Pharm-3A

over 140/90

Stage I: 140-159(SBP); 90-99(DBP)

Stage II: >=160(SBP); >=100(DBP)

• - 1st line therapy for mild to moderate HTN
• - inhibits NaCL reabsorption from distal collecting duct

major differences are half lives and duration of effects

• AE:
• 1. hypokalemia, hyponatremia, hypoMg, hypercalcemia

2. muscle cramps, dizziness, sexual dysfunction, hyperlipidemia, hyperuricemia

• Interactions/contraindications:
• 1. NSAIDS
• 2. Quinidine and digitalis (increased arrythmias)
• 3. not useful in renal failure without adequate urine outpout

• - For edema and volume overload associated w/ heart failure
• - "High ceiling" means most effective diuretic since it works earlier in NaCL absorption
• - blocks Na/Cl symporter in ascending loop

• AE:
• 1. similar to thiazides w/ electrolytes; also Na+ and volume depletion esp. in elderly pts
• 2. hypocalcemia and hypomagnesium
• 3. ototoxicity (IV)
• 4. rash, photosensitive, bone marrow suppression

• DI:
• 1. aminoglycosides
• 2. anticoags (increased)
• 3. digitalis (K+)

• Indications:
• - used in conjunction with loop or thiazide diuretics to minimize risk of hypokalemia

• MOA: 
• - blocks Na+ channels in late DCT and blocks secretion of K+
• - antagonize effects of aldosterone (blocks Na+ reabsorption and K+ secretion)

(Midamor)

K+ Sparing Diuretic

- blocks Na/K+ exchange mechanism in distal nephron

(Dyrenium)

K+ Sparing Diuretic

- blocks Na/K+ exchange mechanism in distal nephron

(Aldactone)

K+ Sparing Diuretic

- severe heart failure

(Inspra)

K+ Sparing Diuretic

-normokalemia is essential

Thiazide diuretic

Thiazide diuretic

Thiazide diuretic

Thiazide diuretic

(Lasix)

Loop diuretic

-Most Common

(Bumex)

Loop diuretic

(Edecrine)

Loop diuretic

- not a sulfonamide...not in US

(Demadex)

Loop diuretic

• AE:
• 1. spironolactone may cause gynecomastia, decreased libido, impotence, menstrual irregularities, diarrhea, and dyspepsia
• 2. hyperkalemia is C/I to taking these; can lead to arrhythmias
• 3. CNS effects

• DI:
• 1. ACE inhibitors and angiotensin II receptor blockers can increase K+

Drugs end in -pril

• 1. HTN
• 2. all patients post MI and heart failure
• 3. diabetic and non-diabetic proteinuria
•     - reduce progression to clinical nephropathy

• 1. rash
• 2. cough
• 3. hyperkalemia (rare)
• 4. acute renal failure and elevated serum creatinine
• 5. hypotension
• 6. angioedema (common in AA pts)
• 7. dysgeusia (distortion of sense of taste)

• C/I
• 1. pregnancy
• 2. angioedema
• 3. bilateral renal artery stenosis
• 4. hyperkalemia

• DI
• 1. NSAIDS (decreased effects)
• 2. DIG and lithium levels can be increased

-blocks the ANG II receptor so action of ANG II is inhibited

-no effect on bradykinin metabolism

-end in "-artan"

• 1. less cough
• 2. less angioedema
• 3. good for pts who cannot tolerate ACEI
• 4. may reduce progression of Type 2 diabetic nephropathy
• 5. same pregnancy C/I

1. Verapamil - most cardiac effects; negative inotropic and chronotropic; slows conduction through AV node

2. Diltiazem - cardiac and peripheral blood vessel effects

• 3. 6 dihydropyridines (more peripheral arteriolar vascular smooth muscle vasodilation)
• -end in "pine"

• Indications:
• 1. HTN
• 2. Angina
• 3. SVT (supraventricular tachyarrhythmias)
• -non-dihidropyradines

• DI:
• 1. metabolized by p450
• 2. verapamil is CYP3A4 inhibitor

• C/I:
• 1. use caution when combine w/ beta blockers
• 2. severe CHF and high degree heart blocks for non-DHP

• 1. dizzy, flushing, HA (vasodilation)
• 2. worsening angina (DHP-type)
• 3. peripheral edemia (vasodation); DHP-type
• 4. constipation (verapamil), GI complaints
• 5. heart conduction abnormalities are possible w/ verapmil and diltiazem

• MOA:
• -block beta receptors in heart and other tissue
• -slows heart rate, reduces contractility and output

• Properties:
• 1. beta 1 selectivity (nonselective vs selective)
• 2. intrinsic sympathomimetic activity (partial agonist)
• 3. lipid soluble (crosses BBB)
• 4. membrane stabilizing (depresses action potential)

• People with HTN and:
• 1. stable angina
• 2. stable heart failure
• 3. post myocardial infarction
• 4. migraine HA
• 5. situational panic
• 6. symptoms related to hyperthyroidism

Non-selective Beta Antagonists (Block Beta1 and Beta2 receptors)

-most commonly used and highly lipophilic

Non-selective Beta Antagonists (Block Beta1 and Beta2 receptors)

-long half life 20 hrs

Non-selective Beta Antagonists (Block Beta1 and Beta2 receptors)

-used for glaucoma

(ISA)

Non-selective Beta Antagonists (Block Beta1 and Beta2 receptors)

(Normodyne)

Non-selective Beta Antagonists (Block Beta1 and Beta2 receptors)

(Coreg)

Non-selective Beta Antagonists (Block Beta1 and Beta2 receptors)

(Lopressor, Toprol XL)

Cardio-selective beta antagonist (greater affinity for beta1 receptors)

-common anti-HTN agent

(Tenormin)

Cardio-selective beta antagonist (greater affinity for beta1 receptors)

Cardio-selective beta antagonist (greater affinity for beta1 receptors)

-short half life, given IV for rapid beta blockade

Cardio-selective beta antagonist (greater affinity for beta1 receptors)

Peripheral Alpha1 blocker

-shorter half life; BID dosing

Peripheral Alpha1 blocker

Peripheral Alpha1 blocker

(Catapres)

Central Alpha2 Receptor Agonist

(Aldomet)

Central Alpha2 Receptor Agonist

• -reserved for moderate to severe caess
• -use with diuretic (avoid Na and water retention)
• -use for HTN in pregnancy

Central Alpha2 Receptor Agonist

Central Alpha2 Receptor Agonist

vasodilator - direct arteriolar smooth muscle relaxation

-used for severe, resistant cases of HTN in combo w/ diuretics, beta blockers

-immunologic reactions such as drug induced lupus

vasodilator - direct arteriolar smooth muscle relaxation

-used for severe, resistant cases of HTN in combo w/ diuretics, beta blockers

• -water/Na retention, increased HR, contractility
• -hypertrichosis (not good for the ladies)

(Aliskiren)

-new class, direct renin inhibitor

• -edema of face, neck, hands
• -renal dysfunction
• -diarrhea, cough

(amlodipine besylate; olmesartan medoxomil)

• New Drug
• -CCB plus ARB

Postganglionic sympathetic inhibitors (not commonly used for HTN)

-deplete NE from postganglionic sympathetic nerve terminals

-blocks effects of NE --> reduces PVR

• -lost of AE's
• -does not cross BBB so less sedation and craziness than reserpine

Postganglionic sympathetic inhibitors (not commonly used for HTN)

–Binds to storage vesicles in central and peripheral adrenergic neurons and makes them dysfunctional so nerves cannot secrete NE

–SEDATION, depression which may lead to suicide (RARE)

For HTN emergencies

-excessive and rapid hypotension

-must use special infusion pump and close monitoring

-toxic accumulation of cyanide 

For HTN emergencies

-effective w/ little effect on HR and CO