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Pharmacology Drugs #

Respiratory, Vasoconstrictors, Vasodilators, HTN, Angina, Heart Failure

What drugs are in the antihistamine class Diphenydramine and Loratidine
Diphenhydramine Mechanism of Action Block H1 and Muscarinic Receptors
Diphenhydramine Kinetics/Dynamics -Crosses BBB easily - increases vasoDILation -increases capillary permiability -decreases nerve sensitivity
Diphenhydramine Indication for/Uses -used for mild to moderate allergies; motion sickness; insomnia; colds
Diphenhydramine Adverse Effects -Confusion/Sedation (due to BBB crossing) -Anticholinergic effects
Diphenhydramine Drug Interactions -alcohol
Loartidine Mechanism of Action Specifically blocks H1 Receptors
Loartidine Kinetics/Dynamics Large and polar (so doesn't cross BBB easily)
Loartidine Indication for/Uses mild to moderate allergies
Intranasal Glucocorticoid Kinetics/Dynamics Need a few weeks to reach peak effect
Intranasal Glucocorticoid Indication for/Uses suppress all of the symptoms of allergic rhinitis
Decongestants Mechanism of Action alpha 1 agonist
Decongestants Kinetics/Dynamics Topical= strong, localized effect Oral= systemic effect
Decongestants Indication for/Uses reduce nasal congestion from allergic rhinitis, sinusitus and colds
Decongestants Adverse Effects topical= rhinitis medicamentosa oral=CNS stimulation (insomnia) and ischemic stroke
Decongestants Quirky Don't give with HTN
Albuterol Mechanism of Action Activate Beta2 in the lung to cause bronchodilation
Albuterol Kinetics/Dynamics Rapid onset of action
Albuterol Indication for/Uses Alleviate acute bronchospasm in an asthma attack. Rescue; PRN
Albuterol Adverse Effects -Tachycardia -Tremors
Salmeterol Mechanism of Action Activate Beta2 in the lung to cause bronchodilation
Salmeterol Kinetics/Dynamics Longer onset of action
Salmeterol Indication for/Uses Stable COPD (NOT asthma)
Salmeterol Adverse Effects Asthma-related death if given by itself
Salmeterol Quirky Must be given in combination with a glucocorticoid
Methylxanthines Mechanism of Action Inhibit PDE
Methylxanthines Kinetics/Dynamics -rapidly absorbed -metabolized by P450
Methylxanthines Indication for/Uses Bronchodilation
Methylxanthines Adverse Effects -Dysrhythmias -Seizures -Death
Methylxanthines Quirky smoking reduces it's half life by 50%
Ipratropium bromide Mechanism of Action Block muscarinic receptors on the lungs
Ipratropium bromide Kinetics/Dynamics Highly polar (so usually stuck in the lungs at site of action)
Ipratropium bromide Indication for/Uses Bronchodilation in COPD
Ipratropium bromide Adverse Effects -Dry mouth d/t inhalation -Throat irritation d/t inhalation
Glucocorticoids Mechanism of Action -Dec inflammatory mediators -Dec edema -Dec mucous production
Glucocorticoids Kinetics/Dynamics Inhaled= low bioavailability systemically, has a high 1st pass effect. Oral= higher bioavailability systemically
Glucocorticoids Indication for/Uses 1st line of defense for asthma control inhaled= daily, for chronic control oral= given RPN for acute control of severe episode
Glucocorticoids Adverse Effects inhaled= oropharyngeal candidiasis oral= short term: hyperglycemia, hyperkalemia, fluid retention, HTN, mood changes oral=long term: adrenal suppression
Glucocorticoids Quirky Long-term use of oral glucocorticoids can cause adrenal suppression, and in kids this can delay growth
Cromolyn Sodium Mechanism of Action stabilized cytoplasmic membrane and prevents the release of inflammatory mediators
Cromolyn Sodium Indication for/Uses prophylaxis treatment! given before exercise for exercise-induced asthma attacks
Cromolyn Sodium Quirky Also inhibits eosinophils, macrophages and other inflammatory cells
Leukotrienes Mechanism of Action Suppress effects of leukotrienes
Leukotrienes Kinetics/Dynamics Metabolized by P450
Leukotrienes Indication for/Uses Used to decrease bronchoconstriction (promote bronchodilation) and decrease the inflammatory response like edema and mucus secretion in the airways
Leukotrienes Adverse Effects possible liver injury
Leukotrienes Quirky Also inhibits eosinophils
Epinephrine Mechanism of Action Acts on Alpha 1, Alpha 2, Beta 1 and Beta 2 receptors to cause vasoconstriction
Epinephrine Indication for/Uses It is used to: -elevate BP -control superficial bleeding -delay absorption of topical anesthetic -treatment for anaphylaxis -reduce nasal congestion
Epinephrine Kinetics/Dynamics -very short half life; it is metabolized quickly by MAO -reuptake proteins pulls epi back into the cell
Epinephrine Adverse Effects -tissue necrosis if it infiltrates the IV site -dysrythmias -HTN crisis -angina -hypergylcemia
Epinephrine Drug Interactions (ALL BAD) -MAO inhibitors -alpha blockers -beta blockers
Epinephrine Quirky No bioavailability if given PO
Dopamine Mechanism of Action Action on Alpha 1 and Beta 1 receptors to cause vasoconstriction
Dopamine Quirky Low dose= dopamine receptor selectivity only Moderate dose= dopamine and beta 1 receptor selective High dose= dopamine, beta 1 and alpha 1 receptor selective
Dopamine Kinetics/Dynamics -very short half life, rapidly metabolized by MAO
Dopamine Indication for/Uses it is used to: -increase blood flow to the kidney -treat Heart Failure -Increase hear rate -increase contractility -increase cardiac shock -treat shock
Dopamine Adverse Effects -tissue necrosis if IV infiltrates -tachycardia -dysrythmias -angina
Prazosin Mechanism of Action Alpha 1 receptor blockade
Prazosin Indication for/Uses Hypertension
Prazosin Adverse Effects -orthostatic hypotension -reflex tachycardia -impotence -nasal congestion
Prazosin Quirky Small initial dose and then incrementally increase
Reserpine Mechanism of Action Deplete stores of norepinephrine in the pre-synaptic neuron and suppresses synthesis of norepi
Reserpine Kinetics/Dynamics highly non-polar (crosses BBB easily)
Reserpine Indication for/Uses -hypertension -decrease beta and alpha activation
Reserpine Adverse Effects -sedation -depression -bradycardia -orthostasis -Parkinson-like symptoms
Clonodine Mechanism of Action turns off alpha 1 and beta 1 receptors by stopping the SNS outflow via activating alpha 2 receptors in the brainstem
Clonodine Indication for/Uses -hypertension -substance withdrawal -menopausal flushing -migraines
Clonodine Kinetics/Dynamics Lipid soluble
Clonodine Adverse Effects -sedation -dry mouth -rebound hypertension
Clonodine Quirky Not given in pregnancy
Captopril Mechanism of Action -prevents conversion of angiotensin 1 to angiotensin 2 (inhibits the ACE enzyme) -prevents breakdown of bradykinin -blocks aldosterone release
Captopril Kinetics/Dynamics short half life
Captopril Adverse Effects -hypotension -cough -angioedema -hyperkalemia -renal failure -fetal injury
Captopril Indication for/Uses -hypertension -congestive heart failure -MI -diabetes mellitus *it lowers BP and increases urine output
Captopril Drug Interactions Good: diuretics and other antihypertensives *need close monitoring if given with another drug that effects potassium
Dopamine Drug Interactions Good: Diuretics Bad: MAO inhibitors; alpha blockers; beta blockers
Losartan Mechanism of Action -block angiotensin 2 receptor site (ARB) -no interactions with bradykinin
Losartan Kinetics/Dynamics Longer half life (Q daily)
Losartan Indication for/Uses hypertension (lowers BP and increases urine output)
Losartan Adverse Effects -small risk of angioedema -fetal injury -much less effect on potassium
Nifedipine Mechanism of Action block calcium channels in arterioles and coronary arteries (vasodilates the vasulature)
Nifedipine Kinetics/Dynamics -rapid-acting forumla -sustained-release formula
Nifedipine Indication for/Uses -hypertension -vasospastic angina (dec BP)
Nifedipine Adverse Effects -flushing -dizziness -headache
Nifedipine Drug Interactions GOOD: given with beta blockers to manage tachycardia
Nifedipine Quirky drop in BP may be too quick; if so, will stimulate baroreceptors to increase heart rate (reflex tachycardia)
Hydralazine Mechanism of Action inhibits/blocks the release of calcium from the sarcoplasmic reticulum
Hydralazine Kinetics/Dynamics acetylase converts hyralazine into its metabolites
Hydralazine Indication for/Uses -hypertension -hypertension crisis
Hydralazine Adverse Effects -refelx tachycardia -water and sodium retention
Hydralazine Drug Interactions GOOD: diuretics and beta blockers to control adverse effects
Hydralazine Quirky may have slow acetylators! they require smaller doses
Nitroprusside Mechanism of Action the nitric oxide in it induces guanylate cyclase to convert gtp to cgmp. cgmp causes dephosphorylation of myosin and results in vaso relaxation
Nitroprusside Kinetics/Dynamics -fast acting -short half-life....give via continuous IV
Nitroprusside Indication for/Uses -hypertension crisis
Nitroprusside Adverse Effects -hypotension -cyanide poisoning -thiocyanate poisoning
Diltizaem, Verapamil Mechanism of Action Block calcium channels in the vasulature AND in the cardiac myocytes
Diltizaem, Verapamil Indication for/Uses it is used to: -dilate the arterioles around the body -dilate coronary arteries -decrease SA node and AV node conductions..... dec HR -act on myocardial cells to dec force of contraction
Diltizaem, Verapamil Adverse Effects -blunted reflect tachycardia -bradycardia -induce AV heart block
Diltizaem, Verapamil Drug Interactions Good: diuretics Bad: digoxin, beta blocker, grape fruit juice
Propranolol Mechanism of Action Block Beta 1 and Beta 2 receptors
Propranolol Indication for/Uses Beta 1 block= decrease HR, decrease stroke volume and decrease renin Beta 2 block = bronchoconstrictuion; decrease glycogenolysis
Propranolol Adverse Effects -bradycardia -hypotension -AV heart block -rebound HTN if stopped abruptly
Propranolol Drug Interactions Bad: insulin; calcium channel blockers Good: other vasodilators
Metoprolol Mechanism of Action Block Beta 1 receptors
Metoprolol Indication for/Uses decrease HR, decrease stroke volume and decrease renin
Metoprolol Adverse Effects -bradycardia -hypotension -AV heart blcok -rebound HTN if stopped abruptly
Metoprolol Drug Interactions Bad: calcium channel blockers Good: other vasodilators
Propranolol Quirky Be cautious giving this to patients with asthma and diabestes
Metoprolol Quirky still some, but not much, teaching needed for diabetic patients
Spironolactone Mechanism of Action Block aldosterone receptor in the cells of the collecting duct
Spironolactone Indication for/Uses heart failure
Spironolactone Adverse Effects -hyperkalemia -dehydration -endocrine effects: gynecomastia; hirsutism; dysmenorrhea
Spironolactone Drug Interactions BAD: 1. potassium supplement; ACE-inhibitor GOOD: Furosemide
Eplerenone Mechanism of Action Block aldosterone in collecting duct, heart and vasculature to cause vasodilation
Eplerenone Indication for/Uses heart failure
Eplerenone Adverse Effects hyperkalemia
Eplerenone Drug Interactions BAD: potassium supplement GOOD: Furosemide
Triamterene Mechanism of Action Block sodium/potassium pump directly in the collecting duct
Triamterene Indication for/Uses -heart failure -hypertension
Triamterene Adverse Effects hyperkalemia
Furosemide Mechanism of Action block sodium reabsorption in the ascending limb of the loop of henle
Furosemide Kinetics/Dynamics PO: 45-60 min onset IV: 5-10 min onset
Furosemide Indication for/Uses -heart failure -hypertension
Furosemide Adverse Effects -Hypokalemia -Hypochloremia -dehydration -hypotension -hyponatremia -hyperglycemia -ototoxicity -hyperuricemia -decrease magnesium
Furosemide Drug Interactions BAD: Gentamycin; vancomycin GOOD: ACE-inhibitors; potassium-sparing diuretics
Furosemide Quirky works well in patients that have decreased/failing kidney
Hydrochlorothiazide Mechanism of Action block sodium reabsorption in the distal convoluted tubule
Hydrochlorothiazide Indication for/Uses -heart failure -hypertension
Hydrochlorothiazide Adverse Effects -hypokalemia -hypochloremia -hyponatremia -dehydration -hyperglycemia -hyperuricemia
Created by: bhundley



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