Alpha Blockers

Drug Mechanism Physiological Effects Therapeutic Uses Side Effects

Prazosin - reversible
- selectively blocks 1 receptors
- decreases blood pressure by blocking 1
- decreased BP triggers baroreceptors
- baroreceptor reflex increases heart rate
- hypertension
- benign prostate hypertrophy
- reflex tachycardia
- postural hypotension
- nasal stuffiness
- inhibition of ejaculation
Phenoxybenzamine - irreversible
- selectively blocks 1 receptors
- binds to 1 via covalent bonds
- blocks 1 receptors for 24 hours
- decreases blood pressure by blocking 1
- decreased BP triggers baroreceptors
- baroreceptor reflex increases HR
- body must synthesize new 1 receptors to recover

- pheochromocytoma
- benign prostate hypertrophy
- reflex tachycardia
- postural hypotension
- nasal stuffiness
- inhibition of ejaculation
Phentolamine - reversible
- non-selective
- blocks 1 and 2 receptors
- decreases blood pressure by blocking 1
- prevents NE feedback inhibition by blocking 2
- 2 can no longer sense high NE in synapse
- increased NE release stimulates 1 receptors
- 1 receptors significantly increase heart rate
- pheochromocytoma - SEVERE reflex tachycardia
- tachy worse w/ non-selective
- postural hypotension
- nasal stuffiness
- inhibition of ejaculation

Alpha blockers are used to treat benign prostate hypertrophy because blocking 1 receptors relaxes the smooth muscle of the bladder to improve urine flow
Pheochromocytoma is a tumor on the adrenal gland that releases norepinephrine and epinephrine; you want to block alpha and beta receptors before
surgical removal because when you manipulate the tumor it will release norepinephrine/epinephrine and could cause hypertensive crisis
EPINEPHRINE REVERSAL is a phenomenon that occurs when both epinephrine and alpha blockers are given to a patient at the same time
o Usually epinephrine decreases blood pressure via activation of 2 receptors and then increases blood pressure via activation of 1 receptors; once
the 1 receptors become activated they win out over the 2 receptors and blood pressure goes up
o If the patient is taking alpha blockers then the epinephrine will not bind to 1 receptors but it will still be able to bind to 2 receptors; the result will
be a decrease in blood pressure with no subsequent increase
In the absence of alpha blockers, epinephrine increases blood pressure and this is known as a pressor response
In the presence of alpha blockers, epinephrine decreases blood pressure and this is know as a depressor response


Beta Blockers


Non-selective beta blockers decrease blood pressure by three mechanisms:
1. Reduced cardiac output cardiac output is reduced because blockage of 1 receptors decreases HR and contractility
2. Reduced renin concentration in the blood renin in the blood is reduced because of blockage of 1 receptors on the JGA of the kidney; this
prevents the renin-angiotensin system from increasing blood pressure
3. Decreased sympathetic tone from the CNS there are 2 receptors in the brain that control sympathetic outflow; when you block these receptors
there is a decrease in sympathetic outflow
Even the most selective beta blockers only have 100 fold selectivity for 1 receptors over 2 receptors; some 2 receptors will always get activated
Drug Mechanism Physiological Effects Therapeutic Uses Side Effects
Propranolol - nonselective beta blocker
- blocks 1 and 2 receptors
- decreased heart rate and C.O. due to 1 blockage
- decreased blood pressure due to the following reasons:
1. reduced cardiac output
2. reduced renin concentration in blood
3. reduced sympathetic tone from CNS
- increased airway resistance due to 2 blockage
- hypertension
- cardiac arrhythmias
- angina
- migraine prophylaxis
- reduce sympathetic tone in MI
- pheochromocytoma
- performance anxiety
- bradycardia
- heart block
- bronchoconstriction
- depression/lethargy
Timolol - nonselective beta blocker
- blocks 1 and 2 receptors
- decreased heart rate and C.O. due to 1 blockage
- decreased blood pressure due to the following reasons:
1. reduced cardiac output
2. reduced renin concentration in blood
3. reduced sympathetic tone from CNS
- decreased aqueous humor production via 1 blockage
- increased airway resistance due to 2 blockage

- glaucoma treatment
- hypertension
- cardiac arrhythmias
- angina
- migraine prophylaxis
- reduce sympathetic tone in MI
- pheochromocytoma
- performance anxiety
- bradycardia
- heart block
- bronchoconstriction
- depression/lethargy
Atenolol - selective beta blocker
- blocks mostly 1 receptors
- there is always some 2 blockage
- decreased heart rate and C.O. due to 1 blockage
- decreased blood pressure
- less 2 blockage but still some increase in airway resistance
- hypertension
- cardiac arrhythmias
- angina
- migraine prophylaxis
- reduce sympathetic tone in MI
- pheochromocytoma
- performance anxiety
- bradycardia
- heart block
- bronchoconstriction (less)
- depression/lethargy
Esmolol - selective beta blocker
- blocks mostly 1 receptors
- there is always some 2 blockage
- half life is only 8 minutes
- decreased heart rate and C.O. due to 1 blockage
- decreased blood pressure
- less 2 blockage but still some increase in airway resistance
- emergency procedures - bradycardia
- heart block
- bronchoconstriction (less)
- depression/lethargy
2 Agonists that Act as Anti-adrenergics

Drug Mechanism Physiological Effects Therapeutic Uses Side effects
Clonidine - binds to 2 receptors in the CNS to decrease sympathetic outflow
- binds to 2 receptors on post-ganglionic sympathetic neurons to
decrease peripheral NE release
- reduce sympathetic outflow from CNS
- decrease peripheral NE release
- essential hypertension
- opioid withdrawal
- ADHD
- glaucoma
- dry mouth
- sedation
Methyl-dopa - first must be metabolized into alpha-methyl-norepinephrine
-binds to 2 receprots in the CNS to decrease sympathetic outflow
- binds to 2 receptors on post-ganglionic sympathetic neurons to
decrease peripheral NE release
- reduce sympathetic outflow from CNS
- decrease peripheral NE release
- essential hypertension
- SAFE IN PREGNANCY
- dry mouth
- sedation
- autoimmune response
- POSITIVE COOMBS TEST

2 receptors in the CNS are located on both the pre and post-synaptic neurons; binding to 2 receptors on either location decreases sympathetic outflow
2 receptors on post-ganglionic sympathetic neurons sense the amount of NE in the synapse and are important in negative NE feedback; when clonidine or
alpha-methyl-NE bind to these receptors it makes the neuron THINK there is a lot of NE in the synapse and the result is that the neuron releases less NE