Term
| Sympathetic agonists are also called ____ or ___ ___. |
|
Definition
- sympathomimetics
- adrenergic agonists |
|
|
Term
| various classifications of adrenergic agonists: |
|
Definition
- catecholamine vs. non-catecholamine
- direct vs. indirect acting
- re-uptake inhibitors |
|
|
Term
| you cannot take catecholamines orally. |
|
Definition
|
|
Term
| Non-catecholamine adrenergic agonists are ___ lasting and __ be taken by mouth. |
|
Definition
|
|
Term
| non-catecholamine alpha agonist: |
|
Definition
|
|
Term
|
Definition
- Albuterol
- Ritodrine
- Terbutaline
beta 2 agonists = art |
|
|
Term
| Indirect acting sympathomimetics: |
|
Definition
|
|
Term
| mixed acting sympathomimetics: |
|
Definition
- ephedrine
- pseudoephedrine |
|
|
Term
| Topical vasoconstrictors: |
|
Definition
- Naphazoline
- Oxymetazoline
- Tetrahydrozaline
topical vasoconstrictors= NOT
these are your nasal sprays |
|
|
Term
|
Definition
|
|
Term
| epinephrine stimulates ___ alpha and beta receptors. |
|
Definition
|
|
Term
| Isoproterenol acts like a catecholamine is an agonist for __ _, _, and _ receptors. |
|
Definition
|
|
Term
| Dopamine acts on what receptors: |
|
Definition
|
|
Term
| Dobutamine acts like a catecholamine and is only an agonist for the ___ ___ receptors. |
|
Definition
|
|
Term
| amphetamines and tyramine can cause ___ release. |
|
Definition
|
|
Term
| the prototypic catecholamine is : |
|
Definition
|
|
Term
| the prototypic noncatecholamine agonist is: |
|
Definition
|
|
Term
| prototypic beta 2 agonist is : |
|
Definition
|
|
Term
| Prototypic indirect acting agonist: |
|
Definition
|
|
Term
|
Definition
|
|
Term
| Oxymetazoline reuptake inhibitor: |
|
Definition
|
|
Term
| a direct mode of action means it acts on a ___. |
|
Definition
|
|
Term
| An indirect mode of action means that it causes the release of ___ from nerve terminals. |
|
Definition
|
|
Term
| Mixed action drugs have both ___ and ___ effects. |
|
Definition
|
|
Term
| Alpha adrenergic effects: |
|
Definition
1. constriction of blood vessels via alpha 1 (to lesser extend alpha 2)
2. mydriasis via alpha 1
3. contraction of the spleen via alpha 1
4. contraction of the uterus via alpha1
5. inhibited release of insulin via alpha2
6.constriction of bladder sphincter alpha 1
7. Increased glycogenolysis in liver beta2
8. ejaculation, vas deferens alpha 1
9. relaxation of intestinal smooth muscle alpha 2 |
|
|
Term
|
Definition
1. Heart: positive ionotropic and chronotropic effects beta 1
2. relaxation of bronchioles beta2
3. relaxation of uterus beta 2
4. relaxation of skeletal muscle arterioles beta 2
5. increased liver glycogenolysis, beta2
6. increased adipose tissue lipolysis beta3
7.increased releasae of insulin beta2
8.stimulate release of renin beta1 |
|
|
Term
|
Definition
- epinephrine
- norepinephrine
- dopamine
- dobutamine
- isoproterenol |
|
|
Term
| Epinephrine is more potent for __ than __ receptors. But clinically, when given at therapeutic doses we see ___ are affected. The concept of __ __ requires knowledge of which receptor response will prevail. |
|
Definition
- beta than alpha
- both
- net effect |
|
|
Term
| epinephrine effects on the heart: |
|
Definition
Via beta 1 receptors:
- positive inotropic effect (contractility)
- positive chronotropic effect (rate)
- increased automaticity (sa node depolarizes more quickly): latent pacemakers become active= increased ectropic beats, arrhythmias may result b/c refractory period is reduced after an ap
- increased conduction rate in the AV node |
|
|
Term
| ultimately epinephrine causes the ___ __ to __ and the __ of ___ to increase, so ___ ___ is ___. Thus ___ consumption ____. |
|
Definition
- heart rate to increase
- force of contraction to increase
- cardiac output is increased
- oxygen consumption is increased |
|
|
Term
| On skeletal muscle arterioles there are ___ _ and ___ __ receptors. At physiological quantities of epinephrine, the ___ receptors are acted on and we see ____. At pharmacologic doses ___ receptors are acted on and we see ____. |
|
Definition
- beta 2 and alpha 1
- physiological> beta 2> vasodilation
- pharmacological> alpha 1> vasoconstriction |
|
|
Term
| Veins have only __ _ receptors so they can only ____ in response to increased sympathetic stimulation. |
|
Definition
- only alpha 1
- constrict |
|
|
Term
| coronary blood vessels ___ in response to epinephrine b/c of ___ _ receptors. |
|
Definition
|
|
Term
| Kidney, skin, and mucosal blood vessels ___ in response to epineprhine b/c of ___ _ receptors. |
|
Definition
|
|
Term
| cerebral blood vessels remain unchanged in presence of epinephrine |
|
Definition
|
|
Term
| Net effect of epinephrine on blood pressure and cardiac function depends on: |
|
Definition
- dose
- circulatory status
- compensatory reflexes- baroreceptors are stretch receptors in carotid sinus and aortic arches that sense blood pressure changes and maintain homeostasis |
|
|
Term
| When baroreceptors sense a change in bp, signals are transmitted to the ___ center in the __ ___to alter parasympathetic and sympathetic outflow to the heart and blood vessels. |
|
Definition
|
|
Term
| If baroreceptors sense a sudden increase in bp, sympathetic tone will be ___ and ___ tone to the ___ node will be ___. |
|
Definition
- sympathetic tone will decrease
- vagal tone to SA node will increase |
|
|
Term
| If baroreceptors sense a sudden drop in bp, symp tone will ___ and parasymp tone will ___. |
|
Definition
|
|
Term
| metabolic effects of epinephrine: |
|
Definition
- calorigenic and tremor effects in skeletal muscle via beta 2
- increased glycogenolysis (beta 2)
- increased lipolysis (beta 3) |
|
|
Term
| Clinical uses of epinephrine: |
|
Definition
1. Bronchial asthma
2. Anaphylactic shock
3. Infiltration with local anesthetics
4. Cardiac resuscitation
5. Topical for hemostasis |
|
|
Term
| how does epinephrine treat bronchial asthma: |
|
Definition
| . Administered by inhalation. Bronchodilation (2) and inhibition of antigen-induced histamine release. |
|
|
Term
| How does epinephrine treat anaphylactic shock? |
|
Definition
| (give IV or SC) Improves breathing by same mechanisms as in 1 above, plus increases blood pressure and reverses edema (1). |
|
|
Term
| epinephrine reverses edema by __ _ receptors |
|
Definition
|
|
Term
| Anaphylaxis is an ___ phenomenon. Three things occur all related to the dump of histamine. list these 3 things. |
|
Definition
1. Bronchoconstriction
2. profound vasodilation so bp drops
3. edema
Epinephrine (epi pen) is ideal treatment for this. Epinephrine is a physiolgical antagonist b/c it diates brochioles (beta 2 effect), raises bp (alpha 1 affect), and edema comes out of venules so epinephrine stops any additional edema from forming and allows present edema to be rid by lymphatics. |
|
|
Term
Lidacane anesthetic injected with epinephrine at dentist, without the epinephrine the lidacaine could be deathly.
Epinephrine constricts the vessels and keeps the lidacaine in the specific area. Epinephrine acts on alpha 1 and beta 2 receptors, but alpha overrides the beta, so as concentration drops beta takes over. So initial constriction with alpha but then after get dilation with beta 2 receptors. |
|
Definition
|
|
Term
| Adverse effects of epinephrine: |
|
Definition
1. arrhythmias (beta 1 effects)
2. cerebral hemorrhage (alpha 1 effects)
3. necrosis distal to site of injection
4. CNS effects: anxiety, headache |
|
|
Term
| Contraindications for epinephrine: |
|
Definition
1. Hypertension
2. Shock
3. Hyperthyroidism
4. Angina pectoris
5. Degenerative heart disease
don't have to memorize these, its just used in emergency situations |
|
|
Term
| Contraindications for epinephrine: |
|
Definition
1. Hypertension
2. Shock
3. Hyperthyroidism
4. Angina pectoris
5. Degenerative heart disease
don't have to memorize these, its just used in emergency situations |
|
|
Term
| Norepinephrine or ____ is selective for __ _, __ _, and __ _ receptors. What are its pharmacological effects? |
|
Definition
- Levophed
- alpha 1
- alpha 2
- beta 1
pharmocologic effects:
1. Heart beta 1 direct effects (iontropic and choriontropic effects)
2. Vasculature: alpha 1 > vasoconstriction which activates the baroreceptors |
|
|
Term
| NE has no beta 2 affects so not used for anaphylactic shock. NE is much shorter acting than epinephrine, so not used to control blood pressure. |
|
Definition
|
|
Term
|
Definition
| - positive inotropic effects but reflex bradycardia with increased systolic and diastolic blood pressures |
|
|
Term
E widens the pulse pressure because it stimulates 2 receptor on arterioles, causing vasodilation
Because E at this dose does not raise mean blood pressure, no vagal reflexes are activated
Contrast these effects of those of NE, which essentially has no stimulant 2 effect |
|
Definition
|
|
Term
| with a low dose of epinephrine you would see the diastolic pressure ___ b/c of __ __ receptors causing ___ ___. You would see the systolic pressure would be ___ b/c of the increased contractility and ejection fraction via ___ _ recptor effects. Thus with epinephrine you see a ___ pulse pressure but has __ effect on mean blood pressure. |
|
Definition
- decreasing
- beta 2
- arteriole dilation
- increasing
- beta 1
- widened pulse pressure
- no change in mean arterial pressure |
|
|
Term
| Isoproterenol has pure ___ effects so it would ___ diastolic pressure even more than epi did, and it would increase contractility even more than epi did so systolic is more increased. So ultimately mean bp ___ a little bit and ___ __ is increased. |
|
Definition
- beta
- decrease
- decrease
- heart rate |
|
|
Term
| w/o parasympathetic input the heart rate would be around: |
|
Definition
|
|
Term
| NE increases pulse pressure via the ___ _ receptor b/c diastolic did not decrease b/c NE does not have ___ action, so you see ___ _ effect of ___. This increased bp is sensed by the barorecptors which in turn causes heart rate to ____. So NE is telling the heart to beat faster but the vagus is telling it so slow down, and when they both are having input, we know the ___ is more powerful. |
|
Definition
alpha 1
beta 2
alpha 1 effect of vasoconstriction
decrease
parasympathetics |
|
|
Term
| inject NE hos is pulse rate, blood pressure, and peripheral resistance affected? |
|
Definition
- peripheral resistance increases
- blood pressure increases
- pulse rate decreases |
|
|
Term
| inject epi, how is peripheral resistance, blood pressure, and heart rate affected? |
|
Definition
- peripheral resistance decreases (at low doses)
- blood pressure stays same
- heart rate increases |
|
|
Term
| inject isoproterenol how is peripherial resistance, blood pressure, and heart rate affected? |
|
Definition
- peripheral resistance decreases
- blood pressure decreases a little
- heart rate increases |
|
|
Term
| LOW DOSES OF EPINEPHRINE> FILL BETA 2 RECEPTORS (DECREASED BP), HIGH DOSES FILL ALPHA RECEPTORS (INCREASED BP) |
|
Definition
|
|
Term
|
Definition
1 and 2 stimulant. (no alpha effects).
Pharmacological effects:
1. Heart: Positive inotropic and chronotropic effect.
2. Vasculature: Vasodilatation of skeletal muscle arterioles (2 receptors on arterioles). |
|
|
Term
| Isoproterenol: Clinical Uses |
|
Definition
Relatively limited because of intense cardiac effects.
1. Bronchial asthma (Aerosol)
2. Heart block. (give by IV. catheter.)
Side effects
Common: tachycardia, flushing, headache, rapid pounding heart.
Serious: arrhythmias, angina |
|
|
Term
| notice that isoproterenol, a pure beta1/beta2 agonist, has a greater ____ effect than E. This is because E is both a beta2 agonist and also an alpha 1 agonist. For E, The alpha 1 effects partly offset the beta2 effects at this dose. Indeed, if the dose of E is raised, only alpha1 agonist effects will be seen because E has more efficacy at alpha1 than beta2 receptors. |
|
Definition
|
|
Term
| Epi is more potent for __ _ receptors but more efficacious at __ _ receptors. |
|
Definition
- more potent at beta 2s
- more efficacious at alpha 1s |
|
|
Term
| Dopamine aka ___ is an agonist at __ receptors and cause ___ in the kidneys. This is also a ___ _ agonist which leads to ___ ___ __. It is also an __ _ agonist which can lead to ___ (less potent here than others though). |
|
Definition
- Intropin
- D1
- vasodilation
- beta 1
- increased cardiac output
- alpha 1
- vasoconstriction |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| dopamine is a precursor to ___ in all ___ neurons. |
|
Definition
norepinephrine
norepinephrine |
|
|
Term
| Shock basically means you have inadequate ___ __, the cardinal sign of shock is ___ ___ __. |
|
Definition
inadequate cardiac output
low blood pressure |
|
|
Term
| If we lose a lot of blood, flow to many organs will stop except for these three: |
|
Definition
- heart
- brain
- kidney
of these 3, the kidneys give up blood flow first |
|
|
Term
| With shock, the sympathetic is so activated that blood is not getting to the kidneys. |
|
Definition
|
|
Term
|
Definition
- shock, especially hypovolemic shock
- beta 1 effects benefit cardiac output
- alpha 1 effects increase blood pressure
- D1 effects vasodilate the kidney arterioles, leading to better maintenance of blood flow |
|
|
Term
| Duration of catecholamines is not very long, it has to be given via IV infusion or it will me metabolized very quickly. |
|
Definition
|
|
Term
| Direct acting non-catecholamines are ___ ___, lacking the ___ moeity. They are analogues for NE and Epi. |
|
Definition
|
|
Term
| Non-catecholamines are longer acting and are metabolized more slowly, why? |
|
Definition
- they are not acted upon as readily by MAO as catecholamines are
- they are not stored in vesicles |
|
|
Term
| some direct acting non-catecholamines are effective p.o. |
|
Definition
|
|
Term
| An alpha adrenergic agonist is ___ aka _____. It acts on the __ _ receptors and causes ___ and __ ___ __. But you can expect ___ ___. |
|
Definition
- Phenylephrine aka Neosynephrine
- alpha 1
- vasconstriction
- increased blood pressure
- reflex bradycardia |
|
|
Term
| ___ is used in decongestant cold meds orally and topically. |
|
Definition
| Phenylephrine aka Neosynephrine |
|
|
Term
|
Definition
1. Nasal decongestant
2. Infiltration with local anesthetics (more likely is the use of metaraminol).
3. Pressor agent to maintain bp
4. Ocular examination. Mydriasis without affecting accommodation. |
|
|
Term
| Beta-2 Selective Adrenergic Agonists are __ to __ times more potent at beta 2 than at beta 1, thus they are more selective for ___ muscle over __ muscle. This is longer acting than ____. Tolerance may develop. |
|
Definition
- 5 to 10 so its affinity is 100 times greater
- smooth over cardiac
- longer acting than catecholamines |
|
|
Term
| primary use of beta 2 selective antagonists: |
|
Definition
| obstructive lung disease: asthma and COPD |
|
|
Term
| Tolerance develops with beta 2 selective agonists b/c the beta receptor is a __ __ coupled receptor. When these are over activated, they ___ which is a form of ___ ___. this is a problem when asthmatics overuse their inhalers. |
|
Definition
- g-coupled
- internalize
- down regulate |
|
|
Term
| Tolerance develops with beta 2 selective agonists b/c the beta receptor is a __ __ coupled receptor. When these are over activated, they ___ which is a form of ___ ___. this is a problem when asthmatics overuse their inhalers. |
|
Definition
- g-coupled
- internalize
- down regulate |
|
|
Term
| Beta 2 adrenergic agonists used to treat bronchial asthma: |
|
Definition
1. Albuterol (Proventil); Levo-albuterol (Xopinex)
2. Metaproterenol (Metaprel, Alupent)
3. Terbutaline(Brethine)
(aerosol and sc; sc for emergency tx of astma; only 2 agent available sc )
iv.and p.o. to delay delivery.
4. Isoetherine (Bronkosol)
5. Salmeterol (Serevent). Once a day agent for chronic but not acute treatment of asthma. Has slow onset of action
A Manly Tone Is Sexy. |
|
|
Term
| Salmeterol lasts longer and was used for quite some time, but last spring it was in advair inhalers (beta 2 long acting affects and the other was topical corticosteroid to slow down inflammation) but FDA said not good for kids>unexpeced cardiac effects (beta 1 effects). |
|
Definition
|
|
Term
| beta 2 agonists used to treat bronchial asthma: |
|
Definition
A Manly Tale Is Sexy.
Albuterol
Metaproterenol
Terbutaline
Isotherine
Salmeterol |
|
|
Term
| Albuterol beta 2 agonist should be in __ form for acute treatment and ___ for chronic treatment of bronchial asthma. |
|
Definition
|
|
Term
| side effects caused by the oral route of albuterol: |
|
Definition
| hypotension (beta 2) , muscle tremors (beta 2), tachycardia (beta 1), hypokalemia. Effects on blood glucose are variable. |
|
|
Term
| Ritodrine is a ___ __ __ agonist used to ___ ___. |
|
Definition
alpha 2 adrenergic agonist
delay labor |
|
|
Term
| beta 2 adrenergic agonist side effects: |
|
Definition
| - skeletal muscle tremors b/c beta 2 receptors on muscle increase energy productin |
|
|
Term
| Indirect Acting Sympathomimetics: |
|
Definition
Tyramine
Amphetamine
many others |
|
|
Term
| Tyramine has the potential to cause a hypertensive crisis in pts on ___ inhibitors. |
|
Definition
|
|
Term
| Tyramine is found in many foods (red wine, aged cheeses, peanuts). It normally has huge first pass effect by ___ by the gut and liver that it never enters circulation. But if person on ___, then can cause ___ __. |
|
Definition
- monoamine oxidase
- MAOI
- hypertensive crisis |
|
|
Term
| tyramine is a ___ __. if it gets into nerve terminals it causes release of ___ . |
|
Definition
decarboxylated tyrosine
norepinephrine |
|
|
Term
|
Definition
Naturally occurring in genus Ephedra
There are four isomers; two of these, ephedrine and psuedoephedrine are clinically effective.
Mechanism: indirect (releases NE).
Relatively insensitive to degradation by MAO and COMT. Effective p.o. |
|
|
Term
| pseudoephedrine used to be used orally as decongestant but much less now. |
|
Definition
|
|
Term
| clincial uses of pseudoephedrine: |
|
Definition
nasal & eustachian tube decongestant
Releases NE – decongestant because of reduced pooling of blood in the venous circulation
Orally active
Does not penetrate CNS significantly – much less dependence potential than ephedrine. Nonetheless, access is now greatly restricted (easy to synthesize methamphetamine from this starting chemical). |
|
|
Term
| pseudoephedrine works as a nasal decongestant b/c it causes release of ___ which reduces ____ ___ in __ circulation. |
|
Definition
- NE
- reduces blood pooling
- venous |
|
|
Term
| pseudephedrine not used much now, b/c easy to make meth from it. |
|
Definition
|
|
Term
| common OTC products with direct and indirect alpha 1 effects: |
|
Definition
Naphazoline (Privine)
Tetrahyrolazine (Tyzine, Visine)- reduces eye redness
Xylometrazoline (Otrivin)
Oxymetazoline(Afrin) |
|
|
