Pharmacology Test 1

How does reserpine work?

Reserpin inhibits VMAT the NE transporter that stores NE in storage granuales inside the nerve. When the nerve can't store NE the celluar concentration of NE becomes too high for it to reuptake much NE out of the synaptic cleft.

What adrenergic agonist is 50% beta, 50% alpha?

Epinephrine

Fill in the chart Location Receptor Agonist response Blood Vessels ___(1)____ constriction ____(2)____ dilation Cardiac Muscle _____(3)____ Increased Contractility AV Node _____(4)____ Increased HR SA Node _____(5)____ Increased HR GI Muscle _____(6)_____ Decreased motility Sphincters ______(7)_____ constriction Bladder sphincter ___(8)___ constriction Penis ____(9)____ ejaculation Uterus ____(10)___ contraction _____(11)____ relaxation Bronchial _____(12)____ dilation/relation

1. Alpha 1 2. Beta 2 3. Beta 1 4. Beta 1 5. Beta 1 6. Beta 2 7. Alpha 1 8.Alpha 1 9. Alpha 1 10. Alpha 1 11. Beta 2 12 Beta 2

______________ agents are drugs that stimulate the sympathetic nervous system aka ____ ____ and ________

Adrenergic adrenergic agonists and sympathomimetics

____________ and _____________ exhibit selectivity for alpha 1 receptors in the urinary track. They are not intended for use as antihypertensives.

Alfuzosin. Silodosin

How does cocaine work?

Cocaine inhibits the NE transporter protein that is part of the normal reuptake of NE back into the nerve cell, out of the synaptic cleft.

_____________ receptors will cause an increase in heart rate, dilation of the following blood vessels, resulting in a increased blood flow renal mesenteric coronary cerebral

Dopamine

__________________ causes maximum reduction in blood pressure 2-6 hours after dosing which is associated with a small increase in standing heart rate. It has a greater effect on blood pressure and heart rate in the standing position.

Doxazosin

Name the alpha 1 blockers that can treat hypertension (3)

Doxazosin, prazosin, and terazosin

__________________ , ________________, and ____________________ selectively block alpha 1 adrenergic receptors. This blockade causes a reduction in the systemic vascular resistance, thus causing an antihypertensive effect. The degree of smooth muscle tone in the prostate and bladder neck is mediated by alpha 1 adrenergic receptors, which is present in high density in the prostate stroma, prostatic capsule, and bladder neck. Blockade of alpha 1 adrenergic receptor decreases urethral resistance and may relieve the obstruction and improve urine flow and BPH symptoms.

Doxazosin, prazosin, and terazosin

All Beta adrenergic receptors are located on the post synaptic effector cells. Beta 1 receptors are located primarily in the ________ though while Beta 2 receptors are located in the smooth muscles of the ___________, arterioles, and visceral organs.

Heart Bronchioles

What adrenergic agonist is pure beta?

Isoproterenol

What sympathomimetics are pure alpha? 2

Methoxamine and norepinephrine

_____________ and ___________ are both beta blckers that are indicated in the treatment of hemodynamically stable patients with definite or suspected acute MI. treatment can be intiated as soon as the patient's clinical condition allows or 3-10 days of the acute event.

Metoprolol atenolol

The classic Agonist of the Alpha 2 receptor is ________ and the anatagonist ? What effect does stimulating the alpha 2 receptor have?

NE It doesn't have one This receptor exists in our body to tell our nerves that their is enough NE in the synaptic cleft, so stimulating will cause a decrease in NE release and therefore decrease in Blood pressure through that feedback mechanism.

Adrenergic receptors are located throughout the body. They are receptors for sympathetic NTs Alpha-adrenergic receptors respond to _____ Beta-adrenergic receptors respond to _____

NE NE

The classic Agonist of the alpha 1 receptor is _______ and the classic antagonist is ___________ What will stimulating the alpha 1 receptor do cause?

NE Phentolamine Vasoconstriction and an increase in BP

fill out the chart for these adrenergic agonists NE _____%Alpha ______ %Beta EPI ______% Alpha _______%Beta Isoproterenol ______%Alpha _____%Beta

NE 95% alpha 5% beta EPI 50% alpha 50% beta Isoproterenol 5% alpha 95% Beta

Adrenergic agents mimic the effects of the SNS neurotransmitters: ___________ and _______________

Norepinephrine (NE) Epinephrine (EPI)

Alpha 1 antagonist that is the primary treatment for Pheochromocytoma?

Phentolamine

What is the parent compound from which synpathomimetic drugs are derived?

Phenylethylamine

________________ , The alpha 1 blocker, lowers blood pressure in the supine and standing positions. This effect is more pronounced on the diastolic blood pressure. The antihypertensive action is not usually accompanied by a reflex tachycardia.

Prazosin

Beta blocker that can treat an essential tremor? such as from parkinson like syndrome from antipsychotic medications

Propanolol

What change of phenylethylamine produces epinephrine and isoproterenol?

Substitution on the amino group

What changes are made to Phenylethylamine to produce catecholamines? How does this affect the drug's potently and method of taking it?

Substitution on the benzene ring. Makes it much less potent, but now is not affected by COMT so can be taken orally

________________ selectively inhibits the alpha 1A adrenergic receptor. Approximately 70% of the alpha 1 adrenergic receptors in the human prostate are of the alpha 1A subtype. This drug is not intended for use as a hypertensive, only to treat BPH.

Tamsulosin

Name the alpha blockers that can treat BPH(5), note which can only treat BPH(3)

Terazosin, Doxazosin Alfuzosin, silodosin, and tamulosin - BPH only

Describe how NE is made, including enzyme names.

Tyrosine is converted into L-DOPA by Tyrosine hydroxylase. L-DOPA is converted into Dopamine by Aromatic L-amino acid decarboxylase. Dopamine is converted into NE by Dopamine B-hydroxylase

What 4 beta blockers are used to treat cardiac arrhythmia? which is specified for ventricular premature beats only? which is to only be used for documented life threatening ventricular arrhythmia like sustained ventricular tachycardia?

acebutolol esmolol propanolol sotalol acebutolol sotalol

Alpha Adrenergic receptors are divided into subsets alpha 1 and alpha 2 receptors. They are differentiated by their location on nerves. Alpha 1 receptors are located on the postsynaptic ___________ cells(the cell, muscle, or organ that the nerve stimulates) Alpha 2 receptors are located on the ___________ nerve terminals and work through a feedback mechanism.

effector presynaptic

What beta blocker is indicated for intraoperative and post operative tachycardia and hypertension?

esmolol

What beta blocker is indicated for sinus tachycardia?

esmolol

What beta blocker is indicated for supraventricular tachycardia?

esmolol

All beta adrenergic blocking agents, except __________ and ____________, are indicated for use for hypertension. They are not indicated for use for hypertensive emergencies.

esmolol sotalol

Stimulating B1 receptors will cause what? Stimulating B2 receptors will cause what?

increase in heart rate relaxation of smooth muscle, bronchodilation, vasodilation

What Beta blockers are indicated for the long term mangement of Angina pectoris? (4)

nadolol atenolol propanolol metoprolol

What beta blocker is indicated for ventricular tachycardias?

porpanolol

What Is a beta blocker used to treat pheochromocytoma in adjunct to alpha 1 blocker? a NE producing kidney tumor

propanolol

What beta blocker is indicated for supraventricular arrhythmias? Like paroxysmal atrial tachycardias, particularly those induced by catecholines, digitalis or associated with Wolff-Parkinson-White syndrome. Or persisent sinus tachy cardia that is noncompensatory and impairs the well being of the patient.

propanolol

What beta blocker is indicated for tachyarrhythmias caused by digitalis intoxication?

propanolol

2 beta blockers for prophylaxsis of migraines?

propanolol timolol

___________ and _____________ are beta blockers that are indicated in clinically stable patients who have survived the acute phase of an MI to reduce CV mortality and risk of reinfarction. initiate treatment 1-4 weeks after infarction.

propanolol timolol

What beta blocker is to treat resistant tachyarrhythmias caused by excessive cathecholamine action during anethesia?

propranolol

What beta blocker is indicated for the maintenance of normal sinus rhythm in patients with highly symptomatic atrial fibrillation/atrial flutter (AFIB/AFL) who are currently in sinus rhythm?

sotalol

__________________ decreases blood pressure gradually over 15 minutes following oral administration. Use in the treatment of Norma tens I've men with BPH did not result in a clinically significant blood pressure lowering effect.

terazosin