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Cardiovascular drugs

Cardiovascular drugs. Prepared by: Dr Rasol M Hasan. Anti- HYPERTENSIVE Drugs. Diuretics. ACE Inhibitors. Vasodilators. Vasodilators. Examples: Clonidine Methyldopa Hexamethonium Guanithidine, reserpine, alpha blockers Amyl nitrate Hydralazine (oral) Minoxidil(parenteral)

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Cardiovascular drugs

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  1. Cardiovascular drugs • Prepared by: • Dr Rasol M Hasan

  2. Anti- HYPERTENSIVE Drugs

  3. Diuretics

  4. ACE Inhibitors Vasodilators Vasodilators Examples: Clonidine Methyldopa Hexamethonium Guanithidine, reserpine, alpha blockers Amyl nitrate Hydralazine (oral) Minoxidil(parenteral) Nesiritide Fenoldopam Na nitroprusside Diazoxide Calicium ch. Blockers ACEI, Angio.recep.blockers Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  5. ACE Inhibitors Sympatholytics Vasodilators • Centrally acting alpha2-agonists CLONIDINE,METHYLDOPA • decreases the sympathetic response from brainstem to peripheral vessels • Stimulate alpha2 receptors: increase vagus activity, decrease cardiac output and decreases serum epinephrine, norepinephrine & renin release • results into reduced peripheral vascular resistance • Side effects: • - drowsiness, dry mouth and nasal mucosa, dizziness, orthostatic hypotension impotence , sodium and fluid retention. Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  6. ACE Inhibitors ACE Inhibitors Vasodilators - Angiotensin Antagonists (Angiotensin-Converting Enzyme [ACE] Inhibitors) Action: - Inhibits ACE which in turn inhibits formation of angiotensin II (vasoconstrictor) and blocks the release of aldosterone Side effects: - Constant irritation cough; Nausea; Vomiting; Diarrhea; Fatigue; Hyperkalemia; Tachycardia Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  7. ACE Inhibitors ACE Inhibitors Vasodilators Indication: - Hypertension (control blood pressure); Prevention of cardiovascular disorders; Preventing kidney damage in people with hypertension or diabetes; Congestive heart failure (CHF); Left ventricular dysfunction Contraindication: - Pregnancy (Lowers placental blood flow); Hypotension Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  8. ACE Inhibitors Vasodilators Vasodilators - Direct Acting Arteriolar Vasodilators eg hydralazine old vasodilator mainly arteriolar dilator Diuretics • Action: • - act as blood vessel dilators • - relaxes vascular smooth muscles which decrease peripheral vascular resistance and therefore reduces blood pressure • Uses of Vasodilators: • Systemic and Pulmonary Hypertension • Heart Failure • Angina Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  9. ACE Inhibitors Vasodilators • Side Effects: • CNS: Headache; Peripheral neuropathy; Dizziness • CVS: Palpitation; Flushing; Reflex tachycardia; Angina; Ischemic arrhythmias • GIT: Nausea; Anorexia • Skin: Sweating; Lupus erythematosus like syndrome characterized by: Myalgia, Arthralgia, Skin rashes, Fever • Renal: Edema • hypotension • ECG changes • Drowsiness • Dry mouth • Fatigue Vasodilators Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  10. ACE Inhibitors Vasodilators Vasodilators • Contraindications: • ischemic heart disease • Lupus erythematosus • acute MI • DM • tachycardia • thyrotoxicosis • Precautions: • - caution should be used in uncompensated heart disease or peptic ulcer disease Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  11. ACE Inhibitors Vasodilators Vasodilators • Pharmacokinetics: • - onset, peak, and duration vary widely among products. Most products are metabolized in the liver and excreted in urine • Interactions: • - varies widely among products • Example of PHARMACOKINETICS OF ` HYDRALAZINE • Oral vasodilator but can be given I/V • Rapidly metabolized by the liver during first pass bioavailability is • low averaging 25% • variable among individuals. • Well absorbed. Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  12. ACE Inhibitors Ca Channel Blockers Vasodilators • 3 CHEMICAL CLASSES: • Phenylalkylamines – Verapamil (Calan, Isoptin, Verelan) • Benzothiazepines – Diltiazem (C ardizem, Dilacor, Tiazac) • Dihydropyridines – Amlodipine (Norvasc), Felodipine (Plendil), Nicardipine (Cardene), Nifedipine (Adalat, Procardia) • Mechanism of action: • Prevents calcium from entering the excitation-contraction process therefore, prevents muscle contraction and, instead, promotes relaxation of the smooth muscles that surrounds the coronary arteries and causes them to dilate. Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  13. ACE Inhibitors Ca Channel Blockers Vasodilators • Indications: • Angina • Hypertension • Supraventricular tachycardia • For short-term management of atrial fibrillation and flutter, migraine Headaches. • Contraindications: • Drug allergy • Acute MI • Second- or third-degree atrioventricular block • Hypotension Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  14. ACE Inhibitors Ca Channel Blockers Vasodilators • Adverse Effects: • Hypotension • Palpitations • Tachycardia or bradycardia • Nausea • Constipation • Dyspnea • Flushing • Peripheral edema • Common Drug Interactions • Beta-Blockers • Digoxin – possible increased digoxin level • H2 blockers – elevated levels of Calcium channel blockers • Grapefruit can reduce the metabolism of Ca channel blockers Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  15. ACE Inhibitors Sympatholytics Vasodilators • 5 groups of drugs: • Beta-adrenergic blockers • Centrally acting alpha2-agonists • Alpha-adrenergic blockers • Adrenergic neuron blockers (Peripherally acting sympatholytics) • Alpha1 and Beta1 adrenergic blockers • Sympatholytics:[anti-adrenergic] • - reduces the physiological effects caused by stimulation of the sympathetic nervous system Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  16. ACE Inhibitors Sympatholytics Vasodilators • Beta-adrenergic blockers • (Beta-blockers) • Step 1- antihypertensive drugs • Step 2 - in combination with diuretics • - also used as antianginals and antidysrhythmics • - reduces cardiac output by blocking the SympathNS response thus decreasing basal sympathetic tone • - continued use: reduces vascular resistance and lowers BP • - reduces HR, contractility and renin release • - can cross the placental barrier and enter breast milk Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  17. ACE Inhibitors Sympatholytics Vasodilators • Beta-adrenergic blockers • (Beta-blockers) • Types: • Nonselective • inhibits beta1 (heart) and beta2 (bronchial) receptors • decrease BP secondary to decrease and bronchoconstriction occurs • Cardioselective • act mainly on beta1; bronchoconstriction less likely to occur • Oral Beta-blockers • Onset of action: 30 mins. or less • Duration: 6 to 12 hours Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  18. ACE Inhibitors Sympatholytics Vasodilators • Beta-adrenergic blockers • (Beta-blockers) • IV Beta-blockers • Onset of action: immediate • Peak: 20 mins. • Duration: 4 to 10 hours • Side Effects: • - dizziness, weakness, wheezes, shortness of breath, • Adverse Reactions: • - Bradycardia, bronchospasms, markedly decrease BP Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  19. ACE Inhibitors Sympatholytics Vasodilators • Beta-adrenergic blockers • (Beta-blockers) • Precaution: • Should not be used by clients with 2nd- or 3rd-degree AV block or sinus bradycardia. • Noncardioselective beta-blocker should not be given in patients with COPD • Inform patients that herbs can interfere with beta-blockers • Example of drugs: • Propanolol • Metoprolol • Acebutolol • Atenolol • Bisoprolol Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  20. ACE Inhibitors Sympatholytics Vasodilators • Centrally acting alpha2-agonists • Adverse reactions: • - Peripheral edema • Example of drugs: • Clonidine • Methyldopa Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  21. ACE Inhibitors Sympatholytics Vasodilators • Alpha-adrenergic blockers • blocks alpha-adrenergic receptors which results in vasodilation and decrease BP • maintains renal blood flow rate • useful in clients with lipid abnormalities • safe for diabetic patients because it does not affect glucose metabolism • Side effects: • - dizziness, headache, vomiting, nausea, drowsiness, and nasal congestion, dry mouth Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  22. ACE Inhibitors Sympatholytics Vasodilators • Alpha-adrenergic blockers • Adverse reactions: • - orthostatic hypotension • Example of drugs: • Prazosin • Terazosin • Doxazosin • Phentolamine Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  23. ACE Inhibitors Sympatholytics Vasodilators • Adrenergic neuron blockers • blocks norepinephrine release, thus lowers BP • decreases cardiac output and peripheral vascular resistance • Side effects: • - dizziness, weakness, nausea, drowsiness • Adverse reactions: • - Orthostatic hypotension, peripheral edema • Example of drugs: • Reserpine • Guanethidine Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  24. ACE Inhibitors Sympatholytics • Alpha1 and Beta1 adrenergic blockers • blocking alpha1 receptor results in dilation of the arterioles and veins. • decreases BP and moderately decreased PR • Side effects: • -dizziness, weakness, nausea and vomiting, nervousness, dry mouth and fatigue • Adverse reactions: • - Orthostatic hypotension • Example of drugs: • Labetalol Vasodilators Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  25. Angiotensin Receptor Blockers ACE Inhibitors Vasodilators • Indications: • Hypertension, alone or when in combination with other anti-hypertensive drugs. • Nephropathy in type II DM • Heart failure in those intolerant to ACE inhibitors • Reduce risk of stroke • Contraindications and Special Considerations • Drug Allergy • Pregnancy and lactation • Elderly patients • Patients with renal dysfunction Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  26. Angiotensin Receptor Blockers ACE Inhibitors Vasodilators • Examples: • Losartan (Cozaar) • Eprosartan (Teveten) • Valsartan (Diovan) • Irbesartan (Avapo) • Candesartan (Atacand) • Olmesartan (Benicar) • Telmisartan (Micardis) Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

  27. Angiotensin Receptor Blockers ACE Inhibitors Vasodilators • Serious Side Effects: • Altered Liver Function • Kidney Impairment • Hyperkalemia • Orthostatic hypotension • Toxicity and Management • Overdose may manifest: • Hypotension • Tachycardia, bradycardia occurs less often • treatment is symptomatic and supportive. It includes the administration of IVFs to expand the blood volume • Drug to Drug Interaction • - can interact with cimetidine, Phenobarbital, and rifampin. Diuretics Ca Channel Blockers Sympatholytics Angiotensin Receptor Blockers

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