Anti-Hypertensive
Malignant HTN/ or HTN emergency
Blood pressure > 200/120 with end organ damage (e.g. retinopathy,
neuropathy, and nephropathy)
Treatment
IV Nitroprusside causes reflex tachycardia and given if patient has
asthma
Give a beta blocker to block the reflex tachycardia
IV Labatelol or Carvedilol non-selective beta blockers with alpha
blocking capability
Treatment of HTN
Diuretics
1stline of defense
Used in moderate HTN
Thiazides and Loop Diuretics
Decrease plasma volume and cause vasodilation
Loop diuretics increase prostacyclin release for vasodilation
Thiazides causes K+ efflux by opening ATP dependent K + channels for
vasodilation
Alpha-2 Agonists Alpha-Methyl Dopa and Clonidine
Reserpine: blocks granular uptake of NE
Beta Blockers
Commonly used
ACE Inhibitors
Commonly used
Angiotensin Receptor Blockers
Gaunithidine: blocks NE release after Ca 2+ influx
Ca2+ Channel Blockers
Ganglion Blocking Agents
Alpha Blockers
ATP Dependent K + Channels
Found on smooth muscle of blood vessels which causes vasodilation
Beta cells of the pancreas
Inhibits insulin release causing diabetes mellitus
,Hassan Mohammed Pharm Exam 2 3
Ca2+ Channel Blockers(CCB)
Blocks voltage gated Ca2+ channels
Cardio-selective CCB
Verapamil
Stimulates negative effects on the heart ionotropy (FoC), chronotropy
(HR), and dromotropy (AV conduction)
Contra-indicated in patients with AV blocks, bradycardia, and congestive
heart failure
Side Effects: bradycardia, AV blocks, constipation
Vaso-selective CCB
“-dipine”
Nifedipine
Nimodipine
Amlodipine
Blocks Ca2+ influx to cause relaxation or vasodilation
Causes arteriolar vasodilation(decreased afterload) more than venular
dilation (decreased preload)
Side Effects are due to excess vasodilation hypotension, reflex
tachycardia, edema, flushing, dizziness, syncope, nasal congestion, and
gingival hyperplasia
Diltiazem blocks CCB on the heart and vessels
Drugs which cause gingival hyperplasia CCB, Cyclosporine, and
Phenytoin
Indications
HTN
Angina stable, unstable, prinzmetal/ vasospastic
Arrhythmias Verapamil and Diltiazem
Prevention of migraines
Peripheral Vascular Diseases (e.g. Raynaud’s Phenomenon)“-dipine”
Note: useful in patients with HTN who also have asthma, DM, angina, and
PVD
, Hassan Mohammed Pharm Exam 2 4
Clonidine
MOA: alpha-2 agonist
Used for management of withdrawal symptoms of drugs of abuse
Must withdraw slowly to prevent rebound HTN
Alpha-Methyl-Dopa
MOA: alpha-2 agonist
Converted to its active form alpha-methyl-NE
Acts in the CNS and decreases sympathetic outflow
Decreases dopamine and NE
Adverse Effects
AIHA or SLE like reaction
Sedation
Xerostomia and hepatopathy
Movement disorders (e..g Parkinson like)
Hyperprolactinemia
Reserpine
MOA: blocks the vesicular/ granular uptake of NE, serotonin, dopamine, etc.
Can be used to treat mild to moderate HTN
Can cross the BBB
Adverse Effects
Sedation
Depression
Bradycardia
To reverse overdose effects, give a direct agonist as indirect will have no
effect due to depletion of the mobile pool
Guanithidine
MOA: inhibits the release of NE after Ca 2+ influx
TCA’s decreases the anti-HTN effects of guanithidine *****
TCA inhibits the reuptake of NE lessening the effects of guanithidine
Can’t cross the BBB or cause depression
Alpha-1 Antagonist
“-zocin” or “-locin”
Uses
HTN
Symptomatic relief of BPH
HTN with dyslipidemia
Adverse Effects
Due to vasodilation
1st dose syncope(unique)
Flushing and edema
Reflex tachycardia
Nasal congestion and miosis
Sexual dysfunction
Note: let the patient sit down and take the first dose to manage hypotension
that may occur
All alpha-blockers are competitive except phenoxybenzamine
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