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Pharmacology Drugs #
Respiratory, Vasoconstrictors, Vasodilators, HTN, Angina, Heart Failure
Question | Answer |
---|---|
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 |