Niño Adonis Melgar April 27, 2009

BSN-2

WRITTEN REPORT ON
ANTILIPIDEMIC AND VASODILATOR
DRUGS
I. ANTILIPIDEMIC Drugs

A. Definition
Antilipidemic or Antilipemic or Hypolipidemic agents are used to lower
abnormally high blood levels of lipids (fatty substances). In normal amounts,
lipids help produce energy, maintain body temperature, and provide the chemical
precursors of certain body constituents. In abnormally high amounts, lipids allow
excess cholesterol to form and deposit in the blood vessels as atherosclerotic
plaques. These plaques contribute to hypertension, slow flow of oxygenated blood
to the heart and other body organs, and increase the risk of coronary artery disease
(CAD), which kills more than 500,000 people in the USA each year.
Lipids are composed of free fatty acids (FFAs), triglycerides (glycerol
esters of FFAs), sterols (cholesterol and cholesterol esters), and phospholipids
(phosphoric acid esters of lipid substances).

B. Lipoprotein Groups

1. chylomicrons
2. very low density lipoproteins (VLDL)
3. low density lipoproteins (LDL)
4. high density lipoproteins (HDL) – only friendly or good lipoprotein
and its main function is to remove cholesterol from blood stream and
deliver it to the liver

C. Nonpharmacologic Methods of Cholesterol Reduction

1. reduction of saturated fats and cholesterol in the diet

2. exercise
3. say no to smoking

D. Types of Antilipidemics

1. Bile acid Sequestrants

• cholesteramin resin
• colesevelem
 • cholestipol HCl

۞Pharmacokinetics
These drugs are not absorbed in the GI tract because of higher
molecular weight. Instead, they remain in the GI tract where they
combine with bile acids for 5 hours. Eventually, it is excreted in the
feces.
۞Pharmacodynamics
These lowers the blood levels of LDL. Since it combines with the
bile acids in the GI tract, the level of bile acids in the liver will
decrease. This triggers the liver to synthesize more bile acids from
cholesterol. And as cholesterol leaves the blood and other areas, the
blood cholesterol level decreases.

2. Fibrates (Fibric Acid)

• clofibrate
• fenofibrate
• gemfibrozil

۞ Pharmacokinetics
These drugs are absorbed readily in the GI tract. After absorption,
95% of the latter is found in plasma proteins. Then they will be
metabolized in the liver to form metabolites and then excreted via
urine and as conjugates of glucoronic acids.
۞Pharmacodynamics
These increases HDL levels in the blood by increasing the
synthesis of apoprotiens (substances derived from proteins), and it
increases the serum’s capacity to dissolve additional cholesterol.

3. Nicotinic Acid
• nicotinic acid
• antihyperlipidemic ezetimibe

۞ Pharmacokinetics
These can be absorbed readily and distributes throughout the body.
Some doses are excreted unchanged in urine.
۞Pharmacodynamics
Inhibits the release of FFA’s from lipid tissues.

4. Statins
• atorvastatin calcium
• fluvastatin sodium
• tovastatin
• pravastatin sodium
• simvastatin
 • rosuvastatin calcium

۞ Pharmacokinetics
These are absorbed from the GI tract, highly protein bound,
metabolized in the liver, and excreted in the urine and feces.
۞Pharmacodynamics
These drugs are responsible for the conversion of hepatic 3-
hydroxy 3-methylglutaryl reductase inhibitor into mevalonate. This
action inhibits the cholesterol synthesis since mevalonate is a
precursor of cholesterol and other sterols.

II. VASODILATORS

A. Definition
Vasodilators increase the blood flow to the extremities. It also decrease the
systolic and the diastolic BP by relaxing arteriolar smooth muscle, leading tpo
arteriolar dilation and decrease peripheral resistance.

B. 2 Main Agents
Direct Vasodilator – acts on arteries, veins, or both
• diazoxide
• hydralazine HCL
• minoxidile
• sodium nitroprusside

Calcium Channel Blockers – preventing the entry of CA2+ into the cells thus
reducing the activity of vascular smooth muscles
• amlodipine besylate
• felodipine
• isradipine
• diltiazem HCl
• nicardipine HCl
• nifedipine
• verapamil HCl

۞ Pharmacokinetics
These drugs are absorbed rapidly and distributed well. They are all
metabolized in the liver and most are excreted in the kidneys.
۞Pharmacodynamics
Direct vasodilators relax peripheral vascular smooth muscles,
lowering BP by ioncreasing the blood vessel caliber and reducing total
peripheral resistance. Calcium channel blockers prevent calcium transport
across the cell membrane, reducing the activity of the vascular smooth
muscle, thus producing vasodilation and lowering the BP.
Reference:
Clinical Pharmacology and Nursing, 3rd edition, Baer and Williams, 1996