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61 Cards in this Set
- Front
- Back
What are the alpha/beta agonists?
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1. E
2. NE |
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What are the alpha agonists?(3)
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1. Phenylephrine
2. Clonidine 3. Apraclonidine |
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What are the beta agonists?(6)
Remember T.R SAID it |
1.Sameterol
2. Albuterol 3. Isoproterinol 4. Dobutamine 5. Tertbutaline 6. Ritodrine |
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What are the D receptor agonists?
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DA
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What are the mixed acting adrenergics?(5)
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1. Ephedrine
2. Methyl Dopa 3. Tyramine 4. Cocaine 5. Dextroamphetamine |
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What receptors does Epi and ephedrine hit?
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All alpha and beta
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What receptors does NE and DA hit?
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1. Alpha 1 and 2
2. Beta 1 |
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What receptors does Phenylephrine hit?
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1. Decongestant
2. Alpha 1 |
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What receptors does clonidine and Apraclonidine hit?
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1. Alpha 2
2. CNS and glaucoma |
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What receptors does isoproterenol hit?
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1. Beta 1,2 and 3
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What is dobutamine for and it's receptors?
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1. Inotropic agent
2. beta 1 |
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What receptors does albuterol, tertbutaline, Salmeterol and Ritodrine hit?
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1. Beta 2 for the lungs
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What is the chemistry of the catecholamines?
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1. Have two OH groups on the benzene ring
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What is the MOA of indirect acting adrenergics?(2)
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1. Stimulate the release of catecholamines
2. Inhibit the reuptake |
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What is the false transmitter concept?
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1. Some drugs like tyramine will be reuptaked into the synapse, displacing the store NE
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What pressures does E effect?
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1. Increase Systole, slight MAP
2. Not Diastole 3. Increase cardiac rate |
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What pressure does NE effect?
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1. Increase Systole, Diastole, and MAP
2. Decrease cardiac rate by reflex change |
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What pressure does isoproterenol effect?(3)
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1. Increase systole a little
2. Nothing else 3. Large increase in cardiac rate |
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What does E do to the CV(3)?
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1. Increase HR, but decrease cardiac efficiency
2. VasoC in GI and renal 3. VasoD in SKM and lungs and cornary arteries |
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What does E do to the BP?
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1. at low dose Beta 2 mostly and decreases to decrease BP
2. At normal or high doses it increases systolic BP, and Decreases diastolic BP |
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What does E do to the respiratory system?
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1. SM relaxation
2. Increased mucociliary clearance 3. no effect on secretions |
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What does E do to the GI system?(3)
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1. Relaxes the SM (A2, B2)
2. Decreases peristalsis 3. Contraction of the sphincters(A1) |
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What are the effects of E on the GU?
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1. Contraction of trigone and internal sphincter
2. Detrusor relaxes to allow bladder to fill 3. Relaxation of pregnant uterus |
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What are the CNS effects of E?
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1. Does not enter the CNS so no direct effect
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What are the E effects on the Eye?
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1. Alpha 1 mydriasis
2. Decreased aq humour production with A2 |
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What are the E effects on the SKM?(3)
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1. Increased contractility
2. Tremor! Beta 2 3. Increased K uptake |
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What are the metabolic effects of E?(4)
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1. Hyperglycemia
2. Inhibit insulin secretion 3. Glucose metabolism 4. Glucagon secretion |
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What are the effects of E in the kidney's, platelets and immune?
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1. Renin secretion(Beta 1)
2. Inhibition of inflammatory mediators(B2) 3. Stimulates platelet aggregation |
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How do you get E in the body?
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1. No oral bioavailability
2. Slow SC 3. Fast IM |
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Where is E distributed?
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1. Peripheral tissues
2. Not in the CNS |
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Where is E biotransformed?
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1. The liver
2. Where COMT and MAO are |
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What are the adverse effects of E in the CNS? Contraindications?(5)
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1. Fear, anxiety. Hemorrhage(BP increase)
2. Hypertension, hyperthyroidism 3. Angina 4. Shock 5. Pregnancy |
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What are the therapeutic uses of E?
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1. Hypersensitivity reactions
2. Prevent surgical bleeding 3. Asthma 4. Open angle Glaucoma (decrease aq humor) 5. CPR in cardiac arrest |
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What is the MOA of NE?
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1. Attacks Beta 1, and alpha 1 and 2
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What are the effects of NE on the heart? Vessels? BP?
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1. Final effect is to decrease the HR with the same CO
2. VasoC except Coronary and pulmonary VasoD 3. Increase sys and dias ...no change in PP |
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What are the adverse effects of NE?
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1. Similar to E but less
2. Necrosis at site of injection |
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What are the therapuetic uses of NE?
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1. Hypotension and VasoD for shock from spinal trauma!
2. Local anesthetics to retard absorption |
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What is the MOA of DA?(3)
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1. @ low D1 receptors
2. increase that and you hit B1 also with NE release 3. @ high you get alpha 1 and D2 also |
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What are the pharm effects of DA?(3)
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1. Low for renal(D1)
2. Intermediate to add inotropic effect(B1) 3. High to increase HR and cause vomitting |
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Where does DA not go and how should u administer it?
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1. Doesn't enter the brain
2. Only IV infusion |
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What are the therapeutic uses of DA?
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1. Cardio, nuero and septic shock when the Renal Beds are involved
2. RENAL |
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What are the effects of the alpha 1 agonists?(3)
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1. Phenylephrine
2. Increase BP 3. Not inactivated by COMT so the stay around longer |
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What are the therapeutic uses for alpha 1 agonists?(4)
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1.Orthostatic hypotension
2. Degongestants 3. Mydriatics 4. Local vasoconstrictors for epistaxis(nose bleed) |
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What are the alpha 2 and imidazoline selective drugs and their uses?
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1. Clonidine for hypertension
2. Apraclonidine for glaucoma |
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What are the Alpha 2 selective agonists?
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1. Tizanidine for the spinal cord
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Where in the brain are the alpha 2 receptors?
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1. In the rostral ventrolateral medulla(decrease CNS) and tractus solitarius
2. Decrease of the RetST firing |
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What are the effects of alpha 2 agonists on the CV(2)? CNS(3)?
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1. Hypotension from Decrease sympathetic
2. Hypertension only at high doses 3. Decrease cravings 4. Sedative 5. Analgesic |
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Where is clonidine(A2) absorbed? Biotransformation? Half life?
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1. In the mouth very well
2. 50% biotransformation in liver 3. Half life 12 hours |
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What are the adverse effects of clonidine?(3)
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1. Drowsiness
2. Hypertensive crisis when withdrawn 3. Xerostomia |
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What are the therapeutic uses of A2 agonists(4)
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1. Hypertension(2nd choice)
2. Glaucoma Open 3. Spinal cord spasticity(tizanidine) 4. Neuropsychiatric disorders(clonidine 5. Withdrawal |
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Isopreteranol is a nonselective Beta agonist and does what in the CV?(4)
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1. All Beta's
2. Increases HR 3. VasoD with Beta2 4. MAP decreases because diastole falls |
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Why use isopreteranol over E? When?(3)
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1. No alpha 2 mediated inhibition of insulin so no hyperglycemia
2. Emergency situations when inotropy is low but resistance is high(surgery) 3. Ventricular tachycardia(torsade de pointes) ... Will get cardiac rythm back to normal! 4. Beta blocker OD 5. Bronchospasm or Asthma |
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When do you use the Beta 1 agonist dobutamine?
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1. Increase contractility and conduction with HR
2. No change in vessels 3. Not orally 4. People in cardiac failure with depressed LV function |
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What are the effects of Beta 2 agonists?(lungs, immune, vessels)
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1. Bronchodialtion and mucociliary clearance
2. Reduce inflammation 3. Reduce microvascular permeability |
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What is a problem with the beta agonists?
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1. Tolerance due to Beta receptor down regulation
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How to administer Beta 2 agonists?
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1. Oral ok but mainly Inhalation
2. Distribution in peripheral tissue |
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What are the short acting beta 2 agonists?
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1. E
2. isoproterenol |
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What are the intermediate acting beta 2 agonists?(2)
Breathe them in |
1. Albuterol
2. Tertbutaline |
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What are the long acting beta 2 agonists?
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1. Salmeterol
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What are the adverse effects of the beta 2 agonists? CNS, CV, respiratory and other?
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1. Tremor, convulsions, restlessness
2. Tachycardia and arrythmia 3. Hypoxemia, pulmonary edema, paradoxical bronchoconstriction(rxn to aerosols) 4. Hypokalemia |
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What are the therapeutic uses of Beta 2 agonists?
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1. Asthma
2. COPD 3. Premature labor |