Sympatholytics (blockers)

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Author:
jaguavai
ID:
120090
Filename:
Sympatholytics (blockers)
Updated:
2011-12-01 15:04:13
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Pharm 420
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Sympatholytics
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  1. Sympatholytic MOA (2)
    • Bind to adrenergic receptors and prevent action
    • Act indirectly by inhibiting synethesis, release or reuptake of norepi
  2. Alpha blocker types (2)
    • Alpha 1 selective (the azosins)
    • Alpha 1 and 2 non-selective (phentolamine, phenoxybenzamine)
  3. Blockade of alpha 1 effects (2)
    • Inhibits vasoconstriction induced by endogenous catecholamines
    • Vasodilation reduces BP, causes reflex tachycardia
  4. Blockade of alpha 2 receptors effects (1)
    increased NE release and stimulation of B1 receptors
  5. 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)
  6. Alpha 2 blocker major adverse events (1)
    Intensification of reflex tachycardia due to decrease in BP (can trigger arrythmias and angina)
  7. If you block alpha 2 on presynaptic sympathetic neuron?
    • INCREASED NE release
    • Opposite if you stimulate alpha 2
  8. Phenoxybenzamine (non-selective alpha blocker) indication
    Hypertenssive crisis due to pheochrmocytoma
  9. Phenoxybenzamine ADR (15
    • Severe postural hypotension
    • Tachycardia
    • FLushing
    • Nasal congestion
    • Sexual disfunction
  10. 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
  11. Alpha 1A selective blockers (3) (BPH)
    • Tamsulosin
    • Alfuzosin
    • Silodosin
  12. First Dose Phenomenon (A1 selective blockers_)
    • Excessive orthostatic hypotension
    • Must start with low dose and increase slowly
    • Avoid driving etc
  13. Alpha 1 blockers in the prostate
    • Alpha 1A receptors in prostats (1B in blood vessels)
    • Blocking them causes relaxation of smooth muscle
  14. Selective alpha 1 antagonist ADR's (2)
    • Floppy Iris syndrome during cataract surgery
    • Priapism (permawood)
  15. Tamsulosin (Flomax) concerns (3)
    • Sulfa allergy
    • Priapism
    • Otrhostatic hypotension
  16. Saw Palmetto use (1)
    BPH
  17. Beta blockers effects due to?
    B1 blockade in the heart
  18. Beta blocker indications (4)
    • Hypertension
    • Angina pectoris
    • Arrhythmias
    • Myocardial infarction
  19. Beta blocker effects in the eye (1)
    Decrease synthesis of aqueous humor (glaucoma)
  20. Beta blocker effect in kidney (1)
    Decrease secretion of Renin
  21. Beta blockers have an unfavorable lipid profile but...
    Beta 1 blockers may have an improved lipid profile
  22. Adverse effects of Beta 1 blockade (6)
    • Bradycardia
    • Decreased Cardiac Output
    • AV block
    • Worsen CHF
    • Arrhythmias
    • Rebound cardiac excitation if DC'd suddenly
  23. Adverse effects of B2 blockade (3)
    • Bronchoconstriction (opposite of B2 agonist)
    • Inhibition of glycogenolysis (opposite of B2)
    • May enhance reflex vasoconstriction
  24. Propranolol facts (4)
    • Prototype non-selective B blocker
    • Highly lipid soluble (adr's - insomnia, depression etc)
    • Wide dosage variations
    • High 1st pass metabolism
  25. Propranolol uses (8)
    • Hypertension
    • Angina
    • Arrhythmias
    • MI
    • Migrain prophylaxis
    • Hyperthyroidism
    • Essentialo tremor
    • "Stage Fright"
  26. 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
  27. Timolol facts (3)
    • Hypertension, MI, migrain, glaucoma (drops)
    • Extensive metabolism by CYP2D6
    • Low to moderate lipip solubility
  28. Pindolol facts (3)
    • High ISA = partial B agonist
    • Hypertension
    • Low to moderate lipid solubility
  29. Beta 1 selective blockers (4)
    • Metoprolol
    • Atenolol
    • Esmolol
    • Bisoprolol
  30. Metoprolol (selective B1 antagonist) facts (4)
    • Hypertension, angina, MI, CHF
    • extensive 1st pass, low bioavailability
    • Moderate lipid solubility
    • metabolized by CYP2D6
  31. Atenolol (selective B1 antagonist) facts (3)
    • Hypertension, angina, MI
    • Very hydrophilic, penetrates CNS to limited extent
    • Excreted unchagned in urine
  32. Esmolol (b1 selective blocker) fact (1)
    Super short acting, used IV for emergency tachycardia
  33. Labetolol Facts (a1, B1&B2 antagonist) (2)
    • IV for severe hypotension, PO for hypotension
    • Extensively metabolized
    • Rare hepatotoxicity
  34. Carvedilil facts (a1, b1&b2 blocker) (3)
    • highly lipophilic
    • Floppy iris syndrome
    • Metabolized by CYP's

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