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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 |