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Pharmacology Exam 4 Drugs
Antiarrhythmia, diuretics/volume reducing agents, antihypertensives, other cardiac drugs
133
Pharmacology
Professional
12/04/2009

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Term
What is vasopressin?
Definition
Antidiuretic Hormone
Term
What is the pharmacological action of Triamterene?
Definition
K-sparing, blocks Na absorbtion in cortiacal collecting duct. DIRECT.
Term
What is triamterene used for (two things)?
How long does it take the drug to act?
Definition
HT, edema, 2-4hrs to act.
Term
What are the adverse effects of Triamterene?
Definition
hyperalkemia, nausea/vomiting, cramps and dizziness
Term
What is the pharmacological action of spironolactone?
Definition
K-sparing, aldosterone cannot increase Na reabsorbtion in cortical collecting duct, leads to increased Na excretion, and decreased K excretion.
Term
What does spironolactone treat and what is the latency of the drug?
Definition
HTN, edema, primary hyperaldosteronism, Decreases mortality in heart failure, 48hrs to act
Term
What are the adverse effects of spironolactone?
Definition
Moobies and hyperalkemia
Term
Classification of Hydrochlorothiazide?
Definition
K-losing loop diuretic
Term
What is the pharmacologic action of HCTZ?
Definition
Thiazide diuretic that blocks Na Cl co-transporter in the distal tubule
Term
What is HCTZ used for primarily?
Other uses?
Definition
Primary hypertension, Decrease the risk of kidney stones, Used in combination with K+ sparing diuretics to mitigate K loss. Used in mild-moderate HTN (low renin or volume-expanded forms)
Term
Can HCTZ be used for Renal failure?
Definition
Yeah, but it does not work very well.
Term
What are the risks of HCTZ?
Definition
Gout, oops too much, Increased lipid levels, HYPOalkemia
Term
Is HCTZ appropriate for monotherapy?
Definition
Not recommended, Best if in combination to prevent adverse effects.
Term
Can HCTZ be used in pregnancy?
Definition
Contraindicated in pregnancy
Term
What are the effects of HCTZ on digoxin and litium?
Definition
Increases effects of Digoxin and litium toxicity
Term
What is the classification of Furosemide, bumetadine, and torsemide?
Definition
K losing loop diuretic
Term
What is the use of furosemide, bumetadine, and torsemide and what is the duration of onset of action?
Definition
Quick, 60 minutes po, 5 minutes if IV. edema, hypertension
Term
What is the mechanism of action of Furosemide, bumetadine, and torsemide?
Definition
Na-K-Cl cotransporter blocker, blocks cotransporter in TAL.
Term
What is the classification of Triamterene?
Definition
Na Channel Blocker
Term
What is the classification of spironolactone?
Definition
Aldosterone Antagonist
Term
What is the drug class of ethacrynic acid?
Definition
K losing loop diuretic
Term
What is the duration of the onset of action for ethacrynic acid?
Definition
Quick onset, 60 min po, 5 min IV,
Term
What is ethacrynic acid used for?
Definition
Edema and HTN
Term
What are the contraindications and drug interactions of ethacrynic acid?
Definition
Contraindicated in pregnancy, Drug interaction with digoxin and lithium
Term
Why is ethacrynic acid particularly useful?
Definition
It can be used in patients with SULFA ALLERGY.
Term
What is the classification of acetazolamide?
Definition
Carbonic anhydrase inhibitor
Term
What is pharmacologic action of acetazolamide?
Definition
It is seldomly used for sodium bicarbonate diuresis,and HYPERchloremic acidosis.
Term
What is acetazolamide used for?
Definition
Treats urinary alkalinazation, metabolic alkalosis, glaucoma, and mountain sickness
Term
What are the risks of ethacrynic acid?
Definition
Higher risk of kidney stones, oops too much, HYPOkalemia, OTOTOXICITY, gout risk, increased lipid levels
Term
What are the adverse effects of acetazolamide?
Definition
Renal stones, potassium wasting, and HYPERchloremic acidosis.
Term
What are the osmotic diuretics?
Definition
Mannitol, Urea, glycerine, isosorbide
Term
What are osmotic diuretics used for?
Definition
decrease intracranial pressure, prophylaxis of renal failure, decreases intraoccular pressure in glaucoma
Term
What is the pharmacologic action of osmotic diuretics (urea, glycerin, mannitol, isosorbide)?
Definition
These are non-reabsorbale solutes that keep water in the proximal tubules-> distal -> urine
Term
How is osmotic diuretics administered and what is the onset of action?
Definition
Administered via IV in large volumes and has an onset of action of 30min to an hour.
Term
What are the risks of administering osmotic diuretics?
Definition
Large volume of administration can exacerbate patients with heart failure as well as cause electrolyte imbalance. Nausea/vomiting/headache
Term
What drug class are the vaptans?
Definition
ADH receptor antagonist
Term
What is the pharm action of the vaptans?
Definition
Vaptans prevent water absorption by the collecting ducts, thereby decreasing the urine osmolality, and decrease plasma volume. There is also an increase in plasma osmolality via increase in plasma
Term
Are there any adverse effects of vaptans and how is it administered?
Definition
Vaptans are administered IV only and are generally well tolerated.
Term
What drug class are "-pril" drugs?
(enalapril, captopril, lisinopril)
Definition
ACE Inhibitors
Term
What is the action of ACE inhibitors? (enalapril, lisinopril, captopril)
Definition
ACE Inhibitors LOWER ANGIOTENSIN 2 levels by working on renin-angiotensin.
Term
What are ace-i used for?
Definition
CHF, arrhythmias, diabetes mellitus, BEST FOR PATIENTS WITH ASTHMA!
GREAT FOR MONOTHERAPY!
ENHANCED BY DIURETICE
Term
What effect does diuretics have on ACE-I?
Definition
DIURETICS enhance the effect of the ACE-I.
Term
What are the contraindications for Ace-INhibitors? (enalapril, lisinopril, and captopril)
Definition
Contraindicated in pregnancy
Term
Are ACE inhibitors good for high renin HTN?
Definition
Best in high renin HT.
Term
What are the side effects of ACE inhibitors (Enalapril, lisinopril, and captopril)?
Definition
Increases bradykinin, but is otherwise well tolerated. rash, neutropenia ANGIONEURONIC EDEMA swells shut throat
Term
Which ACE inhibitor effects taste?
Definition
Captopril
Term
What are the sartans?
Definition
they are Angiotensin II Receptor Blockers
Term
What is the pharmacologic action of the sartans?
Definition
Reduces release of aldosterone by blocking the angiotensin receptors
(works on renin-angiotensin)
Term
What are sartans used for?
Definition
Sartans are used for hypertension, heart failure, and prevention of re-stenosis following angioplasty (rare).
Term
What are the benefits of sartans?
Definition
NO BRADYKININ effects (coughing?)
Term
What are the classifications of -olol's?
Definition
They are B blockers, note: labetAlol is alpha also.
Term
Which are the selective B blockers
Definition
Metoprolol, atenolol, acebutolol
Term
What are the side effects of sartans?
Definition
Dizziness, myalgia, GI effects, congestion.
Term
What are the indications of sartans?
Definition
as with ACE I's, except with angioedema due to ACE-I's.
Term
Which B blocker can also have action at alpha receptors?
Definition
Labet"A"lol
Term
What is the pharmacological action of sartans (Beta blockers)?
Definition
Works on renin-angiotensin to inhibit renin release, -cardiac output, -renin release, -sympathetic outflow
Term
What is the cariological effect of -olol's?
Definition
decrease cardiac output
Term
How does -olo's effect renin?
Definition
inhibition (decreased) renin release
Term
What is the neurological effect of olol's?
Definition
inhibition of sympathetic outflow
Term
How can olol's be used?
(therapy, type of htn)
Definition
monotherapy, best with high renin HTN
Term
When is Labetalol used?
Definition
During high crisis HTN. Reduce the need for nitroglycerin and not for spastic angina (stable only).
Term
What is the purpose of the antiarrythmic effect of beta blockers?
Definition
prevention of MI
Term
What is the relationship of olol's with asthma patients?
Definition
Bad for asthma PTs. Worsening of peripheral vascular disease, heart block, hypoglycemia. Angina attack after abrubt withdrawl. GI and CNS. Sexual dysfxn.
Term
What are the adverse effects of beta blockers?
Definition
Worsens peripheral vascular disease, heart block, HYPOglycemia, GI and CNS effects, sexual dysfunctions.
Term
What is the effect of abrupt withdrawal of beta blockers?
Definition
Angina attack
Term
What is the classification of Ranolazine?
Definition
Inhibition of the late sodium current
Term
What are the side effects of ranolazine?
Definition
arrythmias, n/v, weakness, palpataions, dizziness.
Term
What is the classificaiton of -amines?
Definition
NON-selective alpha blockers
Term
What is the pharmacological effect of -amines?
Definition
Blockade of vascular alpha receptors.
Term
What is the therapeutic use of -amines?
Definition
Hypertension crisis in pheochromocytoma (rare situation)
Term
What are the adverse effects of -amines?
Definition
Postural HYPOtension, reflex tachycardia, FLUID RETENTION (may require diuretic)
Term
What is the classification of -zosin?
Definition
Selective alpha blocker
Term
What is the use for -zosin's?
Definition
Blockade of vascular alpha receptor
Term
What is the pharmacological indication (use) for -zosin's?
Definition
Used for monotherapy and adjunctive therapy of hypertension.
Term
What is the adverse effects of -zosin's?
Definition
FIRST DOSE EFFECTS, TACHYCARDIA, nasal, dry mouth, and GI.
Term
What is the classification of aliskiren?
Definition
Renin inhibitors
Term
What is the pharmacological effect of aliskiren?
Definition
POOR PO ABSORPTION, works on renin-angiotensin.
Term
What is the therapeutic use for aliskerin?
Definition
HTN adjunct therapy
Term
What are the adverse effects of aliskerin?
Definition
NO BRADYKININ EFFECT.
HYPERkalemia
dizziness and diarrhea
Term
What are the contraindication of aliskerin?
Definition
NOT FOR USE IN PREGNANCY or bilateral stenosis
Term
What is the classification of nifedipine?
Definition
Calcium channel blockers of the L type
Term
How effective is nifedipine in vasodilation relative to other ca channel blockers (diltiazem and verapamil)?
Definition
It is the MOST POTENT
Term
What is the pharmacology of nifedipine?
Definition
Dihydropyiridine
Term
What is the therapeutical use for nifedipine?
Definition
initial choice for mild to moderate HT. Given IV in HYPERTENSIVE EMERGENCIES.
Term
What are the adverse effects of nifedipine?
Definition
Nifedipine causes flushing, headache, and edemas. There is also increased risk of cardiac events in short-acting drugs.
Term
What are therapeutic use for L-type calcium channel blockers?
Definition
Treat angina, paroximal tachycardia, atrial flutter, fibrilation, and essential HTN
Term
What are the L-type Calcium channel blockers?
Definition
Verapamil, nifedipine, and diltiazem.
Term
What is the structural classification of verapamil?
Definition
phenylalkylamine
Term
What is the mechanism of action of L-type calcium channel blockers?
Definition
They treat angina, proximal tachycardia, atrial flutter, fibrilation, and essential HTN.
Term
What is the structural pharmacology of diltiazem?
Definition
benzothiazepine
Term
How effective is diltiazem in comparison to the verapamil and nifedipine?
Definition
Diltiazem is the least potent of the CCB's. (nifedipine>verapamil>diltiazem)
Term
What is the therapeutic use for verapamil and diltiazem?
Definition
SLOWS SA NODE!
LACKS Reflex TACHY.
Most useful in low renin HTN, blacks and elderly.
NO FLUID RETENTION.
Ca channel blocker for arrythmia
Class IV
Term
What are the adverse effects of verapamil and diltiazem?
Definition
Flushing, headache, edemas and bradychardia, AV node conduction defects, risk of cardiac events in short-acting drugs.
Term
What pharmacological action of minodixil?
Definition
potassium channel activator
Term
How is minodixil administered?
Definition
Used ONLY IN COMBO therapy orally
Term
What are the adverse effects of minodixil?
Definition
Fluid retention, tachycardia, increased cardiac output which leads to CHF, pericardial effusions, hypertrichosis.
Term
What is the pharmacological action of guanethidine?
Definition
K channel Activator
Term
How is guanethidine administered? i.e. monotherapy, combination
Definition
IN COMBINATION ONLY
Term
What is the pharmacological action of diazoxide?
Definition
K channel activator
Term
What three drugs are K channel activators?
Definition
diazoxide, guanethidine, and minodixil
Term
What is the pharmacological action of hydrALAZine?
Definition
ACTIVATES NO/guanylate cyclase pathway.
Term
What are the therapeutic uses of hydrALAzine?
Definition
ONLY IN COMBINATION, for HTN emergencies.
available po and IV
Term
What are the adverse effects of hydrALAZine?
Definition
tachycardia, palpitations, HYPOtension, n/v, Lupus-like syndrome, and edema
Term
How is nitroprusside administered and why?
Definition
IV in EMERGENCY ONLY!
Term
What is the pharmacologic action of nitroprusside?
Definition
Activation of NO/guanylate cyclase pathway
Term
What are the adverse effects of nitroprusside?
Definition
sweating, tachycardia, nausea, psychosis, formation of cyanate ion
Term
What is the pharmacologic action of epoprostenol / prostacyclin / PGI2?
Definition
IP prostanoid receptor agonist, short acting potent vasodilator.
Term
What is the therapeutic use for epoprostenol/prostacyclin/PGI2?
Definition
IV for pulmonary HT.
Term
What is the pharmcological action of bosentan?
Definition
nonselective alpha/beta endothelin receptor antagonist
Term
How is bosentan administered and what for?
Definition
Oral admin for pulmonary HTN
Term
What is the adverse effect of bosentan?
Definition
oral toxicity
Term
What is the contraindication for bosentan?
Definition
contraindicated in pregnancy
Term
What is the pharmacological action of sildenafil?
Definition
PDE5 inhibition
inhibits cGMP--> GMP
Term
What is the therapeutic use for sildenafil?
Definition
erectile dysfunction
Term
What are the adverse effects of sildenafil?
Definition
dyspepsia, headache, and dizziness
Term
What is the pharmacologic action of fenoldopam?
Definition
D1 dopamine receptor agonists
Increase renal blood flow,
Decrease blood pressure,
SHORT T1/2
Term
What is the therapeutic use for fenoldopam?
Definition
IV emergency HTN situations
Term
What is the pharmacological action of nitroglycerin?
Definition
Activation of NO/ guanylate cyclase pathway.
***Only 10% SURVIVE 1ST PASS METABOLISM
Term
When is nitroglycerin used?
Definition
HTN emergencies
Term
What are the side effects of nitroglycerin?
Definition
HYPOtension, vasodilation, REFLEX TACHYCARDIA
Term
What are the adverse effects of isosorbides (mono and dinitrates)?
Definition
HYPOtension, vasodilation, REFLEX TACHYCARDIA
Term
What is the pharmacological action of alpha methyldopa?
Definition
Alpha-2 agonist
Vasodilation and decrease in heart rate by reducing sympathetic tone
Term
How is alpha methyldopa activated?
Definition
PRODRUG converted to alpha-methylnorepinephrine
Term
How frequently is a-methyldopa used?
Definition
not used often or alone. Old drugs.
Term
What is the mechanism of action of a-methyldopa, clonidine, guanabenz, and guanafacine and the resulting effects?
Definition
IV: smooth muscle vascular a2 receptors open Ca2+ channels causing vasoconstriction. This leads to HYPOtension, sedation, withdrawal syndrome (HTN, Tachy, nervousness, excitement), Dry mouth, stuffiness, contact dermatitis, vivid dreams, restlessness, depression, and rebound HTN.
Term
What is the pharmacological action of clonidine?
Definition
Alpha 2 agonist
Vasodilation and decrease in HR due to reduction in sympathetic tone
Term
What are the alpha-2 agonists that induce vasodilation and decrease in HR by reducing sympathetic tone? Which is a prodrug**?
Definition
a-methyldopa**
guanafacine, guanabenz, clonidine
Term
What is the classification of resperine?
Definition
depleting drug: deplete Norepinephrine from nerve terminals and adrenal medulla
Term
What is the therapeutic use of resperine?
Definition
Hardly any, not used very much, Increases catecholamine sensitivity (i.e. epinephrine)
Term
What is the adverse effect of resperine?
Definition
diarrhea, stuffiness, nausea, nightmares, sedation, fluid retention, decreases libido, tremors, arrhythmia, depression
Term
What is the pharmacological action of guanethadine and guanadrel?
Definition
depleting drug: deplete Norepinephrine from nerve terminals and adrenal medulla
Term
What is the therapuetic use for guanethadine and guanadrel?
Definition
Cant cross BBB
Term
When are Depleting drugs used? guanethadine, guanadrel, and resperine?
Definition
Hardly any, not used very much, Increases catecholamine sensitivity (i.e. epinephrine)
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