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27 Cards in this Set
- Front
- Back
504 PHARM: SYMPATHOLYTIC DRUGS
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504 PHARM: SYMPATHOLYTIC DRUGS
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Propanolol is NON-selective for which receptor?
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Beta adrenergic antagonist
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Propanolol is used to treat what?
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1. HTN
2. Heart disease 3. Angina 4. Cardiac arrhythmias 5. *Muscle tremors |
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Use of propanolol is contraindicated by?
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Asthma since inhibition of Beta 2 in the lungs can cause bronchoconstriction.
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Metoprolol is selective for what receptor?
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Beta 1 adrenergic antagonists
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What is metoprolol used to treat?
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Same as propanolol:
1. HTN 2. Heart disease 3. angina 4. cardiac arryhthmias |
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Why is metoprolol preferred over propanolol?
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Used by cardiac patients that are also asthmatic.
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What are the side effects of Beta blockers?
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1. fatigue and sleep disturbances
2. impaired athletic performance 3. weight gain |
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What's the reasoning behind fatigue and sleep disturbances from using beta blockers?
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Due to the action on Beta receptors in the brain.
Can be alleviated by switching to a beta blocker that does not cross the blood brain barrier. |
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What's the reasoning behind impaired athletic performance from using beta blockers?
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Due to blockade of the increases in CO.
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What's the reasoning behind weight gain from using beta blockers?
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Due to action on Beta receptors in adipose tissue.
Note: Beta 3 receptor is found almost exclusively in adipose tissue where it gets activated to stimulate lipolysis. |
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Phentolamine is NON-selective for which receptor?
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It's a non-selective alpha adrenergic receptor antagonist.
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Phentolamine is used to treat what?
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1. Pheochromocytoma which is a tumor of the adrenal medulla that causes massive release of Epi that leads to over-stimulation of sympathetic.
2. HTN |
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Mono-amine oxidase (MAO)
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Serotonin, melatonin, norepinephrine, and epinephrine are mainly broken down by MAO-A.
Therefore, MAO inhibitor (MAOI) can lead to hyptensive crisis due to excess epinephrine. |
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Prazosin is selective for what receptor?
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Alpha 1 adrenergic receptor.
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What is prazosin used for?
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1. To treat HTN via blockade of alpha 1 receptor activation in vascular smooth muscle. Relieves alpha 1 mediated vasoconstriction.
2. Benign prostatic hyperplasia (BPH). The prostate is rich in alpha 1 receptors which when over-activated would accelerates cell growth. |
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What are the side effects of prazosin?
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1. postural hypotension
2. mild CNS effects, i.e. headaches, dizziness, nausea. |
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What receptor is Yohimbine selective for?
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Selective for alpha 2 adrenergic receptor antagonist.
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What is the use of yohimbine?
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Sold in stores as herbs.
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Yohimbine can be used to treat?
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Sexual dysfunction via inhibiting alpha 2 receptors in CNS (opposite of clonidine).
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Side effects of yohimbine?
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1. HTN
2. Sleep disturbances 3. Can be dangerous when used with sympathomimetics (esp MAO inhibitors). |
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What does Reserpine bind to?
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Binds to vesicular monoamine transporter (VMAT) and blocks it.
Thereby blocking vesicular packaging and release of catecholamines. |
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What type of drug is rserpine?
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An indirectly acting sympatholytic drug.
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What is reserpine used for?
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1. HTN (but NO LONGER)
2. Current use is in treating Raynaud's Syndrome. Note: can strongly induce depression and impaired cognition. |
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What is Raynaud's syndrome?
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Painful vasoconstriction of blood vessels in distal limbs.
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Print out slide 11 and 12
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.
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Symphatolytics
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Drugs that inhibit the functioning of the sympathetic nervous system.
They can all be used as anti-hypertensives. |