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1

Vasodilation mechanism

Endothelial cells have muscarinic receptors; cholinergic agonist bind -> release of NO (EDRF) -> guanylate cyclase -> dec. Ca2+ -> decreased activity of myosin light-chain kinase --> myosin light chain DEphosphorylation and SMC relaxation

2

Order the insulins in terms of earliest to latest peak

Aspart/lispro/glulisine, regular, NPH, detemir, glargine

3

Lithium toxicity symptoms? tx

Tremors, fascicular twitching, agitation, ataxia, delirium; tx with hemodialysis for acute. Can also cause hypothyroidism and nephrogenic diabetes inspidus.

4

Drugs that could increased Li levels?

Thiazides (increased proximal Na reabsorption as compensation to distal effects), ACEi, NSAIDs

5

Name the short benzos?

Alprazolam (Xanax), Triazolam, Oxazepam.
OATs. Tri- and eat your OATs quickly in the morning.

6

Name the long benzos?

Chlordiazepoxide (Librium), Diazepam (Valium), Flurazepam, Clorazepate. Long view: Libreate and Valor.

7

Name the medium benzos?

Lorazepam (Ativan), estazolam, temazepam.
live and LET die. Medium-lvl bond movie.

8

Reverse benzos with?

Flumazenil

9

Acute neonatal narcotic withdrawal?

Pupillary dilation, rhinorrhea, sneezing, d, n/v, chills. tx = diluted tincture of opium

10

Dobutamine?

B-adrenergic agonist B1>B2 --> Positive inotropy, weakly positive chronotropic, increases conduction velocity (arrhythmias), increases myocardial oxygen consumption

11

Anticholinergic toxicity?

Fever, mucosal/axillary dryness, cutaneous flushing, mydriasis (big), cycloplegia, delirium. e.g. TCA's, atropine

12

What drugs more effective against HSV and VZV than CMV/EBV?

Acyclovir, famciclovir, valaciclovir. B/c dependnet on a thymidine kinase to turn into active triphosphate form.

13

Protease inhibitors?

Squinavir, ritonavir

14

Fusion inhibitors

Enfuvirtide

15

RT inhibitors

Efavirenz (NNRTI), tenofovir, lamivudine

16

Integrase inhibitors

Raltegravir

17

CCR5 receptor inhibitors

Maraviroc

18

Surgery + liver damage?

Inhaled anesthetics (e.g. halothane) associated w/ highly lethal fulminant hepatitis - aminotransferase, PTT inc, eosinophilia

19

Finasteride

Blocks peripheral conversion of testosterone to DHT

20

Flutamide/Cyproterone

Androgen hormone-receptor blocker

21

-mab's

Monoclonal Ab

22

-cept's

Receptor molecules

23

-nib's

Kinase inhibitor

24

Origin substem for -mab's

Mouse (-o-), Human (-u-), Chimeric w/ foreign variable (-xi), Humanized w/ completementarity determining regions (-zu), chimeric/humanized hybrid (-xizu)

25

Statin + fibrates

Myopathy risk. Simvastatin has highest risk.

26

Varenicline?

Partial agonist to nicotinic ACh receptors -> reduced nicotine withdrawal and reduced reward. (A4B4 nicotinic receptor)

27

Efficacy vs. potency

Efficacy = intrinsic ability of drug to elicit an effect (maximum effect). E.g. analgesics, abc, antihistamines, decongestants. Potency = dose of drug required to produce a given affect (Km related). Highly potent drugs include chemo, antiHTN, lipid-lowering. Potent dose, Kim! Max, more efficacious please.

28

HCTZ effects

Diuretic. Also side effect = increased Calcium absorption. Therefore, a nice drug for older women with HTN.

29

Pentazocine

Opioid designed for decreased abuse. Partial agonist and weak antagonist at mu receptors. Can lead to withdrawal symptoms in patients who are dependent on opioids.

30

Opioid administration -> sudden RUQ pain?

Biliary colic induced by contraction of SMC.

31

ACEi side effects

Decreased GFR (only care if Cr >30%), hyperKalemia, cough. Angioedema is rare but life-threatening.

32

Lamotrigine side effects

Used for refractor partial sz, generalized tonic-clonic, bipolar. Life-threatening HS reaction that manifests as skin rash = Stevens-Johnson

33

Thioridazine SE

retinal deposits that look like retinitis pigmentosa

34

Chlorpromazine SE

Corneal deposits.

35

Common drug interactions in serotonin syndrome

SSRIs, SNRIs, MAOIs, TCAs, Tramadol, Ondansetron, Linezolid, Triptans

36

Thionamides

Methimazole and propylthiouracil. Inhibit thyroid peroxidase (which oxidizes iodine).

37

What is half-life given Vd and clearance?

t1/2 = (Vd x 0.7) / clearance

38

Efficacy vs. potency

Efficacy = intrinsic ability of drug to elicit an effect (maximum effect). E.g. analgesics, abc, antihistamines, decongestants. Potency = dose of drug required to produce a given affect (Km related). Highly potent drugs include chemo, antiHTN, lipid-lowering. Potent dose, Kim! Max, more efficacious please.

39

Vd = ?

= amount of drug given (mg) / plasma concentration of drug (mg/L) = theoretical volume occupied by total absorbed drug amount at plasma concentration.

40

CYP 450 Inducers

Chronic alcohol, Modafinil, St. John's wort, Phenytoin, Phenobarbital, Nevirapine, Rifampin, Griseofulvin, Carbamazepine. "Grisly St. John Nevir Riffs the Phen-Phen w/o Carbs, Chronic Alcohol, or Modafinil."

41

CYP 450 inhibitors

Acute alcohol, Gemfibrozil, Ciprofloxacin, INH, grapefruit, quinidine, amiodarone, ketoconazole, macrolides, sulfonamides, cimetidine, ritonavir. "'Cip A-Cute Macro Grapefruit at the NIH,' (w)Rit an Amiable Keto Quinn w/ a Sulfur-colored Gem'd Cimetar."

42

Two major variables in M-M kinetics?

Km = 1 / affinity. Vmax is proportional to enzyme concentration. At Km concentration, 1/2 Vmax velocity.

43

Lineweaver-Burk

y-intercept = 1/Vmax. X-intercept = -1/Km (Closer to 0, greater the Km, weaker affinity)

44

Competitive vs. non-competitive inhibitors on Lineweaver-Burk

Competitive inhibitors do NOT affect Vmax = same y-intercept. Non-comp inhibitors do NOT affect affinity -> same x-intercept

45

Reversible, non-reversible comp inhibitors, and non-comp inhibitors potency vs. efficacy?

Reversible comp - don't change Vmax but change Km. decreased potency. Non-reversible competitive and non-competitive inhibitors change Vmax -> decrease efficacy.

46

Pharmacokinetics vs. Pharmacodynamics

Kinetics are body's effect on drug. ADME = absorption, distribution, metabolism, excretion. Dynamics is affect of drug on body - receptor binding, efficacy, potency, toxicity.

47

Bioavailability

Fraction (F) of drug that reaches systemic circulation unchanged. IV is 100%.

48

Low, Middle, High Vd tells you what?

Vd is LOW (4-8L) if drug remains in plasma (bound to plasma proteins, hydrophilic b/c charged). High Vd (e.g. 41) are small MW AND uncharged; in all tissues + fat. Medium Vd (teens) for small MW and hydrophilic b/c in interstitium (ECF). High Vd drugs tend to be cleared hepatically.

49

What do I need to know about half-life?

t1/2 = 0.7 x Vd / clearance. Drug infused at constant rate takes 4-5 half-lives to reach SS. (3.3 half-lives to reach 90% of SS). 1:50% remaining, 2:25%, 3:12.5%, etc.

50

Clearance

Volume of plasma cleared of drug per unit time = rate of elimination of drug / plasma concentration = Vd x Ke (elimination constant)

51

Loading dose calculation

Cp x Vd / F where Cp = target plasma concentration at SS.

52

Maintenance dose calculation

Cp x CL x tau / F where tau = dosage interval.

53

Zero-order elimination vs. 1st-order elimination

Constant rate of elimination (e.g. PEA - Phenytoin, Ethanol, Aspirin) vs. constant fraction is eliminated

54

Trapping drugs in urine?

Ionized forms are trapped and cleared quickly. Weakly acidic drugs (e.g. phenobarbital, MTX, ASA) can be cleared with bicarbonate. Weakly basic drugs (e.g. amphetamines) can be cleared with ammonium chloride.

55

Phase I vs. phase II drug metabolism.

I - CYP450 reduction, oxidation, and hydrolysis leading to slightly polar, water-soluble metabolites. II - GAS (Glucorinidation, Acetylation, and Sulfation) leading to VERY polar, inactive metabolites.

56

Therapeutic index

TITE = TD50/ED50 = median toxic dose / median effective dose. Higher therapeutic index is a SAFER drug.

57

Sympathetic vs. parasympathetic pathway for cardiac and smooth muscle, gland cells, and nerve terminals

Sympathetic - pre-ganglion to chain (ACh). Post-ganglion to muscle (NE, alpha and beta adrenergic receptors). Parasympathetic - pre-ganglionic from medulla. Synapse (ACh), then post-ganglion to muscle (ACh, M receptor)

58

Sympathetic sweat glands pathway?

Chain w/ ACh. Post-ganglionic w/ ACh, M.

59

Sympathetic renal vasculature pathway?

Chain w/ ACh. Post-ganglionic with D, D1. Kidneys are dope, sweat is musty, and the rest is adrenergic.

60

Adrenal medulla pathway?

Directly ACh -> Epi and NE release

61

Nictonic vs. Muscarinic receptors?

Both are ACh receptors. N are ligand-gated Na+/K+ channels. Nn in autonomic ganglia. Nm in NMJ. Muscarinic receptors are GPCRs that act thru 2nd messengers. M1-5.

62

Dopamine GPCRs?

D1 - Gs, relaxes renal vascular SMC. D2 - Gi, modulates transmitter release (esp. brain). Kidneys are DOPE. Brain is okay.

63

Histamine GPCRs

H1 - Gq, increase mucus production, vascular permeability,, contraction of bronchioles, pruritus and pain. H2 - Gs, increased gastric acid secretion. H1 is allergies. H2 is ranitidine.

64

Vasopressin GPCRs

V1 - Gq, increased vascular SMC contraction. V2 - Gs, increased water permeability and reabsorption in collecting tubules of kidney.

65

Parasympathetic GPCRs

M1 - Gq, CNS and enteric (brain is first). M2 - Gi, decreased HR and contractility of atria (heart is second). M3 - Gq, inc. exocrine gland secretion, inc. peristalsis, inc. bladder contraction, bronchoconstriction, miosis, accomodation

66

Sympathetic GPCRs

a1- Gq, vasc SMC contraction, mydriasis, increased intestinal and bladder sphincter contraction. a2 - Gi, decreased sympathetic outflow, decreased insulin, dec lipolysis, inc. PLT aggregation. B1 - Gs, inc HR, inc contractility, inc renin (juxtaglomerular), inc lipolysis. B2 - Gs, vasodilation, bronchodilation, inc HR, inc contractility, inc lipolysis, inc insulin, TOCOlysis, ciliary muscle relaxation (un-accmodate), inc. aqueous humor

67

Acronym for GPCR systems

Sympathetics, Parasympathetics (M1-M3), Dopamine, Histamine, Vasopress. Qiss and Qiq till your siq of sqs

68

Amphetamines

Activates NE release and inhibits reuptake. For narco, obesity, ADHD

69

NE reuptake inhibitors

Amphetamines, cocaine, TCAs

70

Modulation of NE release?

NE negatively feedbacks via alpha-2 receptors. Angiotensi-II activates NE release.

71

Where do ACh esterase inhibitors act?

Post-synaptic membrane

72

Gq GPCR receptors?

HAVe 1 M&M - H1, alpha1, V1, M1, M3

73

Gi GPCR receptors?

MAD 2's - M2, alpha2, D2

74

Cholinomimetic agents

Bethanechol, carbachol, pilocarpine, methacholine.

75

Bethanechol

Postop ileus, neurogenic ileus, urinary retention. Activates Bowel and Bladder SMC. Resistant to AChe. Bethany, let it go!

76

Carbachol

Glaucoma, pupillary constriction, intraocular pressure.

77

Pilocarpine

Stimulator of sweat, tears, saliva. Open (contracts ciliary muscle) and closed-angle glaucoma (constricts pupillary sphincter).

78

Methacholine

Asthma challenge.

79

Indirect agonists for ACh

Neostigmine, Pyridostigmine, Physostigmine, Donepezil/rivastigmine/galatamine, Edrophonium

80

Neostigmine

Post-op and neurogenic ileum, urinary retention, myasthenia gravis, reverse NMJ blockade. Neo = NO CNS penetration.

81

Pyridostigmine

Long-acting for Myasthenia. No CNS. Gets RID of Myasthenia Gravis. Physostigmine gets rid of the stigma f ACh poisoning.

82

Physostigmine

ACh toxicity (Crosses CNS)

83

Cholinesterase inhibitor poisoning

DUMBBELSS - Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of m. and CNS, Lacrimation, Sweating, Salivation. Tx = atropine (Ach antagonist working on M receptors only; won't reverse muscle paralysis based on Nicotnic receptors) + pralidoxime (AChE regenerator)

84

GU Muscarinic antagonists

Reduce urgency in mild cystitis and bladder spasms. Oxybuynin, darifenacin, solifenacin

85

Respiratory muscarinic antagonists

Ipratropium, tiotropium - COPD, asthma

86

CNS muscarininc antagonists

Benztropine for Parkinsons. Scopolamine for motion sickness.

87

GI, resp muscarininc antagonist

Glycopyrrolate - reduce airway secretions, drooling tx, peptic ulcer tx

88

Atropine effects

Pupil dilation, cycloplegia, dec. airway secretions, dec. acid secretions, decreased motility, decreased urgency in cystitis. Used for heart block.

89

Atropine toxicity

Hot as hare, Dry as bone, Red as beet Blind as a bat (cycoplegia), Mad as a hatter.

90

Epinephrine

B > alpha. Inds - anaphylaxis, OA-glaucoma, asthma, hypotension

91

Norepinephrine

alpha1>alpha2>beta. Use for hypotension (but decreased renal perfusion)

92

Isoproterenol

B1=B2. Beta2-mediated vasodilation -> dec. pressure -> increased HR. Inds - for evaluating tachyarrhythmias.

93

Dopamine

D1 = D2 > Beta > alpha. Ind for unstable bradycardia, HF, shock. Inotropic and chronotropic alpha effects at high doses. Low dose - vasodilation to renal and mesenteric vasculature. Higher doses - inotrope via B1. Higher doses - generalized vasoconstriction via alpha-1.

94

Dobutamine

Beta1 > Beta2, alpha. HF, cardiac stress testing

95

Phenylephrine

alpha1 > alpha2. Hypotension, mydriasis, rhinitis (Decongestant)

96

Albuterol, salmeterol, terbutaline

B2 > B1. Acute asthma, COPD. Terbutaline for tocolysis in premature contractions.

97

Ephedrine

Nasal decongestion, urinary incontinence, hypotension

98

Sympatholytics

alpha-agonists. Clonidine and alpha-methyldopa.

99

Clonidine

Clonidine is used for HTN urgency, ADHD, severe pain. Toxicities include CNS depression, brady, hypo, resp depression, miosis.

100

alpha-methyldopa

Used for HTN in pregnancy. Tox -> Direct Coombs + hemolytic anemia.

101

Non-selective alpha blockers

Phenoxybenzamine and phentolamine

102

Phentolamine

Reversible. Used to reverse hypertensive crisis in MAOi taking patients who ate tyramine.

103

Phenoxybenzamine

Irreversible. Used for pehochromocytoma pre-op to prevent HTN crisis

104

Alpha-1 antagonist

=-osins (Prazosin, terazosin, tamsulosin). Used for BPH urinary symptoms, HTN. Tox - 1st dose hypotension.

105

Alpha-2 antagonist

Mirtazapine used for depression. Tox = sedation, inc. chol, inc appetite

106

B1>B2 selective antagonists

A to M. Atenolol, esmolol, metoprolol

107

Non-selective Beta blockers

N to Z. Nadolol, propanolol, timolol

108

Nonselective alpha AND beta-antagonists

Carvedilol and labetalol

109

Beta blocker toxicities

Impotence, CNS, CV, dyslipidemia (metoprolol), exacerbate asthmatics and COPD, cocaine risk-> HTN

110

Beta-blocker tox tx?

Glucagon

111

Cu, As, Au fox treatment?

Penicillamine

112

Cyanide treatment?

Nitrite + thiosulfate, hydroxocobalamin

113

Digitalis fox treatment?

Anti-digitalis Fab fragments

114

Fe tox treatment?

Deferoxamine, deferasirox

115

Lead tox treatment?

EDTA, dimeraprol, succimer, penicillamine

116

Mercury, arsenic, gold tox treatment?

Dimercaprol, succimer

117

Methanol, ethylene glycol tox treatment?

Fomepizole > ethanol, dialysis

118

Methemoglobin tox treatment?

Methylene blue, Vitamin C

119

Salicylate tox treatment?

NaHCO3, dilaysis

120

TCAs tox treatment?

NaHCO3 (plasma alkalinization)

121

tPA, streptokinase, urokinase tox treatment?

Aminocaproic acid

122

Coronary vasospasm drugs?

Cocaine, sumatriptan, ergot alkaloids

123

Cutaneous flushing drugs?

VANC - vancomysin (via histamine release NOT IgE HS reaction), adenosine, niacin (via prostaglandins!), Ca2+ channel blockers (Amlodopine)

124

Dilated cardiomyopathy drugs?

Doxorubicin, daunorubicin; Prevent with dexrazoxane = Fe-chelating agent

125

Torsades de pointes causing drugs?

Class II, IA, macrolides, antipsychs, TCAs

126

Hyperglycemia causing drugs?

Tacrolimus, PIs, Niacin, HCTZ, Beta-blockers, Corticosteroids

127

Hypothyroidism causing drugs?

Li, amiodarone, sulfonamides

128

Focal to massive hepatic necrosis drugs?

HAVAc - halothane, Amanita phalloides, Valproic acid, acetaminophen

129

Pancreatitis causing drugs?

Didanosine, Corticosteroids, Alcohol, Valproic, Azathioprine, Diuretics. "Drugs Causing Violent Abdominal Distress."

130

Agranulocytosis causing drugs?

Dapsone, Clozapine, Carbamazepine, Colchicine, Methimazole, Propylthuiouracil

131

Aplastic anemia causing drugs?

Carbamazepine, Methimazole, NSAIDs, Benzene, Chloramphenicol, Propylthiouracil. "Can't Make New Blood Cells Propylerly."

132

Hemolysis in G6PD?

INH, Sulfa, Dapsone, Primaquine, ASA, Ibuprofen, Nitrofurantoin. "Hemolysis IS D PAIN"

133

Megaloblastic anemia causing drugs?

Phenytoin, Methotrexate, Sulfa. "Having a blast with PMS?"

134

Fat redistribution drugs

PIs, Glucocorticoids

135

Gout causing drugs?

Pyrazinamide, thiazides, furosemide, niacin, cyclosporine "Painful Tophi on Feet Need Care" in gout.

136

Photosensitivity drugs?

Sulfonamides, Amiodarone, Tetracyclines, 5-FU. "SAT For a photo."

137

Stevens-Jonson drugs

Anti-epileptics, allopurinol, sulfa, penicillin

138

SLE like syndrome drugs?

Sulfa, hydralazine, INH, procainamide, phenytoin, etanercept. "Lupus is SHIPP-E"

139

Drugs causing seizures?

INH, bupropion, Imipenem/cilastatin, tramadol, enflurane, metoclopramide. With seizures, I BITE My tongue

140

Drugs causing SIADH?

Carbamazepine, cyclophosphamide, SSRIs

141

Drugs causing pulmonary fibrosis?

Bleomycin, amiodarone, busulfan, methotrexate

142

Substrates for P450?

Always Always Always Always Think When Starting Others. (Anti-eps, antideps, anti-psychs, anesthetics, theophylline, warfarin, statins, OCPs).

143

Sulfa drugs

Popular FACTSSS - Probenecid, Furosemide, Acetazolamide, Celecoxib, Thiazides, Sulfonamide antibiotics, Sulfasalazine, Sulfonylureas.

144

-Azole vs. -bendazole?

Ergosterol synthesis inhibitor vs. Antiparasitic/helmintic

145

Clozapine

Acts on D4 receptors, meaning it doesn't have as bad pseudoparkinsonism, tardive dyskinesia, hyperprolactinemia

146

Which TB drug is more active against intracellular pathogens?

Pyrazinamide, because it requires an acidic environment (such as macrophage phagolysosomes).

147

Etoposide

Chemo that inhibits sealing activity of topi-II. (Topo-I relieves NEG super coil with single strand nicks. Topo-II induces transient dbl stranded breaks to relieve positive and negative supercoiling)

148

Glucocorticoid effects on immune system

Reduce lymphocyte counts (T>B) with redistribution to spleen, LN's, and bone marrow. Inhibition of Ig synthesis and stimulation of lymphocyte apoptosis. Inhibit monocyte to macrophage differentiation. Decreased eosinophils. Reduced basophils. INCREASED neutrophils b/c of demargination from vessel wall.

149

Amiodarone side effects

Thyroid dysfunction, corneal micro-deposits, blue-gray skin discoloration, drug-related hepatitis, pulmonary fibrosisq

150

Streptokinase

Thrombolytic. Converts plasminogen into plasmin ---> degrades fibrin.

151

Opioid receptors

mu - dependence, euphoria, respiratory and cardiac depression, reduced GI motility, sedation; works by opening K+ channels to hyper polarize. Kappa = miosis, dysphoria, sedation. Delta = antidepressant. Nociceptin/orphanin (N/OFQ) = anxiolysis and inc. appetite

152

Psoriasis treatments

Topical vitamin D analogs (calciportiene, calcitriol, tacalcitol), which prevent keratinocyte proliferation. Cyclosporine (inhibits NFAT to stop transcription of IL-2). Ustekinumab is human monoclonal Ab targeting IL-12 and 23. Inhibits differentiation of CD4+ the and Th17. Etanercept is recombinant form of human TNF receptor that binds TNF-alpha to treat mod-severe plaque-type psoriasis.

153

Warfarin side effect early on?

Skin and SQ fat necrosis b/c of inhibition of protein C anticoagulation and it's half-life is shorter than the other factors leading to a transient hyper-coagulable state

154

Hemorrhagic cystitis after chemo?

Associated with nitrogen mustard-based chemotherapeutic agents like cyclophosphamide. Metabolized by kidney into acrolein --> urine -> necrosis. Prevent with hydration and MESNA (binds and inactivates toxic metabolites)

155

Leucovorin

Folinic acid. Drug used for MTX overdose b/c bypasses dihydrofolate reductase step.

156

Amifostine

Cytoprotective free-radical scavenger used to dec. nephrotoxicity of Platinum and alklyating chemo agents

157

Filgrastim

G-CSF analog for minimization of granulocytopenia after myelosuppressive chemo

158

Best drug for decreasing triglycerides?

Fibrates (SE - muscle tox w/ statin and gallstones). Activate PPAR-alpha -> lipoprotein lipase activity.

159

Cromolyn and nedocromil mech?

Inhibit mast cell DEGRANULATION. Prevention of acute attacks.

160

How does digoxin treat AF w/ RVR (2nd line)?

Slows conduction through AV node by acting on VAGUS nerve. Ca+ channel blockers and beta-blockers are first line.

161

Cytarabine

Pyrimidine analog anti-metabolite in DNA leading strand. S-phase specific. Gemcitabine is another pyrimidine analog.

162

Selective COX-2 inhibitors

Used to help avoid PLT and GI side effects of NSAIDs. e.g. celecoxib

163

Non-nucleotide reverse transcriptase inhibitors

Nevirapine, efavirenz, delavirdine. DONT require activation via intracellular phophorylation. AE's common like flu, abdominal pain, jaundice, fever. Stevens-Johnsons.

164

Zidovudine (AZT)

is NOT lamivudine. 3' prevention of elongation. Like zalcitabine, must be converted into monophosphate form via cellular thymidine kinase.

165

Motion sickness receptors?

M1 and H1 stimulation -> nausea and vomiting. 1st-gen antihistamines like meclizine and dimenhydrinate; Scopolamien for only anti-muscarinic. SE's are blurry vision, dry mouth, palpitations, urinary retention, constipation

166

Cladribine

PURINE analog for hairy cell leukemia. Resistant to degradation by adenosine deaminase.

167

Dacarbazine

Cell-cycle non-specific methylating agent requiring enzymatic activation (liver)

168

Cyclophosphamide

Alkylating agent that must be converted to active by hepatic CYP450 2B

169

Lomustine

Nitrosourea agent that acts by DNA alkylation and cross-bridge formation (Requires non-enzymatic hydroxylation in liver). Penetrates CNS b/c lipophilic.

170

Nitroprusside

Quick onset, short duration of action w/ cyanide toxicity with prolonged use, high dose, renal problems. Direct arterial and venous vasodilator.

171

Fenoldopam

Benazepine derivative of dopamine that is a SELECTIVE D-1 agonist with NO effect on alpha or beta receptors. Vasodilation of arterial beds and also improves renal blood flow (and increases sodium excretion)

172

Class III antiarrhythmics

K+ efflux decreased, increased AP. Dofetilide, ibutilide, amiodarone, sotalol.

173

Class IA antiarrhythmics

Disopyramide, Quinidine, Procainamide. "Quinn is a Pro Dicer." Intermediate inhibition of phase 0 and prolonged AP.

174

Class IB antiarrhythmics

Lidocaine, Tocainide, Mexiletine. "Mex The Lido" Weak inhibition of phase 0, and shortened AP.

175

Class 1C antiarrythmics

Moricizine, Flecainide, Propafenone. "Mori is a Pro Flexer!." Strong inhibition of phase 0 with no change in AP.

176

ACEi first dose?

First dose hypotension. Activating the Bezold-Jarisch reflex b/c of decreased AII -> vaguely mediated hypotension and bradycardia. Be careful if already taking thiazides (hyponatremia and hypovolemic)

177

How do you treat Beta-blocker overdose?

Glucagon b/c it increases intracellular cAMP and cardiac contractility

178

Serotonin syndrome vs. TCA tox?

TCA tox leads to antichol, vasodilation, conduction defects and arrhythmias, sz/tremors, sedation. Arrhythmia is the most comman cause of death 2/2 Na+ channel inhibition. Tx w NS and hypertonic NaHCO3

179

Cilostazol

Decreases platelet phosphodiesterase activity -> increased cAMP -> decreased PLT aggregation. Direct arterial vasodilator. Therefore, a PAD tx.

180

Abciximab

Monoclonal Ab that inhibits PLT aggregation via IIb/IIIa receptor. Used prior to PCIs.

181

Cisplatin should be used with?

Amifostine. Cisplatin can cause ATN 2/2 ROS. Amifostine is a free-radical scavenger. A Cl- diuresis via IV NS also works b/c totoplatin will be inactive in higher chloride conc.

182

Calcineurin inhibitors

Tacrolimus and cyclosporine. Calcineurin is essential for IL-2 activation for T-cells.

183

Sucralfate

Binds base of mucosal ulcers to protect from acid for healing.

184

Misoprostol

Prostaglandin E1 analog used to prevent NSAID-induced ulcer disease. Also used for labor induction and abortion.

185

Acute gouty attack drugs?

NSAIDs preferred, then colchicine. Allopurinol (Xanthine oxidase inhibitor) shouldn't be used for acute b/c it can mobilize tissue stores of uric acid (worsen or precipitate attacks)

186

Ototoxic chemo?

Cis-platin

187

1st gen antihistaminergics names and side-effects

Chlorpheniramine, diphenhydramine, promethazine. Sedation, blurry vision.

188

Opioid tolerance - what do I need to know?

I need to know that b/c the body doesn't develop a tolerance to constipation and miosis effects of opiates, ppx tx with fluids and laxatives.

189

What is tachyphylaxis?

A phenomenon where the drug's effect rapidly declines after a few days b/c of decreased production of endogenous agonist. e.g. Rebound rhinorrhea after taking alpha agonists (phenylephrine, xylometazoline, oxymetazolin) for too long. e.g. Nitroglycerine.

190

Anti-motility anti-diarrheals

Bind mu opiate receptors in GI to slow motility. Diphenoxylate.

191

Anti-secretory antidiarrheals

Bismuth subsalicylate, probiotics, octreotide

192

Salicycylate poisoning

Initially 2 abnormalities: respiratory alkalosis 2/2 respiratory center hyperventilation + AG metabolic acidosis occuring aftewards (hours)

193

Ticlodopine side effect

Rarely (<1%) = neutropenia

194

Transplant anti-rejection regimen is generally

A calcineurin inhibitor (tacrolimus, sirolimus, cyclosporine) and a de novo purine synthesis inhibitor T-lymphocyte proliferation inhibitor (azothioprine, mycophenolate mofetil)

195

The only FDA-approved anti-obesity medication?

Orlistat - inhibits intestinal lipase --> inhibiting fat absorption in the gut

196

Probenacid

Inhibits renal tubular secretion of penicillins and most cephalosporins, limiting their excretion. Inhibits reABSORPTION of uric acid (gout, preventive drug)

197

An agent that increases levodopa peripheral metabolism?

Vitamin B6. (Entacapone prevents peripheral methylation 2/2 COMT)

198

Effects of carbidopa with levodopa?

Carbidopa inhibits peropheral conversion of levodopa -> increased dopamine in brain (worsened behavioral changes) but less dopamine in periphery (better peripheral side-effects - arrhythmias, postural hypotension, hot flashes, n/v)

199

What are "permissive" effects of a drug?

Allows another drug to achieve its full potential. NOT synergistic.

200

Echinocandins and their mech?

Mech is blocking the synthesis of Beta (1,3) - D glucan, which is the main component of Candida and Asperillus. e.g. caspofungin

201

Doxorubicin mechanism?

Intercalates DNA, binds cell membranes, and generate oxygen radicals (Heart is particularly sensitive b/c it lacks catalase)