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IPAP JUNIOR SEM. > PHARM II, BLOCK I > Flashcards

PHARM II, BLOCK I Flashcards

(153 cards)

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1
Q

What are the 5 steps of the pain process

A 
Transduction 
Conduction 
Transmission 
Modulation 
Perception
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2
Q

What is somatic pain

A

Nociceptive superficial pain

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3
Q

What is visceral pain

A

Nociceptive organ pain

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4
Q

What are the three types of chronic pains

A

Peripheral Nociceptive
Neuropathic
Centralized

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5
Q

What is the toxic metabolite of Tylenol

A

NAPQI

Damages the liver

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6
Q

What are the doses for Tylenol Toxicity

A

10-15 gm as a single dose is hepatotoxic

20-25 gm is pot. Fatal

Taking more than 4 gm in 24 hours is toxic

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7
Q

What is the antidote to Tylenol OD

A

N-acetyl cysteine

Acetadote/ Mucomyst

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8
Q

What is the MOA of ASA

A

Irreversibly inhibits COX-1 and COX-2 enzymes

Anti-platelet effect lasts for the life of the platelet (7 to 10 days)

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9
Q

Ketorolac can decrease opiod requirement by

A

25- 50 percent

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10
Q

What is the usage limit on ketorolac

A

No more than 5 days ( has a huge bleeding risk)

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11
Q

How does Ketorolac affect LnD

A

may adversely affect fetal circulation and inhibit uterine contractions

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12
Q

What NSAID has the lowest CV risk

A

Naproxen

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13
Q

Naproxen is FDA approved for what arthritic Dx

A

Gout

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14
Q

NSAID of use for gout attack

A

Indomethacin

Naproxen can also be used

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15
Q

What is the DOC for opthalmatic prep

Conjucntival inflammation and reduce pain after abrasions

A

Indomethacin

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16
Q

What is the 1st NSAID that showed accelerate closure of patent ductus arteriosus (PDA)

A

Indomethacin

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17
Q

What are the ADE and contra for Ibuprofen

A

ADE: GI irritation/bleeding (less frequent than with aspirin)
Low GI risk; moderate to high cardiovascular risk
Tinnitus

CONTRA: Angioedema
Aspirin sensitivity— bronchospasm

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18
Q

How does meloxicam interact with COX I and II

A

Preferentially inhibits COX-2 over COX-1 (at lower doses) looses selectivity at doses of 15mg/day

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19
Q

Clinical use of Meloxicam

A

OA and RA

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20
Q

What are the ADE for Diclofenac: an NSAID used to chronic MSK mild to moderate pain

A

High cardiovascular risk; moderate GI risk (oral formulation)
More frequently causes AST/ALT increase

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21
Q

What are the clin use of Celecoxib

A

OA and RA, Juvi RA, Ankylolsing and 1* dysmenorrhea

Developed to minimize ADE of GI
HIGH CV risk
And has a sulf group ( allergies)

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22
Q

Which NSAID has the least CV events

A

Naproxen

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23
Q

What drugs NSAIDS are the best for GI Bleeding Rsk pts

A

Celecoxib or non selective NSAIDS with a PPI or misoprostol

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24
Q

What are the three ways Opiods work

A
  • Inhibit the transmission of nociceptive input from the periphery to the spinal cord
  • Activate descending inhibitory pathways that modulate transmission in the spinal cord
  • Alter limbic system activity (pain perception
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25
What are the 3 kinds of Opiod receptors
Mu kappa Delta
26
How do Mu(1) and Mu(2) receptors affect
μ1: analgesia μ2: respiratory depression, miosis, reduced gastric motility, sedation, euphoria, pruritus, urinary retention, physical dependence
27
What receptors does morphine act on
Mu I and II , Weak affinity for delta and Kappa
28
Half life of morphine
2-4 hours
29
What is the metabolite of morphine
Hydromorphone
30
How often do we have to do REMS training to Rx hydromorphone
Every 2 years
31
What is Dilaudid
Hydromorphone | Metabolite of morphine better oral absorption and more fat soluable
32
Is hydrocodone a partial or full agonist at the Mu receptor
Full ( pure)
33
Oxycodone is metabolized in to what two substances
Noroxycodone and oxymorphone
34
What is oxymorphone
Semi-synthetic Mu receptor agonist | Works way better than morphine
35
What is a prodrug that metabolizes into morphine
Codeine
36
What age group should codeine not be used in
Death Related to Ultra-Rapid Metabolism of Codeine to Morphine - Not recommended for <12 yo - Caution in 12-18 yo with asthma or other breathing problems
37
What receptors does Buprenorphine interact with
Mixed agonist/antagonist Partial mμ receptor agonist and kappa receptor antagonist
38
What is the clin use for buprenorphine
Opiod detox
39
What receptors does butorphanol interact with
Partial agonist Partial mμ and kappa receptor agonist
40
What partial agonist can be use in labor when an epidural is not possible
Butorphanol
41
What effects does Nalbuphine have on receptors
Mixed agonist/antagonist Partial mμ receptor antagonist and strong kappa receptor agonist
42
What is meperidine
Demerol Severe pain Half life 15-30 hrs Renally cleared
43
What patients CAN NOT receive meperidine
Renal or liver impairment or being too old Heart conditions ( negative inotropy) Pts on MAOI
44
How much stronger in fentanyl than morphine
75-125 times stronger
45
What is alfentanil
More rapid onset of fentanyl | Does not accumulate when infused
46
What is sufentanil
Slower onset version of fentanyl but last just as long
47
What is remifentanil
Fentanyl version that is infusion only Rapid onset Shortest duration of the fentanyl derivatives
48
What receptors does methadone act on
Potent agonist at mμ, kappa, and delta receptors Antagonist at NMDA receptor Inhibits serotonin and norepinephrine reuptake
49
What is the half life of methadone and what is the drug used for
Chronic pain syndrome: (neuropathic, cancer pain, and chronic non-cancer pain) For opioid-tolerant patients only Unpredictable t ½ 8-59hrs
50
What the difference between naloxone and naltrexone
Naloxone: Shorter acting used for Opioid rescue No systemic effect when given orally Used orally for opioid induced constipation Naltrexone: Longer acting and slower onset Used in opioid and alcohol addiction 100% absorbed and active orally
51
How often can naloxone be administered
Q 2-5 min
52
How does naltrexone work
Mμ receptor competitive antagonist Competes but does not displace opioids
53
Naltrexone + Bupropion can treat what
Weight managment
54
How does tramadol effect SZR threshold
Lowers it Abuse can cause SZR
55
What is considered opiod tolerant treatment/ exposure
More than 60 mg of MME/ day
56
How should Opiods be tapered
Taper by 20-50% per week (of original dose) for patients who are not addicted; the goal is to minimized adverse/withdrawal effects Tapers slower than 10% per week (5-20% per month) better tolerated and appropriate for patients on long term opioids Considered successful as long as patient is making progress
57
Oral morphine to IV morphine conversion
3:1
58
What does thrombin do
proteolytic enzyme that is formed from prothrombin that facilitates the clotting of blood by converting fibrinogen to fibrin
59
What are the three phases of thrombus formation
Adhesion, Activation, aggregation
60
In platelet homeostasis, what is the role of NO and prostaclyin
NO and prostacyclin induces cAMP synthesis. cAMP decreases intracellular Ca2+ and inhibits GP IIb/IIIa activation
61
What is the receptor for Fibrin formation
GP IIb/IIIa
62
What factor mediates platelet adhesion
Von will factor
63
What chemicals do adhered platelets release
Adhered platelets release numerous chemical mediators including Adenosine Diphosphate (ADP), Thromboxane A2 (TXA2), Serotonin (5HT), Platelet Activation Factor, etc.
64
What is Arachidonic acid converted to by COX
Prostaglandin G2
65
What is the role of 5HT IN PLATELET activation
Causes blood vessel to spasm, increase cytosolic calcium released Results in narrowing the blood vessel, decreasing blood loss until clotting can occur Serotonin release activates other platelets
66
What is the “tissue factor” pathway
EXtrinsic pathway Vit K dependent Inhibited by warfarin which inhibits the hepatic synthesis of several clotting factors
67
What is the “contact activation” pathway
INtrinsic pathway inhibited by Heparin
68
What does protein C do
Destroys activated factors Va and VIIIa
69
What activates Prothrombin (II) into Thrombin (IIa)
Factor Xa
70
What is protein S
Cofactor for protein C
71
What does antithrombin III do
(inactivates IIa, VIIa, IXa, Xa): inhibits clotting factor proteases, especially thrombin, by forming complexes with them
72
What test assesses the EXtrinsic pathway
Prothrombin Time (PT)
73
What is the INR
standardized PT designed to account for differences in thromboplastin
74
What lab test assesses the INtrinsic pathway
APTT
75
Where does Warfarin inhibit the clotting cascade
Factors II, VII, IX and X Inhibits vitamin K cofactors Vitamin K epoxide reductase inhibition reduces available vitamin K needed by the Vit K dependent clotting factors: -factors II, VII, IX, and X as well as endogenous anticoagulant proteins C and S
76
Warfarin blocks what vitamin reducatase?
Vitamin K ( V COR 1)
77
Clinical use of Warfarin
Prophylaxis and treatment of DVT, PE, thromboembolic complications associated with A. fib and/or prosthetic cardiac valve replacement Secondary prevention in the risk of death, recurrent MI, and thromboembolic events such as stroke or systemic embolization after MI Protein C and S deficiency
78
How many days does Warfarin take to go into effect
2-7 days
79
What lab test monitors warfarin treatment
INR
80
What is a normal INR range
0.8 and 1.2
81
What is the INR goal for DVT prophylaxis and Tx of Thrombodic Dz
2-3
82
What is the INR goal for artificial heart valves
2.3-3.5
83
Purple Toe Syndrome is a ADE of what medication
Warfarin
84
Can Warfarin be used in pregnancy
NO ! Cat X
85
What enzyme metabolizes warfarin
CYP2C9
86
What medication that increases GI bleeding should be avoided with Warfarin
NSAIDs
87
What does a high INR mean
The pt takes longer to form a clot
88
What are two PCC drugs | blood coagulation replacement products indicated for the urgent reversal of acquired coagulation factor deficiency
KCentra and Profilnine | Used to correct an active bleed
89
If the INR is about 4.5 what is the Tx
Reduce or skip warfarin does, | Monitor the INR
90
In the INR is 4.5 to 10 what is the Tx
Hold 1-2 doses of warfarin Vit K can be used if urgent surgery is needed or bleeding risk is high
91
If INR is greater than 10 what is the Tx
Hold warfarin and give vitamin K 2.5-5 mg Monitor INR Can give IV Vit K
92
What is the Drug name for Vit K
Mephyton (PO) and Aquamephyton(IM) Admin slow to avoid anaphylactic RXN
93
What factors does heparin act on
Binds to antithrombin III and inhibits Xa and IIa
94
Is heparin absorbed orally
No
95
What is heparin induced thrombocytopenia
Hypercoag state from prolonged heparin exposure, causes a 50% decrease in platelets
96
What are the ADE of heparin
Bleeding, HIT, Osteoporosis and Hyperkalemia
97
What is a normal aPTT time
28-38 seconds
98
An aPTT above 70 indicates..
An aPTT above 70 indicates..
99
What is the preferred anticoagulant in pregnancy
LMWH
100
What is Protamine sulfate
Reversal drug for heparin
101
What is the boxed warning on LMWH
Spinal and epidural hematomas
102
Does LMWH need to be monitored
No
103
What is the DOC for anti coagulation in cancer pts
Dalteparin
104
How does Fondaparinux effect the clotting cascade
Blinds to antithrombin III and selectively inhibits Factor Xa (More specific LMWH)
105
When Tx acute DVT with fondaparinux what drug must be used in combination
Warfarin
106
Does protamine sulfate completely reveres LMWH
NO
107
What are the Three LMWH
Fondaparinux (most specific to Xa) Enoxaparin Dalteparin (Cancer)
108
What are the Three Direct Factor Xa Inhibitors
Rivaroxaban Apixaban Edoxaban
109
Can warfarin be used in pts with prosthetic valves
YES ( one advantage of Warfarin)
110
What factors does heparin act on
Binds to antithrombin III and inhibits Xa and IIa
111
Is heparin absorbed orally
NO
112
What is heparin induced thrombocytopenia
Hypercoag state from prolonged heparin exposure, causes a 50% decrease in platelets
113
What are the ADE of heparin
Bleeding, HIT, Osteoporosis and Hyperkalemia
114
An aPTT above 70 indicates..
28-38 seconds
115
An aPTT above 70 indicates..
May indicate internal bleeding
116
What is the preferred anticoagulant in pregnancy
LWMH
117
When can Edoxaban be used in DVT/ PE Tx
After 5 days of Tx with a parenteral anticoagulant
118
What are Rivaroxaban and Apixaban used for
Stroke prevention and systemic embolism in patients with non-valvular atrial fibrillation Prophylaxis of DVT following hip or knee surgery DVT/PE treatment
119
What is andexxa
(Antidote for Direct Factor Xa inhibitors) Recombinant Factor Xa
120
What is the safest direct factor Xa medication for pregnancy
Apixaban
121
What are the warnings for Direct Factor Xa inhibitors
Avoid in pts with liver problems ( Riva and Apixaban) | or hepatic impairment ( Edoxaban)
122
What is the allergy precaution for Protamine sulfate
Fish allergy
123
What class is Bivalirudin and Argatroban
Direct thrombin inhibitors
124
What is the drugs to use in PCI
Direct Thrombin inhibitors Bivalirudin and Argatroban
125
How is Bivalirudin cleared
Renal
126
How is argatroban cleared
By the liver
127
What two labs are monitored with Bivalirudin and argatroban
``` APTT (1.5-2.5 baseline) and ACT ( >2.5 times baseline) ```
128
What is Dabigatran
Direct thrombin inhibitor prodrug metabolized by P-glycoprotein
129
What drug must be stopped for 2 hours prior to taking dabigatran
Antacids
130
When converting a pt from Warfarin to Dabigatran what must the INR be
Below 2.0
131
What is the antibody for Dabigatran
humanized monoclonal antibody fragment that binds to dabigatran and its metabolites with higher affinity then the binding affinity of dabigatran to thrombin, neutralizes anticoagulant effect ONLY USED in EMERGENCY
132
What is the antidote for Unfiltered Heparin
Protamine sulfate
133
What is the Antidote for LMWH
None really, may consider protamine sulfate
134
What is the antidote for Warfarin
Phytonadione ( VIT K ) May consider PCC > FFP (Prothrombin complex concentrate)
135
What is the antidote for Dabigatran
Idarcuzimab
136
What is the reversal/ antidote for Rivaroxaban, Apixaban, and Edoxaban
Recombinant Factor Xa ( Andexxa)
137
What monitoring is required for LMWH
None
138
What is the MOA of fibrinolytics
dissolve clots by activating the conversion of plasminogen to plasmin that hydrolyzes (cleaves) fibrin, lysing thrombus
139
What is the time frame for best Fibrinolytic Tx
Within 3 hours | some benefit at 12
140
Clinical use of fibrinolytics
Life threatening events STEMI STROKE PE Severe DVT
141
What is the black box warning for ticagrelor
Black Box Warning: decreased effectiveness with aspirin doses greater than 100 mg
142
How does Clopidogrel and prasugrel work compared to ticagrelor
Clopidogrel and Prasugrel: Irreversibly inhibits the binding of adenosine diphosphate (ADP) to its P2Y12 receptor Resulting in inhibition of the GPIIb/IIIa receptors required for platelet aggregation Both are PRODRUGS Ticagrelor: Reversibly inhibits the binding of ADP to its P2Y12 receptor Resulting in inhibition of the GPIIb/IIIa receptors required for platelet aggregation
143
For a non pci capable hospital what is the Tx approach to STEMI
MONA then Transfer to a PCI hospital within 120 min Or Fibrinolytics within 30 min (Tenecteplase, Reteplase, or alteplase) Then Clopidogrel Then Heparin or enoxaprin or Fondaparinux
144
For a PCI capable hospital what is the Tx approach to STEMI
``` MONA Then P2Y12 ( Clopidogrel, Ticagrelor) ``` And/or GPIIb/IIIa Antagonist (Tirofiban High Dose Bolus, Eptifibatide Double Dose) Or Bivalirudin With or without heparin
145
In the absences of contras, what is the medical managment for all patients with a NSTEMI
aspirin (ASA) + P2Y12 receptor inhibitor +/- glycoprotein IIb/IIIa inhibitors ( Clopidogrel, and Eptifibatide)
146
What the clearance for Abciximab vs Eptifibatide and Tirofiban
Abciximab does not require renal adjustment Eptifibatide and Tirofiban does
147
What is the role of GPIIb/IIIa inhibitors
Abciximab: Adjunct to PCI for the prevention of cardiac ischemic complications in patients undergoing PCI In patients with unstable angina not responding to conventional medical therapy when PCI is planned within 24hrs Eptifibatide and Tirofiban: Administered with heparin and aspirin in ACS and PCI to reduce thrombotic cardiac events
148
What are the absolute contra for fibrinolytics
``` History of intracranial hemorrhage History of cerebrovascular lesion Known intracranial neoplasm Ischemic stroke ≤ 3 months Aortic dissection History of head or facial trauma within 3 months Active bleeding / bleeding diathesis ```
149
What are the three GPIIb/IIIa inhibitors
Abciximab (monoclonal Ab) (High risk of causing RXN) Eptifibatide Tirofiban
150
What drugs must be administered with TPA
Asparin and heparin
151
TPA drugs alteplase is approved for? Reteplase and tenecteplase approved for?
Alteplase: STEMI, PE, Ischemic stroke w/in 3 hours, and catheter clearance Reteplase and tenecteplase are only approved for acute STEMI
152
What is the MOA of TPA ( Alteplase, ect)
activate plasminogen that is bound to fibrin in a thrombus, thereby initiating fibrinolysis
153
What is the MOA of Urokinase
THROMBOLYTIC ENZYME human enzyme synthesized by the kidney that directly converts uncomplexed plasminogen to active plasmin, degrades fibrin and clotting factors V and VII (UNCOMPLEXED!! UNBOUND)

IPAP JUNIOR SEM. (43 decks)

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