Top 300 Drugs – Selected Agents Vocabulary Review

Quick-Reference: Common Abbreviations

• pts = patients • Tx = treatment • HTN = hypertension • ASVD = atherosclerotic cardiovascular disease • HF = heart failure • NYHA = New York Heart Association functional class • MBD = metabolic bone disease • DM / DMT2 = diabetes mellitus / type 2 DM • GnRH = gonadotropin-releasing hormone • BPH = benign prostatic hyperplasia • AMI = acute myocardial infarction • CABG = coronary artery bypass graft • BUN = blood urea nitrogen

Endocrine / Metabolic Agents

Incretin-Based Therapies

• Exenatide (Byetta)
‑ GLP-1 receptor agonist → increases glucose-dependent insulin, slows gastric emptying, promotes satiety.
‑ Indication = DMT2.
‑ Forms/Strengths: Sub-Q sol $5\,\text{mcg}/0.02\,\text{mL}$ & $10\,\text{mcg}/0.04\,\text{mL}$ (IR); ER suspension $2\,\text{mg}$ pen.
‑ AE = hypoglycaemia, N/V/D, injection-site rxn; boxed → thyroid C-cell tumors (ER/Bydureon).

• Liraglutide (Victoza)
‑ GLP-1 analog; same physiologic actions as above + weight loss benefit.
‑ Indications = DMT2, chronic weight mgmt.
‑ Pen $18\,\text{mg}/3\,\text{mL}$.
‑ AE = N/V/D, hypoglycaemia; boxed → possible ↑ thyroid cancer risk.

DPP-4 Inhibitors

• Linagliptin (Tradjenta) – $5\,\text{mg}$ tab; risk hypoglycaemia when combined with SU/insulin.
• Saxagliptin (Onglyza) – $2.5$ & $5\,\text{mg}$; similar AE.
• Sitagliptin (Januvia) – $25$/$50$/$100\,\text{mg}$; similar profile.

Sulfonylureas

• Glimepiride (Amaryl) – $1$/$2$/$4\,\text{mg}$; stimulates β-cells, ↑ insulin sensitivity; watch weight gain/hypoglycaemia.
• Glipizide (Glucotrol/XL) – IR $5$/$10\,\text{mg}$; ER $2.5$–$10\,\text{mg}$; AE asthenia.

Thiazolidinedione

• Rosiglitazone (Avandia) $2$ & $4\,\text{mg}$; PPAR-γ agonist → ↑ insulin sensitivity; AE = edema, weight gain, ↑ LDL; caution HF/MI risk.

Bisphosphonate

• Ibandronate (Boniva) $150\,\text{mg}$ monthly (Tx or prophylaxis osteoporosis); MOA = osteoclast inhibition; AE dyspepsia, back pain, RTI.

Insulin Preparations (brief)

• Insulin NPH (Humulin N) – vials $100$ & $500\,\text{U/mL}$; pens $100$–$300\,\text{U/mL}$; AE weight gain, injection pain, bronchospasm (inhaled).
• Rapid-acting (Aspart NovoLog, Lispro Humalog), Long-acting (Detemir Levemir, Glargine Lantus) – strengths product-specific; same physiologic MOA.

Hormonal Agents

• Levonorgestrel (Plan B) – single dose $1.5\,\text{mg}$ emergency contraception; delays ovulation via GnRH suppression; AE heavier menses, N/V, ectopic risk.

• Testosterone (AndroGel) – multiple gels $1–2\%$, pumps $10–20.25\,\text{mg/actuation}$, patches $2$ & $4\,\text{mg}/24\,\text{h}$, etc.; indicated for male hypogonadism; AE PSA rise, BPH, secondary exposure precautions.

• Levothyroxine (Synthroid) – tabs $25$–$300\,\text{mcg}$, caps $13$–$200\,\text{mcg}$; synthetic $T_4$; do NOT use for weight loss.

• Thyroid desiccated (Armour) – tabs $15$–$325\,\text{mg}$; variable $T<em>3/T</em>4$ ratio; ineffective/toxic for obesity therapy.

Cardiovascular Agents

ACE Inhibitors (ACEI)

• Enalapril (Vasotec) – tabs $2.5$–$20\,\text{mg}$; sol $1\,\text{mg/mL}$; pro-drug → enalaprilat; indications = HTN, HF, CKD; AE ↑ SCr; CI pregnancy.
• Lisinopril (Prinivil/Zestril) – tabs $2.5$–$40\,\text{mg}$; solution $1\,\text{mg/mL}$; similar pharmacology/CI.
• Quinapril (Accupril) – $5$–$40\,\text{mg}$; AE nausea.
• Ramipril (Altace) – caps $1.25$–$10\,\text{mg}$; proven post-MI mortality benefit.

Angiotensin II Receptor Blockers (ARBs)

• Losartan (Cozaar) – $25$/$50$/$100\,\text{mg}$; HTN, stroke risk ↓, diabetic nephro-prophylaxis; AE HA; CI pregnancy.
• Olmesartan (Benicar) – $5$/$20$/$40\,\text{mg}$.
• Valsartan (Diovan) – $40$/$80$/$160$/$320\,\text{mg}$; HF, HTN, post-MI; AE dizziness/↑ BUN.

Beta-Adrenergic Blockers

• Labetalol (Normodyne) – $100$–$300\,\text{mg}$ tabs; mixed α1/β blocker; AE dizziness, fatigue.
• Metoprolol Succinate (Toprol-XL) – ER $25$–$200\,\text{mg}$; IR tartrate (Lopressor) also used; avoid abrupt withdrawal (ischemia).
• Nebivolol (Bystolic) – $2.5$/$5$/$10$/$20\,\text{mg}$; β1-selective with NO-mediated vasodilation.
• Propranolol (Inderal) – IR $10$–$80\,\text{mg}$, ER $60$–$160\,\text{mg}$; indications: angina, dysrhythmia, HTN, migraine prophylaxis; avoid abrupt stop.

Calcium-Channel Blockers

• Nifedipine (Adalat/Procardia) – ER $30$/$60$/$90\,\text{mg}$; caps $10$/$20\,\text{mg}$; AE flushing, HA.
• Verapamil (Calan, etc.) – IR $40$–$120\,\text{mg}$; multiple ER preps $120$–$360\,\text{mg}$; AE gingival hyperplasia.

Nitrates & Related Antianginals

• Isosorbide Mononitrate (Imdur) – ER $30$/$60$/$120\,\text{mg}$; IR $10$/$20\,\text{mg}$; AE dizziness/HA.
• Nitroglycerin (Nitrostat) – SL tabs $0.3$–$0.6\,\text{mg}$, ER caps $2.5$–$9\,\text{mg}$, sprays $0.4\,\text{mg}$, patches $0.1$–$0.8\,\text{mg/h}$, ointments/rectal; AE HA.
• Ranolazine (Ranexa) – $500$ & $1000\,\text{mg}$ ER tabs; inhibits late $I_{Na}$ to ↓ intracellular $Ca^{2+}$ → ↓ O₂ demand; chronic angina adjunct when HR/BP limited.

Lipid-Lowering Therapies

• Omega-3 Ethyl Esters (Lovaza) – caps $200$–$1200\,\text{mg}$; TG ↓ via ↓ hepatic VLDL synthesis; AE diarrhea.
• Statins

• Lovastatin (Altoprev) – IR $10$–$40\,\text{mg}$; ER $20$–$60\,\text{mg}$.
• Pravastatin (Pravachol) – $10$/$20$/$40$/$80\,\text{mg}$.
• Simvastatin (Zocor) – $5$–$80\,\text{mg}$ tabs; oral suspension $20$ or $40\,\text{mg}/5\,\text{mL}$.
• Rosuvastatin (Crestor) – tabs $5$/$10$/$20$/$40\,\text{mg}$; sprinkle caps same; AE arthralgia.
  • Niacin (Niaspan) – IR tabs $50$–$500\,\text{mg}$; ER caps/tabs $250$–$1000\,\text{mg}$; AE flushing/HA (counsel aspirin pre-dose).

Anticoagulants / Antiplatelets

• Enoxaparin (Lovenox) – prefilled $30$–$150\,\text{mg}$ syringes; anti-Xa/IIa; AE anemia/bleeding; neuraxial hematoma warning.
• Rivaroxaban (Xarelto) – $2.5$/$10$/$15$/$20\,\text{mg}$; oral Xa inhibitor; boxed → thrombotic rebound & spinal hematoma.
• Warfarin (Coumadin) – tabs $1$–$10\,\text{mg}$ (color-coded); vitamin K epoxide reductase inhibitor; narrow TI, numerous interactions.
• Prasugrel (Effient) – $5$/$10\,\text{mg}$; irreversible P2Y₁₂ blocker; ↑ bleeding esp >$75\,\text{y}$, CABG.
• Ticagrelor (Brilinta) – $60$ & $90\,\text{mg}$; reversible P2Y₁₂; AE dyspnea; avoid aspirin >$100\,\text{mg}$/day.

Diuretics & Electrolyte Modifiers

• Spironolactone (Aldactone) – tabs $25$/$50$/$100\,\text{mg}$; susp $25\,\text{mg}/5\,\text{mL}$; K-sparing/MR antagonist; tumorigenic in animals.
• Triamterene / Hydrochlorothiazide (Dyazide/Maxzide) – caps $37.5/25\,\text{mg}$; tabs $37.5/25$ & $75/50\,\text{mg}$; AE hypotension, hyperkalaemia.

α-Adrenergic Blocker

• Terazosin (Hytrin) – caps $1$/$2$/$5$/$10\,\text{mg}$; indications = BPH, HTN; AE asthenia, dizziness (first-dose syncope).

Vasopressin Antagonist

• Tolvaptan (Samsca) – $15$ & $30\,\text{mg}$; hyper-/euvolemic hyponatraemia; initiate in hospital, monitor $Na^+$ q6-8 h; avoid over-correction (>$12\,\text{mEq}/24\,\text{h}$).

Selected Agents from “Top 300” List (Items 37–50)

• Simvastatin (Zocor) • Quinapril (Accupril) • Ramipril (Altace) • Ranolazine (Ranexa) • Rivaroxaban (Xarelto) • Rosuvastatin (Crestor) • Spironolactone (Aldactone) • Terazosin (Hytrin) • Ticagrelor (Brilinta) • Tolvaptan (Samsca) • Triamterene/HCTZ (Dyazide) • Valsartan (Diovan) • Verapamil (Calan) • Warfarin (Coumadin)

Practical / Ethical / Clinical Connections

• Pregnancy Contra-indication across RAAS blockers (ACEI/ARB) due to fetal renal dysgenesis → counsel women of child-bearing age.
• Statins & pregnancy/lactation: category X (teratogenic, blocks fetal steroid synthesis).
• Thyroid & weight loss: FDA warns against off-label high-dose T₄ or desiccated thyroid for obesity; risk thyrotoxicosis → AF, osteoporosis.
• GLP-1 RAs offer cardiometabolic benefit (ASCVD ↓) – align with ADA/ACC guidelines covered in prior lectures.
• Warfarin vs DOACs: balance of monitoring (INR) vs fixed dosing; peri-procedural bridging considerations (enoxaparin).
• Tolvaptan REMS-like inpatient start highlights principle of "start-low/go-slow" where rapid electrolyte shifts cause osmotic demyelination.
• Testosterone transference risk (children/women) underscores counseling on hand-washing and shirt coverage after gel application.