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Alpha/Beta
Question | Answer |
---|---|
Types of Sympathomimetics | Endogenous catecholamines, Synthetic catecholamines, Synthetic noncatecholamines |
Vessel effects of the Sympathetic Nervous System | Vasoconstriction, Vasodilation (skeletal muscle) |
Pulmonary effects of the Sympathetic Nervous System | Bronchodilation |
Cardiac effects of the Sympathetic Nervous System | Chronotropy, increase HR/ Intotropy, contractility/ Dromotropy, SA node and AV node conduction |
Adipose Tissue/Hepatic effects from Sympathetic Nervous System | Lipolysis, Glycogenolysis |
What other things can be effected by the Sympathetic Nervous System | Insulin/Pituitary Hormone modulation |
CNS effects of the Sympathetic Nervous System | CNS Stimulation |
Sympathomimetic Amines mimic which part of the nervous system? | Sympathetic |
What receptors are stimulated with with sympathomimetic amines? | Adrenergic |
In general, sympathomimetics can be used to treat what problems? | Anaphylaxis, Shock, Heart Failure, Cardiac Resuscitation |
Sympathomimetic Efficacy depends on... | Concentration at receptor site, Affinity for receptor, Population of receptors available for binding |
What is another name for naturally occurring sympathomimetic amines? | Catecholamines |
Examples of Catecholamines | Epinephrine, Norepinephrine, Dopamine |
Ephedrine Class | Synthetic Noncatecholamine Sympathomimetic |
Ephedrine Receptors | Alpha 1, Beta 1, Beta 2 |
Ephedrine Mechanism of Action/Response | INDIRECTLY Stimulates release of endogenous Norepinephrine/ Increases HR/SBP/SVR |
Ephedrine Dose/Onset/Duration of Action/Routes | 5-25mg IV Immediate 15 min. - 1.5 hrs. IV/PO/IM/SQ |
Ephedrine Uses | Hypotension/Bronchoconstriction(PO), OB patients (no decrease in uterine perfusion) |
Ephedrine Special Considerations | Resistant to MAO in the gut, Tachyphlaxis (Trauma/Sepsis/ICU pts.) |
Phenylephrine Class | Synthetic Noncatecholamine Sympathomimetic |
Phenylephrine Receptors | DIRECT Alpha 1 |
Phenylephrine Mechanism of Action | Peripheral vasoconstriction |
Phenylephrine Dose/Onset/Duration of Action/Routes | Bolus 50-200mcg Infusion 25-100mcg/min (start at 10) Immediate 5-20 min IV/Nasal |
Phenylephrine Uses | Hypotension/SAH Pretreat for nasal intubation: Max dose 0.5mg (20mcg/kg in Peds) or **4 drops of 0.25%** |
Phenylephrine Side Effect | Reflex Bradycardia (only those with intact Baroreceptors) |
What patients benefit from Phenylephrine? | CAD, Aortic Stenosis (increases coronary perfusion without chronotropic effects) |
Ephedrine Concentration | 50mg/1ml (Dilute in 9ml volume) |
Phenylephrine Concentration | 10mg/1ml (Dilute 10mg in 100ml = 100mcg/ml) |
Epinephrine Name | Adrenaline |
Epinephrine Receptors | Alpha 1,2 Beta 1,2 |
Epinephrine Uses | Anaphylaxis, CPR, Hypotension, Poor O2 tissue delivery |
Epi Low Doses cause... | Vasodilation (Beta) |
Epi High Doses cause... | Vasoconstriction (Alpha) |
Epi Beta1 considerations | Increases myocardial O2 consumption and demand (Not good for CAD pts.), Dysrhythmias |
Epi Beta 2 considerations | Bronchodilates - Stabilizes mast cells and decreases histamine release (Good for anaphylaxis), +RAAS, +Lipolysis, Gluconeogenesis, Glycogenolysis, Ketones, Hyperkalemia -Insulin |
Epi Anaphylaxis Dose (Asthma) | 0.1-0.5mg (1:1000) SC/IM, 0.1-0.25mg (1:10000) IV over 5-10 min. (MAX 1mg) |
Epi ACLS Dose | 1mg (1:10000) IV q 3-5 min |
Norepinephrine Name | Noradrenaline (potent vasopressor) **SHOCK pts. |
Norepi Receptors | Alpha 1, 2 Beta 1 |
Main effects with Norepi | Increases SBP/DBP (increases Coronary perfusion), Increases SVR, may cause reflex bradycardia |
Norepi Side Effect/Medication? | Extravasation/Dermal Sloughing Can add REGITINE (Phentolamine) 10mg/Liter to norepi drip to treat/prevent |
Dopamine Uses | Systemic Shock, To increase UO |
How is Dopamine metabolized? | MAO |
Dopamine Low Doses | Dopaminergic: <2mcg/kg/min Increases renal blood flow, increases sodium excretion, inhibits aldosterone |
Dopamine Medium Dose | Beta: 2-5mcg/kg/min Indirectly releases norepi, +Inotoropic effects |
Dopamine High Dose | Alpha >10mcg/kg/min Vasocontriction (acts like epi, may switch to epi, dysrhythmias) |
Dopamine Side Effects | IV infiltrate, Use Regitine (Phentolamine mesylate) - Alpha 1 blocker, 5-10mg/10ml, inject within 12 hours |
Vasopressin Name | Arginine Vasopressin |
Vasopressin Class | Antidiuretic Hormone |
Where is Vasopressin formed and Secreted from? | Hypothalamus / Posterior Pituitary |
Vasopressin target organs | Kidneys / Blood vessels |
How does Vasopressin work on the kidneys? | V2 receptors increase water permeability on renal collecting tubules (via cAMP mechanism) |
How does Vasopressin work on blood vessels? | V! binds to vascular smooth muscle and causes vasoconstriction (more on periphery than pulmonary muscles - good for those who have PULM HTN) |
What mechanism does vasopressin use to effect blood vessels? | IP3 signal conduction pathway (release of Calcium from sarcoplasm) |
Vasopressin indications | DI, Cardiac Arrest, Cardiogenic shock refractory to inotropes |
Vasopressin Doses | DI: 5-10 U SC/IM BID-QID, Shock: 0.01-0.04U/min IV, Cardiac Arrest: 40 U IVP |
Isopreterenol Class | Synthetic Sympathomimetic |
Isopreterenol Receptors | Beta 1,2 |
Isopreterenol Dose | 2-20mcg/min |
Isopreterenol Uses | S. Brady unresponsive to Atropine, Status Asthmaticus, Post Heart Transplant (vagal dennervation) |
Dobutamine Receptors | Weak Alpha, Strong Beta 1 |
Dobutamine Uses | CHF |
Dobutamine Side Effect | Hypotension in septic pts. due to decrease in SVR |
What is another name for Phosphodiesterase inhibitors | Nonglycoside non catecholamine |
Phosphodiesterase Inhibitor Mechanism of Action | Inhibit the breakdown for the enzyme Phosphodiesterase, which break down cAMP (more cAMP, more uptake of Calcium) |
Phosphodiesterase Inhibitor examples | Milrinone / Amrinone |
Which is preferred Milrinone/Amrinone? | Milrinone (Primacor) |
Milrinone Considerations vs Amrinone | IV, easy to titrate, 15 more Inotropic potency than Amrinone (Inocor) |
Amrinone Side Effects | PO: GI upset, thrombocytopenia Half life 2-4 hours (Kidneys eliminate) |
What are some cardiac glycosides? | Calcium: Ca+ Chloride 10%/ Ca+ Gluconate 10%, Glucagon |
Calcium Uses | +Inotropic, Hypocalcemia (after PRBCs), Hyperkalemia, Ca+CB/Beta blocker overdoes |
Calcium Dose | 250-1000mg |
Calcium Chloride 10% Concentration | 100mg/1ml (10ml = 1000mg) Provides 270mg Ca+ per gram (3x more than Ca+ gluconate 10%) |
Calcium Gluconate 10% Concentration | Provides 90mg per Ca+ per gram (Less irritating to veins than Ca+ Chloride) |
Glucagon Class | Calcium Glycoside |
Where is glucagon produced? | Alpha cells of pancreas |
What type of action does glucagon have? | +inotropic effects |
What are some problems that glucagon can be used for? | Ca+CB/Beta blocker overdoes, relaxes Sphincter of Oddi |
What are side effects of glucagon? | ST/Hyperglycemia |
Alpha 2 agonist have what effects? | Inhibits SNS outflow, decreases MAC, Negative feedback which inhibits NE, Inhibits substance P. |
What is substance P and where is it inhibited and by what? | Pain transmitter, its release is inhibited in the substangia geliatinosa of the spine (analgesia) by Alpha 2 agonist |
What is the other name for Clonidine? What class of drug is it? | Catapres / Alpha 2 agonist |
Where can Clonidine act? | Peripheral presynaptic Alpha 2 receptors - inhibits Catecholamines (vasodilation), Central postsynaptic Alpha 2 receptors - MAIN ACTION (decreases SNS outflow/renin activity) |
What can abrupt discontinuation of clonidine lead too? | Rebound HTN/ST |
What are some uses of Clonidine? | Pre-op sedative, withdrawal, Catecholamine Suppression test in DX of Pheochromocytoma, TX with alpha blocker 1ST (Prazosin) then beta blocker. |
3 ways to block the action of Clonidine? | A2 antagonist: Regitine, A1 agonist: Neosynephrine, B1 agonist: |
Regitine Class and name? | Alpha Antagonist (Phentolamine) |
Regitine Dose/Onset of Action | Rapid onset, short duration, used for Pheochromocytoma HTN (1-5mg slow IVP) |
What can Regitine also be used for? | Vasoconstrictor local infiltrates (5-10mg/10ml and injected SC) |
What class is Droperidol? Other name? | Alpha Antagonist / Inapsine |
What type of drug is Droperidol and what is it used for? | Butyrophenone / Antiemetic, Mild decrease in BP |
What are some side effects with Droperidol? | Prolonged QT / Leads to Vtach |
What are Beta 2 Agonist used for? | COPD, Asthma, Bronchospasm, premature labor, |
Some Beta 2 Agonist drugs? | Metaproterenol (Alupent), Albuterol (Proventil, Ventolin), |
Which two Beta 2 Agonist are used for OB? | Terbutaline (Brethine) 0.25mg SQ, Ritodrine Hydrochloride (Yutopar) |
Which Beta 2 agonist is the only one approved for labor use in the US? | Ritodrine Hydrochloride (Yutopar) |
Chronic use of Beta 2 agonist can lead to what due to what? | Tachyphylaxis due to down regulation, and also an increased airway hyperresponsiveness. |
Down regulation causes (sensitization/desensitization)? When can it occur? | Desensitization / 1-6 hours of use. |
Beta antagonist therapy leads to what regulation? | Up regulation / Sensitization |
What are some beta antagonist uses? | Angina Pectoris/MI, HTN, SVT, Vdys, WPW syndrome, afib, Cardiomyopathies, preop hyperthyroid pts, Dig induced dys, Migraines, nervousness |
Some problems with beta antagonist use? | Bronchospasm (non-selective), Cardiac failure, Potentiates peripheral vasoconstriction, hyperkalemia. |
What patients should avoid beta antagonist medication? | PVD & Raynaud's disease DM (mask hypoglycemia and can prevent increase in serum glucose levels) |
What can abrupt discontinuation of beta antagonist cause? | Withdrawal syndrome, increases SNS activity |
Should we continue Beta antagonist therapy preoperatively? | YES |
How can beta antagonist be subdivided? | Selectivity for cardiac beta 1 receptors |
What is unique about beta antagonist selectivity? | As dose increases, selectivity diminishes. |
What does Beta 1 receptor blockers cause? | Decreases HR, contractility |
What does Beta 2 blockers cause? | Unwanted bronchospasm, Peripheral vasoconstriction- Propanolol(Inderal), Nadolol(Corgard), Timolol(Blocadren) |
Propanolol Onset/HL/Dose | 15 min, 4 hour HL (longer in hepatic pts.), 1-5 mg IV (start with 0.25-0.50mg) |
Esmolol Onset/HL/DOA//Dose/Metabolism | 2 min, 9 min HL, 10-15 min DOA, 500mcg/kg loading dose then 100-300mcg/kg/min, Bolus: 10-30 mg PRN, Plasma esterase |
Labetalol names? | Normodyne, Trandate |
Labetalol class | Non-selective beta blocker |
Labetalol beta/alpha blockade ratio? | 7:1 |
Is Labetalol good for anesthesia? | No, last 12-18 hours |
Labetalol dose/metabolism | 0.25mg/kg IV, Infusion 2mg/min, Bolus 5-10 mg, Hepatic/renal |
What must a patient have before giving labetalol? | Adequate HR |
What are examples of direct vasodilators? | Sodium Nitroprusside, Nitroglycerin, Hydralazine |
The action of direct vasodilators? | Increases the concentration of nitric oxide. NO stimulates guanylate cyclase to produce cGMP, which activates protein kinase. |
Sodium Nitroprusside uses | HTN, to induce hypotension to prevent blood loss, Pulm edema, blunt intubation 1-2mcg/kg |
Sodium Nitroprusside Onset/concentration/dose/duration | seconds, 25-50ml/500ml D5W, 25mcg/kg or 0.5mcg/kg/min, 1-3 min |
Pharmacological effects of Sodium Nitroprusside | Greater Arterial: decreases preload,after load,O2 consumption |
Some issues with Nipride? | Light sensitive, coronary steal, cyanide toxicity |
What dose can cyanide toxicity occur? | > 8mcg/kg/min (0.5mg/kg/hr) |
Metabolic acidosis from cyanide poisoning can be expressed as what two conditions? | Moderate: base deficit not worse than -10, VSS or Severe: base deficit > -10, unstable |
TX for Cyanide toxicity? | Stop drug, give 100% O2, correct acidosis, Sodium Thiosulfate 150mg/kg IV repeat q 10 min for 3-4 doses |
How to treat severe Cyanide toxicity? | Stop drug, 100% O2, correct acidosis, Sodium Nitrate 5mg/kg IV |
What else can be done for severe Cyanide toxicity? | Break ampule of amyl nitrate in breathing bag, creates methemoglobin which excess cyanide ions can bind. |
Nitroglycerin effects? | Greater venous dilation / Arterial dilation at high doses. |
Nitroglycerin uses | Angina pectoris, ischemia, biliary spasm, HTN, "unloading" of the heart with CHF/MI |
Nitroglycerin Side effects | pulsating HA, increased HR, ST depression if very large decrease in BP |
3 NTG effects overall | Increase O2 supply (vasodilation), Decrease work theory, smooth muscle relaxation |
Sublingual NTG dose | 0.4mg q 5 min x 3 |
IV NTG concentration/dose | 50mg/250ml, 5-10 mcg/min titrate q 1-2 min |
Hydralazine effects? | Arterial relaxation only |
Hydralazine uses | HTN |
Does hydrazine cause HR changes? | NO |
Hydralazine dose/onset/HL/DOA | 2.5-20mg IV, 2-20 min WAIT FOR RE-DOSING, 1 hour HL, 12 hour duration |
Hydralazine side effects | ST depression from decrease BP, Lupus syndrome, N&V (Zofran) |
How do CCBs work? | Depress electrical impulses in the SA/AV nodes |
How do CCB effect inotropy and chronotropy? | negative effects |
CCB indications | Prinzmetal's Angina, HTN, Atrial tachycardia, Post CABG when radial artery used as graft to prevent vasospasm. |
Avoid CCB in which patients? | Wide complex tachycardia, Afib associated with WPW syndrome, Simple atrial tachycardia, CHF, Sick sinus syndrome |
Combining CCB with which medication can lead to which complication? | Fentanyl / bradyarrhythmias |
When would you only use CCB and beta blockers together? | IHSS (Idiopathic Hypertrophic Subaortic Stenosis) decreases HR and contractility |
CCB can influence which medication? Which CCB specifically? | CCB can increase dig levels by 30-70%, especially with Calan(Procardia) |
CCB Examples | Nifedipine(Procardia/Adalat), Nicardipine (Cardene), Diltiazem, Nimodipine, Verapamil |
Which CCB treats atrial tachydysrhythmias? Dose | Verapamil IV 2-5mg, q 30min, onset 10min, duration 2-4 hour |
Which CCB treat cerebral vasospasms? | Nimodipine |
Which CCB treat angina? | Nifedipine/Diltiazem |
Which CCB treat HTN is neroanesthesia? | Nicardipine |
Which CCB is used to stop labor? | Nifedipine |
Nifedipine dose | 10mg SL onset 10-20 min, duration 2-3 hours |
What do ACE inhibitors treat? | CHF/HTN/Post MI |
How do ACE inhibitors work? | Block converse of Angiotensin I to Angiotensin II |
ACE inhibit examples | Catopril (Capoten), Enalapril (Vasotec), Lisinopril (Prinivil, Zestril) |
ACE inhibitor side effects | Cough, angioedema, hyperkalemia |
What problem could occur with ACE inhibitor and anesthesia? | Refractory hypotension / bradycardia |
Angiotensin II receptor blocker effects? | Directly blocks angiotensin II effects |
How does ARBs compare to ACE inhibitors? | ARBs prevent buildup of bradykinin and prostaglandins and prevents cough. |
ARB examples | Saralasin(Serenin), Losartan |
How many Antidyrhythmic Classes are there? | 4 |
How many Class 1 antidysrhythomics are there? | 3 |
Class 1 Antidysrhythmics | Sodium Channel Blockers |
Class 1A drugs | Quinidine, Procainamide, Norpace |
Class 1B drugs | Lidocaine, Tocainide, Dilantin |
Class 1C drugs | Flecainide, Encainide |
Class II Antidysrhythmics | Beta Blockers |
Class III Antidysrhythmics | Potassium Channel Blockers |
Class III drugs | Bretylium, Amiodorone |
Class IV Antidysrhythmics | Calcium Channel Blockers |
What is the resting potential of the cardiac ventricular cell? | -90 mV |
Pase 4 represents? | Diastole / resting membrane potential Na+/K+ ATPase pump restore levels. |
Phase 0 represents? | Rapid depolarization, opening of fast Na+ channels, Na+ into cell. |
Phase 1 represents? | Brief repolarization, CL- channels open move into cell, Na+ channels close, K channels open and K+ moves out. |
Phase 2 represents? | Plateau, Calcium moves into cell, K moves out. |
Phase 3 represents? | Repolarization, Calcium channels close, K continues to move out. |
How effective are class 1A/B/C Na+ Channel Blockers? | 1B: Weak (decrease ERP), 1A: Moderate (increase ERP) 1C: Strong (no change in ERP) |
What does Quinidine treat? | Supraventricular arrythmias, slows afib rate |
What can be effected by Quinidine | Potentiate NMBs |
What can Procanamide treat? | Ventricular Tachydysrhythmias |
What is a problem with chronic use of Procanamide? | Lupus |
What does Lidocaine treat? | Ventricular dysrhythmias (PVC/VT) |
How does Lidocaine treat PVCs? | Delaying phase 4 depolarization and decreasing K+ ion permeability |
Lidocaine dose | Bolus 2mg/kg Infusion 1-4mg/min |
What does Amiodarone Treat? Doses? | Supraventricular Tachydys 200mg PO, Ventricular tachydysrhythmias 400mg PO, IV 5mg/kg over 2-5 min effective for 4 hours |
How does Amiodarone effect the cardiac cycle? | Prolongs ERP |
What can Amiodarone do to the heart? | Prolongs QT interval, Torsades de pointes |
How do you treat Torsades de points? | Magnesium |
What is Bretylium used for? | refractory vent dysrhythmias |
Bretylium dose? | 5-10 mg/kg IV MAX 30mg/kg |
What patients would Bretylium be used with caution? | Renal patients |
What type of drug is Adenosine? | Endogenous Purine Nucleoside |
How is Adenosine formed? | Breakdown od ATP |
How does Adenosine work? | Binds to type 1 A receptors in the myocyte coupled with Gi proteins, this activates the K channels to open causing hyper polarization due to K+ efflux. |
With Adenosine, hyper polarization is seen with what? | Asystole |
What part of the heart is decreased with Adenosine? | AV conduction |
Adenosine Dose/HL | RAPID BOLUS 6 mg IV, followed by 12mg dose within 3 min. HL < 10 seconds |
Where is Adenosine metabolized? | In the RBCs |
What are the indications for Adenosine? | SVT, WPW |
Adenosine Side effects? | Flushing, vasodilation |
Adenosine is contraindicated with what patients? | 2nd & 3rd degree HB |