Part 2 CVS drugs Flashcards
angiotensin converting enzyme inhibitors
- popular antihypertensive agents today
- _____ is released from its storage in _____ and _____ vessels with _____ stimulation
- renin combines with angiotensininogen = _____
- angiotensin 1 goes to the _____ and is acted upon by _____ (_____) to convert to _____
- angiotensin II is a potent _____
- it also stimulates release of _____ from _____
- aldosterone results in _____ reabsorption
- used in _____, _____, and post _____ (_____)
renin afferent efferent adrenergic angiotensin I lungs angiotensin converting enzyme (ACE) angiotensin II vasoconstrictor aldosterone adrenal cortex sodium hypertension heart failure myocardial infarction (MI)
ACE- inhibitors
- widely used, important class of antihypertensive drugs
- all generic names of this drug class end in _____
- _____ (vasotec)
- _____ (altace)
- _____ (prinivil)
- used alone or in combination with other antihypertensives
‘-pril’
enalapril
ramipril
lisinopril
renin angiotensin system
- regulates:
- -_____
- -blood _____ and _____
- -_____ balance
- pathology:
- -_____
- -_____ failure
- -
blood pressure volume fluid electrolyte hypertension heart myocardial infarction
renin angiotensin system
renin secretion:
-1. _____ activation (_____-adrenergic receptors)
-2. reduction in _____ tension in _____ arterioles
-3. reduction in _____ reabsorption by renal ______
angiotensin I; II and III:
- angiotensin I:
- -precursor of II, little or no _____ activity
- angiotensin II:
- -potent _____ degraded to angiotensin III
- angiotensin III:
- -has some biological activity but significantly less than angiotensin II
sympathetic B1 wall renal afferent NaCl renal macula densa biological vasoconstrictor
angiotensin II receptors
- two types: _____ and _____
- -AT: activation results in the
- -increase in _____ (_____) leading to an increase in _____
- -increase in _____ metabolites
- decrease in _____
- -_____ (activation)
- –synthesis and release of _____
- pharmacological actions
- -_____ (arterioles)
- -release of _____
- -alteration of _____ and _____ structure
AT1 AT2 inositol phosphate (IP3) intracellular calcium arachidonic acid metabolites cAMP adrenal cortex aldosterone vasoconstriction aldosterone cardiac vascular
ACE-inhibitors
- _____, _____, _____, _____, _____
- clinical uses:
- -_____; cardiac _____, diabetic _____, _____
- -mechanism: inhibition of _____, inhibits the production of _____
- pharmacological effects
- -vasodilation:
- –blocks _____
- –mainly arterioles, less on _____
- –decrease _____ - decrease in _____
- -both arterial and venous pressure _____
- –what happens to preload and afterload? _____
catopril enalapril fosinopril lisinopril ramipril hypertension failure nephropathy MI ACE angiotensin II vasoconstriction veins PR BP DECREASES BOTH DECREASE
drug interactions of ACE inhibitors
_____ & ______ diuretics:
-augmented _____ and _____ insufficiency
-caution when used in combinations
_________
–combined hypotension
- drugs that increases _____ levels
- -_____ supplements
- -_____-sparing _____
-_____: increase levels of Li+
loop & thiazide hypotension renal antihypertensives potassium K potassium diuretics lithium
side effects of ACE inhibitors
- rash 5-10%
- _____ 5% with _____ (from bradykinin)
- contraindicated in _____, causes severe fetal injury
- -_____ failure
- –in patients with _____
- –patient is dependent on _____ to maintain renal blood flow and glomerular filtration
dry cough lisinipril pregnancy renal bilateral renal artery stenosis angiotensin II
angiotensin II receptor blockers
- angiotensin II has a strong _____ effect due to activation of _____ receptors present on _____
- ARBs compete for these receptors and _____ them
- _____ (cozaar) is the first ARB
- _____ + _____ (Hyzaar) is a combination available
vasoconstrictor angiotensin II blood vessels block losartan losartan hydrochlorothiazide
angiotensin II receptors blockers (ARBs) MOA -blocks activation of \_\_\_\_\_ receptors --vascular smooth muscle: \_\_\_\_\_ of \_\_\_\_\_ --adrenal glands: ---\_\_\_\_\_ and decrease \_\_\_\_\_ secretion ----increase \_\_\_\_\_ and \_\_\_\_\_ excretion ----no significant effect on \_\_\_ levels and do not cause dyspnea, \_\_\_\_\_ or angioedema --the net effect is similar to \_\_\_\_\_\_
angiotensin dilation arterioles vasodilation aldosterone Na+ water K+ cough ACE inhibitors
angiotensin II receptors blockers (ARBs)
- ARBs: Losartan
- -adverse effects:
- –no major adverse effects
- –low incidence of _____
- –DO NOT increase serum _____; _____, or alter _____ levels
- -contraindicated in:
- –_____ - 2nd and 3rd trimester
- –_____ diseases: renal artery stenosis
dizziness glucose uric acid serum lipid pregnancy renal
beta blockers
- sympathetic antagonists at the beta receptors in _____ and _____
- inexpensive agents used with _____ for hypertension
- decrease _____ rate and _____ demand of heart muscle
- block beta 1 receptors and beta 2 or only beta 1
- block the _____ and _____ effect
- decrease rate of spontaneous _____, slow _____ conduction
- end in “_____”: _____, _____, _____
heart blood vessels diuretics pulse oxygen positive inotropic chronotropic depolarization AV lol propranolol metoprolol atenolol
beta blockers
- non-selective beta blockers may block the beta 2 receptors in _____ airways
- results in _____ / life threatening!
- beta blockers may also blunt the _____ that occurs with _____
- recovery from_______ may be delayed
- may block the sympathetic symptoms of _____
bronchial bronchoconstriction glycogenolysis catecholamines hypoglycemia hypoglycemia
uses of beta blockers
- management of _____: acute and chronic
- _____ is cardio-selective: Mx of angina pectoris
- _____: blocks beta receptors on ciliary blood vessels
- decreases production of _____ (IOP)
- _____: Mx of hypertension, angina, SVTs migraine prophylaxis, tremors, social phobia, GAD
- _____ (ultra short acting): critically ill patients
- _____ has intrinsic beta agonist activity, used for chronic hypertension
- _____ is a non selective beta blocker. airway stimulation in a patient may cause bronchoconstriction
hypertension atenolol timolol aqueous humor propranolol esmolol pindolol nadolol bronchoconstriction
propranolol
- _____ to _____ hypertension
- severe hypertension: combine with _____
- blocks _____ and _____ adrenoceptors (non-selective)
- -decreases BP by decreasing _____
- inhibit the stimulation of _____ production
- -(which is via B1 stimulation by _____)
- –depress (partly) the _____ system
- –propranolol is contraindicated in first degree _____, _____, cardiogenic shock COPD and bronchial asthma
- –given _____ for hypertension/ _____ for arrhythmias
mild moderate vasodilators B1 B2 cardiac output renin catecholamines renin-angiotensin-aldosterone heart block CHF orally IV
metoprolol (Lopressor/Toprol XL)
cardioselective
-blocks _____, sparing _____ receptors (except at high doses)
-effects similar to _____: reduces _____ levels too
-advantage for hypertensive patients with history of _____, _____ or peripheral vascular disease
-given _____, onset of action is 5 mins, peaking in 1 hour
-used for _____, _____, _____, _____
-it enhances the effects of _____ (CNS depression)
-if used with _____ to reverse NM blockade, marked _____ has been observed in patients
-it masks signs of _____ and _____
B1 B2 propranalol renin asthma diabetes IV hypertension angina MI congestive heart failure benzodiazepines neostigmine bradycardia hypoglycemia hyperthyroidism
labetalol
- normodyne/trandate
- _____ + _____ and _____ blocker
- alpha: _____, decreased _____, _____ hypotension
- beta: _____ node, _____ node, _____ muscle: _____
- used _____ intra-op
- attenuates hypertension and tachycardia post _____
- used for _____ and _____ withdrawal
- specifically used for _____, _____, general and _____ surgical procedures
alpha 1 beta 1 2 vasodilation PR orthostatic SA AV ventricular bradycardia IV surgery pheochromocytoma clonidine cardiac vascular intracranial
calcium channel blockers
- calcium entry into the cell is essential for _____ to _____
- calcium is a trigger for _____ contraction
- blocking calcium channels inhibits smooth muscle contraction leading to _____ of _____ and _____ and _____ effects on heart
- _____ is used for peri-operative hypertension
- _____ slows SA and AV conduction transmurally
smooth muscles contract cardiac smooth muscle vasodilation arterioles negataive inotropic and chronotropic nifedepine verapamil
calcium channel blockers
- _____: amlodipine, nifedipine
- _____, _____
- very _____ agents
- act directly on smooth muscle in _____ and cause _____
- also decrease _____ and force of _____
- _____ (adalat) is used in acute situations
- minimal effect on cardiac contractility by _____
- decrease _____
dihydropyridines diltiazem verapamil potent arterioles relaxation heart rate contraction nifedipine dihydropyridines peripheral resistance
clinical considerations of CCBs
- _____, _____, _____, _____
- drug induced _____ overgrowth (hypertrophy)
- adequate hydration of the patient reduces the risk of _____ peri-operatively
- increased cardiovascular depressant effects of _____
- _____ increases the sedative effects of benzodiazepines
- increased chances of _____ and _____ with concomitant use of diltiazem and beta blockers
dizziness headache syncope tachycardia gingival hypotension general anesthetics general anesthetics diltiazem hypotension bradyarrhythmias
anti-anginal drugs
- angina: latin/ pain in _____ syndrome
- _____ of the heart muscle
- _____ pain radiating to _____ arm/ chest/ jaw
- deficit in myocardial oxygen supply in relation to demand resulting in _____ depression in EKG
- the ischemia may result from _____ of the coronary artery, _____, increased cardiac_____ or usually a combination of the above
- drug induced: cocaine as well as drugs containing _____ (such as _____)
chest ischemia retrosternal left ST atherosclerosis vasospasm cardiac workload sympathomimetics epinephrine
pathophysiology of angina
- _____ diet/ obesity
- family history of _____
- _____
- age/ race/ gender
- co-existing _____ disease
- _____
- _____
- substances of abuse
- _____ (_____)
high cholesterol MI hypertension cardiac smoking alcohol vasospasm prinzmetal's
symptoms of angina
- classically… _____ pain described as squeezing, constricting, burning
- radiation to _____, _____, _____, _____
- may be associated with _____, vomiting, dizziness, fear of doom
- can a patient be symptom free?
substernal jaw neck shoulder left arm nausea yes
pharmacological management
6 classes of drugs used for management of angina
-1. _____: nitroglycerin
-2. _____ blockers: nifedipine, verapamil
-3. _____ blockers: propranolol, atenolol
-4. _____ and _____: aspirin
-5. _____: approved by FDA in 2006 for chronic angina patients who fail traditional therapy
-6. _____: metabolic agent which decreases oxidation of free fatty acids. used for _____ term control
-all these drugs relieve anginal pain either by reducing _____ demand or increasing _____ supply to myocardium
organic nitrates calcium channel beta antiplatelets anticoagulants ranolazine trimetazidine long oxygen blood
non-pharmacological Mx
- control of _____/ _____
- _____ change
- stop _____
- reduce _____
- develop an _____ program
- surgical ‘revascularization’ - _____
- _____ and _____ therapy
weight diet lifestyle smoking blood pressure exercise CABG stents laser
nitrates
- _____ (nitrostat, nitro-dur patch)
- _____ which converts in the smooth muscle intracellular space
- converted to _____ (NO) which causes _____ of cardiac blood vessels
- dilates both _____ and _____ vasculature
- used _____ in acute angina attacks
- -onset is 1-3 minutes
- -use up to _____ doses
- -_____ are common (use _____)
- -cant be stored in _____ (special IV sets)
nitroglycerin prodrug nitric oxide vasodilation coronary pulmonary sublingually 3 headaches Tylenol plastic
nitrates nitro patches -used prophylactically for \_\_\_\_\_ -given in 0.2, 0.4, 0.6mg/hr patches -applied for 12 hours- off for 12 hours -nitrate free period of 10-12 hours is required or the patient may become \_\_\_\_\_ to the nitrate therapy
- side effects:
- -_____
- -_____, lightheadedness
- -_____
- -_____ can greatly increase the effect of nitrates
angina tolerant headache dizziness hypotension alcohol