Pharma 2 group project
Hi there my name is dylan and with the help of anita nick and jess we will be talking about pcsk9 inhibitors and hypercholesterolemia hypercholesterolemia is a disease characterized by severely elevated serum cholesterol concentrations resulting from a variety of factors patients suffering from the disease are predisposed to suffer from acute coronary heart
Issues due to the elevated levels of cholesterol cholesterol is transported throughout the body in two forms either high or low density lipoprotein known as ldl while in circulation cells expressing an ldl receptor can bind to the ldl and internalize the molecule and reduce its presence in the blood however pcsk9 is a pro protein convertase that binds to the ldl
Receptors causing the receptor to be internalized and degraded this leads the smaller amounts of ldl being transported out of the blood and higher level of cholesterol overall pcsk9 inhibitors are a class of drugs that bind to the receptors in a way that blocks the pcsk9 from binding but still allows for ldl to be internalized into the cell the inhibitors are given
Subcutaneously to the patient fully suppressing all the pcsk9 in the body after four hours of administration the half-life of the inhibitors is between 11 and 14 days giving the drugs longevity and therefore facilitating a fortnightly administration illumination is carried out through either saturable binding to the target or non saturable paralytic pathways pcsk9
Inhibitors are currently the most popular drug used to treat hypercholesterolemia however how do they compare to other recommended drugs for treatment hmg-coa reductase inhibitors tablets which are in class of lipid lowering drug statins work by blocking the enzyme hmg-coa reductase which control cholesterol production in the liver hmg-coa have some considerable
Advantages of a pcsk9 inhibitors these include it can be taken early and it can be prescribed to people who have high cholesterol levels while patients taking pcsk9 inhibitors must meet two key criteria the zetas map is a drug that lowers plasma cholesterol levels by hitting the absorption of cholesterol from the small intestine and decreases the amount of cholesterol
Normally available to liver cells pcsk9 inhibitors beat ezetimibe for low density lipoprotein cholesterol and as it arrived also has significant side effects including muscle and joint pain vytorin is a combination of ezetimibe and reductase inhibitor staff which lower cholesterol by inhibiting the activity of the livers cholesterol synthesizing enzyme vytorin has
Serious side effects including psychological complications such as depression memory problems and confusion when compared to other drugs pcsk9 inhibitors are superior option with considerable advantages pcsk9 inhibitors in this particular study are monoclonal antibodies against pcsk9 what this means is that they are antibodies derived from a cell clone grown in
A lab either from a hybridoma a normal cell which has been fused with a cancer cell or a lymphocyte which has been transformed by a virus monoclonal antibodies are more plentiful and less variable than naturally produced antibodies they can bind specifically to a single site on nearly any selected antigen or they can uncover formerly unknown antigen sites pcsk9
Inhibitors prevent pcsk9 from binding to ldl receptors thereby lowering levels of ldl in the bloodstream some side effects over ever loki map are muscle aches nasopharyngitis gastrointestinal upsets and joint pain which are easily managed the target level of ldl cholesterol varies according to original level but the study by strauss and others showed that less
Than 100 milligrams of cholesterol per deciliter of blood was an appropriate goal the clinical trials for this drug have been so far have been relatively short about 12 weeks results have been encouraging but longer trials will need to be conducted to accurately ascertain the long-term safety of this drug so let’s discuss the pros and cons of hypercholesterolemia
And pcsk9 inhibitors first pcsk9 inhibitors actually are able to treat familial hypercholesterolemia which tends to not be older be treated with with generic drugs of currant try however there are a lot of notable negative things such as the price being about ten thousand dollars a year which is only covered by our pharmaceutical benefits scheme for homozygous
Familial hypercholesterolemia which means it is not viable for most treatments for most people furthermore serious side effects can occur in about 1.5 percent of patients these side effects can include severe neurological problems such as memory loss or allergies due to there being a monoclonal antibody or death thank you for watching we hope you enjoyed others of the year
Transcribed from video
Pharm2.Group01.PCSK9 Inhibitors By Dillan Pienaar