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Sympathomimetics
Pharmacology Test #2.2
| Question | Answer |
|---|---|
| These mimic peripheral effects of the sympathetic nervous system | Sympathomimetics |
| + inotropic= | increased muscular contraction |
| + chronotropic = | increased rate |
| What is a receptor? | the site of biological activity, pharmacologic activity |
| Stimulation of Alpha receptors usually results in what? | excitation |
| Stimulation of Beta 1 receptors results in? | myocardial excitation |
| Stimulation of Beta 2 leads to what? | depression of activity, bronchial and skeletal vasculature relaxation |
| Name the 5 Sympathomimetic drugs that are typical of all the others | epinephrine, norepinephrine, isopropylnorepinephrin(isuprel), ephedrine, amphetamine |
| Sympathomimetics and adrenomimetics are classified into what two groups? | Direct acting amines and indirect acting amines |
| How do direct acting amines work? | they combine directly with postganglionic adrenergic receptors to cause action |
| 3 examples of direct acting amines | Epinephrine, norepinephrine, Isuprel |
| How do indirect acting amines work? | cause most of their activity by releasing sympathetic transmitter from the postganglionic neurons |
| An example of an indirect acting amine is | Aramine |
| Exceptions to rules about Alpha and Beta receptors | Stimulation of Beta 1 receptors results in + HR and SV. Isuprel is an example- its effects are blocked by beta blocking/adrenolytic/sympatholytic agents |
| These receptors are classified as beta even though they are excitatory | cardiac |
| GI smooth muscle receptors contain both alpha and beta receptors but what occurs? | inhibition of tone |
| Ephinephrine(adrenaline) occurs at both _ and _ isomers. _ is 50 times as potent | "l" and "d"; "l" |
| Epinephrine is secreted by | the postganglionic sympathetic terminals and the adrenal medulla |
| Action of epinephrine | Stimulated both alpha(in large doses) and Beta (small doses) |
| Cardiac effects of Epinephrine | increased HR and SV (B1), Heart becomes more susceptible to arrythmias, results in increased systolic pressure |
| Vascular effects of Epinephrine | increases PVR. Constriction of blood vessels in skin, mucosa, spleen, and kidneys d/t alpha stimulation. Dilation of coronary and skeletal muscle vessels d/t Beta effects |
| What happens with the blood after administration of Epi? | it is redistributed to vital areas |
| Bronchial effects of Epi | Bronchial muscle relax(Beta), mucosa constrict (alpha). Raw decreases |
| Eye effects from Epi | pupils dilate d/t alpha receptors |
| GI effects of Epi | muscle tone decreased d/t alpha and beta stimulation. peristalsis reduced. Sphincters are constricted(alpha) |
| Glandular effects of Epi | Secretions decrease(alpha) |
| CNS effects from Epi | anxiety, restlessness and weakness |
| Clinical uses of Epi | acute episodes of Asthma, local anesthetic(vasoconstriction, increase induration), and Cardiac arrest |
| Preparations of Epi | 1-not effective by mouth, 2-1/1000 solution used for IV and SQ use, 3-1/100 solution for inhalation |
| Adverse effects of Epi | exaggerated therapeutic effects |
| Norepinephrine(Levarterenol, Levaphed):The _-isomer is usual sympathetic postganglionic transmitter | l |
| Action of NorEpi | substantial alpha effects, minimal beta effects (VERY IMPORTANT) |
| Cardiovascular effects of NorEpi | increased systolic and diastolic BP d/t increase in vascular resistance. The heart is not directly stimulated |
| Clinical uses for NorEpi | Shock- long used as a vasocontrictor to treat hypotension- action is on peripheral resistance |
| Preparation of NorEpi | 1/1000 solution IV |
| Adverse effects of NorEpi | cardiovascular injury. Local necrosis d/t extravasation of IV causing tissue vasoconstriction and skin necrosis |
| Isopropylnorepinephrine cardiovascular effects | +inotropic and chronotropic effects. vasodilator. |
| Isuprel ___ pulse presure and Systolic pressure | increases |
| Isuprel ____ Mean arterial pressure and diastolic pressure | decreases |
| What drug is the most potent heart stimulant | Isuprel |
| Bronchial effects of Isuprel | dilate bronchi(beta 2), does not constrict mucosa(alpha) |
| Uses of Isuprel | given SL or inhalation to athma patient, serves to stimulate myocardium with heart block until pacemaker placed |
| Preparation of Isuprel | 1/100 and 1/200 solutions inhaltion and IV |
| THis is a naturally occurring catecholamine and precursor to epinephrine that has its own receptors and acts as a mixed amine | Dopamine(Intropin) |
| Cardiovascular effects of dopamine | CO increases, Peripheral resistance decreases, mean arterial pressure and HR unaltered |
| These drugs act directly and indirectly, have a longer duration of action, orally active, and people exhibit tachyphylaxis d/t them | Ephedrine and amphetamine |
| Cardiovascular effects of Ephedrine | slow onset, prolonged action, increase CO and PVR leading to htn |
| Bronchial effects of ephedrine | dilates bronchi, slow, lasts longer |
| Eye effects of ephedrine | dialtes pupils |
| CNS effects of ephedrine | stimulates causing insomnia, restlessness |
| Uses of ephedrine | allergic d/o, asthma, nasal congestions(clears up but may cause rebound congestion and mucosal burning), and for heart block(not usual drug of choice) |
| These are powerful central stimulants, often abused | amphetamines(Benzadrine) |
| Action and use of Amphetamine | Peripheral Nervous system, CNS, Barbituate poisoning, Obesity |
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