Diabetes Drugs Flashcards
Clinical uses of insulin and other hypoglycaemic drugs for injection?
Pharmacokinetic aspects and insulin preparations?
Various dosage regimens are used. Some type 1 patients inject a combination of short- and intermediate-acting insu- lins twice daily, before breakfast and before the evening meal. Improved control of blood glucose can be achieved with multiple daily injections of short-acting insulins with meals, and a longer-acting insulin at night. Insulin pumps are used in hospital and sometimes, by specialists, in out- patients. The most sophisticated forms of pump regulate the dose by means of a sensor that continuously measures blood glucose, but these are not routinely available.
Unwanted side effects of Insulin?
List 3 Oral hypoglycaemic sulfonylurea drugs for diabetes:
- Relative potency?
- Duration of action?
- Pharmacokinetic aspects?
Biguanides
- Example?
- Actions and mechanism? (5)
- Half-life?
Biguanides
- Unwanted effects?
Biguanides
- Clinical Uses?
Metformin is used to treat patients with type 2 diabetes. It does not stimulate appetite (rather the reverse; see above!) and is consequently the drug of first choice in the majority of type 2 patients who are obese, provided they have unimpaired renal and hepatic function. It can be combined with sulfonylureas, gloxazones or insulin. Potential uses outside diabetes include other syndromes with accompanying insulin resistance including polycystic ovary syndrome, non-alcoholic fatty liver disease and some forms of premature puberty, but these indications remain experimental.
Sulfonylureas
- Examples?
- MOA?
Mechanism of action
The principal action of sulfonylureas is on B cells, stimulating insulin secretion and thus reducing plasma glucose. High-affinity receptors for sulfonylureas are present on the KATP channels in B-cell plasma mem- branes, and the binding of various sulfonylureas parallels their potency in stimulating insulin release. Block by sulfo- nylurea drugs of KATP channel activation causes depolarisa- tion, Ca2+ entry and insulin secretion.
Sulfonylureas
- Pharmacokinetic aspects?
Sulfonylureas
- Unwanted effects?
Sulfonylureas
- Drug interactions?
Sulfonylureas
- Clinical Use?
Clinical use
Sulfonylureas are used to treat type 2 diabetes in its early stages, but because they require functional B cells, they are not useful in type 1 or late-stage type 2 diabetes. They can be combined with metformin or with thiazolidinediones.
Thiazolidinediones (glitazones)
- Examples?
- Effects?
Thiazolidinediones (glitazones)
The thiazolidinediones (or glitazones) were developed fol- lowing the chance observation that a clofibrate analogue, ciglitazone, which was being screened for effects on lipids, unexpectedly lowered blood glucose. Ciglitazone caused liver toxicity, as did troglitazone, but there are only rare reports of hepatotoxicity with (rosiglitazone and pioglitazone which is the only drug of this class in clinical use.)
Thiazolidinediones (glitazones)
- MOA?
Thiazolidinediones (glitazones)
- Pharmacokinetic aspects?
- Unwanted effects?
Pharmacokinetic aspects
Pioglitazone is rapidly and nearly completely absorbed, with time to peak plasma concentration of less than 2 h. It is highly (> 99%) bound to plasma proteins, and is subject to hepatic metabolism and has a short (< 7 h) elimination half-life for the parent drug, but substantially longer (up to 24 h) for the metabolite. Pioglitazone is metabolised mainly by a CYP2C isozyme and CYP3A4 to active metab- olites, which are eliminated mainly in bile.
Thiazolidinediones (glitazones)
- Clinical use?
Incretin mimetics and related drugs
- Example?
- MOA?
- Uses?
- Unwanted effects?
Gliptins
- Example?
- MOA?
- Uses?
- Unwanted effects?
Give an overview of the drugs used for Diabetes mellitus:
- Insulin and other injectable drugs?
- Oral hypoglycaemic drugs?
Clinical uses of oral hypoglycaemic drugs?
