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 T3/T4 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.