Pharm Lectures 1-4 Flashcards
(91 cards)
1
Q
OATP
A
organic anion transporting proteins facilitate absorption of some drugs
2
Q
p-glycoprotein
A
actively remove drugs from epithelial cells and prevent absorption. essential mechanism to prevent toxin absorption
3
Q
propranolol
A
Beta blockere
4
Q
Muscarinic
A
acetylcholine receptor at neauroeffector junctions
5
Q
nicotinic
A
acetylcholine receptor at all autonomic ganglia and somatic neuromuscular junctions - leads to contraction of skeletal muscle -at ALL autonomic ganglia- leads to postganglionic release of neurotransmitters at Neuroeffector junctions
6
Q
M1
A
CNS and autonomic ganglia
7
Q
M2
A
cardiac muscle
8
Q
M3
A
smooth muscle and glandular tissue
9
Q
M4 and M5
A
CNS
10
Q
Ach Response - Heart SA node
A
bradycardia
11
Q
Ach response-Heart AV node
A
slow conduction
12
Q
Ach response-blood vessels
A
vasodilation
13
Q
Ach response - GI tract
A
increased tone and secretions sphincters relax
14
Q
Ach response Eye (Iris)
A
Miosis (contraction)
15
Q
Ach response eye (ciliary muscle)
A
accomodation (contraction)
16
Q
Ach response - urinary bladder
A
detrusor muscle contracts, sphincter relaxes
17
Q
ach response- lungs
A
bronchi contract, increase in secretions
18
Q
ach response - exocrine glands
A
increase in tears, sweat, saliva
19
Q
ach response - ganglia (high doses)
A
sympathetic and parasympathertic responses
20
Q
ach response - adrenal medulla
A
release of epinephrine and norepinephrine
21
Q
ach response - skeletal muscle
A
depolarization of end plate
22
Q
acetylcholine
A
-direct acting agent choline ester no therapeutic use, nonselective and short duration
23
Q
methacholine
A
-direct acting choline ester agonist -muscarinic and longer duration
24
Q
carbachol
A
-direct acting choline ester agonist -predominately nicotinic -topical agent for glaucoma
25
bethanechol
-direct acting choline ester agonist -predominately muscarinic - used to stimulate bladder of intestinal tract without having cardiac effects
26
muscarine
-direct acting plant alkalpid agonist -from poisonous mushroom
27
nicotine
-direct acting plant alkaloid agonist -from tobacco -oral, nasal, or transdermal product to assist in smoking cessation
28
pilocarpine
-direct acting plant alkaloid agonist -predominately muscarinic -topical agent for glaucoma and oral agent for xerostomia (dry mouth)
29
cevimeline (evoxac)
-new synthetic direct agonist for xerostomia and dry eyes indicated after radiation treatment or for patients with Sjogren's syndrome
30
neostigmine
-reversible cholinesterase inhibitor -quaternary amine - poor penetration of CNS -can be used to treat myasthenia gravis
31
Edrophonium (Tensilon)
-reversible cholinesterase inhibitor -neostigmine analog with shorter duration -used to diagnose Myasthenia gravis
32
physostigmine
-reversible cholinesterase inhibitor -alkaloid from alabar bean -tertiary amine - can penetrate CNS -can be used to treat myasthenia gravis
33
Myasthenia gravis
-autoimmune disease producing antibodies against nicotinic receptors in skeletal muscle--\>severe muscle weakness -edrophonium used to diagnose it and neostigmine and pyridostigmine are used for treatment
34
Alzheimers Disease (Drugs)
- can use reversible cholinesterase Donepezil (aricept) - once daily -Galantamine (Rizatidine) -Rivastigmine (Exelon)
35
Organophosphate Muscarinic effect
-bradycardia -hypotension -salivation -sweating -lacrimation miosis
36
Organophosphate nicotinic effects
-muscle fibrillation, fasciculations, paralysis
37
Organophosphate CNS effects
-confusion, ataxia, coma, respiratory paralysis
38
SLUDGE
-organophosphate toxicity -Salivation -Lacrimation -Urination -Diarrhea -Gastic -Emptying
39
Atropine
-anticholinergic (plant alkaloid) -muscarinic antagonist -belladonna alkaloid -widely distributed -Half-life = 2 hours -blocks M1, M2, M3 -used for sinus bradycardia and cholinesterase inhibitor overdose
40
scopolamine
-has greater CNS effects than atropine -isolated from henbane - transdermal patch for motion sickness
41
Hyoscyamine
- L isomer of atropine -used for gastrointestinal spasms
42
anticholinergic toxic effects
-Dry mouth -blurred vision -tachycardia -palpitations -urinary rentention -delirium and hallucinations CONTRAINDICATIONS: glaucome, BPH, dementia, delirium
43
Ipratropium (atrovent) and tiotropium (Spiriva)
-muscarinic antagonist - inhaled agents for asthma and COPD
44
Dicyclomine (Bentyl)
-muscarinic antagonist -for irritable bowel disease
45
tropicamide (Mydriacyl)
-muscarinic antagonist -topical agent to facilitate eye exams -short half life
46
benztropine (Cogentin)
-muscarinic antagonist -for drug-induced parkinsonian symptoms from antagonism of dopamine receptors
47
Drugs for overactive bladder
-Oxybutinin (Ditropan) -Tolterodine (Detrol) -Solifenacin (VESIcare)
48
d-tubocurarine
-non-depolarizing neuromuscular blocking agent -used for muscle relaxation during surgery -first isolated from arrow poisons
49
Succinylcholine
-depolarizing neuromuscular blocking Agent (only rug in its class) -has two Ach molecules linked together -binds nicotinic receptor and causes persistent depolarization leading to sustained muscle paralysis - short duration - used in emergency room -no antidote -can cause HYPERkalemia, K should be monitored after use
50
catecholamines
endogenous adrenergic receptor agonists - epi, NE and dopamine -rapidly metabolized by MAO and COMT -given as parenteral drug
51
a1 adrenergic receptors
smooth muscle contraction
52
B2 adrenergic receptors
smooth muscle relaxation
53
B1 adrenergic receptor
cardiac tissue
54
a2 adrenergic recptors
mostly on sympathetic postganglionic neurons -produce feedback inhibition of NT release
55
B3
fat cells and increases lipolysis
56
D1
dopamine receptors in smooth muscle increase dilation in renal blood vessels
57
D2
dopamine receptors in nerve ending - modulate NT release
58
Epinephrine
- a1=a2, and B1=B2 - low doses: B effects predominate -high doses A1 predominates -USE: anaphylactic shock, cardiac arrest and topical vasoconstriction Adverse effects: tremor, palpitations, headaches, arrhytmias
59
Norepinephrine
-nonselective direct acting adrenergic agonist - a1=a2 but B1\>\>B2 -USE: hypotension Adverse effects: similar to epinephrine
60
isoproterenol
-synthetic catecholamine -B1=B2 USE: potent vasodilator, potent inotropic agent (increase contraction force -Adverse effects: tachycardia, arrythmias
61
Dobutamin
-selective B1 agonist -B1\>B2\>\>\>\>\>a USE: Acute heart failure - potent inotropic agent adverse effects: hypertension and tachycardia
62
-terol
-selective B2 agonist -albuterol, levalbuterol (xopenex), salmeterol (serevent) -inhaled bronchodilation for asthma and COPD
63
Terbutaline
-selective B2 agonist PO: bronchodilation for asthma IV- relaxation of uterus
64
phenylephrine
- selective A1-adrenergic agonist -vasoconstriction with increased blood pressure IV: for hypotension and shock PO: popular OTC decongestant
65
oxymetazoline (Afrin nasal spray)
-selective A1 adrenergic agonist -topical nasal decongestant -causes acut rebound congestion if used for more than several days
66
clonidine
-selective a2 adrenergic agonists -centrally acting antihypertensive agents -also used for substance withdrawal -oral or transdermal
67
alpha-methyldopa
-selective a2-adrenergic agonist -centrally acting antihypertensive agent -still useful during pregnancy
68
amphetamine and methamphetamine
-indirect acting adrenergic agonists -stimulate release of NE and dopamine -lipid soluble; can enter CNS -stimulant effects on mood and alertness and an appetit depressant -peripherally vasoconstrictive and a cardiac stimulant
69
methylphenidate (Ritalin)
-indirect acting adrenergic agonist -amphetamine derivative with similar action
70
cocaine
-indirect acting adrenergic agonists -inhibits NE, dopamine and serotonin reuptake -peripherally vasoconstrictive and a cardiac stimulant
71
Tyramine
-indirect acting adrenergic agonist -naturally occuring in fermented products (cheese wine etc) -increases NE release and can cause hypertensive cirisis with MAO inhibitors
72
Dopamine
-mixed acting adrenergic agonist D1=D2\>\>B1\>\>a1 -low doses D receptor increases renal blood flow -medium dose: D +b1 activated -high dose: D + B1 +a1 activated use: cardiogenic shock, acute renal failure adverse effects: similar to NE at high doses
73
ephedrine
-mixed acting adrenergic agonist -ma-huang -alpha and beta agonist and increased NE release
74
pseudoephedrine (Sudafed)
-mixed acting adrenergic agonist -stereoisomer of ephedrine -avoid in patients with hypertension of cardiomypoathy
75
phenoxybenzamine
-nonselective alpha blocker -non-competitive/irreversible -a1\>a2 use: catecholamine excess such as for PHEOCHROMOCYTOMA adverse: postural hypotension and reflex tachychardia
76
phentolamine
* nonselective alpha blocker
* competitive antagonist
* a1=a2
* Uses
* PHEOCHROMOCYTOMA
* reversal of ischemia from extravasation or injection of adrenergic agonists such as epi
* adverse effects: same a phenoxybenzamine
77
Selective a1 blockers (function)
* relax vascular smooth muscle
* relax smooth muscle of bladder neck and prostate
* USES: BPH
* 3rd line agents for hypertension
* adverse effects: 1st dose syncope and reflex tachycardia
78
Prazosin
selective a1 blocker - prototype drug
79
terazosin (hytrin)
selective a1 blocker
80
doxazosin (cardura)
selective a1 blocker
81
Tamsulosin (Flomax)
* selective a1 blocker
* sepecific antagonist of A1a receptor in prostate gland
* helps decrease urinary obstruction from BPH
* causes less vasodilation than other alpha1 blocker and has little effect on blood pressure at normal doses
82
Propanolol
* nonselective beta blocker
* B1=B2
* decreases cardiac contractitlity and heart rate
* bronchoconstiction and decreased glycogenolysis
* USE: hypertension, arrythmias, angina, migrain headache, essential tremor
* adverse effects/cautions: bradycardia, insomnia, heart failure, asthma, diabtetes
83
Nadolol
* low lipophilicity - less CNS adverse effects than propranolol
* renal excretion
* long half life
84
timolol
* non selevtive beta blocker
* used as topical agent for GLAUCOMA
85
Pindolol
* nonselective B blockers
* also partial agonist of B1 and B2 receptors
* intrinsic sympathomimetic activity -causes less bradychardia
86
metoprolol
* selective B1 locker
* B1\>\>B2
* known as cardioselective B clocker
* used for hypertension (higher doses) heart failure (low doses) and angina
* half life: 3- 8 hours
* metabolized by CYP 2D6 phenotype
87
atenolol
* selective B1 blocker
* low lipophilicity - less CNS effect than propranolol
* renal excretion
* long half life
88
bisoprolol (zebeta)
* selective B1 blocker
* moderate lipophilicity
89
esmolol
* selective B1 blocker
* IV only - short acting beta blocker used in hospital by IV
90
Acebutolol
* selective B1 blocker
* partial agonist of B1 receptor
* intrinsic sympathomimetic activity
91
Labetalol and carvedilol
* a and B adrenergic blockers
* B1=B2, a1\>a2
* labetolol for rapid recution of blood pressure
* carvedilol for heart failure
