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Pharmacology II > HTN > Flashcards

HTN Flashcards

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1
Q

Thiazide Diuretic drugs?

A

HCTZ
Chlorthalidone
Metolzaone

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2
Q

Thiazide Diuretic MOA?

A

Inhibits sodium reabsorption in the distal tubule.

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3
Q

Thiazide Diuretic Adverse Effects?

A

– Orthostatic Hypotension

– Electrolyte abnormalities: ↓ K, ↓ Na, ↑ Ca, ↑ uric acid, ↑ glucose

– Photosensitivity

– Increase urination (initially)

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4
Q

Thiazide Diuretic Precautions?

A

– Caution in sulfa allergic patients

– Ineffective in patients with severe renal disease

– Avoid in patients taking lithium– may increase serum lithium concentrations

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5
Q

Loop Diuretics Drugs?

A

– Furosemide (Lasix™)
– Bumetanide (Bumex™)
– Torsemide (Demadex™)

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6
Q

Loop Diuretics MOA?

A

– Inhibits active transport of sodium, chloride and potassium in thick ascending limb of Loop of Henle, causing excretion of these ions

– Collecting duct excretes more water in response

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7
Q

Loop Diuretics Place in Therapy?

A

– CHF (preferred diuretic)
– Edema (both peripheral and pulmonary)
– HTN

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8
Q

Loop Diuretics Adverse effects?

A

– Electrolytes abnormalities: ↓ K, ↓Na, ↓ Ca, ↓ Mg, ↑ uric acid

– Dehydration

– Ototoxicity

– Increase in SCr

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9
Q

Loop Diuretics Precautions?

A

– Caution in sulfa allergic patients

– Nephrotoxicity

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10
Q

Potassium Sparing Drugs?

A

– Triamterene

– Amiloride

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11
Q

Potassium Sparing MOA?

A

– blocks sodium reabsorption and potassium excretion, effect independent of aldosterone

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12
Q

Potassium Sparing Place in Therapy?

A

– Hypertension, often in combination with thiazide

– Spironolactone – Class IV heart failure

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13
Q

Potassium Sparing Adverse effects?

A

– General: Hyperkalemia (caution in patients with renal failure)

– Spironolactone: Gynecomastia, menstrual irregularities

– Eplerenone: More selective thus less side effects

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14
Q

Aldoesterone Receptor Blockers?

A

– Spironolactone (Aldactone™)

– Eplerenone (Inspra)

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15
Q

Aldoesterone Receptor Blockers MOA?

A

• Competes with aldosterone, prevents sodium reabsorption and potassium excretion

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16
Q

ACE Inhibitors Drugs?

A
  • Benazepril (Lotensin)
  • Captopril (Capoten)
  • Enalapril (Vasotec)
  • Fosinopril (Monopril)
  • Lisinopril (Zestril, Prinivil)
  • Moexipril (Univasc)
  • Perindopril (Aceon)
  • Quinapril (Accupril)
  • Ramipril (Altace)
  • Trandolapril (Mavik)
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17
Q

ACE Inhibitors MOA?

A

• Inhibits ACE to block production of AT II

• Inhibits breakdown of bradykinin (vasodilator)
– Benefit: lowers blood pressure
– Disadvantage: inflammatory mediator, probably some common adverse effect of ACE-I

• Dilate the efferent arteriole of kidney

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18
Q

ACE Inhibitors Place in Therapy?

A

– HTN
– CKD
– CHF

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19
Q

ACE Inhibitors Monitor?

A

– Serum K+ & SCr within 4 weeks of initiation or dose increase. You will likely see a benign increase in Scr (<30% from baseline)

– Angioedemia

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20
Q

ACE Inhibitors Adverse effects?

A

– Cough
– Angioedema (rare)
– Hyperkalemia: particularly in patients with CKD or DM

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21
Q

ACE Inhibitors Contraindications?

A

– Pregnancy
– Angioedema
– Renal artery stenosis

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22
Q

ACE Inhibitors Drug interactions?

A

– Potassium supplements
– Potassium-sparing diuretics
– NSAIDs

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23
Q

ACE-I Clinical Differences?

A

• All can be dosed once daily except captopril
– Captopril is dosed twice to three times daily & absorption decreased by 30-40% when given with food

• Enalapril is a prodrug of enalaprilat (only one that is available IV)

• Most commonly used ACE-I: Lisinopril
– Dose is 10-40 mg daily

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24
Q

ARBs Drugs?

A
  • Candesartan (Atacand)
  • Eprosartan (Teveten)
  • Irbesartan (Avapro)
  • Losartan (Cozaar)
  • Olmesartan (Benicar)
  • Telmisartan (Micardis)
  • Valsartan (Diovan)
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25
ARBs MOA?
– Inhibits angiotensin II at its receptor sites | – Does NOT inhibit the breakdown of bradykinin
26
ARBs Place in Therapy?
– One of the first line drug classes in HTN – First line option for CKD – Used in CHF
27
ARBs Dose?
Often once daily
28
ARBs Monitoring?
– Potassium | – Angioedema
29
ARBs Adverse effects?
``` – Hypotension/orthostatic hypotension – Angioedema – Hyperkalemia – Dizziness – Cough (only case reports) ```
30
ARBs Contraindications?
– Pregnancy – “Caution” in pts with renal artery stenosis – ARBs CAN be used in patients who have experienced angioedema when taking an ACE inhibitor- but use caution.
31
ARBs Drug interactions?
– Potassium supplements – Potassium-sparing diuretics – NSAIDs
32
Renin inhibitor- Aliskiren?
* First oral agent that directly inhibits renin * Role in treatment of hypertension is unclear as it is a new agent * Can be used as monotherapy or in combination * ADRs are similar to ACE inhibitors; and similar to ACE inhibitors, this drug should not be used in pregnancy
33
Beta-Blocker drugs?
– Atenolol: once a day – Metoprolol Succinate: Once a day – Metoprolol Tartrate: Twice a day
34
Beta-Blocker Dose?
Depends on the beta-blocker
35
Beta-Blocker Place in Therapy?
Not a first line
36
Who are Beta-Blocker used for?
Reserved for patients that have significant cardiac history: – Heart failure – Post-MI – High coronary artery disease – CKD
37
Beta-Blocker MOA?
– Beta-1 receptors; located in heart and beta-2 receptors are located in the lungs – Beta-blockers block beta-1 receptors thus decreasing the effects of epinephrine, and nor-epinephrine which therefore decrease BP and HR
38
Beta-Blocker differences?
•Cardioselectivity (dose-dependent): – AMEBBA: Atenolol, metoprolol, esmolol, bisoprolol, betaxaolol, acebutolol •Mixed α and β blockers: – Carvedilol and labetalol •ISA (intrinsic sympathomimetic activity): – CAPP: (Carteolol, acebutolol, penbutolol, and pindolol) •Non-Specific: – Nadolol, propranolol, timolol
39
Beta-Blocker Common Adverse Effects?
– Initial: “Beta-blocker blues”: tired, fatigued, depressed, and their chest might feel “different” due to change in heart beat – Other: Sexual dysfunction, rebound HTN if suddenly discontinued
40
Relative contraindications to beta-blockers?
– Asthma and COPD (bronchospasm) – Diabetes (masks hypoglycemic response except sweating) – Severe peripheral vascular disease (decreased output can worsen symptoms) – Heart block – Severe acute heart failure – Pregnancy category C
41
One other beta blockers?
•Sotalol (Betapace) | – Class III anti-arrhythmic agent
42
CCBs types?
TWO categories of calcium channel blockers: 1. Non-dihydropyridines 2. Dihydropyridines
43
CCBs Non-dihydropyridines drugs?
– Verapamil | – Diltiazem
44
CCBs Dihydropyridines drugs?
``` – Amlodipine (Norvasc®) – Felodipine (Plendil®) – Isradipine (Dynacirc®) – Nifedipine (Adalat® CC, Procardia® XL) – Role of Calcium Channels ```
45
CCBs MOA?
–Inhibits calcium influx into cells to prevent muscle contraction –Inhibition at cardiac smooth muscle • Decreases inotropy (force of contraction) • Decreases chronotropy (rate of contraction) –Inhibition at vascular smooth muscle • Vasodilation
46
Dihydropyridines MOA?
Amlodipine, felodipine, isradipine, nifedipine • Inhibits calcium influx into vascular smooth muscle •Result: – Peripheral vasodilation
47
Non-dihydropyridines MOA?
Verapamil and Diltiazem • Inhibits calcium influx into cardiac smooth muscle •Result: – Decrease rate and force of contraction
48
CCBs Place in therapy?
• One of the first line options for hypertension Other uses: • Diltiazem and verapamil: supraventricular tachycardia, atrial fibrillation • Verapamil: migraine prophylaxis
49
CCBs Adverse effects?
• Hypotension
50
Adverse reactions of Non-Dihydropyrinde’s:
``` – Constipation (Verapamil) – Bradycardia – Exacerbation of CHF – Heart block – Gingival hyperplasia ```
51
Adverse effects of the dihydropyridines?
``` – Peripheral edema (worst w/nifedipine) • Amlodipine, felodipine and isradipine OK to use in patients with CHF – Reflex tachycardia – Flushing – Headache ``` Note: Do not use sublingual nifedipine (severe hypotension, reportedly increase risk for MI and death)
52
CCBs Clinical Pearls:
* Dihydropyridines are useful for patients with isolated systolic hypertension (esp. elderly) * Clevidipine I (IV only) is contraindicated in soy or egg allergy •Drug interactions with verapamil: – Metabolized by cytochrome P450 3A4 – Also an inhibitor of this enzyme
53
Alpha 1 Blockers Drugs?
* Prazosin (Minipress®) * Terazosin (Hytrin®) * Doxazosin (Cardura®)
54
Alpha 1 Blockers MOA?
* Competitively inhibits alpha-1 receptors in the periphery which causes vasodilatation * Place in Therapy: Only as an add on especially in males. Not to be used often.
55
Alpha 1 Blockers Uses?
•Hypertension (generally not monotherapy) •Benign prostatic hypertrophy (BPH) – Tamsulosin (Flomax®) – Alfuzosin (Uroxatral®)
56
Alpha 1 Blockers main usage?
Alpha-blockers used ONLY for BPH, minimal systemic effects
57
Alpha 1 Blockers Adverse effects?
* “First dose effect” – significant orthostatic hypotension with first dose and any subsequent dose titrations * Orthostatic hypotension, dizziness, vertigo * Reflex tachycardia, especially early in therapy (not seen if also on beta-blocker, but may worsen orthostatic effects) * Need to slowly titrate dose upward * Fatigue, vivid dreams, depression, dry mouth
58
Alpha 1 Blockers Dose?
* Doxazosin is taken once daily * Terazosin is once to twice daily * Prazosin is two to three times daily
59
Centrally Acting Agents - Alpha 2 Agonists Drugs?
* Methyldopa (Aldomet®) | * Clonidine (Catapres®, Catapres TTS®)
60
Alpha 2 Agonists MOA?
• Stimulates alpha2 receptors in brain, reduces sympathetic outflow from brain, which produces a decrease in BP and peripheral vascular resistance
61
Alpha 2 Agonists Place in Therapy?
•Methyldopa has limited use – Good in pregnancy (category B) •Clonidine is often used for resistant hypertension. Other uses: – Substance abuse treatment (opiate withdrawal and avoidance) – Adjunct in pain management
62
Alpha 2 Agonists Adverse effects?
``` • Orthostatic hypotension , dizziness • Fatigue, depression, sedation • Sodium and water retention • Rebound tachycardia and hypertension if stopped abruptly ``` * Methyldopa: liver toxicities, hemolytic anemia * Clonidine: rash with patch, “anticholinergic-like” side effects (dry mouth, sedation, constipation, urinary retention)
63
Alpha 2 Agonists Clinical Pearl?
•Clonidine is available at a patch (Catapres TTS) – Applied every 7 days – Effects begin within 12-24 hours and last up to 3 days after patch removal
64
Vasodilators Drug?
* Hydralazine | * Minoxidil
65
Vasodilators MOA?
– Direct vasodilator, especially in arteries and arterioles, leading to decreased systemic vascular resistance – Causes peripheral vasodilation
66
Vasodilators Common adverse effects:
* Reflex tachycardia, consider coadministration of beta blocker * Increase in renin as response to vasodilation, consider co-administration with diuretic * Headache is common * Hydralazine: Lupus–like syndrome, dermatitis, drug fever, peripheral neuropathy, hepatitis * Minoxidil: Hirsutism
67
Vasodilators Common Combinations?
* Preferred Combos: * ACE-I/ARB + Thiazide * ACE-I/ARB + Dihydropyridine CCB * Acceptable Combos: * CCB + Thiazide * Thiazide + potassium-sparing diuretic * Beta-blocker + diuretic or dihyropyridine CCB
68
Vasodilators
* Corticosteroids * Excessive alcohol * NSAIDs * ACTH * Amphetamines * Appetite suppressants * Caffeine * Cyclosporine * Estrogen * Pseudoephedrine * Thyroid hormone (in excess) * Duloxetine * Venlafaxine * Bevacizumab * Sorafenib * Erythropoietin * Patient Stopping Medications
69
Treatment Approach to HTN?
•First line options: – Thiazides, CCB’s, ACE-I, ARB’s (all equal in choice) •Note: not the best choice to use ACE-I or ARB’s in a black patient •DM or chronic kidney disease: –ACE-I or ARB’s • JNC 8 states do not use them together •Cardiac history: – Beta-blocker
70
Treatment Approach to HTN Opions?
•1st option: – Start with 1 drug and max the dose and then add on a 2nd agent if still not at goal, and then add on a 3rd agent once the 2nd drug is maxed out if pt. still not at goal. •2nd option: – Start with 1 drug and if not at goal add a 2nd drug prior to maxing out the dose on the first. Then max the dose on both drugs and if not at goal add a 3rd agent •3rd option: – Start with 2 drugs from the beginning if the SBP >160 and/or the DBP >100. Max out the drug doses and add on a 3rd agent if needed.

Pharmacology II (2 decks)

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