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89 Cards in this Set
- Front
- Back
Describe the etiology and tx of Classic "Angina of effort"
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Obstruction, esp with exercise
Drugs or surgery |
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Describe the etiology and tx of Variable/Prinzmetal's Angina
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Spasm or VC
Reversed by nitrates or CCBs |
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O2 demand depends on (3):
Wall tension changed by (2): |
Cardiac workload = HR, contractility, and wall tension
Pressure and volume |
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Coronary blood flow is proportional to (2):
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Perfusion pressure and duration of diastole
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How do antianginal drugs work (2)?
Why is increasing 02 supply inefficient for tx of angina? |
Increase 02 supply
Decrease 02 demand "Coronary steal" phenomenon |
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Which drug classes improve the regional flow distribution to the heart (02 supply)? {3 classes}
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Nitrates, CCBs, BBs
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Which drug classes improve coronary blood flow (02 supply)? {2 classes}
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Nitrates, CCBs
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Which drug classes decrease HR & contractility (02 demand)? {2 classes}
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Some CCBs, BBs
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Which drug classes decrease preload (02 demand)? {1 class}
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Nitrates
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Which drug classes decrease afterload (02 demand)? {1 class}
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CCBs
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Which are the 3 fastest acting nitrates?
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Inhaled amyl nitrite
IV nitroprusside (risk of cyanide poisoning) Sublingual nitroglycerin (bypasses first pass metab) |
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Nitroglycerin & Isosorbide dinitrate
Biochem Mech |
Causes VD by releasing nitrite ion, which is metab to NO, which activates GC, which increases cGMP
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VD by nitrates is uneven. Describe how.
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Large veins are markedly dilated and decrease preload.
Small arterioles are less dilated and decrease afterload. Either way, you still get decreased 02 demand. |
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What are the two general relief mechanisms of nitro tx?
Does total coronary blood flow change? |
Predominant relief mech: decrease 02 demand
Secondary relief mech: redistribution of coronary bloff flow No |
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What other parts of the body will nitro affect (3)?
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Any smooth mm: bronchi, GI, GU.
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What does sodium nitrite have to do with cyanide?
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Sodium nitrite is used to induce methemoglobin formation for tx of cyanide poisoning.
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Nitro drugs
Adverse Effects (3) |
Acute toxicity = marked hypotension, HA, tachycardia
Can result in tolerance Can result in Monday disease. |
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What is Monday Disease?
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Refers to workers who are chronically exposed to high nitrate levels. Their tolerance drops over the weekend, and they experience toxicity sxs on Monday back at work.
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Name the 6 important CCBs for angina tx.
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Verapamil
Diltiazem "- dipines"/dihydropyridines - Nifedipine - Nimodipine - Isradipine - Amlodipine/Norvasc |
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What is the mech of CCBs?
What are the two effects relating to the tx of angina? |
Bind L-type CCs on sm mm.
Decreases cardiac contractility, automaticity, conduction and also causes long-term vasc VD. |
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What two roles does IC Ca play?
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Triggers muscle contraction in myocardium & vasc sm mm
Required for pacemaker activity (SA & AV node) Will also relax other sm mm to lesser extent. |
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In heart and vasc sm mm, what opens Ca channels?
Then, what drug closes them? |
Beta rec stim opens them.
CCBs (duh) |
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Which blood vessels are most sensitive to CCB VD?
Which drug has the greatest impact on arteriolar VD? Which drug has the greatest impact on venous VD? |
Arterioles
CCBs Nitrites |
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Which drugs don't affect venous dilation at all, but have some effect on arteriolar VD?
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Hydralazine and Minoxidil
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What are the three prototypes for CCBs? Compare them.
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Verapamil - strongest cardiac effects (Depress automaticity)
Nifedipine - strongest VD & reflex tachycardia inducer. Also, diff type: dihydropyridine. diltiazem - inbetween. |
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nifedipine
Drug Class: How can it cause MI? General Adverse Effect of CCBs: |
CCB
Causes rapid hypotension, reflex tachycardia. Hyperglycemia & decreased platelet aggregation |
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Verapamil, Diltiazem
Drug Class: Main Adverse Effect: General Adverse Effect of CCBs: Contraindications: |
CCB
Might cause serious cardiac depression through SA/AV node effects Hyperglycemia & decreased platelet aggregation GF inhibits P450 = verapamil toxicity |
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What do Beta Blockers do for angina (2)?
What do Beta Blockers NOT do, ever? |
Decrease SNS = less 02 demand.
Resulting bradycardia increases coronary perfusion time They never produce coronary VD! |
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Beta Blockers
Adverse Effects (4): Which angina do you NOT use Beta Blockers for? |
Bronchoconstriction
Hyperlipidemia Mask hypoglycemia CNS effects Do NOT use them for Variant/Prinzmetal's angina: slows HR, prolongs ejection time, increases LV end-diastolic volume = increased O2 demand. |
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List the 3 PDE5 inhibitors
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sildenafil
vardenefil taladaifil |
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What were PDE5I's first developed for?
What else do they treat, besides ED? |
Tx of angina
Tx of pulmonary HTN |
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Sildenafil
Drug Class: Mech: Why might someone have vision troubles using sildenafil? |
PDE5I
Selective inhibition of cGMP specific PDE, increasing NO release. Somewhat selective for retina-specific PDE6 |
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Sildenafil
PHKs: Interactions: Contraindications: |
Oral: well abs, rapid action
t1/2: 4 hrs P450 3A4 metab Do NOT use with nitro tx, alpha blockers, or 3A4 inhibitors = severe hypotension. NOT for use in children or pregnant women. |
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Vardenifil
Drug Class: How is it different from sildenafil (2)? |
PDE5I
More selective for PDE5, so less visual side effects. Also achieves maximum plasma concentration sooner. Gets the pt into the action faster. |
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Tadalafil (Hey, honey! Ta-da!!!)
Drug Class: How is it different from sildenafil (3)? |
PDE5I
Longer duration: 24-36 hrs Allows for more sexual sponteneity Zero visual disturbances |
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Ranolazine
Drug Class: Mechs (3): Use: |
None mentioned
PFox inhibitor Inhibits late inward Na current Decreases LV stiffness Tx of chronic, stable angina as a last resort |
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Ranolazine
PHKs (3): May cause: |
Oral: 73% bioavail
RExc P450 metab - so lots of interactions expected TdP |
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Bosentan
Drug Class: Mech: Use: Adverse Effects: |
Endothelin rec antagonist
Competitive antagonist for both Type A & B recs Orally, and only for severe pulm HTN P450 rxns, teratogenic |
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What are the two tx goals for angina?
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Increase exercise tolerance
Decrease frequency of attacks |
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List three common drug combos for the tx of angina
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BBs & CCBs
2 CCBs Nitrates & BB or CCBs to decrease reflex tachycardia. |
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What are endothelins?
So, then, what is an example of an endothelin rec inhibitor? |
Peptides that counter NO = VC
Bosentan = VD |
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If your patient has X, tx with ?:
Asthma: DM: HF: HTN: Ulcer: |
Asthma: CCB, NO
DM: CCB, NO HF: NO HTN: BB, CCB Ulcer: BB, NO |
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Which anti-HTNs work at the VMC (2)?
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Clonodine
Methyldopa |
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Which anti-HTNs work at the SNS nerves (2)?
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Reserpine
guanethidine |
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Which anti-HTNs work at the a-recs in blood vessels (1)?
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The "-sins"
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Which anti-HTNs work at the beta-recs in the heart (1)?
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The Beta Blockers - "-olols"
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Which anti-HTNs work at the vasc sm mm and/or cause VD (8)?
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VDs: hydralazine, minoxidil, diazoxide, nitroprusside (VD both arteries & veins)
CCBs: verapamil, diltiazem, "-dipines" D1 rec agonist: fenoldopam |
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Which anti-HTNs work at the kidneys (1)?
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Diuretics
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What does the poly pill consist of (6 drugs)? [tx of FATBAS-tards]
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Folic acid, Aspirin, Thiazides, BBs, ACEIs, Statins
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If your pt is over 65 and has HTN, what do you treat with?
What do you NOT treat with? |
Diuretics, ACEIs, CCBs
(Central acting a-agonist) |
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If your pt is African American and has HTN, what do you treat with?
What do you NOT treat with? |
Diuretics, CCBs
(BBs) |
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If your pt is pregnant and has HTN, what do you treat with?
What do you NOT treat with? |
Methyldopa, labetalol
(ACEI, ARB) |
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If your pt has angina pectoris and has HTN, what do you treat with?
What do you NOT treat with? |
BBs, CCBs
(Central acting a-agonist) |
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If your pt has had an MI and has HTN, what do you treat with?
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BB, ACEI, aldosterone antagonist
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If your pt has CHF and has HTN, what do you treat with?
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Diuretic, ACEI, ARB, BB
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If your pt has asthma and has HTN, what do you treat with?
What do you NOT treat with? |
CCB, ACEI
(Never BB) |
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How do diuretics tx HTN (2)?
Which thiazide is a VD? |
Acutely, they reduce body Na stores, reducing blood volume.
After 6-8 wks, they activate K channels, causing a decrease in periph resistance. Indapamide |
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Thiazides are most effective in what population?
Which diuretic is the 1st choice for HTN tx? |
Old, black men.
Thiazides |
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List the 6 subtypes of sympatholytics used in HTN.
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Central agonists
Ganglion Blockers Neuron Blockers a1 Blockers BBs Combined a & Beta Blockers |
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Clonodine & Methyldopa
Drug Class: Mech (2): Contraindications (2): |
Central a-agonists
Act on a2 recs in brain medulla to decrease SNS tone. Also results in decreased renin. Do NOT use with TCAs or yohimbine |
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Clonodine and Methyldopa both have a risk of severe side effects. What are they?
Which one is a prodrug? |
Clonodine: sudden w/d causes severe hypotension
Methyldopa: may cause hemolytic anemia with + Coomb's test. Prodrug. |
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How can clonodine be administered?
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Orally or transdermally. Don't sit in a hot tub with a clonodine patch on - will pass out.
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Mecamylamine
Drug Class: Class action: Used for: |
Only Ganglion Blocker we need to know.
Complete blockade of PNS & SNS. Bad juju. Not used much due to bad side effects, but this one is being used for tx of Tourette's (Fuck! ASS! Get me a beer!) |
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Guanethidine
Drug Class: Mech: Adverse Effect with IV admin: |
Adrenergic Neuron Blocker
Replaces NE in the vesicles, inhibiting NE release. HTN crisis, esp in pheochromocytoma. |
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What does guanethidine have to do with sex?
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May cause retrograde ejaculation. (along with postural hypotension, diarrhea, fluid retention)
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Reserpine/AKA:
Drug Class: Mech: Contraindications (1): |
Reserpine = the "Dirty Drug"
Adrenergic Neuron Blocker Called "dirty" because it eliminates SNS tone via inhibition of NE transport into vesicle. Serious rx with MAOIs because released NE needs to be metab by MAO. |
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Prazosin (terazosin, doxazosin)
Drug Class: Mech: Huge benefit: |
a1 Blockers
a1 block reduces NE - causes VD of BOTH arteries & veins a1 selection means less reflex tachycardia |
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Prazosin
Adverse Effects (2): Lack of adverse effect (1): |
First-dose phenomenon: hypotension, syncope
Increased renin (& Na & H2O retention) NO hyperlipidemia, though. |
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BBS and HTN
Mechs (3): BBs are more effective for tx of HTN in: |
Heart: reduce CO
Kidney: reduce renin CNS: reduce SNS tone Young white people. |
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Why would you add other HTN drugs to BB tx (2)?
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Reduce reflex tachycardia from extreme VD
Counteract increase in renin |
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Nebivolol
Drug Class: Other Mech: |
BB
Increases prod of NO = periph VD |
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BB
Adverse Effects (3) |
Hyperlipidemia + low HDL = atherosclerosis
Mask hypoglycemia Increase exercise tol for angina pts but decrease for CHF pts |
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BB
Contraindicated conditions (4) Preferred for (3) |
DM
CHF Cardiac Blocks Asthma angina, p MI, migraines |
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Labetalol & Carvedilol
Drug Class: Other details (3): |
Combined a & Beta Blockers = lowered BP
Labetolol is OK in pregnancy but is usually only used in emergencies. They can be hepatotoxic. May cause bronchospasm. |
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Hydralazine
Drug Class: Administration: Mechs (2): Adverse Effects (2): |
VD
Oral Selectively dilates arteries Also increases NO prod SLE in slow acetylators May cause angina due to reflex tachycardia |
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Minoxidil
Drug Class: Administration: Mech: Adverse Effects: Is also a: |
VD
Oral Selectively dilates arteries Hypertrichosis May cause angina due to reflex tachycardia K channel blocker |
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Name two HTN drugs that also act through NO
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Hydralazine
Sodium Nitroprusside |
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What combo HTN tx is incredibly effective in the African American population?
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Hydralazine & isosorbide dinitrate
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Sodium nitroprusside
Drug Class: Administration: Adverse Effects (2): Mech: |
VD
IV Like NO, rapid. Cyanide accum. & metab acidosis |
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Diazoxide
Drug Class: Administration: Mech: Is also a: Also causes: |
VD
IV Activates ATP K channels Non-diuretic thiazide with long duration of action 24-36 hrs Excessive hair growth |
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Fenoldopam
Drug Classes: Administration: Mech: |
VD, D1 rec agonist
IV Stims relax of sm smm. t1/2 = 5 mins |
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What drugs cause gingival hyperplasia (3)?
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"-dipines" (CCBs)
phenytoin cyclosporine |
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What is the most common adverse effect of verapamil?
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Constipation
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How do you tx long term HTN with VDs?
Acute? |
Oral VDs
IV VDs |
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Captopril & Enalapril
Drug Class: Mech: |
ACEI
ACE converts AngI to AngII. When blocked = VD. Also destroys bradykinin, so inhibit = enough bradykinin. |
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Why would you use ACEIs for HTN?
Most effective for who? |
Fewer side effects: no cardiac, CNS, or renal compromise.
Young white people. |
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ACEIs
More benefits (2): Adverse Effects (3): |
Well abs/excreted.
Enhances anti-HTN efficacy of other drugs. Severe hypotension in hypovolemic pts Acute renal failure in stenosis Bad for 2nd & 3rd trimester of preg May cause coughing & angioedema |
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Losartan
Drug Class: Selective for: Better because (2): |
Angiotensin rec Blocker
AT1 recs Reduce mortality better than atenolol No coughing or angioedema like ACEIs |
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Aliskren
Drug Class: Blocks: Contraindicated in: |
Renin inhibitor
Formation of AngI Pregnancy |