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Antianginal Agents and Hypotensive Agents

Antianginal Agents and Hypotensive Agents. 馬偕紀念醫院藥劑室 林育成藥師. Amlodipine besylate (Norvasc). Form: Tab: 5mg Dosage: Hypertension: Initial 2.5-5mg qd, MD 5-10mg qd, Max. 10mg/day Angina: 5-10mg qd, MD 10mg qd. Amlodipine besylate (Norvasc). Precautions aortic stenosis CHF

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Antianginal Agents and Hypotensive Agents

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  1. Antianginal Agents and Hypotensive Agents 馬偕紀念醫院藥劑室 林育成藥師

  2. Amlodipine besylate (Norvasc) • Form: Tab:5mg • Dosage: • Hypertension: Initial 2.5-5mg qd, MD 5-10mg qd, Max. 10mg/day • Angina: 5-10mg qd, MD 10mg qd

  3. Amlodipine besylate (Norvasc) • Precautions • aortic stenosis • CHF • exacerbation of angina during initiation of therapy, after dose increases, or withdrawal of beta blocker therapy • hypotension (initially or after dose increases) • liver impairment • persistent progressive dermatologic reactions

  4. Amlodipine besylate (Norvasc) • Dose adjustments: • renal impairment: NOT recommended in patients with severe renal impairment (CrCl below 30 mL/min/1.73m(2), serum creatinine >/=3 mg/dL) • liver disease: starting dose, 2.5 mg/10 mg • geriatrics: starting dose, 2.5 mg/10 mg

  5. Isosorbide dinitrate (Isordil, Sorbitrate tab, Isoket inj) • Dose: • Oral, initial 5-20 mg q6h, MD 10-40mg q6h ac, • IV infusion, 2-7mg/hr, up to 10mg/hr • Note: • Dosing interval may be bid or tid and last dose no later than 7 PM to minimize nitrate tolerance

  6. Isosorbide mononitrate (Imdur CR) • Form: Tab: 60mg (extended release) • Dose: • Initial 30mg qd for 2-4 days then 60-120 mg qd • Note: • should be taken in the morning • should be swallowed whole not chewed, but it can be administered half of a tablet at a time

  7. Isosorbide monotrate (ISMO-20, Isormol) • Form: Tab:20mg • Dose: • Initial 10mg bid for 2 days then 20-30mg bid • Note: • Asymmetrical dosing regimen of 7AM and 3PM or 9AM and 5PM to allow for a nitrate-free dosing interval to minimize nitrate tolerance • Do not crushor chew but can cut half

  8. Isosorbide monotrate (ISMO-20, Isormol) • Administration: • administer 0.5 hr before or 1 hr after meals • do not crushor chew extended release dosage forms • dose to provide a 10-12 hr drug-free interval

  9. Drug-drug interaction:Organic nitrate and Sildenafil (Viagra) • SILDENAFIL inhibits phosphodiesterase type 5 (PDE5) which is responsible for the metabolic degradation of cyclic guanosine monophosphate (cGMP). • Organic nitrates exert their action by activation of guanylate cyclase, which increases cGMP. Because of the potential for excessive hypotensive effects as a result of increased cGMP, the concomitant use of sildenafil and organic nitrates is contraindicated

  10. Diltiazem HCl (Herbesser, Cartil) • Form: Tab:30mg • Dose: • angina: start with 30mg qid ac, increase dosage gradually until optimal response, average 180-360 mg/ day divide into 3-4 doses

  11. Diltiazem HCl (Diltelan SR) • Form: Cap: 90mg (controlled release) • Dose: Initial 90mg bid for 2 wks, may increase gradually to 360mg/day div. into 2 dose • Hypertension: 240-360mg/day • Angina: 240mg/day • Note: Swallow whole; do not open, chew or crush the capsules

  12. Nicorandil (Sigmart) • Form: Tab:5mg • Dose: 5-20 mg bid, Max. 30mg bid

  13. Mechanism of Nicorandil (Sigmart) • Nicorandil : potassium channel openers or activators, which produce vascular smooth muscle relaxation by increasing potassium flux through adenosine triphosphate (ATP)-sensitive sarcolemmal potassium channels • This leads to hyperpolarization of the cell membrane, and subsequent decreases in levels ofcytoplasmic calcium (calcium channel blockade) and dilation of arterial resistance vessels

  14. Nifedipine (Adalat OROS) • Form: Tab:30 mg (extended release) • Dose: initial 30mg once daily, may be increased to 120mg once daily if needed • Note: Swallow whole; do not crush or chew

  15. Nitroglycerin (Glyceryl trinitrate, NTG, Nitrostat tab, Tridil inj) • Form: Tab:0.6mg, inj:50 mg/10ml amp • Dose: • Sublingal, 0.2-0.6mg every 5 min for max. of 3 doses in 15 min • IV infusion, initial 5mcg/min then increased by 5mcg/min at 3-5 min intervals until a response is noted or the rate is 20mcg/min

  16. Nitroglycerin lingual aerosol • Form: Aerosol: 0.4mg/spray, 200 sprays/set • Dose: • Acute relief of angina pectoris: 1-2 srpays (0.4-0.8mg) every 3-5min if necessary , Max. of 3 doses in 15 min • Prophylaxis angina pectoris: 1-2 sprays, 5-10min before situations

  17. Antiadrenergic agents-centrally acting • Clonindine HCl (Catapres) • Methyldopa (Aldomet)

  18. Captopril (Capoten) • Form: Tab:25mg • Dose: Hypertension : Initial mg bid-tid ac, the dosage being increased to 50mg bid-tid if necessary after 1 or 2 wksCHF: Initial 25mg tid ac, the dosage being increased up to 50mg tid; if further increased in dosage, it is made after an interval of 2 wks, MD 50-100mg bid-tid, Max. 450mg/day

  19. Cotraindication of Capoten • A. Angioedema induced by other angiotensin converting enzyme (ACE) inhibitors during prior exposure • B. Anuric renal failure during prior exposure to ACE inhibitors • C. Hypersensitivity to this or any other ACE inhibitor • D. Hereditary or idiopathic angioedema • E. Pregnancy (second and third trimesters particularly

  20. Enalapril maleate (Renitec) • Form: Tab:20mg • Dose: • Hypertension: Initial 2.5~5mg/day, MD 10-40mg/day divide into 1-2 doses • CHF: initial 2.5mg qd-bid, MD 5-20mg/day divide into 1-2 doses, Max. 40mg/day

  21. Enalapril maleate (Renitec) • MECHANISM : • Enalapril is a weak angiotensin-converting enzyme inhibitor; however, hepatic activation of enalapril to enalaprilat being 10 to 20 times as potent as captopril

  22. Enalapril maleate (Renitec) • Precautions: • ACE-inhibitor induced angioedema • apheresis (low-density lipoprotein) with dextran sulfate • CHF, severe (oliguria and/or progressive azotemia may occur)

  23. Fosinopril Sodium (Monopril) • Form: Tab: 10mg • Hypertension: initial 10mg qd, MD 20~40mg/day qd or bid up to 80mg/day • CHF: initial 10mg qd, MD 20~40mg/day

  24. Fosinopril Sodium (Monopril) • Mechanism : • Fosinopril is a prodrug and must undergo reesterification to its biologically active diacid metabolite, fosinoprilat. Fosinopril has a phosphinic acid binding site and lacks the sulfhydryl group characteristic of captopril

  25. Fosinopril Sodium (Monopril) • Precautions • ACE-inhibitor induced angioedema • apheresis (low-density lipoprotein) with dextran sulfate • CHF, severe (oliguria and/or progressive azotemia may occur) • collagen vascular disease, especially in presence of renal impairment (risk of neutropenia, agranulocytosis)

  26. Perindopril tert-butylamine (Acertil) • Form: Tab: 4mg • Dose: • Hypertenision: Initial 2mg qd, MD 4mg/day, Max. 8mg/day, Max. 8mg/day acCHF: Initial 2mg qd, MD 4mg/day ac

  27. Perindopril tert-butylamine (Acertil) • Mechanism: • Perindopril is an ester prodrug, requiring in vivo hydrolysis to its active diacid metabolite, perindoprilat • Perindoprilat is a long-acting, non-thiol angiotensin converting enzyme (ACE) inhibitor

  28. Rampril (Tritace) • Form: Cap: 2.5mg • Dose:Hypertension: initial 1.25-2.5mg qd, MD 2.5-5mg as a single dosage or in 2 divided doses. Max. 10mg/dayCHF post-MI: initial 2.5mg bid, if hypotension occurs,dosage should be reduced to 1.25mg bid. MD 5mg bid

  29. Rampril (Tritace) • Mechanism : • Ramipril is a prodrug that undergoes enzymatic saponification by esterases in the liver to its biologically active metabolite, ramiprilat. Ramipril is a long active angiotensin converting enzyme inhibitor with hypotensive effects lasting a full 24 hours with single daily dosing.

  30. Clonidine (Catapres) • Form: Tab:75mcg • Dose: • Initial 0.05-0.1mg bid, may be increase by 0.1-0.2 mg/day, • MD 0.2-1.2mg/day divide into 2-4 doses, • Max. 2.4mg/day

  31. Methyldopa (Aldomet) • Form: Tab:250mg • Dose: • Initial 250mg bid-tid for 2 days then being adjusted until the desired response is obtained, • MD 500mg-2g/day divide into 2-4 doses

  32. Indication: Benign prostatic hyperplasia Form: Tab:10mg (prolonged release) Alfuzosin HCl (Xatral XL)

  33. Alfuzosin HCl (Xatral XL) • A. Alfuzosin: a selective -1 adrenoceptor antagonist. • B. dosing information: • benign prostatic hyperplasia :7.5 to 10 mg daily; • hypertension, 5 to 10 mg twice daily. • Dose reductions are suggested in patients with liver disease, and in the elderly.

  34. Alfuzosin HCl (Xatral XL) • CONTRAINDICATIONS • A. Concomitant use of potent CYP3A4 inhibitors (eg, ketoconazole, itraconazole, ritonavir) • B. Hepatic insufficiency (moderate to severe) • C. Hypersensitivity to alfuzosin or other quinazolines

  35. Alfuzosin HCl (Xatral XL) • Precautions: • A. Carcinoma of the prostate and benign prostatichyperplasia may cause the same symptoms and frequently coexist. Prostate cancer should be ruled out prior to treatment. • B. Concomitant use of other alpha-blockers • C. Congenital or acquired QT prolongation syndromes • D. Coronary artery disease

  36. Alfuzosin HCl (Xatral XL) • Precautions: • E. General anesthesia • F. Hepatic disease (mild) • G. Dizziness, lightheadedness • H. Orthostatic hypotension • I. Renal dysfunction (severe) • J. Syncope (First-dose effect)

  37. Doxazosin (Doxaben) • Indications • Benign prostatic hyperplasia • Hypertension • Form: Tab: 1mg • Dose: Initial 1mg qd, MD 2mg qd, if necessary subsequent dosage adjustments can be made by doubling the dose every 2 wks, Max. 16mg/day

  38. Doxazosin (Doxaben) • Precautions • carcinoma of the prostate • concomitant use of other antihypertensives (additive hypotensive effects) • first dose syncope/ sudden loss of consciousness • liver disease • orthostatic hypotension, syncope • recent cerebrovascular accident

  39. Doxazosin (Doxaben) • Administration • first dose phenomenon characterized by excessive postural hypotension, palpitations, syncope, and tachycardia can be minimized by limiting the initial dose to 1 mg, administering the first dose at bedtime, and increasing the dosage slowly

  40. Terazosin • Form: Tab: 2mg • Dose: • Hypertension: Initial 1mg hs, may be increased gradually to 5mg/day, Max. 20mg/day • Benign prostatic hyperplasia: Initial 1mg hs, may be increased in a stepwise manner to 2,5 and 10mg/day as necessary, Max. 20mg/day

  41. Acebutolol Hydrochloride (Sectral) • Angina: 600-1600 mg ORALLY daily (divided 2-3 times/day) • Arrhythmias: initial, 400 mg ORALLY daily (divided twice a day); maintenance, 600-1200 mg ORALLY daily (divided 2-3 times/day) • Hypertension: initial, 400 mg ORALLY daily; maintenance, 400-800 mg ORALLY daily (may be divided twice a day); MAX 1200 mg/day (divided twice a day)

  42. Acebutolol Hydrochloride (Sectral) • Dose Adjustments • geriatric: may require lower maintenance doses (specific guidelines unavailable); doses above 800 mg/day should be avoided • renal impairment: CrCl less than 50 mL/min - reduce usual adult dose by 50% • renal impairment: CrCl less than 25 mL/min - reduce usual adult dose by 75%

  43. Acebutolol Hydrochloride (Sectral) • FDA labeled indications • Arrhythmia • Hypertension • Non-FDA labeled indications • Angina pectoris

  44. Acebutolol Hydrochloride (Sectral) • Contraindications • cardiogenic shock • hypersensitivity to acebutolol • overt cardiac failure • second and third degree AV block • severe sinus bradycardia

  45. Atenolol (Tenormin) • Form: Tab: 50mg • Hypertension (HTN): 50-100 mg ORALLY once daily

  46. Atenolol (Tenormin) • Dose Adjustments: • hemodialysis: 25-50 mg after each dialysis session • renal impairment: CrCl 35 mL/min or greater - normal dosing • renal impairment: CrCl 15-35 mL/min - MAX dose 50 mg once daily • renal impairment: CrCl less than 15 mL/min - MAX dose 25 mg once daily

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