Konorev Antiadrenergic Drugs Part 2 Flashcards
(35 cards)
what are direct acting antiadrenergic α adrenoceptor antagonists?
- Non selective α1 and α2
- phentolamine
- phenoxybenzamine
- α1 selective
- prazosin
- Tamsulosin
- Doxazosin
What are the direct acting antiadrenergic drugs in the mixed blocker class?
- Labetalol
- Carvedilol
- both are B and α1 antagonists
What are the direct acting antiadrenergic drugs that fall into the Beta adrenoceptor blockers?
- B1 and B2 blockers
- propanolol
- pindolol
- Nadolol
- B1 Selective
- Metoprolol
- Betaxolol
- Acebutolol
- Atenolol
What are the indirect acting antiadrenergic drugs that fall under the NE release inhibiitor class?
Guanethidine
What are the indirect acting antiadrenergic drugs that fall under inhibition of tyrosine hydroxylase?
Metyrosine
Pharmacokinetics of Phentolamine?
- reversible competitive α antagonist
- Non covalent binding
- Short acting
- antagonized by high concentrations of agonist
Phenoxybenzamine pharmacokinetics?
- non competitive irreversibole α antagonist
- covalent binding
- longer acting than phentolamine
- Effect is not antagonized by α agonist
Pharmacodynamics of α antagonists on the cardiovascular system?
- Decreased peripheral vascular resistance and BP
- Postural hypotension
- reflex tachycardia
Pharmacodynamics of α antagonists on the GU system?
- relaxation of smooth muscle in prostate
- Decreased resistance to flow of urine
Pharmacodynamics of α antagonists on the eye?
Relaxation of pupillary dilator muscles- miosis
Pheochromocytoma is treated with what drugs?
α antagonists such as:
- Phentolamine
- a direct acting antiadrenergic non selective α1 and α2 receptor antagonist
- Phenoxybenzamine
- a non selective α1 and α2 receptor antagonist
- Metyrosine
- Indirect acting antiadrenergic drug inhibitor of tyrosine hydroxylase
What is chronic (essential) HTN treated with? What are the drug classes?
- Prazosin
- Doxazosin
- Both are α1 selective direct acting antiadrenergic drugs
How is ED treated?
Combination of phentolamine and a non specific vasodilator papaverine
Chronic urinary obstruction secondary to BPH is treated with what drug? What receptor does it prefer?
- Tamsulosin
- impacts α1A more than α1B receptors
AE’s of alpha antagonists?
- seen less with α1 selelctive antagonists
- Postural hypotension- due to antagonism of α1 in venous smooth muscle
- Nasal stuffiness
- Tachycardia
- Retention of fluid and salt
- Imparied ejaculation
What are the Mixed Beta adrenoceptor antagonists?
- Labetalol B and α1
- Carvedilol B and α1
What are the B1 and B2 adrenoreceptor blockers?
- Propanolol
- Pindolol (partial agonist)
- Nadolol
What are the B1 selective adrenoceptor antagonists?
- Metoprolol (inverse agonist)
- Betaxolol (inverse agonist)
- Acebutolol (partial agonist)
- Atenolol
What are the pro’s to using a beta blocker with Intrinsic Sympathomimetic Activity, in other words the drug is a partial agonist at the beta adrenergic receptor?
- They have less risk for bradycardia
- Increase VLDL/HDL
- They block sympathetic effects but have submaximal effects of their own
Pharmacodynamics of beta blockers on the heart?
- Negative inotropic effect
- Negative chronotropic effect
- Slow AV node conduction
Pharmacodynamics of beta blockers on blood vessels?
- Initially see a rise in peripheral vascular resistance but with chronic use it leads to a decrease in PVR (lowering BP)
How do Beta blockers impact Renin angiotensin system?
Inhibit renin release
How do Beta blockers impact respiratory system?
Increase airway resistance
How do Beta blockers impact the eye?
Reduce production of aqueous humor decreasing intraocular pressure
