-
Biguanide:
Metformin
- MOA: decreases glucose production, intestinal absorption, improves insulin sensitivity
- SE: Diarrhe, N/V/flatulence, vit B12 deficency, weight neutral,
- CI: Scr >1.5 (males), 1.4 (females), CrCl <60, metabolic acidosis, w iodinated contrast media, Hypoxia, Hepatic failure
- BBW: Lactic Acidosis
- PREG: B
-
Sulfonylureas:
Chlorpropamide, Glipizide, Glimepiride, Glyburide
- MOA: stimulate insulin secretion from pancreatic beta cells.
- SE: Hypoglycemia, weight gain
- CI: w use of Meglitinides (same MOA)
- Warning: Sulfa Allergy caution
- PREG: C
-
Meglitinides:
Repaglinide, Nateglinide
- MOA: stimulate insulin secretion from pancreatic beta cells
- SE: Hypoglycemia, mild weight gain, URTI
- CI: w use of Sulfonylureas (same MOA)
- PREG: C
-
Thiazolidinediones (TZD)
Pioglitazone, Rosiglitazone
- MOA: PPARgama agonist (increases peripheral insulin sensitivity therefore glucose uptake)
- SE: peripheral edema, weight gain, URTI, CHF, LFTs
- Warning: not if active bladder cancer
- BBW: HF NYHA class III/IV
- PREG: C
-
Alpha-Glucosidase Inhibitors
Acarbose, Miglitol
- MOA: AG-I stops conversion of saccharides to glucose in the brush border of the SI
- SE: GI effects (flatulence, D, abdominal pain), weight neutral
- CI: IBD, Colonic ulceration, intestinal obstruction
- PREG: B
-
Dipeptidyl peptidase IV inhibitors (DPP-4)
Sitagliptin, Saxagliptin, Linagliptin, Alogliptin
- MOA: prevent break down of incretin hormones, glucagon-like peptide-1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP) (increase insulin release from pancreatic beta cells, decrease glucagon secretion from pancreatic alpha cells)
- SE: URTI, UTI, nasopharyngitis, edema, rash, hypoglycemia, (rare-pancreatitiis), weight neutral
- PREG: B
-
Sodium Glucose Co-Transporter-2 Inhibitor (SGLT2)
Canagliflozin (Invokana)
- MOA: increases urinary glucose excretion in proximal renal tubules
- SE: Female genital mycotic infections, UTI, hyperkalemia,↑ (urination, thirst), hypo (volemia, tension, hypoglycemia)
- CI: CrCl<30, ESRD, on dialysis
- Caution: may lower insulin, or insulin secretagogue
- PREG: C
-
Glucagon-Like Peptide-1 agonist (GLP-1)
Exenatide (Byetta)
Liraglutide (Victoza)
MOA: ↑ insulin secretion, ↓ glucagon secretion, slow gastric empyting, improve satiety
- SE: Nausea, V/D/C, Hypoglycemia, weight loss
- Warning: Pancreatitis (hx of pancreatitis, gallstones, alcoholism, high triglycerides), CrCl <30, family hx thyroid cancers
- BBW: possible thyroid C-cell carcinoma,
- PREG: C
-
Synthetic Amylin
Pramlintide (Symlin)
- MOA: produced by beta cells for postprandial glucose control, slow gastric emptiying, prevents increased serum glucose, increases satiety
- SE: Hypoglycemia (reduce meal-time insulins by 50%), Nausea, anorexia, weight loss
- CI: gastroparesis, hypoglycemia unawareness
- BBW: co-administration of insulin
- PREG: C
-
Bile Acid Binding Resins
Colesevelam (Welchol)
- MOA: blocks reabosrption but unknown how it improves glycemic control.
- SE: Constipation, N, bloating, dyspepsia, ↑ TG (5%),
- CI: bowel obstruction, TG>500, hs TG induced pancreatitis
- PREG: B
-
RA Biologic Agents: TNFa-I
Etanercept (Enbrel)
Adalimubab (Humira)
Infliximab (Remicade)
Certolizumab (Cimzia)
Golimumab (Simponi)
- MOA: Tumor Necrosis Factor-α-I
- SE: injection site reactions, HA, N
- CI: active systemic infection
- BBW: Serious infections, lymphomas and malignancies, reactivation of latent TB
- PREG: B
-
RA Biologic Agents: CD20 B-cell
Rituximab (Rituxan)
- SE: flu-like symptoms, bone marrow supression, angioedema
- BBW: fatal infusion reactions, Progressive multifocal leukoencephalopathy (PML), Tumor lysis (acute renal failure), SJS, TEN
- PREG: C
-
RA Biologics:
Anakinra (Kineret) IL-1 receptor antagonist
Abatacept (Orencia) T-cell-I (Binds CD80, 86)
Tocilizumab (Actemra) IL-6 receptor antagonist
- Warning: latent TB
- SE: injection site reations, HA, bone marrow suppression,
- PREG: B (anakinra), C
-
Hypothyroid treatment:
levothyroxine (Synthroid, Levothroid, Levoxyl)
Thyroid Desiccated (Arnour thyroid)
Liothyronine (T3) (Cytomel, Triostat)
Liotrix (T3, T4) (Thyrolar)
- MOA: replaces thyroid hormone
- SE: none if dosed correctly, hyper/hypo thyroid symptoms otherwise,
- BBW: not for obesity or weight loss
- CI: Acute MI, Thyrotoxicosis, uncorrected adrenal insufficiency
- PREG: A
-
Hyperthyroid treatment:
Propylthiouracil (PTU) (Propyl-Thyracil)
Methimazole (Tapazole)
- MOA: blocks oxidation of iodine in thyroid gland
- SE: GI upset, HA, rash, constipation, SLE-like syndrome, Hepatitis, agranulocytosis
- PREG: D, PTU preferred in 1st Trimester, Methimazole in 2, 3rd trimester
-
Immunosuppressive agents:
Antithymocyte Globulin
Atgam (Equine)
Thymocyte (Rabbit)
- MOA: binds T-lymphocytes (activated)
- SE: anaphylaxis, flu-like symptoms, rash, leukopenia, chest pain,
- BBW: anaphylaxis- under direct supervision of experienced physician
- PREG: C
-
Immunosuppressive agents: IL-2 r antagonist
Basiliximab (Simulect)
- MOA: monoclonal antibody prevents activated T-cell
- SE: Hypertension, GI upset N/V/cramping, URTI, cough
- BBW: under physicians care when administered
- PREG: B
-
Cordicosterioids
- MOA: supress inflammation and humoral immune responses
- Short term SE: fluid retention, stomach upset, emotional instability, insomnia, weight gain, ↑ (glucose, BP, and appetite)
Long term SE: Adrenal suppression, impaired wound healing, Glaucoma, osteoporosis, GI bleeding, fat redistribution
-
Immunosuppressive agents: T-lymphocyte I
Mycophenolate (CellCept)
Mycophenolic Acid (Myfortic)
Azathoprine (Azusan, Imuran)
- MOA: inhibit B cell, T-lymphocyte proliferation by altering purine synthesis
- SE: GI upset, bone marrow suppression infections, LFT,
- BBW: Infections, lymphomas,
- Warning: Mycophenolate (congenital malformations, abortifactant), Azathioprine (hematologic toxicities, mutagenic potential)
- PREG: D
-
Immunosuppressive agents: Calcineurin Inhibitors
Tacrolimus (Prograf, Astagraf)
Cyclosporine (Neoral, Gengraf, Sandimmune, Restasis)
- MOA: inhibits T-lymphocyte activiation (unknown)
- SE: Severe GI upset, Nephrotoxicity, QT prolongation, Hyperglycemia, infections, UTI,
- Warning: Cyclosporine- gingival hyperplasia. Tacrolimus not for liver transplant,
- BBW: infection, lymphoma, Renal impairment
- PREG: C
-
Immunosuppressive agents: Mammalian Target Rapamycin Kinase Inhibitor (mTor)
Everolimus (Zortress, Afinitor)
Sirolimus (Rapamune)
Belatacept (Nulojix)
- MOA: inhibits T-lymphocyte activation and proliferaction (synergistic w CNIs)
- SE: GI upset, pneumonia, hyperglycemia, high lipid panel, electrolyte depletion
- BBW: infection, lymphoma
- Warning: Sirolimus, Belatacept not for liver transplant
- PREG: C
-
Bisphosphonates:
Alendronate (Fosamax, Binosto)
Risedronate (Actonel, Atelvia)
Ibandronate (Boniva)
Zoledronic Acid (Reclast) Injectable
- MOA: inhibit osteoclast activity
- SE: Hypocalcemia, bone-joint-muscle pain, dyspepsia, N/V esophagitis, Jaw necrosis
- CI: inability to sit or stand for 30min after dose (hour for Ibandronate)
- Warning: after 3-5 years stop due to risk of femur fracture, exophageal cancer, osteonecrosis of jaw.
- PREG: C
-
Osteoporosis agent:
Teriparatide (Forteo)
- MOA: recombinant human PTH 1-34, stimulates new bone formation, depresses osteoclast activity
- SE: orthostasis, injection site reaction, hypocalcemia, increased HR
- BBW: Osteosarcoma
- PREG: C
-
Osteoporosis agent:
Denosumab (Prolia)
- MOA: monoclonal antibody binds nuclear factor-kappa ligand (RANKL) preventing osteoclast formation
- SE: fatigue, hypocalcemia, rash, limb weakness and pain, N, dyspnea, cough
- CI: hypocalcemia
- Warning: Osteonecrosis of jaw, esophagitis-to cancer, High risk agent
-
Testosterone Products:
AndroGel 1%
Testim gel 1%
Androderm Patch
Striant buccal tabs
Solution (Axiron)
Gel (Fortesta)
Depo-Testosterone IM
- MOA: replaces depleted hormones
- SE: Hepatotoxicity, sensitive nipples, gynecomastia, dyslipidemia, edema, creatinine and PSA increases
- BBW: exposure to children/women.
- CI: Brest-Prostate cancer,
- Warning: increased BPH symptoms, never apply to breast/genital area
-
Estrogen Products:
- MOA: estrogen replacement
- SE: N, bloating, breast tenderness, increased triglycerides and HDL
- CI: abnormal vaginal bleeding, Any clotting disorder or hx, liver disease, hormone dependent cancer.
-
Progestin Only products:
- SE: breast tenderness, HA, fatigue, moody,
- Warning: high risk of clots
-
Pain Management agent:
Acetaminophen (Tylenol)
Duel products with opioids
- MOA: prostaglandin synthesis-I, blocks pain impulse peripherally
- SE: Hepatotoxicity, rare but SJS, TEN, AGEP and nephrotoxicity
- BBW: Hepatotoxicity (>4g/day)
- PREG: B preferred agent in pregnancy
-
Aspirin and NSAIDS:
Ibuprofen (Motrin, Advil)
Naproxen (Aleve, Naprosyn)
Diclofenac (Cataflam, Voltaren)
Indomethacin (Indocin)
Piroxicam (Feldene)
Ketorolac (Toradol, Sprix)
- MOA: inhibit Cox, PG, and Thromboxane
- SE: Dyspepsia, heartburn, GI irritation/bleeding, renal impairment, CNS effects, Rare-SJS, TEN,↑ BP,
- CI: Aspirin in children (<16)w any viral infection, Avoid in 3rd trimester-C/D
- BBW: CV thrombotic events, GI bleed, CABG treatment, MEDGUIDE
- PREG: C/D in 3rd trimester
-
NSAIDs: COX-2 selective
Celecoxib (Celebrex)
Meloxicam (Mobic)
Etodolac (Lodine)
Nabumetone (Relafen)
- MOA: Selective COX-2 inhibition
- SE: Less GI complication than NSAIDS, Increased risk of MI/stroke, Nephrotoxicity,
- CI: sufonamide allergy (celebrex)
- BBW: CV thrombotic events, GI bleed, CABG treatment,
- PREG: C <30 weeks, D ≥30 weeks
-
Opioids:
- MOA: Mu receptor agonist
- SE: N/V/Constipation, CNS (sedation), pruritis, diaphoresis,
- BBW: Respiratory Depression
- PREG: B/C
-
Opioid agonist/SNRI:
Tramadol (Ultram, Ultracet)
Tapentadol (Nucynta)
- MOA: Mu agonist, SNRI
- SE: N/C, insomnia/sedation, HA,
- Warning: Seizure risk, Serotonin Syndrome
- BBW: Tapentadol- respiratory depression
- PREG: C
-
Addiction/Overdose:
Burenorphine (Butrans-patch, Buprenex-Inj)
Naloxone (Nalmefene)
Combo (suboxone)
- MOA: Buprenorphine (Mu agonist), Naloxone (opioid antagonist)
- SE: Sedation, HA, mental impairment, respiratory depression, N/V/C, dry mouth
- BBW: bupronorphine- QT prolongation (patch > 20mcg/hr)
- PREG: C
-
Muscle Relaxant/Spasticity agents:
Baclofen (lioresal)
Cyclobenzaprine (Flexmid, Amrix, Flexeril)
Tizanidine (Zanaflex)
Carisoprodol (Soma)
Metaxalone (Skelaxin)
Methocarbamol (Robaxin)
- MOA: depresses CNS activity- sedation and analgesic effects
- SE: Excessive sedation, dizziness, confusion
- BBW: avoid abrupt withdrawal of intrathecal baclofen causes organ failure and death
- PREG: B (Cyclobenzaprine) C (rest)
-
Triptans:
Almotriptan (Axert)
Eletriptan (Relpax)
Frovatriptan (Frova)
Naratriptan (Amerge)
Rizatriptan (Maxalt)
Sumatriptan (Imitrex, Sumavel)
Zolmitriptan (Zomig)
- MOA: 5HT1 receptor agonist
- SE: N, Somnolence, dizziness, paresthesias, chest/throat/neck tightness/pain
- CI: Cerebrovascular disease, uncontrolled HTN
- Warning: Serotonin syndrome w other 5HT drugs
- PREG: C
-
Gout Agent:
Colchicine (Colcrys)
- MOA: inhibits microtubule polymerization preventing neutrophil migration to gout related activity (exact unknown)
- SE: N/V/D (80%), Myelosuppression, myopathy, neuropathy
- CI: use of P-gp or 3A4 inhibitor in renal/hepatic impairment
- PREG: C
-
Gout Agent: Xanthine Oxidase Inhibitors
Allopurinol (Zyloprim)
Febuxostat (Uloric)
- MOA: block UA production
- SE: Hepatotoxicity, Rash, acute gout attacks, ↑ LFTs
- Warning: hypersensitivity reactions, SJS, TEN, HLA-B 5801 (allopurinol)
- PREG: C
-
Gout Agent: Uricosuric
Probenecid
- MOA: Inhibits UA reabsorption at proximal tubule
- SE: Hypersensitivity reaction, hemolytic anemia
- CI: w aspirin, UA kidney stones, blood dyscrasias, initiate during acute gout attack
- Warning: ↑ hemolytic anemia in G6PD deficiency, not recommended CrCl <50 (monotherapy)
PREG: B
-
Gout Agent:
Pegloticase (Krystexxa)
- MOA: recombinant uricase enzyme, converts UA to inactive water-soluble metabolite
- SE: Antibody formation, gout flare, infusion reaction, N, bruising urticaria
- BBW: anaphylactic reaction, highest if UA>6mg/dL
- Warning: acute flare upon initiation, do not use with Allopurinol
- CI: G6PD deficiency
- PREG: C
-
Thiazide Diuretics:
Chlorothiazide (Diuril)
Chlorthalidone (Thalitone)
Hydrochlorothiazide (Microzide, etc)
Indapamide
Metolazone (Zaroxolyn)
Methyclothiazide
- MOA: inhibit Na reabsorption in distal convoluted tubules
- SE: ↑ (UA, CH, TG, BG, Ca), ↓ (Na, Mg, K), photosensivity, rash,
- CI: Sulfonamide-derived drugs, anuria, renal decompensation (CrCl <30)
- PREG: B
-
Loop Diuretics:
furosemide (Lasix)
Bumetanide (Bumex)
Torsemide (Demadex)
Ethacrynic Acid (Edecin)
- MOA: inhibits reabsorption of Na and Cl in ascending loop of Henle
- SE: ↓ (K, Na, Mg, Cl, Ca), ↑ (UA, BG, TG, TC), photosensitivity, ototoxicity
- BBW: fluid and electrolyte depletion
- CI: Anuria
- PREG: C with extreme caution, semester specific
-
Potassium-Sparing Diurectics:
Amiloride (Midamor)
Triamterene (Dyrenium)
+HCTZ (Maxzide, Dyazide)
Spironolactone (Aldactone)
Eplerenone (Inspra)
- MOA: compete with aldosterone in distal convoluted tubule and collecting ducts
- SE: Hyperkalemia, ↑SCr, impotence, metabolic acidosis (rare), spironolactone (gynecomastia)
- BBW: Spironolactone has tumor risk
- CI: CrCl<30
- PREG: B (Amiloride, Eplerenone), D (Triamterene, Spironolactone)
-
Angiotensin-Converting Enzyme I (ACE-I)
Benazapril (Lotensin)
Captopril (Capoten)
Enalapril (Vasotec)
Lisinopril (Prinivil, Zestril)
Quinapril (Accupril)
Ramipril (Altace)
Fosinopril, Moexipril, Perindopril, Trandolapril
- MOA: inhibit enzyme conversion of AT-1 to AT-2
- SE: Cough, angioedema, hypotension, HyperKalemia
- BBW: Preg Cat D, death or injury to fetus
- CI: Angioedema, bilateral renal artery stenosis, not with Aliskiren in diabetes patients
- Warning: If GFR <60 not with ACE or ARB
- PREG: D
-
Angiotensin R Blocker (ARB):
Valsartan (Diovan)
Losartan (Cozaar)
Irbesartan (Avapro)
Candesartan (Atacand)
Olmesartan (Benicar)
Telmisartan (Micardis)
Eprosartan (Teveten)
Azilsartan (Edarbi)
- MOA: inhibits AT2 binding to vascular smooth muscle
- SE: Hyperkalemia, angioedema, hypotension, acute renal failure
- BBW: Preg Cat D: death or injury to fetus
- CI: Angioedema, bilateral renal artery stenosis, w aliskiren in diabetic patients
- Warning: if GFR <60 not with ACE or ARB
- PREG: D
-
Direct Renin Inhibitor:
Aliskiren (Tekturna)
- MOA: inhibits renin which converts angiotnsinogen to AT-1
- SE: Hyperkalemia, angioedema, hypotension
- BBW: Preg Cat D, injury or death to fetus
- CI: bilateral renal artery stenosis, w ACE or ARB in diabetic patient, Angioedema
- Warning: if GFR <60 no ACE or ARB
- PREG: D
-
Beta-Blockers:
General as a class
- MOA: inhibits NE at beta1 and 2 adrenergic receptors causing reduction of BP and HR
- SE: hypotenison, fatigue, dizziness, depression, reduced (libido, insulin secretion, HDL), increased (BP, TG, weight gain),
- BBW: not withdrawn abruptly,
- CI: 2nd or 3rd degree heart block, active asthma exacerbation, sinus bradycardia
- PREG: C/ D (atenolol)
-
Dihydropyridines (CCB):
Amlodipine (Norvasc)
Felodipine (Plendil)
Nifedipine (Adalat, Procardia, Afeditab)
Nicardipine (Cardene)
- MOA: inhibit Ca in slow (voltage) channel to dilate peripheral smooth muscle
- SE: HA, flushing, tachycardia/reflex, gingival hyperplasia
- PREG: C
-
Non-Dihydropyridines (CCB):
Diltiazem (Cardizem, Cartia, Dilacor, Tiazac)
Verapamil (Calan, Verelan)
- MOA: inhibit Ca in slow (voltage) channels of smooth muscle in myocardium (↓HR-neg inotrope) and reducing vasoconstriction
- SE: Edema, HA, AV block, bradycardia, hypotension Arrhythmias, HF, constipation, gingival hyperplasia
- CI: SBP<90, 2nd, 3rd degree heart block, acute MI, pulmonary ongestion, cardiogenic shock
- PREG: C
-
Central acting Alpha2 Agonist:
Clonidine (Catapres, Duracion-IV)
Guanabenz
Guanfacine (Tenex, Intuniv)
Methyldopa
- MOA: Stimulate alpha2 in brain reducing sympathetic outflow from the CNS
- SE:Bradycardia, drowsiness, hypotension, sexual dysfunction, depression, psychotic reactions,
- Warning: methydopa also hepatitis, myocarditis, hemolytic enemia, Lupus-like syndrome
- Do not stop abruptly, must taper
- PREG: B (Guanfacine, Methyldopa) C (Clonidine, Guanabenz)
-
Direct Vasodilators:
Hydralazine
+ Isosorbide dinitrate (BiDil)
Minoxidil
Isosorbide Mononitrate (Monoket)
- MOA: direct vasodilation of arteriioles, Isosorbide (venous side)
- SE: HA, dizziness, freflex tachycardia, palpitations, anorexia, Lupus-like syndrome
- CI: nitrates (PDE-5 I)
- Warning: need 10-12hr nitrate free interval
- PREG: C
-
Alpha Blockers: for (HTN not BPH)
Prazosin (Minipress)
Terazosin (Hytrin)
Doxazosin (Cardura)
- MOA: bind alpha1 receptors resulting in vasodilation or arterioles and veins
- SE: Orthostatic hypotension, syncope, fatigue HA, fluid retention, Priapism
- PREG: C
-
Statins: HMG-CoA reductase inhibitors
Atorvastatin (Lipitor)
Simvastatin (Zocor)
Rosuvastatin (Crestor)
Pravastatin (Pravachol)
Lovastatin (Mevacor, Altoprev)
Fluvastatin (Lescol)
Pitavastatin (Livalo)
- MOA: prevents conversion of HMG-CoA to mevalonate, rate limiting step in cholesterol synthesis
- SE: Myalgias, arthralgias rhabdomyolysis, cognitive impairment, ↑ (CPK, BG, A1C, cataracts, LFT)
- BBW: active liver disease, pregnancy, breastfeeding
- Warning: skeletal muscle effects
- PREG: X
-
Dyslipidemia: Other
Ezetimibe (Zetia)
+ simvastatin (Vytorin)
+ atrovastatin (Liptruzet)
- MOA: inhibits absorption of cholesterol at the brush border of SI
- SE: URTI, D arthralgias, myalgias, pain
- Warning: avoid in moderate to severe hepatic impairment
- PREG: C (alone)
-
Bile Acid Sequestrants/binding resins:
Cholestyramine (Questran, Prevalite)
Colesevelam (Welchol)
Colestipol (Colestid)
- MOA: bind bile acid in the intestine forming a complex excreted in feces
- SE: Constipation, dyspepsia, N, abdominal pain, cramping, gas, bloating, hypertriglyceridemia, LFTs
- CI: cholestyramine (complete biliary obstruction), Colesevelam (Bowel obstruction, TG>500, TG induced pancreatitis,
- Warning: Binds to everything (DDI)
- PREG: B
-
Fibrates:
Fenofibrate (Tricor, Trilipix, Firicor, Lipofen, Triglide)
Gemfibrozil (Lopid)
- MOA: PPARα activator, enhanced elimination and ↓ synthesis of VLDL
- SE: abdominal pain, dyspepsia, URTI, ↑ LFT and CPK
- CI: Severe Liver disease, CrCl<30, Gallbladder disease, nursing mothers
- Warning: myopathy, higher if w statin, diabetes, renal failure, hypothyroidism, risk of cholelithiasis
- PREG: C
-
Niacin (Vitamin B3):
Niacor, Niaspan, Slo-Niacin
- MOA: decreases rate of hepatic snthesis of VLDL (↓TG/LDL)
- SE: Flushing, pruritus, N/V/D/GI distress, hepatotoxicity, hyperglycemia, hyperuricemia, cough, orthostatic HTN
- CI: active liver diseasse, PUD, arterial bleeding
- Warning: caution unstable angina or acute MI, Hepatotoxicity
- PREG: C
-
Fish oil:
Omega-3 Acid ethyl Esters (Lovaza)
Icosapent ethyl (Vascepa)
- MOA: may be due to reduction of hepatic synthesis of TG
- SE: Eructation, dyspepsia, taste perversions (Lovaza), arthalgias (Vascepa), increased risk of bleeding
- Warning: hypersensitivity to fish/shellfish, possible Afib or flutter during 1st month
- PREG: C
-
Homozygous Familial Hypercholesterolemia (HoFH) agent:
Lomitapide (Juxtapid)
Mipomersen (Kynamro)
- MOA Lomitapide: inhibits microsomal triglyceride transfer protien (MTP) in endoplasmic reticulum, ↓ production of chylomicrons and VLDL
- MOA Mipomersen: oligonucleotide inhibitor of apo B-100 synthesis, lowers VLDL
- SE: D/N/V/C dyspepsia, abdominal pain, flatulence, chest back pain, ↑ LFTs
- BBW: Hepatotoxicity
- CI: active liver disease, w 3A4 inhibitors (Lomitapide)
- Warning: Gi SE significant could lower absorption
- PREG: X (Lomitapide) B (Mipomersen)
-
Positive Inotropes:
Digoxin (Lanoxin, Digitec)
- MOA: inhibits Na/K ATPase pump, results in positive inotropic (↑CO), and neg chronotropic effect (↓HR)
- SE: dizziness, HA, D/N/V, anorexia, mental disturbances
- CI: 2nd, 3rd degree heart block
-
Vasodilators:
Nesiritide (Natrecor)
Nitroglycerin
Nitroprusside (Nitropress)
- MOA: dilate smooth muscle venous but some arterial
- SE: hypotension, HA, tachycardia
- CI: SBP <100 (Nesiritide) SBP <90 (Nitroglycerin, Nitroprusside)
- BBW: Nitroprusside- Cyanide Toxicity
- PREG: C
-
Anticoagulants: Heparin
Heparin
- MOA: binds AT to inactivate thrombin (FIIa, FXa, IXa, XIa, XIIa) and plasmin, also prevents fibrinogen to fibrin
- SE: Bleeding, HIT, Hyperkalemia, Osteoporosis,
- BBW: contains benzyl alcohol, CI in neonates/infants
- CI: uncontrolled active bleeding, severe throbocytopenia, hx of HIT, Pork hypersensitivity
- Warning: do not give IM due to hematoma risk
- Antidote: Protamine
- PREG: C
-
Low Molecular Weight Heparin:
Enoxaparin (Lovenox)
Dalteparin (Fragmin)
- MOA: binds AT to inactivate thrombin (FIIa)(less than heparin), (FXa greater than heparin)
- SE: bleeding, thrombocytopenia, hyperkalemia, anemia
- BBW: epidural, spinal anesthesia or spinal puncture are at risk of hematoma and subsequent paralysis
- CI: Hx HIT, active major bleed, hypersensitivity to pork
- Warning: do not give IM (hematoma)
- Antidote: Protamine only 60%
- PREG: B
-
Indirect Factor Xa Inhibitors:
Fondaparinux (Arixtra SQ)
- MOA: synthetic pentasaccharide inhibits AT to indirectly inhibit FXa
- SE: Bleeding, Thrombocytopenia, anemia, N, injection site reation.
- BBW: hematoma risk in neuraxial anestheis (epidural, spinal, or spinal puncture and subsequent paralysis
- CI: Severe renal impairment CrCl<30, active major bleed,bacterial endocarditis, thrombocytopenia w antibodies, wt<50kg
- Warning: do not give IM (hematoma)
- Antidote: None
- PREG: B
-
Direct FXa Inhibitors:
Rivaroxaban (Xarelto PO)
Apixaban (Eliquis PO)
- MOA: directly bind to inhibit FXa
- SE: Bleeding
- BBW: Neuraxial anesthesia Epidural, spinal, or spinal puncture for risk of hematoma and subsequent paralysis
- CI: Active major bleeding, mod-severe hepatic impairment, severe renal impairment, avoid in prosthetic heart valves
- Antidote: None
- PREG: C
-
Direct Thrombin (FIIa) Inhibitors:
Argatroban (DoC in HIT)
Bivalirudin (Angiomax)
Desirudin (Iprivask)
- MOA: binds Thromin FIIa
- SE: Bleeding, anemia, hematoma
- CI: active major bleeding
- Antidote: None
- PREG: B
-
Vitamin K epoxide reductase enzyme (VKORC1):
Warfarin (Coumadin, Jantoven)
- MOA: binds VKORC1 reducing Vit K epoxide and clotting factors II, VII, IX, X, and protein C, S
- SE: Bleeding, skin necrosis, pruple toe syndrome
- BBW: may cause major or fatal bleeding
- CI: Hemmorrhagic tendencies, blood dyscrasias, Pregnancy, uncontrolled HTN
- Antidote: Vit K (Phytonadione, 4 F prothrombin, 3 F prothrombin)
- PREG: D/X
-
Glycoprotein IIb/IIIa receptor Antagonists (Gp IIb/IIIa:
Abciximab (ReoPro)(irreversible)
Eptifibatide (Integrilin)
Tirofiban (Aggrastat)
- MOA: binds platelet Gp IIb/IIIa inhibiting other factors from activating
- SE: Bleeding, Thrombocytopenia, hypotension
- CI: Thrombocytopenia (<100k), Active internal bleeding, surgery within 6 months, Hx stroke, severe uncontrolled HTN, Hypersensitivity to murine (abciximab)
- PREG: B (eptifibatide, Tirofiban), C (Abciximab)
-
P2Y12 Inhibitors:
Clopidogrel (Plavix)
Prasugrel (Effient)
Ticagrelor (Brilinta)
- MOA: binds P2Y12 subunit on ADP receptors on platelets
- SE: Bleeding, bruising, rash
- BBW: Cyp2C19*2,*3 allele neg (clopidogrel),
- CI: PUD, ICH,
- Warning: do not start 5-7 days before CABG (5 Clopid, Ticag) (7 prasugrel)
- PREG: B (Clop, Pras) C (ticag)
-
Fibrinolytics: STEMI only
Alteplase (t-PA, Activase)
Tenecteplase (TNKase)
Reteplase (Retevase)
Streptokinase (Streptase)
- MOA: binds fibrin and converts plasminogen to plasmin in clots
- SE: Bleeding, hypotension, intracranial hemorrhage, fever
- CI: active internal bleeding, Hx stroke, intracranial surgery/trauma (<3 months), aneurysm, aortic dissection, ischemic stroke (<3 months), Severe uncontrolled HTN, PUD, anticoagulants
- Warning: STEMI only
- PREG: C/ D (streptokinase)
-
Prostacyclin Analogues:
Epoprostenol (Flolan, veletri)
Terprostinil (Remodulin)
Iloprost (Ventavis)
- MOA: replace prostacyclin, vasodilation in pulmonary and systemic vascular beds
- SE: HA, N/V/D, anxiety, chest pain, palpitations, tachycardia, edema, jaw claudication
- Note: chronic use- anxiety, flu-like symptoms, jaw pain, thrombocytopenia
- PREG: B/ C (Iloprost)
-
Endothelin Receptor antagonists (ERAs):
All in REMS program
Bosentan (Tracleer)
Ambrisentan (Letairis)
Macitentan (Opsumit)
- MOA: blocks endothelin receptors on pulmonary artery smooth muscle blocking vsoconstriction, reduced Hgb
- SE: HA, URTI, edma, LFTs, spermatogenesis
- BBW: Hepatoxicity, Pregnancy
- CI: pregnancy, use w cyclosporine or glyburide
- PREG: X
-
Beta2 Agonists:
Short-Acting
Long-Acting
- MOA: Bind Beta2 receptors causing bronchial smooth muscle bronchodilation
- SE: Tremor, shakiness, cough, palpitations, hypokalemia, tachycardia, hyperglycemia
- BBW: Long-acting increase risk of asthma deaths
- PREG: C
-
Corticosteroids:
Inhaled
- MOA: depress migration of polymorphonuclear (PMN) leukocytes, fibroblasts, preventing inflammation
- SE: inhaled- dysphonia, oral candidiasis, cough, hoarseness, URTI, hyperglycemia, fractures, pneumonia, growth retardation
- CI: primary treatment of status asthmaticus
- PREG: C
-
Corticosteroids:
Systemic
- MOA: depress migration of polymorphonuclear (PMN) leukocytes, fibroblasts, preventing inflammation
- SE Short term: wt gain, increase appetite, fluid retention, emotional instability, insomnia, indigestion
- SE Long term: cushings, fat redistribution, impaired wound healing, dermal thinning, hyperglycemia/diabetes, osteoporosis, hirsutism, insomnia, nervousness, GI bleed
- CI: active systemic infection
- PREG: D
-
Leukotriene Modifying Agents:
Zafirlukast (Accolate)
Montelukast (Singulair)
Zileuton (Zyflo)
- MOA: Leukotriene-receptor antagonists, Zileuton is 5-lipoxygenase inhibitor stops formation
- SE: HA, dizziness, abdominal pain LFT, URTI, pharyngitis, sinusitis
- CI: Hepatic impairment (zafilukast), active liver disease (zileuton)
- Warning: neuropsychiatric events, Hepatotoxicity, churg-Strauss possible
- PREG: B
-
1st Generation Antihistamines:
Clemastine (Tavist)
Diphenhydramine (Benadryl)
Carbinoxamine (Karbinal)
Chlorpheniramine (Chlor-Trimeton)
Promethazine (Phenergan)
Brompheniramine
- MOA: block H1 receptors
- SE: Sedation, cognitive impairment, strong anticholinergic effects, seizures, arrhythmias
- CI: Carbinoxamine/ promethazine do not use in children <2, lactation, w MAO-I
- PREG: B/ C (promethazine, carbinoxamine)
-
2nd Generation Antihistamines:
Cetirizine (Zyrtec)
Desloratadine (Clarinex)
Fexofenadine (Allegra)
Levocetirizine (Xyzal)
Loratadine (Claritin)
Intranasal:
Azelastin (Astelin)
Olopatadine (Patanase)
- MOA: Blocks H1 receptors
- SE: less CNS effects then 1st gen
- Warnings: cardiovascular disease, diabetes, glaucoma, prostate enlargement, renal impairment, seizures, thyroid disorders
- PREG: B
-
Decongestants:
Phenylephrine (Sudafed PE)
Pseudoephedrine (Sudafed)
Intranasal:
Naphazoline (Privine)
Oxymetazoline (Afrin)
Phenylephrine (Neo-Synephrine)
Tetrahydrozoline (Tyzine)
Xylometazoline (Otrivin)
- MOA: alpha adrenergic agonists causing vasoconstriction
- SE: Cardiovascular stimulation, CNS stimulation, dizziness, HA, anorexia
- CI: 14 day of MAOI
- Warning: Caution: HTN, CV disease, hyperthyroidism, diabetes, bowel obstruction, gluacoma, BPH
- PREG: C
- Intranasal: stinging, sneezing, dryness, rebound congestion if used > 3 days
-
Erythropoietin Stimulation Agents:
Epoetin alfa (Epogen, Procrit)
Darbepoetin (Aranesp)
- MOA: stimulates bone marrow to produce RBC
- SE: Hypertension, fever, HA, arthralgia/bone pain, pruritis, N, cough thrombosis, edema, chills, dizziness
- BBW: ESAs increase risk of serious cardiovascular events, thromboembolic, target >11g/dL, CKD, Tumorogenesis
- CI: uncontrolled HTN, PRCA,
- PREG: C
-
SSRIs:
Fluoxetine (Prozac, Sarafem)
Paroxetine (Paxil, Brisdelle)
Fluvoxamine (Luvox)
Sertraline (Zoloft)
Citalopram (Celexa)
Escitalopram (Lexapro)
Vilazodone (Viibryd)(+ 5HT1a agonist)
- MOA: increases synaptic 5HT
- SE: Somnolence, insomnia, N, HA< tremor, diaphoresis, Sexual SE, SIADH, Restless leg, ↑ bleeding, fall risk
- BBW: suicidal thinking
- CI: SSRIs w MAOIs
- Warning: Citalopram >20mg d -Qt prolongation
- PREG: C/ D (Paroxetine)
-
SNRIs:
Venlafaxine (Effexor)
Desvenlafaxing (Pristiq)
Duloxetine (Cymbalta)
Levomilnacipran (Fetzima)
- MOA: increase synaptic supply of 5HT and NE
- SE: sexual dysfunction, insomnia, HA, N, tremor, bleeding, fall risk, HTN, pulse dilated pupils, dry mouth, constipation
- BBW: suicidal thinking
- PREG: C
-
TCAs:
Tertiary amines:
amitriptyline (Elavil)
Doxepin (Zonalon)
Clomipramine (Anafranil)
Imipramine (Tofranil)
Trimipramine (Surmontil)
Secondary Amines:
Nortriptyline (Pamelor)
Protriptyline (Vivactil)
Desipramine (Norpramine)
Amoxapine
Maprotiline
- MOA: NE and 5HT reuptake inhibitors and inhibitors of ACh and Histamine
- SE: QT prolongation, orthostatis, tachycardia, brymoutn, blurred vision, urinary retention, constipation, vivid dreams, weight gain Myoclonus
- BBW: suicidal thinking
- CI: w MAOIs. w urinary retention or narrow-angle glaucoma
- PREG: C (Tertiary)/ D (secondary)
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