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Week 5-HTN
drugs for hypertension and diuretics
146
Pharmacology
Graduate
02/28/2013

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Term
Lisinopril
Definition
ACE Inhibitor
Term
Lisinopril MOA
Definition
Selectively suppresses renin-angiotensin-aldosterone system, inhibits ACE which prevents conversion of angiotension I to angiotensin II
Term
Lisinopril Uses
Definition
Mild to moderate HTN, adjunctive therapy of systolic CHF, and acute MI
Term
Lisinopril Contraindications
Definition
Angioedema, Pregnancy (D - 2nd & 3rd trimesters), renal disease, hyperkameia, renal artery stenosis, CHF
Term
Lisinopril Pharmacokinetics
Definition
Onset 1 hr, peak 6-8 hrs, duration 24 hrs, half life = 12 hrs
Term
Lisinopril ADR
Definition
Vertigo, Fatigue, chest pain, hypotension, sinus tachycardia, angioedema, proteinuria, renal insufficiency, sexual dysfunction
Term
Lisinopril & Hyperkalemia
Definition
specifically with potassium sparing diuretics, potassium supplements
Term
Lisinopril drug/food interactions
Definition
high-potassium diet should be avoided or hyperkalemia may occur. Avoid bananas, orange juice, avocados, nuts, spinach
Term
Furosemide
Definition
A loop diuretic (prototype)
Term
Furosemide MOA
Definition
Inhibits Na/K/2Cl transporter in the ascending Loop of Henle - reduces reabsorption of NaCl and increases urinary output
Term
Effects of Furosemide
Definition
Increases urinary excretion of NaCl, K+, Ca++, and Mg++
Term
Furosemide Toxicity
Definition
Hypokalemic metabolic alkalosis, hypomagnesemia, hypochloremia, hyperuricemia, ototoxicity
Term
Clinical uses of Furosemide
Definition
Common uses: Edematous conditions, acute pulmonary edema, CHF (reduces LV filling pressures), HTN. Also: acute hyperkalemia or hypercalcemia, anion overdose
Term
NSAIDs or probenecid
Definition
May interfere with actions of loop diurectics such as furosemide
Term
Furosemide Pharmacokinetics
Definition
Rapid absorption, eliminated by kidneys, duration of effect is 2-3 hrs, half life dependent on renal function
Term
What are contraindications to furosemide?
Definition
hypersensitivity to furosemide or sulfonamides, hepatic cirrhosis, anuria
Term
Potassium
Definition
Patients often require this supplement when taking furosemide
Term
Lorsartan-
Definition
Angiotensin Receptor Blocker (ARB) (commonly end in –sartan)
Term
Lorsartan MOA
Definition
Interfere with binding of angiotensin II to its receptor (AT1)
Term
Lorsartan Side Effects
Definition
Pregnancy category X, cough less common than ACEI with ARB’s, but will still commonly occur, angioedema, hyperkalemia, renal impairment
Term
How effective is Lorsartan?
Definition
As effective as beta blockers, calcium channel blockers, diuretics and ACE inhibitors
Term
What type of monitoring should be done with an ARB?
Definition
BP it will take 4-6 weeks before the full therapeutic effect, and potassium- it can cause an increase in potassium
Term
Lorsartan Clinical Applications
Definition
Hypertension and heart failure
Term
How is Lorsartan renal protective?
Definition
Decrease BP and lower intragolmerular pressure results in decreased albumin excretion, slowing chronic renal failure. However, be careful in pt’s with low fixed renal blood flow (renal artery stenosis, CHF) because renal function is angiotensin dependent and decreasing can lead to acute renal failure.
Term
Verapamil medication class
Definition
Calcium Channel blocker
Term
Verapamil MOA
Definition
inhibits influx of calcium into arterial smooth muscle cells
Term
Cardiac effects of Verapamil
Definition
decreases HR and cardiac output, dilates coronary arteries
Term
Effects of Verapamil toxicity
Definition
Bradycardia, AV block, heart failure
Term
Verapamil adverse effects
Definition
Constipation, flushing, dizziness, nausea, peripheral edema
Term
Propanolol MOA (an "olol")
Definition
non-selective Beta1=Beta2 antagonist; highly lipid soluble; block effects of catecholamines (NE & EPI) at Beta1 receptors in the heart and Beta2 receptors of respiratory, vascular, & uterine smooth muscle; has local anesthetic action
Term
propanolol effects
Definition
Primarily by decreasing CO, but also by decreased HR and decreased renin release, causes decreased BP; initial increase in PVR, but long term decrease in PVR; increases airway constriction (caution in asthma); decreases intraocular pressure; impaired recovery from hypoglycemia (caution in Type I diabetes);
Term
propanolol ADR
Definition
depression, impotence, fatigue, impaired recovery from hypoglycemia, bronchoconstriction, sedation, sleep disturbances. Abrupt withdrawal can precipitate myocardial ischemia due to hypersensitivity to catecholemines which could lead to angina, acute MI, vent. arrhythmia, death.
Term
propanolol caution in discontinuation
Definition
1) reduce dose gradually over 1-2 weeks & monitor (esp. w/ ischemic heart disease; 2) transfer to alternative Beta blocker directly w/ comparable doses
Term
Propanolol clinical uses
Definition
HTN; CHF; angina; post MI; arrhythmias; migraine prophylaxis; situational anxiety; decreases mortality re:to bleeding in cirrhosis; long term use post MI prolongs survival
Term
propanolol kinetics
Definition
undergoes extensive hepatic (1st pass) metaboelilism (low & dose-dependent bioavailability); T1/2=3.5-6 hrs; lipophilic & readily crosses BBB; elimation may be prolonged in liver disease, decreased hepatic blood flow; or hepatic enzyme inhibition
Term
Minoxidil Toxicity/ADR
Definition
Tachycardia, palpitations, angina, and edema when concomittent loop diuretic and beta blocker therapy are inadequate
Common: HA, sweating and hypertrichosis (abnormal hair growth)
Term
Minoxidil MOA and Pharmacokinetics
Definition
Hyperpolarization of smooth muscle membrane through opening of potassium channels; may cause reflex sympathetic stimulation and Na and fluid retention; must be used in combination with a Beta-blocker and loop diuretic; does not cause orthostatic hypotension or sexual dysfunction
Term
Minoxidil Class
Definition
Vasodilator for treatment of HTN (dilates arterioles, not veins)
Term
Nifedipine MOA
Definition
Antagonism of the L-type calcium channels in cardiac and vascular smooth muscle cells. Muscle contractility is dependent on calcium influx across these channels. The end result is relaxation of the vascular muscle (vasodilation) and decreased cardiac contractility.
Term
Nifedipine Special Considerations
Definition
Reflex sympathetic activation can cause slight tachycardia. Short-acting oral nifedipine should not be used for treatment of chronic HTN; has been shown to have an increased risk of MI and death.
Term
Nifedipine Effects
Definition
Decreased PVR (vasodilation); may have slight increase in HR.
Term
How are Calcium Channel-Blockers Differentiated?
Definition
Dihydropyridines (Vascular Effect > Cardiac Effect)
vs. Non-dihydropyridines (Cardiac Effect > Vascular Effect)
Term
Nifedipine is the prototype of which family of Calcium Channel-Blockers?
Definition
The dihydropyridine family; this makes Nifedipine more selective for calcium channels in vascular smooth muscle than in cardiac muscle.
Term
What are the side effects of Nifedipine?
Definition
Hypotension, dizziness and headache. Bronchodilation can lead to cough, decreased motility in the GI tract can cause nausea or obstruction.
Term
Hydralazine MOA
Definition
Vasodilator that causes nitric oxide release resulting in vasodilation and reduction of vascular resistance
Term
Hydralazine Pharmacokinetics
Definition
Low bioavailability because rapidly metabolized by liver
Term
Hydralazine Clinical Uses
Definition
Used in severe hypertension, usually used with other hypertensive drugs
Term
Hydralazine Adverse Reactions
Definition
Headache, n/v, palipitations, sweating and flushing. With high dosages patients can develop arthralgia, myalgia, skin rashes, and fever that resembles lupus erythematosus
Term
Spironolactone MOA
Definition
A synthetic steroid that acts as a competitive agonist to aldosterone. Binds to mineralocoricoid receptors and blunt aldosterone activity.
Term
Spironolactone Pharmacodynamics
Definition
Potassium-sparing diuretic that reduces sodium absorption in the collecting tubules and ducts (potassium absorption and secretion at this site are regulated by adosterone). Has a slow onset of action.
Term
Spironolactone Clinical Uses
Definition
Diuretic whis is also useful in states of mineralosorticoid excess or hyperaldosteronism (aldosteronism). Examples of primary or secondary hyperaldosteronism are Conn's syndrome, hepatic cirrhosis.
Term
Spironolactone Considerations
Definition
Can be inhibited by NSAIDSs. Hyperkalemia is greatly increased in patients with renal insufficiency.
Term
Furosemide MOA
Definition
Selectively inhibits NaCl reabsorption in the thick ascending limb in the loop of henle.
Term
Furosemide ADR
Definition
Toxicity: hypokalemic metabolic acidosis, ototoxicity, hyperuricemia, hypomagnesemia, severe dehydration, occasionally allergic reactions (most loop diuretics are sulfonamides)
Term
Furosemide clinical indications
Definition
Acute pulmonary edema, acute hypercalcemia, acute renal failure, anion overdose
Term
Furosemide class
Definition
Loop diuretics
Term
Furosemide pharmacokinetics
Definition
Orally administered, absorption occurs within 2-3 hours, duration of effect 2-3 hours. T1/2 depends on renal function, eliminated by kidneys
Term
Furosemide contraindications/precautions
Definition
Patients allergic to sulfonamides may exhibit allergic cross-reactivity (rare). Excessive use in patients with hepatic cirrhosis, boderline renal failure, or heart failure can be dangerous
Term
Spironolactone class
Definition
Potassium Sparing Diuretic
Term
Spironolactone MOA
Definition
Competitive Aldosterone Antagonist-
*Binds to mineralocorticoid receptors to block/blunt aldosterone activity.
*Prevents K+ secretion and decreases Na+ absorption by blocking aldosterone in collecting tubules
Term
Sprinonolactone pharmacokinetics
Definition
*Slow onset of action- takes several days to see full therapeutic effect
*Inactivation of spironolactone occurs in the liver
Term
Spironolactone
Clinical Uses
Definition
***MOST IMPORTANT USE: Used with other hypertensives to allow body to HOLD ONTO POTASSIUM (since other hypertensive drugs deplete the body of potassium***

*This drug is not a 'great' diuretic

Other Uses:

1. Hyperaldosteronism/Aldosteronism: state of aldosterone (mineralocorticoid) excess

a) Conditions of Primary Hyperaldosteronism (hypersecretion):
-Conn's Syndrome
-Ectopic adrenocorticotropic hormone production

b) Conditions of Secondary Hyperaldosteronism (d/t other diseases that result in elevated aldosterone):
-Heart Failure
-Hepatic Cirrhosis
-Nephrotic Syndrome

2. Use of other types of diuretics (thiazides, loop diuretics) can lead to Hyperaldosteronism
-Spironolactone may be used in these situations to assist body to blunt/block K+ secretory response and b/c this drug is an aldactone antagonist
Term
Spironolactone
ADR
Definition
-Hyperkalemia
-Hyperchloremic Metabolic Acidosis
-Gynecomastia/impotence/BPH
-Acute Renal Failure

*Rarely used in pts w/ renal insufficiency
*Monitor closely in pts w/ liver disease
Term
Lisinopril
Definition
ACE inhibitor; ↓ angiotensin II; ↓ vasoconstriction; ↓ aldosterone secretion; ↑ bradykinin; ADRs=cough, angioedema, hyperK+, renal impairment, teratogen
Term
Hydralazine (MOA)
Definition
Used to treat hypertension and with combination of other antihypertensives to treat CHF.
Works by dialating the arterioles by releasing nitric oxide causing a decrease in vascular resistance.
Term
Hydralazine (ADR)
Definition
reflex tachycardia, angina, Lupus-like symptoms (aches/pains/skin rash/fever)
Term
Hydralazine (pharmacokinetics)
Definition
Administered orally, rapid 1st pass metabolism by liver,
Term
Nifedipine Clinical Uses
Definition
Calcium Channel blocker used to treat HTN and CP
Term
Nifedipine: Contraindications
Definition
Do not use this drug for patients in cardiogenic shock or other medications that use P450 for metabolism
Term
Nifedipine: Pharmacokinetics
Definition
Metabolized by the liver P450. First pass metabolism
Term
Nifedipine: MOA
Definition
Decreases intracellular calcium levels in cardiac and smooth muscle cells resulting in dilitation of coronary and peripheral arteries
Term
Minoxidil MOA
Definition
Vasodilator. Hyperpolarization of smooth muscle through opening of K+ channels
Term
Minoxidil uses
Definition
HTN, hair loss (rogaine)
Term
Minoxidil ADR
Definition
reflex sympathetic stimulation and Na+/fluid retention
(with inadequate doses of beta blockers and diuretics): Tachycardia, palpitation, angina, edema
(common in women): Headache, sweating, hair growth
Term
Minoxidil treatment consideration
Definition
Minoxidil causes reflex sympathetic stimulation and Na+/fluid retention so it MUST be combined with:
*Beta blocker & Loop diuretic*

Minodixil should replace hydralize when:
- Max dose of hydralize are not effective
-Renal failure or severe HTN do not respond to hydralize
Term
Verapamil MOA
Definition
Calcium Channel Blocker (Class 4 antiarrhythmic): SLOWS the SA node automaticity and AV node conduction velocity; DECREASES cardiac contractility (and CO); REDUCES blood pressure
--greater cardio than vascular effects
Term
Verapamil Clinical Uses
Definition
SVT's, HTN, Angina, CHF, Reynauds
Term
Verapamil AVR
Definition
#NAME?
Term
Losartan MOA
Definition
(ARB), angiotensin II receptor antagonist, irreversible, non-competitive. It deters vasoconstriction and aldosterone-secreting effects by specifically intercepting the binding of angiotensin II to the AT(1) receptor.
Term
Losartan Clinical uses
Definition
Hypertension, heart failure, renal protection
Term
Losartan ADR
Definition
Hypotension; (thrombocytopenia, rhabdomyolysis, and angioedema are rare).
Pregnancy category X
Term
Propranolol Class
Definition
Beta-Adrenoceptor-Blocking Agent
Term
Propranolol MOA
Definition
Non selective beta-blocker; decreases blood pressure by decreasing cardiac output; reduces chronotropic, inotropic and vasodilator responses to beta-adrenergic stimulation by competing for available binding sites that stimulate the beta-adrenergic receptors; depresses renin secretion also preventing vasodilation of cerebral arteries.
Term
Propranolol Clinical Uses
Definition
Chronic Angina, cardiac dysrhythmia, essential tremor, hypertension, migraines, postmyocardial infarction
Term
Propranolol ADR
Definition
CHF, Heart block, Stevens-Johnson Syndrome, Asthma, Bronchospasms, hypotension, bradycardia, agranulocytosis
Term
Propranolol Pharmacokinetics
Definition
Oral or IV, Metabolized in Liver, T 1/2 approx. 4 hours
Term
Spironolactone MOA
Definition
Synthetic steriod that acts as a competitive aldosterone antagonist and a weak estrogen agonist
Term
Spironolactone Adverse Reactions
Definition
Hyperkalemia, gynecomastia, impotence, benign prostatic hyperplasia (very rare), acne, decreased libido, menstrual irregularities
Term
Spironolactone Pharmacokinetics
Definition
Rather slow onset of action, requiring several days before full therapeutic effect is achieved. Substantial inactivation of spironolactone occurs in the liver.
Term
HCTZ (Hydrochlorothiazide) MOA
Definition
An Antihypertensive and diuretic that affects elecrolyte reabsorption at the distal renal tubule (thiazides) increasing sodium and chloride excretion; potassium is excreted in the distal loop of henle and stops reabsorption of water thereby increasing urine output, increasing potassium excretion, and decreasing blood pressure.
Term
HCTZ Pharmacokinetics
Definition
excreted - renal, avoid in renal failure, 1/2 life = 5-15 hrs.
Term
HCTZ Adverse -
Definition
Hypotension, dehydration, headache, muscle cramps, brisk diuresis, phototoxicity, tachycardia, vertigo, hyponatremia, hypercalciiemia, hypokalemia, hypomagnesemiam, cardia dysrhythmias, renal failure, avoid use with breastfeeding
Term
Minoxidil MOA
Definition
Opens potasium channels in smooth muscel membrains, which leads to vasodilation. The increased potassium permeability reduces contractions and dilates arteries, but not veins.
Term
Minoxidil Pharmacokinetics
Definition
Must be taken with a beta blocker and loop diuretic because of reflex sympathetic stimulation and sodium/fluid retention.
Term
Minoxidil Cinical Use
Definition
Treatment of sever hypertension for those who do not respond well to hydralazine. Also can be used to treat hair loss. (Rogaine)
Term
Minoxidil Adverse Effects
Definition
Hypotension, tachycardia, palpitations, angina, edema, and hypertrichosis (excessive hair groth).
Term
Furosemide MOA
Definition
Inhibition of the Na/K/2Cl transporter in the ascedning limb of Henle's loop. (Loop diuretic)
Term
Furosemide pharmacokinetics
Definition
Rapidly absorbed, eliminated by kidney through glomerular filtration and tubular secretion. Reductioin in the secretion of loop diuretics may be as a result of NSAIDS or probenecid which compete for weak acide secretion in the proxminal tube.
Term
Furosemide Adverse effects
Definition
ototoxicity, hypovolemia, k wasting, hyperuricemia, hypomagnesemia, skin rash,
Term
Furosemide clinical uses
Definition
Pulmonary edema, peripheral edema, hypertension, acute hypercalcemia or hyperkalemia, acute renal failure, anion overuse
Term
Nifedipine MOA
Definition
Calcium Channel Blocker of the dihydropyrines (DHP); has a greater effect on the vascular calcium channles than the cardiac calcium channels
Term
Nifedipine Pharmacokinetics
Definition
Reduces vascular resistance and this prolonged relaxation leads to vasodilation and decreased BP. Orally lasts 4-6 hours.
Term
Nifedipine Clinical Uses
Definition
hypertension, angina, prophalxis of angina, Reynauds
Term
Nifedipine Adverse Effects
Definition
constipation, peripheral edema, hypotension, baroreceptor reflex tachycardia
Term
Hydralazine MOA
Definition
causes release of nitric oxide, resulting in arterial vasodilation and a decrease in vascular resistance
Term
Hydralazine Clinical Uses
Definition
Hypertension. Hydralazine is also effective for heart failure in combination with nitrates.
Term
Hydralazine Pharmacokinetics
Definition
Rapidly metabolized by liver during first pass.
Low bioavailability (25%).
Half-life of 1.5-3hrs.
Vascular effect persists longer than blood concentration.
Term
Hydralazine ADR
Definition
tachycardia, headache, nausea, anorexia, palpitations, sweating, flushing.
Angina or ischemic arrhythmias may be provoked by reflex tachycardia and sympathetic stimulation in patients with ischemic heart disease.
Term
Losartan MOA
Definition
Angiotensin receptor blocking agent that blocks
angiotensin II type 1 (AT₁) receptors; has no effect on bradykinin so is a more
selective blocker of angiotensin effects than ACE inhibitors
Term
Losartan pharmacokinetics
Definition
Oral half-life 1-2 hours; active metabolite half-life 3-4 hours. Bioavailability
36%. No dose adjustment required in
renal insufficiency.
Term
Losartan clinical applications
Definition
hypertension and heart failure
Term
Losartan effects
Definition
Reduce angiotensin II levels which reduces vasoconstriction and aldosterone secretion. This leads to decreased peripheral vascular
resistance and decreased sodium and water retention, thus decreasing blood
pressure.
Term
Losartan adverse effects
Definition
angioedema, hyperkalemia, renal impairment, teratogenic (similar to ACE inhibitors)
Term
Lisinopril MOA
Definition
An angiotensin-converting ezyme inhibitor, reduces angiotensin II by inhibiting conversion ffrom angiotensin I to angiotensin II
Term
Lisinopril pharmacokinetics
Definition
Oral, half life is 2-4 h but given in large doses so duration is 12-24 h, the lysine analog of enalapril
Term
Lisinopril Clinical Applications
Definition
HTN, Diabetic renal disease, CHF, Acute MI
Term
Lisinopril Adverse Reactions
Definition
cough, hyperkalemia, angioneurotic edema, dark urine, decreased urine, difficlty swallowing or breathing, hoarseness, yellowing of skin and eyes,
Term
Lisinopril effects
Definition
Arteriolar and venous dilation
reduces aldosterone secretion
reduces cardiac remodeling
Term
Propranolol MOA
Definition
nonselective betablocker, highly lipid soluable, inhibits the stimulation of renin production by catecholoamines, acts on peripheral presynaptic beta adrenoceptors which will inhibit sympathetic nerve activity
Term
Propranolol effects
Definition
decreases: BP, HR, release of renin, intraoccular pressure, HDL, CNS depression, Increases: airway resistance Misc: sleep disturbances, impairs recognition and recovery of hypoglycemia
Term
Propranolol A/R
Definition
depression, impotence, fatigue, blocks s/s of hypoglycemia, abrupt withdrawl can cause miocardial ischemia
Term
Propranolol Clinical Uses
Definition
HTN, CHF, Angina, Post MI, Arrhythimias, Migraines, Situational Anxiety
Term
Propranolol Phramacokinetics
Definition
Beta blocking effects= bradycardia, and decrease in HR during exercise. Use these clinical parameters to adjust dosage. May be given BID also is available as extended slow release
Term
Verapamil
Definition
Calcium channel blocker, MOA = Inhibition of calcium influx into the arterial smooth muscle cells. More effective as a cardiac depressant vs vasodilator. Will decrease heart rate and cardiac output.
Term
Verapamil pharmaconetics
Definition
Half-life = 4 to 6 hours; Bioavailability is 22%; Suggested starting does is 180mg/d with a maintenance dose of 240-480mg/d. Renal insufficiency does not impact dosage.
Term
Lisinopril
Definition
Angiotensin-converting enzyme (ACE) inhibitor. Inhibits the converting enzyme peptidyl dipeptidase that hydrolyzes angiotensin I to angiotensin II. These drugs reduce angiotenisin II levels, reduce vasoconstriction and aldosterone secretion and increase bradykinin.
Term
Clinical uses of Lisinopril
Definition
Hypertension, heart failure, and diabetes
Term
Adverse effects of Lisinopril
Definition
Cough, severe hypotension after initial dose, angioedema, hyperkalemia, acute renal failure, and teratogenic
Term
Minoxidil
Definition
Vasodilator-decreases systemic vascular resistance d/t arterial smooth muscle relaxation. Must be given with beta bl. and loop diuretic d/t reflex sympathetic stimulation. There is an increase in renin and there for an increase in h2o and na retention. Increase in sympathetic tone leads to increase in HR, Contractility and CO. This causes increased O2 demand on heart which may lead to ischemia in patients with limited reserve. ADR: Headache, sweating, and hypertrichosis
Term
Furosemide
Definition
Works in the Loop of Henle, called a loop diuretic. These are the most commonly prescribed diuretic for HTN, CHF, Pulmonary , Hepatic or renally caused edema.
Term
Furosemide
Definition
MOA-blocks reabsorbtion of NA+ and CL- in thick segment of Loop of henle and therfore the passive reabsorption of H2O.
Term
Furosemide
Definition
ADRs- HypoNA, HypoCL, Dehydration, HypoK, hypotension, ototoxicity, hyperglycemia, increased LDLs and decreased HDLs
Term
Furosemide
Definition
Drug interactions- Digoxin- K+ loss can make it higher risk for dysrythmias, NSAIDs can interfere with prostaglandin production in kidney by decreasing the renal blood flow, Lithium- loss of Na+ can lead to toxic levels.
Term
SPIRONOLACTONE
Definition
Potassium sparing diuretic that antagonizes the effects of aldosterone, thus preventing K+ secretion. ADR: hyperkalemia, hyperchloremia metabolic acidosis, gynecomastia, acute renal failure, renal calculi. Caution use in patients with chronic kidney disease and liver impairment or also taking other medications that may increase K+ (ACEI, ARB, BB, supplements).
Term
Verapamil
Definition
Calcium-channel blocker used in HTN treatment and angina control. MOA: decrease impulse conduction through the AV node; relax smooth muscles, dilating blood vessels. Increases O2 supply to the heart and slows electrical activity, controlling heart rate. Oral absorption is high but bioavailability is low (due to first pass metabolism. Half-life is 5-12 hours. Metabolized by liver, excreted by urine. Present in human milk (discontinue use if breast feeding).
Term
Verapamil ADR
Definition
HA, facial flushing, dizziness, swelling, increased urination, galactorrhea, constipation, gingival hyperplasia.
Term
Hydralazine
Definition
An oral vasodilator that works by relaxing smooth muscle in the arterioles, thus reducing systemic vascular resistance. In particular, hydralazine dilates arterioles but no veins. Can be combined with a nitrate drug to manage heart failure. Absorbed well after PO administration. Hepatic elimination. ADR include: headache, nausea, anorexia, palpitations, sweating, and flushing. May have reflex tachycardia if pt has ischemic heart disease. Lupus like symptoms, although rare, may also occur if pts with slow drug metabolism and dosages over 400mg/day.
Term
Losartan MOA
Definition
Angiotensin receptor blocking agent (ARBs), interferes with the binding of angiotensin II to its receptor AT1, noncompetitive antagonist, more selective blocker of angiotensin effects as compared to ACE inhibitors, does not increase bradykinin
Term
Losartan Pharmacokinetics
Definition
Half life 1-2 hours, 36% bioavailability, suggested dose 50mg a day, range of doses between 25-100mg per day, do not need to adjust with renal insufficiency-the drug is renal protective
Term
Losartan Monitoring and ARB
Definition
BP (full effect in 4-6 weeks), potassium elevation, less cough, angioedema, pregnancy category X, less effective in black patients do to less renin.
Term
Losartan Clinical Use
Definition
Treat HTN and CHF
Term
Minoxidil
Definition
Vasodilator-decreases systemic vascular resistance d/t arterial smooth muscle relaxation. Must be given with beta bl. and loop diuretic d/t reflex sympathetic stimulation. There is an increase in renin and there for an increase in h2o and na retention. Increase in sympathetic tone leads to increase in HR, Contractility and CO. This causes increased O2 demand on heart which may lead to ischemia in patients with limited reserve. ADR: Headache, sweating, and hypertrichosis
Term
propanolol
Definition
Prototype B-blocker. Non-selective at B-receptors. Decrease BP by decreasing CO, slowing AV conduction, and decreasing renin release. Does not typically lower BP in normotensive patiens. Propanolol is lipophilic and can cross the BBB. Used to manage HTN, ischemic heart disease, cardiac arrythmias, heart failure (especially after MI); also hyperthyroidism, migraines, stage-fright, and glaucoma. ADRs include bradycardia, worsening of asthma/ lung conditions.
Term
HCTZ MOA
Definition
Inhibition of NA/CL transporter in distal tubules.
Term
HCTZ clinical applications
Definition
Hypertension, mild heart failure, nephrolithiasis, nephrogenic diabetes insipidus.
Term
HCTZ pharmacokinetics/toxicity
Definition
Oral, duration 8-12 hours. Hypokalemic metabolic alkalosis, hyperuricemia, hyperglycemia, hyponatremia
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