Exam 1 Drugs Compilation Flashcards

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1
Q

Cimetidine

A

Imidazole
Inhibitor of CYP enzymes (Phase 1), competitive inhibitor of OCT
n/a for now
Decrease metabolism / increase drug level

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2
Q

Phenobarbital

A

Barbiturate
Activator of CYP enzymes (Phase 1)
n/a for now
Increase metabolism, decrease drug level

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3
Q

Probenecid

A

n/a
competitive inhibitor of OAT
n/a
Decreases secretion of anions

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4
Q

Ethanol

A

n/a
Activator of CYP enzymes
Increase metabolism, decrease drug level

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5
Q

Proadifen

A

n/a
Only known role is as inhibitor of CYPs
Decrease metabolism / increase drug level

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6
Q

Bethanechol

A
Muscarinic Receptor Agonist 
Muscarinic receptor selective
Long acting 
Used to stimulate smooth muscle post-op
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
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7
Q

Carbachol

A

Muscarinic Receptor Agonist
Long acting
Corneal Application for Wide Angle Glaucoma (Increase drainage)
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)

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8
Q

Methacholine

A

Muscarinic Receptor Agonist
Muscarinic receptor selective
Used to test muscarinic receptor function, slow HR and test bronchial hyperactivity
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)

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9
Q

Muscarine

A

Muscarinic Receptor Agonist
Muscarinic Receptor selective
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)

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10
Q

Pilocarpine

A

Muscarinic Receptor Agonist (Natural Alkaloid)
Corneal Application for Wide Angle Glaucoma (increase drainage)
Muscarinic Receptor selective, sweat glands sensitive
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)

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11
Q

Nicotine

A

Nicotinic Receptor Agonist
Competitive Nicotinic Receptor Agonist
Can cause Autonomic hyperactivity (convulsions, coma, death, respiratory arrest)

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12
Q

Varenicline

A

Nicotinic Receptor Agonist
Agonist
Used to quit smoking

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13
Q

Ambemonium

A

Competitive AChE inhibitor
Used to treat myasthenia gravis
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)

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14
Q

Edrophonium

A

Quaternary Simple Alcohol
Competitive AChE inhibitor
Used to diagnose Myesthenia Gravis
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)

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15
Q

Neostigmine

A

Carbamate
Competitive AChE inhibitor
Increases smooth muscle motility, treat paralytic ileus and atony of bladder, treatment and diagnosis of myasthenia gravis, reversal of neuromuscular block
** Used to compete off N2 receptor blockers **
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)

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16
Q

Physostigmine

A

Carbamate
Competitive AChE inhibitor
Topical treatment for wide angle glaucoma
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)

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17
Q

Pyridostigmine

A

Carbamate
Competitive AChE inhibitor
Treatment of myesthenia gravis, pretreatment for nerve gas exposure, reversal of neuromuscular blockade
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)

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18
Q

diisopropylfluorophosphate

A

Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD

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19
Q

echothiophate

A

Organophosphate Derivative
Non - Competitive AChE inhibitor
Treatment of glaucoma
SLUD

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20
Q

Carbaryl

A

Insecticide Carbaryl
Non - Competitive AChE inhibitor
No clinical use
SLUD

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21
Q

Malathion

A

Insecticide Organophosphate Derivative
Non - Competitive AChE inhibitor
Least toxic – used for head lice
SLUD

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22
Q

Parathion

A

Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD

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23
Q

Tetraethylpyrophosphate

A

Insecticide Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD

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24
Q

Sarin

A

Nerve Gas - Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD

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25
Q

Soman

A

Nerve Gas - Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD

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26
Q

Pralidoxime

A

AchE reactivator
Releases phosphoryl moiety to restore AChE activity
Needs to be admin with Atropine, before Aging

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27
Q

Atropine

A

Muscarinic (selective) Antagonist (Long lasting)
Treatment of insecticide poisoning, anti-parkinson, cause mydriasis and cycloplegia, anti-motion sickness, decreased bronchial secretions, slow smooth muscle, Increase HR, Preanesthetic
Can cause hallucinations and amnesia
Atropine fever, dry mouth

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28
Q

Homatropine

A

Muscarinic antagonist (Intermediate lasting)
Used to cause mydriasis and cycloplegia
Can cause hallucinations and amnesia, dry mouth, sedation / excitement

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29
Q

Scopolamine

A

Muscarinic antagonist
Anti-motion sickness, Amnesia before surgery
Can cause hallucinations and amnesia, dry mouth, sedation / excitement

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30
Q

Methscopolamine

A

Muscarinic antagonist

Slow GI tract

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31
Q

Trihexyphenidyl

A

Muscarinic antagonist
Antiparkinson therapy, reduce uncoord. Movt.
Can cause hallucinations and amnesia, dry mouth, sedation / excitement

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32
Q

Tropicamide

A
Muscarinic antagonist (Short acting)
Used to cause mydriasis and cycloplegia
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33
Q

Cyclopentolate

A

Muscarinic antagonist

Used to cause mydriasis and cycloplegia

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34
Q

Ipratropium

A

Muscarinic antagonist (Quaternary)
Bronchodilation, Decreased bronchial secretions,
Shorter acting for COPD

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35
Q

Tiotropium

A

Muscarinic antagonist (Quaternary)
Bronchodilation, Decreased bronchial secretions
Longer acting for COPD

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36
Q

Darifenacin

A

Muscarinic antagonist (M3 Specific)
Slow Smooth muscle, over active bladder (GI / Genitourinary)
Longer Duration of action

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37
Q

Solifenacin

A

Muscarinic antagonist (M3 Specific)
Slow Smooth muscle, over active bladder (GI / Genitourinary)
Longer Duration of action

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38
Q

Tolterodine

A

Muscarinic antagonist (M3 Specific)
Slow Smooth muscle, over active bladder (GI / Genitourinary)
Longer Duration of action

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39
Q

Mecamylamine

A

Ganglionic Blocker
Non-depolarizing competitive antagonist
Good GI absorption
Adjunct for peripheral vascular disease – relieve vasoconstriction and increase perfusion
CNS side effects including tremors, confusion, seizures, mania, depression

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40
Q

Trimethaphan

A

Ganglionic Blocker
Non-depolarizing competitive antagonist
Used IV in OR to decrease BP to control bleeding, adjunct anti-hypotensive

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41
Q

Succinylcholine

A

Non-Competitive Nicotinic N2 blocker
Depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
Hydrolyzed by plasma cholinesterase

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42
Q

Curare (t-tubocurarine)

A

benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Long acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine

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43
Q

Atracurium

A

benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Intermediate acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine

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44
Q

Cisatracurium

A

benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Intermediate acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine

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45
Q

Mivacurium

A

benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Short acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine

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46
Q

Pancuronium

A

Ammonio Steroids
Competitive Nicotinic N2 blocker
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Long acting *
Cross react with Muscarinic and N1 – Tachycardia
Reversed by edrophonium, neostigmine

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47
Q

Vecuronium

A

Ammonio Steroids
Competitive Nicotinic N2 blocker
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Intermediate acting *
Cross react with Muscarinic and N1 – Tachycardia
Reversed by edrophonium, neostigmine

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48
Q

Metaraminol

A

Alpha-1 Selective Agonist
Long acting beta 1 and alpha 1 stimulant
Displaces NE

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49
Q

Methoxamine

A

Alpha-1 Selective Agonist (less alpha 2)

treat hypotensive crisis

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50
Q

Phenylephrine

A

Alpha-1 Selective Agonist (less alpha 2)
Vasoconstriction, prevent shock, nasal decongestant, treat hypotensive crisis, reduce drug diffusion, reduce mucus membrane congestion, mydriasis
Long acting

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51
Q

Alpha methyldopa

A

Alpha-2 Selective Agonist
Decrease NT in synapse – replaces DOPA in synthetic pathway to yield Alpha-methyl norepinephrine (false neurotransmitter)
Used to treat hypertension – acts at brainstem vasomotor center
Side effects diminish over time – sedation, xerostomia, anorexia, fluid retention, vivid dreams, impotence, CNS stimulation

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52
Q

Clonidine

A

Alpha-2 Selective Agonist (less alpha 1)
Decrease NT in synapse (inhibit NE release)
Side effects diminish over time – sedation, xerostomia, anorexia, fluid retention, vivid dreams, CNS stimulation

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53
Q

Guanabenz

A

Alpha-2 Selective Agonist
Decrease NT in synapse (inhibit NE release)
Side effects diminish over time – sedation, xerostomia, anorexia, fluid retention, vivid dreams, CNS stimulation

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54
Q

Amphetamine

A
Alpha and beta adrenergic agonist
Releasing agent (increases NE release), also releases intraneuronal NE – reverse transport
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55
Q

Ephedrine

A

Alpha and beta adrenergic agonist
Releasing agent, Stimulant of most adrenergic receptors
Increase CO and arterial pressure, treat orthostatic hypotension, reduce mucus membrane congestion, stress incontinence
Long acting – Displaces NE

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56
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

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57
Q

Norepinephrine

A

Alpha and beta adrenergic agonist (except beta 2)
IV infusion for shock, increase CO and cause vasoconstriction (increase BP, treat hypotensive crisis), reduce drug diffusion
Binds Beta-2 a lot less than all other adrenergics

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58
Q

Dobutamine

A

Beta 1 Selective agonist (Less beta-2)

Cardiogenic shock, heart failure

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59
Q

Isoproterenol

A

Beta 1 and 2 agonist

Used for relaxation of bronchial smooth muscle, also cardiac stimulation (potent vasodilator)

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60
Q

Albuterol

A

Beta 2 Selective agonist (Less beta-1)

Bronchial asthma

61
Q

Metaproterenol

A

Beta 2 Selective agonist (Less beta-1)

Bronchial asthma

62
Q

Terbutaline

A

Beta 2 Selective agonist (Less beta-1)

Bronchial asthma, relax pregnant uterus

63
Q

Bromocriptine

A

Dopamine Agonist
Anti-parkinson agent (for its CNS effects)
Side effects – postural hypotension and cardiac arrhythmia

64
Q

Dopamine

A

Dopamine Agonist
IV for shock, vasoconstriction, increase CO and dilate renal arteries
Binds Alpha and Beta 1 at high concentrations
Enhance NE release (displaces it)

65
Q

Fenoldopam

A

Dopamine Agonist, DA-1 selective

Vasodilation of renal and mesenteric vessels

66
Q

Doxazosin

A

Alpha-1 Selective antagonist

Urinary obstruction from BPH

67
Q

Prazosin

A

Alpha-1 Selective antagonist (Highly selective)
Antihypertensive (mild / moderate), urinary obstruction from BPH
Little to no tachycardia because doesn’t bind beta receptors
Oral admin

68
Q

Tamsulosin

A

Alpha-1 Selective antagonist

Urinary obstruction from BPH

69
Q

Terazosin

A

Alpha-1 Selective antagonist

Urinary obstruction from BPH

70
Q

Phenoxybenzamine

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

71
Q

Phentolamine

A

Alpha-1 and Alpha-2 Selective antagonist
Competitive antagonist
Dirty drug, binds histamine and muscarinic receptors
Diagnostic for pheochromocytoma, also for its assoc. hypertension
Increases NE release, will cause tachycardia and increased CO

72
Q

Labetalol

A

Alpha and beta antagonist (more beta though)

73
Q

Atenolol

A

Beta-1 Selective antagonist
Antihypertensive, inhibit cardiac output
** better, but still careful with asthma / COPD patients **
Doesn’t cross CNS well

74
Q

Betaxolol

A

Beta-1 Selective antagonist
Major use – glaucoma
(antihypertensive, inhibit cardiac output – if it gets there)
** better, but still careful with asthma / COPD patients **

75
Q

Metoprolol

A

Beta-1 Selective antagonist
Antihypertensive, angina pectoris, inhibit cardiac output
Prevent recurrence of MI
** better, but still careful with asthma / COPD patients **
Side effect – Ataxia and dizziness

76
Q

Nadolol

A
Beta-1 and beta-2 Selective antagonist
Very long acting, antihypertensive
Prevent recurrence of MI 
**Careful with asthma and COPD patients **
Doesn’t cross CNS well
77
Q

Pindolol

A

Beta-1 and beta-2 Selective antagonist
Antihypertensive
Prevent recurrence of MI
**Careful with asthma and COPD patients **

78
Q

Propranolol

A

Beta-1 and beta-2 Selective antagonist
Antihypertensive, anti arrhythmic, anti-migraine, for angina pectoris
Prevent recurrence of MI
**Careful with asthma and COPD patients **
Side effect – Ataxia and dizziness

79
Q

Timolol

A

Beta-1 and beta-2 Selective antagonist
Lower intraocular pressure, Antihypertensive, angina pectoris
Prevent recurrence of MI
**Careful with asthma and COPD patients **

80
Q

Guanethidine

A

Synaptic vesicle depleting agent / membrane stabilizer
Used for only the most severe cases of hypertension
Enters neurons via amine 1 transporter (drugs that interfere will block its actions)
Minimal CNS effects – doesn’t cross BBB

81
Q

Reserpine

A

Synaptic vesicle depleting agent
Blocks transport of NE into the vesicle, reduces amount released
Long duration of action
Side effects – Sedation, depression, Parkinsonism, increased GI motility (ulcers)

82
Q

Cocaine

A

Amine 1 transport inhibitor
No clinical use – vasoconstriction, mydriasis and tachycardia
Interferes with reserpine (Amine 1 transporter)

83
Q

DMI - desmethylimipramine

A

Tricyclic antidepressant
Amine 1 transport inhibitor
Increases NT in synapse

84
Q

Tyramine

A
Releasing Agent (Displaces NE)
Enhance NE release via Amine 1 transporter
85
Q

Pseudoephedrine

A

Releasing Agent

Reduces congestion of mucus membranes

86
Q

Dipivefrin

A

Alpha and beta blocker

Used for eye, metabolized to epinephrine

87
Q

Apraclonidine

A

Alpha 2 selective agonist

88
Q

Carteolol

A

Beta 1 and 2 antagonist

Reduce aqueous humor production in eye

89
Q

Levobunolol

A

Beta 1 and 2 antagonist

Reduce aqueous humor production in eye

90
Q

Metipranolol

A

Beta 1 and 2 antagonist

Reduce aqueous humor production in eye

91
Q

Acetazolamide

A

Carbonic Anhydrase inhibitor

Reduce aqueous humor production in eye (via reducing HCO3 production)

92
Q

Dichlorphenamide

A

Carbonic Anhydrase Inhibitor

Reduce aqueous humor production in eye (via reducing HCO3 production)

93
Q

Dorzolamide

A

Carbonic Anhydrase Inhibitor

Reduce aqueous humor production in eye (via reducing HCO3 production)

94
Q

Botulinum toxin A

A

Muscle Relaxant

Long term – Inhibits NT release by destroying presynaptic SNAP25

95
Q

Azathioprine

A
  • General Growth Inhibitors
  • ## Metabolized to 6-mercaptopurine then 6 thioguanine (blocks purine synthesis). Also incorporates into DNA
  • Inactivated by xanthine oxidase
  • ## Myelosuppression, nausea, vomiting
  • Used for renal and other tissue transplantation, autoimmune disease
96
Q

Cyclophosphamide

A

-General Growth Inhibitors
-Cross links DNA, kills all proliferating cells
-
-
- Myelosuppression, nausea, vomiting,
- Infertility
- Used for autoimmune diseases, bone marrow transplant

97
Q

Leflunomide

A
  • General Growth Inhibitors
  • ## Decreases pyrimidine synthesis-
  • ## Diarrhea, modest hepatotoxicity, reduced myelosuppresion
  • Used for Rheumatoid arthritis, some autoimmune disease
98
Q

Methotrexate

A

-General Growth Inhibitors
- Inhibits dihydrofolate reductase, prevents thymidide and purine synthesis
-
-
- Causes nausea, mucosal ulcers, modest hepatotoxicity, reduced myelosuppression
-
- Rheumatoid arthritis, some autoimmune disease

99
Q

Mycophenolate Mofetil

A

-General Growth Inhibitors
- Prevents Purine synthesis
-
-
- Myelosuppression, nausea, vomiting
-
- Used for solid organ transplant (cyclosporine alternative) autoimmune disease

100
Q

Prednisone

A

-Glucocorticoid
-Upregulates / Downregulates expression of genes assoc. with inflammation and immunosuppression (e.g. IL2 and IFN-gamma)
- No serious bone marrow toxicity
-
-
- Cushings syndrome, osteoporosis, glucose intolerance, hypertension, susceptibility to infection
- Used for solid organ transplantation (first line), stem cell transplantation, autoimmune diseases, asthma, allergic reactions, systemic inflammation

101
Q

Sirolimus

A
  • mTOR inhibitor
  • ## Binds FKBP12 to form complex that inhibits IL2 activation
  • Antagonizes tacrolimus, synergistic with cyclosporine
  • Myelosuppression, hyperlipidemia, hypertension, edema, hepatotoxicity
  • Solid organ transplants, steroid resistant graft v. host disease
102
Q

Cyclosporin

A
  • Calcineurin inhibitor
  • ## Binds Cyclophilin to form complex that inhibits NFAT activation
  • Often combined with other immunosuppressant agents
  • Nephrotoxicity, hypertension, hyperglycemia, liver dysfunction.
  • Increased cancer incidence documented
  • Kidney, liver and cardiac transplants, inflammatory diseases (asthma)
103
Q

Tacrolimus

A
  • Calcineurin inhibitor
  • ## Binds FKBP12 to form complex that inhibits NFAT activation
  • 10-100 X more potent than cyclosporine
  • Nephrotoxicity, hypertension, hyperglycemia, liver dysfunction.
  • Increased cancer incidence documented
  • Kidney, liver and cardiac transplants, inflammatory diseases (asthma)
104
Q

Anti-T cell globulin

A
  • Antibody / Fusion Protein
  • Blocks T cell surface receptors and opsonizes T cells
  • Product of repeated injection of human T cells into animals
  • Cytokine release syndrome (reduce w/ pretreat. With acetaminophen and antihistamine, serum sickness
  • Anaphylaxis potential (with repeat use)
  • Prevent maternal (Rh-) from attacking fetus
105
Q

Alemtuzumab

A
  • Antibody / Fusion Protein
  • Depletes cells expressing CD25 (T and B cells, monocytes, macrophages, NK cells)
  • Prolonged depletion (1 yr) of T cells and other immunecells
  • Myelosuppresion, flu like symptoms
  • -
106
Q

Basiliximab (Anti CD25)

A
  • Antibody / Fusion Protein
  • Blocks and opsonizes alpha chain of IL-2 (CD25), found only on activated T cells
  • Depletes only antigen activated T cell , reduced incidence of infection and malignancy
  • Moderate effect relative to anti-T cell globulin
  • Well tolerated
  • -
107
Q

Rh(D) immune globulin

A
  • Antibody / Fusion Protein
  • ## Binds and clears up D-antigen, prevents mother’s immune rxn
  • Prevent maternal (Rh-) from attacking fetus
108
Q

Belatacept

A
  • Antibody / Fusion Protein
  • ## Binds and clears up D-antigen, prevents mother’s immune rxn
  • Comparable to calcineurin inhibitors in preventing transplant rejection
  • Anemia, neutropenia, peripheral edema
  • Increased risk of infection and malignancy, especially post-transplant lymphoproliferative disorder
  • Use for kidney transplant
109
Q

Interleukin-2

A
  • Cytokines
  • ## Increases proliferation of activated T cells, increases IFN-gamma and cytotoxic killer cell activity
  • Capillary leak syndrome, hypotension, reduced organ perfusion, can be fatal
  • Used to treat metastatic melanoma, renal cell carcinoma
110
Q

IFN-gamma

A
  • Cytokines
  • ## Stimulates activity of cytotoxic cells-
    -
    -
  • Severe recurrent infections
111
Q

BCG

A

-Adjuvant
- Increases APC activity by binding pattern recognition receptors
- Live attenuated bacillus calmette-guerin
- Can’t use systemically, will cause septic shock
-
-
- Used topically for bladder cancer

112
Q

Cetirizine

A
  • H1 antihistamines
  • Second generation antihistamine
  • Poor CNS Penetration
  • ## Increased selectivity at H1 receptors-
  • Antihistamine
113
Q

Cyclizine

A

H1 antihistamines
- First generation antihistamine
-CNS permeable
- Non-specific effects at adrenoreceptors, muscarinics, serotonin and sodium channels
- Drowsiness
-
- Anti-histamine (allergy, uticaria), motion sickness

114
Q

Dimenhydrinate

A

H1 antihistamines
- First generation antihistamine
- CNS permeable
-Non-specific effects at adrenoreceptors, muscarinics, serotonin and sodium channels
- Drowsiness
-
-Anti-histamine (allergy, uticaria), motion sickness

115
Q

Diphenhydramine

A

H1 antihistamines
- First generation antihistamine
- CNS permeable
- Non-specific effects at adrenoreceptors, muscarinics, serotonin and sodium channels
- Drowsiness
-
- Anti-histamine (allergy, uticaria), motion sickness

116
Q

Fexofenadine

A
  • H1 antihistamines
  • Second generation antihistamine
  • Poor CNS Penetration
  • ## Increased selectivity at H1 receptors-
  • Antihistamine
117
Q

Loratidine

A
  • H1 antihistamines
  • Second generation antihistamine
  • Poor CNS Penetration
  • ## Increased selectivity at H1 receptors-
  • Antihistamine
118
Q

Promethazine

A

H1 antihistamines
- First generation antihistamine
- CNS permeable
- Non-specific effects at adrenoreceptors, muscarinics, serotonin and sodium channels
- Drowsiness
-
- Anti-histamine (allergy, uticaria), antiemetic

119
Q

Adalimumab

A
  • anti-TNFalpha agent
  • Binds to TNFalpha, prevents it from binding to its receptor and reduces circulating levels
  • Human antibody to TNFalpha
  • Parenteral administration required
  • increased frequency of infections (upper
    respiratory, urinary)
    -
    -Rheumatoid arthritis, Crohn’s
120
Q

Etanercept

A
  • anti-TNFalpha agent
  • Binds to TNFalpha, prevents it from binding to its receptor and reduces circulating levels
  • Fusion protein containing the ligand binding domain of the
    TNFalpha receptor and the Fc domain of human IgG.
  • Parenteral administration required
  • increased frequency of infections (upper
    respiratory, urinary)
    -
    -Rheumatoid arthritis, Crohn’s
121
Q

Infliximab

A
anti-TNFalpha agent
- Binds to TNFalpha, prevents it from binding to its receptor and reduces circulating levels
- Humanized antibody to TNFalpha
- Parenteral administration required
- increased frequency of infections (upper
respiratory, urinary)
-
-Rheumatoid arthritis, Crohn's
122
Q

Anakinra

A
  • Anti-IL1 agent
  • ## Competitive IL-1 receptor antagonist (IL-1Ra analog)
  • Short half-life, daily injection required
    Increased susceptibility to infection
    -
  • Rheumatoid Arthritis, possibly other inflammatory diseases
123
Q

Tofacitinib

A
  • Jak kinase inhibitor
  • Inhibits all activity of cytokines required for adaptive immunity (eg., IL-2, IL-4, etc.) and inhibits all activities for many inflammatory cytokines (eg., IL-6)
    Distinguishing Chem Characteristics (Unique or “weird” features)
  • oral administration; therapeutic doses chosen to produce incomplete Jak inhibition, because higher doses expected to produce potent
    immunosuppression AND adverse effects.
  • ## Anemia, neutropenia, general myelosuppression, increased risk of infection (especially Herpes Zoster)
  • RA: Currently second line therapy for those failing methotrexate
124
Q

Aspirin

A

Nonselective COX inhibitor
- Irreversible Acetylation of COX enzymes
- Long lasting block
-
-
-Increased bleeding, gastric ulcers, salicylism, Reye’s syndrome, dyspepsia, renal issues
- OTC analgesic / antipyretic, cardiovascular prophylaxis

125
Q

Diclofenac

A
Nonselective COX inhibitor
- Reversible inhibition of COX
-
- Selectivity for COX 2 over COX 1 
-
- Increased bleeding, gastric ulcers, dyspepsia, renal issues, CV events
- RX for arthritis, anti-inflammatory
126
Q

Diclofenac with misoprostol

A
Nonselective COX inhibitor
- Reversible inhibition of COX
-
- Selectivity for COX 2 over COX 1 
- Misoprostol should help GI symptoms 
- Increased bleeding, gastric ulcers, dyspepsia, renal issues, CV events
- RX for arthritis, anti-inflammatory
127
Q

Ibuprofen

A
Nonselective COX inhibitor 
- Reversible inhibition of COX
-
-
-Increased bleeding, gastric ulcers. dyspepsia, renal issues, CV events
- 
-  OTC analgesic, antipyretic,
128
Q

Indomethacin

A

Nonselective COX inhibitor
- Reversible inhibition of COX
-
- Increased inhibition of COX 1 over COX 2
-
- High incidence of GI problems leading to intolerance
- RX for arthritis, anti inflammatory

129
Q

Ketorolac

A
Nonselective COX inhibitor 
- Reversible inhibition of COX
-
- Increased inhibition of COX 1 over COX 2 
-
-
-Post surgical analgesic
130
Q

Naproxen

A

Nonselective COX inhibitor
- Reversible inhibition of COX
-
-
-Increased bleeding, gastric ulcers, dyspepsia, renal issues, CV events
-
- OTC analgesic, antipyretic, RX anti-inflammatory

131
Q

Acetaminophen

A
Nonselective COX inhibitor 
-
-
-
-hepatotoxicity with overdose
-
-
132
Q

Celecoxib

A
Cox-2 selective inhibitor 
-
-
-
-Renal toxicity, increased risk of cardiovascular events
-
-
133
Q

Rofecoxib

A
Cox-2 selective inhibitor 
-
-
-
-Renal toxicity, increased risk of cardiovascular events 
-
-
134
Q

Albuterol

A

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

135
Q

Salmeterol

A

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

136
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

137
Q

Beclomethasome

A

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

138
Q

Budenoside

A

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

139
Q

Fluticasome

A

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

140
Q

Prednisone

A

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

141
Q

Triamcinolone

A

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

142
Q

Montelukast

A

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

143
Q

Zafirlukast

A

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

144
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

145
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
146
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
147
Q

Ipratropium

A
-muscarinic cholinergic antagonist
-
-quaternary ammonium
-shorter DOA, topical inhalant 
-tachycardia, decreased salivation
-bronchodilation and min. mucociliary clearance problems
148
Q

Theophylline

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