MUSCULOSKELETAL, SKIN, AND CONNECTIVE TISSUE- Pharmacology Flashcards
1
Q
Products of Arachidonic Acid
A
Lipoxygenase
Cyclooxygenase
2
Q
Products of Arachidonic Acid
A
Lipoxygenase
Cyclooxygenase
3
Q
What is the product of Phospholipase A2?
A
Arachidonic Acid
4
Q
What produces Phospholipase A2?
A
Membrane lipid (eg. phosphatidylinositol)
5
Q
Which drug inhibit Phospholipase A2 and protein synthesis to Cyclooxigenase?
A
Corticosteroids
6
Q
Drug that inhibits Lipoxigenase pathway
A
Zileuton
7
Q
Which drugs inhibit Leukotrienes?
A
Zafirlukast
Montelukast
8
Q
Which drugs inhibit just Cyclooxygenase?
A
NSAIDS, aspirin, acetaminophen, COX- 2 inhibitors
9
Q
Which pathway yields Leukotrienes?
A
Lipoxygenase
10
Q
Effect of LTB4
A
Neutrophil chemotactic agent
11
Q
Which is the function of LTC4, D4 and E4?
A
Bronchoconstriction, vasoconstriction, contriction of smooth muscle and ↑ vascular permeability
12
Q
Products of Cyclooxygenase
A
Endoperoxides
13
Q
Which are the products of Endoperoxides?
A
Prostacyclin
Prostaglandins
Thromboxane
14
Q
PGI2
A
Prostacyclin
15
Q
Who forms Prostaglandins?
A
PGE2
PGF 2 α
16
Q
Before getting to leukotrienes, what is the product of Lipoxygenase?
A
Hydroperoxides
17
Q
Name effects of PGI2
A
↓ Platelet aggregation
↓ Vascular tone
↓ bronchial tone
↓ uterine tone
18
Q
What is the effect of Prostaglandins?
A
↓ Bronchial tone
↑ Uterine tone
19
Q
Main effects of Prostaglandins
A
↑ Platelet aggregation
↑ Vascular tone
↑ Bronchial tone
20
Q
Mechanism of action of Aspirin
A
Irrevisbly inhibits cyclooxygenase (both COX-1 and COX-2) by covalent acetylation, which ↓ synthesis of both thromboxane A2 (TXA2) and prostaglandins
21
Q
Which cyclooxygenase are inhibited by Aspirin?
A
Both COX-1 and COX-2
22
Q
What is the effect of Aspirin related to bleeding?
A
↑ Bleeding time until new platelets are produced
23
Q
How much time does it takes to produce new plateles?
A
7 days
24
Q
How are coagulation time affected by Aspirin?
A
No effect on PT and PTT
25
How is Aspirin calssified?
A type of NSAID
26
Low dose of Aspirin
27
What is the clinical use of Low dose Aspirin?
↓ low platelet aggregation
28
Intermediate dose of Aspirin
300-2400 mg/day
29
Clinical use for Intermediate dose of Aspirin
Antipyretic and analgesic
30
Dosis consider to be high of Aspirin
2400 - 4000 mg/ day
31
Clinical use for High dose aspirin
As inflammatory
32
Toxic effects caused by Aspirin
Gastric ulceration
| Tinitus (CN VIII)
33
What is the risk of chronic use of Aspirin?
Acute renal failure, interstitial nephritis and upper GI bleeding
34
Respiratory secondary effects caused by Aspirin use
Stimulates respiratory centers, causing hyperventilation and respiratory alkalosis
35
Respiratory secondary effects caused by Aspirin use
Stimulates respiratory centers, causing hyperventilation and respiratory alkalosis
36
What is the product of Phospholipase A2?
Arachidonic Acid
37
What produces Phospholipase A2?
Membrane lipid (eg. phosphatidylinositol)
38
Which drug inhibit Phospholipase A2 and protein synthesis to Cyclooxigenase?
Corticosteroids
39
Drug that inhibits Lipoxigenase pathway
Zileuton
40
Which drugs inhibit Leukotrienes?
Zafirlukast
| Montelukast
41
Which drugs inhibit just Cyclooxygenase?
NSAIDS, aspirin, acetaminophen, COX- 2 inhibitors
42
Which pathway yields Leukotrienes?
Lipoxygenase
43
Effect of LTB4
Neutrophil chemotactic agent
44
Which is the function of LTC4, D4 and E4?
Bronchoconstriction, vasoconstriction, contriction of smooth muscle and ↑ vascular permeability
45
Products of Cyclooxygenase
Endoperoxides
46
Which are the products of Endoperoxides?
Prostacyclin
Prostaglandins
Thromboxane
47
PGI2
Prostacyclin
48
Who forms Prostaglandins?
PGE2
| PGF 2 α
49
Before getting to leukotrienes, what is the product of Lipoxygenase?
Hydroperoxides
50
Name effects of PGI2
↓ Platelet aggregation
↓ Vascular tone
↓ bronchial tone
↓ uterine tone
51
What is the effect of Prostaglandins?
↓ Bronchial tone
| ↑ Uterine tone
52
Main effects of Prostaglandins
↑ Platelet aggregation
↑ Vascular tone
↑ Bronchial tone
53
Mechanism of action of Aspirin
Irrevisbly inhibits cyclooxygenase (both COX-1 and COX-2) by covalent acetylation, which ↓ synthesis of both thromboxane A2 (TXA2) and prostaglandins
54
Which cyclooxygenase are inhibited by Aspirin?
Both COX-1 and COX-2
55
What is the effect of Aspirin related to bleeding?
↑ Bleeding time until new platelets are produced
56
How much time does it takes to produce new plateles?
7 days
57
How are coagulation time affected by Aspirin?
No effect on PT and PTT
58
How is Aspirin calssified?
A type of NSAID
59
Low dose of Aspirin
60
What is the clinical use of Low dose Aspirin?
↓ low platelet aggregation
61
Intermediate dose of Aspirin
300-2400 mg/day
62
Clinical use for Intermediate dose of Aspirin
Antipyretic and analgesic
63
Dosis consider to be high of Aspirin
2400 - 4000 mg/ day
64
Clinical use for High dose aspirin
As inflammatory
65
Toxic effects caused by Aspirin
Gastric ulceration
| Tinitus (CN VIII)
66
What is the risk of chronic use of Aspirin?
Acute renal failure, interstitial nephritis and upper GI bleeding
67
Risk of aspirin use in children
Reye syndrome when treating viral infections`
68
Respiratory secondary effects caused by Aspirin use
Stimulates respiratory centers, causing hyperventilation and respiratory alkalosis
69
NSAIDs
Ibuprofen, naproxen, indomethacin, ketorolac, diclofenac
70
Mechanism of NSAIDs
Reversibly inhibit cyclooxygenase (both COX-1 and COX-2)
| Block PG synthesis
71
Clinical use of NSAIDs
Antypiretic, analgesic, anti-inflammatory
72
NSAID use to close PDA
Indomethacin
73
Alternative use of Indomethacin
NSAID use to close PDA
74
Secondary effects of NSAIDs
Interstitial nephritis, gastric ulcer, renal ischemia
75
Why NSAIDs cause gastric ulcer?
Because they inhibit PGs that protect gastric mucosa
76
Why NSAIDs cause renal ischemia?
Because they inhibit PGs that vasodilate afferent arteriole
77
COX-2 inhibitors
Celecoxib
78
Mechanism of action of Celecoxib
Reversibly inhibits specifically the cyclooxygenase isoform 2
79
Cellular effect of Colchicine
Impairing leukocyte chemotaxis and degranulation
80
Which benefit do COX-2 inhibitors have compared to NSAIDs?
Spares COX-1, which helps maintain the gastric mucosa
| Spares platelet function as TXA-2 production is dependent on COX-1
81
When is recommended the clinical use of Celecoxib?
Rheumatoid arthritis and osteoarthritis; patiens with gastritis or ulcers
82
What are the risks of COX-2 inhibitors use?
↑ risk of thrombosis
| Sulfa allergy
83
Mechanism of action of Acetaminophen
Reversibly inhibits cyclooxygenase, mostly in CNS
84
Where is Acetaminophen inactivated?
Peripherally
85
Effect of Acethaminophen
Antipyretic, analgesic, but not anti-inflammatory
86
Used instead of aspirin to avoid Reye syndrome in children with viral infection
Acetaminophen
87
Secondary effect of acetaminophen overdose
Hepatic necrosis
88
How does acetaminophen produces hepatic necrosis?
Acetaminophen metabolite (NAPQI) deplets glutathione and forms toxic tissue adducts in liver
89
Which is Acetaminophen metabolite?
NAPQI
90
Antidote of Acetaminophen
N acetylcysteine is antidote
91
What is the effect of N acetylcysteine in Acetaminophen overdose?
Regenerates Glutathione
92
Biphosphonates drugs
Alendronate, other -dronates
93
Pyrophosphate analogs
Biphosphonate
94
Mechanism of action of Biphosphonates
Bind hydroxyapatite in bone, inhibiting osteoclast activity
95
Clinical use of Biphosphonates
Osteoporosis, hypercalcemia, Paget disease of bone
96
Toxic effect caused by biphosphonates
Corrosive esophagitis, osteonecrosis of the jaw
97
In order to prevent corrosive esophagitis, what is recommended when indicating biphosphonates?
Patients are advised to take with water and remain upright for 30 minutes
98
How is the treatment for Gout classified?
Chronic gout drugs (preventive)
| Acute gout drugs
99
Chronic gout drugs
Allopurinol
Febuxostat
Probenecid
100
Mechanism of action of allopurinol
Inhibits xanthine oxidase, ↓ conversion of xanthine to uric acid
101
Other clinical use for Allopurinol
Also used in lymphoma and leukemia to prevent tumor lysis associated urate nephropathy
102
What is increased with allopurinol use?
Increases concetration of azathioprine and 6 MP
103
What metabolizes Azathioprine and 6 MP?
By xanthine oxidase
104
What is contraindicated when using allopurinol?
Salicylates
105
Why Salicylates are contraindicated when using allopurinol?
All but the highest doses depress uric acid clearance
106
High doses of Allopurinol
5-6 g/day
| Have only minor uricosuric activity
107
Mechanism of action of Febuxostat
Inhibits xanthine oxidase
108
Inhibits reabsorption of uric acid in PCT (also inhibits secretion of penicillin)
Probenecid
109
Drugs used for Acute gout
NSAIDs
Glucocorticoids
Colchicine
110
NSAIDs recommended for acute gout
Naproxene, indomethacin
111
Administration way of Glucocorticoids for acute gout
Oral or intraarticular
112
Binds and stabilizes tubulin to inhibit microtubule polymerization
Colchicine
113
Cellular effect of Colchicine
Impairing leukocyte chemotaxis and degranulation
114
Risk of using TNF α inhibitors
Predispose to infection, including reactivation of latent TB
115
Why TNF α inhibitors predisposes to infection?
TNF blockade prevents activation of macrophages and destruction of phagocytosed microbes
116
TNF α inhibitors
Etanercept
| Infliximab, adalimumab
117
Fusion protein (receptor for TNF α + IgG1 Fc), produced by recombinant DNA
Etanercept
118
Clinical use of Etanercept
Rheumatoid arthritis, psoriasis, ankylosing spondylitis
119
Mechanism of action of Infliximab, adalimumab
Anti TNF α monoclonal antibody
120
Clinical use for Infliximab, adalimumab
Inflammatory Bowel disease
Rheumatoid arthritis
Ankylosing spondylitis
Psoriasis
