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Pharmacology > Pharmacology - Block 2 > Flashcards

Pharmacology - Block 2 Flashcards

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1
Q

Serotonin synthesis

A

Tryptophan - tryptophan hydroxylase (rate limiting, except in CNS) (need O2 and pteridine cofactor) -> 5-hydroxytryptophan - L-aromatic amino acid decarboxylase (needs pyridoxine cofactor) -> Serotonin (5HT)
- (in pineal gland)-> Melatonin

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2
Q

Serotonin metabolism

A 
Monoamine Oxidase (MAO)
SERT = high affinity reuptake
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3
Q

5-HT1 receptors

A

Gi - inhibits AC, opens K+ channels

A,B,D,E

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4
Q

5-HT2 receptors

A

Gq - PLC -> PIP3->GAP,IP3

A,B,C

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5
Q

5-HT 4,5,6,7

A

Gs - activate AC

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6
Q

5-HT3 receptors

A

Ligand gated cation channel

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7
Q

Serotonin auto-receptors

A

decrease serotonin release

1A and 1D like

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8
Q

Serotonin -> GI

A

slow turnover (1 day)
causes contraction of GI smooth muscle
5-HT3 -> vomiting
carcinoid syndrome = serotonin secreting tumor -> also can get vitamin deficiency bc depletes tryptophan

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9
Q

Serotonin -> CV

A

Vasoconstriction or dilation depending
large arteries + cranial vessels = vasoconstrict (5HT2 on smooth muscle cells, 5HT1D in brain, also indirect by NE displacement)
Arterioles, coronaries, skeletal m = vasodilation
Bezold-Jarisch reflex = serotonin- chemoreceptors in coronaries -> vagal nerve endings -> bradycardia, hypotension, hypoventilation

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10
Q

Serotonin -> CNS

A

Neurotransmitter -> midbrain raphe nucleus

sensory perception, sleep, temp, endocrine, pain, drug abuse, emesis, mental illness

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11
Q

Serotonin-related mental illness

A 
affective disorders - SSRI, SNRI
schizophrenia - atypical anti-psychotics
OCD - SSRI
anxiety - 5-HT1A
aggressive behavior
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12
Q

Lysergic Acid Diethylamide

A

LSD - hallucinogen

5HT2 agonist

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13
Q

Buspirone

A

5HT1A partial agonist

anti-anxiety

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14
Q

Sumatriptan

A

5HT1D agonist
anti-migraine (stop existing headache)
side effects = nausea, vomiting, dizziness

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15
Q

Fluoxetine

A

“Prozac”
SSRI
used for affective disorders, OCD, panic, etc
side effects = sex dysfunction, nausea, etc

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16
Q

Phenelzine

A 
MAO inhibitor
Blocks metabolism of serotonin, NE, DA
Used for depression, narcolepsy
Last ditch effort
side effects = food induced hypertensive crisis
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17
Q

Cyproheptadine

A

5HT2 antagonist
Also Histamine H1 antagonist
treats skin allergies, carcinoid

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18
Q

Ondansetron

A

5HT3 antagonist
treats chemotherapy induced nausea
acts on GI and brain receptors

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19
Q

Alosetron

A

5HT3 antagonist
last ditch treatment for women with diarrhea IBS
has GI side effects

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20
Q

Histamine synthesis

A

L-histidine - histidine decarboxylase (inducible) (uses pyridoxal-5-P cofactor)-> Histamine (inhibited by methyl-histidine)

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21
Q

Histamine pools

A 
Mast cells (tissue) and basophils (blood) - slow turnover, stored in secretory granules with heparin sulfate and ATP
Non-Mast cell stores - rapid turnover, no granules, continuous release
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22
Q

Release of histamine

A

w/i seconds = burning, itching, up HR, down BP
w/i minutes = BP recovers, hives on skin
antigen-antibody reaction
drugs, venoms, etc can cause release
Vancomycin-induced ‘red-man’ syndrome
mechanism = increase intracellular Ca in mast cells

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23
Q

Cromolyn sodium

A

Inhibit histamine release
stabilizes mast cell membranes
inhaled
used for asthma, allergies

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24
Q

Omalizumab

A 
inhibit histamine release
monoclonal antibody decreases antigen specific IgE that binds to mast cells
subcutaneous
can cause life-threatening anaphylaxis
used to treat extreme allergic asthma
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25
H1 receptor
Gq | smooth muscle, endothelial cells, CNS
26
H2 receptor
Gs | gastric parietal cells, cardiac muscle, mast cells, CNS
27
Histamine -> CV
Overall decrease BP vasodilation endothelial cells - H1 -> NO smooth muscle - H2 -> cAMP can vasoconstrict large vessels (H1) Increase vascular permeability - H1 on venules -> endothelial cells contract, expose basement membrane increase contractility, electricals in heart (H2)
28
Histamine -> pulmonary, GI, Neuro
``` Bronchioles - contract (H1) intestinal smooth muscle - contract (H1) GI secretion - increase (H2) Nerve endings - pain (H1) Triple Response of Lewis = red line, red flare, wheal H1= arousal H2= decrease apetite ```
29
Diphenhydramine
1st gen H1 blocker Benadryl, profound sedation used for allergies, motion sickness, Parkinsons
30
Dimenhydrinate
1st gen H1 blocker Dramamine used for motion sickness and vestibular disturbance
31
Chlorpheniramine
1st gen H1 blocker | used for allergies, potent, some sedation
32
Promethazine
1st gen H1 blocker also blocks dopamine Phenergan used for motion sickness and anti-nausea
33
Fexofenadine
2nd gen H1 blocker | Allegra
34
Loratadine
2nd gen H1 blocker | Claritin
35
Desloratadine
2nd gen H1 blocker | Clarinex
36
Cetirizine
2nd gen H1 blocker | Zyrtec
37
1st vs 2nd generation H1 blockers
1st: have sedative and anticholinergic side effects / CNS depression is common, some can be used to treat motion sickness bc anticholinergic 2nd: no anticholinergic or sedative effects, do not cross BBB into CNS / usually metabolized by liver P450s
38
Cimetidine
H2 receptor blocker used for gastric upset / peptic ulcers Inhibits P450 enzymes Tagamet (least potent)
39
Ranitidine
H2 receptor blocker used for gastric upset / peptic ulcers Zantac
40
Famotidine
H2 receptor blocker used for gastric upset / peptic ulcers Pepcid (most potent)
41
Effects of inflammation
vasodilation, increased vessel permeability, pain | harmful: inflammatory cells release lysosomal enzymes, swelling can cause death, obstruction
42
Bradykinin
source: endothelial cells | vasodilation, velles permeability, pain
43
Complement system
Synthesized in liver, circulates in blood | chemotaxis, vascular permeability, promote mediator release from neutrophil
44
C-reactive protein
produced in liver in response to cytokines acute phase reactant activates complement / phagocytosis
45
Cytokines
Source: all inflammatory cells TNFa: acute phase rxn, fever IL-1: acute phase rxn, fibroblast and lymphocyte proliferation, fever (increase COX and lipoxygenases) increase adhesion molecules and collagenase
46
Etanercept
TNFa blocker not orally active, risk of infection used for rheumatoid arthritis
47
Infliximab
TNFa blocker not orally active, risk of infection used for rheumatoid arthritis
48
Adenosine
source: all cells anti-inflammatory inhibits cytokines
49
Cell adhesion molecules
Source: endothelial cells, platelets, leukocytes important for host defense, tissue repair, and recruiting platelets Ca dependent
50
Zileuton
5-lipoxigenase inhibitor (5-LOX) inhibits leukotriene synthesis oral, CYP metabolized use for prophylactic treatment of mild asthma
51
Zafirlukast
cys-leukotriene receptor antagonist oral, CYP metabolized use for prophylactic treatment of mild asthma
52
Glucocorticoids
Source: adrenal cortex anti-inflammatory inhibit cytokines, PLA2, COX2, cell adhesion molecules nuclear receptors
53
Aspirin
NSAID | inhibits COX
54
Synthesis of eicosanoids
phospholipids - PLA2 -> Arachidonic acid (Ca dependent) - - LOXs-> leukotrienes, lipoxins - - COXs-> prostaglandins RAPID inactivation
55
COXs
``` COX1: constitutive COX2: inducible (important) 1. oxygenates to form PGG2 2. peroxidase to PGH2 PGH2 -> PGI2, TXA2, PGE2, PGF2 ```
56
Lipoxygenases
5-LOX -> leukotrienes | requires Ca and FLAP
57
Eicosanoids -> pain
PGE2, PGI2 -> hyperalgesia
58
Eicosanoids -> fever
cytokines-> PGE2->cAMP->fever
59
Eicosanoids -> platelets
TXA2 -> platelet aggregation | PGI2 -> inhibits platelet aggregation
60
Eicosanoids -> uterus
PGI2 = early pregnancy PGE2: labor, ripening PGF2: labor, contractility (also dysmenorrhea)
61
Eicosanoids -> CV
``` Prostaglandins-> usually decrease BP PGE, PGI2 -> vasodilators TXA2, PGF2: vasoconstrictor mostly local effects PGE2 -> ductus arteriosis ```
62
Eicosanoids -> bronchial
primarily bronchoconstrictor response to leukotrienes
63
Eicosanoids -> kidney
PGE2, PGI2 -> increase renal blood flow
64
Eicosanoids -> GI
Generally cytoprotective PGE2 mostly decrease gastric acid, increase mucus, etc
65
Eicosanoids -> immune
LTC4, LTD4 -> increase vascular permeability | LTB4 -> attracts neutrophils
66
Dinoprostone
``` PGE2 analog used for cervical ripening (gel) EP4 - also relaxes cervial muscle can use for abortion at high doses EP1/3 ```
67
Misoprostol
PGE1 analog used for ulcer prevention with long-term NSAID use EP3 in parietal cells -> less gastric acid
68
Alprostadil
``` PGE1 use for erectile dysfunction (injection) EP2/4 Also used for patent ductus arteriosis (IV) EP2/4 ```
69
Epoprostenol
PGI2 used for pulmonary hypertension IV, IP receptor
70
Bimatoprost
PGF2 used for glaucoma and eyelash hypotrichosis ophthalmic soln EP2/4
71
Acetylsalicylic adic
``` Aspirin NSAID IRREVERSIBLE COX inhibitor quickly metabolized to salicylic acid high dose can saturate conjugation -> toxicity Low dose: decrease uric acid excretion high dose: increase uric acid excretion Overdose: delirium, up respirations, nausea Reye's syndrome in kids ```
72
NSAID side effects
GI (major): gastric ulcers/bleeding blood: increased bleeding (platelets) hypersensitivity: due to shunting toward lipoxygenase->leukotrienes Renal: decrease RBF Pregnancy: Contraindicated (decrease contractions, ductus arteriosis
73
Ibuprofen
NSAID | used as usual, also for patent ductus arteriosis
74
Naproxen
NSAID longer half life used for usuals plus arthritis, dysmenorrhea, etc
75
Indomethacin
NSAID | Used for acute gouty arthritis, other arthritis, not usually pain/fever
76
Ketorolac
NSAID | analgesic and anti-pyretic, not anti-inflammatory
77
Nabumetone
``` NSAID COX2>Cox1 prodrug anti-inflammatory and analgesic less side effects ```
78
Piroxicam
NSAID long half life usual uses
79
Sulfasalazine
used to treat active ulcerative colitis, and arthritis | local GI effects to inhibit inflammation
80
Celecoxib
COX2 selective NSAID Contains sulfa moity metabolized by P450s has usual NSAID side effects and usage
81
Acetaminophen
Tylenol mechanism not known Metabolized by P450s, toxicity effects analgesic and anti-pyretic, not anti-inflammatory OD treatment: N-acetylcysteine to replace glutathione
82
Nitroglycerin
NO donor venous dominant vasodilator (but both) use in heart failure
83
Nitroprusside
Similar to nitroglycerin
84
Hydralazine
increase cGMP arterial dominant vasodilator used in heart failure
85
Minoxidil
K channel opener arterial dominant vasodilator used in heart failure and hypertension
86
Diazoxide
K channel activator | used in hypertension
87
Verapamil
``` Phenylalkylam Ca channel blocker arterial dominant vasodilator reduce afterload cardiac cell dominant used for arrhythmias substancial first-pass effect ```
88
Diltiazem
``` Benzothiazapine Ca channel blocker arterial dominant vasodilator reduce afterload cardiac cell dominant used for arrhythmias and angina ```
89
Milrinone
PDE3 inhibitor cAMP-PDE3->AMP in Cardiac m: cAMP causes contraction (P Ca channels and myofilaments, also P K channels to increase rate) in Vascular SM: cAMP causes relaxation (inhibits MLC-Kinase and P K channels) used in heart failure
90
Inamrinone
PDE3 inhibitor cAMP-PDE3->AMP in Cardiac m: cAMP causes contraction (P Ca channels and myofilaments, also P K channels to increase rate) in Vascular SM: cAMP causes relaxation (inhibits MLC-Kinase and P K channels) used in heart failure
91
Cilostazol
PDE3 inhibitor cAMP-PDE3->AMP in Cardiac m: cAMP causes contraction (P Ca channels and myofilaments, also P K channels to increase rate) in Vascular SM: cAMP causes relaxation (inhibits MLC-Kinase and P K channels) used in heart failure
92
Sildenafil
PDE5 inhibitor cGMP-PDE5->GMP cGMP: smooth muscle relaxation used for erectile dysfunction
93
Tadalafil
PDE5 inhibitor cGMP-PDE5->GMP cGMP: smooth muscle relaxation used for erectile dysfunction
94
ACE inhibitors
Decrease Angiotensin II and increase bradykinin | vasodilate, use in hypertension
95
Fenoldopam
Dopamine A1 receptor agonist increase cAMP -> vasodilate use in hypertensive crisis b/c strong RBF dilator -> diuretic
96
Prazosin
alpha adrenergic blocker | vasodilation
97
Albuterol
B2 agonist cAMP/PKA bronchodilator
98
Pirbuterol
B2 agonist cAMP/PKA bronchodilator
99
Tertbutaline
B2 agonist cAMP/PKA bronchodilator
100
Salmeterol
B2 agonist cAMP/PKA bronchodilator
101
Formoterol
B2 agonist cAMP/PKA bronchodilator
102
Ipratropium
anti-cholinergic (muscarinic) | bronchodilator / inhibit mucus
103
Tiotropium
anti-cholinergic (muscarinic) | bronchodilator / inhibit mucus
104
Theophylline
PDE inhibitor adenosine receptor antagonist bronchodilator
105
Aminophylline
PDE inhibitor adenosine receptor antagonist bronchodilator
106
Aldosterone
glucocorticoid (0.2:250 anti-inflam:Na retention) Made in Zona glomerulosa of adrenal controlled by angioitensin II and K
107
Cortisol
glucocorticoid (1:1 anti-inflam:Na retention) Made in Zona fasciculata and reticularis of adrenals Controlled by ACTH
108
Glucocorticoid effects
``` Increases plasma glucose Increases liver glycogen Stimulates amino acid mobilization Redistribute body fat (moon face) Sleepiness Mineralocorticoid effects (increase Na reabsorbtion, increase K secretion, hypertension) Lymphosytopenia and monocytopenia (redistribution) Prevent neutrophil adherence Inhibit chemotaxis Inhibits IL-1 and IL-2 release Inhibits arachidonic acid release Inhibits COX2 (via cytokines) ```
109
Glucocorticoid uses
``` Adrenal insufficiency rheumatoid arthritis osteoarthritis allergies inflammation organ transplant etc Contraindications: infection, esp TB ```
110
Dexamethasone
glucocorticoid (20:0 anti-inflam:Na retention)
111
Prednisolone
glucocorticoid (3:0.8 anti-inflam:Na retention)
112
Fludrocortisone
glucocorticoid (12:100 anti-inflam:Na retention)
113
Metyrapone
glucocorticoid inhibitor blocks 11-B-hydroxylation leads to increase ACTH Used as diagnostic for feedback loop
114
Mifepristone
glucocorticoid inhibitor Progesterone and glucocorticoid receptor antagonist used for termination of pregnancy and to treat Cushing's
115
Spironolactone
Mineralocorticoid/aldosterone antagonist K-sparing diuretic, weak (acts in distal tubule) anti-hypertension, often used with a thiazide or loop diuretic long duration anti-heart failure side effect= hyperkalemia
116
Eplerenone
Mineralocorticoid/aldosterone antagonist K-sparing diuretic, weak (acts in distal tubule) anti-hypertension, often used with a thiazide or loop diuretic long duration anti-heart failure side effect= hyperkalemia
117
Drospirenone
Progesterone, mineralcorticoid, androgen receptor antagonist diuretic used w/ estrogen for hormone replacement and to suppress ovulation
118
Azathioprine
``` cytotoxic anti-immune drug metabolized to 6-MP inhibits purine biosynthesis inhibits both de novo and salvage used for organ transplant and some autoimmune ```
119
Cyclophosphamide
cytotoxic anti-immune cross-links DNA most toxic to B-cells used for auto-immune
120
Methotrexate
cytotoxic anti-immune inhibits folate in purine synthesis (DNA synthesis) used to treat auto-immune
121
Mycophenolate Mofetil
``` cytotoxic anti-immune more selective inhibits IMP dehydrogenase (de novo pathway only, not salvage) lymphocyte specific used for auto-immune ```
122
Cyclosporine
Blocks NFAT, which blocks IL-2 production not lymphotoxic, more selective used for organ transplant and some auto-immune nephrotoxicity side effect
123
Tacrolimus
More potent cyclosporine | less side effects
124
Sirolimus
Inhibits T-cell activation downstream of IL-2 Inhibits mTOR similar to cyclosporine also used to coat cardiac stents
125
Aliskiren
Inhibits renin | used for hypertension, no effect on heart rate
126
Captopril
ACE inhibitor used for hypertension, no effect on heart rate decreases afterload
127
Enalapril
ACE inhibitor used for hypertension, no effect on heart rate decreases afterload
128
Lisinopril
ACE inhibitor used for hypertension, no effect on heart rate decreases afterload
129
Propranolol
B-blocker | reduces renin release
130
Metoprolol
B-blocker | reduces renin release
131
Actions of Angtiotensin II
AT1 receptors = vasoconstriction, aldosterone, etc (Gq) AT2 = vasodilation Vascular SM - AT1 dominant Stimulates aldosterone and ADH and NE
132
Losartan
AT1 receptor antagonist (AngII) used for hypertension, no effect on heart rate decreases afterload contraindicated in pregnancy
133
Nifedipine
``` 1,4-Dihydropyridine Ca channel blocker reduce afterload arterial dominant used with B-clickers for hypertension ```
134
Amlodipine
``` 1,4-Dihydropyridine Ca channel blocker reduce afterload arterial dominant used with B-clickers for hypertension ```
135
Dopamine
Vasodilator diuretic | increase RBF
136
Atriopeptins
Vasodilator diuretic | increase RBF
137
Mannitol
Osmotic diuretic must be IV sort of last-ditch enhanced K excretion
138
Acetazolamide
``` Carbonic anhydrase inhibitor diuretic OAT decreases bicarbonate reabsorbtion urine pH increases K secretion increases used for glaucoma, to alkalinize urine, altitude sickness side effect = metabolic acidosis ```
139
Furosemide
'Lasix' - Loop diuretic OAT inhibits Na-K-Cl symporter in ascending limb potent, fast acting, short lived increases Na-K exchange used for edema and hypertension side effects= hypokalemia, hyperuricemia, hyperglycemia
140
Bumetanide
Loop diuretic | like furosemide
141
Ethacrynic acid
Loop diuretic | like furosemide
142
Hydrochlorothiazide
``` Thiazide diuretic OAT Inhibits Na-Cl symporter in ascending limb intermediate activity, long lasting excrete hypertonic urine used for edema and hypertension side effects= hypokalemia, hyperuricemia, hyperglycemia contraindicated in renal failure ```
143
Chlorothiazide
Thiazide diuretic
144
Metolazone
Thiazide diuretic
145
Triamterene
``` K-sparing diuretic Na-channel blocker in principal cells thus Na-K exchange is blocked used for hypertension with other diuretics and edema side effect= hyperkalemia ```
146
Amiloride
``` K-sparing diuretic Na-channel blocker in principal cells thus Na-K exchange is blocked used for hypertension with other diuretics and edema side effect= hyperkalemia ```
147
Heparin
Unfractionated heterogenous mixture of large neg charged peptides catalyzes inhibition of several coagulation factors via antithrombin (including thrombin and Xa) it does not affect synthesis of clotting factors LMWH: (low molecular weight) - does not inhibit thrombin, just Xa must be given IV or subcu does not cross placenta rapid action, complex half-life monitor action using aPTT used for immediate thrombosis treatment or surgical bipass prophylaxis side effect: bleeding and Heparin-induced thrombocytopenia (drop in platelets, due to antibody production)
148
Enoxaparin
Low molecular weight heparin longer half life, subcu admin more predictable
149
Dalteparin
Low molecular weight heparin longer half life, subcu admin more predictable
150
Lepirudin
direct thrombin inhibitor IV admin used for pts with heparin-induced thrombocytopenia
151
Protamine Sulfate
heparin antagonist positively charged, low molecular weight used to reverse heparin after cardiopulmonary bypass
152
Warfarin
Inhibits VKORC1 VKORC1 converts vitamin K to it's active form (KO->KH2), which is required for activation of clotting factors II, VII, IX, and X. therapeutic effect is delayed hours to days bc existing factors are unaffected Metabolized by CYP2C9 It does cross placenta Normal INR= .8-1.2 Warfarin INR= 2-3 used for long-term prophylaxis for thrombosis/thromoembolism
153
Dabigatran
anti-coagulant prodrug, reversible direct thrombin inhibitor not monitored shorter half-life few adverse rxns, except with altered P-glycoprotein used similar to warfarin
154
Rivaroxaban
``` Anti-coagulant Inhibits Xa, once-daily P450 metabolized few adverse rxns, except with altered P-glycoprotein no monitoring used similar to warfarin ```
155
Alteplase
``` Tissue Plasminogen activator (t-PA) Thrombolytic Binds to fibrin, activates plasminogen to plasmin, which initiates clot resolution (degrades fibrin) given IV, expensive used for STEMI and ischemic stroke ```
156
Aminocaproic acid
Procoagulant inhibitor of fibrinolysis (inhibits plasmin) used for decreasing hemorrage in surgery
157
Aspirin
low dose= anti-platelet used for MI prophylaxis COX1,2 inhibitor in platelets, thus blocks thromboxane formation
158
Dipyramidole
Anti-platelet phosplodiesterase inhibitor, increases cAMP, which inhibits platelet aggregation used with warfarin to prevent thromboemboli
159
Ticlopidine
Similar to Clopidogrel but used less
160
Clopidogrel
Anti-platelet blocks ADP-receptor (P2Y1->Gi) leads to increased cAMP activated by CYP2C19
161
Abciximab
anti-platelet prevents binding of clotting factors to the GPIIb/IIIa receptor on activated platelets given IV used adjunct to percutaneous coronary intervention

Pharmacology (8 decks)

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