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Flashcards in Drugs Deck (214):
1

SSRI Mechanism

Inhibit re-uptake of Serotonin

2

SNRI Mechanism

Inhibit re-uptake of Serotonin and NE

3

TCA Mechanism

Inhibit re-uptake of Serotonin and NE

4

MAOI Mechanism

Inhibit MAO that metabolizes and breaks down Serotonin and NE

5

SSRI Drugs

Fluoxetine, Paroxetine, Sertraline, Citalopram

6

SNRI Drugs

Venlafazine, Duloxetine

7

TCA Drugs

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

8

MAOI Drugs

Tranylcypromine, Phenelzine, Isocarboxazid, Selegiline

9

Atypical Anti-Depressants

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)

10

Selegiline

MAO-B inhibitor that is used for Parkinson's

11

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

Trazodone

12

This anti-depressant lowers seizure threshold:

Bupropion

13

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

Trazodone

14

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

Mirtazapine (Remeron)

15

This anti-depressant can be used for smoking cessation:

Bupropion (Wellbutrin)

16

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

Imipramine

17

TCA overdose symptoms:

"Tri-C's"
Convulsions, Coma, Cardiotoxicity

18

Serotonin Syndrome symptoms:

Hyperthermia; Muscular rigidity, Cardiovascular collapse from autonomic instability

19

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

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

20

Methylphenidate used for...

Psychostimulant used for Narcolepsy, ADHD

21

Modafinil used for...

Narcolepsy, Circadian Rhythm Sleep Disorder

22

Opiate intoxication symptoms

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

23

Opiate withdrawal symptoms

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

24

Treatment for opiate intoxication

Naloxone, Naltrexone

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

183

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

186

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

187

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

188

Cisplatin
a. Mechanism
b. Use
c. Toxicity

a. Cross link DNA
b. Testicular, bladder, ovary, lung
c. NEPHROTOXICITY, ototoxicity

189

Etoposide, Teniposide
a. Mechanism
b. Use
c. Toxicity

a. Etoposide inhibits TOPOisomerase II --> increased DNA degradation
b. Solid tumors
c. Myelosuppression, GI upset, alopecia

190

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

191

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

199

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

201

Which protease inhibitor is known for inhibiting cytochrome P450 and boosting other drug concentrations?

Ritonavir

202

What are S/E of Protease inhibitors?

GI intolerance, Hyperglycemia, Lipodystrophy
Inhibit CYP450 - Ritonavir
Nephropathy, hematuria - Indinavir

203

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

204

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

205

NRTI drug examples?

Zidovudine, Tenofovir, Abacavir, Lamivudine, Didanosine, Emtricitabine

206

Which HIV drug is used for prophylaxis during pregnancy to decrease risk of transmission to fetus?

Zidovudine (NRTI)

207

S/E of NRTI drugs

BM suppression, peripheral neuropathy, lactic acidosis, anemia (Zidovudine), pancreatitis (Didanosine)

208

What are S/E of Zidovudine?

Megaloblastic anemia

209

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

211

S/E of NNRTIs

Rash, hepatotoxicity
Vivid dreams, CNS symptoms - Efavirenz
C/I in pregnancy - Efavirenz, Delavirdine

212

Mechanism of Raltegravir

Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase

213

Enfuvirtide mechanism and S/E

Binds gp41 and inhibits viral entry
S/E include skin reaction at injection site

214

Maraviroc mechanism

Binds CCR-5 on surface of T cells/monocytes and inhibits interaction with gp120