pharmpath Flashcards

1
Q

Lineweaver-Burk plot. What does the X intercept mean and what does the Y intercept mean?

A

X intercept is 1/-Km. So the more to the right that is, the bigger Km is, and the lower the affinity. Y intercept is 1/Vmax. The higher that is, the lower Vmax is. Can remember this because V looks kind of like a Y.

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2
Q

Bioavailabilty equation

A

Fraction of drug that reaches circulation unchanged. F = 100% IV. Area under oral curve/ area under IV cure (227)

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3
Q

Volume of distribution equation

A

Amount of drug in body/ plasma concentration of drug.

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4
Q

What is the range for a low volume of distribution and what are some drug types?

A

Low means mostly in the blood. 4-8 L. Large, charged molecules, plasma protein bound

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5
Q

Where do medium volume of distribution drugs go and what are some drug types?

A

Medium go to the ECF. Small, hydrophilic molecules. Small so can get through, but not lipophilic so can’t really spread too far

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6
Q

Where do high volume of distribution drugs go and what are some drug types?

A

Go to all tissues. Small, lipophilic, bound to tissue proteins

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7
Q

Half life equation. What can you calculate from half life?

A

t1/2 = (.7 x Vd) / CL

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8
Q

How long does a drug infused at a constant rate take to reach steady state?

A

4-5 half lives

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9
Q

Clearance equation

A

Clearance = rate of elimination of drug/ concentration of drug in plasma. = Vd x Ke (elimination constant) –> amount of drug in body x elimination constant/plasma concentration of drug

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10
Q

Loading dose equation

A

Cp x Vd / F. Cp = target plasma concentration. So for loading, need to take into account the spread and how much is going to get hit by first pass. F is how much will make it, so the bigger F is, the lower dose you need. The bigger Vd, the higher dose you

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11
Q

Maintenance dose equation

A

Cp x CL/F. Now we are maintaining, so have to increase dose with clearance and decrease dose if more makes it through first pass.

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12
Q

Zero order vs first order elimination

A

Zero: constant amount eliminated no matter what the concentration. Called capacity dependent elimination (maxed out already so doesn’t matter what concentration is). First order: constant fraction eliminated. Called flow dependent elimination

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13
Q

How can you treat phenobarbital, MTX, and aspirin overdose all at once?

A

Bicarb. These are all weak acids and can get trapped in basic environments by ionizing them.

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14
Q

How can you treat an amphetamine OD?

A

Ammonium chloride. Weak base, can trap with acid.

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15
Q

What do phenytoin, ethanol, and aspirin have in common?

A

Zero order kinetics at high or toxic concentrations

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16
Q

Phase I vs Phase II metabolism

A

Phase I is P450, does reduction, oxidation, hydrolysis that yields slightly polar, water-soluble metabolites (often still active). Phase II does conjugation and yields very polar, inactive metabolites that are excreted. This is where slow acetylators come

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17
Q

Therapeutic index

A

Median lethal dose/ median effective dose. Safer drugs have higher TI’s, takes a way bigger lethal dose than effective dose

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18
Q

Therapeutic window

A

Range of minimum effective dose to minimum toxic dose.

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19
Q

What type of G protein does mydriasis via pupillary dilator muscle contraction?

A

Alpha 1 –> Gq

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20
Q

What type of G protein decreases HR and contractility of atria?

A

M2 is heart –> Gi

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21
Q

What kind of G protein increases sweat?

A

M3 –> Gq. Remember, this one is a muscarinic carrying out sympathetic activity!

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22
Q

What type of G protein does intestinal and bladder sphincter muscle contraction?

A

Apha 1 –> Gq

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23
Q

What kind of G protein relaxes renal vascular smooth muscle?

A

D1 –> Gs

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24
Q

What kind of G protein responds to ADH with increased vascular smooth muscle contraction?

A

V1 –> Gq

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25
Q

What kind of G protein increases aqueous humor production?

A

Beta 2 –> Gs

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26
Q

What kind of G protein decreases insulin release via autonomic signaling?

A

Alpha 2 –> Gi

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27
Q

What kind of G protein increases bladder contraction?

A

M3 –> Gq

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28
Q

What kind of G protein does accommodation?

A

M3 –> Gq

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29
Q

What kind of G protein is associated with the D2 receptor. What does the D2 receptor do?

A

Gi. Modulates transmitter release, especially in the brain

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30
Q

What kind of G protein does increased nasal and bronchial mucus production, contraction of bronchioles, pruritis, and pain

A

H1 –> Gq

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31
Q

What kind of G protein responds to H2. What does it do?

A

H2 –> Gs. Increased gastric acid secretion

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32
Q

What kind of G protein responds to ADH by increasing water reabsorption?

A

V2 –> Gs

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33
Q

What kind of G protein decreases uterine tone in response to an autonomic?

A

Beta 2 –> Gs (tocolytic)

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34
Q

What kind of G protein does ciliary muscle relaxation?

A

M3 –> Gq

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35
Q

What kind of G protein does bronchoconstriction?

A

M3 –> Gq

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36
Q

What kind of G protein does pupillary sphincter muscle contraction (mioisis)?

A

M3 –> Gq

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37
Q

What kind of G protein increases platelet aggregation via autonomic signaling?

A

Alpha 2 –> Gi

38
Q

Now, M1, M2, M3, what do they do and what are their associated G proteins?

A

M1 = CNS –> Gq. M2 = heart –> Gi. M3 = everything else –> Gq

39
Q

D1 and D2: what are their Gs?

A

Gs, Gi. Si! Kidney and brain

40
Q

H1 and H2: what are their Gs?

A

Gq, Gs. Gs –> acid Secretion, Gq –> rest

41
Q

V1 and V2: What are their Gs?

A

Gq, Gs. Gq –> constriction (like alpha 1 that also uses Gq). Gs –> normal ADH stuff

42
Q

Gs has what effect on the heart? Smooth muscle?

A

Gs –> increased PKA –> increases calcium in the heart. PKA also phosphorylates myosin light chain kinase to inhibit it! Inhibits smooth muscle contraction (D1, Beta 2)

43
Q

PTEN: What is it and what is the pathway?

A

Growth factor –> TK –> PI3K –> phosphorylates PIP2 –> PIP3 –> activates Akt –> mTOR –> cell survival and anti-apoptosis. Now, PTEN is a tumor suppressor and dephosphorylates PIP3. See p 231

44
Q

Pyridostigmine, neostigmine, edrophonium, and physostigmine. Who can enter the CNS? Uses?

A

Physostigmine, others can’t. Physo for atropine OD. Use neo and pyrido to treat MG and edrophonium to diagnose MG (short-acting). Neo is also for post-op ileus and urinary retention and reversal of NMJ blockade

45
Q

What G protein does increased gastric acid secretion from autonomics?

A

Gq –> M3.

46
Q

Pralidoxime

A

Regenerates active AChE in cholinesterase inhibitor poisoning

47
Q

Tropicamide

A

Atropine for the eye

48
Q

Glycopyrrolate

A

Muscarinic antagonist for GI and respiratory (reduce airway secretions and treat peptic ulcer)

49
Q

What is the muscarinic receptor on endothelial surfaces?

A

NO (endothelial derived relaxing factor or EDRF). No innervation, only agonists hit it

50
Q

What receptors is isoproterenol selective for? What do you use it to treat?

A

Beta 1 and beta 2 agonist. Treats torsades de pointes (tachy decreases QT interval) and bradyarrythmias (though may worsen ischemia)

51
Q

What receptors does DA act on in increasing doses?

A

Low dose –> D1, medium –> betas, high –> alphas

52
Q

Where does dobutamine act?

A

beta 1 primarily. Use for heart failure, cardiac stress testing (increases conduction speed)

53
Q

Ritodrine. Uses?

A

Beta 2 selective agonist for reducing premature uterine contractions

54
Q

Amphetamine MOA vs ephedrine vs cocaine

A

Amphetamine releases stored catecholamines and decreases reputake, cocaine decreases reuptake, ephedrine releases stored catecholamines

55
Q

What would happen if you gave beta blockers to someone on cocaine?

A

Unopposed alpha 1 activation and extreme HTN

56
Q

Methyldopa MOA

A

alpha 2 agonist, decreases central sympathetic outflow. Can treat HTN, especially with renal disease (doesn’t decrease renal blood flow to kidney). Same with clonidine

57
Q

Name the partial beta agonists

A

Pindolol, acebutolol

58
Q

Name the nonselective alpha and beta antagonists

A

carvedilol, labetolol

59
Q

What do you give someone who overdoses on salicylates

A

Alkalinize the urine (NaHCO3)

60
Q

What do you give someone who overdoses on beta blockers

A

Glucagon.

61
Q

What do you give someone who overdoses on digitalis

A

Normalize K and magnesium, Lidocaine, Anti-Fab,

62
Q

What do you give someone who overdoses on iron

A

Deferoxamine, deferasirox

63
Q

What do you give someone who overdoses on lead

A

CaEDTA, dimercaprol, succimer, penicillamine

64
Q

What do you give someone who overdoses on mercury

A

Dimercaprol, succimer

65
Q

What do you give someone who overdoses on copper

A

Penicillamine

66
Q

What do you give someone who overdoses on arsenic

A

Dimercarpol, succimer, penicillamine

67
Q

What do you give someone who overdoses on gold

A

Dimercaprol, succimer, penicillamine

68
Q

What do you give someone who overdoses on cyanide

A

Nitrate + thiosulfate, hydroxocobalamin

69
Q

What do you give someone for methemeglobin

A

Methylene blue, vitamin C

70
Q

What do you give someone for warfarin OD

A

Vitamin K, fresh frozen plasma (faster)

71
Q

What do you give someone for tPA, streptokinase, or urokinase OD

A

Aminocaproic acid. Inhibits plasmin

72
Q

What do you give someone for theophylline OD

A

Beta blocker

73
Q

3 drugs that cause coronary vasospasm

A

Cocaine, sumatriptan, ergot alkaloids

74
Q

4 drugs that cause cutaneous flushing

A

Vanco, adenosine, niacin, Ca blockers

75
Q

2 drug types that cause torsades

A

Class III and IA antiarrythmics

76
Q

6 drugs that cause agranulocytosis?

A

Clozapine, carbamazepine, colchicine, PTU, methimazole, dapsone (an antibiotic)

77
Q

5 drugs that cause aplastic anemia?

A

Chloramphenicol (gray baby), benzene, NSAIDs, PTU, methimazole

78
Q

What 2 drugs cause direct Coombs positive hemolytic anemia?

A

Methyldopa, PCN

79
Q

6 drugs that cause hemolysis in G6PD deficient patients

A

INH, sulfonamides, primaquine, aspirin, ibuprofen, nitrofurantoin

80
Q

3 drugs that cause megaloblastic anemia?

A

Phenytoin, MTX, sulfa drugs

81
Q

Drug that you think of with acute cholestatic hepatitis and jaundice?

A

Erythromycin

82
Q

3 drugs that cause hepatic granulomatosis?

A

Methyldopa, hydralazine, quinidine

83
Q

3 drugs that cause cholethiasis?

A

Fibrates, octreotide, ceftriaxone

84
Q

5 drugs that cause gynecomastia?

A

Spironolactone, digitalis, cimetidine, chronic alcohol use, ketoconazole

85
Q

5 drugs that cause hyperglycemia?

A

Niacin, tacrolimus and cyclosporine, protease inhibitors, HCTZ, corticosteroids

86
Q

3 drugs that cause hypothyroid?

A

Lithium, amiodarone, sulfonamides

87
Q

4 drugs that cause gout?

A

Furosemide, thiazides, niacin, cyclosporine

88
Q

Which 3 drugs do photosensitivity?

A

Sulfonamides, amiodarone, tetracycline

89
Q

2 drugs that cause siADH

A

Carbamazepine, cyclophosphamide. Cyclophosphamide also causes hemorrhagic cystitis

90
Q

What CNS effects does metoclopramide have?

A

Seizures and PD like symptoms