01b: Pharmacology Flashcards

1
Q

Lineweaver Burk: x-int approaches zero, affinity of enzyme to substrate (increases/decreases).

A

Decreases (Km increases)

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2
Q

Competitive inhibitors decrease (efficacy/potency) and noncompetitive inhibitors decrease (efficacy/potency).

A

Potency; efficacy

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3
Q

Small, hydrophilic compounds likely have (large/small) Vd and distributed mainly in (X) compartment.

A

Medium

X = ECF

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4
Q

Large, charged molecules likely have (large/small) Vd and distributed mainly in (X) compartment.

A

Small

X = intravascular (and bound to plasma proteins)

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5
Q

Drug infused at constant rate takes (X) number of half lives to reach steady state.

A

X = 4-5 (90% at 3.3 half lives)

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6
Q

Drugs: Loading dose calculation

A

(Cp)*(Vd)/(F)

Cp = target plasma conc at steady state
F = bioavailability
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7
Q

Drugs: Maintenance dose calculation (not for continuous infusion)

A

(Cp)(CL)(𝝉)/(F)

Cp = target plasma conc at steady state
𝝉 = time between doses
F = bioavailability
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8
Q

Time until drug reaches steady state is (increased/decreased) with increased (loading/maintenance) dose.

A

Independent of these! Depends primarily on half-life

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9
Q

Aspirin and acetaminophen drug interaction is an example of (X) effect

A

X = additive (their effect together is equal to sum of their individual effects)

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10
Q

Cortisol and catecholamine drug interaction is an example of (X) effect

A

X = permissive (cortisol required for full effects/responsiveness of catecholamines)

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11
Q

Clopidogrel and aspirin drug interaction is an example of (X) effect

A

X = synergistic (effects of them together is greater than sum of their individual effects)

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12
Q

Tachyphylactic drug interaction refers to which phenomenon?

A

Acute decrease in response to drug after initial/repeated administration

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13
Q

Zero-order kinetics: constant (X) of drug eliminated per unit time. List three examples of drugs eliminated in this manner.

A

X = amount

PEA (pea is round like 0)
Phenytoin, EtOH, Aspirin

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14
Q

First-order kinetics: constant (X) of drug eliminated per unit time. Applies to most drugs

A

X = fraction

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15
Q

Half-life (decreases/increases) in (zero/first)-order kinetics as concentration of drug decreases.

A

Decreases in zero order;

Remains constant in first-order

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16
Q

Aspirin overdose can be treated with (X), which will (ionize/neutralize) the urine and result in:

A

X = bicarbonate
Ionize (alkalinize)

Ionization of weak acid drugs (salicylate, phenobarbital, methotrexate) will trap it in urine and clear it quickly

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17
Q

What might be used to (ionize/neutralize) the urine and trap drugs that are weak bases, such as (X)?

A

Ammonium chloride;
Ionize (acidify) urine to then ionize and trap weak bases
X = amphetamines, TCAs

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18
Q

List the phases of drug metabolism. Star the one that geriatric patients lose first.

A

Phase I*: CYP450 (metabolites often still active)

Phase II: Conjugation (methylation, glucoronidation, acetylation, sulfation; inactive metabolites)

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19
Q

Why are patients that are slow acetylators at (increased/decreased) risk of drug side effects?

A

Increased

Decreased Phase II of drug metabolism (conjugation)

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20
Q

Drug efficacy is represented by (low/high) (X). Drug potency is represented by (low/high) (Y).

A

High; X = Vmax (max effect)
Low; Y = EC50 (amount of drug needed for given effect)

These two characteristics are unrelated

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21
Q

Give an example of partial agonism at the opioid mu receptor.

A

Morphine (full agonist) and buprenorphine (partial)

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22
Q

List four drugs that must be monitored carefully due to (low/high) therapeutic index.

A

Low (TD50/ED50)
Mnemonic: Warning! These Drugs are Lethal

  1. Warfarin
  2. Theophylline
  3. Digoxin
  4. Lithium
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23
Q

(X) glands are funky in that they’re part of (sympathetic/parasympathetic) pathway but innervated by (Y) fibers.

A

X = sweat (trying to remember these makes me sweat)
Sympathetic
Y = cholinergic

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24
Q

Botulinum toxin affects (muscarinic/nicotinic) ACh receptors. Repetitive nerve stimulation (can/cannot) increase compound muscle action potential

A

Both (since decreases ACh release from nerve terminals; cleaves SNARE proteins)

Can

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25
Q

T/F: Myasthenia gravis only affects nicotinic ACh receptors.

A

True

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26
Q

Activation of (X) receptor increases pupillary dilator muscle.

A

X = alpha1 (Gq class)

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27
Q

Activation of (X) adrenergic receptor(s) (increases/decreases) contraction of bladder and intestinal sphincters.

A

X = alpha1 (Gq class)

Increases

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28
Q

(X) adrenergic receptor plays important role in (increasing/decreasing) platelet aggregation.

A

X = alpha2 (Gi class)

Increasing

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29
Q

(X) adrenergic receptors play opposite roles in regulating aqueous humor production. They play similar roles in regulation of (Y).

A
X = beta2 (increases) and alpha2 (decreases)
Y = insulin secretion and lipolysis
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30
Q

(X) adrenergic receptors play role in (increasing/decreasing) renin release.

A

X = beta1

Increasing

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31
Q

List the key receptors that work by Gq-protein-linked second messenger

A

Mnemonic: HAVe 1 M&M

H1, alpha1, V1 (vasopressin); M1, M3

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32
Q

List the key receptors that work by Gi-protein-linked second messenger

A

Mnemonic: MAD 2’s (trying to inhibit cAMP)

M2, alpha2, D2

33
Q

Which vasopressin receptor works on kidney?

A

V2 (two for collecting TUbules)

34
Q

Which dopamine receptor works on kidney?

A

D1 (relaxes renal vasculature smooth muscle)

35
Q

(X) histamine receptor (increases/decreases) gastric acid secretion via which G-protein second messenger system?

A

X = H2

Gs (increases)

36
Q

Pyridostigmine primarily used to treat:

A

Myasthenia gravis (anticholinesterase; increases ACh)

PyRIDOstiGMine (gets RID O’ MG)

37
Q

List the meds that are used in AD to (increase/decrease) ACh.

A

Increases (anti-cholinesterases)
“AD patients GALLANTly swim DOwN the RIVer”

  1. Galantamine
  2. Donepezil
  3. Rivastigmine
38
Q

Cholinesterase inhibitor poisoning is often due to (reversible/irreversible) action of (X). Symptoms?

A

Irreversible
X = organophosphates (insecticide)

DUMBBELSS

39
Q

Organophosphate poisoning antidote:

A

Anticholinergics: atropine (competitive inhibitor) AND pralidoxime (regenerates AChE if given early)

40
Q

Scopolamine is primarily used for:

A

Motion sickness treatment; muscarinic (M1-R) antagonist in vestibular nuclei

41
Q

Patient with myasthenia gravis is experiencing classic side effects of (X) drug. Which agent can be given to reduce these side effects?

A

X = pyridostigmine (AChE inhibitor)

Scopolamine (blocks M1-R and decreases muscarinic side effects without impacting therapeutic nicotinic effects)

42
Q

Farmer comes in with diarrhea, miosis, excess sweating and tearing, and muscle weakness. After administration of therapeutic agent, all symptoms resolve except muscle weakness. What was he likely given?

A

Only atropine (muscarinic antagonist); if pralidoxime not given as well, nicotinic ACh effects remain

43
Q

“Gardner’s pupil” is the result of (X) ingestion and treated with (Y).

A
X = Jimson weed (plant alkaloids/muscarinic antagonists resulting in mydriasis)
Y = physostigmine (gets into CNS)
44
Q

(Epi/NE) would be given for bronchoconstriction.

A

Epi (significantly stronger at beta2 effect than NE)

ex: asthma, anaphylaxis

45
Q

Patient with hypotension and shock is immediately given IV solution of (X). Around the IV site, you notice whitening and hardening of the skin. You immediately administer (Y) because:

A
X = NE
Y = phentolamine (in NaCl solution)

Blanching of vein due to NE extravasation into tissue around IV can cause severe alpha1 constriction and result in necrosis

46
Q

List three examples of indirect sympathomimetics

A
  1. Amphetamines
  2. Cocaine
  3. Ephedrine
47
Q

(X) drug should never be administered if cocaine intoxication suspected as it will cause unopposed (Y) adrenergic response.

A
X = beta blocker
Y = alpha1 vasoconstriction (extreme HT)
48
Q

Beta2 receptor effect on vasculature

A

Vasodilation

49
Q

Isoproterenol (increases/decreases) HR, (increases/decreases) CO, and (increases/decreases) MAP via actions primarily on (X) receptors.

A

Significantly increases HR and CO (reflex tachycardia); decreases MAP
X = beta (1 and 2)

50
Q

NE (increases/decreases) HR, (increases/decreases) CO, and (increases/decreases) MAP via actions primarily on (X) receptors.

A

Decreases (reflex bradycardia);
No change on CO
Increases
X = alpha1

51
Q

Phenoxybenzamine: (reversible/irreversible) drug used primarily for…

A

Irreversible (non-competitive) alpha blocker;

Pheochromocytoma (pre-op)

52
Q

Why is orthostatic hypertension a Sx of (X) adrenergic drugs?

A

X = alpha blockers

Body can’t increase SVR/sympathetic tone reflexively after standing up

53
Q

After administering phentolamine, the Epi BP response goes from net (increase/decrease) in BP to net (increase/decrease).

A

Increase (the alpha response); decrease (the beta2 response)

Note: both come into play prior to blockade

54
Q

Selective beta blockers:

A

Mostly go from A-M (selective to beta1; 1 = first half of alphabet):
Acebutolol, atenolol, betaxolol, bisoprolol, esmolol, metroprolol

55
Q

Non-selective beta blockers:

A

Mostly go from N-Z (Non-selective include beta2; 2 = second half of alphabet):

Nadolol, pindolol, propranolol, timolol

56
Q

Non-selective alpha AND beta antagonists:

A

Carvedilol and labetalol (note: modified endings, don’t end with “-olol” like beta-blockers)

57
Q

Pufferfish: (X) toxin with which MOA?

A

X = tetrodotoxin

Binds fast voltage-gated Na channels (cardiac/nerve tissue), preventing depolarization

58
Q

List some examples of drugs that meet the Beers criteria and should be avoided in (X).

A

X = geriatric patient population

  1. Anticholinergics, anti-His, benzos, opioids, anti-depressants (side effects like delirium, falls, sedation, etc.)
  2. PPIs (C dif infection)
  3. NSAIDs (GI bleeding)
  4. Alpha-blockers (hypotension)
59
Q

Acetaminophen toxicity should be treated with (X), which functions to (Y).

A
X = N-acetylcystine
Y = replenish glutathione
60
Q

Pesticide ingestion leads to (X) toxicity and should be treated with (Y).

A
X = arsenic
Y = Dimercaprol (chelator; increases urinary secretion of heavy metals)
61
Q

Benzo toxicity Rx:

A

Flumazenil

62
Q

Cu toxicity Rx:

A

“Cu PENny”

Penicillamine

63
Q

Cyanide toxicity Rx:

A

Nitrite (Met-Hgb formation to sequester CN) and thiosulfate (sulfur donor to promote excretion)

64
Q

Pt presents with abdominal pain, vomiting, watery diarrhea, and garlic breath. You treat with:

A

Dimercaprol (arsenic poisoning)

65
Q

MetHgb toxicity treated with:

A

METhylene blue

66
Q

Rat poison toxicity is due to (X) compound and treated immediately with:

A

X = super-warfarin

FFP

67
Q

List some drugs that cause cutaneous flushing

A

VANNCE makes me blush

  1. Vanco
  2. Adenosine
  3. Nitrates
  4. Niacin
  5. CCBs
  6. Echinocandins
68
Q

List some drugs that cause torsades de pointes

A

ABCDE prolong dat QT

  1. anti-Arrhythmics (class IA, III)
  2. antiBiotics (macrolides)
  3. anti-“C”ychotics (haloperidol)
  4. anti-Depressants (TCAs)
  5. anti-Emetics (odansetron)
69
Q

List some drugs that have hyperglycemia as side effect

A

“Taking Pills Necessitates Having glucose Checked”

  1. Tacrolimus
  2. PIs
  3. Niacin
  4. HCTZ
  5. Corticosteroids
70
Q

Grey baby syndrome is due to (X) drug accumulation in neonate due to lack of:

A

X = chloramphenicol

glucoronidation (conjugation)
Sx: hypothermia, flaccidity, shock

71
Q

List drugs that cause hemolysis in G6PD deficiency.

A

“Hemolysis IS D PAIN”

  1. Isoniazid
  2. Sulfonamides
  3. Dapsone
  4. Primaquine
  5. Aspirin
  6. Ibuprofen
  7. Nitrofurantoin
72
Q

In addition to glucocorticoids, which class of drugs has fat redistribution as a side effect?

A

Anti-retrovirals (esp protease inhibitors)

“fat PiG = PI and glucocorticoids”

73
Q

List the main drugs that can cause Steven Johnson Syndrome

A

“Steven Johnson has epileptic ALLergy to sulfa drugs and penicillin”

  1. anti-epileptics (esp lamotrigine)
  2. Allopurinol
  3. Sulfa drugs
  4. Penicillin
74
Q

List key drugs that can cause Parkinson-like syndrome.

A

“Cogwheel rigidity of the ARM”

  1. Antipsychotics
  2. Reserpine
  3. Metoclopromide
75
Q

List key drugs that cause seizures

A

“with seizures I BITE my tongue”

  1. Isoniazid
  2. Buproprion
  3. Imipenem/cilastatin
  4. Tramadol
  5. Enflurane
76
Q

Key CYP450 inducers

A

“Chronic alcoholics STeal PHEN-PHEN and NEver Refuse GReasy CARBs”

  1. Chronic alcohol use
  2. St. John’s wort
  3. Phenytoin
  4. Phenobarbitol
  5. Nevirapine
  6. Rifampin
  7. Griseofulvin
  8. Carbamazepine
77
Q

Phenytoin is (inducer/inhibitor/substrate) of CYP450.

A

Substrate (broken down, along with other anti-epileptics) and inducer

78
Q

List some key CYP450 substrates.

A

CYP “Substrates Worry About Other Therapeutics”

  1. Statins
  2. Warfarin
  3. Anti-epileptics
  4. OCPs
  5. Theophylline
79
Q

List some key CYP450 inhibitors

A

“Grapes@SICKFACES.COM”

  1. Grapefruit juice*
  2. Acute alcohol abuse
  3. Sodium valproate
  4. Isoniazid
  5. Cimetidine*
  6. Ketoconazole
  7. Fluconazole
  8. Amiodarone*
  9. Ciprofloxacin
  10. Erythromycin
  11. Sulfonamides *
  12. Chloramphenicol
  13. Omeprazole
  14. Metronidazole