16 August, 2010

Fenofibric acid

Fenofibric acid is a lipid regulating agent available as delayed release capsules for oral administration.
Fenofibric acid activates the peroxisome proliferator activated receptor a (PPARa).
PPARs affect the expression of target genes involved in cell proliferation, cell differentiation and in immune and inflammation responses.

fenofibric Acid is specifically indicated for

1) Co-administration Therapy with Statins for the Treatment of Mixed Dyslipidemia
To reduce TG and increase HDLC in patients with mixed dyslipidemia and CHD or a CHD risk equivalent who are on optimal statin therapy to achieve their LDL-C goal.
2) Treatment of Severe Hypertriglyceridemia
3) Treatment of Primary Hyperlipidemia or Mixed Dyslipidemia
To reduce elevated LDL-C, Total-C, TG, and Apo B, and to increase HDL-C.

The recommended intial dose of the drug for co-administration therapy with statins for the treatment of mixed dyslipidemia is 135 mg daily. Co-administration with the maximum dose of a statin should be avoided.

The recommended initial dose of the drug for severe hypertriglyceridemia is 45 to 135 mg once daily.

The recommended initial dose of the drug for primary hyperlipidemia or mixed dyslipidemia is 135 mg once daily.


Mechanism of Action


fenofibric acid is a lipid regulating agent available as delayed release capsules for oral administration. Fenofibric acid activates the peroxisome proliferator activated receptor a (PPARa). Through this mechanism, fenofibric acid increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of Apo CIII (an inhibitor of lipoprotein lipase activity). The resulting decrease in triglycerides produces an alteration in the size and composition of LDL from small, dense particles to large buoyant particles, which have a greater affinity for cholesterol receptors and are catabolized rapidly. PPARa activation also induces an increase in the synthesis of HDL-C and Apo AI and AII.

Side Effects


* Muscle Pain
* Tenderness
* Weakness
* Tiredness
* Fever
* Abdominal Pain
* Nausea
* Vomiting

Bromocriptine & Type 2 Diabetes

Bromocriptine (Parlodel, Cycloset), an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease (PD), Hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes.

Indications


Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegaly may all be caused by pituitary problems, such as hyperprolactinaemia, and therefore, these problems may be treated by this drug. In 2009, bromocriptine mesylate was approved by the FDA for treatment of type 2 diabetes under the trade name Cycloset (VeroScience). It is currently unknown how this drug improves glycemic control, but it has been shown to reduce HbA1c by ~0.5%.

Side effects


Most frequent side effects are nausea, orthostatic hypotension, headaches and vomiting through stimulation of the brainstem vomiting centre.
Bromocriptine can cause worsening of liver problems.
Vasospasms with serious consequences such as myocardial infarction and strong have been reported in connection with the puerperium, appears to be extremely rare event.
Bromocriptine use has been anecdotically associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine).
Pulmonary fibrosis has been reported when bromocriptine was used in high doses for the treatment of Parkinson's disease.

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