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50 Cards in this Set
- Front
- Back
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Edrophonium (simple alcohol)
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Reversible AchE inhibitor
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Carbamic esters of alcohol
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Reversible AchE inhibitor, hydrolyzed in 1 hour
Neostigmine, pyridostigmine (teriary, cross BBB) Physostigmine, carbaryl (quarternary, can't cross BBB) Prophylactic use --> Gulf war syndrome |
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Organophosphates
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Nerve gases
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2-PAM
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Helps with nerve gas poisoning if given quickly (before aging/ hydroxyl group comes off)
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Diazepam (valium)
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Binds to GABA receptors to enhance effect
Used to treat convlusions wtih nerve gas poisoning |
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Clinical uses of AchE inhibitors
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Alzheimers, Postoperature ileus, MG, atropine intoxication
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Atropine
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Muscarine antagonist used for:
CNS =relief of tremor, Parkinson's vistibular disturbances Eye= pupil dilation, cycloplegia, dry eye GI = inhibits mobility and secretion in the gut, inhibits salivary secretion GU = relaxes smooth muscle of the bladder wall and uterus to slow voiding |
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Muscarinic receptor side effects
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Tricyclic antidepressants, antihistamines, antipsychotics, anxiolytics, Gi agents
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M1 antagonists
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Dicyclimine, trihexyphenidyl
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M2 antagonists
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Gallamine
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M3 antagonists
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Darifenacin, solifenacin, oxybutynin, tolterdoine
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Alpha 1
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Vascular smooth muscle
Pupillary dilator muscle Pilomotor smooth muscle Prostate Heart Postsynaptic CNS adrenoreceptors |
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Alpha 2
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Platelets
Adrenergic and cholinergic nerve terminals Vascular smooth muscle Fat cels |
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Beta 1
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Heart
Juxtaglomerular cells |
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Beta 2
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Respiratory, uterine and vascular smooth muscle
Skeletal muscle- potassium uptake Human liver- stimulates glycogenolysis |
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Beta 3
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Fat cells- activates lipolysis
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D1
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dilates smooth muscle blood vessels
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D2
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modulates neruotransmitter release in nerve endings
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NE
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Binds to all except less beta 2
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Epi
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Binds to all AR equally
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Phenylephrine, methoxamine
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alpha 1 > alpha 2 >>>> beta
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Clonidine, methylNE
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alpha 2 > alpha 1 >>>>> beta
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Dobutamine
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beta 1 > beta 2 >>>>> alpha
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Isoprotenerol
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beta 1 = beta 2 >>>> alpha
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Terbutaline, metaproterenol, albuterol, ritodine
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beta 2 >> beta 1 >>>>>>alpha
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Fenoldopam
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D1 >>D2
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Treatment of persistent asthma
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1) Mild = inhaled steroids alone
2) Moderate = add short-acting beta agonist + possibly leukotriene blocker (+ possibly inhaled long-acting beta agoinst) 3) Increase dose of inhaled steroid + possibly inhaled long acting bronchodilaor + possibly leukotriene blocker antagoinst + possibly theophyline + possibly omalizumab 4) Severe = oral steroids |
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Treatment of AE COPD
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Antibiotics
Short-acting beta agoinsts Inhaled anticholinergic Steroids - oral at least 2 weeks or inhaled Treat respiratory failure Non-invasive PP ventilation |
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Methylxanthines (theophylline)
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Possible moleculare mechanisms:
Inhibit PDE --> prevent cAMP breakdown --> relaxes smooh muscle airway Adenosine antagonism Catecholamine release Effects suppressor T cells Narrow therapeutic index, use only in combo |
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Beta 2 agonists
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Activate AC --> cAMP --> smooth muscle relaxation
Also bind to K+ channels All have beta-1 activity Tremor, due to beta-2 skeletal muscle receptors Metabolic effects include hypokalemia, hyperglycemia, especially with cardiac disease |
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SABA
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4-6 hours
Desensitization with regular, prolonged used, use only prn Albuterol, metaprotenerenol, pirbuterol, levalbuterol, terbutaline |
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LABA
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Salmeterol and formaterol: 10-24 hours
Indacaterol: 24 hours Formoterol 20x efficacious > Salmeterol Salmeterol has less side effects, less desensitization, takes >10 minutes to act (vs. Formoterol 2-3 min) |
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Anticholinergics
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Atropine (side effects = glaucoma, urinary retention, dry mouth
Ipratropium (Atrovent) - 4-6 hours, potent bronchodilator, 30 min onset of action, minimal side effects |
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Aclidinium
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12 hours anticholinergic
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Tiotropium (Spiriva)
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12-24 hours Anitcholinergic
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Leukotriene blockers
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Zafirlukast (Accolate): LTD4, LTE4 R antagonists, not for under 7 or nursing.
Interacts with warfarin, theophylline, emycin Adverse effects: eosinophilia, Churg-Strauss Montelukast (Singulair): once a day, not in nursing mothers or pregnancy (is possible) Interacts with phenobarbitol Adverse effects: eosinophilia, Churg-Strauss Zileuton blocks several leukotriene receptors Adverse events: eosinophilia, Churg-Strauss |
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Corticosteroids
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Increase transcription of beta-2 adrenoreceptors, decrease transcription of cytokines and adhesion molecules
Inhibit release of mediators from eosinophils, macrophages, T lymphocytes Enhance bronchodilator actions of beta-2 agonists bid: Beclamethason, dipropionate, tiamcinolne acetonide, flunisolid, budesonide, fluticasone, cicesonide once daily: mometasone |
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Mast cell stabilizers
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Cromolyn sodium and Nedocromil
Prevent responses to allergens, mild effect Block mediator release from mast cells, prevent bronchoconstriction (but does not cause bronchodilation) |
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Monoclonal Anti-IgE antibody
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Omalizumab
Reduces number of exacerbations in severe asthma, half life 2-4 weeks (iv or sc) Expensive |
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Tx Persistent Asthma
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Mild: inhaled steroids
Moderate: Inhaled steroids + SABA prn + inhaled LABA + leukotriene blocker/antagonist + inhaled anticholinergic Severe: all of the above, increase dose of inhaled steroids, could try other drugs |
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Tx acute AE
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Oxygen
IV steroids + oral steroids High dose inhaled beta-2 agonist or inhaled anticholinergic Use oral steroids for a week |
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Tx COPD
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Smoking cessation drugs
Bronchodilators PDE inhibitors AAT Don't use long term oral steroids. Inhaled decrease AE frequency, increase pneumonia risk |
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Smoking cessation
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Nicotine
Buprpion : antidepressant, increases CNS NorEp and dopamine release Vernicline: partial agonist at nicotinic Ach receptor |
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PDE Inhibitor
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Roflumilast prevents cAMP degradation
has GI side effects decreases frequency of exacerbations |
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AAT
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Indicated for pts with AAT <11 umol/L with:
airway obstruction emphysema over 18 non-smoker |
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Tx AECOPD
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Antibiotics, SABA, anticholinergic, steroids (equal inhaled and oral)
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Endothelin 1 antagonist
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Bosentan- blocks A and B
Amrisentan - blocks A ET1 binds to ETA and ETB receptors, increases Ca2+, causes vasoconstriction, proliferation, hypertophy, fibrosis, inflammation |
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PDE-5 blocker
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Sildenifil, tadalifil
Works on NO pathway NO dilates blood vessels, reduces platelet and monocyte stickiness, decreases multiplication of SMC in artery, reduces ROS, reduces LDL cholesterol |
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Prostanoids
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Epoprostenol, trepostinil, iloprost
Potent systemic and pulmonary vasodilator (via cAMP-mediated smooth muscle cell relaxation), anti-platelet effects |
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Indomethacin
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Prostaglandin inhibitor, close ductus arteriosus in preemies
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