Pharmacology Exam 1 - Drugs only

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nielemi
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235376
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Pharmacology Exam 1 - Drugs only
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2013-09-20 07:00:13
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Pharmacology Carver College Medicine Medical School
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First exam, flashcard set of only drugs, not concepts
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  1. Bethanechol
    • A muscarinic receptor stimulant
    • Stimulates smooth muscle post-operatively (whe atony of GI tract following surgery, dysfunction with bladder emptying, and promotion of saliva formation)
    • Not effectively hydrolyzed by AChE, so has a longer half-life than methacholine
  2. Methacholine
    • A muscarinic receptor stimulant
    • Used to test funciton of muscarinic receptors, to slow heart in severe tachycardia (other approaches are tried first), and to test for bronchial hyperactivity
    • Effectively hydrolyzed by AChE, so has a short half-life (10 mins)
  3. Carbachol
    • Muscarinic receptor stimulants
    • Used for corneal application for therapy of wide-angle glaucoma to constrict ciliary muscle, which opens the meshwork of the canal of Schlemm
    • Not effectively hydrolyzed by AChE, so has a longer half-life than methacholine
  4. Pilocarpine
    • Muscarinic receptor stimulants
    • Used to increase salivary secretions
  5. Demecarium
    • Reversible inhibitor of AChE
    • Topically used for glaucoma
  6. Edrophonium
    • Reversible inhibitor of AChE
    • Used to diagnose myasthenia gravis
    • Short acting
    • Is a simple alcohol with quaternary ammonium group
  7. Neostigmine
    • Reversible inhibitor of AChE
    • Increases smooth muscle motility and is useful for paralytic ileus and atony of the bladder from surgery; treatment and diagnosis of myasthenia gravis; and reversal of neuromuscular blockade
    • Intermediate acting
    • Is a carbamate with quaternary ammonium group
  8. Physostigmine
    • Reversible inhibitor of AChE
    • Used topically for therapy of wide-angle glaucoma
    • Is a carbamate with tertiary amine group
  9. Pyridostigmine
    • Reversible inhibitor of AChE
    • Used in the treatment of myasthenia gravis; pretreatment to reduce mortality after exposure to nerve gases; reversal of neuromuscular blockade
    • Is a carbamate
  10. Echothiophate
    • Irreversible inhibitor of AChE
    • Used for glaucoma
    • Is an organo-phosphate
  11. Malathion
    • Irreversible inhibitor of AChE (is an organo-phosphate)
    • Used for treatment of head lice
    • Is an insecticide
  12. Diisopropylfluorophosphate (DFP)
    • Irreversible inhibitor of AChE (is an organo-phosphate)
    • Used in insecticides
  13. Parathion
    • Irreversible inhibitor of AChE (is an organo-phosphate)
    • Used in insecticides and is a common agent of organo-phosphate poisoning
    • These O-Ps are highly toxic and cause 25,000 deaths/year worldwide
  14. Sarin and soman
    • Irreversible inhibitor of AChE (is an organo-phosphate)
    • These are nerve gases that are highly volatile
  15. Atropine
    • Reversible muscarinic receptor antagonist; has little toxicity at nicotinic receptors
    • Used when organo-phosphate intoxication occurs; also useful for making mydriasis and cycloplegia (long-acting); sweat, bronchial, and saliva glands are very sensitive; good treatment for Parkinson disease
    • Elicits some tachycardia, because it blocks vagal slowing of the heart
    • Can also cause reduced gastric secretions, but only at high doses
    • A tertiary amine, capable of crossing the BBB; diffuses quickly
  16. Pralidoxime
    • AChE reactivator
    • Used to reverse nerve gas or insecticidal poisoning
    • Must be given in a timely manner because it works on the inhibited AChE intermediate, not the "aged" AChE
  17. Scopolamine
    • Reversible muscarinic receptor antagonist
    • Used for motion sickness; does cause amnesia
    • A tertiary amine, capable of crossing the BBB; diffuses quickly
  18. Methscopolamine
    • Reversible muscarinic receptor antagonist
    • Used mainly for GI diseases to inhibit secretions (also inhibits secretion of respiratory tract)
    • A quaternary amine, incapable of crossing the BBB
  19. Homatropine and Tropicamide
    • Reversible muscarinic receptor antagonist
    • Used to cause mydriasis and cycloplegia [intermediate (2-4 hours) and short-acting (0.5-1.5 hours), respectively]
    • Tertiary amines, capable of crossing BBB, but are applied topically to the eye
  20. Trihexyphenidyl
    • Reversible muscarinic receptor antagonist
    • Used for Parkinson disease treatment
    • A tertiary amine, capable of crossing the BBB
  21. Oxybutinin
    • Reversible muscarinic receptor antagonist
    • Used for relaxation of smooth muscle of genitourinary system (urinary urgency, urinary retention, or bladder spasm)
    • Some M3 selectivity
  22. Darifenacin, Solifenacin, Tolterodine
    • Reversible muscarinic receptor antagonists
    • Used for relaxation of smooth muscle of genitourinary system (urinary urgency, urinary retention, or bladder spasm)
    • Very specific for M3 receptor blocking; leads to longer duration of action
  23. Trimethaphan
    • Competitive ganglionic blocking agent (N1 blocker)
    • Used to lower arterial pressure to control bleeding
    • May cause excessive hypotension and possible brain anoxia
    • Is short-acting
  24. Mecalmylamine
    • Competitive ganglionic blocking agent (N1)
    • Used to improve absorption from GI tract following oral administration (slows GI movement)
    • A secondary amine, capable of crossing the BBB
    • Causes CNS sie effects including tremors, confusion, seizures, mania, and depression
  25. Curare
    • Competitive inhibitor of acetylcholine
    • Used to cause relaxation of skeletal muscles
  26. Cisatracurium
    • Competitive inhibitor of acetylcholine
    • Used to cause relaxation of skeletal muscles
  27. Vecuronium
    • Competitive inhibitor of acetylcholine
    • Used to cause relaxation of skeletal muscles
  28. Succinylcholine
    • Noncompetitive inhibitor of acetylcholine
    • Causes depolarization of end-plate region (contraction happens first, followed by a persistent relaxation and inhibition)
    • Short acting due to degradation by plasma ChE, but plasma ChE inhibitors can augment effect
    • Phase I inhibition: Membrane is depolarized
    • Phase II inhibition: Membrane repolarizes but is resistant to any other depolarization
    • Used to cause relaxation of skeletal muscles
  29. Ephedrine
    • Used to increase transmission at the neuromuscular junction following blocking, but mechanism is unknown
    • Adrenergic receptor agonist
    • A1 and B1 receptors
    • Has a substitution to benzene ring, making it a poor substrate for COMT inactivation and a longer-acting catecholamine
    • Also has a substitution to the alpha carbon, making it a poor substrate for MAO inactivation, and can displace NE from adrenergic storage vesicles, making it a norepinephrine releasing agent
    • Results in: High cardiac output and arterial pressure; mild stimulation of CNS; mild B2 activity to dilate bronchial smooth muscle; nasal decongestant
    • Used clinically for chronic orthostatic hypotension (A1 and B1); hemostasis during surgery, reducing diffusion of local anesthetics from injection site, reducing congestion of mucous membranes (A1 vasoconstriction); rescuing cardiac function (B1); anaphylaxis; stress incontinence (B2)
  30. Nicotine
    • Increased cardiac rate, vasoconstriction, and plasma levels of epinephrine from stimulation of adrenal medulla; decreased mucociliary movement in lungs; and mild CNS stimulation
    • Also causes small cell carcinoma of the lung and cardiovascular disease
    • Lethal dose: 40mg (same as cigar), but bioavailability is very low
    • Keep in mind that nicotine also stimulates N2 receptors in addition to N1
    • Acute nicotine toxicity can lead to neuromuscular blockade
  31. Isoproterenol
    • Adrenergic receptor agonist
    • Has a substitution to amino group, so has greater B receptor affinity
    • B1 = B2 >>>>>> A
    • Potent vasodilator (B2) to skeletal muscles, resulting in decreased MAP; significant increase in cardiac output (B1)
  32. Dobutamine
    • Adrenergic receptor agonist
    • Has a substitution to amino group, so has greater B receptor affinity
    • B1 > B2 >>>>>> A
    • Used to treat cardiogenic shock following MI (B1)
  33. Terbutaline
    • Adrenergic receptor agonist
    • Has a substitution to amino group, so has greater B receptor affinity
    • B2 >> B1 >>>>>> A
    • Used for bronchial asthma treatment or to relax a pregnant uterus
  34. Metaproterenol
    • Adrenergic receptor agonist
    • B2 >> B1 >>>>>> A
    • Used for bronchial asthma treatment
  35. Albuterol
    • Adrenergic receptor agonist
    • B2 >> B1 >>>>>> A
    • Used for bronchial asthma treatment
  36. Metaraminol
    • Adrenergic receptor agonist
    • Has a substitution to benzene ring, making it a poor substrate for COMT inactivation and a longer-acting catecholamine
    • Also has a substitution to the alpha carbon, making it a poor substrate for MAO inactivation, and can displace NE from adrenergic storage vesicles
    • A1 selective
  37. Phenylephrine
    • Adrenergic receptor agonist
    • Has a substitution to benzene ring, making it a poor substrate for COMT inactivation and a longer-acting catecholamine
    • A1 > A2 >>>>>> B
    • Used to overcome hypotensive crisis to protect cerebral and coronary blood flow (A1); reducing diffusion of local anesthetics (A1); reducing congestion of mucous membranes (A1); eliciting mydriasis to facilitate a retinal exam
  38. Pseudoephedrine
    • Norepinephrine releasing agent
    • Used to reduce congestion of mucous membranes
  39. Methoxamine
    • Adrenergic receptor agonist
    • A1 > A2 >>>>>> B
    • Used to overcome hypotensive crisis to protect cerebral and coronary blood flow
  40. Clonidine and methyl-NE
    • Adrenergic receptor agonists
    • A2 > A1 >>>>>> B
    • Since they are specific for A2, they inhibit norepinephrine release
  41. Guanabenz and a-methyldopa
    • Adrenergic receptor agonists
    • A2
    • Since they are specific for A2, they inhibit norepinephrine release
    • a-methyldopa: Is a false neurotransmitter, because it is incorporated into biosynthesis by replacing DOPA (enters CNS too); a-methyl norepinephrine (MNE) is made and stored in synaptic vesicles instead of norepinephrine
    • MNE is released from terminals, but has little effect on receptors; does also stimulate brainstem to affect the vasomotor center to decrease blood pressure
    • Side Effects: Sedation, dizziness, sleep disturbances, impotence, dry mouth, nasal congestion, postural hypotension in some patients
    • Severe Problems: Brought on by chronic therapy; hemolytic anemia, leukopenia, heatitis, lupus-like problems
  42. Fenoldopam
    • Adrenergic receptor agonist
    • D1 >> D2
  43. Dopamine
    • Adrenergic receptor agonist
    • Released by postanglionic sympathetic nerves of renal and splanchnic vasculature smooth muscle
    • D1 = D2 >> B >> A
    • A1 and B1 are stimulated at HIGHER DOSES
    • Also acts as a norepinephrine releasing agent when taken up by amine I transport (NET) into prejunctional sympathetic terminals
    • Used as a therapy for shock: Increases vasoconstriction (A1), cardiac rate/contractility (B1), blood flow to kidneys and mesentary (D1)
  44. Epinephrine
    • Adrenergic receptor agonist
    • Released from adrenal medulla directly into venous circulation
    • A1 = A2
    • B1 = B2, but are 10x more sensitive to epinephrine than A1/A2
    • In other words, will stimulate B receptors at low doses, resulting in decreased MAP; at higher doses, A1 receptors are stimulated, resulting in vasoconstriction and increased MAP
    • Used as a very potent vasoconstrictor (A1) and cardiac stimulant (B1); vasodilation to skeletal muscle also occurs (B2)
    • MOST POTENT VASOPRESSOR when given at high doses
  45. Norepinephrine
    • Adrenergic receptor agonist
    • Primary neurotransmitter of adrenergic nerves
    • A1 = A2   B1 >> B2
    • Used as a very potent vasoconstrictor (A1) and cardiac stimulant (B1); elicits MAP due to lack of B2 stimulation
  46. Cocaine
    • Amine I transporter (NET) inhibitor (prejunctional sympathetic stimulator)
    • Results in higher synaptic levels of NE, causing sympathetic stimulation
    • Causes vasoconstriction, tachycardia, and mydriasis
    • Used to prevent hemostasis during surgery
  47. Tricyclic antidepressants [DMI]
    • Amine I transporter (NET) inhibitors (prejunctional sympathetic stimulators)
    • Result in higher synaptic levels of NE, causing sympathetic stimulation
    • Causes vasoconstriction, tachycardia, and mydriasis
  48. Haloperidol and chlorpromazine
    • D2 receptor blockers
    • Block negative feedback of postganglionic sympathetic nerve
    • Results in greater dopamine release
    • Used as antipsychotic agents
    • May have peripheral side effects
  49. Tyramine
    • Norepinephrine releasing agent
    • Phenylethylamine derivative that is taken up by NET and displaces NE from storage vesicles, causing greater release in synapse
    • Patients on MAO inhibitors (which cause prolonged amounts of norepinephrine in synapse anyway) should avoid eating cheeses, sausage,or smoked/pockled fish because they are high in tyramine
    • Excessive release of norepinephrine will raise arterial pressure
  50. Amphetamines
    • Norepinephrine releasing agents
    • Taken up by NET and displaces NE from storage vesicles, causing greater release in synapse
    • Also reverses amine I transport (NET) to move norepinephrine out of terminal
    • Also directly stimulates A1 and B1 receptors
    • Results in elevation of arterial pressure
  51. Apraclonidine and brimonidine
    • Adrenergic receptor agonists
    • Used for glaucoma treatment (B2 receptors cause decreased intraocular pressure)
  52. Bromocriptine
    • D2 receptor agonist
    • Results in decreased amounts of norepinephrine released
    • Used as an anti-Parkinson agent for CNS activities
    • Side Effects: Postural hypotension durig initial therapy; development of cardiac arrhythmia
  53. Reserpine
    • Norepinephrine depleting agent
    • Prevents norepinephrine (and epinephrine, dopamine, and serotonin) transport into storage vesicles by VMAT
    • Side Effects: Sedation, depression, Parkinsonian symptoms, increased GI motility & ulcers
  54. Guanethidine
    • Norepinephrine depleting agent via membrane stabilization
    • Prevents norepinephrine release by stabilizing the membranes; norepinephrine becomes trapped within synaptic vesicles
    • Used to elicit hypotension
    • Amine I transport (NET) inhibitors [cocaine, tricyclic antidepressants] antagonize this hypotensive activity by not allowing norepinephrine to be transported back into the cell
    • Benefits: Minimal effects with other biogenic amines (epinephrine, dopamine); minimal adverse side effects in CNS because does not cross BBB
  55. Prazosin
    • Competitive A1 adrenergic blocker
    • A1 >>>>>> A2
    • Used for therapy of hypertension
    • Little or no tachycardia due to selectivity for A1 receptors
    • Long-acting
  56. Tamsulosin
    • A1 adrenergic blocker
    • Likely used for therapy of hypertension
  57. Terazosin and doxazosin
    • A1 adrenergic blockers
    • A1 >>>>>> A2
    • Used for therapy of hypertension
  58. Phenoxybenzamine
    • Irreversible A1 and A2 adrenergic blocker; also inhibits Amine I of norepinephrine
    • Used for treatment of hypertension (as an adjunct) or pheochromocytoma
    • Side Effects: Postural hypotension and tachycardia, which results from reflex activation of adrenergic nervous system due to decreased MAP
    • Long-acting
  59. Phentolamine
    • Competitive A1 adrenergic blocker
    • Inhibits both A1 = A2
    • A1 inhibition results in vasodilation
    • However, A2 inhibition results in increased levels of norepinephrine, which stimulates the B1 receptors, causing increased cardiac output and tachycardia
    • Used for pheochromocytoma preoperative management or for inoperable tumors
    • "Dirty" drug because also interacts with muscarinic and histamine receptors
  60. Labetalol
    Blocks A and B adrenergic receptors
  61. Propranolol
    • B1/B2 adrenergic blocker
    • Is an effective prophylactic agent to prevent recurrence of myocardial infarction
    • Used as an antihypertensive, anti-arrhythmic, chest pain, migraine headache
    • Side Effects: Ataxia and dizziness
    • 3-6 hour half-life
  62. Pindolol
    • B1/B2 adrenergic blocker
    • Used as an antihypertensive
    • 3-6 hour half-life
  63. Timolol
    • B1/B2 adrenergic blocker
    • Is an effective prophylactic agent to prevent recurrence of myocardial infarctoin
    • Used to reduce intraocular pressure in glaucoma patients; as an antihypertensive; and for chest pain
    • 4-5 hour half-life
  64. Nadolol
    • B1/B2 adrenergic blocker
    • Used as an antihypertensive
    • Fewer CNS side effects because cannot cross BBB well
    • 14-24 hour half-life
  65. Betaxolol
    • B1 specific adrenergic blocker
    • Still use cautiously in asthmatic patients
    • Used to treat glaucoma
    • Long half-life
  66. Atenolol
    • B1-specific adrenergic blocker
    • Still use cautiously in asthmatic patients
    • Used to treat hypertension
    • Fewer side effects because cannot cross BBB well
    • 6-9 hour half-life
  67. Metoprolol
    • B1-specific adrenergic blocker
    • Still use cautiously in asthmatic patients
    • Is a super effective prophylactic agent to prevent recurrence of myocardial infarction
    • Used as an antihypertensive and for chest pain
    • Side Effects: Ataxia and dizziness
    • 3-4 hour half-life
  68. Diphenhydramine
    • First-generation antihistamine
    • Causes sedation
  69. Dimenhydrinate
    • First-generation antihistamine
    • Causes sedation
  70. Cyclizine
    • First-generation antihistamine
    • Causes sedation
  71. Promethazine
    • First-generation antihistamine
    • Causes sedation
  72. Loratadine
    • Second-generation antihistamine
    • Low sedation, due to high H1 specificity
  73. Cetirizine
    • Second-generation antihistamine
    • Low sedation, due to high H1 specificity
  74. Fexofenadine
    • Second-generation antihistamine
    • Low sedation, due to high H1 specificity

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