198 Section 4/ Drugs Acting on Cardiovascular & Urinary Systemtriglyceride plasma levels may be due to
reduction in hepatic synthesis of VLDL and
increase in VLDL clearance.
It is completely absorbed from gastro-
intestinal tract and is excreted in urine.
Adverse effects include nausea,
diarrhoea, abdominal pain, dyspepsia,
fatigue, skin rash, weight gain, leucopenia,
alopecia, blurred vision etc.
NICOTINIC ACID
Nicotinic acid and nicotinamide
together represent the essential vitamin
niacin in the diet. Of these two, only nicotinic
acid is active as a lipid modifying drug.
Nicotinic acid is preferred in patients with
triglyceride levels exceeding 200 mg/dl
because bile acid sequestrants tend to raise
triglyceride levels. Nicotinic acid reduces
production of VLDL by liver, thus its
degradation products IDL and LDL are
subsequently reduced. It inhibits lipolysis
in adipose tissue and increases activity of
lipoprotein lipase. It has no effect on
cholesterol and bile acid metabolism.
Combination drug therapy has been shown
to decrease cholesterol levels in
hyperlipidemic patients.
Adverse effects include, flushing,
itching, vomiting, diarrhoea and dyspepsia.
It may also lead to hyperpigmentation of
skin, liver dysfunction, hyperglycaemia and
hyperuricaemia.
It is indicated in type III, IV & V hyper-
triglyceridemia. It lowers VLDL and raise
HDL level and it is administered with HMG
CoA reductase inhibitors e.g. simvastatin.CHOLESTYRAMINE AND COLESTIPOL
They are useful only in hyperlipopro-
teinemias involving elevated levels of LDL
i.e. type IIa, IIb and V. They are basic ion
exchange resins. They are neither digested
nor absorbed in the gut. They bind bile ac-
ids in intestine and interrupt their entero-
hepatic circulation, leading to increased
faecal excretion of bile salts and cholester-
ol. There is increased hepatic conversion of
choles-terol to bile acids. More LDL recep-
tors are expressed on liver cells leading to
increased clearance of IDL, LDL and indi-
rectly of VLDL.
Adverse effects include nausea, heart
burn, constipation and acidosis etc.PROBUCOL
It is cholesterol lowering agent with
antioxidant property. It is only 1 / 10
absorbed when given orally. It reduces the
serum cholesterol levels without reduction
in serum triglycerides level and also reduces
the HDL levels. It has no effect on VLDL and
triglyceride levels.
Adverse effects include headache, dizzi-
ness, diarrhoea and eosinophilia.GUGULIPID
Is an indigenous drug obtained from
gum guggul used for treatment of
hyperlipidemia, hypercholesterolemia and
hypertriglyceridemia.