Weeks 1-6 Flashcards
1
Q
known side-effect of acetylsalicylic acid in susceptible individuals is
A
potential to thin stomach lining
& cause ulcers, bleeding risk
2
Q
Aspirin works as an anticoagulant by inhibiting formation of this molecule:
A
Thromboxane A2
3
Q
Atenolol is an example of a(n)
A
Beta1-blocker
4
Q
Which of the following is an effective treatment for CHF (congestive heart failure), but has a particularly low therapeutic index, and substantial adverse effects?
A
Digoxin (digitalis)
5
Q
Digoxin treats angina primarily by
A
not used for angina?
6
Q
Which of the following is an effective treatment for CHF (congestive heart failure), but has a particularly low therapeutic index, and substantial adverse effects?
A
Digoxin (digitalis)
7
Q
Which of the following is NOT an effective treatment for CHF (congestive heart failure)?
A
Anticoagulants
8
Q
A known side-effect of Celebrex is
A
Increased risk of MI
9
Q
Simvastatin
A
Lowers blood cholesterol by inhibiting synthesis of cholesterol in the liver
10
Q
Myopathy is sometimes a side-effect of:
A
Pravastatin
11
Q
Ezetimibe (Zetia)
A
Lowers blood cholesterol by inhibiting dietary absorption of cholesterol
12
Q
Acetaminophen is
A
An OTC drug that does not affect blood clotting or stomach ulceration
13
Q
Acetylsalicylic acid is
A
An OTC drug that is often prescribed at low doses to reduce risk of MI
14
Q
Verapamil (Calan) is an example of a(n)
A
Ca-channel blocker
15
Q
Verapamil (Calan) is an example of a(n)
A
Ca-channel blocker
16
Q
Promethazine (Phenergan) is an
A
Anti-emetic drug, NOT used with cancer chemotherapy
17
Q
Ondansetron (Zofran)is an
A
Anti-emetic drug, used with cancer chemotherapy
18
Q
Risperidone is an
A
Antipsychotic drug used with schizophrenia
19
Q
Positive symptoms of schizophrenia include
A
Auditory hallucinations
20
Q
Extrapyramidal symptoms
A
Can result from treatment with haloperidol
21
Q
Anti-emetic drugs act on the CTZ (chemical trigger zone) which is found in
A
the medulla oblongata, outside the blood-brain barrier
22
Q
Trazodone (Desyrel)is an example of a(n
A
SARI antidepressant
23
Q
SSRI’s are sometimes prescribed together with amitriptyline to treat this side-effect of SSRI’s
A
Insomnia
24
Q
Biochemically, depression seems to result from
A
Deficiencies of serotonin, dopamine and norepinephrine
25
Which of the following drug classes is also commonly used in treatment of bipolar disorder?
Anti-seizure medications
26
Barbiturate drugs are
Seldom used due to their risk of respiratory depression
27
Which of the following is NOT a side-effect of benzodiazepine drugs:
Respiratory depression
28
Midazolam (Versed) is a benzodiazepine that is
given IV before surgery (or colonoscopy etc) to produce sedation and amnesia.
29
Diazepam (Valium) is a benzodiazepine that is
sometimes used IV for status epilepticus.
30
Buspirone (Buspar) is a non-benzodiazepine drug that is
effective against anxiety and is not sleep-inducing
31
Complex seizures are characterized by
Confusion or loss of consciousness
32
Valproic acid (along with several other anti-seizure medications) is characterized by
Low therapeutic index
33
Phenytoin (along with several other anti-seizure medications) is characterized by:
High potential for teratogenicity
34
In addition to treating seizures, gabapentin is FDA-approved for
Treating shingles pain
35
A drug that is sometimes used IV to stop status epilepticus, but is not generally effective to prevent future seizures is
diazepam
36
Phenobarbital is a drug that is
Used occasionally for treatment of seizures
37
Lorazepam (Ativan) is a benzodiazepine that is:
used to treat a wide variety of conditions, including anxiety, alcoholism withdrawal, and chemotherapy-related nausea
38
Zolpidem (Ambien) is a non-benzodiazepine drug that is
widely prescribed, now available as a generic, and seems to have fewer withdrawal symptoms than benzodiazepines. treats insomnia.
39
Petit mal seizures are uniquely characterized by:
Absence of movement
40
Gabapentin (along with several other anti-seizure medications) is characterized by:
High frequency of off-label prescriptions
41
Valproic acid (along with several other anti-seizure medications) is characterized by:
High potential for teratogenicity
42
In addition to treating seizures, topiramate is FDA-approved for
Migraine prevention
43
Albuterol works by
acting as an agonist of B2 adrenergic receptors
44
Mometasone / Nasonex works as
an anti-inflammatory steroid
45
montelukast / Singulair works by
inhibiting release of inflammatory leukotrienes
46
Salmeterol asthma prescriptions have come into question because:
a recent study shows it relieves symptoms but may increase risk of asthma-related death
47
Which of the following drugs is a β
| blocker that is less specific and no longer widely used?
propranolol
48
Which of the following drugs is a β
| blocker that is now widely used to lower blood pressure?
metoprolol
49
Succinylcholine is used as a(n)
neuromuscular junction blocker in surgery
50
Chantix (varenicline) is used as a(n)
aid to smoking cessation
51
Side effects of excess dopamine in peripheral circulation include
High blood pressure and tachycardia
52
Ropinirole (Requip)is:
a PD drug that works as a dopamine agonist by imitating the action of dopamine.
53
Which of the following drugs is a β
| blocker that is used opthalmologically to treat glaucoma?
timolol
54
Salmeterol / Serevent works by
acting as an agonist of B2 adrenergic receptors
55
Cromolyn sodium works by
stabilizing the membrane of mast cells to prevent histamine release
56
Side effects of excess dopamine in peripheral circulation include
High blood pressure and tachycardia
57
Selegiline is:
a PD drug that works by inhibiting dopamine inactivation in the brain.
58
Chantix (varenicline) is used as a(n)
aid to smoking cessation
59
Succinylcholine is used as a(n)
neuromuscular junction blocker in surgery
60
Sevoflurane is used
as an inhalation anesthetic
61
Stanozolol is an anabolic steroid that works by binding to a receptor protein inside cells, increasing mRNA & protein synthesis in the same way that testosterone does.
Accordingly, that receptor protein works as a(n)
Nuclear receptor
62
Stanozolol is an anabolic steroid that works by binding to a receptor protein inside cells, increasing mRNA & protein synthesis in the same way that testosterone does.
Accordingly, stanozolol works as a(n)
Agonist
63
Digoxin binds to the sodium-potassium pump of cardiac myocytes, inhibiting ion flow. Accordingly, digoxin works as a(n)
Antagonist
64
Albuterol binds to a receptor in the autonomic nervous system, causing that receptor to be activated, expanding the airway. Accordingly, albuterol works as a(n)
Agonist
65
Chronic users of heroin find that it takes more and more drug over time to achieve the same high. Research shows these users have fewer receptors on their neurons than nonusers.
This best illustrates
Pharmacodynamic tolerance
66
A patient, concerned about his blood pressure, started taking 3x the prescribed dose of his metoprolol, a β-blocker. He was disappointed to find that his blood pressure remained about the same as with the regular dose. This best illustrates
Saturation
67
After taking one acetaminophen pill, a patient’s headache is lessened. After taking two pills the headache is gone. This best illustrates
Dose response
68
Ipratropium bromide (Atrovent) is used
to treat COPD
69
Nicotinic acetylcholine receptors are found at
Pre-ganglionic synapses of the sympathetic and parasympathetic systems
70
Adrenergic receptors are found at
Post-ganglionic synapses of the sympathetic system
71
Buspirone binds to a type of serotonin receptor in the CNS, causing that receptor to release a signal, leading to neuron firing. Accordingly, buspirone works as a(n)
Agonist
72
Selegiline binds to an isoform of monoamine oxidase (MAO), preventing MAO from breaking down dopamine. Accordingly, MAO works as a(n)
Enzyme
73
Selegiline binds to an isoform of monoamine oxidase (MAO), preventing MAO from breaking down dopamine. Accordingly, selegiline works as a(n)
Antagonist
74
Albuterol binds to a receptor in the autonomic nervous system, causing that receptor to be activated, expanding the airway. Accordingly, albuterol works as a(n)
Agonist
75
Adrenergic agonists such as methamphetamine can induce xerostomia, aka
dry mouth
76
Select the drug currently used as an inhalation anesthetic in the U.S.
desflurane
77
Patients taking AZT and saquinavir (both anti-HIV drugs) together have much better outcomes than taking either drug individually. This best illustrates
Additive or synergistic effects
78
Patients taking Coumadin (a blood thinner that is quite non-polar/lipophilic) may need to reduce its dosage if they begin taking Dilantin (an anti-seizure drug, also lipophilic). This best illustrates
Competition for serum albumin
79
Patients who stop taking atenolol (a β-blocker) often experience rebound hypertension.
This best illustrates
Physical dependence
80
phase II trials test for
effective treatment of a disease in a few individuals, before it has been approved by the FDA
81
phase I trials test for:
lack of toxicity in a small number of healthy human subjects
82
A sustained release drug is
Often encapsulated in tiny spheres
83
An enteric coated pill is specially treated to
Avoid irritating the stomach lining
84
Category A/B/C etc
| refers to
Level of risk for birth defects
85
A drug with a short half-life
May be quickly broken down by cytochrome P450 enzymes
86
Variations in drug metabolism may occur due to:
Genetics
Kidney disease
Hepatitis or liver cirrhosis
Age (newborns & geriatrics)
87
When naming a drug, the generic name is:
Not capitalized
88
A hydroxyl (-OH) group should be categorized as
Polar
89
Adding acid to an amine-containing drug makes it
An ionic form
90
Category A drugs are ones that:
Have been convincingly demonstrated not to cause birth defects in humans
91
ACE inhibitors and Valium (diazepam) are drugs that are classed
Category D
92
A drug with a high therapeutic index
Has a wide range between when its beneficial effects and its toxic effects occur
93
Illegal drugs with no accepted use in the U.S. are classified as:
Schedule I
94
A transdermal patch is most suitable for a drug that is/has
Lipophilic
95
A drug with a high therapeutic index
Has a wide range between when its beneficial effects and its toxic effects occur
96
Adding acid to an amine-containing drug makes it
More water-soluble
97
Phase I/II/III etc
| refers to
Stage of clinical development and FDA approval
98
The Ames test looks for:
carcinogenicity using bacterial growth plates
99
Category D drugs are ones that:
Have clinical data showing some risk of birth defects in humans, but may sometimes be prescribed anyway.
100
Synthroid (synthetic thyroid hormone) is an example of a drug that is classed
Category A
101
Tolterodine or oxybutynin are used primarily to treat
Incontinence
102
Mometasone is used primarily to treat
Asthma
103
Atenolol is used primarily to treat
Hypertension
104
Phenytoin is used primarily to treat
Seizures
105
Levodopa and carbidopa are used primarily to treat
Parkinson’s disease
106
Aprazolam is used primarily to treat
Anxiety
107
Clonidine is used primarily to treat
Hypertension
108
Zolpidem is used primarily to treat
Insomnia
109
Tolterodine and oxybutynin are classed as
muscarinic antagonists
110
Serevent is classed as a(n)
beta2 agonist
111
Bethanecol is classed as a(n)
muscarinic agonist
112
Timolol is classed as a(n)
non-specific beta blocker
113
Doxazosin and tamsulosin are classed as
alpha blockers
114
Atropine is used to treat
Organophosphate poisoning
115
Bethanecol is used to treat
postsurgical difficulty with urination
116
Tiotropium bromide and ipratropium bromide are used primarily to treat
COPD
117
Methylphenidate is used to treat
ADHD
118
Amphetamine is used to treat
ADHD
119
Blood pressure
cardiac output x systemic vascular
resistance
b.p. = CO x SVR
120
Ways to reduce blood pressure
| pharmacological
```
reduce blood volume
– diuretics
vasodilation – either arteries, veins or both
– Ca channel blockers,
– ACE inhibitors, alpha1 antagonists
– other vasodilators
decrease pumping rate or strength
– beta blockers
```
121
Ways to reduce blood pressure
| NON-pharmacological!
• weight reduction
– 60% hypertensive patients are overweight
• DASH (Diet Approach to Stop Hypertension)
– diet low in saturated fats, high in fruits and vegetables
(April 1997 NEJM)
• cessation of smoking – nicotine causes vasoconstriction
• reducing caffeine – caffeine is a vasoconstrictor
• reducing alcohol
• aerobic exercise
• Na restriction
122
Diuretics
```
-Inhibit Na+ reabsorption:
– Less Na+ reabsorbed causes less water reabsorption
– Net effect lowers blood volume
– Loss of K+ can be a problem
-Also to reduce edema in CHF
```
123
Primary diuretics
-furosemide (Lasix)
-hydrochlorothiazide (HCTZ)
Both cause loss of K+
(hypokalemia) in distal tubule
– Heart arrhythmia, muscle cramps & weakness
124
potassium-sparing diuretics
```
Inhibit Na+
/K+ exchange pump
– in late distal convoluted tubule
– Leaves Na+ in urine, K+ in blood
-Amiloride, triamterene
-Spironolactone
```
125
b1-blockers
Inhibit b1-adrenergic receptors of sympathetic NS
– Decrease heart rate, contractility and cardiac output
Fatigue, dizziness, bradycardia, depression
-Metoprolol
-atenolol
126
ACE inhibitors
Angiotensin converting enzyme
– Part of the renin-angiotensin-aldosterone system
• Hypertension as a complication of diabetes, renal disease
– angiotensin II causes vasoconstriction
• Also increases perfusion pressure in glomeruli
-lisinopril: Net vasodilation, decreased blood pressure
127
Angiotensin II receptor antagonists
Similar principle to ACE inhibitors, but block
the receptor instead of blocking production
-losartan, valsartan, other “-sartan” drugs
-category D
128
Calcium channel blockers
• Calcium channels open & allow Ca2+ into cytoplasm
causing vasoconstriction
• contraction of vascular smooth muscle
– Also increase contraction of heart muscle
• raises pacemaker activity in SA node, raises conduction through AV node
Ca channel blockers work better for African Americans
than ACE inhibitors, b-blockers
• Ca channel blockers lower blood pressure, but their
reduction of cardiovascular mortality may be limited
• Also used for angina, atrial fibrillation
129
Ca channel blocker drugs
nifedipine (Procardia), amlodipine (Norvasc)
– Block VSM contraction, but not heart muscle
• Others: verapamil (Calan), diltiazem (Cardizem)
– block Ca channels in both VSM and heart
– risk of AV heart block in predisposed patients
130
clonidine (Catapres)
• inhibits the sympathetic system via CNS
– decreases heart rate, causes vasodilation
• 40% of patients experience drowsiness,
sedation
• Available in a transdermal patch
131
Angina
• Sudden pain beneath sternum
– often radiating to left shoulder and arm
• Occurs when arteries cannot provide enough
oxygen to the heart
132
Classic angina
– due to partially occluded coronary arteries
– Triggered by physical exertion (or emotional
excitement)
133
Nitroglycerin
Vasodilator, mainly in veins, some in arteries
– Converted to nitric oxide (NO)
– Decreases venous return & strain on heart
• Sublingual pill
– Fast-acting (~1 min) & short acting: t½ 5-7 min
– Avoids liver first pass effect
– [Variant angina: relaxes vasospasm too]
• Extended-release patch: Nitro-dur
– 12h on, 12h off
134
Other angina drugs
Ca channel blockers
– relax vascular smooth muscle, increase oxygen
supply to heart
– Long-acting forms, mostly used prophylactically
• Eg. nifedipine
• b-blockers
– Lower heart rate (and contractility), reducing
oxygen demand of the heart
– Related: b-blockers reduce risk of a 2nd MI
135
Congestive Heart Failure
Ineffective pumping due to lower contractility,
lowers arterial blood pressure causing:
– Reflex tachycardia due to b1 stimulation
– Less filtering by kidneys,
• less urine, more blood volume
– Arterial vasoconstriction due to renin release
• Venous backup of blood, high venous pressure
– Peripheral & pulmonary edema
– Heart enlargement
136
CHF drugs
Diuretics!
– Reduce edema, blood volume, venous pressure
– furosemide (Lasix) most commonly used
digoxin (digitalis)
– From foxglove flowers
– Increases heart contractility
– Low TI, heart dysrhythmias, AV heart block, v-fib
• More likely with hypokalemia
– May not increase life expectancy, but may improve
heart performance
137
Other CHF drugs
• ACE inhibitors (-pril)
– Cause arteriovasodilation.
– Lessen after-load on heart
• Beta blockers
– Lowering heart rate & contractility seems contradictory
– Lowering heart rate can increase ejection fraction
– Also affect renin-angiotensin system
138
Blood clotting
-Too high clotting tendency can trigger MI, ischemic
stroke, DVT, pulmonary embolism
-Clot formation begins with platelet plug aggregation
– Next: fibrinogen converted to fibrin to form a thrombus
– Arterial: due to a rough surface that attracts platelets
– Venous: due to blood stagnation
• Clotting is restrained by antithrombin III, heparin
• Clots are broken down by activating plasmin
139
Anticoagulants
- Heparin
- enoxaparin (Lovenox)
- warfarin (Coumadin)
- ASA (Aspirin)
- thromboxane A2
- clopidrogrel (Plavix)
- tPA (Alteplase)
140
Heparin
```
Sugar polymer, found naturally in blood
• Binds antithrombin III and activates it 1000x
– Blocks blood-clotting cascade
• Prevents thrombin from converting
fibrinogen into insoluble fibrin
• IV administration
– Inactivated by HCl in the stomach
```
141
enoxaparin (Lovenox)
– Low-MW heparin, more reproducible effect, longer t½
– Home SC injections possible bid
• Often used with open-heart surgery, hip/knee replacements
142
warfarin (Coumadin)
```
Antagonist of vitamin
K, which is needed
for synthesis of
several clotting
factors
– Factors VII, IX, X and
prothrombin
– Inhibits further
synthesis, not existing
factors
• Takes 2-5 days to
reach max effect
```
143
Coumadin and diet
Vitamin K is found in many foods, especially
green leafy vegetables
– Day-to-day variations in diet affect coagulation
• Delayed effect
– Risk of either clotting or hemorrhaging
• Low TI, need for ongoing monitoring of PTT
– prothrombin time for clotting
– want INR (international normalized ratio) of 2.0-3.5
– Anticoagulation clinics are a major healthcare business
144
Pentoxifylline
| Trental
```
• Reduces blood viscosity
– Unknown mechanism
• Treats intermittent claudication
– Muscle pain (ache or cramp, often calf muscle)
from exercise
– Generally due to atherosclerosis
```
145
Acetylsalicylic acid
| ASA, Aspirin
• Aspirin inhibits formation
of thromboxane A2
– via COX1 (cyclooxygenase)
enzyme
• Thromboxane triggers
platelet activation &
aggregation, the 1st step in blood clotting
– Thromboxane is similar to prostaglandins
• Both can be related to inflammation
• Low dose (80mg daily) “baby aspirin”
• Aspirin is not literally a “blood thinner”
146
clopidogrel (Plavix)
Extensively used with arterial stents, to
prevent MI, stroke, angina
• Also inhibits platelet activation/aggregation
– Different mechanism than aspirin
– does not have the potential to thin stomach lining
& cause ulcers that aspirin does
• More expensive than aspirin
– Patent expired 2012
• Bleeding is a risk with aspirin or Plavix, but
much less so than with Coumadin
147
tPA (Alteplase)
```
Tissue plasminogen activator
– Causes breakdown of clots
– Used for treatment of MIs, ischemic strokes
• treatment must occur within a few hours of the event
– Hemorrhage is a possible side effect
• Human enzyme (protein)
– produced via genetic engineering
• ~$4000 per treatment
```
148
cholesterol
Synthesized by liver and absorbed in diet
• Some cholesterol is needed in cell membranes
– Some also needed for bile salts, steroid hormones
• Excess cholesterol accumulates via LDL in artery walls
– LDL >135 mg/dl (or total chol > 200) is a cause for concern
– LDL levels are affected by diet, genetics
• HDL is used by circulating macrophages to
scavenge/recycle cholesterol
– More HDL is better, lower ratio (<5) of LDL/HDL is better
– Aerobic exercise & moderate alcohol consumption both increase HDL levels
149
Statin drugs
Lower LDL by blocking synthesis of cholesterol by
the liver
– Does not affect dietary absorption of cholesterol
– Controversy over whether statins for older patients is
worthwhile (benefit of lower chol declines with age)
• Adverse effects:
– Myopathy, liver abnormalities
– GI disturbances, teratogenic (X)
• Generic names all end in “-statin”!
– lovastatin (Mevacor), pravastatin (Pravachol),
simvastatin (Zocor), atorvastatin (Lipitor)
150
Ezetimibe (Zetia)
Inhibits intestinal absorption of cholesterol
from diet
• Can be combined with statin drugs
– Vytorin is ezetimibe + simvastatin
151
EPO (erythropoietin)
```
Natural human protein that
stimulates production of red
blood cells
– Produced by genetic engineering
• Treatment of chronic anemia
– Also cancer patients with
anemia
• Abused by endurance athletes,
especially professional cyclists
```
152
Cholesterol-lowering drugs
```
statin drugs
– lovastatin, pravastatin,
atorvastatin
• Ezetemibe (Zetia)
• erythropoietin (EPO, Procrit)
```
153
CHF
-diuretics
• digoxin (digitalis)
• ACE inhibitors
• beta blockers
154
Angina
nitroglycerin
– Nitro-dur
• beta blockers
• Ca channel blockers
155
“-xaban” drugs
-apixaban (Eliquis), rivaroxaban (Xarelto)
-Specific, competitive inhibitors of factor Xa, Oral bioavailability
Antidote: andexanet alfa: Engineered protein based on factor Xa,
binds more tightly to drug than factor Xa does
156
Pradaxa (dabigatran)
| a specific thrombin inhibitor
Safer than coumadin?
– No particular dietary restrictions
• Frequent INR monitoring not needed
– Higher incidence of GI bleeds
– Similar heart attack risk
Uses: prevent heart attack, stroke, DVT, PE
– With atrial fibrillation, after joint replacement
Antidote: Praxbind (idarucizumab)
– Monoclonal antibody that binds/removes drug,
effective within minutes, approved 2015
