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504 PHARM: SYMPATHOLYTIC DRUGS
504 PHARM: SYMPATHOLYTIC DRUGS
Propanolol is NON-selective for which receptor?
Beta adrenergic antagonist
Propanolol is used to treat what?
1. HTN
2. Heart disease
3. Angina
4. Cardiac arrhythmias
5. *Muscle tremors
Use of propanolol is contraindicated by?
Asthma since inhibition of Beta 2 in the lungs can cause bronchoconstriction.
Metoprolol is selective for what receptor?
Beta 1 adrenergic antagonists
What is metoprolol used to treat?
Same as propanolol:
1. HTN
2. Heart disease
3. angina
4. cardiac arryhthmias
Why is metoprolol preferred over propanolol?
Used by cardiac patients that are also asthmatic.
What are the side effects of Beta blockers?
1. fatigue and sleep disturbances
2. impaired athletic performance
3. weight gain
What's the reasoning behind fatigue and sleep disturbances from using beta blockers?
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.
What's the reasoning behind impaired athletic performance from using beta blockers?
Due to blockade of the increases in CO.
What's the reasoning behind weight gain from using beta blockers?
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.
Phentolamine is NON-selective for which receptor?
It's a non-selective alpha adrenergic receptor antagonist.
Phentolamine is used to treat what?
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
Mono-amine oxidase (MAO)
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.
Prazosin is selective for what receptor?
Alpha 1 adrenergic receptor.
What is prazosin used for?
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.
What are the side effects of prazosin?
1. postural hypotension
2. mild CNS effects, i.e. headaches, dizziness, nausea.
What receptor is Yohimbine selective for?
Selective for alpha 2 adrenergic receptor antagonist.
What is the use of yohimbine?
Sold in stores as herbs.
Yohimbine can be used to treat?
Sexual dysfunction via inhibiting alpha 2 receptors in CNS (opposite of clonidine).
Side effects of yohimbine?
1. HTN
2. Sleep disturbances
3. Can be dangerous when used with sympathomimetics (esp MAO inhibitors).
What does Reserpine bind to?
Binds to vesicular monoamine transporter (VMAT) and blocks it.

Thereby blocking vesicular packaging and release of catecholamines.
What type of drug is rserpine?
An indirectly acting sympatholytic drug.
What is reserpine used for?
1. HTN (but NO LONGER)

2. Current use is in treating Raynaud's Syndrome.

Note: can strongly induce depression and impaired cognition.
What is Raynaud's syndrome?
Painful vasoconstriction of blood vessels in distal limbs.
Print out slide 11 and 12
.
Symphatolytics
Drugs that inhibit the functioning of the sympathetic nervous system.

They can all be used as anti-hypertensives.