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Systemic Toxicity of po or iv corticosteroids for use less than 2 wks
Possibly acute peptic ulcer, rarely acute pancreatitis.
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Systemic Toxicity of po or iv corticosteroids for use more than 2 wks
Adrenal suppression. Iatrogenic Cushing’s Syndrome. Face: round, puffy “moon” face. fat redistribution to trunk and back of neck; increased hair growth on face and body; acne; insomnia; increased appetite; muscle wasting; thinning of skin; hyperglycemia; osteoporosis; diabetes; aseptic necrosis of hip; impaired wound healing
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short acting glucocorticords
hydrocortisone (cortisol), cortisone, prednisone, prednisolone, methylprednisolone
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corticosteroids that are oral only
fludcortisone (mineralcorticoid), cortisone and prednisone are short acting
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corticosteroids that can be injected
hydrocortisone, prednisolone, and methylprednisolone are short acting. triamcinolone is intermediate acting. betamethasone and dexamethasone are long acting
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intermediate acting corticosteroids
triamcinolone
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long acting corticosteroids
betamethasone and dexamethasone
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toxicity of inhaled corticosteroids
hoarsness and oropharyngeal candidiasis. Very long-term use may cause cataracts and osteoporosis
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inhaled corticosteroids
Beclomethasone, Budesonide, Ciclesonide, Flunisolide, Fluticasone, Mometasone, Triamcinolone
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topical corticosteroids
hydrocortisone (short acting), as well as intermediate and long acting corticosteroids (triamcinolone, betamethasone and dexamethasone)
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not absorbed. Stabilize Mast Cells against antigen IgE-sensitized release of Histamine
Cromolyn sodium & Nedocromil
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H1 blocker, anticholinergic
dimenhydrinate (dramamine) and diphenhydramine (benadryl)
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H1 blocker, anticholinergic, alpha-1 block
promethazine
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toxicity of promethazine
drowsiness, strong sedation, orthastatic hypotension, blurred vision, urinary retention
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H1 block, anticholinergic, blocks 5-HT2
Cyproheptadine
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usefulness of cyproheptadine
antiemetic, antimotion, allergy, dermitis, hay fever
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toxicity of cyproheptadine
drowsiness, strong sedation, blurred vision, urinary retention
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competitive H1 blockers, no anticholinergic actions
Fexofenadine (Allegra), Loratadine (Claritin), Citrizine (zyrtec)
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serotonin-improving indirect agonists
Tricyclic Antidepressants (TCA), Imipramine NE, 5-HT, Amitriptyline NE, 5-HT
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Phenelzine
irreversible, inhibits MAO-A, MAO-B. indirect serotonin agonist
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Tranylcypromine
reversibly inhibits MAO-A, -B. indirect serotonin agonist.
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sumatriptan MOA
Partial Agonist at 5-HT-1 receptors. Objective is to overcome vasodilation which causes throbbing pain. Migraine and cluster headaches.
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carcinoid tumor
neoplasm of enterochromaffin cells releases serotonin
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symptoms of carcinoid tumor
Flushing of the head and neck. Abdominal cramps and diarrhea are common. Asthmatic wheezing
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Alpha-1 antagonist (also blocks 5-HT2)
phenoxybenzamine
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DA-2 antagonist (also blocks H1, M3, 5-HT2, Alpha-1)
chlorpromazine
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used for nausea, vomiting or GI hyperactivity
5-HT3 Antagonists
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5-HT3 Antagonists
Ondansetron, Palonosetron, Alosetron is toxic
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blocks 5-HT3 receptor, stops activation of vomiting center in medulla. Prevents nausea and vomiting during cancer chemotherapy
ondansetron
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new, potent 5-HT3 antigonist, can be used during nausea/vomiting to reverse the problem
Palonosetron
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toxic 5-HT3 antigonist, can cause ischemic colitis, but was returned to market to treat severe diarrhea, irritable bowel syndrome in women. FDA warning is attached
alosetron
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PGs from COX-1 pathway are...
cellular protective. regulates angiogenesis and reduces acid & pepsin level in stomach (protective)
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PGs from COX-2 pathway are
healing/destructive
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Acetaminophen action
COX-2 selective blocker
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Thromboxane A2 (TXA2) actions
vasoconstriction, bronchoconstriction
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actions of prostacyclin (PGI2)
Vasodilator. Bronchodilator. Stabilizes platelets, disaggregates platelets
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Epoprostenol
PGI2 agonist – Reversal of pulmonary hypertension
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actions of prostaglandin E1 (PGE1)
Vasodilator. Bronchodilator. Cytoprotective in GI tract (decreases acid and pepsin). Regulates renal blood flow, probably is a local vascular autoregulator of flow. Contracts uterine smooth muscle, active in labor and delivery
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Dinoprostone
PGE1 second trimester abortion
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actions of prostaglandin F2alpha
Vasoconstrictor. Bronchoconstrictor. Pathogenic in asthma
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Latanoprost
PGF2alpha agonist topical for glaucoma
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actions of Alprostadil
PGE1 agonist. vasodilator in peripheral vascular disease. Maintains an open (Patent) Ductus Arteriosus
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GI protective drug
Misoprostol (PGE1)
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COX2 inhibitors (tylenol) lead to...
COX1 pathway activation ---> platelet aggregation via more thromboxane being produced
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blocks lipoxygenase, inhibits leukotriene synthesis
Zileuton
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a leukotriene receptor antagonist. Toxicity is Churg Strauss Syndrome, systemic eosinophilic vasculitis when steroid dose is decreased
Zafirlukast
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leukotriene receptor antagonist. Side effects are GI distress, bleeding and hypersensitivity
Montelukast (Singulair)
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Epi actions
B1, B2, alpha1
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isoproterenol
B1, B2. used in EM
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mast cell stabilizers
cromolyn sodium and nedocromil
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ipratropium
antimuscarinic
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Low dose, non-prescription inhaler. Emergency bronchodilation, sc, im. Acts in 15 min, lasts 60-90 min, sold OTC as Primatene Mist and Bronkaid inhalers, a “Rescue” medication
epinephrine
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Orally available, 4-6 hrs, like EPI
ephedrine
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Inhaled for onset in 1-5 minutes, Duration of action is 2-6 hr
Rapidly acting, used as “Rescue” medications, can be used approx. 15 min before exercise
Metaproterenol, Albuterol, Terbutaline
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Both are inhaled for prophylactic decrease of histamine release. Short and long – term.
Effective when administered before exercise, allergens, cold air, etc
Less than 1% is absorbed into systemic circulation à very safe, absence of side effects
Very high Therapeutic Index (200-500)
cromolyn sodium and nedocromil. stabilize mast cells
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iv, is used in high dose in emergency relief of severe acute asthma
methylprednisolone
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Less potent than Beta-2 Agonists, but are often used in combination.
po 6-12 hrs, iv during acute episodes, sustained release preps for overnight coverage
Therapeutic is 10-15 mg/L blood. Toxicity is significant at 20 mg/L or higher, fatality at 25 mg/L. TI=1.3
aminophylline and theophylline
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Ipratropium has low or high TI?
high. safe, not much absorbed
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LKT4 Receptor Antagonists
- Zafirlukast: po 12 hr
- Montelukast: po 24 hr
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Alternative to CS or Cromolyn
LKT4 receptor antagonist and 5-lipooxygenase blocker
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5-lipooxygenase blocker
Zileuton. po 6 hr
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