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68 Cards in this Set
- Front
- Back
What are the first gen H1 blockers?
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Diphenhydramine
Dimenhydramine chlorpheniramine |
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Mech of action for H1 blockers?
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Reversible inhibitors of H1 histamine receptors
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Uses for first gen H1 blockers?
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Allergy, motion sickness, sleep aid
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Toxicity for first gen H1 blockers?
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Sedation, antimuscarinic, anti-a-adrenergic
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What are the 2nd gen H1 blockers?
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Loratidine, fexogenadine, desloratadine, cetrizine
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Clinical uses of 2nd gen H1 receptor blockers
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Allergies
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Toxicity for 2nd gen H1 blockers?
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Far less sedating than 1st gen because of lowered entry into the CNS.
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What are the B2 agonists used in treating asthma?
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Albuterol, salmeterol, formoterol
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How does albuterol work and when is it used?
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Relaxes smooth muscle in bronchial
Used during an acute exacerbation |
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When are salmeterol and formoterol used and how do they work?
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They are long acting agents used for prophylaxis.
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What is theophylline used for and how does it work?
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Treating asthma, although rarely due to bad side effects.
causes bronchodilation by inhibiting phosphodiesterase, which lowers cAMP hydrolysis. Also blocks action of adenosine |
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Why is theophylline rarely used?
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narrow therapeutic index due to cardio and neuro toxicity.
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What muscarinic antagonist is used in treating asthma?
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Ipratropium
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How does ipratropium work?
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Competitive block of muscarinic receptors, preventing bronchoconstriction.
Can also be used for COPD. |
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What two steroids are used for treatment of chronic asthma?
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Beclomethasone
Fluticasone |
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How do Beclomethasone and Fluticasone work in treating asthma?
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They inhibit the synthesis of virtually all cytokines, and inactivate NF-kB, the transcription factor that helps make TNF-a.
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What are the antileukotrienes used in treating asthma?
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Montelukast, zafirlukast, zileuton
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How do montelukast and zafirlukast work?
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Block leukotriene receptors. Especially useful in treating aspirin-induced asthma
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How does Zileuton work?
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inhibits 5-lipoxygenase pathway
Blocks conversion of arachidonic acid to leukotrienes |
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What is omalizumab and what does it treat?
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Monoclonal anti-IgE antibody. Binds serum iGE.
Used in allergic asthma that is resistant to inhaled steroids and long acting beta agonists. |
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What are the two expectorants commonly used?
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Guaifenesin - thins respiratory secretions; does not suppress cough.
N-acetylcysteine - loosen mucous plugs in CF patients. Also used in acetaminophin OD. |
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Used to treat pulmonary hypertension, this drug competitively antagonizes endothelin-1 receptors, decreasing pulmonary vascular resistance
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Bosenten
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What is dextromethorphan, and what effects can it cause?
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Antitussive (anti cough)
Antagonizes NMDA glutamate receptors Synthetic codiene analog. Has mild opioid effect when used in excess. Nalaxone can be given for overdose. Mild abuse potential. |
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Pseudoephedrine and phenylephrine - Uses?
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Reduce hyperemia, edema, and nasal congestion.
Open obstructed eustacian tubes |
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What is the mech of action for Pseudoephedrine and phenylephrine?
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Sympathomimetic a-agonist nonprescription nasal decongestant
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Toxicity for Pseudoephedrine and phenylephrine?
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Hypertension
CNS stimulation/anxiety (pseudoephedrine) |
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Methacholine - what is it used for?
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Used in the asthma challenge test. Muscarinic receptor agonist
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Insulin - mech of action?
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Bind insulin receptor
Liver: increase glucose stored as glycogen Muscle: increase glycogen and protein synthesis, K uptake Fat: aids TG storage |
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Clinical use for insulin?
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Type I DM, Type 2 DM, Gestational diabetes
life-threatening hyperkalemia stress-induced hyperglycemia |
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Possible toxicity for insulin use?
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hypoglycemia
very rarely hypersensitivity rxns |
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Metformin - clinical use?
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Oral - first line therapy in Type 2 DM.
Can be used in pts without islet fxn. |
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Toxicity of metofrmin?
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GI upset
Most serious is lactic acidosis (contraindicated in renal failure) |
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Sulfonylureas - mech of action?
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Close K channel in B-cell membrane - cell depolarizes and triggers insulin release via Ca influx.
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What are the sulfonylureas?
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1st gen: tolbutamide, chlorpropramide
2nd gen: Glyburide, glimeprimide, glipizide |
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Clinical use for sulfonylureas?
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Stimulate release of endogenous insulin in type 2 DM. Useless in Type 1
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Toxicity of sulfonylureas?
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1st gen: disulfuram-like effects
2nd gen: hypoglycemia |
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Glitazone mech of action?
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increase insulin sensitivity in peripheral tissue. Binds PPAR-y nuclear transcription regulator
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Clinical use for glitazones?
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Monotherapy in Type 2 DM or combined with other agents
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Toxicity of glitazones
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weight gain, edema, liver tox, heart failure
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a-glucosidase inhibitors mech of action?
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inhibit brush border a-glucosidases
Delayed sugar hydrolysis and glucose absorption Lowers postprandial hyperglycemia |
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Clinical uses for a-glucosidase inhibitors?
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Monotherapy in Type 2 DM or with other agents
Can cause GI disturbances |
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What are the a-glucosidase inhibitors?
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Acarbose
Miglitol |
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Mech of action for pramlintide (amylin analog)?
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Lowers glucagon
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Clinical use for pramlintide?
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Type 1 and 2 DM
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Toxicity for Pramlintide?
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Hypoglycemia, nausea, diarrhea
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What are the GLP-1 analogs?
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Exenatide
Liraglutide |
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Mech of action for GLP-1 analogs?
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Increase insulin and decrease glucagon release
Used in Type 2 DM |
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Toxicity for GLP-1 analogs?
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N/V
pancreatitis |
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DPP-4 inhibitors?
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Linagliptin
Saxagliptin Sitagliptin |
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Mech of action for DPP-4 inhibitors?
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Increase insulin, decrease glucagon
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Use for DPP-4 inhibitors?
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Type 2 DM
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Toxicity for DPP-4 inhibitors?
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Mild urinary or respiratory infections
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Propothiouracil and methimazole - Mech of action?
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Block peroxidase, inhibiting organification of iodide and coupling of thyroid hormone synthesis. PTU also blocks 5-deiodinase, which lowers conversion of T4 to T3
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Propothiouracil and methimazole - clinical use?
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Hyperthyroidism
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Propothiouracil and methimazole - Toxicity?
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skin rash, agranulocytosis, aplastic anemia, hepatotoxicity. Methimazole = possible teratogen.
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Levothyroxine and triiodothyronine - mechanism of action?
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Thyroxine replacement
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Levothyroxine and triiodothyronine - clinical use?
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Hypothyroidism and myxedema
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Levothyroxine and triiodothyronine - Toxicity?
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tachycardia, heat intolerance, tremors, arrhythmias
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GH use?
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GH deficiency, turner syndrome
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Somatostatin use?
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acromegaly, carcinoid, gastrinoma, glucagonoma, esophageal varices
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Oxytocin use?
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Stimulates labor, uterine contractions, milk let-down, controls uterine hemorrhage
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ADH use?
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Pituitary (central) Diabetes insipidous
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Demeclocycline - mechanism of action?
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ADH antagonist
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Demeclocycline - clinical use?
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SIADH
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Demeclocycline - Toxicity?
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Nephrogenic DI, photosensitivity, abnormalities of bone and teeth
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Glucocorticoids - mechanism of action?
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lowers production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expression of COX-2
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Glucocorticoids - Clinical use?
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addison's disease, inflammation, immune suppression, asthma
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Glucocorticoids - Toxicity?
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Cushing's syndrome - buffalo hump, central obesity, purple striae, moon facies, muscle wasting, thin skin, easy buisability, osteoporosis, adrenocortical atrophy, peptic ulcers, diabetes.
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