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Sympatholytic MOA (2)
- Bind to adrenergic receptors and prevent action
- Act indirectly by inhibiting synethesis, release or reuptake of norepi
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Alpha blocker types (2)
- Alpha 1 selective (the azosins)
- Alpha 1 and 2 non-selective (phentolamine, phenoxybenzamine)
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Blockade of alpha 1 effects (2)
- Inhibits vasoconstriction induced by endogenous catecholamines
- Vasodilation reduces BP, causes reflex tachycardia
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Blockade of alpha 2 receptors effects (1)
increased NE release and stimulation of B1 receptors
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Alpha one blocker major adverse effects (5)
- orthostatic hypotension (faint after standing)
- Reflex tachycardia
- Nasal congestion due to dilation
- Inhibition of ejaculation
- Miosis (opposite of mydriasis)
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Alpha 2 blocker major adverse events (1)
Intensification of reflex tachycardia due to decrease in BP (can trigger arrythmias and angina)
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If you block alpha 2 on presynaptic sympathetic neuron?
- INCREASED NE release
- Opposite if you stimulate alpha 2
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Phenoxybenzamine (non-selective alpha blocker) indication
Hypertenssive crisis due to pheochrmocytoma
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Phenoxybenzamine ADR (15
- Severe postural hypotension
- Tachycardia
- FLushing
- Nasal congestion
- Sexual disfunction
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Phentolamine (non-selective A blocker) indications (4)
- Hypertensive crisis due to pheochroimocytoma
- Prevent or treat necrosis after extravasation of a agonist
- Reverse toxicity of A agonist
- Reverse local anesthesia
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Alpha 1A selective blockers (3) (BPH)
- Tamsulosin
- Alfuzosin
- Silodosin
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First Dose Phenomenon (A1 selective blockers_)
- Excessive orthostatic hypotension
- Must start with low dose and increase slowly
- Avoid driving etc
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Alpha 1 blockers in the prostate
- Alpha 1A receptors in prostats (1B in blood vessels)
- Blocking them causes relaxation of smooth muscle
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Selective alpha 1 antagonist ADR's (2)
- Floppy Iris syndrome during cataract surgery
- Priapism (permawood)
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Tamsulosin (Flomax) concerns (3)
- Sulfa allergy
- Priapism
- Otrhostatic hypotension
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Beta blockers effects due to?
B1 blockade in the heart
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Beta blocker indications (4)
- Hypertension
- Angina pectoris
- Arrhythmias
- Myocardial infarction
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Beta blocker effects in the eye (1)
Decrease synthesis of aqueous humor (glaucoma)
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Beta blocker effect in kidney (1)
Decrease secretion of Renin
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Beta blockers have an unfavorable lipid profile but...
Beta 1 blockers may have an improved lipid profile
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Adverse effects of Beta 1 blockade (6)
- Bradycardia
- Decreased Cardiac Output
- AV block
- Worsen CHF
- Arrhythmias
- Rebound cardiac excitation if DC'd suddenly
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Adverse effects of B2 blockade (3)
- Bronchoconstriction (opposite of B2 agonist)
- Inhibition of glycogenolysis (opposite of B2)
- May enhance reflex vasoconstriction
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Propranolol facts (4)
- Prototype non-selective B blocker
- Highly lipid soluble (adr's - insomnia, depression etc)
- Wide dosage variations
- High 1st pass metabolism
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Propranolol uses (8)
- Hypertension
- Angina
- Arrhythmias
- MI
- Migrain prophylaxis
- Hyperthyroidism
- Essentialo tremor
- "Stage Fright"
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Nadolol (non-selectibe B blocker) facts (4)
- Lopngest half life, dosed QD
- Hypertension and angina
- Low lipid solubility (few CNS ADR's)
- Excreted unchanged in urine
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Timolol facts (3)
- Hypertension, MI, migrain, glaucoma (drops)
- Extensive metabolism by CYP2D6
- Low to moderate lipip solubility
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Pindolol facts (3)
- High ISA = partial B agonist
- Hypertension
- Low to moderate lipid solubility
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Beta 1 selective blockers (4)
- Metoprolol
- Atenolol
- Esmolol
- Bisoprolol
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Metoprolol (selective B1 antagonist) facts (4)
- Hypertension, angina, MI, CHF
- extensive 1st pass, low bioavailability
- Moderate lipid solubility
- metabolized by CYP2D6
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Atenolol (selective B1 antagonist) facts (3)
- Hypertension, angina, MI
- Very hydrophilic, penetrates CNS to limited extent
- Excreted unchagned in urine
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Esmolol (b1 selective blocker) fact (1)
Super short acting, used IV for emergency tachycardia
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Labetolol Facts (a1, B1&B2 antagonist) (2)
- IV for severe hypotension, PO for hypotension
- Extensively metabolized
- Rare hepatotoxicity
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Carvedilil facts (a1, b1&b2 blocker) (3)
- highly lipophilic
- Floppy iris syndrome
- Metabolized by CYP's
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