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42 Cards in this Set
- Front
- Back
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What are two other sympatholytics?
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Mecamylamine and reserpine
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How does mecamylamine work?
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It is a ganglionic blocker that blocks nicotinic receptors found in the ganglia.
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How does reserpine work?
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It depletes norepi from nerve terminals and from the adrenal medulla. It can also enter the brain and deplete neurotransmitters located there.
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Which drugs act on the vasomotor center?
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Methyldope, clonidine, guanabenz, and guanfacine
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Which drugs are angiotensin II receptor blockers?
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Losartan and others.
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Which drugs target receptors on vascular smooth muscle?
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hydralazine, minoxidil, nitroprusside, diazoxide, verapamil (and other CCBs), and fenoldopam
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Which drugs are ACE inhibitors?
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Captopril and others.
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Which drugs is a renin inhibitor?
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Aliskiren
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What are adverse effects of reserpine?
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diarrhea, increased gastic acid, nasal stuffiness, POSTURAL HYPOTENSION, and fluid retention.
Also, NIGHTMARES, impaired ejaculation, depressed libido, SEDATION, PSYCHOTIC DEPRESSION, and SUICIDAL THOUGHTS. It is a drug of LAST RESORT |
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What are the adverse effects of mecamylamine?
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Tachycardia, urinary retention, blurred vision, mydriasis (dilation of the pupils), and impotence.
Rarely used now for hypertension. Used for CNS action. |
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What does angiotensin do to vessels?
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increases vasoconstriction, inflammation, and atherosclerosis.
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What does angiotensin do to the heart?
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increases fibrosis and hypertrophy.
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What is the effect of ACE inhibitors on bradykinin?
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It stops the suppression of bradykinin so it can do its job of vasodilation, and of increasing capillary permeability.
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What are two examples of ACE inhibitors?
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Lisinoplir and enalapril (a prodrug). These drugs end in, "pril."
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How do ACE inhibitors affect CO and HR?
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They don't.
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What does ACE inhibitors do to remodeling?
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Decreases it.
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When are ACE inhibitors indicated?
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Good choice for monotherapy, drug of choice for diabetic pts, decreases kidney damage, good for pts with CHF/LVH/cardiac arryhthmias. Good for asthmatics. It is most effective in high renin hypertension.
Its efficacy increases by 75% when combined with diuretics. It is also more effective in white pts than african americans and the elderly--mainly because these groups have low amounts of renin. |
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What are some adverse effects of ACE inhibitors?
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cough, hyperkalemia, angioedema, hyper-reninemia (more renin in the blood). They are teratogens during all 3 trimesters.
MINOR AFFECTS: ageusia (no taste), dysgeusia, skin rash, and proteinuria. |
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Why shouldn't ACE inhibitors be used in pts with renal stenosis?
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Because renin is needed to activate Ang. II. Antgiotensin will constrict the efferent arteriole which keeps the kidney functioning.
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What do angiotensin receptor blockers (ARBs) do?
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They specifically bind to angiotensin I receptors.
Competitive antagonist includes Losartan. Non-competitive antagonist includes valsartan (all end in, "sartan.") |
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What do ARBs do?
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They block the ability of angiotensin to increase BP and stimulate cell proliferation.
It is good in CHF patients, to prevent remodeling. |
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What are the adverse effects of ARBs?
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Hypotension, hyperkalemia, avoid with renal stenosis pts. Also these drugs cause hyper-reninemia, and are teratogenic.
However, they have the benefit of not causing bradykinin effects like cough and edema. |
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WHat are the clinical indications for ARBs?
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hypertension, heart failure, and diabetic nephropathy.
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What do renin inhibitors do?
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inhibits renin which is the rate-limiting step in AT II formation.
It is used best in essential hypertension, and only needs to be taken once a day. Combining it with an ARB makes it more effective. |
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What are the adverse effects of aliskarin (the renin inhibitor)?
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Similar to those of ARBs:
hyperkalemia, hypotension, diarrhea, headache, nasophyaringitis. Contraindicated in pregnancy. |
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What drugs are CCBs?
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Amlodipine, diliatazem, verapamil, and nifedipine.
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How do amlodipine and nifedipine work?
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They block L type calcium channels in vascular smooth muscle.
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How do dilatazem and verapamil work?
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They block L type calcium channels in vascular smooth muscle. But also in the heart.
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Which CCBs are most commonly used?
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Dihydropyridines--because there's no cardiac complications.
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What are CCBs best for?
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In low renin hypertension, found in African americans and in the elderly.
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What are adverse effects of short-acting dyhydropyridines?
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A very high DROP in BP that activates baroreceptors, then causes tachycardia while the CCB is decreasing cardiac perfusion.
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What adverse effects are not present in verapamil nor in diltiazem?
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Reflex tachycardia.
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What are two direct vasodilator drugs?
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hydralazine and minoxidil
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How does hydralazine work?
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It inhibits calcium release and creates nitric oxide.
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When is hydralazine used?
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Not for a first line drug or for monotherapy.
Used in combination with a diuretic and used in refractory hypertension. It is more effective in african americans. |
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What are adverse effects of hydralazine?
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Hypotension (then tachycardia and palpitations), fluid retention, A LUPUS-LIKE SYNDROME, dry mouth, headache, nausea, and edema.
Its bioavailability depends on genetic factors. |
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How does minoxidil work?
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It is a K+ channel opener, causing hyperpolarization for vascular smooth muscle relaxation. It directly decreases peripheral resistance. It is used only in refractory hypertension, and has a long duration of action.
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What are the adverse effects of minoxidil?
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Fluid retention, edema, tachycardia, palpitation, HYPERTRICHOSIS--hair growth.
It is used in combination with a beta blocker and a diuretic. |
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What is an example of a centrally acting sympatholytic?
How does it work? |
An alpha-2 AGONIST, such as Clonidine.
It stimulates alpha-2 adrenoreceptors on inhibitory neurons in the brainstem to reduce sympathetic tone. This decreases heart rate and causes vasodilation. |
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When are alpha-2 agonists used?
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In moderate hypertension, not as monotherapy.
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What are adverse effects of alpha-2 agonists (such as clonidine)?
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Fluid retention (use it with a diuretric), hypotension, sedation in 50% of pts, and vivid dreams.
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What are some more direct vasodilators?
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Nitroprusside (nitric oxide), diazoxide (a K+ channel opener), and fenoldopam (a dopamine receptor agonist).
These are used in emergency situations by I.V. |
