation and min. mucociliary clearance problems ```
29
darifenacin
``` - M3 selective cholinergic antagonist - - -longer DOA - - ```
30
solifenacin
``` -M3 selective cholinergic antagonist - - -longer DOA - - ```
31
tolterodine
``` -M3 selective cholinergic antagonist - - - longer DOA - - ```
32
mecamylamine
- 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
33
trimethaphan
- N1 non-depolarizing Cholinergic competitive antagonist - ganglionic blocker - sulfonium+ - shrot DOA, intravenous - hypotension, brain anoxia - surgically to reduce bleeding=controlled hypotension
34
succinylcholine
-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
35
curare
``` -N2 competitive inhibitor - -quaternary nitrogens - - - ```
36
atracurium
-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)
37
cisatracurium
-benzylisoquinolines -N2 competitive inhibitor -Competitive Nicotinic N2 blocker (N2 Specific) -quaternary nitrogens -medium DOA -histamine release -
38
mivacurium
-benzylisoquinolines -N2 competitive inhibitor -Competitive Nicotinic N2 blocker (N2 Specific) - -short DOA -histamine release -
39
pancuronium
- Ammonio Steroids - Competitive Nicotinic N2 blocker - - -long DOA -muscarinic block-vagal blockade, tachycardia -
40
vecuronium
-N2 competitive inhibitor -Competitive Nicotinic N2 blocker -quaternary nitrogens -med DOA -muscarinic block-vagal blockade, tachycardia -
41
albuterol
-Beta-2 agonist -stim adenyl cyclase and cAMP-->relax bronch smooth m. - -short DOA -tachycardia, muscle tremor, headache -bronchodilate acute asthma
42
salmeterol
-Beta-2 agonist -stim adenyl cyclase and cAMP-->relax bronch smooth m - -long DOA -tachycardia, muscle tremor, headache -bronchodilate
43
salmeterol with fluticasone
-Beta-2 agonist with corticosteroid -stim adenyl cyclase and cAMP-->relax bronch smooth m - -combination necessary in maintenance therapy - -maintenance bronchodilation
44
beclomethasone
-corticosteroid -inhibit inflam. response system thru gene expression - -topical inhalation -generally none -long term asthma reduction
45
budesonide
-corticosteroid -inhibit inflam. response system thru gene expression - -topical inhalation -generally none -long term asthma reduction
46
fluticasone
-corticosteroid -inhibit inflam. response system thru gene expression - -topical inhalation -generally none -long term asthma reduction
47
prednisone
-corticosteroid -inhibit inflam. response system thru gene expression - -oral or intravenous - glucose metab.,Cushing's, hypert, increased infection -asthma
48
triamcinolone
-corticosteroid -inhibit inflam. response system thru gene expression - -topical inhalation -generally none -long term asthma reduction
49
montelukast
-leukotriene modulator -receptor antagonist of LTD4 - -oral - -long-term controller of asthma
50
zafirlukast
-leukotriene modulator -receptor antagonist of LTD4 - -oral - - long term controller of asthma
51
zileuton
-leukotriene modulator -inhibitor of 5-lipoxygenase inhibiting synthesis of LTB/D4 - -oral -liver toxicity, and inhibits some CYPs -long term controller of asthma
52
cromolyn
- degranulation inhibitor - possible inhibit of Ca channels in Mast cell degranulation - poorly soluble salt - Topical - well tolerated - long term prophylactic maintenance of asthma
53
nedocromil
- degranulation inhibitor - possible inhibit of Ca channels in Mast cell degranulation - poorly soluble salt - Topical - well tolerated - long term prophylactic maintenance of asthma
54
ipratropium
``` -muscarinic cholinergic antagonist - -quaternary ammonium -shorter DOA, topical inhalant -tachycardia, decreased salivation -bronchodilation and min. mucociliary clearance problems ```
55
theophylline
- Misc. Bronchodilator - inhibit phosphodiesterase degradation of cAMP - methylxanthine - oral, LongDOA - tachycardia and CNS stimulation - long-term maintenance of asthma
56
metaraminol
``` Alpha-1 Selective Agonist - - - Long acting beta 1 and alpha 1 stimulant, Displaces NE - - - ```
57
methoxamine
``` Alpha-1 Selective Agonist (less alpha 2) - - - - - - treat hypotensive crisis ```
58
phenylephrine
``` 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
alpha-methyldopa
*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
clonidine
*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
apraclonidine
*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
guanabenz
*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
amphetamine
``` Alpha and beta adrenergic agonist - - Releasing agent (increases NE release), also releases intraneuronal NE – reverse transport - - - - ```
64
ephedrine
Alpha and beta adrenergic agonist - - - 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
epinephrine
``` Alpha and beta adrenergic agonist - - - Binds all adrenergic receptors equally - - - Potent vasoconstrictor and cardiac stimulant, hemostasis during surgery, reduce drug diffusion, anaphylaxis ```
66
norepinephrine
-Alpha and beta adrenergic agonist (except beta 2) - - - 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
dipivefrin
*Mixed alpha, beta agonist *stim alpha 2 on ciliary body, alpha 1 on ciliary vessels *Prodrug metabolized to Epi. * * * *Open angle glaucoma
68
dobutamine
``` Beta 1 Selective agonist - - -(Less binding to beta-2) - - - Cardiogenic shock, heart failure ```
69
isoproterenol
``` Beta 1 and 2 agonist - - - - - - Used for relaxation of bronchial smooth muscle, also cardiac stimulation (potent vasodilator) ```
70
albuterol
``` Beta 2 Selective agonist - - -(Less binding to beta-1) - - - Bronchial asthma ```
71
metaproterenol
``` Beta 2 Selective agonist - - -(Less binding to beta-1) - - - Bronchial asthma ```
72
terbutaline
``` Beta 2 Selective agonist - - -(Less binding to beta-1) - - - Bronchial asthma, relax pregnant uterus ```
73
bromocriptine
Dopamine Agonist - - - - postural hypotension and cardiac arrhythmia - - Anti-parkinson agent (for its CNS effects)
74
dopamine
Dopamine Agonist - - - Binds Alpha and Beta 1 at high concentrations, Enhance NE release (displaces it) - - - IV for shock, vasoconstriction, increase CO and dilate renal arteries
75
fenoldopam
``` Dopamine Agonist, DA-1 selective - - - - - - Vasodilation of renal and mesenteric vessels ```
76
doxazosin
``` Alpha-1 Selective antagonist - - - - - - Urinary obstruction from BPH ```
77
prazosin
Alpha-1 Selective antagonist (Highly selective) - - - Oral admin - - Little to no tachycardia because doesn’t bind beta receptors - Antihypertensive (mild / moderate), urinary obstruction from BPH
78
tamsulosin
``` Alpha-1 Selective antagonist - - - - - - Urinary obstruction from BPH ```
79
terazosin
``` Alpha-1 Selective antagonist - - - - - - Urinary obstruction from BPH ```
80
phenozybenzamine
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
phentolamine
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
labetalol
``` Alpha and beta antagonist - - Binds beta receptors better than alpha - - - - ```
83
atenolol
*β1 selective antagonist *inhibit CO; class generally pure antagonist (binds but does not activate receptor) *β1 >>> 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
betaxolol
*β1 selective antagonist *block B1 receptors on ciliary body to reduce aq. humor production; inhibit CO; class generally pure antagonist *β1 >>> 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
metoprolol
*β1 selective antagonist *inhibit CO; class generally pure antagonist *β1 >>> 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
nadolol
*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
pindolol
*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
propranolol
*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
timolol
*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
carteolol
*B non-selective antagonist *block B1R's on ciliary body to reduce aq. humor production * *topical * * *Open angle glaucoma
91
levobunol
*B non-selective antagonist *block B1R's on ciliary body to reduce aq. humor production * *topical * * *Open angle glaucoma
92
metipranolol
*B non-selective antagonist *block B1R's on ciliary body to reduce aq. humor production * *topical * * *Open angle glaucoma
93
guanethidine
*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
reserpine
*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
cocaine
*Amine I transport (NET) inhibitor *NE levels rise in synapse -> mimic sympathetic nerve stimulation * * *vasoconstriction, tachycardia, mydriasis * *hemostasis during surgery
96
DMI (desmethylimipramine)
*Amine I transport (NET) inhibitor *NE levels rise in synapse -> mimic sympathetic nerve stimulation * * *vasoconstriction, tachycardia, mydriasis * *
97
tyramine
``` Releasing Agent - - - Enhance NE release via Amine 1 transporter - - - ```
98
pseudoephedrine
``` Releasing Agent - - - - - - Reduces congestion of mucus membranes ```

PHARM 1 Self (6 decks)

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