Adrenergic Agonist (sympathomimetic)

Drug Class
1 agonist

Drug Name
Phenylephrine

Mech of Action

Clinical Use

pharmacokinetic Adverse Effects

1. Angina & Tissue Necrosis 2. Anxiety 3. Hypertension 4. Bradycardia (Reflex effect) 1. Depression 2. Hypotension 3. tachycardia 4. Sedation 5. Orthostatic 1. Depression 2. TOLERANCE (stops working after awhile) 3. Hemolytic Anemia 4. Sedation IV drug Only 1. Arrhythmias/ tachycardia 2. Anxiety

Contraindications Interactions
1.Ventricular Fibrillation/ Tachcardia 2. Hypertension

Notes

*Smooth muscle contraction 1. Decongestant via inc Intracellular Ca 2. Pressor 3. Mydriasis induction Primary effect: Vasoconstriction of vascular smooth muscle DEC SYMPATHETIC TONE (SYMPATHOLYTIC) -Dec NE release via pre syn receptor stimulation 1. Dec HR ( dec C.O.) 2. Hypotension 3. Bradycardia 4. Blood Vessels Dilate *Allows Negative Feedback 1. Skeletal vasodilation ( lowers diastolic) 2. positive inotropic( increase cardiac contraction strength (inc systolic) 3. Positive Chronotropic ( inc heart rate) 4. Bronchodilator 1. Inotrope ( inc force contraction of cardiac muscle 1. skeletal vasodilation/ relaxation 2. relaxation (broncodilation) 3. Glycogenolysis activated 4. relation uterine smooth muscle 1. Hypertension 2. ADHD 3. Mitigate drug withdraw 4. Severe Pain Hypertension in Pregnancy

MAO inhibitors Main site of 1 is on (antidepressants) blood vessles.3

2 agonist

Clonidine

1.Depression Tricyclic *CAUTION* sudden antidepressents withdraw=hypertensi ve crisis and anxiety/ panic attack 1. Depression 2. Person has Hepatic Disease 3. MAOs inhibit therapy

*PNS (Blocks release of NE) and CNS (dec sympathetic)

Methyldopa

*Only CNS (b/c Prodrug) Its metabolized to amethyl-norepinephrine in brain *Used in Hospital settings as emergency drug * Remember: Not hitting a1 so NO VASOCONSTRICTION

Non-selective agonist (hits 1 and 2)

Isoproterenol

1. Cardiac Arrest 2. AV block 3. bradycardia 4. bronchospasms 5. Asthma 6. COPD

1 agonist

Dobutamine

1. congestive heart failure.

1. Arrhythmias/ Tachycardia 2. Hypertension 1. Tremors/Anxiety 2. Nasea ***3. Palpitations*** ***4. tachycardia***

*1 mostly found on heart and also Kidney *At high doses can activate 1 receptors. *2 mostly found on lungs and vasculature. *At high doses can activate 1 producing those effects which is why you get 3 and 4 on Adverse effects.

2 agonist

Albuterol

1. Asthma 2. Acute bronchiospasms and as prophylaxis 3. dec premature labor

Adrenergic Antagonist (sympatholytic)

Drug Class
1 antagonist

Drug Name
Prazosin Doxazosin

Mech of Action

Clinical Use

Pharmokinetics

Adverse Effects
1. Dizziness 2. Hypotension 3. Reflex Tachycardia 4. Nasal Stuffyness 5. TOLERANCE-limits usefulness why we combine drugs. 6. First Dose Phenomenon of syncope**

Contraindications Interactions
1. Hepatic Disease (bc metabolized in liver) 1.Angina 2. MI 1. Fall in BP undesirable

Notes
*Not a First line Drug *Used as an Additive

Non-selective antagonist (blocks 1 and 2)

Phentolamine Phenoxybenzamine

1. Main goal: Dec Peripheral 1.Hypertension Short Half life vascular resistance (dec Treat anxiety vasoconstriction of blood Long Half life vessels)-get vasodilation 2. Inc Heart rate ( in order to 1.Pheochromocytoma Shorter half life maintain BP) 1.Irreversible Anatagonst 2.Very long Half life (24hrs bc has to synthesize new receptors) *All same as Non selective except: -No bronchoconstriction (bc no b2 blocked)= allows for bronchodilation -No inhibition of recovery from hypoglycemia -No Dec Anxiety (allows for anxiety-useful for diabetes) -No inc peripheral resistance= vasodilation remains (skeletal vasodilation) same as propanonol except doesnt treat tremors. 1. Angina Long Half life ***HEART FAILURE*** 3. Hypertension 1. acute MI 2.Cardiac Arrhythmia 3.HYPERTENSIVE URGENCY and PERI/ POST -OPERATIVE HYPERTENSION Onset: (IV) Immediate and 9 min half life ** impt fir hypertensive crisis without plummeting BP

1.HR inc more with nonselective bc no negative feedback form 2

1 antagonist ( blockers)

Atenolol

Bisoprolol

Esmolol

-Same as Non selective 1 antagonist except: 1. Asthma and 2. Bronchospasms are not acontraindications. **ATENOLOL-not used in pregnancy-causes low birth rate

1 have no receptors on blood vesseles or lungs. *Use these with caution on asthma and diabetes patients.

Metoprolol

1. same as Short Half life but propanonol expect comes in extended doesnt treat tremors release ***HEART FAILURE*** 1. (-) Inotropic :Dec HR = dec C.O 2. (-) Dromotropic 3. (-) Chronotropic- Dec Contractility 4. Dec Renin Release 5. Anxiolytic (dec anxiety) 6. Dec Hypertension 7. Dec aq. Humor production of eye 8.Note: block 2- inc peripheral resistance (skeletal vasoconstriction) 9. Bronchioconstriction 10. Dec in: -lipolysis, glycogenolysis, insulin release, HDL, HDL/LDL ratio, and dec in recovery from hypoglycemia. 11. Inc in VLDL and triglycerides. 1. Angina 2. Cardiac Arrhythmias 3. Hypertension 4. MI prophylaxis & Post MI (heart attack) 5. Tremor 6.Pheochromocytoma 7. Glaucoma same as prop, just not for arrhythmias or Angina Hypertension Only for Cardiac Arrythemias (b/c K+ channel blocker) 1.Onset: 2-3weeks. 2. Given in IV 1-3 hrs onset. 3. Offers extended release of 6-11 hrs half life *(good long term treatment for hypertension) 4. Highly bound to plasma protein 1. Dizziness 2. Fatigue/lethargy 3. Sinus bradycardia 4. Hypotension 5. *Excerbation of Asthma/bronchiospasms/ Diabetes 6. SUDDEN WITHDRAW SYNDROME-rebound hypertension, MI, cardiac Arrhythemias, panic attacks 1. Asthma 2.AV block 3. Bradycardia 4. cardiogenic shock 5. Sick Sinus Syndrome 6. Diabetes 7. Hyperthyroidism 1. Drugs hat depress AV conduction 2. Drugs with (-) inotropic actons 3. ***Clonidine Withdraw= extreme hypertention 2 has receptors on blood vessels and lungs but 1 on heart. * First line of therapy for uncomplicated hypertension and people under 60 yrs old.

Propranolol Non-selective antagonist ( blockers) (blocks 1 and 2)

Timolol

Pindolol Sotalol

Mixed 1/ antagonists Carvedilol (blocking 1 and 1 and 2) Labetalol

1. Bronchoconstriction 2. Postural Hypotension 3. Vasodilation 4. Dec HR

1. Hypertension 2. MI /pre MI /Post MI 3. Angina 4.cardiomyopathy ***HEART FAILURE*** 1. Hypertension 2. HYPERTENSIVE EMERGENCY one of best drugs for hypertensive emergency but longer half life then Esmolol

Similar to non selective 1. Hepatic Disease antagonist and 1 antagonist except: 1. no reflex Tachycardia that is seen in 1 2. Less Peripheral vasoconstriction that is seen in 2)

* Beta Blockers are First line defense for hypertension for: 1. Ischemic heart Disease 2. Pre or post MI (STEMI) 3. Left Ventricular systolic dysfunction 4. Left Ventricular Hypertrophy (only if under 60 ys old) 5. Some Arrythmias. *The three drugs used for Heart failure have the longest half lifes which is beneficial for long term. * Methyldopa and Labetalol are first line drugs for hypertension in pregnant women and Atenolol is restricted- causes low birth weight.