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1
Q

SSRI Mechanism

A

Inhibit re-uptake of Serotonin

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2
Q

SNRI Mechanism

A

Inhibit re-uptake of Serotonin and NE

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3
Q

TCA Mechanism

A

Inhibit re-uptake of Serotonin and NE

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4
Q

MAOI Mechanism

A

Inhibit MAO that metabolizes and breaks down Serotonin and NE

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5
Q

SSRI Drugs

A

Fluoxetine, Paroxetine, Sertraline, Citalopram

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6
Q

SNRI Drugs

A

Venlafazine, Duloxetine

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7
Q

TCA Drugs

A

Amitriptyline, Nortriptyline, Imipramine, Desipramine, Clomipramine, Doxepin, Amoxapine

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8
Q

MAOI Drugs

A

Tranylcypromine, Phenelzine, Isocarboxazid, Selegiline

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9
Q

Atypical Anti-Depressants

A

Bupropion - increase NE and Dopamine via unknown mechanism (smoking cessation, add-on to SSRI)
Mirtazapine - Alpha 2 antagonist that increases NE (depression, weight gain)
Trazodone - Blocks 5-HT2 and alpha 1 adrenergic receptors (Insomnia primarily; toxicity causes Priapism)

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10
Q

Selegiline

A

MAO-B inhibitor that is used for Parkinson’s

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11
Q

Priapism is a S/E of this anti-depressant:

A

Trazodone

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12
Q

This anti-depressant lowers seizure threshold:

A

Bupropion

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13
Q

This anti-depressant works well with SSRI and increases REM sleep

A

Trazodone

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14
Q

This anti-depressant is an appetite stimulant that results in weight gain:

A

Mirtazapine (Remeron)

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15
Q

This anti-depressant can be used for smoking cessation:

A

Bupropion (Wellbutrin)

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16
Q

This anti-depressant can be used for bed-wetting in children:

A

Imipramine

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17
Q

TCA overdose symptoms:

A

“Tri-C’s”

Convulsions, Coma, Cardiotoxicity

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18
Q

Serotonin Syndrome symptoms:

A

Hyperthermia; Muscular rigidity, Cardiovascular collapse from autonomic instability

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19
Q

What happens if you ingest Tyramine while on MAOI’s?

A

Hypertensive crisis because you cannot degrade Tyramine and it will be converted to NE that raises BP

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20
Q

Methylphenidate used for…

A

Psychostimulant used for Narcolepsy, ADHD

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21
Q

Modafinil used for…

A

Narcolepsy, Circadian Rhythm Sleep Disorder

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22
Q

Opiate intoxication symptoms

A

Euphoria, respiratory and CNS depression, pupillary constriction (pinpoint pupils), seizures

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23
Q

Opiate withdrawal symptoms

A

Sweating, dilated pupils, piloerection, rhinorrhea, yawning, diarrhea, stomach cramps, nausea,

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24
Q

Treatment for opiate intoxication

A

Naloxone, Naltrexone

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25
Treatment for opiate withdrawal
Methadone, Buprenorphine, Suboxone (Buprenorphine + Naloxone)
26
Measure of alcohol use
Serum gamma glutamyltransferase (GGT)
27
Alcohol withdrawal symptoms
Autonomic hyperactivity and DTs
28
Treatment for alcohol withdrawal
Benzodiazepines: Chlordiazepoxide, Lorazepam, Diazepam
29
Barbiturate intoxication symptoms
Respiratory depression
30
Barbiturate withdrawal symptoms
Delirium, life-threatening cardiovascular collapse
31
BDZ intoxication symptoms
Ataxia, minor respiratory depression
32
Treatment for BDZ intoxication
Flumazenil
33
BDZ withdrawal symptoms
Sleep disturbance, depression, rebound anxiety, seizure
34
Amphetamine intoxication symptoms
Euphoria, grandiosity, pupillary dilation, prolonged wakefulness and attention, HTN, tachycardia, anorexia, paranoia, fever Severe: cardiac arrest, seizure
35
Amphetamine withdrawal symptoms
Anhedonia, increased appetite, hyper somnolence, existential crisis
36
Cocaine intoxication symptoms
Pupillary dilation, hallucinations, paranoid ideations, angina, sudden cardiac death
37
Treatment for cocaine intoxication
BDZs, Haloperidol, alpha blockers
38
Cocaine withdrawal symptoms
Hypersomnolence, malaise, severe psychological craving, depression/suicidality
39
Treatment for Nicotine withdrawal
Bupropion/Varenicline, Nicotine patch
40
PCP Intoxication symptoms
Belligerence, psychomotor agitation, analgesia, vertical and horizontal nystagmus, tachycardia, violence, psychosis, delirium, seizures
41
Treatment for PCP intoxication
BDZs, rapid-acting antipsychotic
42
PCP Withdrawal symptoms
Depression, anxiety, irritability, restlessness, anergia, disturbances of thought and sleep, violence
43
LSD intoxication symptoms
Perceptual distortion (VISUAL), depersonalization, anxiety, paranoid, psychosis, flashbacks
44
Treatment for LSD intoxication
BDZ
45
Cannabinoid intoxication symptoms
Impaired judgement, social withdrawal, euphoria, perception of slowed time, increased appetite, dry mouth, conjunctival injection
46
What is Methadone?
Long-acting oral opiate used for heroin detoxification or long-term maintenance
47
What is Naloxone + Buprenorphine? Mechanism?
Suboxone = antagonist + partial agonist; Naloxone is not orally bioavailable so withdrawal symptoms occur only if injected
48
What is Naltrexone?
Long-acting opioid antagonist used for relapse prevention once detoxified
49
Alprazolam: a. Route of administration b. half life c. metabolism d. use
a. oral b. short duration c. (metabolized by CYP3A4) d. antipanic, anxiolytic
50
Diazepam: a. ROA b. half life c. metabolism d. use
a. oral b. fast onset of action and LONG half life c. (oxidation and glucuronidation); has active metabolites d. anxiety states, sleep disorders, muscle relaxant
51
Lorazepam a. ROA b. onset c. metabolism d. use
a. INTRAMUSCULAR b. slow onset (less lipophilic) c. no active metabolites, only glucuronidation d. anxiety AND sleep
52
Clonazepam | a. Use
a. Acute manic episodes
53
Chlordiazepoxide | a. Use
a. alcohol withdrawal
54
Benzodiazepines used for insomnia:
Flurazepam, Triazolam
55
Zolpidem mechanism
Non-BDZ; binds to BDZ receptor on GABA complex
56
Zaleplon mechanism
Non-BDZ; binds to BDZ receptor on GABA complex
57
Use of Zaleplon
Insomnia; more helpful for falling asleep than staying asleep because it has a short half life and action
58
Flumazenil
Antagonizes effects of BDZ; reduces seizure threshold thought so not used very often
59
Eszopliclone action and use
Interacts with GABA receptor complex; used for insomnia; this is Lunesta
60
Ramelteon action and use
Melatonin MT1 and MT2 receptor agonist; indicated for insomnia characterized by difficulty in falling asleep
61
Baclofen mechanism
GABA-mimetic agent that works at GABA B receptors (only one); causes presynaptic inhibition
62
Baclofen use
Muscle relaxant (as effective as Diazepam and produces less sedation)
63
Tizanidine mechanism
Alpha 2 adrenergic agonist related to Clonidine; may enhance both presynaptic and postsynaptic inhibition
64
Tizanidine use
Muscle relaxant
65
Atypical anti-psychotics used as adjunct in depression
Quetiapine, Olanzapine, Aripiprazole
66
Anti-psychotics used for Tourette's syndrome
Haloperidol, Pimozide (typical)
67
Anti-psychotic used for Schizoaffective disorder
Paliperidone (metabolite of Risperidone - atypical)
68
Misoprostol a. Mechanism b. Use c. Toxicity
a. PGE1 analog that increases production and secretion of gastric mucous barrier, decreased acid production b. Prevent NSAID induced peptic ulcers; (NSAIDS block PGE1 production); maintenance of PDA; off-label for induction of labor c. Diarrhea; C/I in women that are pregnant (abortifacient)
69
Octreotide a. Mechanism b. Use c. Toxicity
a. Long-acting Somatostatin analog; inhibits actions of splanchnic vasoconstriction hormones b. Acute variceal bleeds, acromegaly, VIPoma, Carcinoid tumors c. Nausea, cramps, steatorrhea
70
Antacid meds: a. Names b. Mechanism
a. Aluminum hydroxide, Calcium carbonate, Magnesium hydroxide b. Can affect absorption, bioavailability or urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying
71
Aluminum hydroxide toxicity
Constipation, hypophosphatemia, proximal muscle weakness, osteodystrophy, seizures
72
Calcium carbonate toxicity
Hypercalcemia that causes rebound acid secretion
73
Magnesium hydroxide toxicity
Diarrhea, hyporeflexia, hypotension, cardiac arrest (because it is a smooth muscle relaxer)
74
Sulfasalazine a. Mechanism b. Use c. Toxicity
a. Combo of Sulfapyridine (antibacterial) and 5-aminosalicylic acid (anti-inflammatory); activated by colonic bacteria b. Ulcerative colitis, Crohn disease c. Malaise, nausea, sulfonamide toxicity, reversible oligospermia
75
Osmotic laxatives a. Names b. Mechanism c. Use d. Toxicity
a. Mg hydroxide, Mg citrate, Polyethylene glycol, lactulose b. Provide osmotic load to draw water into GI lumen c. Constipation; Lactulose treats hepatic encephalopathy since it is degraded by gut flora into metabolites that promote nitrogen excretion as NH4+ d. Diarrhea, dehydration, may be abused by bulimics
76
H2 blockers a. Names b. Mechanism c. Use d. Toxicity
a. Cimetidine, Ranitidine, Famotidine, Nixatidine b. Reversible blocker of histamine H2 receptors that cause decreased acid secretion by parietal cells c. Peptic ulcer, gastritis, mild esophageal reflux d. Cimetidine is inhibitor of CYP450, has anti-androgenic effects; all of them can cause thrombocytopenia
77
Proton pump inhibitors a. Names b. Mechanism c. Use d. Toxicity
a. Omeprazole, Lansoprazole, Esomeprazole, Pantoprazole, Dexlansoprazole b. Irreversibly blocks H+/K+ ATPase in stomach parietal cells c. Peptic ulcer, gastritis, esophageal reflux, ZE d. Increased risk of C. difficile infection, pneumonia, long term use causes decreased serum Mg
78
Bismuth a. Mechanism b. Use
a. Binds to ulcer base to provide physical protection and allows bicarbonate secretion to reestablish pH gradient in mucous layer b. Increased ulcer healing, travelers diarrhea
79
Sucralfate a. Mechanism b. Use
Requires acidic environment to polymerize and binds ulcer base to provide physical protection b. Increased ulcer healing, travelers diarrhea (Similar to Bismuth)
80
Ondansetron a. Mechanism b. Use c. Toxicity
a. 5HT3 Serotonin receptor antagonist b. For post-op nausea, morning sickness or chemotherapy induced nausea c. Vasodilation --> headache, constipation
81
Metoclopramide a. Mechanism b. Use c. Toxicity
a. D2 receptor antagonist and 5HT4 agonist; increases resting tone, contractility, LES tone and motility b. Diabetic or post-surgery gastroparesis, anti-emetic c. Parkinsonian effects, tardive dyskinesia, restlessness, drowsiness, fatigue, depression, diarrhea
82
``` Prokinetic Agents (mechanism) 4 types ```
(Increased Ach, Increased 5-HT, Decreased dopamine) 1. Cholinergic agonists (Bethanechol) 2. Acetylcholinesterase inhibitors (Neostigmmine) 3. Metoclopramide (+ 5HT and - D2) 4. Macrolides - stimulate smooth muscle motilin receptors
83
Prodrug of 6-mercaptopurine
Azathioprine
84
Drug that causes phocomelia
Thalidomide
85
Drug that is nephrotoxic in 75% of patients
Cyclosporine
86
S/E's include: acne, osteoporosis, HTN, hyperglycemia, immunosuppression --> infection
Glucocorticoids
87
Inhibits secretion of IL-2 and other cytokines
Tacrolimus
88
What is Neostigmine?
Indirect cholinergic agonist (anti-cholinesterase) used for neurogenic ileum, post-op reversal of NMJ blockade, treatment for myasthenia gravis
89
What is Pyridostigmine?
Indirect cholinergic agonist used for myasthenia gravis
90
What is Edrophonium?
Indirect cholinergic agonist used for diagnosis of Myasthenia gravis
91
What is Physostigmine
Indirect cholinergic agonist used for atropine overdose
92
What are Donepezil, Rivastigmine, and Galantamine?
Indirect cholinergic agonist used for Alzheimer's
93
a. What is Procainamide? b. What is it used for? c. What toxicity can it cause?
a. Class IA anti-arrhythmic b. Wolf Parkinson White syndrome c. Reversible SLE like syndrome
94
a. What is Quinidine? | b. What are toxic side effects of Quinidine?
a. Class IA anti-arrhythmic | b. Cinchonism (headache, dizziness, tinnitus), Thrombocytopenia, Torsades de Pointes
95
a. What is Lidocaine? | b. What is it used for?
a. Type IB anti-arrhythmic | b. Acute ventricular tachyarrhythmias, digitalis-induced arrhythmias, tachyarrhythmias post-MI
96
a. What arrhythmias are beta blockers used for? b. What are the adverse reactions of beta blockers? c. What is their mechanism?
a. SVT, ventricular rate control for atrial fibrillation and atrial flutter b. Bradycardia, AV block, HF exacerbation, asthma, mask effects of hypoglycemia c. Decrease SA and AV nodal activity by decreasing cAMP and Ca currents. They suppress abnormal pacemakers by decreasing the slope of phase 4.
97
a. What is the mechanism of K channel blockers? (type III anti-arrhythmics) b. What are they? c. What is their use? d. What are their adverse reactions?
a. Work at phase 3 to increase to block K depolarization so that AP duration is increased, ERP is increased and QT interval is increased b. Amiodarone, Ibutilide, Dofetilide, Sotalol (AIDS) c. Atrial fibrillaiton, atrial flutter, ventricular tachycardia (Amiodarone used for WPW) d. Torsades de pointes for all Amiodarone causes pulmonary fibrosis, hepatotoxicity, hypo/hyper thyroidism, photosensitivity, bradycardia, neurologic effects, constipation
98
What labs should you check when using Amiodarone?
PFTs (pulmonary fibrosis) LFTs (hepatotoxicity) TFTs (hypo or hyperthyroid - amiodarone is 40% iodine)
99
What drugs cause photosensitivity?
Sulfonamides Amiodarone Tetracycline
100
a. What is the effect of Calcium channel blocker anti-arrhythmics? b. What are they used for? c. What is their toxicity?
a. Cause slow rise of action potential that results in decreased conduction velocity, increased ERP, increased PR interval b. Prevention of nodal arrhythmias, rate control in atrial fibrillation c. Constipation, flushing, edema, CV effects (heart block, HF)
101
a. What is the drug of choice for supra ventricular tachycardia? b. How does it work?
a. Adenosine b. Causes increase K efflux that hypoerpolarizes cell and decreases Ca influx. Very SHORT acting - can't depolarize at all
102
What drugs block the affects of Adenosine?
Theophylline (asthma or COPD patients) | Caffeine
103
How is Mg used for arrhythmias?
Effective in torsades de points and digoxin toxicity
104
Which anti-arrhythmic has the side effect of Cinchonism? What is Cinchonism?
Quinidine; headache and tinnitus
105
What effects will a noncompetitive antagonist have on Vmax and Km?
Vmax will be lower and no effect on Km
106
What is the vasopressor of choice for a. anaphylactic shock? b. cardiogenic shock? c. septic shock
a. Epinephrine b. Dobutamine - because it stimulates Beta 1 receptors c. Norepinephrine because it stimulates alpha 1 without beta 2
107
What are the lengths of the preganglionic and postganglionic sympathetic fibers?
Short preganglionic - close to spine, secrete Ach | Long post ganglionic - secrete NE
108
What do alpha 1 receptors cause?
Increased peripheral resistance | Increased bladder sphincter tone
109
What do alpha 2 receptors cause?
Inhibition of NE release on presynaptic neuron
110
What do beta 1 receptors do?
Increase HR and contractility
111
What do beta 2 receptors do?
Mild vasodilation | Bronchodilation
112
a. What are nonselective alpha blockers? | b. What are they used for?
a. Phenoxybenzamine (irreversible); for Pheochromocytoma | b. Phentolamine (reversible); given to patients on MAO inhibitor who eat foods with tyramine
113
What are side effects of non-selective alpha blockers?
Orthostatic hypotension | Reflex tachycardia
114
a. What are selective a1 blockers? | b. What are they used for?
a. Prazosin, Terazosin, Doxazosin, Tamsulosin | b. Urinary symptoms of BPH, Prazosin for PTSD, HTN (except not Tamsulosin)
115
What are side effects of Prazosin, Terazosin and Tamsulosin?
Orthostatic hypotension Rebound hypotension when you stop Dizziness, headache Reflex tachycardia
116
What is mechanism of Tamsulosin?
Selective Alpha 1A,D blocker
117
a. What is mechanism of Mirtazapine? | b. What is it used for?
a. Alpha 2 receptor blocker | b. Depression
118
What are the non-selective beta blockers?
Nadolol, Propranolol, Timolol
119
What are the B1 selective blockers?
Acebutolol, Atenolol, Betaxolol, Esmolol, Metoprolol
120
What are non selective alpha and beta blockers?
Carvedilol, Labetalol
121
When would you use Acebutolol or Pindolol over other beta blockers? Why?
In patients with HTN and bradycardia; they are weak B1 and B2 agonists (partial agonists) so they don't have the same effect on HR
122
What are therapeutic uses for beta blockers?
``` HTN - drug of choice for aortic dissection MI, angina, SVT, HF Glaucoma Hyperthyroidism Migraine prophylaxis Anxiety ```
123
What are adverse effects of beta blockers?
Bronchoconstriction - from Beta 2 block Prevent symptoms of hypoglycemia! Avoid in cocaine users!! because cocaine causes stimulation of all adrenergic receptors (indirectly from reduced uptake of catecholamines) and blocking beta receptors = unopposed alpha 1 receptors --> increase BP
124
What beta blockers are used for Glaucoma?
Timolol, Nadolol
125
a. What is Clonidine mechanism? b. What is it used for? c. Toxicity
a. alpha 2 agonist --> act centrally to decrease release of NE from presynaptic neuron b. Malignant HTN (outpatient), ADHD, Tourette syndrome c. Rebound HTN when stopped, CNS depression, bradycardia, hypotension, respiratory depression, mitosis
126
a. Methyldopa mechanism b. Use c. Toxicity
a. Alpha 2 agonist; decrease NE from presynaptic terminal b. HTN in pregnancy c. SLE like syndrome;
127
In which patients are beta blockers C/I?
Diabetics COPD/Asthma Cocaine users Bad/uncontrolled CHF
128
Opioid used in treatment of diarrhea
Loperamide, Diphenoxylate
129
Non-addictive weak opioid agonist
Tramadol
130
Partial opioid agonist that causes less respiratory depression
Butorphanol
131
What does Metyrosine do?
Inhibits conversion of Tyrosine to DOPA
132
What does Reserpine do?
Inhibits packaging of NE into vesicles
133
What does Hemicholinium do?
Inhibits transport of choline into cholinergic nerve terminal
134
What does Vesamicol do?
Inhibits storage of Ach into vesicles
135
What drugs can inhibit release of NE from noradrenergic synapse?
Bretylium - K channel blocker | Guanethidine
136
What drugs can stimulate release of NE from noradrenergic synapse?
Amphetamine Ephedrine Tyramine
137
What are other presynaptic receptors that regulate release of NE?
M2 receptors - inhibit release of NE (parasympathetic) | De receptors - inhibit release of NE AT2 receptor - stimulate release of NE
138
Which drugs inhibit reuptake of NE?
Cocaine | TCA drugs
139
How does COMT metabolize NE?
It methylates NE - (it's Catechol-O-methyl transferase)
140
How does MAO metabolize NE?
It oxidizes it
141
What are the actions of these drugs on Ach or NE: a. Amitriptyline b. Amphetamine c. Black widow spider toxin d. Botulinum toxin e. Bretylium f. Cocaine g. Gunaethidine h. Hemicholinium i. Reserpine j. Vesamicol
a. Inhibits NE reuptake b. Stimulates NE release c. Stimulates Ach release d. Inhibits Ach release e. Inhibits NE release f. Inhibits NE reuptake g. Inhibits NE release h. Inhibits choline transport i. Inhibits NE packaging j. Inhibits Ach packaging
142
Which diuretic is used for pseudo tumor cerebri?
Acetazolamide
143
What are the two types of cholinergic receptors?
1. Nicotinic - ligand gated ion channels (DON'T use G proteins) 2. Muscarinic - G protein linked receptors
144
What are the Muscarinic receptors and what are their actions?
M1 - enteric nervous system M2 - decreased HR and contractility of atria (SA node) M3 - increase bladder contraction, gut peristalsis and lacrimation, miosis, bronchoconstriction
145
What are the adrenergic receptors? And what do they cause?
alpha 1 - vasoconstriction, smooth muscle contraction alpha 2 - presynaptic auto receptors that inhibit NE release beta 1 - increase HR and myocardial contractility beta 2 - vasodilation and bronchodilation
146
Besides adrenergic and muscarinic cholinergic (not nicotinic) receptors, which other receptors are G protein linked?
Dopamine receptors Histamine receptors Vasopressin receptors (ADH)
147
What do D1 receptors cause?
Relax renal vascular smooth muscle
148
Where are D2 receptors found?
Brain
149
What do H1 receptors cause?
Nasal secretions Bronchial mucus production Pruritis Bronchoconstriction
150
What do H2 receptors cause?
Increased gastric acid secretion
151
What do V1 receptors do?
Increased vascular smooth muscle contraction
152
What do V2 receptors do?
Increase reabsorption in collecting tubules of the kidney
153
What do M1 M2 and M3 receptors respond to?
Ach
154
What do a1 a2 B1 and B2 receptors respond to?
NE, Epi
155
What does Gq do?
It activates phospholipase C --> acts on PIP2 and cleaves it into DAG and IP3 - DAG activates Protein Kinase C - IP3 increases intracellular Calcium --> smooth muscle contraction
156
What is the mnemonic for Gq receptors? Which ones are Gq receptors?
Cutesies (QC) HAVe 1 M&M H1, alpha1, V1 M1, M3
157
What does Gs do?
Gs --> stimulates adenylyl cyclase --> converts ATP to cAMP --> cAMP activates Protein Kinase A (PKA) --> increase in Ca in heart
158
What does Gi do?
Inhibits adenylyl cyclase --> inhibits production of cAMP --> no production of PKA --> no increase in Ca
159
What is mnemonic for Gi?
MAD 2s | M2 alpha 2 D2
160
Which G protein does the following: a. activates PKA b. less activation of PKA c. activates PKC d. activates Phospholipase C e. increases Calcium f. increases cAMP g. decreases cAMP h. inhibits adenylyl cyclase i. stimulates adnylyl cyclase j. PIP2--> IP3 + DAG
a. Gs b. Gi c. Gq d. Gq e. Gs, Gq f. Gs g. Gi h. Gi i. Gs j. Gq
161
Clopidogrel
ADP receptor inhibitor
162
Prasugrel
ADP receptor inhibitor
163
Ticagrelor
ADP receptor inhibitor (reversible)
164
Ticlodipine
ADP receptor inhibitor (causes Neutropenia)
165
Cilostazol
Phosphodiesterase III inhibitor (increases cAMP in platelets resulting in inhibition of platelet aggregation)
166
Dipyridamole
Phosphodiesterase III inhibitor (increases cAMP in platelets resulting in inhibition of platelet aggregation)
167
GP IIb/IIIa inhibitors | Mechanism and Use
Eptifibatide, Abciximab, Tirofiban They bind to the GP IIb/IIIa receptor on activated platelets and prevent aggregation Used for unstable angina, PTCA
168
Nucleotide synthesis inhibitors (drugs and mechanisms)
1. Methotrexate - folic acid analog that inhibits dihydrofolate reductase 2. 5-FU - pyrimidine analog activated to 5-dUMP that complexes folic acid and inhibits thymidylate synthase 3. 6-Mercaptopurine (Azathioprine is metabolized to 6-MP); Purine analog that inhibits de novo purine synthesis 4. Hydroxyurea inhibits ribonucleotide reductase 5. Cytarabine is a pyrimidine analog that inhibits DNA polymerase
169
What drugs have increased toxicity when taken with Allopurinol or Febuxostat?
Azathioprine, 6-MP; they are both metabolized by Xanthine Oxidase
170
What drug treats Hairy Cell Leukemia?
Cladribine (purine analog that has multiple mechanisms)
171
Clinical use of 5-FU
Basal cell carcinoma | Actinic keratosis
172
What is the rescue agent of 5-FU?
Uridine (because 5-FU is a pyrimidine analog that is activated to 5F-dUMP which binds folic acid and inhibits thymidylate synthase --> decreased dTMP --> decreased DNA synthesis)
173
Clinical use of Methotrexate
Cancer: Leukemia, Lymphoma, Choriocarcinoma Ectopic pregnancy, medical abortion RA, psoriasis, IBD, vasculitis
174
How do you reverse Methotrexate toxicity?
Leucovorin
175
Which cancer drugs inhibit the M phase of cell cycle?
Paclitaxel Vinblastine Vincristine
176
Bleomycin a. Mechanism b. Use c. Toxicity
a. Induces free radical formation --> breaks in DNA strands b. Testicular cancer, Hodgkin lymphoma c. PULMONARY FIBROSIS, skin hyper pigmentation, mucositis
177
Dactinomycin a. Mechanism b. Use c. Toxicity
a. Intercalates in DNA b. CHILDhood tumors; Wilms tumor, Ewing sarcoma, Rhabdomyosarcoma c. Myelosuppression
178
Doxorubicin, Daunorubicin a. Mechanism b. Use c. Toxicity
a. Generate free radicals, intercalate into DNA and cause DNA breaks b. Solid tumors, leukemias, lymphomas c. Cardiotoxicity (dilated cardiomyopathy)
179
Why is the heart susceptible to Doxorubicin?
The heart has a deficiency in superoxide dismutase and therefore has greater susceptibility to free radicals
180
What can be given to prevent cardiotoxicity with Doxorubicin or Daunorubicin?
Dexrazoxane (iron chelating agent)
181
Busulfan a. Mechanism b. Use c. Toxicity
a. Cross-links DNA b. CML c. PULMONARY FIBROSIS, hyperpigmentation, myelosuppression
182
Cyclophosphamide a. Mechanism b. Use c. Toxicity
a. Cross links DNA at guanine N-7. b. Solid tumors, leukemia, lymphomas c. Myelosuppression, HEMORRHAGIC CYSTITIS
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Nitrosureas a. Mechanism b. Use c. Toxicity
a. Require bioactivation (CROSS BLOOD BRAIN BARRIER) b. Brain tumors c. CNS toxicity
184
Why are Nitrosureas useful for brain tumors?
They cross the blood brain barrier and enter the CNS
185
How do you prevent hemorrhagic cystitis from Cyclophosphamide?
Mesna
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Paclitaxel a. Mechanism b. Use c. Toxicity
a. Hyperstabilizes polymerized microtubules in M phase so that mitotic spindle cannot break down b. Ovarian and breast carcinomas c. MYELOSUPPRESSION
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Vincristine, Vinblastine a. Mechanism b. Use c. Toxicity
a. Bind Beta tubulin and inhibit it's polymerization into microtubules --> prevents mitotic spindle formation b. Solid tumors, Leukemias, Hodgkin (vinB) and non-Hodgkin (vinC) lymphomas c. Vincristine - PERIPHERAL NEURITIS, Vinblastine - MARROW SUPPRESSION
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Cisplatin a. Mechanism b. Use c. Toxicity
a. Cross link DNA b. Testicular, bladder, ovary, lung c. NEPHROTOXICITY, ototoxicity
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Etoposide, Teniposide a. Mechanism b. Use c. Toxicity
a. Etoposide inhibits TOPOisomerase II --> increased DNA degradation b. Solid tumors c. Myelosuppression, GI upset, alopecia
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Irinotecan, Topotecan a. Mechanism b. Use c. Toxicity
a. Inhibits topoisomerase I and prevents DNA unwinding/replications b. Colon cancer (irinotecan), ovarian and small cell lung cancers (topotecan) c. Severe myelosuppression, diarrhea
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Hydroxyurea a. Mechanism b. Use c. Toxicity
a. Inhibits ribonucleotide reductase b. Sickle cell, Melanoma, CML c. Severe myelosuppression, GI upset
192
Bevacizumab mechanism
Monoclonal antibody against VEGF
193
Erlotinib mechanism
EGFR tyrosine kinase inhibitor (used for non-small cell lung cancer)
194
Imatinib mechanism
Tyrosine kinase inhibitor of BCR-ABL (used for CML)
195
Rituximab mechanism
Monoclonal Ab against CD20 (used for non-Hodgkin lymphoma, CLL)
196
Tamoxifen, Raloxifene mechanism
Estrogen receptor antagonists in breast and agonists in bone
197
What is an increased risk with Tamoxifene? Why?
Endometrial cancer; Tamoxifen is partial agonist in endometrium --> causes endometrial hyperplasia
198
Trastuzumab mechanism
Monoclonal Ab against HER-2 (tyrosine kinase) --> for HER2 positive breast cancer and gastric cancer
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Trastuzumab toxicity
Cardiotoxicity
200
Mechanism of Protease inhibitors? What do they all end in?
They inhibit the cleavage of polypeptide products of HIV mRNA into their functional parts (prevent maturation of new virus) - All end in -NAVIR
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Which protease inhibitor is known for inhibiting cytochrome P450 and boosting other drug concentrations?
Ritonavir
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What are S/E of Protease inhibitors?
GI intolerance, Hyperglycemia, Lipodystrophy Inhibit CYP450 - Ritonavir Nephropathy, hematuria - Indinavir
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What drug is C/I in patients taking protease inhibitors? And why?
Rifampin; it can decrease protease inhibitor concentration because it is a CYP/UGT inducer
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Mechanism of NRTIs
COMPETITIVELY inhibits nucleotide binding to reverse transcriptase and terminates the DNA chain - they are nucleoside (Tenofovir is nucleotide) analogs and need to be PHOSPHORYLATED to be active
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NRTI drug examples?
Zidovudine, Tenofovir, Abacavir, Lamivudine, Didanosine, Emtricitabine
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Which HIV drug is used for prophylaxis during pregnancy to decrease risk of transmission to fetus?
Zidovudine (NRTI)
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S/E of NRTI drugs
BM suppression, peripheral neuropathy, lactic acidosis, anemia (Zidovudine), pancreatitis (Didanosine)
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What are S/E of Zidovudine?
Megaloblastic anemia
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S/E of Didanosine?
Pancreatitis (It's a NRTI)
210
NNRTI mechanism and drugs?
Bind to reverse transcriptase; NON competitively inhibits; and do NOT require phosphorylation to be active or compete with nucleotides; Efavirenz, Delavirdine, Nevirapine
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S/E of NNRTIs
Rash, hepatotoxicity Vivid dreams, CNS symptoms - Efavirenz C/I in pregnancy - Efavirenz, Delavirdine
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Mechanism of Raltegravir
Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase
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Enfuvirtide mechanism and S/E
Binds gp41 and inhibits viral entry | S/E include skin reaction at injection site
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Maraviroc mechanism
Binds CCR-5 on surface of T cells/monocytes and inhibits interaction with gp120

Step 1 AB (29 decks)

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