Anti-Hypertensive Pharmacology Flashcards

1
Q

BP =

A

CO x Peripiheral Vascular resistance

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2
Q

Factors affecting CO

A
  • inotropic state
  • HR
  • filling pressure
  • regulated by sympathetic/parasympathetic activity, hormones, volume regulation, posture
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3
Q

Factors affecting PVR

A
  • sympathetic/parasympathetic tone
  • vasoconstrictor/dilator hormones
  • blood viscocisty
  • blood volume
  • cardiac fxn
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4
Q

MOA of ACE inhibitors (+major drugs)

A
  • major drugs: captopril, enalapril, and lisinopril
  • inhibit ACE (angiotensin converting enzyme) and decrease production of AngII and destruction of bradykinin
  • create a net vasodilatory effect→↓BP.
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5
Q

Disadvantages of beta-blockers

A
  • CHF patients have a limited cardiac reserve and must be titrated up to the correct dose of beta-blockers.
  • Patients may be uncomfortable and feel worse before they start feeling better (remodelling of the heart takes time—up to 3 – 12 months)
  • some patients may never reach the recommended dose
  • may not be tolerated in Class IV HF due to preexisting limitation in cardiac function
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6
Q

Major beta-blocker drugs

A
  • Metoprolol & atenolol: beta1-AR selective agent
  • Propranolol & timolol: Non-selective beta1- and beta2-ARs
  • Carvedilol & labetalol: relatively nonselective inhibitor of both beta1- and beta2- ARs and also alpha1-ARs (may explain vasodilatory action).
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7
Q

ACE inhibitors (Lisinopril): Site/MOA

A
  • Inhibits ACE conversion of AI to AII, blocking AII induced vasoconstriction; results in decreased pre-load and afterload
  • Decreases AII-induced release of aldosterone
  • Decreases bradykinin inactivation, increasing vasodilation
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8
Q

ACE inhibitors (Lisinopril): Pharmacokinetics

A
  • Well absorbed orally
  • onset of action < 1 hr
  • Once daily dosing for most agents
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9
Q

ACE inhibitors (Lisinopril): Uses

A
  • first line tx of hypertension
  • HF
  • chronic kidney disease
  • diabetic nephropathy
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10
Q

ACE inhibitors (Lisinopril): Adverse effects

A
  • cough
  • hyperkalemia
  • contraindicated in pregnancy
  • hypotension (if hypovolemic)
  • mild increase in serum Cr
  • anemia/angioedema (rare)
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11
Q

Angiotensin Receptor Blockers (Losartan): Site/MOA

A
  • Selective inhibition of AII receptor
  • Similar mechanism of action as ACEIs
    • prevents vasoconstriction + aldosterone release
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12
Q

Angiotensin Receptor Blockers (Losartan): Uses

A
  • HTN
  • HF
  • chronic kidney disease
  • diabetic nephropathy
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13
Q

Angiotensin Receptor Blockers (Losartan): Adverse effects

A
  • Similar to ACEIs but no cough
  • Contraindicated in pregnancy
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14
Q

Examples of Angiotensin II Receptor Blockers (ARBs)

A
  • losartan
  • irbesartan
  • candesartan
  • valsartan
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15
Q

Calcium channel blockers: examples

A
  • dihydropyridines (DHP):
    • amlodipine
    • nislodipine
    • nifedipine
    • felodipine
  • non-dihydropyridines (NDHP)
    • diltiazem
    • verapamil
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16
Q

Calcium channel blockers: MOA

A
  • cause arterial vasodilation via blocking L-type calcium channels => lower peripheral vascular resistance
  • DHP=selective to channels @ vasculature vs. NDHP=channels @ vasculature + heart
    • NDHP = negative chronotropic/inotropic effect
17
Q

Calcium channel blockers: Pharmacokinetics

A
  • readily absorbed, extensive protein binding
  • liver metabolism
  • drug interact: NDHP >> DHP
    • NDHP = CYP P450 metabolism
    • statins, amiodarone, cyclosporine, warfarin, grapefruit juice, St. Johns wort, macrolides
  • once-daily dosing
18
Q

Calcium channel blockers: Adverse effects

A
  • NDHP
    • constipation
    • headache
    • conduction defects
  • DHP
    • peripheral edema
    • headache
19
Q

Calcium channel blockers: uses

A
  • DHP: HTN, migraine prophylaxis
  • NDHP: HTN, migraine prophylaxis, angina, rate control in aFib
20
Q

Beta-blockers: MOA

A
  • Beta1 selective: compete w/catecholamines @ cardiac ARs => decrease CO, suppress renin
  • Beta1/Beta2 nonselective: impact ARs @ heart, bronchial, and vascular system
21
Q

Beta blockers: pharmacokinetics

A
  • once/twice daily dosing
  • generally liver metabolism (not atenolol)
22
Q

Beta blockers: Adverse effects

A
  • fatigue
  • respiratory abnormalities
  • mask sx of hypoglycemia
  • elevate lipids
  • sexual dysfxn
23
Q

Beta blockers: Uses

A
  • Post-MI/CAD
  • HTN
  • angina
  • HF
  • rate control in aFib
24
Q

Direct vasodilators: Examples/MOA

A
  • peripheral vasodilation
  • hydralazine
    • alter calcium metabolism
    • inhibition of calcium movement needed to maintain contract => vasodilation
  • minoxidil
    • K+ channel opener => hyperpolarization of cell membranes
25
Q

Direct vasodilators: pharmacokinetics

A
  • hydralazine
    • peak levles @ 1-2 hrs
    • half-life: 3-7 hrs
    • liver metabolism
  • minoxidil
    • half-life: 4 hrs
    • no clear dose-response
26
Q

Direct vasodilators: adverse effects

A
  • headache
  • anorexia, nausea, vomiting, diarrhea
  • palpitations, tachycardia
  • Hydralazine: SLE-like sx
  • Minoxidil: reflex tachycardia, salt/H20 retention, hair growth
27
Q

Direct vasodilators: uses

A
  • 3rd or 4th line choice:
  • hydralazine: HTN, HF
  • minoxidil: HTN, hair growth (topical)
28
Q

Alpha-1 blockers: examples/MOA

A
  • prazosin, terazosin, doxazosin
  • selective block @ alpha-1 ARs => reduced SVR => lowers HTN
  • also acts @ bladder => decreased urethral resistance => may relieve obstruction/improve urine flow/BPH
29
Q

Alpha-1 blockers: adverse effects

A
  • orthostatic hypotension
  • headache
  • peripheral edema
30
Q

Alpha-1 blockers: Uses

A
  • Benign prostatic hypertrophy (BPH)
  • HTN (3rd or 4th line)
31
Q

Centrally acting agents: examples/MOA

A
  • clonidine
  • stimulation of alpha-2 ARs @ CNS, periphery
  • reduce sympathetic/increase parasympathetic outflow => decreased SVR
    • inhibits norephinephrine release
32
Q

Centrally acting agents: adverse effects

A
  • orthostatic hypotension
  • dry mouth
  • sedation
  • rebound HTN w/abrut stop
33
Q

Centrally acting agents: uses

A
  • HTN (3rd or 4th line)
  • ADHD
  • smoking cessation
  • ETOH withdrawal