Adrenoceptor antagonist 1!! Flashcards
which adrenoceptor antagonist (receptor) is used for hypertension and prostatic hyperplasia?
alpha 1
Which adrenoceptor does not have many clinical uses?
alpha 2
Mixed Alpha 1&2 adrenoceptor antagonists are commonly used for?
pheochromocytoma
Which adrenoceptor antagonists are used for hypertension, arrhythmia, ischemic, heart disease, endocrine and neurologic disorders, glaucoma?
Beta antagonists
Which adrenoceptor antagonists are sympatolytic?
mixed antagonists alpha & beta
Which antagonists cause a lowering of peripheral vascular resistance and blood pressure?
alpha antagonists
Which drugs can prevent the pressor effects of alpha agonists? What are they called?
alpha antagonists
called an “epinephrine reversal”
What often causes postural hypotension and bradycardia?
alpha antagonists
What is the genitourinary effects of alpha antagonists?
decreased resistance to urine flow and can help with urinary retention (especially due to an enlarged prostate)
Which adrenoceptor antagonist drug is used in the management of hypertension?
Prazosin - highly selective for alpha-1- receptors
What does Prazosin not have an effect on?
Does NOT have tachycardic effect of phentolamine or phenoxybenzamine
Which adrenoceptor antagonist drug is used to treat BPH (benign prostatic hyperplasia)?
Terazosin
Which adrenoceptor antagonist drug is used to hypertension and BPH (benign prostatic hyperplasia)?
Doxazosin
Which three alpha antagonistic drugs have a higher affinity for alpha 1 over alpha 2?
Prazosin, terazosin, doxazosin
Which drug has a longer half life than Prazosin or Terazosin?
Doxazosin
Which adrenoceptor antagonist is a great drug for BPH because it inhibits the prostatic smooth muscle? When does it have a less dramatic effect on Blood Pressure?
Tamsulosin (Flowmax)
Less dramatic effect on BP in standing patients
Tamsulosin (Flowmax) is a competitive ______ antagonist.
Alpha 1 antagonist
Which andrenoreceptor antagonist drug causes blockade of long duration at alpha receptors?
Phenoxybenzamine
Which adrenoceptor is phenoxybenzamine selective for?
Alpha-1 (but less so than Prazosine)
What receptors does phenoxybenzamine block?
histamine, acetylcholine, and serotonin receptors
Which adrenoreceptor antagonist causes severe hypotension when patient is upright?
Phenoxybenzamine
What does Phenoxybenzamine inhibit the reuptake of?
norepinephrine
Which adrenoreceptor antagonistic drug is used to treat pheochromocytoma?
Phenoxybenzamine and Phentolamine
What are the adverse effect of Phenoxybenzamine?
- postural hypotension & tachycardia
- nasal stuffiness
- inhibition of ejaculation
Which adrenoreceptor antagonist is a potent competitive antagonist of both alpha1 and alpha 2 receptors and leads to enhanced release of norephinephrine and thus stimulates the heart?
Phentolamine
What are the adverse effects of Phentolamine?
- tachycardia
- arrhythmias
- MI
- Headache
- nasal congestion
What is used to treat pheochchromocytoma and male erectile dysfunction?
Phentolamine
What is ALfuzosin used for?
alpha-1 selective drug used to treat BPH
antihypertensive drug
Indoramin
antihypertensive drug; also treats BPH; only used in Europe
Urapidil
alpha and beta blocking capability
Labetolol
an antidepressant that blocks alpha receptors
trazodone
Alpha 2 selective agent with no specific clinical values as of yet
Yohimbine
adrenal tumor characterized by episodic release of Epi (80%) and NE (20%)
Pheochromocytoma
What is Labetalol still used for in emergencies?
hypertensive emergency
What beta-receptor blocking drugs have intrinsic sympathomimetic properties?
partial agonsists
T/F Beta Receptor Blocking Drugs that are selective for B1 vs B2 are dose related. Selectivity decreases at higher doses.
True
What do all beta receptor blocking drugs have in common?
They all treat hypertension
What ethnic class are beta receptor blocking drugs less efficacious in?
African Americans & Elderly
What class of drugs has been shown to decreases portal vein pressure in patients with cirrhosis?
Beta receptor blocking drugs
How do beta receptor blocking drugs effect blood pressure?
when used chronically beta receptor blocking drugs lower blood pressure in patients with hypertension
T/F When given chronically, beta receptor blocking drugs will give lower BP in patients with hypertension, inhibit renin release, and always causes hypotension in a healthy individual.
FALSE! usually DONT cause hypotension in healthy individual
WHen are cardiovascular effects of beta blockers most strongly indicated?
in the acute phase of a heart attatck
What type of arrhythmias are beta blockers used to treat?
supraventricular and ventricular arrhythmias
What are valuable for the heart following MI, angina, and CHF? (congestive heart failure)
Beta Blockers
T/F Beta Blockers have positive ionotropic and negative chronotropic effects. Most cause tachycardia.
FALSEEE!!!
- negative ionotropic & negative chronotropic effects
- Most cause BRADYCARDIA
T/F Beta Blockers lead to decreased air resistance, especially in patients with asthma.
FALSE!
increased airway resistance, especially with pt’s with asthma
What beta receptors are present in the bronchi?
B2
Should beta blockers be avoided in asthmatics? why?
YES! they should be avoided, because the receptors are not completely selective.
What type of patient with a respiratory disease could tolerate beta blockers? why?
Patients with COPD however may tolerate the drugs and risk/benefit ratio needs to be considered.
i.e. a patient with COPD and severe ischemic heart disease
What is the opthalmic effect of beta blockers?
reduce ocular pressure, especially in the eyes of patients with glaucoma
What is the mechanism of the opthalmic effect of beta blockers?
they decreases the production of aqueous humor
What receptor inhibits the stimulation of lipolysis?
Beta 3
How do beta blockers effect cholesterol?
decrease HDL (the good cholesterol) and increase VLDL --may be less with ISA
Due to the effects that beta blockers have on CHOLESTEROL .. what pt’s should AVOID using beta blockers?
patients with CVD risk
What is partially inhibited by beta blockers?
gycogenolysis
Due to the effect that beta blockers have on glycogenolysis, what patients should avoid using beta blockers?
Diabetic patients, because glycogenolysis is the bodies defense against hypoglycemia
What is the prototypical beta blocking drug?
Propanolol (Inderal)
T/F Propanolol (Inderal) is selective for B1 receptors.
False - nonselective among beta receptor subtypes
What is used in patients who have had an IM to prolong survival and protect the heart?
Propanolol (Inderal)
T/F Propanolol (Inderal) has little effect on alpha receptors.
true
What can be used during thyroid storm (severe hyperthyroidism) to control supraventricular tachycardia?
Propanolol (Inderal)
T/F Propanolol (Inderal) is useless against migraines.
false- can reduce the frequency and intensity of migraines
What is useful in patients who have suffered ischemic heart damage and also with CHF? What receptor is it selective for?
metoprolol (Lopressor) and Atenolol - B-1 selective drugs
What beta blocker is safer to use in patient who suffer from asthma or COPD?
Metoprolol (Lopressor) & Atenoldol
T/F Metoprolol (Lopressor), Atenolol, and Propanolol are useful in treating migraines.
true
What is the most selective beta 1 antagonist?
Nebivolol
What are the 3 things associated with Nebivolol?
- vasodilator by increasing endothelial NO production
- increase insulin sensitivity
- No adverse effect on lipid profile
What is a nonselective Beta blocker that has excellent ocular hypotensive effects when administered topically on the eye?
Timolol