1
Q
ADME: Absorption — what is it?
A
How the drug gets into the bloodstream.
2
Q
Factors that increase absorption
A
High lipophilicity, large surface area, good perfusion.
3
Q
Factors that decrease absorption
A
Diarrhea/vomiting, achlorhydria, chelation interactions, delayed gastric emptying.
4
Q
First-pass metabolism (oral) meaning
A
Liver metabolizes some drug before systemic circulation → ↓ bioavailability (F).
5
Q
Distribution — key protein binding test point
A
Only FREE drug is active/toxic; low albumin → ↑ free drug.
6
Q
Low albumin examples
A
Older adults, liver disease, nephrotic syndrome → ↑ free fraction.
7
Q
Volume of distribution (Vd) meaning
A
Describes where drug “lives” (plasma vs tissues).
8
Q
High Vd implies
A
Drug distributes into tissues/fat → often longer half-life.
9
Q
Low Vd implies
A
Drug stays mainly in plasma.
10
Q
Metabolism: Phase I (CYP) basics
A
Oxidation/reduction/hydrolysis; can activate or inactivate drugs.
11
Q
Metabolism: Phase II basics
A
Conjugation → more water soluble → easier excretion.
12
Q
Elimination: main routes
A
Mostly kidney; also bile/lungs.
13
Q
Renal clearance drops when…
A
GFR decreases → drug accumulation → dose adjust.
14
Q
Steady state occurs after how long?
A
~4–5 half-lives (with constant dosing).
15
Q
After 1 half-life, % remaining
A
0.5
16
Q
After 2 half-lives, % remaining
A
0.25
17
Q
After 3 half-lives, % remaining
A
12.5%.
18
Q
After 4 half-lives, % remaining
A
6.25%.
19
Q
After 5 half-lives, % remaining
A
~3%.
20
Q
Loading dose does what?
A
Changes how fast you reach target concentration.
21
Q
Maintenance dose controls what?
A
Steady-state level.
22
Q
Clearance (CL) definition
A
Volume of plasma cleared of drug per unit time.
23
Q
If clearance decreases, what happens?
A
Drug levels rise unless dose lowered or interval extended.
24
Q
Full agonist definition
A
Produces maximal effect (Emax).
25
Partial agonist definition
Lower Emax; can block full agonist (classic test concept).
26
Competitive antagonist effect on curve
Shifts dose-response curve right (↑ dose needed), same Emax.
27
Noncompetitive/irreversible antagonist effect
Lowers Emax.
28
CYP inhibitors do what to substrate levels?
Increase substrate drug levels → ↑ toxicity risk.
29
CYP inducers do what to substrate levels?
Decrease substrate drug levels → ↑ failure risk.
30
Common CYP inhibitors (raise levels)
Amiodarone, macrolides (clarithro/erythro), azoles, cimetidine, grapefruit, protease inhibitors, verapamil/diltiazem.
31
Common CYP inducers (lower levels)
Rifampin, carbamazepine, phenytoin, phenobarbital, St John’s wort, smoking (CYP1A2).
32
Classic CYP test pattern
Amiodarone + warfarin → INR increases (inhibition).
33
Renal dosing “always mention” meds
DOACs, many antibiotics, digoxin, lithium.
34
Hepatic dosing cautions
Statins (caution), amiodarone (metabolism + toxicity), many psych meds.
35
QT-prolonging “big list” meds
Macrolides, fluoroquinolones, amiodarone, some antipsychotics.
36
Pregnancy contraindications (boards-style)
ACE inhibitors, ARBs, ARNIs, statins.
37
Thiazides examples
HCTZ, chlorthalidone.
38
Thiazides key adverse effects
Hyponatremia, hypokalemia, ↑ uric acid (gout), ↑ glucose.
39
Chlorthalidone vs HCTZ pearl
Chlorthalidone is longer acting.
40
ACE inhibitors examples
Lisinopril, enalapril.
41
ACE inhibitors best for
DM with albuminuria, CKD proteinuria, HFrEF, post-MI.
42
ACE inhibitor adverse effects
Cough, angioedema, hyperK, ↑ creatinine (mild rise expected).
43
ACE inhibitor contraindications
Pregnancy, bilateral renal artery stenosis.
44
ARBs examples
Losartan, valsartan.
45
ARBs benefit vs ACE
Similar benefits, no cough.
46
ARBs adverse effects/contra
HyperK; pregnancy contraindicated (similar to ACE).
47
CCBs: DHP example + role
Amlodipine; vasodilation.
48
DHP CCB adverse effects
Edema, flushing, headache.
49
CCBs: non-DHP examples + role
Diltiazem/verapamil; rate control.
50
Non-DHP CCB adverse effects
Bradycardia; constipation (verapamil); avoid in HFrEF.
51
Beta blockers: when NOT first-line
Uncomplicated HTN (usually not first-line).
52
Beta blockers strong indications
CAD/angina, post-MI, arrhythmias, HFrEF (carvedilol/metoprolol succinate/bisoprolol).
53
Beta blocker adverse effects
Bradycardia, fatigue, ED, masks hypoglycemia; bronchospasm (nonselective).
54
ACE/ARB/ARNI absolute “don’t miss”
Contraindicated in pregnancy.
55
Non-DHP CCB absolute “don’t miss”
Avoid in HFrEF.
56
Beta blocker absolute contraindications
Severe bradycardia/heart block; acute decomp HF initially.
57
High-intensity statins (≥50% LDL reduction)
Atorvastatin 40–80 mg; Rosuvastatin 20–40 mg.
58
Moderate-intensity statins (30–49% LDL reduction)
Atorva 10–20; Rosu 5–10; Simva 20–40 (examples).
59
Who gets high-intensity statin (big 2)
Clinical ASCVD; LDL ≥190.
60
Diabetes age 40–75 statin intensity
At least moderate; consider high if multiple risk factors.
61
Primary prevention statin decision tool
Risk calculation + risk enhancers.
62
Statin titration logic
Target % LDL reduction (thresholds may apply in some scenarios).
63
When to recheck lipids after start/change
~4–12 weeks, then every 3–12 months.
64
Ezetimibe role
Add if not at goal on max tolerated statin.
65
PCSK9 inhibitors role
Very high risk/familial/persistent high LDL despite statin ± ezetimibe.
66
Statin adverse effects
Myalgias, ↑ LFTs (rare severe), very rare rhabdo.
67
Statins with biggest CYP interaction concern
Especially simvastatin (and others) with CYP inhibitors.
68
Meds that reduce future CV events (big picture)
Statins; BP control meds in high risk; antiplatelets when indicated (secondary prevention); HF guideline meds.
69
HFrEF “4 pillars” (mortality benefit)
ARNI (or ACE/ARB) + evidence beta blocker + MRA + SGLT2 inhibitor.
70
Evidence-based beta blockers for HFrEF
Carvedilol, metoprolol succinate, bisoprolol.
71
MRA examples
Spironolactone, eplerenone.
72
SGLT2 inhibitor examples
Dapagliflozin, empagliflozin.
73
HF symptom relief meds (not mortality)
Loop diuretics: furosemide, torsemide, bumetanide.
74
HF monitoring labs
Creatinine + potassium with ACE/ARB/ARNI/MRA/SGLT2i.
75
Expected creatinine change with RAAS meds
Mild rise can be expected; watch large jumps/hyperK.
76
ARNI key indication
Chronic symptomatic HFrEF to reduce mortality/hospitalizations.
77
ARNI ACE inhibitor washout
Stop ACE inhibitor 36 hours before starting ARNI.
78
ARNI contraindications
History of angioedema; pregnancy.
79
ARNI monitoring
BP, potassium, renal function.
80
A-fib rate control options
Beta blocker OR diltiazem/verapamil (avoid non-DHP in HFrEF); digoxin sometimes.
81
Digoxin best niche in A-fib
HFrEF + sedentary patient (sometimes).
82
A-fib rhythm control options
Cardioversion; antiarrhythmics; ablation.
83
CHA2DS2-VASc purpose
Stroke risk stratification → anticoagulation decision.
84
Higher CHA2DS2-VASc score implies…
Anticoagulation indicated (commonly men ≥2; women ≥3 in many frameworks).
85
DOACs preferred in which A-fib?
Non-valvular A-fib.
86
Warfarin preferred for which A-fib scenarios?
Mechanical valves; moderate-severe mitral stenosis; or when DOAC not appropriate.
87
Amiodarone major toxicities
Pulmonary toxicity; thyroid dysfunction; hepatotoxicity; corneal deposits; photosensitivity/blue-gray skin.
88
Amiodarone cardiac risk
QT prolongation (torsades less common than expected but still caution).
89
Amiodarone major interactions
Warfarin, digoxin, many statins (↑ levels).
90
VTE treatment phases
Initial/acute → short-term → extended (based on provoked vs unprovoked + bleeding risk).
91
Common VTE agents
DOACs (apixaban/rivaroxaban); LMWH (enoxaparin); warfarin (often needs bridging depending scenario).
92
VTE complications
Bleeding; HIT (heparin); recurrent VTE; post-thrombotic syndrome.
93
DOAC Xa inhibitors
Apixaban, rivaroxaban, edoxaban.
94
DOAC direct thrombin inhibitor
Dabigatran.
95
Parenteral direct thrombin inhibitors (HIT)
Argatroban, bivalirudin.
96
Anticoagulation absolute contraindication
Active major bleeding.
97
Pregnancy anticoagulation pearl
Warfarin generally contraindicated; heparins preferred.
98
Severe renal impairment anticoagulation
Caution/avoid some DOACs; adjust doses.
99
Clopidogrel key mechanism/prodrug detail
P2Y12 inhibitor prodrug; needs CYP2C19 activation.
100
Clopidogrel reduced effect with…
Poor CYP2C19 metabolizers or CYP2C19 inhibitors.
101
Ticagrelor key difference vs clopidogrel
P2Y12 inhibitor NOT a prodrug; faster/more potent.
102
Ticagrelor key adverse effects
Dyspnea; bradyarrhythmias.
103
Ticagrelor interactions
Strong CYP3A inhibitors/inducers.
104
DAPT scenario use
Ticagrelor or clopidogrel + aspirin used in ACS/PCI (scenario-based).
105
Allergic rhinitis most effective first-line for persistent symptoms
Intranasal corticosteroids (fluticasone, mometasone, budesonide).
106
Intranasal steroid adverse effects
Epistaxis, nasal irritation; rare septal perforation (technique-related).
107
Preferred antihistamines for rhinitis
2nd gen: cetirizine, loratadine, fexofenadine.
108
2nd gen antihistamine sedation pearl
Cetirizine > loratadine/fexofenadine for sedation.
109
Asthma controller big picture
ICS-based; often ICS-formoterol strategies; escalate ICS dose, add LABA, consider LAMA, then biologics for severe phenotypes.
110
Asthma “don’t mess up” rule
LABA should NOT be used alone—must be paired with ICS.
111
Asthma red flag
SABA overuse → poor control.
112
COPD class-based backbone
LAMA/LABA bronchodilators.
113
COPD when to add ICS
Appropriate phenotypes (exacerbations, eosinophils); watch pneumonia risk.
114
COPD supportive management
Vaccines, smoking cessation, pulmonary rehab, oxygen when indicated.
115
Roflumilast indication
PDE-4 inhibitor for severe COPD with chronic bronchitis + frequent exacerbations.
116
Roflumilast adverse effects
Weight loss, GI upset, insomnia, mood changes (watch depression).
117
Chronic azithromycin role in COPD
Reduces exacerbations in select patients.
118
Chronic azithromycin adverse effects
QT prolongation, hearing loss, resistance.
119
ICS adverse effects (general)
Oral candidiasis, dysphonia; ↑ pneumonia risk in COPD.
120
Inhaled beta agonist adverse effects
Tremor, tachycardia, hypokalemia (high doses).
121
Montelukast (LKTRA) major warning
Neuropsychiatric effects (boxed warning) → monitor mood/sleep.
122
Asthma biologic: anti-IgE
Omalizumab.
123
Asthma biologics: anti–IL-5/IL-5R
Mepolizumab, reslizumab, benralizumab.
124
Asthma biologic: anti–IL-4/13
Dupilumab.
Nurs 502
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