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Step 1 2019 First Aid Flashcards > Pharm 1 - Pharmacokenetics/dynamics/ANS p232-246 > Flashcards

Pharm 1 - Pharmacokenetics/dynamics/ANS p232-246 Flashcards

1
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A
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2
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3
Q

How do competitive inhibitors affect Km?

A

Increase Km (dec affinity)

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4
Q

The further to the right the x-intercept (ie, closer to zero), the greater the ___ and the lower ______.

A

The further to the right the x-intercept (ie, closer to zero), the greater the Km and the lower the affinity.

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5
Q

Which type of inhibitor will cross x-intercept of an unihibited substrate?

What does that x-intercept represent?

A

non competitive inhibitor

X-intercept = 1/-Km

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6
Q

What type of inhibitor will cross the y-intercept of an unihibited substrate? What is that y-intercept = to?

A

competitive inhibitor

y-intercept = 1/Vmax

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7
Q

Competitive (-)’r of Diazepam? What is the rec’r?

A

Flumazenil

GABAA- R

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8
Q

Competitive (-)’r vs organophosphates?

A

Atropine

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9
Q

Competitive (-)’r of xanthine oxidase?

A

Allopurinol

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10
Q

ex of competitive ACh antagonist

A

neuromuscular blocking drugs
Atracurium, cisatracurium, pancuronium, rocuronium, tubocurarine, vecuronium

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11
Q

competitive aldosterone receptor antagonists in cortical collecting tubule?

A

Spironolactone, Eplerenone

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12
Q

Competitive inhibitors of progestins at progesterone receptors?

A

Mifepristone, ulipristal.

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13
Q

Nonsteroidal competitive inhibitor at androgen receptors? use?

A

Flutamide; Prostate carcinoma

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14
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15
Q

How does competitive antagonists affect efficacy and potency?

A

dec potency; doesn’t change efficacy

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16
Q

How does a non competitive antagonist affect potency and efficacy?

A

dec potency and efficacy

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17
Q

How does partial agonist affect potency?

A

It doesn’t - it is independent of it.

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18
Q

How does efficacy of a partial agonist compare vs a full agonist?

A

It has less efficacy than a full agonist

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19
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20
Q

How to calc loading dose?

A

(Cp × Vd) / F

Cp - plasma conc

Vd - Vol of distribution

F = bioavail

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21
Q

How to calc maintenance dose?

A

Maintenance dose =
(Cp × CL × τ )/ F
Cp = target plasma concentration at steady state

Cl = clearence
τ = dosage interval (time between doses), if not administered continuousl

F = bioavail

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22
Q

In renal or liver disease, maintenance dose ____ and loading dose is usually ______.

A

In renal or liver disease, maintenance dose Dec and loading dose is usually unchanged.

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23
Q

Time to steady state depends primarily on _____ and is independent of ____ and _____ ________.

A

Time to steady state depends primarily on t1/2 and is independent of dose and dosing frequency.

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24
Q

How to calc t1/2?

A

t1/2 = (0.7 × Vd)/Cl in first-order elimination

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25
Q

Drugs with narrow therapeutic index?

A

Warfarin, Theophylline, Digoxin, Lithium, anti-epitleptics

Warning, These Drugs are lethal

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26
Q

Two drugs with additive effects? What does that mean?

A

Effect of substance A and B together is equal to the sum of their individual effects

Aspirin and acetaminophen

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27
Q

Give ex of a drug that has a permissive effect on another? what does that mean?

A

Presence of substance A is required for the full effects of substance B
Cortisol has a permissive effect on catecholamines, as it upregulates α1-receptors on arterioles, making them more sensitive to Epi/NE (leading to inc BP)

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28
Q

Give ex of two synergistic drugs? define.

A

Effect of substance A and B together is greater than the sum of their individual effects

Clopidogrel with aspirin

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29
Q

What is a tachyphylactic drug interaction?

A

Acute decrease in response to a drug after initial/repeated administration

ex/
Nitrates, niacin, phenylephrine, LSD, MDMA

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30
Q

In regards to drug elimination, _______ are trapped in urine and cleared quickly. ____ ______ can be reabsorbed

A

Ionized species are trapped in urine and cleared quickly. Neutral forms can be reabsorbed

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31
Q

Examples of Weak acids (4)

A

Weak acids

Asprin, Methotrexate, Phenobarbital, Warfarin

WAMP - you’re hit with a Weak Acid

W-arfarin
A-sprin
M-ethotrexate
P-henobarbital

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32
Q

If TCAs are weak bases, why do we treat TCA overdose with sodium bicarbonate (instead of maybe ammonium chloride to acidify the urine and inc elimination of the weak base)

A

TCA toxicity is generally treated with sodium bicarbonate to overcome the sodium channelblocking activity of TCAs, but not for accelerating drug elimination.

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33
Q

Examples of Weak Bases

A

TCAs, Amphetamines

Weak Bases = MAT DACes

(Allopurinol, Diazepam, Cocaine, Methyldopa)

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34
Q

What drugs would be cleared by acidifying the urine?

A

Acidifying urine –> inc ionization of weak bases to inc renal elimination.

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35
Q

What do we give to alkalinize urine?

A

NaHCO3, potassium citrate

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36
Q

What do we give to acidify urine?

A

Ammonium chloride, Vitamin C, Cranberry juice

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37
Q

Drugs with zero order kinetics?

A

Rate of elimination is constant regardless of Cp (ie, constant amount of drug eliminated per unit time). Cp decreases linearly with time.

high dose or toxic concentration

  • Phenytoin
  • Ethanol
  • aspirin

Toxic dose

Salicylates, Cisplatin, Flouxetin, Omeprazole

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38
Q

What happens in phase I drug metabolism?

A

Reduction, Oxidation, Hydrolysis with cytochrome P-450 usually yield slightly polar, water-soluble metabolites (often still active).

R-OH = Phase I

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39
Q

What happens in phase II drug metabolism?

A

Conjugation (Methylation, Glucuronidation, Acetylation, Sulfation) usually yields very polar, inactive metabolites (renally excreted).

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40
Q

Which phase of drug metabolism do the elderly lose first?

A

Phase I

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41
Q

Patients who are slow acetylators have ___ side effects from certain drugs because of _____rate of metabolism (eg, isoniazid).

A

Patients who are slow acetylators have inc side effects from certain drugs because of dec rate of metabolism (eg, isoniazid).

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42
Q

What value of a drug curve represents efficacy?

A

y-intercept = Vmax
the higher the Y intercept, the higher the Vmax, the higher the efficacy

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43
Q

How is efficacy related to potency?

A

Unrelated to potency (ie, efficacious drugs can have high or low potency)

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44
Q

Safer drugs have higher _____ values.

A

Safer drugs have higher TI values.

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45
Q

What are drugs with lower TI values that req monitoring?

A
  • *W**arfarin, Theophylline, Digoxin, Antiepileptic drugs, Lithium;
  • *W**arning! These Drugs Are Lethal!).
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46
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A
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47
Q

Adrenal medulla is directly innervated by __________ __________ ________.

A

Adrenal medulla is directly innervated by preganglionic sympathetic fibers.

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48
Q

Sweat glands are part of the______ _____ but are innervated by _________ _______

A

Sweat glands are part of the sympathetic pathway but are innervated by cholinergic fibers

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49
Q

What is the channel assoc with nicotinic Ach receptors?

A

ligand gated Na/K channels

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50
Q

Subtypes of nicotinic Ach receptors

A

Two subtypes: NN (found in autonomic ganglia, adrenal medulla) and NM (found in neuromuscular junction of skeletal muscle).

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51
Q

Muscarinic Ach Receptors work through which receptors?

A

Muscarinic ACh receptors are G-protein–coupled receptors that usually act through 2nd messengers

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52
Q

Subtypes of Muscarinic Ach-R

A

5 subtypes: M1–5 found in heart, smooth muscle, brain, exocrine glands, and on sweat glands (cholinergic sympathetic).

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53
Q

G protein class of α1 & α2 rec’r?

A

α1 - Gq
α2 - Gi

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54
Q

Major fxn of α1-R?

A

Inc vascular smooth muscle contraction
Inc pupillary dilator muscle contraction (mydriasis)
Inc intestinal and bladder sphincter muscle contraction

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55
Q

Major fxn of α2-R?

A

dec sympathetic (adrenergic) outflow
dec insulin release,
dec lipolysis,
dec aqueous humor production

Inc platelet aggregation,

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56
Q

G protein class of β1, β2, β3 - R?

A

All are Gs

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57
Q

What g proteins are affiliated with M1-3 receptors?

A

M1R = Gq

M2R = Gi

M3R = Gq

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58
Q

Fxn of M1R

A

Mediates higher cognitive functions, stimulates enteric nervous system

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59
Q

Fxn of M2R

A

dec heart rate and contractility of atria

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60
Q

M3R fxn?

A
  • Inc exocrine gland secretions (eg, lacrimal, sweat, salivary, gastric acid)
  • Inc gut peristalsis,
  • Inc bladder contraction,
  • bronchoconstriction,
  • Inc pupillary sphincter muscle contraction (miosis), ciliary muscle contraction (accommodation),
  • Inc insulin release,
  • endothelium-mediated vasodilation
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61
Q

The two dopamine receptors have what g proteins as 2nd messangers?

A

D1R - Gs

D2R - Gi

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62
Q

Fxn of D1R & D2R

A

D1R - Relaxes renal vascular smooth muscle, activates direct pathway of striatum

D2R - Modulates transmitter release, especially in brain, inhibits indirect pathway of striatum

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63
Q

What g proteins are associated with histamine receptors?

A

H1R - Gq

H2R - Gs

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64
Q

Fxn of H1R & H2R

A

H1R
inc nasal and bronchial mucus production, vascular permeability, bronchoconstriction, pruritus, pain

H2R
inc gastric acid secretion

one - lung, two - stomach

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65
Q

Vasopressin receptors - what g protein?

A

V1R - Gq
V2R - Gs

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66
Q

Fxn of V1R & V2R?

A

V1R - Inc vascular smooth muscle contraction

V2R - inc H2O permeability and reabsorption via upregulating aquaporin-2 in collecting twobules (tubules) of kidney, inc release of vWF

67
Q

Release of norepinephrine from a sympathetic nerve ending is modulated by ___ itself, acting on ______ ___________

A

Release of norepinephrine from a sympathetic nerve ending is modulated by NE itself, acting on presynaptic α2-autoreceptors –> negative feedback.

68
Q
A
69
Q
A
70
Q

With cholinomimetic drugs - what should one be on the look out for?

A

Watch for exacerbation of COPD, asthma, and peptic ulcers in susceptible patients.

71
Q

Rx used for urinary retention - MoA?

A

Bethanechol - Activates bladder smooth muscle; resistant to AChE. No nicotinic activity

72
Q

Cholinomimetic rx used to relieve intaocular pressure in open angle glaucoma?

A

Carbachol - Carbon copy of acetylcholine (but resistant to AChE).

Carbachol for glauComa

73
Q

Used to test for asthma? MoA?

A

Methacholine - asthma challenge test - (+) muscarinic receptor in airway when inhaled

74
Q

Cholinomimetic rx that is used to treat glaucoma and the dry mouth of Sjogren?

A

Pilocarpine

75
Q

MoA of Pilocarpine?

A

Contracts ciliary muscle of eye (open-angle glaucoma), pupillary sphincter (closed-angle glaucoma);
resistant to AChE, can cross bloodbrain barrier (tertiary amine).
“You cry, drool, and sweat on your ‘pilow.’ ”

76
Q

Rx 1st line for Alzheimer disease

A

Donepezil, rivastigmine, galantamine

77
Q

Rx that was used to Dx MG? What is used now?

A

Edrophonium;

replaced by anti-AchR Ab

78
Q

Use of Neostigmine?

A
  • Postoperative and neurogenic ileus and urinary retention,
  • myasthenia gravis
  • reversal of neuromuscular junction blockade (postoperative).

NEO - NEuromusc NEurogenic retention post Op

79
Q

Tx for anticholinergic toxicity?

A

Physostigmine

“Phy-xes” (Fixes) anticholingeric tox

Physo-therapy for anticholinergic tox

80
Q

What drugs are used to control the side effects of Pyridostigmine?

A

Used with glycopyrrolate, hyoscyamine, or propantheline to control pyridostigmine side effects.

Use GHP drugs to put Pyrido to sleep (Like GHB)

81
Q

Pyridostigmine used for what disease? and why?

A

MG; long acting, does not penetrate CNS

82
Q

Affects of organophosphates

How to reverse organophosphate poisoning?

A

Diarrhea
Urination,
Miosis,
Bronchospasm,
Bradycardia,
Emesis,
Lacrimation,
Sweating,
Salivation.

DUMBBELSS

Rx/ Atropine

83
Q

What are the nicotinic effects of organophosphate poisoning?

A

Neuromuscular blockade;

like succinyl choline

84
Q

How to reverse the nicotinic effects of organophosphates?

A

Pralidoxime; regenerates AchE if given early

How to rev. nicotinic effects of organophosphates.

PraLID O - Put a LID on nicOtinic effects.

85
Q

CNS effects of organophosphate poisoning?

A

respiratory depression,

lethargy,

seizures, coma

86
Q

Atropine, homatropine, tropicamide works on what body part? used for what?

A

Atropine, homatropine, tropicamide:

to produce mydriasis and cycloplegia

87
Q

Benztropine; trihexyphenidyl has what site of action and application?

A

Benztropine; trihexyphenidyl

used in CNS, for Parkinsons and acute dystonia

Try to Park my Benz

88
Q

Glycopyrrolate has what use in the body?

A

Glycopyrrolate

Parenteral: preoperative use to reduce airway secretions.
Oral: drooling, peptic ulcer.

89
Q

Hyoscyamine
Dicyclomine

A

Hyoscyamine Dicyclomine:

HolD the spasms
GI - antispasmodics for IBS

90
Q

Ipratropium and tiotropium

A

respiratory;

COPD, asthma (“I pray I can breathe soon!”)

91
Q

What muscarinic antagonist is used against bladder spasms and urge urinary incontinence?

A

Bladder spasms and urinary incontinence

Solifenacin
Tolterodine
Oxybutynin

STOP urinary incontinence

Ephedrine (pseudophedrine)

92
Q

used for motion sickness

A

Scopolamine

93
Q

Atropine effects on?

A
94
Q

Atropine blocks ______ effects of anticholinesterases, but not the _____ effects.

A

Atropine blocks muscarinic effects (DUMBBeLSS) of anticholinesterases, but not the nicotinic effects.

95
Q

SE of Atropine

A

inc body temperature (due to dec sweating); Inc HR; dry mouth; dry, flushed skin; cycloplegia; constipation; disorientation

Hot as a hare
Dry as a bone
Red as a beet
Blind as a bat
Mad as a hatter
Full as a flask

96
Q

What can atropine use lead to in the elderly, in men, and infants?

A

Atropine use causes:

Can cause acute angle-closure glaucoma in elderly (due to mydriasis), urinary retention in men with prostatic hyperplasia, and hyperthermia in infants.

97
Q

Albuterol,salmeterol, and terbutaline works on which receptors? used for?

A

β2 > β1
Albuterol for Acute asthma/COPD.
Salmeterol for Serial (long-term) asthma/COPD.
Terbutaline for acute bronchospasm in asthma and tocolysis.

98
Q

Dobutamine - rec’r and use?

A 
β1 \> β2, α
Heart failure (HF), cardiogenic shock (inotropic \> chronotropic), cardiac stress testing.
99
Q

Dopamine - which rec’r and use?

A

D1 = D2 > β > α
Unstable bradycardia, HF, shock;
inotropic and chronotropic effects at lower doses due to β effects;
vasoconstriction at high doses due to α effects

100
Q

Difference between Epi/NE and receptors they use?

A

Epi = β > α

NE = α1 > α2 > β

101
Q

Epi and NE used for?

A

Epi - Anaphylaxis, asthma, open-angle glaucoma; α effects predominate at high doses. Significantly stronger effect at β2-receptor than norepinephrine.

NE - Hypotension, septic shock

102
Q

Fenoldopam - which rec’r and use?

A

D1 R
Postoperative hypertension, hypertensive crisis. Vasodilator (coronary, peripheral, renal, and splanchnic).
Promotes natriuresis.
Can cause hypotension and tachycardia.

Fenoldopam - FENd Off serious HTN

103
Q

Isoproterenol - affect which rec’r ? use?

A

β1 = β2
Electrophysiologic evaluation of tachyarrhythmias. Can worsen ischemia.
Has negligible α effect.

104
Q

rec’r used by Midodrine, what use?

A

α1
Autonomic insufficiency and postural hypotension. May exacerbate supine hypertension

105
Q

Mirabegron - rec’r and use?

A

Mirabegron

β3
urinary incontinence, overactive bladder

Beta 3 = inc lipolysis, thermogenesis, bladder relaxation

106
Q

Phenylephrine - rec’r and use?

A

α1 > α2
Hypotension (vasoconstrictor), ocular procedures (mydriatic), rhinitis (decongestant), ischemic priapism.

 vascular smooth muscle contraction,  pupillary dilator muscle contraction (mydriasis),  intestinal and bladder sphincter muscle contraction

107
Q

List 3 indirect sympathomimetics

A

Amphetamine

Cocaine
Ephedrine

(TCAs)

108
Q

List the mechanisms of Amphetamine, Cocain, Ephedrine

A

Amphetamine - Indirect general agonist, reuptake inhibitor, also releases stored catecholamines
Cocaine - Indirect general agonist, reuptake inhibitor Ephedrine - Indirect general agonist, releases stored catecholamines

109
Q

Why is it dangerous to give BB to a cocaine user?

A

Caution when giving β-blockers if cocaine intoxication is suspected (can lead to unopposed α1 activation –> extreme hypertension, coronary vasospasm).

110
Q

Use of Ephedrine

A

Nasal decongestion (pseudoephedrine), urinary incontinence, hypotension

111
Q

used for hypertension in pregnancy

A

α-methyldopa

112
Q

SE of α-methyldopa

A

Direct Coombs ⊕ hemolysis, drug-induced lupus

α-methyldopa

113
Q

Other drugs that cause drug (+)’d lupus

Drugs that cause COOMBS (+) hemolysis

A

Lupus
Methyldopa, Minocycline, Hydralazine,
Isoniazid, Phenytoin, Sulfa drugs, Etanercept,
Procainamide

Lupus Makes My HIPS Extremely Painful

M SHIPPE

Coombs: Penicillin, methylDopa, Cephalosporins

114
Q

sympatholytic that relieves spasticity

A

Tizanidine

Spastic Tizan

115
Q

Clonidine and Guanfacine applications

A

Clonidine and Guanfacine - alpha 2 agonists

( dec sympathetic (adrenergic) outflow, dec insulin release, dec lipolysis, dec aqueous humor production, INC plat aggregation)

Hypertensive urgency (limited situations), ADHD, Tourette syndrome, symptom control in opioid withdrawa

116
Q

if one abruptly stops taking clonidine/guanfacine, what is the side effect

A

rebound hypertension

117
Q

side effects of α-methyldopa

A

Direct Coombs ⊕ hemolysis, drug-induced lupus

118
Q

Use of Tizanidine & SE.

A

Relief of spasticity
Hypotension, weakness, xerostomia

119
Q

Diff b/w Phenoxybenzamine & Phentolamine

A

Phenoxybenzamine - irreversible α-blocker

Phentolamine - reversible α-blocker

120
Q

Use of Phenoxybenzamine

A

Pheochromocytoma (used preoperatively) to prevent catecholamine (hypertensive) crisis

121
Q

α2 selective (-)’r and use

A

Mirtazapine, use for depression

MirtAZapine = α2

(DEC sympathetic (adrenergic) outflow, insulin release, lipolysis, , aqueous humor production INC platelet aggregation)

122
Q

Examples of partial agonists?

A
  • Danazol - partial agonist at androgen receptor
  • acebutalol - B1 sel partial agonist
  • pindalol - BB, nonselective
  • Tamoxifen - partial agonist in endometrium (SERM)
  • Buprenorphine - partial agonist at opiod receptor
  • Aripiprazole - D2 partial agonist
  • Varenicline - nACh-R partial agonist
  • Vilazodone - 5HT1A-R partial agonist
  • Buspirone - 5HT1A-R partial agonist
  • Butorphanol - mu partial agonist (mixed opiod receptor)
  • Pentazocine - mu antagonist/partial agonist (mixed opiod)
123
Q

Which beta blockers dec mortality in heart failure?

A

Bisoprolol, Carvedilol, Metoprolol (β-blockers Curb Mortality

124
Q

In HTN how do BB help?

A

dec cardiac output, dec renin secretion (due to β1 receptor blockade on JG cells)

125
Q

BB used in hyperthyroidism, actions?

A

Propranolol

Symptom control (dec heart rate, dec tremor), thyroid storm

126
Q

How do BB help in hypertrophic cardiomyopathy

A

dec heart rate –> inc filling time, relieving obstruction

127
Q

How do BB help in MI?

A

dec o2 demand

dec mortality

128
Q

Which BB used for SVT? how do they help?

A

metoprolol

esmolol

dec AV conduction velocity (class II antiarrhythmic)

MESsVT - Metoprolol & Esmolol for SVT

129
Q

BB used in variceal bleeding? MoA?

A

Nadolol, propranolol, carvedilol

dec hepatic venous pressure gradient and portal hypertension (prophylactic use)

Portal VariCeal hypertensioN

P - propranolol

C- Carvedilol

N- nadolol

130
Q

Adverse effects of BB

A
  • Erectile dysfunction
  • cardiovascular (bradycardia, AV block, HF),
  • CNS (seizures, sleep alterations)
  • dyslipidemia (metoprolol)
  • asthma/COPD exacerbations
131
Q

Why must one be wary of using BB in cocaine assoc chest pain?

A

Use of β-blockers for acute cocaine-associated chest pain remains controversial due to unsubstantiated concern for unopposed α-adrenergic stimulation.

132
Q

Ex of B1R (-)’rs?

A

β1-selective antagonists (β1 > β2)—acebutolol (partial agonist), atenolol, betaxolol, bisoprolol, esmolol, metoprolol

133
Q

Nonselective α- and β-antagonists?

A

carvedilol
labetalol

134
Q

Unique features of Nebivolol?

A

Nebivolol combines cardiac-selective β1-adrenergic blockade with stimulation of β3-receptors (activate nitric oxide synthase in the vasculature and dec SVR)

Nebivolol inc NO

135
Q

What type of foods can lead to histamine poisoning?

A

Spoiled dark-meat fish such as tuna, mahimahi, mackerel, and bonito.

136
Q

Action of histamine in scombroid poisoning, and sx?

A

Bacterial histidine decarboxylase converts histidine to histamine. Frequently misdiagnosed as fish allergy.

Mimics anaphylaxis: acute burning sensation of mouth, flushing of face, erythema, urticaria, itching. May progress to bronchospasm, angioedema, hypotension.

137
Q

Tx of Histamine poisoning?

A

Antihistamines. Albuterol and epinephrine if needed.

138
Q

Tetrodotoxin - found in what food? MoA?

A

Pufferfish. Highly potent toxin; binds fast voltagegated Na+ channels in cardiac/nerve tissue, preventing depolarization

139
Q

Sx of TTX poisoning?

A

Nausea, diarrhea, paresthesias, weakness, dizziness, loss of reflexes.

140
Q

Ciguatoxin found in what food?

A

Reef fish such as barracuda, snapper, and moray eel.

141
Q

MoA and Sx of ciguatoxin?

A

Opens Na+ channels, causing depolarization.

Nausea, vomiting, diarrhea; perioral numbness; reversal of hot and cold sensations; bradycardia, heart block, hypotension.

142
Q

What is Beers criteria ?

A

Widely used criteria developed to reduce potentially inappropriate prescribing and harmful polypharmacy in the geriatric population. Includes > 50 medications that should be avoided in elderly patients due to dec efficacy and/or inc risk of adverse events

143
Q

Ex of Rx that meet Beers criteria?

A
  • α-blockers (inc risk of hypotension)
  • Anticholinergics, antidepressants, antihistamines, opioids (inc risk of delirium, sedation, falls, constipation, urinary retention)
  • Benzodiazepines (inc risk of delirium, sedation, falls)
  • NSAIDs (inc risk of GI bleeding, especially with concomitant anticoagulation)
  • PPIs (inc risk of C difficile infection)
144
Q

A man presents with kidney issues and pain - what Rx should one be careful giving him? and why?

A

Morphine - Morphine 6 glucoronide is an active metabolite of morphine and more active than morphine itself. Can be toxic in pt. with kidney issues, since they can’t eliminate it as well

145
Q

A pt has a clotting issue, but is a poor metabolizer. What anti-clotting Rx should we not give him?

A

Not Warfarin - Poor metabolizers will bleed.

146
Q

A pt is on Warfarin but acquires a bacterial infection - which antibiotics would cause bleeding in this patient?

A

Ciprofloxacin, Macrolides (except azithromycin), Sulfonamides.

147
Q

5 drugs that cause pulmonary fibrosis?

A

Bleomycin (w/in weeks -mos), Amiodarone, Busulfan (takes years), Methotrexate, Nitrofurantoin

Pulmonary fibrosis is BBAd, MaN

148
Q

Why does Crohn’s lead to malabsorption?

A

Crohn’s has cobblestone mucosa - the thicker membrane is due to fibrosis, decreasing the absorption in SI

149
Q

What form of a drug is needed to get into the CNS?

A

lipid soluble, Non-ionized, small

150
Q

what form of drug is affected by pK and pH?

A

Ionized, water soluble

151
Q

Why is Heparin the anticoagulant of choice in pregnancy?

A

water soluble, won’t cross blood placental barrier

152
Q

Drug of Choice in hypothyroidism in pregnancy?

A

PTU, 90% protein bound, wont cross blood placental barrier

153
Q

Which Rx would decrease Digoxin’s Vd (volume of distribution) (6)

A

Any Rx that displaces digoxin from its tissue binding site (more tissue bound = greater Vd) - Amiodarone, verapamil, itraconazole, erythromycin, clarithromycin, quinidine.

154
Q

Disruption of which metabolic pathway will lead to poor drug metabolization by cytochromes?

A

Pentose phosphate pathway - Cytochrome p450s require NADPH to function

155
Q

How many half lives does it take to get to 90% of steady state?

A

3.3

156
Q

What drug reverses the action of Heparin? (Chemical antagonism)

A

Protamine sulfate

157
Q

Which drugs bind to an inhibitory Cl- ion channel in the CNS?

A

GABAa Receptor - Benzos, Barbiturates,

158
Q

Which receptors will result in DEC in cAMP? (6)

A

Gi coupled -

M2R, Alpha2-R, D2R, - People who are 2 MAD (-) themselves

Opiate, GABAb, 5-HT1

159
Q

Which receptors activate PLC?

A

Gq coupled -

a1-R, M1-R, M3-R, H1, V1, - HAVE 1 M&M

5-HT2

160
Q

Example of tyrosine kinase receptor blocker? Used for what diseases?

A

Imatinib - CML, GI stromal tumors Erlotinib - non small cell lung carcinoma

161
Q

Single most effective drug for malaria? SE?

A

Artesunate > Quinidine/Doxycyclin - clears parasitemia faster SE// long QT

162
Q

______ is directly proportional to the enzyme concentration

A

Vmax is directly proportional to the enzyme concentration

163
Q

Max concentration of a drug is proportional to ?

A

Dose administered

164
Q

Which antibiotic is contraindicated in neonate because it could lead to kernicterus? why?

A

Sulfonamides, as they displace bilirubin from albumin binding sites.

Step 1 2019 First Aid Flashcards (63 decks)

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