PDA B2 Drugs & Terms Flashcards
Zileuton
Action: 5-Lipoxygenase (5-LOX) Inhibitor (no production of LTs)
Use: Asthma (prophylaxis or chronic treatment - not acute)
Route: Oral
S/E: Minimal, some inc. in liver enzymes
Metab: CYP1A2, 2C9, 3A4
Icatibant
Action: BK2 (Bradykinin) receptor (a GPCR) antagonist
Use: Treatment of Hereditary Angioedema (HAE, have defective/low C1 inhibitor protein), anti-inflammatory
Zafirlukast
Action: Cysteinyl leukotriene receptor antagonist (does NOT inhibit biosynthesis)
Use: Asthma (prophylactic or chronic treatment - not acute)
Route: Oral
S/E: Minimal
Metab: CYP2C9
Dinoprostone
AKA: PGF2
Action: breakdown of collagen, relaxes cervical SM, EP4 receptor –> increases cAMP; uterine contractions via EP1/3 receptors –> inc. Ca2+
Use: Cervical Ripening (Dilation) in pregnancy; termination of early pregnancy (up to 40x higher dose)
Route: Cervical gel; Vaginal suppository
S/E: GI-related, fever, uterine rupture
Metab:
Carboprost
AKA: PGF2alpha
Action: Causes uterine contractions via FP, (EP1/3 ?) inc. Ca2+
Use: Termination of 2nd trimester pregnancy; control postpartum hemorrhage
Route: IM; IV
S/E: GI-related, fever, uterine rupture
Metab:
Misoprostol
AKA: PGE1 analog
Action: Suppresses gastric acid production, stimulates EP3 on parietal cells (dec. cAMP, inc. mucin & bicarb. secretion), increase mucosal blood flow (EP2/4 receptors –> inc. cAMP)
Use: replacement therapy for ulcer prevention caused by long-term NSAID therapy
Route: Oral, 4x/day (short T1/2)
S/E: Diarrhea
Contra: Pregnancy (can terminate)
Alprostadil
AKA: PGE1
Action: Relaxes trabecular SM & dilates cavernosal aa’s; EP2/4 receptors –> inc. cAMP
Use: Erectile Dysfunction; keeps Ductus Arteriosus patent until surgery
Route: Intracavernois injection; IV
S/E: priapism; apnea in 10% of neonates, <2kg weight
Epoprostenol
AKA: PGI2
Action: Increase cAMP via IP receptor, pulmonary artery vascular SM dilation
Use: Primary Pulmonary Hypertension (rare idiopathic disease, young people, esp. Females
Route: Continuous IV infusion
S/E: Nausea, vomiting, headache, flushing, drug interactions w/ anti-platelet and other anti-HT drugs
Bimatoprost
AKA: PGF2alpha
Action: Inc. aqueous humor outflow via EP2/4 –> inc. cAMP; unknown mech. for eyelashes
Use: Glaucoma (Lumigan); Eyelash hypotrichosis (Latisse)
Route: Opthalmic soln
S/E: unwanted hair growth, eye redness/itching, eye color changes (more brown)
Etanercept
Action: TNFalpha receptor analog
Use: Anti-inflammatory
Infliximab
Action: mAb that binds TNFalpha
Use: Anti-inflammatory
Mifepristone
AKA: RU486
Action: Progesterone antagonist; Glucocorticoid antagonist
Use: Termination of pregnancy; Cushing’s Syndrome
Route:
S/E:
Spironolactone / Eplerenone
Action: competitive mineralocortocoid antagonist
Use: Diuretic (w/ Thiazide or loop diuretic) & for Cardiac fibrosis / hypertrophy
Route: Oral
Drospirenone
AKA:
Action: Mineralocortocoid antagonist; Progesterone AGONIST; androgen antagonist
Use: Diuretic; Hormone Replacement Therapy (HRT) & w/ estrogen, suppresses ovulation
Route:
S/E:
Prednisolone
AKA: Prednisone
Action: Synthetic glucocorticoid
Use: Suppress autoimmunity (asthma, rh. arthritis, Crohn’s, SLE, etc.)
Route:
S/E: Cushing’s-like symptoms, acne, constipation, mood swings. Osteoporosis a risk in long-term use
Azathioprine
AKA: Prodrug form of 6-MP
Class: Cytotoxic Agent / Immunosuppressant
Action: Metabolite TIMP blocks ATase, preventing purine synthesis and hindering T&B cell proliferation
Use: Autoimmune diseases, prevention of transplant rejection, historically a cancer drug
Route: Mainly oral, can be IV
S/E: Nausea, vomiting, fatigue, anemia, acute pancreatitis, hair loss
Contra: Pt’s w/ TPMT deficiency (severe marrow suppression)
Drug Int: Allopurinol (inhibits XO, which degrades TIMP)
6-Mercaptopurine
Class: Cytotoxic Agent / Immunosuppressant
Action: Metabolite TIMP blocks ATase, preventing purine synthesis and hindering T&B cell proliferation
Use: Autoimmune diseases, prevention of transplant rejection, historically a cancer drug
Route: Mainly oral, can be IV
S/E: Nausea, vomiting, fatigue, anemia, acute pancreatitis, hair loss
Contra: Pt’s w/ TPMT deficiency (severe marrow suppression)
Drug Int: Allopurinol (inhibits XO, which degrades TIMP)
Cyclophosphamide
Class: Cytotoxic / Immunosuppressant
Action: Alkylating agent, cross-links DNA. More effective on B cells.
Use: Autoimmune diseases w/ other drugs. Not for preventing graft rejection.
Route: Oral
S/E: Bone marrow suppression
Methotrexate
Class: Cytotoxic Agent / Immunosuppressant
Action: Dihydrofolate reductase (DHFR) inhibitor [DHF –> THF blocked], inhibits DNA synthesis (purines, thymidine)
Use: Autoimmune diseases
S/E: Hepatotoxicity
Mycophenolate Mofetil
Class: Cytotoxic agent / Immunosuppressant
Action: prodrug of mycophenoloc acid, IMP dehydrogenase inhibitor (IMP –> GMP). Blocks de novo (not salvage) GMP synth. Lymphocytes MUST use de novo path for GMP, so drug is selective
Use: For autoimmunity & preventing graft rejection. Used w/ cyclosporine & coriticosteroids.
Route: Oral
S/E: GI effects, infection, leukopenia, anemia
Contra: pregnancy (pregnancy loss & teratogen)
Cyclosporine
Class: Cyclosporine-like
Action: Inhibits T cell prolif. via blocking IL-2 production. Calcineurin signaling pathway inhibitor.
Use: prev. of graft rejection. More effective, fewer s/e than others
Route: Oral
S/E: reversible Nephrotoxicity (25-40% pts), hepatotoxicity
Tacrolimus
Class: Cyclosporine-like
Action: Inhibits T cell prolif. via blocking IL-2 production. Binds FK BP-12 - Calcineurin signaling pathway inhibitor. 50-100x more potent than cyclosporin
Use: prev. of graft rejection. More effective, fewer s/e than others
Route: Oral
S/E: less Nephrotoxicity & hepatotoxicity than cyclosporine
Sirolimus
Class: Cyclosporin-like
Action: Binds FK BP-12, BUT THEN binds mTOR, blocking G1–>S phase transition (DOES NOT BLOCK CALCINEURIN)
Use: prev. Of graft rejection; coating of cardiac stents
Metyrapone
Class: Steroid synthesis Inhibitors
Action: Blocks 11-beta hydroxylation, synth stopped at 11-deoxycortisol. ACTH levels increase, driving rerouted production into 17-ketosteroids
Use: Diagnostic testing
Aspirin / Acetylsalicylic Acid / ASA
Class: NSAID
Action: Prodrug to Salicylic acid, Irreversible inhibitor of COX-2 via acetylation of Ser230
Use: Anti-inflammatory, Analgesia, Anti-pyretic; dose dept. uricosuric effects - compete with urate transporter @ high doses
Route: Oral (IV available). Chewing increases absorption rate
Other Preparations: Buffered (less pH alteration in stomach) and enteric (dissolves in intestines, bypassing potl. Stomach irritation)
Elim: Renal
S/E: GI irritation,
Lysergic acid diethylamide
Class: 5-HT agonist
Action: Rel. Nonspecific 5-HT2 receptor agonist. Potent hallucinogen
Buspirone
Class: 5-HT agonist
Action: 5-HT1A receptor partial agonist
Use: Antianxiety
Sumatriptan
AKA: Imitrex
Class: 5-HT agonist
Action: 5-HT1D receptors on cerebral blood vessels. Inhibit CGRP release, promote vasoconstriction.
Use: Treatment of existing migraine headaches.
S/E: GI effects, dizziness, flushing, angina
Contra: Recent Mi
Fluoxetine
Class: Indirect 5-HT agonist
Action: SSRI, increases 5-HT in synapse by preventing reuptake
Use: Affective disorders, OCD, panic attacks
S/E: Sexual dysfunction, nausea
Phenelzine
Class: Indirect 5-HT agonist
Action: inhibits MAO, blocking metabolism of 5-HT, NE, DA.
Use: Affective disorders, narcolepsy (NE)
S/E: Hypertensive crisis
Cyproheptadine
Class: 5-HT Antagonist
Action: 5-HT2 receptor antagonist AND histamine H1 antagonist
Use: Allergies, pruritis, urticaria, carcinoid syndrome (5-HT producing tumor)
Ondansetron
Class: 5-HT antagonist
Action: 5-HT3
Use: Treats post-chemo nausea and vomiting via CNS and GI action
Alosetron
Class: 5-HT antagonist
Action: 5-HT3
Use: Diarrhea - typically IBS in women
S/E: Potential severe GI effects; prescribing is restricted
Verapamil
Class: Phenylalkylamine CCB
Action: Binds deep within L-Type Ca2+ Channel (a1 subunit), use-dependent, slows SA firing and AV conduction with some coronal and periph. vasodilation
Use: Supraventricular arrhythmias (incl. Supravent. Tachycardia)
Route: Oral (high first pass effect) or IV
S/E: Hypotension, headache, flushing, edema, CONSTIPATION, may exacerbate CHF or cause AV block
Int: Other CCBs
Diltiazem
Class: Benzothiazepine CCB
Action: Binds deep within L-Type Ca2+ Channel (a1 subunit), use-dependent, slows SA firing and AV conduction with some coronal and periph. vasodilation
Use: Supraventricular arrhythmias, angina, cardiac ischemia
Route: Oral (low first pass effect) or IV
S/E: Hypotension, headache, flushing, edema, may exacerbate CHF or cause AV block
Int: Other CCBs
Nifedipine
Class: 1,4-Dihydropyridine CCB
Action: Binds SURFACE of L-Type Ca2+ Channel (a1 subunit) of ARTERIES (not veins), voltage-dependent, cause coronary and peripheral vasodilation
Use: Hypertension, often with a beta blocker (propranolol)
Route: Oral (low first pass effect) or IV
S/E: Reflex tachycardia (treat w/ propranolol)
Contra: tachyarrythmias
Int: Other CCBs
Amlodipine
Class: 1,4-Dihydropyridine CCB
Action: Slow-acting, binds SURFACE of L-Type Ca2+ Channel (a1 subunit) of ARTERIES (not veins), voltage-dependent, cause coronary and peripheral vasodilation
Use: Hypertension, often with a beta blocker (propranolol)
Route: Oral (half-life compatible with 1x/day)
S/E: Reflex tachycardia - slow acting, so less so than Nifedipine
Contra: tachyarrythmias
Int: Other CCBs
Dopamine, Fenoldapam, Atriopeptins, Caffeine
Class: Renal vasodilator (diuretic)
Action: Increase RBF w/o changing GFR (decrease filtration fraction) and decrease prox. Tubule Na+ reabsorption, weak diuretics
Use: Limited - Hypertensive crisis & shock
Route: Some orally active
Mannitol
Class: Osmotic Diuretic
Action: Act in tubular lumen as freely filtered, non-reabsorbable solute, osmotically increases excretion of Na, K, Cl, H2O, mannitol
Use: Edema, Glaucoma, Acute renal failure
Route: IV ONLY
S/E: Hypokalemia (?)
Acetazolamide
Class: Carbonic Anhydrase Inhibitor
Action: Filtered & secreted by organic acid transporter (OAT) into lumen, inhib, CA in prox. And dist. Tubule, increase excretion of Na, K, bicarb, and H2O
Use: Glaucoma, alkalinize urine (dec. drug toxicity), altitude sickness, anticonvulsant - acidosis inhibits effects
Route: Oral
S/E: Metab. Acidosis, Hypokalemia
Furosemide, Bumetanide, Ethacrynic Acid
Class: Loop Diuretics
Action: Filtered/secreted by OAT, inhibits Na-K-2Cl symporter, increase excretion of Na, K, Cl, H2O in medullary and cortical parts of ascending loop of Henle; rapid, powerful (20-30% Na), and short-acting
Use: cardiac, renal, hepatic, or pulmonary edema; hypertension
Route: Oral and IV
S/E: Hypokalemia, Alkalosis, Hypovolemia, Hyperuricemia, Hyperglycemia (furosemide only), Ototoxicity
Hydrochlorothiazide, Metolazone
Class: Thiazide-like Diuretics
Action: Excreted/secreted by OAT, Inhibits Na-Cl symporter, cortical segment of dist. Tubule, incr. excretion of Na, K, Cl, H2O, long acting and moderate excretion (8-10% Na) - hypertonic urine, unable to dilute
Use: Edema from CHF, hypertension, hypercalciuria
Route: Oral
S/E: Hypokalemia, Alkalosis, Hyperuricemia, Hyperglycemia, Decrease GFR
Spironolactone, Eplerenone
Class: Aldosterone Antagonist / K+ Sparing Diuretic
Action: Block aldosterone’s effect on collecting duct, incr. Na excretion (2-3% of load) along with Cl and H2O, but WITHOUT K
Use: Edema, Hypertension, Improve survival in CHF, Used in combination with a more potent diuretic
Route: Oral
S/E: Hyperkalemia, Gynecomastia (mostly spironolactone)
Amiloride, Triamterene
Class: Na+ Channel Inhib. / K+ Sparing Diuretic
Action: Block Na entra into principal cells of collecting duct, increase Na (2-3% of load), Cl, and H2O excretion w/o K loss
Use: Edema, Hypertension, often used in combination with a more potent diuretic
Route: Oral
S/E: Hyperkalemia, Mild azotemia, Triamterene reduces RBF and GFR at high doses
Heparin (Sodium)
Class: Anti-coagulant
Action: Mix of sulfated polysaccharides, neg. charged. Increases rate of antithrombin 1000x by making active site more accessible to coagulation factors. Prevents clots, DOES NOT degrade clots.
Use: Acute venous thromboembolism, Cardiopulmonary bypass, prophylaxis against venous thrombosis
Route: IV or SQ
S/E: Bleeding, THROMBOCYTOPENIA (1-5%)
Contra: Bleeding, Uncontrolled HTN, Recent surgery of eye, brain, spinal cord
Note: does not cross placenta; useable during pregnancy
Enoxaparin / Dalteparin
AKA: Low-MW heparins
Class: Anticoagulants
Action: Poorly inhibits Thrombin via AT, but still significantly inhibits factor Xa via AT
Use: Acute & Prophylaxis for AVT, Acute unstable angina / MI, hip replacement surgery
Route: Parenteral
S/E: Bleed and thrombocytopenia risk lower than heparin
Contra: Bleeding, Uncontrolled HTN, Eye/Brain/Spinal Cord surgery, Renal impairment (metabolism)
Lepirudin / Bivalirudin
Class: Anticoagulants
Action: Direct inhibition of thrombin - blocks substrate binding site
Route: IV
Use: Same as other anticoagulants; heparin replacement for pts who have had thrombocytopenia
S/E: Bleeding
Contra: Same as other anticoagulants; Renal impairment (metabolism)
Fondaparinux
Class: Anticoagulant
Action: Directly inhibits Factor Xa
Use: DVT prevention during surgery, acute PE, acute DVT w/o PE
Route: SQ
S/E: Same as other anticoagulants
Contra: Same as others; renal impairment (excreted)
Protamine Sulfate
Class: Heparin antagonist
Action: Positively charged - binds and inactivates heparin 1:1
Use: Heparin OD w/ severe bleeding, reverse heparin after bypass surgery
S/E: Anaphylaxis (fish products, some insulin preps), severe pulmonary HTN, weak anticoagulant itself at high doses or alone
Warfarin
Class: Anticoagulant
Action: Vitamin K analogue - inhibition of VKORC1 prevents gamma-carboxylation (requires Vit K reduced) of prothrombin, factors VII, IX, X, Proteins C and S, impairing their functions. Affects synthesis, so takes up to days to be therapeutic.
Use: thromboembolism prophylaxis (Afib, prosthetic heart valves, dilated cardiomyopathy), venous TE treatment
Route: Oral
Metab: Liver CYP2C9 (*2 and *3 less active; drug/food interactions!), highly plasma protein bound
S/E: Bleeding, Purple Toe Syndrome, skin necrosis / gangrene (protein C deficiency)
Contra: Heparin contras, but also: CYP2C9 polymorph, VKORC1 variations, pregnancy (teratogen), liver/kidney diseases, Vit K deficiency
Dabigitran (Etexilate)
Class: Anticoagulant (Etexilate is given prodrug, via hydrolysis by esterase)
Action: Binds active site of both free AND fibrin-bound thrombin. Shorter T1/2 than warfarin
Use: Nonvalvular Afib w/ risk of stroke or embolism; prophylaxis in knee/hip replacement pts
Route: Oral
Monitoring: NONE
S/E: Bleeding (less than warfarin, but NO antidote), GI upset
Contra: Renal disease (Metab), liver disease (baseline coagulation impaired), PROSTHETIC HEART VALVES
Drug Int: Drugs that induce (rifampin) or inhibit (verapamil, quinidine, others) P-glycoprotein
Rivaroxaban
Class: Anticoagulant
Action: Directly binds and inhibits free and complexed/clot-bound Factor Xa (Pockets S1 and S4) to inhibit more thrombin activation - does not affect existing thrombin. Rapid onset and long duration.
Use: Same as dabigatran
Route: Oral
S/E: Bleeding
Monitoring: If needed (high risk), PT time
Metab: Hepatic CYP3A4/5, 2J2; Kidney AS WELL
Int: P-gp-affecting drugs
Alteplase
AKA: Recombinant Tissue Plasminogen Activator (t-PA)
Class: Thrombolytic
Action: Activates plasminogen to plasmin in order to lyse fibrin at a thrombus
Use: Acute MI, PE, DVT, Stroke
Route: IV (very short T1/2)
S/E: Bleeding (lyse thrombi; systemic lytic state). Greater risk in long term treatment.
Contra: Bleeding, Hx of cerebrovascular trouble, uncontrolled HTN, recent spinal cord surgery or trauma, brain tumor
Aminocaproic Acid
Class: Procoagulant: Plasminogen Inhibitor
Action: Binds Lys-binding sites on plasmin(ogen) to inhibit plasmin binding to fibrin
Use: Reverse acute bleeding effects of excessive fibrinolysis; conc. in urine so useful in stopping urinary tract bleeding
Dipyridamole
Class: Anti-platelet
Action: Inhibits PDE3/5 to increase cAMP in platelets, inhibiting their aggregation. Also a vasodilator.
Use: prophylaxis of thromboemboli in pts with prosthetic heart valves
S/E: Headache, GI upset; secondary prevention of MI or TIA
Ticlopidine, Clopidogrel, Prasugrel, Ticagrelor
Class: Anti-platelet
Action: via P2Y1/12 receptors, inhibit ADP-induced platelet aggregation. All irrev. EXCEPT Ticagrelor. Prasugrel: prodrug activated by esterase and then CYP3A4 & 2B6. Clopidogrel and Ticlopidine are prodrugs activated by CYP2C19.
Use: Angina, NSTEMI, STEMI, MI, Stroke, Periph. Vascular disease, manage pts during surgery
Route: Oral
SE: Bleeding; Ticagrelor - dyspnea; Ticlopidine - neutropenia (not used often)
Int: CYP metabolized drugs!!! See: Clopidogrel + aspirin + omeprazole
Cromolyn sodium
Class: antihistamine
Action: stabilizes mast cell membranes to prevent histamine release
Use: chronic control of asthma, bronchospasm prophylaxis, not for acute attack
Route: inhalation (also oral - mastocytosis, nasal - allergies, opthalmic - conjunctivitis)
S/E: Few
Omalizumab
Class: antihistamine Action: IgG mAb that binds circulating IgE (Fc region) to prevent mast cell activation Use: asthma? Route: SQ S/E: injection site rxn, anaphylaxis
Diphenhydramine
Aka: Benadryl
Class: Antihistamine (ethanolamine, 1st gen)
Action: H1 receptor blocker / inverse agonist. Inhibits capillary permeability but not BP or bronchoconstriction. CNS anticholinergic effects.
Use: allergies (rhinitis, uritcaria, conjunctivitis), non-prescription sleep aid, early stage Parkinson’s
Route: oral, nasal, opthalmic
S/E: profound sedation, paradoxical stimulation in children / overdose, atropine-like effects
Dimenhydrinate
Aka: Dramamine
Class: Antihistamine (ethanolamine, 1st gen)
Action: H1 receptor blocker / inverse agonist. CNS anticholinergic effects.
Use: Motion sickness, vestibular disorders
Route: oral, IV
S/E: sedation, paradoxical stimulation in children / overdose, atropine-like effects
Chlorpheniramine
Class: Antihistamine (alkylamine, 1st gen)
Action: H1 receptor blocker / inverse agonist. Inhibits capillary permeability but not BP or bronchoconstriction. CNS anticholinergic effects.
Use: allergies (rhinitis, uritcaria, conjunctivitis) - among most potent, with less drowsiness than diphenhydramine
Route: Oral, IV, IM, SQ
S/E: sedation, paradoxical stimulation in children / overdose, atropine-like effects
Promethazine
Class: Antihistamine (phenothiazine, 1st gen)
Action: H1 receptor blocker / inverse agonist, ALSO Dopamine2 blocker. CNS anticholinergic effects.
Use: motion sickness, chemo-induced nausea/emesis
Route: oral, IV, topical, IM, rectal
S/E: profound sedation, paradoxical stimulation in children / overdose, atropine-like effects
Fexofenadine
AKA: Allegra
Class: antihistamine (piperidine, 2nd gen)
Action: Terfenadine is the prodrug. H1 receptor inverse agonist
Use: Allergies (rhinitis, urticaria, conjunctivitis)
Route: Oral
S/E: Unlike 1st gens, little anticholinergic or sedative effects in brain (little crosses BBB)
Loratidine
Aka: Claritin / Clarinex (Des- form)
Class: antihistamine (piperidine, 2nd gen)
Action: Prodrug of the active Desloratidine. H1 receptor inverse agonist
Use: Allergies (rhinitis, urticaria, conjunctivitis)
Route: Oral
S/E: Unlike 1st gens, little anticholinergic or sedative effects in brain (little crosses BBB)
Metab: into ACTIVE form by liver CYP3A4/2D6
Cetirizine
Aka: Zyrtec
Class: antihistamine (piperazine, 2nd gen)
Action: hydroxyzine is the prodrug. H1 receptor inverse agonist
Use: Allergies (rhinitis, urticaria, conjunctivitis)
Route: Oral
S/E: Unlike 1st gens, little anticholinergic effect in brain (little crosses BBB). Cetirizine causes most sedation of 2nd gen antihistamines.
Cimetidine
Class: Antihistamine (H2)
Action: H2 receptor blocker
Use: Relief of gastric upset / peptic ulcer disease / GERD via inhibition of gastric acid release by parietal cells. Historic use: Zollinger-Ellison syndrome (now treated with PPI). Least potent of H2 blockers.
Route: oral or IV
S/E: usually minor. Diarrhea, headache, drowsiness. Rare: confusion, delirium, slurred speech. Long term use in men can causes Gynecomastia, impotence via decrease of T binding and estradiol metab
Int: Inhibits CYP enyzymes, prolonging half lives of CYP-metabolized drugs
Ranitidine
Class: Antihistamine (H2)
Action: H2 receptor blocker
Use: Relief of gastric upset / peptic ulcer disease / GERD via inhibition of gastric acid release by parietal cells. Moderate potency among H2 blockers.
Route: Oral or IV
S/E: usually minor. Diarrhea, headache, drowsiness. Rare: confusion, delirium, slurred speech.
Int: Minor inhibition of CYP enzymes (10% of cimetidine), prolonging half lives of CYP-metabolized drugs
Famotidine
Class: Antihistamine (H2)
Action: H2 receptor blocker
Use: Relief of gastric upset / peptic ulcer disease / GERD via inhibition of gastric acid release by parietal cells. High potency among H2 blockers.
Route: Oral or IV
S/E: usually minor. Diarrhea, headache, drowsiness. Rare: confusion, delirium, slurred speech.
Aliskiren
Class: Direct renin inhibitor
Action: active-site, non-peptide inhibitor. Renin only - no inhibition of other aspartic proteases. Decreases plasma angiotensin II and aldosterone levels
Use: Hypertension, typically with another drug
Route: Oral, 1x/day (T1/2 ~ 24hrs)
S/E: Minor / similar to placebo: fatigue, headache, GI symptoms
Losartin
Class: AT1 receptor blocker
Action: competitive angiotensin receptor 1 antagonist. No effect on AT2 receptors.
Use: Essential hypertension, heart failure (lowers afterload), cardiac fibrosis/hypertrophy (lowers preload). Does not cause hyperkalemia.
Route: oral
S/E: dizziness, cough, angioedema, hypotension (esp. w/ diuretics)
Contra: Pregnancy
Captopril, Enalapril, Lisinopril
Class: ACE inhibitors
Action: inhibit angiotensin I converting enzyme, blocking ATII and bradykinin degradation
Use: Essential hypertension (lower BP w/o increasing HR), heart failure (reduces afterload), cardiac fibrosis/hypertrophy (reduces preload). Increases CO.
Route: Oral
S/E: cough, angioedema. Captopril: rash, proteinuria, neutropenia. Lowers aldosterone release to hyperkalemia may occur (can use to offset diuretic-caused hypokalemia)
Metab: Enalapril and Lisinopril are prodrugs of the active enaprilate and lisinoprilate, respectively.
Abciximab
Class: anticoagulant
Action: Fab fragment of mAb that binds platelet GP IIb/IIIa receptor to NON-COMPETITIVELY inhibit fibrinogen binding and cross-linking
Use: prevent thrombosis in coronary angioplasty & stent placement (w/ aspirin and heparin)
Route: IV
S/E: bleeding, thrombocytopenia, hypotension, bradycardia
Eptifibatide
Class: anticoagulant
Action: binds platelet GP IIb/IIIa receptor to COMPETITIVELY, REVERSIBLY inhibit fibrinogen binding and cross-linking ( novel KGD aa sequence, from rattlesnake venom)
Use: prevent coronary thrombosis in unstable angina & MI (w/ LMWH), or during coronary angioplasty / stent placement
Route: IV
S/E: bleeding, thrombocytopenia, hypotension, bradycardia
Contra: renal disease (renal clearance)
Nitroglycerin
Class: nitrates
Action: relaxation of arterial and venous (dominant) SM via donation of NO
Use: heart failure
Route: oral, IV, sublingual, topical/transdermal
S/E: hypotension
Nitroprusside
Class: nitrates
Action: relaxation of arterial and venous SM via donation of NO
Use: heart failure, hypertensive emergencies
Route: IV
S/E: hypotension
Hydralazine
Class: direct vasodilators
Action: dilates ARTERIAL SM by binding and activating K+ channels, causing K+ efflux that hyperpolarizes the cells. Increases cGMP.
Use: heart failure, hypertensive emergencies
Route: oral, IV
S/E: hypotension, headache, tachycardia
Minoxidil
Aka: Rogaine Class: direct vasodilators Action: K+/ATP channel opener, hyperpolarizes arterial SM; hair growth Use: severe HTN; alopecia Route: oral; topical S/E: fluid retention - use with diuretic
Diazoxide
Class: antihypertensive Action: causes K+ efflux to hyperpolarize SM cells; inhibits insulin secretion Use: HTN emergencies, hypoglycemia Route: oral, IV S/E:
Milrinone, Inamrinone, Cilostazol
Class: phosphodiesterase inhibitors Action: inhibit PDE3 to increase cAMP levels in cardiac myocytes, increasing contractility. Also vasodilator effects. Use: heart failure Route: IV, Cilostazol oral S/E:
Sildenafil, Tadalafil
Class: phosphodiesterase inhibitors Action: inhibit PDE5 to increase cGMP levels and cause vasodilation of SM Use: Erectile dysfunction Route: oral S/E:
Albuterol, Pirbuterol, Terbutaline, Salmeterol, Formoterol
Action: b2 adrenergic agonists - promote bronchodilation via cAMP/PKA increase
Use: acute asthma attacks, COPD
Route: inhalation
S/E: tachycardia
Methylxanthine, Theophylline, Aminophylline
Class: bronchodilators Action: adenosine receptor antagonists & PDE inhibitors to increase cAMP and cause bronchodilation Use: asthma and COPD Route: oral, IV S/E:
