Pharma4😅 Flashcards
drugs Depolarize the B cells and cause insulin secretion
Sulfonylurea
Glibenclamide long half life
n Can lead to prolonged hypoglycaemia, especially in elderly
n Gliclazide short half-life and, therefore, preferred agent
Repa-glinide
Non-sulphonylurea insulin secretagogue n Three receptors.
n Similar action to sulphonylureas. Identical efficacy n Requires glucose to have effect
n Short plasma half-life
n 0.5mg with meals, max 16 mg/day
n Weekly increase in dose if required
n Weight neutral n Less severe hypoglycaemia.
A-carb-ose
a-glucosidase inhibitor
n Delays absorption of carbohydrates n Allows beta-cell time to augment response
Decreases HbA1c by 1%, fpg by 1.5mmol/l No change in weight Modest decrease in triglyceride Dosage schedule
n With first bite. Start low, increase every 2 weeks.
Contraindicated in renal failure, IBD & cirrhosis Rarely used owing to poor efficacy and significant GI side effects
Thia-zolidene-diones
PPARg-agonists n 👾👾Improve insulin sensitivity in Liver, skeletal muscle and adipocytes
👾👾Improve beta-cell function n Durable effect on glycaemia n Associated with weight gain
n Part of action of these drugs
😱😱Contraindicated in heart failure n Recent controversy about CV effects and increased risk of bone fractures
Exena-tide
An injectable GLP1 analogous
glip-tins
oral DPP4 inhibitors
Orli-stat
Gastric and pancreatic lipase inhibitor
n Theoretical deficiency of fat soluble vitamins
Sibu-tramine
Norepinephrine and serotonin reuptake inhibitor
n Contraindicated in depression n Blood pressure must be closely monitored
Eze-timibe
can reduce LDL levels by
around 15-20% and is normally given as a monotherapy in statin-intolerant patients; if used synergistically with statins, it can cause a 20% reduction in LDL levels (which is actually better than simply doubling the dose of a statin as it reduces the ADRs of the statin).
Fibrates
Activating PPARs induces the transcription of a number of genes that facilitate lipid metabolism. which acts to significantly reduce triglyceride production, and also lowers LDL and raises HDL. Whilst they can be used in conjunction with statins, they are mainly used directly for hypertriglyceraemias.
Canagliflozin and empagliflozin
an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), which is found almost exclusively in the proximal tubules of nephronic components in the kidneys. SGLT-2 accounts for about 90 percent of glucose reabsorption into the blood. Blocking SGLT-2 reduces blood glucose by blocking glucose reabsorption in the kidney and thereby excreting glucose (i.e., blood sugar) via the urine
Pramlinitide
👾👾it is an amylin agonist secreted by the b cell of the pancreas, help regulate the blood glucose by slowing gastric emptying and promote satiety by hypothalamicreceptor ,and inhibit the inappropriate secretion of the glucagon.
👉🏿👉🏿 Pramlintide has been approved by the FDA, for use by type 1 and type 2 diabetic patients who use insulin.[5] Pramlintide allows patients to use less insulin, lowers average blood sugar levels, and substantially reduces what otherwise would be a large unhealthy rise in blood sugar that occurs in diabetics right after eating.
Dx DM
FBG>=126
Post prandial =>20p
HbAc1=>6.5
How is Diabetes Managed?
Reduce HbA1cto less than 7
Rapid-acting and short-acting insulin preparations
🔴Regular insulin is a short-acting, soluble, crystalline zinc insulin. 🔴Insulin lispro, aspart, and glulisine are classified as rapid-acting insulins.
B. Intermediate-acting insulin
NPH
Long-acting insulin preparations
The isoelectric point of insulin ⚡️glargine [GLAR-geen] is lower than that of human insulin, leading to formation of a precipitate at the injection site that releases insulin over an extended period.
Basal Bolus regimen
🔴 NPH background at night ,,regular 3 times before meal 🥘
🔴glargine or detemir background ,,lispro 3
Pre-mixed insulin combination
NPH/Regular 70:30
Principles of Drug Therapy in Type 2 Diabetes
Therapy should be escalated when previous management has started to fail
n As demonstrated by measurement of HbA 1c
n Patients should be made aware this will occur
n Lifestyle discussed on every occasion
😞😞 Start with oral agents (each lower HbA1c
n Metformin first, unless contraindicated n
Progress to multiple oral agents Progress to insulin
Metformin
👾👾Action not fully understood. Receptor unknown,, Decreased hepatic glucose output by acting on the mitochondria
👾👾Increased glucose uptake in skeletal muscle and fat GLUT 1 and GLUT 4
👉🏿👉🏿Special benefits in overweight patients
Weight-neutral or weight-reducing ,,Improvement in cardiovascular outcomes
🤮🤮Side effects mitigated by slow dose titration (GI upset)
🌺Usual maximum dose is 1g bd
😱😱Contraindicated in metabolic failure (renal failure, hepatic failure and acute heart failure)as it cause lactic acidosis
😱Stop before radiocontrast media and
Thia-zolidene-diones
Used in
Pre DM
DM2
PCOS
Metformin
Used in
DM2,PRE DM
PCOS
NON alcoholic liver disease
Bladder ca
Statin
General info
Statins are the most commonly used and
tolerated drug for lowering LDLs; depending on dosage used, LDL levels can fall between 5-35%, triglycerides by 10-35%, and increasing HDLs by around 5%😍😍😍
Statin mechanism
👾👾Statins work by inhibiting the HMG~CoA reductase enzyme in the liver which would normally be used in the production of cholesterol.
👾👾Decrease in the plasma concentration of cholesterol causes an increase in the number of LDL receptors, which in turn increases the rate of LDL removal from the plasma.
Consequently, statins are used to reduce CVD risk; they are especially important in cases of 👉🏿👉🏿familial hypercholesterolaemia.
Secondary beenfits of statins appear to be as acting as
anti-inflammatories, plaque reduction, and reduction in thrombotic risk.
Statin Adverse Drug Reactions
Statins appear to be well tolerated by the
general population. The only significant ADRs seen involve 🔫🔫increased transaminase levels and 🔫myopathies (more common with increasing age, can be checked by testing the CPK levels), yet only seen in 0.1% of individuals who take high doses. Other miscellaneous complaints reported include GI complaints, joint pain, and headaches.
Cholesterol Absorption Inhibitors
👾👾act by
blocking the specific cholesterol transport protein NPC1L1 in the brush border. This causes a reduction in the amount of dietary cholesterol reaching the liver, which in turn causes a secondary upregulation of LDL transporter expression. Both of these combine to cause a lowered circulating cholesterol level
EX Ezetimibe
