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Pharmacology > Pharm Lectures 1-4 > Flashcards

Pharm Lectures 1-4 Flashcards

1
Q

OATP

A

organic anion transporting proteins facilitate absorption of some drugs

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2
Q

p-glycoprotein

A

actively remove drugs from epithelial cells and prevent absorption. essential mechanism to prevent toxin absorption

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3
Q

propranolol

A

Beta blockere

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4
Q

Muscarinic

A

acetylcholine receptor at neauroeffector junctions

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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

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6
Q

M1

A

CNS and autonomic ganglia

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7
Q

M2

A

cardiac muscle

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8
Q

M3

A

smooth muscle and glandular tissue

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9
Q

M4 and M5

A

CNS

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10
Q

Ach Response - Heart SA node

A

bradycardia

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11
Q

Ach response-Heart AV node

A

slow conduction

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12
Q

Ach response-blood vessels

A

vasodilation

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13
Q

Ach response - GI tract

A

increased tone and secretions sphincters relax

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14
Q

Ach response Eye (Iris)

A

Miosis (contraction)

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15
Q

Ach response eye (ciliary muscle)

A

accomodation (contraction)

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16
Q

Ach response - urinary bladder

A

detrusor muscle contracts, sphincter relaxes

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17
Q

ach response- lungs

A

bronchi contract, increase in secretions

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18
Q

ach response - exocrine glands

A

increase in tears, sweat, saliva

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19
Q

ach response - ganglia (high doses)

A

sympathetic and parasympathertic responses

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20
Q

ach response - adrenal medulla

A

release of epinephrine and norepinephrine

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21
Q

ach response - skeletal muscle

A

depolarization of end plate

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22
Q

acetylcholine

A

-direct acting agent choline ester no therapeutic use, nonselective and short duration

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23
Q

methacholine

A

-direct acting choline ester agonist -muscarinic and longer duration

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24
Q

carbachol

A

-direct acting choline ester agonist -predominately nicotinic -topical agent for glaucoma

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25
Q

bethanechol

A

-direct acting choline ester agonist -predominately muscarinic - used to stimulate bladder of intestinal tract without having cardiac effects

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26
Q

muscarine

A

-direct acting plant alkalpid agonist -from poisonous mushroom

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27
Q

nicotine

A

-direct acting plant alkaloid agonist -from tobacco -oral, nasal, or transdermal product to assist in smoking cessation

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28
Q

pilocarpine

A

-direct acting plant alkaloid agonist -predominately muscarinic -topical agent for glaucoma and oral agent for xerostomia (dry mouth)

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29
Q

cevimeline (evoxac)

A

-new synthetic direct agonist for xerostomia and dry eyes indicated after radiation treatment or for patients with Sjogren’s syndrome

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30
Q

neostigmine

A

-reversible cholinesterase inhibitor -quaternary amine - poor penetration of CNS -can be used to treat myasthenia gravis

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31
Q

Edrophonium (Tensilon)

A

-reversible cholinesterase inhibitor -neostigmine analog with shorter duration -used to diagnose Myasthenia gravis

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32
Q

physostigmine

A

-reversible cholinesterase inhibitor -alkaloid from alabar bean -tertiary amine - can penetrate CNS -can be used to treat myasthenia gravis

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33
Q

Myasthenia gravis

A

-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

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34
Q

Alzheimers Disease (Drugs)

A
  • can use reversible cholinesterase Donepezil (aricept) - once daily -Galantamine (Rizatidine) -Rivastigmine (Exelon)
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35
Q

Organophosphate Muscarinic effect

A

-bradycardia -hypotension -salivation -sweating -lacrimation miosis

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36
Q

Organophosphate nicotinic effects

A

-muscle fibrillation, fasciculations, paralysis

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37
Q

Organophosphate CNS effects

A

-confusion, ataxia, coma, respiratory paralysis

38
Q

SLUDGE

A

-organophosphate toxicity -Salivation -Lacrimation -Urination -Diarrhea -Gastic -Emptying

39
Q

Atropine

A

-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
Q

scopolamine

A

-has greater CNS effects than atropine -isolated from henbane - transdermal patch for motion sickness

41
Q

Hyoscyamine

A
  • L isomer of atropine -used for gastrointestinal spasms
42
Q

anticholinergic toxic effects

A

-Dry mouth -blurred vision -tachycardia -palpitations -urinary rentention -delirium and hallucinations CONTRAINDICATIONS: glaucome, BPH, dementia, delirium

43
Q

Ipratropium (atrovent) and tiotropium (Spiriva)

A

-muscarinic antagonist - inhaled agents for asthma and COPD

44
Q

Dicyclomine (Bentyl)

A

-muscarinic antagonist -for irritable bowel disease

45
Q

tropicamide (Mydriacyl)

A

-muscarinic antagonist -topical agent to facilitate eye exams -short half life

46
Q

benztropine (Cogentin)

A

-muscarinic antagonist -for drug-induced parkinsonian symptoms from antagonism of dopamine receptors

47
Q

Drugs for overactive bladder

A

-Oxybutinin (Ditropan) -Tolterodine (Detrol) -Solifenacin (VESIcare)

48
Q

d-tubocurarine

A

-non-depolarizing neuromuscular blocking agent -used for muscle relaxation during surgery -first isolated from arrow poisons

49
Q

Succinylcholine

A

-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
Q

catecholamines

A

endogenous adrenergic receptor agonists - epi, NE and dopamine -rapidly metabolized by MAO and COMT -given as parenteral drug

51
Q

a1 adrenergic receptors

A

smooth muscle contraction

52
Q

B2 adrenergic receptors

A

smooth muscle relaxation

53
Q

B1 adrenergic receptor

A

cardiac tissue

54
Q

a2 adrenergic recptors

A

mostly on sympathetic postganglionic neurons -produce feedback inhibition of NT release

55
Q

B3

A

fat cells and increases lipolysis

56
Q

D1

A

dopamine receptors in smooth muscle increase dilation in renal blood vessels

57
Q

D2

A

dopamine receptors in nerve ending - modulate NT release

58
Q

Epinephrine

A
  • 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
Q

Norepinephrine

A

-nonselective direct acting adrenergic agonist - a1=a2 but B1>>B2 -USE: hypotension Adverse effects: similar to epinephrine

60
Q

isoproterenol

A

-synthetic catecholamine -B1=B2 USE: potent vasodilator, potent inotropic agent (increase contraction force -Adverse effects: tachycardia, arrythmias

61
Q

Dobutamin

A

-selective B1 agonist -B1>B2>>>>>a USE: Acute heart failure - potent inotropic agent adverse effects: hypertension and tachycardia

62
Q

-terol

A

-selective B2 agonist -albuterol, levalbuterol (xopenex), salmeterol (serevent) -inhaled bronchodilation for asthma and COPD

63
Q

Terbutaline

A

-selective B2 agonist PO: bronchodilation for asthma IV- relaxation of uterus

64
Q

phenylephrine

A
  • selective A1-adrenergic agonist -vasoconstriction with increased blood pressure IV: for hypotension and shock PO: popular OTC decongestant
65
Q

oxymetazoline (Afrin nasal spray)

A

-selective A1 adrenergic agonist -topical nasal decongestant -causes acut rebound congestion if used for more than several days

66
Q

clonidine

A

-selective a2 adrenergic agonists -centrally acting antihypertensive agents -also used for substance withdrawal -oral or transdermal

67
Q

alpha-methyldopa

A

-selective a2-adrenergic agonist -centrally acting antihypertensive agent -still useful during pregnancy

68
Q

amphetamine and methamphetamine

A

-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
Q

methylphenidate (Ritalin)

A

-indirect acting adrenergic agonist -amphetamine derivative with similar action

70
Q

cocaine

A

-indirect acting adrenergic agonists -inhibits NE, dopamine and serotonin reuptake -peripherally vasoconstrictive and a cardiac stimulant

71
Q

Tyramine

A

-indirect acting adrenergic agonist -naturally occuring in fermented products (cheese wine etc) -increases NE release and can cause hypertensive cirisis with MAO inhibitors

72
Q

Dopamine

A

-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
Q

ephedrine

A

-mixed acting adrenergic agonist -ma-huang -alpha and beta agonist and increased NE release

74
Q

pseudoephedrine (Sudafed)

A

-mixed acting adrenergic agonist -stereoisomer of ephedrine -avoid in patients with hypertension of cardiomypoathy

75
Q

phenoxybenzamine

A

-nonselective alpha blocker -non-competitive/irreversible -a1>a2 use: catecholamine excess such as for PHEOCHROMOCYTOMA adverse: postural hypotension and reflex tachychardia

76
Q

phentolamine

A
  • 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
Q

Selective a1 blockers (function)

A
  • 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
Q

Prazosin

A

selective a1 blocker - prototype drug

79
Q

terazosin (hytrin)

A

selective a1 blocker

80
Q

doxazosin (cardura)

A

selective a1 blocker

81
Q

Tamsulosin (Flomax)

A
  • 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
Q

Propanolol

A
  • 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
Q

Nadolol

A
  • low lipophilicity - less CNS adverse effects than propranolol
  • renal excretion
  • long half life
84
Q

timolol

A
  • non selevtive beta blocker
  • used as topical agent for GLAUCOMA
85
Q

Pindolol

A
  • nonselective B blockers
  • also partial agonist of B1 and B2 receptors
  • intrinsic sympathomimetic activity -causes less bradychardia
86
Q

metoprolol

A
  • 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
Q

atenolol

A
  • selective B1 blocker
  • low lipophilicity - less CNS effect than propranolol
  • renal excretion
  • long half life
88
Q

bisoprolol (zebeta)

A
  • selective B1 blocker
  • moderate lipophilicity
89
Q

esmolol

A
  • selective B1 blocker
  • IV only - short acting beta blocker used in hospital by IV
90
Q

Acebutolol

A
  • selective B1 blocker
  • partial agonist of B1 receptor
  • intrinsic sympathomimetic activity
91
Q

Labetalol and carvedilol

A
  • a and B adrenergic blockers
  • B1=B2, a1>a2
  • labetolol for rapid recution of blood pressure
  • carvedilol for heart failure

Pharmacology (2 decks)

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