Term
| histidine decarboxylase action? |
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Definition
| converts histidine to histamine. |
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Term
| what is endogenous source of histamine? |
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Definition
| mast cells & basophils (98%). Hypothalamic histaminergic neurons. enterochromaffin cells. |
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Term
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Definition
| Gq/11 protein coupled receptor; allergic reaction (wheezing, sneezing, itching). Exocrine excretion, constriction of bronchioles, constriction of gastric smooth muscles, sensitization of nerve endings, activation of endothelial cells, decreased AV node conductance |
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Term
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Definition
| Gås protein coupled; increase gastric acid secretion; increase mucous production |
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Term
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Definition
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Term
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Definition
| periphery only; contributes to allergic reactions |
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Term
| mechanism of all Histamine receptors? |
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Definition
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Term
| following PO administration antihistmines...(kinetics) |
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Definition
| are well absorbed; peak within 3 hours; effective within 30 minutes. half life is 3 - 24 hrs. most are hepatic metabolism |
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Term
| what are the classes and main example of first generation antihistamines? |
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Definition
| alkylamines (ex: chlorpheniramine); ethanolamines (ex diphenhydramine); Ethylenediamines (ex tripelennamine); Phenothiazine (promethazine) |
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Term
| what are the classes and main examples of 2nd gen antihistamines? |
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Definition
| piperidines (fexofenadine, loratidine); piperazines (cetirizine) |
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Term
| what are the main toxicities of first gen antihistamines? |
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Definition
| CNS effects b/c crosses BBB; anticholinergic activity; prolonged QT |
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Term
| What are the indications for first gen antihistamines? |
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Definition
| allergies, motionsickness/nausea/morning sickness; sleep aid |
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Term
| Diphenhydramine: class, indication, toxicity |
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Definition
| ethanolamine 1st gen; indication: allergies, motion sickness; sleep aid; anticholinergic (dry mouth), sedation; short half life |
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Term
| chlorpheniramine: class, indication, toxicity |
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Definition
| alkylamine -1st gen; indication: coadministrated for hydrocodone/dextromethorphan or cough suppression; less drowsiness than diphenydramine; |
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Term
| promethazine: class, indication, toxicity |
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Definition
| phenothiazine 1st gen; indication: allergies, nausea, sedation, motion sickness, sleep aid; toxicity: don't give to kids under 2, seizures; antiserotinergic, a-alpha-adrenergic, a-cholinergic |
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Term
| Compare second gen to first gen antihistamines |
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Definition
| second gen don't cross BBB; low or no anticholinergic activity; no sedative or other CNS effets; lower toxicity. Indicated for all forms of allergies but not for sleep induction, nausea or motion sickness |
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Term
| toxicity for second generation antihistamines |
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Definition
| fatigue, dyspepsia, peripheral anticholinergic, CARDIAC ARRYTHMIA (drug interactions with macrolides and antifungal) |
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Term
| fexofenadine: class, indication, toxicity, kinetics |
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Definition
| aka allegra, piperidine, 2nd gen, metabolite of terfenadine, selective peripheral H1 receptor antagonist, t1/2=14hr; |
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Term
| loratadine: class, indication, toxicity, kinetics |
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Definition
| aka claritin, piperidine, 2nd gen; desloratadine is active metabolite; first pass elimination and CYP450; |
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Term
| cetirizine: class, indication, tox; kinetics |
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Definition
| aka zyrtec; metabolite of hydroxyzine (first gen); KIDNEY EXCRETION; |
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Term
| what is an alternative or adjunct for people who have year-round allergies? |
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Definition
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Term
| nasal steroids: examples, mechanism, indication |
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Definition
| ex: fluticasone; mech: direct application on nasal passage to reduce swelling and inflammation; indication: seasonal/year round, allergic nasal sx to relieve itching, runny or congested nose, post-nasal drip and sneezing. 4+ y/o |
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Term
| mechanism for decongestants |
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Definition
| vasoconstrictors via activation of alpha adrenergic receptors (pseudoephedrine, phenylephrine, ephedrine); |
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Term
| Contraindication for combo of antihistamines and decongestants |
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Definition
| children under the age of six |
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Term
| what is the goal of asthma therapy? |
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Definition
| near or complete freedom from asthma symptoms by decreasing inflammation and frequency of attacks |
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Term
| what are the cardinal symptoms of asthma? |
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Definition
| SOB, chest tightness, WHEEZING |
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Term
| what permanant changes occur during chronic asthma |
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Definition
| inflammation, mucosal thickening, increased mucous, increased mast and goblet cells, decreased ciliated cells, basement membrane thickens |
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Term
| what is the action of epinephrine on bronchi? |
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Definition
| sympathetic release of EPI activates ß2 adrenergic receptors = bronchodilation. VIP, PGE2, NO dilate too. |
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Term
| what is the action of ACh on bronchi? |
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Definition
| parasympathetic release of ACh = M3 receptor activation = bronchoconstriction. also by adenosine, histamine, 5-HT, substance P, NPY, PGD2, Leukotriene |
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Term
| what are the two main treatment strategies for asthma? |
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Definition
| bronchodilators (smooth muscle relax &. Antiinflammatory agents |
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Term
| What are the classes of bronchodilators in asthma treatment? |
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Definition
| ß-adrenergic receptor agonists: short and long acting; Muscarinic receptor antagonists; methylxanthines: adenosine receptor antagonists |
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Term
| what are the types of antiinflammatory agents used in asthma treatment? |
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Definition
| Glucocorticoids; leukotriene receptor antagonists; leukotriene synthesis inhibitors; mast cell stabilizers; |
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Term
| Epinephrine: Class, Mech, indication, tox |
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Definition
| non-selective adrenergic agonist; rapid onset & short duration; acts on all alpha and beta receptors; ß receptor = relax bronchial smooth muscle; tox: tremor, blood glucose increase, HR up; BP up; paradoxical bronchospasm; contraindicated in <3 disease, HTN, diabetes, thyroid disease or seizures; interacts with ß-blockers, MAO inhibitors and tricyclic antidepressants; antidiabetic drugs |
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Term
| Isoproterenol: class, mech, ind, tox |
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Definition
| ß-selective adrenergic receptor; B1=B2>>>alpha; ind: acute bronchospasm; mech: relax sm muscle; short duration; similar tox as epinephrine but not as much HTN. reacts with MAO inhibitors, antidepressants and anti-diabetic drugs. |
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Term
| albuterol: class, mech, ind., tox |
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Definition
| class: ß2 selective, short acting; ind: treatment of acute symptoms and maintenance Tx; Tox: reduced CV effects..rare: tachycardia, nausea, nervousness, tremors, headache; paradoxical bronchospasm, sudden death |
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Term
| salmeterol: class, mech, ind, tox |
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Definition
| ß2 selective LONG acting; maintenance tx, improves lung f(x) and QOL in pt with chronic asthma & adjunct tx in exercise induced & nocturnal asthma. side effects rare: headache, dermatitis, paradoxical bronchospasm: small but significant increase in asthma related deaths |
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Term
| ipratropium bromide & tiotropium bromide: class, mech, ind, tox |
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Definition
| muscarinic antagonist; blocks contraction of smooth muscles in response to ACh released from vagus (decreased PS tone); ind: maintenance only, tx of nocturnal, psychogenic, ßblocker induced asthma attacks; no serious side effects |
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Term
| theophylline: class, mech, ind, tox |
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Definition
| methylxanthine bronchodilator; non-selective adenosine receptor antagonist; relaxes bronchial smooth mm; inhibits phosphodiesterase so increases cAMP; inhibits antigen induced degranulation; IND: exercise induced, TOX; narrow TI, reacts with liver met drugs; |
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Term
| Coritocosteroids - overall mechanism |
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Definition
| anti-inflammatory by inhibiting immune cell f(x); decreasing inflammatory mediator synthesis; decreased downreg of ß-receptors;indicated for maint of moderate & severe asthma or adjunct for acute asthma. |
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Term
| Prednisone/Prednisolone: class, mech, ind, tox |
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Definition
| CLASS: systemic corticosteroid anti-inflammatory; MECH: inhibit immune cell f(x); IND: moderate and severe asthma maintenance; TOX: decreased immune function, adrenal suppression, wt gain, |
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Term
| Beclomethasone: class & indication |
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Definition
| inhaled corticosteroid; long term maint only; approved in kids 5-11 y/o |
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Term
| triamcinolone & flunisolide: class & IND |
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Definition
| inhaled corticosteroid; long term maint only; |
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Term
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Definition
| inhaled corticosteroid; used in combo with salmeterol for patients with moderately severe asthma not controlled by inhaled corticosteroids alone |
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Term
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Definition
| pro-inflammatory. induce: bronchoconstriction, mucus secretion, chemotaxis, edema |
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Term
| how are leukotrienes synthesized? |
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Definition
| Arachadonic acid --> LTD4 by 5-lipoxygenase. |
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Term
| What is the LTD4 receptor? what happens when it binds? |
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Definition
| CysLT1/2. inflammation and bronchospasm |
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Term
| Zileuton: class, mech, ind, tox |
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Definition
| CLASS: leukotriene synthesis blocker; MECH: inhibits 5-lipoxygenase decreasing LTD4 levels; IND: maint of mild/severe asthma>12y/o;don't use in pregnant or breastfeeding; TOX: dyspepsia, nausea, liver dysfunction; inhibits CYP450 and alters clearance of theophylline, warfarin, propranolol |
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Term
| Zafirlukast & Montelukast: CMIT |
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Definition
| Class: leukotriene receptor antagonist MECH: blocks CYSTLT1 & CysLT2; IND: Maint only for mild persistent asthma prophylaxis in adults and children > 6. TOX: rare - liver dysfunction, eosinophilia. increased infection in old; limited experience. contraindicated during pregnancy and lactation |
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Term
| Cromylyn sodium & nedocromil sodium: CMIT |
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Definition
| C: mast cell stabilizer; M: inhibits stimulus induced release of inflammatory factors by mast cells; I: maint and prophylaxis only; prevention of acute exercise or allergen induced asthma; ineffective for bronchospasm; TOX: least toxic because not systemic. DRUG OF CHOICE FOR PREGO |
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Term
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Definition
| C: anti-IgE antibody; M: binds free circulating IgE; I: mod/severe asthma induced by allergen & inadequately controlled by corticosteroids in pt >12 y/o. Tox: allergic reaction - anaphylaxis |
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