Cardiovascular Drugs Flashcards
Thiazides, which are used in the treatment of hypertension, may require supplemental administration of: Sodium Chloride Calcium Potassium
Potassium
Which of the following is a beta-adrenergic receptor agent used for the treatment of hypertension? Prazosin (Minipress) Clonidine (Catapres) Atenolol (Tenormin) Hydralazine (Apresoline) Verapamil (Calan)
Atenolol (Tenormin)
What is the goal of cardiovascular pharmacology?
Decrease the workload on the heart–decrease oxygen demand from cardiac muscle
- Blocked coronary arteries: decrease the available oxygen to cardiac tissues
- Hypertension increases the afterload and preload of the heart
Describe how hypertension leads to congestive heart failure
Hyperlipidemia OR hypertension –> angina –> myocardial infarction –> arrhythmias OR congestive heart failure
Lisinopril (Zestril)
Class: Angiotensin Converting Enzyme (ACE) Inhibitors; Volume Regulator
Mechanism of action:
Indication:
- Hypertension
- Heart failure
- MI
Pharmacological effects:
- Decrease concentrations of ATII–> vasodilation
- Increase bradykinin, a vasodilator
- Decrease aldosterone
How this drug might effect dental treatment of patient
oAdverse effects you have to consider:
-Altered or reduced taste sensation
-Hypotension
-Bradykinin: cough in 20% of patients; angioedema of the face and mouth (more common in African American patients)
oContraindicated drugs:
-NSAIDs and ASA inhibit anti-HTN effects
oContraindications:
oWhich analgesic can the patient take:
Valsartan (Diovan)
Class: Angiotensin Receptor Antagonist; Volume Regulator
Mechanism of action:
Indication:
- Heart failure
- Hypertension
- MI
- Prevention of stroke
Pharmacological effects:
- Inhibit vasoconstriction
- Inhibit aldosterone secretion
- Inhibit sodium retention
Comparison to ACE inhibitors:
- Less adverse reactions (cough and angioedema)
- Less effective vasodilation
How this drug might effect dental treatment of patient
oAdverse effects you have to consider:
-GI upset
oContraindicated drugs:
- Increase in anti-HTN effect with fluconazole and ketoconazole (we don’t want BP too low or pt could pass out)
- Increase renal toxicity with NSAIDs
oContraindications:
oWhich analgesic can the patient take:
Angiotensin Receptor Antagonists
Valsartan (Diovan) Losartan (Cozaar) Irbesartan (Avapro) Olmesartan (Benicar) Candesartan (Atacand) Telmisartan (Micardis) Nisoldipine (Sular)
ACE Inhibitors
Lisinopril Captopril Enalapril Ramipril Benazepril Fosinopril Perindopril Quinapril Trandolapril Moexipril
Aldosterone
The cortical collecting duct cells
Mechanism:
-Binds to intracellular mineralocorticoid receptor
-Activation of the receptor
-Increases transcription of mRNAs that encode proteins involved in Na+ handling
-Control of sodium channel expression*
Spironolactone
Class: Aldosterone Antagonist; Potassium Sparing Diuretic; Volume Regulator
Mechanism of action:
-Potassium sparing diuretic
The cortical collecting duct cells
Mechanism
-Binds to intracellular mineralocorticoid receptor
-Activation of the receptor
-Control of sodium channel expression
Spironolactone is a aldosterone antagonist
-Binds to and prevents nuclear translocation of the mineralocorticoid receptor
Indication:
- Hypertension
- Edema states: Heart failure and Hepatic cirrhosis
- Congestive Heart Failure
- Hypokalemia
- Male to female gender transformation
Pharmacological effects:
How this drug might effect dental treatment of patient oAdverse effects you have to consider: Steroid structure -Gynecomastia in men -Menstrual irregularities in women -Hyperkalemia
oContraindicated drugs:
-Decreased anti-HTN effect with NSAIDs
oContraindications:
oWhich analgesic can the patient take:
Nephron anatomy and sites of action of diuretics
- Kidney reabsorbs 99 % of solutes and water that is filtered
- Reabsorption of water is passive following osmotic gradients
- Osmotic gradients are controlled by Na+ reabsorption by the nephrons
- All diuretics act by inhibiting Na+ reabsorption
- Less water reabsorbed: decrease CO
Hydrochlorothiazide (HCTZ)
Class: Thiazide Diuretic; Volume Regulator
Mechanism of action:
- Binds to the Na+Cl- cotransporter in the distal tubule and inhibits turnover
- Reduction in extracellular fluid volume
- K+ is exchanged for Na+ leading to more K+ loss
Indication:
- HTN
- Edema: CHF, Hepatic cirrhosis, Renal dysfunction, Corticosteroid therapy
Pharmacological effects:
- Reduction in NaCl reabsorption
- Increase the reabsorption of Ca+
How this drug might effect dental treatment of patient
oAdverse effects you have to consider:
-Hypokalemia
-Hyponatremia
-Gout
-Dry mouth, lichenoid rxns, orthostatic hypotension
oContraindicated drugs:
- NSAIDS decreases anti-HTN effects
- Increase orthostatic hypotension with opiates
oContraindications:
oWhich analgesic can the patient take:
Furosemide (Lasix)
Class: Loop Diuretic; Volume Regulator
Mechanism of action:
- Inhibition of NaCl reabsorption in the Loop of Henle by binding to the Cl- site of the cotransporter.
- K+ secretion occurs in response to Na+ secretion
- Reduce the extracellular fluid volume and BP with a greater magnitude than with thiazides
Indication:
- HTN
- Acute pulmonary edema
- Edema: CHF, Hepatic cirrhosis, Renal dysfunction
- Hyperkalemia
- Hypercalcemia
Pharmacological effects:
How this drug might effect dental treatment of patient
oAdverse effects you have to consider:
-Same as those for thiazides with respect to hypokalemia and hyponatremia
-Same dental adverse effects
-Ototoxicity (hearing loss in the elderly)
oContraindicated drugs:
-NSAIDs decrease anti-HTN effects
oContraindications:
oWhich analgesic can the patient take:
Summary of Diuretics
Potency
-Loop, Thiazide, K sparing
Dosing
-Usually BID with 8 am and 4 pm administration times
Dental adverse effect
- Dry mouth
- Lichenoid reactions
- Orthostatic hypotension
Organic Nitrate (Nitroglycerin)
Class: Direct-Acting Vasodilators; Vascular Tone
Mechanism of action:
Endothelial regulation of nitric oxide-mediated vascular smooth muscle relaxation
-Nitric Oxide Synthase catalyzes
-Arginine to nitric oxide and citrilline
-NO crosses freely through the cell membrane to convert guanylyl cyclase to the active form
-GMP goes to cGMP
Smooth muscle relaxes
Indication: Short-Acting For acute episodes -Sublingual Tablet 0.4 mg -Oral Spray Long-Acting For Prophylaxis or ischemic heart disease -Tablets -Ointment -Patch At onset of chest pain -1 tablet (spray) under tongue -Can be repeated every 5 minutes for a total of 3 tablets (spray) in 15 minutes
Pharmacological effects:
Sites of action of organic nitrates
-Veins: decrease preload (main action); decreased myocardial O2 demand
-Ateries: decrease afterload; decrease myocardial O2 demand
-Heart: increased myocardial O2 supply bt dilating large epicardial arteries
Biotransformation of organic nitrates and sodium nitroprusside
-Development of tolerance: diminished response of peripheral tissues to nitrates after long term use
How this drug might effect dental treatment of patient
oAdverse effects you have to consider:
-Headache
-Orthostatic hypotension, stroke, dizziness, reflex tachycardia
oContraindicated drugs:
-Opiates ↑ the effects of nitric oxide
oContraindications:
oWhich analgesic can the patient take:
Amlodipine (Norvasc)
Class: Calcium Channel Blockers; Vascular Tone
Mechanism of action:
- Block voltage dependent L-type Ca2+ channels
- Different affinities for different conformation states of the channel
- Differential tissue selectivity
Indication:
- Angina
- Coronary spasm
- HTN
Pharmacological effects:
-Used with beta blockers in HTN
How this drug might effect dental treatment of patient
oAdverse effects you have to consider:
-Gingival hyperplasia
oContraindicated drugs:
-Azole antifungals decrease metabolism
oContraindications:
oWhich analgesic can the patient take:
Diltiazem (Cardizem)
Verapamil (Calan)
Class: Calcium Channel Blockers; Vascular Tone
Mechanism of action:
- Block voltage dependent L-type Ca2+ channels
- Different affinities for different conformation states of the channel
- Differential tissue selectivity
Indication:
- HTN
- Atrial fibrillation
- Supraventricular tachycardia
Pharmacological effects:
-Used with nitroglycerin in HTN
How this drug might effect dental treatment of patient
oAdverse effects you have to consider:
-Gingival hyperplasia
-Verapamil-induced GH has appeared 11 months or more after subjects took daily doses of 240-360 mg.
-Severity : not dose dependent
-Gingivectomy is only successful if CCB therapy is discontinued
-GH regresses markedly 1 week after CCB discontinuance with all symptoms resolving in 2 months.
oContraindicated drugs:
- Azole antifungals decrease metabolism
- Beta blockers are contraindicated
oContraindications:
oWhich analgesic can the patient take:
Site of action of calcium channel blockers
- Act on myocardium and vascular smooth muscle
- Predominantly arteriolar dilators
Doxazosin (Cardura)
Class: α1 Sympathetic Antagonist; Sympathetic Nervous System
Mechanism of action:
- α1 receptor blockade
- Smooth muscle relaxation
- Decrease in TPR**
Indication:
Pharmacological effects:
How this drug might effect dental treatment of patient oAdverse effects you have to consider: -Dry mouth -Dizziness -Orthostatic hypotension
oContraindicated drugs:
oContraindications:
oWhich analgesic can the patient take:
Clonidine (Catapres)
Class: α2 Inverse Agonist (Sympathetic Agonist); Sympathetic Nervous System
Mechanism of action:
- Inverse Agonist—
- Binds to α2 medullary receptors in the brain
- Inhibits sympathetic outflow to the body
- Inhibition of α receptors in blood vessels
Indication:
Pharmacological effects:
How this drug might effect dental treatment of patient oAdverse effects you have to consider: -Dry mouth -Dizziness -Orthostatic hypotension -Abnormal taste
oContraindicated drugs:
oContraindications:
oWhich analgesic can the patient take:
Metoprolol (Toprol XL)
Class: β blockers; Sympathetic Nervous System
Mechanism of action:
-Competitive inhibitor of epinephrine and norepi at β1
Indication:
- Hypertension
- Ischemic heart disease
- Heart failure
- β1 selective-usually for cardiac problems with other cardiac drugs
Pharmacological effects:
Reduce blood pressure in hypertensive patients
-CO decreases**
-HR decreases
-Peripheral resistance decreases
-Reduction in plasma renin activity
-Decrease CNS sympathetic outflow
-Alteration in baroreceptor responsiveness
↓ the force and rate of myocardial contraction
↓ O2 consumption of the heart
↓ of blood pressure in hypertensive patients
How this drug might effect dental treatment of patient oAdverse effects you have to consider: -Altered taste** -Lichenoid Reactions -Orthostatic Hypotension -Dry Mouth
oContraindicated drugs: Antibiotics: -Ampicillin causes ↓ levels of atenolol -Allergic rxns to PCNs more severe because ↑ mediator release from mast cells Epinephrine -↑ BP with bradycardia because of unopposed α stimulation -No epi containing retraction cord NSAIDs -↓ antihypertensive effect -Limit duration to 4 days
oContraindications:
oWhich analgesic can the patient take:
Carvedilol (Coreg)
Class: α1/β blockers; Sympathetic Nervous System
Mechanism of action:
- Antagonist at β1 and α1 receptors
- Isomers bind to α or β receptors
Effects:
- Decrease heart rate and contractility
- Decrease blood pressure through alpha blockade
Indication:
-CHF
Pharmacological effects:
How this drug might effect dental treatment of patient
oAdverse effects you have to consider:
oContraindicated drugs:
oContraindications:
oWhich analgesic can the patient take:
Epinephrine use in cardiac patients
American Heart Association and the ADA:
- “Vasoconstrictors should be used only when the procedure will be shortened or the analgesia rendered more profound. The minimum possible amount of vasoconstrictor should be used.”
- Upper Limit: 0.04 mg total per procedure
Pharmacology of cardiac contractility
- Calcium enters the cell.
- Increase in free calcium
- Heart muscle contracts
- Heart muscle relaxes calcium leaves the cell via the sodium gradient
- Sodium pump keeps the heart muscle hyperpolarized
